Cyclosporine
Contraindicated
Database
Cyclosporine increases rosuvastatin plasma levels 7-11 fold via OATP1B1 inhibition; high myopathy risk
Contraindicated combination
Source: Kimi deep-research + Cla
Drug reference
Rosuvastatin
HMG-CoA reductase inhibitor (statin) · Antilipidemic
Also known as Rosuvastatin calcium, Crestor
START
Start 5-10 mg OD; check baseline lipid panel, LFTs, CK, and T2DM risk; assess for drug interactions
TYPICAL MAX
20 mg/day usual max; 40 mg/day only under specialist supervision
STOP IF
Unexplained muscle pain with CK >5x ULN, jaundice, LFTs >3x ULN, pregnancy
WATCH
Lipids at 4-12 weeks then 3-6 monthly, LFTs at baseline and as clinically indicated, muscle symptoms, HbA1c
CDSCO approvedJan AushadhiNPPA price-controlledATC C10AA07
KDIGO 2024 + manufacturer label
- ONSET
- 1h · absorption onset
- PEAK
- 4h · Peak plasma concentration
- t½
- 19h · Elimination half-life
- DURATION
- 1d · Once-daily dosing
EXCRETION
Fecal (90%, mostly unchanged)
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Contraindicated in pregnancy; cholesterol and products of cholesterol biosynthesis are essential for fetal development
FDA category + note
Top interactionssee all 12 →
- CyclosporineContraindicatedDatabaseKimi deep-research + Cla
- GemfibrozilContraindicatedDatabaseKimi deep-research + Cla · p949
- AtazanavirSevereTextbook-citedKDT 7e · p948
- DarunavirSevereTextbook-citedKDT 7e · p948
Available in India
1,367 branded formulations and 397 fixed-dose combinations. Look up specific brands in the Drugs workspace.
Jan Aushadhi — generic available at GoI pharmacies
Mechanism
Competitive inhibition of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis, leading to upregulation of LDL receptors and increased LDL clearance from plasma
Indications
Primary hypercholesterolemia (heterozygous familial and non-familial)Mixed dyslipidemiaPrevention of cardiovascular events in high-risk patientsSlowing of atherosclerosis progression
Dosing
- Adult
- Start 5-10 mg OD; usual range 5-20 mg OD; max 40 mg OD (for severe hypercholesterolemia/ FH under specialist supervision)
- Pediatric
- 8-10 years (heterozygous FH): 5-10 mg OD; 10-17 years: 5-20 mg OD
- Renal adjustment
- eGFR <30: max 10 mg/day; no adjustment if eGFR >/=30
- Hepatic adjustment
- Contraindicated in active liver disease; avoid in severe hepatic impairment
- Geriatric
- Start at 5 mg/day; increased risk of myopathy
- Max dose
- 40 mg/day (specialist only); 20 mg/day usual maximum
Pharmacokinetics
Onset
1-2 weeks (measurable LDL reduction); peak effect at 4 weeks
Peak effect
3-5 hours (Tmax)
Duration
24 hours
Half-life
19 hours
Bioavailability
~20%
Protein binding
88%
Metabolism
Minimal CYP metabolism (<10%); primarily CYP2C9; most excreted unchanged
Excretion
Fecal (90%, primarily unchanged); renal (10%)
Contraindications
- Active liver disease or unexplained persistent elevated transaminases
- Pregnancy and breastfeeding
- Severe renal impairment (eGFR <30 mL/min) at doses >10 mg
- Concurrent use with cyclosporine
- Hypersensitivity to rosuvastatin
Side effects
Common
HeadacheMyalgiaAstheniaConstipationNauseaAbdominal pain
Serious
- Rhabdomyolysis (rare, <0.1%)
- Hepatotoxicity
- Immune-mediated necrotizing myopathy
- Type 2 diabetes mellitus (increased risk)
- Memory impairment / cognitive effects
Pregnancy & lactation
Pregnancy
Contraindicated in pregnancy; cholesterol and products of cholesterol biosynthesis are essential for fetal development
Lactation
Excreted in breast milk; contraindicated during breastfeeding
Drug interactions
Gemfibrozil
Contraindicated
Database
Increased risk of myopathy/rhabdomyolysis when combined with statins
Avoid combination; use fenofibrate if fibrate needed
Source: Kimi deep-research + Cla · p949
Atazanavir
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy.
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Darunavir
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy.
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Erythromycin
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Fluconazole
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy.
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Itraconazole
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Ketoconazole
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy.
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Lopinavir
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Nicotinic Acid
Severe
Textbook-cited
Increased risk of myopathy and rhabdomyolysis
Use with caution; monitor for muscle symptoms and CK levels
Source: KDT 7e · p949
Ritonavir
Severe
Textbook-cited
Increased risk of rhabdomyolysis and myopathy.
Avoid concurrent use; if needed, use lowest statin dose
Source: KDT 7e · p948
Azole Antifungals
Severe
Textbook
Increased plasma concentrations of statins and their active metabolites, leading to an increased risk of myopathy and rhabdomyolysis.
Consider using pravastatin, fluvastatin, or rosuvastatin, as they are not extensively metabolized by CYP3A4. Carefully weigh the benefits against the risk of myopathy.
Source: G&G 14e · p736
Related guidelines
Ask House about Rosuvastatin
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19