Table 1 Biological factors and common drugs that affect statin metabolism1 57
Factors/drugsExamples/comments
Biological characteristicsAdvanced age, hypothyroidism, renal dysfunction, hepatic dysfunction, alcohol consumption, metabolic muscle diseases, heavy exercise, surgery, CYP450 polymorphisms
Drugs that inhibit CYP450 2C9 (affecting fluvastatin metabolism)Azole antifungals
Drugs that inhibit CYP450 3A4 (affecting simvastatin, atorvastatin and lovastatin metabolism)Amiodarone, tricyclic antidepressants, selective serotonin reuptake inhibitors, macrolide antibiotics, HIV protease inhibitors, verapamil/diltiazem, warfarin, grapefruit juice (contains 6′,7′-dihydroxybergamottin), azole antifungals
FibratesAddition of fibrates to statin monotherapy increases the risk of rhabdomyolysis 12-fold. Gemfibrozil appears to carry the highest risk by inhibiting biliary excretion
  • CYP450, cytochrome P450.