Active substanceMesnaMesna
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  • Dosage form: & nbspSolution for intravenous administration.
    Composition:In 1 ml of solution contains: active substance: mesna - 100 mg; Excipients: sodium benzoate, disodium edetate (Trilon B), sodium hydroxide (sodium hydroxide), water for injection.
    Description:Transparent with light opalescence, colorless or slightly colored liquid.
    Pharmacotherapeutic group:Antidote.
    ATX: & nbsp

    V.03.A.F   Drugs that reduce the toxicity of cytostatic therapy

    Pharmacodynamics:Mesna is an antidote of acrolein, a metabolite of antitumor agents from the group of oxazaphosphorines (ifosfamide, cyclophosphamide), which has an irritant effect on the mucosa of the bladder. The protective properties of mesna are due to the interaction with the double bond of the molecule of acrolein, which leads to the formation of a stable thioether. By reducing the urotoxic effects of oxazaphosphorines, mesna does not weaken their antitumor effect.
    Pharmacokinetics:With intravenous (IV) administration, the active substance is rapidly oxidized to disulfide (dimus). In the epithelium of the renal tubules, the dimene is reduced to a free thiol compound,which irreversibly binds to metabolites of oxazaphosphorines, forming non-toxic stable thioethers. Communication with plasma proteins is 69-75%. The system clearance is 1.23 l / h / kg /.
    After intravenous administration in a dose of 800 mg, the periods of the half-excreta mesna and the dimes in the blood are 0.36 h and 1.17 h, respectively. About 32% and 33% of the administered dose were excreted by the kidneys within 24 hours, respectively, in the form of mesna and dimesna. Most of the reconstituted dose was excreted by the kidneys within 4 hours.
    Indications:Local detoxification of urotoxic effects of cytostatics - derivatives of oxazaphosphorines, incl. in the following cases:
    - with the administration of ifosfamide;
    - with the introduction of oxazaphosphorines in high doses (more than 10 mg / kg);
    - in patients at risk - previous radiation therapy on the pelvic area, development of cystitis during previous therapy with oxazaphosphorines, and a history of urinary system diseases.
    Contraindications:Hypersensitivity to mesene, any other component of the drug or thiol compounds.
    Pregnancy and lactation.
    Dosing and Administration:Mesna-LENS® usually injected intravenously (slowly).A single dose for adults is 20% of a single dose of oxazaphosphorin. The first administration is carried out simultaneously with the first administration of oxazaphosphorin, the second and third injections are administered 4 hours and 8 hours after the administration of the oxazaphosphorin.
    Children have a single dose of Mesna-LENS® is 60% of the dose of cytostatic, the administration of the drug is continued every 3 hours.
    With continuous infusion (24 hours) ifosfamide or cyclophosphamide, the drug Mesna-LENS® should be administered at a dose of 20% of the dose of the cytostatic at the start of the infusion, then at a dose of 100% of the dose of the cytotoxic in the form of a 24-hour infusion and at the end of the introduction of the cytotoxic, the administration of the Mesna-LENS® continue for another 6-12 hours in the same dose.
    In the case of the use of oxazaphosphorines in very high doses, for example, before bone marrow transplantation, the total dose of Mesna-LENS® can be increased to 120-160% of the dose of oxazaphosphorin. After the introduction of 20% Mesna-LENS® at the beginning of cytostatic administration, the remaining calculated dose is recommended to be injected intravenously for a period of 24 hours. Alternatively, a fractional bolus injection is possible: for adults, 3 x 40% (time 0, 4, 8 hours) or 4 x 40% (time 0, 3, 6, 9 hours).Instead of bolus injections, short infusions with a duration of 15 minutes are possible.
    Side effects:Adverse reactions occurring more often than in single cases are listed according to the following gradation: very often (> 10%); often (> 1%, <10%); sometimes (> 0.1%, <1%); rarely (> 0.01%, <0.1%); extremely rare (<0.01%).
    On the part of the digestive system: often - nausea, vomiting, diarrhea, constipation, abdominal pain, flatulence, anorexia;
    From the hematopoiesis: very rarely - thrombocytopenia. Also observed was granulocytopenia, leukopenia, anemia. The causal relationship of these phenomena with the use of mesna has not been established, this could be due to concomitant cytotoxic therapy.
    From the central nervous system: often - dizziness, drowsiness, headache, irritability, depression.
    From the cardiovascular system: often - the "tide" of blood to the face.
    From the immune system: very rarely - hypersensitivity reactions (skin rash, itching, Lyell syndrome, Stevens-Johnson syndrome, urticaria, conjunctivitis, anaphylactoid reactions, lowering blood pressure, increasing blood pressure, tachycardia, tachypnea, myalgia, as well as increasing the activity of a number of functional hepatic samples , transaminases).
    From the respiratory system: often - a cough.
    Local reactions: rarely phlebitis at the injection site, pain and redness.
    Other: often - arthralgia, back pain, fever, chills, flu-like syndrome, pharyngitis; very rarely - pain in the extremities, increased fatigue, weakness, pneumonia, alopecia was also often observed. The causal relationship of these phenomena with the use of mesna has not been established, this could be due to concomitant cytotoxic therapy.
    Overdose:Specific antidote for mesna is not known. Possible symptoms of an overdose: nausea, flatulence, diarrhea, headache, fatigue, pain in the limbs and joints, malaise, weakness, depression, irritability, skin rash, lowering blood pressure, tachycardia.
    Treatment is symptomatic.
    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.
    Pharmaceutically, the drug is incompatible with cisplatin (binding and inactivation of the latter), so mesna should not be mixed in one solution with cisplatin.
    Mesna has no effect on the therapeutic efficacy of doxorubicin, carmustine, cisplatin, methotrexate, vincristine, and the activity of cardiac glycosides.
    Special instructions:Mesna has a protective effect only on the urinary system and does not eliminate other side effects of cytostatics, so when treating drugs with the group of oxazaphosphorines it is necessary to use a full range of maintenance and symptomatic therapy.
    Mesna does not prevent the development of hemorrhagic cystitis in all patients. Therefore, every morning urine sample must be analyzed for hematuria. In the case of hematuria with mesne with oxazaphosphorines according to the recommended dosing regimen, lower doses or discontinuation of oxazaphosphorin therapy may be required.
    Because of the possibility of developing anaphylactic reactions, it is necessary to guarantee the availability of suitable medications for emergency care.
    In patients with autoimmune diseases treated with cyclophosphamide and mesenchymal, hypersensitivity reactions are detected at a higher frequency.In such patients, the protection of the urinary tract by mesna should only be carried out after a thorough analysis of the risk-benefit and under careful medical supervision.
    During treatment, false positive reactions to the presence of ketone bodies in the urine are noted (when carrying out a color reaction to ketones, a reddish-violet staining of urine is possible, which is unstable and immediately disappears when glacial acetic acid is added to the urine).
    Effect on the ability to drive transp. cf. and fur:
    Form release / dosage:The solution for intravenous administration is 200 mg / 2 ml and 400 mg / 4 ml (100 mg / ml) in vials.
    Packaging:Each bottle with instructions for use in a pack of cardboard, or 3, 5 or 10 bottles, along with instruction for use in a pack with partitions or special cardboard sockets. For 50, 85, 100 bottles with instructions for use, based on one instruction for ten bottles, in a box of cardboard (for hospitals).
    Storage conditions:List B.
    In a dry, the dark place at a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:2 years.
    Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001945 / 01
    Date of registration:07.10.2008 / 29.07.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp2016-08-24
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