New drugs in ophthalmology. Ophthalmic drugs

For a long time, diseases of the organs of vision were treated using medications intended for use in the treatment of internal diseases. The nineteenth century was marked by a large number of discoveries that were associated with the discovery of a huge number of organic compounds in plants.

Later they began to be used in the treatment of ophthalmic diseases. For example, in 1832, the medicinal plant Atropa Belladonna (Delladonna belladonna, Solanaceae family) was isolated, which immediately found use among ophthalmologists. In 1875, pilocarpine was isolated; and already in 1877 it was experimentally established that it perfectly lowers intraocular pressure. As a result, it began to be used as a treatment for glaucoma. It is worth noting that he is still not losing ground in modern ophthalmology.

Antimicrobials

Today, many local drugs of different composition and dosage forms are produced for use in ophthalmic practice.

These include :

Bacitracin - erythromycin
- chloramphenicol (chloramphenicol) - gentamicin
- chlortetracycline - norfloxacin
- ciprofloxacin - ofloxacin
- sulfacetamide - sulfafurazole
- polymyxin B - tetracycline
- tobramine

When choosing a drug, you should be guided at least by the results of a medical examination, and ideally also by the results of bacterial culture for antibiotic sensitivity. Complex ophthalmic infections, for example, endophthalmitis and corneal ulcers, are treated using drugs manufactured directly in industrial pharmacies. To do this, the pharmacist needs to know their time parameters for processing in the sterilizer.

Use of drugs

Infections of the skin, lacrimal organs, eyelids and conjunctiva are very widely known in medical practice. Each patient has his own treatment tactics, depending on his specific clinical picture.

Damage to the nasolacrimal duct of an inflammatory or purulent-inflammatory nature. It occurs in both children (more often) and adults. In infants, it is most often associated with obstruction of the duct. In adults, dacryocystitis, as well as dacryocanaliculitis, can be caused by: staphylococci, actinomycetes, fungi of the genus Candida, and actinomycetes.

Characteristic inflammations of the eyelids are, as well as. With barley, the sebaceous (meibomin) and/or Moll glands located at the edges of the eyelids become inflamed. The most common cause is Staphylococcus aureus; in this case, it is prescribed to apply compresses and put antibacterial ointment behind the eyelid. For example, a warming compress and floxal ointment. Blepharitis is a common recurrent inflammation of the ciliary edge of the eyelids, characterized by burning and inflammation, sometimes accompanied by peeling. The most common cause is also staphylococci. The basis of therapy is - eye washing; Often, antibacterial ointments are also used topically in combination with drops, in case of keratitis or conjunctivitis. For example, Okomistin drops will be effective for washing the eyes. You can also use strained warm chamomile decoction or the well-known sleepy black tea for rinsing. And as the main treatment, Tobrex (tobramycin) eye drops, which have both adult and pediatric dosage forms, as well as tetracycline eye ointment, are well suited. Doctors often make up various combinations of the above medications.

This is an inflammation of the lining part of the eyelid and covering the whites of the eyes, a membrane of cylindrical epithelium of varying severity: from simple redness to a severe purulent process. It can be of various origins: bacterial, allergic, viral. In addition, contact lenses, the general condition of the body and immune system, chemical and air pollutants also play a role. Atypical bacterial conjunctivitis is treated empirically.

Endophthalmitis is an acute abscessive inflammation of the eyeball. If inflammation covers all the membranes of the eyeball, this is called panophthalmitis. Endophthalmitis can be caused by fungi, bacteria, and much less commonly, spirochetes. It can occur after surgery on the eyes, after injuries, in patients with weak immunity. Therapy consists of surgery - vitreectomy and antimicrobial therapy, in which the drug is injected directly into the vitreous body.

Antiviral agents

These include :

Idoxuridine - trifluridine
- vidarabine -
- foscarnet - ganciclovir
- fomivirsen - cidofovir

Application

The above medications are prescribed for the treatment of viral keratitis and retinitis, as well as herpes zoster in the ocular form. There is no effective drug to treat inflammation caused by adenovirus, but it usually goes away on its own.

Viral keratitis is a corneal disease that affects the epithelium or stroma. Most often, it is caused by herpes simplex virus (HSV) type 1. Less commonly - HSV type 2, cytomegalovirus and Epstein-Barr virus. Local antiviral agents will be effective for treatment, for example: Zovirax, acyclovir, Oftan Idu, Zirgan. Glucocorticoids stimulate viral replication, therefore drugs of this group are contraindicated for epithelial keratitis of herpetic nature. However, on the contrary, they are recommended in the complex treatment of stromal keratitis.

Herpes zoster in the ocular form is a reactivation of the varicella-zoster virus (VZV), which settles in the trigeminal ganglia. But the severity and possibility of aggravating the infection with complications is reduced if acyclovir is used systemically.

Application

- There are several effective regimens for the treatment of toxoplasmosis.:

1) trimethoprim and/or sulfamethoxazole in combination with clindamycin or without using it,
2) clindamycin, pyrimethamine, clindamycin, calcium folinate, sulfadiazine.
3) monotherapy with clindamycin.
4) pyrimethamine, sulfadiazine, calcium folinate. In parallel, systemic treatment with glucocorticoids, for example prednisolone, is carried out

Finally

Thus, for any eye disease, there is one or several effective treatment regimens that are widely used not only in the Russian Federation, but also abroad. In some cases, it is necessary to resort to surgical intervention. However, as with any other disease, timely consultation with a doctor, as well as the correct use of medications, can shorten its duration and help avoid complications.

Eye drops are used in ophthalmological practice for the prevention and treatment of diseases of the anterior segment of the eye, outer membranes and eyelids. Such products can have different effects on the eyes; they contain one or more components.

Immediately before instilling the drops, the bottle of medicine should be warmed in your hand to body temperature. The procedure should be carried out in a calm environment, after washing your hands. In order for the drop to get to the right place, you should tilt your head back and pull down your lower eyelid. To avoid getting the medicinal solution into the nasal cavity, after instillation, close your eye and press on the inner corner.

An important feature of medicinal eye medications is that they quickly penetrate through the outer mucous membrane of the eye into the deeper parts of the visual apparatus. It is not permissible to use such means on your own. Before starting treatment, it is important to read the instructions.

So, how to put eye drops for various diseases and what kind of eye drops are there in general?

Types of eye drops

Let's look at the list of eye medications depending on their pharmacological action:

• Antimicrobial. They include antibiotics, as well as antiviral, antiseptic and antimycotic drugs;
• Anti-inflammatory.
• Antiglaucoma. They are divided into drugs that improve the outflow of ocular fluid and inhibit the production of aqueous fluid.
• Drugs that improve tissue metabolism.
• Antiallergic.
• Medicines for the treatment of cataracts.
• Moisturizing.
• Diagnostic.

The best eye drops can be prescribed by a specialist, as he understands the composition and pharmacological action of the drug

The best eye drops

Next, we’ll talk about what effective remedies there are in the fight against various types of ophthalmological disorders. You can choose the best drops only after a detailed review and comparative analysis.

Moisturizing

This group of drugs is used for tired and dry eyes. Experts recommend using moisturizers for dry eye syndrome, prolonged use of the computer, and exposure to adverse environmental factors. Such medications are sold without a prescription form, so they can be freely purchased in pharmacy chains.

Moisturizing drops do not affect the tissues of the eye, but are artificial tears. Thanks to this, they have virtually no contraindications. Let's consider popular products from the group of moisturizing drugs:

• Visomitin. The product has a keratoprotective effect, it fights age-related changes in tear fluid, as well as dry eye syndrome. Visomitin has antioxidant activity, which normalizes conjunctival cells, relieves the inflammatory reaction and normalizes the composition of the tear film. Visomitin is drops for cutting, itching, burning and pain in the eyes. This is a unique drug that affects not only the symptoms, but also the very cause of the problem.
• Systane. The relaxing drug effectively eliminates dryness, fatigue and irritation of the eyes. Soon after instillation, unpleasant symptoms such as itching, redness, and burning decrease. When the drops fall on the mucous membrane of the eye, they form a film that protects against drying out.
• Vidisik. The gel has keratoprotective properties. This is a combined remedy, similar in composition to tear fluid. Vidisik forms a delicate film on the surface of the eye that lubricates and moisturizes. The gel stimulates healing processes.
• Hilo chest of drawers. These are drops for relaxing the eyes, which are used for dry eye syndrome, after surgery, and also for feeling comfortable when wearing contact lenses. Hilo-komod contains hyaluronic acid, it does not contain any preservatives and is approved for use during pregnancy. Hilo-chest of drawers are drops for pain, itching and fatigue in the eyes.

Systane is a well-known eye drop for irritation

Activating metabolic processes

Experts prescribe such drops to slow down age-related changes and degenerative processes in the tissues of the visual apparatus, as well as in the treatment of cataracts. The active components included in the composition help the eye receive more oxygen and nutritional components. Medicines in this group improve microcirculation processes, nutrition of the eye and restore functional activity.

Let us highlight the prominent representatives of this group:

• Quinax. Often prescribed for the treatment of lens opacity - cataracts. Quinax has antioxidant activity and protects the lens from the negative effects of free radicals.
• Taufon. The drug is prescribed for dystrophic changes occurring in the organs of vision. Taufon stimulates metabolic and energy processes, and also accelerates healing processes. The product normalizes intraocular pressure and metabolism.
• Catalin. It is used for preventive and therapeutic purposes against diabetic and senile cataracts. Catalin normalizes nutrition, metabolic processes in the lens, and also prevents the appearance and development of cataract symptoms.

Taufon are cheap eye drops that activate metabolic processes in the tissues of the eye.

Antiglaucoma

Antiglaucoma drops are prescribed for increased intraocular pressure. Glaucoma, or eye hypertension, is fraught with the development of atrophic changes in the optic nerve and complete loss of vision. The drugs reduce the production of intraocular fluid and improve its outflow. Such drops are a good method of non-surgical treatment of glaucoma. The preservation of the patient’s vision depends on the correctness of their choice.

Let's talk about four well-known anti-glaucoma drops:

• Pilocarpine. The drug constricts the pupil of the eye and reduces increased intraocular pressure. Pilocarpine is also used during eye examinations, as well as after surgical interventions. The product belongs to the group of alkaloids, which is made from the leaves of a plant of the genus Pilocarpus;
• Betoptik. The drug belongs to the group of selective beta-blockers. Intraocular pressure is reduced by reducing the production of ocular fluid. Betoptik selectively affects the receptors of the visual apparatus. The product does not affect pupil size and twilight vision;
• Fotil. These are combined drops that contain pilocarpine and timolol, a beta-blocker. Fotil causes a spasm of accommodation and constriction of the pupil. Already half an hour after instillation, an effect is observed that can last up to fourteen hours;
• Xalatan. The product improves the outflow of aqueous humor, preventing the progression of glaucoma.

Eye wash drops

Eye rinsing may be necessary in case of injury, as well as exposure to a foreign body or aggressive substances. Doctors also recommend the procedure for inflammatory processes. Let's look at three types of eye wash drops:

• Sulfacyl. Belongs to the group of sulfonamides. It has a bacteriostatic effect on gram-positive and gram-negative microflora. This means that under the influence of the drug, the active growth and reproduction of pathogens is suspended;
• Levomycetin. This is an antibiotic with a wide spectrum of action. Accustoming to Levomycetin occurs slowly.
• Albucid. This is an antibiotic with a bacteriostatic effect that eliminates infectious and inflammatory processes. The active substance has antimicrobial activity and belongs to sulfonamides.

Albucid are antibacterial drops that are used to wash the eyes

Midriatics

The pupil is a hole in the iris of the eye through which sunlight enters and is refracted onto the retina. Drops to dilate the pupil can be used in two cases:

• Therapeutic purpose. In the treatment of inflammatory processes and during surgery.
• Diagnostic purpose. To check the fundus of the eye.

Let's review the famous mydriatics:

• Atropine. The product has a large number of contraindications and is highly toxic. Sometimes the effect of Atropine lasts for ten days. The drug can cause discomfort and blurred vision for a certain period of time;
• Mydriacyl. Approximately twenty minutes after instillation, the product begins to act. The therapeutic activity is maintained for several hours, which means the functions of the eye are quickly restored. The product can be used by both adults and children. You can read more about eye drops for children;
• Irifrin. The product is used for both medicinal and diagnostic purposes. This is due to Irifrin’s ability to lower intraocular pressure.

Irifrin is used for diagnostic purposes to dilate the pupil.

Antiseptic

The main task of antiseptics is to disinfect surfaces. These agents have a wide spectrum of action and therefore bacteria, viruses, protozoa, and fungi are sensitive to them. They are low-allergenic and do not have a systemic effect on the body. The drugs help alleviate the condition of conjunctivitis, keratitis, uveitis and other inflammatory processes. Antiseptics eliminate redness and prevent the effects of pathogens.

Let's consider two well-known antiseptics for the treatment of eye diseases:

• Vitabact. Drops have a wide spectrum of antimicrobial action. Piloxidin is the main active component of the drug. Vitabact is used for infectious lesions of the anterior parts of the eye: conjunctivitis, dacryocystitis, keratitis, blepharitis.
• Okomistin. Benzyldimethyl is the active ingredient in antiseptic drops. Okomistin is prescribed for eye injuries, keratitis, conjunctivitis. It is also used to prevent purulent-inflammatory complications.

Okomistin is an antiseptic drop for eyes and ears.

Antiallergic

This group of drugs is used for allergic manifestations in the eye area:

• redness;
• edema;
• burning;
• photophobia;
• lacrimation.

The peculiarity of antiallergic drops is that they only relieve allergy symptoms, but do not have a therapeutic effect. Such drugs are prescribed for seasonal conjunctivitis, inflammation of the conjunctiva caused by wearing contact lenses, as well as drug-induced inflammation.

Consider the list of antiallergic drops:

• Alomide. It is an antihistamine used to stabilize mast cells. After instillation, temporary itching, burning and tingling may occur.
• Allergodil. The product has an anti-edematous and anti-allergic agent. Allergodil is used for seasonal conjunctivitis, as well as year-round inflammation of an allergic nature. It is allowed to use the product after twelve years. Allergodil may cause eye irritation.
• Opatanol. The active component of the drops is a potent selective antihistamine. Opatanol effectively fights the symptoms of seasonal conjunctivitis: itching, burning, swelling, redness of the mucous membrane.
• Dexamethasone and Hydrocortisone are used strictly as prescribed by the doctor. Dexamethasone is a corticosteroid that relieves inflammation and allergic reactions. Hydrocortisone relieves inflammation, irritation, redness, and also reduces the migration of protective cells at the site of the inflammatory reaction.

Allergodil is an antiallergic drug that is used in the form of eye drops and nasal spray.

Vasoconstrictors

Such remedies are used for swelling and redness of the eye. Such unpleasant sensations may be the result of an allergic, inflammatory reaction or irritation. Constriction of blood vessels leads to swelling and swelling disappearing within just a few minutes. You can use vasoconstrictor drugs strictly as directed by a doctor and for a short time, as they can be addictive.

Let's take a closer look at the representatives of the vasoconstrictor group:

• Octilia. The drug belongs to alpha-adrenergic agonists. Tetrizoline, the active component of Octilia, constricts blood vessels, relieves swelling, stimulates the outflow of intraocular fluid and causes pupil dilation. The product relieves unpleasant symptoms of eye irritation: lacrimation, itching, burning, pain;
• Okumetil. This is a combined anti-inflammatory agent with antiallergic and antiseptic effects. Okumetil relieves swelling and irritation of the eye. After installation, the active component is able to be absorbed into the systemic bloodstream, which can cause serious side effects from internal organs;
• Visine. The active component is an alpha-adrenergic agonist - tetrizoline. Visine constricts blood vessels and relieves swelling. Within a minute, the effect of the drug appears, which lasts for four to eight hours.

Visin eye drops quickly constrict blood vessels

Antibacterial

Antibacterial drugs fight bacterial eye diseases. But it is a bacterial infection that most often becomes the cause of inflammatory processes. Let's talk about effective antibiotics in the form of drops:

• Tobrex. The active component of the drug is tobramycin. This is an antibiotic from the aminoglycoside group. Tobrex is used to treat infectious and inflammatory processes in people of any age, including newborns. Staphylococci, streptococci, Klebsiella, Escherichia coli and diphtheria coli are sensitive to tobramycin;
• Digital The active ingredient is ciprofloxacin, an antibiotic from the fluoroquinolone group. Can cause adverse reactions in the form of allergic reactions;
• Phloxal. This is an antimicrobial drug to which gram-negative bacteria are most sensitive. Floxal is effective in the treatment of styes, conjunctivitis, blepharitis, keratitis and other diseases.

Antiviral

There are two types of antiviral drops:

• Virucidal chemotherapy drugs and interferons. These drugs destroy the viral infection.
• Immunomodulators. Strengthen the resistance, or resistance, of the body, making it easier for it to fight pathogens.

Poludan is an effective antiviral agent

Let's talk about four popular antiviral eye drops:

• Oftan I'm coming. Idoxuridine is the active component of the drug, which is a pyrimidine nucleotide. Its main disadvantage is poor penetration into the cornea and the inability to affect resistant strains of viruses and toxic substances. When Oftan Ida is instilled, itching, burning, pain, and swelling may occur;
• Oftalmoferon. This is a combination drug that has anti-inflammatory, antiviral and immunomodulatory properties. The product is made based on human recombinant interferon. Ophthalmoferon also has local anesthetic and regenerative effects;
• Aktipol. The product not only has an antiviral effect, it has antioxidant, radioprotective and regenerative properties. Aktipol is quickly absorbed into the eye tissue and promotes wound healing, as well as relieving swelling;
• Poludan. Typically, drops are used in the treatment of adenoviral and herpetic lesions of the eye. Poludan also has an immunomodulatory effect. Sometimes the product can cause allergic side effects.

So, eye drops are effective drugs in the fight against various diseases of the visual system. These products are divided into different groups depending on the presence of the active ingredient. For bacterial lesions, antibacterial agents are used, but if the ophthalmological disorder is viral in nature, then specialists prescribe antiviral drops. In case of a fungal disease, antimycotic drops are prescribed. And this is not a complete list of all available eye medications.

Eye drops can be used not only for medicinal purposes, they are also used for prevention and diagnostic testing. Be that as it may, medications for the eyes should be prescribed by a doctor after an examination and an accurate diagnosis.

Do no harm!!!

The doctor's first commandment

Acting cautiously is more important than judging wisely.

Ancient wisdom

26.1. Methods of administration of ophthalmic drugs and features of their pharmacodynamics

In ophthalmology, the most widely used forms of drugs are eye drops And ointments. The volume of the conjunctival sac allows you to administer no more than 1 drop of solution at a time or place a 1cm long strip of ointment behind the lower eyelid.

All active ingredients of drugs penetrate into the cavity of the eyeball mainly through the cornea. However, local and general side effects that occur may be caused by the active substance entering directly into the bloodstream through the conjunctival vessels, vessels of the iris, along with tears through the nasal mucosa. The severity of systemic side effects can vary significantly depending on the individual sensitivity of the patient. Thus, instillation of 1 drop of a 1% solution of atropine sulfate will cause not only mydriasis and cycloplegia, but in children it can also lead to hyperthermia and dry mouth. Local use of β-blockers (timolol maleate) in persons with hypersensitivity can provoke arterial collapse.

Most eye drops and ointments are contraindicated for use while wearing contact lenses due to the risk of cumulative side effects. If several types of eye drops are used simultaneously, the interval between instillations should be at least 10-15 minutes to prevent dilution and washout of the previously administered drops.

Depending on the solutions used for the active ingredients, the duration of action of 1 drop varies. The shortest action is for aqueous solutions, the longest for solutions of viscoactive substances (methylcellulose, polyvinyl alcohol), the maximum for gel solutions. Thus, a single instillation of an aqueous solution of pilocarpine lasts 4-6 hours, a prolonged solution on methylcellulose - 8 hours, a gel solution - about 12 hours.

For acute infectious diseases of the eye (bacterial conjunctivitis), the frequency of instillations can reach up to 8-12 per day, for chronic processes (glaucoma) - no more than 2-3 instillations per day. It should be noted that the volume of the conjunctival sac into which the medicinal substance enters is only 1 drop, so the therapeutic effect does not increase with an increase in the amount of instilled liquid.

All eye drops and ointments are prepared under aseptic conditions. Le-

medicinal forms intended for repeated use, in addition to solvent and buffer components, contain preservatives and antiseptics. Drops manufactured in pharmacies do not contain such substances, so their shelf life and use are limited to 7 and 3 days. If the patient is hypersensitive to additional ingredients, single-dose plastic packaging of medicines that do not contain preservatives or preservatives is produced.

The general shelf life requirements for factory-made drops are 2 years if stored at room temperature out of direct sunlight. The period of use of the drug after the first opening of the bottle is 1 month.

The shelf life of eye ointments is on average about 3 years under the same storage conditions. They are placed behind the lower eyelid into the conjunctival cavity, usually 1-2 times a day. It is not recommended to use eye ointment in the early postoperative period during intracavitary interventions.

An additional route of drug administration in ophthalmology is injection: subconjunctival, parabulbar and retrobulbar. In special cases, specialists administer medications directly into the cavity of the eyeball (into the anterior chamber or intravitreal). As a rule, the amount of the administered drug does not exceed 0.5-1.0 ml.

Antibacterial, anti-inflammatory or vasoactive medications are administered by injection. Subconjunctival and parabulbar injections are indicated for the treatment of diseases and injuries of the anterior part of the eye (scleritis, keratitis, irido-

cyclitis, peripheral uveitis), retrobulbar - with pathology of the posterior segment (chorioretinitis, neuritis, hemophthalmos).

When using the injection method of administering the drug, its therapeutic concentration in the cavity of the eyeball increases significantly compared to that during instillation. However, administering drugs by local injection requires some skill and is not always indicated. Instillation of eye drops six times at intervals of 10 minutes for 1 hour is equivalent in effectiveness to subconjunctival injection.

Intramuscular and intravenous injections and infusions (antibiotics, corticosteroids, plasma-substituting solutions, etc.) are also used to treat eye diseases. In intraocular surgery, only unopened disposable packages containing isotonic solutions with the necessary buffer additives are used to achieve a neutral pH.

Drugs can also be administered through phonophoresis or iontophoresis.

During therapy, the pharmacodynamic and pharmacokinetic characteristics of drugs should be taken into account.

Features of pharmacodynamics ophthalmic dosage forms are selective in their action on eye tissue and low systemic reabsorption. Thus, drugs used in ophthalmology have mainly local pharmacological effects and rarely have systemic effects on the body.

When drugs are administered orally and parenterally, they undergo absorption, biotransformation and excretion. The penetration of medicinal substances into the eye tissue during systemic use depends on their ability to penetrate

through the blood-ophthalmic barrier. Thus, dexamethasone easily penetrates various tissues of the eyeball, while polymyxin practically does not penetrate into them.

26.2. Medicines used in ophthalmology

Classification of drugs used to treat eye diseases

1. Anti-infective drugs.

1.1. Antiseptics.

1.2.Sulfanilamide drugs.

1.3.Antibiotics.

1.4. Antifungal drugs.

1.5. Antiviral drugs.

2. Anti-inflammatory drugs.

2.1. Glucocorticosteroids.

2.2.Non-steroidal anti-inflammatory drugs.

2.3. Antiallergic drugs.

3. Drugs used to treat glaucoma.

3.1.Medications that improve the outflow of intraocular fluid.

3.2. Agents that inhibit the production of intraocular fluid.

4. Anticatarrhal drugs.

5. Mydriatics.

5.1. Long-term (therapeutic) action.

5.2.Short (diagnostic) action.

6. Local anesthetics.

7. Diagnostic tools.

8. Ophthalmic drugs of different groups.

9. Drugs for the treatment of age-related macular degeneration.

26.2.1. Anti-infective drugs

26.2.1.1. Antiseptics

For the treatment and prevention of infectious diseases of the eyelids and conjunctiva, various drugs that have antiseptic, disinfectant, deodorizing and anti-inflammatory effects are widely used.

Antiseptic agents are used to treat the edges of the eyelids in the treatment of blepharitis, barley, for the treatment of conjunctivitis, keratitis and the prevention of infectious complications in the postoperative period, for injuries of the conjunctiva, cornea and foreign bodies entering the conjunctival sac.

Combined preparations containing boric acid - 0.25% zinc sulfate solution, 2% boric acid solution(Zinci sulfas + Acidum borici) - eye drops in dropper tubes of 1.5 ml - used for the treatment of catarrhal forms of infectious conjunctivitis, administered 1 drop 1-3 times a day. Preparations containing boric acid are not recommended for use in dry eye syndrome.

It must be remembered that boric acid easily penetrates the skin and mucous membranes, especially in young children, is slowly eliminated from the body and can accumulate in tissues and organs, resulting in the development of toxic reactions (nausea, vomiting, diarrhea, desquamation of the epithelium, headache pain, impaired consciousness, oliguria), therefore it is not recommended to use drugs containing boric acid during pregnancy, lactation and in pediatric practice, especially in newborns, and also not

preparations containing boric acid solution in concentrations above 2% should be used due to possible teratogenic effects.

Medicines containing silver salts - 1% silver nitrate solution, 2% collargol solution, 1% protargol solution- used for the prevention of blenorrhea in newborns. For this purpose, they are instilled once immediately after the birth of the child. Silver preparations are not compatible with organic substances, chlorides, bromides, iodides. With their long-term use, it is possible to stain the eye tissues with reduced silver (argyrosis).

Antiseptic Miramistin(okomistin) - 0.01% eye drops - used in the treatment of acute and chronic conjunctivitis, blepharoconjunctivitis, keratitis, keratouveitis, in the pre- and postoperative periods for the prevention of infectious complications, and eye injuries. Dosage: 1-2 drops 4-6 times a day until clinical recovery, for prophylactic purposes - 2-3 days before surgery and for 10 days after it, 1-2 drops 3 times a day. Contraindications: age up to 18 years, pregnancy, breastfeeding period.

Antiseptic drugs also include fluoroquinolone derivatives.

Fluoroquinolones. When used systemically, fluoroquinolones easily pass through the blood-ophthalmic barrier into the intraocular fluid.

Drugs in this group (norfloxacin, ciprofloxacin, ofloxacin, lomefloxacin) are used for the treatment of infectious diseases of the eyelids, lacrimal organs, conjunctiva, cornea, including trachoma and paratrachoma, as well as for the prevention of infectious complications after eye surgeries and injuries.

Fluoroquinolones are used in the form of 0.3% eye drops and ointment. In case of a mild infectious process, eye drops containing fluoroquinolones are instilled 1 drop into the conjunctival sac of the affected eye 5-6 times a day or a strip of ointment 1-1.5 cm long is placed behind the lower eyelid 2-3 times a day. In the event of a severe infectious process, the drug is instilled every 15-30 minutes or a strip of ointment 1-1.5 cm long is applied every 3-4 hours. As the severity of inflammation decreases, the frequency of use of the drug is reduced. The duration of treatment is no more than 14 days.

When treating trachoma, 1-2 drops of the drug are instilled into the conjunctival sac of the affected eye 2-4 times a day for 1-2 months.

The drugs should not be used in case of hypersensitivity to it, pregnancy, lactation and in children under 15 years of age.

26.2.1.2. Sulfonamide drugs

Used in ophthalmology sulfacetamide(sulfacyl sodium, Sulfacilum natrium) in the form of 10 and 20% solution (eye drops) and 30% ointment (in tubes), which are used for the prevention and treatment of conjunctivitis, blepharitis and keratitis; A 20% solution is used for the prevention and treatment of gonorrheal eye diseases in newborns and adults.

Sulfonamides are instilled into the conjunctival sac, 1 drop 5-6 times a day, to prevent blenorrhea in newborns - 1 drop of a 20% solution in each eye three times with an interval of 10 minutes.

When sulfonamide drugs are used in combination with novocaine and dicaine, their bacteriostatic effect is reduced, which

due to the content of the residue in the molecule of dicaine and novocaine pair-aminobenzoic acid. Lidocaine and oxybuprocaine do not have an antisulfonamide effect. The incompatibility of sulfonamide drugs with silver salts has been established.

26.2.1.3. Antibiotics

For the prevention and treatment of infectious diseases of the eyeball and its auxiliary apparatus, antibacterial drugs belonging to various groups are used (chloramphenicol, tetracyclines, macrolides, aminoglycosides, fluoroquinolones, fusidic acid, polymyxins). The choice of antibacterial drug depends on the sensitivity of pathogenic microorganisms and the severity of the infectious process.

In the treatment of infectious eye diseases, antibacterial drugs are used not only in the form of ophthalmic dosage forms (eye drops, ointments and films), but also injectable solutions (subconjunctival, parabulbar, intramuscular and intravenous) and intraocular administration of drugs.

Chloramphenicol(Levomycetin, Laevomycetinum). A broad-spectrum antibiotic used in the form of eye drops (0.25% solution), when applied locally and systemically, easily passes the blood-ophthalmic barrier. The therapeutic concentration of chloramphenicol when applied topically is created in the cornea, aqueous humor, iris, and vitreous body; The drug does not penetrate into the lens.

Tetracyclines(Tetracycline). Tetracyclines do not penetrate into the eye tissue through intact epithelium. If the corneal epithelium is damaged, the effective concentration

The concentration of tetracycline in the moisture of the anterior chamber is achieved 30 minutes after application. When used systemically, tetracycline has difficulty passing through the blood-ophthalmic barrier.

In ophthalmology, both tetracycline and ditetracycline, a dibenzylethylenediamine salt of tetracycline, which has a prolonged effect, are used. When applied topically, the antibacterial effect lasts for 48-72 hours. Oxytetracycline is excluded from the list of drugs

funds.

Antibacterial drugs belonging to the tetracycline group are used for the prevention and treatment of infectious conjunctivitis and keratitis, as well as for the treatment of trachoma. It should be noted that tetracycline is used to prevent blenorrhea in newborns. It is not recommended to use these drugs for therapeutic purposes in newborns and children under 8 years of age. An increase in the antibacterial effect of tetracyclines is observed when combined with oleandomycin and erythromycin.

Drugs in this group are produced in the form of 1% eye ointment, which is placed behind the lower eyelid: tetracycline ointment 3-5 times a day, ditetracycline 1 time. It is not recommended to use the drug for more than 10 days, with the exception of treatment of trachoma, the duration of which can be 2-5 months. The duration of treatment is determined by the doctor. To prevent blenorrhea in newborns, a strip of tetracycline ointment 0.5-1 cm long is placed behind the lower eyelid once.

Macrolides. For the treatment of infectious eye diseases and the prevention of blenorrhea in newborns, it is used erythromycin (Erytromycin), which belongs to the group of macrolides.

In the treatment of conjunctivitis, keratitis, trachoma and for the prevention of benorrhea in newborns, erythromycin is used in the form of an eye ointment (10,000 units), which is placed behind the lower eyelid 3 times a day, and in the treatment of trachoma 4-5 times. The duration of treatment depends on the form and severity of the disease, but should not exceed 14 days. For trachoma, treatment should be combined with follicular expression. After the inflammatory process subsides, the drug is used 2-3 times a day. The duration of treatment for trachoma should not exceed 3 months.

To prevent blenorrhea in newborns, a strip of ointment 0.5-1 cm long is placed behind the lower eyelid once.

Glycopeptide antibiotics also include vancomycin (Vancomycin). The drug easily penetrates the tissue of the eyeball when applied locally and systemically. The maximum concentration of the drug in the eye tissues is achieved within 1 hour after administration, the effective concentration is maintained for 4 hours. Vancomycin does not have a toxic effect on the eye tissues when administered intraocularly.

To treat eye diseases, vancomycin is administered intravenously at a dose of 0.5-1 g every 8-12 hours. In addition, intravitreal administration is used.

Aminoglycosides (gentamicin, tobramycin). The simultaneous use of several aminoglycoside antibiotics (possible nephrotoxic and ototoxic effects, disruption of mineral metabolism and hematopoiesis), their combined use with erythromycin and chloramphenicol (due to pharmaceutical incompatibility), polymyxin B, colistin, cephalosporins, vancomycin, furosemide, anesthetics is not recommended.

Aminoglycoside antibiotics are produced in the form of eye drops (0.3% gentamicin solution), 0.3% ointment and ophthalmic medicinal films.

For a moderately severe infection, 1-2 drops of the drug are instilled into the conjunctival sac every 4 hours or a 1.5 cm long strip of ointment is placed behind the lower eyelid of the affected eye 2-3 times a day. In the event of a severe infectious process, the drug is instilled every hour or the ointment is placed behind the lower eyelid every 3-4 hours. As the severity of inflammation decreases, the frequency of drug instillations is reduced. The duration of treatment is no more than 14 days.

Antibiotics from the aminoglycoside group are often used as part of combination antibacterial drugs.

26.2.1.4. Antifungal drugs

Currently, there are no officially registered ophthalmic forms of antifungal drugs in Russia. A 5% natamycin ophthalmic suspension is widely used abroad. Drugs that are used systemically for oral administration include nystatin, ketoconazole, miconazole, fluconazole and flucytosine.

26.2.1.5. Antiviral drugs

In the treatment of viral eye diseases, chemotherapeutic agents (antimetabolites) are used, as well as drugs that have nonspecific and specific immunocorrective effects.

One of the first antimetabolites was synthesized 5-iodo-2-deoxyuridine(idoxuredin, IMU) -

halogenated analogue of thymidine. Idoxuredin is a highly effective antiviral drug, but it has a narrow spectrum of antiviral activity, since it is effective only against the herpes simplex virus. When applied topically in a therapeutic concentration, IDU is determined only in the epithelium and to a lesser extent in the stroma of the cornea; a small amount of it, which does not have a virucidal effect, accumulates in the aqueous humor of the anterior chamber, the iris and the vitreous body.

Taking into account the peculiarities of the pharmacokinetics of IDU, it is used for the treatment of superficial forms of herpetic keratitis in the form of a 0.1% solution, which is instilled 3-5 times a day.

Since long-term use of the drug may develop toxic-allergic reactions of the conjunctiva and cornea (folliculosis, chemosis, diffuse epitheliopathy, corneal edema), the duration of treatment should be no more than 2-3 weeks, and in the absence of signs of remission - 7-10 days.

Acyclovir(Aciclovir) is a highly effective antiviral drug that has a virucidal effect on herpes simplex and herpes zoster viruses, but is less effective against the Epstein-Barr virus and cytomegalovirus. Acyclovir does not affect normal cellular processes and does not delay the process of corneal regeneration.

The drug is used in the form of a 3% eye ointment: a 1 cm long strip of it is placed behind the lower eyelid 5 times a day for 7-10 days. To prevent relapse of the disease, treatment must be continued for 3 days after clinical cure. After applying the ointment, a moderate burning sensation, inflammatory reactions, and punctate keratitis may occur.

In the treatment of deep forms of herpetic keratitis and uveitis, acyclovir is simultaneously used topically, taken orally (200 mg 3-5 times a day for 5-10 days) or administered parenterally (intravenous drip at the rate of 5 mg per 1 kg of body weight every 8 hours within 5 days).

Nonspecific immunotherapy. In the treatment of viral eye diseases, both exogenous interferons and drugs that stimulate the production of endogenous interferons are used. Interferons produced by leukocytes of human donor blood under the influence of a virus and obtained by genetic engineering methods are used as antiviral agents.

Leukocyte interferon human dry (Interferonum leucocyticum humanum siccum) is produced in 2 ml ampoules containing 1000 IU of lyophilized powder for the preparation of a solution. The contents of the ampoule are diluted in 1 ml of sterile distilled water. For superficial keratitis and conjunctivitis, instill 1 drop at least 12 times a day. For stromal keratitis and keratoiridocyclitis, 600,000 IU is administered subconjunctivally daily or every other day. The duration of treatment is 15-25 days.

Oftalmoferon (Ophtalmoferonum) contains 10,000 IU per 1 ml of human recombinant interferon alpha-2. The drug is used for the treatment of adenoviral, hemorrhagic, herpetic conjunctivitis and keratitis, herpetic keratouveitis. In the acute stage of the disease, instill 1 drop 6-8 times a day, when inflammatory phenomena subside - 2-3 times. Treatment is carried out until the symptoms of the disease disappear.

Interferon inducers (interferonogens), when introduced into the human body, stimulate the production of endogenous interferons

different types. Various interferonogens are used to treat viral eye diseases.

Poludan (Poludan) is a biosynthetic interferonogen, which is a complex of polyadenylic and uridylic acids.

The drug is used for viral eye diseases: adenoviral and herpetic conjunctivitis, keratoconjunctivitis, keratitis and keratoiridocyclitis (keratouveitis), iridocyclitis, chorioretinitis, optic neuritis. Poludan is used in the form of eye drops and solutions for subconjunctival injections.

For the treatment of conjunctivitis and superficial keratitis, a solution of poludanum is instilled into the conjunctival sac, 1-2 drops 6-8 times a day. As the inflammatory phenomena subside, the number of installations is reduced to 3-4 times.

For stromal keratitis and keratoiridocyclitis, Poludan solution is administered 0.5 ml subconjunctivally daily or every other day. 15-20 injections are prescribed per course.

Pyrogenal (Pyrogenalum) is a lipopolysaccharide of bacterial origin that has pyrogenic and interferonogenic effects.

The drug is administered subconjunctivally 1 time per day or every 2-3 days. The initial dose is 2.5 mcg (25 MTD), then it is gradually increased to 5 mcg (50 MTD). The course of treatment consists of 5-15 injections depending on the effect.

When treated with pyrogenal, increases in body temperature, headache, nausea, vomiting, and lower back pain are possible.

Cycloferon (Cycloferonum) (Polisan, Russia) - low molecular weight interferon inducer. The drug is administered intramuscularly at a dose of 250 mg once a day. A basic course of 10 injections is carried out according to scheme 1; 2; 4; 6; 8; eleven; 14; 17; 20th and 23rd days.

According to another version, a course of 5 injections is carried out (the first 2 injections are given daily, and then the drug is administered every other day), and then it is repeated after 10-14 days.

For specific immunotherapy normal human immunoglobulin, measles immunoglobulin, chigain (purified human colostrum serum) and antiherpetic vaccine are used. However, these drugs have not received widespread use in clinical practice.

26.2.2. Anti-inflammatory drugs

To treat inflammatory eye diseases, glucocorticosteroids (GCS) and nonsteroidal anti-inflammatory drugs (NSAIDs) are used.

26.2.2.1. Glucocorticosteroids

Depending on the duration of the anti-inflammatory effect, short-, medium-, long- and prolonged-acting GCS are distinguished.

Dosage forms used in ophthalmology contain almost all groups of GCS:

Short-acting corticosteroids (6-8 hours) - hydrocortisone (0.5%; 1% and 2.5% eye ointment);

GCS of medium duration of action (12-36 hours) - prednisolone (0.5% and 1% eye drops);

Long-acting corticosteroids (up to 72 hours) - dexamethasone (0.1% eye drops and ointment); betamethasone (0.1% eye drops and ointment);

Long-acting corticosteroids (7-10 days) - triamcinolone acetonide, betamethasone propionate (injection forms).

GCS, with the exception of hydrocortisone, easily penetrate almost all tissues of the eyeball, including

including into the lens, both with local and systemic use.

Indications for the use of GCS in ophthalmology are quite broad:

Allergic eye diseases (eyelid dermatitis, blepharitis, conjunctivitis and keratoconjunctivitis);

Uveitis;

Sympathetic ophthalmia;

Inflammatory phenomena after injuries and operations (prevention and treatment);

Restoring corneal transparency and suppressing neovascularization after keratitis, chemical and thermal burns (after complete epithelization of the cornea).

GCS is not recommended for use in viral diseases of the cornea (superficial forms of keratitis accompanied by a defect in the epithelium) and conjunctiva, mycobacterial and fungal infections of the eyes. GCS should be used with caution if there is a high risk of increased intraocular pressure.

With long-term use of steroid drugs, an increase in intraocular pressure is possible with the subsequent development of glaucoma, the formation of posterior subcapsular cataracts, a slowdown in the wound healing process and the development of a secondary infection, and fungal infection of the cornea often occurs. The appearance of non-healing ulcers on the cornea after long-term treatment with steroid drugs may indicate the development of fungal invasion. Secondary bacterial infection can occur as a result of suppression of the patient’s protective reaction.

When applied topically, the drug is instilled into the conjunctival sac of the affected eye 3 times a day. Within 24-48 hours of treatment

in case of severe inflammation, the drug can be used every 2 hours. A strip of eye ointment 1.5 cm long is placed behind the lower eyelid 2-3 times a day. Glucocorticosteroids are also used parenterally and orally.

26.2.2.2. Nonsteroidal anti-inflammatory drugs

NSAIDs used in ophthalmology include diclofenac sodium, a derivative of phenylacetic acid, and indomethacin. Diclofenac sodium and indomethacin (0.1% solution - eye drops) have a pronounced anti-inflammatory, antipyretic and analgesic effect, and are also able to inhibit platelet aggregation; with long-term use, they have a desensitizing effect.

NSAIDs are used to inhibit miosis during cataract surgery, treat non-infectious conjunctivitis, prevent and treat postoperative and post-traumatic uveitis, and prevent cystic maculopathy.

Patients tolerate NSAIDs well when applied topically. It is not recommended to use them in the treatment of children, pregnant and lactating women; they should be prescribed with caution to patients with bronchial asthma and severe vasomotor rhinitis.

To prevent pupil constriction during surgery or laser intervention, a 0.1% solution of diclofenac and indomethacin is instilled within 2 hours before the intervention 4 times with an interval of 30 minutes. For therapeutic purposes, the drugs are used 4-6 times a day for 5-14 days. For the prevention of postoperative cystic maculopathy (after cataract extraction, antiglaucomatous op-

radios) NSAIDs are used for a month after the intervention 3 times a day.

26.2.2.3. Antiallergic drugs

Treatment of allergic eye diseases includes the use of corticosteroids, mast cell membrane stabilizers, antihistamines and vasoconstrictors.

Membrane stabilizers. Of the drugs in this group, they are most often used cromoglycic acid (Cromoglic acid). The therapeutic effectiveness of the drug is highest when used for prophylactic purposes. Cromoglicic acid is often used in the treatment of allergic conjunctivitis in conjunction with steroid drugs, thereby reducing the need for them; 2% and 4% solutions (eye drops) of cromoglicic acid are indicated for the treatment of seasonal and other types of allergic conjunctivitis, including hyperpapillary conjunctivitis caused by contact lenses.

A solution of cromoglicic acid is instilled 1 drop into the conjunctival sac 2-6 times a day. Treatment is recommended to begin 7-10 days before the possible development of seasonal allergic conjunctivitis and continue for 7-10 days after the symptoms of the disease disappear.

Immediately after instillation, temporary blurred vision and burning may occur.

In addition to cromoglycic acid, it is used to treat allergic eye diseases. boatsamid (Lodoxamide), which not only

prevents mast cell degranulation, but also inhibits the migration and release of enzymes and cytotactic factors from eosinophils.

Lodoxamide (0.1% solution) is used for the same indications as cromoglycic acid. The drug is instilled 4 times a day. The duration of treatment is no more than 4 weeks. When treating with lodoxamide, side effects are possible: transient burning, tingling, itching in the eyelids, lacrimation, dizziness, blurred vision, swelling of the eyelids, crystal deposition and ulceration of the cornea, fever, dry nasal mucosa, itching.

Antihistamines. These drugs give the fastest effect: in acute allergic conjunctivitis, they quickly reduce itching and swelling of the eyelids, lacrimation, hyperemia and swelling of the conjunctiva. Antihistamines are used to treat allergic eye diseases as both monocomponent and combined drugs. The usual dose is 1 drop 2-3 times a day. It is not recommended to use them during pregnancy and lactation and when treating children under 4 years of age. The most effective are complex preparations that include two components (with antihistamine and vasoconstrictor effects).

Currently, H1 receptor blockers such as olopatadine (Olopatidine), which inhibits the release of allergy mediators from mast cells, has a pronounced antiallergic effect. Doses and application: adults and children over 3 years of age instill 1 drop 2 times a day. Side effects: in some cases (approximately 5%), blurred vision, burning and pain in the eyes, lacrimation, sensation of a foreign body in the eye are noted,

conjunctival hyperemia, keratitis, iritis, swelling of the eyelids, in 0.1-1% of cases - weakness, headache, dizziness, nausea, pharyngitis, rhinitis, sinusitis, bitterness in the mouth, changes in taste.

Vasoconstrictor drugs. Allergic diseases are accompanied by a pronounced vascular reaction, manifested by edema and tissue hyperemia. Sympathomimetic agents that have a vasoconstrictor effect reduce swelling and hyperemia of the conjunctiva.

To reduce the severity of allergy symptoms, use

Table 26.1. Distribution of antihypertensive drugs by application points

monocomponent and combined preparations containing α-adrenergic agonists - tetrazoline naphazoline.

These medications are not recommended for use in cases of hypersensitivity to the drug, in the treatment of patients with angle-closure glaucoma, severe cardiovascular diseases (coronary artery disease, arterial hypertension, pheochromocytoma), metabolic diseases (hyperthyroidism, diabetes mellitus) and children under 5 years of age.

Vasoconstrictor drugs are instilled 2-3 times a day, 1 drop into the conjunctival sac. Continuous use of eye drops for more than 7-10 days is not recommended. If there is no effect within 48 hours, the drug must be discontinued.

Side effects may occur with the use of drugs in this group: blurred vision, irritation of the conjunctiva, increased intraocular pressure, dilation of the pupil. Sometimes systemic side effects are possible: rapid heartbeat, headache, increased fatigue and sweating, increased blood pressure, hyperglycemia.

26.2.3. Drugs used to treat glaucoma

Depending on the effect on the hydrodynamics of the eye, two groups of antiglaucoma drugs are distinguished: those that improve the outflow of intraocular fluid, and those that inhibit its production (Table 25.1).

26.2.3.1. Agents that improve the outflow of intraocular fluid

Cholinomimetics. Of the M-cholinomimetics, pilocarpine and carbachol are used for the treatment of glaucoma.

Pilocarpine (Pilocarpine) is a plant alkaloid obtained from the plant Pilocarpus pinnatifolius Faborandi. The drug is used in the form of pilocarpine hydrochloride or pilocarpine nitrate. Pilocarpine is available in the form of 1%, 2%, 4% or 6% aqueous solution (eye drops), packaged in 1.5 ml dropper tubes or 5, 10 and 15 ml bottles.

The duration of the hypotensive effect with a single instillation of pilocarpine solution varies individually and is 4-6 hours. In this regard, aqueous solutions of the drug must be used 4-6 times a day. The most commonly used are 1% and 2% solutions. A further increase in concentration does not lead to a significant increase in the severity of the hypotensive effect, but the risk of adverse reactions increases significantly. The choice of solution concentration depends on the patient’s individual response to the drug.

In addition, long-acting pilocarpine eye drops are produced, in which a 0.5% or 1% solution of methylcellulose, a 2% solution of carboxymethylcellulose or a 5-10% solution of polyvinyl alcohol is used as a solvent. The duration of action of these drugs with a single instillation is increased to 8-12 hours. The longest-lasting effect is exerted by gel and ointment containing pilocarpine, which are used once a day.

Non-selective sympathomimetics. This subgroup includes epinephrine (Epinephrinum), which is a direct stimulator of α- and β-adrenergic receptors of various localizations.

Epinephrine does not penetrate the cornea well, and to ensure a sufficient therapeutic effect it is necessary to use a high concentration of the drug (1-

2% solutions). In this case, the development of adverse reactions is possible, both local (increased blood pressure, tachyarrhythmia, cardialgia, cerebrovascular disorders) and systemic (burning after instillation, conjunctival hyperemia, deposition of pigment deposits in the conjunctiva and cornea, mydriasis, maculopathy, decreased blood circulation in the optic nerve head ).

Currently, there are no ophthalmic drugs containing adrenaline approved for use in Russia.

Prostaglandins. In recent years, drugs belonging to the prostaglandin subgroup F2a have attracted great interest. By improving the uveoscleral outflow of aqueous humor due to the effect on prostanlandin receptors of various subclasses, these drugs significantly reduce intraocular pressure. According to recent data, increased uveoscleral outflow is caused by a discharge of the extracellular matrix of the ciliary muscle.

The subgroup of prostaglandins F 2a includes two drugs: 0.005% solution latanoprost and 0.004% solution travoprost, Available in 2.5 ml bottles. Drugs of this subgroup have a pronounced hypotensive effect and, according to the literature, improve blood circulation in the tissues of the eye.

Latanoprost (Latanoprost) causes a decrease in IOP approximately 3-4 hours after its administration, the maximum effect is observed after 8-12 hours. The hypotensive effect continues for at least 24 hours. Iphthalmotonus decreases by an average of 35% from the initial level.

3 months after the start of treatment, an increase in pigmentation of the iris from blue to brown is noted. Increased eyelash growth is possible. In rare cases, the severity of anterior uveitis increases and

Travoprost (Travoprost) is a new antiglaucoma agent that effectively stimulates the outflow of intraocular fluid along the uveoscleral pathway. The hypotensive effect corresponds to or exceeds latanoprost.

Prostaglandins are the first choice drugs: they are used to start the treatment of glaucoma.

26.2.3.2. A drug that inhibits the production of intraocular fluid

Selective sympathomimetics.

Drugs in this group include clonidine (Clonidine).

Clonidine helps reduce the production of intraocular fluid. The hypotensive effect appears 30 minutes after administration of the drug, its maximum is observed 3 hours after instillation and lasts up to 8 hours.

Local side effects manifest themselves in the form of burning and a feeling of a foreign body in the eye, dry mouth, nasal congestion, hyperemia and swelling of the conjunctiva, chronic conjunctivitis.

General undesirable effects include drowsiness, slowed mental and motor reactions; bradycardia, constipation, and decreased gastric secretion may occur periodically. The use of clonidine eye drops may be accompanied by a decrease in blood pressure.

It is recommended to use the drug 2-4 times a day. Treatment begins with the appointment of a 0.25% solution. In case of insufficient reduction in IOP, use a 0.5% solution. If adverse reactions occur associated with the use of a 0.25% solution, a 0.125% solution is prescribed.

β -Adrenergic blockers. The drugs of first choice in the treatment of glaucoma in most cases are prostaglandins and beta-blockers.

β 12 -Adrenergic blockers. Non-selective β-blockers include timolol(Timololum).

Timolol inhibits the secretion of intraocular fluid. However, according to some data, with long-term use of timolol, there is an improvement in the outflow of aqueous humor, which is apparently due to the release of the scleral sinus. The hypotensive effect occurs 20 minutes after instillation, reaches a maximum after 2 hours and persists for at least 24 hours. The decrease in IOP is about 35% of the initial level. The difference in the severity of the hypotensive effect of 0.25% and 0.5% timolol solution is 10-15%.

Local side effects: dry eyes, conjunctival irritation, corneal epithelial edema, punctate superficial keratitis, allergic blepharoconjunctivitis.

Treatment begins with the use of a 0.25% solution of timolol 1-2 times a day. If there is no effect, use a 0.5% solution in the same dose. The hypotensive effect should be assessed after 2 weeks of regular use. No less than

Once every six months it is necessary to monitor the condition of the cornea, tear production and visual functions.

β 1 - Adrenergic blockers. Selective β-blockers are widely used in ophthalmology. betoxolol(Betaxolol).

After a single instillation of betaxolol, the hypotensive effect is usually observed after 30 minutes, and the maximum reduction in IOP, amounting to about 25% of the initial level, occurs after

2 hours and persists for 12 hours. According to some data, unlike timolol, betaxolol does not cause

deterioration of blood flow in the optic nerve, but, on the contrary, maintains or even improves it.

Local side effects: short-term discomfort and lacrimation occurring immediately after instillation; punctate keratitis, decreased sensitivity of the cornea, photophobia, itching, dryness and redness of the eyes, anisocoria are rarely observed.

Systemic side effects are similar to those described for timolol. However, the effect on the respiratory system is negligible.

Hybrid (α + β )-adrenergic blockers. In recent years, hybrid adrenergic blockers have attracted interest.

A representative of this group is the original domestic adrenergic blocker proxodolol(Proxodololum), which has a blocking effect on β 12 - and α-adrenergic receptors. The mechanism for reducing ophthalmotonus is to suppress the production of intraocular fluid. The hypotensive effect appears 30 minutes after a single instillation, the maximum reduction in IOP (about 7 mm Hg from the initial level) is observed after 4-6 hours and lasts up to 8-12 hours. The hypotensive effect is significantly pronounced.

Treatment begins with the use of a 1% solution 2-3 times a day. If there is no effect, a 2% solution is prescribed at the same dose. As with the use of other adrenergic blockers, the hypotensive effect of proxodolol develops gradually, so its assessment should be carried out after 2 weeks of regular use.

Side effects: bradycardia, arterial hypotension, bronchospasm in patients sensitive to proxodolol.

Carbonic anhydrase inhibitors. Drugs in this group have a depressing effect on the carbonic anhydride enzyme.

raza, which is contained in the processes of the ciliary body and plays an important role in the production of intraocular fluid.

Brinzolamide (Brinzolamide) is a new topical carbonic anhydrase inhibitor that inhibits the production of intraocular fluid. The drug is released in the form of a 1% ophthalmic suspension. Indications and contraindications for use are the same as for dorzolamide, but patients tolerate brinzolamide better.

Dorzolamide (Dorzolamide) gives the maximum hypotensive effect 2 hours after instillation. The aftereffect persists even after 12 hours. The maximum reduction in IOP is 18-26% of the initial level.

Contraindications: hypersensitivity to the components of the drug.

In 10-15% of patients, punctate keratopathy and an allergic reaction may develop. Visual impairment, lacrimation, and photophobia were noted in 1-5% of patients. Pain, redness of the eyes, development of transient myopia and iridocyclitis are extremely rare. Rarely, systemic side effects may occur, such as headache, nausea, asthenia, urolithiasis, skin rash.

When used as monotherapy, the drug is instilled 3 times a day, when used in combination with other antihypertensive drugs - 2 times. It should be noted that when dorzolamide is used together with other antiglaucoma drugs, the hypotensive effect is enhanced.

Unlike dorzolamide acetazolamide (Acetazolamide) reduces IOP when administered systemically. IOP begins to decrease 40-60 minutes after instillation, the maximum effect is observed after 3-5 hours and IOP remains below the initial level for 6-12 hours.

The drug is used to relieve an acute attack of glaucoma, preoperative preparation

patients, in complex therapy for persistent glaucoma.

When treating glaucoma, acetazolamide is taken orally at 0.125-0.25 g 1-3 times a day. After taking it for 5 days, take a break for 2 days. With long-term treatment with acetazolamide, it is necessary to prescribe potassium preparations (potassium orotate, panangin) and a potassium-sparing diet. When preparing for surgery, acetazolamide is taken 0.5 g on the eve of the operation and in the morning on the day of its execution.

26.2.3.3. Combination drugs

To increase the effectiveness of drug treatment of glaucoma and improve the quality of life of patients, combination drugs have been created containing substances with different mechanisms of hypotensive action, the simultaneous use of which produces an additive effect.

For this purpose, in ophthalmological practice, a combination of β-blockers with cholinomimetics is most often used. One of the most commonly used combinations are a combination of 0.5% solution administration of timolol with 2% pilocarpine solution (fotil, Fotil) or 4% pilocarpine solution (fotil forte, Fotil Forte).

After instillation of these drugs, an effective decrease in IOP occurs starting from the 2nd hour, the maximum effect occurs after 3-4 hours, the duration of the hypotensive effect is about 24 hours. The maximum decrease in IOP is more than 32% of the initial level. Recommended application regimen is 1-2 times a day.

Kosopt - combination of dorzolamide (carbonic anhydrase inhibitor) and ti-

Molola is one of the most effective combinations in the treatment of glaucoma with a pronounced hypotensive effect. The drug is used for the treatment of ocular hypertension, open-angle, including secondary glaucoma, pseudoexfoliative glaucoma. Cosopt is instilled 1 drop 2 times a day. The drug is well tolerated by children aged 2-6 years.

DuoHerbs - a combination of the β-blocker timolol and the prostaglandin travoprost. The drug is used for ocular hypertension and open-angle glaucoma, instilling 1 drop once a day.

26.2.4. Drugs used to treat cataracts

Medicines used to treat cataracts can be divided into several groups: drugs containing inorganic salts in combination with vitamins, cysteine ​​and other drugs that normalize metabolic processes, and drugs containing compounds that normalize redox processes in the lens and inhibit the action quinine compounds.

The group of drugs containing mineral salts and activators of metabolic processes is quite numerous. These drugs may contain one active substance (taurine) or a complex of active substances, such as cytochrome C, adenosine, thiamine, glutathione, nicotinamide and cysteine. The most widely used eye drops oftan-katachrome (OftanCatachrom) and Vitaiodurol.

The second group of drugs is represented by two drugs - pyrenoxine and azapentacene.

Pyrenoxine competitively inhibits the action of quinone substances,

stimulating the transformation of water-soluble protein in the lens into insoluble protein, as a result of which the lens substance becomes cloudy. Pyrenoxine prevents the development of cataracts.

Azapentacene protects sulfhydryl groups of lens proteins from oxidation, activates proteolytic enzymes contained in the moisture of the anterior chamber of the eye.

26.2.5. Midriatics

Mydriasis may be due to an increase in the action of the pupillary dilator under the influence of sympathomimetics, as well as a weakening of the pupillary sphincter due to blockade of cholinergic receptors, while paresis of the ciliary muscle occurs simultaneously. In this regard, M-anticholinergic blockers (indirect mydriatics) and sympathomimetics (direct mydriatics) are used to dilate the pupil.

26.2.5.1. M-anticholinergics

As a result of the blockade of M-cholinergic receptors located in the sphincter of the pupil and the ciliary muscle, passive dilation of the pupil occurs due to the predominance of the tone of the muscle that dilates the pupil and the relaxation of the muscle that constricts it. At the same time, due to relaxation of the ciliary muscle, accommodation paresis occurs.

The intensely pigmented iris is more resistant to dilatation, and therefore, to achieve an effect, it is sometimes necessary to increase the concentration of the drug or the frequency of administration, so one should be wary of over-

redosage of M-anticholinergic drugs. Pupil dilation can trigger an acute attack of glaucoma in patients with glaucoma, people over 60 years of age, and people with farsightedness who are predisposed to developing glaucoma due to the fact that they have a shallow anterior chamber.

Patients should be warned that driving is prohibited for at least 2 hours after the study.

M-anticholinergic agents are distinguished by strength and duration (short, or diagnostic, and long-term, or therapeutic) action.

Long-acting M-anticholinergics are used to achieve cycloplegia for the purpose of studying refraction in children. In addition, they are used to treat spasms of accommodation of a semi-persistent and persistent nature in children with refractive errors and in complex therapy of inflammatory diseases of the anterior region in order to prevent the development of posterior synechiae.

Atropine (Atropinum) has the most pronounced mydriatic and cycloplegic effect. Pupil dilation and cycloplegia after a single instillation of atropine reach a maximum after 30-40 minutes and persist for 10-14 days.

Atropine is used in the form of 0.5% and 1% solution. In adults and children over 7 years of age, a 1% solution is used for therapeutic purposes, which is instilled 2-3 times a day, to achieve cycloplegia - 2 times. In children under 7 years of age, only a 0.5% solution can be used.

The drug is not recommended for use in the treatment of patients with angle-closure glaucoma, severe urination disorders due to prostate adenoma and children under 3 months of age. Atropine should be prescribed with caution to patients with severe diseases of the cardiovascular system.

When treated with atropine, systemic side effects may develop, to reduce the severity of which after instillation it is necessary to clamp the lacrimal canaliculi at the inner corner of the eye.

Local side effects: increased IOP, hyperemia of the skin of the eyelids, hyperemia and swelling of the conjunctiva (especially with long-term use), photophobia.

Atropine is available as 1% eye drops and ointment; 0.5% eye drops containing atropine are prepared ex tempore.

Cyclopentolate (Cyclopentolate) has a less pronounced mydriatic effect than atropine. After a single instillation of cyclopentolate, the maximum pharmacological effect occurs within 15-30 minutes. Mydriasis persists for 6-12 hours, and residual effects of cycloplegia for 12-24 hours.

The drug is used to achieve cycloplegia for the purpose of studying refraction in children, as well as for the treatment of spasms of accommodation of a semi-persistent and persistent nature in children with refractive errors, in complex therapy of inflammatory diseases of the anterior part of the eye in order to prevent the development of posterior synechiae and in preparing patients for cataract extraction.

To examine the fundus, cyclopentolate is instilled 1-3 times, 1 drop at an interval of 10 minutes, to achieve cycloplegia - 2-3 times at an interval of 15-20 minutes. For therapeutic purposes, the drug is used 3 times a day.

Tropicamide (Tropicamid) is a short-acting mydriatic. Pupil dilation after instillation

tropicamide is observed after 5-10 minutes, maximum mydriasis is observed after 20-45 minutes and persists for 1-2 hours, the original pupil width is restored after 6 hours. Maximum paresis of accommodation occurs after 25 minutes and persists for 30 minutes. Complete relief of cycloplegia occurs after 3 hours.

The drug is used in the study of the fundus of the eye, rarely used to determine refraction in young children and for therapeutic purposes in inflammatory eye diseases, for the prevention of posterior synechiae. Tropicamide is available in the form of 0.5% and 1% solutions.

For diagnostic dilatation of the pupil, 1 drop of a 1% solution is instilled once or 1 drop of a 0.5% solution is instilled 2 times with an interval of 5 minutes. After 10 minutes, ophthalmoscopy can be performed. To determine refraction, the drug is instilled 6 times with an interval of 6-12 minutes. After about 25-50 minutes, accommodation paresis occurs and the study can be carried out. For therapeutic purposes, tropicamide is used 3-4 times a day.

The drug should be prescribed with caution to patients with angle-closure glaucoma.

When used, the development of photophobia, increased IOP, and an acute attack of angle-closure glaucoma are possible.

26.2.5.2. Sympathomimetics

Sympathomimetics, being α-adrenergic receptor agonists, increase the tone of the muscle that dilates the pupil, resulting in the development of mydriasis, but paresis of the ciliary muscle and an increase in IOP are not observed. The mydriatic effect is pronounced, but short-lived (4-6 hours), potentiated by M-anticholinergics.

For diagnostic dilation of the pupil and enhancing the effect of anticholinergic drugs, a solution is used before and after surgical interventions on the eyeball phenylephrine (Phenylephrin).

Like M-anticholinergics, phenylephrine is not recommended for use in angle-closure glaucoma. The use of a 10% solution of phenylephrine should be avoided in children and the elderly; in case of cardiovascular diseases it should not be prescribed or a 2.5% solution should be used; it is recommended to use the drug with caution in cases of tachycardia, hyperthyroidism, and diabetes mellitus. Patients should be warned not to drive a car for at least 2 hours after the study.

When using the drug topically, pain and tingling in the eyes may occur (it may be necessary to use local anesthetics a few minutes before instillation of phenylephrine), blurred vision, and photophobia. Sensitive patients may experience systemic side effects: arrhythmia, arterial hypertension, coronary spasm. With simultaneous systemic use of MAO inhibitors, the vasoconstrictor effect may be enhanced.

26.2.6. Local anesthetics

In ophthalmology, local anesthetics are used for conduction, infiltration and surface anesthesia. When using local anesthetics, it is possible to develop local side effects, expressed in damage to the corneal epithelium and allergic reactions, and systemic ones, caused by generalized stabilization of membranes.

To prolong the effect and reduce systemic adverse effects,

For a pleasant effect, local anesthetics can be used in combination with vasoconstrictors.

The most commonly used local anesthetics are novocaine, tetracaine, lidocaine, oxybuprocaine, and proparacaine.

Novocaine (Novocainum) hardly penetrates intact mucous membranes, so it is practically not used for superficial anesthesia. For conduction anesthesia, 1-2% solutions are used, for infiltration anesthesia - 0.25% and 0.5%.

Tetracaine (Tetracaine) is used for superficial anesthesia during outpatient surgical interventions, removal of foreign bodies, and diagnostic procedures (gonioscopy, tonometry, etc.). Anesthesia occurs 2-5 minutes after instillation and persists for 30 minutes-1 hour.

The drug is instilled 1 drop 1-2 times. During outpatient surgical interventions, additional instillations are performed as necessary. Tetracaine is not recommended for use in case of hypersensitivity to it and damage to the corneal epithelium.

The development of such adverse reactions as hyperemia of the mucous membranes, a transient increase in IOP in patients sensitive to the drug, swelling and desquamation of the corneal epithelium, and allergic reactions is possible.

Of the drugs containing tetracaine, the most commonly used dicaine in the form of 1% eye drops (in bottles of 5 and 10 ml).

Lidocaine (Lidocaine) has a more pronounced and prolonged effect compared to other anesthetics. The local anesthetic effect with superficial anesthesia occurs 5-10 minutes after instillation of a 2-4% lidocaine solution and persists for 1-2 hours. With conduction

anesthesia, the effect is observed after 5-10 minutes and persists for

2-4 hours

For superficial anesthesia, lidocaine is used during diagnostic procedures and small-scale outpatient surgical interventions. Before an examination or intervention, instill 1 drop 1-3 times with an interval of 30-60 s; during outpatient surgical interventions, if necessary, it can be instilled additionally.

Oxybuprocaine (Oxybuprocaine) is one of the world's most famous local anesthetics used in ophthalmic practice. Superficial anesthesia of the conjunctiva and cornea occurs within 30 seconds and lasts for 15 minutes.

Long-term (up to 1 hour) anesthesia is provided by instillation of a 0.4% oxybuprocaine solution 3 times with an interval of 4-5 minutes.

The drug is used during diagnostic procedures (immediately before the examination, 1 drop is instilled 1-2 times with an interval of 30-60 s and small-volume outpatient surgical interventions (immediately before the intervention, 1 drop is instilled 3-4 times with an interval of 4-5 minutes).

26.2.7. Diagnostic tools

When performing fluorescein angiography of retinal vessels, optic nerve and anterior segment of the eye, as well as to detect defects in the corneal epithelium, fluorescein sodium(Fluorescein-natrium). Fluorescein angiography of retinal vessels is performed for various forms of retinal abiotrophy, exudative-hemorrhagic forms of central chorioretinopathy of various genes.

for diabetic, hypertensive and postthrombotic retinopathy, nevi and melanoblastomas of the choroid. Fluorescein angiography of the vessels of the optic nerve head is carried out for its swelling, inflammation, pseudocongestion, drusen, etc. In addition, fluorescein angiography of the vascular bed of the anterior segment of the eye is carried out for epibulbar nevi, etc.

The use of fluorescein sodium is contraindicated in case of kidney disease and hypersensitivity to its components. Before using the drug, it is necessary to check the patient's sensitivity to it. To do this, 0.1 ml of a 10% fluorescein solution is injected intradermally. In the absence of a local reaction (redness, swelling, rash), fluorescein angiography is performed after 30 minutes: 5 ml of the drug is administered intravenously quickly (within 2-3 s). Diagnostic testing is performed according to generally accepted methods, taking into account its objectives and the nature of the disease. Repeated administration of fluorescein is possible after 3 days.

When fluorescein is administered, nausea and vomiting are possible; dizziness, short-term fainting, and allergic reactions (urticaria, itching, etc.) are less common. Most of these phenomena go away on their own. In case of severe allergic reactions, desensitizing therapy is carried out.

After administration of fluorescein, a transient yellow discoloration of the skin and mucous membranes (within 6-12 hours) and urine (within 24-36 hours) is sometimes observed. The drug is used in the form of a 10% solution for injection (produced by both domestic industry and foreign companies).

To detect defects in the corneal epithelium, use a 1% solution of fluorescein (eye drops), which is prepared ex tempore.

26.2.8. Ophthalmic drugs of different groups

Moisturizing and astringent eye products (artificial tear preparations). Dry eye syndrome, or keratojunctivitis sicca, develops as a consequence of various eye diseases, as well as systemic diseases (Mikulich syndrome, Sjögren's syndrome, rheumatoid arthritis). In addition, impaired tear secretion occurs with age and as a result of the influence of exogenous factors on the secretion of tear fluid.

Treatment of dry eye syndrome is symptomatic. Therapy mainly consists of replacing the missing tear fluid. As artificial tears, aqueous solutions of varying degrees of viscosity or gel-like tear film substitutes with high viscosity are used.

Substances that can increase viscosity include: semi-synthetic cellulose derivatives in concentrations from 0.5% to 1% (methylcellulose, hydroxypropylmethylcellulose, hydroxyethylcellulose), polyvinylglycol, polyvinylpyrrolidone, polyacrylic acid derivatives, 0.9% dextran solution, carbomer 974 P .

Tear fluid substitutes are used not only for dry eye syndrome, but also for eyelid abnormalities (lagophthalmos, eyelid eversion). These drugs are not recommended for use in infectious diseases of the eyelids, conjunctiva and cornea. The frequency of use is determined individually.

Stimulators of corneal regeneration. In case of diseases of the cornea with damage to the integrity of its surface, injuries and burns of the eye, it is necessary to accelerate its regeneration. For this purpose they use 10% me-

tiluracil ointment, solcoseryl,

cornegel, as well as drugs containing glycosaminoglycans isolated from the cornea of ​​various animals (for example, adgelon). In addition, antioxidants have a stimulating effect on regenerative processes: yeast cytochrome C (0.25% eye drops) and erisod.

Drugs of this group are used in complex therapy of radiation, thermal, chemical burns of the conjunctiva and cornea, injuries of the anterior part of the eye, erosive and dystrophic keratitis. They are usually used 3-6 times a day.

Drugs that have fibrinolytic and antioxidant effects. Many eye diseases are accompanied by the development of hemorrhagic and fibrinoid syndrome, for the treatment of which various fibrinolytic drugs are used.

The most widely used enzymatic preparations are the prolonged streptokinase analogue streptodecase And urokinase. For the treatment of intraocular hemorrhages of various origins and dyscirculatory disorders in the retinal vessels, these drugs are administered parabulbarly in 0.3-0.5 ml (30,000-45,000 FU). In addition, streptodecase can be used in the form of ophthalmic medicinal films.

The RKNPK of the Ministry of Health of the Russian Federation has developed

a drug "Gemaza" - lyophilized powder (in ampoules of 5000 units), which contains recombinant prourokinase. The drug has a pronounced fibrinolytic effect; it is administered parabulbarly and subconjunctivally.

Of significant interest are domestic drugs that have not only a fibrinolytic effect, but also an antioxidant and retinoprojector effect - emoxipine and hystrochrome.

Emoxipin (Emoxipinum) has long been successfully used to treat various eye diseases. It has an antioxidant effect, stabilizes the cell membrane, inhibits platelet and neutrophil aggregation, has fibrinolytic activity, increases the content of cyclic nucleotides in tissues, reduces the permeability of the vascular wall, and also, having retinoprotective properties, protects the retina from the damaging effects of high-intensity light.

The drug is used for the treatment of intraocular hemorrhages of various origins, angioretinopathy (including diabetic retinopathy); chorioretinal dystrophies; thrombosis of the central retinal vein and its branches; complicated myopia. In addition, emoxipine is used for the treatment and prevention of damage to eye tissue by high-intensity light (sun rays, laser radiation during laser coagulation); in the postoperative period in patients with glaucoma accompanied by choroidal detachment; for dystrophic diseases, injuries and burns of the cornea.

The drug is used in the form of a 1% solution for injection and eye drops. Emoxypine solution is administered subconjunctivally (0.2-0.5 ml or 2-5 mg) and parabulbarly (0.5-1 ml or 5-10 mg) once a day or every other day for 10-30 days , treatment can be repeated 2-3 times a year. If necessary, retrobulbar administration of 0.5-1 ml of the drug is possible once a day for 10-15 days.

Histochrome (Hystochrom) - a preparation containing echinochrome - chi-

noid pigment of marine invertebrates. Histochrome acts as an interceptor of free radicals arising from lipid peroxidation and a chelator of free iron cations that accumulate in the area of ​​ischemic damage. In addition to the antioxidant effect, the drug has a retinoprotective and bactericidal effect. Histochrome is used in the form of a 0.02% solution (in ampoules of 1 ml). The drug is administered subconjunctivally and parabulbarly for the treatment of hemorrhagic and fibrinoid syndromes.

Drugs used to treat age-related macular degeneration. Age-related macular degeneration is the most common cause of vision loss in people over 65 years of age in all developed countries. To treat the wet form of age-related macular degeneration, inhibitors of vascular growth in the retina and choroid are used.

Ranibizumab (Lucentis) binds and inactivates all isoforms of vascular endothelial growth factor (VEGF-A), resulting in blocking VEGF-mediated angiogenesis. The drug has a low molecular weight and is able to block the growth of new blood vessels. At intravitreal administration, it suppresses neovascularization and proliferation of choroidal vessels, stops the progression of the exudative-hemorrhagic form of age-related macular degeneration. For neovascular (wet) form of age-related macular degeneration in adults, the drug is used in the form of intravitreal injections of 0.5 mg (0.05 ml) once a month.

At the beginning of the article, we will briefly consider the physiology of the eye, as well as the features and routes of administration of ophthalmic agents. used in the diagnosis of anisocoria and myasthenia, the treatment of glaucoma, and during ophthalmological operations (including laser surgery). prescribed for phlegmon of the orbit, conjunctivitis, keratitis, endophthalmitis, retinitis, uveitis. and, used as adjuncts, and anti-inflammatory drugs are important in the treatment of uveitis, retinitis, optic neuritis. We will focus on artificial tears and other moisturizing agents prescribed for xerophthalmia, as well as osmotic agents used to reduce intraocular pressure. In addition, promising methods of therapeutic ophthalmology are considered: immunotherapy, interventions at the molecular and cellular level (including the use of protein kinase C inhibitors for diabetic retinopathy), and the use of neuroprotective agents for glaucoma.

Historical reference

In Mesopotamia (3000-4000 BC), eye diseases were associated with the presence of evil spirits and were treated with the help of religious rituals, additionally using plant, animal and mineral substances. During the time of Hippocrates (460-375 BC), the founder of ancient Greek medicine, hundreds of remedies were described for the treatment of eye diseases. Galen and Susruta classified eye diseases according to anatomical principles and used the treatment methods proposed by Hippocrates (including surgery) (Duke-Elder, 1962; Albert and Edwards, 1996).

For a long time, eye diseases were treated empirically, using drugs intended for the treatment of internal diseases. So, back in the early 17th century, silver nitrate was used in medicine. Later, Crede proposed using this remedy to prevent conjunctivitis in newborns, which often led to blindness (at that time its main causative agent was Neisseria gonorrhoeae). In the 19th century, numerous organic substances were isolated from plants and began to be prescribed for eye diseases. Belladonna alkaloids were used as a poison, in the treatment of bronchial asthma, for cosmetic purposes, and in the early 1800s. Henbane and belladonna began to be used to treat iritis. In 1832, atropine was isolated, which immediately found application in ophthalmology. Pilocarpine was isolated in 1875; in 1877 it was discovered that it could reduce intraocular pressure, and this drug became the basis for the safe and effective treatment of glaucoma.

Brief information about the anatomy and physiology of the eye

The eye is a highly specialized sensory organ. It is separated from the systemic circulation by several barriers: blood-retina, blood-aqueous humor, blood-vitreous humor. Thanks to this isolation, the eye is a unique pharmacological laboratory for studying, in particular, autonomic influences and inflammatory processes. The eye is the most accessible organ for research. However, drug delivery to ocular tissue is both simple and complex (Robinson, 1993).

Accessory organs of the eye

Figure 66.1. Anatomy of the eyeball, orbit and eyelids.

Figure 66.2. Anatomy of the lacrimal organs.

The bony container for the eyeball is the orbit, which has numerous clefts and openings through which nerves, muscles, and blood vessels pass (Fig. 66.1). Fatty tissue and connective tissue ligaments (including the vagina of the eyeball, or Tenon's capsule) are its support, and six extraocular muscles control movements. Behind the eyeball is the retrobulbar space. To safely administer drugs under the conjunctiva, into the episcleral (Tenon's) or retrobulbar space, you need to have a good knowledge of the anatomy of the orbit and eyeball. The eyelids perform a number of functions, the most important of which - protecting the eye from mechanical and chemical influences - is possible thanks to the eyelashes and abundant sensory innervation. Blinking is a coordinated contraction of the orbicularis oculi muscle, the levator palpebrae superioris muscle, and the Müller muscle; When blinking, tear fluid is distributed over the surface of the cornea and conjunctiva. The average person blinks 15-20 times per minute. The outer surface of the eyelid is covered with thin skin, and the inner surface is lined with the conjunctiva of the eyelids, a mucous rich in blood vessels that continues into the conjunctiva of the eyeball. At the junction of the conjunctiva from the upper and lower eyelids to the eyeball, the upper and lower fornix of the conjunctiva are formed. Medicines are usually injected into the lower fornix.

The lacrimal apparatus consists of glands and excretory ducts (Fig. 66.2). The lacrimal gland is located in the upper outer part of the orbit; in addition, the conjunctiva contains small accessory lacrimal glands (Fig. 66.1). The lacrimal gland is innervated by autonomic fibers (Table 66.1). The blockade of its parasympathetic innervation explains complaints of dry eyes in patients taking drugs with, for example, and. The meibomian glands are located in the thickness of the cartilage of each eyelid (Fig. 66.1), their fatty secretion prevents the evaporation of tear fluid. In case of damage to these glands (with rosacea, meibomitis), the structure and function of the film of tear fluid covering the cornea and conjunctiva may be disrupted.

The tear fluid film can be represented as three layers. The outer layer is mainly formed by lipids secreted by the meibomian glands. The middle layer (accounting for 98%) consists of moisture produced by the lacrimal gland and accessory lacrimal glands. The inner layer bordering the corneal epithelium is mucus secreted by the goblet cells of the conjunctiva. The nutrients, enzymes and immunoglobulins contained in the tear fluid nourish and protect the cornea.

The lacrimal ducts begin from small lacrimal puncta located at the inner corner of the eye on the upper and lower eyelids. When blinking, tear fluid enters the lacrimal puncta, then into the lacrimal canaliculi, lacrimal sac, and finally into the nasolacrimal duct, which opens under the inferior turbinate (Fig. 66.2). The mucous membrane of the lower nasal passage is lined with ciliated epithelium and is abundantly supplied with blood; for this reason, locally applied ophthalmic agents can enter through the lacrimal ducts directly into the bloodstream.

The influence of autonomic nerves on the eye and its auxiliary organs

	Adrenergic receptors		Cholinergic receptors
Corneal epithelium		Not known		Not known
Corneal endothelium		Not known	Indefined	Not known
Pupil dilator
Pupil sphincter
Trabecular meshwork		Not known
Epithelium of ciliary processes 6		Aqueous humor production
Ciliary muscle		Relaxation		Contraction (accommodation)
Lacrimal gland		Secretion		Secretion
Retinal pigment epithelium		Not known; possibly water transport
a The corneal epithelium of most species is rich in acetylcholine and choline acetyltransferase, but the function of acetylcholine is unclear (Baratz et al., 1987; Wilson and McKean, 1986). 6 The epithelium of the ciliary processes is also the point of application of carbonic anhydrase inhibitors. Carbonic anhydrase 11 is present in the inner (containing pigment cells) and outer (pigmentless) layers of the epithelium covering the ciliary body (Wistrand et al., 1986). c Although β 2 -adrenergic receptors mediate relaxation of the ciliary muscle, they have little effect on accommodation.

Eyeball

Figure 66.3. A. Anatomy of the eyeball. B. Anterior part of the eye: cornea, lens, ciliary body, iridocorneal angle.

The anterior and posterior sections of the eye are distinguished (Fig. 66.3, A). The anterior section includes the cornea (including the limbus), anterior and posterior chambers, trabecular meshwork, venous sinus of the sclera (Schlemm's canal), iris, lens, ciliary band (ligament of Zinn), ciliary body. The posterior section consists of the sclera, the choroid itself, the vitreous body, the retina, and the optic nerve.

Anterior section. The cornea is transparent, devoid of blood vessels and consists of five layers: epithelium, anterior limiting plate (Bowman's membrane), stroma, posterior limiting plate (Descemet's membrane), endothelium (Fig. 66.3, B).

The corneal epithelium prevents the penetration of foreign substances, including drugs; its cells are arranged in 5-6 layers. Under the basement membrane of the epithelium lies a layer of collagen fibers - the anterior limiting plate (Bowman's membrane). Approximately 90% of the total thickness of the cornea is permanent stroma. The stroma is hydrophilic and consists of plates of collagen fibers arranged in a special way, which are synthesized by flat process cells (a type of fibroblast). This is followed by the posterior limiting plate (Descemet's membrane), which is the basement membrane of the corneal endothelium. It, in turn, is formed by one layer of cells connected by tight junctions and is responsible for the processes of active transport between the cornea and the aqueous humor of the anterior chamber; Like the epithelium, the endothelium is a hydrophobic barrier. Thus, to penetrate the cornea, the drug must overcome the hydrophobic-hydrophilic-hydrophobic barrier.

The transition zone between the cornea and the sclera is called the limbus; its width is 1-2 mm. Outside the limbus is the epithelium of the conjunctiva (contains stem cells), the vagina of the eyeball and the episclera originate nearby, the venous sinus of the sclera and the trabecular meshwork, including its corneal-scleral part, pass below (Fig. 66.3, B). Like tear fluid, the blood vessels of the limbus provide nutrition and immune protection to the cornea. The anterior chamber holds about 250 µl of aqueous humor. The iridocorneal angle is limited in front by the cornea, and in the back by the root of the iris. Above its apex are the trabecular meshwork and the venous sinus of the sclera. The posterior chamber contains approximately 50 µl of aqueous humor and is limited by the posterior surface of the iris, the anterior surface of the lens, the ciliary band (zinc ligament) and part of the inner surface of the ciliary body.

Exchange of aqueous humor and regulation of intraocular pressure. Aqueous humor is secreted by the ciliary processes, passes through the pupil from the posterior chamber to the anterior chamber, and then seeps through the trabecular meshwork into the venous sinus of the sclera. From there, aqueous humor enters the episcleral veins and then into the systemic circulation. 80-95% of aqueous humor flows out this way, and in glaucoma it serves as the main point of application. Another outflow pathway is uveoscleral (through the ciliary body into the perichoroidal space) - the point of application of some prostaglandin analogues.

Figure 66.4. Autonomic innervation of the eye (A - sympathetic nerves, B - parasympathetic nerves).

Figure 66.5. Diagnostic algorithm for anisocoria.

According to the state of the iridocorneal angle, open-angle and closed-angle glaucoma are distinguished; the first is much more common. Modern drug treatment of open-angle glaucoma is aimed at reducing the production of aqueous humor and increasing its outflow. The preferred method of treating angle-closure glaucoma is iridectomy (including laser), however, medications are used before surgery to immediately stop the attack and eliminate corneal edema. As discussed in other chapters, in people with a predisposition to attacks of angle-closure glaucoma (usually with a shallow anterior chamber of the eye), intraocular pressure may increase sharply after taking M-anticholinergics, adrenergic agents, and H1-blockers. However, usually these people are not aware of the danger that threatens them - they consider themselves healthy and do not even suspect that they are at high risk of an attack of angle-closure glaucoma. In the instructions for the listed drugs, when describing side effects, they do not always indicate the form of glaucoma. For this reason, such drugs are avoided by patients with open-angle glaucoma, which is most common in the United States, although these drugs are not contraindicated in such patients. In the presence of the described anatomical features, M-anticholinergic blockers, adrenergic drugs and H1-blockers can cause pupil dilation and excessive forward displacement of the lens. As a result, the outflow of aqueous humor from the posterior chamber to the anterior chamber is disrupted, the pressure in the posterior chamber increases, the root of the iris is pressed against the wall of the iridocorneal angle and blocks the absorption of aqueous humor in it, which causes intraocular pressure to increase even more.

Iris and pupil. The choroid is divided into three sections: the iris, the ciliary body and the choroid itself. The anterior surface of the iris is formed by stroma, which does not have a clear structure and contains melanocytes, blood vessels, smooth muscles, parasympathetic and sympathetic nerves. The color of the iris is determined by the number of melanocytes in the stroma. These individual differences influence the distribution of drugs that bind to melanin (see below). The posterior surface of the iris is covered with double-layer pigment epithelium. In front of it there is a smooth muscle dilator of the pupil, the fibers of which are located radially and have (Fig. 66.4); When this muscle contracts, the pupil dilates. At the edge of the pupil there is a smooth muscle sphincter of the pupil, which consists of circular fibers and has parasympathetic innervation; its contraction leads to a narrowing of the pupil. The use of mydriatics for pupil dilation (for example, during ophthalmoscopy) and pharmacological tests (for example, for anisocoria in patients with Horner or Holmes-Eydie syndromes), see Table. 66.2. In Fig. 66.5 describes the diagnostic algorithm for anisocoria. Ciliary body. It performs two important functions: the double-layer epithelium of the ciliary processes secretes aqueous humor, and the ciliary muscle provides accommodation. The anterior part of the ciliary body, called the ciliary crown, consists of 70-80 ciliary processes. The back part is called the ciliary circle, or flat part. The ciliary muscle consists of outer longitudinal, middle radial and inner circular fibers. When the parasympathetic nervous system is activated, they contract in concert, leading to relaxation of the fibers of the ciliary girdle, which is why the lens becomes more convex and moves slightly forward, and the image of nearby objects is focused on the retina. This process, called accommodation, allows images of objects located at different distances from the eye to be projected onto the retina; it is suppressed by M-anticholinergic drugs (paralysis of accommodation). When the ciliary muscle contracts, the scleral spur moves back and inward, causing the spaces between the plates of the trabecular meshwork to expand. This is, at least in part, due to the decrease in intraocular pressure when taking M-cholinergic stimulants and AChE inhibitors.

Pupil reaction to drugs

Pilocarpine solutions of the indicated concentration are not available; they are usually prepared by the attending physician or pharmacist. Before the pilocarpine test, you cannot manipulate the cornea (measure intraocular pressure or check its sensitivity) so as not to disrupt its barrier function. Normally, the pupil does not respond to pilocarpine at such a low concentration; however, with Holmes-Eydie syndrome, there is a phenomenon of increased sensitivity of denervated structures, due to which the pupil narrows.

Lens. The diameter of the lens is about 10 mm. It has the shape of a biconvex lens, is transparent, enclosed in a capsule and supported by the fibers of the ciliary girdle extending from the ciliary body. Basically, the lens consists of lens fibers, and the epithelium from which they are formed covers only the anterior part of the capsule from the inside. Fiber formation occurs throughout life.

Posterior. Drug delivery (both topical and systemic) to the posterior eye is particularly challenging due to various barriers (see above).

Sclera. This is the outermost layer of the eyeball. The sclera is covered with episclera, outside of which is the vagina of the eyeball (Tenon's capsule) or conjunctiva. Between the superficial collagen fibers of the sclera, the tendons of the six extraocular muscles originate. The sclera is pierced by numerous vessels that supply the choroid itself, the ciliary body, the optic nerve, and the iris.

The vessels of the choroid proper supply the outer part of the retina through a capillary network located in the choriocapillary plate. Between the outer layers of the retina and the choriocapillary lamina are the basal lamina (Bruch's membrane) and the pigment epithelium; Thanks to the tight contacts between its cells, the retina is separated from the choroid proper. The pigment epithelium performs many functions, including participation in metabolism (Chapter 64), phagocytosis of the outer segment of photoreceptors, and in many transport processes. Retina. This thin, transparent, highly organized membrane consists of neurons, glial cells and blood vessels. Of all parts of the eye, the visual retina has been studied most intensively (Dowling, 1987). Based on the unique structure and biochemistry of photoreceptors, a model of visual perception was proposed (Stryer, 1987). The genes encoding rhodopsin and its molecular structure have been studied (Khorana, 1992), making it an excellent model for study. Perhaps this will help create targeted treatments for some congenital retinal diseases.

Vitreous body. It is located in the center of the eyeball, occupies about 80% of its volume and consists of 99% water, type II collagen, hyaluronic acid and proteoglycans. In addition, it contains glucose, ascorbic acid, amino acids, and many inorganic salts (Sebag, 1989).

Optic nerve. Its function is to transmit nerve impulses from the retina to the central nervous system. The optic nerve is covered with myelin and consists of 1) an intraocular part (when ophthalmoscopy looks like an optic disc with a diameter of 1.5 mm), 2) an orbital part, 3) an intracanal part, 4) an intracranial part. The optic nerve sheaths are a direct continuation of the membranes of the brain. Today, pathogenetic treatment of some diseases of the optic nerve has become possible. For example, for optic neuritis, IV methylprednisolone is most effective (Beck et al., 1992,1993), and in patients with optic neuropathy caused by glaucoma, the first step is to reduce intraocular pressure.

Pharmacokinetics and side effects of ophthalmic drugs

Ways to increase the bioavailability of drugs

The bioavailability of ophthalmic agents is affected by pH, type of salt, dosage form, solvent composition, osmolality, and viscosity. Features of the various routes of administration are listed in Table. 66.3. Most ophthalmic agents are available in aqueous solutions, and poorly soluble substances are available in suspensions.

The longer the drug is in the conjunctival sac, the better it is absorbed. For this purpose, many dosage forms have been developed - eye gels, ointments, films, disposable soft contact lenses, collagen lenses. Ophthalmic gels (eg, 4% pilocarpine gel) are absorbed by diffusion after the soluble polymer shell breaks down. The polymers used are cellulose ethers, polyvinyl alcohol, carbomer, polyacrylamide, copolymer of vinyl methyl ether with maleic anhydride, poloxamer 407. Ointments are usually made on the basis of petroleum jelly or petroleum jelly; Many antibacterial drugs and agents that dilate and constrict the pupil are produced in this dosage form. The release of the drug from the ocular films due to uniform diffusion obeys first-order kinetics, therefore, over a period of time, the drug is released into the tear fluid at a more constant rate (for example, pilocarpine at a rate of 20 or 40 mcg/h) than with the simultaneous administration of the same dose. Despite these advantages, ocular films have not become widely used, perhaps due to high cost and difficulty in use.

Pharmacokinetics

Basic laws that are valid for systemic use do not fully apply to ophthalmic agents (Schoenwald, 1993; DeSantis and Patil, 1994). The principles of absorption, distribution and elimination are the same, but due to the special routes of administration of ophthalmic agents, other important parameters must be taken into account (Table 66.3, Fig. 66.6). Many dosage forms for external use are available. In addition, drugs can be administered subconjunctivally, into the episcleral (Tenon's) space, retrobulbar (Fig. 66.1, Table 66.3). For example, to increase bioavailability, antibacterial drugs and glucocorticoids, as well as anesthetics, are prescribed by injection before surgery. After glaucoma surgery, the antimetabolite fluorouracil can be administered subconjunctivally to slow fibroblast proliferation and prevent scarring. For endophthalmitis, antibacterial drugs are injected into the eyeball (for example, into the vitreous humor). Some antibacterial drugs, even if the therapeutic concentration is slightly exceeded, can have a toxic effect on the retina; therefore, the dose of the drug for intravitreal administration must be carefully selected.

Features of some routes of administration of ophthalmic agents

Route of administration	Suction	Advantages and indications	Disadvantages and precautions
	Fast, depends on the dosage form	Simple, cheap, relatively safe	It is performed independently, so it is possible that the doctor’s instructions are not followed; toxic effect on the cornea, conjunctiva, nasal mucosa; systemic side effects due to absorption in the nasal cavity
Subconjunctival, episcleral space, retrobulbar	Fast or slow, depends on the dosage form	Inflammatory processes of the anterior part of the eye, choroiditis, cystic macular edema	Local side effects, tissue damage (including the eyeball, optic nerve and extraocular muscles), occlusion of the central retinal artery or vein, direct toxic effect on the retina due to accidental puncture of the eyeball
Into the eyeball (anterior and posterior chambers)		Operations on the anterior part of the eye	Toxic effect on the cornea
0 0 700

Drug treatment in ophthalmology has become much more widespread than surgical treatment. This is due to the technical complexity of surgical interventions in the eyeball area and possible risks.

In addition, many ophthalmological pathologies characterized by impaired visual function are successfully corrected with the help of glasses and. Drugs in ophthalmology can be prescribed both for the treatment and prevention of diseases.

Drug therapy

Drops are the most commonly prescribed drug in ophthalmology

The goal of drug treatment is to eliminate the pathological condition and correct possible complications of the disease.

At the same time, doctors prescribe medications for both treatment and prevention of diseases.

As in any other medical field, in ophthalmology, drug therapy can be used together with surgical treatment to achieve a better therapeutic effect.

The advantages of drug therapy include accessibility, ease of use and a low likelihood of developing severe complications. However, doctors rarely have to choose between surgery and drug therapy, since serious eye diseases have strict indications for treatment.

In addition, surgery often provides greater results. Thus, the advantages and disadvantages of treatment methods often depend on the specific pathology.

The prevalence of drug treatment in ophthalmology may also be explained by the lower availability of effective surgical treatments. Eye microsurgery is a high-tech and expensive field of medicine.

Groups of drugs in ophthalmology

Drugs in ophthalmology

For the treatment and prevention of eye pathologies, drugs of various pharmacological groups are used. The following groups are most widespread:

• Antiseptics are substances used to treat the surface of the eye and destroy infectious agents. In ophthalmology, antiseptic drops and solutions are used.
• Antibiotics are antimicrobial drugs needed to treat a bacterial infection. The most commonly used are macrolides, tetracyclines and sulfonamide group antibiotics. For severe infections, intravenous administration may be indicated.
• Antifungal and antiviral agents are medications for the treatment of fungal and viral diseases.
• Corticosteroid drugs. Most often prescribed for the treatment of inflammatory diseases of the eyeball.
• Antihistamines are medications intended to relieve allergic reactions.
• Drugs to facilitate the outflow of intraocular fluid. Typically used to treat glaucoma, characterized by increased fluid outflow in the chambers of the eye due to impaired fluid outflow.
• Anti-inflammatory drugs are drugs of various pharmacological groups necessary to reduce the inflammatory response in tissues. In ophthalmology, steroidal and non-steroidal anti-inflammatory drugs are used.
• Local anesthetics are solutions or drops that reduce pain in a specific area.
• Expansion facilities. Can be used in diagnostics - for example, for ophthalmoscopy.
• Drugs that affect the tone of intraocular vessels.
• Drugs for the treatment of glaucoma and cataracts.
• Moisturizing drops.

Each listed group of drugs combines many drugs with varying effectiveness. For the treatment of most diseases, several drugs of different pharmacological groups are prescribed.

Methods of drug administration

Preparations in ophthalmology: gel

In the field of prevention and symptomatic treatment of eye diseases, the most common are drops and solutions that allow the active components of drugs to be quickly and effectively delivered to the eye tissues.

Usually these are anti-inflammatory, antihistamine, moisturizing or fortified drops. Drops are also used to treat glaucoma and some infectious diseases.

Other methods of drug administration in ophthalmology:

• Injection is the most invasive method of administering medication. This may be an injection into the area of ​​the vitreous body, subcutaneous fatty tissue or conjunctival mucosa. Intraocular injection is a rather complex and sometimes risky procedure.
• Oral administration – delivery of drugs to the digestive organs through the mouth. The most common and safest method of administration.
• Sublingual administration is the resorption of drugs in the oral cavity with subsequent transportation of the active components through the bloodstream. In ophthalmology, this method is used relatively rarely.

In rare cases, intramuscular and intravenous administration of drugs is also used for the treatment of systemic diseases affecting the visual apparatus.

Thus, drugs in ophthalmology are used everywhere. Drug treatment can be no less effective than surgical treatment.