ROSLOY ASP
Composition Rosuvastatin 20/10 mg+ Aspirin 150/ 75 mg Capsules
Indication Hyperlipidaemia,Prophylaxis of ischaemic events,Acute coronary syndrome
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. Aspirin inhibits the formation of thromboxane A2 in the platelets. This inhibits platelet aggregation and coagulation. This action lasts until the enzyme cyclo-oxygenase is regenerated in the platelets.

Pharmacokinetic's

Rosuvastatin:

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.

Aspirin: Rapid absorption (oral).

Distribution: Aspirin: Widely distributed; Protein binding: 80-90%.

Metabolism: Aspirin: Hydrolysed to salicylate in the gut wall; salicylate metabolised hepatically.

Excretion: Aspirin: Via urine by glomerular filtration, active renal tubular secretion and passive tubular reabsorption; haemodialysis (as salicylate); 15-20 minutes (elimination half-life, parent drug).

Side effects

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.

Precaution

Rosuvastatin: 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.

Dosage

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. Tablet; maintenance: 1 tablet/day.