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| | Nebivolol Basic information |
| Product Name: | Nebivolol | | Synonyms: | NEBIVOLOL;Unii-030Y90569u;dl-Nebivolol;[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;NEBILET; BYSTOLIC; R 065824; R065824; R-065824;R 065824;R065824 | | CAS: | 118457-14-0 | | MF: | C22H25F2NO4 | | MW: | 405.43 | | EINECS: | 601-527-4 | | Product Categories: | Nebivolol;Pharmaceuticals | | Mol File: | 118457-14-0.mol |  |
| | 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 Preparation Products And Raw materials |
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