Analgesic properties of loperamide differ following systemic and local administration to rats after spinal nerve injury

European Journal of Pain (United Kingdom)

Volumn 16, Issue 7, 2012, Pages 1021-1032

  Chung, C ^a,b   Carteret, A F ^a   McKelvy, A D ^a   Ringkamp, M ^a   Yang, F ^a   Hartke, T V ^a   Dong, X ^a   Raja, S N ^a   Guan, Y ^a  

^a JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b FAR EASTERN MEMORIAL HOSPITAL   (Taiwan)

Author keywords

[No Author keywords available]

Indexed keywords

17 METHYLNALOXONE; ANALGESIC AGENT; LOPERAMIDE; NALTREXONE; NALTRINDOLE; NALOXONE;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINOCICEPTION; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; HYPERALGESIA; MALE; NERVE INJURY; NERVE LIGATION; NEUROPATHIC PAIN; NONHUMAN; PRIORITY JOURNAL; RAT; SPINAL NERVE; SPINE INJURY; ANALGESIA; ANIMAL; ANIMAL BEHAVIOR; DRUG EFFECT; HEAT; INJURY; METHODOLOGY; PAIN ASSESSMENT; PAIN THRESHOLD; PERIPHERAL NERVE INJURY; SPRAGUE DAWLEY RAT;

ANALGESIA; ANALGESICS; ANIMALS; BEHAVIOR, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; HOT TEMPERATURE; HYPERALGESIA; LOPERAMIDE; MALE; NALOXONE; PAIN MEASUREMENT; PAIN THRESHOLD; PERIPHERAL NERVE INJURIES; RATS; RATS, SPRAGUE-DAWLEY; SPINAL NERVES;

EID: 84871680212     PISSN: 10903801     EISSN: 15322149     Source Type: Journal    
DOI: 10.1002/j.1532-2149.2012.00148.x     Document Type: Article

References (53)

1. Baker, D.E. (2007). Loperamide: A pharmacological review. Rev Gastroenterol Disord 7(Suppl 3), S11-S18.
2. Binning, A.R., Przesmycki, K., Sowinski, P., Morrison, L.M., Smith, T.W., Marcus, P., Lees, J.P., Dahan, A. (2011). A randomised controlled trial on the efficacy and side-effect profile (nausea/vomiting/sedation) of morphine-6-glucuronide versus morphine for post-operative pain relief after major abdominal surgery. Eur J Pain 15, 402-408.
3. Brainin-Mattos, J., Smith, N.D., Malkmus, S., Rew, Y., Goodman, M., Taulane, J., Yaksh, T.L. (2006). Cancer-related bone pain is attenuated by a systemically available deltaopioid receptor agonist. Pain 122, 174-181.
4. Butelman, E.R., Harris, T.J., Kreek, M.J. (2004). Antiallodynic effects of loperamide and fentanyl against topical capsaicininduced allodynia in unanesthetized primates. J Pharmacol Exp Ther 311, 155-163.
5. Cavanaugh, D.J., Lee, H., Lo, L., Shields, S.D., Zylka, M.J., Basbaum, A.I., Anderson, D.J. (2009). Distinct subsets of unmyelinated primary sensory fibers mediate behavioral responses to noxious thermal and mechanical stimuli. Proc Natl Acad Sci U S A 106, 9075-9080.
6. Chao, T., Pham, K., Steward, O., Gupta, R. (2008). Chronic nerve compression injury induces a phenotypic switch of neurons within the dorsal root ganglia 189. J Comp Neurol 506, 180-193.
7. Chen, C.L., Broom, D.C., Liu, Y., de Nooij, J.C., Li, Z., Cen, C., Samad, O.A., Jessell, T.M., Woolf, C.J., Ma, Q. (2006). Runx1 determines nociceptive sensory neuron phenotype and is required for thermal and neuropathic pain. Neuron 49, 365-377.
8. Chu, X., Zhang, Z., Yabut, J., Horwitz, S., Levorse, J., Li, X.Q., Zhu, L., Lederman, H., Ortiga, R., Strauss, J., Li, X., Owens, K.A., Dragovic, J., Vogt, T.F., Evers, R., Shin, M.K. (2012). Characterization of multidrug resistance r1a/P-glycoprotein knockout rats generated by zinc finger nucleases. Mol Pharmacol 81, 220-227.
9. Cunha, T.M., Roman-Campos, D., Lotufo, C.M., Duarte, H.L., Souza, G.R., Verri, W.A. Jr, Funez, M.I., Dias, Q.M., Schivo, I.R., Domingues, A.C., Sachs, D., Chiavegatto, S., Teixeira, M.M., Hothersall, J.S., Cruz, J.S., Cunha, F.Q., Ferreira, S.H. (2010). Morphine peripheral analgesia depends on activation of the PI3Kgamma/AKT/nNOS/NO/KATP signaling pathway. Proc Natl Acad Sci U S A 107, 4442-4447.
10. Dahan, A., van Dorp, E., Smith, T., Yassen, A. (2008). Morphine- 6-glucuronide (M6G) for postoperative pain relief. Eur J Pain 12, 403-411.
11. Danzebrink, R.M., Green, S.A., Gebhart, G.F. (1995). Spinal mu and delta, but not kappa, opioid-receptor agonists attenuate responses to noxious colorectal distension in the rat. Pain 63, 39-47.
12. DeHaven-Hudkins, D.L., Burgos, L.C., Cassel, J.A., Daubert, J.D., DeHaven, R.N., Mansson, E., Nagasaka, H., Yu, G., Yaksh, T. (1999). Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther 289, 494-502.
13. Dobos, I., Toth, K., Kekesi, G., Joo, G., Csullog, E., Klimscha, W., Benedek, G., Horvath, G. (2003). The significance of intrathecal catheter location in rats. Anesth Analg 96, 487-492. table.
14. Elkiweri, I.A., Zhang, Y.L., Christians, U., Ng, K.Y., Tissot Van Patot, M.C., Henthorn, T.K. (2009). Competitive substrates for P-glycoprotein and organic anion protein transporters differentially reduce blood organ transport of fentanyl and loperamide: Pharmacokinetics and pharmacodynamics in Sprague- Dawley rats. Anesth Analg 108, 149-159.
15. Gordh, T., Chu, H., Sharma, H.S. (2006). Spinal nerve lesion alters blood-spinal cord barrier function and activates astrocytes in the rat. Pain 124, 211-221.
16. Guan, Y., Johanek, L.M., Hartke, T.V., Shim, B., Tao, Y.X., Ringkamp, M., Meyer, R.A., Raja, S.N. (2008). Peripherally acting mu-opioid receptor agonist attenuates neuropathic pain in rats after L5 spinal nerve injury. Pain 138, 318-329.
17. Hagiwara, K., Nakagawasai, O., Murata, A., Yamadera, F., Miyoshi, I., Tan-No, K., Tadano, T., Yanagisawa, T., Iijima, T., Murakami, M. (2003). Analgesic action of loperamide, an opioid agonist, and its blocking action on voltage-dependent Ca2+ channels. Neurosci Res 46, 493-497.
18. Hanauer, S.B. (2008). The role of loperamide in gastrointestinal disorders. Rev Gastroenterol Disord 8, 15-20.
19. Hargreaves, K., Dubner, R., Brown, F., Flores, C., Joris, J. (1988). A new and sensitive method for measuring thermal nociception in cutaneous hyperalgesia. Pain 32, 77-88.
20. Jang, J., Yaksh, T.L., Hill, H.F. (1992). Use of 2-hydroxypropylbeta- cyclodextrin as an intrathecal drug vehicle with opioids. J Pharmacol Exp Ther 261, 592-600.
21. Kabli, N., Cahill, C.M. (2007). Anti-allodynic effects of peripheral delta opioid receptors in neuropathic pain. Pain 127, 84-93.
22. Kalvass, J.C., Olson, E.R., Cassidy, M.P., Selley, D.E., Pollack, G.M. (2007). Pharmacokinetics and pharmacodynamics of seven opioids in P-glycoprotein-competent mice: Assessment of unbound brain EC50,u and correlation of in vitro, preclinical, and clinical data. J Pharmacol Exp Ther 323, 346-355.
23. Kim, K.J., Yoon, Y.W., Chung, J.M. (1997). Comparison of three rodent neuropathic pain models 157. Exp Brain Res 113, 200-206.
24. Kim, D.S., Yoon, C.H., Lee, S.J., Park, S.Y., Yoo, H.J., Cho, H.J. (2001). Changes in voltage-gated calcium channel alpha(1) gene expression in rat dorsal root ganglia following peripheral nerve injury 139. Brain Res Mol Brain Res 96, 151-156.
25. Labuz, D., Mousa, S.A., Schafer, M., Stein, C., Machelska, H. (2007). Relative contribution of peripheral versus central opioid receptors to antinociception. Brain Res 1160, 30-38.
26. McCleane, G., Smith, H.S. (2007). Opioids for persistent noncancer pain. Med Clin North Am 91, 177-197.
27. Menendez, L., Juarez, L., Garcia, V., Hidalgo, A., Baamonde, A. (2007). Involvement of nitric oxide in the inhibition of bone cancer-induced hyperalgesia through the activation of peripheral opioid receptors in mice. Neuropharmacology 53, 71-80.
28. Menendez, L., Lastra, A., Meana, A., Hidalgo, A., Baamonde, A. (2005). Analgesic effects of loperamide in bone cancer pain in mice. Pharmacol Biochem Behav 81, 114-121.
29. Nozaki-Taguchi, N., Yaksh, T.L. (1999). Characterization of the antihyperalgesic action of a novel peripheral mu-opioid receptor agonist - loperamide. Anesthesiology 90, 225-234.
30. Nozaki-Taguchi, N., Yaksh, T.L. (2002). Spinal and peripheral mu opioids and the development of secondary tactile allodynia after thermal injury. Anesth Analg 94, 968-974. Table.
31. Obara, I., Makuch, W., Spetea, M., Schutz, J., Schmidhammer, H., Przewlocki, R., Przewlocka, B. (2007). Local peripheral antinociceptive effects of 14-O-methyloxymorphone derivatives in inflammatory and neuropathic pain in the rat. Eur J Pharmacol 558, 60-67.
32. Obara, I., Parkitna, J.R., Korostynski, M., Makuch, W., Kaminska, D., Przewlocka, B., Przewlocki, R. (2009). Local peripheral opioid effects and expression of opioid genes in the spinal cord and dorsal root ganglia in neuropathic and inflammatory pain. Pain 141, 283-291.
33. Portoghese, P.S., Sultana, M., Takemori, A.E. (1988). Naltrindole, a highly selective and potent non-peptide delta opioid receptor antagonist. Eur J Pharmacol 146, 185-186.
34. Ringkamp, M., Tal, M., Hartke, T., Schaefer, K., Guan, Y., Raja, S., Meyer, R. (2011). Loperamide produces a conduction block in unmyelinated afferents. Soc Neurosci Abstr 274.22.
35. Robertson, B., Schulte, G., Elde, R., Grant, G. (1999). Effects of sciatic nerve injuries on delta-opioid receptor and substance P immunoreactivities in the superficial dorsal horn of the rat. Eur J Pain 3, 115-129.
36. Sasaki, A., Nakashima, Y., Takasaki, I., Andoh, T., Shiraki, K., Kuraishi, Y. (2007). Effects of loperamide on mechanical allodynia induced by herpes simplex virus type-1 in mice. J Pharmacol Sci 104, 218-224.
37. Sevostianova, N., Danysz, W., Bespalov, A.Y. (2005). Analgesic effects of morphine and loperamide in the rat formalin test: Interactions with NMDA receptor antagonists. Eur J Pharmacol 525, 83-90.
38. Shannon, H.E., Lutz, E.A. (2002). Comparison of the peripheral and central effects of the opioid agonists loperamide and morphine in the formalin test in rats. Neuropharmacology 42, 253-261.
39. Shinoda, K., Hruby, V.J., Porreca, F. (2007). Antihyperalgesic effects of loperamide in a model of rat neuropathic pain are mediated by peripheral delta-opioid receptors. Neurosci Lett 411, 143-146.
40. Stein, C., Lang, L.J. (2009). Peripheral mechanisms of opioid analgesia. Curr Opin Pharmacol 9, 3-8.
41. Stein, C., Schafer, M., Machelska, H. (2003). Attacking pain at its source: New perspectives on opioids. Nat Med 9, 1003-1008.
42. Stone, L.S., Vulchanova, L., Riedl, M.S., Williams, F.G., Wilcox, G.L., Elde, R. (2004). Effects of peripheral nerve injury on delta opioid receptor (DOR) immunoreactivity in the rat spinal cord. Neurosci Lett 361, 208-211.
43. Suter, M.R., Papaloizos, M., Berde, C.B., Woolf, C.J., Gilliard, N., Spahn, D.R., Decosterd, I. (2003). Development of neuropathic pain in the rat spared nerve injury model is not prevented by a peripheral nerve block. Anesthesiology 99, 1402-1408.
44. Svensson, C.I., Rew, Y., Malkmus, S., Schiller, P.W., Taulane, J.P., Goodman, M., Yaksh, T.L. (2003). Systemic and spinal analgesic activity of a delta-opioid-selective lanthionine enkephalin analog. J Pharmacol Exp Ther 304, 827-832.
45. Tal, M., Bennett, G.J. (1994). Extra-territorial pain in rats with a peripheral mononeuropathy: Mechano-hyperalgesia and mechano-allodynia in the territory of an uninjured nerve 588. Pain 57, 375-382.
46. Tan-No, K., Niijima, F., Nakagawasai, O., Sato, T., Satoh, S., Tadano, T. (2003). Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice. Eur J Pharm Sci 20, 357-363.
47. Tegeder, I., Meier, S., Burian, M., Schmidt, H., Geisslinger, G., Lotsch, J. (2003). Peripheral opioid analgesia in experimental human pain models. Brain 126, 1092-1102.
48. Tiseo, P.J., Yaksh, T.L. (1993). Dose-dependent antagonism of spinal opioid receptor agonists by naloxone and naltrindole: Additional evidence for delta-opioid receptor subtypes in the rat. Eur J Pharmacol 236, 89-96.
49. Vadivelu, N., Mitra, S., Hines, R.L. (2011). Peripheral opioid receptor agonists for analgesia: A comprehensive review. J Opioid Manag 7, 55-68.
50. Vasilyev, D.V., Shan, Q., Lee, Y., Mayer, S.C., Bowlby, M.R., Strassle, B.W., Kaftan, E.J., Rogers, K.E., Dunlop, J. (2007). Direct inhibition of Ih by analgesic loperamide in rat DRG neurons. J Neurophysiol 97, 3713-3721.
51. Yamamoto, T., Sakashita, Y. (1999). Differential effects of intrathecally administered morphine and its interaction with cholecystokinin-B antagonist on thermal hyperalgesia following two models of experimental mononeuropathy in the rat. Anesthesiology 90, 1382-1391.
52. Zhang, G., Mohammad, H., Peper, B.D., Raja, S., Wilson, S.P., Sweitzer, S.M. (2008). Enhanced peripheral analgesia using virally mediated gene transfer of the mu-opioid receptor in mice. Anesthesiology 108, 305-313.
53. Zollner, C., Stein, C. (2007). Opioids. Handb Exp Pharmacol 177, 31-63.