Krupitsky EM, Blokhina EA. Long-acting depot formulations of naltrexone for heroin dependence: a review

Laboratory of Clinical Psychopharmacology of Addictions, Valdman Institute of Pharmacology, St Petersburg State Pavlov Medical University, St Petersburg, Russia.
Current opinion in psychiatry (Impact Factor: 3.94). 03/2010; 23(3):210-4. DOI: 10.1097/YCO.0b013e3283386578
Source: PubMed


The major problem with the oral formulation of naltrexone for heroin dependence is poor compliance (adherence). Long-acting sustained release formulations of naltrexone (implantable and injectable) might help to improve compliance and, thus, increase the efficacy of abstinence-oriented treatment of heroin dependence with naltrexone.
There have been several implantable and injectable formulations of naltrexone developed within the last decade. It was demonstrated that some of them are effective and relatively well tolerated medications for relapse prevention in heroin addicts. However, advantages and disadvantages of these new medications have never been systematically analyzed.
Long-acting sustained release formulations of naltrexone are well tolerated and more effective for relapse prevention in heroin addicts than the oral ones.

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Available from: Evgeny Krupitsky, Jan 21, 2014
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    • "The second SPECT session was conducted 2 weeks after the XRNT injection. The timing of the session coincided with peak naltrexone levels (Krupitsky and Blokhina 2010). Plasma samples were taken on the day of the second SPECT session to assess peak naltrexone levels and its major metabolite 6β-naltrexol (Slawson et al. 2007). "
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    ABSTRACT: Extended-release naltrexone (XRNT), an opioid receptor antagonist, is successfully used in the treatment of opioid dependence. However, naltrexone treatment of opioid-dependent patients may reduce striatal dopamine transporter (DAT) availability and cause depression and anhedonia. The aim of this study is to investigate changes in striatal DAT availability and symptoms of depression (Beck Depression Inventory (BDI)) and anhedonia (Snaith Hamilton Pleasure Scale (SHAPS)) before and during XRNT treatment. At baseline, ten detoxified heroin-dependent patients and 11 matched healthy controls underwent [(123)I]FP-CIT single photon emission computed tomography (SPECT) imaging to assess striatal DAT binding. Patients underwent a second SPECT scan 2 weeks after an intramuscular injection with XRNT. At baseline, the mean binding potential (BPND) in the putamen was at a trend level lower and the mean BDI score was significantly higher in heroin patients (n = 10) than in controls (n = 11) (3.45 ± 0.88 vs. 3.80 ± 0.61, p = 0.067, d = -0.48 and 12.75 ± 7.40 vs. 5.20 ± 4.83, p = 0.019, d = 1.24, respectively). Post hoc analyses in subgroups with negative urine analyses for opioids and cocaine showed significantly lower baseline putamen BPND in heroin patients (n = 8) than controls (n = 10) (3.19 ± 0.43 vs. 3.80 ± 0.64, p = 0.049, d = -1.03). XRNT treatment in heroin patients was not significantly associated with changes in striatal DAT availability (p = 0.348, d = 0.48), but the mean BDI score after XRNT treatment was significantly lower than before treatment (7.75 ± 7.21 vs. 12.75 ± 7.40, p = 0.004, d = -0.68). The results of this study suggest that XRNT treatment does not reduce striatal DAT availability and has no significant effect on anhedonia, but is associated with a significant reduction of depressive symptoms.
    Full-text · Article · Mar 2015 · Psychopharmacology
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    • "Vivitrol is an injectable extended-release formulation of naltrexone that has recently been approved for the treatment of opioid abuse and dependence. Vivitrol addresses the concern of medication adherence as a monthly injectable formulation and has been shown to be more effective than oral naltrexone (Krupitskya & Blokhina, 2010). This was also shown in a recent Phase 3 clinical trial that confirmed vivitrol's safety and efficacy in the prevention of relapse to heroin use in a cohort of injection drug users. "

    Full-text · Chapter · Nov 2011
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    • "The main reason that oral naltrexone treatment is often ineffective involves patients' failure to adhere to the daily regimen (Minozzi et al., 2006; Pettinati, Volpicelli et al., 2000). Vivitrol reduces the adherence problem as confirmed by studies showing blockade of injected opiates for over 30 days (Coviello et al., in press; Krupitsky et al., 2010). During 2007-2008, a multi-site pilot study examined long-acting naltrexone (Depotrex ®) among opioid-dependent parolees and probationers. "
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    ABSTRACT: Creating, implementing and evaluating substance abuse interventions, especially medication-assisted treatments, for prisoners, parolees, and probationers with histories of heroin addiction is an especially challenging endeavor because of the difficulty in coordinating and achieving cooperation among diverse criminal justice, substance abuse treatment, research, and social service agencies, each with its own priorities and agenda. In addition, there are special rules that must be followed when conducting research with criminal justice-involved populations, particularly prisoners. The following case studies will explore the authors' experience of over 10 years conducting pharmacotherapy research using methadone, buprenorphine, and naltrexone with criminal justice populations. The major obstacles and how they were overcome are presented. Finally, recommendations are provided with regard to implementing and conducting research with criminal justice populations.
    Full-text · Article · Nov 2011 · Behavioral Sciences & the Law
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