CRESTOR 20/MG FC TAB 28/FC TAB

Indications

Approved Uses

Adjunct to diet to reduce elevated total-C, LDL-C, ApoB, non-HDL-C and TG and to increase HDL-C in adults with primary hyperlipidemia (including heterozygous familial hypercholesterolemia) and mixed dyslipidemia; adjunct to diet for hypertriglyceridemia; adjunct to diet for primary dysbetalipoproteinemia (Type III); to reduce LDL-C, total-C and ApoB in adults with homozygous familial hypercholesterolemia; to slow the progression of atherosclerosis; and to reduce the risk of myocardial infarction, stroke, and arterial revascularization in adults without clinically evident coronary heart disease but with increased cardiovascular risk (e.g., elevated hs-CRP and other risk factors).

Off-Label Uses

No widely endorsed off-label indications; rosuvastatin has been studied in NAFLD/NASH and CKD-related dyslipidemia, but these are not standard guideline-supported indications.

Dosage & Administration

Dosing by Condition

Primary hyperlipidemia/mixed dyslipidemia: 5-10 mg once daily initially (or 10-20 mg if greater LDL-C reduction needed), titrate to 5-20 mg; max 40 mg/day (restricted use). Homozygous familial hypercholesterolemia: 20 mg once daily initially; max 40 mg/day. Hypertriglyceridemia/Type III dysbetalipoproteinemia: 5-10 mg once daily initially, titrate; max 40 mg/day. Cardiovascular risk reduction (primary prevention in high-risk patients): 20 mg once daily.

Initial Dose

5-10mg once daily (10-20mg once daily for patients with markedly elevated LDL or high cardiovascular risk)

Maintenance Dose

5-40mg once daily, adjusted at 4-week intervals based on lipid response

Maximum Dose

40mg once daily.

Children's Dosage

Heterozygous Familial Hypercholesterolemia (HeFH): ages 8 to <10 years: 5-10 mg orally once daily; ages 10-17 years: 5-20 mg orally once daily. Homozygous Familial Hypercholesterolemia (HoFH): ages 7-17 years: 20 mg orally once daily.

Dose Adjustment Notes

Titrate at intervals of ≥4 weeks; consider 5 mg starting dose in Asian patients; severe renal impairment (CrCl <30 mL/min/1.73 m², not on hemodialysis): start 5 mg once daily and do not exceed 10 mg/day; with cyclosporine: limit rosuvastatin to 5 mg/day (avoid high exposure); with gemfibrozil: avoid if possible-if used, initiate 5 mg and do not exceed 10 mg/day; with certain HIV protease inhibitor regimens (e.g., atazanavir/ritonavir, lopinavir/ritonavir): do not exceed 10 mg/day; 40 mg dose only for patients not at goal on 20 mg and without predisposing risk factors for myopathy.

How to Take

Swallow tablet whole with water. Can be taken at any time of day, with or without food. Take at the same time each day for consistency

Side Effects

Common Side Effects

Headache, myalgia, abdominal pain, asthenia (weakness), nausea, constipation.

Side Effect Frequency

Common (1-10%): headache, dizziness, constipation, nausea, abdominal pain, myalgia, asthenia; Uncommon (0.1-1%): pruritus, rash, urticaria; Rare (<0.1%): rhabdomyolysis, pancreatitis, hepatitis/jaundice, thrombocytopenia; Frequency not known/clinically noted: proteinuria/hematuria (usually transient), increased blood glucose/diabetes risk, peripheral neuropathy, immune-mediated necrotizing myopathy.

Safety & Warnings

Contraindications

Contraindicated in: active liver disease (including unexplained persistent transaminase elevations), pregnancy, breastfeeding, and hypersensitivity to rosuvastatin/excipients; concomitant cyclosporine use is not a formal contraindication in US labeling but requires strict dose limitation (max 5 mg/day) and is generally avoided.

Warnings & Precautions

Key warnings/precautions: myopathy/rhabdomyolysis risk (higher with high dose, renal impairment, hypothyroidism, and interacting drugs-stop if severe symptoms/marked CK elevation), hepatic effects (check baseline LFTs and test if symptoms arise), new-onset diabetes risk (monitor in at-risk patients), and monitor/adjust for major interactions (e.g., cyclosporine, protease inhibitors, gemfibrozil).

Age Restriction

Pediatrics: approved for HeFH in children 8-17 years; approved for HoFH in children 7-17 years. Not established/approved below these ages; other adult indications generally not established <18 years.

Driving Warning

Safe

Drug Interactions

Drug Interactions

Clinically important interactions include: cyclosporine (marked ↑ exposure; limit rosuvastatin to 5 mg/day/avoid), gemfibrozil (↑ exposure/myopathy risk; avoid or limit to 10 mg/day), other fibrates and niacin (↑ myopathy risk), HIV/HCV protease inhibitors (e.g., atazanavir/ritonavir, lopinavir/ritonavir; ↑ exposure-dose limits), warfarin (↑ INR-monitor), aluminum/magnesium antacids (↓ absorption-separate dosing), colchicine (↑ myopathy risk), and fusidic acid (rare severe myopathy/rhabdomyolysis-avoid/temporarily stop statin).

Interaction Severity

MAJOR: Cyclosporine (markedly increases rosuvastatin exposure-limit to 5 mg/day), gemfibrozil (increases exposure and myopathy risk-avoid or max 10 mg/day), systemic fusidic acid (avoid-rhabdomyolysis risk). MODERATE: Warfarin (↑INR-monitor), HIV protease inhibitors such as atazanavir/ritonavir or lopinavir/ritonavir (↑rosuvastatin-max 10 mg/day), other fibrates/niacin (↑myopathy risk). MINOR: Aluminum/magnesium antacids (↓rosuvastatin levels-separate by ~2 hours).

Food Interaction

May be taken with or without food; no clinically meaningful food restriction. Grapefruit juice is not a clinically significant interaction for rosuvastatin (unlike simvastatin/atorvastatin).

Special Populations

Pregnancy

Contraindicated

Breastfeeding

Contraindicated

Children

Heterozygous Familial Hypercholesterolemia (HeFH): ages 8 to <10 years: 5-10 mg orally once daily; ages 10-17 years: 5-20 mg orally once daily. Homozygous Familial Hypercholesterolemia (HoFH): ages 7-17 years: 20 mg orally once daily.

Elderly

No specific dose adjustment required based on age alone; however, elderly patients may be at higher risk for myopathy - initiate at lower doses (5mg) and titrate cautiously

Kidney Impairment

Severe renal impairment (CrCl <30 mL/min/1.73 m², not on hemodialysis): start 5 mg once daily and do not exceed 10 mg once daily; mild-moderate impairment: no adjustment. Hemodialysis: start 5 mg once daily; use caution and generally do not exceed 10 mg/day.

Liver Impairment

Contraindicated in active liver disease/unexplained persistent transaminase elevations; in chronic stable liver disease or mild hepatic impairment use with caution, and avoid use in severe hepatic impairment (Child-Pugh C) due to increased exposure and safety concerns.

Storage & Patient Advice

Stopping the Medicine

May be stopped without tapering, but should not be discontinued without prescriber advice because LDL-C will rise and cardiovascular risk reduction benefit is lost.

Patient Counseling

Take once daily at the same time, with or without food; continue diet/exercise; report unexplained muscle pain/weakness (especially with fever or dark urine); avoid use in pregnancy and breastfeeding and inform the prescriber if pregnancy occurs; limit alcohol and report symptoms of liver injury; check with a clinician before starting interacting drugs (e.g., cyclosporine, gemfibrozil, protease inhibitors, fusidic acid).

Monitoring Requirements

Fasting (or nonfasting per local practice) lipid panel at baseline and 4-12 weeks after initiation or dose change, then every 3-12 months; baseline liver enzymes and repeat if clinically indicated (symptoms/signs of hepatotoxicity); CK only if muscle symptoms or high-risk features; assess for new-onset diabetes risk (glucose/HbA1c as clinically appropriate).

Pharmacology

Mechanism of Action

Selective, competitive inhibition of HMG‑CoA reductase leading to reduced hepatic cholesterol synthesis and upregulation of hepatic LDL receptors, increasing LDL clearance.

Onset of Action

LDL-C lowering begins within ~1 week; maximal effect is typically achieved by ~4 weeks.

Duration of Effect

LDL-C lowering effect persists with continued daily dosing; maximal lipid-lowering effect is typically achieved by ~4 weeks. After discontinuation, lipid levels gradually return toward baseline over several weeks.

Half-Life

Approximately 19 hours.

Bioavailability

Approximately 20% oral bioavailability.

Excretion

Eliminated mainly in feces (~90%) and to a lesser extent in urine (~10%) (predominantly as unchanged drug).

Product Information

Available Dosage Forms

Film-coated tablet (oral).

Composition per Dose

Each film-coated tablet: 20mg rosuvastatin as rosuvastatin calcium

OTC Alternatives

No OTC alternative - prescription required for statins. Omega-3 fatty acid supplements (OTC) may modestly reduce triglycerides but are not equivalent

Lipid Target

Both

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