Preliminary Study of a Pregnanolone Emulsion (Kabi 2213) for I.V. Induction of General Anaesthesia

Abstract

Pregnanolone emulsion was administered i.v. to 13 healthy male volunteers to assess its potential as an agent for i.v. induction of general anaesthesia and to establish a pharmacokinetic profile at two doses. Each subject received 0.5 mg kg-1, 0.75 mg kg-1 and 1.0 mg kg-1 on successive occasions, the rate of administration being constant for each dose. Pregnanolone emulsion was found to produce smooth and reliable induction of general anaesthesia with cardiorespiratory effects comparable to those of other i.v. induction agents.

Preparation, Characterization, and Anesthetic Properties of 2-Hydroxypropyl-β-cyclodextrin Complexes of Pregnanolone and Pregnenolone in Rat and Mouse

“…[42][43][44] Solubility Studies--Two types of solubility trials were conducted. In the first, the solubility of pregnanolone and pregnenolone was determined using various aqueous solutions of HPPCD (5,10,20,25,30,40, and 50% w/v). In these studies, the cyclodextrin solutions were prepared using 18.6 8 deionized water (Barnsted Nanopure I1 Ultrapure Water systems).…”

Insight into the Mechanism of Action of Neuroactive Steroids

“…In vivo, NSs seem to play an important role in the establishment of mood and behavior states. In the clinical setting, administration of NSs can produce a dosedependent graded effect upon the function of the CNS that ranges from sedation to induction of anesthesia (Purdy et al, 1991;Gray et al, 1992;Frye and Duncan, 1994;Romeo et al, 1998;Girdler et al, 2001;Mellon and Griffin, 2002). NSs mediate their effect by targeting membrane-embedded proteins known as ligand-gated ion channels and thereby alter synaptic transmission within the CNS.…”

Ventilatory effects of eltanolone during induction of anaesthesia: comparison with propofol and thiopentone

“…Using eltanolone 0.75 mg kg 91 we found that 30 % of patients were apnoeic for greater than 30 s, with 13 % being apnoeic for more than 60 s. This is a greater incidence than reported by many earlier authors [6,7,15,16] but, except for one study [16], smaller doses of eltanolone were used. After a prior dose of fentanyl, and a dose of 0.59-0.89 mg kg 91 , given over a range of times, Myint, Peacock and Reilly [12] reported that 37 % of their patients were apnoeic for more than 30 s. All patients studied by Kallela and colleagues [17] using eltanolone 0.8 mg kg 91 were apnoeic for more than 60 s, probably because of the generous dose of alfentanil given before induction.…”