Effects of buprenorphine/naloxone in opioid-dependent humans.

Abstract:

RATIONALE:Buprenorphine is a partial mu opioid agonist under development as a sublingual (SL) medication for opioid dependence treatment in the United States. Because buprenorphine may be abused, tablets combining buprenorphine with naloxone in a 4:1 ratio have been developed to reduce that risk. Low doses of injected buprenorphine/naloxone have been tested in opioid-dependent subjects, but higher doses (more than 2 mg of either medication) and direct comparisons to SL buprenorphine/naloxone have not been examined. OBJECTIVES:To assess and compare the effects of intramuscular (i.m.) versus SL buprenorphine/naloxone in opioid-dependent volunteers. METHODS:Opioid-dependent volunteers were maintained on 40 mg per day of oral hydromorphone while on a residential research ward. After safety testing in two pilot subjects, participants (n = 8) were tested with both i.m. and SL buprenorphine/naloxone (1/0.25, 2/0.5, 4/1, 8/2, 16/4 mg); i.m. hydromorphone (10 mg) and naloxone (0.25 mg); both i.m. and SL buprenorphine alone (8 mg); and placebo. Test sessions were twice per week; dosing was double-blind. RESULTS:Intramuscular buprenorphine/naloxone produced dose-related increases on indices of opioid antagonist effects. Effects were consistent with naloxone-precipitated withdrawal, and were short-lived. As withdrawal effects dissipated, euphoric opioid agonist effects from buprenorphine did not appear. Sublingual buprenorphine/naloxone produced neither opioid agonist nor antagonist effects. CONCLUSIONS:Intramuscular injection of buprenorphine/naloxone precipitates withdrawal in opioid dependent persons; therefore, the combination has a low abuse potential by the injection route in this population. Sublingual buprenorphine/naloxone by tablet is well tolerated in opioid dependent subjects, and shows neither adverse effects (i.e., precipitated withdrawal) nor a high abuse potential (i.e., opioid agonist effects).

journal_title

Psychopharmacology

authors

Stoller KB,Bigelow GE,Walsh SL,Strain EC

doi

10.1007/s002130000637

subject

Has Abstract

pub_date

2001-03-01 00:00:00

pages

230-42

issue

3

eissn

0033-3158

issn

1432-2072

journal_volume

154

pub_type

临床试验,杂志文章,随机对照试验
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    authors: Gatley SJ,Volkow ND,Gifford AN,Fowler JS,Dewey SL,Ding YS,Logan J

    更新日期:1999-09-01 00:00:00

  • Comparison of anti-conflict drug effects in three experimental animal models of anxiety.

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    doi:10.1007/BF00427112

    authors: Kilts CD,Commissaris RL,Rech RH

    更新日期:1981-01-01 00:00:00

  • Differential effects on naloxone against the diazepam-induced release of behavior in rats in three aversive situations.

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    doi:10.1007/BF00426529

    authors: Soubrié P,Jobert A,Thiebot MH

    更新日期:1980-01-01 00:00:00

  • Association between major depression and cardiovascular risk: the role of antidepressant medication.

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    authors: Kuehl LK,Muhtz C,Hinkelmann K,Dettenborn L,Wingenfeld K,Spitzer C,Otte C

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  • Adverse effects of single therapeutic doses of diazepam on performance in normal geriatric subjects: relationship to plasma concentrations.

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    pub_type: 临床试验,杂志文章

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    authors: Pomara N,Stanley B,Block R,Guido J,Russ D,Berchou R,Stanley M,Greenblatt DJ,Newton RE,Gershon S

    更新日期:1984-01-01 00:00:00

  • Repeated social-defeat stress, cocaine or morphine. Effects on behavioral sensitization and intravenous cocaine self-administration "binges".

    abstract:RATIONALE:Repeated social stress experiences engender "behavioral sensitization" and may also increase the potential for abuse of psychomotor stimulants, particularly cocaine use during "binges." OBJECTIVE:Experimental protocols were designed to induce behavioral sensitization through exposures to social-defeat stress...

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    authors: Covington HE 3rd,Miczek KA

    更新日期:2001-12-01 00:00:00

  • Dissociable effects of NR2A and NR2B NMDA receptor antagonism on cognitive flexibility but not pattern separation.

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  • Behavioral effects of caffeine, (-)N-((R)-1-methyl-2-phenylethyl)-adenosine (PIA), and their combination in the mouse.

    abstract::The effects of caffeine (1-100 mg/kg, IP), (-)N-((R)-1-methyl-2-phenylethyl)-adenosine (PIA) (0.01-1 mg/kg, IP), and of the two drugs in combination were studied in mice responding under a mult FR30 FI600 s schedule of food presentation. The lowest dose of caffeine, 1 mg/kg, had no effect on responding under either co...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00432506

    authors: Glowa JR,Sobel E,Malaspina S,Dews PB

    更新日期:1985-01-01 00:00:00

  • Comparison between the effects of propranolol and chlordiazepoxide on timing behaviour in the rat.

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    pub_type: 杂志文章

    doi:10.1007/BF00431812

    authors: Salmon P,Gray JA

    更新日期:1985-01-01 00:00:00

  • Hypnotic susceptibility to various depressants in rats selected for differential ethanol sensitivity.

    abstract::MA rats, bred for greater motor impairment following subhypnotic doses of ethanol, were found to be more sensitive to the hypnotic effects of phenobarbital and chloral hydrate than were LA rats. In addition, the previously reported finding of a difference between the two lines of rats in duration of loss of righting r...

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    pub_type: 杂志文章

    doi:10.1007/BF00426674

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    更新日期:1979-02-28 00:00:00

  • Molecular properties of monoamine oxidases A and B.

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    pub_type: 杂志文章

    doi:10.1007/BF02246224

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    更新日期:1992-01-01 00:00:00

  • The time and space machine: continuous measurement of drug-induced behavior patterns in the rat.

    abstract::Because of the increasing demand for refined techniques to record drug-induced motoric changes, we designed and evaluated a computer monitoring system with continuous measurement of different parameters of rat motor activity. This system is particularly useful for chronic drug studies because it can characterize patte...

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    pub_type: 杂志文章

    doi:10.1007/BF00432113

    authors: Stoff DM,Stauderman K,Wyatt RJ

    更新日期:1983-01-01 00:00:00

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    doi:10.1007/BF02244646

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    更新日期:1993-01-01 00:00:00

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    doi:10.1007/s00213-008-1266-9

    authors: Didone V,Quoilin C,Tirelli E,Quertemont E

    更新日期:2008-12-01 00:00:00

  • Interactions among the cannabinoids in the antagonism of the abdominal constriction response in the mouse.

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    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00432273

    authors: Sanders J,Jackson DM,Starmer GA

    更新日期:1979-03-28 00:00:00

  • Alcohol attenuates amygdala-frontal connectivity during processing social signals in heavy social drinkers: a preliminary pharmaco-fMRI study.

    abstract:RATIONALE:Convergent evidence shows that alcohol exerts its effects on social behavior via modulation of amygdala reactivity to affective stimuli. Given that affective processing involves dynamic interactions between the amygdala and the prefrontal cortex (PFC), alcohol's effects are likely to extend beyond regional ch...

    journal_title:Psychopharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1007/s00213-013-3090-0

    authors: Gorka SM,Fitzgerald DA,King AC,Phan KL

    更新日期:2013-09-01 00:00:00

  • [11C]Ro 15-4513, a ligand for visualization of benzodiazepine receptor binding. Preparation, autoradiography and positron emission tomography.

    abstract::Ro 15-4513, a partial inverse agonist at the benzodiazepine (BZ) receptor site was labelled with 11C and used for in vitro autoradiography on human post mortem brain sections and for positron emission tomography (PET) on Cynomolgus monkeys. The total radiochemical yield of [11C]Ro 15-4513 was 30-40% with an overall sy...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02245279

    authors: Halldin C,Farde L,Litton JE,Hall H,Sedvall G

    更新日期:1992-01-01 00:00:00

  • Effects of venlafaxine in the sleep architecture of rats.

    abstract::Different venlafaxine doses (1, 5, and 10 mg/kg) and saline solution were administered to ten male Wistar rats (Latin-Square design). Compared with saline, venlafaxine produced a dose-related suppression of REM sleep and an increase in wake time while slow wave sleep was reduced. This effect is similar to the one that...

    journal_title:Psychopharmacology

    pub_type: 杂志文章

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    更新日期:1997-02-01 00:00:00

  • Aberrant glutamate signaling in the prefrontal cortex and striatum of the spontaneously hypertensive rat model of attention-deficit/hyperactivity disorder.

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    pub_type: 杂志文章

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    pub_type: 杂志文章

    doi:10.1007/BF00174059

    authors: Kantak KM,Miczek KA

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  • Prevention and reversal of social stress-escalated cocaine self-administration in mice by intra-VTA CRFR1 antagonism.

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    journal_title:Psychopharmacology

    pub_type: 杂志文章

    doi:10.1007/s00213-017-4676-8

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    更新日期:2017-09-01 00:00:00

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    pub_type: 杂志文章

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    更新日期:1996-10-01 00:00:00

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    pub_type: 杂志文章

    doi:10.1007/BF00435264

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    更新日期:1982-01-01 00:00:00

  • Opposite environmental regulation of heroin and amphetamine self-administration in the rat.

    abstract:RATIONALE:The circumstances of drug taking are thought to play a role in drug abuse but the evidence of it is anecdotal. Previous studies have shown that the intravenous self-administration of cocaine is facilitated in rats non-residing in the test chambers relative to rats that live in the test chambers at all times. ...

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    pub_type: 杂志文章

    doi:10.1007/s00213-008-1154-3

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    更新日期:2008-06-01 00:00:00

  • The effects of alaproclate on the pupillary responses to tyramine, phenylephrine and pilocarpine in depressed patients.

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    pub_type: 杂志文章

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    更新日期:1985-01-01 00:00:00

  • Intra-amygdala injections of corticotropin releasing factor facilitate inhibitory avoidance learning and reduce exploratory behavior in rats.

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    更新日期:1988-01-01 00:00:00

  • Prenatal exposure to escitalopram and/or stress in rats: a prenatal stress model of maternal depression and its treatment.

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    pub_type: 杂志文章

    doi:10.1007/s00213-013-3030-z

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  • The effect of acute and repeated electroconvulsive treatment on plasma beta-endorphin, growth hormone, prolactin and cortisol secretion in depressed patients.

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    doi:10.1007/BF02439598

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  • A comparison of the effects of d- and l-fenfluramine and d-amphetamine on energy and macronutrient intake in human subjects.

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    journal_title:Psychopharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

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    更新日期:1992-01-01 00:00:00

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    更新日期:2019-12-01 00:00:00