Imatinib

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Generic Name of Imatinib - Learn More

Imatinib

Imatinib Precaution - What You Need to Know

- Pregnancy: Imatinib is classified as a Category D drug in pregnancy, indicating potential harm to a fetus. It should only be used during pregnancy when no alternative therapy is available, and the benefits outweigh the risks. Women should avoid becoming pregnant while using Imatinib, and appropriate contraception should be employed.
- Breastfeeding: It is not recommended to breastfeed while taking Imatinib due to the potential for excretion into breast milk and harm to the infant.
- Hepatic Impairment: Imatinib is extensively metabolized by the liver, and its use in patients with hepatic impairment requires caution. Dose reductions may be necessary for patients with severe liver dysfunction.
- Cardiovascular Concerns: Imatinib has been associated with fluid retention, which can lead to edema, weight gain, or more severe conditions like heart failure. Patients with pre-existing heart conditions should be monitored for these complications.
- Bone Marrow Suppression: Imatinib can cause bone marrow suppression, leading to neutropenia, thrombocytopenia, or anemia. Regular blood counts should be performed to monitor for these effects.
- Monitoring Parameters: Liver function tests, blood counts, and heart function (particularly in those with cardiovascular risk factors) should be monitored during treatment.
- Misuse or Dependency: Imatinib is not associated with misuse or dependency, but adherence to the prescribed regimen is critical to achieving its therapeutic effect.

Imatinib Indication - Uses and Benefits

- Primary Indication: Imatinib is used primarily to treat cancers associated with abnormal tyrosine kinase activity. Its primary indications include:
- Chronic Myelogenous Leukemia (CML): Imatinib is approved for the treatment of Philadelphia chromosome-positive CML, where it targets the BCR-ABL fusion protein, a hallmark of this leukemia.
- Gastrointestinal Stromal Tumors (GISTs): It is also indicated for the treatment of unresectable or metastatic GISTs, which often involve mutations in the KIT gene, a receptor tyrosine kinase.
- Other cancers: Imatinib is used in the treatment of systemic mastocytosis and hypereosinophilic syndrome, both of which involve abnormal tyrosine kinase signaling.
- Off-label Uses:
- Allergic Asthma: Some studies have explored the use of Imatinib in severe asthma as a modulator of IgE production.
- Myelodysplastic Syndromes: Imatinib has been studied for its potential benefit in some cases of myelodysplastic syndromes, though this is still considered an off-label use.
- Evidence-Based Context: Imatinib’s approval is supported by clinical trials showing significant improvement in overall survival and progression-free survival in CML patients. Guidelines such as those from the National Comprehensive Cancer Network (NCCN) recommend Imatinib as first-line therapy for CML and GISTs.

Imatinib Contraindications - Important Warnings

- Hypersensitivity: Imatinib is contraindicated in patients who have shown hypersensitivity or an allergic reaction to it.
- Severe Liver Impairment: In patients with severe hepatic impairment, Imatinib should be avoided unless absolutely necessary, as the drug is metabolized by the liver, and compromised function may lead to toxic drug levels.
- Pregnancy and Breastfeeding: Imatinib is contraindicated during pregnancy and breastfeeding due to potential harm to the fetus and infant.
- Age Considerations: There is limited data on the use of Imatinib in children younger than 2 years, and caution should be used in pediatric patients.
- Rationale: These contraindications exist due to the potential for severe side effects such as liver toxicity, hypersensitivity reactions, and teratogenic effects. If the drug is deemed necessary for a pregnant patient, a specialist in oncology and obstetrics should be consulted.

Imatinib Side Effects - What to Expect

- Common Side Effects:
- Edema and Fluid Retention: Swelling, especially around the eyes, legs, and abdomen, is a common side effect.
- Gastrointestinal Issues: Nausea, diarrhea, and abdominal discomfort are frequently reported during treatment with Imatinib.
- Fatigue: Patients may experience varying degrees of tiredness or lack of energy during therapy.
- Skin Rash: A rash, particularly on the trunk or face, can occur.
- Serious Side Effects:
- Liver Toxicity: Elevations in liver enzymes (AST, ALT) may occur, which can progress to more severe liver damage.
- Cardiovascular Problems: Imatinib may cause heart failure or arrhythmias, particularly in patients with pre-existing heart conditions.
- Bone Marrow Suppression: Severe neutropenia, thrombocytopenia, or anemia can occur, increasing the risk of infections, bleeding, or anemia.
- Gastrointestinal Bleeding: Serious bleeding complications, including gastrointestinal bleeding, can occur, particularly in patients with pre-existing gastrointestinal conditions.
- Long-Term Effects: Long-term use of Imatinib may result in resistance or disease relapse, particularly in patients with CML. Monitoring and adjustments are necessary for optimal treatment outcomes.
- Management: Regular monitoring of liver function, blood counts, and cardiac status is essential. Fluid retention may be managed by diuretics, and rashes may be treated with antihistamines or topical steroids. Severe reactions require dose reduction or discontinuation.

Imatinib Pregnancy Category ID - Safety Information

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Imatinib Mode of Action - How It Works

- Mechanism of Action: Imatinib is a targeted therapy that works by inhibiting specific tyrosine kinases, including the BCR-ABL fusion protein in CML. The BCR-ABL protein results from a genetic mutation called the Philadelphia chromosome, which is present in most CML patients. This protein continuously signals cancerous cell division. Imatinib binds to the ATP-binding site of the BCR-ABL kinase, preventing the phosphorylation of substrates and blocking downstream signaling that drives cell proliferation.
- Pharmacodynamics: Imatinib's action selectively targets the abnormal tyrosine kinase activity that drives the growth of leukemia cells, making it highly effective in CML. It also inhibits other kinases such as c-KIT, which is involved in GISTs, and PDGFR (platelet-derived growth factor receptor), which contributes to other cancers.
- Pharmacokinetics: Imatinib is rapidly absorbed after oral administration, with peak plasma concentrations typically reached within 2-4 hours. It is extensively metabolized in the liver by CYP3A4. The drug has a long half-life of 18-40 hours, allowing for once-daily dosing. Imatinib is excreted mainly through feces and a smaller amount via urine.
- Therapeutic Benefit: Imatinib’s selective inhibition of tyrosine kinases is beneficial because it targets the cancerous cells while sparing most normal cells, minimizing side effects compared to traditional chemotherapy.

Imatinib Drug Interactions - What to Avoid

- Drug-Drug Interactions:
- CYP3A4 Inhibitors/Inducers: Imatinib is metabolized by the CYP3A4 enzyme, and drugs that inhibit or induce this enzyme may significantly affect Imatinib levels. For example, ketoconazole (a strong CYP3A4 inhibitor) can increase Imatinib levels, while drugs like rifampin (a CYP3A4 inducer) may decrease its efficacy.
- Warfarin: Imatinib may alter the metabolism of warfarin, increasing the risk of bleeding. INR should be monitored closely if these drugs are used together.
- Acid-Reducing Agents: Drugs that alter stomach acidity, such as proton pump inhibitors, may reduce the absorption of Imatinib, decreasing its effectiveness.
- Food and Alcohol: While food does not significantly alter the absorption of Imatinib, alcohol consumption should be avoided as it may exacerbate side effects like liver toxicity.
- Clinical Recommendations: If Imatinib is prescribed with a CYP3A4 inhibitor or inducer, the dose may need to be adjusted. Patients should be monitored for signs of toxicity or lack of efficacy. Careful monitoring of INR is advised for patients on warfarin.

Imatinib Adult Dose - Recommended Dosage

- Standard Dosing: For adults with chronic phase CML or GISTs, the typical dose of Imatinib is 400 mg daily. In cases of accelerated phase or blast crisis CML, the dose may be increased to 600 mg daily.
- Administration: Imatinib is taken orally in tablet form, with or without food. Tablets should be swallowed whole with a glass of water to avoid any potential irritation.
- Dose Adjustments: In cases of hepatic impairment or severe side effects, the dose may be reduced. For patients with significant fluid retention or cardiovascular issues, the drug should be used cautiously and with careful monitoring.
- Maximum Allowable Dose: The maximum recommended dose of Imatinib for CML is generally 800 mg per day.
- Titration Schedules: The dose may be escalated gradually, particularly in more aggressive phases of CML, based on clinical response and side effect profile.

Imatinib Child Dose - Dosage for Children

- Pediatric Dosing: Imatinib is used in pediatric patients for CML and GISTs, with dosing generally based on body surface area (BSA). The typical dose for children is 340 mg/m² per day, with a maximum dose of 600 mg daily.
- Safety Considerations: Imatinib has shown efficacy in pediatric CML but may have more pronounced side effects in children, especially regarding growth and development.
- Efficacy and Monitoring: Regular monitoring of growth parameters, blood counts, and liver function is necessary in pediatric patients.
- Adjustments: Dosing adjustments may be needed based on individual tolerability, particularly if significant side effects such as liver toxicity or growth retardation occur. Regular follow-up is essential to assess long-term effects.

Imatinib Renal Dose - Dosage for Kidney Conditions

- Renal Impairment Considerations: Imatinib is not significantly cleared by the kidneys, but renal function should still be monitored during treatment, especially in patients with pre-existing kidney conditions.
- Dosage Adjustment: For patients with moderate to severe renal impairment, Imatinib may be used with caution. However, routine dose adjustments are generally not required unless significant renal dysfunction occurs.
- Monitoring: Kidney function should be regularly monitored during treatment, with particular attention to serum creatinine levels and urine output.
- Management of Toxicity: In cases of renal toxicity, Imatinib should be discontinued, and a dose reduction may be considered upon reintroduction if appropriate.