Active substanceFluorouracilFluorouracil
Similar drugsTo uncover
  • 5-Fluorouracil-Ebwe
    solution in / in c / cavity 
  • Fluorouracil
    solution c / cavity in / vessel. 
    FARM STANDART, OJSC     Russia
  • Fluorouracil-DECO
    solution c / cavity in / vessel. 
    Company DEKO, LLC     Russia
  • Fluorouracil-LENS®
    solution in / vessel. 
    LENS-PHARM, LLC     Russia
  • Fluorouracil-RONTS®
    solution c / cavity in / vessel. 
  • Ftoruracil-Teva
    solution c / cavity in / vessel. 
  • Dosage form: & nbspintravascular solution
    Composition:

    1 ml of the solution contains:

    Active substance: fluorouracil 50 mg

    Excipients: sodium hydroxide - 15,37 mg, water for injection - up to 1 ml.

    Description:

    Transparent colorless or slightly colored liquid

    Pharmacotherapeutic group:antitumour agent, antimetabolite
    ATX: & nbsp

    L.01.B.C.02   Fluorouracil

    Pharmacodynamics:

    Fluorouracil antimetabolite of uracil. The mechanism of action is due to the transformation of the drug in tissues into an active metabolite, fluorouridine monophosphate, which is competitive, an inhibitor of the enzyme thymidylate synthetase, which takes part in the synthesis of nucleic acids. Fluorouracil violates the synthesis of DNA and causes the formation of structurally deficient RNA, inhibiting the division of tumor cells. Active metabolites are localized within the cell.

    Pharmacokinetics:

    After intravenous administration, the drug is rapidly biotransformed and distributed in tumor tissues, intestinal mucosa, bone marrow, liver and other tissues. Easily penetrates the blood-brain barrier, getting into the cerebrospinal fluid and brain tissue. Metabolized mainly in the liver with the formation of inactive metabolites. The half-life of fluorouracil depends on the dose administered and is 8-22 minutes. About 20% of the drug is excreted by the kidneys unchanged for 6 hours (90% of this amount is excreted within 1 hour) and 60-80% through the respiratory tract in the form of CO2, a small amount, excreted with bile.

    Indications:

    Cancer of the colon and rectum, breast cancer, esophageal cancer, stomach cancer, pancreas cancer, primary liver cancer, ovarian cancer, cervical cancer, uterus, bladder cancer, head and neck cancer, prostate cancer, adrenal cancer, cancer of the penis, carcinoid.

    Contraindications:
    • Hypersensitivity to fluorouracil and / or any other component of the drug.

    • Pregnancy and lactation.

    • Severe leukopenia, neutropenia, thrombocytopenia, stomatitis, ulceration of the gastrointestinal mucosa, pseudomembranous enterocolitis.

    Carefully:

    renal and / or hepatic insufficiency, acute infectious diseases of a viral, fungal or bacterial nature (including tuberculosis, chicken pox, shingles), bone marrow infiltration by tumor cells, previously conducted radiation therapy or chemotherapy.

    Pregnancy and lactation:The drug is contraindicated during pregnancy and lactation.
    Dosing and Administration:

    Fluorouracil is included in many chemotherapy regimens, in connection with which the choice of the route of administration, regimen and doses in each individual case should be guided by data from the literature.

    The drug is administered, intravenously struined or by slow infusion intraarterially, intracavitary

    The following doses and regimens are recommended:

    • 500 mg / m2 or 12-13.5 mg / kg daily for 3-5 days, the interval between courses - 4 weeks;

    • 600 mg / m2 or 15 mg / kg (highest single dose 1 g) once a week, 6-10 doses;

    • 600 mg / m2 on days 1 and 8 intravenously in combination with other cytostatics;

    • 1 g / m2 / day intravenously drip in the form of a constant infusion for 96-120 hours;

    When used in combination with calcium folinate, the dose of fluorouracil is usually reduced by 25-30%.

    Precautions for use:

    Fluorouracil-LENS® is a cytotoxic drug, so care must be taken when handling it.

    When stomatitis or diarrhea occurs, the drug should be discontinued until the symptoms disappear.

    The initial dose should be reduced by 1/3 or 1/2 in the following cases: weight loss, postoperative period not less than 30 days after extensive surgery, insufficient bone marrow function, impaired liver or kidney function.

    Care should be taken when prescribing to patients who have previously been exposed to high doses of radiation to the pelvic area or who received alkylating drugs.

    During the treatment it is necessary to control the total number of leukocytes, the absolute number of neutrophils, platelets, to determine hematocrit, hemoglobin, the activity of "liver" samples and the level of bilirubin, to examine the oral cavity of the patient to identify signs of stomatitis.

    Men and women of childbearing age during treatment with fluorouracil-LENS® and at least 3 months afterwards should use reliable methods of contraception.

    Side effects:

    From the hematopoiesis: leukopenia, neutropenia, rarely - thrombocytopenia, anemia. The most significant drop in the number of leukocytes is usually observed from 9 to 14 days (up to 25 days), platelets - from 7 to 17 days of treatment.

    From the digestive system: loss of appetite, nausea, vomiting, inflammation and or ulceration of the mucous membranes of the gastrointestinal tract (including stomatitis), diarrhea, bleeding from the gastrointestinal tract, heartburn and taste change, impaired liver function.

    From the side of cardio-vascular system: very rarely - pain in the heart, arrhythmias, ischemia, myocardial infarction, angina pectoris, heart failure.

    From the nervous system: rarely - cerebellar ataxia, violation sensitivity, disorientation, confusion, euphoria, nystagmus, retrobulbar neuritis, headache.

    From the sense organs: Irritation of the eye mucosa, excessive lachrymation due to duct stenosis (10% -25%), photophobia, cataract, cortical blindness (at high doses), visual impairment.

    On the part of the reproductive system: reversible oppression of the sexual glands, leading to amenorrhea or azoospermia.

    From the skin and skin appendages: alopecia (rarely), hyperpigmentation of the skin, dryness and skin cracks, telangiectasia, palmar-plantar erythrodysesthesia syndrome (tingling sensation in the hands and feet, followed by pain, hyperemia and swelling), nail plate changes and convergence (rarely), photosensitization.

    Allergic reactions: skin rash, dermatitis, urticaria, flushing of the skin of the palms and soles, bronchospasm, anaphylaxis (rarely).

    Other: fever (rare), thrombophlebitis at the injection site, epistaxis, cough, shortness of breath, hyperuricemia, weakness; development of secondary infections.

    Overdose:

    Signs and symptoms of an overdose include nausea, vomiting, diarrhea, ulcerative stomatitis and gastric bleeding, suppression of bone marrow function (thrombocytopenia, leukopenia and agranulocytosis). In case of an overdose, hematopoietic function should be monitored for at least 4 weeks, symptomatic therapy should be performed if abnormalities occur.

    The specific antidote to fluorouracil is not known.

    Interaction:

    Calcium folinate enhances the therapeutic and toxic effects of fluorouracil. Use in combination with other cytostatics and interferon-alpha can also be observed to enhance both the antitumor effect and the toxicity of fluorouracil. With prolonged joint use with mitomycin C, the appearance of hemolytic uremic syndrome was observed.

    With the simultaneous reception with the drug sorivudine marked leukopenia, in some cases, led to death.

    Fluorouracil should not be used after and with therapy with aminophenazone, phenylbutazone and sulfonamide.

    Chlordiazopoxide, disulfiram, griseofulvin and isoniazid can enhance the activity of 5 fluorouracil.

    Fluorouracil may reduce the immunological response to vaccination. With simultaneous administration with a live vaccine, severe antigenic reactions can develop.

    Effect on the ability to drive transp. cf. and fur:

    Side effects caused by taking fluorouracil can adversely affect the ability to drive a vehicle and perform work that requires a high rate of psychomotor reactions.




    Form release / dosage:Solution for intravascular injection 50 mg / ml
    Packaging:

    By 5 ml or 20 ml in bottles of neutral glass 1 of hydrolytic class, hermetically sealed with rubber stoppers, with capping caps of aluminum or aluminum-plastic caps.

    10 vials with instructions for use in a pack with partitions or special cardboard sockets.

    25. 35 or 50 bottles with an equal number of instructions for use in a cardboard box (for hospitals).

    Storage conditions:

    At a temperature of 15 to 25 ° C.

    Keep out of the reach of children!

    Shelf life:2 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N000011 / 01
    Date of registration:19.07.2011
    The owner of the registration certificate:LENS-PHARM, LLC LENS-PHARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp10.11.2015
    Illustrated instructions
      Instructions
      Up