Antihypertensives Flashcards
What is the class for Furosemide (Lasix)
Loop diuretic
What is the mechanism for Furosemide (Lasix)
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
What are the therapeutics for Furosemide (Lasix)
Crisis edema (pulmonary, CHF, cirrhosis), hypercalcemia, drug toxicity/OD; severe hypertension in setting of CHF or cirrhosis
What are the important side effects for Furosemide (Lasix)
Hypokalemia/hypomagnesemia, hypercalcinuria, nephrocalcinosis, ototoxicity (esp. w/aminoglycoside)
What are the other side effects for Furosemide (Lasix)
Hyper -glycemia, -lipidemia, -uricemia; hypo -magnesia, -natremia; gout, photosensitivity, drug interactions; erectile dysfunction
What are the miscellaneous for Furosemide (Lasix)
avoid NSAIDs, take before salty meals, reduce salt intake; useful in patients with renal insufficiency (GFR < 30-40)
What is the class for Hydrochlorothiazide (Microzide)
Thiazide diuretic
What is the mechanism for Hydrochlorothiazide (Microzide)
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
What are the therapeutics for Hydrochlorothiazide (Microzide)
HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus
What are the important side effects for Hydrochlorothiazide (Microzide)
Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine
What are the other side effects for Hydrochlorothiazide (Microzide)
Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions
What are the miscellaneous for Hydrochlorothiazide (Microzide)
avoid NSAIDs, bile sequestrants; ineffective if GFR <30
What is the class for Chlorthalidone (Thalitone)
Thiazide-like diuretic
What is the mechanism for Chlorthalidone (Thalitone)
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
What are the therapeutics for Chlorthalidone (Thalitone)
Reduce stroke risk, CHF events; HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus
What are the important side effects for Chlorthalidone (Thalitone)
Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine
What are the other side effects for Chlorthalidone (Thalitone)
Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions
What are the miscellaneous for Chlorthalidone (Thalitone)
avoid NSAIDs, bile sequestrants; ineffective if GFR <30
What is the class for Metolazone (Zaroxolyn)
Thiazide-like diuretic
What is the mechanism for Metolazone (Zaroxolyn)
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
What are the therapeutics for Metolazone (Zaroxolyn)
HTN (intravascular contraction), chronic edema (cardiac insufficiency), idiopathic hypercalciuria (stones), nephrogenic diabetes insipidus
What are the important side effects for Metolazone (Zaroxolyn)
Hypokalemia/hypomagnesemia, contraction alkalosis, increased BUN & creatinine
What are the other side effects for Metolazone (Zaroxolyn)
Hyper -glycemia, -lipidemia, -uricemia, -calcemia; hypo -magnesia, -natremia; gout, photosensitivity, impotence, drug interactions
What are the miscellaneous for Metolazone (Zaroxolyn)
avoid NSAIDs, bile sequestrants; ineffective if GFR <30
What is the class for Amiloride (Midamor)
Renal ENaC inhibitor
What is the mechanism for Amiloride (Midamor)
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
What are the therapeutics for Amiloride (Midamor)
Combination with other diuretics to prevent hypokalemia; edema, idiopathic hypercalciuria (stones); lithium-induced polyuria & toxicity, Liddle syndrome, mucocilliary clearance
What are the important side effects for Amiloride (Midamor)
Hyperkalemia in patients with renal failure or on ACE inhibitors
What are the miscellaneous for Amiloride (Midamor)
Contraindicated in patients with renal failure (hyperkalemia), ACEi/ARB use; FeNa = 2%
What is the class for Spironolactone (Aldactone)
Aldosterone receptor antagonist
What is the mechanism for Spironolactone (Aldactone)
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
What are the therapeutics for Spironolactone (Aldactone)
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
What are the important side effects for Spironolactone (Aldactone)
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
What are the miscellaneous for Spironolactone (Aldactone)
Contraindicated in patients with renal failure (hyperkalemia); FeNa = 2%; requires a salt-restricted diet; only drug not requiring tubular lumen access
What is the class for Eplerenone (Inspra)
Potassium-sparing diuretic
What is the mechanism for Eplerenone (Inspra)
Block alodesterone; inhibits sodium reabsorption in distal tubule
What are the therapeutics for Eplerenone (Inspra)
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
What are the important side effects for Eplerenone (Inspra)
Hyperkalemia; much lower incidence of gynecomastia and mennorhagia
What are the miscellaneous for Eplerenone (Inspra)
Caution in renal failure, ACEi or ARB use, and in diabetics
What is the class for Captopril (Capoten)
short-acting ACE-I (vasodilators)
What is the mechanism for Captopril (Capoten)
Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)
What are the therapeutics for Captopril (Capoten)
CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)
What are the important side effects for Captopril (Capoten)
Dry cough, angioedema, inhibits renal autoregulation, hypotension
What are the miscellaneous for Captopril (Capoten)
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
What is the class for Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
long-acting ACE-I (vasodilators)
What is the mechanism for Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)
What are the therapeutics for Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)
What are the important side effects for Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
Dry cough, angioedema, decreased renal function, hypotension
What are the miscellaneous for Lisinopril (Prinivil); Benazepril (Lotensin); Quinapril (Accupril); Ramipril (Altace)
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
What is the class for Enalapril (Vasotec)
ACE-I (vasodilators)
What is the mechanism for Enalapril (Vasotec)
Blocks endothelial ACE from converting angiotensin I to angiotensin II (potent vasoconstrictor); as a side effect, also prevents breakdown of bradykinin (potent vasodilator)
What are the therapeutics for Enalapril (Vasotec)
CHF, left ventricular hypertrophy, post-MI (prevents left ventricular remodeling)
What are the important side effects for Enalapril (Vasotec)
Dry cough, angioedema, decreased renal function, hypotension
What are the miscellaneous for Enalapril (Vasotec)
Metabolized to enalaprilat, a more active metabolite;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
What is the class for Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Angiotensin II Recepter Blockers
What is the mechanism for Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Competitive inhibition of angiotensin II in vascular endothelium
What are the therapeutics for Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Fall in peripheral vascular resistance, w/little change in HR or CO; same uses as ACE-I
What are the important side effects for Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Angioedema, decreased renal function, hypotension; dry cough less frequent than with ACE-I
What are the miscellaneous for Losartan (Cozaar); Valsartan (Diovan); Irbesartan (Avapro)
Contraindicated in pregnancy, renal artery stenosis, hyperkalemia, and prior angioedema (no ARB allowed, either); caution in renal failure
What is the class for Aliskiren (Tekturna)
Renin inhibitor
What is the mechanism for Aliskiren (Tekturna)
Renin inhibitor
What are the therapeutics for Aliskiren (Tekturna)
Not very effective
What is the class for Diltiazem (Cardizem); Verapamil (Calan)
Non-dihydropyridine Calcium channel blockers
What is the mechanism for Diltiazem (Cardizem); Verapamil (Calan)
Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes decreased contractility, firing rate of aberrant pacemaker sites, and conduction velocity; prolongs repolarization in SA node and AV node (–> decreases HR); less vasodilation
What are the therapeutics for Diltiazem (Cardizem); Verapamil (Calan)
Hypertension, anti-anginal (chronotropic effects –> decreased myocardial oxygen demand), SVT (class IV anti-arrhythymic)
What are the important side effects for Diltiazem (Cardizem); Verapamil (Calan)
Leg edema, bradycardia, AV nodal blockade, hypotension, worsening heart failure
What are the other side effects for Diltiazem (Cardizem); Verapamil (Calan)
Constipation (most common), headache, flushing
What are the miscellaneous for Diltiazem (Cardizem); Verapamil (Calan)
Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block
What is the class for Amlodipine (Norvasc); Nifedipine (Procardia)
Dihydropyridine Calcium channel blockers
What is the mechanism for Amlodipine (Norvasc); Nifedipine (Procardia)
Interact with L-type voltage gated plasma membrane Ca channel –> decreased calcium entry into vascular smooth muscle cell, preventing contraction; causes dilation of epicardial coronary arteries, arteriolar resistance arteries; less heart-specific activity
What are the therapeutics for Amlodipine (Norvasc); Nifedipine (Procardia)
Hypertension, Raynauds, angina (3rd choice drug)
What are the important side effects for Amlodipine (Norvasc); Nifedipine (Procardia)
Leg edema (less than 1st generation), heart failure, AV nodal blockade, reflex tachycardia (lipophilic agents gain entry to brain and depress vasomotor center, rapidly dropping BP; this causes more reflex sympathetic activation (leading to adverse CV effects); long-acting agents are less lipophilic, and will cause less sympathetic activation and initial fall in BP)
What are the other side effects for Amlodipine (Norvasc); Nifedipine (Procardia)
Constipation (most common), headache, flushing
What are the miscellaneous for Amlodipine (Norvasc); Nifedipine (Procardia)
Contraindicated in overt decompensated heart failure, bradycardia, sinus node dysfunction, high-degree AV block
What is the class for Propranolol (Inderal)
Nonselective ?-blocker
What is the mechanism for Propranolol (Inderal)
Nonselective ?-blocker; primarily reduces cardiac output
What are the important side effects for Propranolol (Inderal)
Bronchospasm, bradycardia (negative chronotrope), CHF (negative ionotrope), masking of hypoglycemia symptoms
What are the other side effects for Propranolol (Inderal)
Decreased exercise capacity, depression (crosses BBB), worsening symptoms of peripheral vascular disease
What is the class for Metoprolol (Lopressor); Atenolol (Tenormin)
?1-selective blocker
What is the mechanism for Metoprolol (Lopressor); Atenolol (Tenormin)
Moderately selective ?1 blockade
What are the important side effects for Metoprolol (Lopressor); Atenolol (Tenormin)
Less likely to have bronchospasm, hypoglycemic awareness, and depression
What is the class for Bisoprolol (Zebeta); Nadolol (Corgard)
?1-selective blocker
What is the mechanism for Bisoprolol (Zebeta); Nadolol (Corgard)
Moderately selective ?1 blockade
What are the important side effects for Bisoprolol (Zebeta); Nadolol (Corgard)
Less likely to have bronchospasm, hypoglycemic awareness, and depression
What are the miscellaneous for Bisoprolol (Zebeta); Nadolol (Corgard)
Longer-acting than other beta-blockers
What is the class for Labetolol (Trandate)
Combined ?? blocker
What is the mechanism for Labetolol (Trandate)
?1 blockade with vasodilatory effects
What are the therapeutics for Labetolol (Trandate)
Hypertensive urgency
What is the class for Carvedilol (Coreg)
Combined ?? blocker
What is the mechanism for Carvedilol (Coreg)
?1 blockade with vasodilatory effects
What are the therapeutics for Carvedilol (Coreg)
Acute coronary syndrome, CHF
What is the class for Esmolol (Brevibloc)
?1-selective blocker
What are the therapeutics for Esmolol (Brevibloc)
AV nodal blockade in unstable patients
What are the miscellaneous for Esmolol (Brevibloc)
Short half-life
What is the class for Terazosin (Hytrin); Doxazosin (Cardura)
?1-adrenergic receptor antagonist
What is the mechanism for Terazosin (Hytrin); Doxazosin (Cardura)
Blocks post-synaptic ?1-adrenergic receptor antagonist on vascular smooth muscle
What are the therapeutics for Terazosin (Hytrin); Doxazosin (Cardura)
BPH; second-tier meds (use when other condition around, not for isolated hypertension)
What are the important side effects for Terazosin (Hytrin); Doxazosin (Cardura)
Orthostatic hypotension, fluid retention, worsening angina (secondary to reflex tachycardia)
What is the class for Clonidine (Catapres)
Central ?2-agonist
What is the mechanism for Clonidine (Catapres)
Stimulation of central ?2a adrenergic receptors –> reduction in sympathetic outflow from vasomotor systems in brainstem; inhibition of renin release (secondary to decreased sympathetic tone)
What are the important side effects for Clonidine (Catapres)
Rebound HTN if abruptly stopped; moderate orthostatic hypotension
What are the other side effects for Clonidine (Catapres)
Sedation, dry mouth, fatigue, depression
What is the class for ?-methyldopa (Aldomet)
Central ?2-agonist
What is the mechanism for ?-methyldopa (Aldomet)
Stimulation of central ?2a adrenergic receptors –> reduction in sympathetic outflow from vasomotor systems in brainstem; inhibition of renin release (secondary to decreased sympathetic tone)
What are the therapeutics for ?-methyldopa (Aldomet)
Hypertension of pregnancy (only)
What are the important side effects for ?-methyldopa (Aldomet)
Rebound HTN if abruptly stopped; moderate orthostatic hypotension
What are the other side effects for ?-methyldopa (Aldomet)
Sedation, dry mouth, fatigue, depression
What are the miscellaneous for ?-methyldopa (Aldomet)
Takes place of dopa, so less NE (also, methyl-NE activates ?2)
What is the class for Reserpine (Serpalan)
Ganglion blocking agent (adrenergic neuron blocking agent)
What is the mechanism for Reserpine (Serpalan)
Blocks transport of NE, DA, and 5HIAA into storage granules in PNS and CNS –> less neurotransmitter available when nerves are stimulated
What are the therapeutics for Reserpine (Serpalan)
Decrease cardiac output and systemic vascular resistance
What are the important side effects for Reserpine (Serpalan)
Sedation, mental depression, Parkinsonism symptoms
What is the class for Hydralazine (Apresoline)
Direct (vasodilators)
What is the mechanism for Hydralazine (Apresoline)
Relax smooth muscle of peripheral arterioles
What are the therapeutics for Hydralazine (Apresoline)
Hypertensive urgency; patients with BOTH advanced CHF and hypertension
What are the important side effects for Hydralazine (Apresoline)
Drug-induced lupus
What are the other side effects for Hydralazine (Apresoline)
reflex tachycardia
What are the miscellaneous for Hydralazine (Apresoline)
Serves as an antioxidant, preventing oxidation of NO
What is the class for Minoxidil (Loniten)
Direct (vasodilators)
What is the mechanism for Minoxidil (Loniten)
Relax smooth muscle of peripheral arterioles
What are the therapeutics for Minoxidil (Loniten)
Refractory hypertension; hair loss
What are the important side effects for Minoxidil (Loniten)
Pericardial effusion; hirsutism
What are the other side effects for Minoxidil (Loniten)
reflex tachycardia
What are the miscellaneous for Minoxidil (Loniten)
Smooth muscle relaxation by opening cardiovascular ATP-sensitive potassium channels