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Beta Blockers

atenolol (Tenormin ® ) betaxolol (Kerlone ®)
bisoprolol (Zebeta ®) carvedilol (Coreg ®, Coreg CR™)
esmolol (Brevibloc ®) labetalol (Normodyne ®)
metoprolol (Lopressor ®) nadolol (Corgard ®)
nebivolol -BYSTOLIC®  
pindolol (Visken ®) propranolol (Inderal ®)
sotalol (Betapace ®) timolol (Blocadren ®)
Please see package insert for additional information and possible updates. The authors make no claims of the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance upon this material. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER.    [  Read the disclaimer    |   <<Back     ]

atenolol (Tenormin ® ) top of page

Receptor(s) affected: ß1 Selective.

Dosing (Adults):  
Hypertension: Oral: 25-50 mg once daily, may increase to 100 mg/day. Doses >100 mg are unlikely to produce any further benefit.
I.V.: Dosages of 1.25 to 5 mg every 6-12 hours have been used in short-term management of patients unable to take oral tabs.

Angina: Oral: 50 mg once daily; may increase to 100 mg/day. Some patients may require 200 mg/day.

Post MI:  I.V.: Early treatment: 5 mg slow I.V. over 5 minutes; may repeat in 10 minutes. If both doses are tolerated, may start oral atenolol 50 mg every 12 hours or 100 mg/day for 6-9 days postmyocardial infarction. Oral: Follow I.V. dose with 100 mg/day or 50 mg twice daily for 6 to 9 days postmyocardial infarction.

 [Supplied: 25, 50, 100mg tablets. Injection: 10ml (0.5mg/ml) ]

betaxolol (Kerlone ®) top of page

Receptor(s) affected: ß1

Dosing (Adults):  
Management of hypertension:
Initially: 5-10 mg orally once daily. May increase dose to 20 mg/day after 7-14 days if desired response is not achieved. Initial dose in elderly: 5 mg/day.
Maximum
: 20 mg/day.

[Supplied: 10, 20mg tablet]

bisoprolol (Zebeta ®) top of page

Receptor(s) affected:: ß1
[Selective inhibitor of beta1-adrenergic receptors; competitively blocks beta1-receptors, with little or no effect on beta2-receptors at doses <10 mg]

Dosing (Adults)
Treatment of hypertension, alone or in combination with other agents:
Initially, 2.5 to 5 mg once daily, may be increased to 10 mg, and then up to 20 mg once daily, if necessary

Hypertension (JNC 7): 2.5-10 mg once daily

Elderly: Initial dose: 2.5 mg/day; may be increased by 2.5-5 mg/day; maximum recommended dose: 20 mg/day

Dosing adjustment in renal/hepatic impairment: Clcr<40 mL/minute: Initial: 2.5 mg/day; increase cautiously.

[Supplied: 5, 10 mg tablets]

carvedilol (Coreg ®,  Coreg CR™) top of page

Receptor(s) affected: ß1,ß2, alpha.   Admin: Administer with food. Extended release capsules should not be crushed or chewed. Capsules may be opened and sprinkled on applesauce for immediate use.

Dosing (Adults)
CHF
:: 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. (Prior to initiating therapy, other heart failure medications should be stabilized and fluid retention minimized.)
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.
Extended release: Initial: 10 mg once daily for 2 weeks; if the dose is tolerated, increase dose to 20 mg, 40 mg, and 80 mg over successive intervals of at least 2 weeks. Maintain on lower dose if higher dose is not tolerated.

Hypertension:: Immediate release: 6.25 mg twice daily; if tolerated, dose should be maintained for 1-2 weeks, then increased to 12.5 mg twice daily. Dosage may be increased to a maximum of 25 mg twice daily after 1-2 weeks. Maximum dose: 50 mg/day.  Extended release: Initial: 20 mg once daily, if tolerated, dose should be maintained for 1-2 weeks then increased to 40 mg once daily if necessary; maximum dose: 80 mg once daily.

Left ventricular dysfunction following MI:: Oral: Note: Should be initiated only after patient is hemodynamically stable and fluid retention has been minimized.   Immediate release: Initial 3.125 to 6.25 mg twice daily; increase dosage incrementally (ie, from 6.25-12.5 mg twice daily) at intervals of 3-10 days, based on tolerance, to a target dose of 25 mg twice daily.    Extended release: Initial: 20 mg once daily; increase dosage incrementally at intervals of 3-10 days. Target dose: 80 mg once daily.

Conversion from immediate release to extended release:
Current dose immediate release tablets 3.125 mg twice daily: Convert to extended release capsules 10 mg once daily.
Current dose immediate release tablets 6.25 mg twice daily: Convert to extended release capsules 20 mg once daily.
Current dose immediate release tablets 12.5 mg twice daily: Convert to extended release capsules 40 mg once daily.
Current dose immediate release tablets 25 mg twice daily: Convert to extended release capsules 80 mg once daily.

[Supplied: 3.125 mg, 6.25 mg, 12.5 mg, 25 mg tablets. Extended release capsule: 10 mg, 20 mg, 40 mg, 80 mg ]

esmolol (Brevibloc ®)  top of page

Receptor(s) affected: ß1

Dosing (Adults)
Intraoperative tachycardia and/or hypertension (immediate control): IV: Initial bolus: 80 mg (~1 mg/kg) over 30 seconds, followed by a 150 mcg/kg/minute infusion, if necessary. Adjust infusion rate as needed to maintain desired heart rate and/or blood pressure, up to 300 mcg/kg/minute. For control of postoperative hypertension, as many as one-third of patients may require higher doses (250-300 mcg/kg/minute) to control blood pressure; the safety of doses >300 mcg/kg/minute has not been studied.

Supraventricular tachycardia or gradual control of postoperative tachycardia/hypertension:: IV: Loading dose: 500 mcg/kg over 1 minute; follow with a 50 mcg/kg/minute infusion for 4 minutes; response to this initial infusion rate may be a rough indication of the responsiveness of the ventricular rate.      Infusion may be continued at 50 mcg/kg/minute or, if the response is inadequate, titrated upward in 50 mcg/kg/minute increments (increased no more frequently than every 4 minutes) to a maximum of 200 mcg/kg/minute. Note: To achieve more rapid response, following the initial loading dose and 50 mcg/kg/minute infusion, rebolus with a second 500 mcg/kg loading dose over 1 minute, and increase the maintenance infusion to 100 mcg/kg/minute for 4 minutes. If necessary, a third (and final) 500 mcg/kg loading dose may be administered, prior to increasing to an infusion rate of 150 mcg/minute. After 4 minutes of the 150 mcg/kg/minute infusion, the infusion rate may be increased to a maximum rate of 200 mcg/kg/minute (without a bolus dose).

Supraventricular tachycardias (SVT); usual dose range: Usual dosage range: 50-200 mcg/kg/minute with average dose of 100 mcg/kg/minute.
Onset of action: Beta-blockade: I.V.: 2-10 minutes (quickest when loading doses are administered)
PHARMACODYNAMICS / KINETICS
Duration of hemodynamic effects: 10-30 minutes; prolonged following higher cumulative doses, extended duration of use.

Half-life elimination: Adults: 9 minutes; elimination of metabolite decreases with end stage renal disease
Supplied:
Infusion [premixed in sodium chloride; preservative free] (Brevibloc®): 2000 mg (100 mL) [20 mg/mL; double strength]; 2500 mg (250 mL) [10 mg/mL]

Injection, solution, as hydrochloride: 10 mg/mL (10 mL) [premixed in sodium chloride]

Brevibloc®: 10 mg/mL (10 mL) [premixed in sodium chloride]; 20 mg/mL (5 mL) [double strength; premixed in sodium chloride]; 250 mg/mL (10 mL)

labetalol (Normodyne ®)  top of page

Receptor(s) affected: ß1,ß2, alpha

Dosing (Adults)
Oral: initial
: 100 mg orally twice a day. Usual: 200-400mg orally twice a day. Maximum: 2400 mg/day.
Hypertensive emergency: 20mg IV slow injection, then 40-80 mg IV every 10 minutes as needed. (up to 300 mg total dose) until desired BP is reached or start continuous infusion: 2 mg/min (range: 1 to 3 mg/min)--titrate to BP.

[Supplied: 100, 200, 300mg tablets; 5 mg/ml--20ml vial]

metoprolol (Lopressor ®)  top of page

Receptor(s) affected: ß1
Dosing (Adults)
Hypertension: Oral: 100-450 mg/day in 2-3 divided doses, begin with 50 mg twice daily and increase doses at weekly intervals to desired effect; usual dosage range (JNC 7): 50-100 mg/day
Extended release: Same daily dose administered as a single dose .

Angina, SVT, MI prophylaxis: Oral: 100-450 mg/day in 2-3 divided doses, begin with 50 mg twice daily and increase doses at weekly intervals to desired effect.  Extended release: Same daily dose administered as a single dose.

Hypertension/ventricular rate control: I.V. (in patients having nonfunctioning GI tract): Initial: 1.25-5 mg every 6-12 hours; titrate initial dose to response. Initially, low doses may be appropriate to establish response; however, up to 15 mg every 3-6 hours has been employed.

Congestive 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, up to 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 15 minutes after last I.V. dose and continue for 48 hours; then administer a maintenance dose of 100 mg twice daily.

Elderly: Oral: Initial: 25 mg/day; usual range: 25-300 mg/day.   Extended release: 25-50 mg/day initially as a single dose; increase at 1- to 2-week intervals.

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Administration:
Regular tablets should be taken with food. Extended release tablets may be taken without regard to meals.
When administered acutely for cardiac treatment, monitor ECG and blood pressure. May administer by rapid infusion (I.V. push) over 1 minute or by slow infusion (ie, 5-10 mg of metoprolol in 50 mL of fluid) over ~30 minutes.
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Supplied:
Injection, solution, as tartrate (Lopressor®): 1 mg/mL (5 mL)
Tablet, as tartrate 25 mg, 50 mg, 100 mg
Tablet, extended release, as succinate (Toprol-XL®): 25 mg, 50 mg, 100 mg, 200 mg.

nadolol (Corgard ®) top of page

Receptor(s) affected: ß1,ß2

Dosing (Adults)
(Hypertension / angina): Initially 20-40mg orally once daily. Maximum: 320mg/day.

 [Supplied: 20, 40, 80, 120, 160mg tablets]

nebivolol -BYSTOLIC® top of page

DESCRIPTION
The chemical name for the active ingredient in BYSTOLIC (nebivolol) tablets is (1RS,1'RS)-1,1'-[(2RS,2'SR)-bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-yl)]- 2,2'-iminodiethanol hydrochloride. Nebivolol is a racemate composed of d-Nebivolol and l-Nebivolol with the stereochemical designations of [SRRR]-nebivolol and [RSSS]-nebivolol, respectively.

INDICATIONS AND USAGE
BYSTOLIC is a beta-adrenergic blocking agent indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.

DOSAGE AND ADMINISTRATION
Hypertension
The dose of BYSTOLIC must be individualized to the needs of the patient. For most patients, the recommended starting dose is 5 mg once daily, with or without food, as monotherapy or in combination with other agents. For patients requiring further reduction in blood pressure, the dose can be increased at 2-week intervals up to 40 mg. A more frequent dosing regimen is unlikely to be beneficial.

Renal Impairment
In patients with severe renal impairment (ClCr less than 30 mL/min) the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed. BYSTOLIC has not been studied in patients receiving dialysis.

Hepatic Impairment
In patients with moderate hepatic impairment, the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed. BYSTOLIC has not been studied in patients with severe hepatic impairment and therefore it is not recommended in that population.

HOW SUPPLIED
Tablets: 2.5, 5, 10, 20 mg

pindolol (Visken ®)  top of page

Receptor(s) affected: ß1,ß2, ISA

Dosing (Adults)
Start
5 mg orally twice a day . Increase as necessary by 10 mg/day every 3-4 weeks.
Maximum of 60mg/day.

[Supplied: 5, 10mg tablet]

propranolol (Inderal ®) top of page

Receptor(s) affected: ß1,ß2

Dosing (Adults)
Initially 20-40 mg orally twice a day. Maximum 640 mg/day. Angina: 80-320 mg/day in 2 to 4 divided doses. Inderal LA: Start 80 mg orally once daily. IV : Life-threatening arrhythmia: usually 1- 3 mg (maximum rate: 1 mg/min)-may dilute in D5W-50ml. May repeat 1 mg dose q5 minutes to maximum of 5 mg total. Subsequent doses no sooner than 4 hours. May start IV infusion: usual rate: 2 to 3 mg/hr. Titrate to HR/BP.
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Angina: Oral: Adults: 80-320 mg/day in doses divided 2-4 times/day.   Long-acting formulation: Initial: 80 mg once daily; maximum dose: 320 mg once daily.

Essential tremor: Oral: Adults: 20-40 mg twice daily initially; maintenance doses: usually 120-320 mg/day.

Hypertension:  Initial: 40 mg twice daily; increase dosage every 3-7 days; usual dose: 320 mg divided in 2-3 doses/day; maximum daily dose: 640 mg; usual dosage range (JNC 7): 40-160 mg/day in 2 divided doses.      Long-acting formulation: Initial: 80 mg once daily; usual maintenance: 120-160 mg once daily; maximum daily dose: 640 mg; usual dosage range (JNC 7): 60-180 mg/day once daily

Hypertrophic subaortic stenosis: Oral: Adults: 20-40 mg 3-4 times/day.  Long-acting formulation: 80-160 mg once daily.

Migraine headache prophylaxis:    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; if satisfactory response not achieved within 6 weeks of starting therapy, drug should be withdrawn gradually over several weeks.    Long-acting formulation: Initial: 80 mg once daily; effective dose range: 160-240 mg once daily.

Myocardial infarction prophylaxis: Oral: Adults: 180-240 mg/day in 3-4 divided doses.

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

Tachyarrhythmias:
Oral: 10-30 mg/dose every 6-8 hours.    Elderly: Initial: 10 mg twice daily; increase dosage every 3-7 days; usual dosage range: 10-320 mg given in 2 divided doses.     IV:  Adults (in patients having nonfunctional GI tract): 1 mg/dose slow IVP; repeat every 5 minutes up to a total of 5 mg; titrate initial dose to desired response.

Thyrotoxicosis:   Oral:  Adults: Oral: 10-40 mg/dose every 6 hours.   I.V.: Adults: 1-3 mg/dose slow IVP as a single dose.

SUPPLIED:
Capsule, extended release, as hydrochloride (InnoPran XL™): 80 mg, 120 mg
Capsule, sustained release, as hydrochloride (Inderal® LA): 60 mg, 80 mg, 120 mg, 160 mg
Injection, solution, as hydrochloride (Inderal®): 1 mg/mL (1 mL)
Solution, oral, as hydrochloride: 4 mg/mL (5 mL, 500 mL); 8 mg/mL (500 mL)
Solution, oral concentrate, as hydrochloride (Propranolol Intensol™): 80 mg/mL (30 mL)
Tablet, as hydrochloride (Inderal®): 10 mg, 20 mg, 40 mg, 60 mg, 80 mg

sotalol (Betapace ®)  top of page

Receptor(s) affected: ß1,ß2

Dosing (Adults)
Sotalol should be initiated and doses increased in a hospital with facilities for cardiac rhythm monitoring and assessment. Proarrhythmic events can occur after initiation of therapy and with each upward dosage adjustment.

Ventricular arrhythmias (Betapace®, Sorine®):
Initial: 80 mg twice daily.    Dose may be increased gradually to 240-320 mg/day; allow 3 days between dosing increments in order to attain steady-state plasma concentrations and to allow monitoring of QT intervals.   Most patients respond to a total daily dose of 160-320 mg/day in 2-3 divided doses.
Some patients, with life-threatening refractory ventricular arrhythmias, may require doses as high as 480-640 mg/day; however, these doses should only be prescribed when the potential benefit outweighs the increased of adverse events.

Atrial fibrillation or atrial flutter (Betapace AF®): Initial: 80 mg twice daily.    If the initial dose does not reduce the frequency of relapses of atrial fibrillation/flutter and is tolerated without excessive QT prolongation (not >520 msec) after 3 days, the dose may be increased to 120 mg twice daily. This may be further increased to 160 mg twice daily if response is inadequate and QT prolongation is not excessive.

Elderly: Age does not significantly alter the pharmacokinetics of sotalol, but impaired renal function in elderly patients can increase the terminal half-life, resulting in increased drug accumulation

Dosage adjustment in renal impairment: Adults: Impaired renal function can increase the terminal half-life, resulting in increased drug accumulation. Sotalol (Betapace AF®) is contraindicated per the manufacturer for treatment of atrial fibrillation/flutter in patients with a Clcr<40 mL/minute.

Ventricular arrhythmias (Betapace®, Sorine®):
Clcr >60 mL/minute: Administer every 12 hours
Clcr 30-60 mL/minute: Administer every 24 hours
Clcr 10-30 mL/minute: Administer every 36-48 hours
Clcr<10 mL/minute: Individualize dose

Atrial fibrillation/flutter (Betapace AF®):
Clcr >60 mL/minute: Administer every 12 hours
Clcr 40-60 mL/minute: Administer every 24 hours
Clcr<40 mL/minute: Use is contraindicated

SUPPLIED:
Tablet, as hydrochloride: 80 mg, 80 mg [AF], 120 mg, 120 mg [AF], 160 mg, 160 mg [AF], 240 mg
Betapace® [light blue]: 80 mg, 120 mg, 160 mg, 240 mg
Betapace AF® [white]: 80 mg, 120 mg, 160 mg
Sorine® [white]: 80 mg, 120 mg, 160 mg, 240 mg

timolol (Blocadren ®)  top of page

Receptor(s) affected: ß1,ß2
Treatment of hypertension and angina, to reduce mortality following myocardial infarction, and for prophylaxis of migraine.

Dosing (Adults):  Start 10 mg orally twice a day.
Usual dosage: 20-40 mg/day. Maximum: 60 mg/day.

Hypertension: Initial: 10 mg twice daily, increase gradually every 7 days, usual dosage: 20-40 mg/day in 2 divided doses; maximum: 60 mg/day

Prevention of myocardial infarction: 10 mg twice daily initiated within 1-4 weeks after infarction

Migraine headache: Initial: 10 mg twice daily, increase to maximum of 30 mg/day

[Supplied: 5, 10, 20mg tablet]

Disclaimer

Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH does not directly or indirectly practice medicine or provide medical services and therefore assumes no liability whatsoever of any kind for the information and data accessed through the Service or for any diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph.  GlobalRPh Inc.
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