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ANTIHYPERLIPIDEMIC DRUGSANTIHYPERLIPIDEMIC DRUGS
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TYPE ITYPE I
Familial hyperchylomicronemia More chylomicrons Lipoprotein lipase deficiency No Risk of CAD Rx – low fat diet
Familial hyperchylomicronemia More chylomicrons Lipoprotein lipase deficiency No Risk of CAD Rx – low fat diet
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TYPE II ATYPE II A
Familial hypercholesterolemia ↑LDL, normal VLDL ↑ IHD Rx – low cholesterol & low saturated fat
diet, drugs such as colestipol or cholestyramine or statins.
Familial hypercholesterolemia ↑LDL, normal VLDL ↑ IHD Rx – low cholesterol & low saturated fat
diet, drugs such as colestipol or cholestyramine or statins.
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TYPE II BTYPE 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.
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.
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TYPE III 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.
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.
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TYPE IV TYPE IV
Familial hypertriglyceridemia ↑VLDL - ↑ Circulating TAG, Normal LDL levels Obese , diabetic. Rx – wt. reduction, diet , Niacin or Gemfibrozil
or Statins.
Familial hypertriglyceridemia ↑VLDL - ↑ Circulating TAG, Normal LDL levels Obese , diabetic. Rx – wt. reduction, diet , Niacin or Gemfibrozil
or Statins.
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TYPE VTYPE V
Familial mixed hypertriglyceridemia ↑ VLDL ↑ chylomicrons ↑ Cholesterol ↑↑ TAG Obese , diabetic Rx– Wt. reduction ,diet control, Niacin,
Clofibrate or Gemfibrozil or Statins.
Familial mixed hypertriglyceridemia ↑ VLDL ↑ chylomicrons ↑ Cholesterol ↑↑ TAG Obese , diabetic Rx– Wt. reduction ,diet control, Niacin,
Clofibrate or Gemfibrozil or Statins.
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Pharmacological Management of Hyperlipidemia
Pharmacological Management of Hyperlipidemia
DIET : ADJUNCT TO DRUGS
AVOID DRUGS : PREGNANT, LACTATING
DIET : ADJUNCT TO DRUGS
AVOID DRUGS : PREGNANT, LACTATING
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NIACINNIACIN
water-soluble vitamin Lipolysis - inhibited Free fatty acids – decreased Triglycerides – decreased VLDL , LDL - REDUCED CHOLESTEROL - REDUCED HDL - INCREASED
water-soluble vitamin Lipolysis - inhibited Free fatty acids – decreased Triglycerides – decreased VLDL , LDL - REDUCED CHOLESTEROL - REDUCED HDL - INCREASED
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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.
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.
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THERAPEUTIC USESTHERAPEUTIC USES
Oral - route Urinary excretion FAMILIAL HYPERTRIGLYCERIDEMIA
MIXED HYPERLIPIDEMIA
HYPERCHOLESTEROLEMIAS
Oral - route Urinary excretion FAMILIAL HYPERTRIGLYCERIDEMIA
MIXED HYPERLIPIDEMIA
HYPERCHOLESTEROLEMIAS
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SIDE EFFECTSSIDE EFFECTS
CUTANEOUS FLUSH , PRURITUS RX : ASPIRIN
NAUSEA , VOMITING
HYPER - URECEMIA & GOUT.
CUTANEOUS FLUSH , PRURITUS RX : ASPIRIN
NAUSEA , VOMITING
HYPER - URECEMIA & GOUT.
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GEMFIBROZIL , CLOFIBRATEGEMFIBROZIL , CLOFIBRATE
LIPO PROTEIN LIPASE – STIMULATED TRIACYLGLYCEROLS – BROKEN VLDL , CHYLOMICRONS – REDUCED
CHOLESTEROL IN BILE - INCREASED
LIPO PROTEIN LIPASE – STIMULATED TRIACYLGLYCEROLS – BROKEN VLDL , CHYLOMICRONS – REDUCED
CHOLESTEROL IN BILE - INCREASED
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GEMFIBROZIL & CLOFIBRATEGEMFIBROZIL & CLOFIBRATE
ORAL- WELL ABSORBED
EXCRETION - RENAL
ORAL- WELL ABSORBED
EXCRETION - RENAL
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USESUSES
MAINLY FOR TRIACYLGLYCEROLS i.e TYPE IV
DYSBETALIPOPROTEINEMIA i.e TYPE III
MAINLY FOR TRIACYLGLYCEROLS i.e TYPE IV
DYSBETALIPOPROTEINEMIA i.e TYPE III
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SIDE EFFECTSSIDE EFFECTS
GIT DISTURBANCES MYOPATHY , MALIGNANCY (Clofibrate) GALL STONE FORMATION CI : GB DISEASE,
–RENAL DISEASE
–LIVER DISEASE
GIT DISTURBANCES MYOPATHY , MALIGNANCY (Clofibrate) GALL STONE FORMATION CI : GB DISEASE,
–RENAL DISEASE
–LIVER DISEASE
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BILE ACID BINDING RESINSBILE 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
WATER INSOLUBLE BIND WITH BILE ACID AND BILE SALTS COMPLEX -NOT ABSORBED ENTEROHEPATIC RECIRCULATION –REDUCED CHOLESTEROL USE – INCREASED LDL LEVELS – FALL CHOLESTEROL LEVEL - FALLS
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CHOLESTYRAMINE , COLESTIPOLCHOLESTYRAMINE , COLESTIPOL
USE - HYPERLIPIDEMIAS Mainly for TYPE II A & II B
SIDE EFFECTS – CONSTIPATION , BLOATING FAT SOL. VITAMIN DEFICIENCY.
USE - HYPERLIPIDEMIAS Mainly for TYPE II A & II B
SIDE EFFECTS – CONSTIPATION , BLOATING FAT SOL. VITAMIN DEFICIENCY.
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HMG Co A REDUCTASE INHIBITORSHMG Co A REDUCTASE INHIBITORS
LOVASTATIN
PRAVASTATIN
FLUVASTATIN
SIMVASTATIN
LOVASTATIN
PRAVASTATIN
FLUVASTATIN
SIMVASTATIN
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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
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
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USES – HYPERLIPIDEMIAS FAMILIAL HYPERCHOLESTEROLEMIA – lack
LDL receptors --LESS EFFECT SIDE EFFECTS : LIVER FUNCTION – RENAL DYSFUNCTION MYOPATHY, RHABDOMYOLYSIS – RARE CI : CHILD, PREGNANT, LACTATING
USES – HYPERLIPIDEMIAS FAMILIAL HYPERCHOLESTEROLEMIA – lack
LDL receptors --LESS EFFECT SIDE EFFECTS : LIVER FUNCTION – RENAL DYSFUNCTION MYOPATHY, RHABDOMYOLYSIS – RARE CI : CHILD, PREGNANT, LACTATING
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PROBUCOLPROBUCOL
Probucol increases the rate of LDL metabolism
block the intestinal transport of cholesterol.
The net result is a significant reduction in plasma cholesterol levels.
Probucol increases the rate of LDL metabolism
block the intestinal transport of cholesterol.
The net result is a significant reduction in plasma cholesterol levels.
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PROBUCOLPROBUCOL
LDL – REDUCED NOT VERY USEFUL USED SOMETIMES FOR II A & II B SIDE EFFECTS – GIT QT INTERVAL PROLONGED CI : PREGNANCY
LDL – REDUCED NOT VERY USEFUL USED SOMETIMES FOR II A & II B SIDE EFFECTS – GIT QT INTERVAL PROLONGED CI : PREGNANCY
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INTERACTIONSINTERACTIONS
MAINLY SEEN WITH WARFARIN
GEMFIBROZIL , CLOFIBRATE CHOLESTYRAMINE , COLESTIPOL HMG Co A INHIBITORS
MAINLY SEEN WITH WARFARIN
GEMFIBROZIL , CLOFIBRATE CHOLESTYRAMINE , COLESTIPOL HMG Co A INHIBITORS
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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.
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.
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Metabolized in the small intestine and liver CI – hepatic insufficiency.
Metabolized in the small intestine and liver CI – hepatic insufficiency.