Antihypertensives Flashcards
Captopril
CLASS: Ace Inhibitor( 1st line)
particularly for diabetics
MOA: No reflex tachycardia, etc. [indirect, 2° mechanisms] Inhibit ACE! ↓Na+ and H2O retention ↑renin & ↑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
Enalapril
CLASS: Ace Inhibitor( 1st line)
particularly for diabetics
MOA: No reflex tachycardia, etc. [indirect, 2° mechanisms] Inhibit ACE! ↓Na+ and H2O retention ↑renin & ↑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
Lisinopril
CLASS: Ace Inhibitor( 1st line)
particularly for diabetics
MOA: No reflex tachycardia, etc. [indirect, 2° mechanisms] Inhibit ACE! ↓Na+ and H2O retention ↑renin & ↑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
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
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
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
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
Diltiazem
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
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
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
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
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
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
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
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
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:
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 & HR!↓BP ↓CNS sympathetic output [especially with exercise] ↓NE & renin (β1)→ ↓ ATII & 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 & HR!↓BP ↓CNS sympathetic output [especially with exercise] ↓NE & renin (β1)→ ↓ ATII & 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
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
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
