anti-hyperlipidemics

Question 1

ezetimibe AE

Answer 1

• low incidence of liver/skeletal muscle damage

Question 2

ezetimibe MOA

Answer 2

cholesterol absorption inhibitor; inhibitor of NPC1L1

Question 3

what are the bile acid binding resins?

Answer 3

cholestyramine, colestipol

Question 4

What ion do the bile acid binding resins excgange

Answer 4

chloride ion for bile acids

Question 5

which statins are not cyp substrates?

Answer 5

pravastatin, pitavastatin

Question 6

which statins are prodrugs?

Answer 6

lovastatin and simvastatin

Question 7

statin MOA

Answer 7

HMG-CoA reductase competitive inhibitors

Question 8

what is HMG co-A reductase?

Answer 8

the rate-limiting enzyme in cholesterol biosynthesis

Question 9

what intermediate in the cholesterol synthesis pathway do statins resemble?

Answer 9

mevalonate (mevalonic acid)/HMG CoA

Question 10

which statins are metabolized by CYP 3A4?

Answer 10

lovastatin, simvastatin, and atorvastatin

Question 11

which statins are metabolized by CYP 2c9?

Answer 11

Fluvastatin, rosuvastatin

Question 12

which statin is excreted in the bile?

Answer 12

pitvastatin (avoid if liver issues?)
enterohepatic recirculation

Question 13

AE of statins

Answer 13

• rhabdomyolysis: myopathy with renal dysfunction.
• monitor CPK (serum creatinine phosphokinase)
• increased incidence with co-adm with cyp inhibitors (gemfibrozil)
• hepatotoxicity: monitor serum transaminase
• increased incidence of T2DM

Question 14

what is the ATP citrate lyase inhibitor?

Answer 14

bempedoic acid (nexletol)

Question 15

MOA of bempedoic acid

Answer 15

• ATP citrate lyase inhibitor
• enzyme upstream of HMG-CoA reductase

Question 16

bempedoic acid use

Answer 16

adjunct to statins in ASCVD and familial hypercholesterolemia

Question 17

SE of bempedoic acid

Answer 17

• excreted renally
• inhibits OAT-2 in renal tubules: hyperuricemia and GOUT

Question 18

what are the pcsk9 inhibitors

Answer 18

• praluent (alirocumab)
• repatha (evolocumab)
• leqvio (inclisiran)

Question 19

use of pcsk9 inhibitors

Answer 19

• known ascvd
• familial hypercholesteremia
• used with statins and diet

Question 20

praluent and repatha MOA

Answer 20

human igG Abs against PCSK9

Question 21

leqvio (inclisiran) MOA

Answer 21

siRNA degradation of PCSK9 in hepatocytes

Question 22

praluent and repatha doses

Answer 22

injection every 2 weeks

Question 23

leqvio dosing

Answer 23

injections at every 3 and then 6 months

Question 24

apo b lipoprotein synthesis inhibitor

Answer 24

juxtapid (lomitapide)