In man, 60-90% of an oral does of primidone is absorbed from the gastointestinal tract, with serum levels peaking about three hours following administration. Absorption is thought to be similar in animals, but primidone is metabolised once absorbed. Oxidation at carbon 2 results in the formation of phenobarbital, and cleavage at the same site gives PEMA. Primidone, phenobarbital and PEMA all possess anticonvulsant activity, but 85% primidone's activity in dogs is due to the phenobarbital it forms. This is because the potentcy of primidone and PEMA is one-thirtieth that of phenobarbital, and phenobarbital accumulates to the highest concentrations since it is the compound with the longest half-life. | In man, 60-90% of an oral does of primidone is absorbed from the gastointestinal tract, with serum levels peaking about three hours following administration. Absorption is thought to be similar in animals, but primidone is metabolised once absorbed. Oxidation at carbon 2 results in the formation of phenobarbital, and cleavage at the same site gives PEMA. Primidone, phenobarbital and PEMA all possess anticonvulsant activity, but 85% primidone's activity in dogs is due to the phenobarbital it forms. This is because the potentcy of primidone and PEMA is one-thirtieth that of phenobarbital, and phenobarbital accumulates to the highest concentrations since it is the compound with the longest half-life. |