Pain and ketoprofen: what is its role in clinical practice?

Sarzi‐Puttini, Piercarlo; Atzeni, Fabiola; Lanata, Luigi; Bagnasco, Michela; Colombo, M.; Fischer, Florian; d’Imporzano, M.

doi:10.4081/reumatismo.2010.172

Cited by 33 publications

(31 citation statements)

References 74 publications

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“…In agreement with its clinical analgesic efficacy in veterinary and human medicine (Nolan, 2000;Sarzi-Puttini et al, 2010), ketoprofen in the present study blocked both acidstimulated stretching and acid-induced depression of ICSS at a dose that had no effect on ICSS in the absence of a noxious stimulus. These results are consistent with the interpretation that ketoprofen reduced sensitivity to the noxious stimulus without producing nonselective motor depressant or stimulant effects.…”

Section: Discussionsupporting

confidence: 71%

Effects of Peripherally Restricted κ Opioid Receptor Agonists on Pain-Related Stimulation and Depression of Behavior in Rats

Negus¹,

O'Connell²,

Morrissey³

et al. 2012

The Journal of Pharmacology and Experimental Therapeutics

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Opioid receptor agonists that do not readily cross the bloodbrain barrier are peripherally restricted and distribute poorly to the central nervous system after systemic administration. Peripherally restricted agonists have promise as candidate analgesics, because they may produce antinociception mediated by peripheral receptors more potently than they produce undesirable sedative and psychotomimetic effects mediated by central receptors. The present study used assays of painrelated stimulation and depression of behavior in rats to compare effects of 1) two peripherally restricted agonists [the, 2) a centrally penetrating agonist (salvinorin A), and 3) several reference drugs, including a nonsteroidal antiinflammatory drug (NSAID; ketoprofen). Intraperitoneal injection of dilute lactic acid served as a noxious stimulus to stimulate a stretching response and depress intracranial self-stimulation (ICSS) maintained by the delivery of electrical brain stimulation to the medial forebrain bundle. Acid-stimulated stretching was blocked by ketoprofen, the peripherally restricted agonists, and salvinorin A. However, acid-induced depression of ICSS was blocked only by ketoprofen. The peripherally restricted agonists had little effect, and salvinorin A exacerbated acidinduced depression of ICSS. These results suggest that peripherally restricted agonists may be safer than centrally penetrating agonists but less efficacious than NSAIDS or opioid receptor agonists to block pain-related depression of behavior; however, the peripheral selectivity of ffir and ICI204448 is limited, and future studies with agonists capable of greater peripheral selectivity are warranted.

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Section: Discussionsupporting

confidence: 71%

Effects of Peripherally Restricted κ Opioid Receptor Agonists on Pain-Related Stimulation and Depression of Behavior in Rats

Negus¹,

O'Connell²,

Morrissey³

et al. 2012

The Journal of Pharmacology and Experimental Therapeutics

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“…This lack of cannabinoid antinociception cannot be attributed to a lack of assay sensitivity. In the present study and a previous study (Negus et al, 2012a), the NSAID ketoprofen blocked acid-stimulated stretching and acid-induced depression of ICSS and feeding, and these data agree with the clinical efficacy of ketoprofen for the treatment of acute pain in animals (Flecknell, 2009) and humans (Sarzi-Puttini et al, 2010). Likewise, the -opioid receptor agonist and clinically effective analgesic morphine also blocked acid-stimulated stretching and acid-induced depression of ICSS in rats (Pereira Do Carmo et al, 2009;Negus et al, 2010b) and acid-induced depression of feeding in mice (Stevenson et al, 2006).…”

supporting

confidence: 78%

“…Feeding is reliably stimulated by THC and other cannabinoid agonists in the absence of pain (Williams et al, 1998;Miller et al, 2004;Jä rbe and DiPatrizio, 2005;Farrimond et al, 2011), suggesting that cannabinoids might be more effective in blocking acid-induced depression of feeding than acid-induced depression of ICSS. The nonsteroidal antiinflammatory drug (NSAID) and clinically effective analgesic ketoprofen (Flecknell, 2009;Sarzi-Puttini et al, 2010) was tested as a positive control in assays of acid-stimulated and acid-depressed behavior.…”

Section: Introductionmentioning

confidence: 99%

Dissociable Effects of the Cannabinoid Receptor Agonists Δ9-Tetrahydrocannabinol and CP55940 on Pain-Stimulated Versus Pain-Depressed Behavior in Rats

Kwilasz

Negus

2012

The Journal of Pharmacology and Experimental Therapeutics

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Cannabinoid receptor agonists produce reliable antinociception in most preclinical pain assays but have inconsistent analgesic efficacy in humans. This disparity suggests that conventional preclinical assays of nociception are not sufficient for the prediction of cannabinoid effects related to clinical analgesia. To extend the range of preclinical cannabinoid assessment, this study compared the effects of the marijuana constituent and low-efficacy cannabinoid agonist ⌬ 9 -tetrahydrocannabinol (THC) and the high-efficacy synthetic cannabinoid agonist 3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-4-(3-hydroxypropyl)cyclohexanol (CP55940) in assays of pain-stimulated and paindepressed behavior. Intraperitoneal injection of dilute lactic acid (1.8% in 1 ml/kg) stimulated a stretching response or depressed intracranial self-stimulation (ICSS) in separate groups of male Sprague-Dawley rats. THC (0.1-10 mg/kg) and CP55940 (0.0032-0.32 mg/kg) dose-dependently blocked acidstimulated stretching but only exacerbated acid-induced depression of ICSS at doses that also decreased control ICSS in the absence of a noxious stimulus. Repeated THC produced tolerance to sedative rate-decreasing effects of THC on control ICSS in the absence of the noxious stimulus but failed to unmask antinociception in the presence of the noxious stimulus. THC and CP55940 also failed to block pain-related depression of feeding in rats, although THC did attenuate satiationrelated depression of feeding. In contrast to the effects of the cannabinoid agonists, the clinically effective analgesic and nonsteroidal anti-inflammatory drug ketoprofen (1 mg/kg) blocked acid-stimulated stretching and acid-induced depression of both ICSS and feeding. The poor efficacy of THC and CP55940 to block acute pain-related depression of behavior in rats agrees with the poor efficacy of cannabinoids to treat acute pain in humans.

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“…Effect of Ketoprofen as an analgesic is very good and fast. 2 The problem of transdermal administration is a barrier provided by human skin for the drug to permeate. [3][4] Enhancer is one of methode that can approach amount of drug permeation in the transdermal drug design.…”

Section: Introductionmentioning

confidence: 99%

In vitro Permeation Study of Ketoprofen Patch with Combination of Ethylcellulose and Polyvynil Pyrrolidone as Matrix Polymers

Mita¹,

Husni²,

Setiyowati³

2018

JYP

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Pain and ketoprofen: what is its role in clinical practice?

Cited by 33 publications

References 74 publications

Effects of Peripherally Restricted κ Opioid Receptor Agonists on Pain-Related Stimulation and Depression of Behavior in Rats

Effects of Peripherally Restricted κ Opioid Receptor Agonists on Pain-Related Stimulation and Depression of Behavior in Rats

Dissociable Effects of the Cannabinoid Receptor Agonists Δ9-Tetrahydrocannabinol and CP55940 on Pain-Stimulated Versus Pain-Depressed Behavior in Rats

In vitro Permeation Study of Ketoprofen Patch with Combination of Ethylcellulose and Polyvynil Pyrrolidone as Matrix Polymers

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