Medications Flashcards
Hydrochlorothiazide
Thiazide Diuretic
Indications: antihypertensives (reduce blood volume, cardiac output, and peripheral resistance)
AE: hypokalemia, hyperglycemia, hyperuricemia, diuresis, hyperlipidemia; AE increase with age
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
more common
monitor electrolytes
Chlorthalamide
Thiazide Diuretic
Preferred! 1.5 - 2 times more effective than hydrochlorothiazide
Indications: antihypertensives (reduce blood volume, cardiac output, and peripheral resistance)
AE: hypokalemia, hyperglycemia, hyperuricemia, diuresis, hyperlipidemia; AE increase with age
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
more common and more effective
monitor electrolytes
Metalozone
Thiazide Diuretic
Indications: antihypertensives (reduce blood volume, cardiac output, and peripheral resistance)
AE: hypokalemia, hyperglycemia, hyperuricemia, diuresis, hyperlipidemia; AE increase with age
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
Indapamide
Thiazide Diuretic
Indications: antihypertensives (reduce blood volume, cardiac output, and peripheral resistance)
AE: hypokalemia, hyperglycemia, hyperuricemia, diuresis, hyperlipidemia; AE increase with age
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
Furosemide
Loop Diuretic
50% bioavailability of oral medication; only give half of IV dose
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
IV used in Acute Heart Failure
Torsemide
Loop Diuretic
100% oral bioavailability
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
IV used in Acute Heart Failure
Bumetamide
Loop Diuretic
100% oral bioavailability
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
IV used in Acute Heart Failure
Ethacrynic Acid
Loop Diuretic
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
IV used in Acute Heart Failure
Amiloderone
Potassium Sparing Diuretic
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
Monitor: electrolytes and renal function
not very effective at diuresis; sometimes used with thiazides and loops to prevent K loss
Triamterene
Potassium Sparing Diuretic
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
Spironolactone
Aldosterone Antagonist/ Potassium Sparing Diuretic
better outcomes in patients with heart failure!
aldosterone antagonist, diminish cardiac remodeling in HF
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
Discontinue: K > 5.5 mEq/L, worsening renal function
Monitor: check K at baseline and after week
Eplerenone
Aldosterone Antagonist/ Potassium Sparing Diuretic
aldosterone antagonist, diminish cardiac remodeling in HF
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; CYP34A substrate – do not use eplerenone with strong 3A4 inhibitors (increase eplerenone plasma concentrations)
Monitor: check K at baseline and after week
Discontinue: K > 5.5 mEq/L, worsening renal function
Nadolol
Beta Blockers: Non-selective without ISA
Indication: Antihypertensive- 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
Propanolol
Beta Blockers: Non-selective without ISA
Indication: Antihypertensive- Block B1 and B2; 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, 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
Timolol
Beta Blockers: Non-selective without ISA
Indication: Antihypertensive- Block B1 and B2; 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, 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
Pindolol
Beta Blockers Non-selective with ISA
Indication: Antihypertensive- Block B1 and B2; 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, 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
Carteolol
Beta Blockers Non-selective with ISA
Indication: Antihypertensive- 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
Penbutolol
Beta Blockers Non-selective with ISA
Indication: Antihypertensive- 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
Atanolol
Beta Blockers Selective without ISA
Indication: Antihypertensive - block B1, Heart Failure (good for patients with HF and hypotension);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
Metoprolol
Beta Blockers Selective without ISA
Indication: Antihypertensive - block B1 only, Heart Failure (good for patients with HF and hypotension); 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
Emolol
Beta Blockers Selective without ISA
Indication: Antihypertensive - block B1 only; 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
Betaxolol
Beta Blockers Selective without ISA
Indication: Antihypertensive - block B1 only; 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
Bisoprolol
Beta Blockers Selective without ISA
Indication: Antihypertensive - block B1 only; Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness; Heart Failure (not FDA approved)
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
Acebutolol
Beta-blocker: Selective with ISA
Indication: Antihypertensive - block B1 only; 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
Labetolol
Beta Blocker with Vasodilation Properties
Indication: Antihypertensive; Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
MOA: Blocks a1, 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
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
Carvedilol
Beta Blocker with Vasodilation Properties
Indication: Antihypertensive, Heart Failure (most BP lowering HF BB; but more dizziness and hypotension); Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
MOA: Blocks a1, B1 and B2
AE: bradycardia, heart block, heart failure, dyspnea, bronchospasm, fatigue, dizziness, lethargy, depression, decreased libido, erectile dysfunction, hyper/hypoglacemia (watch in diabetics)
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
Nebivolol
Beta Blocker with Vasodilation Properties
Indication: Antihypertensive; Class II Antiarrhythmics - Inhibit AV nodal conduction by slowing AV nodal conduction and prolonging AV nodal refractoriness
MOA: Block B1 and B2, and has NO activity
AE: bradycardia, heart block, heart failure, dyspnea, bronchospasm, fatigue, dizziness, lethargy, depression, decreased libido, erectile dysfunction, hyper/hypoglacemia (watch in diabetics)
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
Nifedipine
Calcium Channel Blocker - Dihydropyridine
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
Caution: contaminant use with Beta Blockers – can cause heart block
most have short half-lives, so extended release is preferred
will not help heart failure, but will not hurt
Amlodipine
Calcium Channel Blocker - Dihydropyridine
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
Caution: contaminant use with Beta Blockers – can cause heart block
Safe to use in patients with heart failure/reduced ejection fraction
Long-half life; no extended release
Verapamil
Calcium Channel Blocker - Non -
dihydropyridine
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 HF
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
Diltiazem
Calcium Channel Blocker - Non -
dihydropyridine
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 HF
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
Linsinopril
ACE-I
most common
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
Fosinopril
ACE-I
uncommon
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
Moexipril
ACE-I
uncommon
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
Trandolapril
ACE-I
uncommon
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
Benazepril
ACE-I
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
Captopril
ACE-I
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
Enalapril
ACE-I
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
Perindopril
ACE-I
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
Quinapril
ACE-I
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
Ramipril
ACE-I
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
Aliskren
Direct Renin Inhibitor
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
Doxazosin
Alpha 1 Blocker
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
Prazosin
Alpha 1 Blocker
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
Terazosin
Alpha 1 Blocker
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
Clonidine
Alpha 2 Agonist
common; tablet and patch
Indication: occasionally used for resistant hypertension
MOA: reduce sympathetic outflow (NE); enhance parasympathetic activity, reducing heart rate, cardiac output, and total peripheral resistance
AE: transient sedation initially, vision disturbances, sedation (avoid other sedatives), orthostatic hypotension, dry mouth, muscle weakness
CI: hypersensitivity
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
Alpha 2 Agonist
Indication: occasionally used for resistant hypertension
MOA: reduce sympathetic outflow (NE); enhance parasympathetic activity, reducing heart rate, cardiac output, and total peripheral resistance
AE: transient sedation initially, vision disturbances, sedation (avoid other sedatives), hepatotoxicity, peripheral edema, hemolytic anemia, orthostatic hypotension
CI: hypersensitivity, concurrent use of MAO inhibitor, hepatic disease, pheochromocytoma
first line hypertensive treatment in pregnancy
tolerance may occur after 2-3 mo; increase dose
Guanfacine
Alpha 2 Agonist
Indication: occasionally used for resistant hypertension
MOA: reduce sympathetic outflow (NE); enhance parasympathetic activity, reducing heart rate, cardiac output, and total peripheral resistance
AE: transient sedation initially, vision disturbances, sedation (avoid other sedatives)
CI: hypersensitivity
Gaunabenz
Alpha 2 Agonist
Indication: occasionally used for resistant hypertension
MOA: reduce sympathetic outflow (NE); enhance parasympathetic activity, reducing heart rate, cardiac output, and total peripheral resistance
AE: transient sedation initially, vision disturbances, sedation (avoid other sedatives)
CI: hypersensitivity
Resperpine
Peripheral Sympathetic Inhibitor
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
Isosorbide Nitrate/Hydralazine
Direct Vasodilators
Indication: resistant hypertension
MOA: relax smooth muscles in arterioles and activate baroreceptors
AE: tachycardia
CI: hypersensitivity, 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
Hydralazine
Direct Vasodilators
Indication: resistant hypertension
MOA: relax smooth muscles in arterioles and activate baroreceptors
AE: tachycardia, lupus-like syndrome
CI: hypersensitivity
cause reflex tachycardia and fluid retention; use beta blockers and diuretics too
use caution and review use and monitoring before prescribing for hypertension
Minoxidil
Direct Vasodilators
Indication: resistant hypertension
MOA: relax smooth muscles in arterioles and activate baroreceptors
AE: tachycardia, edema, hypertrichosis
CI: hypersensitivity, pheochromocytoma
cause reflex tachycardia and fluid retention; use beta blockers and diuretics too
use caution and review use and monitoring before prescribing for hypertension
Sacubitril/Valsartan
ARB/Neprilysin Inhibitor
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
Hydralazine + Isosorbide Dinitrate
Heart Failure – for patients intolerant to ACE-I or ARBs; or African Americans
MOA: Nitrates – venous vasodilation, reducing preload; Hydralazine – direct arterial smooth muscle relaxation, reducing afterload
AE: hypotension, headache, tachycardia, lupus; often poorly tolerated
CI: concomitant use of sildenafil, tadalalfil, vardenafil (increase risk of hypotension)
Azilsartan
Angiotensin Receptor Blockers
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
Candesartan
Angiotensin Receptor Blockers
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
Irbesartan
Angiotensin Receptor Blockers
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
Losartan
Angiotensin Receptor Blockers
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
Olmesartan
Angiotensin Receptor Blockers
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
Telmisartan
Angiotensin Receptor Blockers
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
Valsartan
Angiotensin Receptor Blockers
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
Eprosartan
Angiotensin Receptor Blockers
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
Felodipine
Calcium Channel Blocker - Dihydropyridine
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
Caution: contaminant use with Beta Blockers – can cause heart block
most have short half-lives, so extended release is preferred
will not help heart failure, but will not hurt
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
Nitroglycerin
Vasodilator
Indication: Acute Heart Failure (IV)
MOA: acts as source of NO (induces smooth muscle relaxation in arterial and venous system)
AE: hypotension (especially Nesiritide – long half-life)
CI: if cardiac filling depends on venous return, shock
Nitroprusside
Vasodilator
Indication: Acute Heart Failure (IV)
MOA: venous and arterial dilator
AE: hypotension (especially Nesiritide – long half-life)
CI: if cardiac filling depends on venous return, shock
Nesiritide
Vasodilator
Indication: Acute Heart Failure (IV)
MOA: venous and arterial dilation, antagonizes RAAS
AE: hypotension (especially Nesiritide – long half-life)
CI: if cardiac filling depends on venous return, shock
Dobutamine
Inotropic Agent
adrenergic receptor agonist, drug of choice, not as effective if on BB, causes vasodilation
Dopamine
adrenergic receptor agonist; use: low systolic BP, cardiogenic shock; dose dependent effects
Milrinone
phosphodiesterase III inhibitor, vasodilation, limited use
Atrovastatin
High Intensity Statin
Indication: Hypercholesterolemia; reduces risk of ASCVD
MOA: inhibit HMG-CoA, a rate-limiting enzyme in cholesterol biosynthesis, reducing LDL
Common AE: constipation, abdominal pain, diarrhea, dyspepsia, nausea - but mostly well-tolerated
Serious AE: elevations in liver function (monitor LFTs) and liver toxicity (LFT elevations > 3X upper limit of normal), myopathy, rhabdomyolysis
may increase risk of getting diabetes mellitus
CI: NEVER in pregnant women
Discontinue: serum transaminase levels (liver function) rise to 3X upper limit of normal; signs or symptoms of myopathy
check dosage if patients have renal function issues
Interactions: drugs that inhibit metabolism: cyclosporine and gemfibrozil (statins metabolized by cytochrome p-450s)
maximum effect on lipids at 4-6 weeks - follow-up and check cholesterol levels/adherence at this time
Monitor: liver enzymes (LFTs) at baseline and as clinically indicated after; Creatinine Kinase in patients at risk for myopathy or complaining of muscle pain, weakness, tenderness, or brown urine; check for symptoms of myopathy at 6-12 weeks
Re-challenge intolerance after 2-4 weeks except in patients with Rhabdomyolysis
Fluvastatin
Statin
fewer interactions; consider in re-challenges
Indication: Hypercholesterolemia; reduces risk of ASCVD
MOA: inhibit HMG-CoA, a rate-limiting enzyme in cholesterol biosynthesis, reducing LDL
Common AE: constipation, abdominal pain, diarrhea, dyspepsia, nausea - but mostly well-tolerated
Serious AE: elevations in liver function (monitor LFTs) and liver toxicity (LFT elevations > 3X upper limit of normal), myopathy, rhabdomyolysis
may increase risk of getting diabetes mellitus
CI: NEVER in pregnant women
Discontinue: serum transaminase levels (liver function) rise to 3X upper limit of normal; signs or symptoms of myopathy
check dosage if patients have renal function issues
Interactions: drugs that inhibit metabolism: cyclosporine and gemfibrozil (statins metabolized by cytochrome p-450s)
maximum effect on lipids at 4-6 weeks - follow-up and check cholesterol levels/adherence at this time
Monitor: liver enzymes (LFTs) at baseline and as clinically indicated after; Creatinine Kinase in patients at risk for myopathy or complaining of muscle pain, weakness, tenderness, or brown urine; check for symptoms of myopathy at 6-12 weeks
Re-challenge intolerance after 2-4 weeks except in patients with Rhabdomyolysis
Lovastatin
Low Intensity Statin
Indication: Hypercholesterolemia; reduces risk of ASCVD
MOA: inhibit HMG-CoA, a rate-limiting enzyme in cholesterol biosynthesis, reducing LDL
Common AE: constipation, abdominal pain, diarrhea, dyspepsia, nausea - but mostly well-tolerated
Serious AE: elevations in liver function (monitor LFTs) and liver toxicity (LFT elevations > 3X upper limit of normal), myopathy, rhabdomyolysis
may increase risk of getting diabetes mellitus
CI: NEVER in pregnant women
Discontinue: serum transaminase levels (liver function) rise to 3X upper limit of normal; signs or symptoms of myopathy
check dosage if patients have renal function issues
Interactions: drugs that inhibit metabolism: cyclosporine and gemfibrozil (statins metabolized by cytochrome p-450s)
maximum effect on lipids at 4-6 weeks - follow-up and check cholesterol levels/adherence at this time
Monitor: liver enzymes (LFTs) at baseline and as clinically indicated after; Creatinine Kinase in patients at risk for myopathy or complaining of muscle pain, weakness, tenderness, or brown urine; check for symptoms of myopathy at 6-12 weeks
Re-challenge intolerance after 2-4 weeks except in patients with Rhabdomyolysis
Pravastatin
Low Intensity Statin
not metabolized by cytochrome 450
fewer interactions; consider in re-challenges
Indication: Hypercholesterolemia; reduces risk of ASCVD
MOA: inhibit HMG-CoA, a rate-limiting enzyme in cholesterol biosynthesis, reducing LDL
Common AE: constipation, abdominal pain, diarrhea, dyspepsia, nausea - but mostly well-tolerated
Serious AE: elevations in liver function (monitor LFTs) and liver toxicity (LFT elevations > 3X upper limit of normal), myopathy, rhabdomyolysis
may increase risk of getting diabetes mellitus
CI: NEVER in pregnant women
Discontinue: serum transaminase levels (liver function) rise to 3X upper limit of normal; signs or symptoms of myopathy
check dosage if patients have renal function issues
Interactions: drugs that inhibit metabolism: cyclosporine and gemfibrozil (statins metabolized by cytochrome p-450s)
maximum effect on lipids at 4-6 weeks - follow-up and check cholesterol levels/adherence at this time
Monitor: liver enzymes (LFTs) at baseline and as clinically indicated after; Creatinine Kinase in patients at risk for myopathy or complaining of muscle pain, weakness, tenderness, or brown urine; check for symptoms of myopathy at 6-12 weeks
Re-challenge intolerance after 2-4 weeks except in patients with Rhabdomyolysis
Pitavastatin
Statin
not metabolized by cytochrome 450
Indication: Hypercholesterolemia; reduces risk of ASCVD
MOA: inhibit HMG-CoA, a rate-limiting enzyme in cholesterol biosynthesis, reducing LDL
Common AE: constipation, abdominal pain, diarrhea, dyspepsia, nausea - but mostly well-tolerated
Serious AE: elevations in liver function (monitor LFTs) and liver toxicity (LFT elevations > 3X upper limit of normal), myopathy, rhabdomyolysis
may increase risk of getting diabetes mellitus
CI: NEVER in pregnant women
Discontinue: serum transaminase levels (liver function) rise to 3X upper limit of normal; signs or symptoms of myopathy
check dosage if patients have renal function issues
Interactions: drugs that inhibit metabolism: cyclosporine and gemfibrozil (statins metabolized by cytochrome p-450s)
maximum effect on lipids at 4-6 weeks - follow-up and check cholesterol levels/adherence at this time
Monitor: liver enzymes (LFTs) at baseline and as clinically indicated after; Creatinine Kinase in patients at risk for myopathy or complaining of muscle pain, weakness, tenderness, or brown urine; check for symptoms of myopathy at 6-12 weeks
Re-challenge intolerance after 2-4 weeks except in patients with Rhabdomyolysis
Rosuvastatin
High Intensity Statin
fewer interactions; consider in re-challenges
Indication: Hypercholesterolemia; reduces risk of ASCVD
MOA: inhibit HMG-CoA, a rate-limiting enzyme in cholesterol biosynthesis, reducing LDL
Common AE: constipation, abdominal pain, diarrhea, dyspepsia, nausea - but mostly well-tolerated
Serious AE: elevations in liver function (monitor LFTs) and liver toxicity (LFT elevations > 3X upper limit of normal), myopathy, rhabdomyolysis
may increase risk of getting diabetes mellitus
CI: NEVER in pregnant women
Discontinue: serum transaminase levels (liver function) rise to 3X upper limit of normal; signs or symptoms of myopathy
check dosage if patients have renal function issues
Interactions: drugs that inhibit metabolism: cyclosporine and gemfibrozil (statins metabolized by cytochrome p-450s)
maximum effect on lipids at 4-6 weeks - follow-up and check cholesterol levels/adherence at this time
Monitor: liver enzymes (LFTs) at baseline and as clinically indicated after; Creatinine Kinase in patients at risk for myopathy or complaining of muscle pain, weakness, tenderness, or brown urine; check for symptoms of myopathy at 6-12 weeks
Re-challenge intolerance after 2-4 weeks except in patients with Rhabdomyolysis
Sivastatin
Statin
not metabolized by cytochrome 450
fewer interactions; consider in re-challenges
Indication: Hypercholesterolemia; reduces risk of ASCVD
MOA: inhibit HMG-CoA, a rate-limiting enzyme in cholesterol biosynthesis, reducing LDL
Common AE: constipation, abdominal pain, diarrhea, dyspepsia, nausea - but mostly well-tolerated
Serious AE: elevations in liver function (monitor LFTs) and liver toxicity (LFT elevations > 3X upper limit of normal), myopathy, rhabdomyolysis
may increase risk of getting diabetes mellitus
CI: NEVER in pregnant women
Discontinue: serum transaminase levels (liver function) rise to 3X upper limit of normal; signs or symptoms of myopathy
check dosage if patients have renal function issues
Interactions: drugs that inhibit metabolism: cyclosporine and gemfibrozil (statins metabolized by cytochrome p-450s)
maximum effect on lipids at 4-6 weeks - follow-up and check cholesterol levels/adherence at this time
Monitor: liver enzymes (LFTs) at baseline and as clinically indicated after; Creatinine Kinase in patients at risk for myopathy or complaining of muscle pain, weakness, tenderness, or brown urine; check for symptoms of myopathy at 6-12 weeks
Re-challenge intolerance after 2-4 weeks except in patients with Rhabdomyolysis
Ezetimibe
Cholesterol Absorption Inhibitor
Indication: sometimes recommended for hypercholesterolemia
MOA: inhibits cholesterol absorption in the small intestine, preventing delivery to liver, causing an increase in cholesterol clearance from the blood
AE: similar to placebo, possible increase in transaminases
CI: similar to placebo, possible increase in transaminases
primary used in combination with a statin when adequate reductions in cholesterol is not achieved, in patients that are intolerant to statins, or when patients can only tolerate moderate intensity statins
Alirocumab
PCSK9 Inhibitor
Indications: sometimes recommended for hypercholesterolemia
MOA: inhibits binding of PCSK9 to LDL receptors on hepatocytes; LDL receptors are not degraded and stay to clear LDL from circulation
AE: well tolerated, injection site reactions, flu, common cold, itching, serious allergic reaction
new; don’t know long-term effects
expensive ($14,000/year)
consider as add-on for familial hypercholesterolemia
Evolocumab
PCSK9 Inhibitor
Indications: sometimes recommended for hypercholesterolemia
MOA: inhibits binding of PCSK9 to LDL receptors on hepatocytes; LDL receptors are not degraded and stay to clear LDL from circulation
AE: well tolerated, injection site reactions, flu, common cold, itching, serious allergic reaction
new; don’t know long-term effects
expensive ($14,000/year)
consider as add-on for familial hypercholesterolemia
Cholestyramine
Bile Acid Sequesterants (Resins)
Indications: not generally recommended for hypercholesterolemia
MOA: bind to bile acids I the gut, which are then excreted; hepatic cholesterol converts to bile, more LDL receptors are made to make-up for loss of cholesterol inside of the liver, cholesterol is removed from the blood
AE: nausea, constipation, bloating, flatulence, may worsen elevated triglycerides, impair absorption of fat soluble vitamins (remains in GI tract, so AE remain here)
Interactions: may prevent absorption of other drugs; take 1 hour before or 4 hours after other medications
Dosing: start low and go slow
only hypercholesterolemia treatment recommended for pregnant women
usually with a statin
reduce CHD events in patients with CHD
Colesevelam
Bile Acid Sequesterants (Resins)
less likely to cause AE
Indications: not generally recommended for hypercholesterolemia
MOA: bind to bile acids I the gut, which are then excreted; hepatic cholesterol converts to bile, more LDL receptors are made to make-up for loss of cholesterol inside of the liver, cholesterol is removed from the blood
AE: nausea, constipation, bloating, flatulence, may worsen elevated triglycerides, impair absorption of fat soluble vitamins (remains in GI tract, so AE remain here)
Interactions: may prevent absorption of other drugs; take 1 hour before or 4 hours after other medications
Dosing: start low and go slow
only hypercholesterolemia treatment recommended for pregnant women
usually with a statin
reduce CHD events in patients with CHD
Colestipol
Bile Acid Sequesterants (Resins)
Indications: not generally recommended for hypercholesterolemia
MOA: bind to bile acids I the gut, which are then excreted; hepatic cholesterol converts to bile, more LDL receptors are made to make-up for loss of cholesterol inside of the liver, cholesterol is removed from the blood
AE: nausea, constipation, bloating, flatulence, may worsen elevated triglycerides, impair absorption of fat soluble vitamins (remains in GI tract, so AE remain here)
Interactions: may prevent absorption of other drugs; take 1 hour before or 4 hours after other medications
Dosing: start low and go slow
only hypercholesterolemia treatment recommended for pregnant women
usually with a statin
reduce CHD events in patients with CHD
Niacin ER, IR, or SR
Nicotinic Acid
Indication: generally not recommended for Hypercholesterolemia
MOA: inhibits fatty acid release from adipose tissue and inhibits fatty acid and triglyceride production in liver cells
AE: flushing (IR), itching, gastric distress, headache, hepatotoxicity (SR), hyperglycemia, hyperuremia
reduce flushing by taking aspirin or NSAID 30 min prior; take with food; start at low dose
also known as vitamin B3, but the lipid treatment is a higher dose than the nutritional supplement
Fenofibrate
Fibric Acid Derivatives
Indications: generally not recommended for Hypercholesterolemia
MOA: work by activating PPAR-alpha, which leads to destruction and removal of triglycerides and causes an increase in HDL production
AE: nausea, diarrhea, flatulence, fatigue, gallstones, myositis, hepatitis
CI: gallbladder disease, liver dysfunction, or severe kidney dysfunction
Interactions: increase risk of rhabdomyolysis with statin, increase risk of bleeding with warfarin
most effective triglyceride lowering drug; decrease by 20-50%
max effect 2 weeks for Fenofibrate and 3-4 weeks for gemfibrozil
Gemfibrozil
Fibric Acid Derivatives
Indications: generally not recommended for Hypercholesterolemia
MOA: work by activating PPAR-alpha, which leads to destruction and removal of triglycerides and causes an increase in HDL production
AE: nausea, diarrhea, flatulence, fatigue, gallstones, myositis, hepatitis
CI: gallbladder disease, liver dysfunction, or severe kidney dysfunction
Interactions: increase risk of rhabdomyolysis with statin, increase risk of bleeding with warfarin
most effective triglyceride lowering drug; decrease by 20-50%
max effect 2 weeks for Fenofibrate and 3-4 weeks for gemfibrozil
Lovaza
Omega 3 Fatty Acid
AE: eructation (burping), dyspepsia, taste perversion
Indication: generally not recommended for hypercholesterolemia
MOA: reduced synthesis and increased clearance of triglycerides
Caution: hypersensitivity to fish/shellfish
Interactions; anticoagulant or antiplatelet agents (may increase risk of bleeding and hemorrhagic stroke)
Vascepa
Omega 3 Fatty Acid
AE: arthralgia
Indication: generally not recommended for hypercholesterolemia
MOA: reduced synthesis and increased clearance of triglycerides
Caution: hypersensitivity to fish/shellfish
Interactions; anticoagulant or antiplatelet agents (may increase risk of bleeding and hemorrhagic stroke)
Epanova
Omega 3 Fatty Acid
AE: diarrhea, nausea, abdominal pain or discomfort
Indication: generally not recommended for hypercholesterolemia
MOA: reduced synthesis and increased clearance of triglycerides
Caution: hypersensitivity to fish/shellfish
Interactions; anticoagulant or antiplatelet agents (may increase risk of bleeding and hemorrhagic stroke)
Omtrya
Omega 3 Fatty Acid
AE: eructation (burping), dyspepsia, taste perversion
Indication: generally not recommended for hypercholesterolemia
MOA: reduced synthesis and increased clearance of triglycerides
Caution: hypersensitivity to fish/shellfish
Interactions; anticoagulant or antiplatelet agents (may increase risk of bleeding and hemorrhagic stroke)
Lomitapide
Microsomal Transfer Protein Inhibitor
Indication: generally not recommended for hypercholesterolemia
MOA: oral inhibitor of microsomal triglyceride transfer protein; prevents assembly of Apo-B lipoproteins, ultimately reducing LDL
AE: GI side effects (low fat diet may reduce), elevation in liver enzymes and hepatic fat, hepatotoxicity
CI: NEVER in pregnancy
Interactions: strong and moderate cytochrome P-450 3A4 inhibitors, warfarin, lovastatin, simvastatin
available only through the Risk Evaluation and Mitigation Strategy program (REMS)
metabolized extensively by CYP450
Quinidine
Class IA Antiarrhythmic
intermediate potency
IV
MOA: blocks sodium from entering cardiac cell, making it harder to depolarize
AE: proarrhythmic, increased risk of death (consult)
Procainamide
Class IA Antiarrhythmic
intermediate potency
IV
MOA: blocks sodium from entering cardiac cell, making it harder to depolarize
AE: hypotension, torsades due pointes, proarrhythmic, increased risk of death (consult)
Disopyramide
Class IA Antiarrhythmic
intermediate potency
IV
MOA: blocks sodium from entering cardiac cell, making it harder to depolarize
AE: proarrhythmic, increased risk of death (consult)
Lidocaine
Class IB Antiarrhythmics - lowest potency, minimal effect on conduction velocity at normal heart rates
IV
MOA: blocks sodium from entering cardiac cell, making it harder to depolarize
AE: proarrhythmic, increased risk of death (consult)
Mexiletine
Class IB Antiarrhythmics - lowest potency, minimal effect on conduction velocity at normal heart rates
IV
MOA: blocks sodium from entering cardiac cell, making it harder to depolarize
AE: GI distress, tremor, dizziness, fatigue, seizures (if dose too high)
Flecainide
Class IC Antiarrhythmics - greatest potential for slowing ventricular conduction
Conversion to Sinus Rhythm, Maintenance of Sinus Rhythm
oral
MOA: blocks sodium from entering cardiac cell, making it harder to depolarize
AE: dizziness, blurred vision, HF exacerbation, proarrhythmic, increased risk of death (consult)
Propafenone
Class IC Antiarrhythmics - greatest potential for slowing ventricular conduction
oral
Conversion to Sinus Rhythm, Maintenance of Sinus Rhythm
MOA: blocks sodium from entering cardiac cell, making it harder to depolarize
AE: dizziness, blurred vision, proarrhythmic, increased risk of death (consult)
Amiodarone
Potassium Channel Blockers (also has CCB and BB activity)
Class III Antiarrhythmic (technically can work as all four classes); Ventricular Rate Control (second-line)
Conversion to Sinus Rhythm, Maintenance of Sinus Rhythm
MOA: blocks potassium from leaving cardiac cell, slowing repolarization
AE: IV: hypotension, sinus bradycardia
Oral: blue-gray skin, photosensitivity, corneal microdeposits, pulmonary fibrosis, pulmonary toxicity, hepatotoxicity, sinus bradycardia, hypo or hyperthyroidism, peripheral neuropathy, weakness, AV block, exacerbated arrhythmias
Dafetilide
Potassium Channel Blockers
Class III Antiarrhythmic
Conversion to Sinus Rhythm and Maintenance of Sinus Rhythm
MOA: blocks potassium from leaving cardiac cell, slowing repolarization
AE: torsades de pointes, hospitalize for initiation, correct potassium first, proarrhythmic, death
Dronedarone
Potassium Channel Blockers
Class III Antiarrhythmic
Maintenance of Sinus Rhythm
MOA: blocks potassium from leaving cardiac cell, slowing repolarization
AE: diarrhea, asthenia, n/v abdominal pain, bradycardia, GI distress, hepatotoxicity, worsening HF, increased risk of stroke, arrhythmias, death
CI: do not use in severe HF-increase death by 2X!
Ibutilide
Potassium Channel Blockers
Class III Antiarrhythmic
Conversion to Sinus Rhythm
MOA: blocks potassium from leaving cardiac cell, slowing repolarization
Soltolol
DOES NOT WORK AS BB - FOR ARRHYTHMIAS
Potassium Channel Blockers
Class III Antiarrhythmic
Maintenance of Sinus Rhythm
MOA: blocks potassium from leaving cardiac cell, slowing repolarization
AE: sinus bradycardia, AV block, fatigue, torsades de pointes, hospitalize for initiation, do not abruptly discontinue, monitor QT, proarrhythmic, death
Adenosine
Non-class Antiarrhythmic - drug of choice for PVST
IV Push
MOA: causes direct AV node inhibition
AE: chest pain (not ischemia), flushing, shortness of breath (bronchospasm possible), sinus bradycardia, AV block
Interactions: dipyridamole and carbamazepine = increase response to adenosine
successful in 90-95% of patients
extremely short half-life: 10 seconds
must administer very quickly
Warfarin
Anticoagulant
Fondaparinux
Indirect Xa Inhibitor
Anticoagulant
Rivaroxaban
Direct Xa Inhibitor
Anticoagulant
Apixaban
Direct Xa Inhibitor
Anticoagulant
Lepiruidin
Direct Thrombin Inhibitor
Anticoagulant
IV
No longer in use
Bivalirudin
Direct Thrombin Inhibitor
Anticoagulant
IV
Desirudin
Direct Thrombin Inhibitor
Anticoagulant
SubQ
Aragatroban
Direct Thrombin Inhibitor
Anticoagulant
IV
Unfractionated Heparin
Anticoagulant
Dalteparin
Low Molecular Weight Heparin
Enoxaparin
Low Molecular Weight Heparin
Asprin
Antiplatelet
Dipyridamole
antiplatelet that is expensive, but sometimes added to aspirin
Clopidogrel
P2Y12 Inhibitor
Prasugrel
P2Y12 Inhibitor
Ticagrelor
P2Y12 Inhibitor
Congrelor
P2Y12 Inhibitor
Abciximab
Glycoprotein IIb/IIIc Receptor Inhibitors
Eptifbatide
Glycoprotein IIb/IIIc Receptor Inhibitors
Tirofiban
Glycoprotein IIb/IIIc Receptor Inhibitors
Alteplase
Fibrin Specific Fibrinolytic
Reteplase
Fibrin Specific Fibrinolytic
Tenecteplase
Fibrin Specific Fibrinolytic
Streptokinase
Fibrin Non-Specific Fibrinolytic
Urokinase
Fibrin Non-Specific Fibrinolytic
Nitroglycerin
Short-Acting Nitrates
Nitroglycerin ER
Long-Acting Nitrates
Isosorbide dinitrate
Long-Acting Nitrates
Isosorbide Mononitrate
Long-Acting Nitrates
Ranolazine
Treats Angina