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QuickView for Nebivolol (compound)

Summary
General Info

PubChem

PubChem Compound 11626384

PubChem Compound 11626384

Name:	nebivolol
PubChem Compound ID:	11626384
Molecular formula:	C₂₂H₂₆ClF₂NO₄
Molecular weight:	441.896 g/mol

DrugBank

Identification

Name:	nebivolol
Name (isomeric):	DB04861
Drug Type:	small molecule
Synonyms:	Nebivololum [latin]
Brand:	Nebipill, Nebilet, Nebicard-5, PI-21858, Bystolic, Nodon, Nubeta, Nebilong, Lobivon
Category:	Vasodilator Agents, Adrenergic beta-Antagonists, Antihypertensive Agents
CAS number:	99200-09-6

Pharmacology

Indication:	For the treatment of essential hypertension.
Pharmacology:	Nebivolol is a competitive and highly selective beta-1 receptor antagonist with mild vasodilating properties, possibly due to an interaction with the L-arginine/nitric oxide pathway. In preclinical studies, nebivolol has been shown to induce endothelium-dependent arterial relaxation in a dose dependent manner, by stimulation of the release of endot... show more » Nebivolol is a competitive and highly selective beta-1 receptor antagonist with mild vasodilating properties, possibly due to an interaction with the L-arginine/nitric oxide pathway. In preclinical studies, nebivolol has been shown to induce endothelium-dependent arterial relaxation in a dose dependent manner, by stimulation of the release of endothelial nitric oxide. Nitric oxide acts to relax vascular smooth muscle cells and inhibits platelet aggregation and adhesion. show less «
Mechanism of Action:	Nebivolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Nebivolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the relea... show more » Nebivolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Nebivolol blocks these receptors which reverses the effects of epinephrine, lowering the heart rate and blood pressure. In addition, beta blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. At high enough concentrations, this drug may also bind beta 2 receptors. show less «
Absorption:	The absorption of nebivolol is rapid and not affected by food.
Protein binding:	98%
Biotransformation:	Hepatic (CYP2D6-mediated)
Half Life:	10 hours
Toxicity:	The most common signs and symptoms associated with nebivolol overdosage are bradycardia and hypotension. Other important adverse events reported with nebivolol overdose include cardiac failure, dizziness, hypoglycemia, fatigue and vomiting. Other adverse events associated with β-blocker overdose include bronchospasm and heart block. The largest known ingestion of nebivolol worldwide involved a patient who ingested up to 500 mg of nebivolol along with several 100 mg tablets of acetylsalicylic acid in a suicide attempt. The patient experienced hyperhydrosis, pallor, depressed level of consciousness, hypokinesia, hypotension, sinus bradycardia, hypoglycemia, hypokalemia, respiratory failure and vomiting. The patient recovered.
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Terazosin	Increased risk of hypotension. Initiate concomitant therapy cautiously.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Targets

Beta-1 adrenergic receptor

Beta-2 adrenergic receptor

Enzymes

Cytochrome P450 2D6