Rosuvastatin

Indications

Rosuvastatin is used for: Hyperlipidaemias, Primary hypercholesterolaemia (heterozygous familial hypercholesterolaemia), mixed dyslipidaemia, homozygous familial hypercholesterolaemia, Stroke prevention

Adult Dose

Oral Hypercholesterolemia, Hypertriglyceridemia, hyperlipidemia, mixed dyslipidemiaProphylaxis of cardiovascular events in high-risk patients Adult: Initially, 5 or 10 mg once daily, may increase dose at 4-wkly intervals to 20 mg daily if necessary. Max: 40 mg once daily. Active liver disease: Use is contraindicated

Child Dose

Oral Child Heterozygous familial hypercholesterolaemia: >10 yr Initially, 5 mg once daily, may be adjusted at intervals of at least 4 wk. Max: 20 mg once daily.

Renal Dose

Renal impairment Severe (CrCl <30 mL/min/1.73m²) and not on hemodialysis: Decrease starting dose to 5 mg PO qDay; not to exceed 10 mg PO qDay CrCl>30mL/min/1.73m²: Dose adjustment not necessary

Administration

May be taken with or without food.

Contra Indications

Severe renal impairment, active liver disease, unexplained persistent elevations of serum transaminases; hypersensitivity. Pregnancy, lactation.

Precautions

Patients w/ predisposing factors for myopathy (e.g. untreated hypothyroidism, renal impairment), history of chronic liver disease and alcoholism. Monitoring Parameters Monitor creatine kinase (CK) periodically and LFT. Discontinue treatment if there is significant or persistent increase in CK levels, serum aminotransferase levels or evidence of myopathy. Lactation Contraindicated

Pregnancy-Lactation

Interactions

May increase serum levels of warfarin and oral contraceptives. May increase serum levels w/ itraconazole, HIV protease inhibitors. May decrease serum levels w/ erythromycin and antacids. May increase risk of myopathy w/ fenofibrate, niacin. Potentially Fatal: Increased risk of rhabdomyolysis w/ gemfibrozil and ciclosporin.

Adverse Effects

Side effects of Rosuvastatin : >10% Myalgia (3-13%) 1-10% Arthralgia (10%),Diabetes mellitus, new onset (3%),Pharyngitis (9%),Headache (6%),Asthenia (up to 5%),Dizziness (4%),CPK increased (3%),Nausea (3%),Abdominal pain (2%),ALT increased (2%),Constipation (2%),Flulike illness (2%),UTI (2%) <1% Jaundice,Myopathy,Rhabdomyolysis Potentially Fatal: Rhabdomyolysis with acute renal failure.

Mechanism of Action

Rosuvastatin is a selective and competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. It increases the number of hepatic LDL receptors on the cell surface, enhancing uptake and catabolism of LDL. It also decreases apolipoprotein B, triglycerides and increases HDL.