BYSTOLIC® (nebivolol) tablets
| HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use BYSTOLIC safely and effectively. See full prescribing information for BYSTOLIC.
BYSTOLIC® (nebivolol) tablets, for oral use
Initial U.S. Approval: 2007
| CLINICAL PHARMACOLOGY
Nebivolol is a β-adrenergic receptor blocking agent. In extensive metabolizers (most of the population) and at doses less than or equal to 10 mg, nebivolol is preferentially β1 selective. In poor metabolizers and at higher doses, nebivolol inhibits both β1 - and β2 - adrenergic receptors. Nebivolol lacks intrinsic sympathomimetic and membrane stabilizing activity at therapeutically relevant concentrations. At clinically relevant doses, BYSTOLIC does not demonstrate α1-adrenergic receptor blockade activity. Various metabolites, including glucuronides, contribute to β-blocking activity.
Mechanism of Action
Plasma levels of d–nebivolol increase in proportion to dose in EMs and PMs for doses up to 20mg. Exposure to l-nebivolol is higher than to d-nebivolol but l-nebivolol contributes little to the drug's activity as d-nebivolol's beta receptor affinity is > 1000-fold higher than l-nebivolol. For the same dose, PMs attain a 5-fold higher Cmax and 10-fold higher AUC of d-nebivolol than do EMs. d-Nebivolol accumulates about 1.5-fold with repeated once-daily dosing in EMs.
Mean peak plasma nebivolol concentrations occur approximately 1.5 to 4 hours post-dosing in EMs and PMs.
Food does not alter the pharmacokinetics of nebivolol. Under fed conditions, nebivolol glucuronides are slightly reduced. BYSTOLIC may be administered without regard to meals.
Indications and usage
| 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.
|WARNINGS AND PRECAUTIONS
--Acute exacerbation of coronary artery disease upon cessation of therapy: Do not abruptly discontinue
--Diabetes: Monitor glucose as β-blockers may mask symptoms of hypoglycemia
| ADVERSE REACTIONS
Most common adverse reactions:
To report SUSPECTED ADVERSE REACTIONS, Contact Forest Laboratories, Inc. at 1-800-678-1605 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Dosage and administration
| DOSAGE AND ADMINISTRATION
| Package Insert data:
Rev. June 2011
Licensed from Mylan Laboratories, Inc.
Under license from Janssen Pharmaceutica N.V., Beerse, Belgium
Actidose-Aqua® is a registered trademark of Paddock Laboratories, Inc.
© 2010 Forest Laboratories, Inc.
FOREST PHARMACEUTICALS, INC.
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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