|Composition||Rosuvastatin 20/10/5 mg tablets|
|Mechanism of Action||
Rosuvastatin is a selective and competitive inhibitor of HMG-coareductase, 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
Absorption: Incompletely absorbed from the GI tract. Time to peak plasma concentration: Approx. 5 hr. Absolute bioavailability: Approx. 20%.
Distribution: Volume of distribution: 134 L. Plasma protein binding: Approx 90%.
Metabolism: Limited metabolism via CYP2C9 isoenzyme.
Excretion: Via faeces (approx. 90%); urine (approx. 5% as unchanged drug). Elimination half-life: Approx. 19 hr.
Headache, dizziness, constipation, nausea, vomiting, abdominal pain, myalgia, chest pain, peripheral oedema, depression, insomnia, rash, paraesthesia, asthenia, abnormal LFT, elevated serum transaminase levels. Potentially Fatal: Severe rhabdomyolysis w/ acute renal failure. Hepatitis, pancreatitis. Rare: Stevens-Johnson syndrome, anaphylaxis, toxic epidermal necrolysis.
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.
Adult: PO Hyperlipidaemias; Prophylaxis of CV events in high-risk patients Initial: 5 or 10 mg/day, may increase at 4-wk intervals to 20 mg/day if needed. Max: 40 mg/day.