Delving into the Latest Updates on Rociverine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Rociverine (INN), Rilaten

+ [1]

Target-

Mechanism-

Therapeutic Areas

Nervous System DiseasesDigestive System Disorders

Active Indication

Gastrointestinal spasmSpasm biliary

Inactive Indication

Pain

Originator Organization

Laboratori Guidotti SpA

Active Organization

Laboratori Guidotti SpA

Inactive Organization

French International Public Relations Company

Drug Highest PhaseApproved

First Approval Date

CN (18 Aug 2015),

Gastrointestinal spasmSpasm biliary

Regulation-

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Structure

Molecular FormulaC20H37NO3

InChIKeyXPYLKZZOBVLVHB-FRWHHYCTSA-N

CAS Registry53716-44-2

阐明健康受试者经单次和多次静脉给予罗西维林注射液后，药物在体内的动态变化规律（即药物吸收、分布、代谢和排泄的过程和特点）；阐明本药在中国人体药代动力学特征，为罗西维林注射液进行下一步临床研究提供依据。

[Translation]

To clarify the dynamic changes of the drug in the body after single and multiple intravenous administration of roxivirine injection to healthy subjects (i.e. the process and characteristics of drug absorption, distribution, metabolism and excretion); to clarify the pharmacokinetic characteristics of this drug in Chinese humans, and to provide a basis for the next clinical study of roxivirine injection.

Start Date22 Aug 2011

Sponsor / Collaborator

French International Public Relations Company

100 Clinical Results associated with Rociverine

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100 Translational Medicine associated with Rociverine

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100 Patents (Medical) associated with Rociverine

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33

Literatures (Medical) associated with Rociverine

01 Dec 2011·Acta Obstetricia et Gynecologica ScandinavicaQ3 · MEDICINE

Use of an antispasmodic (rociverine) to shorten the length of labor: a randomized, placebo‐controlled trial

Q3 · MEDICINE

Article

Author: Pierfrancesco Bolis ; Massimo Agosti ; Antonella Cromi ; Fabio Ghezzi ; Nicoletta Piazza ; Stefano Uccella ; Maurizio Serati

AbstractObjective. To determine the effectiveness of rociverine, an antispasmodic drug, for reducing the duration of labor among nulliparous women managed according to a standard intrapartum protocol. Design. Randomized controlled trial. Setting. An academic tertiary care hospital. Population. Nulliparae in spontaneous active labor, with cervical dilatation between 3 and 5cm. Methods. Participants were randomly assigned to receive either an intramuscular injection of 20mg rociverine (n=55) or the same volume of saline (n=56). Main Outcome Measure. Cervical dilatation rate (from administration of study drug to full dilatation). Results. Laboring women who received rociverine had faster cervical dilatation than those assigned to placebo (2.43±1.84 vs. 1.85±1.38cm/hour, p=0.03). The time interval from treatment administration to full cervical dilatation was shorter in the rociverine group than in the placebo group (220±125 vs. 278±129min, p=0.04). No difference was found in any other obstetric outcome. No adverse effects have been recorded from rociverine administration. Conclusions. Intrapartum administration of rociverine to nulliparous women may help to reduce the duration of the first stage of labor in a context of uniform labor management.

01 Jun 2008·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

Validation of an HPLC–MS method for rociverine tablet dissolution analysis

Q3 · MEDICINE

Article

Author: Massimo Ricciutelli ; Ela Hoti ; Roberta Censi ; Luciano Barboni ; Maurizio Valleri ; Piera Di Martino ; Sante Martelli ; Ledjan Malaj

The aim of this work was to develop and validate a method to assess the dissolution behaviour of rociverine sugar-coated tablets. In our laboratories, an HPLC-MS in reverse phase method of analysis was developed for the dosage of unknown rociverine solution. This analytical method was applied to determine the dissolution rate of rociverine tablets produced by the industrial procedure, because there is no official method description. Dissolution tests were carried out in sink conditions as follows: dissolution medium HCl 0.01 N, paddle rotation speed 50 rpm and vessel volume 1000 ml. The dissolution test gave satisfactory results: 95% of the drug was dissolved within 30 min and drug dissolution was concluded after 60 min. The method was demonstrated to be adequate for Quality Control of rociverine tablets. Validation was inferred from specificity, linearity, precision, accuracy and robustness.

01 Jul 1995·European Journal of Pharmacology: Molecular PharmacologyQ3 · MEDICINE

Stereoselective inhibition of muscarinic receptor subtypes by the eight stereoisomers related to rociverine

Q3 · MEDICINE

Article

Author: R Maggio ; P Barbier ; Francesca Vaglini ; C Di Bugno ; L Turbanti ; Francesco Fornai ; Ar Renzetti ; Giovanni Umberto Corsini

The chemical structure corresponding to 1-hydroxy[1,1'-bicyclohexyl]-2-carboxylic acid 2-(diethylamino)-1-methylethyl ester has the classical profile of ester-type antimuscarinic drugs. The presence of three chiral carbons leads to eight stereoisomers and the substitutions on the cyclohexyl ring generate cis-isomers (1, named rociverine) and trans-isomers (2). The aim of this study was to determine the binding pattern of the eight stereoisomers and two derived compounds, (1S,2S)-1-hydroxy[1,1'-bicyclohexyl]-2-carboxylic acid 2-(dimethylamino)-1-ethyl ester (3) (1S,2S)-1-hydroxy[1,1'-bicyclohexyl]-2-carboxylic acid (S)-2-(diethylamino)-1-methylethyl ester methyl iodide (4), at the five cloned muscarinic receptors stably expressed in chinese hamster ovary cells, in order to define how stereochemical modifications could affect the affinity. Our data showed that cis-stereoisomers exhibited higher variations in affinity than trans-stereoisomers. Among the cis-stereoisomers, those with the (1R,2R) configuration showed considerably higher affinities (up to 240-fold) than those with the (1S,2S) configuration. The (1S,2S) configuration was important for binding selectivity; this was confirmed also by the use of the two additional compounds.

100 Deals associated with Rociverine

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External Link

KEGG	Wiki	ATC	Drug Bank
D07078	Rociverine	A03AA06	DB13581

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Gastrointestinal spasm	CN	Laboratori Guidotti SpA	18 Aug 2015
Spasm biliary	CN	Laboratori Guidotti SpA	18 Aug 2015

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Gastrointestinal spasm	Phase 1	CN	French International Public Relations Company	02 Dec 2012
Pain	Phase 1	CN	French International Public Relations Company	02 Dec 2012
Spasm biliary	Phase 1	CN	French International Public Relations Company	02 Dec 2012