Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Antiepileptics
ATC code: N03AX03

Sulthiame belongs to the group of carbonic anhydrase inhibitors and displays an anticonvulsant effect in the electroconvulsion test (rat and mouse) and in the convulsion test with pentamethylene tetrazole (mouse).

Pharmacokinetic Properties

5.2 Pharmacokinetic properties

Sulthiame pharmacokinetics were not systematically investigated in different age categories in children and adolescents.

Absorption
After oral administration, sulthiame is rapidly and completely absorbed, predominantly from the upper section of the small intestine. Peak plasma concentrations are measured after 1 - 5 hours.
In a single dose pharmacokinetic study with 16 probands, the influence of food intake on the absorption of Ospolot 200 mg tablets was examined. The results show that intake of Ospolot with food leads to a moderately reduced bioavailability of sulthiame.


Distribution
About 29% of the active substance is bound to plasma proteins.
Elimination
80 to 90% is eliminated with the urine and 10 to 20% with the faeces after biliary secretion. Within 24 hours, 32% of the administered dose is excreted unchanged via the kidneys. In a single dose pharmacokinetic study with 16 healthy adult probands, a half-life of approximately 12 h was determined. Based on published pharmacokinetic studies, a shorter half-life is assumed in children.