B: 21-24 Flashcards
Dyslipidemia drugs
Atorvastatin Rosuvastatin Simvastatin Ezetimib Fenofibrate Colesevelam
Statins MOA
HMG-CoA reductase inhibitors which is the rate limiting step of endogenous cholesterol synthesis
Statins actions
Liver cholesterol ↓ LDL-R expression ↑ Plasma LDL ↓ (20-50% reduction) VLDL synthesis by liver ↓ Plasma TG ↓
Atorvastatin
Rosuvastatin
Simvastatin
Difference
Atorvastatin: Active as given
Rosuvastatin: Active as given
Simvastatin: Prodrug
Atorvastatin
Rosuvastatin
Simvastatin
Metabolism
CYP450
Atorvastatin
Rosuvastatin
Simvastatin
Indications
Atherosclerotic vascular disease
Acute coronary syndrome
Reduced risk of cardiovascular disease
Reduced mortality in ischemi heart dieseas
Statins side effects
Hepatotoxicity
Myalgia
Rhabdonyolysis
Statins contraindications
Teratogenic
Liver diseas caution
Colesevelam MOA
Large non absorbable polymers that bind bile acidsand prevent their absorption which divers hepatic cholesterol to the synthesis of new bile
Bile acid sequestrans drug
Colesevelam
Colesevelam how to give and when?
Oral
With meals
Dont give togather with other drugs (wait btw. 4 h)
Colesevelam indications
Primary hypercholesterolemia type IIA (LDL↑)
With Statins
Colesevelam side effects
VLDL ↑ TG ↑ GI Vit. ADEK malabsorption Hyperglycemia Gall stones
Sterol absorption inhibitors
Ezetimibe
Ezetimibe MOA
Block NPC1L1 in intestine Reduce cholesterol absorption Liver cholesterol ↓ LDL-R expression ↑ Plams LDL ↓ (20% reduction)
Carbonic Anhydrase inhibitors
Acetazolamide
Acetazolamide indicaitons
Diuretic use if edema+metabolic alkalosis Glaucoma Mountain sickness Innr ear disorder Urinary alkalosis
Acetazolamide side effects
Metabolic acidosis
Renal stones
Loop diuretics MOA and names
Furosemide
Ethacrynic acid
Inhibition of Na/K/2Cl in the thick ascending limb
Inhibition of Na/K/2Cl in the thick ascending limb will cause
Loss of NaCl Loss of luminal positive potential (Mg,Ca reab.↓) K and H wasting Hypokalemic metabolic alkalosis XOX-2 ↑ → GFR ↑
Furosemide drug interactions
NSAID’s
Aminoglycosides
Lithium
Digoxin
How are they different?
Furosemide is a Sulfa drug
Ethacrynic acid is not a Sulfa drug