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Pathway Description
Thiopental Action Pathway
Homo sapiens
Drug Action Pathway
Thiopental is a barbiturate utilized for inducing general anesthesia, managing convulsions, and reducing intracranial pressure. Administered intravenously, this barbiturate is employed to induce general anesthesia promptly, achieve temporary complete anesthesia, induce hypnosis, and control convulsive conditions. Notably, it has been employed in neurosurgical contexts to alleviate elevated intracranial pressure. Although it lacks excitatory effects, its analgesic and muscle relaxant properties are limited. It has been shown that low doses can counteract analgesia and lower the pain threshold. Thiopental finds application as the sole anesthetic for brief procedures, as an induction agent preceding other anesthetics, to supplement regional anesthesia, to provide hypnosis alongside other agents for analgesia or muscle relaxation, for managing convulsions during inhalation or local anesthesia, in neurosurgical cases with heightened intracranial pressure, and for narcoanalysis and narcosynthesis in psychiatric disorders. Functioning as an ultrashort-acting central nervous system depressant, thiopental induces rapid hypnosis and anesthesia, yet it lacks analgesic properties. Its binding to a specific site linked to a Cl- ionopore at the GABAA receptor extends the opening duration of the ionopore, thereby prolonging GABA's inhibitory effect in the thalamus. This results in prolonged post-synaptic inhibition. The drug's rapid binding to fatty tissues leads to anesthetic accumulation, producing prolonged effects due to gradual drug release.
References
Thiopental Pathway References
Wishart DS, Feunang YD, Guo AC, Lo EJ, Marcu A, Grant JR, Sajed T, Johnson D, Li C, Sayeeda Z, Assempour N, Iynkkaran I, Liu Y, Maciejewski A, Gale N, Wilson A, Chin L, Cummings R, Le D, Pon A, Knox C, Wilson M: DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. doi: 10.1093/nar/gkx1037.
Pubmed: 29126136
Morgan DJ, Blackman GL, Paull JD, Wolf LJ: Pharmacokinetics and plasma binding of thiopental. II: Studies at cesarean section. Anesthesiology. 1981 Jun;54(6):474-80
WINTERS WD, SPECTOR E, WALLACH DP, SHIDEMAN FE: Metabolism of thiopental-S35 and thiopental-2-C14 by a rat liver mince and identification of pentobarbital as a major metabolite. J Pharmacol Exp Ther. 1955 Jul;114(3):343-5
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