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Last update 23 Jan 2025

Diphemanil Methylsulfate

Last update 23 Jan 2025

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Diphemanil Metilsulfate, Diphemanil metilsulfate (INN)

+ [1]

Target

mAChRs

Mechanism

mAChRs antagonists(Muscarinic acetylcholine receptor antagonists)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Schering Corp.

Active Organization-

Inactive Organization

Schering Corp.

Drug Highest PhaseWithdrawn

First Approval Date

US (17 May 1976)

Regulation-

Structure/Sequence

Molecular FormulaC21H27NO4S

InChIKeyBREMLQBSKCSNNH-UHFFFAOYSA-M

CAS Registry62-97-5

100 Clinical Results associated with Diphemanil Methylsulfate

100 Translational Medicine associated with Diphemanil Methylsulfate

100 Patents (Medical) associated with Diphemanil Methylsulfate

Literatures (Medical) associated with Diphemanil Methylsulfate

01 Mar 2007·Archives de PédiatrieQ4 · MEDICINE

Enquête française sur l'utilisation du diphémanil méthylsulfate (Prantal®) dans les unités de néonatologie

Q4 · MEDICINE

Article

Author: C. Flamant ; M. Lachtar ; A. Chauty ; F. Gold ; Y. Aujard ; J. Novakova ; I. Lavallée ; C. Perrot ; D. Mitanchez ; V. Biran-Mucignat

Diphemanil methylsulfate (Prantal) is a quaternary ammonium with parasympathicolytic properties. It is used in premature and term neonates with bradycardias related to vagal hyper reflectivity (HRV).OBJECTIVESTo assess the use of Prantal in the French neonatal and intensive care units: its indications, its modalities of use, its side effects and the number of patients treated during 1 year (2004) in France.METHODSA questionnaire was electronically sent to all neonatology units and all neonatal intensive care units in France.RESULTSAmong 202 units, 121 (60%) answered the questionnaire. Prantal was reported to be used in 51 (42.1%) units. Among them, 38 (31.4%) actually treated 169 patients in 2004 with a mean number of patients treated by unit of 4. The diagnostic of HRV was supported by: a history of malaise (84.3%), bradycardia (94.1%), oculocardiac reflex (74.5%), cardiac Holter (76.4%), cardiorespirographic recording (19.6%), esophageal pHmetry (35.2%) and esophageal fibroscopy (21.5%). The mean starting dosing was 4.7 mg/kg/d, the mean maximal dosing was 9 mg/kg/d and the mean daily intakes were initially 2.3 and secondary 2.9. Prantal dosing was adjusted to weight in 54.9%, every month in 85.7%. Treatment was stopped at the mean post-natal age of 6 months, mostly in a progressive manner and without monitoring help.CONCLUSIONPrantal was seldom used in 2004 in France for different reasons: HRV is an uncertain entity, the efficacy of Prantal has not been validated and atropinic side effects can be encountered.

01 Jan 2007·Journal of Chromatography BQ3 · MEDICINE

Sensitive quantification of diphemanil methyl sulphate in human plasma by liquid chromatography–tandem mass spectrometry

Q3 · MEDICINE

Article

Author: B. Do ; N. Adoui ; H. Graffard ; M.D. Le Hoang ; D. Pradeau ; S. Goulay-Dufaÿ ; F. Guyon

A simple detection system with a high-performance liquid chromatography (HPLC) with positive ionisation-tandem mass spectrometry (ESI-MS/MS) for determining diphemanil methylsulphate (DMS) levels in human plasma using 4-diphemanylmethylene,1-methylpiperidine as an internal standard (I.S.), is proposed. The acquisition was performed with the multiple reactional monitoring (MRM) mode, by monitoring the transitions: m/z 278>262 for DMS and m/z 263>247 for the I.S. The method involved a simple single-step deproteinisation with acetonitrile. The analyte was chromatographed on a Zorbax C18 reversed-phase chromatographic column by isocratic elution with 10(-3)M ammonium acetate and 10(-3)M hexafluorobutyric acid, adjusted to pH 7.0 with ammoniac/acetonitrile (40/60, v/v). The results were linear over the studied range (0.5-50.0 ng mL(-1)) and the total analysis time for each run was 10 min. The mean extraction apparent recoveries expressed at the 95% intervals of confidence were 94-104% for DMS and 92-106% for the I.S. The intra- and inter-assay precisions were 4.6-8.4% and 2.9-10.6%, respectively. The limit of quantification was 0.15 ng mL(-1). The devised assay was successfully applied to the residual concentrations monitoring in infant.

01 Jun 2002·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

LC determination of diphemanil methylsulfate: application to stability study of stored pharmaceutical formulations

Q3 · MEDICINE

Article

Author: F Guyon ; G Gouaillard ; D Pradeau ; J.J Houri ; V Acar ; M.D Le Hoang

Diphemanil methylsulfate (DMS) is a synthetic antimuscarinic agent classically used in infants for vagal hypertonia-related symptoms. A normal-phase, isocratic liquid chromatographic method was developed for the quantitative determination of DMS in bulk drugs and in pharmaceutical forms. The method has been completely validated and robustness of this method has been studied. The limit of detection (LOD) for DMS impurities namely, impurity 1 and 2 were found to be 11 and 46 ng/ml. The limit of quantitation (LOQ) was found to be 49 and 139 ng/ml for impurity 1 and 2, respectively. The stability studies have been performed for 2 and 10 mg DMS tablets subjected at various temperatures: 25 degrees C (long term storage condition) and 40 degrees C (accelerated storage condition) for 18 and 6 months, respectively. At 25 degrees C, the samples were found to be stable for the study period. At 40 degrees C, 2 and 10 mg DMS tablets showed degradation up to 5 and 10% over a 6-month period.

100 Deals associated with Diphemanil Methylsulfate

External Link

KEGG	Wiki	ATC	Drug Bank
D06878	Diphemanil Methylsulfate	A03AB15	DB00729

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