Ampicillin - instructions for use, dose, side effects, contraindications

Antibacterial bactericidal agent from the group of semisynthetic penicillins, obtained by acetylation of 6-aminopenicillanoic acid with an aminophenylacetic acid residue, is acid-fast. Inhibits the peptidoglycan polymerase and transpeptidase, prevents the formation of peptide bonds and disrupts the late stages of the synthesis of the cell wall of the fissile microorganism, which leads to a decrease in the osmotic stability of the bacterial cell and causes its lysis.

It is active against Gram-positive (alpha and beta-hemolytic streptococci, and Streptococcus pneumoniae, Staphylococcus spp., Bacillus anthracis, Clostridium spp., most enterococci, incl. Enterococcus faecalis) and gram-negative (Haemophilus influenzae, Neisseria meningitidis, Proteus mirabilis, Pasteurella multocida many species Salmonella spp., Shigella spp., Escherichia coli) microorganisms, aerobic non-spore-forming bacteria (Listeria spp.).

Ineffective against penicillinase-producing strains Staphylococcus spp., all strains Pseudomonas aeruginosa, most strains Klebsiella spp. and Enterobacter spp.

Pharmacokinetics:

It is evenly distributed in the organs and tissues of the body, it is found in therapeutic concentrations in pleural, peritoneal, amniotic and synovial fluids, cerebrospinal fluid, contents of blisters, urine (high concentrations), intestinal mucosa, bones, gall bladder, lungs, female genital tract, bile , in a bronchial secretion (in the purulent bronchial secretion, the accumulation is weak), paranasal sinuses, middle ear fluid, saliva, fetal tissues. Poorly penetrates the blood-brain barrier (permeability increases with inflammation of the meninges).

It is excreted mainly by the kidneys (70-80%), and in the urine very high concentrations of the unchanged antibiotic are created; partially with bile, in nursing mothers - with milk. Do not cumulate.Removed during hemodialysis.

Indications:

Bacterial infections caused by sensitive microflora: respiratory tract and ENT organs (sinusitis, tonsillitis, pharyngitis, otitis media, bronchitis, pneumonia, lung abscess), infections of the kidneys and urinary tract (pyelonephritis, pyelitis, cystitis, urethritis), infections of the biliary system cholangitis, cholecystitis), gonorrhea, chlamydial infections in pregnant women (with erythromycin intolerance), cervicitis, skin and soft tissue infections: erysipelas, impetigo, secondarily infected dermatoses; infections of the musculoskeletal system; pasteurellosis, listeriosis, gastrointestinal tract infections (typhoid and paratyphoid, dysentery, salmonellosis, salmonella, peritonitis), endocarditis (prevention and treatment), meningitis, bacterial septicemia.

Contraindications:

Hypersensitivity (including to other penicillins, cephalosporins, carbapenems), infectious mononucleosis, lymphocytic leukemia, liver failure, gastrointestinal diseases in the anamnesis (especially colitis associated with the use of antibiotics), lactation period, children's age (up to 1 month).

Carefully:Bronchial asthma, hay fever, etc.allergic diseases, renal insufficiency, bleeding in the anamnesis, pregnancy.

Dosing and Administration:

Intramuscularly or intravenously (struyno and drip).

Intramuscularly. For infections of moderate-to-moderate course, adults are given intramuscularly 0.25-0.5 g every 6-8 hours; with severe infections - 1-2 g 3-4 times a day. Listeriosis - 50 mg / kg every 6 hours.

With meningitis - 14 g / day; the frequency of administration is 6-8 times.

With gonococcal urethritis - inside 3, 5 g once or intramuscularly 0.5 g 2 times for one day; with gonorrheal uncomplicated urethritis - once 0.5 g.

Children with severe and moderate infections - intramuscularly at 25-50 mg / kg 4 times a day; when meningitis daily dose - 100-200 mg / kg for 6-8 injections.

With a mild infection in children, oral administration in the form of a suspension is preferable.

Solution for intramuscular injection is prepared ex tempore, adding to the contents of the bottle 2 ml of water for injection.

The duration of treatment depends on the severity of the disease (from 5-10 days to 2-3 weeks, and in chronic processes - for several months).

For intravenous fluid administration, a single dose of the drug (not more than 2 g) is dissolved in 5-10 ml of water for injection or isotonic sodium chloride solution and injected slowly for 3-5 minutes(1-2 g for 10-15 minutes).

With a single dose exceeding 2 g of the drug, injected intravenously, drip. For intravenous drip single dose (2-4 g) was dissolved in a small volume of water for injections (7,5-15 ml respectively), then the resulting antibiotic solution is added to 125-250 ml of isotonic sodium chloride solution or a 5-10 % glucose solution and injected at a rate of 60-80 drops per minute. In the case of dropping in, 5-10% glucose solution is used as a solvent for children (30-50 ml depending from the age).

Solutions used immediately after preparation, it is unacceptable to add other medicines to them. The daily dose is divided into 3-4 injections.

Duration of treatment is 5-7 days, with the subsequent transition (if necessary) to intramuscular injection.

Side effects:

Allergic reactions: Possible - flaking skin, pruritus, urticaria, rhinitis, conjunctivitis, angioedema, rarely - fever, arthralgia, eosinophilia, erythematous and maculopapular rash, exfoliative dermatitis, exudative erythema multiforme, Stevens-Johnson syndrome, reactions similar to serum sickness in single cases - anaphylactic shock.

From the digestive system: dysbacteriosis, stomatitis, gastritis, dry mouth, taste change, abdominal pain, vomiting, nausea, diarrhea, glossitis, impaired liver function, moderate increase in the activity of "liver" transaminases, pseudomembranous enterocolitis.

From the central nervous system: agitation or aggressiveness, anxiety, confusion, behavior change, depression, convulsions (with high-dose therapy).

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

Local Reactions: pain at the injection site, infiltrates with intramuscular injection. Other: interstitial nephritis, nephropathy, superinfection (especially in patients with chronic diseases or reduced resistance of the body), candidiasis of the vagina.

Overdose:

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

Treatment: gastric lavage, Activated carbon, salt laxatives, preparations to maintain the water-electrolyte balance and symptomatic.It is excreted by hemodialysis.

Interaction:

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) - synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic. Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives (it is necessary to use additional methods of contraception), drugs that metabolize parahaminobenzoic acid, ethinyl estradiol (in the latter case, the risk of bleeding "breakthrough" increases).

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that block tubular secretion increase the concentration (due to a decrease in tubular secretion).

Allopurinol increases the risk of skin rash.

Reduces clearance and increases the toxicity of methotrexate.

Increases the absorption of digoxin.

Special instructions:

In course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

It is possible to develop superinfection due to the growth of insensitive microflora, which requires a corresponding change in antibacterial therapy.

In the treatment of patients with bacteremia (sepsis), the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

In patients who are hypersensitive to penicillins, there may be cross-allergic reactions with cephalosporin antibiotics.

In the treatment of mild diarrhea against the background of course treatment, antidiarrheal drugs should be avoided, which reduce intestinal peristalsis; it is possible to use kaolin- or attapulgite-containing antidiarrhoeic agents. With severe diarrhea, you should see a doctor.

Treatment should necessarily continue for another 48 - 72 hours after the disappearance of clinical signs of the disease.

If estrogen containing oral contraceptives and amoxicillin are used concomitantly, other or additional methods of contraception should be used whenever possible.

Form release / dosage:

Powder for solution for intravenous and intramuscular injection 0.5 g.

Packaging:

By 0.5 g of active substance into glass bottles, hermetically sealed with rubber stoppers, crimped with aluminum caps or caps with aluminum combined.

1 bottle with instructions for the use of the drug are placed in packs of cardboard.

For 10 vials with instructions for use are placed in bundles with cardboard partitions.

For hospitals. For 1-50 vials with the application of an equal number of instructions for use are placed in boxes with partitions made of cardboard.

Storage conditions:

List B. In a dry, protected from light, out of reach of children, at a temperature of no higher than 20 ° C.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-002726

Date of registration:30.11.2011 / 19.04.2016

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp21.08.2017

Illustrated instructions

Instructions

Ampicillin (Ampicillin)