nebivolol

nebivolol

Bystolic

Pharmacologic class: Beta-adrenergic blocker

Therapeutic class: Antihypertensive

Pregnancy risk category C

Action

Not fully known. The following factors may be involved: decreased heart rate, reduced myocardial contractility, decreased tonic sympathetic outflow to periphery from cerebrovasomotor centers, suppressed renin activity, vasodilation, and decreased peripheral vascular resistance.

Availability

Tablets: 2.5 mg, 5 mg, 10 mg

Indications and dosages

➣ Hypertension

Adults: Individualized; 5 mg P.O. daily. If patient requires further blood pressure reduction, dosage may be increased at 2-week intervals up to 40 mg P.O. daily.

Dosage adjustment

• Moderate hepatic impairment or severe renal impairment (creatinine clearance less than 30 ml/minute)

Contraindications

• Hypersensitivity to drug or its components

• Severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless permanent pacemaker is in place)

• Severe hepatic impairment

Precautions

Use cautiously in:

• moderate hepatic impairment

• severe renal impairment

• congestive heart failure (CHF)

• peripheral vascular disease

• bronchospastic disease (use not recommended)

• diabetic patients receiving hypoglycemic drugs

• known or suspected pheochromocytoma

• concurrent use of myocardial depressants, AV conduction inhibitors (such as cardiac glycosides and certain calcium antagonists), or antiarrhythmics (such as disopyramide)

• perioperative use with anesthetics that depress myocardial function (such as ether, cyclopropane, or trichloroethylene)

• pregnant patients

• breastfeeding patients (use not recommended)

• children (safety and efficacy not established).

Administration

• Give with or without food.

• Be aware that drug may be used alone or in combination with other antihypertensives.

• Know that drug shouldn't be combined with other beta blockers. Closely monitor patients receiving catecholamine-depleting drugs (such as reserpine or guanethidine), because added beta blockade may decrease sympathetic activity excessively. In patients receiving nebivolol with clonidine, discontinue nebivolol for several days before gradually tapering clonidine.

Don't withdraw drug abruptly; taper over 1 to 2 weeks when possible. Drug may mask signs and symptoms of hyperthyroidism, such as tachycardia; abrupt withdrawal may exacerbate signs and symptoms of hyperthyroidism or may trigger thyroid storm.

Adverse reactions

CNS: headache, fatigue, dizziness, insomnia

CV: bradycardia

GI: nausea, diarrhea

Respiratory: dyspnea

Skin: rash

Other: chest pain, peripheral edema

Interactions

Drug-drug. Antiarrhythmics (such as disopyramide), myocardial depressants or AV conduction inhibitors (such as cardiac glycosides and certain calcium antagonists): increased risk of slowed AV conduction and bradycardia

Cimetidine: increased d-nebivolol (active isomer) blood level

CYP2D6 inhibitors (such as fluoxetine, paroxetine, propafenone, quinidine): increased d-nebivolol blood level

Other beta-adrenergic blockers: excessive reduction of sympathetic activity Sildenafil: decreased effect of sildenafil

Drug-diagnostic tests. Blood urea nitrogen, triglycerides, uric acid: increased levels

Cholesterol, high-density lipoproteins, platelet count: decreased

Patient monitoring

Be aware that beta blockade may further depress myocardial contractility and trigger more severe heart failure in patients with compensated CHF. If CHF worsens, consider discontinuing drug.

During perioperative use, closely monitor patients receiving anesthetics that depress myocardial function, such as ether, cyclopropane, or trichloroethylene. Also, know that if drug is withdrawn before major surgery, the heart's impaired ability to respond to reflex adrenergic stimuli may increase risks of general anesthesia and surgery.

• Because of significant negative inotropic and chronotropic effects in patients treated with verapamil- or diltiazem-type beta blockers or calcium channel blockers, use caution in patients treated concomitantly with these agents; monitor ECG and blood pressure.

Patient teaching

• Tell patient drug may be taken with or without food.

• Advise patient not to stop taking drug unless prescriber approves.

Instruct patient to immediately report difficulty breathing, increasing shortness of breath, excessively slow pulse, or weight gain.

• Caution patient to avoid driving and other hazardous activities until drug's effects on alertness are known.

• Advise breastfeeding patient not to breastfeed during therapy.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above.

nebivolol

(ne-bi-vi-lole) ,

Bystolic

(trade name)

Classification

Therapeutic: antihypertensives
Pharmacologic: beta blockers

Pregnancy Category: C

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 effects

Lowering of BP.

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)

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

Contraindications/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; Obstetric: 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 (↓ 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); Geriatric: Consider increased sensitivity, concurrent chronic diseases, medications and presence of age-related decrease in clearance; Obstetric: Use in pregnancy only if maternal benefit outweighs fetal risk; Pediatric: Safe use in children <18 yr not established.

Adverse Reactions/Side Effects

Central nervous system

• dizziness
• fatigue
• headache

Interactions

Drug-Drug interaction

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 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

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

Hepatic/Renal Impairment

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

Availability

Tablets: 2.5, 5 mg, 10 mg

Nursing implications

Nursing assessment

• Monitor BP, ECG, and pulse prior to and periodically during therapy.
• Monitor intake and output ratios and daily weights. Assess routinely for signs and symptoms of HF (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

• Oral: May be administered without regard to food.
  • When discontinuation is planned, observe patient carefully and advise to minimize physical activity. Taper over 1–2 wk 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 BP. Instruct them to check pulse 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. 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 HF (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 breast feeding should be avoided during nebivolol therapy.

Evaluation/Desired Outcomes

• Decrease in BP.