Coklav

Amoxicillin trihydrate, potassium clavulanate.

FC tab: Coklav 625: 1 film-coated tablet contains Amoxicillin 500 mg (as amoxicillin trihydrate) and Clavulanic acid 125 mg (as potassium clavulanate).
Coklav 1000: 1 film-coated tablet contains Amoxicillin 875 mg (as amoxicillin trihydrate) and Clavulanic acid 125 mg (as potassium clavulanate).
Susp: Per 156 mg/5 mL suspension contains Amoxicillin trihydrate equivalent to amoxicillin 125 mg, clavulanate potassium 31 mg.
Per 312 mg/5 mL suspension contains Amoxicillin trihydrate equivalent to Amoxicillin 250 mg, clavulanate potassium 62 mg.

Pharmacology: Pharmacodynamics: Mechanism of Action: Amoxicillin and clavulanate potassium usually is bactericidal in action. Concurrent administration of clavulanic acid does not alter the mechanism of action of amoxicillin. However, because clavulanic acid has a high affinity for and binds to certain β-lactamases that generally inactivate amoxicillin by hydrolyzing its β-lactam ring, concurrent administration of the drug with amoxicillin results in a synergistic bactericidal effect which expands the spectrum of activity of amoxicillin against many strains of β-lactamases-producing bacteria that are resistant to amoxicillin alone.
Clavulanic acid generally acts as an irreversible, competitive inhibitor of β-lactamases. The mechanism by which clavulanic acid binds to and inhibits β-lactamases varies depending on the specific β-lactamase involved. Because clavulanic acid is structurally similar to penicillins and cephalosporins, it initially acts as a competitive inhibitor and binds to the active site on the β-lactamases. An inactive acyl intermediate is then formed but it is only transiently inactive since the intermediate can be hydrolyzed, resulting in restoration of β-lactamases activity and release of clavulanic acid degradation products. With many types of β-lactamases, however, subsequent reactions occur that lead to irreversible inactivation of the β-lactamases.
Pharmacokinetics: Amoxicillin trihydrate and clavulanate potassium are both generally stable in the presence of acidic gastric secretions and are well absorbed following oral administration of amoxicillin and clavulanate potassium. Peak serum concentrations of amoxicillin and clavulanic acid are generally attained within 1-2.5 hours following oral administration of a single dose of conventional preparations of amoxicillin and clavulanate potassium in fasting adults. Following administration of amoxicillin and clavulanate potassium, amoxicillin and clavulanic acid are both distributed into the lungs, pleural fluid, and peritoneal fluid. Low concentrations (i.e., less than 1 mcg/ml) of each drug are attained in sputum and saliva. Amoxicillin and clavulanic acid readily cross the placenta. Amoxicillin and clavulanic acid are distributed into milk in low concentrations. Amoxicillin has an elimination half-life of 1-1.3 hours and clavulanic acid has an elimination half-life of 0.78-1.2 hours. Approximately 50 to 73% of the amoxicillin and approximately 25 to 45% of the clavulanic acid are excreted unchanged in the urine within the 6-8 hours after administration.

FC tab: Amoxicillin/clavulanate is indicated for short-term treatment of bacterial infections at the following sites: Upper respiratory tract infections (including ENT) e.g. tonsillitis, sinusitis, otitis media.
Lower respiratory tract infections e.g. acute exacerbations of chronic bronchitis, lobar and bronchopneumonia.
Genito-urinary tract infections e.g. cystitis, urethritis, pyelonephritis.
Skin and soft tissue infections e.g. boils, abscesses, cellulitis, wound infections.
Bone and joint infections e.g. osteomyelitis.
Dental infections e.g. dentoalveolar abscess.
Other infections e.g. specific abortion, puerperal sepsis, intra-abdominal sepsis.
Susp: For treatment of infections due to Amoxicillin susceptible bacteria including β-lactamase producing bacteria at the following sites: Upper respiratory tract infections eg, tonsillitis, sinusitis, otitis media; lower respiratory tract infections eg, acute and chronic bronchitis, lobar and bronchopneumonia;- genito-urinary tract infections eg, cystitis, urethritis, pyelonephritis, skin and soft-tissue infections eg, boils, abscesses, cellulitis, wound infection, bone and joint infections, dental infections.

FC tab: Coklav 625: Adults and children over 12 years: 1 tablet 2 times a day or every 12 hours.
Children: Children weighing 40 kg or more should be dosed according to the adult recommendations. (See Adults for dosing recommendations.)
Dosage in renal impairment: (see Table).

Click on icon to see table/diagram/image

Coklav 1000: Adults: The Coklav 1000 mg tablet should only be used in patients with a glomerular filtration rate of > 30 ml/min.
Mode of Administration: Amoxicillin and clavulanate potassium is administered orally. Because GI absorption of amoxicillin and clavulanate potassium is not affected by food following oral administration of conventional preparations of the drug, these preparations may be administered orally without regard to meals. However, administration of oral amoxicillin and clavulanate potassium with meals reportedly may minimize adverse GI effects.
Susp: Children 7-12 years old: 2 teaspoons.
Children 2-7 years old: 1 teaspoon.
Children 9 months old to 2 years old: ½ teaspoon.

Gastrointestinal symptoms and disturbance of the fluid and electrolyte balances may be evident. Gastrointestinal symptoms may be treated symptomatically with attention to the water/electrolyte balance.
Amoxicillin crystalluria, in some cases leading to renal failure, has been observed.
Amoxicillin and clavulanate potassium can be removed from the circulation by haemodialysis.

Amoxicillin and clavulanate potassium is contraindicated in patients who are hypersensitive to any penicillin and cephalosporins.
Amoxicillin and clavulanate potassium is contraindicated in patients with a previous history of amoxicillin/clavulanate potassium-associated cholestatic jaundice/hepatic dysfunction.

Prior to initiation of therapy with amoxicillin and clavulanate potassium, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins, or other drugs.
Because a high percentage of patients with infectious mononucleosis have developed rash during therapy with amoxicillin and clavulanate potassium should not be used in patients with disease.
Renal, hepatic and hematologic function should be evaluated periodically during prolonged therapy with amoxicillin and clavulanate potassium. Because Clostridium difficile-associated diarrhea and colitis has been reported with the use of anti-infective agents including amoxicillin and clavulanate potassium, it should be considered in the differential diagnosis of patients who develop diarrhea during amoxicillin and clavulanate potassium therapy.
Susp: Severely impaired liver or renal function. Newborn & infants.

Pregnancy Category B. There are no adequate or controlled studies using amoxicillin and clavulanate potassium in pregnant women and the drug should be used during pregnancy only when clearly needed.
Coklav 1000: As with all medicines, use should be avoid in pregnancy, especially during the first trimester, unless considered essential by the physician.
Because amoxicillin and clavulanic acid are distributed into milk, amoxicillin and clavulanate potassium should be used with caution in nursing women.

>10%: Gastrointestinal: Diarrhea (3% to 34%; incidence varies upon dose and regimen used).
1% to 10%: Dermatologic: Diaper rash, skin rash, urticaria.
Gastrointestinal: Abdominal discomfort, loose stools, nausea, vomiting.
Genitourinary: Vaginitis, vaginal mycosis.
Miscellaneous: Moniliasis.
<1% (Limited to important or life-threatening): Alkaline phosphatase increased, cholestatic jaundice, flatulence, headache, hepatic dysfunction, hepatitis, liver function test increased, prothrombin time increased, thrombocytosis, vasculitis (hypersensitivity).
Susp: Indigestion, transient hepatitis.

Tab: Concomitant administration of amoxicillin and clavulanate potassium and probenecid can decrease the rate of renal tubular secretion of amoxicillin and produces higher and prolonged serum concentrations of amoxicillin.
Concomitant administration of amoxicillin and allopurinol can increase incidence of rash reportedly occurs in patients with hyperuricemia. There are no data to date on concomitant administration of amoxicillin and clavulanate potassium and allopurinol.
Susp: Oral contraceptives & probenecid.

Store in a dry place below 30°C.

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.

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