Uromes Mechanism of Action

Pharmacology: Pharmacodynamics: Mesna is an antidote, and offers the possibility of reliably preventing urotoxic side-effects associated with aggressive cancer chemotherapy using oxazaphosphorine cytostatics. Extensive and wide-ranging pharmacological and toxicological investigations have shown that mesna has no intrinsic pharmacodynamics and low toxicity. The pharmacological and toxicological inertness of mesna administered systemically and its excellent detoxifying effect in the efferent urinary tract and bladder, are due to the nature of its pharmacokinetics.
Pharmacokinetics: Following IV or oral administration, Mesna is rapidly and almost completely oxidized in systemic circulation to dimesna (mesna disulfide). In a limited number of healthy adults who received a single 800-mg IV dose of Mesna, peak plasma concentrations of Mesna and dimesna averaged 18.2 and 59.7 μg/mL, respectively. The volume of distribution for Mesna has been reported to be approximately 0.65 L/kg in healthy adults. The drug does not cross the blood-brain barrier.
Mesna and dimesna are eliminated principally in urine. Following IV administration of a single 800-mg Mesna dose, peak urine concentrations are achieved within 4 hours and average 1.57 and 1.4 mg/mL for Mesna and dimesna, respectively. A urine Mesna concentration of 0.1 mg/mL has been proposed as the minimum effective uroprotective concentration.