Fluvastatin inhibits HMG-CoA reductase, the enzyme responsible for cholesterol biosynthesis in the liver. This inhibition:

1. Reduces Hepatic Cholesterol Synthesis: Depletes intracellular cholesterol, prompting upregulation of LDL receptors.
2. Enhances LDL Clearance: Increases hepatic uptake of LDL cholesterol from the bloodstream.
3. Improves Lipid Profile:
   • Lowers LDL cholesterol by 20–35%.
   • Modestly reduces triglycerides (10–15%) and raises HDL cholesterol (5–10%).

Fluvastatin is metabolized primarily by CYP2C9, with minor contributions from CYP3A4 and CYP2C8, distinguishing its pharmacokinetic profile from other statins (Lippincott Textbook of Pharmacology).

1. Primary Hypercholesterolemia and Mixed Dyslipidemia:
   • Management of elevated LDL cholesterol and triglycerides.
2. Cardiovascular Risk Reduction:
   • Secondary Prevention: Reduces recurrent cardiovascular events (e.g., post-MI, post-revascularization).
3. Renal Impairment:
   • Preferred in patients with chronic kidney disease (CKD) due to minimal renal excretion (BNF).

• Adults:
  • Immediate-Release (IR): 20–40 mg once daily at bedtime.
  • Extended-Release (XL): 80 mg once daily (any time).
• Special Populations:
  • Renal Impairment: No dose adjustment required (non-renally excreted).
  • Hepatic Impairment: Contraindicated in active liver disease or persistent transaminase elevation.
• Administration:
  • Take IR tablets at bedtime for optimal efficacy (aligns with peak cholesterol synthesis).
  • Avoid concurrent bile acid sequestrants (e.g., cholestyramine); administer 2 hours apart (Lange Basic & Clinical Pharmacology).

• Common (≥1%):
  • Myalgia (muscle pain), headache, gastrointestinal disturbances (dyspepsia, diarrhea).
  • Transient transaminase elevation (1–3% of patients).
• Serious (Rare):
  • Rhabdomyolysis: Severe muscle breakdown (risk <0.1%).
  • Hepatotoxicity: Discontinue if ALT/AST >3× upper limit of normal (ULN).
  • New-Onset Diabetes: Slight increased risk with long-term use (BNF).

• Contraindications:
  • Active liver disease or unexplained transaminase elevation.
  • Pregnancy and lactation (risk of fetal harm).
• Monitoring:
  • Baseline liver function tests (LFTs) and lipid profile.
  • Repeat LFTs at 12 weeks, then annually.
  • Check creatine kinase (CK) if myalgia develops.
• Patient Counseling:
  • Report unexplained muscle pain, weakness, or dark urine.
  • Avoid excessive alcohol consumption.

1. CYP2C9 Inhibitors (e.g., fluconazole): ↑ Fluvastatin levels (↑ toxicity risk).
2. Gemfibrozil: ↑ Risk of myopathy (avoid combination).
3. Warfarin: Monitor INR (fluvastatin may ↑ anticoagulant effect).
4. Cyclosporine: ↑ Fluvastatin exposure (max dose: 40 mg/day) (Lippincott Textbook of Pharmacology).

• Generic Name: Fluvastatin sodium.

Brand Names: Lescol (IR), Lescol XL (XL), and generics