Ambroxol, a Nav1.8-preferring Na+ channel blocker, effectively suppresses pain symptoms in animal models of chronic, neuropathic and inflammatory pain

Neuropharmacology

Volumn 49, Issue 8, 2005, Pages 1220-1227

  Gaida, Wolfram ^a   Klinder, Klaus ^a   Arndt, Kirsten ^a   Weiser, Thomas ^a  

^a BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

Author keywords

Ambroxol; Chronic pain; Inflammatory pain; Na+ channel; Nav1.8; Neuropathic pain

Indexed keywords

AMBROXOL; FORMALDEHYDE; GABAPENTIN; SODIUM CHANNEL; SODIUM CHANNEL BLOCKING AGENT;

ALLODYNIA; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINOCICEPTION; ARTICLE; CHRONIC PAIN; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG EFFECT; HYPERALGESIA; MALE; MONARTHRITIS; MONONEUROPATHY; NEONATAL RESPIRATORY DISTRESS SYNDROME; NEUROPATHIC PAIN; NONHUMAN; PAIN ASSESSMENT; PAIN THRESHOLD; PAW EDEMA; PRIORITY JOURNAL; RAT;

AMBROXOL; AMINES; ANALGESICS; ANIMALS; BEHAVIOR, ANIMAL; CONSTRICTION, PATHOLOGIC; CYCLOHEXANECARBOXYLIC ACIDS; DOSE-RESPONSE RELATIONSHIP, DRUG; EXCITATORY AMINO ACID ANTAGONISTS; FORMALDEHYDE; GAMMA-AMINOBUTYRIC ACID; INFLAMMATION; LIGATION; MALE; NERVE TISSUE PROTEINS; PAIN; PAIN MEASUREMENT; RATS; RATS, WISTAR; SCIATIC NEUROPATHY; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS;

EID: 27744521224     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2005.08.004     Document Type: Article

References (49)

1. I. Akiba, T. Seki, M. Mori, M. Iizuka, S. Nishimura, S. Sasaki, K. Imoto, and E.L. Barsoumian Stable expression and characterization of human PN1 and PN3 sodium channels Receptors and Channels 9 5 2003 291 299
2. S.K. Back, S.Y. Won, S.K. Hong, and H.S. Na Gabapentin relieves mechanical, warm and cold allodynia in a rat model of peripheral neuropathy Neuroscience Letters 368 3 2004 341 344
3. + channels in pain pathways Trends in Pharmacological Science 22 1 2001 27 31
4. G.J. Bennett, and Y.K. Xie A peripheral mononeuropathy in rat that produces disorders of pain sensation like those seen in man Pain 33 1 1988 87 107
5. S.M. Carlton, and S. Zhou Attenuation of formalin-induced nociceptive behaviors following local peripheral injection of gabapentin Pain 76 1-2 1998 201 207
6. O. Chiara, G. Bevilacqua, P. Padalino, P. Guadalupi, L. Bigatello, and A. Nespoli The prevention of postoperative ARDS. Double-blind clinical testing about the effects of ambroxol on pulmonary gas exchange Urgentis Chirurgiae Commentaria 6 1/2 1983 1 6
7. W. Couet, J. Girault, B.G. Reigner, I. Ingrand, J. Bizouard, D. Acerbi, P. Chiesi, and J.B. Fourtillan Steady-state bioavailability and pharmacokinetics of ambroxol and clenbuterol administered alone or combined in a new oral formulation. International Journal of Clinical Pharmacology Therapy and Toxicology 27 9 1989 467 472
8. F.E. D'Amour, and D.L. Smith A method for determining loss of pain sensation Journal of Pharmacology and Experimental Therapeutics 72 1941 74 79
9. + channel blockers in two rat models of neuropathic pain European Journal of Pharmacology 458 3 2003 275 282
10. D. Faroongsarng, M. Rojpibulstit, S. Kasiwong, and N. Phadoongsombat Ambroxol lozenge bioavailability: part II - analysis of additional systemic availability Clinical Drug Investigation 24 11 2004 681 688
11. F.M. Ferrante, J. Paggiol, S. Cherukuri, and G.R. Arthur The analgesic response to intravenous lidocaine in the treatment of neuropathic pain Anaesthesia and Analgesia 82 1996 91 97
12. M.J. Field, M.I. Gonzalez, R.J. Tallarida, and L. Singh Gabapentin and the neurokinin(1) receptor antagonist CI-1021 act synergistically in two rat models of neuropathic pain Journal of Pharmacology and Experimental Therapeutics 303 2 2002 730 735
13. M.J. Field, S. McCleary, J. Hughes, and L. Singh Gabapentin and pregabalin, but not morphine and amitriptyline, block both static and dynamic components of mechanical allodynia induced by streptozocin in the rat Pain 80 1-2 1999 391 398
14. A. Fox, C. Gentry, S. Patel, A. Kesingland, and S. Bevan Comparative activity of the anti-convulsants oxcarbazepine, carbamazepine, lamotrigine and gabapentin in a model of neuropathic pain in the rat and guinea-pig Pain 105 1-2 2003 355 362
15. I. Hirotsu, T. Kihara, S. Nakamura, Y. Hattori, M. Hatta, Y. Kitakaze, K. Takahama, Y. Hashimoto, T. Miyata, T. Ishihara, and F. Satoh General pharmacological studies on N-(2,6-dimethylphenyl)-8- pyrrolizidineacetamide hydrochloride hemihydrate. 1st Communication: effect on the central nervous system Arzneimittelforschung (Drug Research) 38 10 1988 1398 1409
16. J.C. Hunter, K.R. Gogas, L.R. Hedley, L.O. Jacobson, L. Kassotakis, J. Thompson, and D.J. Fontana The effect of novel anti-epileptic drugs in rat experimental models of acute and chronic pain European Journal of Pharmacology 324 2-3 1997 153 160
17. R.W. Hurley, D. Chatterjea, M. Rose Feng, C.P. Taylor, and D.L. Hammond Gabapentin and pregabalin can interact synergistically with naproxen to produce antihyperalgesia Anesthesiology 97 5 2002 1263 1273
18. L. Igwemezie, G.N. Beatch, M.J.A. Walker, and K.M. McErlane Tissue distribution of mexiletine enantiomers in rats Xenobiotica 21 9 1991 1153 1158
19. B. Jarvis, and A.J. Coukell Mexiletine: a review of its therapeutic use in painful diabetic neuropathy Drugs 56 4 1998 691 707
20. P. Jequier, R. Jones, and A. Mackintosh Fatal mexiletine overdose Lancet 1 1976 429
21. M.F. Jett, J. McGuirk, D. Waligora, and J.C. Hunter The effects of mexiletine, desipramine and fluoxetine in rat models involving central sensitization Pain 69 1/2 1997 161 169
22. S. Kiguchi, T. Imamura, K. Ichikawa, and M. Kojima Oxcarbazepine antinociception in animals with inflammatory pain or painful diabetic neuropathy Clinical and Experimental Pharmacology and Physiology 31 1-2 2004 57 64
23. Y. Kimya, S. Kucukkomurcu, H. Ozan, and G. Uncu Antenatal ambroxol usage in the prevention of infant respiratory distress syndrome - beneficial and adverse effects Clinical and Experimental Obstetrics and Gynecology 22 3 1995 204 211
24. J. Lai, M.S. Gold, C.S. Kim, D. Bian, M.H. Ossipov, J.C. Hunter, and F. Porreca Inhibition of neuropathic pain by decreased expression of the tetrodotoxin-resistant sodium channel, NaV1.8 Pain 95 1-2 2002 143 152
25. H.J. Lee, S.K. Joung, Y.G. Kim, J.Y. Yoo, and S.B. Han Bioequivalence assessment of ambroxol tablet after a single oral dose administration to healthy male volunteers Pharmacological Research 49 1 2004 93 98
26. Z. Li, X. Xu, and Y. Shen Bioequivalence evaluation of domestic ambroxol hydrochloride tablets in healthy subjects Chinese Pharmacological Journal (Beijing) 34 8 1999 541 543
27. M. Luerti, A. Lazzarin, E. Corbella, and G. Zavattini An alternative to steroids for prevention of respiratory distress syndrome (RDS): multicenter controlled study to compare ambroxol and betamethasone Journal of Perinatal Medicine 15 1987 227 238
28. M. Mezzetti, L. Colombo, M.G. Marini, V. Crusi, P. Pierfederici, and E. Mussini A pharmacokinetic study on pulmonary tropism of ambroxol in patients under thoracic surgery Journal of Emergency Surgery and Intensive Care 13 3 1990 179 185
29. S. Nagasako, M. Hayashibara, Y. Katagiri, and K. Iwamoto Salivary excretion of mexiletine after bolus intravenous administration in rats Journal of Pharmacy and Pharmacology 44 1992 55 57
30. M. Nobilis, J. Pastera, D. Svoboda, J. Kvetina, and K. Macek High-performance liquid chromatographic determination of ambroxol in human plasma Journal of Chromatography (B) Biomedical Applications 581 1992 251 255
31. K. Ohashi, A. Ebihara, T. Hashimoto, S. Hosoda, K. Kondo, and T. Oka Pharmacokinetics and the anti-arrhythmic effect of mexiletine in patients with chronic ventricular arrhythmias Arzneimittelforschung (Drug Research) 34 1984 503 507
32. B. Oosterhuis, G. Storm, P.J.G. Cornelissen, C.A.P.F. Su, F.A.E. Sollie, and J.H.G. Jonkman Dose-dependent uricosuric effect of ambroxol European Journal of Clinical Pharmacology 44 3 1993 237 241
33. S. Patel, S. Naeem, A. Kesingland, W. Froestl, M. Capogna, L. Urban, and A. Fox The effects of GABA(B) agonists and gabapentin on mechanical hyperalgesia in models of neuropathic and inflammatory pain in the rat Pain 90 3 2001 217 226
34. S. Püschmann, and R. Engelhorn Pharmacological study on the bromhexine-metabolite ambroxol Arzneimittelforschung (Drug Research) 28 1978 889 898
35. T.P. Rohrig, and L.E. Harty Postmortem distribution of mexiletine in a fatal overdose Journal of Analytical Toxicology 18 6 1994 354 356
36. M. Rojpibulstit, S. Kasiwong, S. Juthong, N. Phadoongsombat, and D. Faroongsarng Ambroxol lozenge bioavailability: an open-label, two-way crossover study of the comparative bioavailability of ambroxol lozenges and commercial tablets in healthy Thai volunteers Clinical Drug Investigation 23 4 2003 273 280
37. M.A. Rose, and P.C. Kam Gabapentin: pharmacology and its use in pain management Anaesthesia 57 5 2002 451 462
38. G.J. Schillings, and J. Probst Ambroxol in the treatment of ARDS in polytraumatised patients - a report Klinikarzt 21 8 1992 2 8
39. + currents by lidocaine and bupivacaine reduce firing frequency in DRG neurons Journal of Neurophysiology 79 1998 1746 1754
40. A. Scholz, and W. Vogel Tetrodotoxin-resistant action potentials in dorsal root ganglion neurons are blocked by local anesthetics Pain 89 2000 47 52
41. Z. Seltzer, R. Dubner, and Y. Shir A novel behavioral model of neuropathic pain disorders produced in rats by partial sciatic nerve injury Pain 43 2 1990 205 218
42. C.J. Sinnott, J.M. Garfield, A. Zeitlin, S. Teo, M. Wu, J. Chen, S.L. Shafer, and G.R. Strichartz Enantioselective relief of neuropathic pain by systemic mexiletine in the rat Journal of Pain 1 2 2000 128 137
43. H. Vergin, G.B. Bishop-Freudling, M. Miczka, V. Nitsche, K. Strobel, and F. Matzkies Pharmacokinetics and bioequivalence of different formulations of ambroxol Arzneimittelforschung (Drug Research) 35 10 1985 1591 1595
44. J. Villacampa, F. Alcantar, J.M. Rodriguez, J.M. Morales, J. Herrera, and R. Rosete Pharmacokinetic properties of single-dose loratadine and ambroxol alone and combined in tablet formulations in healthy men Clinical Therapeutics 25 8 2003 2225 2232
45. K.O. Vollmer, A. von Hodenberg, and E.U. Kolle Pharmacokinetics and metabolism of gabapentin in rat, dog and man Arzneimittelforschung (Drug Research) 36 5 1986 830 839
46. H. Wada, Y. Takesue, N. Nishikawa, T. Makita, and Y. Hashimoto Toxicological studies on ambroxol (NA-872). (1) Acute toxicity in mice and rats Iyakuhin Kenkyu 12 1981 263 272
47. T. Weiser, Y. Qu, W.A. Catterall, and T. Scheuer Differential interaction of R-mexiletine with the local anesthetic receptor site on brain and heart sodium channel alpha-subunits Molecular Pharmacology 56 6 1999 1238 1244
48. T. Weiser, and N. Wilson Inhibition of tetrodotoxin (TTX)-resistant and TTX-sensitive neuronal Na(+) channels by the secretolytic ambroxol Molecular Pharmacology 62 3 2002 433 438
49. G. Woolfe, and A.D. MacDonald The evaluation of the analgesic action of pethidine hydrochloride (Demerol) Journal of Pharmacology and Experimental Therapeutics 80 1944 300 307