Hyperlipidemia - Hockerman

Question 1

What is the MOA of bile acid sequestrants?

Answer 1

-inhibits reabsorption of bile acids from intestine (binds it up to be excreted in feces)
-up regulates LDL receptors in liver

Question 2

AE’s of bile acid sequestrants?

Answer 2

constipation, bloating

Question 3

What is the MOA of Ezetimibe?

Answer 3

-inhibits intestinal absorption of cholesterol from the diet and reabsorption of cholesterol excreted in the bile
-targets NPC1L1

Question 4

AE’s of Ezetimibe?

Answer 4

-low incidence of liver/skeletal muscle damage

Question 5

What is the MOA of statins?

Answer 5

-inhibits HMG-CoA reductase
-up regulates LDL receptors

Question 6

AE’s of statins?

Answer 6

rhabdomyolysis; hepatotoxicity, increased incidence of T2DM

Question 7

PCSK9 inhibitors AE’s & MOA

Answer 7

-inhibits PCSK9 that works to degrade LDL receptors in liver
AE: injection site reaction, arthralgia

Question 8

Lomtapide MOA?

Answer 8

inhibits MTTP which prevents Apo-B lipoproteins synthesis(liver and intestine)–interferes with assembly of VLDLs & chylomicrons
AE: liver damage

Question 9

mipomersen MOA?

Answer 9

selectively inhibits Apo B100 in liver
AE: liver damage

Question 10

Bempedoic acid MOA?

Answer 10

inhibits ATP-citrate Lyase (enzyme in cholesterol synthesis pathway)

Question 11

Fibrates MOA & AE’s?

Answer 11

-bind to PPAR-a and regulate gene transcription with RXR (retinoic acid receptor)
AE: gallstones, rhabdomyolysis

Question 12

Niacin MOA & AE’s?

Answer 12

-works on GPR109A & hormone-sensitive lipase that suppresses cAMP production, liberates FFA
AE: facial flushing, itching, headache

Question 13

What statins are prodrugs?

Answer 13

Lovastatin and simvastatin

Question 14

What do the dihydropyridines do?

Answer 14

-interfere with gating (enantiomers block/potentiate gating)
-selective in vasculature over cardiac muscle
-tonic block (can bind closed channels)
AE: reflex tachycardia

Question 15

What do the phenylalkylamines do?

Answer 15

Verapamil
-less potent vasodilation
-frequency dependent block

Question 16

What do the Benzothiazepines do?

Answer 16

Diltiazem
-less potent vasodilation
-initial reflex tachycardia but not as bad as DHPs
frequency and tonic block
-directly inhibits the heart less than verapamil bit nore than DHPs

Question 17

What is special about nimodipine?

Answer 17

-selective for cerebral arteries (used for brain bleeds)

Question 18

What is special about amlodipine?

Answer 18

-slow onset, long duration of action
-no reflex tachycardia

Question 19

What are the nonselective B-adrenergic antagonists?

Answer 19

Propranolol, Nadolol, Timolol, Pindolol

Question 20

What are the a1 antagonists?

Answer 20

Prazosin, terazosin, Doxazosin

Question 21

What are the a2 antagonists?

Answer 21

clonidine, methyldopa, guanfacine

Question 22

What are the B1 selective B-adrenergic antagonists?

Answer 22

Metoprolol, Atenolol, esmolol, Nebivolol

Question 23

What is special about Esmolol?

Answer 23

super short half-life
-given IV & easily metabolized

Question 24

What are the mixed beta adrenergic antagonists?

Answer 24

nonselective for B/a1 antagonists
-carvedilol, labetalol

Question 25

Friedewald Equation

Answer 25

LDL= TC-HDL-TG/5

Question 26

What are the two hydrophillic statins?

Answer 26

Pravastatin, Rosuvastatin