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Antihypertensives
USES ACTION

Treatment of mild to severe hypertension.
Many groups of medications are used in the treatment of
hypertension.
ACE inhibitors: Decrease conversion of angiotensin I to
angiotensin II, a potent vasoconstrictor, reducing periph-
eral vascular resistance and B/P.
Alpha agonists (central action): Stimulate alpha2-
adrenergic receptors in the cardiovascular centers of the
CNS, reducing sympathetic outflow and producing an
antihypertensive effect.
Alpha antagonists (peripheral action): Block alpha1-
adrenergic receptors in arterioles and veins, inhibiting
vasoconstriction and decreasing peripheral vascular re-
sistance, causing a fall in B/P.
Angiotensin receptor blockers: Block vasoconstrictor
effects of angiotensin II by blocking the binding of angio-
tensin II to AT1 receptors in vascular smooth muscle,
helping blood vessels to relax and reduce B/P.
Antihypertensives
Beta blockers: Decrease B/P by inhibiting beta1-
adrenergic receptors, which lowers heart rate, heart
workload, and the heart’s output of blood.
Calcium channel blockers: Reduce B/P by inhibiting flow
of extracellular calcium across cell membranes of vascu-
lar tissue, relaxing arterial smooth muscle.
Diuretics: Inhibit sodium (Na) reabsorption, increasing
excretion of Na and water. Reduce plasma, extracellular
fluid volume, and peripheral vascular resistance.
Renin inhibitors: Directly inhibit renin, decreasing plasma
renin activity (PRA), inhibiting conversion of angiotensino-
gen to angiotensin, producing antihypertensive effect.
Vasodilators: Directly relaxe arteriolar smooth muscle,
decreasing vascular resistance. Exact mechanism
unknown.
ANTIHYPERTENSIVES

Name Availability Dosage Range Side Effects
(ACE) Inhibitors
Benazepril T: 5 mg, 10 mg, 20 mg, 40 mg 20–80 mg/day as single Postural dizziness, headache, cough
(Lotensin) or 2 divided doses
Enalapril (Vasotec) T: 2.5 mg, 5 mg, 10 mg, 20 mg 2.5–40 mg/day in Hypotension, chest pain, syncope, headache, dizziness,
1–2 divided doses fatigue
Lisinopril T: 2.5 mg, 5 mg, 10 mg, 20 mg, 10–40 mg/day Hypotension, headache, fatigue, dizziness, hyperkalemia,
(Prinivil, Zestril) 30 mg, 40 mg cough
Quinapril T: 5 mg, 10 mg, 20 mg, 40 mg 10–40 mg/day Hypotension, dizziness, fatigue, headache, myalgia,
hyperkalemia
Ramipril (Altace) T or C: 1.25 mg, 2.5 mg, 5 mg, 2.5–20 mg/day Cough, hypotension, angina, headache, dizziness,
10 mg hyperkalemia
Alpha Agonists: Central Action
Clonidine (Catapres) T: 0.1 mg, 0.2 mg, 0.3 mg PO: 0.1–0.8 mg/day Sedation, dry mouth, constipation, sexual dysfunction,
P: 0.1 mg/hr, 0.2 mg/hr, 0.3 mg/hr Topical: 0.1–0.6 mg/wk bradycardia, xerostomia, drowsiness, headache

Antihypertensives
Methyldopa T: 125 mg, 250 mg, 500 mg PO: 250–1,000 mg/day Nausea, vomiting, weight gain, impaired memory, depression,
(Aldomet) in 2 divided doses nasal congestion
Alpha Agonists: Peripheral Action
Doxazosin (Cardura) T: 1 mg, 2 mg, 4 mg, 8 mg PO: 2–16 mg/day Dizziness, vertigo, headaches
Prazosin (Minipress) C: 1 mg, 2 mg, 5 mg PO: 6–20 mg/day Dizziness, light-headedness, headaches, drowsiness
Terazosin (Hytrin) C: 1 mg, 2 mg, 5 mg, 10 mg PO: 1–20 mg/day Dizziness, headaches, asthenia (loss of strength, energy)
Angiotensin Receptor Blockers
Azilsartan (Edarbi) T: 40 mg, 80 mg 40–80 mg/day Diarrhea, hypotension, nausea, cough

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CLASSIFICATIONS
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ANTIHYPERTENSIVES—cont’d
Name Availability Dosage Range Side Effects

Antihypertensives
Candesartan T: 4 mg, 8 mg, 16 mg, 32 mg 8–32 mg/day Hypotension, dizziness, headache, hyperkalemia
(Atacand)
Losartan (Cozaar) T: 25 mg, 50 mg, 100 mg 25–100 mg/day Chest pain, fatigue, hypoglycemia, weakness, cough,
hypotension
Olmesartan T: 5 mg, 20 mg, 40 mg 20–40 mg/day Dizziness, headache, diarrhea, flu-like symptoms
(Benicar)
Valsartan (Diovan) T: 80 mg, 160 mg, 320 mg 80–320 mg/day Dizziness, fatigue, increased BUN
Beta Blockers
Atenolol (Tenormin) T: 25 mg, 50 mg, 100 mg 25–100 mg/day Fatigue, bradycardia, reduced exercise tolerance, increased
triglycerides, bronchospasm, sexual dysfunction, masked
hypoglycemia
Bisoprolol (Zebeta) T: 5 mg, 10 mg 2.5–10 mg/day Fatigue, insomnia, diarrhea, arthralgia, upper respiratory
infections
Metoprolol T: 25 mg, 50 mg, 100 mg 50–100 mg/day Hypotension, bradycardia, fatigue, 1st degree heart block,
(Lopressor) dizziness
Metoprolol XL T: 25 mg, 50 mg, 100 mg, 200 mg 50–100 mg/day Same as metoprolol
(Toprol XL)
Calcium Channel Blockers
Amlodipine T: 2.5 mg, 5 mg, 10 mg 2.5–10 mg/day Headache, fatigue, peripheral edema, flushing, worsening
(Norvasc) heart failure
Diltiazem CD C: 120 mg, 180 mg, 240 mg, 180–420 mg/day Dizziness, headache, bradycardia, heart block, worsening
(Cardizem CD) 300 mg heart failure, edema, constipation
Felodipine (Plendil) T: 2.5 mg, 5 mg, 10 mg 2.5–20 mg/day Headache, flushing, peripheral edema

Nifedipine XL T: 30 mg, 60 mg, 90 mg 90–120 mg/day Flushing, peripheral edema, headache, dizziness, nausea
(Adalat CC,
Procardia XL)
Verapamil SR T: 120 mg, 180 mg, 240 mg T (Immediate- Headache, gingival hyperplasia, constipation
(Calan SR) T (Sustained-Release): 120 mg, Release):
180 mg 80–320 mg/day
T (Sustained-Release):
120–480 mg/day
Diuretics
Chlorthalidone T: 25 mg, 50 mg 12.5–25 mg/day Same as hydrochlorothiazide
(Hygroton)
Hydrochlorothiazide T: 25 mg, 50 mg 12.5–50 mg/day Hypokalemia, hyperuricemia, hypomagnesemia, hyperglycemia
(Hydrodiuril)
Renin Inhibitor
Aliskiren (Tekturna) T: 150 mg, 300 mg PO: 150–300 mg/day Diarrhea, dyspepsia, headache, dizziness, fatigue, upper
respiratory tract infection
Vasodilators

Antihypertensives
Hydralazine T: 10 mg, 25 mg, 50 mg, 100 mg PO: 40–300 mg/day Anorexia, nausea, diarrhea, vomiting, headaches, palpitations
(Apresoline)
Minoxidil (Loniten) T: 2.5 mg, 10 mg PO: 10–40 mg/day Rapid/irregular heartbeat, hypertrichosis, peripheral edema
C, Capsules; P, patch; T, tablets.

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CLASSIFICATIONS