TABLE 11-6 - Antihypertensive drugs: Beta-adrenergic blocking agents

Drug	Proprietary Name	Initial Dosage	Dosage Range	Cost per Unit	Cost for 30 Days' Treatment (Based on Average Dosage)1	ß1 Selectivity2	ISA3	MSA4	Lipid Solubility	Renal vs Hepatic Elimination	Comments5
Acebutolol	Sectral	200 mg once daily	200-1200 mg in 1 or 2 doses	$1.34/400 mg	$40.20	+	+	+	+	H > R	Positive ANA; rare LE syndrome; also indicated for arrhythmias. Doses > 800 mg have ß1 and ß2 effects.
Atenolol	Tenormin	25 mg once daily	25-200 mg once daily	$0.83/50 mg	$24.90	+	0	0	0	R	Also indicated for angina pectoris and post-MI. Doses > 100 mg have ß1 and ß2 effects.
Betaxolol	Kerlone	10 mg once daily	10-40 mg once daily	$0.88/10 mg	$26.40	+	0	0	+	H > R
Bisoprolol and hydrochlorothiazide	Ziac	5 mg/6.25 mg	2.5-10 mg plus 6.25 mg	$1.14/2.5/6.25 mg	$34.20	+	0	0	0	R = H	Low-dose combination approved for initial therapy. Bisoprolol also effective for heart failure.
Carteolol	Cartrol	2.5 mg once	2.5-10 mg daily	$1.32/5 mg once daily	$39.60	0	+	0	+	R > H
Carvedilol	Coreg	6.25 mg	12.5-100 mg in 2 doses	$1.73/25 mg	$103.80 (25 mg bid)	0	0	0	+++	H > R	a:ß blocking activity 1:9; may cause orthostatic symptoms; effective for congestive heart failure.
Labetalol	Normodyne, Trandate	100 mg bid	200-1200 mg in 2 doses	$0.68/200 mg	$40.80	0	0/+	0	++	H	a:ß blocking activity 1:3; more orthostatic hypotension, fever, hepatotoxicity.
Metoprolol	Lopressor	50 mg in 1 or 2 doses	50-200 mg in 1 or 2 doses	$0.55/50 mg	$33.00	+	0	+	+++	H	Also indicated for angina pectoris and post-MI. Approved for heart failure. Doses > 100 mg have ß 1 and ß 2 effects.
	Toprol XL (SR preparation)	50 mg once daily	50-200 mg once daily	$1.14/100 mg	$34.20
Nadolol	Corgard	20 mg once daily	20-160 mg once daily	$1.04/40 mg	$31.20	0	0	0	0	R
Penbutolol	Levatol	20 mg once daily	20-80 mg once daily	$1.54/20 mg	$46.20	0	+	0	++	R > H
Pindolol	Visken	5 mg bid	10-60 mg in 2 doses	$0.69/5 mg	$41.40	0	++	+	+	H > R	In adults, 35% renal clearance.
Propranolol	Inderal	20 mg bid	40-320 mg in 2 doses	$0.51/40 mg	$30.60	0	0	++	+++	H	Once-daily SR preparation also available. Also indicated for angina pectoris and post-MI.
Timolol	Blocadren	5 mg bid	10-40 mg in 2 doses	$0.38/10 mg	$22.80	0	0	0	++	H > R	Also indicated post-MI. 80% hepatic clearance.

ISA = intrinsic sympathomimetic activity; MSA = membrane-stabilizing activity; 0 = no effect; +, ++, +++ = some, moderate, most effect.
¹Cost to pharmacist (average wholesale price, generic when possible) for quantity listed. Source: Drug Topics Red Book, May 2003; Vol. 22, No. 5.
²Agents with ß1 selectivity are less likely to precipitate bronchospasm and decreased peripheral blood flow in low doses, but selectivity is only relative.
³Agents with ISA cause less resting bradycardia and lipid changes.
⁴MSA generally occurs at concentrations greater than those necessary for beta-adrenergic blockade. The clinical importance of MSA by beta-blockers has not been defined.
⁵Adverse effects of all beta-blockers: bronchospasm, fatigue, sleep disturbance and nightmares, bradycardia and atrioventricular block, worsening of congestive heart failure, cold extremities, gastrointestinal disturbances, impotence, ?triglycerides, ?HDL cholesterol, rare blood dyscrasias.