Abstract:
:Topiramate [2,3:4, 5-bis-O-(1-methyl-ethylidene-)-beta-D-fructopyranose sulfamate], administered intraperitoneally (i.p.) up to 5 mg/kg, did not influence the threshold for electroconvulsions. In doses of 10-30 mg/kg, topiramate significantly raised the threshold. This novel antiepileptic drug, in subprotective doses, enhanced the protective activity of i.p. given valproate, carbamazepine, dihenylhydantoin and phenobarbital against maximal electroshock-induced convulsions in mice. The potentiation induced by topiramate (2.5-5 mg/kg) was most profound for carbamazepine and phenobarbital. The anticonvulsive activity of valproate and diphenylhydantoin was potentiated by topiramate only at 5 mg/kg. Topiramate (5 mg/kg) combined with valproate, phenobarbital and diphenylhydantoin did not alter their free plasma levels but its combination with carbamazepine resulted in an increased free plasma level of this antiepileptic drug. Treatment with topiramate (5 mg/kg) alone or in combination with the studied antiepileptics (providing 50% protection against maximal electroshock) resulted in no adverse effects, as measured in the chimney test (motor coordination) or passive avoidance task (long-term memory). In contrast, valproate administered alone at its ED(50) against maximal electroshock impaired motor coordination. It is noteworthy that valproate and carbamazepine at their respective ED(50) values of 248 and 11.2 mg/kg disturbed long-term memory. The results provide an experimental basis for rational polytherapy.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Swiader M,Kotowski J,Gasior M,Kleinrok Z,Czuczwar SJdoi
10.1016/s0014-2999(00)00365-4keywords:
subject
Has Abstractpub_date
2000-06-30 00:00:00pages
35-41issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(00)00365-4journal_volume
399pub_type
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