Nilotinib

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Generic Name of Nilotinib - Learn More

Nilotinib

Nilotinib Precaution - What You Need to Know

Before starting treatment with Nilotinib, it is crucial for patients to consult their healthcare provider, especially due to the potential risks and side effects associated with the drug. Key precautions include:
- Cardiovascular Disease: Nilotinib may cause QT interval prolongation, which can lead to serious arrhythmias (irregular heart rhythms), including torsades de pointes. Patients with pre-existing heart conditions, especially those with a history of QT prolongation, should be closely monitored during treatment.
- Liver Disease: Nilotinib is metabolized by the liver, so patients with hepatic impairment (e.g., cirrhosis or hepatitis) should use it cautiously. Liver function tests should be regularly monitored during therapy.
- Electrolyte Imbalances: Hypokalemia (low potassium) and hypomagnesemia (low magnesium) can exacerbate QT prolongation. Electrolyte levels should be corrected before starting Nilotinib, and they should be monitored during treatment.
- Pancreatitis Risk: Patients with a history of pancreatitis or those at higher risk (e.g., individuals with high alcohol intake or gallstones) should be carefully monitored for signs of pancreatitis (e.g., abdominal pain, nausea, vomiting).
- Pregnancy and Lactation: Nilotinib is classified as Category D for pregnancy, meaning it can harm the developing fetus and should only be used if the benefits outweigh the risks. It is unknown whether Nilotinib passes into breast milk, so breastfeeding should be avoided during treatment.
- Risk of Tumor Lysis Syndrome: In patients with high tumor burden, especially those with chronic myelogenous leukemia (CML), there is an increased risk of tumor lysis syndrome, a potentially life-threatening condition caused by the rapid breakdown of cancer cells. This should be monitored in patients starting therapy.

Nilotinib Indication - Uses and Benefits

Nilotinib is primarily indicated for the treatment of chronic myelogenous leukemia (CML) in chronic phase and accelerated phase, particularly in patients who are resistant or intolerant to imatinib. It works by targeting and inhibiting the BCR-ABL fusion protein, which is a hallmark of CML. The therapeutic indications include:
- Chronic Phase CML: Nilotinib is used as first-line therapy for patients with chronic phase CML who are resistant to imatinib or have certain mutations in the BCR-ABL gene.
- Accelerated Phase CML: Nilotinib is used for patients with accelerated phase CML who are not responding to other treatments, such as imatinib.
- Philadelphia Chromosome-Positive CML: As a tyrosine kinase inhibitor, Nilotinib specifically targets and inhibits the BCR-ABL protein, helping to control cell division in Philadelphia chromosome-positive CML.

Nilotinib Contraindications - Important Warnings

Nilotinib should not be used in the following situations:
- Hypersensitivity: It is contraindicated in patients with known hypersensitivity to Nilotinib or any of its components.
- Severe QT Prolongation: In patients with a history of severe QT prolongation, Nilotinib should not be used due to its potential to exacerbate this condition and increase the risk of life-threatening arrhythmias.
- Concurrent Use with Strong CYP3A4 Inhibitors: Nilotinib is metabolized by the liver enzyme CYP3A4, and its use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) should be avoided due to the risk of elevated drug levels and increased side effects.
- Severe Liver Impairment: Nilotinib is contraindicated in patients with severe hepatic impairment due to its hepatic metabolism, which could result in increased drug concentrations and toxicity.
- Pregnancy: Nilotinib should not be used during pregnancy unless absolutely necessary, as it can cause fetal harm.

Nilotinib Side Effects - What to Expect

Nilotinib may cause a variety of side effects, ranging from mild to severe:
- Common Side Effects:
- Nausea and vomiting
- Headache
- Fatigue or tiredness
- Rash or itching
- Muscle pain or cramps
- Diarrhea
- Elevated liver enzymes (indicating liver stress or damage)

- Serious Side Effects:
- Cardiovascular issues, including QT prolongation, arrhythmias, and syncope (fainting)
- Pancreatitis, characterized by upper abdominal pain, nausea, and vomiting
- Hematologic effects, including anemia, thrombocytopenia (low platelets), or neutropenia (low white blood cells)
- Liver toxicity, manifested by jaundice (yellowing of the skin or eyes) or abnormal liver function tests
- Tumor lysis syndrome, a potentially life-threatening condition in patients with high tumor burden.

Nilotinib Pregnancy Category ID - Safety Information

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Nilotinib Mode of Action - How It Works

Nilotinib is a tyrosine kinase inhibitor that specifically targets the BCR-ABL fusion protein, which is produced by the Philadelphia chromosome in patients with CML. The BCR-ABL protein drives the uncontrolled growth of leukemia cells. By inhibiting the BCR-ABL tyrosine kinase, Nilotinib blocks the signaling pathways that promote cell proliferation and survival, leading to apoptosis (programmed cell death) of the cancerous cells. Unlike older drugs like imatinib, Nilotinib binds more tightly to the BCR-ABL protein and can overcome resistance mechanisms present in some patients with mutations in the BCR-ABL gene.

Nilotinib Drug Interactions - What to Avoid

Nilotinib can interact with a variety of medications and substances, which may affect its efficacy or lead to harmful side effects:
- CYP3A4 Inhibitors and Inducers: As Nilotinib is metabolized by the CYP3A4 enzyme, medications that inhibit or induce CYP3A4 can impact its blood levels. Strong inhibitors (e.g., ketoconazole, ritonavir) may increase Nilotinib levels, while CYP3A4 inducers (e.g., rifampin, carbamazepine) may decrease its effectiveness.
- Antacids: Use of antacids, particularly those containing magnesium or aluminum, may reduce the absorption of Nilotinib, decreasing its effectiveness.
- QT-prolonging Drugs: Concurrent use with other drugs that prolong the QT interval, such as amiodarone, erythromycin, or certain antipsychotics, can increase the risk of life-threatening arrhythmias.
- Warfarin: Nilotinib may interact with anticoagulants like warfarin, altering their blood-thinning effect and potentially increasing the risk of bleeding.
- Digoxin: Nilotinib may increase blood levels of digoxin, a drug used for heart failure, potentially leading to toxicity.

Nilotinib Adult Dose - Recommended Dosage

The typical dose of Nilotinib for adults is:
- For Chronic Phase CML: The recommended dose is 300 mg twice daily (total 600 mg/day). In some cases, the dose may be adjusted based on response and tolerance.
- For Accelerated Phase CML: The usual dose is 400 mg twice daily (total 800 mg/day).
- For Resistant CML: The dose is typically 400 mg twice daily.

Nilotinib Child Dose - Dosage for Children

Nilotinib is not typically recommended for use in children under the age of 18 for CML treatment unless under special circumstances and after careful evaluation by an oncologist. Dosing in pediatric patients should be determined by a healthcare professional based on the child's specific condition and response to treatment.

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Important Note:
Patients must consult their healthcare provider before initiating Nilotinib to ensure appropriate monitoring for side effects, drug interactions, and proper dosing. Nilotinib requires regular cardiac, liver, and hematologic assessments to ensure safe use and to minimize the risk of serious adverse events.

Nilotinib Renal Dose - Dosage for Kidney Conditions

Nilotinib is primarily metabolized by the liver, and there is limited evidence to suggest that it requires adjustment in patients with renal impairment. However, in patients with severe renal impairment (e.g., creatinine clearance < 30 mL/min), caution should be exercised, and treatment should be monitored closely due to potential accumulation of the drug or its metabolites.