Uromitexan, ampoules 400mg, 4ml, 15pcs

Composition

1 ampoule of concentrate for preparation of infusion solution contains:

Active ingredient:

mesna 400 mg in 4 ml

. excipients:

sodium edetate,

sodium hydroxide,

water for injection

Pharmacological action

Pharmacodynamics

Mesna is an antidote to acrolein, a metabolite of antitumor agents from the group of oxazaphosphorins (ifosfamide, cyclophosphamide), which irritates the bladder mucosa. The protective properties of mesna are due to the interaction with the double bond of the acrolein molecule, which leads to the formation of a stable non-toxic thioester. By reducing the urotoxic effects of oxazaphosphorins, mesna does not weaken their antitumor effect.

Pharmacokinetics

When administered intravenously, Uromitexane is rapidly oxidized to disulfide, and in the kidneys it is reduced to a free thiol compound, which irreversibly binds to alkylating derivatives, forming non-toxic stable thioesters. Maximum elimination is 2-3 hours after intravenous injection.

The half-life after intravenous use at a dose of 60 mg / kg in the fast phase is 0.17 hours, in the slow phase – 1.08 hours. It is completely excreted by the kidneys within 8 hours, and in the first 4 hours it is excreted in the form of SH-mesna,32% of the dose – in the form of thiol and 33% – disulfide. When taken orally, absorption occurs in the small intestine.

The average peak concentration of free thiol compounds in the urine is reached after 2-4 hours. About 25 + 10% of the dose taken is detected in the urine as a free mesna in the first 4 hours.

In a dose of 2-4 g / sq. m.. the half-life of ifosfamide is about 4-8 hours. To maintain an adequate level of mesna in the bladder during the elimination of urotoxic metabolites of ifosfamide, an appropriate frequency of use is necessary.

Indications

Local detoxification of urotoxic effects of cytostatics-oxazaphosphorin derivatives, including in the following cases:

• with the introduction of oxazaphosphorins in high doses (more than 10 mg / kg);
• in patients at risk
• , previously performed radiation therapy for the pelvic region,

the development of cystitis during previous therapy with oxazaphosphorins, a history of urinary system diseases.

Contraindications

Hypersensitivity to mesna or any component of Uromitexan. Pregnancy and lactation.

Side effects

Nausea, vomiting, diarrhea (with a single dose of more than 60 mg / kg of body weight).

Rarely – phlebitis at the injection site, hematuria, allergic reactions on the skin and mucous membranes.

Interaction

Mesna is compatible with cyclophosphamide and ifosfamide, so it can be administered with them in the same solution, while the antitumor activity of the latter does not change.

Pharmacologically, the drug is incompatible with cisplatin (binding and inactivation of the latter), and therefore mesna should not be mixed in the same solution with cisplatin.

Mesna has no effect on the therapeutic efficacy of adriamycin, carmustine, cisplatin, methotrexate, vincristine, as well as on the activity of cardiac glycosides.

How to take, course of use and dosage

Uromitexan is administered intravenously in a slow jet, with a single dose of 20% of the single dose of oxazaphosphorin. The first injection is performed simultaneously with the first use of oxazaphosphorin, the second and third injections – 4 hours and 8 hours after the use of oxazaphosphorin.

With continuous infusion (24 hours) of ifosfamide or cyclophosphamide, Uromitexan should be administered at a dose of 20% of the cytostatic dose at the beginning of the infusion, then at a dose of 100% of the cytostatic dose in the form of a 24 – hour infusion, and after the end of cytostatic use, Uromitexan should be continued for another 6-12 hours at the same dose.

Combined intravenous and oral therapy. Uromitexan is administered intravenously (slowly) simultaneously with the first use of oxazaphosphorin, a single dose is 20% of the single dose of oxazaphosphorin. 2 and 6 hours after intravenous use, tablets are taken orally at a dose of 40% of the oxazaphosphorin dose.

Experience in treating children with Uromitexan tablets shows that more frequent (for example, every 3 hours) and longer (for example, up to 6 times) use of the drug is advisable.

Special instructions

Mesna has a protective effect only on the urinary system and does not eliminate other side effects of cytostatics, so when treating with drugs of the oxazaphosphorins group, it is necessary to use a full complex of maintenance and symptomatic therapy.

During the treatment period, false-positive reactions to the presence of ketone bodies in the urine are noted. Possible reddish-purple staining of the urine, which is unstable and immediately disappears when icy acetic acid is added to the urine.

Form of production

Concentrate for preparation of solution for infusions

Storage conditions

Store at a temperature not exceeding +25°C.

Shelf

life is 5 years.

Active ingredient

Mesna

Conditions of release from pharmacies

By prescription

Dosage form

infusion solution