Pharmacokinetic/pharmacodynamic relationship of gabapentin in a CFA-induced inflammatory hyperalgesia rat model

Pharmaceutical Research

Volumn 33, Issue 5, 2016, Pages 1133-1143

  Larsen, Malte Selch ^a   Keizer, Ron ^b   Munro, Gordon ^c   Mørk, Arne ^c   Holm, René ^c   Savic, Rada ^b   Kreilgaard, Mads ^a,d  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c H LUNDBECK A S   (Denmark)

^d NOVO NORDISK A S   (Denmark)

Author keywords

brain; gabapentin; pain; PKPD modelling; rat

Indexed keywords

FREUND ADJUVANT; GABAPENTIN; 4 AMINOBUTYRIC ACID; AMINE; ANALGESIC AGENT; CYCLOHEXANECARBOXYLIC ACID DERIVATIVE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COMPARTMENT MODEL; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG EFFECT; EXTRACELLULAR FLUID; MALE; MECHANICAL HYPERALGESIA; MICRODIALYSIS; NONHUMAN; PHARMACODYNAMICS; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; RAT; ANIMAL; BIOAVAILABILITY; BIOLOGICAL MODEL; BRAIN; COMPUTER SIMULATION; HYPERALGESIA; METABOLISM; SPRAGUE DAWLEY RAT;

AMINES; ANALGESICS; ANIMALS; BIOLOGICAL AVAILABILITY; BRAIN; COMPUTER SIMULATION; CYCLOHEXANECARBOXYLIC ACIDS; GAMMA-AMINOBUTYRIC ACID; HYPERALGESIA; MALE; MODELS, BIOLOGICAL; RATS; RATS, SPRAGUE-DAWLEY;

EID: 84954427750     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-016-1859-7     Document Type: Article

References (40)

1. Yawn BP, Wollan PC, Weingarten TN, Watson JC, Hooten WM, Melton Iii LJ. The prevalence of neuropathic pain: clinical evaluation compared with screening tools in a community population. Pain Med. 2009;10(3):586-93.
2. Kukkar A, Bali A, Singh N, Jaggi AS. Implications and mechanism of action of gabapentin in neuropathic pain. Arch Pharm Res. 2013;36(3):237-51.
3. Woolf CJ, Salter MW. Neuronal plasticity: increasing the gain in pain. Science. 2000;288(5472):1765-9.
4. Boulton AJM. Treatment of symptomatic diabetic neuropathy. Diabetes Metab Res Rev. 2003;19(S1):16-21.
5. Moore RA, Wiffen PJ, Derry S, McQuay HJ. Gabapentin for chronic neuropathic pain and fibromyalgia in adults. Cochrane Database Syst Rev. 2011;3:1-91.
6. Gidal BE, DeCerce J, Bockbrader HN, Gonzalez J, Kruger S, Pitterle ME, et al. Gabapentin bioavailability: effect of dose and frequency of administration in adult patients with epilepsy. Epilepsy Res. 1998;31(2):91-9.
7. Larsen M, Frølund S, Nøhr M, Nielsen C, Garmer M, Kreilgaard M, et al. In vivo and In vitro evaluations of intestinal gabapentin absorption: effect of dose and inhibitors on carrier-mediated transport. Pharm Res. 2014:1-12.
8. Luer MS, Hamani C, Dujovny M, Gidal B, Cwik M, Deyo K, et al. Saturable transport of gabapentin at the blood-brain barrier. Neurol Res. 1999;21(6):559-62.
9. Urban TJ, Brown C, Castro RA, Shah N, Mercer R, Huang Y, et al. Effects of genetic variation in the novel organic cation transporter, OCTN1, on the renal clearance of gabapentin. Clin Pharmacol Ther. 2008;83(3):416-21.
10. Hurley RW, Chatterjea D, Rose Feng M, Taylor CP, Hammond DL. Gabapentin and pregabalin Can interact synergistically with naproxen to produce antihyperalgesia. Anesthesiology. 2002;97(5):1263-73.
11. Iyengar S, Webster AA, Hemrick-Luecke SK, Xu JY, Simmons RMA. Efficacy of duloxetine, a potent and balanced serotonin-norepinephrine reuptake inhibitor in persistent pain models in rats. J Pharmacol Exp Ther. 2004;311(2):576-84.
12. Todorovic SM, Rastogi AJ, Jevtovic-Todorovic V. Potent analgesic effects of anticonvulsants on peripheral thermal nociception in rats. Br J Pharmacol. 2003;140(2):255-60.
13. Taneja A, Troconiz IF, Danhof M, Della PO. Semi-mechanistic modelling of the analgesic effect of gabapentin in the formalin-induced rat model of experimental pain. Pharm Res. 2014;31(3):593-606.
14. Taneja A, Nyberg J, de Lange ECM, Danhof M, Della PO. Application of ED-optimality to screening experiments for analgesic compounds in an experimental model of neuropathic pain. J Pharmacokinet Pharmacodyn. 2012;39(6):673-81.
15. Lockwood P, Cook J, Ewy W, Mandema J. The use of clinical trial simulation to support dose selection: application to development of a new treatment for chronic neuropathic pain. Pharm Res. 2003;20(11):1752-9.
16. Swanson LW. The rat brain in stereotaxic coordinates. In: Paxinos G, Watson C, editors. Academic Press, San Diego (1982), vii + 153, ISBN: 0 125 47620 5. Trends Neurosci. 1984;7(2):53.
17. Munro G, Erichsen HK, Rae MG, Mirza NR. A question of balance - Positive versus negative allosteric modulation of GABAA receptor subtypes as a driver of analgesic efficacy in rat models of inflammatory and neuropathic pain. Neuropharmacology. 2011;61(1-2):121-32.
18. Bauer RJ. NONMEM users guide. Ellicott City: ICON Development Solutions; 2011.
19. Keizer RJ, Karlsson MO, Hooker A. Modeling and simulation workbench for NONMEM: tutorial on Pirana, PsN, and Xpose. CPT Pharmacometrics Syst Pharmacol. 2013;2, e50.
20. Development Core Team R. R: A language and environment for statistical computing. Vienna: R Foundation for Statistical Computing; 2013.
21. Jonsson EN, Karlsson MO. Xpose - an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. Comput Methods Prog Biomed;58(1):51-64.
22. Wickham H. ggplot2: elegant graphics for data analysis. New York: Springer; 2009.
23. Wang Y, Welty D. The simultaneous estimation of the influx and efflux blood-brain barrier permeabilities of gabapentin using a microdialysis-pharmacokinetic approach. Pharm Res. 1996;13(3):398-403.
24. Gur E, Waner T. The variability of organ weight background data in rats. Lab Anim. 1993;27(1):65-72.
25. Radulovic LL, Türck D, von Hodenberg A, Vollmer KO, McNally WP, DeHart PD, et al. Disposition of gabapentin (neurontin) in mice, rats, dogs, and monkeys. Drug Metab Dispos. 1995;23(4):441-8.
26. Upton RN, Mould DR. Basic concepts in population modeling, simulation, and model-based drug development: part 3 - introduction to pharmacodynamic modeling methods. CPT Pharmacometrics Syst Pharmacol. 2014;3, e88.
27. Bergstrand M, Hooker AC, Wallin JE, Karlsson MO. Prediction-corrected visual predictive checks for diagnosing nonlinear mixed-effects models. AAPS J. 2011;13(2):143-51.
28. Dumas E, Pollack G. Opioid tolerance development: a pharmacokinetic/pharmacodynamic perspective. AAPS J. 2008;10(4):537-51.
29. Stewart BH, Kugler AR, Thompson PR, Bockbrader HN. A saturable transport mechanism in the intestinal absorption of gabapentin is the underlying cause of the lack of proportionality between increasing dose and drug levels in plasma. Pharm Res. 1993;10(2):276-81.
30. Welty DF, Schielke GP, Vartanian MG, Taylor CP. Gabapentin anticonvulsant action in rats: disequilibrium with peak drug concentrations in plasma and brain microdialysate. Epilepsy Res. 1993;16(3):175-81.
31. Vollmer KO, von Hodenberg A, Kölle EU. Pharmacokinetics and metabolism of gabapentin in rat, dog and man. Arzneimittelforschung. 1986;36(5):830-9.
32. Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, et al. XP13512 [(±)-1-([(α-Isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004;311(1):324-33.
33. Yang RH, Xing JL, Duan JH, Hu SJ. Effects of gabapentin on spontaneous discharges and subthreshold membrane potential oscillation of type a neurons in injured DRG. Pain. 2005;116(3):187-93.
34. Chen SR, Xu Z, Pan HL. Stereospecific effect of pregabalin on ectopic afferent discharges and neuropathic pain induced by sciatic nerve ligation in rats. Anesthesiology. 2001;95(6):1473-9.
35. Pan HL, Eisenach JC, Chen SR. Gabapentin suppresses ectopic nerve discharges and reverses allodynia in neuropathic rats. J Pharmacol Exp Ther. 1999;288(3):1026-30.
36. Yang J-L, Xu B, Li S-S, Zhang W-S, Xu H, Deng X-M, et al. Gabapentin reduces CX3CL1 signaling and blocks spinal microglial activation in monoarthritic rats. Mol Brain. 2012;5(1):1-12.
37. Luo ZD, Chaplan SR, Higuera ES, Sorkin LS, Stauderman KA, Williams ME, et al. Upregulation of dorsal root ganglion α2δ calcium channel subunit and its correlation with allodynia in spinal nerve-injured rats. J Neurosci. 2001;21(6):1868-75.
38. Porchet HC, Benowitz NL, Sheiner LB. Pharmacodynamic model of tolerance: application to nicotine. J Pharmacol Exp Ther. 1988;244(1):231-6.
39. Yi H, Kim MA, Back SK, Eun JS, Na HS. A novel rat forelimb model of neuropathic pain produced by partial injury of the median and ulnar nerves. Eur J Pain. 2011;15(5):459-66.
40. Whiteside GT, Adedoyin A, Leventhal L. Predictive validity of animal pain models? A comparison of the pharmacokinetic-pharmacodynamic relationship for pain drugs in rats and humans. Neuropharmacology. 2008;54(5):767-75.