Dosing and uses of Vidaza (azacitidine)
Adult dosage forms and strengths
powder for injection
- 100mg/vial
Myelodysplastic Syndrome
75 mg/m² SC/IV qDay for 7 days every 4 weeks
May increase 100 mg/m² if no benefit after 2 treatment cycles and no toxicity (other than nausea/vomiting)
Monitor: CBC, hematologic responses, renal toxicity
Acute Myeloid Leukemia (Orphan)
Orphan indication sponsor
- Celgene Corporation; 9900 W. 109th Street, Suite 300; Overland Park, KS 66210
Pediatric dosage forms and strengths
powder for injection
- 100mg/vial
Myelodysplastic Syndrome (Off-label)
AML and ANLL: 250 mg/m² days 4 and 5 q4Weeks
AML induction: 300 mg/m² days 4 and 5 q4Weeks
Vidaza (azacitidine) adverse (side) effects
>10%
Nausea (70.5%)
Anemia (69.5%)
Thrombocytopenia (65.5%)
Pyrexia (51.8%)
Leukopenia (48.2%)
Diarrhea (36.4%)
Fatigue (35.9%)
Inj site erythema (35%)
Constipation (33.6%)
Neutropenia (32.3%)
Ecchymosis (30.5%)
Cough (29.5%)
Dyspnea (29.1%)
Weakness (29.1%)
Rigors (25.5%)
Petechiae (23.6%)
Injection site pain (22.7%)
Arthralgia (22.3%)
Headache (21.8%)
Anorexia (20.5%)
Pain in limb (20%)
Pharyngitis (20%)
Contusion (18.6%)
Edema peripheral (18.6%)
Back pain (18.6%)
Dizziness (18.6%)
Erythema (16.8%)
Chest pain (16.4%)
Epistaxis (16.4%)
Febrile neutropenia (16.4%)
Myalgia (15.9%)
Wt loss (15.9%)
Abd pain (15.5%)
Pallor (15.5%)
Nasopharyngitis (14.5%)
Pitting edema (14.5%)
Skin lesion (14.5%)
Dyspnea exertional (14.1%)
Inj site bruising (14.1%)
Rash (14.1%)
Anxiety (13.2%)
Appetite decr (12.7%)
Hypokalemia (12.7%)
Fatigue aggravated (12.7%)
URI (12.7%)
Pruritus (12.3%)
Abd tenderness (11.8%)
Depression (11.8%)
Productive cough (11.4%)
Abd pain upper (10.5%)
Crackles lung (10.5%)
Malaise (10.9%)
Pneumonia (10.9%)
Sweating incr (10.5%)
<10%
Cardiac murmur (10%)
Rhinorrhea (10%)
Gingival bleeding (9.5%)
Hematoma (8.6%)
Lethargy (7.7%)
Stomatitis (7.7%)
Hypotension (6.8%)
Injection site pruritus (6.8%)
Postprocedural hemorrhage (5.9%)
Urticaria (5.9%)
Loose stools (5.5%)
Chest wall pain (5%)
Dry skin (5%)
Injection site granuloma/swelling (5%)
Injection site pigmentation change (5%)
Mouth hemorrhage (5%)
Skin nodule (5%)
Postmarketing Reports
Interstitial lung disease
Tumor lysis syndrome
Injection site necrosis
Sweet’s syndrome (acute febrile neutrophilic dermatosis)
Necrotizing fasciitis (including fatal cases)
Warnings
Contraindications
Hypersensitivity to azacitidine or mannitoL
Advanced malignant hepatic tumors
Pregnancy/lactation
Cautions
Should not get pregnant/father children while on this drug
Renal tubular acidosis, and renal failure reported
Thrombocytopenia, neutropenia, and anemia are common occurrence
Hepatotoxicity reported
Thoroughly monitor hematologic responses
Pregnancy and lactation
Pregnancy category: d
Lactation: It is not known whether azacitidine or its metabolites are excreted in milk. Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into consideration the importance of the drug to the mother.
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Vidaza (azacitidine)
Mechanism of action
Hypomethylation of DNA and direct cytotoxic effect on abnl hematopoietic cells in bone marrow
Absorption
Bioavailability: 89%
Peak Plasma Concentration: 350-1150 ng/mL
Peak PlasmaTime: 0.5 hr
Distribution
Vd: 76 ± 26 L
Elimination
Half-Life: 4 hr
Excretion: primarily in urine (50-85%); feces (minor)
Administration
IV Incompatibilities
Dextrose 5% solns, Hespan, bicarbonate-containing solns
IV Preparation
Reconstitute each vial with 10 mL SWI.
Vigorously shake or roll the vial until all solids are dissolved & clear. The resulting solution will contain azacitidine 10 mg/mL.
Withdraw the required amount & inject into a 50-100 mL infusion bag of either NS or Lr
IV Administration
Infuse over 10-40 min
Infusion should be completed within 1 hr of reconstitution
SC Preparation
100 mg lyophilized powder reconstituted with 4 mL SWI
Contents of syringe must be resuspended by inverting syringe 2-3x & gently rolling syringe between palms for 30 sec immediately prior to administration
4 mL dose should be equally divided into 2 syringes & injected into 2 separate sites; rotate sites for each injection
May be stored for 1 hr at room temp & up to 8 hr in fridge
