Drugs For Hyperlipidemia

Question 1

Statins

Answer 1

simvastatin ,lovastatin&raquo_space;prodrug >activated by hydrolysis

-inhibiting de novo cholesterol synthesis , plasma cholesterol is reduced, by both decreased cholesterol synthesis and increased LDL catabolism ,also decrease triglyceride levels and may increase HDL cholesterol levels in some patients. [but has also antiatherosclerotic effect]
- Pitavastatin, rosuvastatin, and atorvastatin are the most potent LDL cholesterol–lowering statins, followed by simvastatin, pravastatin, and then lovastatin and fluvastatin.
-effective in lowering plasma cholesterol levels in all types of hyperlipidemias. However, pt who are homozygous for familial hypercholesterolemia lack LDL receptors and, therefore, benefit much less from treatment with these drugs.
- eliminated principally through bile and feces, but some urinary elimination (small %)
S.E. :-
-Elevated liver enzymes may occur with statin therapy. Therefore, liver function should be evaluated
-Myopathy and rhabdomyolysis (disintegration of skeletal muscle; rare) , pts usually had renal insufficiency or were taking drugs such as erythromycin, gemfibrozil, or niacin ,inhibitors of liver enzyme () may increase the risk of rhabdomyolysis ,Plasma creatine kinase levels should be determined in patients with muscle complaints
-may also increase the effect of warfarin. Thus, it is important to evaluate international normalized ratio (INR) frequently
-contraindicated during pregnancy and lactation