PACLITAXEL ACTAVIS 100mg/16.67ml Infusion/Concentrate for

What is PACLITAXEL ACTAVIS 100mg/16.67ml

Paclitaxel ACTAVIS is a chemotherapy drug that belongs to the taxane class, a group of medications used primarily to treat a variety of cancers. It is available as an infusion concentrate in a 16.67ml glass vial, which contains 100mg of paclitaxel per vial. This medication is commonly prescribed for conditions such as ovarian cancer, breast cancer, non-small cell lung cancer, and Kaposi’s sarcoma, among others.

Paclitaxel works by interfering with the normal function of microtubules, structures essential for cell division. By stabilizing microtubules and preventing their disassembly, paclitaxel disrupts cell division and induces cell death, particularly in rapidly dividing cancer cells.

Indications for Paclitaxel ACTAVIS:

• Ovarian Cancer: Often used in combination with cisplatin or carboplatin.
• Breast Cancer: Frequently used alone or in combination with other chemotherapy agents.
• Non-Small Cell Lung Cancer: Given in combination with cisplatin for advanced-stage disease.
• Kaposi’s Sarcoma: Used to treat HIV-related advanced cases of Kaposi’s sarcoma.
• Head and Neck Cancers: It may also be used in combination with other therapies to treat advanced cancers of the head and neck.

How to use PACLITAXEL ACTAVIS 100mg/16.67ml

Paclitaxel ACTAVIS is administered as an intravenous (IV) infusion in a healthcare setting. This ensures the drug is given in the proper manner while allowing medical staff to monitor for side effects and adverse reactions.

Preparation and Administration:

• Form: It is a concentrated solution that must be diluted before use.
• Route of Administration: Intravenous (IV) infusion, typically over 3 hours, depending on the protocol prescribed.
• Preparation: Prior to administration, paclitaxel is diluted in an appropriate IV solution, such as 0.9% sodium chloride or 5% dextrose in water (D5W). The concentration of the diluted solution will depend on the specific dosage regimen.
• Premedication: Patients are often premedicated with corticosteroids (such as dexamethasone), antihistamines (e.g., diphenhydramine), and H2 blockers (e.g., ranitidine) to reduce the risk of hypersensitivity reactions during infusion.

Infusion Guidelines:

• The infusion should be given slowly, typically over a 3-hour period, to minimize the risk of hypersensitivity reactions and to ensure proper pharmacokinetics.
• Monitor for allergic reactions during the infusion, especially during the first dose. Emergency equipment should be available to handle potential reactions.

Post-Administration Monitoring:

• After infusion, patients should be monitored for adverse effects such as fever, chills, and signs of anaphylaxis or myelosuppression.
• Laboratory tests to assess blood cell counts (e.g., white blood cells, platelets) are essential to detect myelosuppression early.

Mode of Action PACLITAXEL ACTAVIS 100mg/16.67ml

Paclitaxel ACTAVIS functions by disrupting the normal dynamics of microtubules during cell division. Microtubules are dynamic structures that help in the separation of chromosomes during mitosis (cell division), which is a critical process in cell proliferation. By interfering with this process, paclitaxel effectively halts the growth and spread of cancer cells.

Mechanism of Action:

• Microtubule Stabilization: Paclitaxel binds to β-tubulin subunits of microtubules, promoting their stabilization. This prevents microtubules from disassembling, a necessary step for normal mitosis.
• Inhibition of Mitotic Spindle Formation: The stabilized microtubules prevent the proper formation of the mitotic spindle. This inhibits the ability of cells to undergo proper mitosis, resulting in cell cycle arrest in the G2/M phase.
• Induction of Apoptosis: The prolonged cell cycle arrest triggers cellular stress responses, leading to apoptosis (programmed cell death). This is particularly effective against cancer cells, which are often rapidly dividing.

Cancer Cell Targeting:

• Because cancer cells typically divide more quickly than normal cells, they are more susceptible to paclitaxel-induced mitotic disruption.
• As paclitaxel targets dividing cells, its effect is most prominent in tissues with a high proliferation rate, such as tumors.

PACLITAXEL ACTAVIS 100mg/16.67ml Interactions PACLITAXEL ACTAVIS 100mg/16.67ml

Paclitaxel can interact with a variety of medications, which may either increase its toxicity or reduce its effectiveness. Understanding these interactions is critical to optimizing therapy and preventing adverse effects.

Common Drug Interactions:

• CYP3A4 Inhibitors: Medications that inhibit the CYP3A4 enzyme (e.g., ketoconazole, ritonavir, clarithromycin) may increase paclitaxel blood levels, leading to heightened toxicity, particularly neutropenia and peripheral neuropathy.
• CYP3A4 Inducers: Drugs like rifampin, phenytoin, and carbamazepine can accelerate the metabolism of paclitaxel, reducing its effectiveness.
• Myelosuppressive Drugs: Concomitant use of paclitaxel with other chemotherapy agents that suppress bone marrow function (e.g., cisplatin, cyclophosphamide) increases the risk of severe myelosuppression.
• Anticoagulants: Paclitaxel may increase the risk of bleeding when used with anticoagulants like warfarin and other blood thinners. Monitoring of INR levels is essential in such cases.
• Grapefruit Juice: Grapefruit juice inhibits CYP3A4, which may lead to increased paclitaxel levels, heightening the risk of side effects such as neutropenia.

Other Considerations:

• Herbal Supplements: Some herbal products, such as St. John’s Wort, may alter paclitaxel metabolism, either by inducing or inhibiting CYP enzymes.
• Monitoring Drug Interactions: Careful monitoring is advised when starting or discontinuing drugs that affect paclitaxel metabolism, adjusting the dose as necessary.

Dosage of PACLITAXEL ACTAVIS 100mg/16.67ml

The dosage of Paclitaxel ACTAVIS varies depending on the type of cancer, the combination therapy used, and the patient's overall health. The standard dosage is calculated based on the patient's body surface area (BSA) or weight, and the medication is typically given every three weeks, but the exact schedule depends on the regimen.

Standard Dosage Guidelines:

• Ovarian Cancer: The recommended dose is 175 mg/m² administered as an IV infusion over 3 hours, usually every 3 weeks, often in combination with carboplatin.
• Breast Cancer: A typical dose is 175 mg/m² every 3 weeks, often in combination with doxorubicin or cyclophosphamide.
• Non-Small Cell Lung Cancer (NSCLC): Paclitaxel is usually administered at 200 mg/m² every 3 weeks, in combination with cisplatin.
• Kaposi’s Sarcoma: A lower dose of 100 mg/m² may be given weekly in patients with HIV-related Kaposi’s sarcoma.

Adjustments for Toxicity:

• If significant side effects occur, such as neutropenia or peripheral neuropathy, dose reduction or delay may be necessary.
• In patients with liver dysfunction, dose adjustments may be required, based on liver function tests.

Possible side effects of PACLITAXEL ACTAVIS 100mg/16.67ml

Paclitaxel ACTAVIS can cause a range of side effects, varying from mild to severe, depending on the individual patient's response. Below are some of the most common and serious side effects associated with this medication.

Common Side Effects:

• Myelosuppression: A decrease in white blood cells (leukopenia), red blood cells (anemia), and platelets (thrombocytopenia) is common, which can lead to increased risk of infections, bleeding, and fatigue.
• Neuropathy: Peripheral neuropathy, manifesting as tingling, numbness, and pain in the extremities, is common, especially with prolonged use.
• Gastrointestinal Disturbances: Nausea, vomiting, diarrhea, and mucositis (inflammation of the mucous membranes) are also reported.
• Fatigue: Many patients experience extreme tiredness and weakness, which can interfere with daily activities.

Serious Side Effects:

• Hypersensitivity Reactions: Severe reactions can include fever, chills, rash, and difficulty breathing, requiring immediate medical attention.
• Liver Toxicity: Monitoring liver function is critical, as paclitaxel can lead to elevated liver enzymes, potentially causing hepatotoxicity.
• Cardiovascular Effects: Paclitaxel may cause arrhythmias or hypotension, which can be life-threatening in some cases.
• Infections: The immunosuppressive effect of paclitaxel increases susceptibility to infections, and patients should be closely monitored for any signs of infection.

PACLITAXEL ACTAVIS 100mg/16.67ml Contraindications PACLITAXEL ACTAVIS 100mg/16.67ml

There are several contraindications and precautions that must be considered before administering Paclitaxel ACTAVIS to a patient.

Contraindications:

• Allergy to Paclitaxel or Polyoxyl 35 Castor Oil: Paclitaxel is formulated with polyoxyl 35 castor oil, which can cause severe allergic reactions in sensitive individuals.
• Severe Bone Marrow Suppression: Due to its cytotoxic nature, paclitaxel is contraindicated in patients with significant pre-existing bone marrow suppression.
• Liver Disease: Paclitaxel is metabolized in the liver; thus, it should not be used in patients with severe liver dysfunction.
• Pregnancy: As a category D drug, paclitaxel is contraindicated during pregnancy due to potential teratogenic effects.
• Breastfeeding: Paclitaxel should not be used in breastfeeding women, as it is excreted in breast milk and could harm a nursing infant.

Storage of PACLITAXEL ACTAVIS 100mg/16.67ml

Paclitaxel ACTAVIS should be stored properly to maintain its potency and avoid degradation. Following storage guidelines ensures the drug remains safe for use.

Storage Recommendations:

• Unopened Vials: Store unopened vials at 2°C to 8°C (36°F to 46°F). Do not freeze.
• Diluted Solutions: After dilution, the solution should be used within 24 hours when stored at room temperature. If refrigerated, it should be used within 24 hours.
• Avoid Light: Keep paclitaxel away from light, as exposure can reduce its effectiveness.
• Safety: Store in a safe place, away from children and pets, to prevent accidental misuse.