CRESTOR 10/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 (heterozygous familial and nonfamilial) and mixed dyslipidemia; to reduce TG in adults with hypertriglyceridemia; to treat adults with primary dysbetalipoproteinemia; to reduce LDL-C, total-C and ApoB in adults with homozygous familial hypercholesterolemia; to reduce risk of stroke, MI, and arterial revascularization in adults with established cardiovascular disease or at high risk (including those with elevated hs-CRP plus additional risk factor[s]).

Dosage & Administration

Dosing by Condition

Primary hypercholesterolemia/mixed dyslipidemia: 5-10 mg once daily initially (some patients may start 10-20 mg based on LDL goal), titrate to 5-40 mg once daily (max 40 mg); hypertriglyceridemia: 5-40 mg once daily; homozygous familial hypercholesterolemia: 20 mg once daily initially, may increase to 40 mg once daily; cardiovascular risk reduction: 20 mg once daily (or intensity based on ASCVD risk and tolerability).

Initial Dose

5-10 mg once daily

Maintenance Dose

5-20 mg once daily

Maximum Dose

40 mg once daily

Children's Dosage

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

Dose Adjustment Notes

Assess lipids and titrate at ~4-week intervals; consider lower starting dose (e.g., 5 mg) in Asian patients; in severe renal impairment (CrCl <30 mL/min, not on hemodialysis) start 5 mg and do not exceed 10 mg/day; with cyclosporine limit rosuvastatin to 5 mg/day (avoid higher doses); with gemfibrozil avoid if possible-if used, do not exceed 10 mg/day; with certain HIV protease inhibitors use the lowest effective dose and follow label-specific maximums (often not exceeding 10 mg/day with several PI regimens).

How to Take

Swallow tablet whole with water. May 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, nausea, constipation (arthralgia can also occur).

Side Effect Frequency

Very common (>10%): None consistently established. Common (1-10%): headache, dizziness, constipation, nausea, abdominal pain, myalgia, asthenia; proteinuria can occur. Rare/very rare: myopathy/rhabdomyolysis, pancreatitis, hepatitis/jaundice, thrombocytopenia, peripheral neuropathy, memory disturbance; diabetes risk is recognized as a class effect.

Safety & Warnings

Contraindications

Contraindicated in: active liver disease (including unexplained persistent elevations of hepatic transaminases), pregnancy, and breastfeeding/lactation; also contraindicated with hypersensitivity to rosuvastatin or excipients.

Warnings & Precautions

Major warnings/precautions: skeletal muscle effects (myopathy/rhabdomyolysis-higher risk with interacting drugs, renal impairment, hypothyroidism, older age), liver enzyme elevations/hepatotoxicity (check baseline LFTs and as clinically indicated), increased blood glucose/HbA1c (new-onset diabetes risk), and rare interstitial lung disease; consider urinalysis/proteinuria monitoring mainly with higher doses.

Age Restriction

Pediatrics: approved for heterozygous familial hypercholesterolemia (HeFH) in ages 8-17 years and for homozygous familial hypercholesterolemia (HoFH) in ages 7-17 years. Not established/approved for other indications in patients <18 years; use pediatric dosing only for these approved indications.

Driving Warning

Safe

Drug Interactions

Drug Interactions

Key interactions: cyclosporine (contraindicated/avoid-markedly increases rosuvastatin exposure), gemfibrozil (avoid or limit rosuvastatin dose due to myopathy risk), protease inhibitors (e.g., atazanavir/ritonavir, lopinavir/ritonavir-raise levels; dose limits), warfarin (may increase INR-monitor), aluminum/magnesium antacids (reduce absorption-separate dosing), other fibrates/niacin (additive myopathy risk), colchicine (myopathy risk).

Interaction Severity

MAJOR: Cyclosporine (markedly increases exposure-limit rosuvastatin to 5 mg/day); Gemfibrozil (increases exposure/myopathy risk-avoid or max 10 mg/day). MODERATE: Warfarin (may increase INR-monitor), HIV protease inhibitors (increase levels-dose-limit per regimen), other fibrates/niacin (additive myopathy risk), colchicine (myopathy risk). MINOR: Aluminum/magnesium antacids (reduce absorption-separate by ≥2 hours).

Food Interaction

No clinically meaningful food restriction-may be taken with or without food.

Special Populations

Pregnancy

Contraindicated

Breastfeeding

Contraindicated

Children

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

Kidney Impairment

CrCl ≥30 mL/min: no adjustment generally required; CrCl <30 mL/min (not on hemodialysis): start 5 mg once daily and do not exceed 10 mg/day; hemodialysis: start 5 mg once daily and do not exceed 10 mg/day (use caution).

Storage & Patient Advice

Stopping the Medicine

Can be stopped without taper, but should not be discontinued without prescriber advice because LDL-C will rise and long-term ASCVD risk reduction benefit is lost.

Overdose

No specific antidote; manage with symptomatic/supportive care, consider decontamination if recent ingestion, monitor for myopathy/rhabdomyolysis and hepatic effects; hemodialysis is unlikely to be beneficial.

Patient Counseling

Take once daily at the same time, with or without food; continue diet/exercise; report unexplained muscle pain/weakness (especially with fever/malaise) or dark urine; avoid excessive alcohol; contraindicated in pregnancy-stop and contact prescriber if pregnant and use effective contraception; separate aluminum/magnesium antacids by at least 2 hours; attend lipid monitoring and follow-up.

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; liver enzymes at baseline and thereafter only if clinically indicated (symptoms/signs of hepatotoxicity); CK only if muscle symptoms or high-risk features; assess for secondary causes and drug interactions; consider urinalysis/proteinuria evaluation if using 40 mg or if clinically indicated.

Pharmacology

Mechanism of Action

Competitive inhibition of HMG‑CoA reductase reduces hepatic cholesterol synthesis and upregulates LDL receptors, increasing clearance of circulating LDL-C.

Onset of Action

LDL-C reduction begins within ~1 week; near-maximal effect is typically achieved by ~2-4 weeks of continued therapy.

Duration of Effect

LDL-C lowering effect begins within ~1 week; near-maximal effect is typically achieved by ~2-4 weeks of continued therapy. With continued once-daily dosing, the lipid-lowering effect is maintained; after discontinuation, lipid levels gradually return toward baseline over several weeks.

Half-Life

Approximately 19-20 hours.

Bioavailability

Approximately 20% oral bioavailability.

Metabolism

Minimal metabolism; ~10% is metabolized hepatically, mainly via CYP2C9 (minor CYP2C19), with most circulating drug as unchanged rosuvastatin.

Excretion

Primarily fecal/biliary excretion (~90%), with a minor urinary/renal component (~10%).

Protein Binding

Approximately 88%, primarily to albumin

Product Information

Available Dosage Forms

Film-coated tablet (oral).

Composition per Dose

Each film-coated tablet: 10 mg rosuvastatin (as rosuvastatin calcium)

Generic Availability

Yes

OTC Alternatives

No OTC alternative.

Lipid Target

Both

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