Adrenergic Antagonists

Phentolamine: acts on alpha1

Route and Dosage: Subcut: 5–10 mg in 10 mL NS injected into extravasation area to prevent dermal necrosis

Uses and Considerations: Antidote for dopamine, dobutamine, phenylephrine, epinephrine, norepinephrine, and necrosis from extravasation. May cause pain at injection site. PB: UK; t½: 19 min

Doxazosin: alpha1

Route and Dosage: PO: Initially 1 mg/d at bedtime; max: 16 mg/d

Uses and Considerations: For hypertension and BPH. May cause dizziness, headache, asthenia, fatigue, edema, visual impairment, erectile dysfunction, and orthostatic hypotension. PB: 98%; t½: 22 h

Prazosin: alpha1

Route and Dosage: A: PO: Initially 1 mg bid/tid; maint: 6–15 mg/d in divided doses; max: 20 mg/d
Older A: PO: Initially 1 mg qd/bid; max: 20 mg/d

Uses and Considerations: For hypertension. May cause headache, dizziness, drowsiness, fatigue, weakness, orthostatic hypotension, peripheral edema, nausea, and palpitations. PB: 97%; t½: 2–4 h

Terazosin: alpha1

Route and Dosage: Hypertension:
A: PO capsules: Initially 1 mg at bedtime; maint: 1–5 mg/d; max: 20 mg/d

Uses and Considerations: For hypertension and BPH. May cause nasal congestion, dizziness, drowsiness, headache, peripheral edema, orthostatic hypotension, nausea, weakness, palpitations, and erectile dysfunction. PB: 90%–94%; t½: 12 h

Carvedilol: alpha1, beta1, beta2

Route and Dosage: Heart failure:
Regular release:
A: PO: 3.125 mg bid for 2 wk; max: 50 mg/bid
Extended release:
A: Initially 10 mg/d; max: 80 mg/d

Uses and Considerations: For hypertension and HF. May cause drowsiness, dizziness, orthostatic hypotension, bradycardia, weight gain, dyspnea, fatigue, headache, diarrhea, peripheral edema, hyperglycemia, diarrhea, erectile dysfunction, and weakness. PB: 98%; t½: 7–11 h

Labetalol: alpha1, beta1, beta2

Route and Dosage: Chronic hypertension:
A: PO: Initially 100 mg bid; dose may be increased q2–3d; maint: 200–400 mg bid; max: 2400 mg/d

Uses and Considerations: For acute/chronic hypertension. May cause orthostatic hypotension, nasal congestion, dizziness, fatigue, nausea, paresthesia, erectile/ejaculation dysfunction, hyperhidrosis, and depression. PB: 50%; t½: 6–8 h

Propranlol: beta1, beta2

Route and Dosage: Hypertension:
Immediate release:
A: PO: Initially: 40 mg bid; may increase q3–7d; maint: 160–480 mg/d in 2–3 divided doses; max: 640 mg/d
Extended release:
A: PO: Initially 80 mg/d, may increase q3–7d; maint: 120–160 mg/d; max: 640 mg/d

Uses and Considerations: For hypertension, angina, MI, HF, dysrhythmia, and migraine prophylaxis. May cause agitation, fatigue, dizziness, visual impairment, erectile dysfunction, bradycardia, hyperkalemia, and seizures. PB: 90%; t½: 2–6 h

Nadolol: beta1, beta2

Route and Dosage: A: PO: Initially 40 mg/d; maint: 40–80 mg/d; max: 320 mg/d for hypertension and 240 mg/d for angina

Uses and Considerations: For hypertension and angina. May cause dizziness, drowsiness, fatigue, bradycardia, hypotension, palpitations, and erectile dysfunction. PB: 30%; t½: 10–24 h

Pindolol: beta1, beta2

Route and Dosage: A: PO: Initially 5 mg bid; maint: 10–30 mg in 2–3 divided doses; max: 60 mg/d

Uses and Considerations: For hypertension. May cause bradycardia, hypotension, edema, fatigue, myalgia, dizziness, visual impairment, and dyspnea. PB: 40%–60%; t½: 3–4 h

Sotalol: beta1, beta2

Route and Dosage: Atrial flutter/fibrillation:
A: PO: 80 mg bid; may increase gradually; max: 320 mg/d

Uses and Considerations: For ventricular dysrhythmias, atrial flutter, and atrial fibrillation. May cause headache, dizziness, dyspnea, asthenia, bradycardia, palpitations, hypotension, HF, hyperhidrosis, nausea, vomiting, fatigue, and dysrhythmia exacerbation. PB: 0%; t½: 12 h

Timolol: beta1, beta2

Route and Dosage: Hypertension:
A: PO: Initially 10 mg bid; maint: 10–20 mg bid; max: 60 mg/d

Uses and Considerations: For hypertension and glaucoma treatment and for migraine prophylaxis. May cause blurred vision, conjunctivitis, ocular irritation, weakness, dizziness, nausea, bradycardia, dyspnea, HF, pulmonary edema, and dysrhythmias. PB: 10%; t½: 3–4 h

Selective Beta-adrenergic blockers

Metoprolol: beta1

Route and Dosage: Angina:
Regular release:
A: PO: Initially 25–50 mg bid; maint: 100–400 mg/d in 2 divided doses; max: 450 mg/d
Extended release:
A: PO: Initially 100 mg/d; maint: 100–400 mg/d; max: 400 mg/d

Uses and Considerations: For hypertension, angina, HF, and acute MI. May cause bradycardia, dizziness, drowsiness, fatigue, nightmares, diarrhea, depression, insomnia, palpitations, erectile dysfunction, hypotension, flushing, syncope, peripheral insufficiency/edema, HF, and dysrhythmias. PB: 10%–12%; t½: 3–7 h

Atenolol: beta1

Route and Dosage: Anaphylaxis:
A: IM/subcut: 0.3 mg EpiPen auto injector, may repeat in 5–20 min; max: 2 doses
IV: 0.1–0.25 mg of 0.1 mg/mL solution, may repeat q5–15min PRN; may follow with 1–4 mcg/min infusion

Uses: To treat nasal congestion, allergic reaction, anaphylaxis, asthma exacerbation, bronchospasm, angioedema, status asthmaticus, cardiac arrest, cardiac resuscitation

Considerations: Parkinsonism, closed-angle glaucoma, cerebrovascular disease, labor, hypertension, cardiac disease, hyperthyroidism, diabetes mellitus, renal dysfunction, hypovolemia, renal disease, breastfeeding, pregnancy

Acebutolol: beta1

Route and Dosage: Hypertension:
A: PO: Initially: 400 mg/d; maint: 400–800 mg/d; max: 1200 mg/d
Older adults: Initially 200 mg/d; max: 800 mg/d

Uses and Considerations: For hypertension and dysrhythmias. May cause bradycardia, hypotension, dizziness, fatigue, headache, nausea, diarrhea, constipation, visual impairment, edema, and dyspnea. PB: 26%; t½: 3–4 h

Betaxolol: beta1

Route and Dosage: Hypertension:
A: PO: Initially 10 mg/d; max: 20 mg/d
Older adult: Initially 5 mg/d; max: 20 mg/d

Uses and Considerations: For hypertension and glaucoma. May cause bradycardia, headache, dizziness, insomnia, fatigue, nausea, arthralgia, edema, and chest pain. PB: 50%; t½: 15 h

Bisoprolol: beta1

Route and Dosage: A: PO: Initially: 2.5–5 mg/d; max: 20 mg/d

Uses and Considerations: For hypertension. May cause dizziness, bradycardia, headache, fatigue, arthralgia, diarrhea, orthostatic hypotension, weakness, and peripheral edema. PB: 30%; t½: 9–12 h

Esmolol: beta1

Route and Dosage: Paroxysmal supraventricular tachycardia:
A: IV: LD: Initially 50 mcg/kg/min continuous infusion; max: 500 mcg/kg/min per dose or 300 mcg/kg/min continuous infusion

Uses and Considerations: For paroxysmal supraventricular tachydysrhythmia and hypertension. May cause hypotension, dizziness, drowsiness, bradycardia, diaphoresis, nausea, and injection site reaction. PB: 55%; t½: 9 min