Fluorouracil (fluorouracil) solution for injections 50 mg/ml. 20 ml. №1 vial

$59.00

Manufacturer: Germany

Treatment of breast cancer and colorectal cancer (in the form of monotherapy or in combination with other Antineoplastic agents). Treatment of stomach cancer, head and neck cancer, and pancreatic cancer.

Category:

Description

Fluorouracil №1 vial Storage
active substance: fluorouracil;

1 ml of solution contains fluorouracil 50 mg;

Excipients: sodium hydroxide, water for injections.

Fluorouracil №1 vial Dosage form
Solution for injection.

Basic physical and chemical properties: transparent, colorless or almost colorless liquid.

Fluorouracil №1 vial Pharmacotherapeutic group
L01B C02.

Pharmacological properties
Pharmacodynamics.

Fluorouracil is an analogue of uracil, a component of ribonucleic acid. It is believed that the drug functions as an antimetabolite. After intracellular conversion to the active deoxynucleotide, it inhibits DNA synthesis by blocking the conversion of deoxyuridic acid to thymidyl acid by the cellular enzyme thymidylate synthetase. Fluorouracil may also interfere with RNA synthesis.

Pharmacokinetics.

Absorption Fluorouracil after oral administration is absorbed with very high variability in the gastrointestinal tract by first-pass metabolism caused by different levels of dihydropyrimidine dehydrogenase (DPD), the first enzyme of catabolic conversion of fluorouracil.

Distribution After intravenous fluorouracil is distributed in all body fluids and excreted from the blood within 3 hours. It is mainly absorbed by actively proliferating tissues and tumors after its conversion into a nucleotide. Fluorouracil readily crosses the blood-brain barrier and brain tissue.

Biotransformation Dihydropyrimidine dehydrogenase is the initial enzyme of fluorouracil catabolism, which causes catabolism of more than 85% of the administered dose to dihydrofluorouroracil. Dihydrofluorouracil is then converted to fluoro-β-ureidopropionate and then to fluoro-β-alanine. Deficiency of enzymes in this process can lead to severe and even life-threatening toxicity of fluorouracil. In case of hepatic insufficiency, the metabolism of fluorouracil is slowed down, which may require dose adjustment.

Intracellularly, fluorouracil is converted to the active metabolites fluorodeoxyuridine monophosphate, fluorodeoxyuridine triphosphate and fluorouridine triphosphate by a number of enzymes.

Elimination Following intravenous administration, the plasma half-life of fluorouracil is approximately 10-20 minutes and depends on the dose administered. After a single intravenous injection of fluorouracil, approximately 15% of the dose is excreted unchanged in the urine within 6 hours; more than 90% of the dose is excreted from the body within the first hour. The residue is metabolized mainly in the liver by the body’s normal mechanisms for uracil.

Indication
treatment of metastatic colorectal cancer;
adjuvant therapy for colon and rectal cancer;
treatment of advanced gastric cancer;
treatment of advanced pancreatic cancer;
treatment of advanced esophageal cancer;
treatment of advanced or metastatic breast cancer;
adjuvant therapy for operable primary invasive breast cancer;
treatment of inoperable locally advanced squamous cell carcinoma of the head and neck in patients without prior treatment;
treatment of local recurrent or metastatic squamous cell carcinoma of the head and neck.

Contraindication
significant deviations from the norm of the number of formed elements in the blood;
bleeding;
stomatitis, ulcers of the mucous membrane of the mouth and gastrointestinal tract;
severe diarrhea;
severe renal impairment;
plasma bilirubin level> 85 μmol / l;
vaccination with living organisms should be avoided during treatment with fluorouracil;
hypersensitivity to fluorouracil or to any of the excipients;
severe infectious diseases (shingles, chicken pox);
bone marrow suppression after radiation therapy or after treatment with other anticancer drugs;
patient with severe exhaustion;
severe liver dysfunction;
should not be used to treat benign tumors;
should not be used concomitantly with brivudine, sorivudine or their analogues (brivudine, sorivudine and analogues – potent inhibitors of the enzyme dihydropyrimidine dehydrogenase, which destroys fluorouracil);
complete deficiency of dihydropyrimidine dehydrogenase (DPD) (see section “Features”);
fluorouracil is absolutely contraindicated during pregnancy or breastfeeding.