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The bioavailability of rectally administered morphine.

T Jonsson1, C B Christensen, H Jordening

  • 1Department of Anaesthesia, Finsen Institute, Denmark.

Pharmacology & Toxicology
|April 1, 1988
PubMed
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Rectal morphine administration offers 53.3% bioavailability, avoiding first-pass metabolism. This study tracked plasma morphine levels for 24 hours, showing potential for alternative drug delivery.

Area of Science:

  • Pharmacology
  • Clinical Pharmacy
  • Drug Metabolism

Background:

  • Morphine is a potent opioid analgesic.
  • Intravenous administration provides rapid but potentially high first-pass metabolism.
  • Alternative routes for morphine administration are being explored to optimize therapeutic outcomes.

Purpose of the Study:

  • To determine the bioavailability of morphine following rectal administration.
  • To compare plasma morphine concentrations after intravenous and rectal routes.
  • To investigate the potential for avoiding first-pass elimination of morphine via rectal delivery.

Main Methods:

  • Eight patients received 10 mg of morphine chloride intravenously and rectally.
  • Plasma morphine concentrations were measured over 24 hours using radioimmunoassay.

Related Experiment Videos

  • A validated extraction procedure separated morphine from its metabolites.

    • Main Results:

    • Rectal morphine administration yielded a bioavailability of 53.3% +/- 17.8%.
    • Peak plasma concentrations (16.3 +/- 8.7 ng/mL) were achieved at 59 +/- 16 minutes post-rectal administration.
    • Radioimmunoassay demonstrated significant plasma morphine levels over the 24-hour period.

    Conclusions:

    • Rectal administration of morphine provides significant bioavailability.
    • This route may partially circumvent the hepatic first-pass effect associated with oral morphine.
    • Rectal morphine presents a viable alternative route for opioid analgesia.