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. It is a mitotic inhibitor. Paclitaxel specifically binds to the beta-tubulin of microtubules, disrupting the process of depolymerization of this key protein, which leads to suppression of the normal dynamic reorganization of the microtubule network, which plays a decisive role during interphase and without which it is impossible to perform cellular functions in the mitosis phase. In addition, paclitaxel causes the formation of abnormal microtubule beams throughout the entire cell cycle and the formation of several centrioles during mitosis.
PHARMACOKINETICS
Binding to plasma proteins is 89-98%. Biotransformiruetsya mainly in the liver. It is excreted as kidneys in unchanged form, and with bile (both unchanged and in the form of metabolites).
INDICATIONS
Ovarian cancer (including with ineffectiveness of platinum drugs), breast cancer, lung cancer, esophagus cancer, head and neck 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
On the part of the hematopoiesis system: leukopenia, thrombocytopenia, anemia.
On the part of the digestive system: nausea, vomiting, diarrhea, mucositis, impaired appetite, constipation (rarely - the phenomenon of intestinal obstruction), an increase in the blood activity of hepatic enzymes and bilirubin level.
Allergic reactions: skin rash, angioedema, rarely - bronchospasm.
From the cardiovascular system: arterial hypotension, bradycardia, conduction disorders, peripheral edema.
Other: arthralgia, myalgia, peripheral neuropathy.
Local reactions: thrombophlebitis, with extravasation - necrosis.
CONTRAINDICATIONS
Severe neutropenia (less than 1500 / Ојl), pregnancy, hypersensitivity to paclitaxel.
PREGNANCY AND LACTATION
Paclitaxel is contraindicated in pregnancy. If it is necessary to use lactation, breastfeeding should be discontinued.
Women of childbearing age should apply reliable contraceptive methods during the use of paclitaxel.
In experimental studies , it has been established that paclitaxel has a teratogenic and embryotoxic effect.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
When using paclitaxel in patients with impaired liver function, a dosage regimen may need to be adjusted.
SPECIAL INSTRUCTIONS
With caution use paclitaxel in patients with angina pectoris, rhythm and conduction disorders, chronic heart failure, with chickenpox (including recently transferred or after contact with the sick), herpes zoster and other acute infectious diseases, and within 6 months after a recent myocardial infarction.
When using paclitaxel in patients with impaired liver function, a dosage regimen may need to be adjusted.
To prevent the occurrence of hypersensitivity reactions, all patients should undergo premedication (GCS, histamine H 1 - and H 2 -receptor blockers).
In the process of treatment, a systematic control of the peripheral blood pattern, control of blood pressure, ECG is necessary. Do not take another infusion of paclitaxel until the number of neutrophils exceeds 1500 / Ојl, and the platelet count is 100,000 / ОјL.
When using paclitaxel in patients with impaired liver function, a dosage regimen may need to be adjusted.
Do not recommend the vaccination of patients and their families.
When preparing and introducing a solution of paclitaxel, you should not use PVC infusion systems.
In experimental studies , it has been established that paclitaxel has a mutagenic effect.
DRUG INTERACTION
When conducting laboratory studies in patients who received consistent infusions of paclitaxel and cisplatin, a more pronounced myelotoxic effect was found when paclitaxel was administered after cisplatin; mean values ​​of total clearance of paclitaxel decreased by approximately 20%.
The previous administration of cimetidine does not affect the average values ​​of total clearance of paclitaxel.
Based on the data obtained in vivo and in vitro, it can be assumed that in patients receiving ketoconazole, a suppression of paclitaxel metabolism is observed.
