Antihyperlipidemic Drugs

Question 1

what is the normal serum cholesterol according to the AHA

Answer 1

normal up to 200 mg/dl
borderline is up to 239
elevated is above 240

Question 2

what is the equation for LDL cholesterol

Answer 2

total cholesterol-HDL- (TG/5)

Question 3

Answer 3

Question 4

what are the 6 classes of antihyperlipidemic drugs

Answer 4

1. statins (HMG-CoA reductase inhibitor)
2. bile acid sequestrants
   3.nicotinic acid (niacin)
3. fibrates
4. cholesterol uptake inhibitors
5. mipomersen

Question 5

what is the MOA of statins

Answer 5

inhibit the rate limiting step in cholesterol biosynthesis

(when intrinsic cholesterol synthesis is blocked, the liver increases the uptake of cholesterol from the plasma)

Question 6

what does the increase in cholesterol uptake from the plasma (due to statins) lead to (2 things)

Answer 6

upregulation of hepatic LDL receptors and decreases plasma LDL

Question 7

what are the therapeutic effects of statins

Answer 7

decrease LDL, VLDL, and triglycerides

Question 8

why are statins used for secondary prevention of heart disease

Answer 8

they improve endothelial function, modulate inflammatory response, maintain plaque stability and increase NO and decrease mRNA for endothelin-1 causing vasodilation

Question 9

what are the three drug interactions of statins

Answer 9

inhibitors of P450
grapefruit juice
red yeast rice

Question 10

adverse effects of statins

Answer 10

1. myopathy
2. hepatotoxicity: elevated AST (stop if >3x normal)

Question 11

what is the MOA of bile acid sequestrants

Answer 11

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.

Question 12

why are bile acid sequestrants contraindicated in hypertriglyceridemia

Answer 12

they increase VLDL and TG

Question 13

what are the adverse effects of bile acid sequestrants

Answer 13

Fat malabsorption (steatorrhea) and malabsorption of Fat-soluble vitamins ADEK

Question 14

what are the three common bile acid sequestrants

Answer 14

Cholestyramine
Colestipol
Colesevelam

Question 15

what is the MOA of nicotinic acid (niacin)

Answer 15

Inhibits the hepatic production of VLDL and its metabolite LDL
Increases HDL by delaying hepatic HDL clearance
Increase lipoprotein lipase activity

Question 16

what are the adverse effects of niacin

Answer 16

Flushing
Pruritis, paresthesia and nausea due to release of prostaglandins
Pretreatment with aspirin may reduce the side effects
Hyperuricemia

Question 17

what are the drugs of choice for hypertriglyceridemia

Answer 17

Fibrates (fenofibrate and gemfibrozil)

Question 18

what are the two most common fibrates

Answer 18

fenofibrate and gemfibrozil

Question 19

what is the MOA of fibrates (fenofibrate and gemfibrozil)

Answer 19

(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

Question 20

we don’t use fibrates unless the triglyceride levels exceed ____mg/dl

Answer 20

500

Question 21

what are the adverse effects of adverse effects of fibrates

Answer 21

Myositis (when combined with statins)
Hepatitis
Cholelithiasis (gall stones)

Question 22

what class of drug is ezetimibe

Answer 22

cholesterol uptake inhibitor

Question 23

what is the MOA of ezetimibe

Answer 23

Inhibits the absorption of dietary and biliary cholesterol at the intestine by inhibiting
Niemann Pick C1 like protein (cholesterol transporter)

Question 24

cholesterol uptake inhibitors (ezetimibe) is used effectively with ________ to reach LDL goal in patients with ____ and Modestly reduces LDL

Answer 24

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

Question 25

what are the adverse effects of ezetimibe

Answer 25

headache, myalgia, sinusitis, and pharyngitis

Question 26

what is the antihyperlipidemic drug that is given as an injection weekly

Answer 26

mipomersen

Question 27

what are the adverse effects of mipomersen

Answer 27

hepatic fat accumulation and pain @ injection site

Question 28

what is the MOA of mipomersen

Answer 28

antisense oligonucleotide against Apo B-100 mRNA

Question 29

what drugs fall under the class of PCSK9 Inhibitors

Answer 29

evolocumab (repatha)
Alirocumab (praluent)

Question 30

what is the MOA of PCSK9 inhibitors

Answer 30

MOA: Inhibits (PCSK9)
proprotein convertase subtilisin kexin type 9
decrease recycling of LDL

Question 31

what drug is Indicated in heterozygous familial hypercholesterolemia
Used as adjunct or in patients who cannot tolerate statins

Answer 31

evolocumab or alirocumab (PCSK9 inhibitors)

Question 32

adverse effects of PCSK9 inhibitors (evolocumab and alirocumab)

Answer 32

Injection site reaction and hypersensitivity reaction
ALT, AST increased
Musculoskeletal Pain

Question 33

what drugs can be indicated or obesity

Answer 33

amphetamine derivatives, orlistat, lorcaserin, or a combo of phentermine and topiramate

Question 34

what is the MOA of orlistat

Answer 34

decrease fat absorption by blocking gastric and pancreatic lipases

Question 35

what is the MOA of lorcaserin

Answer 35

5-HT2c agonist
anorexiant