Absorption: IV administration results in complete bioavailability; 89% absorbed following subcutaneous administration; bioavailability of oral administration 11% relative to subcutaneous administration.
Distribution: Widely distributed to extravascular tissues.
Metabolism/Excretion: 85% excreted in urine; some hepatic metabolism may occur. Less than 1% fecal elimination.
Half-life: IV or subcut 4 hr; Oral 30 min.
Contraindicated in:
Use Cautiously in:
Derm: acute febrile neutrophilic dermatosis, ecchymosis.
F and E: hypokalemia.
GI: abdominal pain, constipation, ↓appetite, diarrhea, nausea, vomiting, HEPATOTOXICITY.
GU: ↓fertility, NEPHROTOXICITY, renal tubular acidosis.
Hemat: anemia, neutropenia, thrombocytopenia.
Local: injection site erythema.
MS: arthralgia.
Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), TUMOR LYSIS SYNDROME.
Myelodysplastic Syndromes
Juvenile Myelomonocytic Leukemia
1 yr and
10 kg): 75 mg/m2once daily on Days 17 of each 28day cycle. Continue for at least 3 cycles and a maximum of 6 cycles (as long as patient continues to benefit).
1 mo-<1 yr or <10 kg): 2.5 mg/kg once daily on Days 17 of each 28day cycle. Continue for at least 3 cycles and a maximum of 6 cycles (as long as patient continues to benefit).Acute Myeloid Leukemia
(Generic available)
Grade 1. If symptoms reoccur, hold dose until resolved to
Grade 1. Resume at reduced dose of 200 mg. If a symptoms continue after dose reduction, reduce the treatment duration by 7 days. If the symptoms continue or reoccur after dose and schedule reduction, discontinue azacitidine.
0.5 x 109/L. If neutrophils <1 x 109/L and 1st occurrence, Hold therapy until neutrophils
1 x 109/L. If occurs in 2 consecutive cycles, Hold therapy until neutrophils
1 x 109/L, then resume at reduced dose of 200 mg. If febrile neutropenia continues after dose reduction, reduce treatment duration by 7 days. If febrile neutropenia reoccurs after dose and schedule reduction, discontinue azacitabine. If platelets <50 x 109/L and 1st occurrence, Hold therapy until platelets
50 x 109/L. If occurs in 2 consecutive cycles,Hold therapy until platelets
50 x 109/L, then resume at reduced dose of 200 mg. If thrombocytopenia with bleeding continues after dose reduction, reduce the treatment duration by 7 days. If thrombocytopenia with bleeding reoccurs after dose and schedule reduction, discontinue azacitabine. For IV or subcut doses:If baseline WBC
3 x 109/L, ANC
1.5 x 109/L, and platelets
75 x 109/L, then dose is adjusted based on nadir counts for each cycle. If ANC <0.5 x 109 and platelets <25 x 109, then ↓ dose by 50%. If ANC is 0.51.5 x 109 and platelets are 2550 x 109, then ↓ dose to 67% in next course. If ANC >1.5 x 109 and platelets >50 x 109, then 100% of dose can be given in subsequent cycle. If baseline WBC <3 x 109/L, ANC <1.5 x 109/L, or platelets <75 x 109/L, adjust dose based on nadir counts and bone marrow biopsy cellularity at time of nadir for each cycle. If WBC or platelet nadir decrease 5075% in counts from baseline and bone marrow biopsy cellularity is 3060% at time of nadir, give 100% of dose next course. If WBC or platelet nadir decrease 5075% in counts from baseline and bone marrow biopsy cellularity is 1530% at time of nadir, give 50% of dose next course. If WBC or platelet nadir decrease 5075% in counts from baseline and bone marrow biopsy cellularity is <15% at time of nadir, give 33% of dose next course. If WBC or platelet nadir decrease >75% in counts from baseline and bone marrow biopsy cellularity is 3060% at time of nadir, give 75% of dose next course. If WBC or platelet nadir decrease >75% in counts from baseline and bone marrow biopsy cellularity is 1530% at time of nadir, give 50% of dose next course. If WBC or platelet nadir decrease >75% in counts from baseline and bone marrow biopsy cellularity is <15% at time of nadir, give 33% of dose next course. Administer next course 28 days after start of preceding course, if both WBC and platelet counts are >25% above nadir and rising. If >25% ↑ above nadir is not seen by day 28, reassess counts every 7 days. If a 25% increase is not seen by day 42, reduce scheduled dose by 50%.IV Administration:
NDC Code*