nebivolol

Contraindicated in:

Hypersensitivity;
Severe bradycardia, heart block greater than first-degree cardiogenic shock, decompensated HF, or sick sinus syndrome (without pacemaker);
Severe hepatic impairment;
Bronchospastic disease;
Lactation: Lactation.

Use Cautiously in:

Coronary artery disease (rapid cessation should be avoided);
Compensated HF;
Major surgery (anesthesia may augment myocardial depression);
Diabetes mellitus (may mask signs of hypoglycemia);
Thyrotoxicosis (may mask symptoms);
Moderate hepatic impairment;
Severe renal impairment (↓ initial dose if CCr <30 mL/min);
History of severe allergic reactions (↑ intensity of reactions);
Pheochromocytoma (alpha blockers required prior to beta blockers);
OB: Use during pregnancy only if potential maternal benefit outweighs potential fetal risk;
Pedi: Safety and effectiveness not established in children;
Geri: Consider ↑ sensitivity, concurrent chronic diseases, medications, and presence of age-related ↓ in clearance in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Endo: hypoglycemia

Neuro: dizziness, fatigue, headache

Interactions ⬆ ⬇

Drug-drug:

CYP2D6 inhibitors, including fluoxetine, cimetidine, quinidine, propafenone, and paroxetine, may ↑ levels and risk of toxicity.
Anesthetic agents, including ether, trichloroethylene, and cyclopropane, as well as other myocardial depressants or inhibitors of AV conduction, such as diltiazem verapamil, digoxin, clonidine, and ivabradine, may ↑ risk of myocardial depression and bradycardia.

Availability ⬆ ⬇

(Generic available)

Tablets: 2.5; 5 mg; 10 mg; 20 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 5 mg once daily initially; may increase at 2 wk intervals up to 40 mg/day.

Hepatic/Renal Impairment

PO (Adults ): 2.5 mg once daily initially; titrate upward cautiously.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Blocks stimulation of beta adrenergic receptor sites; selective for beta₁ (myocardial) receptors in most patients. In some patients (poor metabolizers), higher blood levels may result in some beta₂ (pulmonary, vascular, uterine) adrenergic blockade.

Therapeutic effects:

Lowering of BP.

Classifications ⬆ ⬇

Therapeutic Classification: antihypertensives

Pharmacologic Classification: beta blockers (selective)

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: 98%.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP2D6 isoenzyme; the CYP2D6 enzyme system exhibits genetic polymorphism; ∼7% of population may be poor metabolizers and may have significantly ↑ nebivolol concentrations and an ↑ risk of adverse effects.; minimal excretion of unchanged drug.

Half-Life: Extensive metabolizers: 12 hr; Poor metabolizers: 19 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	1.5–4 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take nebivolol as directed, at the same time each day, even if feeling well. If a dose is missed, skip missed dose and take next scheduled dose; do not double doses. Do not discontinue without consulting health care professional. Abrupt withdrawal may precipitate life-threatening arrhythmias, hypertension, or myocardial ischemia.
Advise patient to ensure that enough medication is available for weekends, holidays, and vacations. A written prescription may be kept in the wallet for emergencies.
Reinforce the need to continue additional therapies for hypertension (weight loss, sodium restriction, stress reduction, regular exercise, moderation of alcohol consumption, smoking cessation). Medication controls but does not cure hypertension.
Teach patient and family how to check HR and BP. Instruct them to check HR daily and BP biweekly and to report significant changes to health care professional.
Instruct patient to consult health care professional before taking any Rx, OTC, or herbal products, especially cold preparations, concurrently with this medication. Patients on antihypertensive therapy should also avoid excessive amounts of coffee, tea, and cola.
May mask some signs of hypoglycemia, especially tachycardia. Patients with diabetes should closely monitor blood sugar, especially if weakness, malaise, irritability, or fatigue occurs. Medication does not block dizziness or sweating as signs of hypoglycemia.
May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to notify health care professional if difficulty breathing or signs and symptoms of worsening HF (weight gain, ↑ shortness of breath, excessive bradycardia) occur.
Instruct patient to inform health care professional of medication regimen before treatment or surgery.
Advise patient to carry identification describing disease process and medication regimen at all times.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Monitor neonates of mothers who used nebivolol during the 3rd trimester for hypotension, bradycardia, hypoglycemia, and respiratory depression.

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Indications ⬇

Contraind./Precautions ⬆ ⬇