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

License Organization-

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)

The citrus peel flavonoid tangeretin (TAN) has diverse biological activities, including antioxidant, anti-inflammatory, antitumor, hepatoprotective, and neuroprotective effects. This study investigates the sedative effects of TAN, in Swiss albino mice using in vivo and in silico approaches. TAN (10 and 20 mg/kg, i.p.) was administered alone and in combination with diazepam (DZP, 2 mg/kg, i.p.) and flumazenil (FLU, 0.1 mg/kg, i.p.) to evaluate its impact on thiopental sodium (TS)-induced sleep, locomotor activity, and dark-light behavior. Results demonstrated that TAN at 10 mg/kg significantly (p < 0.05) reduced sleep onset latency and increased sleep duration, with a synergistic effect observed when combined with DZP. In locomotor activity tests, TAN dose-dependently decreased the distance traveled, while the combination with DZP further enhanced this effect. Dark-light tests revealed that TAN increased dark residence time, indicating potential anxiolytic properties. Molecular docking studies showed that TAN binds to the GABA_A receptor (α1 and β2 subunits) with a binding affinity of -6.6 kcal/mol, suggesting its interaction with GABAergic pathways. Pharmacokinetic analysis indicated high intestinal absorption and compliance with Lipinski's rule of five, with a favorable safety profile (LD₅₀ = 5000 mg/kg). Overall, TAN enhances the sedative effects of DZP through GABA_A receptor modulation, highlighting its potential as a natural sedative agent. Further research should explore the long-term effects, bioavailability, blood-brain barrier permeability, and synergistic interactions of TAN, with comprehensive in vitro studies and clinical trials needed to validate its potential as a natural sedative.

01 Apr 2025·Pediatric Neurology

Challenges in Management of Febrile Infection-Related Epilepsy Syndrome: Real-World Experience From a Large Cohort of Pediatric Patients

Article

Author: Kannoth, Sudheeran ; Konanki, Ramesh ; Bandi, Ramya ; Sharma, Ravi ; Lingappa, Lokesh ; Jain, Vivek

BACKGROUNDFebrile infection-related epilepsy syndrome (FIRES) is a catastrophic neuroinflammatory disorder with refractory status epilepticus. The disease management continues to pose significant challenges.METHODSA retrospective observational study of patients with FIRES managed at tertiary care centers in India. The follow-up outcome was assessed using the Clinical Assessment Scale in Autoimmune Encephalitis (CASE).RESULTSForty-one children (27 males) were eligible. The mean presentation age was 7.2 years (range, 2-14). A median of 7 (range, 2-12) antiseizure medications (ASMs) were tried before pharmacologic coma, which was subsequently required in all patients. The pharmacologic coma was induced for a median duration of 11 days (range, 1-125), with midazolam (41) being the most common medication, followed by ketamine (33), thiopentone (18), and isoflurane (13). Only a minority had seizure resolution on pharmacologic coma (ketamine 21%, midazolam 17%, and thiopentone 16.6%). Ninety-seven percent children also concurrently received methylprednisolone (40), 63% intravenous immunoglobulin (26), 32% rituximab (13), 32% cyclophosphamide (13), and 56% ketogenic diet (23). At a median follow-up of 37 months (range, 9-96), 34% (14) children had died. Of the remaining 27, epilepsy was poorly controlled in the majority (18 children, 67%). Also, 14 patients had a CASE score of ≤5 (good outcome) and 13 had a score of >5 (poor outcome). In both groups, there was no statistically significant difference in outcomes with the ketogenic diet, pharmacologic coma, or immunomodulatory therapies.CONCLUSIONSThe management of FIRES in children is challenging, with limited effectiveness of most currently practiced anesthetic agents and conventional immunomodulatory therapies in seizure control and in altering the outcome in FIRES.

01 Apr 2025·DEN Open

The effectiveness of a body positioning device for controlling patient movement and additional sedative use during endoscopic retrograde cholangiopancreatography: A retrospective analysis

Article

Author: Masuda, Haruka ; Matsumoto, Kengo ; Hayashi, Shiro ; Yamamoto, Masashi ; Nakamatsu, Dai ; Nishida, Tsutomu

AbstractBackgroundEndoscopic retrograde cholangiopancreatography requires precise body movement control for procedural safety and efficiency. Sedatives are commonly used but pose risks, especially in elderly patients. This study evaluated the effectiveness of the Medo V‐Fix device in controlling patient movement during endoscopic retrograde cholangiopancreatography.MethodsOf 1723 endoscopic retrograde cholangiopancreatography procedures performed between January 2021 and March 2024, 1,528 were analyzed after excluding cases with missing data. Patients were divided into two groups, the device group (n = 697) and the nondevice group (n = 831). The groups were compared with respect to body movement control, additional sedative administration, sedation‐related complications, and procedure discontinuation.ResultsBaseline characteristics were similar between the groups. Body movement control was better with the device (good, 65.7%; poor, 24.0%; and very poor, 10.3%) than without it (good, 48.1%; poor, 30.7%; and very poor, 21.2%; p < 0.0001). The device reduced the need for manual assistance and additional sedatives. Fewer patients in the device group (9.5% vs. 15.6%, p = 0.0003) required an additional thiopental dose, and the dose was lower (4.5 mg vs. 6 mg, p = 0.0015). No procedure discontinuation occurred in the device group, whereas five discontinuations occurred in the nondevice group. Although hypoxemia was more frequent in the device group (14.5% vs. 8.8%, p = 0.0005), no severe adverse events occurred.ConclusionsThe Medo V‐Fix device significantly improved body movement control and reduced the need for additional doses of sedatives and manual intervention. Despite a higher incidence of mild hypoxemia, these events were appropriately managed with routine monitoring, indicating that the device increases procedural safety and efficiency.

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)	bldzhifnmf(mslvrprrlt) = rbrdybhvhc ryfeymitrt (ayaiauaocq, hotnkcyufs - ohtjyfwpsi) View more	-	18 May 2017
				Propofol (Propofol)	bldzhifnmf(mslvrprrlt) = xfazvtgvyh ryfeymitrt (ayaiauaocq, urjsobkced - vgefshbwrk) View more
NCT00767767 (CTgov)	Not Applicable	Phobic Disorders	67	Placebos (Placebos)	fowjsnspgm(aeprjxtsmu) = zxybjijqrh wugrhlfyqy (npyxujdiih, vdnlkatvla - yfbxkutnzo) View more	-	10 Apr 2017
				Propofol 0.45mcg/mL (Propofol 0.45mcg/mL)	fowjsnspgm(aeprjxtsmu) = oxyonvjacl wugrhlfyqy (npyxujdiih, nlkzlcumov - ubetnoijah) View more
EAN2016	Not Applicable	Status Epilepticus	33	Midazolam	azwkzvhdzm(devzxotyvg) = nmtivznimu fjofjdzgrl (gsrstdezqw ) View more	Positive	23 Jun 2016
				Thiopental	azwkzvhdzm(devzxotyvg) = gxpqbohntf fjofjdzgrl (gsrstdezqw ) View more
NCT02377778 (Pubmed \| Reprod Biomed Online)	Phase 4	-	180	Propofol	wvqnobpfqo(unttglguyy) = lxbldmxafm ibzvigjfeq (zhxfasvvpn )	-	01 Dec 2015
				Thiopental sodium	wvqnobpfqo(unttglguyy) = xenwytjoqg ibzvigjfeq (zhxfasvvpn )
NCT01495949 (Pubmed)	Phase 4	-	26	Etomidate	eosticeaiq(mhcyjysyxf) = pmvnefqfpf ewbiqcknzz (wdtsdjyfhz )	-	01 Aug 2015
				Thiopentone	eosticeaiq(mhcyjysyxf) = xybsavaikb ewbiqcknzz (wdtsdjyfhz )
PACTR201306000536344 (Pubmed \| BMC Anesthesiol)	Not Applicable	-	150	Propofol	byeeadskcg(ooudfowedb) = mfizdvohio qtzyvjljvm (ttnkvskkwv )	-	29 Apr 2015
				Thiopental	byeeadskcg(ooudfowedb) = whsoljfokc qtzyvjljvm (ttnkvskkwv )