Imatinib Mesylate interactions

Food & lifestyle

• grapefruit juice

  Moderate

  Metabolism

  Coadministration of imatinib with strong CYP450 3A4 inhibitors such as grapefruit juice, may significantly increase the plasma concentrations of imatinib, a known substrate of CYP450 3A4. The proposed mechanism is inhibition of CYP450 3A4-mediated metabolism of imatinib by certain compounds present in grapefruits.

  What to do: Patients treated with imatinib should preferably avoid the consumption of grapefruit or grapefruit juice. If coadministration is unavoidable, monitor for prolonged and/or increased pharmacologic effects of imatinib, including edema, hematologic toxicity and immunosuppression.

  3 sources

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):
  2. Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
  3. Cerner Multum, Inc. "Australian Product Information." O 0

Conditions

Conditions in which Imatinib Mesylate needs care, as documented in this source.

• Bone Marrow Failure Disorders

  Moderate

  Thrombocytopenia, aplastic anemia, agranulocytosis and neutropenia occur with BCR-ABL tyrosine kinase inhibitors. Therapy with these drugs should be administered cautiously in patients with preexisting bone marrow suppression. A complete blood count should be performed every 1-2 weeks for the first month of therapy and then monthly thereafter, or as clinically indicated. To manage myelosuppression, withhold, reduce dose, or discontinue therapy as necessary.

  4 sources

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):
  2. "Product Information. Sprycel (dasatinib)." Bristol-Myers Squibb (2006):
  3. "Product Information. Tasigna (nilotinib)." Novartis Pharmaceuticals (2007):
  4. "Product Information. Bosulif (bosutinib)." Pfizer U.S. Pharmaceuticals Group (2012):

• Cardiovascular Diseases

  Moderate

  Cardiovascular events, including arterial vascular occlusive events, peripheral arterial occlusive events and ischemic cerebrovascular events have been reported in patients receiving tyrosine kinase inhibitors. If acute signs or symptoms of cardiovascular events occur, patients should seek immediate medical attention. The cardiovascular status and risk factors of patients should be evaluated prior to therapy and cardiovascular monitoring and management should take place during treatment.

  3 sources

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):
  2. "Product Information. Sprycel (dasatinib)." Bristol-Myers Squibb (2006):
  3. "Product Information. Tasigna (nilotinib)." Novartis Pharmaceuticals (2007):

• Gastrointestinal Diseases

  Moderate

  Imatinib has been sometimes associated with GI irritation, and it should be taken with food and a large glass of water to minimize this problem. There have been rare reports, including fatalities, of gastrointestinal perforation. Caution should be used in patients with history of GI disorders.

  1 source

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):

• Hepatic Insufficiency

  Moderate

  Patients with severe hepatic impairment tend to have higher exposure to both imatinib and its metabolite than patients with normal hepatic function, and dose might need to be adjusted accordingly. Additionally, there have been reports of hepatotoxicity both with short and long term use of imatinib. Liver function should be monitored before initiation of treatment and regularly during therapy. Dose reduction or interruption might be needed if laboratory abnormalities are found.

  1 source

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):

• Hypothyroidism

  Moderate

  Hypothyroidism cases have been reported in thyroidectomy patients undergoing levothyroxine replacement therapy during treatment with imatinib. Caution should be used in these patients and TSH levels should be monitored closely.

  1 source

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):

• Kidney Diseases

  Moderate

  The mean exposure to imatinib is increased in patients with renal impairment compared to those with normal renal function. Dose reductions are necessary in patients with moderate and severe renal impairment.

  1 source

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):

• Water-Electrolyte Imbalance

  Moderate

  Fluid retention occurs with BCR-ABL tyrosine kinase inhibitors therapy and may manifest as pericardial effusion, pleural effusion, pulmonary edema, and/or peripheral edema. Caution should be taken when using these drugs in patients with preexisting fluid retention or congestive heart failure. Monitor and manage patients using standards of care. Interrupt, reduce dose or discontinue therapy as necessary.

  4 sources

  1. "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals (2022):
  2. "Product Information. Sprycel (dasatinib)." Bristol-Myers Squibb (2006):
  3. "Product Information. Tasigna (nilotinib)." Novartis Pharmaceuticals (2007):
  4. "Product Information. Bosulif (bosutinib)." Pfizer U.S. Pharmaceuticals Group (2012):