nebivolol

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.