Mercaptopurine
Generic Name: mercaptopurine
Brand Names:
Mercaptopurine
11 DESCRIPTION Mercaptopurine is a nucleoside metabolic inhibitor, the chemical name is 6 H -purine-6-thione, 1,7-dihydro-, monohydrate. The molecular formula is C 5 H 4 N 4 S • H 2 O and the molecular weight is 170.20. Its structural formula is: Mercaptopurine is a yellow, crystalline powder. Mercaptopurine is practically insoluble in water and in ether. It has a pKa of 7.8, an average tapped density of 1.0 g/mL and average bulk density of 0.85 g/mL.
Overview
11 DESCRIPTION Mercaptopurine is a nucleoside metabolic inhibitor, the chemical name is 6 H -purine-6-thione, 1,7-dihydro-, monohydrate. The molecular formula is C 5 H 4 N 4 S • H 2 O and the molecular weight is 170.20. Its structural formula is: Mercaptopurine is a yellow, crystalline powder. Mercaptopurine is practically insoluble in water and in ether. It has a pKa of 7.8, an average tapped density of 1.0 g/mL and average bulk density of 0.85 g/mL.
Uses
1 INDICATIONS AND USAGE Mercaptopurine Tablets is a nucleoside metabolic inhibitor indicated for treatment of adult and pediatric patients with acute lymphoblastic leukemia (ALL) as part of a combination chemotherapy maintenance regimen. (1.1) 1.1 Acute Lymphoblastic Leukemia Mercaptopurine Tablets are indicated for treatment of adult and pediatric patients with acute lymphoblastic leukemia (ALL) as part of a combination chemotherapy maintenance regimen.
Dosage
2 DOSAGE AND ADMINISTRATION The recommended starting dose of Mercaptopurine Tablets is 1.5 mg/kg to 2.5 mg/kg orally once daily as part of a combination chemotherapy maintenance regimen. Adjust dose to maintain desirable absolute neutrophil count and for excessive myelosuppression. (2.1) Renal Impairment: Use the lowest recommended starting dose or increase the dosing interval. (2.3, 8.6) Hepatic Impairment: Use the lowest recommended starting dose. (2.3, 8.7) 2.1 Recommended Dosage The recommended starting dosage of Mercaptopurine Tablets is 1.5 mg/kg to 2.5 mg/kg orally once daily as part of combination chemotherapy maintenance regimen. A recommended dosage for patients less than 17 kg is not achievable, because the only available strength is 50 mg.
Side Effects
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Myelosuppression [see Warnings and Precautions ( 5.1 )] Hepatotoxicity [see Warnings and Precautions ( 5.2 )] Immunosuppression [see Warnings and Precautions (5.3)] Treatment related malignancies [see Warnings and Precautions (5.4 )] Macrophage activation syndrome [see Warnings and Precautions ( 5.5 )] The most common adverse reaction (>20%) is myelosuppression, including anemia, leukopenia and thrombocytopenia. Adverse reactions occurring in 5% to 20% of patients include anorexia, nausea, vomiting, diarrhea, malaise and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc.
Interactions
7 DRUG INTERACTIONS Allopurinol : Reduce the dose of Mercaptopurine Tablets when co-administered with allopurinol. (2.4, 7.1) Warfarin : Mercaptopurine Tablets may decrease the anticoagulant effect. (7.2) 7.1 Allopurinol Allopurinol can inhibit the first-pass oxidative metabolism of mercaptopurine by xanthine oxidase, which can lead to an increased risk of mercaptopurine adverse reactions (i.e., myelosuppression, nausea, and vomiting) [see Warnings and Precautions ( 5.1 ), Adverse Reactions ( 6.1 )]. Reduce the dose of Mercaptopurine Tablets when coadministered with allopurinol [see Dosage and Administration ( 2.4 )]. 7.2 Warfarin The concomitant administration of Mercaptopurine Tablets and warfarin may decrease the anticoagulant effectiveness of warfarin.
Warnings
5 WARNINGS AND PRECAUTIONS Myelosuppression: Monitor complete blood count (CBC) and adjust the dose of Mercaptopurine Tablets for excessive myelosuppression. Consider testing in patients with severe myelosuppression or repeated episodes of myelosuppression for thiopurine S-methyltransferase (TPMT) or nucleotide diphosphatase (NUDT15) deficiency. Patients with homozygous or homozygous TPMT or NUDT15 deficiency may require a dose reduction. (2.2, 5.1) Hepatotoxicity: Monitor transaminases, alkaline phosphatase and bilirubin. Withhold Mercaptopurine Tablets at onset of hepatotoxicity. (5.2) Immunosuppression: Response to all vaccines may be diminished and there is a risk of infection with live virus vaccines. Consult immunization guidelines for immunocompromised patients. 4 CONTRAINDICATIONS None. None.
Pregnancy
8.1 Pregnancy Risk Summary Mercaptopurine Tablets can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )]. Pregnant women who receive mercaptopurine have an increased incidence of miscarriage and stillbirth (see Data). Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population(s) is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Mercaptopurine Tablets, USP 50 mg supplied as pale yellow, biconvex tablets, with product identification “54 420” on one side and a score on the other side. NDC 51407-983-25: Bottle of 250 Tablets Store at 20°C to 25°C (68°F to 77°F). [See USP Controlled Room Temperature.] Store in a dry place.
Frequently Asked Questions
What is Mercaptopurine used for?▼
1 INDICATIONS AND USAGE Mercaptopurine Tablets is a nucleoside metabolic inhibitor indicated for treatment of adult and pediatric patients with acute lymphoblastic leukemia (ALL) as part of a combination chemotherapy maintenance regimen. (1.1) 1.1 Acute Lymphoblastic Leukemia Mercaptopurine Tablets are indicated for treatment of adult and pediatric patients with acute lymphoblastic leukemia (ALL) as part of a combination chemotherapy maintenance regimen.
What are the side effects of Mercaptopurine?▼
6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Myelosuppression [see Warnings and Precautions ( 5.1 )] Hepatotoxicity [see Warnings and Precautions ( 5.2 )] Immunosuppression [see Warnings and Precautions (5.3)] Treatment related malignancies [see Warnings and Precautions (5.4 )] Macrophage activation syndrome [see Warnings and Precautions ( 5.5 )] The most common adverse reaction (>20%) is myelosuppression, including anemia, leukopenia and thrombocytopenia. Adverse reactions occurring in 5% to 20% of patients include anorexia, nausea, vomiting, diarrhea, malaise and rash. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc.
Can I take Mercaptopurine during pregnancy?▼
8.1 Pregnancy Risk Summary Mercaptopurine Tablets can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )]. Pregnant women who receive mercaptopurine have an increased incidence of miscarriage and stillbirth (see Data). Advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population(s) is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S.
What are the important warnings for Mercaptopurine?▼
5 WARNINGS AND PRECAUTIONS Myelosuppression: Monitor complete blood count (CBC) and adjust the dose of Mercaptopurine Tablets for excessive myelosuppression. Consider testing in patients with severe myelosuppression or repeated episodes of myelosuppression for thiopurine S-methyltransferase (TPMT) or nucleotide diphosphatase (NUDT15) deficiency. Patients with homozygous or homozygous TPMT or NUDT15 deficiency may require a dose reduction. (2.2, 5.1) Hepatotoxicity: Monitor transaminases, alkaline phosphatase and bilirubin. Withhold Mercaptopurine Tablets at onset of hepatotoxicity. (5.2) Immunosuppression: Response to all vaccines may be diminished and there is a risk of infection with live virus vaccines. Consult immunization guidelines for immunocompromised patients. 4 CONTRAINDICATIONS None. None.
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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.