Hypertension Drugs Flashcards

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1
Q

Candesartan
Irbesartan
Losartan
Valsartan

A

AT1 antagonists (ARBs)

  • Non-peptide competitive agonists of AT1 receptors (inhibits vasoconstriction, Na retention, and renin feedback), reduce plasma volume, decrease cellular hypertrophy, residual AT2 stimulation (promote vasodilation and natriuresis), increase Ang-(1-7)
  • Fewer side effects than ACEIs – hypotension, hyperkalemia, acute renal failure, not for pregnancy or nursing moms
  • Hypertension, heart failure, diabetes, chronic kidney disease, prevent secondary MI
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2
Q
Catopril
Enalapril
Lisinopril
Fosinopril
Quinapril
A

ACE Inhibitors

  • More potent arterial than venous dilators (reduce afterload and increase SV and CO)
  • Block conversion of AI to AII and AIII (classical RAS pathway), elevate bradykinin levels, decrease peripheral resistance, decrease aldosterone, increase plasma renin, increase Ang-(1-7)
  • DRY COUGH, angioedema, hypotension, hyperkalemia, acute renal failure, rash, not for pregnancy or nursing moms
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3
Q

Conivaptan

A

Vasopressin Receptor Antagonists

  • V1/V2 receptor antagonist
  • Hyponatremia caused by SIADH (IV to hospitalized patients
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4
Q

Tolvaptan

A

Vasopressin Receptor Antagonists

  • Selective V2 receptor antagonist - oral
  • Hypervolemic and euvolemic hyponatremia resistant to fluid restriction (heart failure, cirrhosis, SIADH)
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5
Q

Aliskiren

A

Renin Inhibitor

  • Direct, competitive inhibitor of renin – increase plasma renin but not renin activity
  • GI/allergic symptoms, hypotension, hyperkalemia, acute renal failure, not for pregnancy or nursing moms
  • Essential Hypertension
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6
Q
Atenolol  (oral/IV)
Metoprolol (oral/IV)
Acebutolol
Esmolol (IV only)
Bisoprolol
A

Sympatholytics

  • B1 Receptor Antagonists
  • Decrease CO, renin secretion, central sympathetic outflow, resetting of baroreceptors, decrease HR and contractility, improve LV structure and function, improved abnormal Ca handling
  • Nausea, vomiting, confusion, fatigue, sleep disorders, avoid in asthmatics or PVD, increase in type 2 diabetes, hypoglycemia, hyperlipidemia, bradycardia, impotence, hypotension
  • Alone or in combo for hypertension, coronary heart disease w/o signs of acute heart failure (combo with nitrates), heart failure due to LVEF, atrial arrhythmias, slow AV node conduction, prevent sudden cardiac death post MI
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7
Q
Propranolol (oral/IV)
Nadolol
Pindolol
Timolol
Carvedilol (also a1
A

Sympatholytics

  • Nonselective beta antagonists
  • Decrease CO, renin secretion, central sympathetic outflow, resetting of baroreceptors, decrease HR and contractility, vasoconstriction, bronchoconstriction, impaired glycogenolysis, improve LV structure and function, improved abnormal Ca handling
  • Nausea, vomiting, confusion, fatigue, sleep disorders, avoid in asthmatics or PVD, increase type 2 diabetes, hypoglycemia, hyperlipidemia, bradycardia, impotence, hypotention
  • Alone or in combo for hypertension, coronary heart disease w/o signs of acute heart failure (combination with nitrates), heart failure due to LVEF, atrial arrhythmias, slow AV node conduction
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8
Q

Doxazosin
Prazosin
Terazosin

A

Sympatholytics

  • A receptor antagonists. Blockade of a1 receptors on VSM – dilation of arterioles and capacitance veins
  • Reflex tachycardia, orthostatic hypotension, fluid retention, GI upset, palpitation, tinnitus, headache, dizziness, urinary incontinence
  • Alone or in combination of hypertension, pheochromocytoma
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9
Q

Carvedilol

A

Sympatholytics

  • Mixed a/b antagonists
  • Non-selective B and a1 receptor antagonist
  • Antioxidant and antiprolifeartive – hypertension and heart failure
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10
Q

Labetalol

A

Sympatholytics

  • Mixed a/b antagonists
  • Non-selective B and a1 receptor antagonist
  • Chronic hypertension and hypertensive emergencies
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11
Q

Reserpine

A

Inhibitor of Peripheral Transmission

  • Deplete NE from adrenergic nerve endings, inhibits reuptake of NE into storage terminal, decrease peripheral resistance and CO
  • Postural hypotension, sedation, dry mouth, nightmares, sodium and water retention
  • Mild to moderate hypertension - can use low dose in combination with thiazide diuretic
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12
Q

a-methyldopa
Clonidine
Guanabenz

A

Central-Mediated Agents

  • Stimulate brainstem a2 adrenergic receptors (decrease sympathetic outflow), vagal activity to heart increased, decreased PVR and CO
  • Withdrawal/rebound, sedation, dry mouth, depression, drowsiness, sodium and water retention, postural hypotension
  • Resistant hypertension (clonidine), pregnancy induced hypertension (methyldopa)
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13
Q

Epoprostenol

A

Vasodilators

  • Prostacyclin – direct vasodilator via cAMP, counteracts thromboxane A2
  • Potent antihypertensive (continuously administered), primary pulmonary hypertension
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14
Q

Hydralazine

A

Vasodilators

  • Arterial vasodilator. Mechanism unclear – reduced intracellular Ca, preferential effect on arterioles, decrease PVR/MAP, reflex increase in HR, contractility, CO, increase renal blood flow.
  • Headache, anorexia, nausea, dizziness, sweating, angina or ischemic arrhythmias, incrased renin and fluid retention, Lupus
  • Mild to moderate hypertension in combination with diuretic and B-blocker, advanced heart failure
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15
Q

Minoxidil

A

Vasodilators

  • Preferential effect on arterioles, decrease PVR, activates K channels and VSM relaxation, reflex increase in HR, contractility, CO, renin secretion, fluid retetntion
  • Fluid retention, decreased PVR, activates K channels/VSM relaxation, reflex increase in HR
  • Resistant hypertension in combination with diuretic and B-blocker
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16
Q

Nitroglycerin

A

Nitrovasodilators

  • Short duration of action, tolerance, give sublingual
  • Effects mostly veins (decrease preload) and large arteries (relieve vasospam), generates nitric oxide through mtALDH which activates guanyyl cyclase, increase in cGMP, inhibits platelet aggregation
  • Headache (really bad), orthostatic hypotension, dizziness, flushing, syncope, reflex tachy, GI distress, don’t use with PDE5 inhibitors
  • Produce hypotension in surgery and hypertensive emergencies, CHD, angina, L sided heart failure due to acute MI
17
Q

Nitroprusside

A

Nitrovasodilators

  • IV only. Direct vasodilator, generates nitric oxide which activates guanylyl cyclease, increase in cGMP, effects on veins (decrease preload) and arteries (relieve vasospasm), inhibits platelet aggregation
  • Rapid decrease in MAP, cyanide accumulation, headache (really bad), orthostatic hypotension, dizziness, flushing, syncope, reflex tachy, GI distress, don’t use with PDE5 inhibitors
  • Produce hypotension in surgery and hypertensive emergencies, CHD, angina, decompensated heart failure
18
Q

Riociguat

A

Vasodilators

  • Directly stimulates guanylyl cyclase – increase cGMP
  • Headache, nausea, dizziness, diarrhea, hypotension, birth defects
  • Priamry pulmonary hypertension, thromboembolic pulmonary hypertension, combined with ET receptor blockers
19
Q

Diltiazem

Verapamil

A

Ca channel blockers

  • Cardioselective – negative chronotropic. Block voltage sensitive L-type Ca channels, decrease contractility of cardiac myocytes, decrease MAP, slow conduction.
  • Contraindicated in heart failure (edema), depresses AV conduction and contractility, headache, dizziness, nausea, gingival inflammation, arrhythmias, constipation
  • Best for African Americans with hypertension, chronic CHD, cerebral hemorrhage or vasospasm, re-entry SVTs involving AV node
20
Q

Amlodipine
Nicardipine
Nifedipine
Nimodipine (SAH only – lipophilic)

A

Ca channel blockers

  • Vasoselective. Block voltage sensitive L-type Ca channels, relax and dilate arteries (minimal effect on veins), prevent vasospasm, decrease MAP
  • Contraindicated in heart failure (edema), depresses AV conduction and contractility, headache, dizziness, nausea, gingival inflammation, arrhythmias, constipation
  • Best for African Americans with hypertension, chronic CHD, supraventricular arrhythmias, cerebral hemorrhage or vasospasm
21
Q

Chlorothiazide
Chlorthalidone
Hydrochlorothiazide

A

Diuretic - thiazide

  • Block Na-Cl symporter in DCT – moderate diuresis (reduced by NSAIDs)
  • Hypokalemia, decrease uric acid excretion, sulfa cross-reactivity
  • Hypertension (1st line) and heart failure
22
Q

Ethacrynic acid
Bumetanide
Furosemide
Torsemide

A

Diuretic – loop agents

  • Block Na-K-2Cl cotransporter in thick ascending limb of Loop of Henle
  • Hypokalemia, decrease uric acid excretion, deafness, allergic reaction
  • Hypertension and heart failure, use with edema (most effective)
23
Q

Amiloride

Triamterene

A

Diuretic – K+ sparing agents

  • Late distal tubule and collecting duct – Na channel blockers
  • Hyperkalemia
  • Hypertension and heart failure (use with thiazides)
24
Q

Eplerenone

Spironolactone

A

Aldosterone Receptor Antagonist

  • Collecting duct – block Na and H2O reabsorption, K sparing – inhibits aldosterone adverse effects on structure/function of heart
  • Hyperkalemia – don’t use without diuretics
  • Mild diuresis – resistant hypertension and CHF with hypertension, moderately sever heart failure or LV dysfunction after MI
25
Q

Avanafil
Sildenafil
Tadalafil
Vardenafil

A

PDE5 inhibitor

  • Increase levels of cGMP, modest drop in blood pressure
  • Hypotension when combined with nitrates or a blockers (excess cGMP), headache, rhinitis, flushing, back pain, loss of hearing/vision
  • ED and primary pulmonary hypertension (sildenafil)