Universal reference book for medicines
Name of the preparation: FLUOROURACIL

Active substance: fluorouracil

Type: Antitumor drug.
Antimetabolite
Manufacturer: PHARMSTANDART (Russia) manufactured by PHARMSTANDART-BIOLEC (Ukraine)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

PHARMACHOLOGIC EFFECT
Antitumor agent from the group of antimetabolites.
Inhibits the process of cell division by blocking the synthesis of DNA (due to inhibition of the enzyme activity of thymidylate synthetase) and the formation of structurally deficient RNA (due to the introduction of fluorouracil into its structure).
PHARMACOKINETICS
Penetrates through the BBB.
Rapidly metabolized in tissues with the formation of an active metabolite - fluorouridine monophosphate. Catabolic cleavage occurs in the liver.
T 1/2 of fluorouracil in the initial phase is 10-20 minutes.
T 1/2 in the final phase may be about 20 hours, presumably due to the deposition of metabolites in the tissues.
It is released through the respiratory tract - 60-80% in the form of carbon dioxide, and also by the kidneys - 7-20% unchanged.

INDICATIONS
Skin cancer, colon cancer, rectal cancer, breast cancer, stomach cancer, liver cancer, uterine cancer, ovarian cancer, bladder cancer.

DOSING MODE
Established individually, depending on the indications and stage of the disease, the state of the hematopoiesis system, the scheme of antitumor therapy.

SIDE EFFECT
From the digestive system: diarrhea, stomatitis, esophagitis, nausea, vomiting.

On the part of the hematopoiesis system: anemia, leukopenia, thrombocytopenia.

From the coagulation system of blood: hemorrhage.

From the side of the central nervous system: ataxia, optic neuritis, headache, nystagmus, visual impairment, photophobia, euphoria, confusion, disorientation.

From the cardiovascular system: myocardial ischemia, stenocardia, thrombophlebitis.

From the side of the reproductive system: azoospermia, amenorrhea.

Dermatological reactions: alopecia, dermatitis, hyperpigmentation.

Allergic reactions: urticaria, bronchospasm.

CONTRAINDICATIONS
Peptic ulcer of the stomach and duodenum in the phase of exacerbation, bleeding of any location, high risk of gastrointestinal bleeding;
severe anemia, leukopenia, thrombocytopenia; pregnancy.
PREGNANCY AND LACTATION
Fluorouracil is contraindicated in pregnancy.
If necessary, use during lactation should stop breastfeeding.
Women of childbearing age should apply reliable contraceptive methods during fluorouracil therapy.

In experimental studies , teratogenic and embryotoxic effects of fluorouracil have been established.

APPLICATION FOR FUNCTIONS OF THE LIVER
For violations of kidney function, lower doses should be used.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
If violations of the liver function, lower doses should be used.

SPECIAL INSTRUCTIONS
It is not recommended to use fluorouracil in patients with chickenpox (including recently transferred or after contact with the diseased), herpes zoster and other acute infectious diseases.

Caution is used fluorouracil in patients who have previously received cytotoxic drugs or radiation therapy.

Do not recommend the vaccination of patients and their families on the background of therapy.

If violations of the liver or kidney function, lower doses should be used.

When stomatitis or diarrhea occurs, treatment should be stopped until these symptoms disappear.

Before and during fluorouracil therapy, monitor the picture of peripheral blood, laboratory indicators of liver and kidney function.

The most significant decrease in the number of leukocytes is usually observed between the 9th and 14th day of the first course of therapy, but delayed myelodepression (up to 20 days) is possible.
The normalization of the number of leukocytes occurs by the 30th day.
In experimental studies, a carcinogenic and mutagenic effect of fluorouracil has been established.

DRUG INTERACTION
With simultaneous use with other drugs that cause myelodepression, additive oppression of bone marrow function is possible;
with interferon alpha-2b - an increase in the initial concentration of fluorouracil in the blood plasma and a decrease in fluorouracil clearance.
In patients with colorectal cancer, concomitant use with metronidazole may increase the toxicity of fluorouracil.

In the case of prior use of fluorouracil, the cytotoxic action of paclitaxel may be inhibited.

In the case of prior application of cimetidine, an increase in the concentration of fluorouracil in the blood plasma is possible.

With the simultaneous use with allopurinol, methotrexate, a possible change in the antitumor effect of fluorouracil;
with calcium folinate - may enhance the antitumor and toxic effects of fluorouracil, especially on the gastrointestinal tract.
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