COMPOSITION: Each Tablet contains :-
Amoxicillin 500 mg
Clavulanate 125 mg
Amoxicillin kills bacteria by interfering with the production of the bacterial cell wall (outer coating of bacteria). As a result, the bacterial cell wall is weakened and ruptured, thereby killing the bacteria.
Clavulanic acid belongs to a group of medicines called beta-lactamase inhibitors. It blocks the activity of a chemical (beta-lactamase), which is secreted by bacteria to protect themselves from antibiotic drugs like amoxicillin, thereby allowing the antibiotics to act against the bacteria. It does not kill bacteria and is never used alone to treat infections
Amoxicillin and clavulanic acid, are fully dissociated in aqueous solution at physiological pH. Both components are rapidly and well absorbed by the oral route of administration. Absorption of amoxicillin/clavulanic acid is optimised when taken at the start of a meal. Following oral administration, amoxicillin and clavulanic acid are approximately 70% bioavailable. The plasma profiles of both components are similar and the time to peak plasma concentration (Tmax) in each case is approximately one hour.
The pharmacokinetic results for a study, in which amoxicillin/clavulanic acid (500 mg/125 mg tablets three times daily) was administered in the fasting state to groups of healthy volunteers are presented below.
|Mean (± SD) pharmacokinetic parameters|
|Active substance(s) administered||Dose||Cmax||Tmax *||AUC (0-24h)||T 1/2|
500 mg/125 mg
|AMX – amoxicillin, CA – clavulanic acid
* Median (range)
Amoxicillin and clavulanic acid serum concentrations achieved with amoxicillin/clavulanic acid are similar to those produced by the oral administration of equivalent doses of amoxicillin or clavulanic acid alone.
About 25% of total plasma clavulanic acid and 18% of total plasma amoxicillin is bound to protein. The apparent volume of distribution is around 0.3-0.4 l/kg for amoxicillin and around 0.2 l/kg for clavulanic acid.
Following intravenous administration, both amoxicillin and clavulanic acid have been found in gall bladder, abdominal tissue, skin, fat, muscle tissues, synovial and peritoneal fluids, bile and pus. Amoxicillin does not adequately distribute into the cerebrospinal fluid.
From animal studies there is no evidence for significant tissue retention of drug-derived material for either component. Amoxicillin, like most penicillins, can be detected in breast milk. Trace quantities of clavulanic acid can also be detected in breast milk (see section 4.6).
Both amoxicillin and clavulanic acid have been shown to cross the placental barrier.
Amoxicillin is partly excreted in the urine as the inactive penicilloic acid in quantities equivalent to up to 10 to 25% of the initial dose. Clavulanic acid is extensively metabolized in man and eliminated in urine and faeces and as carbon dioxide in expired air.
The major route of elimination for amoxicillin is via the kidney, whereas for clavulanic acid it is by both renal and non-renal mechanisms.
Amoxicillin/clavulanic acid has a mean elimination half-life of approximately one hour and a mean total clearance of approximately 25 l/h in healthy subjects. Approximately 60 to 70% of the amoxicillin and approximately 40 to 65% of the clavulanic acid are excreted unchanged in urine during the first 6 h after administration of single Augmentin 250 mg/125 mg or 500 mg/125 mg tablets. Various studies have found the urinary excretion to be 50-85% for amoxicillin and between 27-60% for clavulanic acid over a 24 hour period. In the case of clavulanic acid, the largest amount of drug is excreted during the first 2 hours after administration.
INDICATION : Used to treat bacterial infections of the respiratory tract (bronchitis, pneumonia), genital and urinary tract (gonorrhoea, ), skin and soft tissue, ear (otitis media); nose, sinus, and throat (tonsillitis, sinusitis); heart (endocarditis), kidney, urethra or bladder, blood (septicemia), teeth and gums (abcesses), typhoid and paratyphoid fever
DOSAGE : As directed by the physician
SIDE EFFECTS : Headache, Nausea, Skin rash, Vomiting, Vaginal itching and discharge, Severe skin allergies, Stomach pain, Diarrhea