| Identification | Back Directory | [Name]
Nebivolol | [CAS]
118457-14-0 | [Synonyms]
R065824
R-065824
R 065824
NEBIVOLOL
dl-Nebivolol
Unii-030Y90569u
Nebivolol USP/EP/BP
Nebivolol (R 065824)
Nebivolol, racemic mixture
NEBILET; BYSTOLIC; R 065824; R065824; R-065824
2H-1-Benzopyran-2-methanol, α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-, (αR,α'R,2R,2'S)-rel-
[2R*[R*[R*(S*)]]]-alpha,alpha'-[Iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol
(1S)-1-[(2R)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-[[(2S)-2-[(2S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-hydroxyethyl]amino]ethanol
Nebivolol D4Q: What is
Nebivolol D4 Q: What is the CAS Number of
Nebivolol D4 Q: What is the storage condition of
Nebivolol D4 Q: What are the applications of
Nebivolol D4 | [EINECS(EC#)]
601-527-4 | [Molecular Formula]
C8H11NO4 | [MOL File]
118457-14-0.mol | [Molecular Weight]
185.178 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
pKa 8.22(H2O,t =25±1,Iundefined,Ar) (Uncertain) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
Antihypertensive (β-blocker). | [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. |
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J S LABS
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