Antihyperlipidemic drugs Flashcards
Atorvastatin Simvastatin Pravastatin Rosuvastatin Lovastatin
What is the MOA of these drugs?
Statins inhibit the rate limiting step in cholesterol biosynthesis When intrinsic cholesterol synthesis is blocked, the liver increases the uptake of Cholesterol from the plasma which leads to: Upregulation of hepatic LDL receptors Decreases plasma LDL
What is the Therapeutic effects of statins:
Decrease LDL, VLDL and triglycerides Mild increase in HDL
Statins are used for________
secondary prevention of heart diseases
Improve endothelial function
Modulate inflammatory response
Maintain plaque stability
Increase NO and decrease mRNA for endothelin-1 causing vasodilation
What is the drug interaction of statin that you gave to Bill, what should you tell Bill to avoid?
Inhibitors of P450, and grapefruit juice Red yeast rice
What is the side effects of statins?
Myopathy
Range from myalgia, myositis to rhabdomyolysis
Risk increases with concurrent therapy of gemfibrozil and nicotinic acid
2. Hepatotoxicity: Elevated AST (discontinue if more than 3x normal)
Name Bile Acid sequestrants drugs
Cholestyramine Colestipol Colesevelam
What is the MOA of Cholestyramine?
Bind to bile acids in the GI and from an insoluble complex that is excreted in the feces. Cholesterol is used to make more bile acid thus lowering LDL from the plasma.
What is the contraindicated in using bile acid sequestrants with your patient
Contraindicated in hypertriglyceridemia because they increase VLDL and TG
What is the side effect of Colestipol?
Fat malabsorption (steatorrhea) and malabsorption of Fat-soluble vitamins ADEK
Cholestyramine is used in Rx of pruritis due to biliary obstruction as the liver cannot eliminate bile
What is the MOA of Niacin?
For lipid lowering effects, nicotinic acid is given in much higher doses than as vitamin
Inhibits the hepatic production of VLDL and its metabolite LDL Increases HDL by delaying hepatic HDL clearance
Increase lipoprotein lipase activity
What is the side effects of niacin?
Flushing
Pruritis, paresthesia
Nausea due to release of prostaglandins
Pretreatment with aspirin may reduce the side effects Hyperuricemia
What is the MOA of Gemfibrozil?
PPAR-α) Peroxisome proliferator-activated receptor alpha agonist.
They regulate gene transcription controlling carbohydrates and fat metabolism
Activate lipoprotein lipase
Decrease VLDL, TG and LDL
Jan comes in with TG’s levels of 700 mg/dl what will you give her to bring the levels down and what is the side effects?
Fibrates:FenoFIBRATES,GemFIBRozil
Indicated in treatment of Hypertriglyceridemia (>500 mg/dl) Mildly increase HDL
Adverse effects
Myositis (when combined with statins) Hepatitis
Cholelithiasis (gall stones)
What the name of the medication inhibits Niemand Picks Cl and inhibits the absorption of dietary and biliary cholesterol
Ezetimibe
Sarah has high cholesterol what med can you use that will be effective with statin to reach LDL goal in patients with MI
Ezetimibe