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All about: Azacitidine

Big Image Pronouncation: (AZE-ah-SIGH-tih-deen)
Class: DNA demethylation agent

Trade Names:
- Powder for injection, lyophilized 100 mg

Mechanism of Action


Believed to cause hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in bone marrow.



Rapidly absorbed after subcutaneous administration; C max 750 ng/mL in 0.5 h. Subcutaneous bioavailability 89% compared with IV administration.


Mean Vd is 76 L.


Mean apparent subcutaneous Cl is 167 L/h and mean t ½ is 41 min. After subcutaneous administration, mean urinary excretion 50%. Mean elimination t ½ 4 h.

Indications and Usage

Treatment of myelodysplastic syndrome subtypes: refractory anemia or refractory anemia with ringed sideroblasts (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia.


Advanced malignant hepatic tumors; hypersensitivity to mannitol or azacitidine.

Dosage and Administration


Subcutaneous Recommended starting dose is 75 mg/m 2 daily for 7 days, every 4 wk. Premedicate patient for nausea and vomiting. Increase dose to 100 mg/m 2 if no beneficial effect seen after 2 treatment cycles and if no toxicity other than nausea and vomiting occur. Recommended that patients be treated for a minimum of 4 cycles. Treatment may be continued as long as patient continues to benefit.

Dosage Adjustments Based on Hematologic Laboratory Values

Subcutaneous For patients with WBC at least 3 × 10 9 /L, ANC at least 1.5 × 10 9 /L and platelets at least 75 × 10 9 /L at the start of treatment, adjust dose based on nadir counts for any given cycle as follows:

  • ANC less than 0.5 × 10 9 /L, platelets less than 25 × 10 9 /L administer 50% of dose in next course.
  • ANC 0.5 to 1.5 × 10 9 /L, platelets 25 to 50 × 10 9 /L administer 67% of dose in next course.
  • ANC greater than 1.5 × 10 9 /L, platelets greater than 50 × 10 9 /L administer 100% of dose in next course.
  • For patients with WBC less than 3 × 10 9 /L, ANC less than 1.5 × 10 9 /L, or platelets less than 75 × 10 9 /L at the start of treatment, base dose adjustments on nadir counts and bone marrow biopsy cellularity at time of nadir as follows, unless there is clear improvement in differentiation (percentage of mature granulocytes is higher and ANC is higher than at onset of course) at time of next cycle, in which case continue the dose of the current treatment.
  • WBC or platelet nadir percent decrease in counts from baseline is 50% to 75% and bone marrow biopsy cellularity at time of nadir is 30% to 60%, give 100% of dose in next course.
  • WBC or platelet nadir percent decrease in counts from baseline is 50% to 75% and bone marrow biopsy cellularity at time of nadir is 15% to 30%, give 50% of dose in next course.
  • WBC or platelet nadir percent decrease in counts from baseline is 50% to 75% and bone marrow biopsy cellularity at time of nadir is less than 15%, give 33% of dose in next course.
  • WBC or platelet nadir percent decrease in counts from baseline is greater than 75% and bone marrow biopsy cellularity at time of nadir is 30% to 60% give 75% of dose in next course.
  • WBC or platelet nadir percent decrease in counts from baseline is greater than 75% and bone marrow biopsy cellularity at time of nadir is 15% to 30% give 50% of dose in next course.
  • WBC or platelet nadir percent decrease in counts from baseline is greater than 75% and bone marrow biopsy cellularity at time of nadir is less than 15% give 33% of dose in next course.
  • If a nadir as defined above has occurred, give the next course of treatment 28 days after the start of the preceding course provided that both WBC and platelet counts are greater than 25% above the nadir and rising. If a greater than 25% increase above nadir is not seen by day 28, reassess counts every 7 days. If a 25% increase is not seen by day 42, treat the patient with 50% of the scheduled dose.
Dosage Adjustments Based on Renal Function and Serum Electrolytes

Subcutaneous If unexplained reductions in serum bicarbonate levels to less than 20 mEq/L occur, reduce dosage 50% on next course. If unexplained elevations of BUN or serum creatinine occur, delay the next cycle until values return to normal or baseline and reduce dose 50% on next treatment course.

General Advice

  • Reconstitute powder with 4 mL sterile water for injection. Inject diluent slowly into vial then invert vial 2 to 3 times and gently rotate until a uniform suspension is obtained. Resulting suspension contains 25 mg/mL of azacitidine.
  • Draw contents into syringe. Divide doses greater than 4 mL equally into 2 syringes.
  • Immediately prior to administration resuspend the contents by inverting syringe 2 to 3 times and gently rolling the syringe between the palms for 30 sec.
  • Rotate sites for each injection (eg, thigh, abdomen, upper arm). Give new injections at least 1 inch from an old site and never into areas where the site is tender, bruised, red, or hard.
  • Discard unused portions of vial. Do not save any unused portions for future use.


Store unopened vials at controlled room temperature (59° to 86°F). If not used immediately, reconstituted suspension may be held for up to 1 h at room temperature (77°F) but must be administered within 1 h of reconstitution. The reconstituted suspension may be refrigerated immediately and held in refrigerator (36° to 46°F) for up to 8 h. After removal from refrigerator, the suspension may be allowed to equilibrate to room temperature for up to 30 min.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Cardiac murmur (10%); tachycardia (9%); hypotension (7%); atrial fibrillation, cardiac failure, CHF, cardio-pulmonary arrest, congestive cardiomyopathy, orthostatic hypotension (less than 5%).


Fatigue (36%); headache (22%); dizziness (19%); anxiety, aggravated fatigue, decreased appetite (13%); depression (12%); insomnia (11%); syncope (6%); hypoesthesia (5%); convulsions, intracranial hemorrhage, confusion (less than 5%).


Petechiae (24%); erythema (17%); pallor (16%); skin lesion (15%); rash (14%); pruritus (12%); increased sweating (11%); night sweats (9%); urticaria (6%); skin nodule, dry skin (5%); pyoderma gangrenosum, pruritic rash, skin induration (less than 5%).


Pharyngitis (20%); epistaxis (16%); nasopharyngitis (15%); rhinorrhea (10%); nasal congestion (6%).


Nausea (71%); vomiting (54%); diarrhea (36%); constipation (34%); anorexia (21%); abdominal pain (16%); abdominal tenderness (12%); upper abdominal pain (11%); gingival bleeding (10%); oral mucosal petechiae, stomatitis (8%); hemorrhoids, dyspepsia (7%); abdominal distention, loose stools (6%); mouth hemorrhage, dysphagia, tongue ulceration (5%); diverticulitis, GI hemorrhage, melena, perirectal abscess (less than 5%).


Dysuria, UTI (8%); hematuria, loin pain, renal failure (less than 5%).


Anemia (70%); thrombocytopenia (66%); leukopenia (48%); neutropenia (32%); febrile neutropenia (16%); lymphadenopathy (10%); hematoma (9%); aggravated anemia, postprocedural hemorrhage (6%); agranulocytosis, bone marrow depression, splenomegaly (less than 5%).


Cholecystitis (less than 5%).


Anaphylactic shock, hypersensitivity (less than 5%).

Lab Tests

Hypokalemia (13%).


Injection site erythema (35%); ecchymosis (31%); injection site pain (23%); injection site bruising or reaction (14%); injection site pruritus (7%); injection site granuloma, injection site pigmentation changes, injection site swelling (5%); catheter site hemorrhage (less than 5%).


Peripheral edema (19%); decreased weight (16%); pitting edema (15%); peripheral swelling (7%); dehydration (less than 5%).


Arthralgia (22%); myalgia (16%); muscle cramps (6%); aggravated bone pain, muscle weakness, neck pain (less than 5%).


Cough (30%); dyspnea (29%); exertional dyspnea (14%); upper respiratory tract infection (13%); productive cough, crackles in lung, pneumonia (11%); wheezing, rales (9%); decreased breath sounds, rales (8%); pleural effusion, rhonchi (6%); exacerbated dyspnea, atelectasis, sinusitis (5%); hemoptysis, lung infiltration, pneumonitis, respiratory distress (less than 5%).


Pyrexia (52%); weakness (29%); rigors (26%); limb pain (20%); back pain, contusion (19%); chest pain (16%); pain, malaise (11%); herpes simplex (9%); cellulitis, lethargy (8%); transfusion reaction (7%); chest wall pain; postprocedural pain (5%); general physical health deterioration, systemic inflammatory response syndrome, limb abscess, bacterial infection, blastomycosis, Klebsiella sepsis, streptococcal pharyngitis, Klebsiella pneumonia, sepsis, staphylococcal bacteremia, staphylococcal infection, toxoplasmosis, leukemia cutis, cholecystectomy (less than 5%).



Renal function

Ensure that renal function is evaluated prior to starting therapy and before each cycle. If unexplained elevations in BUN or creatinine occur, delay next cycle until values return to normal or baseline, and reduce the dose 50% on the next treatment course.


Category D .




Safety and efficacy not established.


Because elderly patients are more likely to have decreased renal function, it may be useful to monitor renal function.

Renal Function

Monitor for toxicity because azacitidine and its metabolites are primarily excreted by the kidneys.

Hepatic Function

Use with caution.


Neutropenia and thrombocytopenia may occur; monitor CBC.

Renal abnormalities

Elevated serum creatinine, renal failure, and death may occur.

Skin/Mucus membranes

Avoid contact with skin and mucus membranes. If accidental skin contact occurs, wash thoroughly with soap and water. If mucus membrane contact occurs, flush thoroughly with water. If eye contact occurs, flush eyes using standard irrigation techniques.

Use in men

Advise men to use effective contraception during treatment.



Bone marrow suppression, diarrhea, nausea, vomiting.

Patient Information

  • Advise patient that medication will be prepared and administered by health care providers in a health care setting.
  • Review dosing schedule with patient.
  • Advise patient to immediately report any of the following to health care provider: rash; hives; difficulty breathing; fever, chills, or other signs of infection; unusual bleeding or bruising; pain, redness, or swelling at injection site.
  • Advise patient to report any of the following to health care provider: persistent nausea, vomiting or appetite loss; persistent or worsening general body weakness.
  • Caution men to use effective contraception during therapy.
  • Caution women of childbearing potential to avoid becoming pregnant during therapy.

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