Pharmacokinetic-pharmacodynamic correlation of lamotrigine, flunarizine, loreclezole, CGP40116 and CGP39551 in the cortical stimulation model

Epilepsy Research

Volumn 40, Issue 1, 2000, Pages 41-52

  Della Paschoa, Oscar E ^a   Hoogerkamp, Arendien ^a   Edelbroek, Peter M ^b   Voskuyl, Rob A ^b,c   Danhof, Meindert ^a  

^a LEIDEN UNIVERSITY   (Netherlands)

^b LEIDEN UNIVERSITY MEDICAL CENTER   (Netherlands)

^c STICHTING EPILEPSIE INSTELLINGEN NEDERLAND SEIN   (Netherlands)

Author keywords

Anti convulsant effect; CGP39551; CGP40116; Drug potency; Flunarizine; Lamotrigine; Loreclezole; PK PD modelling

Indexed keywords

2 AMINO 4 METHYL 5 PHOSPHONO 3 PENTENOIC ACID; 2 AMINO 4 METHYL 5 PHOSPHONO 3 PENTENOIC ACID ETHYL ESTER; FLUNARIZINE; LAMOTRIGINE; LORECLEZOLE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICONVULSANT ACTIVITY; ARTICLE; BRAIN CORTEX; BRAIN DEPTH STIMULATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; CONVULSION; DOSE TIME EFFECT RELATION; FEMALE; GRAND MAL SEIZURE; MODEL; NONHUMAN; PHARMACODYNAMICS; PHARMACOKINETICS; PRIORITY JOURNAL; RAT; SEIZURE THRESHOLD;

ANIMALS; ANTICONVULSANTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION; ELECTRIC STIMULATION; EXCITATORY AMINO ACID ANTAGONISTS; FEMALE; INJECTIONS, INTRAVENOUS; MOTOR CORTEX; OSMOLAR CONCENTRATION; RATS; RATS, WISTAR; SEIZURES;

EID: 0034213043     PISSN: 09201211     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0920-1211(00)00102-9     Document Type: Article

References (45)

1. Ashton D., Fransen J., Heeres J., Clincke G.H., Janssen P.A. In vivo studies on the mechanism of action of the broad spectrum anti-convulsant loreclezole. Epi. Res. 11:1992;27-36.
2. Ashton D., Willems R. In vitro studies on the broad spectrum anti-convulsant loreclezole in the hippocampus. Epi. Res. 11:1992;75-88.
3. Benetello P. New antiepileptic drugs. Pharmacol. Res. 31:1995;155-162.
4. Bialer M. Comparative pharmacokinetics of the newer antiepileptic drugs. Clin. Pharmacokinet. 24:1993;441-452.
5. Breimer D.D., Danhof M. Relevance of the application of pharmacokinetic-pharmacodynamic modelling concepts in drug development: the 'wooden shoe' paradigm. Clin. Pharmacokinet. 32:1997;259-267.
6. Chapman A.G., Graham J.L., Patel S., Meldrum B.S. Anti-convulsant activity of two orally active competitive N-methyl-D-aspartane antagonists, CGP 37849 and CPG 39551 against sound induced seizures in DBA/2 mice and photically induced myoclonus in Papio papio. Epilepsia. 32:1991;578-587.
7. Cheung H., Kamp D., Harris E. An in vitro investigation of the action of lamotrigine on neuronal voltage-activated sodium channels. Epi. Res. 13:1992;107-112.
8. Cotterell K.L., Croucher M.J., Bradford H.F. Weak anti-convulsant activity of CGP 37849 and CGP 39551 against kindled seizures following systemic administration. Eur. J. Pharmacol. 22:1992;285-287.
9. Croucher M.J., Cotterell K.L., Bradford H.F. Competitive NMDA receptor antagonists raise electrically kindled generalized seizure thresholds. Neurochem. Res. 17:1992;409-413.
10. Dailey J.W., Seo D.O., Yan Q.S. et al. The anti-convulsant effect of the broad spectrum anti-convulsant loreclezole microdialysis study. Neurosci. Lett. 178:1994;179-183.
11. Danhof M., Mandema J.W., Hoogerkamp A., Mathôt R.A. Pharmacokinetic-pharmacodynamic modelling in pre-clinical investigations: principles and perspectives. Eur. J. Drug. Metab. Pharmacokinet. 18:1993;41-47.
12. Dawson G.R., Curnow R., Bayley P., Rambridge A., Tricklebank M.D. Lack of effect of flumazenil and CGS 8216 on the anxiolytic-like properties of loreclezole. Eur. J. Pharmacol. 252:1994;325-328.
13. Della Paschoa O.E., Mandema J.W., Voskuyl R.A., Danhof M. Pharmacokinetic-pharmacodynamic modelling of the anti-convulsant and EEG effects of phenytoin in rats. J. Pharmacol. Exp. Ther. 284:1998;460-466.
14. Desai C.K., Dikshit R.K., Mansuri S.M., Shah U.H. Comparative evaluation of anti-convulsant activity of calcium channel blockers in experimental animals. Indian. J. Exp. Biol. 33:1995;931-934.
15. Endrenyi L., Zha J. Comparative efficiencies of randomized concentration- and dose-controlled clinical trials. Clin. Pharmacol. Ther. 56:1994;331-338.
16. Fisher J.L., Macdonald R.L. Functional properties of recombinant GABAA receptors composed of single or multiple ( subunit subtypes). Neuropharmacology. 36:1997;1601-1610.
17. Gaudreault J., Varin F., Pollack G.M. Anti-convulsant pharmacodynamics and disposition of triazolam in rats. J. Pharm. Sci. 85:1996;999-1004.
18. Gibaldi M., Perrier D. Noncompartmental analysis based on statistical moment theory. Pharmacokinetics. 2nd:1982;409-424 Marcel Dekker, New York.
19. Handforth A., Mai T., Treiman D.M. Rising dose study of safety and tolerance of flunarizine. Eur. J. Clin. Pharmacol. 49:1995;91-94.
20. Hevers W., Lüddens H. The diversity of GABAA receptors: pharmacological and electrophysiological properties of GABAA channel subtypes. Mol. Neurobiol. 18:1998;35-86.
21. Holmes B., Brogden R.N., Heel R.C., Speight T.M., Avery G.S. Flunarizine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic use. Drugs. 27:1984;6-44.
22. Hoogerkamp A., Vis P.W., Danhof M., Voskuyl R.A. Characterization of the pharmacodynamics of several antiepileptic drugs in a direct cortical stimulation model of anti-convulsant effect in the rat. J. Pharmacol. Exp. Ther. 269:1994;521-528.
23. Hoogerkamp A., Arends R.H., Bomers A.M. et al. Pharmacokinetic/pharmacodynamic relationship of benzodiazepines in the direct cortical stimulation model of anti-convulsant effect. J. Pharmacol. Exp. Ther. 279:1996;803-812.
24. Hoppu K., Nergardh A.R., Eriksson A.S., Beck O., Forssblad E., Boreus L. Flunarizine of limited value in children with intractable epilepsy. Pediatr. Neurol. 13:1995;143-147.
25. Krupp E., Löscher W. Anti-convulsant effect in the direct cortical ramp-stimulation model in rats: comparison with conventional models. J. Pharmacol. Exp. Ther. 285:1998;1137-1149.
26. 2+ channels in rat aorta smooth muscle cells in primary culture. Circ. Res. 67:1990;469-480.
27. Löscher W., Schmidt D. Which animal model should be used in the search for new antiepileptic drugs? a proposal based on experimental and clinical considerations. Epi. Res. 2:1988;145-181.
28. Löscher W., Hönack D. Anti-convulsant and behavioral effects of two novel competitive N-methyl-D-aspartic acid receptor antagonists, CGP 37849 and CGP59551, in the kindling model of epilepsy: comparison with MK-801 and carbamazepine. J. Pharmacol. Exp. Ther. 256:1991;432-440.
29. Parsons D.N., Dickins D., Morley T.J. Lamotrigine: absorption, distribution and excretion. Levy R.H., Mattson R.H., Meldrum B.S. Antiepileptic Drugs. Fourth edition:1995;877-881 Raven Press, New York.
30. Perucca E. The new generation of antiepileptic drugs: advantages and disadvantages. Br. J. Clin. Pharmacol. 42:1996;531-543.
31. Pledger G.W., Treiman D.M. Design of an individualized fixed-dose clinical trial to test the antiepileptic efficacy of a plasma flunarizine concentration. Control. Clin. Trials. 12:1991;768-779.
32. Sannita W.G. Dose-related and treatment-dependent quantitative EEG effects of antiepileptic compounds in humans. Clin. Neuropharmacol. 15(Suppl 1):1992;423A-424A.
33. Schapel G.J., Beran R.G., Vajda F.J. et al. Double-blind, placebo controlled, crossover study of lamotrigine in treatment resistant partial seizures. J. Neurol. Neurosurg. Psych. 56:1993;448-453.
34. Schmutz M., Portet C., Jeker A. et al. The competitive NMDA receptor antagonists CGP 37849 and CGP 39551 are potent, orally-active anti-convulsants in rodents. Naunyn Schmiedebergs Arch. Pharmacol. 342:1990;61-66.
35. Sieghart W. Structure and pharmacology of (-aminobutyric acidA receptor subtypes. Pharmacological. Rev. 47:1995;181-234.
36. Takahashi K., Akaike N. Calcium antagonist effects on low-threshold (T-type) calcium current in rat isolated hippocampal CA1 pyramidal neurons. J. Pharmacol. Exp. Ther. 256:1991;169-175.
37. Treiman D.M., Pledger G.W., DeGiorgio C., Tsay J.Y., Cereghino J.J. Increasing plasma concentration tolerability study of flunarizine in comedicated epileptic patients. Epilepsia. 34:1993;944-953.
38. Vajda F.J. New anti-convulsants. Curr. Opin. Neurol. Neurosurg. 5:1992;519-525.
39. Voskuyl R.A., Dingemanse J., Danhof M. Determination of the threshold for convulsions by direct cortical stimulation. Epi. Res. 3:1989;120-129.
40. Voskuyl R.A., Hoogerkamp A., Danhof M. Properties of the convulsive threshold determined by direct cortical stimulation in rats. Epi. Res. 12:1992;111-120.
41. Voskuyl R.A., Vreugdenhil M., Kang J.X., Leaf A. Anti-convulsant effect of polyunsaturated fatty acids in rats, using the cortical stimulation model. Eur. J. Pharmacol. 341:1998;145-152.
42. Walker M.C., Sander J.W.A.S. Lamotrigine. Eadie M.J., Vajda F.J.E. Handbook of Experimental Pharmacology, Vol 138. Antiepileptic drugs, pharmacology and therapeutics. 1999;331-358 Springer, Berlin.
43. Wingrove P.B., Wafford K.A., Bain C., Whiting P.J. The modulatory action of loreclezole at the (-aminobutyric acid type A receptor is determined by a single amino acid in the (2 and (3 subunit). Proc. Natl. Acad. Sci. 91:1994;4569-4573.
44. Wlaz P., Baran H., Löscher W. Effect of the glycine/NMDA receptor partial agonist, D-cycloserine, on seizure threshold and some pharmacodynamic effects of MK-801 in mice. Eur. J. Pharmacol. 257:1994;217-225.
45. Yamashita S., Furuno K., Moriyama M., Kawasaki H., Gomita Y. Effects of various antiepileptic drugs on plasma levels of lamotrigine, a novel antiepileptic, in rats. Pharmacology. 54:1997;319-327.