Crestor

Rosuvastatin Ca

Adjunct to diet when response to diet & exercise is inadequate in patients w/ primary hypercholesterolaemia (type IIa, including heterozygous familial hypercholesterolaemia) or mixed dyslipidaemia (type IIb). Reduction of elevated LDL-C, total cholesterol, triglycerides & Apo B & increase in HDL-C. Adjunct to diet & other lipid-lowering treatment (eg, LDL aphaeresis) in patients w/ HoFH.

Individualized 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 wk, if necessary. Patient w/ severe hypercholesterolaemia at high CV risk (in particular those w/ familial hypercholesterolaemia), who do not achieve the treatment goal on 20 mg, & whom routine follow-up will be performed Max dose: 40 mg. Elderly >70 yr, patient w/ predisposing factors to myopathy & Asian patient Initially 5 mg. Patient w/ severe renal impairment (CrCl <30 mL/min/1.73 m²) not on hemodialysis Initially 5 mg once daily & not to exceed 10 mg once daily. Patient w/ hepatic impairment (Child-Pugh score 8 & 9) Not to exceed 20 mg once daily.

May be taken with or without food.

Hypersensitivity. Active liver disease including unexplained, persistent elevations of serum transaminases & any serum transaminase elevation >3x ULN; myopathy. Concomitant cyclosporin therapy. Women of childbearing potential not using appropriate contraceptive measures. Pregnancy & lactation.

Discontinue therapy in markedly elevated creatinine kinase (>5x ULN) or if muscular symptoms are severe & cause daily discomfort. Discontinue use if myasthenia gravis or ocular myasthenia is induced or aggravated. Discontinue use or reduce dose if serum transaminases level is >3x ULN. Not to be used in any patient w/ acute, serious condition 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). Consider renal function assessment during routine follow-up in patients treated w/ 40 mg dose. Patients who consume excessive quantities of alcohol &/or have a history of liver disease; w/ secondary hypercholesterolemia caused by hypothyroidism or nephrotic syndrome; predisposing factors for myopathy/rhabdomyolysis. Increased HbA1c & serum glucose level in patients at high risk for developing diabetes. Asian patients. Patients should be advised to report promptly any inexplicable muscle pain, weakness or cramps, particularly if associated w/ malaise or fever. Renal impairment, hypothyroidism, personal or family history of hereditary muscular disorders, previous history of muscular toxicity w/ another HMG-CoA reductase inhibitor or fibrate, alcohol abuse, situations where an increase in plasma levels may occur, concomitant use of fibrates. Perform LFTs prior to initiation of therapy & 3 mth later. Additional neuromuscular & serologic testing may be necessary. LFTs should be carried out prior to, & 3 mth following, the initiation of treatment. May affect ability to drive & use machines. Not recommended in paed use.

DM; headache, dizziness; constipation, nausea, abdominal pain; myalgia; asthenia. DRESS, lichenoid drug eruption.

Increased plasma conc & risk of myopathy w/ inhibitors of OATP1B1 & BCRP transporters. Increased exposure w/ PIs. Increased C_max and AUC w/ gemfibrozil. Increased risk of myopathy w/ gemfibrozil, fenofibrate, other fibrates & niacin. Increased AUC w/ ezetimibe in hypercholesterolaemic subjects. Decreased plasma conc w/ antacid susp containing Al & Mg hydroxide. Decreased AUC & C_max w/ erythromycin. Increased AUC w/ sofosbuvir/velpatasvir/voxilaprevir, voxilaprevir, ciclosporin, darolutamide, regorafenib, atanazavir/ritonavir, simeprevir, velpatasvir, ombitasvir/paritaprevir/ritonavir/dasabuvir, teriflunomide, grazoprevir/elbasvir, glecaprevir/pibrentasvir, lopinavir/ritonavir, capmatinib, clopidogrel, fostamatinib, febuxostat, gemfibrozil, eltrombopag, darunavir/ritonavir, tipranavir/ritonavir, dronedarone, itraconazole, ezetimibe. Decreased AUC w/ erythromycin, baicalin. May either increase or decrease INR w/ vit K antagonists (eg, warfarin or another coumarin anticoagulant). Increased AUC of ethinyl estradiol & norgestrel. Increased exposure in patients known to have the c.521CC or c.421AA genotype.

Dyslipidaemic Agents

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

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