Alternate-day buprenorphine dosing is preferred to daily dosing by opioid-dependent humans

Amass, Leslie; Bickel, Warren K.; Crean, John P.; Blake, Joan E.; Higgins, Stephen T.

doi:10.1007/s002130050559

Cited by 56 publications

(44 citation statements)

References 17 publications

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“…On the other hand, because buprenorphine has high affinity for opioid receptors (Hambrook and Rance 1976;Sadee et al 1982;Lewis et al 1983), moderately high BUP doses can block subjective and physiological effects of mu-opioids for more than 1 day (Jasinski et al 1978;Rosen et al 1994;Schuh et al 1999). Consistent with this human laboratory evidence, BUP has been shown to retain its efficacy using less-than-daily dosing schedules in several clinical trials (Fudala et al 1990;Amass et al 1994Amass et al , 1998Amass et al , 2000Johnson et al 1995b;Bickel et al 1999;Petry et al 1999).…”

Section: Introductionmentioning

confidence: 76%

Effects of buprenorphine sublingual tablet maintenance on opioid drug-seeking behavior by humans

et al. 2002

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Section: Introductionmentioning

confidence: 76%

Effects of buprenorphine sublingual tablet maintenance on opioid drug-seeking behavior by humans

et al. 2002

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“…Its unique therapeutic advantages include a low risk for clinically significant respiratory depression, long duration of action allowing less-than-daily dosing, and mild withdrawal symptoms upon cessation of use (e.g., Amass et al, 1998;Jasinski et al, 1978;Strain, 2006;Walsh et al, 1995), all of which are attributable, in part, to its partial agonist profile with less-than-maximal intrinsic activity and its high lipophilicity (see Walsh and Eissenberg, 2003 for review). Buprenorphine is marketed in a single drug formulation and also in combination with naloxone, which is intended to deter illicit diversion to the parenteral route.…”

Section: Buprenorphine: Laboratory Evaluation Of a Partial Agonist Trmentioning

confidence: 99%

The role of human drug self-administration procedures in the development of medications

Comer

Ashworth²,

Foltin

et al. 2008

Drug and Alcohol Dependence

136

148

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The purpose of this review is to illustrate the utility and value of employing human self-administration procedures in medication development, including abuse liability assessments of novel medications and evaluation of potential pharmacotherapies for substance use disorders. Traditionally, human abuse liability testing has relied primarily on subjective reports describing drug action by use of questionnaires; similarly, drug interactions between putative treatment agents and the drugs of abuse have relied on these measures. Subjective reports are highly valued because they provide qualitative and quantitative information about the characteristics of central and peripheral pharmacodynamic effects as well as safety and tolerability. However, self-administration procedures directly examine the behavior of interest -that is, drug taking. The present paper 1) reviews the most commonly used human self-administration procedures, 2) discusses the concordance of subjective reports and selfadministration within the context of medications development for substance use disorders, focusing primarily on illustrative examples from development efforts with opioid and cocaine dependence, and 3) explores the utility of applying self-administration procedures to assess the abuse liability of novel compounds, including "abuse deterrent" formulations (ADFs). The review will focus on opioid and cocaine dependence because a rich database from both clinical laboratory and clinical trial research exists for these two drug classes. The data reviewed suggest that drug-induced changes in self-administration and subjective effects are not always concordant. Therefore, assessment of selfadministration in combination with subjective effects provides a more comprehensive picture that may have improved predictive validity for translating to the clinical setting.

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Section: Introductionmentioning

confidence: 99%

“…In the treatment of opioid addiction, a long-lasting effect of a medication may produce better treatment effectiveness (Kreek, 1992(Kreek, , 1996. Although buprenorphine has a relatively longer duration of action compared with other opioids, it still requires daily or alternate-day dosing (Fudala et al, 1990;Amass et al, 1998), which gives rise to great medical burdens and may reduce patient compliance under some circumstance. Therefore, new partial opioid agonists with higher oral bioavailability and longer duration of action than buprenorphine may improve the treatment for opioid addiction.…”

mentioning

confidence: 99%

Thienorphine Is a Potent Long-Acting Partial Opioid Agonist: A Comparative Study with Buprenorphine

Yu¹,

Yue²,

Cui³

et al. 2006

J Pharmacol Exp Ther

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A strategy in the development of new treatment for opioid addiction is to find partial opioid agonists with properties of long duration of action and high oral bioavailability. In a search for such compounds, thienorphine, a novel analog of buprenorphine, was synthesized. Here, we reported that, like buprenorphine, thienorphine bound potently and nonselectively to -, ␦-, and -opioid receptors stably expressed in CHO (Chinese hamster ovary) cells and behaved as a partial agonist at -opioid receptor. However, some differences were observed between the pharmacological profiles of thienorphine and buprenorphine. In vitro, thienorphine was more potent than buprenorphine in inhibiting Additionally, the bioavailability of thienorphine was greatly higher than that of buprenorphine after oral administration. Moreover, compared with buprenorphine, thienorphine showed a similar long-lasting antinociceptive effect but a much longer antagonism of morphine-induced lethality (more than 15 days). These results indicate that thienorphine is a potent, long-acting partial opioid agonist with high oral bioavailability and may have possible application in treating addiction.Opioid abuse and dependence remain a serious worldwide health problem. The drugs currently in clinical use for treating opioid dependence are either full-opioid agonist, methadone, and LAAM or antagonist naltrexone (Johnson et al., 2003). Although these drugs proved extremely effective in reducing illicit opioid use, they have some drawbacks; the agonist merely substitutes one addiction for another, and the antagonist is unable to retain patients in treatment due to a lack of desired positive subjective effects (Johnson et al., 2003). Buprenorphine, a derivative of thebaine, has unique pharmacological properties; it is a high-affinity, low-intrinsic activity agonist at -opioid receptor and has an antagonist activity at -opioid receptor (Cowan et al., 1977;Dum and Herz, 1981;Negus et al., 1989). Buprenorphine, as a partial agonist, either alone or in combination with naloxone, has been shown to be effective in treating opioid dependence experimentally and clinically (for reviews, see Johnson et al., 2003;Davids and Gastpar, 2004). With its unique pharmacological properties, buprenorphine gains advantages over the agonist or antagonist medication in the treatment of opioid addiction, showing an acceptable effectiveness as well as a good safety profile, particularly with respect to lower respiratory depression and physical dependence relative to a full--opioid receptor agonist (Walsh et al., 1994(Walsh et al., , 1995.Buprenorphine is safe and has low abuse liability, whereas its use in the treatment of opioid dependence has been restricted by its very low oral bioavailability (Heel et al., 1979), which results in a somewhat inconvenient administration of sublingual preparations in clinic (Mendelson et al., 1997;Schuh and Johanson, 1999). In addition, it has been shown that buprenorphine can cause dependence both in physical and psychological studies, probabl...

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Alternate-day buprenorphine dosing is preferred to daily dosing by opioid-dependent humans

Cited by 56 publications

References 17 publications

Effects of buprenorphine sublingual tablet maintenance on opioid drug-seeking behavior by humans

Effects of buprenorphine sublingual tablet maintenance on opioid drug-seeking behavior by humans

The role of human drug self-administration procedures in the development of medications

Thienorphine Is a Potent Long-Acting Partial Opioid Agonist: A Comparative Study with Buprenorphine

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