Last update 01 Nov 2024

Dropropizine

Last update 01 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Dropropizine (INN/BAN)

+ [10]

Target-

Mechanism-

Therapeutic Areas

Respiratory Diseases

Active Indication

Cough

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure

Molecular FormulaC13H20N2O2

InChIKeyPTVWPYVOOKLBCG-UHFFFAOYSA-N

CAS Registry17692-31-8

100 Clinical Results associated with Dropropizine

100 Translational Medicine associated with Dropropizine

100 Patents (Medical) associated with Dropropizine

Literatures (Medical) associated with Dropropizine

17 Feb 2021·Critical Reviews in Analytical ChemistryQ2 · CHEMISTRY

Characteristics, Properties and Analytical Methods for Determination of Dropropizine and Levodropropizine: A Review

Q2 · CHEMISTRY

Review

Author: Machado, Anna Karolina Mouzer da Silva ; Todeschini, Vitor ; Nemitz, Marina Cardoso ; Sangoi, Maximiliano da Silva

Dropropizine is a peripheral antitussive drug that acts by inhibiting cough reflex through its action on the peripheral receptors and their afferent conductors. It is marketed in a racemic form or its pure enantiomer called levodropropizine and both are available worldwide in various drug dosage formulations such as tablets, sirup and oral solution. Due to the widespread use of antitussives in the clinic it is necessary to develop efficient analytical methodologies for quality control and also for pharmacokinetic, bioavailability and bioequivalence studies. This review presents a survey of the characteristics, properties and analytical methods used for drug determination, being carried out through scientific articles as well as in official compendia. From the analyzed studies, the majority reports the use of HPLC/UV techniques for drug determination, but also spectrophotometric UV/Vis methods as well as gas chromatography, and voltammetric, potentiometric and conductometric titration methods. In addition, the methodologies addressed the determination of dropropizine or levodropropizine in different types of matrices such as raw material, pharmaceutical formulations, plasma and urine. Despite the extensive clinical use of dropropizine, data from this review evidenced a still limited number of studies dealing with analytical methods for its determination in different matrices, which may be of concern since the applicability of these methods is important for quality assurance, efficacy and safety of the medicine.

07 Jan 2021·ChemSusChemQ2 · CHEMISTRY

Catalytic, Kinetic, and Mechanistic Insights into the Fixation of CO₂ with Epoxides Catalyzed by Phenol‐Functionalized Phosphonium Salts

Q2 · CHEMISTRY

Article

Author: Frey, Anna ; Kubis, Christoph ; Hu, Yuya ; Spannenberg, Anke ; Werner, Thomas ; Jiao, Haijun ; Wei, Zhihong ; Ren, Chang‐Yue

AbstractA series of hydroxy‐functionalized phosphonium salts were studied as bifunctional catalysts for the conversion of CO2 with epoxides under mild and solvent‐free conditions. The reaction in the presence of a phenol‐based phosphonium iodide proceeded via a first order rection kinetic with respect to the substrate. Notably, in contrast to the aliphatic analogue, the phenol‐based catalyst showed no product inhibition. The temperature dependence of the reaction rate was investigated, and the activation energy for the model reaction was determined from an Arrhenius‐plot (Ea=39.6 kJ mol−1). The substrate scope was also evaluated. Under the optimized reaction conditions, 20 terminal epoxides were converted at room temperature to the corresponding cyclic carbonates, which were isolated in yields up to 99 %. The reaction is easily scalable and was performed on a scale up to 50 g substrate. Moreover, this method was applied in the synthesis of the antitussive agent dropropizine starting from epichlorohydrin and phenylpiperazine. Furthermore, DFT calculations were performed to rationalize the mechanism and the high efficiency of the phenol‐based phosphonium iodide catalyst. The calculation confirmed the activation of the epoxide via hydrogen bonding for the iodide salt, which facilitates the ring‐opening step. Notably, the effective Gibbs energy barrier regarding this step is 97 kJ mol−1 for the bromide and 72 kJ mol−1 for the iodide salt, which explains the difference in activity.

01 Feb 2020·XenobioticaQ4 · MEDICINE

Stereoselective pharmacokinetics and tissue distribution of levodropropizine after administration of pure levodropropizine and therac-dropropizine to Sprague–Dawley rats

Q4 · MEDICINE

Article

Author: Todmal, Umesh ; Saini, Neeraj Kumar ; Zainuddin, Mohd ; Srinivas, Nuggehally R. ; Balaji, Narayanan ; Sulochana, Suresh P. ; Balakrishna, Vinod A. ; Gabani, Bhavesh Babulal ; Timmapuram, Ashok ; Mullangi, Ramesh ; Shuvranshu, Praharaj

Levodropropizine (LDP) is a non-opioid anti-tussive. The stereoselective pharmacokinetics and tissue distribution (TD) of LDP vs. dextrodropropizine (DDP) have been characterized after oral and intravenous (IV) administration of LDP and rac-dropropozine in rats.Oral/IV doses of 50/5.0 mg/kg and 25/2.5 rac-dropropizine and LDP were employed. TD study focused on tissues such as liver, lung and kidney. Blood samples were collected for pharmacokinetic and TD evaluation. Validated methods were used to quantitate LDP, DDP and rac-dropropizine.No stereoselectivity in pharmacokinetics was observed between LDP vs. DDP following rac-dropropizine. However, LDP pharmacokinetics after LDP administration (oral/IV) appeared to be different compared to LDP derived from rac-dropropizine.TD data were similar between the two enantiomers regardless of oral/IV rac-dropropizine administration. When LDP alone was administered, levels were comparable to those derived for LDP from rac-dropropizine after oral/IV. However, in the lung and kidney tissues, the exposure after oral dosing was higher for LDP alone as compared to LDP from rac-dropropizine.In summary, complete characterization of stereoselective pharmacokinetics and TD of rac-dropropizine has been reported after oral/IV routes. It was evident that the presence of DDP, increased the plasma/tissue exposure of LDP which was evident after oral rac-dropropizine dosing.

100 Deals associated with Dropropizine

External Link

KEGG	Wiki	ATC	Drug Bank
D07393	Dropropizine	R05DB19	DB13785

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Cough	-	-	-

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