Source: Υπουργείο Υγείας (CY) Revision Year: 2016 Publisher: MEDOCHEMIE LTD, 1-10 Constantinoupoleos street, 3011 Limassol, Cyprus
Pharmacotherapeutic group: Penicillins with extended spectrum, Beta-lactam antibacterials, penicillins
ATC code: J01CA01
Ampicillin is a beta-lactam antibiotic, it is an aminopenicillin. The presence of the amino group side chain attached to the basic penicillin structure enables it to better penetrate the outer membrane of some Gram negative bacteria. It is inactivated by beta-lactamases. As with other penicillins, ampicillin exhibits its bacteriostatic and bactericidal action by inhibiting bacterial cell wall synthesis.
Ampicillin is relatively stable in gastric acid and is moderately well absorbed following oral administration. Food interferes with the absorption thus it should be administered at least 30 minutes before meals. Peak plasma concentrations are reached one to two hours post dose and following 500mg range from 2μg/ml-6μg/ml.
Following intramuscular administration of 500mg, peak plasma concentrations are reached in about an hour and range from 7μg/ml-14μg/ml.
Ampicillin is widely distributed and therapeutic concentrations can be reached in ascitic, pleural and joint fluids. It crosses the placental barrier and small amounts are excreted in breast milk. There is little diffusion into the cerebrospinal fluid in the absence of meningeal inflammation. It is about 20% plasma protein bound, plasma half life is about 1-1.5 hours, this is prolonged in neonates and the elderly and may be up to 20 hours in severe renal failure.
It undergoes some metabolism to penicilloic acid, which is excreted in the urine.
Renal clearance is by a combination of glomerular filtration and tubular secretion; about 20%-40% of an oral dose is excreted unchanged in the urine in 6 hours with urinary concentration of 0.25mg/ml-1mg/ml after a 500mg dose. After parenteral administration, about 60%-80% is excreted within six hours. There are high biliary concentrations; it undergoes enterohepatic recirculation and some faecal excretion occurs.
Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction and development.
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