Fluorouracil belongs to the category of cytostatics - antitumor drugs that effectively inhibit the development of malignant epithelial neoplasms, most often affecting the structure of the intestine, lungs, stomach and pancreas.
It is noted that fluorouracil is most effective in the treatment of malignant neoplasms of the gastrointestinal tract;its use in the treatment of cases of glandular cancer is much less effective.
Composition, form and storage conditions
Fluorouracil is available:
- In the form of a solution for injection , which is a completely clear liquid of a white or slightly yellowish color. The chemical composition of one milliliter of the finished 5% solution contains 50 mg of active ingredient( fluorouracil), sterile water and sodium hydroxide( sodium hydroxide) as auxiliary components. The dosage of ampoules with the prepared solution is 250 and 500 mg. A set of five ampoules is put in a cardboard pack.
- In the form of a concentrate for the preparation of medicinal solution , packaged in dark glass bottles, closed with rubber stoppers, having aluminum running-in and protective Teflon covers. The dosage of the drug in this dosage form is 250, 500, 1000 and 5000 mg.
- In the form of 5% cream "5-fluorouracil" , packed in a 20-gram tube, enclosed in an individual cardboard pack.
Fluorouracil is manufactured at specialized enterprises of leading pharmaceutical companies located in different parts of the globe:
- The drug "Ftoruracil Ebove" is manufactured by the Austrian company Ebeve Pharma.
- Drug "Fluorouracil Lance" is the development of the Russian pharmaceutical company Lance Farm.
- The drug "Ftoruratsil-Darnitsa" is produced at the enterprises of the Russian OJSC "Novosibkhimpharm" and the Ukrainian CJSC "Pharmacological company Darnitsa".
- The rights to manufacture the drug "Ftoruracil-Teva" belong to the Israeli pharmaceutical company Teva.
Indications for use
Fluorouracil is prescribed in cancer:
- of the skin;
- of the breast;
- of the stomach( in case of tumor recurrence, its metastasis to internal organs or impossibility of performing a surgical operation);
- of the intestine( with the localization of the tumor process in the tissues of the colon and rectum);
- of the bladder;
- of the pancreas;
- of the ovaries;
- of the adrenal gland;
- of esophagus;
- of the uterus;
- of the prostate;
- of the cervix;
- of the penis.
Fluorouracil has proven effective in treating:
- different precancerous conditions;
- scaly lichen( psoriasis);
- malignant neoplasms localized on the face, head and neck;
- nails( such as onycholysis).
5% cream "5-fluorouracil" is prescribed to treat:
- of sunny( actinic) keratosis - a benign skin disease provoked by too long exposure to the sun or by aging;
- vulvar condylomatosis;
- by carcinoma( basal cell);
- epithelial tumors on the skin;Genital warts and
- of papillomavirus infection( PID).
Fluorouracil is contraindicated:
- to women bearing a fetus;
- for mothers breastfeeding;
- with bleeding;
- in patients with allergic reactions to the drug in their medical history;
- to patients with an acute ulcer of the duodenum and stomach;
- for ulcerative colitis;
- in patients with severe anemia;
- with a deficit of leukocytes( leukopenia) and platelets( thrombocytopenia) in each unit of blood volume;
- for patients with severe infectious diseases;
- with pronounced protein deficiency, caused by a number of reasons: a violation of protein absorption in the intestine, a violation of protein synthesis( due to chronic liver diseases) or increased protein loss along with urine;
- to patients with severe kidney and liver pathologies;
- in the presence of conditions with an increased risk of bleeding;
- patients with multiple or extensive metastases in the brain tissue;
- with cancer cachexia( state of extreme exhaustion of the body);
- to patients who have just undergone surgery or have completed chemotherapy or radiotherapy;
- at the terminal stages of cancer, accompanied by pathological changes in the body of a sick person, which inevitably result in the growing death of all of its tissues.
Once in the patient's body, fluorouracil quickly transforms into a number of biologically active substances - metabolites, which begin to accumulate in the internal structures of cancer cells.
In the initial stages of treatment, excretion( medics call it half-life) of the drug from the patient's body occurs within twenty minutes.
With prolonged use, the half-life of fluorouracil is at least twenty hours, since active metabolites tend to accumulate in tissues.
Derivation of a larger( up to 80%) part of the drug, transformed into carbon dioxide, occurs through the lungs;remnants( about 20%) of the drug leave the human body through the kidneys. A small amount of the drug can be excreted with bile.
Having overcome the GEB( blood-brain barrier), fluorouracil penetrates into the cerebrospinal fluid and into the brain cells, after which it accumulates in all biological fluids of the human body, in the mucous membranes of the gastrointestinal tract, in the tissues of the bone marrow and liver.
Instruction for the use of fluorouracil
The drug is intended for intracavitary, intra-arterial and intravenous( by jet or slow infusion through the dropper) administration, and also for external use( in the form of 5% ointment).
Fluorouracil is a highly sought after component of numerous chemotherapy regimens.
The dosage, the treatment regimen and the route of administration of the drug in each case depend on the disease and are assigned by the treating specialist taking into account the condition of the sick person.
An exemplary list of fluorouracil treatment regimens looks like this:
- The drug( at a dosage of 13 milligrams per kilogram of total body weight or 500 milligrams of active substance per square meter of body surface) is administered daily for 3-5 days. After four weeks, a repetition of the course is possible.
- The patient continuously - for 36-48 hours - lies under a dropper( fluorouracil is administered intravenously, by the method of constant infusion).Dosage is carried out from the calculation: one gram of preparation per one square meter of body area.
- Once every seven days, the patient is given fluorouracil( at a rate of 15 mg per kg body weight, but not more than one gram at a time).The full course of this treatment involves taking 6-10 single doses of the drug.
- When fluorouracil is included in the complex treatment regimen providing for the use of other cytotoxic drugs, it is administered intravenously on the first and eighth day from the beginning of the course. Dosage is six hundred milligrams per one square.meter body surface.
The use of fluorouracil may be performed only by a highly qualified specialist with a solid experience in the use of cytotoxic drugs for the therapy of oncological tumors.
When treating fluorouracil, it is necessary to monitor the blood condition.
For this, the patient must take tests( at least three times during the week).The repeated use of fluorouracil( if it was possible to restore the cellular characteristics of the blood composition) after treatment with cytostatic drugs or after a course of chemotherapy is possible only after six weeks.
The same pause in the treatment with fluorouracil should be sustained after performing a complex surgical procedure.
If the drug is used for the treatment of condylomatosis, a drug consisting of one part of a solution of fluorouracil, the same amount of distilled water and four parts of dimexide is prepared.
The prepared mixture is used to make five-minute trays. After completing the procedure, a swab is placed inside the vagina, soaked in the same solution and kept in it for an hour. The duration of treatment is at least twelve days.
Side effect of
The main side effect of fluorouracil is the allergic reactions manifested in the appearance of:
- anaphylactic shock;
- severe itching and redness of the skin;
- bronchial spasms;
- attacks of nausea and vomiting;
- of liver failure;
- pronounced urticaria;
- severe diarrhea;
- of ulcerative stomatitis;
- bleeding from the gastrointestinal tract( manifested by bloody vomiting and black color feces);
- blood in the urine.
In addition, the following conditions may appear in the list of side effects of fluorouracil:
- The patient may have photophobia and visual disturbances, as well as attacks of severe headaches. Sometimes some patients are immersed in a state of euphoria, while others lose the ability to navigate in space.
- Some patients taking fluorouracil may experience increased lacrimation and a taste disorder. Examination of such patients can reveal the presence of nystagmus( involuntary and very rapid oscillatory movements of the eyeballs), inflammation of the optic nerve, dysarthria( difficulty articulation).Sometimes they can develop cataracts.
- Side effects of fluorouracil on the skin can provoke symptoms of dermatitis, the emergence of foci of hyperpigmentation, subcutaneous hemorrhage, hair loss. Skin covers, becoming very dry, become prone to cracking. A slight tingling in the feet and hands can soon be replaced by pain, the appearance of redness and swelling: this condition is called palmar-plantar erythrodysesthesia.
- Side effects of fluorouracil on the organs of the cardiovascular system can provoke myocardial ischemia, angina pectoris, thrombophlebitis.
- A general blood test can show a sharp decrease in the number of all kinds of cells( as is known, they are represented by red blood cells, leukocytes and platelets).The concentration of hemoglobin also decreases sharply.
- Taking fluorouracil may provoke a temporary disruption of the reproductive functions of the human body( eg, azoospermia - absence of sperm in the ejaculate or amenorrhea - no monthly).
An overdose of the drug may indicate the appearance of:
- attacks of nausea and vomiting;
- of ulcerative stomatitis;
- quantitative changes in blood composition( agranulocytosis, thrombocytopenia, erythrocytopenia, leukopenia);
- The use of fluorouracil is a contraindication to vaccination with live vaccines of host patients and relatives living with them, as the drug can reduce the production of antibodies or accelerate the spread of viruses in the body of a sick person. As a result, the vaccine can not be effective.
- During treatment with fluorouracil it is necessary to avoid contact with people suffering from infectious diseases. It is also necessary to refrain from engaging in traumatic sports and in every way avoid traumatic situations.
- High toxicity of fluorouracil is associated with the inevitable oppression of hematopoiesis. This effect can be observed during treatment, and one to two weeks after the completion of the therapeutic course.
- During the course of treatment, a constant( at least three times a week) control of the quantitative characteristics of peripheral blood is necessary. In the presence of the first signs of oppression of hematopoies, blood tests should be taken daily. Severe oppression of hematopoiesis is an indication for the urgent transfusion of leukocyte concentrate and fresh blood, the use of hemopoietic stimulants and the introduction of shock doses of vitamins. In the scheme of therapy necessarily include the intake of vitamins of group B.
- During the administration of fluorouracil, hygienic oral care should be particularly careful.
- All dental problems associated with the removal and treatment of teeth, it is advisable to decide before the use of fluorouracil, since the action of the drug can worsen the healing of mucosal lesions, provoke the appearance of increased bleeding, and the attachment of infection, fraught with the development of viral or infectious stomatitis.
- Preparation of a solution of fluorouracil requires great care and can only be carried out by specially trained medical personnel in a special cabinet equipped with a hood. On the employee at the same time must be a protective suit, disposable gloves, goggles and a mask. Used syringes, needles, ampoules and unused solution remain to be destroyed in accordance with the necessary precautions.
- Fluorouracil is incompatible with phenylbutazone and sulfanilamide preparations, so it can not be used in a joint treatment with them, nor can it be used after therapy with these drugs.
- If fluorouracil is used with calcium folinate, its dosage is reduced by 30%, since the effect of this agent can enhance both the therapeutic and toxic effects of the drug.
- Combination of fluorouracil with cytostatic drugs and with alpha interferon also enhances its anti-tumor and toxic effects.
- Given the immunosuppressive effect of fluorouracil, the patient can be vaccinated no earlier than three months( and in some cases after one year) after the end of treatment with this drug.
- Fluorouracil activity increases when it is used together with Isoniazid, Chlordiazepoxide, Griseofulvin, and Disulfiram.
- It is undesirable to include fluorouracil in one therapeutic regimen with metronidazole, since this drug is capable of increasing its toxicity.
- In order not to provoke the patient's hemolytic-uremic syndrome - a systemic illness that threatens the patient's life, do not use fluorouracil together with mitomycin for a long time.
My mom( she is 75 years old) went through one course of chemotherapy with this drug. A side effect manifested itself in constant nausea, vomiting, fever and severe weakness. In the reclining position, she felt more or less tolerable, and all attempts to get up and do the most simple housework ended in dizziness and nausea. She could not move for a long time and spent most of the time in bed. Appetite was completely absent. Even from the type of food and chewing people, she had nausea.
I was diagnosed with a second stage of adenocarcinoma of the sigmoid colon. Resection of the affected organ was performed. Two months later, a tumor was found in the liver. The results of the biopsy were sent to a laboratory study. I underwent two chemotherapy courses with fluorouracil. For both felt comfortable. On the third day after the completion of the second course, I started some incredible diarrhea. All attempts to consolidate the stool result in severe vomiting. The state is agonizing, it is not yet possible to normalize the state. Very much I ask competent people to help or assist advice or council how to cope with a diarrhea.
Price for Moscow
The average cost of fluorouracil( manufactured by the Austrian pharmaceutical company Ebove) in pharmacies in Moscow is given in the following list:
- Fluorouracil( 50 mg / ml), 1 bottle with 20 ml infusion solution - 280 rub.
- Fluorouracil 250 mg in 5 ml ampoules( 5 pieces) - 1250 rub.
- Fluorouracil 500 mg in ampoules of 10 ml( 5 pieces) - 2950 rub.
Analogues of fluorouracil
The analogues of fluorouracil are preparations:
Synonyms for the preparation
On the shelves of modern pharmacies, fluorouracil is represented by a number of medications registered under trademarks:
All these names are synonymous with the same medicinal product.