5-fluorouracil injection 1000mg 20ml vial 20ml N1
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Description
5-Fluorouracil-Ebeve is an effective drug that is used to treat cancers of the stomach, breast and other organs. 5-Fluorouracil-Ebeve is used as both the main and auxiliary drugs during the course of chemotherapy.
Active ingredients
Fluorouracil
Release form
Solution
Composition
Active ingredient: fluorouracil 1000 mg. Excipients: sodium hydroxide, distilled water.
Pharmacological effect
Fluorouracil is an antimetabolite of uracil. The mechanism of action is due to the transformation of the drug in tissues into the active metabolite fluorouridine monophosphate, which is a competitive inhibitor of the enzyme thymidylate synthetase, which is involved in the synthesis of nucleic acids. Fluorouracil disrupts DNA synthesis and causes the formation of structurally imperfect 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, falling into the cerebrospinal fluid and brain tissue. Metabolized mainly in the liver to form 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 eliminated during the 1st hour) and 60-80% through the respiratory tract in the form of CO2, a small amount is excreted in the bile.
Indications
Colon and rectal cancer, breast cancer, esophagus cancer, stomach cancer, pancreatic cancer, primary liver cancer, ovarian cancer, cervical cancer, bladder cancer, head and neck cancers, prostate cancer, adrenal cancer, genital cancer member carcinoid.
Contraindications
Hypersensitivity to fluorouracil and / or any other component of the drug, pregnancy, breast-feeding, severe leukopenia, neutropenia, thrombocytopenia, stomatitis, ulceration of the gastrointestinal mucosa, pseudomembranous enterocolitisWith care: renal and / or liver failure, acute infectious diseases of a viral, fungal or bacterial nature (including tuberculosis, chicken pox, shingles), bone marrow infiltration with tumor cells, previous radiation therapy or chemotherapy.
Precautionary measures
In the event of side effects from the gastrointestinal tract, blood, central nervous system and heart treatment should be stopped immediately. Assign with caution in severe bone metastasis.
Use during pregnancy and lactation
Contraindicated in pregnancy, during lactation.
Dosage and administration
Dose and treatment regimen are determined individually depending on the patient's condition and type of cancer, and also depending on whether 5-fluorouracil is used as monotherapy or in combination with other drugs. It is necessary to begin treatment in the conditions of a hospital. The drug is administered intravenously in a stream or by slow infusion, intraarterially, intrathecal. The daily dose of 5-fluorouracil should not exceed 1 g. 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 is 4 weeks, 600 mg / m2 or 15 mg / kg (the highest single dose of 1 g) once a week, 6-10 doses, 600 mg / m2 in 1 and 8 days intravenously in combination with other cytostatics, 1 g / m2 / day intravenously in the form of a constant infusion in within 96-120 hours. When used in combination with calcium folinate, the dose of fluorouracil is usually reduced by 25-30%.
Side effects
On the part of the blood-forming organs: 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. On the part of the digestive system: loss of appetite, nausea, vomiting, inflammation and or ulceration of the mucous membranes of the gastrointestinal tract (t . stomatitis), diarrhea, bleeding from the gastrointestinal tract, heartburn and a change in taste, abnormal liver function. From the cardiovascular system: very rarely - pain in the heart, arrhythmias, ischemia, myocardial infarction, angina, heart failure. nervous system: rarely - my Zhechkov ataxia, sensory disorder, disorientation, confusion, euphoria, nystagmus, optic neuritis,headache. On the part of the sense organs: irritation of the mucous membrane of the eyes, excessive tearing due to duct stenosis (10-25%), photophobia, cataracts, cortical blindness (at high doses), impaired vision. On the part of the reproductive system: reversible inhibition of the function of the sex glands , leading to amenorrhea or azoospermia. On the side of the skin and skin appendages: alopecia (rare), skin hyperpigmentation, dryness and cracks of the skin, telangiectasia, erythrodestosis hand and foot syndrome (tingling sensation in hands and feet after blowing pain, hyperemia and swelling), changing and converging nail plates (rare), photosensitization. Allergic reactions: skin rash, dermatitis, urticaria, hyperemia of the skin of the palms and soles, bronchospasm, anaphylaxis (rare). Others: fever (rare), thrombophlebitis at the injection site, nosebleeds, cough, shortness of breath, hyperuricemia, weakness, the development of secondary infections.
Overdose
Symptoms: nausea, vomiting, diarrhea, ulcerative stomatitis and gastric bleeding, suppression of bone marrow function (thrombocytopenia, leukopenia and agranulocytosis). In case of overdose, monitor the hematopoietic function of patients for at least 4 weeks, if symptoms occur, symptomatic therapy is performed. The specific antidote to fluorouracil is not known.
Interaction with other drugs
Calcium folinate enhances the therapeutic and toxic effects of fluorouracil. When used in combination with other cytostatics and interferon-alpha, there can also be an increase in both the antitumor effect and the toxicity of fluorouracil. With prolonged joint use with mitomycin C, hemolytic uremic syndrome was observed. When taken concurrently with sorivudin, a marked leukopenia was noted, in some cases resulting in a lethal outcome. Fluorouracil should not be used after and in conjunction with therapy with aminophenazone, phenylbutazone and sulfonamide. Chlordiazooxide, disulfiram, griseofulvin and isoniazid can enhance the activity of fluorouracil. Fluorouracil can reduce the immunological response to vaccination. When administered simultaneously with a live vaccine, severe antigen reactions can develop.
special instructions
Fluorouracil is a cytotoxic drug, so care must be taken when handling it. When stomatitis or diarrhea appears, treatment with the drug must be stopped before these symptoms disappear. The initial dose should be reduced by 1/3 or 1/2 in the following cases: weight loss, postoperative a period of at least 30 days after extensive surgery, insufficient bone marrow function, impaired liver or kidney function. Caution should be exercised when prescribing to patients who have previously exposed Exposure to high doses of radiation on the pelvic area or treated with alkylating agents. During treatment, it is necessary to monitor the total number of leukocytes, the absolute number of neutrophils, platelets, determine hematocrit, hemoglobin, liver function tests and bilirubin level, examine the patient’s mouth for signs of stomatitis. Men and women of childbearing age during treatment with fluorouracil and for at least 3 months. then you should use reliable methods of contraception. Impact on the ability to drive vehicles and control mechanisms. The side effects caused by taking fluorouracil may adversely affect the management of the vehicle.