Rosuvastatin


Full Prescribing Info
Dosage/Direction for Use

Oral
Hypercholesterolaemia
Adult: Dosage is individualised based on treatment goals, patient response and clinical practice guidelines. Initially, 5 or 10 mg once daily; may increase after 4 weeks if necessary. Usual Max: 20 mg once daily; a Max of 40 mg once daily may be used only in patients with severe hypercholesterolaemia at high CV risk who do not achieve the target cholesterol concentration at lower doses and who do not have risk factors for adverse effects. Patients with homozygous familial hypercholesterolaemia may be started on 20 mg once daily. Dosage may be increased at intervals of 2-4 weeks.
Child: Heterozygous familial hypercholesterolaemia: Initially, 5 mg once daily. Usual dose range: 6-9 years
5-10 mg once daily; 10-17 years 5-20 mg once daily. Familial homozygous hypercholesterolaemia: 6-17 years Initially, 5 or 10 mg once daily, depending on age, weight and prior statin use, may titrate dose up to Max of 20 mg once daily according to individual response and tolerability, and depending on treatment recommendations.
Elderly: >70 years Initially, 5 mg once daily.
Renal impairment:
CrCl (ml/min)Dosage Recommendation
<30 Contraindicated.
30-60Initially, 5 mg once daily (Max: 20 mg once daily).
Hepatic impairment: Active liver disease: Contraindicated.

Oral
Mixed dyslipidaemia
Adult: Dosage is individualised based on treatment goals, patient response and clinical practice guidelines. Initially, 5 or 10 mg once daily; may increase after 4 weeks if necessary. Usual Max: 20 mg once daily; a Max of 40 mg once daily may be used only in patients with severe hypercholesterolaemia at high CV risk who do not achieve the target cholesterol concentration at lower doses and who do not have risk factors for adverse effects. Patients with homozygous familial hypercholesterolaemia may be started on 20 mg once daily. Dosage may be increased at intervals of 2-4 weeks.
Child: Heterozygous familial hypercholesterolaemia: Initially, 5 mg once daily. Usual dose range: 6-9 years
5-10 mg once daily; 10-17 years 5-20 mg once daily. Familial homozygous hypercholesterolaemia: 6-17 years Initially, 5 or 10 mg once daily, depending on age, weight and prior statin use, may titrate dose up to Max of 20 mg once daily according to individual response and tolerability, and depending on treatment recommendations.
Elderly: >70 years Initially, 5 mg once daily.
Renal impairment:
CrCl (ml/min)Dosage Recommendation
<30 Contraindicated.
30-60Initially, 5 mg once daily (Max: 20 mg once daily).
Hepatic impairment: Active liver disease: Contraindicated.

Oral
Prophylaxis of cardiovascular events in high-risk patients
Adult: 20 mg once daily.
Elderly: >70 years
Initially, 5 mg once daily.
Renal impairment:
CrCl (ml/min)Dosage Recommendation
<30 Contraindicated.
30-60Initially, 5 mg once daily (Max: 20 mg once daily).
Hepatic impairment: Active liver disease: Contraindicated.

Special Populations: Patients of Asian ancestry; those with predisposing factors to myopathy (e.g. hypothyroidism, personal or familial history of hereditary muscular disorders; alcohol abuse): Initially, 5 mg once daily. 40 mg dose is contraindicated. Patients receiving concomitant therapy: Ciclosporin: Avoid use. If use cannot be avoided, Max rosuvastatin dose is 5 mg once daily. Gemfibrozil: Avoid use. If use cannot be avoided, initiate rosuvastatin at 5 mg once daily. Max: 10 mg once daily. Atazanavir/ritonavir, lopinavir/ritonavir, or simeprevir: Initiate rosuvastatin at 5 mg once daily. Max: 10 mg once daily.
Administration
May be taken with or without food.
Contraindications
Active liver disease, including unexplained, persistent elevations of serum transaminases; myopathy. Severe renal impairment (CrCl <30 mL/min). Pregnancy and lactation.
Special Precautions
Patient with hypothyroidism; history of hereditary muscular disorders or muscular toxicity with another HMG-CoA reductase inhibitor or fibrates; excessive alcohol consumption, history of liver disease, severe respiratory failure. Patients of Asian ancestry, those with predisposing factors to myopathy or those taking concomitant ciclosporin, gemfibrozil, atazanavir/ritonavir, lopinavir/ritonavir, or simeprevir. Patient with SLCO1B1 and ABCG2 polymorphism. Moderate renal impairment (CrCl 30-60 mL/min). Children and elderly. Monitoring Parameters Obtain lipid panel (HDL, LDL, total cholesterol, triglycerides) prior to therapy, then every 4-12 weeks after initial therapy and every 3-12 months thereafter; LFT prior to therapy and as needed thereafter; creatine phosphokinase when myopathy is considered or in high-risk patients.
Adverse Reactions
Significant: Myopathy, myalgia, diabetes mellitus, haematuria, proteinuria, interstitial lung disease, liver enzyme abnormalities, increased creatine phosphokinase levels. Blood and lymphatic system disorders: Rarely, thrombocytopenia. Gastrointestinal disorders: Abdominal pain, constipation, nausea. General disorders and administration site conditions: Asthenia. Hepatobiliary disorders: Rarely, pancreatitis, hepatitis, jaundice. Immune system disorders: Hypersensitivity (e.g. angioedema). Musculoskeletal and connective tissue disorders: Rarely, arthralgia, muscle rupture, Lupus-like syndrome. Nervous system disorders: Dizziness, headache, peripheral neuropathy. Psychiatric disorders: Depression, sleep disorders (e.g. insomnia, nightmares). Reproductive system and breast disorders: Rarely, gynaecomastia. Skin and subcutaneous tissue disorders: Pruritus, rash, urticaria.
Potentially Fatal: Rarely, rhabdomyolysis with acute renal failure secondary to myoglobinuria, hepatic failure.
Drug Interactions
Increased exposure with certain protease inhibitors (e.g. ritonavir-boosted regimens, simeprevir), gemfibrozil, ezetimibe, ciclosporin, colchicine. Decreased plasma concentration with Al- and Mg-containing antacids, erythromycin. May increase INR when given with vit K antagonists (e.g. warfarin). May increase the plasma concentration of oral contraceptives. May increase risk of myopathy with concurrent use of strong CYP3A4 inhibitors (e.g. clarithromycin, itraconazole), fenofibrate, nicotinic acid.
Action
Rosuvastatin selectively and competitively inhibits 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis. It increases the number of hepatic LDL receptors on the cell surface, thereby enhancing the uptake and catabolism of LDL. It also decreases apolipoprotein B, triglyceride and increases HDL concentrations.
Onset: Within 1 week.
Absorption: Incompletely absorbed from the gastrointestinal tract. Time to peak plasma concentration: 3-5 hours. Bioavailability: Approx 20%.
Distribution: Enters breast milk. Volume of distribution: 134 L. Plasma protein binding: Approx 90%, mainly to albumin.
Metabolism: Limited metabolism in the liver via CYP2C9 isoenzyme into N-desmethyl (approx 50% less active) and lactone metabolites (inactive).
Excretion: Via faeces (approx 90%, mainly as unchanged drug); urine (approx 5%, as unchanged drug). Elimination half-life: Approx 19 hours.
Storage
Oral: Store between 20-25°C. Protect from moisture.
ATC Classification
C10AA07 - rosuvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
Disclaimer: This information is independently developed by CIMS based on rosuvastatin from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2021 CIMS. All rights reserved. Powered by CIMSAsia.com
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