Azacitidine

Drug #67

Azacitidine is a cytadine analogue that can be incorporated into RNA and DNA. Azacitidine is investigational antineoplastic drug. Azacitidine is antineoplastic agent. It belongs to antimetabolites. Antimetabolites are the compounds that bear a structural similarity to a naturally occuring substance, such as vitamin, nucleoside or amino acid. Azacitidine is effective in the treatment of different cancers to slow or stop the growth of abnormal cells. Azacitidine is used in combination with different anticancerous drugs to obtain most excellent therapeutic effects and minimize unwanted effects or toxicities. it has been used mainly in the treatment of acute non-lymphoblastic leukemia.

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Primary Characteristics

It is of Synthetic origin and belongs to Ribofuranosyltriazin.

It belongs to RNA polymerase substrate pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agent pharmacological group. It is also classified under Chemotherapeutic Regimens .

Molecular Weight: 244.2 · Solubility in Water: 8.9E+004mg/L · Solubility in Alcohol: 1 in 1000 · Non-proprietary name: Azacitidine.

Pharmacokinetics

Distribution: Azacitidine has a volume of distribution is 0.7 l/kg. plasma protein binding is < 1%.

Elimination: it is metabolised via extensive by liver, plasma half-life is 4 hr, renal excretion is 80%.

Indications

Azacitidine is primarily indicated in conditions like Acute myeloid leukemia, Beta thalassaemia, Sickle cell anaemia.

Contraindications

Azacitidine is contraindicated in conditions like Non malignant conditions.

Dosage

Azacitidine's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
1.458 mg/sq.meter	1.458 mg/sq.meter	—	IV Inf	Upto 2 hours for 5 days a week per 2 weeks
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

None recorded.

Side Effects

Azacitidine in overdosage may give rise to further complications which include Carcinogenic risk , Myeloid leukemia .

Azacitidine produces potentially life-threatening effects which include Severe Hypotension . Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Azacitidine are Myelosuppression , Vomiting, Diarrhea, Hypotension, Nausea.

Azacitidine is known to cause more or less tolerable side effects which are usually transient. These include Diarrhea, Nausea, Vomiting .

Warnings / Precautions

Azacitidine is not recommended for use during pregnancy or lactation. Immunosuppressant drug should not be given, where possible, to patients with acute infection, dosage reduction or withdrawal should be considered if infection develops, until the infection has been controlled. Blood counts and measurment of haemoglobin concentration should be carried out routinely, it help to predict the onset of bone marrow depression. It must be handled with great care and avoid contact with skin and eyes and should not be inhaled.

Available Brands

None recorded.

Storage Conditions

Azacitidine should be stored solutions,injections,powder.

Drug Classification

1.8.2 — Cytotoxic (anti-neoplastic) drugs