Tizanidine increases antinociceptive effect and prevents gastric damage induced by ketorolac in the rat

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Abstract

Preclinical Research Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug (NSAID) effective in the treatment of moderate to severe pain. Tizanidine, an α-2-adrenoceptor agonist with myospasmolytic action, is indicated for the treatment of back pain either as monotherapy or in combination with NSAIDs. However, side effects may limit their use. As both drugs produce side effects that are dose dependent, a combination of these drugs appears in order to reduce the dose required for efficacy and, consequently, side effects. In this study, we evaluated the potential synergistic effect of these drugs in the thermal paw stimulation model and their effect on gastric ulcer production in response in the rat. Dose-response curves for ketorolac and tizanidine were constructed and from these, an ED40 value was obtained. Isobolographic analysis was carried out based on 0.5:0.5 proportions. In addition, protective effect of tizanidine against ketorolac-induced gastric damage was evaluated. A synergistic interaction in thermal hyperalgesia and gastroprotective activity was observed, suggesting a good therapeutic potential of this combination in the treatment of pain. © 2012 Wiley Periodicals, Inc.
Original languageAmerican English
Pages (from-to)38-42
Number of pages5
JournalDrug Development Research
DOIs
StatePublished - 1 Feb 2013

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Ketorolac
Stomach
Ketorolac Tromethamine
Pain
Hyperalgesia
Non-Steroidal Anti-Inflammatory Agents
Drug Combinations
Stomach Ulcer
Therapeutics
Back Pain
Drug-Related Side Effects and Adverse Reactions
Pharmaceutical Preparations
Adrenergic Receptors
Anti-Inflammatory Agents
Hot Temperature
tizanidine
Research

Cite this

@article{d543f4141ad94ea09dd26bac5bb9618b,
title = "Tizanidine increases antinociceptive effect and prevents gastric damage induced by ketorolac in the rat",
abstract = "Preclinical Research Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug (NSAID) effective in the treatment of moderate to severe pain. Tizanidine, an α-2-adrenoceptor agonist with myospasmolytic action, is indicated for the treatment of back pain either as monotherapy or in combination with NSAIDs. However, side effects may limit their use. As both drugs produce side effects that are dose dependent, a combination of these drugs appears in order to reduce the dose required for efficacy and, consequently, side effects. In this study, we evaluated the potential synergistic effect of these drugs in the thermal paw stimulation model and their effect on gastric ulcer production in response in the rat. Dose-response curves for ketorolac and tizanidine were constructed and from these, an ED40 value was obtained. Isobolographic analysis was carried out based on 0.5:0.5 proportions. In addition, protective effect of tizanidine against ketorolac-induced gastric damage was evaluated. A synergistic interaction in thermal hyperalgesia and gastroprotective activity was observed, suggesting a good therapeutic potential of this combination in the treatment of pain. {\circledC} 2012 Wiley Periodicals, Inc.",
author = "Juan Rodr{\'i}guez-Silverio and S{\'a}nchez-Mendoza, {Mar{\'i}a Elena} and Jes{\'u}s Arrieta-Valencia and Rocha-Gonzalez, {H{\'e}ctor Isaac} and Flores-Murrieta, {Francisco Javier}",
year = "2013",
month = "2",
day = "1",
doi = "10.1002/ddr.21054",
language = "American English",
pages = "38--42",
journal = "Drug Development Research",
issn = "0272-4391",
publisher = "John Wiley and Sons Inc.",

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TY - JOUR

T1 - Tizanidine increases antinociceptive effect and prevents gastric damage induced by ketorolac in the rat

AU - Rodríguez-Silverio, Juan

AU - Sánchez-Mendoza, María Elena

AU - Arrieta-Valencia, Jesús

AU - Rocha-Gonzalez, Héctor Isaac

AU - Flores-Murrieta, Francisco Javier

PY - 2013/2/1

Y1 - 2013/2/1

N2 - Preclinical Research Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug (NSAID) effective in the treatment of moderate to severe pain. Tizanidine, an α-2-adrenoceptor agonist with myospasmolytic action, is indicated for the treatment of back pain either as monotherapy or in combination with NSAIDs. However, side effects may limit their use. As both drugs produce side effects that are dose dependent, a combination of these drugs appears in order to reduce the dose required for efficacy and, consequently, side effects. In this study, we evaluated the potential synergistic effect of these drugs in the thermal paw stimulation model and their effect on gastric ulcer production in response in the rat. Dose-response curves for ketorolac and tizanidine were constructed and from these, an ED40 value was obtained. Isobolographic analysis was carried out based on 0.5:0.5 proportions. In addition, protective effect of tizanidine against ketorolac-induced gastric damage was evaluated. A synergistic interaction in thermal hyperalgesia and gastroprotective activity was observed, suggesting a good therapeutic potential of this combination in the treatment of pain. © 2012 Wiley Periodicals, Inc.

AB - Preclinical Research Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug (NSAID) effective in the treatment of moderate to severe pain. Tizanidine, an α-2-adrenoceptor agonist with myospasmolytic action, is indicated for the treatment of back pain either as monotherapy or in combination with NSAIDs. However, side effects may limit their use. As both drugs produce side effects that are dose dependent, a combination of these drugs appears in order to reduce the dose required for efficacy and, consequently, side effects. In this study, we evaluated the potential synergistic effect of these drugs in the thermal paw stimulation model and their effect on gastric ulcer production in response in the rat. Dose-response curves for ketorolac and tizanidine were constructed and from these, an ED40 value was obtained. Isobolographic analysis was carried out based on 0.5:0.5 proportions. In addition, protective effect of tizanidine against ketorolac-induced gastric damage was evaluated. A synergistic interaction in thermal hyperalgesia and gastroprotective activity was observed, suggesting a good therapeutic potential of this combination in the treatment of pain. © 2012 Wiley Periodicals, Inc.

U2 - 10.1002/ddr.21054

DO - 10.1002/ddr.21054

M3 - Article

SP - 38

EP - 42

JO - Drug Development Research

JF - Drug Development Research

SN - 0272-4391

ER -