Buprenorphine and Naloxone for Heroin Dependence

Abstract

The pharmacology of buprenorphine is unique because of its partial agonist profile at the mu-opioid receptor (ie, high affinity, low intrinsic activity and slow dissociation). This unique profile results in greater safety, less physical dependence, and greater flexibility in dose scheduling. Buprenorphine has been investigated in combination with the opioid antagonist, naloxone, with the goal of decreasing abuse, misuse, and diversion. When combined with naloxone in a sublingual tablet, buprenorphine has been shown to be effective 1) in retaining patients in treatment, 2) in reducing opioid use and craving, and 3) when dosed less-than-daily. The pharmacologic effects of buprenorphine are not altered by the addition of naloxone when administered to the population in an appropriate combination ratio. However, if taken intravenously by individuals dependent on short- or long-acting opioids a precipitated withdrawal syndrome is observed, which should reduce its abuse potential. This review discusses the rationale for development and evidence supporting the use of a buprenorphine/naloxone combination product. The buprenorphine/naloxone combination product should be considered for use in primary care office-based settings as a safe and effective treatment that is likely to increase the availability of agonist treatment for opioid dependence.

Dysregulation of Nociceptin/Orphanin FQ Activity in the Amygdala Is Linked to Excessive Alcohol Drinking in the Rat

“…In fact, the opioid agonist/partial agonist buprenorphine, that has long been in clinical use for the treatment of pain (14,15,16) and management of heroin dependence (17,18,19) reduces alcohol drinking in msP rats via activation of NOP receptors (20). Consistent with this finding there are clinical data indicating that buprenorphine given to heroin addicts lowers not only opiate but also alcohol consumption (17,19).…”

Buprenorphine and a CRF1 Antagonist Block the Acquisition of Opiate Withdrawal-Induced Conditioned Place Aversion in Rats

“…Buprenorphine is an opioid partial agonist at the m opioid receptor and a k opioid antagonist (Cowan et al, 1977). Buprenorphine's partial agonist properties limit its abuse liability (Jasinski et al, 1978), and it recently has been approved for use in the treatment opiate dependence (Johnson and McCagh, 2000;Tzschentke, 2002;Substance Abuse and Mental Health Services Administration, 2002). Buprenorphine has high affinity for the m, q, and k opioid receptors but moderate intrinsic activity (Cowan, et al, 1977).…”

Craving e dependência química: conceito, avaliação e tratamento

“…É possível observar que as técnicas de manejo do craving pesquisadas e utilizadas na prática clínica 11,18,19,27,45,46,[53][54][55][56][57][58][59] provêm de diversas fundamentações, podendo ser categorizadas como comportamentais, cognitivas ou psicofarmacoló-gicas. Percebe-se que, muitas vezes, é necessária a integração de várias dessas técnicas para controlar o craving, conforme preconizam Johnson et al 49 e Baker 54 , e, que, mesmo assim, nem sempre se obtém sucesso nesse intuito.…”