Sublingual absorption of selected opioid analgesics

Title

Sublingual absorption of selected opioid analgesics

Creator

Weinberg DS; Inturrisi CE; Reidenberg B; Moulin DE; Nip TJ; Wallenstein S; Houde RW; Foley KM

Publisher

Clinical Pharmacology And Therapeutics

Date

1988

Subject

Humans; Adult; Analgesics; Time Factors; Analysis of Variance; Non-U.S. Gov't; P.H.S.; Research Support; U.S. Gov't; Comparative Study; Administration; Biological Availability; Buprenorphine/pharmacokinetics; Fentanyl/pharmacokinetics; Heroin/pharmacokinetics; Hydromorphone/pharmacokinetics; Levorphanol/pharmacokinetics; Methadone/pharmacokinetics; Morphine/blood/pharmacokinetics; Mouth/metabolism; Naloxone/pharmacokinetics; Opioid/administration & dosage/pharmacokinetics; Oxycodone/pharmacokinetics; Sublingual

Description

Ongoing interest in the improvement of pain management with opioid analgesics had led to the investigation of sublingual opioid absorption. The present report determined the percent absorption of selected opioid analgesics from the oral cavity of normal subjects under conditions of controlled pH and swallowing when a 1.0 ml aliquot of the test drug was placed under the tongue for a 10-minute period. Compared with morphine sulfate at pH 6.5 (18% absorption), buprenorphine (55%), fentanyl (51%), and methadone (34%) were absorbed to a significantly greater extent (p less than 0.05), whereas levorphanol, hydromorphone, oxycodone, heroin, and the opioid antagonist naloxone were not. Overall, lipophilic drugs were better absorbed than were hydrophilic drugs. Plasma morphine concentration-time profiles indicate that the apparent sublingual bioavailability of morphine is only 9.0% +/- 11.9% (SD) of that after intramuscular administration. In the same subjects the estimated sublingual absorption was 22.4% +/- 9.2% (SD), indicating that the sublingual absorption method may overestimate apparent bioavailability. When the oral cavity was buffered to pH 8.5, methadone absorption was increased to 75%. Thus, an alkaline pH microenvironment that favors the unionized fraction of opioids increased sublingual drug absorption. Although absorption was found to be independent of drug concentration, it was contact time dependent for methadone and fentanyl but not for buprenorphine. These results indicate that although the sublingual absorption and apparent sublingual bioavailability of morphine are poor, the sublingual absorption of methadone, fentanyl, and buprenorphine under controlled conditions is relatively high.
1988

Rights

Article information provided for research and reference use only. PedPalASCNET does not hold any rights over the resource listed here. All rights are retained by the journal listed under publisher and/or the creator(s).

Type

Journal Article

Citation List Month

Backlog

Pages

335-342

Issue

3

Volume

44

Citation

Weinberg DS; Inturrisi CE; Reidenberg B; Moulin DE; Nip TJ; Wallenstein S; Houde RW; Foley KM, “Sublingual absorption of selected opioid analgesics,” Pediatric Palliative Care Library, accessed October 19, 2021, https://pedpalascnetlibrary.omeka.net/items/show/12510.

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