Ampicillin

General characteristics. Structure:

Active agent: 5 ml ready сусп. contains ampicillin (in the form of trihydrate) 250 mg

Excipients: sodium saccharinate, gum guar, Natrium benzoicum, симетикон S.

Pharmacological properties:

Antibacterial microbicide of a broad spectrum of activity from group of semi-synthetic penicillin, кислотоустойчив. Inhibits a polymerase of a peptidoglikan and transpeptidase, interferes with formation of peptide bonds and breaks late stages of synthesis of a cell wall of the sharing microorganism that leads to decrease in osmotic stability of a bacterial cell and causes its lysis.
It is active concerning gram-positive (alpha and beta and hemolitic streptococci, Streptococcus pneumoniae, Staphylococcus spp., Bacillus anthracis, Clostridium spp., majority of enterococci, including Enterococcus faecalis) and gram-negative microorganisms (Haemophilus influenzae, Neisseria meningitidis, Proteus mirabilis, Pasteurella multocida, Salmonella spp., Shigella spp., Escherichia coli), aerobic asporous bacteria (Listeria spp.).
He is effective concerning penitsillinazoprodutsiruyushchy strains of Staphylococcus spp., all strains of Pseudomonas aeruginosa, majority of strains of Klebsiella spp. and Enterobacter spp.

Pharmacokinetics. Absorption after intake - bystry, high, bioavailability - 40%; time of achievement of Cmax at oral administration of 500 mg - 2 h, Cmax - 3-4 ng/ml. Communication with proteins of plasma - 20%.

It is evenly distributed in bodies and body tissues, it is found in therapeutic concentration in pleural, peritoneal, amniotic and synovial liquids, liquor, contents of blisters, urine (high concentration), a mucous membrane of intestines, bones, a gall bladder, lungs, fabrics of female generative organs, bile, in a bronchial secret (in a purulent bronchial secret accumulation weak), paranasal sinuses, liquid of a middle ear, saliva, fruit fabrics. Badly gets through a blood-brain barrier (permeability increases at an inflammation). It is removed preferential by kidneys (70-80%), and in urine very high concentration of not changed antibiotic are created; partially with bile, at nursing mothers - with milk. Does not kumulirut. Is removed at a hemodialysis.

Indications to use:

The bacterial infections caused by sensitive microflora:
— airways and ENT organs (sinusitis, tonsillitis, pharyngitis, average otitis, bronchitis, pneumonia, lung abscess);
— infections of kidneys and urinary tract (pyelonephritis, pyelitis, cystitis, urethritis);
— infections of biliary system (cholangitis, cholecystitis);
— chlamydial infections at pregnant women (at intolerance of erythromycin);
— cervicitis;
— infections of skin and soft tissues: the ugly face, impetigo for the second time infected a dermatosis;
— musculoskeletal system infections;
— pasteurellosis;
— listeriosis;
— GIT infections (typhoid and paratyphoid, dysentery, salmonellosis, salmonellonositelstvo, peritonitis);
— endocarditis (prevention and treatment);
— meningitis;
— bacterial septicaemia.

Route of administration and doses:

Inside, the adult - on 250 mg of 4 times/days for 0.5-1 h to food with a small amount of water; if necessary the dose is increased to 3 g/days.
Infections of a GIT and bodies of urinogenital system - on 500 mg of 4 times/days.
At a gonococcal urethritis - in 3.5 g once.

Suspension is recommended to be accepted to children with not heavy course of infections: the newborn since 1 month - 150 mg/kg of body weight/; till 1 year - at the rate of 100 mg/kg of mass of body/days; from 1 to 4 years - 100-150 mg/kg of mass of body/days; to children 4 years are more senior appoint 1-2 g/days. The daily dose is divided into 4-6 receptions.

Duration of treatment depends on disease severity (from 5-10 days to 2-3 weeks, and at chronic processes - within several months).

Suspension preparation: to add water to risks to a bottle and it is good to shake up. The prepared suspension is stable at the room temperature within 14 days. Before each use suspension needs to be shaken up. 5 ml of the prepared suspension (1 measured spoon) contain 250 mg of ampicillin.

Features of use:

At course treatment it is necessary to carry out control of a condition of function of bodies of a hemopoiesis, a liver and kidneys.

Development of superinfection due to growth of microflora, insensitive to it, is possible that demands corresponding change of antibacterial therapy.

At treatment of patients with bacteremia (sepsis) development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.

At the patients having hypersensitivity to penicillin cross allergic reactions with others beta лактамными antibiotics are possible.

At treatment of slight diarrhea against the background of course treatment it is necessary to avoid the antidiarrheal drugs reducing an intestines peristaltics; it is possible to use a kaolin - or attapulgitsoderzhashchy antidiarrheal means, drug withdrawal. At heavy diarrhea it is necessary to see a doctor.

Treatment has to continue surely for 48-72 more h after disappearance of clinical signs of a disease.

Side effects:

Allergic reactions: the skin peeling, an itch, a small tortoiseshell, rhinitis, conjunctivitis, a Quincke's edema are possible; seldom - fever, an arthralgia, an eosinophilia, erythematic and makulopapulezny rash, exfoliative dermatitis, a mnogoformny exudative erythema, including Stephens-Johnson's syndrome, reactions similar to a serum disease; in isolated cases - an acute anaphylaxis.

From the alimentary system: dysbacteriosis, stomatitis, gastritis, dryness in a mouth, taste change, an abdominal pain, vomiting, nausea, diarrhea, stomatitis, a glossitis, an abnormal liver function, moderate increase in level of hepatic transaminases, a pseudomembranous coloenteritis.

From TsNS: agitation or aggression, uneasiness, confusion of consciousness, change of behavior, a depression, spasms (at therapy by high doses).

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

Others: intersticial nephrite, a nephropathy, superinfection (especially at patients with chronic diseases or reduced resistance of an organism), vagina candidiasis.

Interaction with other medicines:

Antacids, glycosamine, purgatives, food slow down and reduce absorption; ascorbic acid increases absorption.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) – sinergidny action; bacteriostatic drugs (macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) antagonistic.

Increases efficiency of indirect anticoagulants (suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio); reduces efficiency of estrogensoderzhashchy oral contraceptives (it is necessary to use additional methods of contraception), medicines in the course of which metabolism para-aminobenzoic acid is formed, ethinylestradiol (in the latter case the risk of development of bleedings of break increases).

Diuretics, Allopyrinolum, оксифенбутазон, the phenylbutazone, NPVS, drugs blocking canalicular secretion increase concentration of ampicillin in plasma (due to decrease in canalicular secretion).

Allopyrinolum increases risk of development of skin rash.

Reduces clearance and increases toxicity of a methotrexate.

Strengthens digoxin absorption.

Contraindications:

— infectious mononucleosis;
— lymphoid leukosis;
— liver failure;
— gastrointestinal diseases in the anamnesis (especially the colitis connected using antibiotics);
— lactation period;
— children's age (up to 1 month);
— hypersensitivity (including to other penicillin, cephalosporins, karbapenema).

With care: bronchial asthma, hay fever, allergic diseases, a renal failure, bleedings in the anamnesis, pregnancy.

Use of the drug AMPICILLIN at pregnancy and feeding by a breast
With care use drug at pregnancy. It is contraindicated in the period of a lactation.

Use at abnormal liver functions
It is contraindicated:
— liver failure.

Use at renal failures
With care at a renal failure.

Use for children
Suspension is recommended to be accepted to children with not heavy course of infections: the newborn since 1 month - 150 mg/kg of mass of body/days; till 1 year - at the rate of 100 mg/kg of mass of body/days; from 1 to 4 years - 100-150 mg/kg of mass of body/days; to children 4 years are more senior appoint 1-2 g/days. The daily dose is divided into 4-6 receptions.

Overdose:

Symptoms: manifestations of toxic action on TsNS (especially at patients with a renal failure); nausea, vomiting, diarrhea, disturbance of water and electrolytic balance (as a result of vomiting and diarrhea).

Treatment: a gastric lavage, absorbent carbon, salt laxatives, drugs for maintenance of water and electrolytic balance and symptomatic. It is removed by means of a hemodialysis.

Storage conditions:

List B. To store in the unavailable to children, dry, protected from light place at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Granules for пригот. сусп. for intake of 250 mg / 5 ml: фл. 100 ml.