Apo-Rosuvastatin

Patients w/ primary hypercholesterolaemia & mixed dyslipidaemia (including Fredrickson type IIa, IIb) as an adjunct to diet when response to diet & exercise is inadequate. Patients w/ primary dysbetalipoproteinaemia (Fredrickson type III hyperlipoproteinaemia) as an adjunct to diet when response to diet & exercise is inadequate. Reduces elevated LDL-C, total cholesterol (total-C) & triglycerides & increases HDL-C. Lowers Apo B, nonHDL-C, VLDL-C, LDL-C/HDL-C, total-C/HDL-C, nonHDL-C/HDL-C, Apo B/Apo A-I rations; increases Apo A-I. Patients w/ homozygous familial hypercholesterolaemia, either alone or as an adjunct to diet & other lipid-lowering treatments (eg, LDL apheresis). Primary prevention of CV disease (reduces risk of stroke, MI & arterial revascularization procedures). Reduction of total-C, LDL-C & Apo B levels in childn & adolescents 10-17 yr as an adjunct to diet.

Statin-naive patient or those who switched from another HMG-CoA reductase inhibitor Initially 5 or 10 mg once daily. May be increased to the next dose level after 4-6 wk, if necessary. Patient w/ severe hypercholesterolaemia at high CV risk May be increased to 40 mg. Asian patient Initially 5 mg once daily. Childn Initially 5 mg once daily. Max daily dose: 10 mg. Adjustments should be made at ≥4 wk intervals. Patient w/ c.521CC or c.421AA genotype Max: 20 mg once daily. In combination w/ fibrates or niacin (≥1 g daily) Max: 10 mg daily.

May be taken with or without food.

Hypersensitivity. Active liver disease or unexplained, persistent elevations of serum transaminases. Patients receiving concomitant cyclosporin. Severe renal impairment (CrCl <30 mL/min). Women of child-bearing potential not using appropriate contraceptive measures. Pregnancy & lactation.

Periodically re-evaluate long-term risk/benefit for patients using doses >20 mg. Asian subjects including Japanese, Chinese, Malay & Indian ancestry. Reported to induce de novo or aggravate pre-existing myasthenia gravis or ocular myasthenia; discontinue use in case of aggravation of symptoms; reported recurrences when same or different statin was re-administered. Consider dose reduction in patients w/ unexplained, persistent proteinuria during routine urinalysis testing. Assess renal function during routine follow-up of patients treated w/ 40 mg dose. Skeletal muscle effects (eg, myalgia, myopathy & rarely, rhabdomyolysis; immune-mediated necrotising myopathy). DM; possible increase in HbA1c & serum glucose levels. Do not start treatment if creatinine kinase (CK) levels are significantly elevated at baseline (>10x ULN). Predisposing factors for myopathy/rhabdomyolysis [eg, renal impairment, hypothyroidism, hereditary muscular disorders (personal or family history), history of muscular toxicity w/ other HMG-CoA reductase inhibitor, fibrate or niacin, alcohol abuse, elderly ≥65 yr, situations where increased plasma levels occur & concomitant use of fibrate or niacin]. Treat underlying disease prior to initiating therapy in patients w/ secondary hypercholesterolaemia caused by hypothyroidism or nephrotic syndrome. Instruct patients to immediately report inexplicable muscle pain, weakness or cramps particularly if associated w/ malaise or fever. Discontinue use if CK levels are markedly elevated (>10x ULN) or muscular symptoms are severe & cause daily discomfort (even if CK levels ≤10x ULN). Increased incidence of myositis & myopathy in patients receiving other HMG-CoA reductase inhibitors w/ fibric acid derivates including gemfibrozil, cyclosporin, nicotinic acid, azole antifungals, PIs & macrolide antibiotics. Temporarily w/hold in 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). Excessive alcohol consumption &/or history of liver disease. Perform LFTs before & 3 mth following treatment initiation & any dose increase & periodically (semi-annually) thereafter. Discontinue or reduce dose if serum transaminases level >3 ULN. Concomitant use w/ certain PIs is not recommended unless rosuvastatin dose is adjusted. Increased systemic exposure in patients w/ moderate hepatic impairment (Child-Pugh scores 8 or 9). Dizziness may affect ability to drive or use machines. Use is limited to 1 yr period in childn & adolescents 10-17 yr.

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

Increased plasma conc & risk of myopathy w/ transporter protein inhibitors. Increased AUC_(0-t) w/ cyclosporin. May strongly increase exposure w/ PIs. Increased C_max, AUC_(0-t) & risk of myopathy w/ gemfibrozil. Increased risk of myopathy w/ fenofibrate, other fibrates & lipid-lowering doses of niacin (≥1 g daily); ticagrelor. Decreased plasma conc w/ antacid susp containing Al & Mg hydroxide. Decreased AUC_(0-t) & C_max w/ erythromycin. Increased INR w/ warfarin. Increased AUC of OC (ethinyl oestradiol & norgestrel). Not recommended in combination w/ fusidic acid; reported muscle-related events including rhabdomyolysis. Concomitant use w/ drugs that may decrease levels or activity of endogenous steroid hormones (eg, ketoconazole, spironolactone, cimetidine).

Dyslipidaemic Agents

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

POM