Ампициллин-Ферейн®

General characteristics. Structure:

Active ingredient: 0,25 g, 0,5 g or 1 g of ampicillin in 1 bottle (in the form of sodium salt).

Pharmacological properties:

Pharmacodynamics. Ampicillin - an antibacterial microbicide from group of semi-synthetic penicillin, a broad spectrum of activity. Suppresses synthesis of a cell wall of bacteria. Кислотоустойчив.

It is active concerning gram-positive (alpha and beta and hemolitic streptococci, Streptococcus pneumoniae, Staphylococcus spp., Bacillus anthracis, Clostridium spp., it is moderately active against most Enterococcus spp., including Enterococcus faecalis), Listeria spp., and non-negative (Haemophilus influenzae, Neisseria gonorrhoae, Neisseria meningitidis, Proteus mirabilis, Yersinia multocida (before Pasteurella), many types of Salmonella spp., Shigella spp., Escherichia coli) microorganisms, aerobic asporous bacteria.

It is not effective concerning penitsillinazoprodutsiruyushchy strains of Staphylococcus spp., all strains of Pseudomonas aeruginosa, majority of strains of Klebsiella spp. and Enterobacter spp.

Pharmacokinetics. At parenteral administration 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 (at its inflammation), saliva, fruit fabrics. Badly gets through a blood-brain barrier (permeability increases at an inflammation of a meninx).

It is removed preferential by kidneys (70-80%), 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 activators, sensitive to ampicillin: airways and ENT organs (sinusitis, tonsillitis, pharyngitis, average otitis, bronchitis, pneumonia, lung abscess), infection of kidneys and urinary tract (pyelonephritis, pyelitis, cystitis, urethritis), gonorrhea, infections of biliary system (cholangitis, cholecystitis), 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), abdominal infections (peritonitis), endocarditis (prevention and treatment), meningitis, sepsis.

Route of administration and doses:

Intramusculary, intravenously (struyno or kapelno). Doses and the mode of dosing choose individually depending on weight of a current, localization of an infection and sensitivity of the activator. The Sredneterapevtichesky dose for adults and children with body weight more than 40 kg - 0,25 - 0,5 g which enter in oil or into each 6 h.

In case of a heavy infection the daily dose can be increased to 10 g.

For treatment of gonorrhea enter 2 doses on 0,5 g at an interval of 8 or 12 h.

For treatment of bacterial meningitis and sepsis the daily dose of drug makes 150 - 200 mg/kg which is shared on 6-8 in/in introductions with an interval of 3-4 h. The maximum daily dose - 8-14 g.

For prevention of a bacterial endocarditis at the patients from group of high risk who are exposed to dental, endoscopic interventions, "small" ENT organs operations, and also operations on bodies digestive tract or biliary tract - 2 g in/in or in oil in 30 min. prior to the procedure or operation; if necessary, in 6 h enter repeatedly in a dose 1 g.

Children with body weight have less than 40 kg for treatment of respiratory infections, skin and soft tissues a daily dose of ampicillin makes 25-50 mg/kg; for treatment of infections of an abdominal cavity or urinary tract enter 50 - 100 mg/kg a day. The daily dose is divided into 4 introductions with an interval of 6 h.

For treatment of a septicaemia or infections of the central nervous system (bacterial meningitis) the daily dose equal of 100-200 mg/kg, share on 6-8 in/in introductions with an interval between introductions of 3-4 h.

For prevention of a bacterial endocarditis - 50 mg/kg in/in or in oil in 30 min. prior to the procedure or operation; if necessary, in 6 h enter repeatedly in a dose 25 mg/kg.

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. It is recommended to continue administration of ampicillin of 48-72 more h after disappearance of clinical signs of a disease.

Solution for intramuscular introduction is prepared by extepore, adding to soderzhiyomy a bottle (0,25 g, 0,5 g and 1 g) of 2 ml of water for injections.

For intravenous administration the single dose of drug (no more than 2 g) is dissolved in 5-10 ml of water for injections or isotonic solution of sodium of chloride and entered slowly within 3-5 minutes (1-2 g within 10-15 minutes). At the single dose exceeding 2 g the drug administer intravenously kapelno.

For intravenous drop administration a single dose of drug (2-4 g) dissolve in a small amount of water for injections 7,5-15 ml respectively, then add the received solution of an antibiotic to 125-250 ml of isotonic solution of sodium of chloride or 5-10% to solution of a dextrose and enter with a speed of 60-80 thaws a minute.

At drop introduction to children as solvent use 5-10% dextrose solution (30-50 ml depending on age). Solutions use right after preparation, addition to them of other medicines is inadmissible.

Features of use:

Pregnancy and lactation. Use of drug during pregnancy is possible only if the estimated advantage for mother exceeds potential risk for a fruit. Ampicillin gets into breast milk in low concentration. If necessary use of drug in the period of a lactation it is necessary to stop breastfeeding.

Before use of medicine it is necessary to consult with the doctor.

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 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 others beta лактамными antibiotics are possible.

At treatment of the slight diarrhea arising 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 medicines, drug withdrawal is shown. 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.

Influence on ability to manage vehicles and mechanisms. During treatment it is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Allergic reactions: the skin peeling, an itch, a small tortoiseshell, rhinitis, conjunctivitis, a Quincke's edema, fever, an arthralgia, an eosinophilia, erythematic and makulopapulezny rash, exfoliative dermatitis, a multiformny exudative erythema, a malignant exudative erythema (Stephens-Johnson's syndrome), reactions similar to a serum disease, an acute anaphylaxis, not allergic ampitsillinovy rash, can disappear without drug withdrawal.

From digestive tract: dysbacteriosis, stomatitis, gastritis, dryness of a mucous membrane of an oral cavity, taste change, abdominal pain, vomiting, nausea, diarrhea, glossitis, increase in activity of "hepatic" transaminases, pseudomembranous colitis.

From the central nervous system: agitation, aggression, uneasiness, confusion of consciousness, change of behavior, a depression, a headache, a tremor, are possible spasms (at therapy by high doses).

From bodies of a hemopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, anemia.

Local reactions: pain in an injection site, infiltrates in places at intramuscular introduction, phlebitis at intravenous administration in large numbers.

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

Interaction with other medicines:

Pharmaceutical it is incompatible with aminoglycosides.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) have sinergidny effect; bacteriostatic medicines (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 paraaminobenzoic acid is formed, ethinylestradiol (in the latter case the risk of development of bleedings of "break" increases).

Diuretics, Allopyrinolum, оксифенбутазон, the phenylbutazone, non-steroidal anti-inflammatory drugs and other medicines blocking canalicular secretion increase concentration of ampicillin in plasma (due to decrease in canalicular secretion).

Allopyrinolum increases risk of development of skin rash. Ampicillin reduces clearance and increases toxicity of a methotrexate. Strengthens digoxin absorption.

Let's combine with antibiotics streptomycin, Kanamycinum.

Contraindications:

Hypersensitivity to ampicillin (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 1 month).

With care. bronchial asthma, hay fever and other 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: medicines for maintenance of water and electrolytic balance, symptomatic therapy. In hard cases it is removed by means of a hemodialysis.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intravenous and intramuscular administration of 0,25 g, 0,5 g, or 1 g. On 0,25 g, 0,5 g or 1 g of active agent (ampicillin) in the bottles with a capacity of 10 ml which are hermetically corked by traffic jams from rubber mix, pressed out by aluminum caps. 1 bottle together with the application instruction place in a pack from a cardboard or a cardboard chrome-ersatz of coated. 5 bottles place in a blister strip packaging from a film polyvinyl chloride. 5 bottles with drug place in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. 1 or 2 blister strip packagings with the application instruction place in a pack from a cardboard. 5 or 10 bottles together with the application instruction place in a pack. Packaging for hospitals: on 10, 20, 30, 40, 50 blister strip packagings with application instructions place in a box from a cardboard.