Classifications: antineoplastic agent; antimetabolite (pyrimidine);
; antimetabolite
Prototype: Fluorouracil
Pregnancy Category: D


100 mg powder for injection


Causes changes in DNA in abnormal blood-forming cells in the bone marrow, resulting in restoration of normal function to tumor-suppressor genes that are responsible for regulating cell differentiation and growth.

Therapeutic Effect

Cytotoxic effects of azacitidine cause the death of rapidly dividing cancer cells that are no longer responsive to normal growth control mechanisms.


Treatment of myelodysplastic syndrome, specifically refractory anemia.

Unlabeled Uses

Refractory acute lymphocytic and myelogenous leukemia


Hypersensitivity to azacitidine or mannitol; advanced malignant hepatic tumors, myelodysplastic syndrome with hepatic impairment; vaccination; active infection; dental work; intramuscular injections, if platelets <50,000 mm3; pregnancy (category D), lactation. Safety and efficacy in children have not been established.

Cautious Use

Hypoalbuminemia (<3 g/dL), hepatic disease; elderly; bone marrow depression; dental disease; history of varicella zoster or other herpes infections; renal impairment, renal failure; older adults.

Route & Dosage

Myelodysplastic Syndrome
Adult : SC 75 mg/m2 once daily for 7 d every 4 wk; may increase to 100 mg/m2 if no beneficial response is seen after 2 treatment cycles and no toxicity other than nausea and vomiting has occurred

Renal Impairment
If unexplained elevations of BUN or creatinine occur, the next cycle should be delayed until the values return to normal or baseline, and the dose should be reduced by 50% in the next course.


  • Reconstitute by slowly injecting 4 mL of sterile water for injection into 100 mg vial to yield 25 mg/mL. Invert 2–3 times and gently rotate until a uniform suspension is achieved. The suspension will be cloudy. If not used immediately, see directions for storage.
  • Doses greater than 4 mL should be divided equally into 2 syringes and injected into 2 separate sites. Rotate sites for each injection (thigh, abdomen, or upper arm). Give subsequent injections at least 1 in from an old site and never into areas where the site is tender, bruised, red, or hard.
  • Storage: Reconstituted suspension may be kept in the vial or syringe. May refrigerate for up to 8 h. Before use, suspension may be kept at room temperature for up to 30 min. Resuspend by inverting the syringe 2–3 times and gently roll between the palms for 30 sec immediately before administration.

Adverse Effects (≥1%)

Body as a Whole: Fever, fatigue, malaise, weakness, asthenia, limb pain, back pain, lymphadenopathy, hematoma, night sweats, cellulitis, lethargy. CNS: Dizziness, headache, depression, syncope. CV: Chest pain, cardiac murmur, tachycardia, hypotension. GI: Nausea, vomiting, diarrhea, constipation, anorexia, weight loss, abdominal pain, stomatitis, dyspepsia. Hematologic: Anemia, thrombocytopenia, leukopenia, neutropenia, ecchymosis, febrile neutropenia. Metabolic: Peripheral edema. Musculoskeletal: Myalgia, arthralgia, muscle cramps. Respiratory: Cough, dyspnea, pharyngitis, nasopharyngitis, pneumonia, wheezing, pleural effusion, rhonchi. Skin: Injection site erythema, injection site reactions, rash, pruritus, sweating, urticaria. Urogenital: Dysuria, urinary tract infection.


Drug: anticoagulants, nsaids, antiplatelet agents may increase risk of bleeding; filgrastim, sargramostim may interfere with the efficacy of azacitidine if given within 24 h of azacitidine dose.


Peak: 30 min. Metabolism: In liver. Elimination: By kidneys. Half-Life: 4 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor for S&S of drug toxicity in those with renal insufficiency.
  • Lab tests: Obtain LFTs and serum creatinine before initiation of therapy; monitor CBC with differential before each treatment cycle and prn.
  • Withhold drug & notify physician for S&S of hepatic or renal insufficiency; lab values that indicate leukopenia, neutropenia, thrombocytopenia, or hepatic or renal insufficiency; or serum bicarbonate levels less than 20 mEq/L.

Patient & Family Education

  • Promptly report S&S of infection or indication of unusual bleeding tendencies (e.g., dark, tarry stools and easy bruising).
  • Women should avoid becoming pregnant and men should not father a child while taking this drug.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

© 2006-2023 Last Updated On: 01/24/2023 (0)
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