Tolerance to the analgesic effect of buprenorphine, butorphanol, nalbuphine, and cyclorphan, and cross-tolerance to morphine

Gringauz, Michael; Rabinowitz, Ruth; Stav, Anatoli; Korczyn, Amos D.

doi:10.1007/s005400170004

Cited by 16 publications

(10 citation statements)

References 13 publications

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“…Previous studies have failed to reveal cross tolerance between the rate-decreasing effects of morphine and nalbuphine in assays of schedule-controlled responding for food (Oliveto et al , 1991; Picker and Yarbrough, 1991; Smith et al , 1997), but nalbuphine rate-decreasing effects in these studies occurred only at high doses, were variable across subjects, and may have been associated with precipitated withdrawal during morphine treatment (see below). The present findings agree with previous reports of cross tolerance between other effects of morphine and nalbuphine, such as discriminative stimulus effects (Walker et al , 1997) and thermal antinociceptive effects (Gringauz et al , 2001). …”

Section: Discussionsupporting

confidence: 93%

Abuse-related effects of µ-opioid analgesics in an assay of intracranial self-stimulation in rats

Altarifi

Rice

Negus

2013

Behavioural Pharmacology

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Intracranial self-stimulation (ICSS) is an operant procedure in which responding is maintained by electrical brain stimulation. Stimulation frequency can be rapidly varied to maintain a wide range of baseline response rates, and drugs effects can be simultaneously evaluated on both low ICSS rates maintained by low stimulation frequencies and high ICSS rates maintained by high stimulation frequencies. ICSS “facilitation” denotes drug-induced increases in low ICSS rates and is often interpreted as an abuse-related effect, whereas ICSS “depression” denotes decreases in high ICSS rates and may indicate abuse-limiting effects. This study examined the roles of drug efficacy and of prior mu agonist exposure as determinants of mu agonist effects on ICSS in rats with electrodes implanted in the medial forebrain bundle. The high-, intermediate- and low-efficacy mu agonists methadone, fentanyl and nalbuphine were tested during escalating regimens of morphine exposure (Vehicle, 3.2, 18 mg/kg/day). During vehicle treatment, methadone and fentanyl primarily depressed ICSS, whereas nalbuphine produced weak facilitation that was not dose-dependent. Chronic morphine produced tolerance to ICSS depression and increased expression of ICSS facilitation. These results suggest that mu agonist exposure increases expression of abuse-related ICSS facilitation by mu agonists with a broad range of efficacies at mu receptors.

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Section: Discussionsupporting

confidence: 93%

Abuse-related effects of µ-opioid analgesics in an assay of intracranial self-stimulation in rats

Altarifi

Rice

Negus

2013

Behavioural Pharmacology

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“…A high degree of cross-tolerance develops between different opioid compounds that are acting through the same receptor (Craft and Dykstra 1990;Moulin et al 1988). Morphine and buprenorphine show considerable cross-tolerance to analgesia (Barrett et al 2001;Gringauz et al 2001;Walker and Young 2001), consistent with findings that the μ-opioid receptor is critical for the analgesic effects of both agonists (Ide et al 2004;Sora et al 1997). However, the extent to which buprenorphine and morphine show cross-tolerance in their anxiolytic-like effects is not known.…”

supporting

confidence: 66%

Anxiolytic-like effects of morphine and buprenorphine in the rat model of fear-potentiated startle: tolerance, cross-tolerance, and blockade by naloxone

Glover

Davis

2008

Psychopharmacology

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“…assays of acid-stimulated stretching in rats and mice (Cowan et al, 1977;Fürst, 1991;Stevenson et al, 2006;Pereira Do Carmo et al, 2009). Previous studies have also shown that m-opioid agonists block other examples of pain-stimulated behavior, such as tail-or paw-withdrawal responses from noxious thermal stimuli Holtzman, 1991, 1992;Gringauz et al, 2001;Taracha et al, 2009) or withdrawal responses in subjects rendered hypersensitive to thermal or mechanical stimuli by inflammatory or neuropathic manipulations (Wang et al, 2006;Cobos et al, 2012;Jagla et al, 2014). m-Agonist effects on pain-stimulated behaviors are often interpreted as evidence consistent with clinical analgesic efficacy .…”

Section: Discussionmentioning

confidence: 99%

Effects of μ-Opioid Receptor Agonists in Assays of Acute Pain-Stimulated and Pain-Depressed Behavior in Male Rats: Role of μ-Agonist Efficacy and Noxious Stimulus Intensity

Altarifi

Rice

Negus

2015

The Journal of Pharmacology and Experimental Therapeutics

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Pain is associated with stimulation of some behaviors and depression of others, and m-opioid receptor agonists are among the most widely used analgesics. This study used parallel assays of pain-stimulated and pain-depressed behavior in male SpragueDawley rats to compare antinociception profiles for six m-agonists that varied in efficacy at m-opioid receptors (from highest to lowest: methadone, fentanyl, morphine, hydrocodone, buprenorphine, and nalbuphine). Intraperitoneal injection of diluted lactic acid served as an acute noxious stimulus to either stimulate stretching or depress operant responding maintained by electrical stimulation in an intracranial self-stimulation (ICSS). All m-agonists blocked both stimulation of stretching and depression of ICSS produced by 1.8% lactic acid. The high-efficacy agonists methadone and fentanyl were more potent at blocking acid-induced depression of ICSS than acid-stimulated stretching, whereas lowerefficacy agonists displayed similar potency across assays. All m-agonists except morphine also facilitated ICSS in the absence of the noxious stimulus at doses similar to those that blocked acid-induced depression of ICSS. The potency of the low-efficacy m-agonist nalbuphine, but not the high-efficacy m-agonist methadone, to block acid-induced depression of ICSS was significantly reduced by increasing the intensity of the noxious stimulus to 5.6% acid. These results demonstrate sensitivity of acid-induced depression of ICSS to a range of clinically effective m-opioid analgesics and reveal distinctions between opioids based on efficacy at the m-receptor. These results also support the use of parallel assays of pain-stimulated and -depressed behaviors to evaluate analgesic efficacy of candidate drugs.

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Tolerance to the analgesic effect of buprenorphine, butorphanol, nalbuphine, and cyclorphan, and cross-tolerance to morphine

Abstract: Of the four agonist-antagonists tested, butorphanol seems to be least likely to produce cross-tolerance with morphine.

Cited by 16 publications

References 13 publications

Abuse-related effects of µ-opioid analgesics in an assay of intracranial self-stimulation in rats

Abuse-related effects of µ-opioid analgesics in an assay of intracranial self-stimulation in rats

Anxiolytic-like effects of morphine and buprenorphine in the rat model of fear-potentiated startle: tolerance, cross-tolerance, and blockade by naloxone

Effects of μ-Opioid Receptor Agonists in Assays of Acute Pain-Stimulated and Pain-Depressed Behavior in Male Rats: Role of μ-Agonist Efficacy and Noxious Stimulus Intensity

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