Beta-blockers is a topic covered in the Johns Hopkins Diabetes Guide.

To view the entire topic, please or purchase a subscription.

Johns Hopkins Guides provide diagnosis, management, and treatment guidance for infectious diseases, diabetes, and psychiatric conditions. Explore these free sample topics:

Johns Hopkins Guides

~~ The first section of this topic is shown below ~~

INDICATIONS

FDA

  • With or without diabetes, treatment of HTN alone or in conjunction with other antihypertensive agents
  • Management of angina pectoris
  • Secondary prevention of post-MI
  • Supraventricular arrhythmias
  • Pheochromocytoma
  • Essential tremor
  • Prophylaxis for migraine headaches
  • Symptomatic treatment of hypertrophic subaortic stenosis
  • Mild-to-severe heart failure of ischemic or cardiomyopathic origin (carvedilol and metoprolol only)
  • See table below for specific FDA indications for each beta-blocker.

Cardioselective Beta-blocker

FDA Indications

Usual adult dose for "other" indications

Dose adjustment with Renal or Hepatic insufficiency

Absorption, metabolism, excretion (t1/2)

Brand name/ Formulation/ Cost

Atenolol

Treatment of HTN alone or in conjunction with others; management of angina pectoris; secondary prevention of post-MI

Post-MI: Give after IV dose, with 100 mg/day or 50 mg BID for 6-9 days after MI

CLcr 15-35 mL/min: 50 mg/day max

CLcr < 15 mL/min: 50 mg every other day max

HD: dose after dialysis, or 25-50 mg additional dose.

Absorption: incomplete

Metabolism: limited hepatic

Excretion (t1/2): 50% feces, 40% urine. t1/2-- 6-9 hrs in normal renal function. Prolonged with renal impairment. 15-35 hrs in ESRD

Tenormin. Generic available

Generic: 25 mg (90 tablets): $14.99

Generic: 100 mg (90 tablets): $19.99

Bisoprolol

Treatment of HTN, alone or in combination with other agents

CLcr < 40 mL/min: 2.5 mg/day initially. Increase cautiously.
Not dialyzable

Absorption: rapid and almost complete

Metabolism: Extensively hepatic, 20% first pass effect.

Excretion (t1/2): 50%. t1/2-9-12 hrs in normal renal function. 27-36 hrs in Clcr < 40 mL/min. 8-22 hrs in hepatic cirrhosis.

Zebeta
Generic available

Generic: 5 mg (30 tabs): $35.99

Generic: 10 mg (30 tabs): $35.15

Metoprolol

Treatment of angina pectoris, HTN, or hemodynamically stable acute MI

Extended release: as above, in addition to reduction of mortality and hospitalization in patients with heart failure (HYHA Class II and III) already receiving ACE inhibitor, digoxin, and/or diuretics.

Angina: Oral:
Immediate release: Initial: 50 mg twice daily; usual dosage range: 50-200 mg twice daily; maximum: 400 mg/day; increase dose at weekly intervals to desired effect

Extended release: Initial: 100 mg/day (maximum: 400 mg/day)

Heart failure: Oral: Extended release: Initial: 25 mg once daily (reduce to 12.5 mg once daily in NYHA class higher than class II); may double dosage every 2 weeks as tolerated (maximum: 200 mg/day)

Myocardial infarction:
Acute: I.V.: 5 mg every 2 minutes for 3 doses in early treatment of myocardial infarction; thereafter, give 50 mg orally every 6 hours beginning 15 minutes after last I.V. dose and continue for 48 hours; then administer a maintenance dose of 100 mg twice daily.

May need to dose-adjust in hepatic insufficiency

Absorption: rapid and complete.

Metabolism: extensively hepatic via CYP2D6, 50% first pass effect.

Excretion (t/12): urine (< 5% to 10%). t1/2-3-8 hrs, dependant on rate of CYP2D6 metabolism

Toprol-XL , Lopressor. Generic available.

Immediate release:

Generic metoprolol tartrate:
25mg(30 tabs) $12.99

Generic metoprolol tartrate:
50mg(60 tabs) $12.99

Generic metoprolol succinate:
100mg (60 tabs) $15.99

Extended release:

Generic metoprolol succinate: 25mg (30 tabs): $34.99

Generic metoprolol succinate: 50mg (30 tabs): $33.88

Generic metoprolol succinate: 100mg (30 tabs): $41.99

Generic metoprolol sucinate: 200mg (90 tabs): $204.58

Non-cardioselective Beta-blocker

Nadolol

Treatment of HTN and angina pectoris; prophylaxis for migraine headaches.

Angina: Oral: Initial: 40-80 mg/day, increase dosage gradually by 40-80 mg increments at 3- to 7-day intervals until optimum clinical response is obtained with profound slowing of heart rate. Doses up to 160-240 mg/day

CLcr 31-40 mL/min: Give dose ever 24-36 hrs, or give 50% of usual dose.

Clcr 10-30 mL/min: Give ever 24-48 hrs, or give 50% of usual dose.

CLcr < 10 mL/min: Give every 40-60 hrs, or give 25% of usual dose.

HD: 20-50% dialyzable. Administer dose post-dialysis, or give 40 mg supplemental dose.

Hepatic impaired patient do not need adjustments.

Absorption: 30-40%

Metabolism: not metabolized

Excretion (t1/2): urine. t1/2-10-24 hrs in normal renal function. 45 hrs in ESRD.

Corgard
Generic available.

Generic 20mg (30 tabs): $13.99

Generic 40mg (30 tabs): $15.99

Generic 80mg (30 tabs): $19.99

Generic 160mg(30 tabs):
$33.59

Propranolol

Management of HTN; angina pectoris; pheochromocytoma; essential tremor; supraventricular arrhythmias (such as atrial fibrillation and flutter, AV nodal re-entrant tachycardias), ventricular tachycardias (catecholamine-induced arrhythmias, digoxin toxicity); prevention of MI; migraine headache prophylaxis; symptomatic treatment of hypertrophic subaortic stenosis (hypertrophic obstructive cardiomyopathy)

Hypertrophic subaortic stenosis: Oral: 20-40 mg 3-4 times/day
Inderal® LA: 80-160 mg once daily

Migraine headache prophylaxis: Oral: Initial: 80 mg/day divided every 6-8 hours; increase by 20-40 mg/dose every 3-4 weeks to a maximum of 160-240 mg/day given in divided doses every 6-8 hours

Pheochromocytoma: Oral: 30-60 mg/day in divided doses

Post-MI mortality reduction: Oral: 180-240 mg/day in 3-4 divided doses

Stable angina: Oral: 80-320 mg/day in doses divided 2-4 times/day
Inderal® LA: Initial: 80 mg once daily; maximum dose: 320 mg once daily

Tachyarrhythmias:
Oral: 10-30 mg/dose every 6-8 hours
I.V.: 1-3 mg/dose slow IVP; repeat every 2-5 minutes up to a total of 5 mg; titrate initial dose to desired response

Drug is not dialyzable, no need for additional dose post dialysis.

In chronic liver disease patients, there is noticeable decreased heart rate on normal dose; give low initial dose, and monitor heart rate regularly.

Absorption: rapid and complete.

Metabolism: hepatic via CYP2D6 and CYP1A2 to active and inactive compounds. Extensive first-pass effect.

Excretion (t1/2): urine.
t1/2-immediate release: 3-6hrs. Extended release: 8-10 hrs.

Inderal.
Generic available.

Immediate release:

Generic
10 mg (100 tabs): $12.99

Generic
20 mg (100 tabs): $13.99

Generic
40 mg (30 tabs): $12.99

Generic
60 mg (60 tabs): $55.99

Generic
80 mg (90 tabs): $15.99

Extended release:

Generic
60 mg (100 caps):
$115.97

Generic
80 mg (100 caps): $134.99

Generic
120 mg (30 caps): $59.99

Generic
160 mg (100 caps): $219.99

Timolol

Oral: Treatment of HTN and angina; to reduce mortality following MI; prophylaxis of migraine

Prevention of MI: Oral: 10 mg twice daily initiated within 1-4 weeks after infarction.

Migraine prophylaxis: Oral: Initial: 10 mg twice daily, increase to maximum of 30 mg/day.

CLcr < 10 mL/min: adjust dose based on clinical response, and monitor blood pressure; significant hypotensive responses have occurred in dialysis patients after receiving 20 mg by mouth of daily maintenance dose.

Dose reduction (up to 50 %) may be needed in patients with hepatic impairment.

Absorption: rapid and complete.

Metabolism: extensively hepatic; extensive first pass effect.

Excretion (t1/2): urine. t1/2-2-2.7 hrs. Longer in those with renail impairment.

Generic available

Generic
5 mg (60 tabs): $22.99

Generic
10 mg (60 tabs): $25.99

Generic
20 mg (60 tabs): $41.99

Mixed alpha and beta-blocker

Labetalol

Treatment of mild-to-severe HTN

HTN: Initial: 100 mg twice daily, may increase as needed every 2-3 days. Usual dose range (JNC 7): 200-800 mg/day in 2 divided doses

Not removed by dialysis; no need for additional dose post-dialysis.

Dosage reduction may be necessary in hepatically impaired patients.

Absorption: complete.
Metabolism: hepatic via glucoronide conjugation. Extensive first pass effect.
Excretion (t1/2): urine. t1/2-6-8 hrs.

Trandate
Generic available.

Generic
100 mg (60 tabs): $20.99

Generic
200 mg (60 tabs): $28.99

Generic
300 mg (60 tabs): $38.99

Carvedilol

Mild-to-severe heart failure of ischemic or cardiomyopathic origin (usually in addition to standard therapy); left ventricular dysfunction following MI (clinically stable with LVEF < 40%); management of HTN

Heart failure: Oral:
Immediate release: 3.125 mg twice daily for 2 weeks; if this dose is tolerated, may increase to 6.25 mg twice daily. Double the dose every 2 weeks to the highest dose tolerated by patient.

Maximum recommended dose:
Mild-to-moderate heart failure:
< 85 kg: 25 mg twice daily
>85 kg: 50 mg twice daily
Severe heart failure: 25 mg twice daily

No need to adjust dose in renal impairment.

Use is contra-indicated in patients with severe hepatic impairment.

Absorption: rapid and extensive.

Metabolism: Extensively hepatic, via CYP2C9, 2D6, 3A4, and 2C19; three active metabolites; first-pass effect; plasma levels in with cirrhotic liver disease are 4-7 times higher, respectively

Excretion (t1/2): primarily feces. t1/2-7-10 hrs.

Coreg
Immediate release formulation has generic availability.

Extended release is still brand name only.

Immediate release:

Generic
3.125 mg (30tabs): $25.99

Generic
6.25 mg (30 tabs): $14.99

Generic
12.5 mg (30 tabs): $14.99

Generic
25 mg (30 tabs): $16.00

Extended release:

10 mg (30 caps): $135.28

20 mg (30 caps): $135.28

40 mg (30 caps): $135.28

80 mg (30 caps): $135.28

**Patient Assistant Programs:

http://www.patientassistance.com…

https://s3.amazonaws.com…


https://www.rxhope.com…

http://www.patientassistance.com…

https://www.rxhope.com…


** Information gathered by Heather Tran and Gladimir Elysee

~~ To view the remaining sections of this topic, please
or purchase a subscription ~~

Last updated: September 26, 2013