Antihypertensives Flashcards by Sarah Zarzeczny

Captopril

CLASS: Ace Inhibitor( 1st line)
particularly for diabetics

MOA: No reflex tachycardia, etc.
[indirect, 2° mechanisms]
Inhibit ACE! ↓Na+ and H2O
retention
↑renin &amp; ↑Angiotensin I
↑bradykinin [potent vasodilator

USES:HTN– most effective in young white pts. DOC for Post-MI

AE:Hyperkalemia, dry hacking cough, rash, fever, altered taste, and hypotension

Acute renal failure in pts w/ bilateral renal aa. stenosis

Contraindicated in pts w/ bilateral renal aa. stenosis and
Pregnancy

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Enalapril

CLASS: Ace Inhibitor( 1st line)
particularly for diabetics

MOA: No reflex tachycardia, etc.
[indirect, 2° mechanisms]
Inhibit ACE! ↓Na+ and H2O
retention
↑renin &amp; ↑Angiotensin I
↑bradykinin [potent vasodilator

USES:HTN– most effective in young white pts. DOC for Post-MI

AE:Hyperkalemia, dry hacking cough, rash, fever, altered taste, and hypotension

Acute renal failure in pts w/ bilateral renal aa. stenosis

Contraindicated in pts w/ bilateral renal aa. stenosis and
Pregnancy

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Lisinopril

CLASS: Ace Inhibitor( 1st line)
particularly for diabetics

MOA: No reflex tachycardia, etc.
[indirect, 2° mechanisms]
Inhibit ACE! ↓Na+ and H2O
retention
↑renin &amp; ↑Angiotensin I
↑bradykinin [potent vasodilator

USES:HTN– most effective in young white pts. DOC for Post-MI

AE:Hyperkalemia, dry hacking cough, rash, fever, altered taste, and hypotension

Acute renal failure in pts w/ bilateral renal aa. stenosis

Contraindicated in pts w/ bilateral renal aa. stenosis and
Pregnancy

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Losartan

CLASS: ARB,

MOA: Very similar to ACE-I’s
↓ PVR → ↓ BP
↓aldosterone! ↓Na+ and H2O
retention
↓ diabetic nephrotoxicity
No effect on bradykinin

USES: HTN, Lostarn helps pts with Gout, alternative to ACE-I

AE:Similar to ACE-Is excepts that angioedema risk is much lower
[related to bradykinin] and NO dry cough

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Valsartan

CLASS: ARB,

MOA: Very similar to ACE-I’s
↓ PVR → ↓ BP
↓aldosterone! ↓Na+ and H2O
retention
↓ diabetic nephrotoxicity
No effect on bradykinin

USES: HTN, alternative to ACE-I

AE:Similar to ACE-Is excepts that angioedema risk is much lower
[related to bradykinin] and NO dry cough

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Aliskiren

CLASS: Renin Inhibitor

MOA:Inhibits renin!prevent
conversion of angiotensinogen to
ATI!↓production of both ATII & aldosterone

USES: HTN

AE:Similar to ACE-Is excepts that angioedema risk is much lower [related to bradykinin] and NO dry cough

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Verapamil

CLASS: Ca channel blocker (1st line) , Non Dihydropyridine

MOA: Bind to L-type Ca2+ channels in the
Heart and Muscle of the
peripheral vasculature→
↓calcium entry → relaxation of muscle → -ve inotropism and/or vasodilation
Intrinsic natriuretic effect!no
need for diuretic

USES:Angina
SVT tachyarrhythmia
HTN (black and/or elderly pts)
Migraine
Cerebral vasospasm
Useful in pts with asthma,
diabetes, and peripheral
vascular resistance

AE:Constipation
Contraindicated in pts on β-blockers, 2n/3rd° AV block or severe LV systolic
dysfx

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Diltiazem

CLASS: Ca channel blocker (1st line) , Non Dihydropyridine

USES:Angina
SVT tachyarrhythmia
HTN (black and/or elderly pts)
Migraine
Cerebral vasospasm
Useful in pts with asthma,
diabetes, and peripheral
vascular resistance

AE:Constipation
Contraindicated in pts on β-blockers, 2n/3rd° AV block or severe LV systolic
dysfx

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Nifedipine [1st gen]

CLASS: Ca channel blocker (1st line) , Dihydropyridine

MOA: Greater affinity for vasculature Ca
channels! No ↓CO
Intrinsic natriuretic effect!no
need for diuretic

USES:HTN (black and/or elderly pts)
Angina Useful in pts with asthma,
diabetes, and peripheral
vascular resistance

AE:Hypotension
Peripheral edema
Dizzy, HA, fatigue, flushing
Gingival hyperplasia
Reflex tachycardia

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Amlodipine [2nd gen]

CLASS: Ca channel blocker (1st line) , Dihydropyridine

MOA: Greater affinity for vasculature Ca
channels! No ↓CO
Intrinsic natriuretic effect!no
need for diuretic

USES:HTN (black and/or elderly pts)
Angina Useful in pts with asthma,
diabetes, and peripheral
vascular resistance

AE:Hypotension
Peripheral edema
Dizzy, HA, fatigue, flushing
Gingival hyperplasia
Reflex tachycardia

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Chlorthalidone

CLASS:Thiazide Diuretic(1st line)

MOA:↑Na+ & H2O excretion →↓ECF → ↓CO & renal blood flow [in the long term, thereis normal plasma volume, but
↓ PVR]

USES:Counteract Na+ & H2O
retention caused by other
anti HTN drugs [useful in
combination therapy]

DOC for Blacks and elderly
[with normal renal and
cardiac fxn]

AE:Hypokalemia
Hyperuricemia
Hyperglycemia
Hypomagnesemia
Hyperlipidemia

Contraindicated in diabetics

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Hydrochlorothiazide

CLASS:Thiazide Diuretic(1st line)

MOA:↑Na+ & H2O excretion →↓ECF → ↓CO & renal blood flow [in the long term, thereis normal plasma volume, but
↓ PVR]

USES:Counteract Na+ & H2O
retention caused by other
anti HTN drugs [useful in
combination therapy]

DOC for Blacks and elderly
[with normal renal and
cardiac fxn]

AE:Hypokalemia
Hyperuricemia
Hyperglycemia
Hypomagnesemia
Hyperlipidemia

Contraindicated in diabetics

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Metolazone

CLASS:Thiazide Diuretic(1st line)

MOA:↑Na+ & H2O excretion →↓ECF → ↓CO & renal blood flow [in the long term, thereis normal plasma volume, but
↓ PVR]

USES:Counteract Na+ & H2O
retention caused by other
anti HTN drugs [useful in
combination therapy]

DOC for Blacks and elderly
[with normal renal and
cardiac fxn]

AE:Hypokalemia
Hyperuricemia
Hyperglycemia
Hypomagnesemia
Hyperlipidemia

Contraindicated in diabetics

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Furosemide

CLASS:Loop diuretic

MOA:↓ renal vascular resistance ↑ renal blood flow

USES:DOC for pts with poor
renal function or
unresponsive to other
diuretics i.e. thiazides

AE:More potent and can cause more side effects

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Torsemide

CLASS:Loop diuretic

MOA:↓ renal vascular resistance ↑ renal blood flow

USES:DOC for pts with poor
renal function or
unresponsive to other
diuretics i.e. thiazides

AE:More potent and can cause more side effects

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Amiloride

CLASS:K sparing diuretics, 2nd line agents

MOA:Decrease the K+ lost in urine caused by thiazide or loop diuretics

USES:Used in combo with other diuretics

AE:

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Triamterene

CLASS:K sparing diuretics, 2nd line agents

MOA:Decrease the K+ lost in urine caused by thiazide or loop diuretics

USES:Used in combo with other diuretics

AE:

Spironolactone

CLASS:K sparing diuretics, 2nd line agents

MOA:Aldosterone antagonists → inhibition of Na+ and H2O retention
→ inhibition of vasoconstriction

USES:1st line in patients with
HTN and severe LV dysfunction

AE:Reduced K+ excretion → risk of hyperkalemia

Eplerenone

CLASS:K sparing diuretics, 2nd line agents

MOA:Aldosterone antagonists → inhibition of Na+ and H2O retention
→ inhibition of vasoconstriction

USES:1st line in patients with
HTN and severe LV dysfunction

AE:Reduced K+ excretion → risk of hyperkalemia

Propranolol

CLASS:B-Blockers(2nd line), Non Selective B

MOA:↓CO, contractility &amp;
HR!↓BP
↓CNS sympathetic output
[especially with exercise]
↓NE &amp; renin (β1)→ ↓ ATII &amp;
Aldosterone secretion

USES:More effective in
young/white pts
DOC only for patients with
CAD, HF or post-MI

AE:Bradycardia, CNS effects, hypotension,
↓libido, impotence, lipid disturbance
[↓HDL, ↑TAG]
Abrupt withdrawal→ angina and MI in pts
with heart disease

Contraindicated in asthma and COPD

Mask symptoms of hypoglycemia

Pindolol

CLASS:B-Blockers(2nd line), Partial B agonist

MOA:↓CO, contractility &amp;
HR!↓BP
↓CNS sympathetic output
[especially with exercise]
↓NE &amp; renin (β1)→ ↓ ATII &amp;
Aldosterone secretion

USES:More effective in
young/white pts
DOC only for patients with
CAD, HF or post-MI

Preferred B-blocker in pregnancy

AE:Bradycardia, CNS effects, hypotension,
↓libido, impotence, lipid disturbance
[↓HDL, ↑TAG]
Abrupt withdrawal→ angina and MI in pts
with heart disease

Mask symptoms of hypoglycemia

Doxazosin

CLASS:a-blockers

MOA:Competitive inhibition of a1 receptors

↓PVR and MAP by relaxation of arterial and venous smooth muscle

Minimal change in CO, renal
blood flow & GFR → no long
term tachycardia

USES:Mild to moderate HTN in combination with
propranolol or a diuretic
[less common now due to
adverse effects]

BPH

AE:Reflex tachycardia and orthostatic hypotension may be seen with first dose, but not long term (α2 blocks
response by inhibiting NE) → add β-blocker

Dizziness, drowsiness, HA, fatigue, nausea, palpitations

Doxazosin has been shown to ↑rate of CHF

Prazosin

CLASS:a-blockers

MOA:Competitive inhibition of a1 receptors

↓PVR and MAP by relaxation of arterial and venous smooth muscle

Minimal change in CO, renal
blood flow & GFR → no long
term tachycardia

USES:Mild to moderate HTN in combination with
propranolol or a diuretic
[less common now due to
adverse effects]

BPH

AE:Reflex tachycardia and orthostatic hypotension may be seen with first dose, but not long term (α2 blocks
response by inhibiting NE) → add β-blocker

Dizziness, drowsiness, HA, fatigue, nausea, palpitations

Labetalol

CLASS: Mixed a/b blocker

MOA:NO reflex tachycardia or ↑CO [β1 effect is greater]
Safe in pregnancy

USES:Long term treatment of
HTN

HTN emergencies: IV
admin→ rapid drop in BP

AE:Orthostatic hypotension

Contraindicated in pheochromocytoma

Clonidine

CLASS:Central acting α2 -agonist MOA:↓sympathetic outflow[NE] by acting on presynaptic autoreceptors→ ↓PVR and CO→ ↓BP USES: 2nd line when HTN does not respond to TXT with 2+ drugs AE:Sedation, dry mouth, dizziness, HA, sexual dysfunction! common Abrupt withdrawal! Rebound HTN (avoid use w/ β-blocker)

Methyldopamine

CLASS:Central acting α2 -agonist MOA:↓ sympathetic outflow → ↓ PVR and BP [CO not affected] USES: DOC for pregnancy induced HTN Renal Insufficiency AE:Same as Clonidine + nightmares, mental depression, vertigo +ve coombs test can develop!hemolytic anemia, hepatitis & drug fever

Hydralazine

CLASS:Direct Vasodilators [3rd line], NEVER FIRST LINE MOA:Opening of K+ channels in smooth muscle → Arteriolar dilation [NOT venous) Direct acting smooth muscle relaxant. USES:DOC pregnancy induced hypertensive emergencies related to eclampsia AE:HA, tachycardia, nausea, sweating, flushing Lupus like syndrome [NAT] Reflex tachycardia and fluid retention [coadminister with a diuretic & β-blocker] Volume overload → edema and CHF

Hydralazine

Minoxidil | [Rogaine]

CLASS:Direct Vasodilators [3rd line], NEVER FIRST LINE MOA:Opening of K+ channels in smooth muscle → Arteriolar dilation [NOT venous) Direct acting smooth muscle relaxant. USES:Severe malignant HTN Male pattern baldness AE:HA, tachycardia, nausea, sweating, flushing Lupus like syndrome [NAT] Reflex tachycardia and fluid retention [coadminister with a diuretic & β-blocker] Volume overload → edema and CHF

Epoprostenol

CLASS:Prostaglandin, synthetic PGI2 MOA:Lowers peripheral, pulmonary and coronary resistance USES:Pulmonary HTN, continuous IV AE:Flushing, HA, jaw pain, diarrhea, arthralgia

Bosentan

CLASS: Non selective endothelin receptor blocker, PDE5 inhibitor MOA:Blocks endothelin mediated vasoconstriction by blocking initial transient depressor (ETA) and the prolonged pressor (ETB) USES:Pulmonary HTN, continuous IV AE:Pregnancy category X

Sildenafil

CLASS:Phosphodiesterase Inhibitor,PDE5 inhibitor MOA:↑cGMP causing vasodilation USES:Pulmonary HTN AE:HA, flushing, dyspepsia, cyanopsia (seeing everything blue) Contraindicated: Nitrates

Sodium | Nitroprusside

CLASS:DOC for hypertensive emergencies MOA:Prompt vasodilation and venodilation Reflex tachycardia [also given β-blocker] USES: hypertensive emergencies AE:Hypotension [overdose] Abdominal cramping, nausea, vomiting, goose bumps Cyanide toxicity: can be treated with sodium thiosulfate infusion→ thiocyanate→ elimination

Labetalol

CLASS:Combined α/β blocker MOA:NO reflex tachycardia USES: hypertensive emergencies AE:Contraindicated in pts with asthma, COPD 2nd or 3rd degree AV block Bradycardia

Fenoldopam

CLASS:Peripheral D1 agonist Safe in pts with renal insufficiency MOA:Arteriolar dilation Maintains renal perfusion as it lowers BP [protects the kidney] Promotes natiuresis USES: hypertensive emergencies AE:Contraindicated in patients with glaucoma

Nicardipine

CLASS:Ca2+ Channel blocker (Dihydropyridine MOA:Vascular smooth muscle relaxation USES: hypertensive emergencies AE:Reflex tachycardia

Nitroglycerin

CLASS:DOC for HTN emergencies in pts with cardiac ischemia, angina, or past cardiac bypass MOA:Vasodilation (veins>arteries) USES: hypertensive emergencies AE:

Diazoxide

CLASS:DOC for HTN emergencies in pts with cardiac ischemia, angina, or past cardiac bypass MOA:Vasodilation (veins>arteries) USES: hypertensive emergencies AE:

Diazoxide

CLASS: MOA:muscle contraction by opening K+ channels and stabilizing the membrane potential USES: hypertensive emergencies Can also be used to treat hypoglycemia secondary to an Insulinoma by inhibiting insulin release AE:Hypotension Reflex tachycardia Na+ and H2O retention

Phentolamine

DOC for pts with catecholamine release emergencies [pheochromocytoma

Esmolol

Used for aortic dissection or post-op HTN

Hydralazine

DOC for pregnancy induced hypertensive emergencies related to eclampsia