[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Antimetabolites](https://durgical.com/en/pharmacology/classes/antimetabolites/) › Azacitidine # Azacitidine ## Antimetabolites? Antimetabolites ## High alert? An error with this medicine can cause serious harm: double checks and protocols are used. A cytidine analogue that traps DNA methyltransferase and switches silenced genes back on. Used for myelodysplastic syndromes. Updated Nov 1, 2026 Also called: 5-azacytidine ## Quick facts **Group** [Antimetabolites](https://durgical.com/en/pharmacology/classes/antimetabolites/) **Target** DNA methyltransferase (DNMT1), trapped on DNA **Used for** Myelodysplastic syndromes **Key effects** Nausea · Anaemia · Injection-site redness and bruising **Monitor** Liver function · Bicarbonate **ATC** L01BC07 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Clinical What the labels mean - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action Azacitidine is cytidine with a nitrogen in place of a carbon in its ring. It enters cells through nucleoside transporters and is built into DNA, where it binds DNA methyltransferase covalently and depletes the enzyme, so newly made DNA loses methyl marks (hypomethylation). Genes silenced by methylation, including some that control blood cell maturation, can be switched back on. At higher concentrations it is also directly toxic to abnormal marrow cells. - Azacitidine is built into DNA - It traps DNA methyltransferase on DNA - New DNA loses its methyl marks - Silenced genes switch back on; abnormal cells mature or die ## Indications - Myelodysplastic syndromes (the main subtypes, including those with excess blasts); it reduces transfusion needs and can improve survival. [Myelodysplastic syndromes →](https://durgical.com/en/conditions/myelodysplastic-syndromes/) ## Adverse effects ### Common - Nausea, vomiting, constipation, diarrhoea - Anaemia, neutropenia, thrombocytopenia - Injection-site redness and bruising - Fever, fatigue ### Serious (rare, important) - Severe cytopenias with infection or bleeding - Liver toxicity, especially with advanced liver disease - Kidney toxicity and renal tubular acidosis - Tumour lysis syndrome ## Contraindications - Advanced malignant liver tumours - Hypersensitivity to azacitidine or mannitol ## Key interactions **Other myelosuppressive drugs** Deeper cytopenias. **Oral azacitidine products** Not interchangeable with the injection: a different product with a different schedule. ## What is monitored - Complete blood count before each cycle and often during treatment - Liver function and serum creatinine before each cycle - Bicarbonate (renal tubular acidosis) ## Administration and safety - The injection and the oral tablets are different products and are never substituted for each other. - Subcutaneous doses above a set volume are split between sites; injection sites are rotated. - Hazardous drug: chemotherapy handling precautions. ## Pregnancy and breastfeeding Can cause fetal harm; women and men with partners who could become pregnant use effective contraception. ## Nursing care - Rotate injection sites and check them for redness or bruising. - Antiemetics before doses as prescribed. - Check counts and creatinine before each cycle; report fever or bleeding. - Teaching: effective contraception for women and men. ## Pharmacokinetics **Absorption** Subcutaneous (rapidly absorbed) or intravenous injection. **Metabolism** Rapid spontaneous hydrolysis and deamination by cytidine deaminase; its effect lasts longer because it stays in DNA. **Elimination** Mainly by the kidneys, with its metabolites. ## Memory aid «AZAcitidine wakes genes from A to Z»: a hypomethylating drug that traps DNA methyltransferase in myelodysplastic syndromes. ## Test yourself Think of the answer, then tap the question to see it. ## How does azacitidine change gene expression? It traps DNA methyltransferase, causing DNA hypomethylation that reactivates silenced genes. ## Which condition is the main use of azacitidine? Myelodysplastic syndromes. ## Can oral and injectable azacitidine be substituted for each other? No: they are different products with different schedules and indications. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/azacitidine/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## What the labels mean **High alert** An error with this medicine can cause serious harm: double checks and protocols are used. ## Connections ## Related drugs 2 - [Cytarabine](https://durgical.com/en/pharmacology/cytarabine/) - [Lenalidomide](https://durgical.com/en/pharmacology/lenalidomide/) ## Related conditions 1 - [Myelodysplastic syndromes](https://durgical.com/en/conditions/myelodysplastic-syndromes/) [← Back to the class: Antimetabolites](https://durgical.com/en/pharmacology/classes/antimetabolites/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [DailyMed - AZACITIDINE injection, powder, lyophilized, for solution](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a6a5ca37-37e8-ab65-bc0b-9c0682ab52f7) (DailyMed (U.S. National Library of Medicine), 2026); [Azacitidine Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a607068.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01BC07) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/azacitidine/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/azacitidine/