235. Alfaxalone

Nomenclature

CAS number: 23930-19-0
(3α,5α)-3-Hydroxypregnane-11,20-dione; alphaxalone; GR-2/234.
C21H32O3; mol wt 332.48.
C 75.86%, H 9.70%, O 14.44%.

Description and references

Prepn: Nagata et al., Helv. Chim. Acta 42, 1399 (1959); Browne, Kirk, J. Chem. Soc. C 1969, 1653; Davis et al., DE 2030402; ZA 7003861 (both 1971 to Glaxo), C.A. 75, 20793n, 64114w (1971). Mass spectral data: Ende, Spiteller, Monatsh. Chem. 102, 929 (1971). Review of pharmacology and clinical efficacy of mixture with alfadolone acetate, q.v.: Postgrad. Med. J. 48, Suppl. 2, 1-139 (1972). See also Child et al.; Campbell et al.; Br. J. Anaesth. 43, 2-24 (1971); Lancet 1, 888 (1972). Pharmacology and toxicity data: M. I. Al-Khawashki et al., J. Egypt. Med. Assoc. 62, 191 (1979).

Chemical structure

Properties

Colorless prisms from ether, mp 172-174°. [α]D26 +113.4° (c = 1.2 in chloroform). LD50 i.v. in mice: 43 mg/kg (Al-Khawashki).

Derivative

Mixture with alfadolone acetate.

Nomenclature

CAS number: 8067-82-1
Alphadione; alfadione; CT-1341; Alfatésin (Glaxo); Althesin (Glaxo); Saffan (Mallinckrodt).

Properties

LD50 in mice (mg/kg): 140 i.p., 47 i.v. (Al-Khawashki).

Therapeutic Category

Combination with alfadolone acetate as anesthetic (intravenous).

Therapeutic Category (Veterinary)

Combination with alfadolone acetate as anesthetic (intravenous).

Keywords

Anesthetic (Intravenous)