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Opioid Abuse Medication

  • Author: Adrian Preda, MD; Chief Editor: Eduardo Dunayevich, MD  more...
 
Updated: Jun 07, 2016
 

Medication Summary

The goals of pharmacotherapy are to treat the addiction of the chemical substances that cause them.

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Opioid analgesics

Class Summary

Two uses for opioid analgesics are as follows: (1) Oral substitution therapy or maintenance therapy or opioid agonist therapy (OAT) refers to substitution of an oral opioid for injected heroin, with the goal of reducing harmful behaviors associated with heroin use. (2) Detoxification, or controlled withdrawal with the goal of abstinence, is based on the principle of cross-tolerance in which one opioid is replaced with another and then slowly withdrawn.

Methadone (Dolophine)

 

Inhibits ascending pain pathways, diminishing the perception of and response to pain. There are inpatient facilities and a few, specialized, licensed, outpatient, drug treatment programs that provide opioid detoxification using methadone. Also a preferred agent for opioid agonist maintenance. Some experts feel that laboratory measures of plasma levels should be used to adjust the dose and that 400 ng/mL seems sufficient to stop craving and drug hunger.

Benefits include good treatment retention, psychosocial adjustment, and reduced criminal activity.

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Antidotes for opioids

Class Summary

Inhibit opioid effects by inhibiting opioid agonists at receptor sites.

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Alpha 2 adrenergic agonists

Class Summary

Used primarily for the treatment of hypertension.

Clonidine (Catapres)

 

May reduce norepinephrine release. In opioid withdrawal, seems to be most effective in suppressing autonomically mediated signs and symptoms of abstinence but less effective for subjective symptoms.

Used in higher doses for detoxification than for treating hypertension. Benzodiazepine may be beneficial as adjuvant therapy for muscle cramps and insomnia. Clonidine also has anticraving effect for opioids. Clonidine in combination with naltrexone, which is a potent long-acting narcotic antagonist, also is referred to be as rapid detoxification. This approach is designed to shorten the time course of withdrawal to 5 d. Clonidine alone and in combination has been demonstrated to be feasible in primary care settings as an outpatient.

Treatment is initiated after confirmation of physical dependence by naloxone challenge test.

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Opioid Antagonists

Class Summary

Reverses opioid effects by inhibiting opioid agonists at receptor sites.

Naloxone (Evzio, Narcan)

 

Pure opioid antagonist. Used to reverse opioid intoxication.

If patients do not respond to multiple doses of naloxone, consider alternative causes of unconsciousness. Need of ongoing substance abuse treatment should be established while caring for overdose. The injectable solution is available in vials and syringes (0.4 mg/mL, 1 mg/mL) for IV/IM/SC administration by healthcare providers. It is also available as an autoinjector (delivers 0.4 mg IM/SC) for home use by family or caregivers.

Naloxone intranasal (Narcan Nasal Spray)

 

Competitive opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. The intranasal form is indicated for the emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression.

Naltrexone (ReVia, Vivitrol)

 

Used in combination with clonidine for rapid (4-5 d) detoxification.

Very effective long-acting opioid antagonist that was thought to be an ideal maintenance agent because it blocks receptor sites and, hence, opioid reinforcing properties. However, clinical results are not very promising when compared with methadone maintenance. Craving may continue during naltrexone maintenance. For groups of patients such as health care professionals or business executives for whom external incentives to stay away from drugs are important, naltrexone therapy has been very effective.

Indicated for prevention of relapse to opioid dependence following opioid detoxification.

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Contributor Information and Disclosures
Author

Adrian Preda, MD Professor of Clinical Psychiatry and Human Behavior, Director of Residency Program in Psychiatry, Vice-Chair, Department of Psychiatry and Human Behavior, University of California, Irvine, School of Medicine

Adrian Preda, MD is a member of the following medical societies: American Association for the Advancement of Science, American Psychiatric Association, International College of Neuropsychopharmacology, International Congress of Schizophrenia Research, Schizophrenia International Research Society, Society of Biological Psychiatry

Disclosure: Nothing to disclose.

Specialty Editor Board

Francisco Talavera, PharmD, PhD Adjunct Assistant Professor, University of Nebraska Medical Center College of Pharmacy; Editor-in-Chief, Medscape Drug Reference

Disclosure: Received salary from Medscape for employment. for: Medscape.

Chief Editor

Eduardo Dunayevich, MD Executive Director, Clinical Development, Amgen

Eduardo Dunayevich, MD is a member of the following medical societies: Schizophrenia International Research Society

Disclosure: Received salary from Amgen for employment; Received stock from Amgen for employment.

Additional Contributors

Barry I Liskow, MD Professor of Psychiatry, Vice Chairman, Psychiatry Department, Director, Psychiatric Outpatient Clinic, The University of Kansas Medical Center

Disclosure: Nothing to disclose.

Acknowledgements

The authors and editors of Medscape Drugs & Diseases gratefully acknowledge the contributions of previous authors Ziaur Rehman, MD, Suzan Khoromi, MD, James E Douglas, MD, Steven A Adelman, MD, and William J Meehan, MD, PhD to the development and writing of this article.

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