Drugs-MOA and site only Flashcards
Acetazolamide Diamox
MOA
renal site of action
- Inhibition of renal carbonic anhydrase to decrease sodium and bicarb reabsorption
- PCT
verapamil Covera-HS, Calan
Calcium channel blockers - vasodilators
non-dihydropyridines: Prefer open confirmation of L-type calcium channel (heart) and block it
labetalol Trandate
labetalol Trandate
B1/B2/a1 antagonist (7:1)
A1: decrease in SVR
B1: prevents reflex increase in heart rate
nifedipine Procardia, Adalat
nifedipine Procardia, Adalat
Calcium channel blockers - vasodilators
Dihydropyridines; prefer to bind to the inactivated state of L-type calcium channel and block it
captopril Capoten
ACE inhibitors: decrease angiotensin II levels and increase bradykinin levels
desmopressin/DDAVP
- V2 selective agonist, : more potent antidiuretic as compared to vasopressin
- Vasopressin Receptor Agonist
- Collecting Duct
Sodium thiosulfate
Treatment of cyanide toxicity
3% sodium nitrate
Treatment of cyanide toxicity
bosentan Tracleer
Endothelin (ET) receptor antagonist
Nonselective
Endothelin (Gq coupled) leads to contraction of smooth muscle; thereby relaxation is caused by antagonism
losartan Cozaar
ARB
Angiotensin receptor blockers (ARB) at AT1 receptors
Vasodilation, renal vasodilation on efferent, block Na+ reabsorption, block SNS discharge, inhibit ADH release
isoproterenol
Beta adrenergic agonist (synthetic agonist with relative selectivity for Beta1 > Beta2)
Beta1 - Positive inotrope, chronotrope, lusitrope.
Beta2 - peripheral vasodilation and hypotension. No activity on alpha
vasopressin /pitressin
MOA
renal site of action
- Vasopressin Receptor Agonist
- V1: Gq coupled on vascular smooth muscle, V1: vasoconstriction
- V2: Gs coupled on vascular endothelium and collecting duct: phosphorylation of AQP2, V2: release of coagulation factors, water reabsorption, Conserve body fluid, prevent fluid loss, maintain perfusion
- Collecting Duct
atenolol Tenormin
MOA
B1 selective antagonists
dopamine
Beta adrenergic agonist
Low dose: D1 vasodilation and increase in renal blood flow
Intermediate: B2 and B1: increase HR/contractility, decreased SVR
High: A1 peripheral vasoconstriction
bumetanide/bumex
MOA
renal area of action
loop diuretic
Inhibition of Na+ reabsorption in thick ascending Loop of Henle by blocking NKCC2 (Na+/K+/Cl-) transporter
Thick ascending limb of LOH
ambrisentan Letairis
Endothelin (ET) receptor antagonist
Selective
triamterene Dyrenium
moa
site of action
potassium sparing diuretic
collecting duct
Liddle’s syndrome (super ENaC Na channel)
Block ENacC Na channel.
Contradications - ACE, ARBs, renal insufficiency with hyperkalemia
hydralazine Apresoline
Decrease vascular smooth muscle tone (Mechanism unclear)
Direct relaxation of arteriolar smooth muscle (mechanism unclear)
lisinopril Prinivil, Zestril
ACE inhibitors: decrease angiotensin II levels and increase bradykinin(vasodilation) levels
epinephrine
Beta adrenergic agonist
Low dose - Beta1 - positive inotrope, lusitrope, chronotrope, and dromotrope, also vasodilation in SKM;
High dose - alpha1 - generalized peripheral vasoconstriction increasing afterload
phenoxybenzamine Dibenzyline
phenoxybenzamine Dibenzyline
alpha1, alpha 2 antagonist
A1 and A2 adrenergic receptor antagonist- irreversibleblocks resulting in longer half life and very long duration of action (central dogma)
hydrochlorothiazide HCTZ
MOA
site of action in kidney
- hydrochlorothiazide HCTZ
- Block Na+/2Cl- cotransporter in the DCT, inhibition of NaCl reabsorption in the DCT, increase absorption of Ca2+
- Vasodilatory effect
- Thiazides
- DCT
amlodipine Norvasc
Calcium channel blockers - vasodilators
Dihydropyridines; prefer to bind to the inactivated state of L-type calcium channel and block it
phentolamine OraVerse, Regitine
alpha1, alpha 2 antagonist
metoprolol Lopressor, Toprol
MOA
B1 selective antagonists
Antagonism of B1 in the heart, renal juxtaglomerular cells
mannitol/osmitrol
MOA
renal site of action
- mannitol/osmitrol
- PCT (primary), loop of Henle (secondary)
- osmotic diuretic, Molecules that are filtered into the glomerulus and not reabsorbed, limits reabsorption of water
irbesartan Avapro, Aprovel
ARB
Angiotensin receptor blockers (ARB) at AT1 receptors
Vasodilation, renal vasodilation on efferent, block Na+ reabsorption, block SNS discharge, inhibit ADH release
dobutamine
Beta adrenergic agonist (synthetic sympathomimetic amine)
fenoldopam Corlopam
D1 dopamine receptor agonist
Peripheral D1 dopamine receptor agonist
Decrease SVR, increase renal blood flow
digoxin Digox, Lanoxin
Cardiac glycosides
raise intracellular calcium by inhibiting Na/K ATPase pump on sarcolemma
Conivaptan/vaprisol
MOA
renal site of action
- Nonselective vasopressin antagonist
V1 blockade: vasodilation - V2 blockade: water excretion from collecting duct
- Collecting Duct
diltiazem Cardizem, Dilacor
Calcium channel blockers - vasodilators
non-dihydropyridines: Prefer open confirmation of L-type calcium channel (heart) and block it
aliskiren Tekturna
Renin inhibitor
Decreases SVR and Na+ absorption by kidney
Spironolactone Aldactone
MOA
site of action
- potassium sparing,
- Spironolactone Aldactone
- Aldosterone/mineralcorticoid receptor antagonist, inhibit synthesis of ENaC Na+ channel
- Collecting duct
norepinephrine
Beta adrenergic agonist
Low dose - Beta1 - positive inotrope, lusitrope, chronotrope, and dromotrope,
alpha1 - vasoconstriction with increased afterload.
Little effect on Beta2
milrinone Primacor
Phosphodiesterase (PDE)3 Inhibitor
Positive inotrope (improves diastolic dysfunction), vasodilation. Blocks metabolism of cAMP (inotropic effects), cGMP (vasodilatory effects)
Increased inotropy, increased lusitropy, decreased SVR, decreased preload (increased venous capacitance)
methylene blue MB
eNOS inhibitor
Vasoconstriction
doxazosin Cardura
alpha1 antagonist
Hydroxocobalamin Vitamin B12
Treatment of cyanide toxicity
tolvaptan/samsca
MOA
renal site of action
- V2 selective, Vasopressin Receptor Antagonist
V2 blockade: water excretion - Collecting Duct
terlipressin
MOA
renal site of action
- V1 selectivity and partial agonist
- Vasopressin Receptor Agonist
- Collecting Duct
minoxidil Loniten, Rogaine, Renewal
Potassium channel opener
arterial dilation and renal venodilation
Opening of ATP-modulated K+ channels resulting in hyperpolarization
furosemide/lasix
MOA
renal site of action
loop diuretic,
Inhibition of Na+ reabsorption in thick ascending Loop of Henle by blocking NKCC2 (Na+/K+/Cl-) transporter
Thick ascending limb of LOH
Digibind
Anti-digoxin antibodies
chlorothiazide/diuril
MOA
site of action
thiazides
DCT
Block Na+/2Cl- cotransporter in the DCT, inhibition of NaCl reabsorption in the DCT, increase absorption of Ca2+
amiloride Midamor
MOA
site of action
- amiloride Midamor
- potassium sparing diuretic
- collecting duct
- Pharmacological blockage of ENaC Na+ channel (not synthesis of the channel like Spironolactone)
Liddle’s syndrome (super ENaC Na channel)
propranolol Inderal, Innopran
MOA
Nonselective beta antagonist
terazosin Hytrin
alpha1 antagonist
prazosin Minipress
alpha1 antagonist
Block A1 adrenergic receptors, greater effect in arterioles resulting in vasodilation
eplerenone Inspra
MOA
site of action
- eplerenone Inspra
- Aldosterone/mineralcorticoid receptor antagonist - potassium sparing
- Collecting duct
