Hyperlipidemic drugs

Question 1

Statin MOA

Answer 1

inhibition of HMG coa reductase

Question 2

Statin effect

Answer 2

great for lowering ldl, some lowering of TG and increase in HDL

Question 3

Statin that doesn’t use Cyp 450 system

Answer 3

pravastatin- less drug interactions and less chance for rhabdo

Question 4

Cyp3A4 statins

Answer 4

Lovastatin
Simvastatin
Atorvastatin
inhib of 3a4: grapefruit juice, cyclosporine, ritonavir, ittraconalol, erythromycin
induc of 3a4: phyenytoin, barbiturate, rifampin, thiazides

Question 5

Cyp 2c9 statin

Answer 5

Fluvastatin

inhibit of 2c9: azole drugs

Question 6

Cyp 2C19 statin

Answer 6

Rosuvastatin

Question 7

State AE and contra

Answer 7

AE: myalgia, and RHABDO (less with pravastatin)
Contra: pregnancy and liver ailure.
GEMFIBROZIL inhibit OATP2 transport into liver…risk for rhabdo increases

Question 8

Bile acid binding resins

Answer 8

Chelestyramine, colestipol, colesevelam

Question 9

Bile acid binding resins MOA

Answer 9

bind to bile acids and prevent respsorption in intestine

Question 10

Bile acid binding resins effect

Answer 10

modest decrease in LDL (use in pregnant women who cant take statins…or in combo with statins)…but INCREASE IN TGs

Question 11

Bile acid bindin resins AE and contra/ drug

Answer 11

AE: well tolerated, but can cause lack of absorption of vit (ADEK), …NOT colesvelam
also interacts with any drugs (NOT colesevelam)
contraindications: high triglycerides

Question 12

Ezetimibe MOA

Answer 12

Cholesterol absorption inhibitor…works by inhibiting Niemann pick C1 like protein (NPC1L1)

Question 13

Ezetimibe effects

Answer 13

reduce LDL minimally…no other effects…combine w/ statin

Question 14

Ezetimibe SE

Answer 14

well tolerated, some GI

Question 15

PCSK9 inhibitors

Answer 15

Alirocumab

Evolocumab

Question 16

PCSK9 inhibit MOA and indications

Answer 16

antibodies inhibiting protein PCSK9…which destroys LDL receptors
indications: heterozygous FH, r not achieved goals with Statins

Question 17

Lopmitapide MOA and indication

Answer 17

indication: homozygous FH
moa: inhibitor of MTP (stopping assembly of chylomicrons and VLDL

Question 18

Mipomersen MOA and indication

Answer 18

indication: homozygous FH
MOA: reduces expression of apoB100, decreasing produciion of VLDL

Question 19

Niacin effects

Answer 19

decrease LDL, raise HDL (best), and decrease TG. Reduce risk of MI and used in combo withothers

Question 20

Niacin MOA

Answer 20

dec lipolysis= decreasing FFA and VLDL
inhib DGAT2= dec VLDL synthesis
inhibit APOCIII= inc VLDL clearance
increase apoAI expression: inc HDL prod
dec Lp(a)= dec thrombosis

Question 21

Niacin AE

Answer 21

Skin flushing (can help with NSAID)
increased risk of Gout
Peptic ulcers worst

Question 22

Fibrates

Answer 22

Gemfibrozil

Fenofibrate

Question 23

Fibrate effect

Answer 23

reduce TG, mild reduction in LDL, increase HDL

Question 24

Fibrate MOA

Answer 24

activate PPARa (transcription facto: promoting genes involved in lipoprotein structure

Question 25

Fibrinate AE

Answer 25

increased gallstones

Rhabdo: especially with gemfibrozil (increased with STATINS!

Question 26

Fibrate drug interaction

Answer 26

anti oags- increased bleeding

sulfonylureas: enhanced glucose lowering

Question 27

Fibrate contraindications

Answer 27

Severe renal / hepatic diseaase