Antihyperlipidemic Drugs Flashcards
what is the normal serum cholesterol according to the AHA
normal up to 200 mg/dl
borderline is up to 239
elevated is above 240
what is the equation for LDL cholesterol
total cholesterol-HDL- (TG/5)
what are the 6 classes of antihyperlipidemic drugs
- statins (HMG-CoA reductase inhibitor)
- bile acid sequestrants
3.nicotinic acid (niacin) - fibrates
- cholesterol uptake inhibitors
- mipomersen
what is the MOA of 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)
what does the increase in cholesterol uptake from the plasma (due to statins) lead to (2 things)
upregulation of hepatic LDL receptors and decreases plasma LDL
what are the therapeutic effects of statins
decrease LDL, VLDL, and triglycerides
why are statins used for secondary prevention of heart disease
they improve endothelial function, modulate inflammatory response, maintain plaque stability and increase NO and decrease mRNA for endothelin-1 causing vasodilation
what are the three drug interactions of statins
inhibitors of P450
grapefruit juice
red yeast rice
adverse effects of statins
- myopathy
- hepatotoxicity: elevated AST (stop if >3x normal)
what is the MOA of bile acid sequestrants
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.
why are bile acid sequestrants contraindicated in hypertriglyceridemia
they increase VLDL and TG
what are the adverse effects of bile acid sequestrants
Fat malabsorption (steatorrhea) and malabsorption of Fat-soluble vitamins ADEK
what are the three common bile acid sequestrants
Cholestyramine
Colestipol
Colesevelam
what is the MOA of nicotinic acid (niacin)
Inhibits the hepatic production of VLDL and its metabolite LDL
Increases HDL by delaying hepatic HDL clearance
Increase lipoprotein lipase activity
what are the adverse effects of niacin
Flushing
Pruritis, paresthesia and nausea due to release of prostaglandins
Pretreatment with aspirin may reduce the side effects
Hyperuricemia
what are the drugs of choice for hypertriglyceridemia
Fibrates (fenofibrate and gemfibrozil)
what are the two most common fibrates
fenofibrate and gemfibrozil
what is the MOA of fibrates (fenofibrate and 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 cholesterol
we don’t use fibrates unless the triglyceride levels exceed ____mg/dl
500
what are the adverse effects of adverse effects of fibrates
Myositis (when combined with statins)
Hepatitis
Cholelithiasis (gall stones)
what class of drug is ezetimibe
cholesterol uptake inhibitor
what is the MOA of ezetimibe
Inhibits the absorption of dietary and biliary cholesterol at the intestine by inhibiting
Niemann Pick C1 like protein (cholesterol transporter)
cholesterol uptake inhibitors (ezetimibe) is used effectively with ________ to reach LDL goal in patients with ____ and Modestly reduces LDL
Statin; MI
what does this mean? adjunct drug if the patient isn’t reaching the goal of 70 and they are maxed out on statins
what are the adverse effects of ezetimibe
headache, myalgia, sinusitis, and pharyngitis
what is the antihyperlipidemic drug that is given as an injection weekly
mipomersen
what are the adverse effects of mipomersen
hepatic fat accumulation and pain @ injection site
what is the MOA of mipomersen
antisense oligonucleotide against Apo B-100 mRNA
what drugs fall under the class of PCSK9 Inhibitors
evolocumab (repatha)
Alirocumab (praluent)
what is the MOA of PCSK9 inhibitors
MOA: Inhibits (PCSK9)
proprotein convertase subtilisin kexin type 9
decrease recycling of LDL
what drug is Indicated in heterozygous familial hypercholesterolemia
Used as adjunct or in patients who cannot tolerate statins
evolocumab or alirocumab (PCSK9 inhibitors)
adverse effects of PCSK9 inhibitors (evolocumab and alirocumab)
Injection site reaction and hypersensitivity reaction
ALT, AST increased
Musculoskeletal Pain
what drugs can be indicated or obesity
amphetamine derivatives, orlistat, lorcaserin, or a combo of phentermine and topiramate
what is the MOA of orlistat
decrease fat absorption by blocking gastric and pancreatic lipases
what is the MOA of lorcaserin
5-HT2c agonist
anorexiant
