Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1    Pharmacodynamic properties
Pharmacotherapeutic group: Detoxification agent for the treatment with cytostatic agents, antidote to oxazaphosphorines.
ATC code: V03AF01

The mode of action of the uroprotector mesna is based on the stabilisation of the urotoxic hydroxy metabolites of oxazaphosphorines on the one hand and on the other hand on formation of non-toxic compounds with acrolein. A regional detoxification in the kidneys and the lower urinary tract is achieved due to this reaction.

Pharmacokinetic Properties

5.2     Pharmacokinetic properties
Following administration, the free thiol compound mesna is rapidly metabolised to mesna metabolite mesna disulphide in serum, which is again reduced in considerable amounts to the free thiol compound following glomerular filtration. Mesna is almost exclusively eliminated via the kidneys. Renal elimination begins immediately after application. During the first 4 hours after single application the elimination is performed mainly as free SH compound, afterwards almost exclusively in form of disulphide. After about 8 hours the renal elimination is largely completed.

With regard to protection of the urinary bladder, the relevant compartment is the urine, where approx. 30% is bioavailable as free SH mesna after intravenous administration.