The new generation of GABA enhancers: Potential in the treatment of epilepsy

CNS Drugs

Volumn 15, Issue 5, 2001, Pages 339-350

  Czuczwar, Stanislaw J ^a,b   Patsalos, Philip N ^c,d  

^a MEDICAL UNIVERSITY OF LUBLIN   (Poland)

^b INSTITUTE OF AGRICULTURAL MEDICINE   (Poland)

^c UNIVERSITY COLLEGE LONDON   (United Kingdom)

^d Chalfont St Peter   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 AMINOPROPYLBUTYLPHOSPHINIC ACID; 4 AMINOBUTYRATE AMINOTRANSFERASE; 4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID B RECEPTOR BLOCKING AGENT; 4 AMINOBUTYRIC ACID C RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; ANTICONVULSIVE AGENT; BARBITURIC ACID DERIVATIVE; BENZODIAZEPINE DERIVATIVE; CARBAMAZEPINE; CARRIER PROTEIN; CLOBAZAM; CLONAZEPAM; FELBAMATE; GABAPENTIN; GANAXOLONE; PHENOBARBITAL; PHENYTOIN; PREGABALIN; PROTEIN GAT1; RETIGABINE; TIAGABINE; TOPIRAMATE; UNCLASSIFIED DRUG; VALPROIC ACID; VIGABATRIN;

4 AMINOBUTYRIC ACID METABOLISM; 4 AMINOBUTYRIC ACID UPTAKE; AMINO ACID SYNTHESIS; ANTICONVULSANT ACTIVITY; CALCIUM TRANSPORT; CLINICAL TRIAL; DRUG APPROVAL; DRUG INDUCED DISEASE; DRUG MECHANISM; DRUG RECEPTOR BINDING; ENZYME INHIBITION; EPILEPSY; EPILEPTOGENESIS; GABAERGIC SYSTEM; HUMAN; INTRACTABLE EPILEPSY; META ANALYSIS; NERVE CELL INHIBITION; PRIORITY JOURNAL; REVIEW;

EID: 0035009415     PISSN: 11727047     EISSN: None     Source Type: Journal    
DOI: 10.2165/00023210-200115050-00001     Document Type: Review

References (76)

1. 1. Sander JW. Shorvon SD. Epidemiology of the epilepsies. J Neurol Neurosurg Psychiat 1996; 61: 433-43
2. 2. Meldrum BS. Gamma-aminobutyric acid and the search for new anticonvulsant drugs. Lancet 1978; ii: 304-6
3. 3. Kuriyama K, Roberts E, Rubinstein MK. Elevation of γ-aminobutyric acid in the brain with aminooxyacetic acid and susceptibility to convulsive seizures in mice: a quantitative re-evaluation. Biochem Pharmacol 1966; 15: 221-36
4. 4. Schechter PJ, Tranier Y, Jung MJ, et al. Audiogenic seizure protection by elevated brain GABA concentration in mice: effects of γ-acetylenic-GABA and γ-vinyl-GABA, two irreversible GABA-T inhibitors. Eur J Pharmacol 1977; 45: 319-28
5. 5. Kleinrok Z, Czuczwar SJ, Kozicka M. Effect of dopaminergic and GABA-ergic drugs given alone or in combination on the anticonvulsant action of phenobarbital and diphenylhydantoin in the electroshock test in mice. Epilepsia 1980; 21: 519-29
6. 6. Czuczwar SJ. Effect of combined treatment with dopaminergic and GABA-ergic drugs on the threshold for maximal electroconvulsions in mice. Pol J Pharmacol 1981; 33: 25-35
7. 7. Antkiewicz-Michaluk L. Receptor and voltage-operated ion channels in the central nervous system. Pol J Pharmacol 1995; 47: 253-64
8. 8. Kostowski W. Recent advances in the GABA-A-benzodiazepine receptor pharmacology. Pol J Pharmacol 1995; 47:237-46
9. C receptors. Vision Res 1998; 38: 1431-41
10. 10. Chapman AG, Keane AP, Meldrum BS. et al. Mechanism of action of valproate. Prog Neurobiol 1982; 19: 315-59
11. 11. Bernasconi R, Klein M, Martin P, et al. The specific protective effect of diazepam and valproate against isoniazid-induced seizures is not correlated with increased GABA levels. J Neural Transm 1985; 63: 169-89
12. 12. Patsalos PN, Duncan SD. The pharmacology and pharmacokinetics of vigabatrin. Rev Contemp Pharmacother 1995; 6: 447-56
13. 13. Löscher W. GABA and the epilepsies. Experimental and clinical considerations. In: Bowery NG, Nistico G, editors. GABA: basic research and clinical applications. Rome: Pythagora Press, 1989; 260-300
14. 14. Kalviainen R, Keranen T, Riekkinen PJ. Place of newer antiepileptic drugs in the treatment of epilepsy. Drugs 1993; 46: 1009-24
15. 15. Petroff OAC, Rothman DL, Behar KL, et al. Human brain GABA levels rise following initiation of vigabatrin therapy, but fail to rise further with increasing dose. Neurology 1996; 46: 1459-63
16. 16. Suzdak PD, Jansen JA. A review of the preclinical pharmacology of tiagabine: a potent and selective anticonvulsant GABA uptake inhibitor. Epilepsia 1995; 36: 612-26
17. 17. Patsalos PN. New antiepileptic drugs. Ann Clin Biochem 1999; 36: 10-19
18. 18. Meldrum BS, Croucher MJ, Krogsgaard-Larsen P. GABA-up-take inhibitors as anticonvulsant agents. In: Okada Y. Roberts E, editors. Problems in GABA research: Ffom brain to bacteria. Amsterdam-Oxford-Princeton: Excerpta Medica 1981: 182-91
19. 2δ subunit of a calcium channel. J Biol Chem 1996; 271: 5768-76
20. 20. Löscher W, Hönack D. Taylor CP. Gabapentin increases aminooxyacetic acid-induced GABA accumulation in several regions of rat brain. Neurosci Lett 1991; 120: 150-4
21. 21. Meldrum BS. Update on the mechanism of action of antiepileptic drugs. Epilepsia 1996; 37 Suppl. 6: 4S-11S
22. 22. Petroff OAC, Rothman DL. Behar KL, et al. The effect of gabapentin on brain gamma-butyric acid in patients with epilepsy. Ann Neurol 1996; 39: 95-9
23. 23. Shank RP, Gardocki JF, Vaught JL, et al. Topiramate: preclinical evaluation of a structurally novel anticonvulsant. Epilepsia 1994; 35: 450-60
24. 24. Swinyard EA, Sofia RD, Kupferberg HJ. Comparative anticonvulsant activity and neurotoxicity of felbamate and four prototype antiepileptic drugs in mice and rats. Epilepsia 1986; 27: 27-34
25. A receptor system. Epilepsia 1991; 32: 389-91
26. 26. Kuzniecky R, Hetherington H, Ho S, et al. Topiramate increases GABA in healthy humans. Neurology 1998; 51: 627-9
27. 27. Petroff OAC, Hyder F, Mattson RH, et al. Topiramate increases brain GABA, homocarnosine, and pyrrolidinone in patients with epilepsy. Neurology 1999; 52: 473-8
28. 28. Löscher W. New visions in the pharmacology of anticonvulsion. Eur J Pharmacol 1998; 342: 1-13
29. 29. Marescaux C, Vergnes M, Depaulis A. Genetic absence epilepsy in rats from Strasbourg: a review. J Neural Transm 1992; 35: 37-69
30. 30. Parker AP, Agathonikou A, Robinson RO, et al. Inappropriate use of carbamazepine and vigabatrin in typical absence seizures. Dev Med Child Neurol 1998; 40: 517-9
31. 31. Puigcerver A, van Luijtelaar ELJM, Drinkenburg WHIM, et al. Effects of the GABA-B antagonist CGP 35348 on sleep-wake states, behaviour, and spike-wave discharges in old rats. Brain Res Bull 1996; 40: 157-62
32. 32. Peeters BWMM, van Rijn CM, Vossen JMH, et al. Effects of GABA-ergic agents on spontaneous non-convulsive epilepsy, EEG and behaviour, in the WAG/Rij inbread strain of rats. Life Sci 1989; 45: 1171-6
33. 33. Sheth RD, Buckley D, Penney S, et al. Vigabatrin in childhood epilepsy: comparable efficacy for generalized and partial seizures. Clin Neuropharmacol 1996; 19: 287-304
34. 34. Wohlrab G, Boltshauser E, Schmitt B. Vigabatrin as a first-line drug in West syndrome: clinical and electroencephalographic outcome. Neuropediatrics 1998; 29: 133-6
35. 35. Siemes H, Brandl U, Spohr HL, et al. Long-term follow-up study of vigabatrin in pretreated children with West syndrome. Seizure 1998; 7: 293-7
36. 36. Engelborghs S, Pickut BA, D'Hooge R, et al. Behavioral effects of vigabatrin correlated with whole brain gamma-aminobutyric acid metabolism in audiogenic sensitive rats. Arzneimittelforschung 1998; 48: 713-6
37. 37. Michelucci R, Tassinari CA. Response to vigabatrin in relation to seizure type. Br J Clin Pharmacol 1989; 27: 119-25
38. 38. Kalviainen R, Nousiainen I, Mantyjarvi M, et al. Vigabatrin, a gabaergic antiepileptic drug, causes concentric visual field defects. Neurology 1999; 22: 922-6
39. 39. Lawden MC, Eke T, Degg C, Harding GF, Wild JM. Visual field defects associated with vigabatrin therapy. J Neurol Neurosurg Psychiatry 1999; 67: 716-22
40. 40. Wild JM, Martinez C, Reinshagen G, et al. Characteristics of a unique visual field defect attributed to vigabatrin. Epilepsia 1999; 40: 1784-94
41. 41. Harding GFA. Severe persistent visual field constriction associated with vigabatrin - four posible explanations exist. Br Med J 1997; 314: 1694
42. 42. Sills GJ, Patsalos PN, Butler E, et al. Visual field constrictions: accumulation of vigabatrin but not tiagabine in the retina. Neurology. In Press
43. 43. Adkins JC, Noble S. Tiagabine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the management of epilepsy. Drugs 1998; 55: 437-60
44. 44. Luer MS, Rhoney DH. Tiagabine: a novel antiepileptic drug. Ann Pharmacother 1998; 32: 1173-80
45. 45. Bialer M, Johanessen SI, Kupferberg HJ, et al. Progress report on new antiepileptic drugs: a summary of the fourth Eilat conference (EILAT IV). Epilepsy Res 1999; 34: 1-41
46. 46. Sachdeo RC, Reife RA, Lim P, Pledger G. Topiramate monotherapy for partial onset seizures. Epilepsia 1997; 38: 294-300
47. 47. Patsalos PN. The pharmacokinetic profile of topiramate. Rev Contemp Pharmacother 1999; 10: 155-62
48. 48. Patsalos PN. The mechanism of action of topiramate. Rev Contemp Pharmacother 1999; 10: 147-53
49. 49. Lhatoo SD, Walker MC. The safety and adverse event profile of topiramate. Rev Contemp Pharmacother 1999; 10: 185-91
50. 50. Ben-Menachem E. The clinical efficacy of topiramate in the treatment of epilepsy. Rev Contemp Pharmacother 1999; 10: 163-84
51. 51. Carter RB, Wood PL, Wieland S, et al. Characterisation of the anticonvulsant properties of ganaxolone (CCD 1042; 3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20one), a selective, high affinity, steroid modulator of the gamma-aminobutyric acis(A) receptor. J Pharmacol Exp Ther 1997; 280: 1284-95
52. 52. Gasior M, Carter RB, Witkin JM. Neuroactive steroids: potential therapeutic use in neurological and psychiatric disorders. Trends Pharmacol Sci 1999; 20: 107-12
53. 53. Gasior M, Beekman M, Carter RB, et al. Antiepileptogenic effects of the novel synthetic neuroactive steroid, ganaxolone, against pentylenetetrazol-induced kindled seizures: comparison with diazepam and valproate. Drug Dev Res 1998; 44: 21-33
54. 54. Snead OC. Ganaxolone, a selective, high-affinity steroid modulator of the gamma-aminobutyric acid-A receptor, exacerbates seizures in animal models of absence. Ann Neurol 1998; 44: 688-91
55. 55. Lechtenberg R, Villeneuve N, Monaghan EP, et al. An open-label dose-escalation study to evaluate the safety and tolerability of ganaxolone in the treatment of refractory epilepsy in pediatric patients. Epilepsia 1996; 37 (5 Suppl.): 204
56. 56. Laxer K, Blum D, Abou-Khalil BW, et al. Assessment of ganaxolone's anticonvulsant activity using a randomized, double-blind, presurgical trial design. Ganaxolone Presurgical Study Group. Epilepsia 2000; 41: 1187-94
57. 57. Monaghan EP, Navalta LA, Shum L, et al. Initial human experience with ganaxolone, a neuroactive steroid with antiepileptic activity. Epilepsia 1997; 38: 1026-31
58. 58. Kapetanovic IM, Yonekawa WDS, Kupferberg HJ. The effects of D-23129, a new experimental anticonvulsant drug, on neurotransmitter amino acids in the rat hippocampus in vitro. Epilepsy Res 1995; 22: 167-73
59. + channels in neuronal cells. Eur J Pharmacol 1997; 336: 243-9
60. ++ model in the hippocampal slice preparation. Epilepsy Res 2000; 38: 53-66
61. 61. Schroeder BC. Kubisch C, Stein V, et al. Moderate loss of function of cyclic-AMP modulated KCNQ2/KCNQ3 K channels causes epilepsy. Nature 1998; 396: 687-90
62. 62. Wang HS, Pan X, Shi W, et al. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 1998; 282: 1890-3
63. 63. Rundfeldt C, Netzer R. The novel anticonvulsant retigabine activates M-currents in Chinese hamster ovary-cells transfected with human KCNQ2/3 subunits. Neurosci Lett 2000; 282: 73-6
64. 64. Dailey JW, Cheong JH, Ko KH, et al. Anticonvulsant properties of D-20443 in genetically-prone rats: prediction of clinical response. Neurosci Lett 1995; 195: 77-80
65. 65. Rostock A, Tober C, Rundfeldt C, et al. D-23129; a new anticonvulsant with broad spectrum activity in animal models of epileptic seizures. Epilepsy Res 2000; 23: 211-23
66. 66. Tober C, Rostock A, Rundfeldt C, et al. D-33129: a potent anticonvulsant in the amygdala kindling model of complex partial seizures. Eur J Pharmacol 1996; 303: 163-9
67. 67. Bialer M, Johannessen SI, Kupferberg HJ, et al. Progress report on new antiepileptic drugs: a summary of the Fifth Eilat conference (EILAT V). Epilepsy Res 2001; 43: 11-58
68. 68. Taylor CP, Vartanian MG, Yuen PW, et al. Potent stereospecific anticonvulsant activity of 3-isobutyl GABA relates to in vitro binding at the novel site labelled by tritiated gabapentin. Epilepsy Res 1993; 14: 11-5
69. 69. Taylor CP, Vartanian MG. Profile of the anticonvulsant activity of Cl-1008 (pregabalin) in animal models. Epilepsia 1997; 38 (8 Suppl.): 35
70. 70. Beydoun A, Uthman B, Ramsey RE, et al. Pregabalin add-on trial: multi-center study in patients with partial epilepsy. Epilepsia 1999; 40 (7 Suppl.): 108
71. 71. French JA, Malicsi MJR, Kugler AR, et al. Pregabalin adjunctive therapy in patients with partial seizures. Epilepsia 1999; 40 (7 Suppl.): 106
72. B receptor antagonists on absences and convulsive seizures. Eur J Pharmacol 1997; 332: 245-55
73. B receptor antagonism on the development of pentylenetetrazol-induced kindling in mice. Brain Res 1998; 809: 182-8
74. B receptor antagonists on learning and memory retention in a rat model of absence epilepsy. Eur J Pharmacol 1997; 320: 9-13
75. 75. Walker MC, Sander JWAS. The impact of new antiepileptic drugs on the prognoosis of epilepsy: seizure freedom should be the ultimate goal. Neurology 1996; 46: 912-4
76. 76. Marson AG, Kadir ZA, Hutton JL, et al. The new anti-epileptic drugs: a systematic review of their efficacy and tolerability. Epilepsia 1997; 38: 859-80