Ampicillin

General characteristics. Structure:

Powder for preparation of suspension for intake of white color with a yellowish shade, with a specific smell; the prepared suspension of white color with a yellowish shade.

Active ingredient: ampicillin (in the form of trihydrate) 250 mg

Excipients: polyvinylpirrolidone, sodium glutamate acid 1-water, sodium phosphate disubstituted or dinatrium phosphate anhydrous, Trilonum of B, Dextrosum, vanillin, essence aromatic food (crimson), refined sugar or icing sugar refining.
60 g (5 g active in-va) - bottles (1) complete with a dosing spoon - packs cardboard.

Powder for preparation of solution for injections of white color, hydroscopic.

Active ingredient: ampicillin (in the form of sodium salt) 1 g

Powder for preparation of solution for injections of white color, hydroscopic.

Active ingredient:  ampicillin (in the form of sodium salt) 2 g.

Pharmacological properties:

Pharmacodynamics.  Ampicillin – an antibiotic of a broad spectrum of activity from group of semi-synthetic penicillin. Works bakteritsidno due to suppression of synthesis of a cell wall of bacteria. 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 in the relation:
 gram-positive aerobic bacteria: Staphylococcus spp. (the strains which are not developing a penicillinase and other beta lactamelements, Streptococcus spp. (including alpha and beta and hemolitic streptococci, Streptococcus pneumoniae), Bacillus anthracis, Listeria spp. It is moderately active against the majority of enterococci of Enterococcus spp. (including Enterococcus faecalis);
 gram-negative aerobic bacteria (the strains which are not developing some beta lactamazu): Haemophilus influenzae, Bordetella pertussis, Neisseria meningitidis, Proteus mirabilis, Yersinia multocida (before Pasteurella), many types of Salmonella spp., Shigella spp., Escherichia coli;
 anaerobe bacterias: Clostridium spp.
 It is inactive concerning penitsillinazoprodutsiruyushchy strains of Staphylococcus spp., all strains of Pseudomonas aeruginosa, Proteus vulgaris, majority of strains of Klebsiella spp.i Enterobacter spp., some strains of Escherichia coli, mycoplasmas, chlamydias, rickettsiae.

Pharmacokinetics.  Communication with proteins of plasma – 20%. At parenteral administration (in/in, in oil) concentration in blood exceeds created at intake. 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, but its permeability increases at an inflammation of a meninx.

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to ampicillin, including:

— respiratory infections (including bronchitis, pneumonia, lung abscess);

— infections of ENT organs (including tonsillitis);

— infections of biliary tract (including cholecystitis, cholangitis);

— infections of urinary tract (including pyelitis, pyelonephritis, cystitis);

— GIT infections (including salmonellonositelstvo);

— gynecologic infections;

— infections of skin and soft tissues;

— peritonitis;

— sepsis, septic endocarditis;

— meningitis;

— rheumatism;

— ugly face;

— scarlet fever;

— gonorrhea.

Route of administration and doses:

Establish individually depending on weight of a current, localization of an infection and sensitivity of the activator.

At intake the single dose for adults makes 250-500 mg, a daily dose - 1-3 g. The maximum daily dose makes - 4 g.

To children drug appoint in a daily dose 50-100 mg/kg, to children with body weight to 20 kg - 12.5-25 mg/kg.

The daily dose is divided into 4 receptions. Duration of treatment depends on weight of an infection and efficiency of treatment.

Pill is taken inside irrespective of meal.

For preparation of suspension with powder add 62 ml of the distilled water to a bottle. Dose ready suspension the special spoon having 2 tags: lower corresponds to 2.5 ml (125 mg), upper - 5 ml (250 mg). Suspension should be washed down with water.

At parenteral administration (in oil, in/in struyno or in/in kapelno) the single dose for adults makes 250-500 mg, a daily dose - 1-3 g; at heavy infections the daily dose can be increased to 10 g and more.

To newborn children 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 divided into 4-6 introductions with an interval of 4-6 h. Duration in oil of introduction - 7-14 days. Duration in/in uses of 5-7 days, with the subsequent transition (if necessary) to introduction in oil.

Solution for introduction in oil is prepared, adding to bottle contents 2 ml of water for injections.

For in/in jet introductions dissolve a single dose of drug (no more than 2 g) in 5-10 ml of water for injections or isotonic solution of sodium of chloride and enter slowly within 3-5 min. (1-2 g within 10-15 min.). At the single dose exceeding 2 g, the drug is administered in/in kapelno. For this purpose the single dose of drug (2-4 g) is dissolved in 7.5-15 ml of water for injections, then the received solution is added to 125-250 ml of isotonic solution of sodium chloride or 5-10% of solution of glucose and entered with a speed of 60-80 кап. / min. At in drop introduction to children as solvent use 5-10% glucose solution (30-50 ml depending on age).

Solutions use right after preparation.

Features of use:

With care and against the background of simultaneous use of the desensibilizing means it is necessary to appoint drug at bronchial asthma, hay fever and other allergic diseases.

In the course of use systematic control of function of kidneys, a liver and a picture of peripheral blood is necessary.

At a liver failure drug should be used only under control of function of a liver.

Patients with renal failures need correction of the mode of dosing depending on KK.

At use of drug in high doses at patients with a renal failure perhaps toxic action on TsNS.

At use of drug for treatment of sepsis reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.

At emergence of allergic reactions against the background of use of Ampitsillina-AKOS drug it is necessary to cancel and appoint the desensibilizing therapy.

At the weakened patients at prolonged use of drug the superinfection caused by microorganisms, steady against ampicillin, can develop.

For prevention of development of candidiasis along with Ampitsillinom-AKOS it is necessary to appoint nystatin or levorinum, and also vitamins of group B and C.

Side effects:

Allergic reactions: skin rash, small tortoiseshell, Quincke's edema, itch, exfoliative dermatitis, multiformny erythema; in rare instances - an acute anaphylaxis.

From the alimentary system: nausea, vomiting, diarrhea, glossitis, stomatitis, pseudomembranous colitis, intestinal dysbacteriosis, increase in activity of hepatic transaminases.

From system of a hemopoiesis: anemia, leukopenia, thrombocytopenia, agranulocytosis.

The effects caused by chemotherapeutic action: oral cavity candidiasis, vaginal candidiasis.

Interaction with other medicines:

Probenetsid at simultaneous use with Ampicillin - reduces canalicular secretion of ampicillin therefore its concentration in a blood plasma increases and the risk of toxic action increases.

At simultaneous use of Ampicillin with Allopyrinolum the probability of emergence of skin rash increases.

At simultaneous use with Ampicillin - efficiency of estrogenosoderzhashchy oral contraceptives decreases.

At simultaneous use with Ampicillin efficiency of anticoagulants and antibiotics aminoglycosides increases.

Contraindications:

— hypersensitivity to antibiotics from group of penicillin and to other betalaktamny antibiotics;

— the expressed abnormal liver functions (for parenteral use).

 

Use of drug at pregnancy and feeding by a breast
Use of drug at pregnancy according to indications is possible when the advantage for mother exceeds potential risk for a fruit.

Ampicillin is emitted with breast milk in low concentration. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

 

Use at abnormal liver functions
Parenteral use is contraindicated at the expressed abnormal liver functions.

 

Use at renal failures
Patients with renal failures need correction of the mode of dosing depending on KK.

At use of drug in high doses at patients with a renal failure perhaps toxic action on TsNS.

 

Use for children
At intake to children drug appoint in a daily dose 50-100 mg/kg, to children with body weight to 20 kg - 12.5-25 mg/kg. To parenterally newborn children 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.

Overdose:

Now about cases of overdose of drug it was not reported.

Storage conditions:

List B. Drug should be stored in the dry, protected from light place; powder for preparation of solution for injections - at a temperature not above 20 °C. A period of validity of tablets, powder for preparation of suspension and powder for preparation of solution for injections - 2 years.

The prepared suspension should be stored in the refrigerator or at the room temperature no more than 8 the Prepared solutions for in oil and in/in introductions are not subject to storage.

Issue conditions:

According to the recipe

Packaging:

Bottles of 10 ml (1) - packs cardboard.
Bottles of 10 ml (10) - packs cardboard.
Bottles of 10 ml (50) - boxes cardboard.

Bottles of 10 or 20 ml (1) - packs cardboard.
Bottles of 10 or 20 ml (10) - packs cardboard.
Bottles of 10 or 20 ml (50) - boxes cardboard.