Drugs for Lipid Disorders - Kruse

Question 1

VLDL

Answer 1

transports TGs from liver to adipose and muscle tissue - made in the liver

Question 2

LDL

Answer 2

transports cholesterol to extrahepatic tissue - made in circulation from VLDL

Question 3

HDL

Answer 3

promotes transport of cholestrol from extrahepatic tissue to the liver for excretion

Question 4

factors the increase LDL

Answer 4

cholesterol, saturated and trans fats

Question 5

factors the increase TGs

Answer 5

total fat, alcohol, excess calories

Question 6

statin with best oral absorption

Answer 6

fluvastatin

Question 7

T1/2 of most statins

Answer 7

1-3 h

Question 8

T1/2: atorvastatin

Answer 8

14h

Question 9

T1/2: rosuvastatin

Answer 9

19h

Question 10

Statins that use CYP34A

Answer 10

lovastatub, simvastatin, and atorvastatin

Question 11

statins that use CYP2C9

Answer 11

fluvastatin and rouvastatin

Question 12

statins that use CYP450

Answer 12

pitavastatin (limited)

Question 13

potency of statins

Answer 13

atorva- = rousva- > sima- > pitava- = lova- = prava- > fluva-

Question 14

only lipid lowering agent that significatlyreguce Lp(a)

Answer 14

niacin

Question 15

most effective agent to increase HDL levels

Answer 15

niacin

Question 16

MOA: niacin

Answer 16

inhibition of lipolysis of TGs in adipose tissue; reduces fibrinogen and increases tissue plasminogen activator to help reduces edothelial cell dysfunction

Question 17

AE: statins

Answer 17

• elevated serum aminotransferase
• increased creatine kinase
• rhabdomyolysis
• myopathy
• increases warfarin levels

Question 18

CI: statins

Answer 18

• pregnancy, lactation
• liver dz
• skeletal mm myopathy
• concomitant use of other drugs that utilize CYP450 (phenytoin, griseofulvin)

Question 19

AE: niacin

Answer 19

• skin flushing
• pruitis, rash, dry skin/mm
• ancanthosis nigricans (esp in DM)
• hyperglycemia in DM

Question 20

CI: niacin

Answer 20

• hepatic dz

- active peptic ulcer

Question 21

T1/2: gemfibrozil

Answer 21

1.5h

Question 22

T1/2: fenofibrate

Answer 22

20h

Question 23

MOA: fibrates

Answer 23

angonist ligand for PPAR(apha) which regulates expression of genes involved in lipoprotein structure and function

Question 24

Therapeutic uses: fibrates

Answer 24

• tx increased VLDL hyperTGemia
• tx hyperTGemia resulting from anti-viral tx
• dysbetalipoproteinemia

Question 25

AE: fibrates

Answer 25

- mild GI disturbances - lithasis > gallstones - mysitis, myopathy, and possible rhabdo - potentiation of antigoagulant action

Question 26

CI:fibrates

Answer 26

- hepatic dz | - renal dysfunction

Question 27

MOA: resins

Answer 27

postively chds cmpds bind negatively chgd bile acids; increases LDL clearance

Question 28

AE: resins

Answer 28

- GI effect | - impaired abs of other drugs (take 1 our before of 2 hours after resins)

Question 29

CI: resins

Answer 29

- diverticulitis - preexisting bowel dz - cholestasis

Question 30

cholesterol absorption inhibitors

Answer 30

ezetimibe

Question 31

T1/2: ezetimibe

Answer 31

22h

Question 32

vytorin

Answer 32

ezetimibe + simvastatin

Question 33

tx: lomitapide

Answer 33

homozygous familia hypercholserolemia

Question 34

MOA: lomitapide

Answer 34

- binds microsolmal tiglyceride transfer protein - reduces chylomicron and VLDA - reduces plasma LDL levels

Question 35

AE: lomitapmide

Answer 35

- inhibitis CYP3A4 - GI symptoms - increased liver aminotransferae levels - hepatic fat accumulation

Question 36

tx: mipomersen

Answer 36

homozygous familial hypercholesterolemia

Question 37

MOA: mipomersen

Answer 37

disruption of apolipoprotein B-100 (binds LDL)

Question 38

AE: mipomersen

Answer 38

- injection site reaction - flu-like s/s - HA - elevated liver enzymes