Fluorouracil-LENS 50mg/ml vials 5ml, 10pcs

Composition

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1 ml of the solution contains:  

Active ingredient:

fluorouracil 50 mg

Auxiliary substances:

sodium hydroxide – 15.37 mg,

water for injection-up to 1 ml

Pharmacological action

Fluorouracil is an antimetabolite of uracil.

The mechanism of action is due to the conversion of the drug in tissues to the active metabolite fluoruridine monophosphate, which is a competitive inhibitor of the thymidylate synthetase enzyme 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 inside the cell

Indications

Colon and rectal cancer, breast cancer, esophageal cancer, stomach cancer, pancreatic cancer, primary liver cancer, ovarian cancer, cervical cancer, bladder cancer, head and neck cancers, prostate cancer, adrenal cancer, penile cancer, carcinoid.

Use during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

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, pseudomebranous enterocolitis.

With caution: use in patients with renal and / or hepatic insufficiency, acute infectious diseases of viral, fungal or bacterial nature (including tuberculosis, chickenpox, shingles), infiltration of the bone marrow with tumor cells, previous radiation therapy or chemotherapy.

Side effects

Hematopoietic disorders: leukopenia, neutropenia, rarely-thrombocytopenia, anemia. The most significant drop in the number of white blood cells is usually observed from 9 to 14 days (up to 25 days), platelets – from 7 to 17 days of treatment.

From the digestive system: decreased appetite, nausea, vomiting, inflammation and / or ulceration of the gastrointestinal mucosa (including stomatitis), diarrhea, bleeding from the gastrointestinal tract, heartburn and taste changes, impaired liver function.

From the cardiovascular system: very rarely-pain in the heart, arrhythmias, ischemia, myocardial infarction, angina pectoris, heart failure.

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

From the sensory organs: irritation of the eye mucosa, excessive lacrimation due to ductal stenosis (10% -25%), photophobia, cataracts, cortical blindness (at high doses), visual impairment.

From the reproductive system: reversible suppression of the function of the sex glands, leading to amenorrhea or azoospermia.

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

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

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

Interaction

of Calcium folinate enhances the therapeutic and toxic effects of fluorouracil. When used in combination with other cytostatics and interferon-alpha, an increase in both the antitumor effect and the toxicity of fluorouracil can also be observed. Long-term concomitant use with mitomycin C resulted in the appearance of hemolytic uremic syndrome.

When taking sorivudine concomitantly, severe leukopenia was observed, in some cases leading to a fatal outcome.

Fluorouracil should not be used after or in combination with aminophenazone, phenylbutazone, or sulfonamide therapy.

Chlordiazopoxide, disulfiram, griseofulvin, and isoniazid may enhance the activity of 5-fluorouracil. Fluorouracil may reduce the immunological response to vaccination. When administered concomitantly with a live vaccine, severe antigenic reactions may develop.

How to take, course of use and dosage

Fluorouracil is included in many chemotherapeutic treatment regimens, and therefore, when choosing the route of use, regimen and doses in each individual case, you should be guided by the data of the specialized literature.

The drug is administered intravenously in a jet or by slow infusion, intravenously, intracavitarily.

The following doses and regimens are recommended:

• 500 mg/m 2 or 12-13,5 mg/kg daily for 3-5 days, the interval between courses of 4 weeks;
• 600 mg/m 2 or 15 mg/kg (maximum single dose 1 g) 1 time/week,6-10 doses;
• 600 mg/m 2 in 1 days and 8/in combination with other cytostatics;
• 1 g/m 2 /day/drip in the form of a continuous infusion for 96-120 h;

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

Overdose

Symptoms: nausea, vomiting, diarrhea, ulcerative stomatitis and gastric bleeding, suppression of bone marrow function (thrombocytopenia, leukopenia and agranulocytosis).

Treatment: symptomatic therapy. A specific antidote to fluorouracil is not known. In case of overdose, the hematopoietic function of patients should be monitored for at least 4 weeks.

Functional features

After intravenous use, the drug is rapidly biotransformed and distributed in tumor tissues, intestinal mucosa, bone marrow, liver and other tissues. It easily penetrates the blood-brain barrier, entering the cerebrospinal fluid and brain tissue. It is mainly metabolized in the liver by collecting inactive metabolites. The half-life of fluorouracil depends on the administered dose and is 8-22 minutes. About 20% of the drug is excreted unchanged by the kidneys within 6 hours (90% of this amount is excreted within 1 hour) and 60-80% – through the respiratory tract in the form of C02, a small amount is excreted with bile.

Special instructions

Fluorouracil-LANCE® is a cytotoxic drug, so caution should be exercised when handling it.

If stomatitis or diarrhea occurs, treatment with the drug should be discontinued until these symptoms disappear.

The initial dose should be reduced by 1/3 or 1/2 in the following cases: weight loss, postoperative 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 been exposed to high doses of radiation in the pelvic area or who have received alkylating drugs.

During treatment, it is necessary to monitor the total number of white blood cells, the absolute number of neutrophils, platelets, determine hematocrit, hemoglobin, the activity of “liver” tests and the level of bilirubin, examine the patient’s oral cavity for signs of stomatitis.

Men and women of childbearing age should use reliable methods of contraception during treatment with Fluorouracil-LANCE® and for at least 3 months thereafter.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

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

Form of production

Solution for intravascular and intracavitary use

Storage conditions

At a temperature of 15-25 °C

Shelf life

2 years

Active ingredient

Fluorouracil

Conditions of release from pharmacies

By prescription

Dosage form

infusion solution