Nebivolol

Trade Names:
Bystolic
- Tablets 2.5 mg
- Tablets 5 mg
- Tablets 10 mg
- Tablets 20 mg

Pharmacology

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Blocks beta receptors, which may decrease heart rate and myocardial contractility, diminish tonic sympathetic outflow to the periphery from cerebral vasomotor centers, suppress renin activity, and decrease peripheral vascular resistance. Lacks intrisic sympathomimetic activity at therapeutically relevant doses.

Pharmacokinetics

Absorption

Mean C _max is approximately 1.5 to 4 h postdosing.

Distribution

Protein binding is 98%, primarily to albumin.

Metabolism

Predominantly metabolized via direct glucuronidation and to a lesser extent via N-dealkylation and oxidation by CYP2D6. Stereospecific metabolites contribute to the pharmacologic activity.

Elimination

In extensive metabolizers, elimination is 38% in urine and 44% in feces, while, in poor metabolizers, elimination is 67% in urine and 13% in feces.

Special Populations

C _max increases 3-fold, AUC increases 10-fold, and apparent Cl decreases 86% in patients with moderate hepatic function impairment.

Indications and Usage

Treatment of hypertension.

Contraindications

Severe bradycardia, heart block more than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless a permanent pacemaker is in place), severe hepatic function impairment, hypersensitivity to any component of the product.

Dosage and Administration

PO Recommended starting dose is 5 mg/day. The dose can be increased at 2-week intervals up to 40 mg/day.

PO Start with 2.5 mg/day and cautiously titrate dose upward if needed. Studies have not been conducted in patients receiving dialysis.

PO Start with 2.5 mg/day and cautiously titrate dose upward if needed. Studies have not been conducted in patients with severe hepatic function impairment.

General Advice

• May be given with or without food.
• May be given with other antihypertensive medications.

Storage/Stability

Store at 68° to 77°F. Protect form light.

Drug Interactions

Risk of bradycardia may be increased.

Nebivolol plasma concentrations may be increased.

In patients receiving clonidine and nebivolol concurrently, discontinue nebivolol several days before gradually tapering clonidine dose.

Excessive sympathetic activity may occur.

Nebivolol plasma concentrations may be elevated, increasing pharmacologic effects and adverse reactions.

Sildenafil and nebivolol plasma concentrations may be reduced slightly with coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Bradycardia, chest pain (1%); MI, peripheral ischemia/claudication, second- and third-degree AV block, syncope (postmarketing).

CNS

Headache (9%); fatigue (5%); dizziness (4%); asthenia, paresthesia (at least 1%); insomnia (1%); somnolence, vertigo (postmarketing).

Dermatologic

Rash (1%); pruritus, psoriasis (postmarketing).

GI

Diarrhea, nausea (3%); abdominal pain (at least 1%); vomiting (postmarketing).

Genitourinary

Acute renal failure, erectile dysfunction (postmarketing).

Hematologic-Lymphatic

Thrombocytopenia (postmarketing).

Hepatic

Abnormal hepatic function, including increased ALT, AST, and bilirubin (postmarketing).

Lab Tests

Decreased HDL cholesterol and platelet count, increased BUN, triglycerides, and uric acids (at least 1%).

Metabolic-Nutritional

Hypercholesterolemia, hyperuricemia (at least 1%).

Respiratory

Dyspnea (1%); acute pulmonary edema, bronchospasm (postmarketing).

Miscellaneous

Peripheral edema (1%); hypersensitivity (including urticaria, allergic vasculitis, and angioedema), Raynaud phenomenon (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

No overall difference in efficacy or adverse reactions between older and younger patients.

Renal Function

Use with caution and adjust dose in severe renal function impairment.

Hepatic Function

Use with caution and reduce dose in patients with moderate hepatic function impairment.

Abrupt discontinuation

Ventricular arrhythmias and MI have occurred in patients with coronary artery disease following abrupt discontinuation of therapy.

Anaphylactic reactions

Patients receiving beta-blockers and who have a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge. Such patients may be unresponsive to the usual dose of epinephrine used to treat allergic reactions.

Anesthesia and surgery

If nebivolol use is continued perioperatively, closely monitor when anesthetic agents that depress myocardial function (eg, ether) are used.

Bronchospastic disease

Avoid use.

Cardiac failure

Severe cardiac failure may be precipitated because of depression of myocardial contractility.

Diabetes and hypoglycemia

Use with caution because beta-blockers may mask symptoms of hypoglycemia (eg, tachycardia) and nonselective beta-blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels.

Peripheral vascular disease

Use with caution in patients with peripheral vascular disease because symptoms of arterial insufficiency may be precipitated.

Thyrotoxicosis

May mask signs of hyperthyroidism (eg, tachycardia); abrupt withdrawal may exacerbate symptoms of hyperthyroidism or potentiate thyroid storm.

Overdosage

Symptoms

Bradycardia, bronchospasm, cardiac failure, dizziness, fatigue, heart block, hypoglycemia, hypotension, vomiting.

Patient Information

• Advise patients that this medicine may be taken with or without food.
• Advise patients that if a dose is missed, to take the next scheduled dose only and not to double the dose
• Advise patients not to operate automobiles, use machinery, or engage in tasks requiring alertness until they know how they react to this medicine.
• Instruct patients to consult health care provider if they experience difficulty in breathing, develop signs or symptoms of worsening of CHF such as weight gain or increasing shortness of breath, or excessive bradycardia.
• Advise patients subject to spontaneous hypoglycemia or diabetic patients receiving insulin or oral hypoglycemic agents that some symptoms of hypoglycemia (eg, tachycardia) may be masked.
• Caution patients to avoid sudden position changes to prevent orthostatic hypotension.

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