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
Ezetimbe is MOST EFFECTIVE when used with what type of drug?
Statin
Statin + Ezetimbe
Vytorin
Adverse effects:
Sinusitis and pharyngitis
Headache, myalgia