PURINETHOL- mercaptopurine tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

MERCAPTOPURINE (UNII: E7WED276I5) (MERCAPTOPURINE ANHYDROUS - UNII:PKK6MUZ20G)

Available from:

Stason Pharmaceuticals, Inc.

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

PURINETHOL is indicated for treatment of adult and pediatric patients with acute lymphoblastic leukemia (ALL) as part of a combination chemotherapy maintenance regimen. None. PURINETHOL 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. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Women receiving mercaptopurine in the first trimester of pregnancy have an increased incidence of miscarriage; the risk of malformation in offspring surviving first trimester exposure is not known. In a series of 28 women receiving mercaptopurine after the first trimester of pregnancy, 3 mothers died prior to delivery, 1 delivered a stillborn child, and 1 aborted; there were no cases of macroscopically abnormal fetuses. Mercaptopurine was embryo-lethal and teratogenic in several animal species (rat, mouse, rabbit, and hamster) at doses less than the recommended human dose. There are no data on the presence of mercaptopurine or its metabolites in human milk, the effects on the breastfed child, or the effects on milk production. Because of the potential for serious adverse reactions in the breastfed child, advise women not to breastfeed during treatment with PURINETHOL and for 1 week after the last dose. PURINETHOL can cause fetal harm when administered to pregnant women [see Use in Specific Populations (8.1)] . Verify the pregnancy status in females of reproductive potential prior to initiating PURINETHOL  [see Use in Specific Populations (8.1)] . Advise females of reproductive potential to use effective contraception during treatment with PURINETHOL and for 6 months after the last dose. Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective contraception during treatment with PURINETHOL and for 3 months after the last dose [see Nonclinical Toxicology (13.1)] . Based on findings from animal studies, PURINETHOL can impair female and male fertility [see Nonclinical Toxicology (13.1)] . The long-term effects of mercaptopurine on female and male fertility, including the reversibility have not been studied. Safety and effectiveness of PURINETHOL has been established in pediatric patients. Use of PURINETHOL in pediatrics is supported by evidence from the published literature and clinical experience. Symptomatic hypoglycemia has been reported in pediatric patients with ALL receiving mercaptopurine. Reported cases were in pediatrics less than 6 years of age or with a low body mass index. Clinical studies of mercaptopurine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or another drug therapy. Use the lowest recommended starting dosage for PURINETHOL or increase the dosing interval to every 36-48 hours in patients with renal impairment (CLcr less than 50 mL/min). Adjust the dose to maintain absolute neutrophil count (ANC) at a desirable level and for adverse reactions [see Dosage and Administration (2.3)] . Use the lowest recommended starting dosage for PURINETHOL in patients with hepatic impairment. Adjust the dose to maintain absolute neutrophil count (ANC) at a desirable level and for adverse reactions [see Dosage and Administration (2.3)] .

Product summary:

PURINETHOL is supplied as biconvex, round, pale yellow to buff, scored tablets containing 50 mg mercaptopurine, imprinted with “9|3” available in: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Store in a dry place. Dispense in tight container as defined in the USP. PURINETHOL is a cytotoxic drug. Follow special handling and disposal procedures 1 .

Authorization status:

New Drug Application

Summary of Product characteristics

PURINETHOL- MERCAPTOPURINE TABLET
STASON PHARMACEUTICALS, INC.
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HIGHLIGHTS OF PRESCRIBING INFORMATION
THESE HIGHLIGHTS DO NOT INCLUDE ALL THE INFORMATION NEEDED TO USE
PURINETHOL SAFELY AND
EFFECTIVELY. SEE FULL PRESCRIBING INFORMATION FOR PURINETHOL.
PURINETHOL (MERCAPTOPURINE) TABLETS, FOR ORAL USE
INITIAL U.S. APPROVAL: 1953
RECENT MAJOR CHANGES
Warnings and Precautions, Treatment Related Malignancies ( 5.4) 4/2020
Warnings and Precautions, Macrophage Activation Syndrome ( 5.5) 4/2020
INDICATIONS AND USAGE
PURINETHOL 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)
DOSAGE AND ADMINISTRATION
The recommended starting dose of PURINETHOL is 1.5mg/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)
DOSAGE FORMS AND STRENGTHS
Tablets: 50 mg ( 3)
CONTRAINDICATIONS
None .
WARNINGS AND PRECAUTIONS
Myelosuppression: Monitor complete blood count (CBC) and adjust the
dose of PURINETHOL 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 PURINETHOL 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. ( 5.3)
Treatment Related Malignan