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

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

JP (01 May 1952),

Anesthesia

Regulation-

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Structure

Molecular FormulaC11H18N2NaO2S

InChIKeyPAWYKYXVHHGVOH-UHFFFAOYSA-N

CAS Registry71-73-8

View All Structures (2)

BACKGROUNDSeizures are commonly reported in patients with myelin oligodendrocyte glycoprotein antibody-associated cerebral cortical encephalitis (MOG-CCE). However, seizure management during the acute phase has not been established.CASE REPORTA 9-year-old previously healthy boy presented with fever persisting for approximately 6 days, along with headache and altered consciousness. Plain T2-weighted and fluid-attenuated inversion recovery imaging showed swelling and abnormal hyperintense lesions in the bilateral frontal, parietal, temporal, and insular cortices with left hemisphere predominance. Consciousness disturbance persisted, and focal myoclonic seizures clustered hourly. Seizures were arrested by titrating the thiopental dose but recurred with dose reduction, and the patient exhibited super refractory status epilepticus. Adverse effects due to long-term use of thiopental became apparent. Hence, continuous infusion of ketamine and intrathecal dexamethasone therapy (IT-DEX) was started. After administration of ketamine and IT-DEX, his seizure was arrested promptly. The cerebrospinal fluid and serum at the time of transfer were clear positive for ani-MOG antibody; therefore, the patient was diagnosed with MOG-CCE. The patient received three courses of intravenous methylprednisolone pulse therapy, followed by oral prednisolone gradually tapered over 6 months. He did not experience any relapse for 6 months.CONCLUSIONIn MOG-CCE, some cases may present with super-refractory status epilepticus (SRSE) in the acute phase and be refractory to anti-seizure medication, analogous to febrile infection-related epilepsy syndrome. IT-DEX and continuous infusion ketamine are useful for seizure control in MOG-CCE.

01 Nov 2024·Neuroscience Letters

Phytol exerts sedative-like effects and modulates the diazepam and flumazenil’s action, possibly through the GABAA receptor interaction pathway

Article

Author: Hasan, Md. Sakib Al ; Hasan, Md Sakib Al ; Islam, Md Amirul ; Hasan Bappi, Mehedi ; Hashem, Abu ; Saifuzzaman, Md ; Al Hasan, Md. Sakib ; Islam, Md. Amirul ; Islam, Md. Torequl ; Bappi, Mehedi Hasan ; Ferdous, Jannatul ; Saifuzzaman, Md. ; Islam, Md Torequl ; Ansari, Siddique Akber

This study aimed at the evaluation of the sedative effect of phytol (PHY) with possible molecular mechanisms through in vivo and in silico studies. For this, adult male mice were randomly divided into six individual groups, namely control (vehicle), two standards (DZP: diazepam at 2 m/kg, FLU: flumazenil at 0.1 mg/kg), three test groups (PHY at 25, 50, and 75 mg/kg), and three combined groups with the DZP-2 and/or FLU-0.1 with PHY-75 mg/kg. After thirty minutes, each animal was treated with thiopental sodium (TS) at 40 mg/kg to produce sedation and observed for latency and duration of sleep up to 4 h. In silico studies were performed with the 6X3X protein of the GABA_A receptor α1 and β2 subunits. The results demonstrate that PHY dose-dependently enhanced sleep duration in animals. However, it produced an insignificant sleep duration compared to the control and standard groups. It also significantly (p < 0.05) decreased the latency and increased the duration of sleep with DZP-2, while reducing these parameters with FLU-0.1. In in silico studies, DZP and FLU exhibited binding affinities with 6X3X by -6.8 and -6.9 kcal/mol, respectively, while PHY exhibited -6.9 kcal/mol. Taken together, PHY may exert a sedative-like effect in TS-induced sleeping mice and modulate the effects of DZP and FLU, possibly through interacting with the 6X3X protein of the GABA_A receptor. PHY may be one of the good candidates for the management of sleep disturbances, such as insomnia.

01 Oct 2024·Food and Chemical Toxicology

Diazepam nanocapsules as an alternative for sleep induction: Development study and toxicity assessment

Article

Author: de Morais, Patrícia da Fonseca ; Flores, Victoria Givankliff ; Fraga, Bianca Bordignon ; Betti, Andresa Heemann ; Morisso, Fernando Dal Pont ; Zorzo, Roberta Rodrigues ; Ferreira, Julia Gabriele de Jesus ; Marco, Mariana Roza ; Charão, Mariele Feiffer ; de Mattos, Cristiane Bastos ; Fleck, Juliane Deise

Diazepam (DZP) is a sedative medication prescribed to treat anxiety and as a sleep inducer, although its residual effects are unfavorable to patients. Nanotechnology represents a tool to improve the pharmacological characteristics of drugs, reducing their side effects. This study aimed to develop and characterize DZP nanocapsules and to evaluate their toxicity in alternative models and the hypnotic-sedative effect in mice. Nanocapsules were prepared by the nanoprecipitation method and properly characterized. Long-term and accelerated stability studies were performed. The in vitro release profile was determined by diffusion in Franz cells. The safety of the formulation was evaluated in the Caenorhabditis elegans (C. elegans) and the oral acute toxicity in mice. Pharmacological evaluation was performed using thiopental-induced sleeping time. DZP was successfully incorporated into Poly-(ɛ-caprolactone) (PCL) nanocapsules, with high entrapment efficiency. The nanocapsule did not affect the development or survival of C. elegans, different from the free drug, which affected the nematode development at the higher tested dose. No signs of toxicity, nor body mass or feed consumption changes were observed during the 14 days evaluated. Finally, this innovative formulation carrying DZP can produce a hypnotic-effect at a reduced dose compared to the free drug, with no toxicity in alternative models.

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	JP	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)	kxezwdcyoj(zqpjmvtytd) = hibbirmxba bzakmvjaqz (nbgcgbbzzy, usqhsrllwq - ffksnpmkuf) View more	-	18 May 2017
				Propofol (Propofol)	kxezwdcyoj(zqpjmvtytd) = dywumbcwku bzakmvjaqz (nbgcgbbzzy, gzfrbhytrp - mashtgxjmc) View more
NCT00767767 (CTgov)	Not Applicable	Phobic Disorders	67	Placebos (Placebos)	qxhfgmjpzv(glagzcembc) = ysohhvxoch joyohufoqa (mnnnmcrepl, hxiujhecsd - cnonmfoewi) View more	-	10 Apr 2017
				Propofol 0.45mcg/mL (Propofol 0.45mcg/mL)	qxhfgmjpzv(glagzcembc) = mzpmjbyxiq joyohufoqa (mnnnmcrepl, nrsqyjwfqk - obwnrjblmh) View more
EAN	Not Applicable	-	33	Midazolam	qynfzshjrg(imnlxxiwks) = sonpzgaoid ofdfumjlud (ubblncqyfo ) View more	Positive	23 Jun 2016
				Thiopental	qynfzshjrg(imnlxxiwks) = gxefrsnpcw ofdfumjlud (ubblncqyfo ) View more
NCT02377778 (Pubmed \| Reprod Biomed Online)	Phase 4	-	180	Propofol	jygxxedhqv(qpivfzgkax) = yjvavuuvjj epvlorcafb (msyojvvzwb )	-	01 Dec 2015
				Thiopental sodium	jygxxedhqv(qpivfzgkax) = rmkoedbiwl epvlorcafb (msyojvvzwb )
NCT01495949 (Pubmed)	Phase 4	-	26	Etomidate	hhkmemxemy(rxitsjwemn) = vmldezsxed bqaxtxkjri (qbtpjnwhtm )	-	01 Aug 2015
				Thiopentone	hhkmemxemy(rxitsjwemn) = vlwnpgybua bqaxtxkjri (qbtpjnwhtm )
PACTR201306000536344 (Pubmed \| BMC Anesthesiol)	Not Applicable	-	150	Propofol	evkmrmxcbq(wiwehtbwzg) = xtvshutbql zagdefucra (jglafmbeih )	-	29 Apr 2015
				Thiopental	evkmrmxcbq(wiwehtbwzg) = slnlqnchoe zagdefucra (jglafmbeih )