Davis's Drug Guide

nebivolol

General

Pronunciation
ne-BI-vi-lole

Trade Name(s)

• Bystolic



Pregnancy Category
Category C

Ther. class.
antihypertensives

Pharm. class.
beta blockers
selective

Indications

Hypertension (alone and with other antihypertensives)

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 Effect(s):
Lowering of blood pressure

Pharmacokinetics

Absorption: Well absorbed following oral administration

Distribution: Unknown

Protein Binding: 98%

Metabolism and Excretion: Mostly metabolized by the liver, including the CYP2D6 enzyme system; some have antihypertensive action; minimal excretion of unchanged drug

Half-life: Extensive metabolizers—12 hr; poor metabolizers—19 hr

TIME/ACTION PROFILE (blood levels)

ROUTEONSETPEAKDURATION
POunknown1.5–4 hr24 hr

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity

• Severe bradycardia, heart block greater than first degree. cardiogenic shock, decompensated heart failure or sick sinus syndrome (without pacemaker)

• Severe hepatic impairment (Child-Pugh >B)

• Bronchospastic disease

OB: Lactation



Use Cautiously in:

• Coronary artery disease (rapid cessation should be avoided)

• Compensated congestive heart failure.

• Major surgery (anesthesia may augment myocardial depression)

• Diabetes mellitus (may mask signs of hypoglycemia)

• Thyrotoxicosis (may mask symptoms)

• Moderate hepatic impairment ( metabolism)

• 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)

Geri: Consider increased sensitivity, concurrent chronic diseases, medications and presence of age-related decrease in clearance

OB: Use in pregnancy only if maternal benefit outweighs fetal risk

Pedi: Safe use in children <18 yr not established

Adverse Reactions/Side Effects

CNS: dizziness, fatigue, headache.

*CAPITALS indicates life-threatening.
*italic indicates most frequent.

Interactions

Drug-Drug

• Drugs that affect the CYP2D6 enzyme system are expected to alter levels and possibly effects of nebivolol; dose alterations may be required.

Fluoxetine, a known inhibitor of CYP2D6, levels and effects; similar effects may be expected from quinidine, propafenone, and paroxetine

• Blood levels are also by cimetine

• Anesthetic agents including ether, trichloroethylene, and cyclopropane as well as other myocardial depressants or inhibitors of AV conduction such as diltiazem and verapamil may risk of myocardial depression and bradycardia

• Avoid concurrent use with beta blockers

• Concurrent use with reserpine or guanethidine may excessively reduce sympathetic activity

• If used concurrently with clonidine, nebivolol should be tapered and discontinued several days prior to gradual withdrawal of clonidine

Route/Dosage

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

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

Availability

Tablets: 2.5, 5 mg, 10 mg

Assessment

• Monitor blood pressure, ECG, and pulse prior to and periodically during therapy

• Monitor intake and output ratios and daily weights. Assess routinely for signs and symptoms of CHF (dyspnea, rales/crackles, weight gain, peripheral edema, jugular venous distention)



Lab Test Considerations

• May cause BUN, uric acid, triglycerides and HDL cholesterol and platelet court

Potential Nursing Diagnoses

• Decreased cardiac output (Side Effects)

Implementation

PO: May be administered without regard to food

» When discontinuation is planned, observe patient carefully and advise to minimize physical activity. Taper over 1–2 wks when possible. If angina worsens or acute coronary insufficiency develops, reinstitute nebivolol promptly, at least temporarily

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, and smoking cessation). Medication controls but does not cure hypertension

• Teach patient and family how to check pulse and blood pressure. Instruct them to check pulse daily and blood pressure 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. Diabetics 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 patients 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 CHF (weight gain, increasing shortness or 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

• Advise female patients that breastfeeding should be avoided during nebivolol therapy

Evaluation/Desired Outcomes

Decrease in blood pressure



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