Dosing & Uses
Dosage Forms & Strengths
tablet
- 2.5mg
- 5mg
- 10mg
- 20mg
Hypertension
5 mg/day PO; may be increased every 2 weeks; not to exceed 40 mg/day
Dosing Modifications
Renal impairment
- CrCl >30-80 mL/min: Dose adjustment not listed by the manufacturer
- CrCl <30 mL/min: 2.5 mg/day PO initially; increased cautiously
Hepatic impairment
- Mild impairment (Child-Pugh A): Dose adjustment not listed by the manufacturer
- Moderate Impairment (Child-Pugh Class B): 2.5 mg PO once daily; increase cautiously if initial response inadequate
- Severe impairment (Child-Pugh Class C): Contraindicated
Safety and efficacy not established
Hypertension
5 mg/day PO; may be increased every 2 weeks; not to exceed 40 mg/day
Heart Failure
<70 years: Not established
>70 years: 1.25 mg/day PO; may be increased by 2.5 mg/day every 1 or 2 weeks; not to exceed 10 mg/day
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
1-10%
Headache (6-9%)
Fatigue (2-5%)
Dizziness (2-4%)
Diarrhea (2-3%)
Nausea (1-3%)
Increased triglyceride levels and insulin resistance, decreased high-density lipoprotein (HDL) levels (1%)
Insomnia (1%)
Peripheral edema (1%)
Weakness (1%)
<1%
Bradycardia
Chest pain
Dyspnea
Warnings
Contraindications
Hypersensitivity
Severe hepatic impairment
Cardiogenic shock
Sick sinus syndrome (if no pacemaker)
2°/3° heart block (if no pacemaker)
Bradycardia (HR <50 beats/min)
Decompensated heart failure
Severe hepatic impairment (Child-Pugh Class C)
Cautions
Anesthetics that cause myocardial depression, bradycardia, 1° heart block, ischemic heart disease, Prinzmetal angina, untreated congestive heart failure (CHF)
Patients with bronchospastic disease should not receive beta-blockers; patients with bronchospastic disease who do not respond to other therapies, initial low doses may be employed and used cautiously; monitor closely; patient should have immediate access to beta2-agonist
May mask hyperthyroidism, including tachycardia; abrupt withdrawal may exacerbate symptoms of hyperthyroidism or precipitate thyroid storm; if thyrotoxicosis suspected, carefully manage and treat
Severe renal impairment decreases clearance; adjust dose in severe renal failure
Moderate hepatic impairment decreases metabolism ; adjust dose in moderate hepatic impairment (Child-Pugh class B); contraindicated in severe hepatic impairment (Child-Pugh class C)
May potentiate hypoglycemia in patients with hypoglycemia and/or mask signs and symptoms
Sudden discontinuance can exacerbate angina and lead to MI; to discontinue therapy, taper gradually over 1-2 weeks to avoid acute tachycardia, ischemia, and/or hypertension; temporary but prompt resumption of beta-blocker therapy may be necessary if angina symptoms or acute coronary insufficiency symptoms worsen
Can precipitate or worsen symptoms of arterial insufficiency in patients with peripheral and Raynaud disease (intermittent claudication); use caution; monitor for progression of arterial obstruction
Renal disease, cerebrovascular insufficiency, use in pheochromocytoma (alpha blocker should be started before beta blocker)
Increased risk of stroke after surgery; routine withdrawal of chronic beta-blocker therapy not recommended prior to major surgery
Use with caution in patients with myasthenia gravis
Use with caution in patients taking calcium-channel blockers or cardiac glycosides or using inhaled anesthetics
Drug loses receptor selectivity in poor metabolizers and in high doses (blocks both beta1 and beta2)
Excerbation or induction of psoriasis associated with psoriasis; use caution
Not shown to reduce morbidity or mortality in heart failure population; bisoprolol, carvedilol, and extended release metoprolol only beta blockers proven to reduce mortality; use caution in patients with compensated heart failure and monitor for worsening of condition; temporarily discontinue or reduce dose if condition worsens; stabilize patients on heart failure regimen before initiating beta-blocker therapy; initiate therapy at very low doses; may require adjustment of other medications, including ACE inhibitors and/or diuretics
May cause or exacerbate CNS depression; use caution in patient with psychiatric disorder
Pregnancy & Lactation
Pregnancy category: C
Lactation: Not known whether drug is excreted into breast milk; use not recommended
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
Competitive and selective beta1-receptor antagonist; has little or no effect on beta2 receptors at doses <10 mg; possesses mild vasodilating properties; reduces systemic vascular resistance
Absorption
Bioavailability: Extensive metabolizers, 12%; poor metabolizers, 96%
Peak plasma time: 1.5-4 hr
Distribution
Protein bound: 98%
Vd: 8-12 L/kg
Metabolism
Metabolized by CYP2D6 via alicyclic and aromatic hydroxylation, N-dealkylation, glucuronidation
Elimination
Half-life: Extensive metabolizers, 10-12 hr; poor metabolizers, 19-32 hr
Excretion: Urine (38-67%), feces (13-44%)
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Patient Handout
Formulary
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