Duan: Antihyperlipidemic Drugs

Question 1

What are these?

lovastatin
simvastatin
pravastatin
fluvastatin
atorvastatin
rosuvastatin

Answer 1

HMG-CoA reductase inhibitors

**inhibit conversion of HMG-CoA to mevalonate, a cholesterol precursor

Question 2

What do HMG-CoA reductase inhibitors do to LDL, HDL, and TAGs?

Answer 2

decrease LDL
increase HDL
decrease TAGs

Question 3

What are these?

cholestyramine
colestipol
colesevelam

Answer 3

bile acid resins

Question 4

How do bile-acid resins work?

Answer 4

essentially they bind bile acids in the intestine, prevent their intestinal absorption, and increase their fecal secretion

**this causes the liver to use cholesterol to make more bile acids (results in increased production of LDL receptors and an increase in activity of HMG-CoA reductase)

Question 5

What is the main effect of bile acid resins, in regards to LDL, HDL, and TAGs?

Answer 5

decreases LDL!
modest increase in HDL and TAGs

**used in patients with elevated LDL

Question 6

Inhibits lipolysis in adipose tissue; reduces hepatic VLDL synthesis leading to decreased LDL

Answer 6

niacin

**use reduces apoB-containing lipoprotein (VLDL, IDL, LDL) synthesis

Question 7

What does niacin do to LDL, HDL, and TAGs?

Answer 7

decreases LDL and TAGs, slight increase in HDL

• *used to treat most forms of hyperlipoproteinemia (except familial lipoprotein lipase deficiency)
• *drug of choice for hypertriglyceridemia associated with elevated chylomicrons

Question 8

One side effect to consider with nicotinic acid (niacin)?

Answer 8

intense cutaneous flush (red flushed face) and itching

**can also cause hyperglycemia and hyperuricemia

Question 9

List two fibrates we should know about

Answer 9

Gemfibrozil

Fenofibrate

Question 10

What is the mechanism of action of fibrates?

Answer 10

activate PPAR-alpha to induce HDL synthesis
upregulate LPL to decreases TAGs

**increase HDL
decrease LDL and TAGs

Question 11

When are fibrates useful?

Answer 11

for lowering VLDL levels in patients with hypertriglyceridemia

Question 12

What is one BONUS to fibrate use?

Answer 12

they raise HDL!

Question 13

Selectively inhibits cholesterol absorption in the intestinal lumen at the enterocyte brush border

Answer 13

Ezetimibe

**decreases LDL

Question 14

Inhibits activity of intestinal lipases. A portion of the dietary fat is not digested and excreted with the feces

Answer 14

Orlistat

**used for treatment of obesity

Question 15

When is Orlistat contraindicated?

Answer 15

in pts with medical causes of obesity or gallbladder disease

Question 16

Gallstone solubilizing agent, which causes dissolution of radiolucent gallstones
Increases concentration at which saturation of
cholesterol occurs, so slowly dissolve.

Answer 16

Ursodiol

Question 17

What is the optimal LDL cholesterol level?
What is the optimal total cholesterol level?
What is the optimal HDL cholesterol level?

Answer 17

LDL:
less than 100

Total cholesterol:
less than 200

HDL:
>40 (men), >50 (women)

Question 18

Prescribed for lowering LDL
For heterozygous forms of familial hypercholestrolemia
For secondary hypercholesterolemia caused by diabetes mellitus

Answer 18

statins

Question 19

What should you combine statins with to have greater additive effects with up to 50% reduction in LDL levels?

Answer 19

bile-binding resin or ezetimibe

Question 20

When should statins be taken?

Answer 20

before bed!

**this is when the majority of cholesterol is synthesized

Question 21

What can cause the myopathy associated with statin use?

Answer 21

grapefruit or grapefruit juice which interferes with metabolism of statins in liver

Question 22

What should bile-acid binding resins be combined with to have an additive effect in lowering LDL?

Answer 22

niacin

statins

Question 23

Drug of choice for severe hypertriglyceridemia associated with elevated chylomicrons

Answer 23

Niacin

Question 24

Lowers triglycerides

Reduces levels of postprandial chylomicrons and VLDL

Answer 24

Omega-3 acid ethyl esters

Question 25

Define the requirements for metabolic syndrome

Answer 25

Any 3 of following risk factors:

Abdominal obesity – men >40”, women > 35”

TG greater than 150 mg/dL

HDL – men < 40 mg/dL, women < 50 mg/dL

Blood pressure greater than 130 / 85 mm Hg

Fasting glucose greater than 100 mg/dL