Dosing & Uses
Dosage Forms & Strengths
tablet
- 20mg
- 40mg
- 80mg
Hypertension
40-320 mg PO qDay
Angina Pectoris
Initial 40 mg/day PO, increase gradually q 3-7Days
Doses up to 160-240mg qDay may be needed
SVT, Maintenance (Off-label)
60-160 mg/day PO
Aggressive Behavior; Upper GI Rebleed (Off-label)
40-160 mg/day PO
Migraine, Prophylaxis (Off-label)
40-80 mg PO qDay (up to 240 mg/day)
Renal Impairment
CrCl >50 mL/min: Give qDay
CrCl 31-50 mL/min: Give q24-36hr
CrCl 10-30 mL/min: Give q24-48hr
CrCl <10 mL/min: Give q40-60hr
Hepatic Impairment
Dose adjustments not necessary
Additional Information
Less effective than thiazide diuretics in black and geriatric patients
Shown to decrease mortality in hypertension and post-myocardial infarction
Other Indications & Uses
Off-label: Arrhythmias, GI bleed, hyperthyroidism, reduce IOP, SVT
Not approved
Hypertension
20-320 mg PO qDay
Angina Pectoris
Initial 20 mg/day PO, increase gradually q 3-7Days
Doses up to 160-240mg qDay may be needed
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Drowsiness
Insomnia
Decreased sexual ability
1-10%
Bradycardia (2%)
Dizziness (2%)
Fatigue (2%)
Hypotension (1%)
<1%
Abdominal discomfort
Constipation
Diarrhea
Nausea
Cough
Nasal congestion
Frequency Not Defined
Bronchospasm, depression, decreased exercise tolerance, Raynaud's phenomenon
May increase triglyceride levels and insulin resistance, and decrease HDL levels
Warnings
Black Box Warnings
May exacerbate ischemic heart disease following abrupt withdrawal
Hypersensitivity to catecholamines has been observed during withdrawal
Exacerbation of angina and, in some cases, myocardial infarction occurrence after abrupt discontinuation
When discontinuing chronically administered beta-blockers (particularly with ischemic heart disease) gradually reduce dose over 1-2 wk and carefully monitor
If angina markedly worsens or acute coronary insufficiency develops, reinstate beta-blocker administration promptly, at least temporarily (in addition to other measures appropriate for unstable angina)
Warn patients against interruption or discontinuation of beta-blocker without physician advice
Because coronary artery disease is common and may be unrecognized, slowly discontinue beta-blocker therapy, even in patients treated only for hypertension
Contraindications
Hypersensitivity
Overt cardiac failure, 2°/3° heart block, cardiogenic shock
Asthma/COPD
Avoid during breastfeeding
Sinus bradycardia
Sick sinus syndrome without permanent pacemaker
Cautions
Anesthesia/surgery (myocardial depression); chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery, however the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures
Nonallergenic bronchospasm, cerebrovascular insufficiency, well-compensated CHF, DM, hyperthyroidism/thyrotoxicosis, liver disease, renal impairment, peripheral vascular disease
Sudden discontinuation can exacerbate angina and lead to myocardial infarction
Increased risk of stroke after surgery
Use in pheochromocytoma
Pregnancy & Lactation
Pregnancy Category: C
Lactation: concentrated in breast milk, use caution (AAP Committee states compatible w/ nursing)
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Blocks response to beta-adrenergic stimulation to beta1 and beta2 receptors; may reduce portal pressure through beta2 receptor, which reduces portal blood flow
Pharmacokinetics
Half-Life: 10-24 hr
Onset: 3-4 hr
Duration: 17-24 hr
Vd: 1.9 L/kg (1.88-2.02 L/kg)
Peak Plasma Time: 2-4 hr
Bioavailability: 20-40%
Protein Bound: 28-30%
Metabolism: None
Excretion: Urine
Dialyzable: Yes (HD)
Images
Patient Handout
Formulary
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