No

Antineoplastic Agent, Antimetabolite

Remission induction, consolidation, and maintenance therapy of acute myelogenous (nonlymphocytic) leukemia; treatment of chronic myelogenous leukemia and granulocytic leukemia

D

History of previous therapy resistance with either thioguanine or mercaptopurine (there is usually complete cross resistance between these two); hypersensitivity to thioguanine or any component

The U.S. Food and Drug Administration (FDA) currently recommends that procedures for proper handling and disposal of antineoplastic agents be considered. Use with caution and reduce dose of thioguanine in patients with renal or hepatic impairment; thioguanine is potentially carcinogenic and teratogenic; myelosuppression may be delayed.

>10%:

Hematologic: Myelosuppressive:

WBC: Moderate

Platelets: Moderate

Onset (days): 7-10

Nadir (days): 14

Recovery (days): 21

1% to 10%:

Dermatologic: Skin rash

Endocrine & metabolic: Hyperuricemia

Gastrointestinal: Mild nausea or vomiting, anorexia, stomatitis, diarrhea

Emetic potential: Low (<10%)

Neuromuscular & skeletal: Unsteady gait

<1%: Neurotoxicity, photosensitivity, hepatitis, jaundice, veno-occlusive hepatic disease

Symptoms of overdose include bone marrow suppression, nausea, vomiting, malaise, hypertension, sweating

Treatment is supportive; dialysis is not useful

Increased toxicity:

Allopurinol can be used in full doses with 6 TG unlike 6-MP

Busulfan hepatotoxicity and esophageal varices

The (investigational) parenteral preparation is supplied as a 75 mg vial and should be stored in the refrigerator. It is reconstituted with 5 mL of 0.9% NaCl for injection, providing a concentration of 15 mg/mL, which is stable for at least 24 hours under refrigeration. When this solution is further diluted in 500 mL D₅W or 0.9% NaCl, it is stable for at least 24 hours at room temperature, or under refrigeration of thioguanine (1 vial). The resultant solution is reported to be stable for 8 hours at room temperature or under refrigeration.

Purine analog that is incorporated into DNA and RNA resulting in the blockage of synthesis and metabolism of purine nucleotides

Absorption: Oral: 30%

Distribution: Crosses placenta

Metabolism: Rapidly and extensively in the liver to 2-amino-6-methylthioguanine (active) and inactive compounds

Half-life, terminal: 11 hours

Time to peak serum concentration: Within 8 hours

Elimination: In urine

Total daily dose can be given at one time; offers little advantage over mercaptopurine; is sometimes ordered as 6-thioguanine, with 6 being part of the drug name and not a unit or strength

Infants and Children <3 years: Combination drug therapy for acute nonlymphocytic leukemia: 3.3 mg/kg/day in divided doses twice daily for 4 days

Children and Adults: 2-3 mg/kg/day calculated to nearest 20 mg or 75-200 mg/m²/day in 1-2 divided doses for 5-7 days or until remission is attained

Dosing comments in renal or hepatic impairment: Reduce dose

Enhanced absorption if administered between meals

CBC with differential and platelet count, liver function tests, hemoglobin, hematocrit, serum uric acid

None reported

Myelosuppression is common; avoid clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

You may experience nausea and vomiting, diarrhea, or loss of appetite (frequent small meals may help/request medication) or weakness or lethargy (use caution when driving or engaging in tasks requiring alertness until response to drug is known). Use good oral care to reduce incidence of mouth sores. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). May cause headache (request medication). Report signs or symptoms of infection (eg, fever, chills, sore throat, burning urination, fatigue), bleeding (eg, tarry stools, easy bruising), vision changes, unresolved mouth sores, nausea or vomiting, CNS changes (hallucinations), or respiratory difficulty. Avoid crowds or exposure to infected persons; you will be susceptible to infection. Pregnancy/breast-feeding precautions: Do not get pregnant; use appropriate contraceptive measures to prevent possible harm to the fetus. The drug may cause permanent sterility and may cause birth defects. Consult prescriber if breast-feeding.

Monitor CBC with differential and platelet count, liver function tests, hemoglobin, hematocrit, serum uric acid

Tablet, scored: 40 mg

A 40 mg/mL oral suspension compounded from tablets which were crushed, mixed with a volume of Cologel® suspending agent equal to 1/3 the final volume, and brought to the final volume with a 2:1 mixture of simple syrup and cherry syrup was stable for 84 days when stored in an amber bottle at room temperature

Culbert SJ, Shuster JJ, Land VJ, et al, "Remission Induction and Continuation Therapy in Children With Their First Relapse of Acute Lymphoid Leukemia: A Pediatric Oncology Group Study," Cancer, 1991, 67(1):37-42.

Jeffrey LP, Chairman, National Study Commission on Cytotoxic Exposure. Position Statement. "The Handling of Cytotoxic Agents by Women Who Are Pregnant, Attempting to Conceive, or Breast-Feeding," January 12, 1987.

Steuber CP, Civin C, Krischer J, et al, "A Comparison of Induction and Maintenance Therapy for Acute Nonlymphocytic Leukemia in Childhood: Results of a Pediatric Oncology Group Study," J Clin Oncol, 1991, 9(2):247-58.