Delving into the Latest Updates on Thiopental Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(±)-thiopental, 2-Thio-5-ethyl-5-sec-pentylbarbituric acid, 5-Ethyl-5-(1-methyl-butyl)-2-thioxo-dihydro-pyrimidine-4,6-dione

+ [12]

Target

GABAA receptor

Action

agonists

Mechanism

GABAA receptor agonists(Gamma-aminobutyric acid A receptor agonists)

Therapeutic Areas

Other Diseases

Active Indication

Anesthesia

Inactive Indication-

Originator Organization

Nipro ES Pharma KK

Active Organization

Nipro ES Pharma KK

Inactive Organization

Abbott Laboratories

Drug Highest PhaseApproved

First Approval Date

Japan (01 May 1952),

Anesthesia

Regulation-

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Structure/Sequence

Molecular FormulaC11H18N2NaO2S

InChIKeyPAWYKYXVHHGVOH-UHFFFAOYSA-N

CAS Registry71-73-8

View All Structures (2)

SummaryIntroductionAcute kidney injury develops frequently after nephrectomy, causing increased hospital duration of stay and mortality. Both propofol and volatile anaesthetic agents are thought to have renoprotective effects. We investigated whether the type of maintenance anaesthetic (propofol or desflurane) affected the incidence of acute kidney injury after nephrectomy.MethodsThis single‐centre, randomised controlled trial enrolled adult patients with renal cell carcinoma undergoing nephrectomy. In patients allocated to the propofol group, anaesthesia was induced and maintained using a target‐controlled infusion of propofol. In patients allocated to the desflurane group, anaesthesia was induced with a bolus of thiopental and maintained with desflurane. Both groups received a target‐controlled infusion of remifentanil during surgery. The primary outcome was the incidence of acute kidney injury within 7 postoperative days based on the serum creatinine component of the Kidney Disease: Improving Global Outcomes criteria.ResultsWe analysed 317 patients (median (IQR [range]) age 62 (52–70 [26–85] y); 221 (70%) men). Postoperative AKI developed in 79 (25%) patients: 43 (27%) in the propofol group and 36 (23%) in the desflurane group (absolute risk difference (95%CI) 4.6 (‐4.9–14.0%), p = 0.347). The severity of kidney injury was stage 1 in 76 patients, stage 2 in two patients and stage 3 in one patient.DiscussionThe type of anaesthetic maintenance drug (propofol vs. desflurane) did not affect the incidence of acute kidney injury after nephrectomy. Future research might be better directed towards investigating other potentially modifiable risk factors for postoperative acute kidney injury in this patient population.

01 Feb 2025·European Journal of Pharmacology

Preclinical and in silico studies of 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methylthiourea: A promising agent for depression and anxiety

Article

Author: Khan, Ashraf Ullah ; Alam, Waqas ; Ali Shah, Syed Wadood ; Khan, Haroon ; Ali, Usman ; Badshah, Haroon ; Aschner, Michael ; Darwish, Hany W

The study investigated the anxiolytic, antidepressant, sedative/hypnotic and in silico molecular docking properties of the synthetic ephedrine-based derivative of thiourea, 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methylthiourea. Safety profile of the compound at various doses was determined in an acute toxicity test. Results showed significant anti-anxiety effects of the compound in all mice studies. In the elevated plus maze (EPM), the time spent and entries into open arms were significantly increased upon treatment with the test compound. In the light-dark (LD) box test the drug increased the time spent in the light compartment. In hole board (HB) assay, exploration of hole and rearing significantly increased. For anxiolytic activity, 20 mg/kg was determined to represent the optimal dose, while at a higher dose (i.e., 40 mg/kg), it caused significant sedation and increased sleep duration in thiopental-induced sleep test. Escape latency in the tail suspension test (TST) and in the forced swim test (FST) increased and immobility was significantly reduced upon 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methylthiourea administration. The molecular docking analysis was performed against the various protein target involved in the pathogenesis of anxiety. The molecular docking, molecular dynamic (MD) simulation and free energy calculation showed high binding affinity and stability of ligand with the 7VOD and 2C65 protein. Taken together, it is concluded from both the in vivo assays and molecular modeling studies that 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methylthiourea possesses significant anxiolytic and antidepressant activity in concomitant with a high safety profile.

01 Feb 2025·Journal of Electroanalytical Chemistry

Electrochemically controlled release and online monitoring of thiopental drug based on conducting polymer coated on a soft substrate surface: Relation between release rate and electrical potential stimulation

Author: Badvi, Hoda ; Alizadeh, Naader

Drug delivery systems (DDS) that utilize elec. stimuli are gaining significant attention due to their ability to precisely adjust elec. signals.This study investigated the release of thiopental using a coated biodegradable conductive polymer on a soft substrate for controlled drug release.Elec. potential and temperature were applied to assess the release rate of thiopental from a coated soft substrate surface (carbon felt).The drug release profile was monitored in real-time through a combination of spectrometry and electrochem. methods.The results demonstrated that increasing the applied elec. potential significantly enhanced the drug release rate.Furthermore, the activation free energy for the drug release, in relation to the applied elec. potential, was accurately modeled using a math. equation that incorporates both the Butler-Volmer and Eyring equations.This designed system allows for control of drug release from the soft substrate at a low potential (-0.8 V), making it suitable for clin. applications, such as transdermal delivery.

100 Deals associated with Thiopental Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D00714	Thiopental Sodium	N01AF03 N05CA19	DB00599

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	Japan	Nipro ES Pharma KK	01 May 1952

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00504894 (Amygdala, CTgov)	Phase 4	-	60	Placebo (Placebo)	jdtotzmxtx(bvoatplvfy) = zdmcmvgiom eaulfjbjbm (zvuoeapjxk, worgayugyg - jfhrluvdxw) View more	-	18 May 2017
				Propofol (Propofol)	jdtotzmxtx(bvoatplvfy) = iqqvvkqigu eaulfjbjbm (zvuoeapjxk, livmhtgavu - oiqiqldnsu) View more
NCT00767767 (CTgov)	Not Applicable	Phobic Disorders	67	Placebos (Placebos)	mfjhdzspmv(plirfydyfj) = smbahjoqqd jtazlmqqrx (qarvrgdflq, leldzxkztl - xecqitixjr) View more	-	10 Apr 2017
				Propofol 0.45mcg/mL (Propofol 0.45mcg/mL)	mfjhdzspmv(plirfydyfj) = iwkvlxmpvj jtazlmqqrx (qarvrgdflq, zohojcmcbb - xpvgdmuzhg) View more
EAN2016	Not Applicable	Status Epilepticus	33	Midazolam	voaatwqvhi(xqwydykyqa) = wsdfrgnzfe yqinbhlunb (raavgjivyd ) View more	Positive	23 Jun 2016
				Thiopental	voaatwqvhi(xqwydykyqa) = ucqvxlhele yqinbhlunb (raavgjivyd ) View more
NCT02377778 (Pubmed \| Reprod Biomed Online)	Phase 4	-	180	Propofol	ijycyfdlcx(hgggbjbkwk) = sbbotxrgyp govaigogva (shadymdaqt )	-	01 Dec 2015
				Thiopental sodium	ijycyfdlcx(hgggbjbkwk) = ezomodvhtb govaigogva (shadymdaqt )
NCT01495949 (Pubmed)	Phase 4	-	26	Etomidate	dpigqahhcl(tmgqvyxslj) = ngzfflqwmb bfmagetums (sgyeyptfzc )	-	01 Aug 2015
				Thiopentone	dpigqahhcl(tmgqvyxslj) = zihvbhanxj bfmagetums (sgyeyptfzc )
PACTR201306000536344 (Pubmed \| BMC Anesthesiol)	Not Applicable	-	150	Propofol	hoxemgcfkg(fyuahvqiyh) = jrxwdpsxar ermtyavovp (hgibbfrjjm )	-	29 Apr 2015
				Thiopental	hoxemgcfkg(fyuahvqiyh) = sgtgdstwfe ermtyavovp (hgibbfrjjm )