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Beta-blockers

Emily Pherson, Pharm.D., Paul A. Pham, Pharm.D. BCPS
Beta-blockers is a topic covered in the Johns Hopkins Diabetes Guide.

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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 obstructive cardiomyopathy
  • Mild-to-severe heart failure of ischemic or cardiomyopathic origin (carvedilol and metoprolol only)
  • See Table Table 1. for specific FDA indications for each beta-blocker
Table 1.

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; 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 (100 tablets): $81.76

Generic: 50 mg (1000 tablets): $792.49

Generic: 100 mg (100 tablets): $125.15

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.

Generic only

Generic: 5 mg (30 tabs): $36.59

Generic: 10 mg (30 tabs): $36.59

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, dependent on rate of CYP2D6 metabolism

Toprol-XL , Lopressor. Generic available.

Immediate release:

Generic metoprolol tartrate:
25 mg (100 tabs) $24.25

Generic metoprolol tartrate 37.5 mg (100 tablets): $55.50


Generic metoprolol tartrate:
50 mg (100 tabs) $55.50

Generic metoprolol tartrate:
75 mg (100 tabs) $243.63

Generic metoprolol tartrate:
100 mg (100 tabs) $80.10



Extended release:

Generic metoprolol succinate: 25mg (100 tabs): $105.38

Generic metoprolol succinate: 50mg (100 tabs): $105.38

Generic metoprolol succinate: 100mg (100 tabs): $158.35

Generic metoprolol sucinate: 200mg (100 tabs): $251.95

Nebivolol

Management of hypertension

CrCL 30 - 80 mL/minute: no dosage adjustment provided.

CrCl < 30 mL/minute: 2.5 mg once daily initially, can increase cautiously, if needed.

HD: no dosage adjustment provided due to no data available in this population.

Moderate hepatic impairment: initial dose of 2.5 mg daily, increase cautiously, if needed

Severe impairment: use is contraindicated

Absorption: rapid

Metabolism: hepatic via glucuronidation and CYP2D6

Excretion (t 1/2): urine; t 1/2 12 hours (extensive metabolizers), 19 hours (poor metabolizers)

Bystolic (brand only)

2.5 mg (30 tablets): $156.97

5 mg (30 tablets): $156.97

10 mg (30 tablets): $156.97

20 mg (30 tablets): $156.97

Non-cardioselective Beta-blocker

Nadolol

Treatment of HTN and angina pectoris.

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 (100 tabs): $339.39

Generic 40mg (100 tabs): $396.90

Generic 80mg (100 tabs): $537.85


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 obstructive cardiomyopathy, treatment of proliferating infantile hemangioma requiring systemic therapy

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 and Inderal XL.
Generic available.

Immediate release:

Generic
10 mg (100 tabs): $40.76

Generic
20 mg (100 tabs): $50.95

Generic
40 mg (100 tabs): $71.59

Generic
60 mg (100 tabs): $174.22

Generic
80 mg (100 tabs): $89.67

Extended release:

Generic
60 mg (100 caps):
$204.13

Generic
80 mg (100 caps): $238.47

Generic
120 mg (30 caps): $298.22

Generic
160 mg (100 caps): $388.36

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 only.

Generic
5 mg (100 tabs): $137.66

Generic
10 mg (100 tabs): $170.30

Generic
20 mg (100 tabs): $314.20

Mixed Alpha and Beta-blocker

Labetalol

Treatment of 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.

Generic only.

Generic
100 mg (100 tabs): $56.63

Generic
200 mg (100 tabs): $92.79

Generic
300 mg (100 tabs): $105.79

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 and Coreg CR. Generic available.

Immediate release:

Generic
3.125 mg (100 tabs): $213.40

Generic
6.25 mg (100 tabs): $213.40

Generic
12.5 mg (100 tabs): $213.40

Generic
25 mg (100 tabs): $213.40

Extended release:

Generic 10 mg (30 caps): $297.28

Generic 20 mg (30 caps): $297.28

Generic 40 mg (30 caps): $297.28

Generic 80 mg (30 caps): $297.28

Patient Assistant Programs available via: https://www.needymeds.org/.

*Prices represent cost per unit specified, are representative of "Average Wholesale Price" (AWP).

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Last updated: February 3, 2019

Citation

Pherson, Emily, and Paul A Pham. "Beta-blockers." Johns Hopkins Diabetes Guide, 2019. Johns Hopkins Guide, www.hopkinsguides.com/hopkins/view/Johns_Hopkins_Diabetes_Guide/547016/all/Beta_blockers.
Pherson E, Pham PA. Beta-blockers. Johns Hopkins Diabetes Guide. 2019. https://www.hopkinsguides.com/hopkins/view/Johns_Hopkins_Diabetes_Guide/547016/all/Beta_blockers. Accessed March 19, 2019.
Pherson, E., & Pham, P. A. (2019). Beta-blockers. In Johns Hopkins Diabetes Guide. Available from https://www.hopkinsguides.com/hopkins/view/Johns_Hopkins_Diabetes_Guide/547016/all/Beta_blockers
Pherson E, Pham PA. Beta-blockers [Internet]. In: Johns Hopkins Diabetes Guide. ; 2019. [cited 2019 March 19]. Available from: https://www.hopkinsguides.com/hopkins/view/Johns_Hopkins_Diabetes_Guide/547016/all/Beta_blockers.
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TY - ELEC T1 - Beta-blockers ID - 547016 A1 - Pherson,Emily,Pharm.D. AU - Pham,Paul,Pharm.D. BCPS Y1 - 2019/02/03/ BT - Johns Hopkins Diabetes Guide UR - https://www.hopkinsguides.com/hopkins/view/Johns_Hopkins_Diabetes_Guide/547016/all/Beta_blockers DB - Johns Hopkins Guide DP - Unbound Medicine ER -