Showing papers on "Buprenorphine published in 2004"
TL;DR: The pharmacokinetic drug-drug interactions of methadone do not have life-threatening consequences for the patients, but they usually cause a decrease of the concentrations and of the effects of the drug, which in turn can cause symptoms of withdrawal and increase the risk of relapse into heroin abuse.
334 citations
TL;DR: Evidence is provided demonstrating that the ORL-1 receptor plays a functional role not only in the antinociceptive effect of buprenorphine but also in other actions of the drug as well.
Abstract: Buprenorphine, an opioid with mixed agonist-antagonist activity at classical opioid receptors, has been approved recently for the treatment of opioid dependency. Buprenorphine is also used as an analgesic. The buprenorphine dose-response curve is sometimes submaximal, or even bell-shaped, in nociceptive assays, depending upon the nature and intensity of the noxious stimulus. Moreover, buprenorphine, when administered with full agonists, such as morphine, antagonizes the action of these drugs. Partial agonism at the mu opioid receptor and, in some cases, antagonism at the kappa or delta opioid receptor have been considered as possible underlying mechanisms for the ceiling effect and bell-shaped dose-response curve of buprenorphine. While ceiling effects can be explained by partial agonist activity of buprenorphine, the bell-shaped dose-response curve cannot be a consequence of this property of the drug. Recently, buprenorphine has been shown to activate the opioid receptor-like (ORL-1; also known as NOP) receptor. Supraspinal activation of the ORL-1 receptor counteracts the antinociceptive and rewarding actions of morphine, raising the possibility that these actions of buprenorphine can also be altered by its ability to concomitantly activate the ORL-1 receptor. The use of molecular biological techniques has advanced our knowledge regarding the role of opioid receptors in modulation of pain and reward. In particular, generation of opioid receptor knockout mice has proven useful in this regard. Indeed, using knockout mice, we have recently shown that the antinociceptive effect of buprenorphine mediated primarily by the mu opioid receptor is attenuated by the ability of the drug to activate the ORL-1 receptor. Thus, the goal of this review is to provide evidence demonstrating that the ORL-1 receptor plays a functional role not only in the antinociceptive effect of buprenorphine but also in other actions of the drug as well.
275 citations
TL;DR: The French model raises questions about the value of tight regulations on prescribing BUP imposed by many countries throughout the world.
Abstract: In most European countries, methadone treatment is provided to only 20–30% of opiate abusers who need treatment due to regulations and concerns about safety. To address this need in France, all registered medical doctors since 1995 have been allowed to prescribe buprenorphine (BUP) without any special education or licensing. This led to treating approximately 65,000 patients per year with BUP, about ten times more than with more restrictive methadone policies. French physician compensation mechanisms, pharmacy services, and medical insurance funding all minimized barriers to BUP treatment. About 20% of all physicians in France are using BUP to treat about half of the estimated 150,000 problem heroin users. Daily supervised dosing by a phamacist for the first six months resulted in significantly better treatment retention (80% vs 46%) and lower heroin use. Intravenous diversion of BUP may occur in up to 20% of BUP patients and has led to various infections and relatively rare overdoses in combination with ...
239 citations
01 Jan 2004
TL;DR: These guidelines address the pharmacology and physiology of opioids, opioid addiction, and treatment with buprenorphine; describe patient assessment and the choice of opioid addiction treatment options; provide detailed treatment protocols for opioid withdrawal and maintenance therapy with buPrenorphines; and include information on the treatment of special populations.
Abstract: This Treatment Improvement Protocol (TIP), Clinical Guidelines for the Use of Buprenorphine in the Treatment of Opioid Addiction, provides consensus‐ and evidence‐based treatment guidance for the use of buprenorphine, a new option for the treatment of opioid addiction. The goal of this TIP is to provide physicians with information they can use to make practical and informed decisions about the use of buprenorphine to treat opioid addiction. These guidelines address the pharmacology and physiology of opioids, opioid addiction, and treatment with buprenorphine; describe patient assessment and the choice of opioid addiction treatment options; provide detailed treatment protocols for opioid withdrawal and maintenance therapy with buprenorphine; and include information on the treatment of special populations, e.g., pregnant women, adolescents, and polysubstance users. This TIP represents another step by the Center for Substance Abuse Treatment (CSAT) toward its goal of bringing national leaders together to improve substance use disorder treatment in the United States.
196 citations
TL;DR: Data from the CTN field experience suggest that buprenorphine-naloxone is practical and safe for use in diverse community treatment settings, including those with minimal experience providing opioid-based pharmacotherapy and/or medical detoxification for opioid dependence.
Abstract: In October 2002, the U.S. Food and Drug Administration approved buprenorphine-naloxone (Suboxone) sublingual tablets as an opioid dependence treatment available for use outside traditionally licensed opioid treatment programs. The NIDA Center for Clinical Trials Network (CTN) sponsored two clinical trials assessing buprenorphine-naloxone for short-term opioid detoxification. These trials provided an unprecedented field test of its use in twelve diverse community-based treatment programs. Opioid-dependent men and women were randomized to a thirteen-day buprenorphine-naloxone taper regimen for short-term opioid detoxification. The 234 buprenorphine-naloxone patients averaged 37 years old and used mostly intravenous heroin. Direct and rapid induction onto buprenorphine-naloxone was safe and well tolerated. Most patients (83%) received 8 mg buprenorphine-2 mg naloxone on the first day and 90% successfully completed induction and reached a target dose of 16 mg buprenorphine-4 mg naloxone in three days. Medication compliance and treatment engagement was high. An average of 81% of available doses was ingested, and 68% of patients completed the detoxification. Most (80.3%) patients received some ancillary medications with an average of 2.3 withdrawal symptoms treated. The safety profile of buprenorphine-naloxone was excellent. Of eighteen serious adverse events reported, only one was possibly related to buprenorphine-naloxone. All providers successfully integrated buprenorphine-naloxone into their existing treatment milieus. Overall, data from the CTN field experience suggest that buprenorphine-naloxone is practical and safe for use in diverse community treatment settings, including those with minimal experience providing opioid-based pharmacotherapy and/or medical detoxification for opioid dependence.
154 citations
TL;DR: The transmucosal, transdermal and epidural routes offer novel methods for administration of analgesic drugs and have considerable potential for improving techniques in feline pain management.
Abstract: Opioids have an unjustified reputation for causing mania in cats, but with refinements in dosing they are now used successfully in this species. The mu-opioid agonists are generally considered the best analgesics. Morphine (0.1–0.3 mg/kg) is effective in a clinical setting. Methadone (up to 0.5 mg/kg) has a similar profile to morphine. Pethidine (Demerol, meperidine; 2–5 mg/kg) is a useful analgesic with a faster onset but shorter duration of action than morphine. Oxymorphone and hydromorphone (0.05–0.1 mg/kg) are widely used in the USA. These opioids are more potent (up to 10 times), and longer acting than morphine in cats. Butorphanol (0.1–0.4 mg/kg) is a mu-opioid antagonist that produces its analgesic actions through kappa agonist activity. It rapidly reaches a ceiling effect, is short acting and is a weaker analgesic than pure mu opioids. Buprenorphine (0.01–0.02 mg/kg), a partial mu-agonist, is the most popular opioid used in small animal practice in the UK, other parts of Europe, Australia and South Africa. In clinical studies it has produced better analgesia than several other opioids and appears to be highly suitable for perioperative pain management in cats. NSAIDs are also used in cats for pain management, although cats metabolise these differently from other species. With appropriate dosing, carprofen (1–4 mg/kg) and meloxicam (0.3 mg/kg) have proved highly effective with few side effects. The use of ketoprofen (2 mg/kg), tolfenamic acid (4 mg/kg) and vedaprofen (0.5 mg/kg) has been reported in cats. Other less traditional analgesics such as ketamine, medetomidine and local anaesthetics are also used for clinical pain management. The transmucosal, transdermal and epidural routes offer novel methods for administration of analgesic drugs and have considerable potential for improving techniques in feline pain management.
153 citations
TL;DR: Buprenorphine is evaluated for the treatment of concomitant cocaine and opiate dependence and its efficacy for cocaine dependence is uncertain.
Abstract: Buprenorphine is a partial μ-opiate agonist and κ-opiate antagonist marketed in the United States and worldwide as a parenteral or sublingual analgesic1 and as maintenance treatment for opiate dependence.2 However, its efficacy for treatment of dually (cocaine and heroin) dependent individuals has not been established.
For the treatment of opiate dependence, sublingual doses of 8 to 16 mg daily of buprenorphine are as effective as 55 to 80 mg of oral methadone in reducing opiate use.3,4 There is some evidence that sublingual doses as low as 2 mg daily may reduce opiate use.5 Because buprenorphine has a relatively long duration of action, every-other-day and 3-times-weekly dosing have also shown efficacy.6-9
A large proportion of opiate users use cocaine, even during opiate agonist substitution treatment for opiate dependence. Cocaine use during opiate agonist maintenance treatment is associated with increased opiate use, poorer treatment outcomes, and premature dropout from treatment.10 Methadone and levomethadyl acetate (INN, levacetylmethadol) do not seem efficacious for the treatment of cocaine dependence in opiate-dependent individuals. Thus a medication that effectively reduced both opiate and cocaine use would offer a therapeutic advantage over methadone or levomethadyl acetate alone for the many patients who are using or are dependent on both opiates and cocaine.
Buprenorphine was found to have such potential in preclinical studies. It significantly reduced cocaine self-administration in monkeys without interfering with appetitive behaviors such as eating.11-14 However, attempted replications of these effects in humans have yielded inconsistent results. In some human laboratory studies, buprenorphine treatment reduced self-reported cocaine craving and cocaine self-administration; other studies have failed to replicate those results.15-18
Currently, there is no consensus in the literature about the clinical efficacy of buprenorphine for treatment of concurrent cocaine and heroin dependence. In some clinical trials with opiate-dependent subjects, buprenorphine treatment has been associated with reductions in cocaine use,19-21 whereas other trials have found no evidence of efficacy.18,22 One negative trial used buprenorphine doses of 4 mg and 12 mg/d22; the other used a mean dose of 11.2 mg.18 The positive studies have used buprenorphine doses up to 16 mg daily, with more reduction of cocaine use at higher doses.
The purpose of this study was to evaluate the efficacy of sublingual buprenorphine maintenance (10 weeks) in reducing cocaine and opiate use in dually (cocaine and opiate) dependent outpatients.
148 citations
TL;DR: The results indicate that fentanyl and buprenorphine exert different immune effects, and opioidid‐induced immunosuppression is less relevant in chronic administration than in acute or short‐time administration.
Abstract: It is known that morphine has a negative impact on the immune responses. The potent opioids fentanyl and buprenorphine have recently become available as transdermal preparation for the treatment of chronic pain. We analyze the effect of fentanyl and buprenorphine on splenic cellular immune responses in the mouse. The parameters evaluated were lymphoproliferation, natural killer cell activity and interleukin-2 and interferon-γ production. Drugs were administered acutely at the equianalgesic doses of 0.25 mg/kg for fentanyl and 5 mg/kg for buprenorphine, or delivered continuously with osmotic pumps for 24 h, 3 and 7 days at the rate of 7.5 μg/h per mouse (fentanyl) and 12.5 μg/h per mouse (buprenorphine). After acute administration, a significant decrease of lymphoproliferation is observed in fentanyl-treated animals only. After 24 h of fentanyl administration all the parameters were significantly reduced. After 3 days of fentanyl infusion NK activity had returned to normal values, while all the other parameters were still significantly reduced. In 7 day fentanyl-treated animals immunological tolerance had developed, since no differences with controls were present. In contrast no immune alterations were ever present in buprenorphine-treated animals. No tolerance to the antinociceptive effect of drugs had yet developed. After 1 week of infusion with fentanyl and buprenorphine, new pumps were implanted releasing double amounts of drugs. Neither fentanyl nor buprenorphine-treated animals showed altered immune responses at any time considered. These results indicate that fentanyl and buprenorphine exert different immune effects. Opioid-induced immunosuppression is less relevant in chronic administration than in acute or short-time administration.
145 citations
TL;DR: The data suggest a stepped model of care in which depression is evaluated and observed during the outset of treatment for opiate dependence and if it does not improve, specific psychosocial interventions or antidepressant medications tried.
139 citations
TL;DR: BUP seems to be more effective than METH in patients affected by depressive traits and dysphoria, probably due to antagonist action on kappa-opioid receptors, while METH was found unrelated to urinalyses results in METH patients.
134 citations
TL;DR: Analysis of causes of death reveals the difficulties in determining the role of substitution drugs in the death process, as many other factors may be involved, including circumstances surrounding death, past history, differential selection of subjects into either substitution modality and concomitant intake of other drugs (especially benzodiazepines and neuroleptics).
Abstract: Aims To assess the trends in the number, mortality and the nature of forensic cases involving toxicological detection of buprenorphine or methadone among toxicological investigations performed in Paris from June 1997 to June 2002. Design Retrospective, 5 year study with review of premortem data, autopsy, police reports, hospital data, and post-mortem toxicological analyses. Setting and participants 34 forensic cases of buprenorphine and 35 forensic cases of methadone detection among 1600 toxicological investigations performed at the Laboratory of Toxicology in the Medical Examiner’s Office in Paris. Measurements and results Therapeutic, toxic or lethal drug concentrations were defined based upon the results of blood analyses and the published literature. Drug concentrations were cross-referenced with other available ante- and post-mortem data. Subsequently, we classified a ‘clear responsibility’, ‘possible responsibility’ or ‘not causative’ role for buprenorphine or methadone in the death process, or ‘no explanation of death’. Buprenorphine and methadone can be regarded as being directly implicated in, respectively, four of 34 death cases (12%) and three of 35 death cases (9%), and their participation in the lethal process is strongly plausible in eight (buprenorphine) and 11 (methadone) additional deaths. Conclusions Analysis of causes of death reveals the difficulties in determining the role of substitution drugs in the death process, as many other factors may be involved, including circumstances surrounding death, past history, differential selection of subjects into either substitution modality and concomitant intake of other drugs (especially benzodiazepines and neuroleptics). The potential for synergistic or additive actions by other isolated molecules—particularly opioids, benzodiazepines, other psychotropes and alcohol—must be also considered.
TL;DR: Mainstreaming opioid addiction treatment has many advantages; its success will depend on resolution of ethical and delivery system issues as well as improved and expanded training of physicians in addiction medicine.
Abstract: Almost 3 million Americans have abused heroin. The most effective treatment for this concerning epidemic is opioid replacement therapy. Although, from a historical perspective, acceptance of this therapy has been slow, growing evidence supports its efficacy. There are 3 approved medications for opioid maintenance therapy: methadone hydrochloride, levomethadyl acetate, and buprenorphine hydrochloride. Each has unique characteristics that determine its suitability for an individual patient. Cardiac arrhythmias have been reported with methadone and levomethadyl, but not with buprenorphine. Due to concerns about cardiac risk, levomethadyl use has declined and the product may ultimately be discontinued. These recent safety concerns, specifics about opioid detoxification and maintenance, and new federal initiatives were studied. Opioid detoxification has a role in both preventing acute withdrawal and maintaining long-term abstinence. Although only a minority of eligible patients are engaged in treatment, opioid maintenance therapy appears to offer the greatest public health benefits. There is growing interest in expanding treatment into primary care, allowing opioid addiction to be managed like other chronic illnesses. This model has gained wide acceptance in Europe and is now being implemented in the United States. The recent Drug Addiction Treatment Act enables qualified physicians to treat opioid-dependent patients with buprenorphine in an office-based setting. Mainstreaming opioid addiction treatment has many advantages; its success will depend on resolution of ethical and delivery system issues as well as improved and expanded training of physicians in addiction medicine.
TL;DR: Buprenorphine TDS was well tolerated, with adverse events generally similar to those associated with other opioids, and patients' assessments of pain intensity and pain relief suggested better analgesia with buprenorphin TES than with placebo, although the differences did not reach statistical significance.
TL;DR: It was concluded that the most acutely painful effects of surgery in this model lasted for between 270 and 390 min, and that this was alleviated throughout its duration by subcutaneously administered carprofen or buprenorphine, and also bupenorphine administered orally.
Abstract: Prevention of unnecessary pain in laboratory animals requires reliable and practically useful tools for assessing pain severity and analgesic efficacy. We have used a behaviour-based pain scoring system to determine the duration of pain resulting from laparotomy, and the duration of analgesia afforded by orally administered (p.o.) buprenorphine and subcutaneously administered (s.c.) carprofen or buprenorphine in rats. One hour before laparotomy Fisher 344 rats received either saline as a control (0.2 ml/100 g s.c.), carprofen (5 mg/kg s.c.) or buprenorphine (0.05 mg/kg s.c. or 0.4 mg/kg p.o.). The rats were housed singly for 10-min periods of behaviour recording, beginning 30 min after completing surgery. Recording was repeated at three time points every 2 h. The behaviour of controls was distinct from that of the analgesic-treated animals throughout recording; however, the major signs of pain (back-arching, staggering and writhing) were prominent during only the first 270 min in the saline group. This was followed by a period of more subtle differences between the saline- and drug-treated groups. It was concluded that the most acutely painful effects of surgery in this model lasted for between 270 and 390 min, and that this was alleviated throughout its duration by subcutaneously administered carprofen or buprenorphine, and also buprenorphine administered orally. The study demonstrates a clinically relevant and practically useful approach to assessing the duration of post-surgical abdominal pain and analgesic effects in rats.
TL;DR: Individuals who leave pharmacotherapies for opioid dependence experience higher overdose and death rates compared with those in treatment, and Clinicians should alert naltrexone treatment patients in particular about heroin overdose risks.
Abstract: Aims The study estimated serious adverse event (SAE) rates among entrants to pharmacotherapies for opioid dependence, during treatment and after leaving treatment. Design A longitudinal study based on data from 12 trials included in the Australian National Evaluation of Pharmacotherapies for Opioid Dependence (NEPOD). Participants and settings A total of 1.244 heroin users and methadone patients treated in hospital, community and GP settings. Intervention Six trials included detoxification; all included treatment with methadone, buprenorphine, levo-alpha-acetyl-methadol (LAAM) or naltrexone. Findings During 394 person-years of observation, 79 SAEs of 28 types were recorded. Naltrexone participants experienced 39 overdoses per 100 person-years after leaving treatment (44% occurred within 2 weeks after stopping naltrexone). This was eight times the rate recorded among participants who left agonist treatment. Rates of all other SAEs were similar during treatment versus out of treatment, for both naltrexone-treated and agonist-treated participants. Five deaths occurred, all among participants who had left treatment, at a rate of six per 100 person-years. Total SAE rates during naltrexone and agonist treatments were similar (20, 14 per 100 person-years, respectively). Total SAE and death rates observed among participants who had left treatment were three and 19 times the corresponding rates during treatment. Conclusions Individuals who leave pharmacotherapies for opioid dependence experience higher overdose and death rates compared with those in treatment. This may be due partly to a participant self-selection effect rather than entirely to pharmacotherapy being protective. Clinicians should alert naltrexone treatment patients in particular about heroin overdose risks. Duty of care may extend beyond cessation of dosing.
TL;DR: For pain and mood, the chronic opioid user under the influence of the drug does not experience an opioid effect diminished by tolerance but a state opposite to the effect of theDrug, which may contribute to the motivation for continued drug use and the dysfunction associated with drug dependence.
TL;DR: Federal and non-federal regulatory and monitoring agencies, national and international researchers, national professional organizations, researchers involved in monitoring, opioid treatment programs and the pharmaceutical industry met to synthesize and disseminate practical information to guide training, practice, monitoring, regulation and evaluation efforts with these medications.
TL;DR: To assess the extent of doctor‐shopping for buprenorphine maintenance therapy in a French region with a specific indicator, a large number of patients with a history of addiction are referred to a clinic for treatment.
Abstract: SUMMARY Purpose To assess the extent of doctor-shopping for buprenorphine maintenance therapy in a French region with a specificindicator.Methods Use of a quasi-exhaustive prescription database in a French region (information system of the French GeneralHealth Insurance Scheme). Extraction of all buprenorphine prescriptions between September 1999 and December 2000.Definition and calculation of three quantities for each patient: delivered, prescribed and doctor-shopping quantity. The cal-culation of these three quantities is done by an automated and reproducible method determining the overlaps in prescriptionperiods of different physicians for a given patient. Calculation of the corresponding daily dose was done for each quantity.Results A total of 64326 prescriptions of buprenorphine by 1313 physicians to 3259 patients were extracted. Quantitiesand doses were calculated for 2587 patients. The total doctor-shopping quantity represented 18.6% of the delivered quantity.Doctor-shopping involved a minority of patients and was highly concentrated: 87 patients with doctor-shopping doses super-ior to 16mg/day were responsible for 45.4% of the total doctor-shopping quantity.Conclusions Doctor-shopping appears to be an important problem for buprenorphine maintenance treatment in France butmay be resolved by regulatory interventions. The use of adequate indicators on prescription databases may help to limit theeffects of such interventions on legitimate care. The method presented here may be used with slight adaptations for othermedications to assess their abuse potential. Copyright # 2003 John Wiley & Sons, Ltd.key words—doctor-shopping; prescription database; buprenorphine; maintenance treatment
TL;DR: The thevinols and orvinols derived from the baine via the thebaine-methylvinyl ketone adduct (thevinone) were thoroughly investigated in the 1960's and 1970's by the Reckitt group, and a number of important opioids emerged.
Abstract: The thevinols and orvinols derived from thebaine via the thebaine-methylvinyl ketone adduct (thevinone) were thoroughly investigated in the 1960's and 1970's by the Reckitt group. From this work a number of important opioids emerged. Buprenorphine is a mu partial agonist, kappa/delta-antagonist that is now used primarily in the treatment of heroin abuse and dependence though it was initially launched as an analgesic for the treatment of moderate to severe pain. Etorphine and dihydroetorphine are very potent mu agonists that have found application in veterinary and human medicine respectively. Diprenorphine is primarily a mu antagonist though it also has some kappa-partial agonist effects. It has high affinity for all types of opioid receptors and as a "universal" opioid ligand has been much in demand as a pharmacological tool. It has also been converted into a [11C] version for use in Positron Emission Tomography (PET) studies of brain function related to the opioid receptor system. More recent medicinal chemistry investigations have been concerned with gaining a greater understanding of buprenorphine's unique opioid profile. This has involved the synthesis and evaluation of a number of series of buprenorphine analogues in which the C20 t-butyl group has been constrained in a ring system. These studies have suggested that the methyls in the t-butyl group inhibit the conformational changes in the kappa-receptor required for generation of an agonist response. Introduction of a 7alpha-cinnamoylaminomethyl group in place of the orvinol tertiary alcohol function leads to selective irreversible mu antagonism.
TL;DR: Less than dose-proportional increases in plasma buprenorphine concentrations may contribute to the observed plateau for most pharmacodynamic effects as the dose is increased, according to the evaluated pharmacokinetics and pharmacodynamics of expected therapeutic doses.
Abstract: Objective: Buprenorphine and buprenorphine/naloxone combinations are effective pharmacotherapies for opioid dependence, but doses are considerably greater than analgesic doses. Because dose-related buprenorphine opioid agonist effects may plateau at higher doses, we evaluated the pharmacokinetics and pharmacodynamics of expected therapeutic doses. Design: The first experiment examined a range of sublingual buprenorphine solution doses with an ascending dose design (n = 12). The second experiment examined a range of doses of sublingual buprenorphine/naloxone tablets along with one dose of buprenorphine alone tablets with a balanced crossover design (n = 8). Participants: Twenty nondependent, opioid-experienced volunteers. Methods: Subjects in the solution experiment received sublingual buprenorphine solution in single ascending doses of 4, 8, 16 and 32mg. Subjects in the tablet experiment received sublingual tablets combining buprenorphine 4, 8 and 16mg with naloxone at a 4: 1 ratio or buprenorphine 16mg alone, given as single doses. Plasma buprenorphine, norbuprenorphine and naloxone concentrations and pharmacodynamic effects were measured for 48–72 hours after administration. Results: Buprenorphine concentrations increased with dose, but not proportionally. Dose-adjusted areas under the concentration-time curve for buprenorphine 32mg solution, buprenorphine 16mg tablet and buprenorphine/naloxone 16/4mg tablet were only 54 ± 16%, 70 ± 25% and 72 ± 17%, respectively, of that of the 4mg dose of sublingual solution or tablet. No differences were found between dose strengths for most subjective and physiological effects. Pupil constriction at 48 hours after administration of solution did, however, increase with dose. Subjects reported greater intoxication with the 32mg solution dose, even though acceptability of the 4mg dose was greatest. Naloxone did not change the bioavailability or effects of the buprenorphine 16mg tablet. Conclusion: Less than dose-proportional increases in plasma buprenorphine concentrations may contribute to the observed plateau for most pharmacodynamic effects as the dose is increased.
TL;DR: Clinicians will be using this drug for detoxification or for maintenance of opioid addiction, and Suboxone contains a mixture of buprenorphine and naloxone, which is designed to discourage intravenous use.
TL;DR: An overview of 5 Cochrane reviews of different approaches for treating opioid withdrawal finds methadone detoxification results in higher retention in treatment, lower relapse rate and fewer side effects when compared with adrenergic agonists, while buprenorphine appears to have an advantage over adren allergic agonists on withdrawal symptoms and side effects.
TL;DR: The two major goals of pharmacotherapy are to relieve the severity of opiate withdrawal symptoms during the managed withdrawal of the opioid and to prevent relapse to heroin use either after abstinence initiation or after being stabilised on a long-acting opiate agonist, such as methadone.
Abstract: Pharmacotherapies for heroin addiction may target opiate withdrawal symptoms, facilitate initiation of abstinence and/or reduce relapse to heroin use either by maintenance on an agonist or antagonist agent. Available agents include opioid agonists, partial opioid agonists, opioid antagonists and alpha 2 -agonists for use during managed withdrawal and long-term maintenance. Experimental approaches combine alpha 2 -agonists with naltrexone to reduce the time of opiate withdrawal and to accelerate the transition to abstinence. Recently, buprenorphine has been introduced in the US for office-based maintenance, with the hope of replicating the success of this treatment in Europe and Australia. Naloxone has been added to buprenorphine in order to reduce its potential diversion to intravenous use, whilst facilitating the expansion of treatment. Although comprehensive substance abuse treatment is not limited to pharmacotherapy, this review will focus on the rationale, indications and limitations of the range of existing medications for detoxification and relapse prevention treatments. The two major goals of pharmacotherapy are to relieve the severity of opiate withdrawal symptoms during the managed withdrawal of the opioid and to prevent relapse to heroin use either after abstinence initiation or after being stabilised on a long-acting opiate agonist, such as methadone.
TL;DR: The aim of the paper is to review, from a clinical perspective, the current status of what is known about the pharmacology of buprenorphine, with a particular emphasis on the issues of maintenance therapy in heroin addiction.
TL;DR: There may be greater bioavailability of buprenorphine/naloxone versus bupenorphine alone tablets, and that the bioavailability from the former is very similar to that seen with solution after 2 weeks of stabilization on each formulation.
TL;DR: Further data are required to determine whether buprenorphine can be considered as a good alternative to methadone treatment in pregnant women, but no alarming results were observed concerning pregnancy outcomes.
Abstract: Aim To report results on the prospective follow-up of 34 pregnant women exposed to buprenorphine maintenance for opiate dependence Design and setting Prospective multicentre study: all pregnant women receiving buprenorphine as maintenance therapy were included as early as possible during their pregnancy Participants The pregnant women were recruited from opiate maintenance therapy centres, general practitioner-networks involved in addiction, maternity hospitals and centres for drug information during pregnancy Measurements Women: drugs and medications consumed, medical and obstetrical events; offspring: withdrawal syndrome, malformation, neonatal disease Findings The buprenorphine-exposed pregnancies resulted in 31 live births, one stillbirth, one spontaneous abortion and one voluntary termination A neonatal withdrawal syndrome was observed in 13 cases (419%) and eight of these babies required opiate treatment Two neonates had a malformation: a premature ductus arteriosus stricture and a tragus appendix Conclusion Taken together with other prospective studies, no alarming results were observed concerning pregnancy outcomes However, further data from the comparative prospective study are required to determine whether buprenorphine can be considered as a good alternative to methadone treatment in pregnant women
TL;DR: Depressive symptoms improved in all subjects, with no difference between methadone and buprenorphine groups, suggesting no differential benefit on depressive symptoms for bupenorphine compared to methadon.
TL;DR: The results of the investigation on the roles of μ-, δ-, and κ-opioid receptors in antinociceptive responses and place preferences induced by buprenorphine support the ideas that μ-opIOid receptors mediate most of analgesic properties of bupenorphine, but thatμ- and δ- and/or λ-opiosid receptors are each involved in the rewarding effects of this drug.
TL;DR: This article reviews requirements for physician and staff training and needs for additional research on this unique medication, buprenorphine, and how it is used in opioid withdrawal as well as maintenance treatment.
Abstract: Buprenorphine is a new and attractive medication option for many opioid-addicted adults and their physicians. Before initiating buprenorphine treatment, providers must be aware of such critical factors as how the medication works, its efficacy and safety profile, how it is used in opioid withdrawal as well as maintenance treatment, and how patients can best be selected, educated about buprenorphine, and monitored throughout treatment. This article reviews these important issues as well as requirements for physician and staff training and needs for additional research on this unique medication.
TL;DR: Results from the present study suggest that depot buprenorphine offers significant promise for enhancing the delivery of effective opioid agonist treatment while minimizing risk for abuse of the medication.