10 mg Film-Coated Tablet
ANTIHYPERCHOLESTEROLEMIA / ANTIDYSLIPIDAEMIA

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Each film-coated tablet contains:
Rosuvastatin (as calcium) ................................................................... 10 mg

PRODUCT DESCRIPTION:
Light pink, circular, slightly biconvex film coated tablet plain on both sides.

PHARMACOLOGICAL ACTION:
Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol (total C), LDL-C, ApoB, and
nonHDL-C (total cholesterol minus HDL-C) in patients with homozygous and heterozygous familial hypercholesterolemia, nonfamilial forms of hypercholesterolemia, and mixed dyslipidemia. Rosuvastatin also reduces TG and produces increases in HDL-C. Rosuvastatin reduces total-C, LDL-C, VLDL-cholesterol (VLDL-C), ApoB, nonHDL-C and TG, and increases

HDL-C in patients with isolated hypertriglyceridemia. The effect of Rosuvastatin on cardiovascular morbidity and mortality has not been determined.

PHARMACODYNAMIC PROPERTIES:
Pharmacotherapeutic group: HMG-CoA reductase inhibitors.

Mechanism of action
Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor for cholesterol. The primary site of action of
Rosuvastatin is the liver, the target organ for cholesterol lowering.
Rosuvastatin increases the number of hepatic LDL receptors on the cell-surface, enhancing uptake and catabolism of LDL and it inhibits the hepatic synthesis of VLDL, thereby reducing the total number of VLDL and LDL particles.

PHARMACOKINETICS:
Absorption: The absolute bioavailability of Rosuvastatin is approximately 20%. Plasma concentrations of Rosuvastatin do not differ following evening or morning drug administration. Significant LDL-C reductions are seen
when Rosuvastatin is given with or without food, and regardless of the time of day of drug administration.
Distribution: Mean volume of distribution at steady-state of Rosuvastatin is approximately 134 liters. Rosuvastatin is 88% bound to plasma proteins. This binding is reversible and independent of plasma concentrations.
Metabolism: Rosuvastatin is not extensively metabolized, approximately 10% of a radio labeled dose is recovered as metabolite. The major metabolite is N-desmethyl Rosuvastatin, which is formed principally by cytochrome P450 2C9, and in vitro studies have demonstrated that N-desmethyl Rosuvastatin has approximately one-sixth to onehalf the HMG-CoA reductase inhibitory activity of Rosuvastatin.
Excretion: Following oral administration, Rosuvastatin and its metabolites are primarily excreted in the feces (90%). The elimination half-life of Rosuvastatin is approximately 19 hours.