Anti Lipid Drugs

Question 1

moa of HMG CoA reductase inhibs

Answer 1

block synthesis of CE and increase LDL uptake via receptors

Question 2

extra CV benefit of statins

Answer 2

reduce plt activation and VTE risk

Question 3

when to take statins

Answer 3

at night, peak CE synth b/w midnight and 2

Question 4

pregnancy and statins

Answer 4

bad! category X, CE necessary for embryo formation, switch to BABAs for lipid control

Question 5

statin toxicities

Answer 5

hepatotoxicity- esp w/ underlying liver disease

myopathy-low baseline risk but higher w/ age, dose, hepatic/renal dysfn, other drugs; can progress to rhabdomyolysis

some risk of insulin insensitivity

Question 6

3 key drugs that interfere with statin metabolism and the enzyme involved

Answer 6

gemfibrozil, amlodipine, warfarin- inhibit CYP3A4 which inactivates simvastatin, lovastatin, atorvastatin

Question 7

amlodipine and statins

Answer 7

lower dose, inhibition of CYP3A4 raises risk of myopathy

Question 8

major effect of statins

Answer 8

significant lowering of LDL and TG, nothing for HDL

Question 9

BABA moa

Answer 9

increase elimination of bile acids, pushing CE towards more bile acid formation

Question 10

BABA ex

Answer 10

colestipol

Question 11

PK of BABA

Answer 11

needs to be given in GRAMS, used as alt to statins in pregnancy, can be used w/ statins

Question 12

BABA toxicities

Answer 12

no systemic toxicities, but GI may be severe

Question 13

drug interaction w/ BAB

Answer 13

BABA reduce absorption of drugs from GIT, take other drugs hours before or after BABA

Question 14

effect of BABAs

Answer 14

lower LDL, slight raise in HDL

Question 15

what is niacin how much is given

Answer 15

vitamin B3, doses of 1-2 grams

Question 16

niacin moa

Answer 16

inhibit synthesis of TG in liver

Question 17

toxicities of niacin

Answer 17

flushing and pruritus

hepatotoxicity and insulin resistance (caution w/ diabetics)

Question 18

niacin effects

Answer 18

lowers LDL, SIGNIFICANT TG lowering, significant HDL raising

Question 19

fibric acid derivatives moa

Answer 19

increase LDL receptor expression, activate LPL, increase FFA metabolism

Question 20

toxicities of fibric acids

Answer 20

myopathy when used in common w/ high dose statins (FAD inhibit statin absorption in liver)

Question 21

important drug interaction for FADs

Answer 21

oral anti coag like warfarin, competes at albumin binding site and increases serum free warfarin and bleeding risk

Question 22

2 FAD exs

Answer 22

gemfibrozil, fenofibrate

Question 23

effects of FAD

Answer 23

variable LDL lowering, significant TG lowering, minor HDL increase

Question 24

ezetimibe moa

Answer 24

blocks CE absorption from intestines at NPC1 receptor, indirectly stimulating LDL-R expression

Question 25

homeostatic response to ezetimibe/statins

Answer 25

to ezetimibe- increase CE synthesis, to statins- increase absorption

Question 26

vytorin moa

Answer 26

combine ezetimibe and statins- block absorption and synthesis

Question 27

ezetimibe effects

Answer 27

lower LDL only

Question 28

vytorin effects

Answer 28

even more significant lowering of LDL than statins alone

Question 29

PSK9 inhibitor mechanism

Answer 29

promote CE uptake in liver by inhibiting PSK9 protein that induces LDL-R degredation therefore raising number of LDL-R

Question 30

PSK9 inhib ex and structure

Answer 30

alirocumab, mab and must be injected biweekly, very expensive

Question 31

PSK9 inhib effect

Answer 31

very significant LDL reduction, more than statins