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CeruvinCERUVIN
(Clopidogrel 75 mg Tablets)

COMPOSITION
CERUVIN TABLETS

Each film-coated tablet contains:

Clopidogrel bisulphate

equivalent to Clopidogrel ....... 75 mg

PRODUCT DESCRIPTION
Pink coloured, round, film-coated tablets with 'C4' debossed on one side and plain on the other side.

DESCRIPTION
CERUVIN TABLETS contain clopidogrel bisulphate. Clopidogrel inhibits platelet aggregation. It is a thienopyridine derivative which is chemically related to ticlopidine. It is chemically designated as methyl (+)-(S)-α-(2-chlorophenyl)-6, 7-dihydrothieno [3, 2-c] pyridine-5(4H)-acetate sulphate (1:1). The empirical formula of clopidogrel bisulphate is C16H16CINO2SH2SO4 and its molecular weight is 419.9. The structural formula of clopidogrel bisulphate is given below

Ceruvin

PHARMACOLOGY
Mechanism of Action
Clopidogrel is a thienopyridine derivative which inhibits platelet aggregation. In people with established atherosclerosis, the incidence of morbid events (such as unstable angina, myocardial infarction, stroke, transient ischemic attacks, or the need for vascular bypass or angioplasty) has been shown to decrease with the use of drugs inhibiting platelet function. This demonstrates the involvement of platelets in the initiation and/or evolution of such events, and that inhibition of platelet aggregation can reduce the morbidity rate.

Pharmacokinetics
Absorption: The absorption of clopidogrel is rapid but incomplete after oral administration; absorption appears to be at least 50%. Intake of food does not significantly modify the bioavailability of clopidogrel.

The plasma levels of the parent compound are low and fall below the quantification limit beyond 2 hours after dosing, even after repeated 75 mg doses of clopidogrel.

Metabolism: Clopidogrel is a prodrug which is extensively metabolized by liver. The main circulating metabolite is a carboxylic acid derivative (inactive) which accounts for approximately 85% of the circulating drug-related compounds in plasma. Peak plasma concentration of the carboxylic acid derivative is approximately 3 mg per liter, achieved about 1 hour after dosing (on repeated doses of 75 mg). Thiol derivative is the active metabolite but has not been identified in plasma.

The glucuronide derivative of the carboxylic acid metabolite is also observed in plasma and urine.

The pharmacokinetics of the main circulating metabolite are linear in the dose range of 50 to 150 mg.

Clopidogrel and it carboxylic acid derivative have very high protein binding (98% and 94%, respectively). The binding is nonsaturable in vitro up to a concentration of 100 g/mL.

Elimination: Both urine and faeces are involved in the excretion of clopidogrel. After both single and repeated administration, the elimination half-life of the main circulating metabolite has been seen to be 8 hours. 2% of radiolabelled drug binds to platelets by covalent bond, which accounted for a half-life of 11 days.

Special Populations
Geriatric:
As compared to young healthy volunteers, the plasma concentrations of the carboxylic acid derivative are significantly higher in elderly (≥75 years). However, the higher plasma levels have not led to differences in platelet aggregation and bleeding time. Dosage adjustment is not required in the elderly patients.

Renal Insufficiency:
After repeated doses of 75 mg/day, plasma levels of carboxylic acid derivative have been found to be lower in patients with severe renal impairment [Creatinine clearance (CCr) 5 -15 mL/min] than in subjects with moderate renal impairment (CCr 30 - 60 mL/min) or healthy subjects. Although inhibition of ADP-induced platelet aggregation have been found to be lower (25%) compared to that reported in healthy subjects, the prolongation of bleeding time have been found to be similar compared to that of healthy subjects receiving 75 mg/day clopidogrel.

Gender:
The plasma concentration of the carboxylic acid derivative (main circulating metabolite) does not show significant difference between males and females. The incidence of clinical effects, undesirable events and abnormal laboratory values has been found to be comparable in both men and women.

Race:
Difference in pharmacokinetic properties of clopidogrel has not been reported in different races.

INDICATIONS
CERUVIN (clopidogrel 75 mg tablets) is indicated for prevention of atherothrombotic events in patients suffering from
Myocardial infarction (from a few days until < 35 days),
Ischemic stroke (from 7 days until < 6 months) or established peripheral arterial disease;
Non-ST segment elevation acute coronary syndrome (unstable angina or non-Q-wave myocardial infarction) in combination with Acetylsalicylic Acid (ASA).

DOSAGE AND ADMINISTRATION
MI, Ischaemic stroke or peripheral artery disease:
The recommended daily dose of CERUVIN (clopidogrel 75 mg tablets) is 75 mg as a single daily dose with or without food.

Non-ST segment elevation acute coronary syndrome (unstable angina or non-Q-wave myocardial infarction) in combination with Acetylsalicylic Acid (ASA)

CERUVIN (clopidogrel 75 mg tablets) treatment should be initiated with a single 300-mg loading dose and then continued at 75 mg once a day (with ASA 75-325 mg daily).

Since higher doses of ASA were associated with higher bleeding risk, it is recommended that the dose of ASA should not be > 100 mg. The optimal duration of treatment has not been formally established. Use up to 12 months has been studied and the maximum benefit is seen at 3 months.

Dosage in Children and Adolescent:
Safety and efficacy in subjects below the age of 18 have not been established.

Dosage in Elderly Patients:
No dosage adjustment is required for elderly patients.

Dosage in Patients with Renal Impairment:
No dosage adjustment is required.
However, experience is limited in patients with severe renal impairment. CERUVIN (clopidogrel) should be used with caution in this population.

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