Drugs for Management of Dyslipidemia Lecture PDF

Question 1

What is the rate limiting step of cholesterol formation

Answer 1

3 hydroxy 3 methylglutaryl coenzyme A (HMG-CoA)

Question 2

One of the most serious reactions to statin drugs

Answer 2

-fatal rhabdomyolysis

Question 3

Statin mech of action

Answer 3

Inhibition of HMG CoA reductase resulting in increase # of LDL cholesterol receptors in the liver ultimately decreasing overall level of LDL in bloodstream

Question 4

Most statins are given in the evening because…

Answer 4

….cholesterol synthesis increases during night

Question 5

Only statin with FDA approval for increasing of HDL cholesterol even though many do this to some extent anyways

Answer 5

simvastatin (zocor)

Question 6

Statin therapeutic uses (6)

Answer 6

• hypercholesterolemia (lowering LDL-C)
• primary prevention of CV events
• 2ndary prevention of CV events
• primary prevention in those with normal LDL levels
• Post MI therapy
• diabetes even those without high cholesterol who have just one additional risk factor

Question 7

Statin administration

Answer 7

PO, 30-90% bioavailable and acts on liver

Question 8

Statin drug interactions which 4 agents and what 4 drugs

Answer 8

4 agents (artovastatin, cervivastatin, lovastatin, and smivastatin) can see interaction with

• itraconazole
• cyclosporine
• erythromycin
• grapefruit juice

Question 9

Statins ADR’s (4)

Answer 9

• GI disturbances
• hepatotoxicity (recommends baseline liver enzyme measurement before starting statins)
• rhabdomyolysis (rare but needs warning to patient)
• new onset of diabetes (risk less than benefits)

Question 10

Statin use is completely contraindicated in…

Answer 10

….pregnancy

Question 11

Ezetimibe (zetia) drug class and mech of action

Answer 11

• Cholesterol absorption inhibitor
• selectively inhibits intestinal absorption of dietary and biliary choesterol at brush border of small intestine leading to decreased delivery to liver and therefore reducing all overall blood cholesterol levels

Question 12

Ezetimibe (zetia) ADR’s (3)

Answer 12

• diarrhea
• rhabdo
• hepatitis

Question 13

PCSK9 inhibitors mech of action

Answer 13

Binds to LDL receptors on hepatocytes promoting receptor degradation thereby preventing LDL-C clearance from blood increasing serum LDL-C conc.

Question 14

PSCK9 inhibitors ADR

Answer 14

-neurocognitive events

Question 15

Alirocumab (praluent)/Evolocumab (repatha) drug class and therapeutic use

Answer 15

• PCSK9 inhibitor

- approved as adjunct to diet and statin therapy for adults with hypercholesterolemia

Question 16

Bile acid binding resins function and 3 example agents

Answer 16

Were once main drug for decreasing LDL level, today primarily reserved for adjunct therapy with statins that form insoluble complex with bile acids in intestine, relies on liver’s ability to produce LDL receptors

includes cholestyramine, colestipol, and colesvelam

Question 17

Bile binding resins drug interactions (1)

Answer 17

-form insoluble complexes with other drugs preventing absorption including statins, require medication be given 2 hours before or 4-6 hrs after

Question 18

Fibrates function and what is it the most effective drug for?

Answer 18

Activate nuclear transcription factor peroxisome proliferator activated receptor (PPAR a) which regulates genes that control lipid and glucose metabolism, inflammation, and endothelial function, most effective drug for decreasing triglycerides

Question 19

Gemfibrozil (lopid) therapeutic uses (2)

Answer 19

• lower VLDL and triglycerides

- raise HDL

Question 20

fenofibrate (tricor, lofibra, triglide, anatara) function

Answer 20

Treat hypertriglyceridemia in pts not responding to dietary measurements, lowers triglycerides by decreasing VLDL

Question 21

Nicotinic acid (niacin) function

Answer 21

Lowers all plasma lipoproteins and triglycerides

Question 22

Long chain omega 3 polyunsaturated fatty acids (PUFA’s) function

Answer 22

Lower triglycerides and decrease fasting conc. by 20-50% b

Question 23

Alirocumab function and drug class

Answer 23

Human monoclonal Ab that acts as a PCSK9 inhibitor

Question 24

Only fibrate with demonstrated beneficial effects on CV outcomes, but contraindicated in use with statins for risk of myopathy

Answer 24

-Gemfibrozil