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HMG-CoA Reductase Inhibitor for Dyslipidemia Management
Primary Hypercholesterolemia:
Heterozygous/homozygous familial hypercholesterolemia (HeFH/HoFH)
Non-familial hypercholesterolemia
Mixed Dyslipidemia: Fredrickson Types IIa/IIb
Hypertriglyceridemia: Fredrickson Type IV
Dysbetalipoproteinemia: Fredrickson Type III
Cardiovascular Risk Reduction:
Asymptomatic or symptomatic CAD with elevated LDL-C
Post-renal transplantation or diabetes-associated hypercholesterolemia
Adjunct to diet/lifestyle modifications
(Use under registered physician's guidance)
Competitive inhibition of HMG-CoA reductase → ↓ hepatic cholesterol synthesis
↑ Hepatic LDL receptor expression → enhanced LDL clearance
| Parameter | Profile |
|---|---|
| Bioavailability | 14% (parent drug); 30% (total activity) |
| Tₘₐₓ | 1-2 hours |
| Protein Binding | 98% |
| Metabolism | CYP3A4 (major) → Active ortho-/para-hydroxylated metabolites (70% activity) |
| Half-life | 14 hours (parent); 20-30 hours (active metabolites) |
| Excretion | Biliary (95%); <2% renal |
| Indication | Initial Dose | Titration | Max Dose |
|---|---|---|---|
| Primary Prevention | 10-20 mg daily | ↑ by 10-20 mg q4 weeks | 80 mg daily |
| HeFH/HoFH | 10 mg daily | ↑ to 40-80 mg q4 weeks | 80 mg daily |
| Pediatrics (10-17 yrs) | 10 mg daily | ↑ to 20 mg q4 weeks* | 20 mg daily |
Take any time of day, with/without food
*LDL-C goal: ≥50% reduction from baseline*
(Follow registered physician's advice)
Active liver disease or unexplained transaminase elevation
Pregnancy/lactation
Hypersensitivity to statins
Concurrent use with cyclosporine
Common (≥5%):
Myalgia • Headache • Constipation • Flatulence • Arthralgia
Serious (Monitor Closely):
Hepatotoxicity: ↑ ALT/AST (0.7% at 80 mg dose)
Myopathy/Rhabdomyolysis: ↑ CK levels, myalgia with weakness
New-Onset Diabetes: HbA1c elevation (particularly with risk factors)
| Drug Class | Effect | Action |
|---|---|---|
| CYP3A4 Inhibitors (Azoles, Macrolides) | ↑ Atorvastatin exposure | Avoid or limit dose to 20 mg daily |
| Fibrates/Niacin | ↑ Myopathy risk | Avoid combination |
| Oral Contraceptives | ↑ Ethinyl estradiol (20-30%) | Monitor for side effects |
| Grapefruit Juice | ↑ AUC up to 37% | Avoid >1.2 L daily |
Hepatic Monitoring:
Check LFTs at baseline, 12 weeks, then annually (discontinue if ALT/AST >3× ULN)
Musculoskeletal:
Check CK if myalgia occurs (discontinue if CK >10× ULN)
Renal Impairment:
No dose adjustment needed
Special Populations:
Elderly: ↑ Exposure (↓ initial dose in frail patients)
Asian Patients: Consider 50% lower starting dose
Pregnancy (Category X):
Discontinue immediately if pregnancy occurs → fetal structural abnormalities
Lactation: Contraindicated (excreted in animal milk)
Symptoms: Elevated LFTs, myopathy
Treatment:
Symptomatic support + hydration
Monitor CK/LFTs for 72h
No hemodialysis benefit (high protein binding)
HMG-CoA Reductase Inhibitor (Statin)
Below 30°C • Protect from light/moisture
Keep out of children's reach
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