Hyperlipidemia - Hockerman Flashcards
What is the MOA of bile acid sequestrants?
-inhibits reabsorption of bile acids from intestine (binds it up to be excreted in feces)
-up regulates LDL receptors in liver
AE’s of bile acid sequestrants?
constipation, bloating
What is the MOA of Ezetimibe?
-inhibits intestinal absorption of cholesterol from the diet and reabsorption of cholesterol excreted in the bile
-targets NPC1L1
AE’s of Ezetimibe?
-low incidence of liver/skeletal muscle damage
What is the MOA of statins?
-inhibits HMG-CoA reductase
-up regulates LDL receptors
AE’s of statins?
rhabdomyolysis; hepatotoxicity, increased incidence of T2DM
PCSK9 inhibitors AE’s & MOA
-inhibits PCSK9 that works to degrade LDL receptors in liver
AE: injection site reaction, arthralgia
Lomtapide MOA?
inhibits MTTP which prevents Apo-B lipoproteins synthesis(liver and intestine)–interferes with assembly of VLDLs & chylomicrons
AE: liver damage
mipomersen MOA?
selectively inhibits Apo B100 in liver
AE: liver damage
Bempedoic acid MOA?
inhibits ATP-citrate Lyase (enzyme in cholesterol synthesis pathway)
Fibrates MOA & AE’s?
-bind to PPAR-a and regulate gene transcription with RXR (retinoic acid receptor)
AE: gallstones, rhabdomyolysis
Niacin MOA & AE’s?
-works on GPR109A & hormone-sensitive lipase that suppresses cAMP production, liberates FFA
AE: facial flushing, itching, headache
What statins are prodrugs?
Lovastatin and simvastatin
What do the dihydropyridines do?
-interfere with gating (enantiomers block/potentiate gating)
-selective in vasculature over cardiac muscle
-tonic block (can bind closed channels)
AE: reflex tachycardia
What do the phenylalkylamines do?
Verapamil
-less potent vasodilation
-frequency dependent block
What do the Benzothiazepines do?
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
What is special about nimodipine?
-selective for cerebral arteries (used for brain bleeds)
What is special about amlodipine?
-slow onset, long duration of action
-no reflex tachycardia
What are the nonselective B-adrenergic antagonists?
Propranolol, Nadolol, Timolol, Pindolol
What are the a1 antagonists?
Prazosin, terazosin, Doxazosin
What are the a2 antagonists?
clonidine, methyldopa, guanfacine
What are the B1 selective B-adrenergic antagonists?
Metoprolol, Atenolol, esmolol, Nebivolol
What is special about Esmolol?
super short half-life
-given IV & easily metabolized
What are the mixed beta adrenergic antagonists?
nonselective for B/a1 antagonists
-carvedilol, labetalol
