Reference

Studies on the absorption and disposition of meptazinol following rectal administration

Studies on the absorption and disposition of meptazinol following rectal administration. Franklin, R. A.; Southgate, P. J.; Coleman, A. J. (Wyeth Lab., Maidenhead/Berkshire, Engl.). Br. J. Clin. Pharmacol., 4(2), 163-7 (English) 1977. CODEN: BCPHBM. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Rectal administration of the new analgesic drug, meptazinol-HCl (I) [59263-76-2], resulted in rapid absorption of the compd. both in the monkey and in man. Peak plasma levels were obsd. within 0.5 h of dosing. Absorption of the drug following rectal administration was extensive as shown by the recovery of 65-90% of the dose in the urine. Despite substantial inter-individual variation in the obsd. max. plasma concns. of the drug, it was still evident that concns. after rectal dosage were considerably higher than when the same dosage was given orally. Elimination of the drug from plasma took place rapidly in an apparently mono-exponential manner in both species. The half-life of elimination in monkeys was 1.25 h and in man 2.0 h.

Meptazinol and derivatives

Meptazinol and derivatives. Buxade Vinas, Antonio (Laboratorios Vinas S. A., Spain). Span. 105734-86-9 and 59263-76-2 are cas registry numbers. These chemicals are also mentioned in this article. ES 541065 A1 16 Nov 1985, 9 pp. (Spain) CODEN: SPXXAD. CLASS: ICM: C07D223-04. ICS: A61K031-55. APPLICATION: ES 85-541065 8 Mar 1985. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1 Hexahydroazepines I (R1 and R2 are alkyl; R3 = H, aroyl) were prepd., and they are useful as analgesics (no data). A 2,2-disubstituted cyclohexanone was treated with NaN3 and H2SO4, and the e-caprolactam deriv. obtained was successively N-methylated, reduced by LiAlH4, and treated with 2N HCl to give I (R1 = Me, R2 = Et, R3 = H) (Meptazinol). .