Pactalek (Concentrate) Instructions for Use

Marketing Authorization Holder

Pharmatsel, LLC (Russia)

Manufactured By

Biolek Joint-Stock Company, JSC (Ukraine)

ATC Code

L01CD01 (Paclitaxel)

Active Substance

Paclitaxel (Rec.INN registered by WHO)

Dosage Form

Pactalek

Concentrate for solution for infusion 6 mg/1 ml: 5 ml, 16.7 ml, 25 ml, 35 ml, 41 ml or 50 ml vial 1 pc.

Dosage Form, Packaging, and Composition

5 ml – vials (1) made of glass tubing – cardboard packs.
5 ml – glass vials (1) – cardboard packs.
16.7 ml – glass vials (1) – cardboard packs.
25 ml – glass vials (1) – cardboard packs.
35 ml – glass vials (1) – cardboard packs.
41 ml – glass vials (1) – cardboard packs.
50 ml – glass vials (1) – cardboard packs.

Clinical-Pharmacological Group

Antineoplastic drug

Pharmacotherapeutic Group

Antineoplastic agent – alkaloid

Pharmacological Action

Antineoplastic agent. It is a mitosis inhibitor.

Paclitaxel specifically binds to the beta-tubulin of microtubules, disrupting the depolymerization process of this key protein, which leads to the suppression of the normal dynamic reorganization of the microtubule network, which plays a crucial role during interphase and without which the performance of cellular functions in the mitosis phase is impossible.

Furthermore, Paclitaxel causes the formation of abnormal microtubule bundles throughout the entire cell cycle and the formation of multiple centrioles during mitosis.

Pharmacokinetics

Plasma protein binding is 89-98%.

It is biotransformed primarily in the liver.

It is excreted both by the kidneys in unchanged form and with bile (both in unchanged form and as metabolites).

Indications

Ovarian cancer (including in cases of ineffectiveness of platinum drugs), breast cancer, lung cancer, esophageal cancer, head and neck cancer, bladder cancer.

ICD codes

Dosage Regimen

Determine the dosage individually based on the specific malignancy, disease stage, and the chosen chemotherapy regimen.

Administer the calculated dose as an intravenous infusion over 3 hours. Do not administer as a bolus injection.

For ovarian cancer, use a dose of 175 mg/m² every 3 weeks. For breast cancer, a dose of 175 mg/m² every 3 weeks is standard.

For non-small cell lung cancer, administer 175 mg/m² over 3 hours every 3 weeks.

Premedicate all patients approximately 30-60 minutes prior to the infusion to prevent severe hypersensitivity reactions. The standard premedication regimen includes a corticosteroid (e.g., dexamethasone) and histamine H1 and H2 receptor antagonists.

Monitor the complete blood count frequently during therapy. Withhold therapy if the neutrophil count is below 1500 cells/mcL or the platelet count is below 100,000 cells/mcL.

Perform dose adjustments for subsequent cycles based on the severity of observed neutropenia or peripheral neuropathy.

For patients with hepatic impairment, reduce the dose. Do not administer to patients with severe baseline hepatic impairment.

Dilute the concentrate prior to infusion in 0.9% Sodium Chloride Injection or 5% Dextrose Injection to a final concentration of 0.3 to 1.2 mg/ml.

Use an in-line filter with a microporous membrane not greater than 0.22 microns during administration. Do not use PVC infusion containers or administration sets.

Adverse Reactions

From the hematopoietic system: leukopenia, thrombocytopenia, anemia.

From the digestive system: nausea, vomiting, diarrhea, mucositis, loss of appetite, constipation (rarely – symptoms of intestinal obstruction), increased activity of liver enzymes and bilirubin levels in the blood.

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/mcL), pregnancy, hypersensitivity to paclitaxel.

Use in Pregnancy and Lactation

Paclitaxel is contraindicated for use during pregnancy.

If it is necessary to use during lactation, breastfeeding should be discontinued.

Women of childbearing potential should use reliable methods of contraception during the use of paclitaxel.

In experimental studies, it has been established that Paclitaxel has teratogenic and embryotoxic effects.

Use in Hepatic Impairment

For patients with hepatic insufficiency and the associated increased risk of toxicity (in particular, grade III-IV myelosuppression), a dose adjustment of paclitaxel is recommended.

It is necessary to establish careful monitoring of the patients’ condition.

Special Precautions

Paclitaxel should be used with caution in patients with angina pectoris, arrhythmias and conduction disorders, chronic heart failure, with chickenpox (including recently contracted or after contact with sick individuals), herpes zoster and other acute infectious diseases, as well as within 6 months after a myocardial infarction.

For patients with hepatic insufficiency and the associated increased risk of toxicity (in particular, grade III-IV myelosuppression), a dose adjustment of paclitaxel is recommended. It is necessary to establish careful monitoring of the patients’ condition.

To prevent the occurrence of hypersensitivity reactions, all patients should receive premedication (corticosteroids, histamine H₁– and H₂-receptor blockers).

During treatment, systematic monitoring of the peripheral blood count, blood pressure, and ECG is necessary. The next infusion of paclitaxel should not be administered until the neutrophil count exceeds 1500/mcL and the platelet count exceeds 100,000/mcL.

Vaccination of patients and their family members is not recommended.

When preparing and administering the paclitaxel solution, infusion systems made of PVC should not be used.

In experimental studies, it has been established that Paclitaxel has a mutagenic effect.

Drug Interactions

Laboratory studies in patients receiving sequential infusions of paclitaxel and cisplatin revealed a more pronounced myelotoxic effect when paclitaxel was administered after cisplatin; in this case, the mean values of the total clearance of paclitaxel decreased by approximately 20%.

Prior administration of cimetidine does not affect the mean values of the total clearance of paclitaxel.

Based on data obtained in vivo and in vitro, it can be assumed that patients receiving ketoconazole experience suppression of paclitaxel metabolism.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.