Page 95 - ITPS-7-3

INNOSC Theranostics

and Pharmacological Sciences

REVIEW ARTICLE
A historical perspective on clonidine as an

alpha-2A receptor agonist in the treatment
of addictive behaviors: Focus on opioid

dependence

5
1
Mark S. Gold , Kenneth Blum 2,3,4,5,6,7,8,9,10,11 * , Abdalla Bowirrat ,
5
Albert Pinhasov , Debasis Bagchi 12,13 , Catherine A. Dennen ,
14
Panayotis K. Thanos 5,15,16 , Colin Hanna 15,16 , Kai-Uwe Lewandrowski 17,18,19 ,
Alireza Sharafshah , Igor Elman 5,21 , and Rajendra D. Badgaiyan 22,23
20
1 Department of Psychiatry, Washington University School of Medicine, St. Louis, Missouri, United
States of America
2 Division of Addiction Research and Education, Center for Sports, Exercise and Global Mental
Health, Western University Health Sciences, Pomona, California, United States of America
3 The Kenneth Blum Behavioral and Neurogenetic Institute LLC, Austin, Texas, United States of
America
4 Department of Psychology, Faculty of Education and Psychology, Institute of Psychology, Eötvös
Loránd University Budapest, Budapest, Hungary
5 Department of Molecular Biology and Adelson School of Medicine, Ariel University, Ariel, Israel
6 Division of Personalized Medicine, Cross-Cultural Research and Educational Institute, San
Clemente, California, United States of America
7 Centre for Genomics and Applied Gene Technology, Institute of Integrative Omics and Applied
*Corresponding author: Biotechnology, Nonakuri, West Bengal, India
Kenneth Blum
(drd2gene@ariel.a.c.il) 8 Department of Clinical Psychology and Addiction, Institute of Psychology, Faculty of Education and
Psychology, Eötvös Loránd University, Budapest, Hungary
Citation: Gold MS, Blum K,
Bowirrat A, et al. A historical
perspective on clonidine as an Abstract
alpha-2A receptor agonist in the
treatment of addictive behaviors: Clonidine operates through agonism at the alpha-2A receptor, a specific subtype
Focus on opioid dependence. of the alpha-2-adrenergic receptor located predominantly in the prefrontal cortex.
INNOSC Theranostics and By inhibiting the release of norepinephrine, which is responsible for withdrawal
Pharmacological Sciences.
2024;7(3):1918. symptoms, clonidine effectively addresses withdrawal-related conditions such
doi: 10.36922/itps.1918 as anxiety, hypertension, and tachycardia. The groundbreaking work by Gold et
Received: September 26, 2023 al. demonstrated clonidine’s ability to counteract the effects of locus coeruleus
stimulation, reshaping the understanding of opioid withdrawal within the field.
Accepted: March 27, 2024
In the 1980s, the efficacy of clonidine in facilitating the transition to long-acting
Published Online: July 29, 2024 injectable naltrexone was confirmed for individuals motivated to overcome opioid
Copyright: © 2024 This is an use disorders (OUDs), including physicians and executives. Despite challenges with
OpenAccess article distributed compliance, naltrexone offers sustained blockade of opioid receptors, reducing the
under the terms of the Creative risk of overdose, intoxication, and relapse in motivated patients in recovery. The
Commons AttributionNoncommercial
License, permitting all non- development of clonidine and naltrexone as treatment modalities for OUDs, and
commercial use, distribution, potentially other addictions, including behavioral ones, underscores the potential for
and reproduction in any medium, translating neurobiological advancements from preclinical models (bench) to clinical
provided the original work is
properly cited. practice (bedside), ushering in innovative approaches to addiction treatment.
Publisher’s Note: AccScience
Publishing remains neutral with Keywords: Behavioral addictions; Clonidine; Opioid use disorder; Substance use disorder;
regard to jurisdictional claims in
published maps and institutional Naltrexone; Locus coeruleus
affiliations.

Volume 7 Issue 3 (2024) 1 doi: 10.36922/itps.1918