lipid meds

Question 0

drug absorption blocked by cholestyramine

Answer 0

vitamin k
folic acid
ascorbic acid
iron salts
asa
digoxin
warfarin
thaizides
pravastatin and fluvastatin
ezetimide

Question 1

cholestyramine

Answer 1

first gen bile salts sequestrants
Large polymeric cationic exchange resin
must be taken with meals (powder, not appetizing)
prevent reabsorption and lead to increase in LDL receptors
increase serum Triglycerides by 15-20%
AE: dyspepsia, constipation, bloating, diarrhea
block absorption of many drugs

Question 2

colesevelam

Answer 2

second gen bile salts sequestrants
Large polymeric cationic exchange resin
capsule form
prevent reabsorption and lead to increase in LDL receptors
increase serum Triglycerides by 15-20%
AE (less than cholestyramine): dyspepsia, constipation, bloating, diarrhea
block absorption of many drugs

Question 3

drug absorption blocked by colesevelam

Answer 3

Vitamin k
folic acid
ascorbic acid
iron salts
asa
thiazides
ezetimide

Question 4

nicotinic acid (niacin)

Answer 4

regular or time release
inhibits VLDL secretion-> decreases LDL production
decrease triglycerides more than cholesterol
increase HDL
no effect on bile production
AE flush (prostaglandin mediated cutaneous vasodilation)
reversible increased LFT, hepato dysfunction w/ OTC sustained release
may increase insulin resistance of DM
Hyperuricemia (competitive for renal secretion)

Question 5

Lovastatin, simvastatin, atorvastatin

Answer 5

HMG Coa reductase competitive inhibitors
prodrugs
decrease synthesis and increase LDL receptors
First pass metabolism
CYP3A4
glycosylation-> elevated levels with gemgibrozil
AE increase LFT, increased Creatine kinase (CK), myopathy, rare rhabdomyolysis

Question 6

CYP3A4 interactions

Answer 6

increased levels with inhibitors: macrolides, cyclosporine, ketoconazole, fibrates, tacrolimus, paroxetine, grapefruit juice

decreased levels with inducers: phenytoin, barbiturates, rifampin

Question 7

CYP2C9

Answer 7

increased levels with inhibitors: ketoconazole, metronidazole, amiodarone

Question 8

pravastatin, fluvastatin, rovusastatin

Answer 8

HMG Coa reductase competitive inhibitors
decrease synthesis and increase LDL receptors
First pass metabolism
CYP2C9
glycosylation-> elevated levels with gemgibrozil
AE increase LFT, increased Creatine kinase (CK), myopathy, rare rhabdomyolysis

Question 9

gemfibrozil, clofibrate, fenofibrate

Answer 9

fibrates
activate PPARalpha receptor-> increase lipoprotein lipase, AI and AII
clear VLDL and increases HDL (modest decrease of LDL)
insulin sensitizing, antiproliferative, antifibrotic, antiinflammatory
tx high triglycerides
AE: rashes, GI symptoms, arrhythmias, decreased potassium, increased LFT, increased risk of cholesterol gall stones
gemfibrozil interact with statins (increased serum levels)

Question 10

ezetimibe

Answer 10

inhibits intestinal sterol absorption (NPCL1L)
metabolized by gluconidation (not by CYP)
excreted in bile
lowers LDLs