Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
ONLS
АТХ:L.01.B.C.06 Capecitabine
Pharmacodynamics:In vivo is converted to 5-fluorouracil, followed by conversion to 5-fluoro-2-deoxyuridine monophosphate and 5-fluorouridine tri-phosphate. These metabolites inhibit the substances responsible for the formation of DNA, slow cell division, trigger the synthesis of defective RNA, violate protein synthesis. The main pharmacological effect of the drug, therefore, is antineoplastic.
Pharmacokinetics:Bioavailability decreases when taken with food; in the process of absorption becomes active metabolites, which are the effector substance. Half-life is about 45 minutes.Link with plasma proteins less than 60%, is eliminated after taking more than 70% of the kidneys. The primary biotransformation is carried out by liver enzymes. Secondary transformation of the active substance undergoes directly in cells.
Indications:Various forms of breast cancer resistant to other chemotherapy (for example, to paclitaxel), or if there are contraindications to them.
II.C50.C50 Malignant neoplasm of breast
Contraindications:Hypersensitivity to the drug, as well as to fluorouracil, fluoropyrimidine; pregnancy and the period of breastfeeding; children under 18 years of age (safety and efficacy not studied).
Pregnancy and lactation:Do not use during pregnancy! The action category for the fetus by FDA is D. Lactation: if necessary, treat capecitabine to stop breastfeeding. There is no data on the penetration of the drug into breast milk.
Dosing and Administration:The drug is taken inwards, 30 minutes after eating. The starting dose is 2.5 g / m2/ day (for 2 sessions) for 2 weeks, then take a break for 1 week. The total daily dose depends on the surface area of the body.
| < 1,24 m2 | 3 g |
| 1.25 - 1.36 m2 | 3.3 g |
| 1.37-1.51 m2 | 3.6 g |
| 1.52 - 1.64 m2 | 4 grams |
| 1.65-1.76 m2 | 4.3 g |
| 1.77-1.91 m2 | 4.6 g |
| 1.92 - 2.04 m2 | 5 grams |
| 2.05 - 2.17 m2 | 5.3 g |
| > 2.18 m2 | 5.6 g |
Dose change depending on the degree of toxic effects (Canadian classification of cytotoxicity).
1 degree - do not change the dose.
2 degree - at the first appearance of signs of toxicity, it is necessary to stop therapy until they disappear or decrease to the 1 st degree.
Renewal treatment with 100% of the recommended dose. When the second degree of cytotoxicity reappears, the dose after a break is reduced to 75%, then to 50%, with the fifth appearance of the second degree of cytotoxicity, the drug is canceled permanently.
3 degree - cancel the drug before returning to symptoms of the level of 1-st degree of toxicity. Renewal treatment with 75% of the recommended dose. In case of repeated manifestation of cytotoxicity of the third degree, the next attempt of treatment is made with a 50% dosage, with the fourth manifestation of toxicity signs the drug is canceled.
4 degree of toxicity - the drug is canceled.
Side effects:Diarrhea. Dose-dependent, develops in 50% of patients. May lead to dehydration. According to the National Cancer Institute, severe manifestations of diarrhea due to the use of capecitabine are relatively rare: diarrhea of 3rd and 4th degree occurs in 12% and 3%, respectively. The "Hand and Foot" syndrome, which is also known as acryl erythremia, induced by chemotherapy. It is manifested by skin peeling, blistering of the hands and feet, decreased sensitivity, cold skin. Occurs in 13-74% of patients.
Depression of bone marrow hemopoiesis - anemia (74%), neutropenia (26%) or neutropenia (24%).
Cough of 4.6%.
Hypotension.
Infections of the upper respiratory tract - rhinitis, pharyngitis.
Hyperuricemia or gout, leukopenia, thrombocytopenia, back pain.
Interaction:Antithrombotic preparations of coumarin (warfarin) - violation of coagulation parameters. There are deaths even after the month of withdrawal of capecitabine in the application of coumarins. Control international normalized attitude, prescribe anticoagulants in reduced doses. Means that inhibit bone marrow hematopoiesis, radiation therapy - an increase in symptoms. It is necessary to appoint capecitabine in reduced doses.
Avoid the use of live viral vaccines in the treatment with capecitabine - the immune response is compromised. Do not administer live viral vaccines for at least 3 months from the last chemotherapy cycle.
Special instructions:Before starting treatment, a specialist consultation is necessary. In the process of treatment, individual dose selection is carried out. The following parameters are carefully monitored: international normalized attitude, alkaline phosphatase, hepatic transaminases, bilirubin, red and white blood, creatinine.
The safety of use in patients with renal insufficiency is not established.
The appointment of anticoagulants coumarinovogo number is possible not earlier than 1 month after the end of chemotherapy capecitabine.
The patient at the time of admission should be careful when driving and performing other precise work that requires concentration of attention and a high reaction rate.
Capecitabine is immediately canceled with diarrhea of the 2nd degree of severity and higher (4-6-fold chair per day, stool at night); with the syndrome "hand and leg" of the 2nd degree of severity and higher (painful erythema and / or edema of the palms or feet, causing discomfort); the increase in bilirubin is 1.5 times higher than before treatment; when vomiting more than 5 times a day; the drug is canceled until the symptoms are normalized or reduced. Then you can resume treatment with capecitabine at reduced doses.