Medications Grouped Flashcards
Thiazide Diuretics
Hydrochlorothiazide - more common
Chlorthalidone - more common and more effective
Metolazone
Indapamide
Indications: antihypertensives (reduce blood volume, cardiac output, and peripheral resistance)
AE: hypokalemia, hyperglycemia, hyperuricemia, diuresis, hyperlipidemia; AE increase with dosage
CI: GFR <30
Caution: renal function declines with age; diabetics (increased uric acid and insulin resistance)
Interactions: steroids, NSAIDs, class IA or III antiarrythmics that prolong QT interval (induce torsades de pointes with hypokalemia), probenecid and lithium, and digoxin
dose in morning to prevent nocturia
monitor electrolytes
Loop Diuretics
Furosemide - 50% oral bioavailability
Toresemide - 100% oral bioavailability
Bumetanide 100% oral bioavailability
Ethacrynic Acid
Indications: antihypertensives and treat symptoms of heart failure and edema
MOA: prevent reabsorption of Na and Cl in the kidneys, reduce renal vascular resistance and increase renal flow
AE: hypokalemia, hypo Ca, hypo Mg (can cause arrhythmias), excessive diuresis (hyponatremia, hypotension, renal insufficiency), reflex activation of RAAS, hypouricemia
Caution: diuresis continues despite dehydration; watch for drugs that aggravate hyperglycemia, dyslipidemias, and hyperuricemia; watch kidney function with ARBs or ACE-I
Interactions: aminoglycosides, NSAIDs, class IA or III antiarrhythmics, probenacid
Monitor: electrolytes and renal function
Use IV in Acute Heart Failure
Potassium Sparing Diuretics
Amiloride
Triamterene
Indications: antihypertensive
MOA: inhibits sodium transport at late distal and collecting ducts
AE: hyperERkalemia, especially in those with severe renal impairment, or those receiving potassium sparing drugs (ACE-I, ARBs, K supp, and NSAIDs
Interactions: ACE-I – may increase risk of hyperkalemia; Indomethacin – decrease in renal function when combined with triamterene; Cimetidine: increases bioavailability and decreases clearance of triamterene
Monitor: electrolytes and renal function
not very effective at diuresis; sometimes used with thiazides and loops to prevent K loss
Beta Blockers: Non-selective without ISA
Nadolol
Propanolol
Timolol
Indication: Antihypertensive
MOA: Block B1 and B2
Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
AE: bradycardia, heart block, heart failure, dyspnea, bronchospasm, fatigue, dizziness, lethargy, depression, decreased libido, erectile dysfunction, hyper/hypoglacemia (watch in diabetics), hypokalemia, hyperlipidemia
Caution: Heart Rate <60, respiratory disease, abrupt discontinuation – rebound hypertension or ischemic syndrome (taper), may mask signs of hypoglycemia, hypokalemia with diuretic use
CI: hypersensitivity, sinus node dysfunction (okay with pacemaker), severe sinus bradycardia, heart block, cardiogenic shock, acute decompensated heart failure, asthma
Beta Blockers Non-selective with ISA
Pindolol
Carteolol
Penbutolol
Indication: Antihypertensive
MOA: Block B1 and B2
Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
AE: bradycardia, heart block, heart failure, dyspnea, bronchospasm, fatigue, dizziness, lethargy, depression, decreased libido, erectile dysfunction, hyper/hypoglacemia (watch in diabetics), hypokalemia, hyperlipidemia
Caution: Heart Rate <60, respiratory disease, abrupt discontinuation – rebound hypertension or ischemic syndrome (taper), may mask signs of hypoglycemia, hypokalemia with diuretic use
CI: hypersensitivity, sinus node dysfunction (okay with pacemaker), severe sinus bradycardia, heart block, cardiogenic shock, acute decompensated heart failure, asthma; not with ACS
Beta Blockers Selective without ISA
Atanolol Metoprolol - heart failure (good for patients with HF and hypotension) Emolol Betaxolol Bisoprolol (HF, but not FDA approved)
Indication: Antihypertensive
Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
AE: bradycardia, heart block, heart failure, dyspnea, bronchospasm, fatigue, dizziness, lethargy, depression, decreased libido, erectile dysfunction, hyper/hypoglacemia (watch in diabetics), hypokalemia
Caution: Heart Rate <60, respiratory disease, abrupt discontinuation – rebound hypertension or ischemic syndrome (taper), may mask signs of hypoglycemia, hypokalemia with diuretic use
CI: hypersensitivity, sinus node dysfunction (okay with pacemaker), severe sinus bradycardia, heart block, cardiogenic shock, acute decompensated heart failure; Not with ACS
use low doses only; can use with asthma, COPD, peripheral vascular disease, but avoid non-selective with these patients
Beta Blockers Selective with ISA
Acebutolol
Indication: Antihypertensive
Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
AE: bradycardia, heart block, heart failure, dyspnea, bronchospasm, fatigue, dizziness, lethargy, depression, decreased libido, erectile dysfunction, hyper/hypoglacemia (watch in diabetics), hypokalemia
Caution: Heart Rate <60, respiratory disease, abrupt discontinuation – rebound hypertension or ischemic syndrome (taper), may mask signs of hypoglycemia, hypokalemia with diuretic use
CI: hypersensitivity, sinus node dysfunction (okay with pacemaker), severe sinus bradycardia, heart block, cardiogenic shock, acute decompensated heart failure; Not with ACS
ISA beta blockers are not recommended for patients with previous acute coronary syndrome (ACS)
use low doses only; can use with asthma, COPD, peripheral vascular disease, but avoid non-selective with these patients
Beta Blockers with Vasodilation Properties
Labetolol (block a1)
Carvedilol (block a1) (Heart Failure - not FDA approved)
Nebivolol (NO activity)
Indication: Antihypertensive
Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
MOA: Block B1 and B2
AE: bradycardia, heart block, heart failure, dyspnea, bronchospasm, fatigue, dizziness, lethargy, depression, decreased libido, erectile dysfunction, hyper/hypoglacemia (watch in diabetics), hypokalemia (less with carvedilol and neivolol)
Caution: Heart Rate <60, respiratory disease, abrupt discontinuation – rebound hypertension or ischemic syndrome (taper), may mask signs of hypoglycemia, hypokalemia with diuretic use
CI: hypersensitivity, sinus node dysfunction (okay with pacemaker), severe sinus bradycardia, heart block, cardiogenic shock, acute decompensated heart failure
Calcium Channel Blockers - Dihydropyridines
Nifedipine
Amlodipine
Felodipine
MOA: dilate the arterioles by blocking the movement of calcium into smooth muscle cells preventing their contraction, and causing relaxation and dilation; greater affinity for vascular calcium channels than calcium channels in the heart
AE: bradycardia, peripheral edema, headache, flushing, gingival hyperplasia, reflex tachycardia
CI: Hypersensitivity, reduced ejection fraction (amlodipine is okay)
Caution: contaminant use with Beta Blockers – can cause heart block
most have short half-lives, so extended release is preferred; amlodipine is the exception (long half-life)
will not hurt HF, but will not help
Calcium Channel Blockers - Non-dyhydropyridines
Verapamil
Diltiazem
Class IV Antiarrhythmics - blocks calcium from entering cardiac cell; inhibits AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
Hypertensives - MOA: dilate the arterioles by blocking the movement of calcium into smooth muscle cells preventing their contraction, and causing relaxation and dilation; affects both vascular and heart calcium channels
AE: bradycardia, heart block, constipation, peripheral edema, headache, flushing, may worsen heart failure
CI: sinus node dysfunction, severe sinus bradycardia (pacemaker okay), heart block, afib/flutter associated with accessory bypass tract
Caution: heart rate <60, contaminant use with Beta Blockers – can cause heart block
hypersensitivity, reduced ejection fraction
most have short half-lives, so extended release is preferred
Angiotensin Converting Enzyme Inhibitors
Lisinopril - most common Fosinopril - uncommon Moexipril - uncommon Trandolapril - uncommon Benazepril Captopril Enalapril Perindopril Quinapril Ramipril
Indication: antihypertensive
MOA: inhibit conversion of angiotensin I to angiotensin II; lowers output of SNS, increases vasodilation of smooth muscle, and lowers retention of sodium and water
AE: hyperkalemia, especially when starting or increasing dose and with NSAID use; persistent dry cough; reduced GFR and serum creatine (monitor); acute renal failure; angioedema
Absolute CI: pregnancy, bilateral renal artery stenosis, history of angioedema
Relative CI: unilateral renal artery stenosis, renal insufficiency, hypotension (go slow), hyperkalemia (greater than 5 mEq/L)
Caution: baseline hyperkalemia, NSAIDs, can potentially cause declined renal function
Dosage Adjustments: renal impairment, elderly, volume depleted, diuretic therapy
Monitor: electrolytes (K+), GFR and serum creatine
Direct Renin Inhibitor
Aliskren
Indication: Antihypertensive
MOA: directly inhibits Renin
AE: hyperkalemia, hypotension
CI:with ACE-I or ARB in diabetics, pregnancy
Caution: severe renal impairment, deteriorating renal function, renal artery stenosis
Monitor: K+, GFR and serum creatine
Interactions: ACE-I, ARB, cyclosporine, any potassium supplements, furosemide concentration decreased, ketoconazole increases aliskirin levels
Alpha 1 Blockers
Doxazosin
Prazosin
Terazosin
Indication: hypertension
MOA: block alpha 1 receptors
AE: first dose – syncope, dizziness, palpitations; orthostatic hypertension
CI: hypersensitivity
not for monotherapy for hypertension
may cause increase in cardiovascular events
used in really resistant patients as a back-up
Alpha 2 Agonsists
Clonidine - common; patch or tablet
Methyldopa - common
Guanfacine
Guanabenz
Indication: resistant hypertension
AE: Clonidine - orthostatic hypotension, dry mouth, muscle weakness; Methyldopa - hepatotoxicity, peripheral edema, hemolytic anemia, orthostatic hypotension; all - transient sedation initially, vision disturbances, sedation (avoid other sedatives)
CI: Methyldopa - concurrent use of MAO inhibitor, hepatic disease, pheochromocytoma; all - hypersensitivity
Clonidine - discontinuation results in severe rebound hypertension, so it much be tapered; if on a beta blocker, taper it before starting clonidine – too much PNS activity; clonidine withdrawal – too much SNS activity
Methyldopa - first line hypertensive treatment in pregnancy; tolerance may occur after 2-3 mo; increase dose
Peripheral Sympathetic Inhibitors
Reserpine
Indication: hypertension
MOA: reduces sympathetic tone and peripheral resistance; depletes NE from nerve endings
AE: gastric ulceration, depression, sexual side effects, orthostatic hypotension, nasal congestion, fluid retention, peripheral edema, diarrhea, increased gastric secretion
CI: hypersensitivity, peptic ulcer disease, ulcerative colitis, history of depression, history of ECT
Direct Vasodilators
Isosorbide Dinitrate/Hydralazine
Hydralazine
Minoxidil
Indication: resistant hypertension
MOA: relax smooth muscles in arterioles and activate baroreceptors
AE: tachycardia; hydralazine - lupus-like syndrome; Minoxidil - edema, hypertrichosis
CI: hypersensitivity; Minoxidil - pheochromocytoma; Isosorbide Dinitrate/Hydralazine - increased cranial pressure
cause reflex tachycardia and fluid retention; use beta blockers and diuretics too
use caution and review use and monitoring before prescribing for hypertension
Aldosterone Antagonists
Spironolactone
Eplerenone
Indications: anithypertensives and prevent remodeling in patients with heart failure
MOA: modulate vascular tone and cause diuresis (increase NaCl excretion, decrease K+ excretion)
AE: hyperkalemia, especially with impaired renal function, ACE, ARBs, direct renin inhibitors, K sup, K salts subs, NSAIDs); gynecomastia or breast tenderness; menstrual irregularities, hirsutism
Caution: elderly, diabetics (increased risk of hyperkalemia), and patients with poor renal function
Interactions: ACE-I, ARBs, NSAIDs, Digoxin (increased plasma concentration of spironolactone), K supplements
Eplerenone Interactions: CYP34A substrate – do not use eplerenone with strong 3A4 inhibitors (increase eplerenone plasma concentrations)
Monitor: check K at baseline and after week
ARB/Neprilysin Inhibitor
Sacubitril/Valsartan
Indication: Heart Failure
MOA: ACE-I/ARB Combo; Sacubitril increases natriuretic peptides (involved in diuresis) by preventing their breakdown, but causes increase in AT II; Valsartan blocks AT II’s receptor
AE: new; theoretical risk of increasing peptides associated with Alzheimer’s
NEW - don’t be the first, don’t be the last!
may improve HF outcomes
Angiotensin Receptor Blockers
Azilsartan Candesartan Irbesartan Losartan Olmesartan Telmisartan Valsartan Eprosartan
Indications: hypertension; heart failure (improves symptoms and outcomes/heals the heart)
MOA: block angiotensin II from binding to angiotensin receptor
AE: hyperkalemia, renal function deterioration, angioedema, hypotension/syncope
Absolute CI: pregnancy, bilateral renal artery stenosis, history of angioedema
Relative CI: unilateral renal artery stenosis, renal insufficiency, hypotension (go slow), hyperkalemia (greater than 5 mEq/L)
Dose Adjustments: renal impairment, elderly, volume depleted, diuretic therapy
Monitor: electrolytes (K+), GFR and serum creatine
Digoxin
Indications: heart failure; add digoxin for patients who are symptomatic despite optimized ACE I and Beta Blocker and Diuretic, or if concomitant Afib – digoxin slows rate (beta blockers are better)
MOA: binds to Na+ and K+ ATP pumps, leading to incrased intracellular Na concetnrations; more intracellular Ca is then available during systole; regulates heart rate (slows); Neurohormonal (RAAS, SNS) modulation – may be related to restoration of baroreceptor
Antiarrhythmic - vagal stimulation (PNS), direct AV nodal inhibition, prolongs AV node refractoriness
Digoxin Toxicity: fatigue, weakness, CNS effects (confusion, delirium, psychosis), GI effects (nausea, vomiting, anorexia), visual disturbances (halos, photophobia, color perception problems – red-green or yellow-green vision), cardiac effects (arrhythmias, ventricular tachycardia and fibrillation, AV node block, and sinus bradycardia) – increased with electrolyte disturbances (hypo K, hyper Ca, hypo Mg)
Many Interactions
digoxin conc <1.2 ng/mL – no adverse effect on survival
digoxin conc >1.2 ng/mL – increased relative risk of mortality
desired concentration range = 0.5 - 0.9 ng/mL; preferably at or less than 0.8 ng/mL
slow onset of action – need loading dose in emergent situations
Adjust Dose: age, renal function, weight, risk for toxicity, indication (HF vs arrhythmia)
routine monitoring of serum drug concentrations not required, but recommended if there are changes in renal function, there is suspected toxicity, or after addition or
