NEBIVOLOL HYDROCHLORIDE

Details

Stereochemistry	RACEMIC
Molecular Formula	C22H25F2NO4.ClH
Molecular Weight	441.896
Optical Activity	( + / - )
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.[H][C@]1(CCC2=CC(F)=CC=C2O1)[C@H](O)CNC[C@@H](O)[C@@]3([H])CCC4=C(O3)C=CC(F)=C4

InChI

InChIKey=JWEXHQAEWHKGCW-VCVZPGOSSA-N

InChI=1S/C22H25F2NO4.ClH/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22;/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2;1H/t17-,18-,21-,22+;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C22H25F2NO4
Molecular Weight	405.435
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	4 / 4
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.drugbank.ca/drugs/DB04861 | https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_LBL.pdf | https://www.ncbi.nlm.nih.gov/pubmed/18485134 | https://www.ncbi.nlm.nih.gov/pubmed/9825177 | https://www.ncbi.nlm.nih.gov/pubmed/21283024 | https://www.ncbi.nlm.nih.gov/pubmed/1681809 | https://www.ncbi.nlm.nih.gov/pubmed/1357130https://www.drugbank.ca/drugs/DB04861 | https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_LBL.pdf | http://www.bystolic.com/

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. 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. Marketed under the brand name BYSTOLIC, Nebivolol is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Beta-1 adrenergic receptor 158 Target ID: CHEMBL213 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2455841 \| https://www.ncbi.nlm.nih.gov/pubmed/2462161 \| https://www.allergan.com/assets/pdf/bystolic_pi \| https://www.ncbi.nlm.nih.gov/pubmed/11309254	Antagonist 2737		0.7 nM [Ki]
Beta-1 adrenergic receptor 158 Target ID: CHEMBL213 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21283024 \| https://www.ncbi.nlm.nih.gov/pubmed/1681809	Antagonist 2737		0.35 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 546 Sources: https://www.allergan.com/assets/pdf/bystolic_pi https://www.drugs.com/pro/nebivolol.html https://www.ncbi.nlm.nih.gov/pubmed/19393838	Primary		Approved 8307	BYSTOLIC Approved Use BYSTOLIC is a beta-adrenergic blocking agent indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. BYSTOLIC may be used alone or in combination with other antihypertensive agents . Launch Date 1.19784958E12
Hypertension 546 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7596131 https://www.ncbi.nlm.nih.gov/pubmed/7692155 https://www.ncbi.nlm.nih.gov/pubmed/18485134 https://www.ncbi.nlm.nih.gov/pubmed/1357130	Primary		Approved 8307	BYSTOLIC Approved Use BYSTOLIC is a beta-adrenergic blocking agent indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. BYSTOLIC may be used alone or in combination with other antihypertensive agents . Launch Date 1.1977632E12

C_max

Value	Dose	Co-administered	Analyte	Population
1.48 ng/mL REVIEW https://pubmed.ncbi.nlm.nih.gov/18083889/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		NEBIVOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
7.76 ng × h/mL REVIEW https://pubmed.ncbi.nlm.nih.gov/18083889/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		NEBIVOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
11 h REVIEW https://pubmed.ncbi.nlm.nih.gov/18083889/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		NEBIVOLOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
2% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf	unknown		NEBIVOLOL plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	Disc. AE: Hyperhidrosis, Pallor... AEs leading to discontinuation/dose reduction: Hyperhidrosis Pallor Depressed level of consciousness Hypokinesia Hypotension Sinus bradycardia Hypoglycemia Hypokalemia Respiratory failure Vomiting Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4	unhealthy n = 6545 Health Status: unhealthy Condition: Hypertension Population Size: 6545 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4	Disc. AE: Headache, Nausea... AEs leading to discontinuation/dose reduction: Headache (0.4%) Nausea (0.2%) Bradycardia (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4
5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: valsartan, oral(80 mg, qd) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206302s000lbl.pdf Page: p.1	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206302s000lbl.pdf Page: p.1	Disc. AE: Disorder fetal... AEs leading to discontinuation/dose reduction: Disorder fetal Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206302s000lbl.pdf Page: p.1

AEs

AE	Significance	Dose	Population
Depressed level of consciousness	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Hyperhidrosis	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Hypoglycemia	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Hypokalemia	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Hypokinesia	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Hypotension	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Pallor	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Respiratory failure	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Sinus bradycardia	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Vomiting	Disc. AE	500 mg single, oral Overdose Dose: 500 mg Route: oral Route: single Dose: 500 mg Co-administed with:: acetylsalicylic acid, oral(>100 mg) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8	healthy n = 1 Health Status: healthy Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.8
Bradycardia	0.2% Disc. AE	40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4	unhealthy n = 6545 Health Status: unhealthy Condition: Hypertension Population Size: 6545 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4
Nausea	0.2% Disc. AE	40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4	unhealthy n = 6545 Health Status: unhealthy Condition: Hypertension Population Size: 6545 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4
Headache	0.4% Disc. AE	40 mg 1 times / day multiple, oral Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4	unhealthy n = 6545 Health Status: unhealthy Condition: Hypertension Population Size: 6545 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf Page: p.4
Disorder fetal	Disc. AE	5 mg 1 times / day multiple, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Co-administed with:: valsartan, oral(80 mg, qd) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206302s000lbl.pdf Page: p.1	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206302s000lbl.pdf Page: p.1

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1670	inhibitor 1695	substrate 1168 inhibitor 1789

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1463 CYP2A6 670 CYP2B6 770 CYP2C8 869 CYP2C19 1410 CYP3A4/5 261

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1620	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no
CYP2A6 702	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no
CYP2B6 946	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no
CYP2C19 1484	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no
CYP2C8 923	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no
CYP2C9 1747	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no
CYP2D6 1826	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no
CYP3A4/5 314	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 50, 55	no

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP3A4 1670	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/021742s000_ClinPharmR_P1.pdf Page: 28, 50, 55	minor
CYP2D6 1168	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/206302Orig1s000ClinPharmR.pdf Page: 17.0	yes		yes (co-administration study) Comment: from product label: fluoxetine coadministration led to increased AUC by 8% and Cmax by 3-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/206302Orig1s000ClinPharmR.pdf Page: 17.0

Sourcing

Vendor/Aggregator	ID	URL
AChemBlock	10241
AK Scientific	M753
Aronis	BBC/719
BOC Sciences	118457-15-1
IBScreen	BB_SC-12513
IBScreen	Bio-0068
Lab Network	LN01346236
MolPort	MolPort-003-849-342
MolPort	MolPort-023-276-830
ShangHai Biochempartner	BCP21038
Tocris	3517
Toronto Research Chemicals	N387896
Vitas-M Laboratory	STK637549
ZINC	ZINC000003951631	http://zinc15.docking.org/substances/ZINC000003951631
eMolecules	29703203
eMolecules	300435536
eMolecules	30387256
mcule	MCULE-7932280679

PubMed

Title	Date	PubMed
Studies on the effect of alcohols on the chiral discrimination mechanisms of amylose stationary phase on the enantioseparation of nebivolol by HPLC.	2001 Apr 24	11356487
Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium.	2001 Aug	11498519
Nebivolol induces calcium-independent signaling in endothelial cells by a possible beta-adrenergic pathway.	2001 Aug	11483868
Protective role of nebivolol in hydroxyl radical induced injury.	2001 Dec	11811388
Effects of nebivolol on human platelet aggregation.	2001 Dec	11707696
HPLC enantiomeric resolution of nebivolol on normal and reversed amylose based chiral phases.	2001 Mar	11265585
[Nebivolol, a beta blocker of the 3rd generation: modern therapy of arterial hypertension. Results of a multicenter observation study].	2001 Mar 15	11293936
Nebivolol and airway responsiveness in the rabbit.	2001 Mar 23	11324721
[Heart and lung disease. Are beta blockers allowed in asthma?].	2001 May 24	11420835
[Pharma-clinics medication of the month. Nebivolol (Nobiten)].	2001 Nov	11789394
Endothelial adrenoceptors.	2001 Nov	11602826
Integrated effects of the vasodilating beta-blocker nebivolol on exercise performance, energy metabolism, cardiovascular and neurohormonal parameters in physically active patients with arterial hypertension.	2001 Oct	11607802
What drug must be used to avoid the most common hypertensive complications?	2001 Oct	11533550
[Nebivolol treatment in essential arterial hypertension].	2001 Oct-Dec	12092233
[Functional and biochemical characteristics of the vasodilator effects of nebivolol in patients with arterial hypertension].	2002	12577837
[Effects of nebivolol on microcirculation, platelet aggregation and blood viscosity in patients with essential hypertension].	2002	12494141
[Effect of nebivolol on dynamics of microalbuminuria, renal blood flow and 24-hour blood pressure profile in patients with hypertension].	2002	12494075
[Effect of nebivolol on remodeling of the heart and vessels and the state of hemodynamics in patients with hypertension].	2002	12494053
[Assessment of safety and antihypertensive efficacy of a cardioselective beta-blocker nebivolol in patients with hypertension and concomitant chronic obstructive bronchitis].	2002	12494034
[Antihypertensive efficacy and tolerability of nebivolol].	2002	12494015
[Autonomic nervous system function and effects of beta-adrenoblockers on heart rhythm variability in patients with myocardial infarction].	2002	12416220
Nebivolol vs amlodipine as first-line treatment of essential arterial hypertension in the elderly.	2002	12126265
[Effects of nebivolol on serum levels of NO2 and NO3 oxides in patients with type 2 diabetes mellitus].	2002	11944352
Effect of nebivolol on left ventricular function in patients with chronic heart failure: a pilot study.	2002 Dec	12453547
The pharmacologic treatment of uncomplicated arterial hypertension in patients with airway dysfunction.	2002 Jan	11796456
Nitric-oxide-mediated relaxations in salt-induced hypertension: effect of chronic beta1 -selective receptor blockade.	2002 Mar	11875309
[Despite antihypertensive treatment with beta-blocker patients remain incapacitated].	2002 May 2	12422716
Study of the Effects of Nebivolol Intervention on Outcomes and Rehospitalisation in Seniors with Heart Failure (SENIORS). Rationale and design.	2002 Nov	12243852
[Beta blockade plus NO release. Patients with heart failure can be loaded more].	2002 Oct 10	12474368
Nebivolol: a selective beta(1)-adrenergic receptor antagonist that relaxes vascular smooth muscle by nitric oxide- and cyclic GMP-dependent mechanisms.	2002 Sep	12223176
Effects of nebivolol and atenolol on small arteries and microcirculatory endothelium-dependent dilation in hypertensive patients undergoing isometric stress.	2002 Sep	12195121
Allergic contact dermatitis to nebivolol.	2002 Sep	12169193
[Nebivolol effects on platelet aggregation and anticoagulation system].	2003	14603912
[Heart rate control with nebivolol in patients with tachysystolic atrial fibrillation].	2003	14593370
[The use of nebivolol in menopausal women with hypertension].	2003	14593358
[Pharmacological modulation of NO synthesis in patients with arterial hypertension and endothelial dysfunction].	2003	12934313
Nebivolol prevents vascular NOS III uncoupling in experimental hyperlipidemia and inhibits NADPH oxidase activity in inflammatory cells.	2003 Apr 1	12692005
Involvement of the beta3 adrenoceptor in nebivolol-induced vasorelaxation in the rat aorta.	2003 Aug	12883327
Efficacy and tolerability profile of nebivolol vs atenolol in mild-to-moderate essential hypertension: results of a double-blind randomized multicentre trial.	2003 Dec	14761075
[Beta blocker improves the endothelial function. Gas-forming blood vessel protection].	2003 Dec 18	14974334
The combination of nebivolol plus pravastatin is associated with a more beneficial metabolic profile compared to that of atenolol plus pravastatin in hypertensive patients with dyslipidemia: a pilot study.	2003 Jun	12808486
A comparison of the beta1-selectivity of three beta1-selective beta-blockers.	2003 Jun	12795776
Third-generation beta-blockers stimulate nitric oxide release from endothelial cells through ATP efflux: a novel mechanism for antihypertensive action.	2003 Jun 3	12742996
[Beta-1 blockade plus NO release. Additional organ protection for patients with hypertension].	2003 Oct 2	14603611
Long-term treatment with nebivolol improves arterial reactivity and reduces ventricular hypertrophy in spontaneously hypertensive rats.	2003 Sep	12960679
The shift in the "paradigm" of the pharmacology of hypertension.	2004	14965315

Patents

Sample Use Guides

In Vivo Use Guide

After a 4-week placebo run-in period, 30 patients (mean age 48 years) were randomly allocated to double-blind treatment with either DL-nebivolol 5 mg or D-nebivolol 2.5 mg once daily for 4 weeks.

Route of Administration: Oral

In Vitro Use Guide

Nebivolol and d-nebivolol (SRRR) inhibited noradrenaline-induced cAMP accumulation with IC50 values of 22 and 15 nM, respectively in rat living cardiac cells.

Substance Class	Chemical Created by `admin` on `Fri Dec 16 18:27:13 UTC 2022` Edited by `admin` on `Fri Dec 16 18:27:13 UTC 2022`
Record UNII	JGS34J7L9I
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NEBIVOLOL HYDROCHLORIDE

Official Name

English

BYSTOLIC

Brand Name

English

BYVALSON COMPONENT NEBIVOLOL HYDROCHLORIDE

Brand Name

English

NEBIVOLOL HYDROCHLORIDE [USP-RS]

Common Name

English

(1RS,1'RS)-1,1'-((2RS,2'SR)-BIS(6-FLUORO-3,4-DIHYDRO-2H-1-BENZOPYRAN-2-YL))-2,2'-IMINODIETHANOL HYDROCHLORIDE

Common Name

English

NEBIVOLOL HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

NEBIVOLOL HYDROCHLORIDE [MART.]

Common Name

English

R067555

Code

English

2H-1-BENZOPYRAN-2-METHANOL, .ALPHA,.ALPHA.'-(IMINOBIS(METHYLENE))BIS(6-FLUORO-3,4-DIHYDRO-, HYDROCHLORIDE, (.ALPHA.R,.ALPHA.'R,2R,2'S)-REL-

Common Name

English

Nebivolol hydrochloride [WHO-DD]

Common Name

English

R-067555

Code

English

NEBIVOLOL HYDROCHLORIDE [USAN]

Common Name

English

NEBIVOLOL HCL

Common Name

English

NEBIVOLOL HYDROCHLORIDE COMPONENT OF BYVALSON

Brand Name

English

NEBIVOLOL HYDROCHLORIDE [MI]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29576