Azacitidine
Generic Name: azacitidine
Brand Names:
Azacitidine
11 DESCRIPTION Azacitidine for injection contains azacitidine, which is a nucleoside metabolic inhibitor. Azacitidine is 4-amino-1-β-D-ribofuranosyl-s-triazin-2(1H)-one. The structural formula is as follows: The empirical formula is C 8 H 12 N 4 O 5 . The molecular weight is 244. Azacitidine is a white to off-white solid.
Overview
11 DESCRIPTION Azacitidine for injection contains azacitidine, which is a nucleoside metabolic inhibitor. Azacitidine is 4-amino-1-β-D-ribofuranosyl-s-triazin-2(1H)-one. The structural formula is as follows: The empirical formula is C 8 H 12 N 4 O 5 . The molecular weight is 244. Azacitidine is a white to off-white solid.
Uses
1 INDICATIONS AND USAGE Azacitidine for injection is a nucleoside metabolic inhibitor indicated for the treatment of: Adult patients with the following FAB myelodysplastic syndrome (MDS) subtypes: Refractory anemia (RA) or refractory anemia with ringed sideroblasts (RARS) (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts (RAEB), refractory anemia with excess blasts in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL).
Dosage
2 DOSAGE AND ADMINISTRATION Do not substitute azacitidine for injection for oral azacitidine. The indications and dosing regimen for azacitidine for injection differ from that of oral azacitidine ( 2.1 , 5.1 ). MDS: The recommended starting dosage for the first treatment cycle, for all patients regardless of baseline hematology values, is azacitidine for injection 75 mg/m2 daily for 7 days to be administered by subcutaneous injection or intravenous infusion. See full prescribing information for schedule for subsequent cycles. Premedicate for nausea and vomiting ( 2.2 ). Continue treatment as long as the patient continues to benefit; ( 2.3 ). Monitor all patients for hematologic response and for renal toxicity; delay or reduce dosage as appropriate ( 2.3 , 2.6 , 2.7 ).
Side Effects
6 ADVERSE REACTIONS The following adverse reactions are described in other labeling sections: Anemia, Neutropenia and Thrombocytopenia [see Warnings and Precautions ( 5.2 )] Hepatotoxicity in Patients with Severe Pre-existing Hepatic Impairment [see Warnings and Precautions ( 5.3 )] Renal Toxicity [see Warnings and Precautions ( 5.4 )] Tumor Lysis Syndrome [see Warnings and Precautions ( 5.5 )] Most common adverse reactions (>30%) in adult patients with MDS by subcutaneous route are: nausea, anemia, thrombocytopenia, vomiting, pyrexia, leukopenia, diarrhea, injection site erythema, constipation, neutropenia and ecchymosis. Most common adverse reactions by intravenous route also included petechiae, rigors, weakness and hypokalemia ( 6.1 ).
Warnings
5 WARNINGS AND PRECAUTIONS Risks of Substitution with Other Azacitidine Products: Do not substitute azacitidine for injection for oral azacitidine ( 2.1 , 5.1 ). Anemia, Neutropenia and Thrombocytopenia: Monitor complete blood counts (CBC) frequently ( 5.2 ). Hepatotoxicity: Patients with severe preexisting hepatic impairment are at higher risk for toxicity ( 5.3 ). Renal Toxicity: Monitor patients with renal impairment for toxicity since azacitidine and its metabolites are primarily excreted by the kidneys ( 5.4 ). Tumor Lysis Syndrome: Azacitidine may cause fatal or serious tumor lysis syndrome, including in patients with MDS. Assess baseline risk and monitor and treat as appropriate ( 5.5 ). Embryo-Fetal Toxicity: Azacitidine can cause fetal harm. 4 CONTRAINDICATIONS Advanced Malignant Hepatic Tumors ( 4.1 ). Hypersensitivity to Azacitidine or Mannitol ( 4.2 ). 4.1 Advanced Malignant Hepatic Tumors Azacitidine for injection is contraindicated in patients with advanced malignant hepatic tumors [see Warnings and Precautions ( 5.3 )] .
Pregnancy
8.1 Pregnancy Risk Summary Based on its mechanism of action and findings in animals, azacitidine can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no data on the use of azacitidine in pregnant women. Azacitidine was teratogenic and caused embryo-fetal lethality in animals at doses lower than the recommended human daily dose (see Data). Advise pregnant women of the potential risk to the fetus. The background rate of major birth defects and miscarriage is unknown for the indicated population.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied Azacitidine for injection is supplied as a lyophilized powder in 100 mg single-dose vials packaged in cartons of 1 vial (NDC 60505-6271-1). Storage Store unreconstituted vials at 25º C (77º F); excursions permitted to 15º to 30º C (59º to 86º F) [See USP Controlled Room Temperature] .
Frequently Asked Questions
What is Azacitidine used for?▼
1 INDICATIONS AND USAGE Azacitidine for injection is a nucleoside metabolic inhibitor indicated for the treatment of: Adult patients with the following FAB myelodysplastic syndrome (MDS) subtypes: Refractory anemia (RA) or refractory anemia with ringed sideroblasts (RARS) (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts (RAEB), refractory anemia with excess blasts in transformation (RAEB-T), and chronic myelomonocytic leukemia (CMMoL).
What are the side effects of Azacitidine?▼
6 ADVERSE REACTIONS The following adverse reactions are described in other labeling sections: Anemia, Neutropenia and Thrombocytopenia [see Warnings and Precautions ( 5.2 )] Hepatotoxicity in Patients with Severe Pre-existing Hepatic Impairment [see Warnings and Precautions ( 5.3 )] Renal Toxicity [see Warnings and Precautions ( 5.4 )] Tumor Lysis Syndrome [see Warnings and Precautions ( 5.5 )] Most common adverse reactions (>30%) in adult patients with MDS by subcutaneous route are: nausea, anemia, thrombocytopenia, vomiting, pyrexia, leukopenia, diarrhea, injection site erythema, constipation, neutropenia and ecchymosis. Most common adverse reactions by intravenous route also included petechiae, rigors, weakness and hypokalemia ( 6.1 ).
Can I take Azacitidine during pregnancy?▼
8.1 Pregnancy Risk Summary Based on its mechanism of action and findings in animals, azacitidine can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no data on the use of azacitidine in pregnant women. Azacitidine was teratogenic and caused embryo-fetal lethality in animals at doses lower than the recommended human daily dose (see Data). Advise pregnant women of the potential risk to the fetus. The background rate of major birth defects and miscarriage is unknown for the indicated population.
What are the important warnings for Azacitidine?▼
5 WARNINGS AND PRECAUTIONS Risks of Substitution with Other Azacitidine Products: Do not substitute azacitidine for injection for oral azacitidine ( 2.1 , 5.1 ). Anemia, Neutropenia and Thrombocytopenia: Monitor complete blood counts (CBC) frequently ( 5.2 ). Hepatotoxicity: Patients with severe preexisting hepatic impairment are at higher risk for toxicity ( 5.3 ). Renal Toxicity: Monitor patients with renal impairment for toxicity since azacitidine and its metabolites are primarily excreted by the kidneys ( 5.4 ). Tumor Lysis Syndrome: Azacitidine may cause fatal or serious tumor lysis syndrome, including in patients with MDS. Assess baseline risk and monitor and treat as appropriate ( 5.5 ). Embryo-Fetal Toxicity: Azacitidine can cause fetal harm. 4 CONTRAINDICATIONS Advanced Malignant Hepatic Tumors ( 4.1 ). Hypersensitivity to Azacitidine or Mannitol ( 4.2 ). 4.1 Advanced Malignant Hepatic Tumors Azacitidine for injection is contraindicated in patients with advanced malignant hepatic tumors [see Warnings and Precautions ( 5.3 )] .
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.