What is Penicillin? Instructions for use, price, who invented it

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.

Composition and release form

The composition of the medication depends on what type of drug is being considered. Today penicillins are divided into 4 groups;

natural;
semi-synthetic;
with an extended spectrum of action;
with a wide antibacterial spectrum of influence.

Powder for injection is packaged in glass bottles, sealed with rubber stoppers and metal caps, or in ampoules.

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.

Release form and composition

The active ingredient of Penicillin is aminopenicillic acid, consisting of 3 carbon atoms and 1 nitrogen atom.

Pharmacological companies produce many dosage forms of penicillin:

Tablets can have dosages ranging from 50,000 to 10,000 units. There is a separate form of tablets intended for resorption in the oral cavity (their dosage is 5000 units).
Intramuscular injection products are white powder, packaged in bottles made of dark glass. They are closed with rubber caps, reinforced with metal plugs on top. Each dose may contain 50,000 to 300,000 units of oxacillin sodium salt. The powder requires dilution using special substances.
In injections (penicillin in ampoules) are glass ampoules with a sealed tip. Their capacity can vary from 1 to 3 ml. Each milliliter of the finished composition contains 5000 units of ampicillin sodium salt.

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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.

Penicillin: a natural born killer

The story of the discovery of penicillin sounds like a medical joke. At the beginning of the twentieth century, a certain Alexander Fleming, a bacteriologist, later a professor and Nobel laureate, lived and worked in Scotland. During the First World War, he, not surprisingly, served as a military doctor. And there was nothing funny about it, of course. At that time, antibiotics did not yet exist and people died from any inflammation. This infuriated Fleming: how could it be that the operation after a wound was successful, and then gangrene or sepsis begins, and the person still dies! And doctors are powerless... As soon as the opportunity arose, Fleming began to look for ways to combat wound and other infections. Let us remember that in those years doctors already had the concept of sterility, examined bacteria under a microscope and guessed that it was the latter that, when they got on a wound, led to such fatal consequences.

But then a really funny chain of accidents and coincidences begins.

Nobel Prize in Physiology or Medicine 1945

For what? For the discovery of penicillin and its healing effects in various infectious diseases.

Who: Alexander Fleming, Ernst Boris Chain and Howard Walter Florey (Great Britain).

What came of it? Penicillin marked the beginning of a new era in medicine - the treatment of diseases with antibiotics.

Sloppy Scientist

By the 20s of the century of the same name, Fleming had already established himself in scientific circles as a talented and persistent researcher. At the same time, oddly enough, he was a terrible slob, and this played a decisive role in his discovery. Then experiments with bacteria were carried out in the simplest bioreactor - the so-called Petri dish. This is a wide glass cylinder with low walls and the same lid, which was supposed to be sterilized after each experiment. And then one day, Fleming, who had a cold, sneezed directly into a Petri dish, where he had just placed another culture of Micrococcus lysodeicticus bacteria. A normal doctor would have thrown everything out and re-sterilized, but Fleming didn’t.

A few days later he came across this cup again and found that in some places the bacteria had died! Apparently - in those where mucus got from his nose when he sneezed. Accident? Fleming was an educated and talented bacteriologist, so he started checking.

So in 1922, lysozyme was discovered - a natural enzyme in the mucus of humans, animals and, as it later turned out, some plants. It destroys the walls of bacteria and dissolves them, while being harmless to healthy tissues. (By the way, dogs, by licking their wounds, reduce the risk of inflammation due to the high content of lysozyme in their saliva.)

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 .

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

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.

Penicillin-Teva

Benzylpenicillin sodium salt is administered intramuscularly, intravenously, subcutaneously, endolumbarally, intratracheally.

For moderate disease (infections of the upper and lower respiratory tract, urinary and biliary tract, soft tissue infection, etc.) - 4-6 million units/day for 4 administrations. For severe infections (sepsis, septic endocarditis, meningitis, etc.) - 10-20 million units/day; with gas gangrene - up to 40-60 million units/day.

The daily dose for children under 1 year of age is 50-100 thousand units/kg, over 1 year of age – 50 thousand units/kg; if necessary - 200-300 thousand units/kg, for “vital” indications - increase to 500 thousand units/kg. Frequency of administration - 4-6 times a day, intravenous - 1-2 times a day in combination with intramuscular injections.

It is administered endolumbarally for purulent diseases of the brain, spinal cord and meninges. Depending on the disease and the severity of its course: adults - 5-10 thousand units, children - 2-5 thousand units once a day for 2-3 days intravenously, then prescribed intramuscularly.

For intravenous jet administration, a single dose (1-2 million units) is dissolved in 5-10 ml of sterile water for injection or 0.9% NaCl solution and administered slowly over 3-5 minutes. For intravenous drip administration, 2-5 million units are diluted with 100-200 ml of 0.9% NaCl solution or 5-10% dextrose solution and administered at a rate of 60-80 drops/min. When administered dropwise to children, a 5-10% dextrose solution (30-100 ml depending on the dose and age) is used as a solvent.

Solutions are used immediately after preparation, without allowing other drugs to be added to them.

Endolumbar. The drug is diluted in sterile water for injection or in 0.9% NaCl solution at the rate of 1 thousand units/ml. Before injection (depending on the level of intracranial pressure), 5-10 ml of CSF is removed and added to the antibiotic solution in equal proportions.

Inject slowly (1 ml/min), usually once a day for 2-3 days, then proceed to intravenous or intramuscular injections.

In case of suppurative processes in the lungs, a solution of the drug is administered intratracheally (after thorough anesthesia of the pharynx, larynx and trachea). Usually 100 thousand units are used in 10 ml of 0.9% NaCl solution.

For eye diseases (acute conjunctivitis, corneal ulcer, gonoblennorrhea, etc.), eye drops containing 20-100 thousand units in 1 ml of 0.9% NaCl solution or distilled water are sometimes prescribed. Inject 1-2 drops 6-8 times a day.

For ear drops or nasal drops, solutions containing 10-100 thousand units/ml are used.

Benzylpenicillin potassium salt is administered only intramuscularly and subcutaneously, in the same doses as benzylpenicillin sodium salt.

Benzylpenicillin procaine salt is administered only intramuscularly. Average therapeutic dose for adults: single - 300 thousand units, daily - 600 thousand units. The highest daily dose for adults is 1.2 million units. Children under the age of 1 year are prescribed 50-100 thousand units/kg/day, over 1 year - 50 thousand units/kg/day. The frequency of administration is 1-2 times a day.

The duration of treatment with benzylpenicillin, depending on the form and severity of the disease, is 7-10 days.

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.

Instructions for the use of Penicillin in injections

Before administering the solution, a subcutaneous test must be performed to check compatibility.

Preparation of solutions using powder

To obtain a solution for injection, Penicillin must be diluted with saline solution, injection water, or Novocaine. The solvent must have a temperature of +18…+20°C.

Using ampoules for injections

Penicillin in ampoules is diluted in the same way as in bottles.

Treatment regimen and dosage regimen

The drug can be injected into a muscle, vein, under the skin or into the spinal canal. The dose is calculated in such a way that there is always 0.1-0.3 units of medication in 1 ml of blood. For this reason, the interval between injections should not be more than 4 and less than 3 hours.

When treating pneumonia, syphilis, meningitis and other diseases, the regimen should be prescribed by the attending physician.

The course of therapy can last from 10 to 14 days. It is recommended to use the medication for another 2 days after the symptoms disappear.

Undesirable effects and overdose

If the dosage has been greatly exceeded, gastrointestinal disorders may occur in the form of vomiting and stool disorders.

In some cases, the following negative consequences occur:

nausea and vomiting;
loose stools;
convulsions;
sensitivity to external stimuli;
headache and loss of consciousness;
fungal infections of the mouth and vagina.

If injections are given for a long time, Penicillin can cause allergic reactions, which manifest themselves in the form of rashes, swelling, and increased body temperature.

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 and precautions

With an intramuscular injection, no more than 5 ml of medication can be injected into one place. A different area of the body is selected for the next injection.

Rapid administration may cause cerebral seizures.

If the patient’s condition does not improve within 3-5 days of therapy, it is necessary to visit the doctor again so that he can prescribe additional medications or another antibacterial medication.

Taking antibiotics can cause a fungal infection, so it is advisable to take antifungal agents at the same time. 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.

During treatment with penicillins, you must strictly follow the prescribed regimen and do not change the dosage yourself. If a dose is missed, the dose should be taken as soon as possible. You cannot interrupt the course of treatment.

Medicines that have expired may be poisonous and should not be taken.

Treatment of children

The drug can be prescribed to children from birth. However, the medication is used with caution in young patients who are under 2 years of age.

A special treatment regimen is prescribed for premature babies and those with impaired renal function.

Use during pregnancy and lactation

Since the active substance penetrates the placental barrier and after 2 hours reaches the same concentration in the fetal blood plasma as in the mother, if a woman is carrying a child, the possibility of Penicillin therapy is determined by the attending physician.

A nursing mother should stop breastfeeding during antibiotic treatment because penicillin passes into breast milk (in small quantities) and can cause a negative reaction in the fetus. Breastfeeding can be resumed one day after completion of treatment.

For patients with liver and kidney failure

Since this medication is excreted by the kidneys, if their functions are impaired, the medicine is used only under the constant supervision of a doctor.

Antibiotics put a strain on the liver, so if this organ is impaired, therapy should be carried out under medical supervision.

Interaction with other drugs

Antibacterial agents enhance the effect of Penicillin, and bacteriostatic agents cause the opposite reaction. It is not recommended to use the medication with drugs that dissolve blood clots, retain potassium and promote rapid urine output.

It is not allowed to dilute Penicillin and aminoglycosides in the same syringe, since these agents are physicochemically incompatible.

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

Alcohol compatibility

Compatibility of the medication with alcohol is possible, but not recommended.

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.

Directions for use: special instructions

How to dilute Penicillin, what dosage to administer, how long to continue therapy? All these questions will be answered by the specialist who prescribed antibacterial therapy. What remains unclear can be clarified by reading the instructions that come with each dosage form of the drug.

A high antibacterial effect is achieved when the drug is administered by intramuscular injection. This method of administration allows for rapid penetration of penicillin into the systemic bloodstream.

It should be remembered that the active substance is in the blood for no more than 4 hours, so regular injections are indicated (at regular intervals, approximately 4 times a day).

The specialist may prescribe subcutaneous administration of the drug, or its introduction into the spinal canal. It all depends on the severity and localization of the ongoing infection.

Before injecting penicillin, you need to make sure that the patient will not suffer from hypersensitivity reactions to cephalosporin and penicillin antibacterial agents. It is worth remembering that people with high sensitivity to cephalosporins should not forget about the possibility of developing a cross-reaction.

If a person has a history of severe reaction to antibiotic therapy using penicillin therapy, such treatment should not be started. It is necessary to inform a specialist about pre-existing cases of allergic reactions so that he can select another adequate therapy. If these facts are not taken into account, there is a high probability of developing a serious anaphylactic reaction, which can only be stopped with the use of adrenaline, steroids and treatment of respiratory failure.

To prepare a solution for injection, you need:

dilute in 10 ml of water no more than 10 million international units of benzylpenicillin (intravenous injection);
to prepare a solution containing 10 to 20 million international units of penicillin, use 100 to 200 ml of water for injection;
solutions containing sodium cannot be used to dilute the powder;
novocaine can be used to dilute the composition, which will be administered intramuscularly.

How long can penicillin diluted with Novocaine be stored? According to the rules described in the instructions, the prepared solution can be stored for no more than 24 hours, but only in a refrigerator.

Features of injection administration of the drug:

when injections are given intramuscularly, no more than 5 ml of the drug is indicated per site;
repeated injections require changing the injection site4
for children, the intravenous method of administering the medicine is preferable, because the intramuscular method can provoke unpleasant reactions;
rapid administration of the drug can provoke the occurrence of cerebral attacks;
the duration of therapy usually lasts from 10 days to 2 weeks;
it is very important to continue therapy for at least another 2 days after the disappearance of negative symptoms of the disease.

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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.

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

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