"Capecitabine": instructions for use, reviews, analogs, form of release, manufacturer. "Capecitabine-TL": instructions

Capecitabine (Latin Capecitabinum ) is a substance that is a derivative of fluoropyrimidine carbamate. It is referred to the group of antimetabolites - special compounds that can inhibit the growth of malignant tumors. Interest in such substances arose in 1960. First, positive data were obtained by research on laboratory mice. After some time, their effectiveness in the treatment of some human cancer was found.

To date, many antitumor drugs contain capecitabine as an active ingredient. The opinions of many patients indicate the success of using such drugs in anticancer therapy.

Pharmacological group and properties

The capecitabine formula is 5'-deoxy-5-fluoro-N - [(pentyloxy) carbonyl] cytidine. The chemical group of antimetabolites is represented by a number of substances that are close in nature to the products of human metabolism (metabolism). They are able to enter into metabolic reactions, correct them and inhibit some biochemical processes. This disrupts the normal functioning of tumor cells and inhibits their growth when using drugs based on the substance capecitabine. The opinions of people speak about the reduction in the size of the neoplasm. This mechanism of action is called cytostatic.

Such properties of antimetabolite substances allow using them in antitumor therapy. Their effectiveness in relation to malignant neoplasms of the gastrointestinal tract and mammary glands is proved. In this case, a good result is obtained by either monotherapy or combination with other means. To date, more than 800 preparations have been created on the basis of antimetabolites, but the search for new groups of compounds is still ongoing.

Mechanism of action

Activation of capecitabine occurs in the tissues of the tumor itself, after which it begins to exert a toxic effect on its cells (cytotoxic mechanism). This substance is involved in the metabolic reaction and leads to the fact that both healthy and tumor cells will be converted into cytotoxic analogs. At the same time, there is a disruption in the production of the substance necessary for the synthesis of DNA and, accordingly, the fission process.

So the cells stop increasing their numbers. According to another scenario, "substitution" of one substance for another occurs, as a result of which protein synthesis is violated when taking drugs based on the capecitabine compound. The instruction describes this process in detail.

The mechanism of this transformation minimizes the possibility of damage to healthy cells. Capecitabine is more concentrated in the tumor itself than in the surrounding tissues. This feature is less harmful to the body when a person is treated with a drug based on the substance capecitabine. Instruction for use recommends taking the medication in strictly prescribed doses, which is determined by the attending physician.

Staying in the body

After taking capecitabine, it is rapidly absorbed in the gastrointestinal tract. If at this time to eat, then the process will slow down. Therefore, drugs based on antimetabolites are taken after meals. Further transformations of the substance occur in the liver, a certain amount of capecitabine and its metabolites bind to proteins (eg, blood albumin). The peak content in blood plasma is achieved after 1.5 -3 hours after application of the drug. This is indicated in the instruction for the drug "Capecitabine" instruction. Analogs have similar pharmacokinetics.

Most of the substance is excreted in the urine, the smaller part - with feces. And the body leaves not only capecitabine in an unchanged form (about 3%), but also its derivatives. Some of them are metabolized to less active compounds. The presence and transformation of capecitabine in the body is not affected by sex, age, race.

When appoint?

Capecitabine in the form of various drugs is prescribed for patients with breast cancer, including at the stage of metastasis. In this case, the substance is used in the monotherapy, or combined treatment in the presence of contraindications or lack of efficacy of chemotherapy. Most often, capecitabine is combined with docetaxel.

Also, patients with cancer of the colon, esophagus, stomach, pancreas, colorectal cancer are prescribed both at the stage of local spread and during the metastasis. In the treatment of colon cancer, "Capecitabine" is also prescribed. Instructions for use recommend that you carefully follow the dosage and follow the advice of your doctor.

Interaction with other means

If chemotherapy courses are not effective, an oncologist may appoint a combination treatment, where "Capecitabine" will be involved. The instruction for use lists the means with which a successful combination is possible.

For example, with "Docetaxel" - a preparation of a cytotoxic type of action, which is of vegetable origin. It can persist for a long time in cells in high concentrations. However, this combination of drugs is contraindicated for people with a platelet count and neutrophil count of 100,000 / μL and 1500 / μL, respectively. Also, "Docetaxel" is not used for patients with an increased norm of bilirubin. In this case, unpleasant consequences are possible. If "Docetaxel" for some reason "drops out" of the treatment scheme, continue therapy with "Capecitabine", but in reduced doses.

If a hypersensitivity reaction occurs, treatment with "Capecitabine" and "Docetaxel" discontinues and eliminates the symptoms. The scheme of combined intake of drugs is developed by a competent oncologist. In the event of toxic effects, this scheme is adjusted.

"Capecitabine" is not prescribed concomitantly with "Sorivudine" - an antiviral agent. This combination can increase the toxicity of the first drug. Joint use with an antiepileptic drug "Phenytoin" increases the concentration of the latter in blood plasma. It is also possible to disrupt blood clotting when using coumarin anticoagulants and drugs, where the main component is capecitabine. Instruction for use warns of possible consequences, so it is necessary to familiarize yourself with it beforehand.

Who is contraindicated?

The reasons for which the drug is contraindicated or restricted may be:

• High sensitivity (hypersensitivity reaction).
• The presence of severe form of renal and hepatic insufficiency.
• Different stages of pregnancy (the drug affects the fetus), except cases when the mother's life is given priority;
• Feeding a newborn baby.

Also capecitabine intake is restricted for people with coronary heart disease (CHD), with a state of increased bilirubin concentration in the blood, liver damage with metastases with a violation of its basic functions. For young children and people of advanced age, the drug is not recommended. This confirms the instruction to the drug "Capecitabine" instruction. The patient's testimonies speak of a lot of side effects and toxic manifestations in the treatment. Therefore, therapy with capecitabine is carried out under the strict supervision of an oncologist.

Are there side effects?

After taking the drug, there is a headache, a state of rapid fatigue, apathy, weakness. There may be insomnia, or, on the contrary - drowsiness. In rare cases - a violation of coordination and balance, confusion.

A side effect on the cardiovascular system is anemia (anemia). To a lesser extent, the emergence of angina pectoris, myocardial ischemia, heart attack, heart failure, and others. If breathing is involved in the process, dyspnea, a feeling of sore throat, coughing may appear. Very rarely - pulmonary embolism, spasm of the lungs.

When used as a part of monotherapy or combined treatment, a negative effect on the musculoskeletal system is possible. It manifests itself in pain in the limbs and lower back, the appearance of hypertonic muscles (myalgia), joint pain (arthralgia).

Skin can also be affected. Dermatitis, erythema, excessive dryness of the skin, redness, tingling, numbness, peeling, itching, increased pigmentation, damage affects the nails. In rare cases, skin cracks occur, increased sensitivity to ultraviolet radiation, detachment and increased fragility of the nail plates.

Among other side effects may occur infectious processes in the background of a decrease in the body's defenses. After all, therapy with the drug causes a decrease in the blood of platelets and white blood cells. Such manifestations describe the instructions for use for the drug "Capecitabine". Analogues give the same effects.

Reception of the drug

"Capecitabine" is suitable for internal use only. Usually it is washed down with water after half an hour after eating, but not later. The daily dose is determined by the treating oncologist, depending on the size of the neoplasm, the stage of development and the total body surface area. It is desirable that the specialist already had the skills to work with this drug. Most often appoint a two-time reception - morning and evening. At the same time, the entire course takes two weeks, then a seven-day break, followed by a repeat treatment.

For patients with renal failure, daily doses are reduced. With a decrease in the number of leukocytes (leukopenia) and neutrophilic granulocytes (neutropenia) in the blood continue to take the drug. So recommends the tool "Capecitabine" instructions for use. Synonyms or analogues are prescribed at the initiative of the attending physician.

Degree of toxicity

There are several degrees, according to which the toxic effect of the drug "Capecitabine" (instruction for use) develops. The opinions of many people say that this process is purely individual.

There are several degrees of toxicity:

• 1 degree. There are minor side effects.
• 2 degree. Intensive diarrhea (up to 4 times a day), accompanied by swelling of the extremities, redness, impaired activity, a sharp increase in bilirubin. At this stage, the reception of capecitabine is interrupted until the appearance of signs of toxicity of the 1 st stage.
• 3 degree. Diarrhea becomes more frequent up to 9 times a day. There is a violation of absorption (malabsorption syndrome). In this case, there is a strong skin peeling, redness, the appearance of ulcers and blisters. There are sharp pains in the extremities, a decrease in working capacity. Bilirubin rises 3 times. At this stage, treatment is interrupted, and with the development of 1 degree of toxicity, the medication is continued in a reduced dose.
• 4 degree. More frequent diarrhea - up to 10 times a day. Fecal masses with an admixture of blood. There is a need to introduce medicines, bypassing the gastrointestinal tract. When there are signs of this degree, treatment is stopped and no longer renewed.

What precautions should be observed?

The course of treatment should be under close medical supervision. The specialist should detect toxic manifestations in time - be it nausea, diarrhea, etc. If these signs are found, the treatment is adjusted. If necessary, eliminate symptoms, reduce the daily dose, take a break. Treatment continues if signs of toxicity do not pose a threat to life.

For people with coronary heart disease, the supervision of a specialist should be particularly thorough. In this case, it is necessary to identify the negative impact on the cardiovascular system in time and take the necessary measures in time.

Experts refrain from using the substance in the practice of pediatrics. The effectiveness of its use for children is not established. If a woman of childbearing age is exposed to treatment, she should be warned about the effect of capecitabine on the fetus. During the course of therapy, she should use reliable contraceptives.

Preparations and analogues

There are several means on the basis of capecitabine. On the Russian market there are 7 trade names of drugs produced by several domestic and foreign companies. For example:

• "Capecitabine."
• "Capecitabine-TL".
• "Tutabin".
• "Xeloda."
• "Cabecin".
• "Capecitover".
• "Capametin FS".

Since the basis of all these drugs is the same active substance - capecitabine, the instruction for them will be similar. Usually it shows the table for calculating the dosage taking into account the body weight and the treatment correction scheme for the appearance of signs of toxicity of different degrees.

It is important to understand that the first thing to be familiar with when, for example, "Capecitabine TL" was prescribed is the instruction. The information given in it is not suitable for independent application of funds! All calculations related to the dose setting and treatment regimen are made by the attending physician - an oncologist with sufficient competence in this matter. Self-administration of antitumor drugs causes irreparable harm to the body.

Let us consider some of the preparations in more detail.

Description of preparations

• "Capecitabine - TL" is produced by the Russian company LLC "Technology of medicines". The key component is capecitabine. Instructions for use, the form of release is of interest to many. Let's consider more in detail These are film-coated tablets. The content of the active substance is 150 or 500 mg. Auxiliary components: cellulose, lactose, croscarmellose sodium, hypromellose, magnesium stearate. In one package can be 60 or 120 tablets, depending on the dosage of the drug "Capecitabine - TL". The instruction must contain detailed information about the use of the tool.
• "Capecitabine" is a domestic preparation with the same active ingredient. Its description is similar to the means given above. The form of the drug "Capecitabine" is a tablet. Instructions for use are also enclosed in the packaging.
• "Kabattsin" is an antitumor drug of Russian manufacture (LLC "Company" Decaux "). The form of the release is a tablet in a film coating of 150 or 500 mg of the active substance. Secondary components: microcrystalline cellulose, crospovidone, starch, magnesium stearate. Leave from pharmacies only by prescription.
• "Capecitover" is a product of the Russian company "Veropharm". This antitumor drug is available in tablets of 150 or 500 mg in quantities of 60 to 120 pieces. In addition to capecitabine, the formulation includes lactose, cellulose, croscarmellose sodium, sodium stearate and hypromellose.
• "Capametin FS" - produced by the Russian company "Nativa" - an active participant in the import substitution program for medicines. "Capametin FS" is released with a dosage of 150 - 500 mg, the active ingredient is capecitabine. Instructions for use (the manufacturer in it, too, is indicated) will tell you how many in the package of tablets - 60 or 120.
• "Tutabin" is a foreign preparation based on capecitabine. It is produced by the Argentine company Laboratorio VARIFARMA SA, which is also the registrar of the facility. "Tutabin" is released in the form of tablets with an active substance content of 500 mg. Packing is a cardboard box with the attached instruction.
• "Xeloda" is an antitumor agent. Produced in Switzerland by the firm F. Hoffman La Roche, as well as its subsidiaries and offices in other countries - Mexico and the United States. On the Russian market there are 5 preparations with such a trade name. Form release - tablets (150 - 500 mg) for 60 or 120 pcs. In one package.

Reviews

Reviews about the work of drugs based on capecitabine are very different. Most of them are positive, but there are also negative reviews. However, this does not characterize these means, either good or bad, because the factor of the individuality of the organism of each individual person should always be taken into account. The reception of the same remedy by different people never gives the same result. Of great importance is the organ that was affected by the neoplasm and how long ago it has occurred.

People who took the drug, talk about a strong toxic effect after several days of admission. However, many people note a significant improvement in their condition and even entry into the period of remission. An important condition for the drug to work as well as possible for a single person is the advice of an oncologist and a clear adherence to his instructions for treatment.