Nebivolol Chemical Properties

Melting point:

155-156°C

Boiling point:

600.5±55.0 °C(Predicted)

Density 

1.309

storage temp. 

-20°C Freezer

solubility 

DMSO (Slightly), Methanol (Slightly, Heated)

pka

pKa 8.22(H2O,t =25±1,Iundefined,Ar) (Uncertain)

form 

Solid

color 

White to Off-White

Nebivolol Usage And Synthesis

Uses

Antihypertensive (β-blocker).

Uses

Nebivolol is a cardioselective beta-1 receptor blocking agent.

Definition

ChEBI: (R,S,S,S)-nebivolol is a 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] that has (1S,1'S,2R,2'S)-configuration. It is a conjugate base of a (R,S,S,S)-nebivolol(1+). It is an enantiomer of a (S,R,R,R)-nebivolol.

Clinical Use

Beta-adrenoceptor blocker:
Essential hypertension
Adjunct in heart failure

Drug interactions

Potentially hazardous interactions with other drugs
Anaesthetics: enhanced hypotensive effect.
Analgesics: NSAIDs antagonise hypotensive effect.
Anti-arrhythmics: increased risk of myocardial depression and bradycardia; increased risk of bradycardia, myocardial depression and AV block with amiodarone; increased risk of myocardial depression and bradycardia with flecainide.
Antidepressants: enhanced hypotensive effect with MAOIs.
Antihypertensives; enhanced hypotensive effect; increased risk of withdrawal hypertension with clonidine; increased risk of first dose hypotensive effect with post-synaptic alpha-blockers such as prazosin.
Antimalarials: increased risk of bradycardia with mefloquine.
Antipsychotics enhanced hypotensive effect with phenothiazines.
Calcium-channel blockers: increased risk of bradycardia and AV block with diltiazem; hypotension and heart failure possible with nifedipine and nisoldipine; asystole, severe hypotension and heart failure with verapamil.
Cytotoxics: possible increased risk of bradycardia with crizotinib.
Diuretics: enhanced hypotensive effect.
Fingolimod: possibly increased risk of bradycardia. Moxisylyte: possible severe postural hypotension.
Sympathomimetics: severe hypertension with adrenaline and noradrenaline and possibly with dobutamine.

Metabolism

Nebivolol is extensively metabolised in the liver by acyclic and aromatic hydroxylation, N-dealkylation, and glucuronidation. Hydroxylation is by cytochrome P450 isoenzyme CYP2D6, partly to active hydroxy-metabolites. It is excreted in the urine and faeces, almost entirely as metabolites.

Nebivolol(118457-14-0)Related Product Information

• (+)-Nebivolol
• Nebivolol
• Nebivolol
• 3-(4-FLUOROPHENOXY)PROPAN-1-AMINE HYDROCHLORIDE