Buprenorphine and naloxone co-administration in opiate-dependent patients stabilized on sublingual buprenorphine.
Buprenorphine and naloxone sublingual (s.l.) dose formulations may decrease parenteral buprenorphine abuse. We evaluated pharmacologic interactions between 8 mg s.l. buprenorphine combined with 0, 4, or 8 mg of naloxone in nine opiate-dependent volunteers stabilized on 8 mg s.l. buprenorphine for 7 days. Combined naloxone and buprenorphine did not diminish buprenorphine's effects on opiate withdrawal nor alter buprenorphine bioavailability. Opiate addicts stabilized on buprenorphine showed no evidence of precipitated opiate withdrawal after s.l. buprenorphine-naloxone combinations. Buprenorphine and naloxone bioavailability was approximately 40 and 10%, respectively. Intravenous buprenorphine and naloxone produced subjective effects similar to those of s.l. buprenorphine and did not precipitate opiate withdrawal.
Harris
D S
DS
Drug Dependence Research Center, Langley Porter Psychiatric Institute, and Department of Biopharmaceutical Sciences, University of California, San Francisco, 401 Parnassus Avenue, 94143-0984, San Francisco, CA 94143-0984, USA.
Jones
R T
RT
Welm
S
S
Upton
R A
RA
Lin
E
E
Mendelson
J
J
D000286:Administration, Sublingual; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D002047:Buprenorphine / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D009270:Naloxone / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D009292:Narcotic Antagonists / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D009293:Opioid-Related Disorders / Q000534:rehabilitation*; D013997:Time Factors
D009292:Narcotic Antagonists; D009270:Naloxone; D002047:Buprenorphine