Oxazolidinediones

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Chapter: Medicinal Chemistry : Anticonvulsants

Anticonvulsants - Oxazolidinediones - Synthesis and Drug Profile - a. Trimethadione (Tridione) b. Paramethadione (Paradione) - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE


Oxazolidinediones

General method for synthesis of oxazolidine dione derivatives



a. Trimethadione (Tridione)

Synthesis

Route-I. From Ethyl-2-hydroxy propanoate


RouteII. From: Propane-2-one


Metabolism: It is metabolized by N-demethylation to putative active metabolite dimethadone and it is further excreted unchanged.

Properties and uses: It is a colourless or almost colourless crystals, soluble in water and alcohol. It is first drug introduced specifically for treating absence seizures. It is important as a prototype structure for antiabsence seizure compounds. It is used as an antipetitmal agent. It causes nephrosis, aplastic anaemia and bone marrow depression.

Assay: Assayed by adopting gas chromatography technique.

Storage: It should be stored in well-closed airtight containers.

Dose: The usual dose is 900 mg to 2.4 g per day; usually 300 to 600 mg 2 to 4 times daily.


b. Paramethadione (Paradione)


Synthesis


Properties and uses: It is an oily liquid, slightly soluble in water and freely soluble in ethanol. It is used as an anticonvulsant.

Dose: The usual dose is 300 mg to 2.4 g daily.


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