Delving into the Latest Updates on Tilidine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Tilidine hydrochloride (USAN), 盐酸替立定, W-5759A

+ [1]

Target

Opioid receptors

Action

agonists

Mechanism

Opioid receptors agonists(Opioid receptors agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Pain

Inactive Indication-

Originator Organization

Hebei Aoxing Group Pharmaceutical Co. Ltd.

Active Organization

Hebei Aoxing Group Pharmaceutical Co. Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

China (15 May 2015),

Pain

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC17H24ClNO2

InChIKeyMUWDJVKYGSDUSH-WQSQCKSQSA-N

CAS Registry27107-79-5

Exhaled breath (EB) aerosol was in principle shown to be a suitable matrix for bioanalysis of volatile but also non-volatile compounds. This attracted particular interest in the field of drug analysis. However, a big gap still exists in the understanding how and which drugs and/or their metabolites are excreted into exhaled breath and could thus actually be detected. The current study aimed to develop an analytical workflow for the qualitative detection of non-volatile drugs in EB aerosol microparticles.

RESULTS:

The analyte selection covered different drug classes such as antihypertensives, anticonvulsants or opioid analgesics to investigate and understand the excretion of drugs and their metabolites into EB aerosol. A device for collecting aerosol particles from the lung through impaction was used for the non-invasive sampling procedure. Three expiration cycles per participant and device were collected. The sample preparation consisted of a collector extraction with methanol. Qualitative method development and validation were performed using reversed-phase liquid chromatography (LC) coupled to orbitrap-based high-resolution mass spectrometry (HRMS). Qualitative method validation was done according to published recommendations and international guidelines. Parameters such as selectivity, carry-over, limits of detection and identification, recovery, matrix effects, and long-term stability were evaluated. The limits of detection ranged from 100 pg/collector to 10,000 pg/collector. The procedure was finally used to analyze a total of 31 patient EB samples and demonstrated that e.g., tilidine and its metabolite nortilidine as well as tramadol and its active metabolite O-desmethyltramadol can be detected in EB aerosol.

SIGNIFICANCE AND NOVELTY:

The work shows a comprehensive workflow for elucidating drug excretion into exhaled breath aerosol. This bioanalytical strategy and the corresponding novel data from this study are the foundation for further method development and to better understand, which drugs and their metabolites can be addressed by exhaled breath aerosol bioanalysis.

01 Feb 2023·Drug Testing and Analysis

Optimization, validation and application of a high‐throughput 96‐well elution protocol for the quantification of psychoactive substances in influent wastewater

Article

Author: Laimou‐Geraniou, Maria ; Boogaerts, Tim ; Maes, Florence ; van Nuijs, Alexander L. N. ; Van Wichelen, Natan ; Covaci, Adrian ; Aertgeerts, Bert ; Heath, Ester ; Quireyns, Maarten ; Pussig, Bram

Abstract:

Wastewater‐based epidemiology (WBE) is based on the analysis of human metabolic excretion products (biomarkers) of xenobiotics in wastewater, to gain information about various lifestyles and health aspects of a population in an evidence‐based manner. Due to the complex wastewater matrix and trace level occurrence of human biomarkers in the sewage network, it is crucial to have sensitive analytical procedures available. Additionally, to improve the value of WBE as a complementary epidemiological source, there is increasing pressure on the analysis of more compounds, more locations and more samples. A high‐throughput method based on 96‐well Oasis MCX solid‐phase extraction (SPE), requiring less influent wastewater (2 mL), was developed in accordance with the European Medicines Agency guidelines. Validation was successful for 28 parent drugs and metabolites of antidepressants, opioids and drugs of abuse. The selection of biomarkers and quantification limit was chosen to be relevant for WBE and was predominantly 10 ng/L or below. The final method was successfully applied to 24‐h composite samples of October 2019 (n = 27), obtained from an urban wastewater treatment plant in Leuven (Belgium).

01 Sep 2022·Drug and alcohol dependence

Five-year incidence of substance use and mental health diagnoses following exposure to opioids or opioids with benzodiazepines during an emergency department encounter for traumatic injury

Article

Author: Johnson, Keilan ; Lewis, Daniel ; Sprunger, Joel G ; Winhusen, T John ; Kaelber, David C

BACKGROUND:

Benzodiazepines and opioids are used alone or in conjunction in certain care settings, but each have the potential for misuse.

OBJECTIVE:

This longitudinal observational study evaluated substance use and mental health outcomes associated with providing opioids with or without benzodiazepine to treat traumatic injury in the emergency department (ED) setting.

METHODS:

We analyzed a limited dataset obtained through the IBM Watson Health Explorys. Matched cohorts were defined for: 1) patients treated with opioids during the ED encounter (ED-Opioid) vs. neither opioid or benzodiazepine treatment (No medication) (n = 5372); 2) patients treated with opioids and benzodiazepines during the ED encounter (ED-Opioid+Benzodiazepines) vs. No Medication (n = 2454); and 3) ED-Opioid+Benzodiazepines vs. ED-Opioid (n = 2454). Patients consisted of adults with an emergency department encounter in the MetroHealth System (Cleveland, Ohio) with a chief complaint of traumatic injury and medical records for five years following the encounter. Control patients for each cohort were matched to the exposure patients on demographics, body mass index, and residential zip code median income. Outcomes were five-year incidence rates for alcohol, substance use, depression, and anxiety-related diagnoses.

RESULTS:

Our results indicate that, although receiving opioids during the ED visit predicted a relatively lower likelihood of subsequent substance use and mental health diagnoses, the brief co-use of benzodiazepines was strongly associated with poorer outcomes.

CONCLUSIONS:

Even brief exposure to co-prescribed opioids and benzodiazepines during emergency traumatic injury care may be associated with negative substance use and mental health consequences in the years following the event.

100 Deals associated with Tilidine Hydrochloride

Login to view more data