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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ANTIMETABOLITES › Purine analogues
tioguanine
L01BB03
Forms & Strengths
- Tioguanine 40mg tablets
- Available in 40mg tablets for oral administration
Adult Dosing
- Initial dose: 2mg/kg/day, rounded to the nearest 40mg
- Maintenance dose: 1-3mg/kg/day, adjusted for hematologic and hepatic toxicity
Pediatric Dosing
- Initial dose: 2mg/kg/day, rounded to the nearest 40mg
- Adjust for body surface area, not weight, in children
Indications
- Acute lymphoblastic leukemia
- Acute myeloid leukemia
- Chronic myeloid leukemia
- Some solid tumors and lymphomas
Mechanism of Action
- Inhibits nucleic acid synthesis through incorporation into DNA and RNA
- Acts as a purine antagonist, interfering with nucleotide metabolism
Contraindications
- Hypersensitivity to tioguanine or mercaptopurine
- Liver disease with significant elevation of liver enzymes
- Pregnancy, unless benefits outweigh risks
Adverse Reactions
- Myelosuppression, including anemia, neutropenia, and thrombocytopenia
- Hepatotoxicity, including elevated liver enzymes and jaundice
- Nausea, vomiting, and diarrhea
- Mucositis
Drug Interactions
- Warfarin: monitor INR due to potential increased anticoagulant effect
- Allopurinol: avoid concomitant use due to increased risk of toxicity
- Immunosuppressants: monitor for increased risk of infection
Curated Content: Needs Vetting Before Put to Clinical Use