Amocla

Amoxicillin trihydrate, clavulanate potassium.

Each tablet contains combination of amoxicillin trihydrate and clavulanate potassium equivalent to 500mg amoxicillin and 125mg clavulanic acid as active ingredients.
AMOCLA is an oral antibacterial combination consisting of the semisynthetic antibiotic amoxicillin and the β-lactamase inhibitor, clavulanate potassium (the potassium salt of clavulanic acid). Amoxicillin is an analog of ampicillin, derived from the basic penicillin nucleus, 6-aminopenicillanic acid. The amoxicillin molecular formula is C₁₆H₁₉N₃O₅S·3H₂0 and the molecular weight is 419.46. Clavulanic acid is produced by the fermentation of Streptomyces clavuligerus. It is a β-lactam structurally related to the penicillins and possesses the ability to inactivate a wide variety of β-lactamases by blocking the active sites of these enzymes. Clavulanic acid is particularly active against the clinically important plasmid mediated β-lactamases frequently responsible for transferred drug resistance to penicillins and cephalosporins. The clavulanate potassium molecular formula is C₈H₈KNO₅ and the molecular weight is 237.25.

Pharmacology: Amoxicillin and clavulanate potassium are well absorbed from the gastrointestinal tract after oral administration of AMOCLA. Dosing in the fasted or fed state has minimal effect on the pharmacokinetics of amoxicillin. While AMOCLA can be given without regard to meals, absorption of clavulanate potassium when taken with food is greater relative to the fasted state. In one study, the relative bioavailability of clavulanate was reduced when AMOCLA was dosed at 30 and 150 minutes after the start of a high fat breakfast. The safety and efficacy of AMOCLA have been established in clinical trials where AMOCLA was taken without regard to meals.
Amoxicillin serum concentrations achieved with AMOCLA are similar to those produced by the oral administration of equivalent doses of amoxicillin alone. The half-life of amoxicillin after the oral administration of AMOCLA is 1.3 hours and that of clavulanic acid is 1.0 hour.
Approximately 50% to 70% of the amoxicillin and approximately 25% to 40% of the clavulanic acid are excreted unchanged in urine during the first 6 hours after administration of a single AMOCLA 625mg tablet.
Concurrent administration of probenecid delays amoxicillin excretion but does not delay renal excretion of clavulanic acid.
Neither component in AMOCLA is highly protein-bound; clavulanic acid has been found to be approximately 25% bound to human serum and amoxicillin approximately 18% bound.
Amoxicillin diffuses readily into most body tissues and fluids with the exception of the brain and spinal fluid. The results of experiments involving the administration of clavulanic acid to animals suggest that this compound, like amoxicillin, is well distributed in body tissues.

Susceptibility range of microorganism: AMOCLA is bactericidal to a wide range of Gram-positive and Gram-negative organisms including many clinically important penicillin resistant pathogens by producing β-lactamase.
Gram-Positive: Aerobes: *Staphylococcus aureus, *Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Streptococcus faecalis, Listeria monocytogenes, Bacillus anthracis, Corynebacterium species.
Anaerobes: Clostridium species, Peptococcus species, Peptostreptococcus species.
Gram-Negative: Aerobes: *Branhamella catarrhalis, *Bordetella pertussis, Brucella species, Campylobacter jejuni, *Escherichia coli, Gardnerella vaginalis, *Haemophilus ducreyi, *Haemophilus influenzae, *Klebsiella species, *Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella multocida, *Proteus mirabilis, *Proteus vulgaris, *Salmonella species, *Shigella species, Vibrio cholerae, *Yersinia enterocolitica.
Anaerobes: *Bacteroides species (including Bacteroides fragilis).
(*: including β-lactamase producing strains).
Uses: Tonsilitis, Sinusitis, Otitis media; Acute and chronic bronchitis, Pneumonia, Thoracic empyema, Lung abscess; Boils & abscesses, Cellulitis, Wound infection, Intra-abdominal sepsis; Cystitis, Urethritis, Nephropyelitis, Septic abortion, Puerperal sepsis, Pelvic infection, Chancroid, Gonorrhoea; Osteomyelitis; Septicaemia; Surgical prophylaxis; Peritonitis.

The usual adult dose is 1 tablet every 12 hours.
It should be adjusted to age and degree of symptoms.

Problems of overdosage with AMOCLA are unlikely to occur. As problems of overdosage gastrointestinal disturbances or imbalance of body fluid or electrolytes may occur. In these cases, patients should be treated symptomatically with attention to water & electrolytes balance. This drug may be removed by hemodialysis.

Patients with a history of hypersensitivity to any penicillin.
Patients with infectious mononucleosis.
Patients with a previous history of AMOCLA or any penicillin-associated cholestatic jaundice/hepatic dysfunction.

It should be administered carefully to the following patients: Patients with severe hepatic dysfunction.
Patients with moderate or severe renal dysfunction (Dose interval should be adjusted for the patients because blood concentration of the drug can be prolonged).
Patients with a previous history of hypersensitivity to penicillins or cephems.
Patients who or whose family have a tendency to show allergic symptoms such as bronchial asthma, rashes, urticaria, etc.
Patients who are mal-nutritioned orally or who are parenterally nutritioned, the elderly patients, and patients with bad systemic condition (vitamin K deficiency may occur).
General precautions: Serious and occasionally fatal hypersensitivity reactions (including anaphylactoid and severe cutaneous adverse reactions) have been reported in patients on penicillin therapy. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity. These reactions may also occur in both oral and parenteral therapy, but more frequently in parenteral therapy. If an allergic reaction occurs, AMOCLA must be discontinued and appropriate alternative therapy instituted. Serious anaphylactic reactions require immediate emergency treatment with adrenaline. Oxygen, intravenous steroids and airway management (including intubation) may also be required.
The long term treatment with AMOCLA may result in overgrowth of nonsusceptible organisms, thus careful observation is required for more than 14 days treatment.
Changes in liver function test have been observed in some patients receiving AMOCLA. The clinical significance of these changes is uncertain, but AMOCLA should be used with caution in patient with evidence of hepatic failure. Serious and usually reversible cholestatic jaundice have been reported rarely. Signs and symptoms may not occur in appearance until six weeks after treatment has ended.
In patients with moderate and severe renal dysfunction dose of AMOCLA should be adjusted following "Dosage & Administration".
Erythematous rashes have been associated with glandular fever in patients receiving amoxicillin, thus use of AMOCLA should be avoided in case that glandular fever is worried.
Use in Pregnancy & Lactation: Animal studies have shown no teratogenic effects; however, safe use of AMOCLA during pregnancy has not been definitely established. Thus, this drug should be used during pregnancy only when the potential benefits justify the possible risks to the fetus. Especially AMOCLA should not be administered during first trimester of pregnancy.
During lactation, trace quantities of penicillin can be excreted in breast milk.

Animal studies have shown no teratogenic effects; however, safe use of AMOCLA during pregnancy has not been definitely established. Thus, this drug should be used during pregnancy only when the potential benefits justify the possible risks to the fetus. Especially AMOCLA should not be administered during first trimester of pregnancy.
During lactation, trace quantities of penicillin can be excreted in breast milk.

Gastrointestinal reactions: Diarrhoea, pseudomembranous colitis, indigestion, nausea, and vomiting may occur. Candidiasis and antibiotic-associated colitis (including pseudomembranous colitis and haemorrhagic colitis) have been reported rarely. Nausea, although uncommon, is more often with higher oral dosages. If gastrointestinal side effects occur with oral therapy they may be reduced by taking AMOCLA at the start of meals. As with other antibiotics the incidence of gastrointestinal side effects may be raised in children under two years. In clinical trials, however, only 4% of children under two years were withdrawn from treatment.
Hepatic effects: Sometimes rise in AST, ALT, and Al-P have been reported. Hepatitis and cholestatic jaundice have been reported rarely. These have been reported more frequently in the adult, elderly, and male. Signs and symptoms usually occur during treatment, but in some case may not occur until six weeks after treatment has ended. Hepatic reactions are usually reversible but very rarely, deaths have been reported. Hepatic reactions have been reported more frequently in males and elderly patients, and they are estimated to be related to long-term treatment.
Hypersensitivity reactions: Urticarial and erythematous rashes sometimes occur. Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, and exfoliative dermatitis have been reported rarely. Treatment should be discontinued if one of these disorders occurs. In common with other β-lactam antibiotics angioedema, anaphylaxis, serum sickness-like syndrome and hypersensitive vasculitis have been reported.
Skin and subcutaneous tissue disorders: Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) have been reported very rarely.
Haematological effects: As with other β-lactams transient leucopenia (including eosinopenia and deficiency disease of granulocytes), transient thrombocytopenia, haemolytic anaemia, thrombocytopenic purpurea, eosinophilia, leukopenia and agranulocytosis have been reported rarely.
CNS effects: CNS effects have been seen very rarely. They include reversible hyperactivity, dizziness, headache and convulsions. Convulsions may occur with impaired renal function or in those receiving high doses.
Renal effects: Severe renal dysfunction such as acute renal failure, and interstitial nephritis may occur rarely.
Thus, renal function should be evaluated periodically. Whenever abnormalities occur, the drug should be discontinued and the patients are properly treated.
Nervous system disorders: Very rare: Aseptic meningitis.

Probenecid decreases the renal excretion of amoxicillin. Concurrent use with AMOCLA may result in increased and prolonged blood levels of amoxicillin.
The concurrent administration of allopurinol and ampicillin increases the incidence of rashes in patients receiving both drugs as compared to patients receiving ampicillin alone. But it is not known whether this potentiation of ampicillin rash is due to allopurinol or the hyperuricemia present in these patients.
AMOCLA should not be co-administered with disulfiram.
Prolongation of bleeding time and prothrombin time have been reported in some patients receiving AMOCLA.
Thus, this drug should be used with care in patients on anticoagulation therapy.
AMOCLA may reduce the effect of oral contraceptives, and the caution should be given to patients.
Laboratory test interactions: AMOCLA results in high urine concentration. High urine concentration of ampicillin may result in false-positive reactions when testing for the presence of glucose in urine using Clinitest, Benedict or Fehling's solution.

Store in a dry place below 25°C and in a tight container. Protect from light.

Penicillins

J01CR02 - amoxicillin and beta-lactamase inhibitor ; Belongs to the class of penicillin combinations, including beta-lactamase inhibitors. Used in the systemic treatment of infections.

POM