Antinociceptive effects of tramadol in co-administration with metamizol after single and repeated administrations in rats

Moreno-Rocha, Luis Alfonso; Domínguez-Ramírez, Adriana Miriam; Cortés-Arroyo, Alma Rosa; Bravo, Gerardo Ferrando; López‐Muñoz, Francisco

doi:10.1016/j.pbb.2012.07.011

Cited by 18 publications

(13 citation statements)

References 42 publications

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“…The results obtained after administration of the combination of metamizol and tramadol after a single dose, confirmed the potentiation of the antinociceptive effect elicited by the drugs given alone ( P < 0.05). Similar results were found with this combination using the “plantar test model” (Moreno-Rocha et al, 2012).…”

Section: Discussionsupporting

confidence: 82%

“…The development of tolerance to the antinociceptive effect was significantly increased with the drug co-administration of both drugs. An increase in the rate of development of tolerance to the antinociceptive effect of metamizol co-administered with tramadol was previously reported using the plantar-test model (Moreno-Rocha et al, 2012). Nevertheless, when the effect attained by the combination after chronic treatment was compared with the effect of the individual drugs after the 4-day treatment, an increase in the global effect was observed ( P < 0.05), which is equivalent to the sum of the individual effects (additive effect).…”

Section: Discussionmentioning

confidence: 65%

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Effect of tramadol on metamizol pharmacokinetics and pharmacodynamics after single and repeated administrations in arthritic rats

Moreno-Rocha

López‐Muñoz

López

et al. 2016

Saudi Pharmaceutical Journal

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Combined administration of certain doses of opioid compounds with a non-steroidal anti-inflammatory drug can produce additive or supra-additive effects while reducing unwanted effects. We have recently reported that co-administration of metamizol with tramadol produces antinociceptive effect potentiation, after acute treatment. However, none information about the effect produced by the combination after chronic or repeated dose administration exists. The aims of this study were to investigate whether the antinociceptive synergism produced by the combination of metamizol and tramadol (177.8 + 17.8 mg/kg, s.c. respectively) is maintained after repeated treatment and whether the effects observed are primarily due to pharmacodynamic interactions or may be related to pharmacokinetics changes. Administration of metamizol plus tramadol acute treatment significantly enhanced the antinociceptive effect of the drugs given alone ( < 0.05). Nevertheless, this effect decreased about 53% after the chronic treatment (3 doses per day, for 4 days). No pharmacokinetic interaction between metamizol and tramadol was found under acute treatment ( > 0.05). The mechanism involved in the synergism of the antinociceptive effect observed with the combination of metamizol and tramadol in single dose cannot be attributed to a pharmacokinetic interaction, and other pharmacodynamic interactions have to be considered. On the other hand, when metamizol and tramadol were co-administered under repeated administrations, a pharmacokinetic interaction and tolerance development occurred. Differences found in metamizol active metabolites' pharmacokinetics ( < 0.05) were related to the development of tolerance produced by the combination after repeated doses. This work shows an additional preclinical support for the combination therapy. The clinical utility of this combination in a suitable dose range should be evaluated in future studies.

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Section: Discussionsupporting

confidence: 82%

Section: Discussionmentioning

confidence: 65%

Effect of tramadol on metamizol pharmacokinetics and pharmacodynamics after single and repeated administrations in arthritic rats

Moreno-Rocha

López‐Muñoz

López

et al. 2016

Saudi Pharmaceutical Journal

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“…Tolerance is a pharmacological phenomenon that often occurs during prolong drug treatment. For example, daily treatment with the opioids tramadol or morphine at an antinociceptive dose for 4 to 7 days is sufficient to induce significant tolerance to their antinociceptive effects 10 11 . Twice daily treatment with the cannabinoid delta9-tetrahydrocannabinol for 9 days leads to greater than 4-fold rightward shift of the delta9-tetrahydrocannabinol dose-effect curve in its antinociceptive effects 12 .…”

Section: Discussionmentioning

confidence: 99%

Antinociceptive effects of sinomenine in a rat model of neuropathic pain

Zhu

Sun

Zhu

et al. 2014

Sci Rep

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Sinomenine is a principal ingredient of traditional Chinese medicine, Sinomenium Acutum, which has been reported to have various pharmacological effects including anti-rheumatism and immunomodulation. This study examined the effects of sinomenine in rats that received chronic constriction injury (CCI), a model of peripheral neuropathic pain. CCI injury on the right sciatic nerve led to long-lasting mechanical hyperalgesia. Acute sinomenine treatment (10–40 mg/kg, i.p.) significantly and dose-dependently reversed mechanical hyperalgesia. In addition, the antinociceptive effects of sinomenine remained stable during repeated daily treatment for up to 2 weeks. Although sinomenine did not alter the duration of immobility in the forced swimming test in healthy animals, it dose-dependently reversed the increased immobility time in rats receiving CCI, suggesting that sinomenine attenuated chronic pain-induced depressive-like behavior. The antinociceptive effects of sinomenine were blocked by the GABAa receptor antagonist bicuculine. The doses of sinomenine studied here did not significantly alter the spontaneous locomotor activity. Together, these results suggested that sinomenine exerts significant antinociceptive effects for neuropathic pain via GABAa-mediated mechanism, which suggests that sinomenine may be useful for the management of chronic painful conditions such as neuropathic pain.

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“…Furthermore, combining agents with different modes of action may provide multimodal coverage of a broad spectrum of pain (Raffa, 2001). Several studies on combinations of opioids with drugs belonging to other classes have been conducted in various animal models (Argüelles et al, 2002;Díaz-Reval et al, 2010;Espinoza et al, 2012;Moreno-Rocha et al, 2012;Zhang et al, 2011). Flupirtine (FLP) is a centrally acting non-opioid analgesic, without antipyretic or anti-inflammatory effects (Singal et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test

Lee

Vito

Giorgi

et al. 2015

European Journal of Pharmacology

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Antinociceptive effects of tramadol in co-administration with metamizol after single and repeated administrations in rats

Cited by 18 publications

References 42 publications

Effect of tramadol on metamizol pharmacokinetics and pharmacodynamics after single and repeated administrations in arthritic rats

Effect of tramadol on metamizol pharmacokinetics and pharmacodynamics after single and repeated administrations in arthritic rats

Antinociceptive effects of sinomenine in a rat model of neuropathic pain

Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test

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