Mercaptopurine

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Mercaptopurine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Rabin Bista, M.B.B.S. [2]

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Overview

Mercaptopurine is a Antineoplastic, antimetabolite that is FDA approved for the treatment of maintenance therapy of acute lymphatic (lymphocytic, lymphoblastic) leukemia as part of a combination regimen. Common adverse reactions include Bone marrrow toxicity, Hepatotoxicity, skin rashes, Diarrhoea, nausea, vomiting and anorexia.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indication

  • maintenance therapy of acute lymphatic (lymphocytic, lymphoblastic) leukemia as part of a combination regimen.
  • The response to this agent depends upon the particular subclassification of acute lymphatic leukemia and the age of the patient (pediatric or adult).

Dosage

Maintenance Therapy
  • Once a complete hematologic remission is obtained, maintenance therapy is considered essential. Maintenance doses will vary from patient to patient. The usual daily maintenance dose of mercaptopurine is 1.5 to 2.5 mg/kg/day as a single dose. It is to be emphasized that in pediatric patients with acute lymphatic leukemia in remission, superior results have been obtained when mercaptopurine has been combined with other agents (most frequently with methotrexate) for remission maintenance. Mercaptopurine should rarely be relied upon as a single agent for the maintenance of remissions induced in acute leukemia.
Dosage with Concomitant Allopurinol
  • When allopurinol and mercaptopurine are administered concomitantly, the dose of mercaptopurine must be reduced to one third to one quarter of the usual dose to avoid severe toxicity.
Dosage in TPMT-deficient Patients
  • Patients with inherited little or no thiopurine-S-methyltransferase (TPMT) activity are at increased risk for severe mercaptopurine toxicity from conventional doses of mercaptopurine and generally require substantial dose reduction. The optimal starting dose for homozygous deficient patients has not been established
Dosage in Renal and Hepatic Impairment
  • It is probably advisable to start with lower dosages in patients with impaired renal function, due to slower elimination of the drug and metabolites and a greater cumulative effect. Consideration should be given to reducing the dosage in patients with impaired hepatic function.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Mercaptopurine in adult patients.

Non–Guideline-Supported Use

Indications

  • Acute myeloid leukemia[1]
  • Chronic myeloid leukemia
  • Crohn's disease[2][3]

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding FDA-Labeled Use of Mercaptopurine in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition1
  • Developed by:
  • Class of Recommendation:
  • Strength of Evidence:
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Guideline-Supported Use of Mercaptopurine in pediatric patients.

Non–Guideline-Supported Use

Condition1
  • Dosing Information
  • Dosage
Condition2

There is limited information regarding Off-Label Non–Guideline-Supported Use of Mercaptopurine in pediatric patients.

Contraindications

  • Condition1

Warnings

  • Description

Precautions

  • Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Mercaptopurine in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Mercaptopurine in the drug label.

Body as a Whole
Cardiovascular
Digestive
Endocrine
Hematologic and Lymphatic
Metabolic and Nutritional
Musculoskeletal
Neurologic
Respiratory
Skin and Hypersensitivy Reactions
Special Senses
Urogenital
Miscellaneous

Drug Interactions

  • Drug
  • Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Mercaptopurine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Mercaptopurine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Mercaptopurine with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Mercaptopurine with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Mercaptopurine with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Mercaptopurine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Mercaptopurine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Mercaptopurine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Mercaptopurine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Mercaptopurine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Mercaptopurine in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral
  • Intravenous

Monitoring

There is limited information regarding Monitoring of Mercaptopurine in the drug label.

  • Description

IV Compatibility

There is limited information regarding IV Compatibility of Mercaptopurine in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

  • Description

Management

  • Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Mercaptopurine in the drug label.

Pharmacology

There is limited information regarding Mercaptopurine Pharmacology in the drug label.

Mechanism of Action

Structure

File:Mercaptopurine01.png
This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Mercaptopurine in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Mercaptopurine in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Mercaptopurine in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Mercaptopurine in the drug label.

How Supplied

Storage

There is limited information regarding Mercaptopurine Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Mercaptopurine in the drug label.

Precautions with Alcohol

  • Alcohol-Mercaptopurine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. Canpolat C, Jeha S, Lockhart S, Ramirez I, Zipf T, Pinkel D (1997). "High-dose mercaptopurine and intermediate-dose cytarabine during first remission of acute myeloid leukemia". Cancer Invest. 15 (2): 121–6. PMID 9095207.
  2. Nagy F, Molnar T, Szepes Z, Farkas K, Nyari T, Lonovics J (2008). "Efficacy of 6-mercaptopurine treatment after azathioprine hypersensitivity in inflammatory bowel disease". World J Gastroenterol. 14 (27): 4342–6. PMC 2731186. PMID 18666323.
  3. Kim PS, Zlatanic J, Korelitz BI, Gleim GW (1999). "Optimum duration of treatment with 6-mercaptopurine for Crohn's disease". Am J Gastroenterol. 94 (11): 3254–7. doi:10.1111/j.1572-0241.1999.01532.x. PMID 10566725.
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