Dosing and uses of Bystolic (nebivolol)
Adult dosage forms and strengths
tablet
- 2.5mg
- 5mg
- 10mg
Hypertension
5 mg/day PO; may be increased every 2 weeks; not to exceed 40 mg/day
Dosing Modifications
Renal impairment
- CrCl <30 mL/min: 2.5 mg/day PO initially; increased cautiously
Hepatic impairment
- 2.5 mg/day PO initially; increased cautiously
Pediatric dosage forms and strengths
<18 years: Safety and efficacy not established
Geriatric dosage forms and strengths
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
Bystolic (nebivolol) adverse (side) 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
Uncontrolled heart failure
Sick sinus syndrome (if no pacemaker)
2°/3° heart block (if no pacemaker)
History of bronchospasm and bronchial asthma
Chronic obstructive pulmonary disease (COPD)
Bradycardia (HR <50 beats/min)
Hypotension
Cautions
Anesthetics that cause myocardial depression, bradycardia, COPD, diabetes, 1° heart block, history of psoriasis, ischemic heart disease, peripheral circulatory disorders (Raynaud disease, intermittent claudication), Prinzmetal angina, untreated congestive heart failure (CHF)
May mask symptoms of thyrotoxicosis
Severe renal impairment decreases clearance
Moderate hepatic impairment decreases metabolism
Sudden discontinuance can exacerbate angina and lead to MI
Renal disease, cerebrovascular insufficiency, use in pheochromocytoma (alpha blocker should be started before beta blocker)
Increased risk of stroke after surgery
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)
Pregnancy and 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 of Bystolic (nebivolol)
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%)
