Bystolic (nebivolol HCl)

Nebivolol is a beta-adrenergic blocking agent (beta-blocker).

Nebivolol is a beta-adrenergic blocking agent (beta-blocker). In patients who are extensive metabolizers of substrates of cytochrome P-450 (CYP) isoenzyme 2D6 (most of the population) and at doses of 10 mg or less, nebivolol selectively inhibits beta1-adrenergic receptors. In poor metabolizers and at doses exceeding 10 mg, nebivolol inhibits both beta1- and beta2-adrenergic receptors.

Nebivolol also exhibits vasodilatory effects mediated through stimulation of endothelial nitric oxide activity; the precise mechanism of this effect has not been fully elucidated. The drug does not exhibit intrinsic sympathomimetic (beta1-agonist) activity, membrane-stabilizing (local anesthetic) activity, or alpha1-adrenergic blocking activity at clinically relevant concentrations. The precise mechanism of nebivolol's hypotensive action has not been fully elucidated.

However, nebivolol may reduce blood pressure by decreasing heart rate, myocardial contractility, and sympathetic outflow from the CNS; suppressing renin activity; and/or decreasing peripheral vascular resistance as a result of its vasodilating effects.

Nebivolol hydrochloride is a racemic mixture. Only the d-isomer has substantial beta-adrenergic blocking activity; the l-isomer appears to be pharmacologically active, but its precise contribution to the pharmacologic effects of the drug has not been fully established.

Nebivolol undergoes first-pass hepatic metabolism. The drug is metabolized extensively, mainly via glucuronidation of the parent drug and, to a lesser extent, via N-dealkylation and oxidation by CYP2D6. Although exposure to the parent drug is increased substantially in patients who are poor metabolizers of CYP2D6 substrates, both the parent drug and the main circulating metabolites of nebivolol contribute to the drug's beta-adrenergic blocking activity, and clinical efficacy and safety of nebivolol appear to be similar in poor and extensive metabolizers.

Following oral administration of a single, radiolabeled dose of nebivolol in extensive metabolizers, 38% of the dose was eliminated in urine, and 44% was eliminated in feces. In poor metabolizers, 67% of the dose was eliminated in urine, and 13% was eliminated in feces. In both extensive and poor metabolizers, less than 0.5% of an absorbed oral dose of nebivolol is eliminated in urine and feces as unchanged drug.

USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Nebivolol belongs to a class of drugs known as beta blockers.

It works by blocking the action of certain natural substances in your body, such as epinephrine, on the heart and blood vessels. This effect lowers heart rate, blood pressure, and strain on the heart.

Generic name: nebivolol HCl
Pronunciation: (ne-BIV-oh-lol)

The following indications are listed for Bystolic:

• Hypertension

Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.

No ICD codes are available for this drug.