BPS 334 Lecture Notes - Lecture 38: Hmg-Coa Reductase, Low-Density Lipoprotein, Ezetimibe
27 Nov 2016
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Document Summary
Statins (atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastatin and simvastatin): (hmg coa reductase inhibitors) Inhibits hmg coa reductase: essential for formation of cholesterol: hepatic (liver) cholesterol synthesis is therefore reduced: decreasing liver ldl, low ldl causes up-regulation of ldl receptors: removing more ldl from blood, this lowers ldl levels in the circulation. Other effects: decrease plasma triglycerides (decrease vldl production and increase remnant absorption) Cyp3a4 metabolism: powerful and mild cyp3a4 inhibitors decrease metabolic clearance which increases plasma concentrations in the presence of the inhibitor, powerful inhibitors=itraconazole, ketoconazole, ritonavir, nelfinavir, mild inhibitors=cyclosporine, erythromycin, verapamil, diltiazem, amiodarone and components in grapefruit juice. Indicated by elevations in serum aminotransaminase: skeletal muscle=statin-induced myopathy. Increased creatine kinase activity indicates skeletal muscle toxicity occurring as rhabdomyolysis (generalized skeletal muscle pain, tenderness or weakness) May enhance the myopathic (rhabdomyolysis) effect of statins, May increase the serum concentration of statins. Contraindicated in pregnant and lactation: because cholesterol is an important precursor for synthesis of steroids and cell membranes in development.
