Long-acting opioid-agonists in the treatment of heroin addiction: why should we call them "substitution"?
Many studies have documented the safety, efficacy, and effectiveness of long-acting opioids (L-AOs), such as methadone and buprenorphine, in the treatment of heroin addiction. This article reviews the pharmacological differences between L-AO medications and short-acting opioids (heroin) in terms of reinforcing properties, pharmacokinetics, effects on the endocrine and immune systems. Given their specific pharmacological profile, L-AOs contribute to control addictive behavior, reduce craving, and restore the balance of disrupted endocrine function. The use of the term "substitution," referring to the fact that methadone or buprenorphine replace heroin in binding to brain opioid receptors, has been generalized to consider L-AOs as simple replacement of street drugs, thus contributing to the widespread misunderstanding of this treatment approach.
Gerra
G
G
Health and Human Development Section Division for Operations, United Nations Office on Drugs and Crime, Vienna, Austria. gilberto.gerra@unodc.org
Maremmani
I
I
Capovani
B
B
Somaini
L
L
Berterame
S
S
Tomas-Rossello
J
J
Saenz
E
E
Busse
A
A
Kleber
H
H
D001143:Arousal / Q000187:drug effects; D001921:Brain / Q000187:drug effects; D002047:Buprenorphine / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D003932:Heroin / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics; D006556:Heroin Dependence / Q000534:rehabilitation*; D006801:Humans; D007121:Immunocompetence / Q000187:drug effects; D008691:Methadone / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D009042:Motivation; D009294:Narcotics / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D011957:Receptors, Opioid / Q000187:drug effects; D016896:Treatment Outcome
D003692:Delayed-Action Preparations; D009294:Narcotics; D011957:Receptors, Opioid; D002047:Buprenorphine; D003932:Heroin; D008691:Methadone