It is a HMG-COA reeducates inhibitor also known as strains, the rate limiting enzymes that convert 3-hydroxy-3-methylgutaryl coenzyme A to mevalonate, a cholesterol precursor. It works by two ways, First it increases hepatic LDL receptors on cell surface to enhance uptake and Catabolism of LDL, second by inhibiting hepatic synthesis of VLDL.

The absolute bioavailability of Rosuvastatin is approximately 20 %.

Rosuvastatin was found to be mainly excreted in the faecas (90%) and 10% via urine after. I.V. use 28 % cleares by renal and rest by hepatic route. Terminal half life of drug is 18-20 hrs.

INDICATIONS: Hypercholesterolemia and dyslipidemia.

CONTRAINDICATION: Hypersensitivity to the drug and its metabolites. Severe renal impairment active liver disorder.

SAFETY PROFILE: Liver functions should be monitored before and at 12 week interval following initial therapy.

ADVERSE EFFECTS: Myalgia, constipation, nausea, asthenia, stomachache.

DRUG INTERACTIONS: Cyclosporine and gemfibrozil increase the activity of rosuvastatin, if used concomitantly while antacids reduce the activity. Co administration of oral contraceptives with rosuvastatin results in increase plasma concentration of estradiol and norgestrel.

DOSAGE: Initially 10 mg O.D. Very high cholesterol patients 20 mg O.D. patients with nonresponder to 20 mg: 40 mg (at high cardiovascular risk) cholesterol lowering diet is recommended before and during therapy.