Trimethadione anticonvulsant

The oxa2ohdinedione trimethadione [127-48-0] C H NO (50), at one time the dmg of choice for the treatment of absence sei2ures, has been replaced by ethosuximide (41) and valproate (49). (50) has a distinct profile from that of phenytoin but causes photophobia and night blindness in approximately 30% of the patients taking it and has the CNS and sedative properties seen for other anticonvulsants together with moderate neutropenia, hepatitis, and skin rashes (13). Trimethadione does not appear to produce its effects via modulation of GABA-mediated responses. 

The profiles of anticonvulsant effects for phenobarbital, pheny-toin, and trimethadione were also determined in the PTZ model. 

The most common drugs responsible for acneform eruptions are ACTH, androgenic hormones, anticonvulsants (hydantoin derivatives, phenobarbital, trimethadione), corticosteroids, danazol, disulfiram, halogens (bromides, chlorides, iodides), lithium, oral contraceptives, tuberculostatics (ethionamide, isoniazid, rifampin), vitamins B2, B6, and B12. 

Richards and Everett reported on the anticonvulsant activity of trimethadione (17),... 

Trimethadione is rapidly absorbed when given orally, and its binding to plasma proteins is negligible. Trimethadione is demethylated to dimethadione, which is an active anticonvulsant. The rate of conversion of trimethadione to dimethadione is rapid, but its rate of elimination is slow. As a result, the plasma ratio of dimethadione to trimethadione is 20 to 1. 

It is employed as an anticonvulsant in grand mal epilepsy to arrest status epilepticus and in petit mal epilepsy as a means of resisting control to other treatments. When administered alone trimethadione... 

DM0 (XXIa), a inetabolite of trimethadione, TMO (XXIb), was reported to have similar anticonvulsant properties in rats and mice but it is... 

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