Succinimides

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Chapter: Medicinal Chemistry : Anticonvulsants

Anticonvulsants : Succinimides - Synthesis and Drug Profile - a. Ethosuximide (Zarontin) b. Methsuximide (Celontin) c. Phensuximide (Milontin) - Structure, Properties, uses, Synthesis, Assay, Storage, Dosage forms, Dose | Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE


Succinimides

Mode of action: Succinimides selectively acts on the transient current in calcium channels for the influx of calcium ions and inhibits the amplification of spikes.


a. Ethosuximide (Zarontin)


Metabolism: It is metabolized into 3-(1-hydroxyethyl) compound.

Properties and uses: It is a white or an almost white powder or waxy solid. Freely soluble in water, ethanol, and methylene chloride. It conforms very well to the general structural pattern for antiabsence activity. The drug is more active and less toxic than Trimethadione. It is a calcium-T channel blocking drug, effective in the cure of petitmal epilepsy.

Assay: Dissolve the sample in dimethylformamide and titrate with 0.1 M tetrabutylammonium hydroxide. Determine the end point by potentiometric titration.

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

Synthesis


Dose: The usual dose is 500 mg/day, in divided doses.

Dosage forms: Ethosuximide syrup I.P., Ethosuximide capsules I.P., B.P., Ethosuximide oral solution B.P.


b. Methsuximide (Celontin)


Synthesis


Metabolism: It is metabolized into N-demethylsuximide and the metabolite is also an active compound. 

Properties and uses: It is more active than phensuximide, and used in the treatment of petitmal epilepsy. 

Dose: The usual dose is, 300 mg/day; maintenance 0.3 to 1.2 g daily.


c. Phensuximide (Milontin)


Synthesis


Meatbolism: N-demethylation occurs to yield active metabolite, both phensuximide and N-demethyl metabolites are inactived by para hydroxylation and conjugation.

Properties and uses: It is a crystalline solid, soluble in water and freely soluble in ethanol. It has low potency and is therefore relegated to secondary status. The phenyl substituent confers some activity against generalized tonic-clonic and partial seizures. It is used in the treatment of petitmal epilepsy.

Dose: The usual dose is 500 mg to 1 g 2 to 3 times/day.


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