Dosing and uses of Monocor, Zebeta (bisoprolol)
Adult dosage forms and strengths
tablet
- 5mg
- 10mg
Hypertension
2.5-20 mg PO qDay
Heart Failure
1.25 mg PO qDay; not to exceed 10 mg/day
Renal Impairment
<40 mL/minute: 2.5 mg/day initially; titrate slowly and monitor
Other 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: angina, SVT, PVC
Pediatric dosage forms and strengths
Safety & efficacy not established
Geriatric dosage forms and strengths
Hypertension
2.5-20 mg PO qDay
Heart Failure
1.25 mg PO qDay; not to exceed 10 mg/day
Monocor, Zebeta (bisoprolol) adverse (side) effects
1-10%
Dizziness (10%)
Dyssomnia (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
Warnings
Contraindications
Sinus bradycardia, 2°/3° heart block, cardiogenic shock, overt cardiac failure, hypersensitivity, sick sinus syndrome without permanent pacemaker
Cautions
Anesthesia/surgery (myocardial depression), bronchospastic disease, cerebrovascular insufficiency, CHF, cardiomegaly, DM, hyperthyroidism/thyrotoxicosis, liver disease, renal impairment, peripheral vascular disease, use in pheochromocytoma, IDDm
Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery; however, the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and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
Pregnancy and lactation
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.
Pharmacology of Monocor, Zebeta (bisoprolol)
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.
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: half renal, half non-renaL
