In what cases is acyclovir taken? Acyclovir: instructions for use, side effects, contraindications

Antiviral agent. Active against herpes simplex virus ( Herpes simplex) type 1 and 2, herpes zoster virus ( Varicella zoster), Epstein-Barr virus and cytomegalovirus. After penetration into a cell infected with a virus, acyclovir is transformed by thymidine kinase into active acyclovir triphosphate. The latter interacts with the viral DNA polymerase and is integrated into the DNA that is synthesized for new viruses. In this way, defective viral DNA is formed, which leads to suppression of the replication of new generations of viruses.
After oral administration, acyclovir is partially absorbed from the digestive tract. After intravenous administration, the half-life of acyclovir in adults is about 2.9 hours. Most of the active substance is excreted unchanged in the urine. Plasma protein binding is 9-33%. The only metabolite of acyclovir is 9-carboxymethoxymethylguanine. In patients with chronic renal failure, the half-life of acyclovir increases. The concentration of the active substance in the CSF is approximately 50% of the concentration in the blood plasma.
When applied to the skin, acyclovir is not detected in the blood serum. From ophthalmic ointment, acyclovir quickly penetrates the corneal epithelium and reaches therapeutic concentrations in the intraocular fluid.

Indications for use of the drug Acyclovir

Infections caused by a virus Herpes simplex, including herpes of newborns (treatment and prevention); herpes zoster; chicken pox (treatment).
Ointment and cream for external use are used to treat herpes simplex of the skin and mucous membranes, primary and recurrent genital herpes. Eye ointment - to treat keratitis caused by a virus Herpes simplex.

Use of the drug Acyclovir

Orally during the day with an interval of 4, 6 or 12 hours. For adults and children over 2 years of age for infections caused by the herpes simplex virus, acyclovir is prescribed 200 mg 5 times a day for 5 days; if necessary, the course of treatment is extended to 10 days. Children under 2 years of age are prescribed 1/2 the dose for adults. For the prevention of recurrent genital herpes - 400 mg 2 times a day or 200 mg 4 times, course - from 6 months to 1 year. To prevent herpetic infection in patients with immunodeficiency or after bone marrow transplantation, acyclovir is prescribed 400 mg 4 times a day during the entire period of risk of developing infection. During treatment Herpes zoster oftalmicus- at a dose of 800 mg 5 times a day for 7-10 days.
For chickenpox, children under 2 years old are prescribed a dose of 200 mg, from 2 to 6 years old - 400 mg, over 6 years old - 800 mg 4 times a day for 5 days (on average at the rate of 20 mg/kg body weight per dose, but not more than 800 mg).
In patients with chronic renal failure with creatinine clearance less than 10 ml/min, acyclovir is used at a dose of 200 mg every 12 hours in the treatment of infections caused by the virus Herpes simplex, and up to 800 mg every 12 hours when treating infections caused by a virus Herpes zoster.
Ointment or cream (5%) for external use is applied to the affected areas of the skin 5 times a day during the daytime with an interval of 4 hours; Duration of treatment is 5-10 days.
A 10 mm long column of 3% ophthalmic ointment is placed behind the lower eyelid every 4 hours, 5 times a day. The duration of treatment for ulcerative forms of keratitis is 7-10 days, interstitial - 10-12 days. Treatment should be continued for 3 days after the symptoms of the disease disappear.
Acyclovir solution is administered intravenously slowly over 1 hour.
Adults and children over 12 years of age with infections caused by viruses Herpes simplex(except herpetic encephalitis) or Varicella zoster, administer an intravenous infusion of acyclovir at a dose of 5 mg/kg every 8 hours; children from 3 months to 12 years - at a dose of 250 mg/m2 every 8 hours for 5-7 days.
Patients with an immunodeficiency state, patients with herpetic encephalitis or infections caused by a virus Varicella zoster, acyclovir is administered at a dose of 10 mg/kg body weight every 8 hours (adults and children over 12 years of age) or 500 mg/m2 every 8 hours (children aged 3 months to 12 years) for 7-10 days.
For prevention purposes, regardless of the type of infection and the age of the patient, intravenous infusions of acyclovir are carried out at a dose of 250 mg/m2 every 8 hours.
Acyclovir is administered to newborns at the rate of 10 mg/kg body weight every 8 hours.
For patients with renal failure, the dose for intravenous infusion is set taking into account creatinine clearance: if the indicator is 20-50 ml/min, acyclovir at a dose of 5-10 mg/kg is administered every 12 hours; with a creatinine clearance of 10-25 ml/min, the recommended dose (5-10 mg/kg) is administered every 24 hours; if the value is less than 10 ml/min, 1/2 of the standard dose is administered every 24 hours immediately after the dialysis session.

Contraindications to the use of the drug Acyclovir

Hypersensitivity to acyclovir.

Side effects of the drug Acyclovir

Possible skin rash, nausea, vomiting, diarrhea, headache, and increased fatigue.

Special instructions for the use of the drug Acyclovir

Treatment with acyclovir should be started as early as possible, if possible during the prodromal period of the disease. The use of acyclovir during pregnancy is possible only for health reasons. The active substance passes into breast milk, so breastfeeding must be stopped during treatment.

Drug interactions Acyclovir

Probenecid, when used simultaneously, increases the concentration of acyclovir in the blood plasma.

Overdose of the drug Acyclovir, symptoms and treatment

In case of oral administration of more than 5 g of acyclovir, it is recommended to monitor the functional state of the kidneys. A single intravenous administration of 80 mg/kg does not cause signs of overdose. Acyclovir is removed from the body during hemodialysis.

List of pharmacies where you can buy Acyclovir:

• Saint Petersburg

An antiviral drug used to treat and prevent infections of the skin and mucous membranes caused by herpes simplex, shingles and chickenpox viruses. Available in the form of tablets, ointment, cream or solution for intravenous infusion.

Instructions for use:

The drug was developed in 1976 by English researcher Gertrude Elion. The scientist received the Nobel Prize for developing the drug. The medicine became widely used in the mid-80s. last century.

Acyclovir is a synthetic analogue of a purified nucleoside. Highly active against herpes simplex virus types 1 and 2, herpes zoster virus, Varicella zoster and Epstein-Barr viruses, as well as cytomegalovirus.

The antiviral activity of Acyclovir is achieved by suppressing the proliferation of viral particles. It is most often used for the treatment of herpes and is highly effective when used before the vesicular stage of the rash.

When used later, it accelerates healing and resolution of elements. The instructions for use of acyclovir indicate that the drug has an immunostimulating effect.

Important: The description of the drug Acyclovir is not intended for prescribing treatment without the participation of a doctor.

Pharmacological properties

Pharmacodynamics

Acyclovir is active against herpes simplex virus types 1 and 2, herpes zoster virus (Varicella zoster), and Epstein-Barr virus. Cytomegalovirus is less sensitive to the action of acyclovir.

The molecular biological mechanism of the antiviral activity of acyclovir is due to competitive interaction with viral thymidine kinase and sequential phosphorylation with the formation of mono-, di- and triphosphate. Acyclovir triphosphate is incorporated instead of deoxyguanosine into the DNA of the virus, inhibits the latter's DNA polymerase and suppresses the replication process.

For herpes, acyclovir prevents the formation of new rash elements, reduces the likelihood of skin dissemination and visceral complications, and accelerates the formation of crusts. Helps reduce pain in the acute phase of herpes zoster.

Pharmacokinetics

When taken orally, regardless of food intake, about 20% of acyclovir is absorbed. Plasma protein binding is relatively low (9-33%). The concentration in the cerebrospinal fluid is approximately 50% of the concentration in plasma. The maximum concentration is determined after 1.5-2 hours.

The half-life of acyclovir when taken orally is about 4 hours. It is excreted mainly by the kidneys unchanged, partially (10-15%) in the form of a metabolite - 9-carboxymethoxymethylguanine.

In case of renal failure, the half-life increases significantly (up to 19.5 hours). Acyclovir penetrates the blood-brain and placental barriers and is excreted in breast milk.

Indications for use of Acyclovir

Acyclovir tablets 0.2 g are used:

Directions for use and doses

The drug is taken orally with plenty of water.

Acyclovir for herpes

For the treatment of infections of the skin and mucous membranes caused by herpes simplex viruses, 1 tablet (0.2 g) is prescribed 5 times a day (except at night).

To prevent infections of the skin and mucous membranes caused by herpes simplex viruses in patients with immune system disorders, adults are prescribed 1 tablet (0.2 g) 4 times a day.

For the treatment of infections caused by herpes zoster viruses, 4 tablets (0.8 g) are prescribed 4-5 times a day. For rectal herpes infection, 2 tablets (0.4 g) are prescribed 5 times a day for 10 days.

For genital herpes, 1 tablet (0.2 g) is prescribed 5 times a day; to prevent relapses of genital herpes infection - 2-5 times a day for 5 days.

Children under two years of age are prescribed half the adult dose; Children over 2 years of age are prescribed the dose for adults.

The duration of treatment is usually 5 days. For infections caused by herpes zoster viruses, treatment is continued for another 3 days after the signs of the disease disappear.

Preventive treatment for organ transplantation is carried out for 6 weeks. The use of the drug in newborns is not recommended.

Acyclovir for chickenpox

The doctor should calculate the dosage of Acyclovir tablets for chickenpox in children based on the child’s body weight and age:

• Up to 2 years – 2–3 r. per day 1 tablet 200 mg.
• After 2 years – up to 5 r. per day, 2 tablets at a time.
• For adolescents and adults, tablets 3–5 r. per day 1–2 pcs.

The duration of oral use of Acyclovir is 5-10 days.

At a 5% concentration, the drug is released in the form of ointment and cream, which accelerate the healing of chickenpox blisters in adults and children. But you cannot apply the ointment to the entire surface of the dermis, because... it makes skin breathing difficult. During treatment, only the affected areas of the body are treated, if possible lubricating the elements in a targeted manner.

Use Acyclovir ointment 5–6 r. per day, no treatment is carried out at night. The product helps to significantly reduce the number of rashes and reduce itching on the 2nd – 3rd day of use.

Features of the use of Acyclovir

Side effects

When taking the drug orally, it is possible

• headache,
• increased fatigue,
• neurological disorders,
• nausea,
• vomit,
• diarrhea.

In addition, there may be an increase in the content of bilirubin, urea and creatinine in the blood serum, and a transient increase in the activity of liver transaminases.

• skin allergic reactions,
• increase in body temperature,
• swelling,
• lymphadenopathy.

Interaction with other drugs

Probenecid slows down the elimination of acyclovir (blocks tubular secretion).

Contraindications

Hypersensitivity to acyclovir.

Pregnancy and lactation

Restrictions on taking the drug include pregnancy and lactation (breastfeeding should be stopped during treatment).

Overdose

Symptoms:

• headache,
• neurological disorders,
• dyspnea,
• nausea,
• vomit,
• diarrhea,
• renal failure,
• lethargy,
• convulsions,
• coma.

Treatment: maintenance of vital functions, hemodialysis.

Acyclovir price

Prices in pharmacies: 60–400 rubles.

Acyclovir analogs

• Zovirax,
• Virolex,
• Acyclovir-Teva,
• Herperax,
• Medovir,
• Acyclostad.

Modern medicine knows eight varieties of the herpes virus. They affect various parts of the human body, leading to serious health consequences. It is impossible to completely cope with such a problem, so treatment is aimed at eliminating the symptoms and transferring the pathogen to a dormant state. The most effective medication is considered to be acyclovir for herpes. It quickly suppresses the activity of viruses. The main thing is not to forget about the features of the product and the rules for its use.

Features of the drug

The herpes virus lives in the body of 90% of all inhabitants of the planet. But it manifests itself in only 5%. The reason for this is a sharp decrease in immunity, hypothermia, prolonged exposure to a stressful situation, or the presence of serious illnesses. Taking antiviral drugs helps to cope with the problem.

The most effective remedy is Acyclovir. It belongs to the group of synthetic ones and is an analogue of a purified nucleoside. Does not have a toxic effect on mammalian cells.

Acyclovir prevents the appearance of rashes, reduces the likelihood of complications, and relieves pain during exacerbation of the disease. The active substance promotes the rapid formation of crusts at the site of rashes.

The bioavailability of the drug varies from 15 to 30%. It spreads quickly throughout the tissues of the body. Metabolized in liver cells. Three hours later it is excreted from the body in the urine.

The dosage and treatment regimen are selected by a specialist based on the patient’s health condition. The location of the virus and the age of the patient are taken into account. During a primary infection, the dosage of the active substance must be high, since the body does not have a sufficient amount of antibodies that fight the disease. It is also allowed to take acyclovir for the prevention of herpes.

The drug is available in two forms:

• Ointment. Packaged in tubes of 2, 5, 10 and 20 grams. Contains a 5% concentration of the active substance. Additional components: chicken fat, polyethylene oxide, water and emulsifiers. Thanks to them, the drug is better absorbed by the skin.
• Pills. The dosage of the active substance in them is 200, 400 or 800 mg. The following auxiliary components are used: lactose, starch, calcium stearate.

The choice of a specific type of drug is made taking into account the nature of the disease and the localization of the virus. On average, ointment costs from 14 to 50 rubles, and tablets from 170 to 190 rubles. There are many positive reviews on the Internet about this drug from people who drank it or used the ointment. This once again emphasizes its effectiveness.

The drug is in tablet form

Acyclovir tablets appear to be an effective treatment for simple and genital herpes. Shingles can also be treated with it. It is often recommended to take it for moderate severity of the disease. It copes poorly with severe forms due to low bioavailability. Only 30% of the total amount of active substance is attacked by the virus. The rest of it doesn't reach him.

The components of the product enter the bloodstream, where infected cells circulate. Viruses produce enzymes that help them maintain their vital functions. Acyclovir reacts with these enzymes and transforms them. The substance loses its ability to integrate into the DNA of the virus, which leads to its death.

The virus settles in the nerve ganglia. This area is not accessible to the immune system and to the drug. Therefore, Acyclovir effectively fights only viruses located on the surface. After completing the course of therapy, part of the infection continues to live in the human body, passing into a latent form.

A course of treatment with the drug allows you to achieve the following results:

• Rapid healing of herpetic wounds.
• No new foci of infection appear.
• Unpleasant symptoms are eliminated: redness, itching, soreness.

After treatment, the disease goes into a latent form for a long time. A sharp decrease in immunity can provoke an exacerbation. Therefore, special attention during and after treatment is paid to increasing the protective functions of the body.

Read also on the topic

What is the incubation period of the herpes virus?

For people with immunodeficiency, the use of the drug is not effective, since their body does not produce enough enzymes that support the functioning of the virus. Therefore, treatment with Acyclovir in patients with HIV or who have undergone chemotherapy is not advisable.

The sooner the use of the drug is started, the higher its effectiveness will be. Take the tablets only with clean water. Drink as much fluid as possible throughout the course of therapy. This helps remove toxic substances from the body. The dosage of the medication is selected individually for each patient by the attending physician. Instructions for use suggest the following treatment regimens:

• Adults drink 200 mg of the drug 5 times a day to treat primary infections. The course of treatment is five days. It can be extended as prescribed by the doctor. For immunodeficiency, the dosage is increased to 400 mg at a time. To treat the Varicella zoster virus, which causes chickenpox, you should drink 800 mg of the drug every four hours a day. At night they take an eight-hour break.
• If acyclovir is used to prevent herpes, then it is taken 200 mg four times a day. If necessary, the regimen is changed and 400 mg is taken twice a day.
• For children, the scheme for taking acyclovir is slightly different. Four doses of 200 mg at a time are enough per day. The duration of therapy is five days. For children under six years of age, the dosage is halved and half a tablet is taken four times a day. For children under three years of age, treatment with acyclovir is contraindicated. Taking a tablet of this medication provokes the development of complications.

It is better to take tablets after meals. This will reduce their negative impact on the stomach. If you miss a dose of acyclovir, do not take two tablets at the same time. First use one, and after a while the other.

Contraindications

Your doctor will tell you how to take acyclovir for the herpes virus in a particular case. Before starting therapy, carefully read the contraindications. This drug should not be taken by patients suffering from the following problems:

• Adrenal dysfunction.
• Disturbances in the functioning of the central nervous system.
• The period of feeding the baby with breast milk.
• Pregnancy.
• Senile age.

If there are such contraindications, taking herpes pills is prohibited. The doctor selects another treatment method that will be safe for the patient.

Possible side effects

During treatment with acyclovir tablets, side effects may occur. Among them are:

• Nausea and bouts of vomiting.
• Pain in the lumbar region.
• Malfunctions of the digestive system.
• The person becomes lethargic and constantly wants to sleep.
• Pain occurs during urination.
• The limbs swell.
• Signs of jaundice.
• Anemia.
• Migraine attacks.
• Cramps.
• Allergic reactions.
• Hair loss.

In rare cases, long-term treatment with acyclovir causes coma. If after therapy you begin to feel unwell or other unpleasant symptoms, consult your doctor.

Application of ointment

Modern pharmacies offer not only ointments and tablets, but also Acyclovir cream. Many people believe that cream and ointment are the same thing. Actually the difference is in the composition. The ointment is based on fatty substances: lanolin, petroleum jelly or others. The cream is less greasy, due to which the active substance is absorbed faster and begins to act.

Read also on the topic

Herpes on the eyelid and around the eye

The choice of product is determined by the location of its application. If you buy acyclovir for herpes on the lips, it is better to give preference to ointment. It will fight viruses and have a moisturizing effect. This will prevent the formation of non-healing wounds and will allow you to quickly cope with the manifestations of the disease. It is better to use cream against genital herpes. It is quickly absorbed into the skin and does not stain underwear.

The methods for using ointment and cream are the same. In such forms, acyclovir is effectively used to prevent herpes. Periodically, problem areas of the body are lubricated with it.

Application rules and dosage

Acyclovir for genital herpes, as well as for other types of this disease, is applied directly to the affected areas. It is allowed to be used not only by adults, but also by children. When applying the product, follow the following rules:

• Before starting the treatment procedure, wipe the area where the drug is applied with a cotton pad soaked in warm water. This will cleanse and prepare the skin.
• The ointment is applied in a thin layer to all affected areas. Do this every four hours. Avoid getting the product on sores located in the mouth. Relief will come on the second day.
• Since the drug is applied pointwise, it is better to use a cotton swab for this. This way, herperviruses will not spread to healthy tissue. For the same purpose, it is recommended to wear gloves during the procedure.
• Treatment for herpes takes seven days. If the wounds do not heal, the course is extended to 10 days.
• Be careful not to get the product into your eyes. It is prohibited to mix it with any cosmetic products.

If herpes appears near the eyes, do not try to treat it yourself; consult a doctor immediately. Otherwise, the virus will spread to the mucous surface of the eye. This provokes partial or complete loss of vision.

Side effects

It is believed that acyclovir ointment does not cause side effects. In rare cases, an allergic reaction to the components of the product is possible. It is manifested by itching, flaking of the skin and redness.

For genital herpes, trying to quickly cope with the problem, some combine all available types of the drug. This leads to a negative reaction from the body. The consequence of improper treatment of the genitals is the development of vulvitis.

Analogs

Acyclovir is not the only drug that successfully treats herpes. Among its closest analogues are:

• Zovirax. In addition to the active substance, it contains propylene glycol. It prevents skin from drying out and relieves puffiness. The cost of this drug is significantly higher compared to Acyclovir.
• Vivorax. The attending physician prescribes this drug if the patient has an allergic reaction to Acyclovir. Despite the fact that the active substance of both drugs is the same, Vivorax does not cause side effects. This is due to the supply of the component in bound form. This product should not be used during pregnancy as it may cause harm to the fetus.
• Gervirax. Contains not only acyclovir, but also propylene glycol, cetyl alcohol, petroleum jelly, nipazole and cremophor. If the permissible dosage is exceeded, peeling of the skin, itching and redness occurs.
• Virolex. The use of this product is not recommended during pregnancy. In rare cases, it provokes headaches, neuralgic disorders, and allergies.

Acyclovir is an effective drug to combat herpes. It can be used only after consultation with a specialist. Only a doctor can correctly determine how many days to use it and in what dosage. Strictly follow all recommendations, and the manifestations of the disease will quickly disappear.

Pharmacodynamics
Mechanism of action
Acyclovir is a synthetic analogue of purine nucleoside that has the ability to inhibit in vitro And in vivo human herpes viruses, including herpes simplex virus (HSV) types 1 and 2, varicella zoster virus (VZV), Epstein-Barr virus (EBV) and cytomegalovirus (CMV). In cell culture, acyclovir has the most pronounced antiviral activity against HSV-1, followed in descending order of activity by: HSV-2, VZV, EBV and CMV.
The effect of acyclovir on herpes viruses (HSV-1, HSV-2, VZV, EBV, CMV) is highly selective. Acyclovir is not a substrate for the thymidine kinase enzyme in uninfected cells, therefore acyclovir is of low toxicity to mammalian cells. Thymidine kinase of cells infected with HSV, VZV, EBV and CMV viruses converts acyclovir into acyclovir monophosphate, a nucleoside analogue, which is then sequentially converted into diphosphate and triphosphate under the action of cellular enzymes. The incorporation of acyclovir triphosphate into the viral DNA chain and subsequent chain termination block further replication of the viral DNA.
In patients with severe immunodeficiency, long-term or repeated courses of acyclovir therapy may lead to the emergence of resistant strains, so further treatment with acyclovir may be ineffective. The majority of isolated strains with reduced sensitivity to acyclovir had a relatively low content of viral thymidine kinase and a disorder in the structure of the viral thymidine kinase or DNA polymerase. Effect of acyclovir on HSV strains in vitro can also lead to the formation of strains less sensitive to it. A correlation has not been established between the sensitivity of HSV strains to acyclovir in vitro and the clinical effectiveness of the drug.
Pharmacokinetics
Suction
In adults, the maximum steady-state concentrations (Cssmax) of acyclovir after a one-hour infusion at a dose of 2.5 mg/kg, 5 mg/kg, 10 mg/kg and 15 mg/kg were 22.7 μmol/L (5.1 μg/ml) ; 43.6 µmol/l (9.8 µg/ml); 92 µmol/L (20.7 µg/ml) and 105 µmol/L (23.6 µg/ml), respectively. The minimum steady-state concentrations of acyclovir in plasma (Css min) 7 hours after infusions were respectively 2.2 µmol/l (0.5 µg/ml); 3.1 µmol/l (0.7 µg/ml); 10.2 µmol/L (2.3 µg/ml) and 8.8 µmol/L (2.0 µg/ml). In children over 1 year of age, comparable Cssmax and Cssmin were observed when administered at a dose of 250 mg/m2 equivalent to 5 mg/kg (adult dose) and at a dose of 500 mg/m2
equivalent to 10 mg/kg (adult dose). In neonates (0 to 3 months) who received acyclovir infusions of 10 mg/kg over more than one hour every 8 hours, Cssmax was 61.2 µmol/L (13.8 µg/ml), and Cssmin - 10.1 µmol/l (2.3 µg/ml).
Distribution
The concentration of acyclovir in the cerebrospinal fluid is approximately 50% of its concentration in plasma.
Acyclovir binds to plasma proteins to a small extent (9-33%), so drug interactions due to displacement from plasma protein binding sites are unlikely.
Removal
In adults, after intravenous administration of acyclovir, the plasma half-life is about 2.9 hours. Most of the acyclovir is excreted unchanged by the kidneys. The renal clearance of acyclovir significantly exceeds the clearance of creatinine, which indicates that acyclovir is eliminated through not only glomerular filtration, but also tubular secretion. The main metabolite of acyclovir is 9-carboxymethoxymethylguanine, which accounts for about 10-15% of the administered dose of the drug in the urine. When acyclovir was administered 1 hour after taking 1 g of probenecid, the half-life of acyclovir and AUC (area under the concentration-time curve) increased by 18 and 40%, respectively.
Special patient groups
The half-life of acyclovir in newborns is approximately 3.8 hours.
In elderly people, the clearance of acyclovir decreases with age in parallel with a decrease in creatinine clearance, but the half-life of acyclovir changes slightly.
In patients with chronic renal failure, the half-life of acyclovir averaged 19.5 hours; during hemodialysis, the average half-life of acyclovir was 5.7 hours, and plasma acyclovir concentrations were reduced by approximately 60%.

Indications for use

Treatment of infections caused by the herpes simplex virus in people with immunodeficiency;
- prevention of infections caused by the herpes simplex virus in people with immunodeficiency;
- initial manifestations of genital herpes in persons without immunodeficiency;
- treatment of encephalitis caused by the herpes simplex virus;
- treatment of infections caused by the herpes simplex virus in newborns and children aged 3 months and older;
- treatment of infections caused by the Varicella zoster virus.

Directions for use and doses

The drug is used only in a hospital setting.
Adults
In obese patients, dosages are recommended as in adults with normal body weight.
Treatment of infections caused by herpes simplex viruses (HSV; excluding herpes encephalitis) and varicella zoster virus (VZV)
Intravenous infusions at a dose of 5 mg/kg body weight every 8 hours.
Treatment and prevention of infections caused by HSV, VZV, and herpetic encephalitis in patients with immunodeficiency
Intravenous infusions at a dose of 10 mg/kg body weight every 8 hours provided that renal function is preserved.
Special patient groups
Children
The dose of acyclovir for newborns and children aged 3 months to 12 years is calculated depending on body surface area.
For children aged 3 months and older with infection caused by herpes simplex virus (excluding herpetic encephalitis) or Varicella zoster virus, the recommended dose is 250 mg per square meter of body surface area every 8 hours, provided renal function is preserved.
For the treatment of infections caused by the Varicella zoster virus and herpetic encephalitis in children with immunodeficiency, intravenous infusions of acyclovir are prescribed at a dose of 500 mg per square meter of body surface area every 8 hours, provided that renal function is preserved.
For newborns and children up to 3 months of age acyclovir doses for intravenous infusion are calculated based on body weight.
The recommended dose of the drug Acyclovir, lyophilized powder for the preparation of a solution for infusion, for newborns with or suspected of herpes is 20 mg/kg body weight intravenously every 8 hours for 21 days for disseminated lesions and CNS lesions, or for 14 days in case of a disease limited to the skin and mucous membranes.
Newborns and children with reduced kidney function it is necessary to adjust the dose according to the degree of impairment:
Elderly patients
In the elderly, the clearance of acyclovir in the body decreases in parallel with a decrease in creatinine clearance. In elderly patients with reduced creatinine clearance, a dose reduction should be considered.
Patients with kidney failure
Intravenous infusions of Acyclovir should be administered with caution in patients with renal failure. The following dose adjustment scheme has been proposed depending on the degree of decrease in creatinine clearance:
The course of treatment with Acyclovir by intravenous infusion is usually 5 days, but may vary depending on the patient's condition and response to therapy. The duration of treatment for herpetic encephalitis and HSV infections in newborns is usually 10 days.
The duration of prophylactic use of the drug Acyclovir for intravenous infusion is determined by the duration of the period when there is a risk of infection.

Preparation of solution and method of administration

The recommended dose of Acyclovir should be administered as a slow intravenous infusion over 1 hour.
To prepare a solution of the drug Acyclovir containing 25 mg of acyclovir in 1 ml of the resulting solution, dilution solutions are used (water for injection or sodium chloride solution for injection (0.9%)) in the following volume:

The recommended volume of dilution solution must be added to the vial or bottle of Acyclovir powder and shaken gently until the contents of the vial or bottle are completely dissolved.
After dilution, the Acyclovir drug solution can be administered as an intravenous infusion using a special infusion pump that regulates the rate of drug administration.
Another method of infusion administration is possible, when the prepared solution is diluted further to obtain an acyclovir concentration not exceeding 5 mg/ml (0.5%).
To do this, you need to add the prepared solution to the selected infusion solution, which is recommended below, and shake well until the solutions are completely mixed.
For children and newborns who need to administer minimal volumes of infusion, it is recommended to add 4 ml of the prepared solution of the drug Acyclovir (100 mg of acyclovir) to 20 ml of solvent.
For adults, it is recommended to use infusion solutions in 100 ml packs, even if this will give an acyclovir concentration significantly lower than 0.5%. Thus, one 100 ml infusion solution can be used for any dose of acyclovir between 250 mg and 500 mg (10 and 20 ml diluted solution). For doses between
500 and 1000 mg of acyclovir should be used with another solution for infusion of this volume (100 ml).
Acyclovir is compatible with the following infusion solutions and, when diluted with them, remains stable for 12 hours at room temperature (15 to 25°C):
- sodium chloride for intravenous infusion (0.45% and 0.9%);
- sodium chloride (0.18%) and dextrose (4%) for intravenous infusion;
- sodium chloride (0.45%) and dextrose (2.5%) for intravenous infusion;
- Hartmann's solution.
When preparing Acyclovir solution for infusion, as indicated above, the concentration of Acyclovir is no more than 0.5%.
Dissolution and dilution must be carried out completely under aseptic conditions immediately before administration of the drug. Unused solution is discarded. If the solution becomes cloudy or crystals fall out, it should be destroyed.

Side effect

The adverse events presented below are listed depending on the anatomical and physiological classification and frequency of occurrence. The frequency of occurrence is defined as follows: very often (≥1/10), often (≥1/100 and<1/10), нечасто (≥1/1000 и <1/100), редко (≥1/10000 и <1/1000), очень редко (<1/10000, включая отдельные случаи).
Blood and lymphatic system disorders: uncommon - decreased hematological parameters (anemia, thrombocytopenia, leukopenia).
Immune system disorders: very rarely - anaphylaxis.
Nervous system disorders: very rarely - headache, dizziness, agitation, confusion, tremor, ataxia, dysarthria, hallucinations, psychotic symptoms, convulsions, drowsiness, encephalopathy, coma.
The above phenomena are usually reversible and are usually observed in patients with impaired renal function and other predisposing factors.
Vascular disorders: often - phlebitis.
Respiratory, thoracic and mediastinal disorders: very rarely - shortness of breath.
Gastrointestinal disorders: often - nausea, vomiting; very rarely - diarrhea, abdominal pain.
Disorders of the liver and biliary tract: often - a reversible increase in the activity of liver enzymes; very rarely - a reversible increase in bilirubin concentration, jaundice, hepatitis.
Skin and subcutaneous tissue disorders: often - itching, urticaria, rash (including photosensitivity); very rarely - angioedema.
Renal and urinary tract disorders: often - increased concentrations of urea and creatinine in the blood. The rapid increase in blood urea and creatinine concentrations is thought to be related to peak plasma levels and the patient's hydration status. To avoid this effect, the drug should be administered as a slow intravenous infusion over 1 hour. Very rarely - impaired renal function, acute renal failure and pain in the kidney area. Adequate hydration of patients should be maintained. Impaired renal function during treatment with Acyclovir usually resolves quickly when patients are rehydrated and/or the dose of the drug is reduced or discontinued. Progression to acute renal failure occurs in extremely rare cases.
Pain in the kidney area may be due to renal failure or crystalluria.
General and administration site disorders: very rare: fatigue, fever, local inflammatory reactions.
Severe local inflammatory reactions, sometimes leading to skin damage, 5
observed in case of unintentional introduction of the drug into extracellular tissues.

Contraindications

Hypersensitivity to acyclovir or valacyclovir.
Carefully:
- with dehydration, renal failure, neurological disorders, during the development of reactions to cytotoxic drugs (with their intravenous administration) and if there is a history of such, electrolyte disturbances, severe hypoxia, during pregnancy and lactation.
- with extreme caution, the drug should be combined (monitoring of renal function is necessary) with drugs that impair renal function (for example, cyclosporine, tacrolimus).
- the combined use of acyclovir and mycophenolate mofetil (an immunosuppressive drug) used in organ transplantation leads to an increase in the blood concentration of acyclovir and the inactive metabolite of mycophenolate mofetil.
- pregnancy.

Overdose

Overdoses of the drug Acyclovir cause an increase in the concentration of serum creatinine, blood urea nitrogen and renal failure. Neurological symptoms include confusion, hallucinations, agitation, seizures and coma. Hemodialysis significantly enhances the removal of acyclovir from the blood, therefore it is indicated for an overdose of acyclovir.

Precautionary measures

In case of renal failure, the dose of Acyclovir should be adjusted according to its degree in order to prevent the accumulation of acyclovir in the body.
Elderly patients and patients with renal insufficiency have an increased risk of developing adverse reactions from the central nervous system, therefore these patients should be under close medical supervision for timely detection of relevant symptoms. According to the registered reports of these adverse reactions, they are usually reversible and stop after cessation of treatment (see section "Side effects").
Long-term or repeated courses of treatment with acyclovir in persons with significantly weakened immune systems may result in the emergence of strains of the virus with reduced sensitivity, which may not respond to continued therapy with acyclovir.
In patients receiving high doses of Acyclovir for herpetic encephalitis, it is necessary to monitor renal function, especially if it is initially impaired or there is dehydration.
The prepared solution of the drug Acyclovir has a pH of 11, so it cannot be used orally. The prepared solution should not be stored in the refrigerator.

Use during pregnancy and lactation

Acyclovir crosses the placental barrier and accumulates in breast milk. The use of the drug during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. Following oral administration of acyclovir at a dose of 200 mg 5 times/day, acyclovir was detected in breast milk at concentrations ranging from 0.6 to 4.1 (60 to 410%) of the corresponding plasma concentrations. At these concentrations in breast milk, breastfed infants can receive acyclovir in doses up to 0.3 mg/kg/day. Therefore, it is recommended to exercise caution when prescribing acyclovir to nursing women. The decision to interrupt breastfeeding is made by the doctor.

An enhanced effect is observed with the simultaneous administration of immunostimulants.
Tubular secretion blockers reduce the tubular secretion of intravenously administered acyclovir, which can lead to an increase in the concentration of acyclovir in the blood serum and cerebrospinal fluid (CSF), a slowdown in the elimination of acyclovir (increased half-life) from the blood and CSF, and increased toxic effects.
Other nephrotoxic drugs increase the risk of nephrotoxicity from acyclovir.
Acyclovir is excreted unchanged through the kidneys by active tubular secretion. All drugs with a similar route of elimination may increase plasma concentrations of acyclovir. Thus, probenecid and cimetidine increase the AUC of acyclovir and reduce its renal clearance. However, no dose adjustment is required due to the wide range of therapeutic doses of acyclovir.
In patients receiving Acyclovir, caution is required when prescribing drugs that compete for the elimination pathway due to the potential for increased plasma concentrations of one, both drugs, or their metabolites. The combined use of acyclovir and mycophenolate mofetil (an immunosuppressive drug) used in organ transplantation leads to an increase in the AUC for acyclovir and the inactive metabolite mycophenolate mofetil.
When lithium is used concomitantly with high doses of intravenous acyclovir, serum lithium concentrations should be carefully monitored due to the risk of toxicity.

Best before date

3 years.
Do not use after the expiration date.

Catad_pgroup Antiviral for herpes

Acyclovir-Akrikhin tablets - instructions for use

Registration number:

LS-000044

Trade name of the drug:

Acyclovir-Akrikhin

International nonproprietary name:

acyclovir

Dosage form:

pills

Compound

active substance: acyclovir in terms of 100% substance - 200 mg and 400 mg;
Excipients: microcrystalline cellulose 21.46 mg or 42.92 mg, povidone 1.17 mg or 2.34 mg, magnesium stearate 2 mg or 4 mg, indigo carmine 0.1 mg or 0.2 mg, sodium carboxymethyl starch 12.5 mg or 25 mg, purified water 12.77 mg or 25.54 mg, respectively.

Description

Blue tablets with dark and light blue inclusions and possible white spots, flat-cylindrical, with a chamfer and a score.

Pharmacotherapeutic group:

antiviral agent

ATX Code: J05AB01

Pharmacological properties

Pharmacodynamics

The antiviral drug is a synthetic analogue of an acyclic purine nucleoside that has a highly selective effect on herpes viruses. In infected cells containing viral thymidine kinase, phosphorylation occurs and is converted to acyclovir monophosphate. Under the influence of acyclovir guanylate cyclase, monophosphate is converted into diphosphate and, under the action of several cellular enzymes, into triphosphate.

Acyclovir triphosphate is integrated into the viral DNA chain and blocks its synthesis through competitive inhibition of viral DNA polymerase. The specificity and very high selectivity of action are also due to its predominant accumulation in cells affected by the herpes virus.

Highly active against Herpes simplex virus types 1 and 2; the virus that causes chickenpox and herpes zoster (Varicella zoster); Epstein-Barr virus. Moderately active against cytomegalovirus.

In case of herpes, it prevents the formation of new rash elements, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and reduces pain in the acute phase of herpes zoster.

Pharmacokinetics.

When taken orally, the bioavailability is 15-30%. Acyclovir penetrates well into all organs and tissues of the body; concentration in cerebrospinal fluid is 50% of its concentration in blood plasma. Penetrates through the blood-brain and placental barriers and accumulates in breast milk. Communication with plasma proteins - 9-33%. The maximum concentration (Cmax) in blood plasma after oral administration of 200 mg 5 times a day is 0.7 mcg/ml. The time to reach maximum concentration in blood plasma is 1.5-2 hours.

Metabolized in the liver to form a pharmacologically inactive metabolite - 9-carboxymethoxymethylguanine. The half-life (T 1/2) when taken orally is 2-3 hours. In patients with severe renal failure, T 1/2 is 20 hours, with hemodialysis - 5.7 hours (at the same time, the concentration of acyclovir in plasma decreases to 60% of original value).

It is excreted by the kidneys unchanged (about 84%) and in the form of a metabolite (about 14%). Less than 2% is excreted through the gastrointestinal tract; trace amounts are determined in exhaled air.

Indications for use

• treatment of infections of the skin and mucous membranes caused by the Herpes simplex virus types 1 and 2, both primary and secondary, including genital herpes;
• prevention of exacerbations of recurrent infections caused by Herpes simplex virus types 1 and 2 in patients with normal immune status;
• prevention of primary and recurrent infections caused by the Herpes simplex virus types 1 and 2 in patients with immunodeficiency;
• as part of complex therapy in patients with severe immunodeficiency: with HIV infection (stage AIDS, early clinical manifestations and detailed clinical picture) and in patients who have undergone bone marrow transplantation;
• treatment of primary and recurrent infections caused by the Varicella zoster virus (chickenpox, herpes zoster).

Contraindications

Hypersensitivity to acyclovir, ganciclovir, valacyclovir or components of the drug, lactation period, children under 3 years of age.

Carefully

Pregnancy, old age, dehydration, renal failure, neurological disorders or neurological reactions to cytotoxic drugs (including a history).

Use during pregnancy and lactation

Use during pregnancy is only possible if the expected benefit to the mother outweighs the potential risk to the fetus.
If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Directions for use and doses

Take orally, during or immediately after a meal, with a sufficient amount of water.
The dosage regimen is set individually depending on the severity of the disease.

For treating infections of the skin and mucous membranes caused by the Herpes simplex virus types 1 and 2
Adults - 200 mg 5 times a day (every 4 hours while awake, excluding night sleep) for 5 days, for treatment genital herpes- 10 days, if necessary, the duration of treatment can be extended.

As part of complex therapy for severe immunodeficiency, including with a full-blown clinical picture of HIV infection (including early clinical manifestations of HIV infection and the stage of AIDS), after bone marrow implantation, 400 mg is prescribed 5 times a day.

To prevent relapses of infections caused by Herpes simplex virus types 1 and 2 in patients with normal immune status
Adults - 200 mg 4 times a day every 6 hours, course duration from 6 to 12 months.

For the prevention of infections caused by Herpes simplex virus types 1 and 2 in patients with immunodeficiency
Adults - 200 mg 4 times a day every 6 hours, maximum dose - up to 400 mg 5 times a day, depending on the severity of the infection.

In the treatment of herpes zoster- 800 mg 5 times a day (every 4 hours while awake, excluding night sleep) for 7-10 days.
For children over 3 years of age, the drug is prescribed at the same dose as for adults.

Treatment of chickenpox: adults and children over 6 years old - 800 mg 4 times a day; children 3-6 years old - 400 mg 4 times a day. More accurately, the dose can be determined at the rate of 20 mg/kg.
The course of treatment is 5 days.

In patients with impaired renal function, dose adjustment and dosage regimen are necessary depending on the magnitude of creatinine clearance and the type of infection. For the treatment of infection caused by Herpes simplex, with creatinine clearance less than 10 ml/min, the daily dose of the drug should be reduced to 400 mg, divided into 2 doses (with intervals between them of at least 12 hours, i.e. 200 mg 2 times a day). day).

In the treatment of infections caused by Varicella zoster, and in the maintenance therapy of patients with severe immunodeficiency - patients with a creatinine clearance of 10-25 ml/min are prescribed the drug 800 mg 3 times a day with an interval of 8 hours, with a creatinine clearance of less than 10 ml/min - 800 mg 2 times a day with an interval of 12 hours.

Side effect

From the digestive system:
nausea, vomiting, diarrhea, abdominal pain; rarely - a reversible increase in bilirubin content and the activity of liver enzymes.

From the hematopoietic system:
very rarely - anemia, leukopenia, thrombocytopenia.

From the urinary system:
rarely - increased levels of urea and creatinine in the blood;
very rarely - acute renal failure.

From the central nervous system:
headache, weakness, dizziness, increased fatigue, confusion, hallucinations, drowsiness, paresthesia, convulsions, decreased concentration, agitation.

Allergic reactions:
itching, rash, Lyell's syndrome, urticaria, erythema multiforme, incl. Stevens-Johnson syndrome, angioedema, anaphylaxis.

Other:
fever, lymphadenopathy, peripheral edema, blurred vision, myalgia, alopecia.

Overdose

Symptoms: agitation, coma, convulsions, lethargy. Precipitation of acyclovir in the renal tubules is possible if its concentration exceeds the solubility in the renal tubules (2.5 mg/ml).
Treatment: symptomatic.

Interaction with other drugs When used simultaneously with probenecid, the average half-life of acyclovir increases and the clearance of acyclovir decreases.
When used simultaneously with nephrotoxic drugs, the risk of developing renal dysfunction increases.

special instructions

When taking the drug, kidney function should be monitored (blood urea and plasma creatinine levels).

When using the drug, it is necessary to ensure the supply of a sufficient amount of fluid. Long-term or repeated treatment with acyclovir in patients with reduced immunity can lead to the emergence of strains of viruses that are insensitive to its action. Most isolated strains of viruses that are insensitive to acyclovir show a relative lack of viral thymidine kinase; strains with altered thymidine kinase or with altered DNA polymerase were isolated. In vitro the effect of acyclovir on isolated strains of the Herpes simplex virus may cause the emergence of less sensitive strains.

Acyclovir does not prevent the sexual transmission of herpes, so during the treatment period it is necessary to abstain from sexual intercourse, even in the absence of clinical manifestations.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Release form

Tablets 200 mg and 400 mg.
10 tablets in a blister pack.
2 blister packs along with instructions for use in a cardboard pack.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Best before date

4 years. Do not use after the expiration date.

Conditions for dispensing from pharmacies

On prescription.

Manufacturer/Organization accepting consumer complaints

Open Joint Stock Company "Chemical and Pharmaceutical Plant "AKRIKHIN"
(JSC AKRIKHIN), Russia
142450, Moscow region, Noginsky district, Staraya Kupavna, st. Kirova, 29.