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     Capsaicin

     Lidocaine

     Opiates

     Paclitaxel and Gabapentin

     Resiniferatoxin (RTX)

    Tolterodine

 

 

 

Capsaicin - Capsaicin selectively binds to the to the transient receptor potential cation channel, subfamily V, member 1 (TRPV1). TRPV1 stimulates and then inactivates heat and vanilloid-responsive nociceptive neurons, namely small myelinated Aδ and unmyelinated C fibers with no effect on the large myelinated Aβ fibers.(a, b)

a)  Caterina MJ, Schumacher MA, Tominaga M, Rosen TA, Levine JD, Julius D. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature. 1997;389:816–824.
b)  Helliwell RJ, McLatchie LM, Clarke M, Winter J, Bevan S, McIntyre P. Capsaicin sensitivity is associated with the expression of the vanilloid (capsaicin) receptor (VR1) mRNA in adult rat sensory ganglia. Neurosci Lett. 1998;250:177–180.

  1. Fujiuchi, A., Toga, T. Pharmacologocal effect of capsaicin on rat avoidance behaviours elicited by sine-wave electrical stimulation of different frequencies by Neurometer. Journal of Pharmacy and Pharmacology Vol. 60(4):467-71, 2008.

  2. Lee, Y-S., Kho, H-S., Kim, Y-K., Chung, S-C. Influence of Topical Capsaicin on Facial Sensitivity in Response to Experimental Pain. Journal of Oral Rehabilitation. Vol 34(1):9-14, 2006,

  3. Kiso, T., Nagakura,, Y., Toya, T., Matsumoto, N., Tamura, S., Ito, H., Okada, M., Yamaguchi, T. Neurometer measurement of current stimulus threshold in rats. The Journal of Pharmacology and Experimental Therapeutics, Vol 297(1):352-356, 2001.

  4. Matsumoto M, Inoue M, Hald A, Yamaguchi A, Ueda H: Characterization of three different sensory fibers by use of neonatal capsaicin treatment, spinal antagonism and a novel electrical stimulation-induced paw flexion test. Molecular Pain Vol 2:16, 2006. http://www.molecularpain.com/content/2/1/16

 

Lidocaine
  1. Kanai, A., Suzuki, A. Okamoto, H. Comparison of Cutaneous Anesthetic Effect of 8% Lidocaine Spray with Lidocaine Patch Using Current Perception Threshold Test. Pain Medicine. epub. ahead of press, Jan. 2010.
  2. Oda, M., Kitagawa, N., Yang, B-X., Totoki, T. Morimoto, M. Quantitative and fiber-selective evaluation of dose-dependent nerve blockade by intrathecal lidocaine in rats. The Journal of Pharmacology and Experimental Therapeutics, Vol 312(3):1132-1137, 2005.
  3. Finkel, J.C., Yang, C.I. Yarvitz, J.L. Patel, K.M. Neuroselective sensory electrodiagnostic evaluation of 4% liposomal lidocaine. Anesthesia and Analgesia, Vol 94,:1259-62, 2002.
  4. Tankano, K., Muramori, S. Masaomi, T., Iseki, M., Suzuki,T., Tomono, K., Goto, H., Miyazaki, T, Nishitani, A., Watanabe, J. Quantitative Investigation of the Effect of Sensory Nerve Anesthesia with 9% Lidocaine Ointment on Healthy Subjects by use of the Neuroselective Current Perception Threshold. J. Pharm. Sci. Technol., (Yakuzaigaku Jpn.), Vol 62(3):105-112, 2002.
  5. Sakura, S., Sumi, M., Kushizaki, H., Saito, Y., Kosaka, Y. Concentration of Lidocaine Affects Intensity of Sensory Block During Lumbar Epidural Anesthesia. Anesthesia and Analgesia, Vol 88(1):123-7, 1998.
  6. Tay, B., Wallace, M.S., Irving, G. Quantitative Assessment of Differential Sensory Blockade after Lumbar Epidural Lidocaine. Anesthesia and Analgesia, Vol 84:1071-1075, 1997.
  7. Liu, S., Kopacz, D.J., Carpenter, R.L. Quantitative Assessment of Differential Sensory Nerve Block after Lidocaine Spinal Anesthesia. Anesthesiology, Vol 82(1):60-63, 1995.

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Opiates selectively block pain transmission.  In humans and rat studies spinal opiates are observed to have an isolated effect on 5 Hz measures, in contrast systemic administration effects 5 Hz and 250 Hz measures and in rats at high doses 2000 Hz measures as well. Examples of publications:

  1. Gustorff, B., Hoerauf, K.H., Lierz, P., Kress, H.G. Comparison of different quantitative sensory testing methods during remifentanil infusion in volunteers. British Journal of Anaesthesia. Vol. 91(2):203-8, 2003.

  2. Kiso, T., Nagakura,, Y., Toya, T., Matsumoto, N., Tamura, S., Ito, H., Okada, M., Yamaguchi, T. Neurometer measurement of current stimulus threshold in rats. The Journal of Pharmacology and Experimental Therapeutics, Vol 297(1):352-356, 2001.

  3. Liu, S.S., Gerancher, J.C., Bainton, B.G., Kopacz, D.J., Carpenter, R.L: Effects of Electrical Stimulation at Different Frequencies on Perception and Pain in Human Volunteers: Epidural Versus Intravenous Administration of Fentanyl. Anesthesia & Analgesia, Vol 82:98-102, 1996.

 

Paclitaxel and Gabapentin

  1. Matsumoto, ,M. Inoue, M., Hald, A., Xie, W., Ueda, H. Inhibition of Paclitaxel-Induced A-Fiber Hypersensitization by Gabapentin. The Journal of Pharmacology and Experimental Therapeutics Vol. 318(2): 318:735–740, 2006.

 
Resiniferatoxin (RTX) - RTX is a naturally occurring analogue of capsaicin. RTX functions as an ultra potent capsaicin analogue but also has unique effects such as desensitization without excitation (Szallasi, A. and Blumberg, P. M.: Vanilloid receptors: new insights enhance potential as a therapeutic target. Pain, 68: 195, 1996).
  1. Yokoyama, T., Nozaki, K., Fujita, O., Nose, H., Inoue, M., Kumon, H. Role of C afferent fibers and monitoring of intravesical resiniferatoxin therapy for patients with idiopathic detrusor overactivity. Journal of Urology, Vol 172(2):596-600, 2004.
 

Tolterodine

  1. Gater, L. Tolterodine Causes Measurable Restoration of Urethral Sensation in Women With Urge Urinary Incontinence. Paper 56. Presented at the American Urogynecologic Society 29th Annual Scientific Meeting (AUGS), 2008.

 

 
 
 
 

 

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rev 05/31/10