Unit 4-Antihypertensives Flashcards
Furosemide
Drug class
Loop diuretic
Furosemide
Mechanism
Inhibits Cl portion of Na-K-2Cl cotransporter in luminal membrane at medullary and cortical (proximal) talH –> decreased Ca++ and Na+ (and water) reabsorption, resultant K+ loss
Furosemide
Uses
Crisis edema (pulmonary, CHF, cirrhosis), hypercalcemia, drug toxicity/OD; severe hypertension in setting of CHF or cirrhosis;
useful in patients with renal insufficiency (GFR < 30-40)
Furosemide
Side effects
Hypokalemia/hypomagnesemia, hypercalcinuria, nephrocalcinosis, ototoxicity (esp. w/aminoglycoside)
Hyper -glycemia, -lipidemia, -uricemia; hypo -magnesia, -natremia; gout, photosensitivity, drug interactions; erectile dysfunction
Hydrochlorothiazide
Drug class
Thiazide diuretic
Hydrochlorothiazide
Mechanism
Inhibits the Cl portion of the Na-Cl cotransporter in the luminal membrane at the early distal tubule –> decreased Na+ (and water) reabsorption, increased Ca++ reabsorption, resultant K+ loss
Hydrochlorothiazide
Uses
HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus
Hydrochlorothiazide
Side effects
Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine
Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions
avoid NSAIDs, bile sequestrants; ineffective if GFR <30
Chlorthalidone
Drug class
Thiazide-like diuretic
Chlorthalidone
Mechanism
Inhibits the Cl portion of the Na-Cl cotransporter in the luminal membrane at the early distal tubule –> decreased Na+ (and water) reabsorption, increased Ca++ reabsorption, resultant K+ loss
Chlorthalidone
Uses
Reduce stroke risk, CHF events; HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus
Chlorthalidone
Side effects
Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine
Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions
avoid NSAIDs, bile sequestrants; ineffective if GFR <30
Metolazone
Drug class
Thiazide-like diuretic
Metolazone
Mechanism
Inhibits the Cl portion of the Na-Cl cotransporter in the luminal membrane at the early distal tubule –> decreased Na+ (and water) reabsorption, increased Ca++ reabsorption, resultant K+ loss
Metolazone
Uses
HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus
Metolazone
Side effects
Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine
Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions
avoid NSAIDs, bile sequestrants; ineffective if GFR <30
Amiloride
Drug class
Renal ENaC inhibitor
Amiloride
Mechanism
Blocks Na channel and Na/H antiporter in lumenal membrane at the late distal tubule and collecting duct –> decreased K+ secretion and distal tubule acid secretion, increased Ca++ absorption
Amiloride
Uses
Combination with other diuretics to prevent hypokalemia; edema, idiopathic hypercalciuria (stones); lithium-induced polyuria & toxicity, Liddle syndrome, mucocilliary clearance
Amiloride
Side effects
Hyperkalemia in patients with renal failure or on ACE inhibitors
Contraindicated in patients with renal failure (hyperkalemia), ACEi/ARB use; FeNa = 2%
Spironolactone
Drug class
Aldosterone receptor antagonist
Spironolactone
Mechanism
Competes for aldosterone receptor, inhibiting mRNA transcription and translation –> decreased Na and K channels, decreased number and activity of Na-K-ATPase pumps in the late distal tubule and collecting duct –> decreased K+ secretion, distal tubule acid secretion
Spironolactone
Uses
Reduction in CHF mortality (30% in NYHA class III and IV); combination with other diuretics to prevent hypokalemia; edema; primary and secondary aldosteronism; hypertension; anti-testosterone agent
Spironolactone
Side effects
Hyperkalemia in patients with renal failure or on ACE inhibitors; male patients may have gynecomastia, erectile dysfunction, and loss of libido; female patients may have amenorrhea, breast soreness, and oligomenorrhea
Contraindicated in patients with renal failure (hyperkalemia); FeNa = 2%; requires a salt-restricted diet; only drug not requiring tubular lumen access
Eplerenone
Drug class
Potassium-sparing diuretic
Eplerenone
Mechanism
Block alodesterone; inhibits sodium reabsorption in distal tubule
Eplerenone
Uses
Reduction in CHF mortality (30% in NYHA class III and IV); combination with other diuretics to prevent hypokalemia; edema; primary and secondary aldosteronism; hypertension; anti-testosterone agent
Eplerenone
Side effects
Hyperkalemia; much lower incidence of gynecomastia and mennorhagia
Caution in renal failure, ACEi or ARB use, and in diabetics
Captopril
Drug class
short-acting ACE-I (vasodilators)
Captopril
Mechanism
Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)
Captopril
Uses
CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)
Captopril
Side effects
Dry cough, angioedema, inhibits renal autoregulation, hypotension
Short-acting; contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure; reduces incidence of future CAD events, may reduce risk of diabetes
Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
Drug class
long-acting ACE-I (vasodilators)
Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
Mechanism
Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)
Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
Uses
CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)
Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
Side effects
Dry cough, angioedema, decreased renal function, hypotension
Long-acting; contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure; reduces incidence of future CAD events; may reduce risk of diabetes
Enalapril
Drug class
ACE-I (vasodilators)
Enalapril
Mechanism
Metabolized to active form enalaprat
Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)
Enalapril
Uses
CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)
Enalapril
Side effects
Dry cough, angioedema, decreased renal function, hypotension
contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure; reduces incidence of future CAD events; may reduce risk of diabetes
Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Drug class
Angiotensin II Recepter Blockers
Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Mechanism
Competitive inhibition of angiotensin II in vascular endothelium
Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Uses
Fall in peripheral vascular resistance, w/little change in HR or CO; same uses as ACE-I