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ANTIHYPERLIPIDEMIC DRUGS

ANTIHYPERLIPIDEMIC DRUGS. TYPE I. Familial hyperchylomicronemia More chylomicrons Lipoprotein lipase deficiency No Risk of CAD Rx – low fat diet. TYPE II A. Familial hypercholesterolemia ↑LDL, normal VLDL ↑ IHD

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ANTIHYPERLIPIDEMIC DRUGS

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  1. ANTIHYPERLIPIDEMIC DRUGS

  2. TYPE I • Familial hyperchylomicronemia • More chylomicrons • Lipoprotein lipase deficiency • No Risk of CAD • Rx – low fat diet

  3. TYPE II A • Familial hypercholesterolemia • ↑LDL, normal VLDL • ↑ IHD • Rx – low cholesterol & low saturated fat diet, drugs such as colestipol or cholestyramine or statins.

  4. TYPE II B • Familial Mixed Hyperlipidemia • TYPE II A + • ↑ VLDL – over production of VLDL by liver • Rx -- low cholesterol & low saturated fat diet, drugs such as colestipol or cholestyramine or statins or Niacin.

  5. TYPE III • Familial Dysbetalipoproteinemia • ↑IDL caused by over production or underutilization, due to mutant apoE • ↑ TAG , ↑ Cholesterol levels • Xanthomas & CAD risk increased • Rx – Wt reduction, Exercise & diet control, Niacin or Clofibrate or statins.

  6. TYPE IV • Familial hypertriglyceridemia • ↑VLDL - ↑ Circulating TAG, Normal LDL levels • Obese , diabetic. • Rx – wt. reduction, diet , Niacin or Gemfibrozil or Statins.

  7. TYPE V • Familial mixed hypertriglyceridemia • ↑ VLDL ↑ chylomicrons ↑ Cholesterol • ↑↑ TAG • Obese , diabetic • Rx– Wt. reduction ,diet control, Niacin, Clofibrate or Gemfibrozil or Statins.

  8. Pharmacological Management of Hyperlipidemia • DIET : ADJUNCT TO DRUGS • AVOID DRUGS : PREGNANT, LACTATING

  9. NIACIN • water-soluble vitamin • Lipolysis - inhibited • Free fatty acids – decreased • Triglycerides – decreased • VLDL , LDL - REDUCED • CHOLESTEROL - REDUCED • HDL - INCREASED

  10. Nicotinic acid: Nicotinic acid reduces the plasma levels of both VLDLs and LDLs by inhibiting hepatic VLDL secretion, as well as suppressing the flux of FFA release from adipose tissue by inhibiting lipolysis. Because of its ability to cause large reductions in circulating levels of cholesterol, nicotinic acid is used to treat Type II, III, IV and V hyperlipoproteinemias.

  11. THERAPEUTIC USES • Oral - route • Urinary excretion • FAMILIAL HYPERTRIGLYCERIDEMIA • MIXED HYPERLIPIDEMIA • HYPERCHOLESTEROLEMIAS

  12. SIDE EFFECTS • CUTANEOUS FLUSH , PRURITUS • RX : ASPIRIN • NAUSEA , VOMITING • HYPER - URECEMIA & GOUT.

  13. GEMFIBROZIL , CLOFIBRATE • LIPO PROTEIN LIPASE – STIMULATED • TRIACYLGLYCEROLS – BROKEN • VLDL , CHYLOMICRONS – REDUCED • CHOLESTEROL IN BILE - INCREASED

  14. GEMFIBROZIL & CLOFIBRATE • ORAL- WELL ABSORBED • EXCRETION - RENAL

  15. USES • MAINLY FOR TRIACYLGLYCEROLS • i.e TYPE IV • DYSBETALIPOPROTEINEMIA • i.e TYPE III

  16. SIDE EFFECTS • GIT DISTURBANCES • MYOPATHY , • MALIGNANCY (Clofibrate) • GALL STONE FORMATION • CI : GB DISEASE, • RENAL DISEASE • LIVER DISEASE

  17. BILE ACID BINDING RESINS • WATER INSOLUBLE • BIND WITH BILE ACID AND BILE SALTS • COMPLEX -NOT ABSORBED • ENTEROHEPATIC RECIRCULATION –REDUCED • CHOLESTEROL USE – INCREASED • LDL LEVELS – FALL • CHOLESTEROL LEVEL - FALLS

  18. CHOLESTYRAMINE , COLESTIPOL • USE - HYPERLIPIDEMIAS • Mainly for TYPE II A & II B SIDE EFFECTS – • CONSTIPATION , BLOATING • FAT SOL. VITAMIN DEFICIENCY.

  19. HMG Co A REDUCTASE INHIBITORS • LOVASTATIN • PRAVASTATIN • FLUVASTATIN • SIMVASTATIN

  20. HMG Co A REDUCTASE – RATE LIMITING STEP FOR CHOLESTEROL SYN. • LDL – BROKEN DOWN • KINETICS : ORAL ABS. – GOOD • FIRST PASS METABOLISM – GOOD • SITE OF ACTION - LIVER • EXCRETION – MAINLY BILE, STOOL

  21. USES – HYPERLIPIDEMIAS • FAMILIAL HYPERCHOLESTEROLEMIA – lack LDL receptors --LESS EFFECT • SIDE EFFECTS : • LIVER FUNCTION – • RENAL DYSFUNCTION • MYOPATHY, RHABDOMYOLYSIS – RARE • CI : CHILD, PREGNANT, LACTATING

  22. PROBUCOL • Probucol increases the rate of LDL metabolism • block the intestinal transport of cholesterol. • The net result is a significant reduction in plasma cholesterol levels.

  23. PROBUCOL • LDL – REDUCED • NOT VERY USEFUL • USED SOMETIMES FOR II A & II B • SIDE EFFECTS – GIT • QT INTERVAL PROLONGED • CI : PREGNANCY

  24. INTERACTIONS • MAINLY SEEN WITH WARFARIN • GEMFIBROZIL , CLOFIBRATE • CHOLESTYRAMINE , COLESTIPOL • HMG Co A INHIBITORS

  25. Cholesterol absorption inhibitors • Ezetimibe • Selectively inhibits intestinal absorption of dietary and biliary cholesterol in small intestine leading to a decrease in the delivery of intestinal cholesterol to the liver. This leads to a depletion in the hepatic cholesterol stores.

  26. Metabolized in the small intestine and liver • CI – hepatic insufficiency.

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