Summary
We have studied the pharmacokinetics of the centrally-acting analgesic meptazinol after oral and rectal administration to 15 healthy men. Each subject took a standard 200 mg tablet orally and Witepsol H12 suppositories containing 75, 100, and 150 mg of the drug in a cross-over design.
Meptazinol plasma concentrations were measured by HPLC using fluorescence detection and the pharmacokinetics determined.
The tmax values for the 100 mg and 150 mg suppositories (median =0.5 h) were statistically significantly shorter than for the tablet (median =1.13 h), suggesting that meptazinol was more rapidly absorbed via the rectal route.
Despite substantial intersubject variation in Cmax the plasma concentrations after rectal dosage were higher than after oral administration. There was a statistically significant (p<0.001) improvement in systemic availability for each of the suppository doses (mean approximately 15.5% compared with the oral tablet (mean approximately 4.5%).
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Anderson P, Arner S, Bondesson U, Boreus LO, Hartvig P (1981) Clinical pharmacokinetics of ketobemidone. Its bioavialability after rectal administration. Eur J Clin Pharmacol 19: 217–223
De Boer AG, De Leede LGJ, Breimer DD (1984) Drug absorption by sublingual and rectal routes. Br J Anaesth 56: 69–82
De Leede LGJ, De Boer AG, Havermans JPJM, Breimer DD (1984) Avoidance of “first-pass” elimination of rectally administered propranolol in relation to the site of absorption in rats. Pharm Res 1: 164–168
Ellison NM, Lewis GO (1984) Plasma concentrations following single doses of morphine sulphate in oral solution and rectal suppository. Clin Pharm 3: 614–617
Franklin RA, Southgate PJ, Coleman AJ (1977) Studies on the absorption and disposition of meptazinol following rectal administration. Br J Clin Pharmacol 4: 163–167
Frost T (1981) Determination of meptazinol in plasma by high performance liquid chromatography with fluorescence detection. Analyst 106: 999–1001
Lindahl S, Olsson AK, Thomson D (1981) Rectal premedication in children. Use of diazepam, morphine and hyoscine. Anaesthesia 36: 376–379
Moolenaar F, Yska JP, Visser J, Meijer DKF (1985) Drastic improvement in the rectal absorption profile of morphine in man. Eur J Clin Pharmacol 29: 119–121
Murray GR, Franklin RA, Graham DF, Lewis R, Bolland M (1987) Parental pharmacokinetics of meptazinol in the elderly. Eur J Clin Pharmacol 31: 733–736
Norbury HM, Franklin RA, Graham DF (1983) Pharmacokinetics of the new analgesic meptazinol, after oral and intravenous administration to volunteers. Eur J Clin Pharmacol 25: 77–80
Price RKJ, Latham AN (1982) Double-blind comparison of meptazinol (200 mg) and dextropropoxyphene/paracetamol in a multi-centre general practice setting. Curr Med Res Opin 8: 54–60
Rance MJ, Shillingford JS (1977) The metabolism of phenolic opiates by rat intestine. Xenobiotica 7: 529–536
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Murray, G.R., Petitjean, O., Franklin, R.A. et al. The systemic availability of meptazinol in man after oral and rectal doses. Eur J Clin Pharmacol 36, 279–282 (1989). https://doi.org/10.1007/BF00558160
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00558160