[Modified procedure for screening anticonvulsants. Re-evaluation of sodium diphenylhydantoin and phenobarbital].
A modified antiepileptic screening procedure to test anticonvulsant drugs is shown. Diphenylhydantoin sodium salt (DFH-Na) and phenobarbital (Phb) were tested throughout 8 h, at hourly intervals after a single oral drug intake in rats. Another group was tested at steady stage of DFH-Na during 7 days period. A single dose of DFH-Na was orally administrated to male and female rats (30 mg/kg) and after testing throughout 8 h: 0, 5, 28, 38, 52, 70 and 75% and 10, 18, 50, 35, 62, 50 and 70% protection against MES, was found. Only 20% protection was found in females to METsc test on the 6th and 7th h. However, 80, 60, 60 and 20% males were found protected against METsc test from the 4th to the 8th hour. Maximum blood serum levels were 2 micrograms/ml. Phenobarbital at doses 12 mg/kg in males and females as well showed: 30, 64, 66, 74, 84, 90, 40, 34% and 14, 36, 53, 41, 55, 70, 82 and 82% protection against MES, respectively. On the other hand, 60, 60, 46, 47, 94, 100, 80 and 20% and 80, 80, 46, 70, 60, 40, 80 and 20% of males and females were protected against METsc test, respectively. An average of 8 micrograms/ml and 12 micrograms/ml of Phb serum levels were found since the 1 to the 8th and 5th hours, correspondingly. A 28% protection of both male and female rats to MES test was found following 7 days of treatment with DFH-Na (30 mg/kg) treatment. Also an average of 10% female and males were found protected against METsc test.
Garzón
P
P
Divisón de Bioquímica Farmacológica, Unidad de Investigación Biomédica de Occidente, IMSS, México.
Navarro-Ruíz
A
A
Domínguez-Rodríguez
J
J
García-Estrada
J
J
González-Hita
M
M
Bastidas-Ramírez
B
B
Román-Maldonado
S
S
Navarro-Ruíz
I
I
D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use*; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004558:Electric Stimulation / Q000009:adverse effects; D005260:Female; D008297:Male; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors / Q000633:toxicity; D010634:Phenobarbital / Q000627:therapeutic use*; D010672:Phenytoin / Q000627:therapeutic use*; D000091402:Prohibitins; D051381:Rats; D011919:Rats, Inbred Strains; D011930:Reaction Time / Q000187:drug effects; D012640:Seizures / Q000209:etiology / Q000517:prevention & control*
D000927:Anticonvulsants; C000717332:Phb protein, rat; D000091402:Prohibitins; D010672:Phenytoin; D010433:Pentylenetetrazole; D010634:Phenobarbital
Procedimiento modificado para tamizaje anticonvulsionante. Reevalucación del difenilhidantoinato sódico y el fenobarbital.