| 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 -adrenergic receptor blocking agent. In extensive metabolizers (most of the population) and at doses less than or equal to 10 mg, nebivolol is preferentially 1 selective. In poor metabolizers and at higher doses, nebivolol inhibits both 1 – and 2 – adrenergic receptors. Nebivolol lacks intrinsic sympathomimetic and membrane stabilizing activity at therapeutically relevant concentrations. At clinically relevant doses, BYSTOLIC does not demonstrate 1-adrenergic receptor blockade activity. Various metabolites, including glucuronides, contribute to -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
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 -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
| 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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