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The Metabolism of 3-methyl-5-ethyl-5-phenylhydantoin (Mephenytoin) to 5-ethyl-5-phenylhydantoin (Nirvanol) in Mice in Relation to Anticonvulsant Activity

The Metabolism of 3-methyl-5-ethyl-5-phenylhydantoin (Mephenytoin) to 5-ethyl-5-phenylhydantoin (Nirvanol) in Mice in Relation to Anticonvulsant Activity

H J Kupferberg, W Yonekawa

Drug Metab Dispos. Jan-Feb 1975;3(1):26-9.

PMID: 234831

Abstract:

Mephenytoin (3-methyl-5-ethyl-5-phenylhydantoin) is metabolized to Nirvanol (5-ethyl-5-phenylhydantoin). Both compounds block the hind leg tonic extensor phase of the Maximal Electroshock Seizure (M.E.S.) Test in mice. The M.E.S. ED50 of mephenytoin is 42 mg/kh at 30 min and 35 mg/kg at 2 hr after ip administration. The M.E.S. ED50 for Nirvanol at 30 min and 2 hr was 23 and 30 mg/kg, respectively. Brain and plasma levels of mephenytoin and Nirvanol were determined by gas-liquid chromatography after ip administration of 40 mg of mephenytoin per kg. At 30 min the brain levels of mephenytoin and Nivanol were 19.2 and 8.1 mug/g, respectively. The brain levels of mephenytoin fell to 5.8 mug/g and those of Nirvanol rose to 18.2 mug/g at 2 hr. The total molar concentration of mephenytoin and Nirvanol, however, did not change more than 10% during the 2-hr period. Although the anticonvulsant activity of mephenytoin did not vary greatly during 2 hr after administration, the early activity is due in major part fo mephenytoin and the later activity to Nirvanol.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP631072	(±)-Nirvanol		631-07-2	Price

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