Ampicillin

General characteristics. Structure:

Active ingredient: 250 mg of Ampicillini trihdras in terms of ampicillin.

Excipients: potato starch, talc, calcium stearate.

Antibacterial microbicide of a broad spectrum of activity from group of semi-synthetic penicillin.

Pharmacological properties:

Pharmacodynamics. The antibacterial microbicide of a broad spectrum of activity from group of semi-synthetic penicillin received by acetylation of 6-aminopenicillanic acid by the rest of aminophenylacetic acid, 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 cage 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 (Haemophilus influenzae, Neisseria meningitides, Proteus mirabilis, Pasteurella multocida many types of Salmonella spp., Shigella spp., Escherichia coli) microorganisms, 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 of 40%; time of achievement of the maximum concentration at oral administration of 500 mg of 2 h, the maximum concentration of 3-4 ng/ml. Communication with proteins of plasma of 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 gemato-intsefalichesky 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), infection of kidneys and urinary tract: (pyelonephritis, a pyelitis, cystitis, an urethritis), infections of biliary system (a cholangitis, cholecystitis), gonorrhea, chlamydial infections at pregnant women (at intolerance of erythromycin), a cervicitis, infections of skin and soft tissues: the ugly face, impetigo for the second time infected a dermatosis; musculoskeletal system infections; pasteurellosis, listeriosis, digestive tract infections (typhoid and paratyphoid, dysentery, salmonellosis, salmonellonositelstvo, peritonitis), endocarditis (prevention and treatment), meningitis, bacterial septicaemia.

Route of administration and doses:

Inside, the adult on 0,25 g 4 times a day 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 digestive tract and bodies of urinogenital system: 0,5 g 4 times a day.

At a gonococcal urethritis in 3,5 g once.

At not heavy course of infections at children reception in the form of suspension is more preferable. To children 4 years are more senior appoint 1-2 g a day. 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).

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 tsefalosporinovy 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.

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

At simultaneous use of estrogensoderzhashchy oral contraceptives and amoxicillin, it is necessary to use whenever possible other or additional methods of contraception.

Side effects:

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

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 the central nervous system: 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 Paro-amino-benzoic acid is formed, ethinylestradiol (in the latter case the risk of development of bleedings of "break" increases).

Diuretics, Allopyrinolum, оксифенбутазон, phenylbutazone, non-steroidal anti-inflammatory drugs; the drugs blocking canalicular secretion increase concentration (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:

Hypersensitivity (including to other penicillin, cephalosporins, karbapenema), an infectious mononucleosis, a lymphoid leukosis, a liver failure, digestive tract diseases in the anamnesis (especially the colitis connected using antibiotics), the lactation period, children's age (up to 4 years).

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

Overdose:

Symptoms: manifestations of toxic action on the central nervous system (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 place, dry, unavailable to children, at a temperature not above 25 °C. A period of validity - 2 years. Not to apply after expiry date.

Issue conditions:

According to the recipe

Packaging:

Tablets on 0,25 g. On 10 tablets in planimetric bezyacheykovy packaging; on 10, 20, 30 tablets in a blister strip packaging; on 20, 30 tablets in banks from glass melt or in glass jars, or banks polymeric. Each can or 1, 2, 3, 10 planimetric packagings together with the application instruction in a pack.