bisoprolol (Rx)

1-10%

Dizziness (10%)

Insomnia (8%-10%)

Bradyarrhythmia (9%)

Upper respiratory infection (5%)

Diarrhea (4%)

Rhinitis (4%)

Arthralgia (3%)

Cough (3%)

Dyspnea (2%)

Nausea (2%)

Pharyngitis (2%)

Sinusitis (2%)

Vomiting (2%)

<1%

Cold extremities

Hypotension

Depression

Dyspepsia

Bronchospasm

Frequency Not Defined

Aggravate CHF

Decrease HDL

Hypertriglyceridemia

Mask symptoms of hypoglycemia

Decreased exercise tolerance

Raynaud's phenomenon

May increase triglyceride levels and insulin resistance

Contraindications

Sinus bradycardia, 2°/3° heart block, cardiogenic shock, overt cardiac failure, hypersensitivity, sick sinus syndrome without permanent pacemaker

Cautions

Use caution in anesthesia/surgery (myocardial depression), bronchospastic disease, cerebrovascular insufficiency, CHF, cardiomegaly, DM, hyperthyroidism/thyrotoxicosis, myasthenia gravis, liver disease, renal impairment, peripheral vascular disease, use in pheochromocytoma, IDDM, history of psychiatric disease, pre-existing sick sinus syndrome or similar cardiac conditions

Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery; the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures

Exacerbation of psoriasis reported with use

Less effective than thiazide diuretics in black and geriatric patients

Shown to decrease mortality in hypertension and post-myocardial infarction

Pregnancy Category: C

Lactation: excretion in milk unknown; use caution

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.

Mechanism of Action

Blocks response to beta-adrenergic stimulation; cardioselective for beta-1 at low doses with little or no effect on beta-2 receptors at doses ≤ 20 mg

Pharmacikinetics

Half-Life: 9-12 hr (normal renal function); 27-36hr (<40 mL/min); 8-22 hr (hepatic cirrhosis)

Peak Plasma Time: 2-4 hr

Bioavailability: 80%

Onset of action: 1-2 hr

Metabolism: Hepatic

Protein Bound: 30%

Excretion: Renal (50%); feces (<2%)