Drugs for hyperlipidemia

Question 1

What are the primary drugs in the bile acid resin binding agents?

Answer 1

Cholestyramine (Questran)
Colestipol (Colestid)
Colesevelam (WelChol)

Question 2

What population will bile acid resin not have effect in?

Answer 2

Familial Hyperlipidemia (no LDL receptor)

Question 3

What is the hallmark side effect of bile acid resins?

Answer 3

Constipation and bloating

Question 4

What is the MOA of bile acid-binding resins?

Answer 4

Bind bile acids and prevent their intestinal absorption

Question 5

What overall effect will a decrease in bile acids have on LDL receptors? In whom is this effect not seen?

Answer 5

An increase in expression of LDL receptors leads to more LDL uptake to create bile acids; familial hypercholesterolemia

Question 6

What is the primary indication for bile acid-binding resins?

Answer 6

Whenever LDL is elevated

Question 7

When should bile acid-binding resins be taken?

Answer 7

With meals. Not absorbed (obviously) which makes them the safest

Question 8

What are two rare side effects of bile acid-binding resins?

Answer 8

Gallstone formation in obese patients, hypoprothrombinemia due to Vit K malabsorption

Question 9

Absorption of these drugs may be impaired by use of bile acid binding resins

Answer 9

digitalis, thiazides, STATINS, tetracyclines, aspirin, thyroxine

Question 10

What is the MOA for Niacin?

Answer 10

lowers plasma VLDL and LDL by inhibiting VLDL secretion by the liver.

Question 11

What is the primary indication for Niacin use?

Answer 11

to increase levels of HDL

Question 12

What are the hallmark adverse effects of niacin?

Answer 12

Cutaneous vasodilation (“niacin flush”), elevated aminotransferases or alkaline phosphatases will decrease glucose tolerance

Question 13

What drugs are in the HMG-CoA reductase inhibitors?

Answer 13

Statins: Atorvastatin, fluvastatin, pravastatin, rosuvastatin

Question 14

What is the MOA of HMG-CoA reductase inhibitors?

Answer 14

structural analogs of HMG-CoA reductase intermediate in mevalonate synthesis

Question 15

How do statins reduce plasma LDL?

Answer 15

By inhibiting the reductase to increase high-affinity LDL receptors (still effective in LDL receptor deficiency because they have another MOA)

Question 16

What are the indications and therapeutic effects of statins?

Answer 16

DECREASE LDL (most effective), decrease TG, increase HDL

Question 17

What other benefits come from statins?

Answer 17

Decrease in CRP, increase plaque stability, decreases platelet aggregation

Question 18

Which two statins are inactive and hydrolyzed to active form?

Answer 18

Lovastatin and simvastatin

Question 19

When should statins be taken?

Answer 19

at night

Question 20

Which drug for hyperlipidemia has a high first pass rate and liver metabolism, therefore has many drug interactions?

Answer 20

Statins

Question 21

What are the adverse side effects of statins?

Answer 21

Increase in serum aminotransferase (reversible and often asymptomatic), increased serum CK, can lead to rhabdomyolysis (myoglobinuria)
Liver damage

Question 22

What are absolute contraindications for the use of statins?

Answer 22

PREGNANCY and ACTIVE HEPATIC DISEASE

Question 23

What are P450 inhibitors that will increase the plasma concentrations of statins?

Answer 23

Grapefruit juice, macrolides, ketoconazole, verapamil, cyclosporine

Question 24

Wha are P450 activators that will decrease plasma concentration of statins?

Answer 24

phenytoin, griseofulvin, barbituates, rifampin

Question 25

What other antihyperlipidemia drug will inhibit the metabolism of statins?

Answer 25

Gemfibrozil and other fibrates

Question 26

What is the MOA of fibric acid derivatives?

Answer 26

Upregulate LPL and other genes involved to increase LPL activity and increase catabolism of VLDL

Question 27

What is the overall effect of fibrates?

Answer 27

TO DECREASE TGs by lowering VLDL concentration, will also decrease cholesterol

Question 28

What is a hallmark adverse effect of fibrates? What serum level of a lipid panel would also elevate with use of fibrates?

Answer 28

increased cholelithiasis or gallstones; increase LDL

Question 29

What is the MOA for Ezetimibe (zetia)?

Answer 29

Selectively blocks the intestinal absorption of cholesterol and sterols

Question 30

When is ezetimibe indicated? When does it work well?

Answer 30

To decrease moderate LDL; produces reductions as great as 25% of that achieved by a statin alone if combined with a statin

Question 31

What can you do to prevent niacin flush?

Answer 31

Take aspirin beforehand (decrease PG)