Antihypertensives Flashcards
Captopril
Enalapril
Lisinopril
Class: ACE Inhibitor
First line agent
MOA:
- Inhibit ACE
- Dec. peripheral vascular resistance
- Dec. Na & H2O retention
- Inc. bradykinin
- Inc. renin
- Inc. angiotensin I
- Dec. angiotensin II
Use(s):
- HTN (whites, young); + diuretic (blacks)
- Preserve renal function (diabetic or non-diabetic nephropathy)
- CHF
- Following MI
Action(s):
- Dilate efferent arteriole, glomerulus
Adverse Effect(s):
- Dry hacking cough
- Hyperkalemia
- Hypotension
- Angioedema (rare)
- Acute renal failure
- Rash, fever, altered taste
Contraindication(s):
- Pregnancy
- Patients w/bilateral rental artery stenosis
- Patients w/angioedma
Losartan
Valsartan
Class: ARB
First-line agent
MOA:
- Block angiotensin II type I receptors
- Dec. BP via vasodilation
- Block aldosterone secretion
- Dec. Na & H2O retention
- Dec. diabetic nephropathy
- Inc. renin, angiotensin I & II
Use(s):
- HTN
- Preserve renal function
- CHF
- Following MI
Action(s):
- Losartan
- Dec. plasma uric acid via inhibiting URAT1, patient w/gout
Adverse Effect(s):
- Hyperkalemia
- Hypotension
- Angioedema (rarer)
- Acute renal failure
- Rash, fever, altered taste
Contraindication(s):
- Pregnancy
- Patients w/bilateral renal artery stenosis
Aliskiren
Class: Renin Inhibitor
MOA:
- Inhibit enzyme activity of renin
- Angiotensin -/-> angiotensin I
- Inhibit angiotensin II & aldosterone production
Use(s):
- HTN
Adverse Effect(s):
- Hyperkalemia
- Hypotension
- Angioedema (rare)
- Acute renal failure
- Rash, fever, altered taste
Contraindication(s):
Verapamil
Class: Ca-Channel Blocker
Non-dihydropyridine
First-line agent
MOA:
- Dec. free Ca
- Myofibril/vascular relaxation
Use(s):
- Angina
- Supraventricular tachyarrhythmias
- HTN
- Migraine
- Cerebral vasospasm
Adverse Effect(s):
- Constipation
- Negative inotropic effects
- Gingival hyperplasia
Contraindication(s):
- Patients taking B-blockers
- Patients w/2nd or 3rd degree heart block
- Patients w/severe left ventricular systolic dysfunction
Diltiazem
Class: Ca-Channel Blocker
Non-dihydropyridine
First-line agent
MOA:
- Dec. free Ca
- Myofibril/vascular relaxation
Use(s):
- Angina
- Supraventricular tachyarrhythmias
- HTN
- Cerebral vasospasm
Adverse Effect(s): - Negative inotropic effects
Contraindication(s):
- Patients taking B-blockers
- Patients w/2nd or 3rd degree heart block
- Patients w/severe left ventricular systolic dysfunction
Amlodipine
Nifedipine
Class: Ca-Channel Blocker
Dihydropyridines
MOA:
- Dec. free Ca
- Myofibril/vascular relaxation
- Great affinity for vascular Ca
- Peripheral vasodilation
- Lower BP
Use(s):
- HTN
Adverse Effect(s):
- Hypotension
- Peripheral edema
- Reflex tachycardia
- Dizziness
- Headache
- Fatigue
- Gingival hyperplasia
- Flushing
Hydrochlorothiazide
Chlorthalidone
Metolazone
Class: Diuretic, Thiazides
MOA:
- Inc. Na & H2O excretion
- Dec. extracellular volume
- Dec. CO & renal blood flow
- Dec. extracellular volume
- Dec. peripheral resistance
Use(s):
- HTN (black and/or elderly)
- Counteract Na & H2O retention
Adverse Effect(s):
- Hypokalemia
- Hyperuricemia
- Hyperglycemia
- Hypomagnesemia
- Hypercholesterolemia
- Sexual dysfunction
Furosemide
Class: Loop diuretic
3rd-line due to potency
MOA:
- Dec. renal vascular resistance
- Inc. renal blood floww
Use(s):
- Patients not responding to thiazide therapy
- Poor renal function
- Heart failure
Spironolactone
Eplerenone
Class: K-sparing diuretic
MOA:
- Aldosterone antagonist
Use(s):
- Dec. K loss from other diuretics
- HTN
- Heart failure
Amiloride
Triamterene
Class: K-sparing diuretic
MOA:
- ENaC blocker -/-> Dec. Na/K exchange
Use(s):
- Dec. K loss from other diuretics
- HTN
- Heart failure
Atenolol
Metoprolol
Pindolol
Propranolol
B-blockers
Add-on therapy
Atenolol: Selective B1 antagonist
Metoprolol: Selective B1 antagonist
Pindolol: Non-selective partial agonist
Propranolol: Non-selective antagonist
MOA:
- Dec. CO, contractility, HR
- Blunt sympathetic reflex w/exercise
- Inhibit both NE & renin release
Use(s):
- Patients w/coronary artery disease
- Patients w/heart failure
- Patients post-op MI
Adverse Effect(s):
- Bradycardia
- CNS effects
- Hypotension
- Dec. libido & impotence
- Disturb lipid metabolism
- Hypoglycemia
- Drug withdrawl
Contraindication(s):
- Non-selective, asthma & COPD
Prazosin
Doxazosin
a1-Blockers
MOA:
- Competitively block a1-adrenoceptors
- Dec. peripheral vascular resistance
- Dec. arterial BP by relaxing vessel SM
- No long-term tachycardia
Use(s):
- HTN
- BPH
- Heart failure (rare)
Action(s):
- Na retention
- H2O retention
Adverse Effect(s):
- Orthostatic hypotension
- Dizziness
- Drowsiness
- Headache
- Lack of energy
- Nausea
- Palpitations
- CHF (Doxazosin)
Labetalol
a-/B-blocker (Mixed)
MOA:
Use(s):
- HTN management
Adverse Effect(s): - Orthostatic hypotension
Clonidine
a2-Agonist
MOA:
- Dec. sympathetic outflow
- Dec. PVR
Use(s):
- HTN management
- HTN crises
Adverse Effect(s):
- Drowsiness
- Dry mouth
- Dizziness
- Headache
- Sexual dysfunction
- Rebound HTN, abrupt withdrawl
Methyldopa
a2-Agonist
MOA:
- Dec. sympathetic outflow
- Dec. PVR
Use(s):
- HTN management
- Pregnancy-induced HTN
Adverse Effect(s):
- Drowsiness
- Dry mouth
- Dizziness
- Headache
- Sexual dysfunction
- Sedation
- Hypoprolactinemia
- Nightmares
- Mental depression
- Reversible lupus-like syndrome
- Positive Coombs test
