Аmpicillin trihydrate

Аmpicillin trihydrate

Active substance (INN):

Ampicillin (as sodium salt)

ATC code: J01CA01

Pharmacotherapeutic group:

Antibiotics (penicillin group)

 

 

Pharmacological properties

Ampicillin is an antibiotic of a wide range of action from the group of semisynthetic penicillins. It acts bactericidally suppressing the synthesis of a cellular wall of microorganisms. It is destroyed by penicillinase, acid-resistant. The following microorganisms are constantly sensitive to the drug: Staphylococcus spp.. Streptococci A, B, C, F, G; Str. pneumoniae not producing penicillinases; L. monocytogenes, Corynebacterium diphtheriae, Erysipelotrix rhusopathiae, Eikenellia, N. meningilidis, Bordetella pertussis, Clostridium spp., Propioniobacterium acnes, Peptostreptococcus spp., Actinomyces spp., Leptospira spp., Treponema; ones not permanently sensitive: Enterococcus faecalis, E. Coli, Proteus mirabilis, Salmonella spp., Vibrio cholerae, H. Influenzae, N. gonorrhoeae, Fusobacterium spp., Prevotella. The following organisms are resistant to the drug: catarrhalis, Klebsiella spp., Enterobacter spp., diversus, freundii, Proteus vulgaris, Providencia rettgeri, Morganella morganii, Y. enterocolitica, Pseudomonas spp., Acinetabacter spp., Xanthomonas spp., Flavobacterium spp., Alcaligenes spp., Nocardia spp., Campylobacter spp., Legionella pneumophila, Mycobacterium spp. Bacteroidesspp., Mycoplasmaspp.,Chlamydiaspp.

Pharmacokinetics

Following a parenteral administration the drug permeates into tissues and bodily liquids. Its therapeutic concentrations are found in pleural, peritoneal and synovial liquids and bile. The drug passes through the placental barrier and is excreted into maternal milk. The half-life period is about 1 hour, increasing to 12-20 hours in anuria. The bulk of it is excreted from the body with kidneys and the concentration of the antibiotic in urine is very high. The drug does not cumulate at repeated administrations enabling to administer it in great doses and continuously.

Indications to use

Bacterial infections: bronchitis, pneumonia, dysentery, salmonellosis, long-term carriage of salmonellas, cholecystitis, whooping cough, pyelonephritis, urethritis, endocarditis, infections of the skin and soft tissues, gynecologic infections, infections of the ear, throat and nose, dontogenous infections, meningitis, sepsis and other infections caused by drug-sensitive microorganisms.

Administration and dosage

Intramuscularly and intravenously. Adults are prescribed 250 to 500 mg 4-6 times daily; in serious infections a daily dose can be increased to 10 g and over; a daily dose for children depends on age: newborns are prescribed 100 mg/kg, those under 1 year - 50 mg/kg, 1 to 4 years - 50-75 mg/kg, those over 4 years - 50 mg/kg. Duration of treatment depends on severity of the state and treatment efficacy (from 5-10 days to 2-3 weeks and over).

Side effects

Allergic responses (urticaria, erythema, Quincke's edema, rhinitis, conjunctivitis; seldom: fever, joint pains, eosinophilia; extremely seldom: anaphylactic shock). A toxic action on the central nervous system is possible (if high doses are used in patients with renal insufficiency), dyspeptic events (diarrhea, nausea, vomiting), candidiasis, intestinal dysbacteriosis.

Contraindications

Hypersensitivity (including to other penicillins, cephalosporins, carbapenems), severe disturbances of the liver function, breast feeding (it should be suspended during treatment).

Drug interaction

Mutual antagonism can occur in simultaneous administration with bacteriostatic antibiotics (tetracycline, chloramfenicol, erythromycin, etc.). If administered with aminoglycoside antibiotics, synergy in antimicrobic efficiency is observed. Joint administration of probenecide lowers excretion of the drug with urine and results in rising of its content in blood serum and that with allopyrinol slows down the drug metabolism and increases a frequency of dermal eruption incidence. In rare cases, the drug weakens the action of oral contraceptives.

Special warnings

Should allergic responses occur, it is necessary to discontinue the drug administration and to undertake desensitizing therapy. When the drug is used in patients with sepsis, a bacteriolysis reaction (Yarish - Gerksheimer reaction) may occur. A long-term treatment in weakened patients may result in development of superinfection caused by drug-resistant microorganisms (yeast-like fungi, Gram-negative microorganisms). When such patients are treated with the drug, it is expedient to prescribe them vitamins of group B and vitamin C and give them nystatin or levorin if needed. In bronchial asthma, hay fever and other allergic diseases, the drug is used in simultaneous administration of desensitizing agents according to the case. The drug is prescribed with caution to pregnant and breast feeding women. A regular monitoring of the function of the kidneys, liver and a blood picture is needed. Caution should be used in prescribing the drug to patients with renal insufficiency.

Supply

Powder, 0.5 g or 1.0 g in vials

Storage conditions

To be kept in a dry and protected from light place at room temperature.

Shelf life

2 years

Dispensed with a prescription

Not to be used after the expiry date indicated on the package. To be stored out of the reach to children