Crestor

Rosuvastatin Ca

Primary hypercholesterolaemia & mixed dyslipidaemia (including Fredrickson type IIa, IIb & heterozygous familial hypercholesterolaemia) as an adjunct to diet when response to diet & exercise is inadequate. Primary dysbetalipoproteinaemia (Fredrickson type III hyperlipoproteinaemia) as an adjunct to diet when response to diet & exercise is inadequate. Reduction of elevated LDL-C, total-C, triglycerides & increase of HDL-C. Reduction of ApoB, nonHDL-C, VLDL-C, VLDL-TG, LDL-C/HDL-C, total-C/HDL-C, nonHDL-C/HDL-C, ApoB/ApoA-I ratios & increase of ApoA-I. HoFH, either alone or as an adjunct to diet & other lipid-lowering treatments (eg, LDL apheresis). Primary prevention of CV disease; reduce risk of stroke, MI & arterial revascularization procedures. Reduction of total-C, LDL-C & ApoB levels in childn & adolescents 10-17 yr as an adjunct to diet.

Individualised dosage. Initially 5 or 10 mg once daily in both statin-naive patients or patients switched from another HMG-CoA reductase inhibitor. May be adjusted to the next dose level after 4-6 wk if necessary. Severe hypercholesterolaemia at high CV risk May increase to 40 mg. Asian patient Consider initiation of therapy w/ 5 mg once daily. Patient w/ c.521CC or c.421AA genotype Max: 20 mg daily. Childn w/ heterozygous familial hypercholesterolaemia Initially 5 mg once daily. Max: 10 mg daily. Adjustments should be made at ≥4-wk intervals.

May be taken with or without food.

Hypersensitivity. Active liver disease or unexplained, persistent elevations of serum transaminases. Concomitant cyclosporin therapy. Severe renal impairment (CrCl <30 mL/min).

Closely supervise initiation of doses >20 mg; periodically re-evaluate the long-term risk/benefit for individual patient. Increased exposure in Asian patients. Consider dose reduction in patients w/ unexplained persistent proteinuria during routine urinalysis. Recommended to assess renal function during routine follow-up in patients treated w/ 40 mg dose. Possible skeletal muscle effects (eg, myalgia, myopathy, rhabdomyolysis). Additional neuromuscular & serologic testing may be necessary in case of immune-mediated necrotising myopathy; treatment w/ immunosuppressants may be required. May induce or aggravate myasthenia gravis or ocular myasthenia; use w/ caution in patients w/ these conditions & discontinue if they are induced or aggravated. Do not measure creatine kinase (CK) following strenuous exercise or in presence of plausible alternative cause of increased CK. Predisposing factors for myopathy/rhabdomyolysis (eg, renal impairment, hypothyroidism, personal or family history of hereditary muscular disorders, history of muscular toxicity w/ other HMG-CoA reductase inhibitors, fibrates or niacin, alcohol abuse, age ≥65 yr, situations where increased plasma levels may occur & concomitant use of fibrates or niacin). Measure CK levels in patients w/ inexplicable muscle pain, weakness or cramps particularly if associated w/ malaise or fever. Increased risk of myositis & myopathy in patients receiving other HMG-CoA reductase inhibitors w/ fibric acid derivatives including gemfibrozil, cyclosporin, nicotinic acid, azole antifungals, PIs & macrolides. Dose should not exceed 10 mg daily when used in combination w/ fibrates or lipid-lowering doses of niacin (≥1 g daily). Temporarily w/hold in patients w/ acute serious conditions suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis, hypotension, major surgery, trauma, severe metabolic, endocrine & electrolyte disorders; or uncontrolled seizures). Possible increased HbA1c & serum glucose levels; may exceed threshold for DM diagnosis. Patients who consume excessive quantities of alcohol &/or have history of liver disease. Perform LFTs before & at 3 mth following both initiation of treatment & any increase of dose & periodically (semi-annually) thereafter. Monitor patients w/ increased transaminases level until abnormalities resolve; discontinue use or reduce dose if serum transaminases level is >3 ULN. Concomitant use w/ PIs. Moderate & severe hepatic impairment. Dizziness may occur when driving vehicles or operating machines. Not recommended for use in pregnant & breastfeeding women; discontinue as soon as pregnancy is recognized but consider benefit risk in patients w/ very high risk of CV events. Childn & adolescents 10-17 yr; evaluation of linear growth, wt, BMI & secondary characteristics of sexual maturation by Tanner staging is limited to 1 yr. Doses >20 mg in paed population; treatment experience in paed patients w/ heterozygous familial hypercholesterolaemia is limited to 52 wk.

Headache, myalgia, asthenia, constipation, dizziness, nausea, abdominal pain, DM.

May increase plasma conc & risk of myopathy w/ hepatic uptake transporter OATP1B1 & efflux transporter BCRP inhibitors. Increased steady-state AUC_(0-t) w/ cyclosporin. Exposure may be strongly increased by PIs. Increased C_max & AUC_(0-t) w/ gemfibrozil. Increased risk of myopathy w/ gemfibrozil, fenofibrate, other fibrates & lipid-lowering doses of niacin (≥1 g/day). Decreased plasma conc w/ Al- & Mg-containing antacids. Decreased AUC_(0-t) & C_max w/ erythromycin. May increase INR when co-administered w/ warfarin. Increased AUC of ethinyl oestradiol & norgestrel. Concomitant use w/ drugs that may decrease endogenous steroid hormone levels or activity (eg, ketoconazole, spironolactone, cimetidine). Possible muscle-related events including rhabdomyolysis w/ fusidic acid.

Dyslipidaemic Agents

C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.

POM