Ampitsillin-Zdorovye tab. of 250 mg No. 24

General characteristics. Structure:

International and chemical names: ampicillin; (2S,5R,6R)-6-[(2R)-2-amino-2-fenilatsetil] amine] - 3,3-dimethyl-7-oxo-4-thia-1-azabitsiklo [3.2.0] - heptane-2-carboxylic acid; main physical and chemical properties: tablets of color, white or white with a yellowish shade, with a flat surface, risky and a facet; structure: 1 tablet contains Ampicillini trihdras in terms of 100% ampicillin – 250 mg; excipients: potato starch, talc, calcium stearate or magnesium stearate.

Pharmacological properties:

Antibiotic of group of semi-synthetic penicillin of the third generation with a broad spectrum of activity.
Pharmacodynamics. Has bactericidal effect due to suppression of synthesis of a cell wall of bacteria; it is active concerning proliferating bacteria. The bactericidal effect is caused by ability of ampicillin to connect and inactivate the penitsillinsvyazyvayushchy proteins located on an inner membrane of a cell wall of bacteria. Late stages of synthesis of a cell wall of the sharing microorganism are as a result broken, osmotic stability of a bacterial cell decreases that leads to her death (lysis).
Possesses a broad spectrum of activity. It is active concerning gram-positive ά-and β-hemolitic streptococci, Streptococcus pneumoniae, Staphylococcus spp., Bacillus anthracis, Clostridium spp., it is moderately active against the majority of enterococci, including Enterococcus faecalis), Listeria spp., and gram-negative (Haemophilus influenzae, Neisseria meningitidis, Proteus mirabilis, Yersinia multocida, many types of Salmonella spp., Shigella spp., Escherichia coli, microorganisms, aerobic asporous bacteria.
It is inefficient concerning penitsillinazoprodutsiruyushchy strains of Staphylococcus spp., all strains of Pseudomonas aeruginosa, majority of strains of Klebsiella spp. and Enterobacter spp.

Pharmacokinetics. At intake it is quickly soaked up from digestive tract, without collapsing in acid medium of a stomach. Absorption of ampicillin decreases at a concomitant use with food. Bioavailability makes 40%. The maximum concentration in a blood plasma at reception of 500 mg (2 tablets) is reached in 2 hours, making 3–4 mkg/ml, and slowly decreases during 6 h. Contacts proteins of plasma for 10–30%.
Well gets into fabrics and biological liquids of an organism, 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, bile, lungs, fabrics of female generative organs, in a bronchial secret (in a purulent bronchial secret accumulation weak), paranasal sinuses, liquid of a middle ear (at its inflammation), saliva, fruit fabrics. Badly gets through a blood-brain barrier, permeability increases at an inflammation of a meninx.
Practically is not exposed to biotransformation – in a liver 10–30% of the accepted dose are metabolized. Elimination half-life 1–1,5 hour. It is removed preferential by kidneys
(70–80%), and in urine very high concentration of not changed drug are created; it is partially removed with bile (20%). It can be allocated with breast milk (in low concentration).
In an organism does not kumulirut. Is removed at a hemodialysis.

Indications to use:

The infections caused by microorganisms, sensitive to ampicillin: airways and ENT organs (sinusitis, tonsillitis, pharyngitis, average otitis, bronchitis, pneumonia, lung abscess), an infection of kidneys and urinary tract (pyelonephritis, a pyelitis, cystitis, an urethritis), gonorrhea, infections of biliary system (a cholangitis, cholecystitis), chlamydial infections at pregnant women (at intolerance to erythromycin), a cervicitis, infections of skin and soft tissues: the ugly face, impetigo for the second time infected a dermatosis; musculoskeletal system infections; digestive tract infections (typhoid and paratyphoid, dysentery, salmonellosis, salmonellezny carriage), abdominal infections (peritonitis), endocarditis (prevention and treatment), meningitis, sepsis.

Route of administration and doses:

Appoint inside, without chewing, washing down with water. The daily dose is established individually depending on disease severity, by localizations of an infection and sensitivity of the activator. The daily dose is divided into 4–6 receptions.
For adults and children 14 years a single dose are more senior makes 250–500 mg (1–2 tablets), daily – 1–3 g (4–12 tablets). The maximum daily dose – 3 g (12 tablets). At heavy infections appoint up to 6 g/days (24 tablets).
At a gonorrheal uncomplicated urethritis, cystitis and pyelonephritis appoint on 500 mg (2 tablets), at respiratory infections – on 250 mg (1 tablet), at infections of a digestive tract – on 500–750 mg (2–3 tablets), at a typhoid and a carriage of bacilli – on 1–1,5 g (4–6 tablets) every the 6th hour.
At a gonococcal urethritis appoint once 3,5 g of ampicillin (14 tablets) in combination with 1 g of a probenetsid.
To children 3 years usually are more senior appoint 30–50 mg/kg of body weight in a daily dose that makes 125–250 mg 4 times a day. The maximum daily dose – 2 g.
Duration of treatment depends on disease severity (from 5–10 days to 2–3 weeks, at chronic processes – within several months). Treatment has to continue surely for 2-3 more days after disappearance of clinical signs of a disease.

Features of use:

At course treatment it is necessary to carry out control of a condition of function of kidneys, a liver (especially at a liver failure), pictures of peripheral blood. Patients with a renal failure, and also the elderly patient need correction of the mode of dosing according to values of clearance of creatinine. Use of high doses of drug for patients with a renal failure can lead to toxic action on the central nervous system. With a liver failure of dose adjustment it is not required from patients.
Restrictions to a medical use of drug are bronchial asthma, a pollinosis and other allergic diseases, in need of ampicillin use at the same time appoint the desensibilizing drugs. At emergence of allergic reactions drug is cancelled and carry out the desensibilizing therapy. In a case emergence of signs of an acute anaphylaxis urgent measures are necessary for the patient's conclusion from this state.
At the weakened patients at prolonged treatment development of superinfection due to growth insensitive to it microflorae (candidiasis) is possible; to such patients co-administration of vitamins of group B and vitamin C, if necessary – nystatin or levorinum is reasonable. Corresponding change of antibacterial therapy can be required.
At appointment as the patient with sepsis development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible. At the patients having hypersensitivity to penicillin cross allergic reactions with other β-laktamny antibiotics are possible. At treatment of slight diarrhea against the background of course treatment it is necessary to avoid the antidiarrheal medicines reducing an intestines peristaltics; it is possible to use a kaolin or attapulgitsoderzhashchy antidiarrheal drugs, drug withdrawal is shown. At heavy diarrhea appoint inside antibiotics (metronidazole or Vancomycinum). It is impossible to apply loperamide. Use at pregnancy is possible only in that case when the expected therapeutic effect exceeds potential risk for a fruit. For the period of treatment it is necessary to stop feeding by a breast.

Data on influence of drug on ability to control of vehicles and on performance of potentially dangerous types of activity are absent.

Side effects:

Allergic reactions: skin rash, small tortoiseshell, Quincke's edema, itch, exfoliative dermatitis, multiformny exudative erythema (including Stephens-Johnson's syndrome); seldom – an acute anaphylaxis. From the alimentary system: vomiting, nausea, diarrhea, a glossitis, stomatitis, pseudomembranous colitis (both during treatment, and several weeks later after its termination), intestinal dysbacteriosis, gastritis, dryness in a mouth, taste change, an abdominal pain. From system of a hemopoiesis: anemia, leukopenia, thrombocytopenia, agranulocytosis. From secretory system: seldom – intersticial nephrite. From a nervous system and sense bodys: headache, tremor, rhinitis, conjunctivitis. Laboratory indicators: moderate increase in activity of "hepatic" transaminases, lactate dehydrogenases, alkaline phosphatase, creatinine, false positive result of the glyukozurichesky test, false positive reaction of Koombs. Other: oral cavity candidiasis, vaginal candidiasis (the superinfection caused by resistant strains).

Interaction with other medicines:

Antacids, glycosamine, laxative medicines, aminoglycosides and food slow down and reduce ampicillin absorption; ascorbic acid increases its absorption. Ampicillin increases efficiency of anticoagulants and antibiotics of an aminoglikozidny row; reduces efficiency of estrogensoderzhashchy oral contraceptives (it is necessary to use additional methods of contraception). Probenetsid and other medicines reducing canalicular secretion increase concentration of ampicillin in plasma. Simultaneous use with Allopyrinolum considerably increases risk of development of skin rash. Reduces clearance and increases toxicity of a methotrexate. Strengthens digoxin absorption. In high doses reduces the level of an atenolol in blood therefore it is recommended to accept these drugs separately, and атенолол to accept before ampicillin use.

Contraindications:

Hypersensitivity to antibiotics of group of penicillin and other β-laktamny antibiotics (cephalosporins, karbapenema), an infectious mononucleosis, a lymphoid leukosis, a heavy liver failure, the feeding period a breast (for the period of treatment to interrupt), children's age up to 3 years.

Overdose:

Symptoms: signs 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, purpose of absorbent carbon, salt laxatives, medicines for maintenance of water and electrolytic balance and symptomatic. At patients with a renal failure peritoneal dialysis is not effective, is removed by means of a hemodialysis.

Storage conditions:

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

Period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

On 24 tablets in a blister strip packaging and in a pack.