Penicillin g sodium salt. When is the tablet form of penicillin prescribed?

Currently, 6 groups of penicillins are known:

1. natural penicillins;
2. Isoxazolpenicillins;
3. Amidinopenicillins;
4. Aminopenicillins;
5. Carboxypenicillins;
6. Ureidopenicillins.

All penicillins have fundamentally the same pharmacodynamics. They disrupt the formation of the microbial wall during mitosis, as they are competitive inhibitors of transpeptidases, enzymes that catalyze the formation of interpeptide bridges of the cell wall. In addition, they can disrupt the synthesis of adhesins - proteins that cover the microbe like hairs and ensure its binding to the cells of the macroorganism. Only in this way is a fixed microbial cell capable of reproduction. Pharmacological effect - bactericidal.

Differences between named groups of penicillins

Each drug penicillin has its own characteristics. Differences are mainly related to the features of their spectrum of action, pharmacokinetics and undesirable effects.

Natural penicillins - antibiotics of the penicillin group

Natural penicillins (benzylpenicillins, bicillins, phenoxymethylpenicillin). These are narrow spectrum antibiotics. They mainly affect Gr. "+" bacteria (corynebacteria, anthrax bacilli, clostridia, spirochetes) and cocci (staphylococci, streptococci, pneumococci). It should be noted the very high sensitivity of microorganisms to natural penicillins (MIC = 0.0X - 0.00X µg / ml), it is much higher than to other groups of penicillins.

Penicillin for children - instructions for use

The sodium salt of benzylpenicillin (penicillin G) can be administered intramuscularly (IM), intravenously (IV), endolumbally and into various cavities. Potassium and novocaine salts of benzylpenicillin are used only intramuscularly.

With intramuscular injection of therapeutic doses, the average therapeutic concentration (MTC) in the blood plasma occurs after 15 minutes (after 30-40 minutes - when using novocaine salt). In this case, only 40-60% of the drug is associated with blood proteins, and the remaining 50% are free. Therefore, benzylpenicillin is an emergency remedy.

From the blood, penicillin penetrates into the mucous membranes, lungs, kidneys, heart, intestinal wall, pleural and synovial fluid, in which its concentration is 25-50% of the concentration in blood plasma, Benzylpenicillin penetrates poorly through the blood-brain barrier, even with inflammation of the meninges, the maximum the concentration in the cerebrospinal fluid is 10% of the level in the blood.

The time of maintaining the therapeutic concentration in the blood ranges from 3 to 4 hours. Therefore, the frequency of prescribing benzylpenicillin 6 times a day (in practice, it is more often prescribed 4 times a day, the continuation of the drug's action is provided by increasing the dose, such a possibility of dosing benzylpenicillin is explained by its very large breadth of therapeutic action) after a month of life. The exception is the novocaine salt of the drug (benzylpenicillin procaine), which is administered 2 times a day.

The elimination half-life is 30 minutes, but in case of renal insufficiency it can increase to 6-20 hours, since the main route of excretion is filtration in the glomeruli of the kidneys unchanged. Therefore, when the clearance of endogenous creatinine is less than 30 ml / min, a correction of the dosing regimen is required. In newborns, the frequency of administration for benzylpenicillin: up to 1 week of life - 2 times a day, up to 1 month - 3-4 times a day. This is due to the anatomical and physiological characteristics of the kidneys of young children. Penicillins are effective in acidic urine.

Pharmacokinetic features of penicillin:

Penicillin can only be administered parenterally (intramuscularly, intravenously). Piperacillin is only 16% bound to plasma proteins.

Excretion of drugs involves not only the kidneys, but also the liver.

Multiplicity of appointment - 3 times a day.

Secondary resistance to the listed groups of penicillins (except for carboxy- and ureidopenicillins) develops slowly. Interaction of penicillins with drugs from other groups. Penicillins are incompatible with many substances: bases, solutions of salts of heavy and alkaline earth metals, heparin, gentamicin, lincomycin, levomycetin, tetracyclines, amphotericin B, immunoglobulins, barbiturates, aminophylline, etc. Therefore, penicillins should be administered with a separate syringe.

Penicillins are pharmacodynamically incompatible with macrolides, tetracyclines, polymyxin M (mutual decrease in effectiveness). Synergistic is the combination of penicillins with aminoglycosides, cephalosporins, monobactams. In meningitis caused by meningococcus, pneumococcus or Haemophilus influenzae type "b" - aminopeaicillins synergists of levomycetin, which has a bactericidal effect on these microbes. Penicillins are pharmacokinetically incompatible with butadione, furosemide and glucocorticoids, since the latter accelerate the elimination of the former from the body.

Side effects of penicillins

Natural penicillins, isoxazolpenicillins, amidinopenicillins, aminopenicillins are low-toxic antibiotics with a wide range of therapeutic effects, so they can be administered in large doses. Undesirable effects are most frequent with the introduction of these drugs allergic reactions (both immediate and delayed types). It should be noted that when using ampicillin relatively often (in 5-10% of patients), a kind of "ampicillin" spotty-nodular rash (of non-allergic origin) appears, localized first on the skin of the trunk, then on the limbs and head, accompanied by itching and fever.

This side effect occurs most often on the 5th to 10th day of treatment with ampicillin, in the treatment of large doses of the drug in children with lymphadenopathy and viral infections or with concomitant use of allopurinol, and in almost all patients with infectious mononucleosis. To a certain extent, this complication is associated with the release of endotoxins of dead microorganisms, especially those that are part of the normal intestinal microflora.

When high concentrations of drugs are created in the blood plasma, they penetrate into the cerebrospinal fluid and the brain, which leads to neurotoxic effects: hallucinations, delirium, dysregulation of blood pressure, seizures. All these phenomena are the result of antagonism with gamma-aminobutyric acid (an inhibitory mediator in the central nervous system).

When using ampicillin, cases of pseudomembranous colitis have been described.

Local infiltrates and vascular complications in the form of Onet's syndromes (ischemia and gangrene of the extremities with accidental injection into the artery) or Nicolau (embolism of the pulmonary and cerebral vessels when injected into a vein).

Carboxypenicillins and ureidopenicillins are drugs with a small breadth of therapeutic action. Their use may be accompanied by the appearance of: allergic reactions, symptoms of neurotoxicity, acute interstitial nephritis, intestinal dysbacteriosis, thrombocytopenia, neutropenia, leukopenia, eosinophilia, hypokalemia and hypocaligistia, hypernatremia (the last two complications ureidopenicillins usually do not cause).

Combination preparations containing clavulanic acid can cause acute liver damage.

Isoxazolpenicillins - antibiotics of the penicillin group

Oxacillin, cloxacillin, flucloxacillin are isoxazolpenicillins. This group of penicillins also includes methicillin, nafcillin and dicloxacillin, which are practically not used due to high toxicity and / or low efficiency. These are the so-called anti-staphylococcal penicillins.

It must be emphasized that isoxazolpenicillins for children, like all other beta-lactam antibiotics, do not affect the so-called methicillin-resistant staphylococci. Their spectrum of action is similar to the spectrum of natural penicillins, but the greatest activity of these drugs is manifested in the effect on staphylococci, including staphylococci that produce beta-lactamase.

Pharmacokinetic differences between isoxazolpenicillins and benzylpenicillin:

Isoxazolpenicillins can be administered both parenterally (in / m, in / in) and orally 1-1.5 hours before meals. Compliance with the rule of taking the drug in relation to food intake is mandatory, since these antibiotics have low resistance to hydrochloric acid. In particular, for this reason, their bioavailability ranges from 30 to 50%.

These drugs have a high ability to bind to blood plasma proteins, it is more than 90%, they cannot be removed from the body using hemodialysis.

Excretion is carried out in large quantities (especially oxacillin) by the liver. Therefore, in non-severe renal insufficiency, their use does not require correction of the dosing regimen.

Amidinopenicillins - antibiotics of the penicillin group

Amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin are narrow-spectrum antibiotics, but their spectrum of action lies in the region of Gr. "-" enterobacteria (escherichia, shigella, salmonella, klebsiella, proteus).

Pharmacokinetic differences between amidinopenicillins and benzylpenicillin:

All drugs (except amdinocillin) can be administered orally. They have sufficient bioavailability (about 40%). It should be noted that enteral forms of the drug are inactive in the lumen of the gastrointestinal tract, they practically do not cause dysbacteriosis.

More volume of distribution. Drugs penetrate better through the blood-brain barrier and into cells.

Microorganisms practically do not develop secondary resistance to amidinopenicillins.

In order to increase the spectrum of action, amidinopenicillins for children can be combined with isoxazolpenicillins, natural penicillins and other antibiotics.

Aminopenicillins - antibiotics of the penicillin group

Ampicillin, amoxicillin, thalampicillin, bacampicillin, pivampicillin are broad-spectrum antibiotics. Their spectrum of action overlaps the spectrum of all the above groups of narrow-spectrum penicillins, and they additionally affect Listeria, Enterococci, Haemophilus influenzae, Bordetella, Helicobacter pylori and Actinomycetes. Gr. are more sensitive to aminopenicillins. "+" bacteria than Gr. "-".

However, it should be noted that aminopenicillins for children do not affect staphylococci that produce beta-lactamase. In other words, they do not solve the problem of hospital infection, where staphylococcus and other beta-lactamase-producing microbes play an important role. Therefore, combined preparations have been created: ampiox (ampicillin + oxacillin), clonac-R (ampicillin + cloxacillin), unazine and its oral analogues sulacillin, sultamicillin (ampicillin + sulbactam, which is a beta-lactamase inhibitor), clonac X (amoxicillin + cloxacillin) and augmentin and its analogue amoxiclav (amoxicillin + clavulanic acid, which is also a beta-lactamase inhibitor).

Pharmacokinetic differences between aminopenicillins and benzylpenicillin:

Inside, you can prescribe all the drugs in this group. However, ampicillin must be taken 1-1.5 hours before meals, its bioavailability is about 40%; Amoxicillin is taken regardless of food intake, its bioavailability is 70-80%. Amoxicillin in a special dosage form Flemoxin Solutab has a bioavailability of 93%. Such high bioavailability several times reduces the load on the flora of the gastrointestinal tract, and this reduces the risk of dysbacteriosis.

In addition, the contact time of the drug with the intestinal mucosa is reduced to a minimum, therefore, dyspeptic disorders appear less frequently. Finally, the dose of the drug taken orally is almost equal to the dose of the same drug administered parenterally. A tablet of modified amoxicillin - flemoxin solutab can be broken, chewed and dissolved, which makes it easier to swallow the drug, and, therefore, compliance with the regimen (or, as they say now, compliance).

It is known that 30% of patients who regularly take medications have difficulty swallowing tablets and capsules; 25% of patients (more often children, elderly people) prefer dissolved forms of drugs. It should be emphasized that non-compliance with the antibiotic regimen leads to treatment failure, recurrence or chronicity of the disease and the spread of resistant infection. Tal-, bak and pavampicillins have sufficient bioavailability, they are not active in the intestinal lumen, therefore they rarely cause dysbacteriosis and dyspeptic disorders.

Aminopenicillins in the blood remain in free form, about 80%. Drugs penetrate better into many tissues and fluids. With meningitis, the concentration of drugs in the cerebrospinal fluid can be 70-95% of their concentration in blood plasma.

The multiplicity of the appointment of combined drugs 2-3 times a day.

Carboxypenicillins - antibiotics of the penicillin group

Carbenicillin, carfecillin, carindacillin, ticardillin - carboxypenicillins. These are the so-called antipseudomonal antibiotics, since these microbes are most sensitive to them. Although many other microorganisms fall into their spectrum of action (streptococci, pneumococci, neisseria, clostridia, corynebacteria, anthrax bacilli, spirochetes, escherichia, shigella, salmonella, klebsiella, proteus, bacteroids).

However, it should be noted that staphylococci do not fall into the spectrum of influence of carboxypenicillins. Therefore, in some cases, carboxypenicillins for children must be combined with isoxazolpenicillins; A special combined preparation, timentin, has also been created. (ticarcillin + clavulanic acid).

Pharmacokinetic differences between carboxypenicillins and benzylpenicillin:

Carfecillin and carindacillin are the phenyl and indanyl esters of carbenicillin. These drugs are administered by mouth, their bioavailability is about 40%. Carbenicillins and ticarcillins are practically not absorbed from the gastrointestinal tract.

Drugs almost do not penetrate the blood-brain barrier.

Multiplicity of appointment - 4 times a day.

Secondary microbial resistance develops rapidly.

Cephalosporin group

There are 4 generations (generations) of cephalosporins. Their division is based not on a chronological criterion, but mainly on the features of the spectrum of action and pharmacokinetics. At the same time, all cephalosporins are characterized by varying degrees of resistance to some staphylococcal beta-lactamases, so they suppress most benzylpenicillin-resistant strains of these microorganisms.

For all cephalosporins, there is a risk of cross-allergy with other beta-lactam antibiotics (penicillins, carbapenems, monobactams). Finally, all cephalosporins have the same pharmacodynamics. They, like penicillins, disrupt the synthesis of the microbial wall at the time of mitosis. Pharmacological effect - bactericidal. Cephalosporins are broad spectrum antibiotics. Different generations of cephalosporins differ significantly from each other.

Group of cephalosporins of the first generation:

For parenteral administration - cephaloridine (ceporin), cephalothin (keflin), cefazolin (kefzol), cefapirin, cefacitril (cephalospor).

For oral administration - cephalexin (keflex, ospexin, ceporex), cefadroxil (ultracef, duracef), cefradin (velocef). The latter drug can also be administered parenterally.

The spectrum of action of 1st generation cephalosporins is quite wide. They affect Gr. "+" and Gr. "-" cocci (except enterococci and methicillin-resistant staphylococci), corynebacteria, anthrax bacilli, spirochetes, escherichia, shigella, salmonella, moraxella, klebsiella, proteus, hemophilic bacilli, bordetella, yersinia. The greatest sensitivity to cephalosporins of the first generation in Gr. "+" bacteria and cocci (except for enterococci and methicillin-resistant staphylococci), significantly less in Gr. "-" bacteria. To increase the effectiveness or expand the spectrum (due to the effect on Pseudomonas), these antibiotics can be combined with amidinopenicillins or with monobactams, aminoglycosides, etc.

Group II generation cephalosporins:

For parenteral administration - cefuroxyl (ketocef, zinacef), cefamandol (mandole, lecacef), cefoxitin (mefoxin, mefoxitin), cefotetan (cetofan), cefotiam (galospor), cefonicide (monocide), ceforanide (precef), cefmetazole, cefatidime, cephaloglycine , cefatrizine.

For oral administration - cefuroxime (zinnat), cefaclor (ceclor, ceflor, vercef, alfacet), cefaprozil, loracarbef.

The spectrum of action of second-generation cephalosporins coincides with the spectrum of first-generation cephalosporins, but antimicrobial activity against Gr. "-" flora is most pronounced in II generation cephalosporins. At the same time, second-generation cephalosporins are resistant to some beta-lactamase Gr. "-" bacteria. In addition, cefoxitin and cefotetan showed activity against bacteroids; in cefamandol - to methicillin-resistant staphylococci. To expand the spectrum of action or increase the effectiveness of these antibiotics can be combined with isoxazolpenicillins, aminoglycosides, etc.

III generation cephalosporin group:

For parenteral administration - cefotaxime (claforan), ceftazidin (fortum, kefadim, tazidin, tizacef), deftriaxone (rodefin, longacef), cefoperazone (defobide), ceftizoxime (epocelin, cefizox), moxalactam (moxam, lamoxef), cefmenoxime (cefmax) , cefsulodin (cefomonide), cefodizyme (modivide), latamoxef.

For oral administration - ceftibuten (cedex), cefixime (cefspan), cefetamet pivoxil, cefpodoxime proxetil.

The spectrum of action of third-generation cephalosporins is greater than that of the previous two generations. It additionally includes: pseudomonas, morganella, serrations, clostridia (except CI. difficile) and bacteroids. Moreover, the activity of III generation cephalosporins is even more, in comparison with II generation cephalosporins, shifted towards Gr. "-" flora. III generation cephalosporins are also resistant to some beta-lactamase Gr. "-" bacteria. It should be noted the moderate activity of most antibiotics of this group to Pseudomonas, serrations, morganella and anaerobes.

The exceptions are the following drugs: Pseudomonas is highly sensitive to ceftazidime and cefoperazone; in anaerobes - to latamoxef, cefotaxime and ceftriaxone. To expand the spectrum of action or increase the effectiveness of the use of III generation cephalosporins, they can be combined with natural penicillins, isoxazolpenicillins (to increase the effect on Gr. "+" bacteria, cocci and clostridia), aminopenicillins (to expand the spectrum due to the effect on enterococci, listeria), carboxy- and ureidopenicillins, aminoglycosides (to increase the effect on pseudomonads, serrations, anaerobes), a synthetic anti-infective drug - metronidazole (to increase the effect on anaerobes), etc.

IV generation cephalosporins:

Cefepime (Maxipim), Cefpirome (Katen), Cefclidin, Cefquinome, Cefozopran, Cefoseliz. All drugs are administered only parenterally (in / m, in / in). The spectrum of action of IV generation cephalosporins is very wide. It is larger than previous generations.

IV generation cephalosporins affect the same microorganisms as III cephalosporins and additionally - on citro-, entero- and acinetobacter. Moreover, they are equally highly active in relation to Gr. "+", and in relation to Gr. "-" flora. IV generation cephalosporins affect multi-resistant microorganisms resistant to extended spectrum beta-lactamases. This is due to the ability of drugs to easily penetrate the cell membrane, due to their high affinity for penicillin-binding proteins (PBP), and create high concentrations in the periplasmic space.

All this determines the high activity of cefepime (Maxipim) and similar drugs against strains of microorganisms resistant to other cephalosporins and, sometimes, even to carbapenems. However, bacteroids fall out of the zone of influence of these drugs, therefore, to expand the spectrum, they can be combined with carboxy- and ureidopenicillins, metronidazole, etc. Secondary resistance of microorganisms to all cephalosporins develops slowly.

Ureidopenicillins - antibiotics of the penicillin group

Azlocillin, mezlocillin, piperacillin - ureidopenicillins. These are also antipseudomonal antibiotics. Their spectrum of action coincides with carboxypenicillins. The most active drug from this group is piperacillin. Its combined drug is tazocin (piperacillin + tazabactam, the latter is a beta-lactamase inhibitor).

Penicillin is an antimicrobial antibiotic for the prevention and control of infectious diseases in the human body. It belongs to a group of drugs, the purpose of which is to neutralize the development of pathogenic bacteria in the human body.

The composition and properties of penicillin tablets

This drug was discovered by accident by the English scientist Alexander Fleming in 1928 on the basis of spores of the fungus Penicillium notatum. In Russia, the first samples of penicillin were obtained in 1932 by biologists Yermolyeva and Balezina.

A positive effect is achieved due to the fact that aminopenicillanic acid destroys the cell walls of pathogenic bacteria, as a result of which this prevents their reproduction and they die.

Preparations of the penicillin family are used for various kinds of diseases that occur due to a weakened immune system and the ingestion of infectious bacteria such as staphylococci, streptococci, pneumococci, etc.

The most commonly used drugs are two types from the penicillin family: penicillin G (benzylpenicillin) and penicillin V (phenoxymethylpenicillin). The benzylpenicillin group includes Benzylpenicillin and its analogues (Retarpen, Benzylpenicillin-KMP and Benzylpenicillin sodium salt), and the phenoxymethylpenicillin group includes Phenoxymethylpenicillin and its analogues (Penicillin V, Penicillin B, Ospen and others). Now let's look at some of these drugs in more detail.

The main drugs of penicillin and their use

Phenoxymethylpenicillin (Phenoxymethylpenicillin)

Release form

Packing - 10 tablets, 1 tablet contains 100 mg of phenoxymethylpenicillin.

Indications for use

It is used to treat pneumonia, bronchitis, tonsillitis, stomatitis, abscess, furunculosis, scarlet fever, anthrax, diphtheria, inflammation of the lymph nodes, syphilis, gonorrhea and other diseases.

It is rapidly absorbed by the stomach and reaches the blood plasma in 40-50 minutes. It is mainly excreted from the body with urine.

How to use

Adults and adolescents over 14 years of age should take 0.5-1 g 2-3 times a day 40-60 minutes before meals. One-year-old children 10-15 mg/kg once a day, and children from 1 year to 6 years 15-20 mg/kg.

Side effect

With prolonged use for two weeks, allergic side effects are possible: conjunctivitis, urticaria, joint pain. From the digestive tract: heartburn, diarrhea, vomiting, nausea.

Contraindications for use

Phenoxymethylpenicillin should be taken with caution in patients with allergic diseases (bronchial asthma, fever, diathesis), as well as those suffering from vomiting and diarrhea.

Price from 17 rubles. for 10 pcs

V-Penicillin (instruction for use)

Release form

The package contains 10 tablets, 1 tablet contains 250 or 500 mg of phenoxymethylpenicillin.

Indications for use

It is used to treat pharyngitis, pneumonia, infectious skin diseases, fever, erysipelas of the skin caused by staphylococci, streptococci and pneumococci. It has an effect on some Escherichia coli, forms of Proteus and Salmonella.

Mode of application

Adults and adolescents over 14 years of age should take 500 mg twice a day 40-60 minutes before meals. The drug is taken for 1-2 weeks.

According to the latest clinical studies, it is recommended to increase the dose and frequency of taking the drug in the first two days, i.e. take 500 mg three times a day, and then continue taking 500 mg 1-2 times a day during the week.

Side effect

With prolonged use and taking large doses of the drug, headache, heartburn, nausea, vomiting and gastrointestinal disorders may occur.

Contraindication for use

In order to avoid exacerbation of certain diseases, patients who suffer from allergies, kidney failure and have diseases of the gastrointestinal system should take this drug with caution, adjusting the dosage and duration of its use.

The price is about 45 rubles. for 20 pcs.

Ospen (instruction for use)

Release form

This drug is available in tablets, granules and syrup. Tablets per pack - 20 pcs. One tablet contains 250 mg of phenoxymethylpenicillin.

Indications for use

It is used for infectious diseases of the respiratory system (bronchitis, pneumonia), ear, throat, nose (tonsillitis, pharyngitis, scarlet fever, otitis media), for infected wounds and burns (furunculosis, abscesses, phlegmon).

Mode of application

For infections of mild to moderate severity, adults and adolescents from 14 years of age take 500 mg 2-3 times a day for about 7-10 days. The drug is taken regardless of food intake. Children aged 1-6 years - 250 mg 2 times a day, children aged 6-12 years - 500 mg twice a day.

Side effect

Prolonged use of the drug can cause an upset of the digestive system and cause heartburn, nausea, vomiting and diarrhea, as well as cause allergy symptoms in the form of dermatitis, urticaria or edema, therefore, after the appearance of side effects, it is necessary to consult with your doctor about further use of the drug.

Contraindications for use

A contraindication to the use of the drug may be the presence in patients of bronchial asthma, allergic diathesis, severe forms of gastrointestinal diseases, which are accompanied by heartburn, diarrhea, nausea and vomiting.

The benzylpenicillin group includes drugs that are obtained by biosynthesis, which is why they are quickly destroyed in the acidic environment of the stomach, so they are produced in powder form and injected into the body.

Benzylpenicillin (sodium salt)

Release form

Produced as a powder in vials. 1 bottle contains 1 million units or 10 ml and 500 thousand units or 5 ml.

Indications for use

It is used for pneumonia, pleurisy, endocarditis, sepsis, meningitis, infections of the biliary and urinary tract, tonsillitis, skin infections, diphtheria, anthrax, scarlet fever, gynecological and ENT diseases, syphilis, gonorrhea.

Mode of application

The drug in the form of a solution is administered intramuscularly and intravenously. With an average severity of the disease, 4–6 million units per day for 4 injections. With a severe degree of the disease, 10–20 million units per day.

Side effects

• Adverse reactions can manifest as urticaria, rashes on the mucous membranes and skin, nephritis, edema, cardiac arrhythmia.
• Contraindications for use
• Hypersensitivity to drugs of the penicillin group, as well as to patients suffering from epilepsy.
• The price of a bottle of 10 ml is 60 rubles.

Retarpen (instruction for use)

Release form

Produced as a powder for injection in vials of 6, 12 and 24 ml.

Indications for use

It is used in the treatment of scarlet fever, skin diseases, acute tonsillitis and syphilis.

Mode of application

To maintain a positive therapeutic effect, fast-absorbing drugs of the penicillin group are first prescribed and then treatment is continued, administering the drug to patients weekly. For children: 1 injection of 12 ml with an interval of 1 week. For adults: 1 injection of 24 ml with an interval of 1 week.

Side effect

The possibility of an allergic reaction.

Contraindications for use

Hypersensitivity to penicillin antibiotics.

The price for a bottle of 24 ml is 756 rubles.

One of the substitutes for penicillin is Rifogal, which is available in ampoules and is used for injections and injections. It is an antibiotic derived from the fungus Streptomyces mediterranea. It is used in patients with hypersensitivity to penicillin and does not interact with other antibiotics. It is excreted from the body with bile and partly with urine.

Rifogal (instruction for use)

Release form

The drug is produced in ampoules. One vial for intramuscular injection contains 125 or 250 mg of rifamycin (sodium salt), and 1 ampoule for intravenous administration contains 500 mg.

Indications for use

The drug is used to treat tuberculosis, gonorrhea, syphilis, biliary tract infections, i.e. in diseases caused by staphylococci, streptococci and pneumococci.

Mode of application

Rifogal can be administered intravenously, intramuscularly and into the lesion, i.e. locally. Adults and children over 6 years of age are administered 500 mg intramuscularly twice a day. Children under 6 years of age 125 mg every 12 hours.

Side effect

The drug is well tolerated by patients, but with prolonged use, allergic reactions may occur, in patients with liver disorders, signs of jaundice, as well as diarrhea, heartburn, nausea, and vomiting.

Contraindications for use

Hypersensitivity to drugs of the rifamycin group, lactation, impaired renal function, the first period of pregnancy.

Preparation of solution for injection

Finally, I would like to say how dilute powder for injection. To do this, use a solution of novocaine, water for injection or saline NaCl (sodium chloride). For intramuscular injections, any of the solutions is suitable, but care must be taken that it is not too hot.

A solution of novocaine is used to dilute the powder if it is necessary to reduce pain and burning at the injection site of benzylpenicillin into the body.

When administered intramuscularly, the drug can be diluted with water for injection and take 1.5 ml of water per 250 mg of powder in a vial, and 500 mg 3 ml of water.

Penicillin is one of the main representatives of the group of antibiotics, the drug has a wide range of bacteriostatic and bactericidal action (of penicillin preparations, benzylpenicillin is the most active).

Indications and dosage:

The use of penicillin is indicated:

• With sepsis (especially streptococcal)
• In all sulfanilamide-resistant cases of relevant infections (pneumococcal, gonococcal, meningococcal infections, etc.)
• With extensive and deeply localized infectious processes (osteomyelitis, severe phlegmon, gas gangrene)
• After injuries with involvement in the process and infection of large musculoskeletal arrays
• In the postoperative period for the prevention of purulent complications
• For infected third and fourth degree burns
• For soft tissue injuries
• For chest injuries
• With purulent meningitis
• For brain abscesses
• With erysipelas
• With gonorrhea and its sulfanilamide-resistant forms
• With syphilis
• With severe furunculosis
• With sycosis
• With various inflammations of the eye and ear

In the clinic of internal diseases, Penicillin is used to treat lobar pneumonia (together with sulfanilamide drugs), focal pneumonia, acute sepsis, cholecystitis and cholangitis, protracted septic endocarditis, as well as for the prevention and treatment of rheumatism.

In children Penicillin is used: for umbilical sepsis, septicopyemia and septic-toxic diseases of newborns, pneumonia in newborns and infants and young children, otitis media in infants and young children, septic form of scarlet fever, septic-toxic form of diphtheria (necessarily in combination with a special serum ), pleuropulmonary processes that are not amenable to the action of sulfanilamide drugs, purulent pleurisy and purulent meningitis, with gonorrhea.

The antimicrobial effect of Penicillin is achieved both with resorptive and with its local action.

Penicillin preparations can be administered intramuscularly, subcutaneously and intravenously, into cavities, into the spinal canal, by inhalation, sublingually (under the tongue), inside; locally - in the form of eye and nasal drops, rinses, washes.

When administered intramuscularly, penicillin is rapidly absorbed into the blood, but after 3-4 hours, penicillin almost completely disappears from it. For the effectiveness of therapy in 1 ml of blood should be 0.1-0.3 IU of penicillin, therefore, to maintain the therapeutic concentration of the drug in the blood, it should be administered every 3-4 hours.

The use of Penicillin for the treatment of gonorrhea, syphilis, pneumonia, cerebrospinal meningitis is carried out according to special instructions.

Overdose:

Not described.

Side effects:

Treatment with benzylpenicillins, bicillins and other penicillin-containing drugs may be accompanied by side effects, most often of an allergic nature.

The occurrence of allergic reactions to penicillin preparations is usually associated with sensitization of the body to them as a result of the previous use of these drugs, as well as as a result of their long-term exposure: professional sensitization of nurses, people working in the production of antibiotics.

Less commonly, allergic reactions are observed upon first contact with penicillin. They occur mainly in people suffering from allergic diseases (urticaria, bronchial asthma). Allergic reactions to penicillin from the skin are expressed in erythema, limited or widespread rashes, urticaria and urticaria-like rashes, macular, vesicular, pustular rashes, sometimes life-threatening exfoliative dermatitis. Numerous cases of contact dermatitis have been registered (medical staff of medical institutions).

Contact dermatitis and reactions from the skin and mucous membranes are observed both with general exposure and with topical application of Penicillin in the form of ointments, lotions, drops for the nose and eyes.

• On the part of the respiratory organs, rhinitis, pharyngitis, laryngopharyngitis, asthmatic bronchitis, bronchial asthma are noted.
• From the gastrointestinal tract, allergic reactions are expressed in stomatitis, nausea, vomiting, and diarrhea.

In some cases, the distinction between toxic and allergic genesis of side effects is difficult. The allergic origin of these phenomena is indicated by their combination with skin rashes; under the influence of penicillin, the development of agranulocytosis is also possible.

If allergic reactions occur from the skin, respiratory tract, gastrointestinal tract, treatment with penicillin should be stopped or its dose should be reduced, the patient should be prescribed Diphenhydramine, Pipolfen, Suprastin, calcium chloride, vitamin B1.

It should be remembered about the possibility of sensitization of the body even in the prenatal period during the treatment of pregnant women with penicillin preparations.

Contraindications:

The use of penicillin is contraindicated in:

• Hypersensitivity to penicillin
• Bronchial asthma
• Urticaria
• Hay fever and other allergic diseases
• Hypersensitivity of patients to antibiotics, sulfonamides and other drugs

Possible sensitization of the body to penicillin during fetal development in the treatment of pregnant women with its antibiotics, penicillin preparations.

Interaction with other drugs and alcohol:

Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Care must be taken when combining penicillins active against Pseudomonas aeruginosa with anticoagulants and antiplatelet agents (potential risk of increased bleeding). It is not recommended to combine penicillins with thrombolytics. When combined with sulfonamides, the bactericidal effect may be weakened. Oral penicillins may reduce the effectiveness of oral contraceptives due to impaired enterohepatic estrogen circulation. Penicillins can slow down the excretion of methotrexate from the body (inhibit its tubular secretion). The combination of ampicillin with allopurinol increases the likelihood of a skin rash. The use of high doses of the potassium salt of benzylpenicillin in combination with potassium-sparing diuretics, potassium preparations, or ACE inhibitors increases the risk of hyperkalemia. Penicillins are pharmaceutically incompatible with aminoglycosides.

Drinking alcohol during treatment with penicillin preparations is strictly contraindicated.

In the culture of mold strains of fungi Penicillium Notatum on the basis of an accidental discovery that mold fungus entering the culture of bacteria from the external environment has a bactericidal effect on the culture.

pharmachologic effect

Antibiotic of the biosynthetic penicillin group. It has a bactericidal effect by inhibiting the synthesis of the cell wall of microorganisms.

Active against Gram-positive bacteria: Staphylococcus spp., Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis;

Gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis;

anaerobic spore-forming rods;

Strains resistant to benzylpenicillin Staphylococcus spp. that produce penicillinase. Decomposes in an acidic environment.

The novocaine salt of benzylpenicillin, compared with potassium and sodium salts, is characterized by a longer duration of action due to low solubility and the formation of a depot at the injection site.

Pharmacokinetics

Indications

Treatment of diseases caused by microorganisms sensitive to benzylpenicillin: lobar and focal pneumonia, pleural empyema, sepsis, septicemia, pyemia, acute and subacute septic endocarditis, meningitis, acute and chronic osteomyelitis, infections of the urinary and biliary tract, tonsillitis, purulent infections of the skin, soft tissues and mucous membranes, erysipelas, diphtheria, scarlet fever, anthrax, actinomycosis, treatment of pyoinflammatory diseases in obstetric and gynecological practice, ENT diseases, eye diseases, gonorrhea, blennorrhea, syphilis.

Dosing regimen

Individual. Enter in / m, in / in, s / c, endolumbally. With the / m and / in the introduction of adults, the daily dose varies from 250,000 to 60 million units. The daily dose for children under the age of 1 year is 50,000-100,000 IU / kg, over 1 year - 50,000 IU / kg; if necessary, the daily dose can be increased to 200,000-300,000 IU / kg, according to vital indications - up to 500,000 IU / kg. Multiplicity of introduction 4-6 times / day. Depending on the disease and the severity of the course, it is administered endolumbally for adults - 5000-10,000 IU, for children - 2000-5000 IU 1 time / day for 2-3 days, then they switch to intramuscular injection. S / c benzylpenicillin is used for chipping infiltrates (100,000-200,000 IU in 1 ml of 0.25% -0.5% novocaine solution). In the cavity (including the abdominal, pleural) is administered at a concentration of 10,000-20,000 IU / 1 ml for adults, and 2000-5000 IU / 1 ml for children. The duration of the introduction is 5-7 days, then they switch to the / m administration. Benzylpenicillin potassium salt is used only in / m and s / c, in the same doses as benzylpenicillin sodium salt. Benzylpenicillin novocaine salt is used only in / m. The average therapeutic dose for adults: single - 300,000 IU, daily - 600,000 IU. Children under the age of 1 year - 50,000-100,000 U / kg / day, over 1 year - 50,000 U / kg / day. Multiplicity of introduction 3-4 times / day. The duration of treatment with benzylpenicillin, depending on the form and severity of the course of the disease, can range from 7-10 days to 2 months or more.

Side effect

From the digestive system: diarrhea, nausea, vomiting. Effects due to chemotherapeutic action: vaginal candidiasis, oral candidiasis. From the side of the central nervous system: when using benzylpenicillin in high doses, especially with endolumbar administration, neurotoxic reactions may develop: nausea, vomiting, increased reflex excitability, symptoms of meningism, convulsions, coma. Allergic reactions: fever, urticaria, skin rash, rash on mucous membranes, joint pain, eosinophilia, angioedema. Cases of anaphylactic shock with a fatal outcome are described.

Contraindications

Hypersensitivity to benzylpenicillin and other drugs from the group of penicillins and cephalosporins. Endolumbar administration is contraindicated in patients suffering from epilepsy.

Pregnancy and lactation

special instructions

Use with caution in patients with impaired renal function, with heart failure, predisposition to allergic reactions (especially with drug allergies), with hypersensitivity to cephalosporins (due to the possibility of cross-allergy). If after 3-5 days after the start of the application of the effect is not observed, you should switch to the use of other antibiotics or combination therapy. In connection with the possibility of developing fungal superinfection, it is advisable to prescribe antifungal drugs in the treatment with benzylpenicillin. It should be borne in mind that the use of benzylpenicillin in subtherapeutic doses or early termination of treatment often leads to the emergence of resistant strains of pathogens. Benzylpenicillin in the form of a powder for injection is included in the Vital and Essential Drugs List.

drug interaction

Probenecid reduces the tubular secretion of benzylpenicillin, resulting in an increase in the concentration of the latter in the blood plasma, and an increase in the half-life. With simultaneous use with antibiotics that have a bacteriostatic effect (tetracycline), the bactericidal effect of benzylpenicillin decreases.

Links

• K.V. Rusanov. Penicillin priority: at the front line. (newspaper "Medicine and Pharmacy News", 2007, No. 11)

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See what "Penicillin" is in other dictionaries:

PENICILLIN, ANTIBIOTIC, formed by fungi of the genus Penicillum (Penicillum). The first of the antibiotics obtained by scientists (discovered by Alexander FLEMING in 1928). Later acquired a soluble form, and today it can be produced ... ... Scientific and technical encyclopedic dictionary

- (Penicillin U) natural penicillin, resistant to those of gastric juice. The spectrum of action is similar to benzylpenicillin (see). Enter orally in tablets of 0.25 0.5 g 4 times a day. High concentrations in the blood are not created, so its ... ... Dictionary of microbiology

PENICILLIN, a, husband. An antibiotic derived from certain molds or synthetically. penicillin injections. | adj. penicillin, oh, oh. Explanatory dictionary of Ozhegov. S.I. Ozhegov, N.Yu. Shvedova. 1949 1992 ... Explanatory dictionary of Ozhegov

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

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

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

What is penicillin?

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

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

What is penicillin for?

Penicillin is able to destroy gram-positive and gram-negative bacteria, anaerobic rods, gonococci and actinomycetes.


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

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

What is penicillin made of?

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

In 1897, the French physician Ernest Duchen was the first to test the effect of mold on guinea pigs and was able to cure them of typhus. The scientist presented the results of his discovery at the Pasteur Institute in Paris, but his research was not approved by medical luminaries.

Who discovered penicillin?

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


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

History of the discovery of penicillin

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

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

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