Dyslipidemias

Question 0

Name two fibrates

Answer 0

gemofibrazole, fenofibrate

Question 1

What are the five statins?

Answer 1

Atorvastatin, simvastatin, lovastatin, fluvastatin, rosuvastatin

Question 2

bile acid binding resins

Answer 2

colestipol, cholestyramine

Question 3

combination drugs

Answer 3

niacin/lovastatin, niacin/simvastatin, ezetimibe/simvastatin

Question 4

Statins MOA

Answer 4

inhibit the enzyme HMG CoA reductase (involved in lipid synthesis)

Question 5

Statin ADME

Answer 5

All are PO
lo, ator, sim metabolized by CYP3A4
fluva, rusuvastatin metabolized by CYP2C9

Question 6

Statin Adverse Effects

Answer 6

Muscle toxicity (myopathy, rhabdomyolyis), liver tox (elevated liver enzymes including aminotransferase and creatine kinase), diabetes, contraindicated in pregnancy

Question 7

Fibrate MOA

Answer 7

ligands for transcription factor peroxisome proliferator-activated receptor alpha (PPAR-alpha), leads to increase in FA oxidation in liver and skeletal muscle

Question 8

PPAR-alpha downregulates and upregulates what?

Answer 8

upreg: lipoprotein lipase (LPL), Apo A-I, Apo A-II
downreg: Apo C-III

Question 9

Fibrates ADME

Answer 9

oral, binds plasma proteins tightly, eliminated mostly unchanged through the kidney

Question 10

fibrate toxicities

Answer 10

do watch for many of the same tox as statins. in combo with statins, further increases myopathies and rhabdomyolysis. caution used in patients with hepatic or renal dysfunction, biliary tract disease. potentiates effects of warfarin

Question 11

niacin (nicotinic acid) MOA

Answer 11

inhibits VLDL secretion, leading to decreases in LDL. increases HDL

Question 12

niacin (nicotinic acid) ADME

Answer 12

oral, some converted to niacinamide and incorporated into NAD. excreted by the kidneys unchanged or modified.

Question 13

niacin (nicotinic acid) tox

Answer 13

vasodilation, warm flush. pruritus, rashes, dry skin, acanthosis nigricans, hyperuricemia, macular edema

Question 14

bile acid binding resins MAO

Answer 14

large cationic resins that bind bile acids and prevent their reabsorption in the intestines. THis increases LDL receptors on liver cells and thus increases the uptake of LDL by the liver.

Question 15

bile acid binding resins ADME

Answer 15

oral, non-absorbed

Question 16

bile acid binding resins toxicities

Answer 16

constipating, bloating, Vit K malabsorption, many drug drug interactions

Question 17

sterol absorption inhibitors (ezetimibe) MOA

Answer 17

blocks transport of cholesterol through the NPC1L1 transporter. NPC1L1 intiates a clathrine mediated uptake of cholesterol in micelles with bile-acids.

Question 18

sterol absorption inhibitors (ezetimibe) ADME

Answer 18

oral, converted to active from by phase II metabolism (glucuronidation) . some systemic absorption, but 80% excreted in feces.

Question 19

sterol absorption inhibitors (ezetimibe) toxicities

Answer 19

very few since limited absorption. rare: myositis

Question 20

statin major indication

Answer 20

in patients with CHD or at high risk (statins decrease LDL)

Question 21

fibrate usage

Answer 21

hypertriglyceridemias

Question 22

niacin use

Answer 22

low HDL or high VLDL

Question 23

bile acid binders use

Answer 23

mild to moderate LDL or in combo

Question 24

use for absorption inhibitors

Answer 24

unclear