Rosuvastatin

It 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.

Indications

Primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia) or mixed dyslipidaemia (type IIb), including familial hypercolesterolaemia.

Dosage

The recommended starting dose is 10mg orally once daily. A dose adjustment to 20mg can be made after 4 weeks .

Contra-Indications

Severe renal impairment, active liver disease, hypersensitivity to rosuvastatin, myopathy, cyclosporin, pregnancy and lactation .

Side Effects

Headache, dizziness, constipation, nausea, abdominal pain, myalgia and asthenia.

Drug Interactions

Cyclosporin, warfarin, gemfibrozil, erythromycin, antacids, oral contraceptive/hormone replacement therapy (HRT).