Experiences with Hydroxydione

Ditzler, John W.; Dumke, Paul

doi:10.1213/00000539-195711000-00009

Cited by 4 publications

(1 citation statement)

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“…1 ), a water-soluble ester of pregnanedione, was an effective anesthetic. While the onset of anesthesia was delayed in comparison to thiopental sodium, it had a higher therapeutic index (LD 50 /ED 50 ) and was introduced as an anesthetic for humans [ 33 ]. Undesirable side effects including pain on injection, prolonged onset, slow recovery and thrombophlebitis led to the gradual disappearance of hydroxydione from clinical practice [ 34 ].…”

Section: Neurosteroids As Anestheticsmentioning

confidence: 99%

Neurosteroids and their potential as a safer class of general anesthetics

Tateiwa,

Evers

2024

J Anesth

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Neurosteroids (NS) are a class of steroids that are synthesized within the central nervous system (CNS). Various NS can either enhance or inhibit CNS excitability and they play important biological roles in brain development, brain function and as mediators of mood. One class of NS, 3α-hydroxy-pregnane steroids such as allopregnanolone (AlloP) or pregnanolone (Preg), inhibits neuronal excitability; these endogenous NS and their analogues have been therapeutically applied as anti-depressants, anti-epileptics and general anesthetics. While NS have many favorable properties as anesthetics (e.g. rapid onset, rapid recovery, minimal cardiorespiratory depression, neuroprotection), they are not currently in clinical use, largely due to problems with formulation. Recent advances in understanding NS mechanisms of action and improved formulations have rekindled interest in development of NS as sedatives and anesthetics. In this review, the synthesis of NS, and their mechanism of action will be reviewed with specific emphasis on their binding sites and actions on γ-aminobutyric acid type A (GABAA) receptors. The potential advantages of NS analogues as sedative and anesthetic agents will be discussed.

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Section: Neurosteroids As Anestheticsmentioning

confidence: 99%