Table 11-7

Table 11-7. Antihypertensive drugs: β-adrenergic blocking agents.

						Special Properties
Drug	Proprietary Name	Initial Dosage	Dosage Range	Cost per Unit	Cost of 30 Days Treatment (Based on Average Dosage)¹	β₁ 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 β₁ and β₂ 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 β₁ and β₂ effects.
Betaxolol	Kerlone	10 mg once daily	10-40 mg once daily	$1.10/10 mg	$33.00	+	0	0	+	H > R
Bisoprololand 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 daily	2.5-10 mg once daily	$1.37/5 mg	$41.10	0	+	0	+	R > H
Carvedilol	Coreg	6.25 mg	12.5-100 mg in 2 doses	$1.83/25 mg	$109.80 (25 mg twice a day)	0	0	0	+++	H > R	α:β-Blocking activity 1:9; may cause orthostatic symptoms; effective for congestive heart failure.
Labetalol	Normodyne, Trandate	100 mg twice daily	200-1200 mg in 2 doses	$0.71/200 mg	$42.60	0	0/+	0	++	H	α:β-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 β₁ and β₂ effects.
Toprol XL (SR preparation)	50 mg once daily	50-200 mg once daily	$1.36/100 mg	$40.80
Nadolol	Corgard	20 mg once daily	20-160 mg once daily	$1.05/40 mg	$31.50	+++	0	0	0	R
Penbutolol	Levatol	20 mg once daily	20-80 mg once daily	$1.87/20 mg	$56.10	0	+	0	++	R > H
Pindolol	Visken	5 mg twice daily	10-60 mg in 2 doses	$0.70/5 mg	$42.00	0	++	+	+	H > R	In adults, 35% renal clearance.
Propranolol	Inderal	20 mg twice daily	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 twice daily	10-40 mg in 2 doses	$0.38/10 mg	$ 22.80	0	0	0	++	H > R	Also indicated for post-MI. 80% hepatic clearance.

¹Average wholesale price (AWP, for AB-rated generic when available) for quantity listed. Source: Red Book Update, Vol. 25, No. 1, January 2006. AWP may not accurately represent the actual pharmacy cost because wide contractual variations exist among institutions.

²Agents with β₁ 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 β-adrenergic blockade. The clinical importance of MSA by β-blockers has not been defined.

⁵Adverse effects of all β-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.

ISA = intrinsic sympathomimetic activity; MSA = membrane-stabilizing activity; ANA = antinuclear antibody; LE = lupus erythematosus; MI = myocardial infarction; SR = sustained release; 0 = no effect; +, ++, +++ = some, moderate, most effect.