Brand Name: ROVALIP
Generic Name: Rosuvastatin
Preparations: 5/ 10/ 20 mg Tablets
Pharmacological Category: HMG-CoA reductase inhibitor
Mechanism of Action (MOA)
ROVALIP (Rosuvastatin) is a competitive inhibitor of HMG-CoA reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. Decreased hepatic cholesterol concentrations stimulate the upregulation of hepatic low density lipoprotein (LDL) receptors which increases hepatic uptake of LDL.
ROVALIP also inhibits hepatic synthesis of very low density lipoprotein (VLDL). The overall effect is a decrease in plasma LDL and VLDL.
Pharmacokinetics
Absorption: Absorbed from Gastrointestinal tract
Bioavailability: About 20%
Peak Plasma Concentration: About 5 hours
Metabolism: Limited by cytochrome P450 isoenzyme CYP2C9
Protein Binding: About 90%
Half-life Elimination: About 19 hours
Excretion: Faeces (about 90%); urine (remaining)
Indications and Dosage
• Hyperlipidaemias
• Primary hypercholesterolaemia (type IIa)
• Mixed dyslipidaemia (type IIb)
• Hypertriglyceridaemia (type IV)
• Atherosclerosis
Usual initial dose: 5 or 10 mg once daily, depending on plasma-cholesterol concentrations, cardiovascular risk factors, and risk factors for adverse effects
Maintenance dose: 5 to 40 mg once daily, although the 40-mg dose is reserved for patients with high cardiovascular risk who do not achieve their target cholesterol concentration at lower doses and who do not have risk factors for adverse effects.
Renal impairment
Creatinine clearance 30 to 60 mL/minute: initial dose of 5 mg once daily and a maximum dose of 20 mg once daily
Creatinine clearance below 30 mL/minute: contraindicated
Side Effects
COMMON: gastrointestinal disturbances
Other: headache, skin rashes, dizziness, blurred vision, insomnia, and dysgeusia.
REPORTED: hepatitis and pancreatitis. Myopathy, characterized by myalgia and muscle weakness and associated with increased creatine phosphokinase concentrations, has been reported, especially in patients also taking ciclosporin, fibric acid derivatives, or nicotinic acid.
RARE: rhabdomyolysis
Hypersensitivity reactions including anaphylaxis and angioedema have also occurred.
Contraindications
Active liver disease, unexplained persistently raised serum-aminotransferase concentrations, pregnancy
Warnings/ Precautions
• Reversible increase in serum-aminotransferase concentrations may occur and liver function should be monitored.
• Should be stopped if marked or persistent increase in serum-aminotransferase concentrations occurs.
• Caution in patients at risk of rhabdomyolysis, and particularly in patients taking drugs that increase plasma concentrations of the statin; the statin should be stopped if creatine phosphokinase increases significantly or if myopathy is diagnosed.
Drug Interactions
• Increased plasma-rosuvastatin concentrations have been reported with cyclosporin, HIV protease inhibitors, and such combinations should be avoided. If they must be given together, lower doses of rosuvastatin should be used.
• It increases INR in patient taking coumarin anticoagulants.
• Myopathy has been reported when rosuvastatin is used along with colchicine.
Pregnancy Category: X
Presentations
ROVALIP 5: 5 X 10’ s
ROVALIP 10: 10 X 10’ s
ROVALIP 20: 5 X 10’ s
