Medicinal chemistry of Thiamylal Sodium

Introduction : Thiamylal Sodium belongs to the group of Anesthetics particularly General Anesthetics as Intravenous Anesthetics.. Descrip...

Introduction:
Thiamylal Sodium belongs to the group of Anesthetics particularly General Anesthetics as Intravenous Anesthetics..

Description 
It is an ultra-short acting barbiturate mainly used for intravenous anaesthesia in conditions of comparatively short-duration. It is also effective for the termination of convulsions of unknown origin.

A barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. (From Martindale, The Extra Pharmacopoeia, 30th ed, p919)

Categories

• Hypnotics and Sedatives
• GABA Modulators
• Anesthetics, Intravenous

Analysis

sodium 5-allyl-4,6-dioxo-5-(pentan-2-yl)-1,4,5,6-tetrahydropyrimidine-2-thiolate
Chemical Formula: C12H17N2NaO2S
Exact Mass: 276.09
Molecular Weight: 276.33
m/z: 276.09 (100.0%), 277.09 (14.5%), 278.09 (4.7%), 278.10 (1.2%)
Elemental Analysis: C, 52.16; H, 6.20; N, 10.14; Na, 8.32; O, 11.58; S, 11.60

Pharmacology of Thiamylal Sodium

Indication	Used for the production of complete anaesthesia of short duration, for the induction of general anaesthesia, and for inducing a hypnotic state.
Pharmacodynamics	Thiamylal, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia.
Mechanism of action	Thiamylal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

Structure and Synthesis of Thiamylal Sodium