Anti-hyperlipidemia/dyslipidemia drugs

Question 1

high-intensity statins?

Answer 1

atorvastatin & rosuvastatin

Question 2

moderate intensity statins?

Answer 2

atorvastatin, rosuvastatin, simvastatin, pravastatin, lovastatin, fluvastatin, pitavastatin

Question 3

low intensity statins?

Answer 3

simvastatin, pravastatin, lovastatin, fluvastatin, pitavastatin

Question 4

MOA of statin?

Answer 4

inhibit HMG-CoA reductase, inhibits cholesterol production, increases cholesterol uptake from blood stream by increasing LDL receptors, PCSK9 upregulation

Question 5

distinguishing characteristics: variable onset, peaks effectively typically in a few weeks, duration variable, metabolism variable & typically involves a CYP

Answer 5

atorvastatin

Question 6

statins that don’t utilize CYP3A4?

Answer 6

rosuvastatin
pravastatin
pitavastatin

Question 7

predicted action for statins? uses?

Answer 7

first line therapy for primary & secondary prevention of ASCVD and familial hypercholesterolemia
uses: ASCVD, hypercholesterolemia

Question 8

C/I in active liver dz, PG & breast feeding; can cause myopathy, increase in liver enzymes, nausea, H/A

Answer 8

statins

Question 9

natural products that interact w/statin therapy?

Answer 9

red yeast rice will propagate
niacin might increase response
alcohol induces toxicity
grapefruit inhibits CYP3A4

Question 10

BAS used as tx for hyperlipidemia?

Answer 10

cholestyramine

Question 11

MOA: resins that bind bile acids in the intestines, reduces enterohepatic recycling, increases hepatic conversion of cholesterol to bile acid, upregulates LDL receptors on the liver
distinguishing characteristics: not metabolized
uses: hypercholesterolemia for high risk pt who is intolerant to other main tx or are on maximal dose of other tx

Answer 11

cholestyramine

Question 12

MOA: prevents absorption of dietary biliary cholesterol, upregulates LDL receptors in liver, lowers plasma LDL
distinguishing characteristics: 30% undergoes glucoronide conjugation in the small intestine and liver; about 80% excreted in the feces
uses: adjunctive tx in homozygous familial hypercholeseterolemia and primary hyperlipidemia, typically used when intolerant to other main tx
C/I in PG and breast feeding, increase in liver enzymes when administered w/other main tx
inhibits sterol absorption in the gut and would lower effectiveness of green tea, omega-3 FAs, sitostanol and b-sitosterol

Answer 12

ezetimibe

Question 13

2 fibrates?

Answer 13

fenofibrate

gemifibrozil

Question 14

MOA: lowers production & increased clearance of VLDL, increases HDL production, lowers TG & increases HDL but has variable effect on LDL
distinguishing characteristics: metabolized through glucuronidation in the liver or KD, excretion is ~60% in the urine

Answer 14

fibrates: fenofibrate and gemifibrozil

Question 15

uses: hypercholesterolemia or mixed dyslipidemia as adjunct therapy or monotherapy in pts who can’t tolerate other main tx; hypertriglyceridemia (first line tx)
C/I in liver dz, severe renal impairment, ESRD, pre-existing GB dz, break feeding
SEs: dyspepsia, gallstones, myopathy
interaction w/red rice yeast may increase myopathy risk, niacin might increase hepatotoxicity of this tx, alcohol might increase hepatotoxicity

Answer 15

fibrates: fenofibrate & gemifibrozil

Question 16

2 supplements that might help w/dyslipidemia?

Answer 16

niacin & omega 3 FAs

Question 17

MOA: unclear, may increase lipoprotein lipase activity, enhance TG removal from plasma, reduce TG synthesis, increase HDL-C levels
distinguishing characteristics: metabolized into NAD+ in liver, but pathways become saturated at doses used to tx hyperlipidemia, ~70% excreted in urine
uses: hypercholesterolemia or mixed dyslipidemia as adjunct therapy for pts who do not tolerate fibrates or omega 3 FAs or monotherapy for pts who don’t tolerate statins, BAS or fibrates

Answer 17

niacin

Question 18

C/I in active liver dz, gout, PUD

SEs: hepatotoxicity, hyperglycemia, hyperuricemia, upper GI distress, flushing, itching

Answer 18

niacin

Question 19

MOA: Inhibits the release of FA from adipose tissue; inhibits beta oxidation of hepatic FA; inhibits FA synthesis; increase VLDL clearance; lowers TG and increases HDL
distinguishing characteristics: metabolized by lipid enzymes in liver & other tissues
use: hypertriglyceridemia 2nd line pharmacotherapy
C/I in pts who are sensitive to this tx option
SEs: eructations, dyspepsia, taste changes, may increase bleeding time

Answer 19

omega 3 FAs