Lipid Lowering Drugs

Question 1

with cholesterol synthesis inhibitors, what is the target molecule, why

Answer 1

HMG CoA reductase
*rate limiting enzyme of cholesterol synthesis

Question 2

how do statins work

Answer 2

they’re structural analogs of mevalonate, competitively inhibiting HMG CoA reductase

Question 3

how to statins affect metabolism

Answer 3

decrease cholesterol synthesis
increase LDL receptors in liver

Question 4

what are the 4 main side effects of statins

Answer 4

hepatotoxicity
myopathy
encephalopathy
hyperglycemia

Question 5

what type of familial hypercholesterolemia are statins ineffective in treating

Answer 5

IIa

Question 6

what 4 molecule production do statins decrease

Answer 6

dolichol
protein prenylation
level of Heme-A
Coenzyme Q

Question 7

how does ezetimibe act

Answer 7

blocks dietary cholesterol transporter so there is reduced cholesterol in chylomicrons

Question 8

what is the effect of decreased cholesterol on number of LDL receptors

Answer 8

lower cholesterol= increase LDL receptors
*cholesterol needs to be brought in from outside due to decreased ability to synthesis endogenous cholesterol, decreasing plasma cholesterol levels

Question 9

what is the effect of phytosterols, found in plant based oils, on absorptions of dietary fat

Answer 9

decreases

Question 10

what is the prefix of drugs used as bile acid sequesters

Answer 10

chole- or cole-

Question 11

what is the effect of bile acid sequestering drugs

Answer 11

prevent resorption of bile acids, increasing conversion of cholesterol to bile to be excreted in stool

Question 12

how do Alirocumab and Evolocumab work

Answer 12

PCSK9 inhibitors which prevent degradation of surface LDL receptors, allowing for increased LDL internalization and decreased LDL in plasma

Question 13

what does the suffix -mab mean in drugs

Answer 13

monoclonal antibody

Question 14

how does Niacin (nicotinic acid, vit B3) work

Answer 14

inhibits lipolysis in fat cells

Question 15

when is Niacin mainly used

Answer 15

when HDL is low

Question 16

what are the 3 main side effects of Niacin

Answer 16

flushing
itching
obesity

Question 17

how do fibrates work

Answer 17

activate PPAR-alpha transcription factor, increasing lipoprotein lipase activity

Question 18

what is the effect of increased lipoprotein lipase activity with fibrate usage

Answer 18

TAG–>3FA+glycerol–>decreased plasma TAG

Question 19

what is the effect of fibrate drugs on fatty acid oxidation

Answer 19

increases (decreases TAG synthesis and decreased VLDL)

Question 20

what are the side effects of fibrates

Answer 20

cholesterol gallstones (increased LDL

Question 21

Fibrates are mainly used with patients with what plasma levels

Answer 21

high triglycerides

Question 22

MTTP inhibitors such as Lomitapide block what

Answer 22

chylomicron and VLDL synthesis, lowering plasma triglyceride and cholesterol

Question 23

what is the main side effect of MTTP inhibitors

Answer 23

lipid filled enterocytes and hepatocytes

Question 24

how do pancreatic lipase inhibitors such as Orlistat work

Answer 24

inhibit pancreatic and gastric lipases, preventing digestion/reabsorption of dietary fats, decreasing chylomicrons (TAG and cholesterol reduction)

Question 25

what are 3 plasma affects of omega 3 fatty acids (Lovaza- ALA, EPA, DHA)

Answer 25

decrease plasma TAG
increase HDL
may increase LDL

Question 26

what are the best drug class to decrease total cholesterol

Answer 26

statins

Question 27

what is the best drug class to decrease LDL

Answer 27

statins

Question 28

what is the best drug class to increase HDL

Answer 28

Niacin

Question 29

what are the 2 best drug classes to decrease TAG levels

Answer 29

Niacin and Fibrates

Question 30

what is the only drug class to increase HDL

Answer 30

Niacin