Source: Health Products Regulatory Authority (ZA) Revision Year: 2021 Publisher: Ranbaxy Pharmaceuticals (Pty) Ltd, 14 Lautre Road, Stormill Ext. 1, Roodepoort 1724, South Africa
Category and class: A 20.1.2 Penicillins
Pharmacotherapeutic group: penicillins with extended spectrum
ATC code: J01CA04
Amoxycillin is a semisynthetic, broad-spectrum, beta-lactam penicillin antibiotic that inhibits one or more enzymes (often referred to as penicillin-binding proteins, PBPs) in the biosynthetic pathway of bacterial peptidoglycan, which is an integral structural component of the bacterial cell wall. Inhibition of peptidoglycan synthesis leads to weakening of the cell wall, which is usually followed by cell lysis and death.
Amoxycillin is susceptible to degradation by beta-lactamases produced by resistant bacteria and therefore the spectrum of activity of amoxycillin alone does not include organisms which produce these enzymes.
Amoxycillin exhibits in vitro bactericidal activity against a wide range of Gram-negative and Gram-positive organisms including: (in vitro sensitivity does not necessarily imply in vivo efficacy):
Amoxycillin may also have some effect against the following organisms:
Bacteroides fragilis*, Proteus mirabilis* and Nocardia*.
* Sensitivity tests must be formed.
Most species of the following organisms are resistant to amoxycillin:
Enterobacter, Pseudomonas, Klebsiella, Serratia, Acinetobacter and indole-positive Proteus.
Amoxycillin is well absorbed orally. After oral administration, there is no significant difference between the peak serum levels in fasting and non-fasting subjects. The presence of food does not interfere with the absorption of amoxycillin and may therefore, be taken with meals.
There is a linear/dose response in peak serum levels after oral administration.
There is insufficient evidence at present to show that amoxycillin penetrates into the cerebro spinal fluid in therapeutic quantities and it should, therefore, not be used in the treatment of cerebro spinal infections.
Amoxycillin is partly excreted in the urine as the inactive penicilloic acid in quantities equivalent to up to 10 to 25% of the initial dose.
Approximately 60% of an oral dose of amoxycillin is excreted unchanged in the active form into the urine within six hours.
The elimination half-life of amoxycillin is similar for children aged around 3 months to 2 years and older children and adults. For very young children (including preterm newborns) in the first week of life the interval of administration should not exceed twice daily administration due to immaturity of the renal pathway of elimination.
Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.
Following oral administration of amoxycillin to healthy males and female subjects, gender has no significant impact on the pharmacokinetics of amoxycillin.
The total serum clearance of amoxycillin decreases proportionately with decreasing renal function (see sections 4.4).
Hepatically impaired patients should be dosed with caution and hepatic function monitored at regular intervals.
Non-clinical data reveal no special hazard for humans based on studies of safety pharmacology, repeated dose toxicity, genotoxicity and toxicity to reproduction and development.
Carcinogenicity studies have not been conducted with amoxycillin.
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