Penicillin is one of the the most famous antibiotics in the history of mankind. According to a survey by the London Science Museum, the discovery of penicillin is the second most important in the ranking. greatest discoveries humanity. Its discovery occurred at the beginning of the 20th century, and the active use of penicillin as a medicine began during the Second World War.

Penicillin is a waste product of the Penicillium mold fungus. Its therapeutic effect extends to almost all gram-positive and some gram-negative bacteria (staphylococci, gonococci, spirochetes, etc.).

Use of penicillin

The good tolerability of penicillin makes it possible to use it in large quantities diseases:

• sepsis;
• gas gangrene;
• extensive lesions skin as a result of injuries;
• erysipelas;
• brain abscess;
• sexually transmitted diseases (gonorrhea, syphilis);
• burns high degree(3 and 4);
• cholecystitis;
• lobar and focal pneumonia;
• furunculosis;
• ophthalmic inflammation;
• ear diseases;
• upper respiratory tract infections.

In pediatrics, treatment with penicillin can be prescribed for:

• septicopyemia (a type of sepsis with the formation of interconnected abscesses in different organs);
• sepsis umbilical region in newborns;
• otitis, pneumonia in newborns and children early age;
• purulent pleurisy and meningitis.

Penicillin dosage forms

Penicillin is produced in powder form, which is diluted with a special solution before injection. Injections can be given intramuscularly, subcutaneously, intravenously. Penicillin solution can also be used as inhalation and drops (for ears and eyes).

Penicillin group drugs

Due to its effect on bacterial cells (inhibition chemical reactions, necessary for the life and reproduction of bacterial cells), penicillin-based drugs are allocated to a separate classification group. Drugs of the natural penicillin group include:

• Procaine;
• Bicillin;
• Retarpen;
• Ospen;
• benzylpenicillin sodium salt;
• benzylpenicillin potassium salt.

Natural penicillins have the most gentle effect on the body. Over time, bacteria became resistant to natural penicillins and the pharmaceutical industry began to develop semi-synthetic penicillins:

• Ampicillin;
• Oxycellin;
• Ampiox.

Side effects of semi-synthetic drugs are more pronounced:

• gastrointestinal disorders;
• dysbacteriosis;
• cutaneous allergic reactions;
• anaphylactic shock.

Currently, the fourth generation of drugs containing penicillin has been developed.

Penicillin pharmacology

Pharmacodynamics

Water-soluble benzylpenicillin, which has a bactericidal effect on sensitive microorganisms, is a brief description of medicine Penicillin. Active substance The drug - sodium salt of benzylpenicillin - suppresses the biosynthesis of the cell wall due to the blockade of penicillin-binding proteins.

Resistance

Not in front of everyone bacterial diseases Penicillin shows its effect. Mechanism of action active component the drug does not work when:

• inactivation by beta-lactamase: benzylpenicillin is sensitive to beta-lactamase and therefore inactive against bacteria that produce beta-lactamase (for example, staphylococci or gonococci);
• decreased affinity of penicillin-binding proteins to penicillin as a result of mutations;
• insufficient penetration of penicillin in gram-negative bacteria through their outer cell wall, which leads to insufficient inhibition of penicillin-binding proteins;
• triggering of reflux pumps that remove sodium salt benzylpenicillin from the cell;
• cross-resistance to other penicillins and cephalosporins.

Information on pathogen resistance

Favorable views

Aerobic gram-positive microorganisms: Actinomyces israelii, Corynebacterium diphtheriae, Erysipelothrix rhusiopathiae, Gardnerella vaginalis, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus dysgalactiae subsp. Equisimilis (Group C & G streptococci)

Aerobic gram-negative microorganisms: Borrelia burgdorferi, Eikenella corrodens, Haemophilus influenzae, Neisseria meningitidis.

Anaerobic microorganisms: Clostridium perfringens, Clostridium tetani, Fusobacterium spp., Peptoniphilus spp., Peptostreptococcus spp., Veillonella parvula.

Other microorganisms: Treponema pallidum.

Species in which acquired resistance may be a treatment problem

Aerobic gram-positive microorganisms: Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis.

Aerobic gram-negative microorganisms: Neisseria gonorrhoeae.

Naturally resistant species

Aerobic gram-positive microorganisms: Enterococcus faecium, Nocardia asteroids.

Aerobic gram-negative microorganisms: all Enterobacteriaceae species, Moraxella catarrhalis, Pseudomonas aeruginosa.

Anaerobic microorganisms: Bacteroides spp.

Other microorganisms: Chlamydia spp., Chlamydophila spp., Legionella pneumophila, Mycoplasma spp.

Pharmacokinetics

Suction

Benzylpenicillin is NOT acid-fast and is therefore administered parenterally only. Alkaline salts of benzylpenicillin are quickly and completely absorbed after injection. Maximum plasma levels of 150-200 IU/ml are achieved 15-30 minutes after administration of 10 million IU. After short-term infusions (30 minutes), levels can reach a maximum of 500 IU/ml. Plasma protein binding accounts for approximately 55% of the total dose.

Distribution

After the use of penicillin in high doses, therapeutic concentrations are also achieved in hard-to-reach tissues such as heart valves, bones and cerebrospinal fluid. Benzylpenicillin crosses the placenta. 10-30% of the concentration in maternal plasma is found in fetal blood. High concentrations are also achieved in amniotic fluid. On the other hand, penetration into breast milk is low. The volume of distribution is about 0.3-0.4 l/kg; in children it is about 0.75 l/kg. Plasma protein binding is about 55%.

Metabolism and excretion

It is excreted mainly (50-80%) as unchanged substance through the kidneys (85-95%) and to a lesser extent in the active form with bile (about 5%). The half-life is about 30 minutes in adults with healthy kidneys.

Clinical characteristics

Penicillin prescription

Infectious diseases caused by penicillin-sensitive microorganisms:

• sepsis;
• wound and skin infections;
• diphtheria (as an addition to antitoxin);
• pneumonia;
• empyema;
• erysipeloid;
• pericarditis;
• bacterial endocarditis;
• mediastinitis;
• peritonitis;
• meningitis;
• brain abscesses;
• arthritis;
• osteomyelitis;
• genital tract infections caused by fusobacteria.

Specific infections:

• anthrax;
• infections caused by clostridia, including tetanus, listeriosis, pasteurellosis;
• fever caused by rat bites;
• fusospirochetosis, actinomycosis;
• treatment of complications caused by gonorrhea and syphilis;
• Lyme borreliosis after the first stage of the disease.

Contraindications

• hypersensitivity to beta-lactam antibiotics (penicillins and cephalosporins), the possibility of cross-allergy should be taken into account;
• newborns whose mothers have increased sensitivity to antibiotics of the penicillin group;
• epilepsy (with intralumbar administration);
• severe allergic reactions and bronchial asthma in the anamnesis.

Interaction with other drugs and other types of interactions

• with bacteriostatic antibiotics, since penicillins act on proliferating microbes;
• with glucose;
• with anti-inflammatory drugs;
• with antirheumatic drugs;
• with antipyretics (indomethacin, phenylbutazone, salicylates in high doses);
• with thiazide diuretics;
• with furosemide;
• with ethacrynic acid;
• with allopurinol;
• with preparations of copper, mercury and zinc.

The use of benzylpenicillin may in some cases lead to a decrease in the effectiveness of oral contraceptives.

Impact on laboratory test results

• a positive direct Coombs test is common (≥ 1% to<10%) у пациентов, получающих 10000000 МЕ (эквивалентно 6 г) бензилпенициллину или более в сутки. После отмены пенициллина, тест может оставаться положительным в течение от 6 до 8 недель;
• determination of protein in urine using precipitation methods (sulfosalicylic acid, trichloroacetic acid), the Folin-Ciocalteu-Loury method or the Biuret method may lead to false-positive results. Therefore, caution should be used when interpreting the results of such tests in patients receiving penicillin. Penicillin does not affect protein determination using the strip test;
• equally, determination of uric acid using ninhydran may lead to false-positive results;
• penicillins bind to albumin. In electrophoresis methods for determining albumin, there may be false pseudobisalbuminemia;
• During penicillin therapy, non-enzymatic determination of glucose in urine may be false-positive. Urinary glucose enzyme tests should be used in patients taking penicillin as they are not affected by this interaction;
• when determining 17-ketosteroids (using the Zimmerman reaction) in urine, an increase in their value may be observed.

Features of application

Before starting treatment, it is necessary to do a preliminary test for the possibility of a hypersensitivity reaction to penicillins and cephalosporins. In patients with hypersensitivity to cephalosporins, the possibility of cross-allergy should be considered.

Severe and sometimes fatal cases of hypersensitivity (anaphylactic reactions) have been observed in patients receiving penicillin therapy. Such reactions occur more often in patients with a known history of severe allergic reactions. Treatment with the drug must be discontinued and replaced with another appropriate treatment. Treatment of symptoms of an anaphylactic reaction may be necessary, such as immediate administration of epinephrine, steroids (intravenous), and emergency treatment for respiratory failure.

The drug should be used with extreme caution in patients with the following diseases and conditions:

• allergic diathesis (urticaria or hay fever) or asthma ( increased risk development of hypersensitivity reactions);
• severe cardiovascular disease or severe electrolyte disturbances of any other origin;
• renal failure;
• liver damage;
• epilepsy, cerebral edema or meningitis (increased risk of seizures, especially when high doses (> 20 IU million) of penicillin are administered);
• existing mononucleosis (increased risk of developing skin rash);
• in the treatment of concomitant infections in patients with acute lymphocytic leukemia (increased risk of skin reactions);
• ringworm.

Use during pregnancy or breastfeeding

Benzylpenicillin penetrates the placental barrier and its concentration in the fetal blood plasma 1-2 hours after administration corresponds to the concentration in the maternal blood serum. Available data on the use of the drug during pregnancy indicate the absence negative influence for the fetus/newborn. The drug can be used during pregnancy after a careful assessment of the benefit/risk ratio.

Benzylpenicillin passes into breast milk in small quantities, so the risk of hypersensitivity in a breastfed baby cannot be excluded. The use of the drug during this period is possible only when the expected benefit to the mother exceeds potential risk for a child.

In infants who are on partial artificial feeding, breast-feeding should be discontinued if the mother is taking benzylpenicillin. Recovery breastfeeding possibly 24 hours after stopping treatment.

The ability to influence the reaction rate when driving vehicles or other mechanisms

There were no negative effects on reaction speed when driving vehicles or operating other mechanisms.

Penicillin dosage and method of administration

Before administration, it is necessary to collect a history of drug tolerance from the patient and conduct a preliminary intradermal test to determine its tolerance. To prepare the solution, use only water for injection.

Age (body weight)	Usual dose (i.m., i.v. injection)	High dose (IV introduction)
Premature and newborn babies (up to 2 weeks)	0.03-0.1 million MO/kg/day 2 introductions	0.2-0.5 million MO/kg/day 2 introductions
Newborn babies (from 2 to 4 weeks)	0.03-0.1 million MO/kg/day 3-4 injections	0.2-0.5 million MO/kg/day 3-4 injections
Infants from 1 month and children up to 12 years	0.03-0.1 million MO/kg/day 4-6 injections	0.1-0.5 million MO/kg/day 4-6 injections
Adults and children over 12 years old	1-5 million MO/day 4-6 injections	10-40 million MO/day 4-6 injections

For premature and newborn babies (up to 2 weeks), the dose interval should be at least 12 hours.

Dosing for renal impairment

In patients with severe renal impairment single doses and the intervals between them should be set in accordance with creatinine clearance.

Adults and teenagers

Infants from 1 month and children up to 12 years

Creatinine clearance, ml/min
Serum creatinine, mg%
Daily dose of the drug	0.03-0.1 million MO/kg/day divided into 4-6 doses	0.02-0.06 million MO/kg/day divided into 2-3 doses	0.01-0.4 million MO/kg/day divided into 2 doses

If kidney function is moderate to severely impaired (rate glomerular filtration= 10-50 ml / min / 1.73 m2), the normal dose is administered every 8-12 hours. Very severe cases impaired renal function or renal failure(glomerular filtration rate<10 мл / мин / 1,73 м2), нормальную дозу вводить через каждые 12 часов.

Premature and newborn babies (under 4 weeks of age)

Do not use for premature babies or newborns with impaired renal function.

Patients with liver dysfunction

No dose reduction is required provided that renal function is not impaired.

Mode of application

The drug is administered (i.v.) in the form of injections or short-term infusions and intramuscularly (i.m.).

To prepare a solution for intravenous injection, dissolve no more than 10 million IU of benzylpenicillin in 10 ml of water for injection.

When administered intramuscularly, the total volume of injected fluid should not exceed 5 ml per injection site. With repeated injections, the injection site of the drug should be changed. High doses should be administered intravenously. Children may experience severe local reactions when administered, so it is advisable to use the intravenous route of administration.

To prepare an infusion solution, dissolve 10-20 million IU of benzylpenicillin in 100 or 200 ml of water for injection, respectively. At the indicated ratios, a solution close to isotonic is obtained.

Caution: Cerebral seizures may occur with rapid administration.

The usual duration of treatment is 10 - 14 days for most indications. However, the duration of treatment should be adjusted according to the severity of the infection, the sensitivity of the pathogen, and the clinical and bacteriological status of the patient. Treatment should be continued for another 2-3 days after the main symptoms of the disease disappear.

Children and the drug

Prescribe to children from birth. The drug should be used with extreme caution in children under 2 years of age.

Overdose

Symptoms of overdose largely correspond to the nature of the side effects. Gastrointestinal disorders and disturbances in water and electrolyte balance are possible. There may be increased neuromuscular excitability or a tendency to cerebral spasms.

Treatment: there is no specific antidote. Treatment includes hemodialysis, gastric lavage and symptomatic therapy; Particular attention should be paid to water and electrolyte balance.

Penicillin side effects

High allergenicity and the incidence of adverse events are characteristic of the drug Penicillin. Side effects have the following evaluation criteria: very often (≥ 1/10), often (≥ 1/100,<1/10), нечасто (≥ 1/1000, <1/100), редко (≥ 1/10000, < 1/1000), очень редко (<1/10000).

From the blood and lymphatic system: rarely - eosinophilia, leukopenia, neutropenia, granulocytopenia, thrombocytopenia, agranulocytosis, pancytopenia. In addition, hemolytic anemia, blood clotting disorders, and a positive Coombs test result are possible. Prolongation of bleeding time and prothrombin time has been reported.

From the immune system: isolated - allergic reactions: urticaria, angioedema, erythema multiforme, exfoliative dermatitis, contact dermatitis, fever, joint pain, anaphylactic or anaphylactoid reactions (asthma, thrombocytopenic purpura, gastrointestinal symptoms). Paraallergic reactions may occur in patients with dermatomycosis, as they may be a consequence of antigenicity between penicillin and the metabolic products of dermatophytes. Serum sickness and the Jarisch-Herxheimer reaction have been reported in combination with spirochete infections (syphilis and tick-borne borreliosis).

From the nervous system: rarely - with a large dose infusion (adults more than 20 million IU), there is a particularly high risk of seizures in patients with severe renal impairment, epilepsy, meningitis, cerebral edema or when using a machine for extracorporeal circulation, neurotoxic reactions, including hyperreflexia, myoclonic twitching; coma, symptoms of meningism, paresthesia. Neuropathy.

From the side of metabolism and nutrition: rarely - an imbalance of electrolytes, which is possible with rapid administration of a dose of over 10 million IU, an increase in the level of nitrogen in the blood serum.

From the digestive tract: rarely - stomatitis, glossitis, black tongue, nausea, vomiting, diarrhea. If diarrhea occurs during treatment, the possibility of pseudomembranous colitis should be considered.

From the digestive system: very rarely - hepatitis, bile stagnation.

From the skin: pemphigoid.

From the kidneys and urinary system: rarely - interstitial nephritis, nephropathy (with intravenous administration of a dose over 10 million IU), albuminuria, cylindruria and hematuria. Oliguria or anuria usually resolves within 48 hours after discontinuation of therapy. Diuresis can be restored after using a 10% mannitol solution.

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

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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 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.

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.

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 likelihood of fungal superinfection occurring 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.

Everyone knows about the existence of antibiotics, but much fewer people can tell how they were first obtained and began to be used. Today it is difficult to imagine that before the invention of these miraculous drugs one could die from a simple bacterium entering the body. At the same time, the widespread use of antibiotics has led to their uncontrolled use. The modern rhythm of life does not allow a person to get sick, so if this does happen, he tries to recover as quickly as possible, and is ready to swallow any pills that helped his colleagues, friends or relatives. At the same time, the patient is in no hurry to seek advice from a doctor.

Many people sincerely believe that antibiotics can cure absolutely everything. The drug "Penicillin", the instructions for use of which are often thrown away as unnecessary immediately after its purchase, occupies one of the top lines in the list of medicines taken for other purposes.

The emergence of the antibiotic "Penicillin"

This medicine, which is so important for medicine, got its name from one of the varieties of mold, namely Penicillium chrysogenum. Today, the drug "Penicillin" is the most important representative of the antibiotic group of drugs. It has both bactericidal and bacteriostatic effects. The emergence of the first natural antibiotic was due to a great deal of luck. Alexander Fleming, who devoted most of his life to studying the mechanisms of the human body’s fight against bacterial infections, showed untidiness unacceptable for a scientist and used dirty Petri dishes for cultivation in the experiment. After the staphylococcus colonies were grown, a strange pattern emerged: all the bacteria around the mold islands were dead. This phenomenon prompted the scientist to more closely examine the fungus of the Penicilium family. In 1928, Alexander Fleming managed to isolate a molecule that was responsible for destroying the infectious agent. Even this first antibiotic revolutionized the field of medicine.

However, it was not until 1938 that the technology was tested to produce pure penicillin in sufficient quantities. Thanks to this drug, many soldiers operated on in the field remained alive during the Second World War. For their outstanding services, Fleming and two of his followers - Florey and Chain - were awarded the Nobel Prize in 1945.

Spectrum of action

The drug "Penicillin", the use of which in reasonable quantities is absolutely safe for most people, can defeat a number of pathogenic bacteria. Its action extends to microorganisms such as streptococci, meningococci, pneumococci and gonococci. In addition, the causative agents of staphylococcus, tetanus, diphtheria, anthrax and gas gangrene have increased sensitivity to this antibiotic. At the same time, the antibiotic penicillin turns out to be practically useless in cases where it is necessary to destroy dysenteric intestinal bacteria, whooping cough and tuberculosis bacilli, or Pseudomonas aeruginosa and Friedlander pathogens.

Classification

Today we can talk about the existence of 4 groups of penicillins, each of which has its own characteristics and varying effectiveness. A natural antibiotic synthesized by mold fungi has a narrow spectrum of action, but has the least toxic effect on the human body. This category includes drugs such as Ifenoxymethylpenicillin and Benzylpenicillin. Semi-synthetic penicillins, improved in the laboratory, are used to combat microorganisms such as cocci, staphylococci, gram-positive and gram-negative bacteria. Prominent representatives of this group are the drugs “Nafcillin”, “Amoxicillin”, “Oxacillin”, “Ampicillin” and “Methicillin”. Carboxypenicillins and synthetic penicillins with a broad antibacterial spectrum are a kind of “heavy weapon”. Therefore, it is necessary to use antibiotics of these groups, which include Ticarcillin, Mezlocillin, Carbenicillin, Azlocillin, only in extreme cases and after consultation with your doctor.

Mechanism of action

How does the antibiotic penicillin work? The instructions for using the drugs answer this question only briefly. Meanwhile, it is very interesting and educational. The bacteriocidal effect of the drug "Penicillin" is based on the fact that it interferes with the synthesis of peptidoglycan. This substance is an essential component of the cell membrane of microorganisms. Thus, a bacterium that is unable to recover is doomed to death. But some of the pathogens have learned to counteract this remedy. Resistance to the drug is provided by beta-lactamase, the molecular structure of which cannot be destroyed by natural penicillin. Synthetic antibiotics do not have this disadvantage. They suppress the activity of inhibitors responsible for the production of beta-lactamase, thereby preventing bacteria from defending themselves.

Indications for use

Antibiotics belonging to the penicillin group have a wide spectrum of action. They are used for sepsis, meningococcal, pneumococcal and gonococcal infections, osteomyelitis, gas gangrene and severe phlegmon. This is not a complete list of problems that the drug Penicillin can cope with. The instructions for use also inform about the need to use an antibiotic for infected 3rd and 4th degree burns, soft tissue wounds, purulent meningitis, erysipelas, brain abscess, gonorrhea, syphilis, sycosis, furunculosis. Doctors also prescribe a course of the drug for prevention in the postoperative period. The antibiotic Penicillin is also used in the treatment of some childhood diseases. These include ailments such as umbilical sepsis, pneumonia in newborns and infants, otitis media, scarlet fever, and meningitis. During pregnancy, doctors recommend avoiding taking any medications as much as possible. It is simply impossible to predict how each of the components of the drug will affect the development of the fetus. However, in some situations, the drug Penicillin is permitted during pregnancy. Research shows that this is one of the safest types of antibiotics in such cases, since its use extremely rarely leads to undesirable consequences.

Mode of application

Most antibiotics are available in tablet form, as well as injections and drops. In this regard, the drug Penicillin is no exception. The instructions for use of the medication must contain information about the method of its use.

It has been established that the greatest effect is achieved with intramuscular administration of the antibiotic. However, rinsing solutions, as well as drops for the nose and eyes, have been successfully used to treat localized disease. The duration of treatment and dosage should be determined exclusively by the attending physician.

Contraindications

For any drug there are contraindications for use, and antibiotics are no exception. A special feature of the drug "Penicillin" is that it can act as a powerful allergen for some people.

If a patient who is hypersensitive to the drug is administered intramuscularly, anaphylactic shock may occur. In addition to individual intolerance, there are a number of ailments for the diagnosis of which the use of Penicillin is not recommended. These include bronchial asthma, hay fever, and urticaria. Combining the drug with alcohol consumption is also not allowed.

Side effects

For the vast majority of people, taking the antibiotic Penicillin does not cause any negative side effects. However, some patients may experience allergic reactions, of which a significant proportion are skin rashes. Less common but more severe are respiratory problems and anaphylactic shock. To completely eliminate unwanted effects, it is necessary to conduct a series of tests and consult with a specialist before using an antibiotic. The presence of penicillin intolerance must be reflected in the patient's medical record.

Penicillin is one of the most commonly used bactericidal drugs, available in tablet form and as a powder for injection. The medicine has a wide range of applications and is actively used to eliminate many pathologies of a bacterial nature. The most effective form of using the drug is injections.

Description and composition of the drug

Penicillin is the first bactericidal agent obtained from the waste products of microorganisms. Its inventor is called Alexander Fleming, who discovered the antibiotic by accident, discovering its antimicrobial effect.

The first samples of the drug were obtained in the USSR by scientists Balezina and Ermolyeva in the mid-twentieth century. After this, the medicine began to be produced on an industrial scale. At the end of the fifties of the twentieth century, synthetic penicillins were also obtained.

Currently, four groups of penicillins are used in medicine:

• natural origin;
• semi-synthetic compounds;
• broad-spectrum aminopenicillins;
• broad-spectrum bactericidal penicillins.

For injection use penicillin G sodium salt 500 thousand units or 1 million units. In pharmacy chains, such powder can be purchased in glass bottles sealed with a rubber stopper. Before direct administration, the powder is diluted with water. The drug can be obtained from a pharmacy with a doctor's prescription.

Pharmacological characteristics

In terms of its chemical composition, Penicillin is an acid for producing salts. Its biosynthetic products act on anaerobic spore-forming rods, gram-positive and gram-negative bacteria, inhibiting the synthesis of their walls. Benzylpenicillin is considered the most active and relevant drug today.

The penicillin drug is administered intramuscularly and immediately after direct use it enters the bloodstream and quickly concentrates in muscles and joints, and tissue lesions. The highest degree of concentration of the composition is observed half an hour to an hour after the procedure.

The concentration of the drug in the cerebrospinal fluid and abdominal cavity is minimal. The composition is excreted through the kidneys and bile. The half-life is up to one and a half hours.

Indications for use

Penicillin treatment with injections is carried out for the development of bacterial infections, including:

• focal and lobar pneumonia;
• chronic and acute osteomyelitis;
• pleural empyema;
• blood poisoning;
• acute and subacute types of endocarditis;
• tonsillitis;
• scarlet fever;
• infectious inflammatory processes of the brain;
• erysipelas;
• anthrax;
• furunculosis and its complications;
• acute cholecystitis;
• gonorrhea;
• rheumatism;
• inflammatory bacterial pathologies of the urinary tract and reproductive organs;
• diphtheria;
• ENT pathologies;
• purulent dermatological lesions;
• pyemia;
• actinomycosis.

Important: Penicillin is used not only to treat human diseases, but also to eliminate pathologies in animals and is one of the most inexpensive drugs of its kind.

Methods of treatment using Penicillin

According to the instructions for use, the drug is allowed to be administered in four main ways, depending on the type and extent of the lesion:

• into the spinal canal;
• intravenously;
• intramuscularly;
• subcutaneously

Injections are given every three to four hours, maintaining the content of the composition so that for each milliliter of the patient’s blood there is a concentration of 0.1-0.3 units. In most cases, the treatment regimen is selected individually for each patient. The same applies to the course of treatment.

Special instructions for use

In order for treatment to be as effective and safe as possible, it is necessary to take into account the following therapy problems:

1. Before starting to use the medicine, it is necessary to test for possible intolerance to antibiotics.
2. The medication must be replaced if three to five days later, if the therapy shows insufficient effectiveness.
3. To prevent the occurrence of mycotic superinfection, it is necessary to take antifungal medications during treatment. It is also important to pay attention to the likelihood of colonization of the body with resistant strains of bacteria.
4. It is possible to dilute the medicine for injection only with water for injection, strictly following the proposed proportions.
5. It is not recommended to skip injections. If missed, it is necessary to administer the drug as soon as possible and restore the regimen.
6. After the expiration date, the medicine becomes toxic and dangerous to use.

Limitations and main contraindications

Penicillin has relatively few contraindications. The main one is hypersensitivity to the antibiotic itself and other drugs in its group. In addition, the medication is not recommended for use if:

• manifestations of allergies in the form of urticaria, asthma and hay fever;
• manifestations of intolerance to antibiotics and sulfonamides.

It is necessary to use the medicine under the supervision of a doctor for pathologies of the kidneys and cardiovascular system.

Side effects and complications

An overdose of medication does not pose a threat to the patient's life. In this case, nausea and vomiting and a general deterioration in health may occur. In addition, the development of hyperkalemia is likely with the simultaneous use of potassium supplements. In rare cases, epileptic seizures are possible. Exceeding the prescribed dosage is treated symptomatically.

With prolonged use of the antibiotic, allergic reactions are likely to occur (urticaria, swelling, rash formation, anaphylactic manifestations, and, extremely rarely, death). Treatment in this situation is symptomatic. Typically, adrenaline is administered intravenously. In other situations the following are also possible:

• disturbance of digestive processes and stool;
• dysbacteriosis;
• fungal diseases of the oral cavity and vagina;
• neurotoxic manifestations, seizures, coma.

Important: In order to reduce the likelihood of negative reactions to therapy, it is recommended not to exceed the established dosages and not to extend the course of treatment without the consent of the doctor.

Interaction of Penicillin with other drugs

Concomitant treatment with Probenecid increases the half-life of the antibiotic components. The use of Tetracycline and sulfonamides significantly reduces the effectiveness of Penicillin. Cholistyramine seriously reduces the bioavailability of the antibiotic.

Due to incompatibility, you cannot give an injection of Penicillin and any aminoglycoside at the same time. The combined use of thrombolytics is also prohibited.

The risk of bleeding increases with the simultaneous use of anticoagulants and Penicillins against Pseudomonas aeruginosa. Therefore, treatment in this case should be supervised by a specialist.

Antibiotic therapy slows down the elimination of methotrexate and also reduces the effectiveness of oral contraceptives.

Penicillin analogues

1. Cefazolin. A drug from the group of cephalosporins, which can be used in case of intolerance to penicillin medications. It is used for intramuscular and intravenous administration and retains its therapeutic properties after the procedure for ten hours.
2. Ceftriaxone. The cephalosporin medication is most often used in a hospital setting. Intended for the treatment of inflammatory processes caused by bacterial pathogens, it is active against gram-negative bacteria and anaerobic infections.
3. Extensillin. It is one of the long-acting beta-lactam antibiotics. The medication is available in powders and is not recommended for use simultaneously with non-steroidal drugs against inflammatory processes.

Among the drugs for oral administration containing a similar active ingredient are:

• Ampicillin trihydrate;
• Amoxicillin;
• Flemoxin Solutab;
• Amosin;
• Amoxicar;
• Ecobol.

Important: Replacement is made if it is impossible to give injections, intolerance to penicillins, as well as if the latter are insufficiently effective.

Conclusion

Penicillin is a first-generation antibiotic that has been tested over the years and through long-term trials. Currently, the drug is used to treat many bacterial infections in a modernized form and is relatively safe for humans. Penicillins are actively used in veterinary medicine and have several varieties, which are selected for therapy depending on the type of disease and the individual characteristics of the patient.