scholarly journals Is Kratom the New ‘Legal High’ on the Block?: The Case of an Emerging Opioid Receptor Agonist with Substance Abuse Potential

2017 ◽  
Vol 1 (21;1) ◽  
pp. E195-E198 ◽  
Author(s):  
George C. Chan ge Chien
Keyword(s):  
Substance Abuse ◽  
Chronic Pain ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
Abuse Potential ◽  
Herbal Extract ◽  
Opioid Overdose ◽  
Opioid Receptor Agonist ◽  
Chronic Pain Patients ◽  
Pain Patients

Kratom is an unscheduled herbal extract that contains alkaloids with opioid receptor agonist activity. It is currently available in the form of dietary supplements and is used and abused by chronic pain patients on prescription opioids. Active alkaloids isolated from Kratom such as mitragynine and 7-hydroxymitragynine are thought to act on mu and delta opioid receptors as well as alpha 2 adrenergic and 5-HT2A receptors. Animal studies suggest that Kratom may be more potent than morphine. Consequently, Kratom consumption produces analgesic and euphoric feelings among users. Some chronic pain patients on opioids take Kratom to counteract the effects of opioid withdrawal. Although the Food and Drug Administration has banned its use as a dietary supplement, Kratom continues to be widely available and easily accessible on the internet at much lower prices than other opioid replacement therapies like buprenorphine. There are no Federal regulations monitoring the sale and distribution of this substance. Consumption of Kratom has been associated with hallucination, delusion, depression, myalgia, chill, nausea/vomiting, respiratory depression, hepatotoxicity, seizure, coma and death. A search of the pain literature shows past research has not described the use and potential deleterious effects of this extract. Many pain physicians are not familiar with Kratom. As providers who take care of high-risk chronic pain patients using prescribed opioids, knowledge of all current substances with opioid receptor agonists with abuse potential is of paramount importance. The goal of this article is to introduce Kratom to pain specialists and identify issues for further studies that will be required to help better understand the clinical and long-term effects of Kratom use among chronic pain patients. Key words: Opioid receptor agonist, Kratom, Mitragynine, opioid overdose, chronic pain, substance abuse :

Does co-administration of paroxetine change oxycodone analgesia: An interaction study in chronic pain patients

2010 ◽  
Vol 1 (1) ◽  
pp. 24-33 ◽  
Author(s):  
K.K. Lemberg ◽  
T.E. Heiskanen ◽  
M. Neuvonen ◽  
V.K. Kontinen ◽  
P.J. Neuvonen ◽  
...  
Keyword(s):  
Chronic Pain ◽  
Adverse Effects ◽  
Opioid Receptor ◽  
Placebo Administration ◽  
Rescue Analgesia ◽  
Analgesic Effects ◽  
Patient Reported ◽  
Chronic Pain Patients ◽  
Μ Opioid Receptor ◽  
Pain Patients

AbstractOxycodone is a strong opioid and it is increasingly used in the management of acute and chronic pain. The pharmacodynamic effects of oxycodone are mainly mediated by the μ-opioid receptor. However, its affinity for the μ-opioid receptor is significantly lower compared with that of morphine and it has been suggested that active metabolites may play a role in oxycodone analgesia. Oxycodone is mainly metabolized by hepatic cytochrome (CYP) enzymes 2D6 and 3A4. Oxycodone is metabolized to oxymorphone, a potent μ-opioid receptor agonist by CYP2D6. However, CYP3A4 is quantitatively a more important metabolic pathway. Chronic pain patients often use multiple medications. Therefore it is important to understand how blocking or inducing these metabolic pathways may affect oxycodone induced analgesia. The aim of this study was to find out whether blocking CYP2D6 would decrease oxycodone induced analgesia in chronic pain patients.The effects of the antidepressant paroxetine, a potent inhibitor of CYP2D6, on the analgesic effects and pharmacokinetics of oral oxycodone were studied in 20 chronic pain patients using a randomized, double-blind, placebo-controlled cross-over study design. Pain intensity and rescue analgesics were recorded daily, and the pharmacokinetics and pharmacodynamics of oxycodone were studied on the 7th day of concomitant paroxetine (20 mg/day) or placebo administration. The patients were genotyped for CYP2D6, 3A4, 3A5 and ABCB1.Paroxetine had significant effects on the metabolism of oxycodone but it had no statistically significant effect on oxycodone analgesia or use of morphine for rescue analgesia. Paroxetine increased the dose-adjusted mean AUC0–12h of oxycodone by 19% (−23 to 113%; P = 0.003), and that of noroxycodone by 100% (5–280%; P < 0.0001) but decreased the AUC0–12 h of oxymorphone by 67% (−100 to −22%; P < 0.0001) and that of noroxymorphone by 68% (−100 to −16%; P < 0.0001).Adverse effects were also recorded in a pain diary for both 7-day periods (placebo/paroxetine). The most common adverse effects were drowsiness and nausea/vomiting. One patient out of four reported dizziness and headache during paroxetine co-administration, whereas no patient reported these during placebo administration (P = 0.0471) indicating that these adverse effects were due to paroxetine.No statistically significant associations of the CYP2D6 or CYP3A4/5 genotype of the patients and the pharmacokinetics of oxycodone or its metabolites, extent of paroxetine–oxycodone interaction, or analgesic effects were observed probably due to the limited number of patients studied.The results of this study strongly suggest that CYP2D6 inhibition does not significantly change oxycodone analgesia in chronic pain patients and that the analgesic activity of oxycodone is mainly due to the parent compound and that metabolites, e.g. oxymorphone, play an insignificant role. The clinical implication of these results is that induction of the metabolism of oxycodone may lead to inadequate analgesia while increased drug effects can be expected after addition of potent CYP3A4/5 inhibitors particularly if combined with CYP2D6 inhibitors or when administered to poor metabolizers of CYP2D6.

scholarly journals Psychological factors as predictors of opioid abuse and illicit drug use in chronic pain patients

2007 ◽  
Vol 3 (2) ◽  
pp. 89 ◽  
Author(s):  
Laxmaiah Manchikanti, MD ◽  
James Giordano, PhD ◽  
Mark V. Boswell, MD, PhD ◽  
Bert Fellows, MA ◽  
Rajeev Manchukonda, BDS ◽  
...  
Keyword(s):  
Substance Abuse ◽  
Chronic Pain ◽  
Drug Abuse ◽  
Drug Use ◽  
Illicit Drug ◽  
Illicit Drug Use ◽  
Opioid Abuse ◽  
Somatization Disorder ◽  
Chronic Pain Patients ◽  
Pain Patients

Background: Psychopathology (depression, anxiety, somatization disorder) and substance abuse (opioid mis-use and illicit drug use) are common in patients with chronic pain and present problems for public health and clinical management. Despite a body of literature describing various methods for identifying psychopathology, opioid misuse, and illicit drug use in chronic pain patients, the relationship between psychopathologies, substance abuse, and chronic pain has not been well characterized.Methods: This report describes a total of500 consecutive pain patients prescribed and receiving stable doses of opioids. The patients were evaluated for psychopathology, opioid abuse, and illicit drug use during the course of regular pain management treatment. The relationships between psychopathology and drug abuse and/or illicit drug use in chronic pain patients were examined, and psychological evaluation for depression, anxiety, and somatization disorder was performed.Results: Depression, anxiety, and somatization disorder were documented in 59, 64, and 30percent of chronic pain patients, respectively. Drug abuse was significantly higher in patients with depression as compared to patients without depression (12percent with depression versus 5percent without). Current illicit drug use was higher in women with depression (22 percent) than women without depression (14percent) and in men with or without depression (12percent). Current illicit drug use was also higher in men with somatization disorder (22 percent) than men without (9 percent).Conclusion: This study demonstrated that the presence of psychological features of depression and somatization disorder may be markers of substance abuse diathesis in chronic pain patients.

Poster 146 CR845, a Novel Peripherally-Acting Kappa Opioid Receptor Agonist, Has Low Abuse Potential Compared With Pentazocine

PM&R ◽  
2015 ◽  
Vol 7 ◽  
pp. S139-S140
Author(s):  
Lynn Webster ◽  
Frédérique Menzaghi ◽  
Joseph W. Stauffer ◽  
Paul J. Tiseo ◽  
Robert H. Spencer
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
Kappa Opioid Receptor ◽  
Abuse Potential ◽  
Kappa Opioid ◽  
Opioid Receptor Agonist

Substance abuse treatment for high risk chronic pain patients on opioid therapy

2009 ◽  
Vol 10 (4) ◽  
pp. S62 ◽  
Author(s):  
R. Jamison ◽  
A. Wasan ◽  
E. Michna ◽  
E. Ross ◽  
L. Chen ◽  
...  
Keyword(s):  
Substance Abuse ◽  
Chronic Pain ◽  
High Risk ◽  
Substance Abuse Treatment ◽  
Opioid Therapy ◽  
Chronic Pain Patients ◽  
Abuse Treatment ◽  
Pain Patients

The kappa opioid receptor agonist SA14867 has antinociceptive and weak sedative effects in models of acute and chronic pain

2011 ◽  
Vol 671 (1-3) ◽  
pp. 53-60 ◽  
Author(s):  
Yaeko Tsukahara-Ohsumi ◽  
Fumio Tsuji ◽  
Masashi Niwa ◽  
Taeko Hata ◽  
Minoru Narita ◽  
...  
Keyword(s):  
Chronic Pain ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Opioid Receptor Agonist ◽  
Sedative Effects
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