Penicillin analogues. Antibiotics of the penicillin group: indications, instructions for use

Despite its impressive age, penicillin continues to be one of the most commonly used antibiotics for the treatment of sore throat. Even a large number of analogues and antibiotics of other families, during the isolation and development of which pharmacists tried to circumvent the shortcomings of penicillin, could not displace it from medical practice. Penicillin for sore throat is widely used in both adults and children, although its use is associated with some difficulties and limitations.

Note

Other names for penicillin (mainly used in the scientific community) are benzylpenicillin and penicillin G. At the same time, compounds such as benzathine benzylpenicillin or procaine benzylpenicillin, although they are its analogs and belong to the penicillin family, differ from the original substance in some properties.

Three-dimensional model of the molecule of the first antibiotic - penicillin

The effectiveness of penicillin for angina

Penicillin is a bactericidal antibiotic. When it enters the source of infection, it interferes with the synthesis and restoration of bacterial cell walls, which leads to their rapid death. Due to this, by the way, penicillin acts very quickly, and patients notice signs of improvement after taking it within the first day after the first injection.

Initially, penicillin effectively destroyed both pathogens of sore throat - streptococcus and staphylococcus, and therefore, immediately after its introduction into the arsenal of doctors, it was used to effectively treat sore throat in all situations.

Today, in most cases of the disease, staphylococcus is resistant to penicillin, since over several decades of use of this antibiotic it has managed to develop resistance to it.

At the same time, staphylococcal tonsillitis occurs on average in 10% of cases, and in another 10% the disease is caused by a mixed staphylococcal and streptococcal infection. This means that penicillin for sore throat may be ineffective in about one case out of five. In other situations, this also works quite effectively for adults.

The causative agents of bacterial sore throat are streptococcus and staphylococcus

Note

In addition, strains of staphylococci sensitive to penicillin are sometimes found today. However, this happens less and less every year. If the doctor knows that a sore throat is caused by a staphylococcal or mixed staphylococcal-streptococcal infection, in order to prescribe penicillin he needs to obtain data on the sensitivity of the pathogen to antibiotics. Only after such an examination will he be able to say whether penicillin will help with sore throat.

Penicillin is also effective in cases of atypical gonococcal tonsillitis. This is partly why the diagnosis itself is made less often than the disease actually happens: sore throat caused by gonococcus is very similar to streptococcal and even if the doctor makes a mistake in diagnosis, it is successfully cured using this remedy.

In some countries today there is an increase in the number of cases in which the use of penicillin is unsuccessful even against streptococcal infections. For example, in some cities in Germany, in 28% of cases the use of penicillin does not produce results, and some authors indicate even 35-38%, that is, in every third case, after several days of unsuccessful use, penicillin has to be replaced with other antibiotics.

Gonococcus is the causative agent of gonorrhea; if it gets into the throat it can cause gonococcal sore throat.

More often, this is not due to the development of resistance in the streptococcus itself (although this is being noted more and more often), but due to the fact that, along with streptococcus, other bacteria are present in the deep tissues of the tonsils that do not cause inflammation, but produce enzymes that break down penicillin. Thus, these bacteria (usually non-pathogenic staphylococci or Haemophilus influenzae) protect the causative agent of sore throat from the antibiotic.

Interestingly, the more often inflammation of the tonsils occurs (even not associated with a sore throat), the more copathogen bacteria are present in them and the greater the likelihood that penicillin will not work specifically for sore throat.

How to determine whether an infectious agent is resistant to penicillin or not?

To identify resistance, a smear of mucus from the tonsils is taken from the patient and a bacteriological examination is carried out. Based on the results of the analysis, it becomes known which bacterium caused the sore throat, which antibiotics it is sensitive to, and which it is resistant to. Such an examination takes several days, and in severe cases of the disease, when there may not be time, the doctor usually prescribes antibiotics that are likely to act even on resistant bacteria - a mixture of amoxicillin with clavulanic acid, antibiotics of the macrolide family, and others. This allows you to quickly begin treatment and in most cases ensures recovery.

A smear from the tonsils will help to accurately determine the causative agent of a sore throat, but during its analysis, in most cases, the disease can already be cured

Advantages and disadvantages of penicillin

Penicillin has several advantages, thanks to which it successfully competes with many more modern antibiotics. Among these positive qualities:

On the other hand, it is precisely the shortcomings of penicillin that require pharmacists to constantly strive to develop more advanced analogues. Here are the main disadvantages of penicillin:

A specific property of penicillin is its rapid elimination from the body. It acts for 3-4 hours after administration, after which most of the substance is eliminated from the body and the injection must be repeated. This rate of elimination has both positive and negative sides. The disadvantage is the need to frequently repeat injections (and therefore the need for hospital treatment), the advantage is the ability to quickly stop therapy if side effects occur.

Other penicillin preparations, in particular its procaine and benzathine salts, on the contrary, are characterized by a very long presence in the body, due to which they are used to prevent complications of angina.

Penicillin preparations

There are a large number of penicillin preparations on the market today. Moreover, in different products the antibiotic is contained in two different chemical forms:

Benzylpenicillin potassium salt;
Sodium salt of benzylpenicillin.

Penicillin is sold in this form in pharmacies.

Procaine and benzathine salts of benzylpenicillin are also actively used, but they have different pharmacokinetics and are used as part of bicillins - long-acting drugs for the prevention of complications of angina.

Here are just the main penicillin preparations:

Bicillins - Bicillin-1, Bicillin-3, Bicillin-5, Retarpen, Extensillin
Capicillin;
Angincillin;
Novopen;
Cracillin;
Christacillin;
Pradupen;
Pharmacillin;
Lanacillin;
Falapen...

Procaine salts of penicillin are used in bicillins

...and others. Basically, all of them are imported products, some are no longer produced today. In our country, benzine penicillin salts, packaged in special vials, are usually used for injection.

Rules of application

To treat angina, penicillin preparations are administered intramuscularly into the gluteal muscle, sometimes intravenously (sodium salt only). The doses of these drugs for the treatment of sore throat are the same.

For angina, it is prescribed in the amount of 3-6 million units per day (about 1.8-3.6 g) for 4-6 injections. The specific amount is prescribed by the doctor depending on the severity of the disease.

Injections are the main method of introducing penicillin into the body.

Penicillin for angina for children is prescribed in quantities of 50-150 thousand units per kg of body weight per day. The total dose is divided into 4-6 injections. As a rule, for children aged from six months to 2 years, a single dose is 240-250 mg, from 2 to 6 years - 300-600 mg, 7-12 years - 500-900 mg.

During treatment, it is very important to maintain the frequency of injections without missing injections. The general course of using penicillin for angina should be approximately 10-12 days, but not less than a week. If complications are suspected, the doctor may extend treatment to 21 days, or prescribe a course of bicillin prophylaxis.

Premature cessation of treatment or irregular injections are fraught with the development of complications of angina.

What to do if penicillin against a sore throat does not help?

If penicillin is clearly ineffective in a particular case, it is replaced with antibiotics of other groups - macrolides, cephalosporins, and sometimes lincosamides. Sometimes products based on penicillin antibiotics with auxiliary components - clavulanic acid or sulbactam - can be effective. In this case, clear signs of the action of penicillin should appear within a few hours, most likely after 1-2 days of treatment. Practice shows that if effective treatment begins during the first 9 days of illness, angina is extremely rarely complicated. Accordingly, if you consult a doctor in a timely manner, it is quite acceptable to try injecting penicillin, and if it does not help, prescribe another drug.

Safety, side effects and contraindications

The main side effects after using penicillin are allergies, and in some cases they can be very severe. They usually manifest themselves with the following set of symptoms:

Skin rash all over the body;
Bronchospasm;
Increase in temperature;
Eosinophilia.

Model of an eosinophil, a type of blood cell that helps the body fight bacteria

Also, when treated with penicillin, heart rhythm disturbances are possible (potassium salt can lead to cardiac arrest, sodium salt can lead to a decrease in the pumping function of the myocardium). Potassium salts also sometimes cause hyperkalemia.

If any significant side effects develop, penicillin is usually replaced with antibiotics from other groups.

During pregnancy, penicillin can be prescribed by a doctor if further use of the antibiotic will proceed under his supervision. The doctor must very correctly assess the balance between the risk of the drug affecting the fetus and the danger of the sore throat itself. Penicillin penetrates the placental barrier, but does not have a negative effect on the fetus. In the first months of pregnancy, the use of true penicillin can increase the contractile activity of the uterus and cause the risk of spontaneous abortion. Other penicillins - amosicillin, ampicillin - are safer.

As a rule, when using penicillin, it is not necessary to transfer the child to formula milk

Breastfeeding is usually not interrupted while penicillin is used during lactation. Penicillin penetrates into breast milk, and with it into the baby’s digestive tract, but since it is not absorbed from the gastrointestinal tract, it does not have a systemic effect on the baby’s body. In cases of dysbacteriosis, the doctor can either replace the penicillin itself or prescribe the child means to restore the intestinal microflora.

In children themselves, penicillin for sore throat can be used from birth, but only under the strict supervision of a doctor. In this case, it does not enter the stomach and intestines and, therefore, rarely causes allergies and dysbiosis.

Rules of choice: when to prescribe penicillin and when to prescribe other antibiotics

Josamycin-based tablets - an alternative to penicillin injections

Today, all over the world, injections of penicillin are increasingly being replaced by taking tablets and other oral medications based on its analogues - amoxicillin, ampicillin - as well as antibiotics of other groups - cefadroxil, erythromycin, josamycin. This is done primarily for sore throat in children, so as not to traumatize their psyche with painful injections and not cause fear of the doctor. Also, the doctor may prefer other antibiotics for a sore throat to penicillin for the following reasons:

Conversely, doctors prefer to prescribe penicillin itself for angina in the following situations:

Conclusions:

Penicillin is often used for angina and, when prescribed by a doctor, in most cases can cure the disease;
Penicillin can only be used by injection. You can’t “drink” it;
Dosages and duration of treatment with penicillin are prescribed only by a doctor, taking into account the severity of the disease and the patient’s condition.

Video: How does a doctor choose an antibiotic?

At the beginning of the last century, many diseases were incurable or difficult to treat. People died from simple infections, sepsis and pneumonia.
Wikimedia Commons/Carlos de Paz ()

A real revolution in medicine occurred in 1928, when penicillin was discovered. In all of human history, there has never been a drug that has saved as many lives as this antibiotic.

Over the course of decades, it has cured millions of people and remains one of the most effective medications to this day. What is penicillin? And to whom does humanity owe its appearance?

What is penicillin?

Penicillin is part of the group of biosynthetic antibiotics and has a bactericidal effect. Unlike many other antiseptic drugs, it is safe for humans, since the fungal cells that make up it are fundamentally different from the outer shells of human cells.

The action of the drug is based on inhibition of the vital activity of pathogenic bacteria. It blocks the substance peptidoglycan they produce, thereby preventing the formation of new cells and destroying existing ones.

What is penicillin for?

Penicillin is capable of destroying gram-positive and gram-negative bacteria, anaerobic bacilli, gonococci and actinomycetes.

Since its discovery, it has become the first effective drug against pneumonia, skin and biliary tract infections, anthrax, ENT diseases, syphilis and gonorrhea.

Nowadays, many bacteria have managed to adapt to it, mutated and formed new species, but the antibiotic is still successfully used in surgery to treat acute purulent diseases and remains the last hope for patients with meningitis and furunculosis.

What does penicillin consist of?

The main component of penicillin is the mold fungus penicillium, which forms on products and leads to their spoilage. It can usually be seen as a blue or greenish colored mold. The healing effect of the fungus has been known for a long time. Back in the 19th century, Arab horse breeders removed mold from damp saddles and smeared it on the wounds on the backs of horses.

In 1897, the French doctor Ernest Duchesne was the first to test the effects of mold on guinea pigs and managed to cure them of typhus. The scientist presented the results of his discovery at the Pasteur Institute in Paris, but his research did not receive the approval of medical luminaries.

Who discovered penicillin?

The discoverer of penicillin was the British bacteriologist Alexander Fleming, who managed to completely accidentally isolate the drug from a strain of fungi.

For a long time after the discovery, other scientists tried to improve the quality of the drug, but only 10 years later, bacteriologist Howard Flory and chemist Ernst Chain were able to produce a truly pure form of the antibiotic. In 1945, Fleming, Florey and Chain received the Nobel Prize for their achievements.

History of the discovery of penicillin

The history of the discovery of the drug is quite interesting, since the appearance of the antibiotic was a happy accident. During those years, Fleming lived in Scotland and was engaged in research in the field of bacterial medicine. He was quite messy, so he didn’t always clean up the test tubes after tests. One day, a scientist left home for a long time, leaving Petri dishes with staphylococcus colonies dirty.

When Fleming returned, he found that mold was growing on them, and in some places there were areas without bacteria. Based on this, the scientist came to the conclusion that mold is capable of producing substances that kill staphylococci.

Wikimedia Commons/Steve Jurvetson ()
The bacteriologist isolated penicillin from fungi, but underestimated his discovery, considering the manufacture of the medicine too difficult. The work was completed for him by Flory and Chain, who managed to come up with methods for purifying the drug and launching it into mass production.

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Penicillin instructions for use, analogues, contraindications, composition and prices in pharmacies

Shelf life of penicillin: The shelf life of penicillin is 5 years.

Storage conditions of the drug: Should be stored at a temperature not exceeding 25 degrees, in a dry place.

Conditions for dispensing from pharmacies: By doctor's prescription

Composition, release form, Pharmacological action of penicillin

Composition of the drug penicillin

The composition of drugs that relate to antibiotics groups penicillins , depends on what kind of medicine we are talking about.

Currently, four groups are used:

natural penicillins;
semisynthetic penicillins;
aminopenicillins, which have an extended spectrum of action;
penicillins, which have a wide antibacterial spectrum of influence.

Release form of the drug penicillin

Injectable preparations are available, as well as penicillin tablets.

The injection product is produced in glass bottles, which are closed with rubber stoppers and metal caps. The vials contain different doses of penicillin. It is dissolved before administration.

Penicillin-ecmoline tablets are also produced for resorption and oral administration. Sucking tablets contain 5000 units of penicillin. In tablets for oral administration - 50,000 units.

Penicillin tablets with sodium citrate may contain 50,000 and 100,000 units.

Pharmacological action of the drug penicillin

Penicillin is the first antimicrobial agent that was obtained using waste products of microorganisms as a basis. The history of this medicine begins in 1928, when the inventor of the antibiotic, Alexander Fleming, isolated it from a strain of the fungus Penicillium notatum. In the chapter that describes the history of the discovery of penicillin, Wikipedia testifies that the antibiotic was discovered by accident; after the bacteria entered the culture from the external environment of a mold fungus, its bactericidal effect was noted. Later, the formula for penicillin was determined, and other specialists began to study how to obtain penicillin. However, the answer to the questions of what year this drug was invented and who invented the antibiotic is clear.

The further description of penicillin on Wikipedia testifies to who created and improved the drugs. In the forties of the twentieth century, scientists in the USA and Great Britain worked on the industrial production process of penicillin. The first use of this antibacterial drug for the treatment of bacterial infections occurred in 1941. And in 1945, for the invention of penicillin, the Nobel Prize was received by its creator Fleming (the one who invented penicillin), as well as by the scientists who worked on its further improvement - Flory and Chain.

Speaking about who discovered penicillin in Russia, it should be noted that the first samples of the antibiotic were obtained in the Soviet Union in 1942 by microbiologists Balezina and Ermolyeva. Then industrial production of the antibiotic began in the country. In the late fifties, synthetic penicillins appeared.

When this drug was invented, for a long time it remained the main antibiotic used clinically throughout the world. And even after other antibiotics without penicillin were invented, this antibiotic remained an important drug for the treatment of infectious diseases. There is a claim that the medicine is obtained using cap mushrooms, but today there are different methods for its production. Currently, so-called protected penicillins are widely used.

The chemical composition of penicillin indicates that the drug is an acid, from which various salts are subsequently obtained. Penicillin antibiotics include Phenoxymethylpenicillin (penicillin V), Benzylpenicillin (penicillin G), etc. The classification of penicillins involves their division into natural and semi-synthetic.

Biosynthetic penicillins provide bactericidal and bacteriostatic effects, inhibiting the synthesis of the cell wall of microorganisms. They act on some gram-positive bacteria (Streptococcus spp., Staphylococcus spp., Bacillus anthracis, Corynebacterium diphtheria), on some gram-negative bacteria (Neisseria meningitidis, Neisseria gonorrhoeae), on anaerobic spore-forming bacilli (Spirochaetaceae Actinomyces spp.), etc.

The most active of the penicillin drugs is benzylpenicillin. Resistance to the influence of benzylpenicillin is demonstrated by strains of Staphylococcus spp. that produce penicillinase.

Penicillin is not effective against bacteria of the enteric-typhoid-dysenteric group, causative agents of tularemia, brucellosis, plague, cholera, as well as whooping cough, tuberculosis, Friedlander's, Pseudomonas aeruginosa and viruses, rickettsia, fungi, protozoa.

Indications for use of the drug penicillin

Indications for use of the drug penicillin are:

Antibiotics of the penicillin group, the names of which will be prompted directly by the attending physician, are used to treat diseases caused by microorganisms sensitive to penicillin:

pneumonia (lobar and focal);
pleural empyema;
septic endocarditis in acute and subacute forms;
sepsis;
pyemia;
septicemia;
osteomyelitis in acute and chronic form;
meningitis;
infectious diseases of the biliary and urinary tract;
purulent infectious diseases of the skin, mucous membranes, soft tissues;
angina;
scarlet fever;
erysipelas;
anthrax;
actinomycosis;
diphtheria;
gynecological purulent-inflammatory diseases;
ENT diseases;
eye diseases;
gonorrhea, syphilis, blenorrhea.

Contraindications to the use of penicillin

Contraindications to the use of penicillin are:

Tablets and injections are not used in the following cases:

with high sensitivity to this antibiotic;
for urticaria, hay fever, bronchial asthma and other allergic manifestations;
when patients exhibit high sensitivity to sulfonamides, antibiotics, as well as other drugs.

penicillin - Instructions for use

Antimicrobial action is observed with local and resorptive action of penicillin.

Instructions for the use of penicillin in injections

The drug can be administered subcutaneously, intramuscularly, or intravenously. The drug is also injected into the spinal canal. For therapy to be as effective as possible, the dose must be calculated so that there is 0.1–0.3 units of penicillin in 1 ml of blood. Therefore, the drug is administered every 3-4 hours.

For the treatment of pneumonia, syphilis, cerebrospinal meningitis, etc., a doctor prescribes a special regimen.

Instructions for use of penicillin tablets

The dosage of penicillin tablets depends on the disease and on the treatment regimen prescribed by the attending physician. As a rule, patients are prescribed 250-500 mg, the drug should be taken every 8 hours. If necessary, the dose is increased to 750 mg. It is recommended to take tablets half an hour before meals or two hours after meals. The duration of treatment depends on the disease.

Prices in pharmacies

Side effects

During use, the patient must understand what penicillin is and what side effects it can cause. During treatment, allergy symptoms sometimes appear. As a rule, such manifestations are associated with sensitization of the body due to earlier use of these drugs. Allergies can also occur due to prolonged use of the medicine. When using the medicine for the first time, allergies are observed less frequently. There is a possibility of sensitization of the fetus during pregnancy if a woman takes penicillin.

The following side effects may also develop during the course of treatment:

Digestive system: nausea, diarrhea, vomiting.
Central nervous system: neurotoxic reactions, signs of meningism, coma, convulsions.
Allergies: urticaria, fever, rash on mucous membranes and skin, eosinophilia, edema. Cases of anaphylactic shock and death have been recorded. With such manifestations, adrenaline should be immediately administered intravenously.
Manifestations associated with chemotherapeutic effects: oral candidiasis, vaginal candidiasis.

penicillin - drug analogues

Analogues of the drug penicillin are:

penicillin with alcohol

penicillin during pregnancy and lactation

No data

penicillin for children

It is used to treat children only after a doctor’s prescription and under his supervision.

Special instructions

Before using penicillin, it is important to conduct tests and determine sensitivity to the antibiotic.

Prescribe the medicine with caution to people who have impaired renal function, as well as patients with acute heart failure, people who have a tendency to allergic manifestations or severe sensitivity to cephalosporins.

If 3-5 days after the start of treatment there is no improvement in the patient’s condition, it is important to consult a doctor who will prescribe other antibiotics or combination treatment.

Since there is a high probability of fungal superinfection while taking antibiotics, it is important to take antifungal agents during treatment. It is also important to consider that when using subtherapeutic doses of the drug or with an incomplete course of therapy, the emergence of resistant strains of pathogens is possible.

When taking the drug orally, you should take it with plenty of liquid. It is important to strictly follow the instructions on how to dilute the product.

During treatment with penicillins, it is necessary to strictly follow the prescribed treatment regimen and not skip doses. If a dose is missed, the dose should be taken as soon as possible. You cannot interrupt the course of treatment.

Since expired medicine may be toxic, it should not be taken.

The discovery of penicillin by the English scientist A. Fleming in 1928 caused a real revolution in medicine associated with the treatment of numerous infectious diseases. A. Fleming discovered that the active substance of the filamentous green mold fungus (Penicillium notatum) has antibacterial activity and the ability to cause the death of staphylococci at the cellular level. Already in the forties of the last century, doctors began to use penicillin treatment, especially during the Second World War, it helped in localizing infectious processes after wounds of the chest and soft tissues, as well as in preventing gangrene.

Penicillin is an antibiotic that includes natural compounds formed by various types of mold fungus Penicillium, as well as some semi-synthetic substances. A characteristic feature of penicillin is its powerful bactericidal effect on microbes harmful to the human body, and young microorganisms that are in the growth stage are more sensitive to this antibiotic than old ones. Of the penicillin drugs, benzylpenicillin has the greatest activity, unlimited quantities of which have become available for clinical use since the fifties of the last century. It is a natural antibiotic and contains sodium and potassium salts. Currently, when treating with penicillin, drugs that have semi-synthetic compounds obtained as a result of chemical modification of various natural components are also used: aminopenicillins, carboxypenicillins, ureidopenicillins and others.

The use of drugs containing penicillin has an extremely wide spectrum and is associated, first of all, with the suppression of infections caused by pathogens sensitive to them. With the greatest success, penicillin is used to treat streptococcal sepsis, osteomyelitis, gas gangrene, purulent meningitis, erysipelas, anthrax, diphtheria, brain abscesses, furunculosis, severe forms of gonorrhea and syphilis. The use of penicillin drugs after various wounds for the restoration of musculoskeletal tissues, as well as for the prevention of purulent complications in the postoperative period, is important. Treatment with penicillin is extremely effective for lobar and focal pneumonia, cholecystitis, rheumatism, and prolonged septic endocarditis. In ophthalmology, penicillin drugs play a significant role in the treatment of various eye inflammations. Penicillin is even used to treat diseases in newborns, infants and young children suffering from umbilical sepsis, otitis media, scarlet fever, and purulent pleurisy.

In the treatment of the above diseases, penicillin drugs have high chemotherapeutic activity, but are rather ineffective against viruses, such as influenza, as well as tuberculosis bacilli, intestinal bacteria of the typhoid-dysentery group, cholera, and plague. Penicillin must be used as prescribed by a doctor and only under his supervision. Insufficient doses of this antibiotic or early cessation of treatment can lead to the development of resistant microbial strains, which will have to be eliminated with the help of additional medications. Treatment with penicillin is carried out in a variety of ways; it can be administered intramuscularly, intravenously, subcutaneously, by inhalation, rinsing, and washing. Intramuscular administration of drugs is considered the most effective, when penicillin is actively absorbed into the blood and quickly passes into the muscle structure, joint cavities, lungs, and wound tissues.

When treated with penicillin drugs, complications are relatively rare; this antibiotic is low-toxic. It is excreted from the body mainly as a result of the activity of the kidneys, some of it is destroyed in the liver. But it must be remembered that some people have increased sensitivity to antibiotics associated with allergic reactions. It is recommended to first test the body’s perception of penicillin, otherwise the allergy may not appear immediately, but in the middle of treatment. Allergic reactions are manifested by headaches, fever, and there are even cases of anaphylactic shock with a fatal outcome. In addition, penicillin is contraindicated for people suffering from bronchial asthma, hay fever, and urticaria. Drinking alcohol while administering penicillin is strictly prohibited.

We must pay tribute to this antibiotic, because penicillin is a real discovery of the 20th century, which helped restore the health of many people.

What was life like before the invention of antibiotics? Banal purulent tonsillitis led to severe complications from the heart, kidneys, joints and, often, death. Pneumonia was a death sentence in most cases. And syphilis slowly and surely deformed the human body. Any inflammatory complication during childbirth almost always led to the death of both mother and newborn. Many of those who today campaign against the use of antibiotics (and there are many of them) simply do not imagine that before the discovery of these drugs, any infectious disease meant inevitable death.

It is for this reason that August 6, 1881 can be called the most important date in modern medicine, because it was on this day that the scientist Alexander Fleming was born, who in 1928 discovered the first antibiotic - penicillin. How did this happen, what niche did this drug occupy, and does it have a place in modern practice for the treatment of infectious diseases? Details in a new article.

An unknown Dr. Fleming worked for a long time at St. Mary's Hospital in Scotland. He was a general practitioner, but was actively interested in infectious agents and how they cause various diseases. At that time there was no specific way to treat them. However, doctors still tried to save the lives of such patients. To do this they used various methods.

During an infectious process, bloodletting was often performed, which made it possible to remove blood containing a large number of pathogens. After this, the patient was forced to drink a lot of fluid to replenish blood loss. For this procedure, either an incision was made in the area of a large blood vessel or leeches were applied.
Various herbs with bactericidal effects were used. They were applied to the wound area, or they were given decoctions and infusions to drink.
The historical treatment for syphilis was mercury, which was taken orally and injected with thin rods directly into the urethra. Arsenic was an alternative, but its use cannot be called more effective or safer.
Charcoal was applied to the wounds, which drew out the pus, and sometimes a bromine solution. The latter caused a serious burn, but the bacteria also died.

But basically the human body itself coped with the infection. Or I couldn't cope. In this case, natural selection acted: people with weak immunity quickly died, and those with strong immunity recovered and gave birth to offspring.

The First World War exposed the vulnerabilities of medical science: a large number of soldiers with infected wounds died, even if they were completely surgically treated. But these strong and healthy people could recover and participate in hostilities again if there was a more effective way to help them. While treating soldiers, Fleming began looking for drugs that could kill bacteria. He conducted many experiments that were not successful. However, one fine day, a piece of moldy bread fell onto a cup containing microorganisms in a nutrient medium. The scientist noticed that at the point of contact all bacteria disappeared. This fact interested him extremely. According to another version, the mold got on the colonies of streptococci that the scientist was growing because he did not always sterilize his cups; often he did not even wash them after previous experiments.

As a result, after numerous experiments, he was able to isolate a substance in its pure form, which he named penicillin. However, he could not apply it in practice: it was very unstable. And, nevertheless, Fleming proved that it destroys a large number of the most common microorganisms (streptococcus, staphylococcus, diphtheria bacillus, anthrax, etc.).

The further fate of the first drug from the group of antibiotics

The Second World Wave was the impetus for the further development of microbiology. And the reason was still the same: there was a need to treat wounded soldiers. As a result, two British scientists, Flory and Chain, were able to isolate penicillin in its pure form and create a medicine that was first administered to a young man with sepsis in 1941. His condition improved for some time, but he still died, since the administered doses were insufficient to destroy all pathogenic bacteria. A few months later, penicillin was administered to a boy with the same sepsis, the dose was adjusted correctly, and as a result he eventually recovered. Scientists heroically preserved the results of their scientific works and did not stop experiments even during bomber raids of Nazi Germany.

Since 1943, penicillin has been widely used to treat infectious diseases and complications after injuries. As a result, all three - Fleming, Florey and Chain - received the Nobel Prize in 1945. Already in 1950, the pharmaceutical companies Pfizer and Merck each produced 200 tons of this medicine.

Penicillin was quickly called the “drug of the 20th century”, because it saved more lives than all the others combined.

Of course, Soviet intelligence quickly found out that in England and the USA they were developing some kind of super-powerful antibacterial medicine based on mold. The country's leadership has challenged scientists to get ahead of foreign researchers and obtain this substance themselves. However, they did not have time to do this earlier: for the first time, domestic penicillin was isolated in its pure form in 1942, and since 1944 it began to be used as a medicine. The author of the works and scientific experiments was Zinaida Ermolyeva, but her name is known only to specialists in the field of microbiology.

Since 1947, factory production of this antibiotic was established, the quality of which significantly exceeded the results of the first experiments. Given the presence of the “Iron Curtain,” domestic scientists had to go through the entire process of discovering this drug on their own, since they could not benefit from the experience of their foreign colleagues from the USA and Great Britain.

How does penicillin work?

The mechanism of action of the antibiotic penicillin is very simple: it contains 6-aminopenicillanic acid, which destroys the cell wall of some bacteria. This quickly leads to their death. Initially, a very wide range of microbes turned out to be vulnerable to this medicine: among them are streptococci, staphylococci, E. coli, typhus, cholera, diphtheria, syphilis, etc. However, bacteria are living beings, and they quickly began to develop resistance to this drug. Thus, if its initial doses were several thousand conventional units 2-3 times a day, then in order for the medicine to have a clinical effect today much larger doses are required: 1-2 million conventional units per day. Some diseases generally require daily administration of 40-60 million conventional units.

The drug is used only in the form of injections (intramuscular or intravenous). It usually comes in powder form, which the nurse dilutes with saline or anesthetic before administering. After all, as you know, penicillin injections are very painful.

Another negative point in treatment with penicillin is that its half-life is 3-5 hours. That is, in order for a certain therapeutic dose to be maintained in the blood, six-fold administration is necessary. Thus, the patient is given injections every 3 hours. This is quite debilitating and after 2-3 days it turns his buttocks into a sieve on which it is impossible to sit or lie down.

Currently, the drug is not active against gram-negative bacteria and bacilli, but retains a satisfactory effect against streptococci, staphylococci, the causative agent of diphtheria, anthrax and gonorrhea. However, the resistance (sustainability) of these bacteria is 25% or even higher in some regions of our country, which significantly reduces the likelihood of a successful outcome of therapy.

And yet, the structure of natural penicillin and its mechanism of action served as the basis for the further development of antimicrobial chemotherapy. Scientists began to create more modern, effective and easy-to-use medicines. He was the first representative of a whole group of antibiotics, including the well-known Ampicillin, Amoxicillin, Amoxiclav, etc. These drugs are much more active against all of the above microorganisms, each of them has its own spectrum of action and indications for use.

Thus, we can say that natural penicillin is practically not used today. The only exceptions are small hospitals in remote corners of our country. There are several reasons:

low efficiency,
the need for six intramuscular injections,
extreme pain of injections.

Penicillin is still actively used to treat all stages of syphilis, because Treponema pallidum retains good sensitivity to this drug. In addition, its advantage is that it is allowed during pregnancy and breastfeeding, because during this period it is very important that the woman is treated for this serious disease.
Penicillin often causes allergic reactions, including anaphylactic shock. It is characterized by cross-reaction with other beta-lactam antibiotics, that is, in case of intolerance to the latter, none of them should be used. Only a doctor will be able to select an adequate alternative to this drug, which is still available.
Alexander Fleming, who first discovered penicillin, always denied the very fact of this discovery. He says that mold existed before him, he could only prove its bactericidal effect. For this reason, most likely, the scientist never received a patent for his invention.
Natural penicillin was produced exclusively in the form of injections, although several attempts were made to make a tablet form. Success was achieved only after this drug was obtained synthetically - this is how aminopenicillins appeared.
There is a monument to penicillin in the city of Zadonsk, Lipetsk region. It is located in the courtyard of the veterinary hospital and is a red and blue pillar entwined with a worm, on the top of which there is a pill. This very strange architectural structure, to which only some residents of the city of Zadonsk can show the way, is the only monument to penicillin. It is also unclear whether there are tablets in its structure, since the drug is administered only by injection.
The name “Penicillin” was given to a new modern artillery reconnaissance complex. At the moment, its state tests are being carried out and its mass production is planned to begin in 2019.
In May 2017, news appeared that biological scientists were able to “teach” ordinary yeast to produce natural penicillin. So far, these experiments do not go beyond ordinary laboratory tests, but experts are making optimistic predictions: this fact can significantly reduce the cost of this antibiotic. True, the goal is not entirely clear, because today almost everywhere only synthetic forms of penicillin antibiotics are used.

Once penicillin saved millions of lives, with its discovery medical science received a powerful boost. Thousands of scientists around the world began to work on the issue of inventing other more effective and safe antibiotics.