Paclitaxel actavis

Paclitaxel Actavis belongs to the pharmacological group of antitumor agents (cytostatics) of plant origin. Synonymous drugs: Taxol, Paclitaxel, Paclitaxel Ebeve, Paclitax, Paxen, Paklinor, Paclitaxel-Teva, Pactalik, Paclitera, Docetaxel, Abitaxel, Intaxel, Mitotax, Sindaxel, Taxacad, Yutaxan.

Indications Paclitaxel actavis

Indications for the use of Paclitaxel Actavis include the following oncological diseases:

• ovarian cancer;
• breast cancer;
• non-small cell lung cancer (adenocarcinoma, squamous cell and undifferentiated bronchoalveolar, large cell, mixed cell carcinoma);
• transitional cell carcinoma of the bladder;
• esophageal cancer;
• lymphocytic and non-lymphocytic leukemia;
• multiple hemorrhagic skin lesions ( Kaposi's sarcoma ).

For patients with diffuse ovarian cancer or residual neoplasia who have undergone laparotomy, Paclitaxel Actavis is a first-line therapy; in case of metastases after ineffective standard treatment - a second-line therapy.

In case of malignant breast tumors, Paclitaxel Actavis is used in postoperative (adjuvant) treatment - in the presence of affected lymph nodes, in case of relapse of the disease or the appearance of metastases.

In the treatment of non-small cell lung cancer, this drug is prescribed when surgery or radiation therapy is not expected. The use of Paclitaxel Actavis in Kaposi's sarcoma is indicated for patients with AIDS.

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Release form

The drug is available in a concentrated liquid form for the preparation of an infusion solution.

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Pharmacodynamics

The active ingredients of the drug Paclitaxel Actavis and its synonyms are taxanes - nitrogen-containing organic compounds (alkaloids) from the bark of a coniferous tree of the genus Taxus, the Pacific yew.

The mechanism of cytostatic action is based on the ability of the substance paclitaxel, obtained from taxanes, to inhibit the process of cellular mitosis in the initial phases.

Indirect division (mitosis) of eukaryotic cells begins with the formation of a mitotic apparatus in their cytoskeleton - an achromatic spindle, the mobile threads of which (microtubules) connect the poles of the cell and its center. After DNA doubling, the daughter chromosomes at the metaphase stage are concentrated in the center of the cell, and the task of the microtubules of the achromatic spindle is to move these chromosomes to different poles of the cell, where two new cells appear at the telophase stage.

Microtubules are formed by polymerization of the cytoplasmic globular protein tubulin, and paclitaxel, due to the similarity of taxane to tubulin, binds to free tubulin molecules. This increases the intensity and degree of tubulin polymerization and activates the process of microtubule formation, resulting in the formation of an excess of microtubules. And due to the suppression of the process of tubulin depolymerization, microtubules lose the ability to perform their functions. All this leads to a violation of not only the process of formation of the mitotic apparatus of cells, but also to the cessation of their division.

In addition, under the influence of Paclitaxel Actavis (and all drugs with paclitaxel), the normal arrangement of microtubules in the cytoskeleton is disrupted and many of their abnormal bundles and condensations appear.

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Pharmacokinetics

After entering the bloodstream, 89% to 98% of Paclitaxel Actavis binds to proteins. Within 30 minutes, half of the drug penetrates into the tissues of the intestine, liver, spleen, pancreas, heart and muscles.

The concentration of paclitaxel in the blood plasma after intravenous administration decreases in stages. Biological transformation of Paclitaxel Actavis occurs in the liver under the influence of cytochrome P450 enzymes - in the process of hydroxylation reaction, with the formation of the metabolite 6a-hydroxypaclitaxel.

The half-life of the drug varies widely - from 3 hours to two days. Paclitaxel actavis is excreted from the body mainly with bile; part of the drug is eliminated unchanged by the kidneys with urine.

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Dosing and administration

All cyclostatic drugs of the taxane group are administered in a hospital setting, under the control and supervision of an oncologist.

In order to prevent the development of a hypersensitivity reaction to the drug Paclitaxel Actavis, patients should be given corticosteroids before using it.

Method of administration Paclitaxel actavis - intravenous drip administration (for 3-24 hours). Individual dose is determined in accordance with the treatment protocol. Standard dosage: 135-175 mg/m2 ^. Repeated administration of the drug is performed after 21 days.

Paclitaxel Actavis concentrate is diluted before administration (to 0.3-1.2 mg/ml), for which one of the injection solutions is used - sodium chloride or glucose.

It should be borne in mind that the ready-to-use solution cannot be stored in the refrigerator, and its stability in the light and at a temperature of +25°C is maintained for a maximum of 27 hours.

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Use Paclitaxel actavis during pregnancy

The use of Paclitaxel Actavis during pregnancy and breastfeeding is contraindicated. It has been established that paclitaxel not only has an embryotoxic effect, but also reduces the reproductive capabilities of women of childbearing age.

Contraindications

The cytostatic drug Paclitaxel Actavis is contraindicated in cases of increased individual sensitivity to paclitaxel, acute infectious diseases, ischemic heart disease, a history of myocardial infarction, and also in cases of decreased levels of neutrophilic granulocytes in the blood (neutropenia).

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Side effects Paclitaxel actavis

The use of Paclitaxel Actavis may be accompanied by side effects in the form of: hair loss; nausea, vomiting and diarrhea; urticaria and skin itching; shortness of breath; edema; heart rhythm disturbances (tachycardia or bradycardia); increased or decreased blood pressure; joint and muscle pain; renal failure; anemia, neutropenia or thrombocytopenia.

In the presence of inflammatory pathologies, their aggravation may be observed. Side effects from the central and peripheral nervous system also appear, namely: paresthesia, impaired coordination of movements and vision, encephalopathic symptoms (weakness, headache, dizziness, rapid fatigue, sleep disorders, memory loss from consciousness).

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Overdose

In case of overdose of Paclitaxel Actavis, the most common symptoms are shortness of breath, a drop in blood pressure, angioedema, extensive urticaria, redness and erosive-ulcerative lesions of the mucous membranes of the oral cavity and pharynx, as well as hypoplastic anemia (due to suppression of the hematopoietic function of the bone marrow).

There is currently no specific antidote for paclitaxel, so symptomatic treatment is indicated. In case of significant overdose, the administration of Paclitaxel Actavis should be stopped.

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Interactions with other drugs

A number of drugs - ethinyl estradiol, retinoic acid, quercetin, ketoconazole, verapamil, diazepam, quinidine, dexamethasone, cyclosporine, vincristine - inhibit the metabolism of Paclitaxel Actavis.

The use of Paclitaxel Actavis in combination with the antitumor antibiotic doxorubicin produces side effects in the form of stomatitis and severe neutropenia.

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Storage conditions

The drug is on List B and requires storage in a dark place, at room temperature or in a refrigerator (at a temperature not lower than -2°C). Storing unopened vials in the refrigerator may cause sediment to form, which should dissolve at room temperature. Otherwise, the drug becomes unsuitable for use.

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Shelf life

The shelf life of the drug is 24 months.

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