MEDICAL INTELLIGENCE ARTICLE Dennis M. Fisher, M.D., Editor Anesthesiology 2000; 93:539 – 47 © 2000 American Society of Anesthesiologists, Inc. Lippincott Williams & Wilkins, Inc. Gender Differences in Opioid-mediated Analgesia Animal and Human Studies Benjamin Kest, Ph.D.,* Elise Sarton, M.D.,Albert Dahan, M.D., Ph.D. EXOGENOUSLY administered opioids display marked in- terindividual differences with respect to their intended (analgesia) and unwanted (e.g., respiratory depression, nausea and vomiting) pharmacologic effects. In addition to the well-documented effects of age or development and genetic background, the contribution of gender and hormonal status as factors in opioid potency is becoming increasingly appreciated. We review recent findings on the interaction of sex and opioid analgesic potency and discuss possible mechanisms. Although most of the lit- erature on sex differences in opioid analgesia comes from work with rodents, the available human data also indicate the presence of sex differences. Because opi- oids exert their analgesic effects through -, -, and -opioid receptor (OR) subtypes, each with a unique pharmacology and role in pain control, 1 each OR sub- type is considered separately. In general, progress in the area has been slow. This may reflect the overwhelming use of male subjects to circumvent controlling for estrous or menstrual status or the failure of some researchers to examine their data for sex differences. The lack of consistent sex differences in opioid analgesia may reflect differences in the method- ology (e.g., species, strain and age of subjects, particular nociceptive assay employed, quantification of analgesia) employed by each laboratory. It is beyond the scope of this paper to detail comprehensive methodologic details of all the reports cited in this article. We provide details of some studies in which apparently contradictory or complimentary findings necessitate elaboration. None- theless, findings from the increasing number of well- controlled animal and human studies directly examining the issue of sex in the potency of opioids show that patient sex may impact on the clinical efficacy of opioids for pain. Animal Studies -Opioid Receptor Agonists In rats and mice, the majority of studies report that the potency (i.e., ED 50 values) and efficacy (i.e., drug-in- duced increase in pain response latency) of morphine administered systemically are higher in male than in female animals 2–13 (table 1). The enhanced sensitivity to morphine analgesia displayed by male animals has been documented with several pain assays, including those assessing thermal (hot-plate tests 2,6,9,10,13 ), somatic (tail- flick–withdrawal tests 2,3,5,14 ), chemical (abdominal writhing after acetic acid 2 ), visceral (hypertonic saline 4 ), and electric shock (jump test 14 ) nociception. Studies utilizing central routes of administration suggest that sex differences in opioid analgesia are probably mediated, at * Assistant Professor, Department of Psychology, The College of Staten Island—City University of New York. † Resident, Department of Anesthesiology, Leiden University Medi- cal Center. ‡ Associate Professor, Department of Anesthesiology, Leiden Univer- sity Medical Center. Received from Department of Psychology, The College of Staten Island—City University of New York, Staten Island, New York; and Department of Anesthesiology, Leiden University Medical Center, Lei- den, The Netherlands. Submitted for publication August 26, 1999. Accepted for publication March 23, 2000. Supported solely by institu- tional and/or departmental sources. Address reprint requests to Dr. Kest: Department of Psychology (4S-223), The College of Staten Island—City University of New York, Staten Island, New York 10314. Address electronic mail to: kest@postbox.csi.cuny.edu Individual article reprints may be purchased through the Journal Web site, www.anesthesiology.org Key words: Antinociception; gender; hormones; morphine; pain. 539 Anesthesiology, V 93, No 2, Aug 2000 Downloaded from http://pubs.asahq.org/anesthesiology/article-pdf/93/2/539/408660/0000542-200008000-00034.pdf by guest on 06 November 2021