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The antiepileptic activities of methylphenobarbitone (Prominal®) (7.13), primidone (Mysoline®) (7.14) and methsuximide (7.15) have also been shown to be related to the plasma levels of active metabolites. The active metabolites are obtained on demethylation of methylphenobarbitone and oxidation of primidone. Methsuximide is also demethylated and at steady state the metabolite of this compound has been shown to be present at 700-fold greater concentrations than the parent drug.

The non-steroidal anti-inflammatory drug sulindac (Clinoril®) (7.16) is also a prodrug which is reduced to the active metabolite (7.17) although some of the inactive sulphone (7.18) is formed by oxidation.

The in vivo hydrolysis of aspirin (7.19) to salicylic acid (7.20) by esterases allows the administration of aspirin in preference to salicylic acid which is more corrosive to the gastrointestinal mucosa.

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