Imatinib mesylate
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DRUG STATUS
Approvals
US(FDA), UK(BNF)
Essential Medicine
YES
Teratogenicity
Definite
Pharmaceutical Class
N/A
Imatinib mesylate
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Click HereSummary
Imatinib mesylate is primarily used to treat chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GISTs). It is also effective in treating acute lymphoblastic leukemia (ALL) and some rare blood and skin cancers.
Imatinib mesylate is a tyrosine kinase inhibitor. It works by blocking specific proteins (BCR-ABL, c-KIT) that promote the growth of cancer cells. This targeted approach slows down the progression of the disease and improves patient survival.
For CML, adults usually take 400-600 mg once daily. For GISTs, the usual dose is 400 mg daily, which can be increased to 800 mg if needed. For children, the dosage is based on body weight (260-340 mg/m daily). Always follow your doctor's prescription.
Common side effects include nausea, fatigue, diarrhea, muscle cramps, and fluid retention. Serious risks include liver toxicity, heart failure, and severe bleeding. Rare but severe effects include bone marrow suppression and lung complications.
People with severe liver disease, heart failure, or a history of severe allergic reactions should avoid Imatinib. Pregnant women should not take it due to potential harm to the fetus. It should be used cautiously in people with kidney issues or severe infections.
Indications and Purpose
What is Imatinib mesylate used for?
Imatinib is mainly used for chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GISTs). It is also effective in acute lymphoblastic leukemia (ALL) and some rare blood and skin cancers. Its targeted mechanism makes it a first-line treatment for these conditions.
How does Imatinib mesylate work?
Imatinib blocks BCR-ABL, c-KIT, and PDGFR proteins, which drive cancer growth. By inhibiting these enzymes, it stops abnormal cell proliferation and prevents tumor growth in leukemia and GISTs. This selective action makes it an effective targeted therapy.
Is Imatinib mesylate effective?
Yes, clinical studies show Imatinib significantly improves survival rates in CML and GIST patients. It has transformed CML into a manageable chronic disease, increasing the 5-year survival rate to over 90%. Its effectiveness depends on patient adherence and disease progression.
How does one know if Imatinib mesylate is working?
Doctors monitor response through blood tests (CBC, BCR-ABL levels) and imaging (CT/MRI scans for tumors). A decline in leukemic cells in CML or tumor shrinkage in GISTs indicates effectiveness. Patients may also feel better with fewer symptoms.
Directions for Use
What is the usual dose of Imatinib mesylate?
For CML, the usual dose for adults is 400–600 mg once daily. In GISTs, the dose is usually 400 mg daily, which may be increased to 800 mg if needed. For children, the dosage is based on body weight (260–340 mg/m² daily). Always follow your doctor's prescription.
How do I take Imatinib mesylate?
Take Imatinib with food and a full glass of water to reduce stomach upset. Swallow the tablets whole, without crushing or chewing. Avoid grapefruit and grapefruit juice, as they may increase drug levels in the blood and cause side effects.
For how long do I take Imatinib mesylate?
Treatment duration varies depending on the condition. For CML, patients often take Imatinib long-term or even lifelong. In GISTs, treatment continues as long as the disease is controlled. Always follow your doctor’s guidance, and do not stop the medicine without consulting them.
How long does it take for Imatinib mesylate to start working?
Imatinib starts working within a few weeks, but noticeable clinical benefits may take several months. In CML, blood counts may improve within 1–3 months, while tumor shrinkage in GISTs can take a few months. Regular monitoring is necessary to assess response.
How should I store Imatinib mesylate?
Store Imatinib at room temperature (20–25°C), away from moisture and direct sunlight. Keep it in its original container, tightly closed, and out of reach of children. Do not store in the bathroom.
Warnings and Precautions
Who should avoid taking Imatinib mesylate?
People with severe liver disease, heart failure, or a history of severe allergic reactions should avoid Imatinib. Pregnant women should not take it due to potential fetal harm. It should be used cautiously in people with kidney issues or severe infections.
Can I take Imatinib mesylate with other prescription drugs?
Imatinib interacts with blood thinners, certain antibiotics, antifungals, seizure medications, and heart drugs. It can alter their effectiveness or increase side effects. Inform your doctor about all medications to prevent harmful interactions.
Can I take Imatinib mesylate with vitamins or supplements?
Some vitamins and herbal supplements, especially St. John’s Wort, grapefruit, and vitamin C in high doses, may interfere with Imatinib’s effectiveness. Always consult your doctor before taking supplements, as some may increase toxicity or reduce drug levels.
Can Imatinib mesylate be taken safely while pregnant?
No, Imatinib is not safe during pregnancy, as it can cause birth defects and fetal harm. Women of childbearing age should use effective contraception. If pregnancy occurs, alternative treatments should be considered.
Can Imatinib mesylate be taken safely while breastfeeding?
No, Imatinib passes into breast milk and may harm the baby. Breastfeeding is not recommended during treatment. Mothers should switch to formula feeding while on this medication.
Is Imatinib mesylate safe for the elderly?
Yes, but older adults may be more prone to fluid retention, heart problems, and liver toxicity. They should be closely monitored for side effects, and dose adjustments may be needed.
Is it safe to exercise while taking Imatinib mesylate?
Yes, but moderate exercise is recommended. Some patients experience fatigue, muscle cramps, or shortness of breath, so listen to your body and avoid overexertion. Low-impact activities like walking, yoga, or light strength training can help maintain strength and energy. If you feel too weak or dizzy, consult your doctor before continuing intense workouts.
Is it safe to drink alcohol while taking Imatinib mesylate?
It is not recommended to drink alcohol while taking Imatinib, as it can increase liver toxicity and worsen side effects like nausea, dizziness, and fatigue. If you do drink, limit intake and monitor for any worsening symptoms. Always consult your doctor before consuming alcohol.
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