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

Semisynthetic penicillin, a broad spectrum of action, has a bactericidal effect. Suppresses the synthesis of the bacterial cell wall. Acid-resistant. It is active against Gram-positive (alpha and beta-hemolytic streptococci, Streptococcus pneumoniae, Staphylococcus spp., Bacillus anthracis, Clostridium spp., moderately active against the majority of enterococci, incl. Enterococcus faecalis), Listeria spp., 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.

Not effective against penicillinase-producing strains Staphylococcus spp., all strains Pseudomonas aeruginosa, most strains Klebsiella spp. and Enterobacter spp.

Pharmacokinetics:

With intramuscular injection, the concentration in the blood exceeds that produced when ingested.

Evenly distributed in organs and tissues of the body, found at therapeutic concentrations in the pleural, peritoneal, amniotic and synovial fluids, cerebrospinal fluid, the contents of the blisters, the urine (high concentration), intestinal mucosa, bones, gall bladder, lung, tissues of female sex organs, bile in bronchial secretions (in suppurative bronchial secretions accumulation weak), paranasal sinuses, middle ear fluid, saliva, fetal tissues. Poorly penetrates the blood-brain barrier (permeability increases during inflammation of the meninges).

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

Indications:

Bacterial infections caused by susceptible pathogens: respiratory infections and ENT (sinusitis, tonsillitis, pharyngitis, otitis media, bronchitis, pneumonia, lung abscess), kidney and urinary tract infection (pyelonephritis, pyelitis, cystitis, urethritis)gonorrhea, infections of the biliary system (cholangitis, cholecystitis), 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; infectious diseases of the gastrointestinal tract (typhoid and paratyphoid, dysentery, salmonellosis, salmonella carcinoma), abdominal infections (peritonitis); endocarditis (prevention and treatment), meningitis, sepsis.

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 and other allergic diseases, renal failure, bleeding history, pregnancy.

Dosing and Administration:

The drug is administered intramuscularly.

For infections of moderate-to-moderate course, adults are injected with 0.25-0.5 g every 6-8 hours; at a serious current of 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 - 0.5 g 2 times for one day; with gonorrhea uncomplicated urethritis - once 0.5 g.

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

Children over 4 years of age are prescribed 1-2 g / day; up to 1 year - at the rate of 100 mg / kg; 1-4 years - 100-150 mg / kg; Newborns from 1 month - 150 mg / kg. The daily dose is divided into 4-6 receptions.

Solution for intramuscular injection is prepared extepore, adding to the contents of the vial (0.25 or 0.5 g) 2 ml of water for injection.

The duration of treatment depends on the severity of the disease (7-14 days or more).

Side effects:

Allergic reactions: possible - skin peeling, itching, hives, rhinitis, conjunctivitis, Quincke's edema, rarely - fever, arthralgia, eosinophilia, erythematous and maculopapular rash, exfoliative dermatitis, multiforme exudative erythema, malignant exudative erythema (Stevens-Johnson syndrome), reactions similar to serum sickness, in single cases - anaphylactic shock, non-allergic ampicillin rash, may disappear without discontinuing the drug.

From the gastrointestinal tract: dysbacteriosis, stomatitis, gastritis, dry mouth, taste change, abdominal pain, vomiting, nausea, diarrhea, stomatitis, glossitis, moderate increase in the level of "liver" transaminases, pseudomembranous enterocolitis.

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

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

Local reactions: pain in the injection site, infiltrates.

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, violation 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:

Antacids, glucosamine, laxatives, food and aminoglycosides slow down and reduce absorption; ascorbic acid increases absorption.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) have a synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.

Ampicillin, when combined, 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, in the process of metabolism of which is formed PABC, ethinyl estradiol (in the latter case, the risk of bleeding "breakthrough" increases).

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs, drugs that block tubular secretion increase the concentration of ampicillin (due to lower tubular secretion).

Allopurinol, when combined with ampicillin, increases the risk of skin rash.

Ampicillin reduces clearance and increases the toxicity of methotrexate.

Increases the absorption of digoxin.

Special instructions:

At 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.

With the appointment of patients with sepsis, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

In patients who have increased sensitivity to penicillins, there may be cross-allergic reactions with other beta-lactam antibiotics.

In the treatment of mild diarrhea against the background of course treatment, antidiarrheal drugs should be avoided, which reduce intestinal peristalsis; You can use kaolin- or attapulgite-containing antidiarrhoeic drugs, drug cancellation. 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.

Form release / dosage:Powder for solution for intramuscular injection 0.25 g, 0.5 g.

Packaging:

0.25 g, 0.5 g of active substance in 10 ml vials.

1 bottle with instructions for use in a pack of cardboard.

10 bottles with instructions for use in a cardboard box.

For hospital:

- 50 bottles and 1-5 instructions for use in a cardboard box;

- 1 bottle with instructions for use (from 1 to 50 bottles with an equal number of instructions for use) in a cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

After the expiry date of the drug, unused vials should be carefully opened, the contents dissolved in a large amount of water and drained into the drain.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N003497 / 01

Date of registration:09.06.2009 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp21.08.2017

Illustrated instructions

Instructions

Ampicillin (Ampicillin)