Ampitsillin-KMP

General characteristics. Structure:

Active ingredient: ampicillin;
1 bottle contains ampicillin of sodium salt sterile, in terms of ampicillin
0,5 g or 1,0 g.

Pharmacological properties:

Pharmacodynamics. Ampicillin possesses a wide range of antibacterial (bactericidal) action. It is active concerning gram-positive microorganisms (Staphylococcus spp., except for the strains producing a penicillinase; Streptococcus spp., including S. pneumoniae; Corynebacterium diphtheriae, Bacillus anthracis, Clostridium spp., majority of enterococci) and gram-negative (Escherichia coli, Shigella spp., Salmonella spp., Neisseria meningitidis, N. gonorrhoeae, Proteus mirabilis, some strains of Klebsiella pneumoniae, Haemophilus influenzae) microorganisms. Drug collapses a penicillinase and therefore does not affect penitsillinazoobrazuyushchy strains of bacteria. Drug 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 microorganisms.
The arising defects of a cover reduce osmotic stability of a bacterial cell that leads of it to death (lysis).

Pharmacokinetics. At intramuscular or intravenous administration circulates in high concentration in blood. The maximum concentration in blood is found in 15 minutes at intravenous administration and in 0,5-1,0 hour – after intramuscular. At intramuscular introduction of 0,5-1 g of ampicillin with an interval between introductions of 4-6 hours of blood therapeutic concentration is maintained. Well gets into fabrics and liquids of an organism, it is found in therapeutic concentration in pleural, peritoneal and synovial fluid. In bile it can be found in concentration 4-100 times higher, than in blood. Rather small part (10-30%) contacts proteins of plasma. Through a blood-brain barrier does not get. Almost is not exposed to biotransformation. It is allocated generally with kidneys, partially – with bile, at the women nursing it is excreted in milk. Within 12 hours with urine 45-70% of the entered dose are excreted. At disturbance of secretory function of kidneys drug level in blood increases and its removal is slowed down. At clearance of creatinine less than 10 ml/min. antibiotic level in blood can be 10 times higher, than at patients with normal function of kidneys. The elimination half-life increases from 1-2 o'clock normal till 10-12 o'clock. Ampicillin at repeated introductions does not kumulirut that gives the chance to apply it in high doses and is long.
Pharmaceutical characteristics.
Main physical and chemical properties: powder of white color, is hygroscopic. Incompatibility. It is inadmissible to mix ampicillin in one capacity with other medicamentous means. Drug pharmaceutical is incompatible with tetracycline, chloramphenicol (levomycetinum), Amphotericinum, clindamycin, erythromycin, lincomycin, metronidazole, polymyxin B, Acetylcysteinum,
Chlorpromazinum, gidralaziny, dopamine, heparin, Metoclopramidum.

Indications to use:

The infections caused by microorganisms, sensitive to drug: infections of biliary system (cholangitis, cholecystitis); respiratory infections (pneumonia, bronchitis, abscess of lungs); meningitis; the gastroenteritis caused by shigellas or salmonellas, a typhoid and a paratyphoid; bacterial endocarditis; infections of urinogenital system (pyelitis, pyelonephritis, cystitis, urethritis); septicaemia; infections of skin and soft tissues.

Route of administration and doses:

Before use it is necessary to take skin samples on portability. Drug is accepted on doctor's orders. Ampicillin is entered intramusculary or intravenously (struyno or kapelno). Treatment duration is established by Ampicillin individually (7-14 days and more), depending on the course of a disease, age of the patient, efficiency of therapy and a condition of function of kidneys. After disappearance of clinical signs of a disease it is necessary to accept Ampicillin 2-3 more days. The recommended single standard dose for adults and children is more senior than 14 years makes 0,25-0,5 g each 4-6 hours. The mode of dosing is set by the doctor. At heavy infections it is possible to increase a daily dose to 10 g and more. The newborn drug appoint in a daily dose 100 mg/kg, to children of other age groups – 50 mg/kg. At the heavy course of an infection the specified doses can be doubled. The daily dose is entered in
4-6 receptions with an interval between receptions of 4-6 hours. Intravenous administration. Solution for intravenous jet administration is prepared by ex tepore, the single dose of drug (no more than 2 g) is dissolved in 5-10 ml of sterile water for injections or 0,9% of solution of sodium of chloride and enter slowly within 3-5 minutes. At the single dose exceeding 2 g, the drug is administered intravenously kapelno. The adult for intravenous drop administration the single dose of drug (2-4 g) is dissolved in the small volume of water for injections (respectively in 7,5-15 ml), then the received solution of an antibiotic add 0,9% of solution of sodium of chloride or 5% of solution of glucose to 125-250 ml and entered with a speed of 60-80 thaws a minute. At drop introduction to children as solvent use 5-10% glucose solution (30-50 ml depending on age). Solutions enter right after preparation. The daily dose is distributed on 3-4 introductions. Duration of treatment makes 5-7 days with the subsequent (if necessary) transition to intramuscular introduction. Intramuscular introduction. Solution for intramuscular introduction is prepared by ex tempore, adding to bottle contents 2 ml (0,5 g) or 4 ml (1,0 g) of sterile water for injections.
Correction of the mode of dosing is necessary for patients with a heavy renal failure (clearance of creatinine less than 10 ml/min.): it is necessary to reduce a dose of drug or to increase an interval between introductions.

Features of use:

Before therapy it is necessary to exclude existence at the patient of hypersensitivity to ampicillin and other β-laktamny antibiotics. In the course of treatment systematic control of function of kidneys, a liver and a picture of peripheral blood is necessary. At bronchial asthma, hay fever and others
allergic diseases drug is used along with the desensibilizing means.
At use of high doses for patients with a renal failure perhaps toxic action on TsNS. Prolonged or repeated use can lead to rapid growth of resistant microflora, development of the superinfection caused by resistant microorganisms. Ability to influence speed of response at control of motor transport or work with other mechanisms. During treatment by drug at some patients emergence of side reactions from the central nervous system is possible (see the section "Side reactions") therefore it is necessary to be careful at control of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Allergic reactions: rash, an itch, a hyperemia, urticaria, rhinitis, conjunctivitis, it is rare – fever, a joint pain, an eosinophilia, exfoliative dermatitis, a purpura, a multiformny exudative erythema, Stephens-Johnson's syndrome, is very rare – a Quincke's edema, an acute anaphylaxis.
From a digestive tract: nausea, vomiting, diarrhea, taste changes, an abdominal pain, stomatitis, a glossitis, dryness in a mouth, intestinal dysbacteriosis, gastritis, a coloenteritis, hemorrhagic colitis. In the course of treatment or within several weeks after the end of antibiotic treatment there is a probability of development of pseudomembranous colitis.
From a liver and gepatobiliarny system: hepatitis, cholestatic jaundice.
From the central and peripheral nervous system: at use of high doses for patients with a renal failure – dizziness, a headache, a tremor, spasms, neuropathy.
Local reactions: hypostasis, an itch, a hyperemia in an injection site.
Laboratory indicators: moderate increase in activity of "hepatic" transaminases, lactate dehydrogenases, alkaline phosphatase, creatinine, lozhnopolozhitelena results of non-enzymatic glyukozurichesky tests and Koombs's reaction.
Others: reversible disturbances of a hemogenesis (leukopenia, thrombocytopenia, hemolitic anemia, agranulocytosis), intersticial nephrite, superinfection, candidiasis. At use of Ampicillin for patients with bacteremia (sepsis) reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.

Interaction with other medicines:

Ampicillin increases effect of anticoagulants, antibiotics of an aminoglikozidny row, reduces effect of oral contraceptives. At simultaneous use of Ampicillin with peroral estrogensoderzhashchy drugs decrease in their efficiency due to easing hepatic is noted
circulation of estrogen. Probenetsid reduces canalicular secretion of Ampicillin therefore the risk of development of its toxic action increases. The probability of emergence of skin rash raises Allopyrinolum. High doses of Ampicillin reduce the level of an atenolol in a blood plasma therefore
it is recommended to use these drugs separately, at first to accept атенолол, and after it - Ampitsillin. Ampicillin reduces clearance and increases toxicity of a methotrexate, strengthens
digoxin absorption.
At interaction of ampicillin with macroleads, paromomitsiny, tetracyclines, chloramphenicol the effect of both drugs decreases. Ampicillin can reduce effect of Natrium benzoicum.
At simultaneous use with blockers of β-adrenoceptors the probability of emergence of anaphylactic reactions increases.

Contraindications:

Hypersensitivity to ampicillin and to other β-laktamny antibiotics (penicillin, cephalosporins, karbapenema); heavy abnormal liver functions and kidneys; infectious mononucleosis; leukemia; HIV - infections; diseases of a gastrointestinal path / colitis, connected using antibiotics; feeding period breast.

Use during pregnancy or feeding by a breast. The teratogenic effect of Ampicillin is not revealed. However use of Ampicillin at pregnancy is possible only in that case when the expected advantage for the woman exceeds potential risk for a fruit.
Ampicillin gets into breast milk in low concentration. During treatment by drug it is necessary to stop feeding by a breast.
Children. It is necessary to be careful at drug use to children, especially if in the anamnesis of mother there is a reference to hypersensitivity to β-laktamny antibiotics.

Overdose:

At overdose perhaps toxic impact on the central nervous system (dizziness, a headache), the dispeptic phenomena (nausea, vomiting, a liquid chair), allergic reactions in the form of skin rash. In case of symptoms of overdose drug should be cancelled immediately and if necessary to carry out a symptomatic treatment: gastric lavage, use of activated
coal, salt laxatives, correction of water and electrolytic balance, hemodialysis. At an allergy the antihistaminic and desensibilizing means are shown.

Storage conditions:

Period of validity 2 years. To store in original packaging at a temperature not above 25 °C. To store in the unavailable place.

Issue conditions:

According to the recipe

Packaging:

On 0,5 g or 1,0 g in bottles; in bottles No. 10 in a pack.