Cardio & Renal 4: Antihyperlipidemic Drugs Flashcards
Antihyperlipidemic Drugs: Statins MOA
Inhibit the rate limiting step in cholesterol biosynthesis
Antihyperlipidemic Drugs: Buzz word
Statins
Inhibit HMG-CoA reductase inhibitors
(3-hydroxy-3-methylGlutaryl CoA reductase inhibitors)
Atorvastatin
Simvastatinn
Pravastatin
Rosvastatin
Lovastatin
Statin reduce LDL, cholesterol, and triglycerides
Statin increase HDL (good cholesterol)
Antihyperlipidemic Drugs: Statins Indications (3)
- Hyperlipoproteinemia
- Hypercholesterolemia
- Hypertriglyceridemia
Antihyperlipidemic Drugs: Statins Adverse Reactions
Buzz word: Myopathy
From muscle ache, myalgia, myositis to rhabdomyolysis (break down of skeletal muscle) —> renal failure
Antihyperlipidemic Drugs: Statins Latest Study
Statin are used for 2 yr prevention of heart disease
Statin increases NO and decrease mRNA for endothelin-1 —> vasodilation
Antihyperlipidemic Drugs: Bile Acid Sequestrants Buzzword
Cholestyramine
Cholestipol
Cholesvelam
Antihyperlipidemic Drugs: Bile Acid Sequestrants *MOA
Bind bile acids in the GI —> form an insoluble complex that’s excreted in the feces
So cholesterol is used to make more bile acid (thus lowering LDL, bad cholesterol)
**not used in hypertriglyceridemia because they increase VLDL and TG
Antihyperlipidemic Drugs: Bile Acid Sequestrants Adverse reactions (3)
Constipation
Malabsorption of fat soluble vitamins (ADEK)
Malabsorption of digoxin, thiazide, and warfarin
Antihyperlipidemic Drugs: Bile Acid Sequestrants: Special Indication for Choletyramine
Rx of pruritis due to biliary obstruction
How? In biliary obstruction the liver can’t eliminate bile
Antihyperlipidemic Drugs: Nicotinic Acid (Niacin, B3)
Inhibits VLDL synthesis
Activates lipoprotein lipase
Adverse effects:
Flushing and pruritis Hyperuricemia Gastric irritation Myopathies Glucose intolerance
Antihyperlipidemic Drugs: Fibirc Acid Deritivatives
Gemfibrozil
Clofibrate
Fenobibrate
Antihyperlipidemic Drugs: Fibirc Acid Deritivatives - Action and MOA
Activates lipoprotein lipase
Decrease VLDL, TG, and LDL
By activating the peroxisome proliferator-activated receptor-alpha (PPAR-alpha) in the nuclei that regulates gene transcription
Antihyperlipidemic Drugs: Fibirc Acid Deritivatives - Adverse Effects (4)
Flu-like muscle aches
Gallstones
Allergic reactions
Blood cell deficiencies
New Cholesterol Lowering Drug
Ezetimbe
Ezetimbe MOA
Inhibits cholesterol absorption in the small intestine