Antibiotic penicillin: what is it for and when is it used

Compound

The composition of drugs that belong to penicillin group of antibiotics 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

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.

Overboard

Due to the impossibility of industrial production in England during the war, they decided to transport all the results and the penicillin strain to the USA. Fearing that exporting biomaterials would be difficult, Chain and Flory soaked the linings of coats, jackets and even pockets with penicillin extract! But suddenly everything changed. Without any explanation, Flory flew to America with Norman Hatley. Boris, who actually discovered the method of laboratory production using evaporation, was removed from the list. Since his father was involved in the chemical industry, Chain understood that penicillin in production would bring fabulous profits. There is a version that the leaders of the Rockefeller Center did not like his left-wing pro-communist views. He was not a communist, but he sympathized with the mysterious country in the east, the homeland of his parents. And when his mother died in 1942, Boris, according to many sources, decided to selflessly help his failed fellow countrymen.

pharmachologic effect

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 of 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.

BETA-LACTAM ANTIBIOTICS

β-lactam antibiotics (β-lactams), which are united by the presence of a β-lactam ring in their structure, include penicillins, cephalosporins, carbapenems

and
monobactams
, which have a bactericidal effect. The similarity of the chemical structure determines the same mechanism of action of all β-lactams (impaired bacterial cell wall synthesis), as well as cross-allergy to them in some patients.

Penicillins, cephalosporins and monobactams are sensitive to the hydrolyzing action of special enzymes - β-lactamases, produced by a number of bacteria. Carbapenems are characterized by significantly higher resistance to β-lactamases.

Given their high clinical efficacy and low toxicity, β-lactam antibiotics form the basis of antimicrobial chemotherapy at the present stage, occupying a leading place in the treatment of most infections.

Penicillins are the first antimicrobial drugs developed on the basis of biologically active substances produced by microorganisms. The ancestor of all penicillins, benzylpenicillin, was obtained in the early 40s of the 20th century. Currently, the group of penicillins includes more than ten antibiotics, which, depending on the sources of production, structural features and antimicrobial activity, are divided into several subgroups (Table 1).

Table 1. Classification of penicillins

General properties:

• Bactericidal action.
• Low toxicity.
• Excretion is mainly through the kidneys.
• Wide range of dosages.
• Cross-allergy between all penicillins and some cephalosporins and carbapenems.

Pharmacokinetics and pharmacodynamics

The most effective method is intramuscular administration. After such use, the active component very quickly enters blood . The highest concentration of the product is observed 30-60 minutes after application. After a single administration, only trace concentrations are determined.

It is quickly detected in muscles, wound exudate, in joint cavities, and in muscles.

A small amount of it is observed in the cerebrospinal fluid. A small amount will also enter the pleural cavities and abdominal cavity, so direct local action of the drug is required if necessary.

Penetrates to the fetus through the placenta. It is excreted from the body through the kidneys, so about 50% of the drug is eliminated. Also, part of it is excreted in bile.

If a patient takes penicillin in tablets, he needs to take into account that when taken orally, the antibiotic is poorly absorbed, and part of it is destroyed under the influence of gastric juice and beta-lactamase, which is produced by intestinal microflora .

References

1. Medical Immunology. Federal clinical guidelines / ed. R.M. Khaitova, N.I. Ilyina. - M.: FarmarusPrint Media, 2014. - T. 13. - No. 4-5. - 2011. - T. 13, No. 4-5. — 126 s.
2. Clinical recommendations “Allergology and clinical immunology” / ed. R.M. Khaitova, N.I. Ilyina. - M.: GEOTAR-Media, 2021. - 336 p.
3. Goldberg, A., Confino-Cohen, R. Skin testing and oral penicillin challenge in patients with a history of remote penicillin allergy. AnnAllergyAsthmaimmunol, 2008. - Vol. 100. - P. 37-43.

Indications for use

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

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.

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 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. Adrenaline should be immediately administered intravenously.
• Manifestations associated with chemotherapeutic effects: oral candidiasis

Operation Dunkirk

In violation of all traditions, the experiment was carried out on Saturday.
The day before, news had arrived that the Wehrmacht had surrounded British troops in France and Belgium, pinning them to the sea at Dunkirk. Things were taking a serious turn - the war promised to be long and bloody. It was necessary to test antibiotics as quickly as possible to begin treating septic wounded people. And Flory canceled the weekend until the end of the war. In Dunkirk, the most combat-ready and experienced part of the British army was blocked - almost 400 thousand people. The enemy stopped the offensive and, without any haste, methodically exterminated them with artillery fire and bombing. Having learned about this, the British, who had private yachts and boats, moved on their ships to Dunkirk. Together with the navy, they evacuated more than 300 thousand British and French soldiers. Along the way, their ships sank submarines, destroyed bombers, and waited for mines scattered from planes. But they reached England and returned to Dunkirk while there was someone there to save.

The government did not order them to bail out the army, and did not order Flory to deal with penicillin. Moreover, it did not finance his work during the most difficult period, so the decisive part of the research was carried out with a foreign grant.

British soldiers walk from Dunkirk beach through shallow water to board the warship evacuating them. End of May 1940.

Instructions for use of penicillin (Method and dosage)

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.

The first successes of penicillin

Then there were successes. 14-year-old boy who injured his leg; A 6-month-old infant with urethritis is the first patient to receive oral penicillin. Finally, Flory himself, having become infected with streptococcus, gargled with penicillin. As he said, “it tastes disgusting, but it works.” It was necessary to expand production, but outside the department, Flory could not guarantee that the technology would not fall into the hands of the enemy. The government refused to provide security, and it became clear that it was time to move to the United States - to account for the grant and organize the production of penicillin on an industrial scale. Scientists wanted to patent penicillin, but the government refused them this too: “People paid for the research, and they should enjoy its fruits.” Flory agreed - there is no time for royalties during the war. Chain said that this was idiotic, and the heroes quarreled. At the first opportunity, the biochemist left the team.

If in England food was rationed, and finding a nutrient medium for mold was a problem, then in America there was an ideal free nutrient medium - “corn liquor,” that is, stillage remaining after the extraction of corn starch. Millions of tons of this “liquor” were simply poured out as waste, without knowing what to do with them. As soon as mold began to be grown on stillage, an American government commission proposed producing penicillin. The companies agreed only on the condition that the government, at the expense of the budget, would build and donate factories to them. At the same time, the technology was developed using budget money, so much so that in 1944 penicillin was already 1000 times cheaper than in 1943.

Overdose

It should be borne in mind that when taking large doses of penicillin, an overdose can occur, which can cause unpleasant symptoms in the form of nausea, vomiting, and diarrhea . But this condition is not life-threatening.

hyperkalemia may develop in patients suffering from renal failure .

When large doses of the drug are administered intraventricularly or intravenously, epileptic seizures may occur. But such a symptom appears in adult patients only after administration of at least 50 million units. medications. In this case, the patient is prescribed barbiturates or benzodiazepines.

Interaction

When taken simultaneously with Probenecid, of benzylpenicillin decreases , which leads to an increase in its concentration in plasma and an increase in the half-life.

If combined use with tetracycline , the bactericidal effect of benzylpenicillin is reduced.

Dilution in the same syringe or in the same system for infusion of penicillin and aminoglycosides , since these agents are physicochemically incompatible.

If large doses of benzylpenicillin potassium salt in combination with potassium supplements, potassium-sparing diuretics or ACE inhibitors, there is an increased risk of hyperkalemia.

When taking penicillins that demonstrate activity against Pseudomonas aeruginosa with antiplatelet agents and anticoagulants, caution should be exercised, as there is a risk of increased bleeding.

It is not recommended to take simultaneously with thrombolytics .

Sulfonamides weaken the bactericidal effect of the antibiotic.

When taking Cholestyramine and penicillins simultaneously, the bioavailability of the latter decreases.

When taking oral penicillins simultaneously with oral contraceptives, the effectiveness of the latter may be reduced due to disruption of the enterohepatic circulation of estrogen .

When taking an antibiotic, the process of removing methotrexate from the body may slow down due to inhibition of its tubular secretion.

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 in the process of taking antibiotics there is a high probability of fungal superinfection , 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.

Choosing an antibiotic in a child

Previously, we reviewed the main diseases of the upper and lower respiratory tract, for which antimicrobial agents can be used. Now we will analyze the main drugs that can be used for this or that pathology, and also indicate the required dosage of the drug.

Do not take antibiotics without a doctor's prescription.

Do not use medications yourself! The medications and dosages listed below are for informational purposes only and are not equivalent to treatments prescribed by a physician.

Acute otitis media

The drug of choice is amoxicillin 40-90 mg/kg/day in 3 divided doses. Duration of therapy is 10 days in children <5 years old, 5-7 days in children >5 years old. The second-line drug is amoxicillin/clavulanate. The third-line drug is josamycin.

Acute rhinosinusitis

Similar to the use of antibacterial agents for acute otitis media.

Acute tonsillitis

The drug of choice is amoxicillin 45-60 mg/kg in 3 doses, phenoxymethylpenicillin 25-50 mg/kg 3-4 times a day. The second-line drug is cefixime. The third-line drug is josamycin. Duration of therapy is 10 days.

Community-acquired pneumonia

The therapy of choice is amoxicillin IV 45-90 mg/kg/day in 3 divided doses. The second line drug is amoxicillin/clavulanate, cefuroxime IM, ceftriaxone IM. The third line drug is josamycin 40-50 mg/kg/day in 2 doses.

Antibiotics are indispensable drugs in the fight against bacterial infection. These medications should be prescribed solely for medical reasons. It is very important to adhere to the prescribed regimen of using the antibacterial agent. Do not self-medicate. If signs of infection occur, contact your pediatrician, who will help establish the diagnosis, cause of the disease, and prescribe adequate treatment.

Analogs

Level 4 ATC code matches:
Hiconcil

Ampioks

Ampicillin Trihydrate

Ampicillin

Ospamox

Amoxicar

Flemoxin Solutab

Amoxicillin

Amosin

Amoxil

Ecoball

There are a number of penicillin drugs; the most optimal antibiotic is determined by the doctor individually.

Sources

• Shi SL., Shi QY., Jin HX., Yao GD., Liu Y., Guo YH. [Clinical outcomes of intracytoplasmic sperm insemination with micro amount frozen-thawed diagnostic sperm in the treatment of azoospermia]. // Zhonghua Yi Xue Za Zhi - 2021 - Vol101 - N8 - p.591-596; PMID:33663191
• Westlander G., Schmidt J., Westin C. [Microdissection testicular sperm extraction (MD-TESE) is a new sperm recovery technique helping men with non-obstructive azoospermia]. // Lakartidningen - 2021 - Vol116 - NNULL - p.; PMID:31334817
• Shah R., Gupta C. Advances in sperm retrieval techniques in azoospermic men: A systematic review. // Arab J Urol - 2021 - Vol16 - N1 - p.125-131; PMID:29713543
• Corona G., Pizzocaro A., Lanfranco F., Garolla A., Pelliccione F., Vignozzi L., Ferlin A., Foresta C., Jannini E.A., Maggi M., Lenzi A., Pasquali D., Francavilla S. Sperm recovery and ICSI outcomes in Klinefelter syndrome: a systematic review and meta-analysis. // Hum Reprod Update - 2021 - Vol23 - N3 - p.265-275; PMID:28379559
• Roque M., Valle M., Marques F., Sampaio M., Geber S. Intracytoplasmic sperm injection outcomes with cryopreserved testicular sperm aspiration samples. // Andrologia - 2021 - Vol48 - N3 - p.252-6; PMID:25998234
• Oldereid NB., Hanevik HI., Bakkevig I., Romundstad LB., Magnus Ø., Hazekamp J., Hentemann M., Eikeland SN., Skrede S., Reitan IR., Tanbo TG. Pregnancy outcome according to male diagnosis after ICSI with non-ejaculated sperm compared with ejaculated sperm controls. // Reprod Biomed Online - 2014 - Vol29 - N4 - p.417-23; PMID:25131554
• Raviv G., Madgar I., Elizur S., Zeilig G., Levron J. Testicular sperm retrieval and intra cytoplasmic sperm injection provide a favorable outcome in spinal cord injury patients, failing conservative reproductive treatment. // Spinal Cord - 2013 - Vol51 - N8 - p.642-4; PMID:23689394
• Ishikawa T. Surgical recovery of sperm in non-obstructive azoospermia. // Asian J Androl - 2012 - Vol14 - N1 - p.109-15; PMID:22120931

Penicillin price, where to buy

The price of Penicillin tablets depends on the drug and ranges from 30 rubles. per package. You can buy Penicillin in ampoules at a price of 60 rubles per 1 ampoule.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

LuxPharma* special offer

• Penicillin G (Infectocillin, Extensillin) 5 million IU No. 1
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• Ospen (Phenoxymethylpenicillin) tab. 1 million ME No. 12

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• Ospen (Phenoxymethylpenicillin) syrup 750000 IU/5 ml 60 ml

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• Penicillin G sodium salt Austria 1 million. ME N1

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Pharmacy24

• Penicillin G sodium salt No. 100 powder for the preparation of solution for injection Sandoz GmbH, Austria
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• Benzylpenicillin-KMP 500,000 IU powder PAT "Kievmedpreparat", Ukraine

  6 UAH order

• Benzylpenicillin-KMP 1,000,000 IU powder for the preparation of solution for injection PAT"Kievmedpreparat", Ukraine

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• Penicillin bottle Penicillin G sodium salt powder for the preparation of solution for injection 1000000IU bottles No. 100 Austria, Sandoz

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• Benzylpenicillin bottle Benzylpenicillin sodium salt powder for injection 1000000IU Ukraine, Kievmedpreparat OJSC

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To prison for courage

The authorities really wanted to punish someone for trying to reveal Soviet military secrets, especially when Flory was nominated for the Nobel Prize. It was somehow inconvenient to arrest Ermolyeva, who had just received the Stalin Prize. Therefore, Professor Wolf Dorfman, the first Soviet doctor who used penicillin in his clinical practice (September 1942), was given 8 years for espionage. Unfortunately for him, the professor knew English and served as a translator for Ermolyeva.

Sources: 1) Lennard Bickel. Rise up to Life. A Biography of Howard Walter Florey who gave Penicillin to the World. New York, 1972 2) Tamara Iosifovna Balezina (1913-2010), personal interview.

Mikhail Shifrin

Mikhail Shifrin