Pharmacological action

Antibiotic of a group of semisynthetic penicillins of a broad spectrum of action. It has a bactericidal effect by suppressing the synthesis of the bacterial cell wall.

Active against gram-positive aerobic bacteria: Staphylococcus spp. (except for strains producing penicillinase), Streptococcus spp. (including Enterococcus spp.), Listeria monocytogenes; gram-negative aerobic bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Bordetella pertussis, some strains of Haemophilus influenzae.

It is destroyed by the action of penicillinase. Acid resistant.

Pharmacokinetics

Absorption

After oral administration, it is well absorbed from the gastrointestinal tract without being destroyed in the acidic environment of the stomach. After parenteral administration (i / m and i / v), it is found in blood plasma in high concentrations.

Distribution

Penetrates well into tissues and body fluids, is found in therapeutic concentrations in pleural, peritoneal and synovial fluids. Penetrates the placental barrier. Poorly penetrates the blood-brain barrier, however, with inflammation of the meninges of the brain, the BBB permeability increases sharply.

Metabolism

30% of ampicillin is metabolized in the liver.

Excretion

T1/2 - 1-1.5 hours. It is excreted mainly in the urine, and very high concentrations of the unchanged drug are created in the urine. Partially excreted in the bile.

With repeated administrations, it does not cumulate.

Indications of the drug AmpicillinInfectious and inflammatory diseases caused by microorganisms sensitive to ampicillin, including:

• respiratory tract infections (including bronchitis, pneumonia, lung abscess);
• ENT infections (including tonsillitis);
• infections of the biliary tract (including cholecystitis, cholangitis);
• urinary tract infections (including pyelitis, pyelonephritis, cystitis);
• gastrointestinal tract infections (including salmonella);
• gynecological infections;
• infections of the skin and soft tissues;
• peritonitis;
• sepsis, septic endocarditis;
• meningitis;
• rheumatism;
• erysipelas;
• scarlet fever;
• gonorrhea.

Dosage regimen

Set individually depending on the severity of the course, localization of the infection and the sensitivity of the pathogen.

When taken orally, a single dose for adults is 250-500 mg, the daily dose is 1-3 g. The maximum daily dose is 4 g.

For children, the drug is prescribed in a daily dose of 50-100 mg / kg, for children weighing up to 20 kg - 12.5-25 mg / kg.

The daily dose is divided into 4 doses. The duration of treatment depends on the severity of the infection and the effectiveness of treatment.

The tablets are taken orally, regardless of the meal.

To prepare the suspension, 62 ml of distilled water is added to the vial with the powder. The finished suspension is dispensed with a special spoon having 2 marks: the lower one corresponds to 2.5 ml (125 mg), the upper one - 5 ml (250 mg). The suspension should be taken with water.

For parenteral administration (i / m, i / v stream or i /drip), a single dose for adults vis 250-500 mg, a daily dose is 1-3 g; in severe infections, the daily dose may be increased to 10 g or more.

For newborns, the drug is prescribed in a daily dose of 100 mg / kg, for children of other age groups - 50 mg / kg. In severe cases of infection, these doses can be doubled.

The daily dose is divided into 4-6 injections with an interval of 4-6 hours. The duration of the intramuscular injection is 7-14 days. Duration of intravenous administration is 5-7 days, followed by the transition (if necessary) to intramuscular injection.

A solution for i / m administration is prepared by adding 2 ml of water for injection to the contents of the vial.

For intravenous jet injection, a single dose of the drug (no more than 2 g) is dissolved in 5-10 ml of water for injection or isotonic sodium chloride solution and injected slowly over 3-5 minutes (1-2 g for 10-15 minutes) ... With a single dose exceeding 2 g, the drug is injected intravenously. To do this, a single dose of the drug (2-4 g) is dissolved in 7.5-15 ml of water for injection, then the resulting solution is added to 125-250 ml of isotonic sodium chloride solution or 5-10% glucose solution and injected at a rate of 60-80 drops. / min. For intravenous drip administration to children, a 5-10% glucose solution is used as a solvent (30-50 ml, depending on age).

The solutions are used immediately after preparation.

Contraindications for use

hypersensitivity to antibiotics from the penicillin group and other beta-lactam antibiotics;

severe liver dysfunction (for parenteral use).

Application during pregnancy and lactation

It is possible to use the drug during pregnancy according to indications in cases where the benefit to the mother outweighs the potential risk to the fetus.

Ampicillin is excreted in breast milk in low concentrations. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.

Application for violations of liver function

Parenteral use is contraindicated in severe violations of liver function.

Application for impaired renal function

Patients with impaired renal function require correction of the dosage regimen depending on the CC.

When using the drug in high doses in patients with renal insufficiency, a toxic effect on the central nervous system is possible.

Application in children

When administered to children, the drug is prescribed in a daily dose of 50-100 mg / kg, for children weighing up to 20 kg - 12.5-25 mg / kg. For parenteralinfants, the drug is prescribed in a daily dose of 100 mg / kg, for children of other age groups - 50 mg / kg. In a severe course of infection, the indicated doses can be doubled.

Special instructions

With caution and against the background of the simultaneous use of desensitizing agents, the drug should be prescribed for bronchial asthma, hay fever and other allergic diseases.

In the process of using Ampicillin-AKOS, systematic monitoring of the function of the kidneys, liver and the picture of peripheral blood is necessary.

In liver failure, the drug should be used only under the control of liver function.

Patients with impaired renal function require correction of the dosage regimen depending on CC.

When using the drug in high doses in patients with renal insufficiency, a toxic effect on the central nervous system is possible.

When using the drug for the treatment of sepsis, a bacteriolysis reaction is possible (Jarisch-Herxheimer reaction).

If allergic reactions occur while using Ampicillin-AKOS, the drug should be canceled and desensitizing therapy should be prescribed.

In debilitated patients, with prolonged use of the drug, superinfection may develop, caused by microorganisms resistant to ampicillin.

To prevent the development of candidiasis, nystatin or levorin, as well as B and C vitamins, should be prescribed simultaneously with Ampicillin-AKOS.

Overdose

Currently, no cases of overdose of Ampicillin-AKOS have been reported.

Drug interaction

Probenecid, when used simultaneously with Ampicillin-AKOS, reduces tubular secretion of ampicillin, as a result of which its concentration in blood plasma increases and the risk of toxic effects increases.

With the simultaneous use of Ampicillin-AKOS with allopurinol, the likelihood of a skin rash increases.

With simultaneous use with Ampicillin-AKOS, the effectiveness of estrogen-containing oral contraceptives decreases.

With simultaneous use with Ampicillin-AKOS, the effectiveness of anticoagulants and antibiotics-aminoglycosides increases.

Storage conditions of the drug Ampicillin

List B. The drug should be stored in a dry, dark place; tablets and powder for preparation of suspension - at a temperature of 15 ° to 25 ° C, powder for preparation of solution for injections - at a temperature not exceeding 20 ° C.

Shelf life of the drug Ampicillin

Shelf life of tablets, powder for suspension and powder for preparation of solution for injection - 2 years.

The prepared suspension should be stored in a refrigerator or at room temperature for no more than 8 days. The prepared solutions for intramuscular and intravenous administration are not subject to storage.

Side effects

Allergic reactions: possible - itching and peeling of the skin, urticaria, rhinitis, conjunctivitis, angioedema, rarely - fever, arthralgia, eosinophilia, erythematous and maculopapular rash, exfoliative dermatuditis, t. ), reactions similar to serum sickness, in isolated cases - anaphylactic shock, non-allergic ampicillin rash, may disappear without discontinuation of the drug. From the digestive system: dysbiosis, stomatitis, gastritis, dry mouth, change in taste, abdominal pain, vomiting, nausea, diarrhea, stomatitis, glossitis, moderate increase in the activity of "hepatic" transaminases, pseudomembranous enterocolitis.

From the side of the central nervous system: headache, tremor, convulsions (with high-dose therapy).

Laboratory indicators: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, anemia.

Local reactions: pain at the injection site, infiltrates with intramuscular injection, phlebitis with intravenous administration in large doses.

Others: interstitial nephritis, nephropathy, superinfection (especially in patients with chronic diseases or reduced body resistance), vaginal candidiasis.

Overdose. Symptoms: manifestations of toxic effects on the central nervous system (especially in patients with renal failure); nausea, vomiting, diarrhea, imbalance in water and electrolyte balance (as a result of vomiting and diarrhea).

Treatment: gastric lavage, activated charcoal, saline laxatives, drugs to maintain water and electrolyte balance and symptomatic. It is excreted using hemodialysis.