HMG-CoA Reductase Inhibitors Flashcards
Drugs
Atorvastatin Fluvastatin Lovastatin Pitavastatin Pravastatin Rosvuastatin Simvastatin
M.O.A
Competitive inhibition of Hmg-CoA reductase -> Inhibited conversion of Hmg-CoA to mevalonic acid which is the rate limiting step in cholesterol biosynthesis -> Compensatory increase LDL receptors = Increased LDL-C uptake.
Indications
Hypercholesterolemia (Rosuvastatin - doc, Atovarstatin - 2nd)
Mixed Hyperlipidemia (Atorvar and Rosvu - best effect on TG levels)
Protection - Osteoporosis and cancer
Most Common Adverse Effects
Abdominal cramps Constipation Diarrhea Heartburn Less Frequently: Hepatitis Increased hepatic enzymes
Most serious Adverse Effects
Myopathy - 0,2%
Myalgia
Myositis
Rhabdomyolysis -> Acute renal failure (myoglobinuria = DISCONTINUE)
Interactions
Increase plasma levels Ator, Lova and Simva:
Erythromycin
Itraconazole
Ritonavir
NSAIDS - Fluva
All Statins increase Wafarin levels
Contraindicated - Fibric acids (myopathies)