Delving into the Latest Updates on Nipradilol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Nipradilol (JAN/INN)

+ [3]

Target

β-adrenoceptors

Action

antagonists

Mechanism

β-adrenoceptors antagonists(Beta adrenergic receptors antagonists)

Therapeutic Areas

Nervous System DiseasesCardiovascular DiseasesEye Diseases+ [1]

Active Indication

GlaucomaOcular HypertensionAngina Pectoris+ [1]

Inactive Indication-

Originator Organization-

Active Organization

Teika Pharmaceutical Co., Ltd.

Kowa Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (20 Sep 1988),

Angina PectorisHypertension

Regulation-

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Structure/Sequence

Molecular FormulaC15H22N2O6

InChIKeyOMCPLEZZPVJJIS-UHFFFAOYSA-N

CAS Registry81486-22-8

AbstractBackgroundTo evaluate and compare the long‐term efficacy of medical treatments for normal tension glaucoma (NTG) in controlling intraocular pressure (IOP), and establish a hierarchical ranking based on their effectiveness. ‘Long‐term’ is defined as a treatment duration of over 12 weeks in randomised controlled trials (RCTs).MethodsThis systematic review and model‐based network meta‐analysis (MBNMA) collected data of 795 patients with 997 eyes from RCTs. Patients with NTG were selected based on strict inclusion/exclusion criteria, with randomsation procedures and masking as reported in the individual trials. Eight different medications were compared, including prostaglandin analogues, beta‐blockers, brimonidine, unoprostone isopropyl, brovincamine, and palmitoylethanolamide (PEA). Notably, PEA is an oral medication, while other drugs are topical agents.ResultsPrimary outcome is the long‐term efficacy of IOP control across medications with different follow‐up durations. Among the eight medications, PEA demonstrates the highest efficacy (Surface under the cumulative ranking, SUCRA = 7.46%), followed by two prostaglandin analogues: travoprost (SUCRA = 6.86%) and latanoprost (SUCRA = 6.76%), then two beta‐blockers: nipradilol (SUCRA = 4.90%) and timolol (SUCRA = 4.89%). Both brimonidine and unoprostone isopropyl have SUCRA scores below 4.0%, indicating modest but limited efficacy. Brovincamine has the lowest SUCRA score (1.32%), reflecting minimal effectiveness.ConclusionsThis study revealed PEA as a promising agent for long‐term IOP control in NTG patients, suggesting potential use as primary or adjunctive therapy. The outcomes call for PEA's consideration in clinical practice and highlight the need for further research into its long‐term efficacy and safety for NTG.

01 Feb 2024·Advances in Therapy

The Effect of β-Blocker Eye Drops on Pulse Rate, Ocular Blood Flow, and Glaucoma Progression: A Retrospective Longitudinal Study

Article

Author: Kiyota, Naoki ; Omodaka, Kazuko ; Shiga, Yukihiro ; Yokoyama, Yu ; Nakazawa, Toru ; Himori, Noriko ; Pak, Kyongsun ; Ninomiya, Takahiro ; Tsuda, Satoru

INTRODUCTIONOur study was conducted to determine factors associated with the effectiveness of a β-blocker eye drop add-on in altering pulse rate (PR) in glaucoma patients.METHODSThis retrospective study examined 236 eyes of 138 patients who received a β-blocker eye drop add-on during follow-up. Patients were included if at least one PR measurement was available both before and after the add-on was started. We collected data on ophthalmic parameters: longitudinal PR; longitudinal choroidal blood flow, represented by laser speckle flowgraphy-measured mean blur rate (MBR); and diacron-reactive oxygen metabolites (d-ROMs). We used a multivariable linear mixed-effects model to investigate the effectiveness of the β-blocker eye drop add-on in altering PR and examined factors contributing to a larger PR alteration after the add-on was started by analyzing the effect on PR of the interaction term between the add-on and clinical factors. We used the k-means method to classify the patients.RESULTSThe β-blocker eye drop add-on reduced PR (- 7.61 bpm, P < 0.001). Female gender, higher PR when the add-on was started, lower central corneal thickness, and a higher d-ROM level were associated with greater reduction in PR (P < 0.05). In a cluster of patients with these clinical features, choroidal MBR increased by + 3.42% when we adjusted for change over time; MD slope, which represents the speed of glaucoma progression, improved by + 0.64 dB/year (P < 0.05).CONCLUSIONSWe identified a glaucoma subgroup in which PR decreased, choroidal blood flow increased, and glaucoma progression slowed after a β-blocker eye drop add-on was started.

27 Jun 2022·Reviews in Inorganic Chemistry

NO, CO and H₂S based pharmaceuticals in the mission of vision (eye health): a comprehensive review

Author: Khan, Mohd Washid ; Maurya, Ram Charitra ; Mir, Jan Mohammad

AbstractA set of well defined signaling molecules responsible for normal functioning of human physiology including nitric oxide along with carbon monoxide and hydrogen sulphide are referred as “gasotransmitters”. Due to their involvement in almost every system of a human body, the care of highly sensitive organs using these molecules as drugs represents highly fascinating area of research. In connection with these interesting aspects, the applied aspects of these gaseous molecules in maintaining healthy eye and vision have been targeted in this review. Several examples of eye-droppers including NORMs like latanoprost and nipradiol, CORMs like CORM-3 and CORM-A1, and Hydrogen sulfide releasing system like GYY4137 have been discussed in this context. Therefore the relation of these trio-gasotransmitters with the ophthalmic homeostasis on one hand, and de-infecting role on the other hand has been mainly highlighted. Some molecular systems capable of mimicking gasotransmitter action have also been introduced in connection with the titled theme.

100 Deals associated with Nipradilol

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External Link

KEGG	Wiki	ATC	Drug Bank
D01691	Nipradilol	S01EA	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	Japan	Teika Pharmaceutical Co., Ltd.	16 Jun 1996
Ocular Hypertension	Japan	Teika Pharmaceutical Co., Ltd.	16 Jun 1996
Angina Pectoris	Japan	Kowa Co., Ltd.	20 Sep 1988
Hypertension	Japan	Kowa Co., Ltd.	20 Sep 1988

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ARVO2011	Not Applicable	-	8	Topical Nipradilol	(bigednzluj) = nmpbkadrgk vfrtajevtl (inxxwjmusx ) View more	-	01 Apr 2011
ARVO2004	Not Applicable	Diabetic Retinopathy	-	Nipradilol-treated eyes	(jydyjybtmr) = qozseigfmb rtydzqqgvd (eegcwwxsiq )	-	01 May 2004
				topical nipradilol (Non-treated eyes)	(jydyjybtmr) = ggyawdeftu rtydzqqgvd (eegcwwxsiq )
ARVO2002	Not Applicable	-	-	Nipradilol (1%)	(osmooywqxs) = kceuybgexm gezciirdqa (tboacscxzj )	Positive	01 Dec 2002
				Timolol (0.5%) and Bunazosin (0.125%)	(osmooywqxs) = rahfdkbfls gezciirdqa (tboacscxzj )