Which drugs cause macrocytosis?

Updated: Dec 16, 2020
  • Author: Vincent E Herrin, MD, FACP; Chief Editor: Emmanuel C Besa, MD  more...
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Drug-induced macrocytosis is the most common cause in nonalcoholic patients. Usually, no associated anemia is present. The following categories of drugs are known to cause macrocytosis:

  • Folate antagonists (eg, methotrexate [12] )
  • Purine antagonists (eg, 6-mercaptopurine [6-MP])
  • Pyrimidine antagonists (eg, cytosine arabinoside [ara-C])
  • Alkylating agents (eg, cyclophosphamide)
  • Tyrosine kinase inhibitors (eg, sunitinib, and imatinib) [13]
  • Zidovudine (AZT)
  • Trimethoprim
  • Oral contraceptive pills
  • Phenytoin
  • Arsenic

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