Mercaptopurine

Mercaptopurine is a purine antagonist that is prescribed along with other agents for the maintenance therapy of acute lymphocytic leukemia.

Purinethol

Mercaptopurine

6MP and other generic brands

100

Zydus Cadila and others

Tablet

50 mg

India

Mercaptopurine

I. Introduction

Brief History of Mercaptopurine

Mercaptopurine, often referred to as 6 MP, was initially created during the 1950s in the pursuit of developing antineoplastic drugs. Its development represented progress in the realm of chemotherapy.

Importance in Modern Medicine

This medication is primarily used to treat types of blood cancers and autoimmune disorders. Its ability to effectively address medical conditions makes it an essential part of modern treatment plans.

Objective of the Article

The main purpose of this article is to provide detailed information about the pharmacological characteristics of Mercaptopurine, including its approved and off-label applications, potential side effects, and necessary precautions.

II. Composition of Mercaptopurine

Chemical Structure

Mercaptopurine falls under the category of purine analogs in terms of its chemical classification. Its molecular structure is represented by the formula C5H4N4S, which showcases a complex arrangement of atoms.

Pharmacological Class

Belonging to the category of drugs, Mercaptopurine hinders the synthesis of DNA and RNA by imitating crucial components necessary for their formation.

Active and Inactive Ingredients

The main component of this product is Mercaptopurine. Other ingredients include lactose monohydrate, magnesium stearate, and starch.

III. How Mercaptopurine Works

Mechanism of Action

Mercaptopurine undergoes a metabolic process that results in the formation of thioinosinic acid. This compound acts as an inhibitor of purine synthesis, leading to decreased availability of DNA and RNA building blocks.

Cellular Level Interactions

At a level, Mercaptopurine has a significant influence on cells that are actively dividing as well as those in a dormant state, which makes it incredibly potent, against the diverse nature of cancer cells.

Importance in Inhibiting DNA Synthesis

Its ability to stop DNA synthesis is crucial for its effectiveness in fighting against cancer. By disrupting the process of DNA replication, it effectively slows down the growth of cells.

IV. Uses of Mercaptopurine

Approved Uses

Treatment of Acute Lymphoblastic Leukemia (ALL)

Mercaptopurine is an antineoplastic agent used to treat acute lymphoblastic leukemia (ALL) 12It is often used in combination with other chemotherapy drugs 1.

Here are some references that provide more information about mercaptopurine:

  1. American Cancer Society: Treating Acute Lymphocytic Leukemia (ALL)
  2. DrugBank Online: Mercaptopurine

Treatment of Chronic Myeloid Leukemia (CML)

Mercaptopurine is an antineoplastic agent that is used to treat acute lymphoblastic leukemia (ALL) 12It is often used in combination with other chemotherapy drugs 1.

Here are some references that provide more information about mercaptopurine:

  1. American Cancer Society: Treating Acute Lymphocytic Leukemia (ALL)
  2. DrugBank Online: Mercaptopurine

Inflammatory Bowel Disease Management

Mercaptopurine is an antineoplastic agent that is used to treat acute lymphoblastic leukemia (ALL) 12It is often used in combination with other chemotherapy drugs 1.

In addition to its use in blood-related cancers, mercaptopurine has also been used to treat inflammatory bowel diseases (IBD), such as Crohn’s disease and ulcerative colitis 345.

Here are some references that provide more information about mercaptopurine:

  1. American Cancer Society: Treating Acute Lymphocytic Leukemia (ALL)
  2. DrugBank Online: Mercaptopurine
  3. UpToDate: Overview of azathioprine and mercaptopurine use in inflammatory bowel disease
  4. UpToDate: Thiopurines: Pretreatment testing and approach to therapeutic drug monitoring for adults with inflammatory bowel disease
  5. National Cancer Institute: Mercaptopurine

Off-label Uses

Autoimmune Disorders

Mercaptopurine is an antineoplastic agent that is used to treat acute lymphoblastic leukemia (ALL) 12It is often used in combination with other chemotherapy drugs 1.

While mercaptopurine has not been approved by the FDA for the treatment of lupus erythematosus or rheumatoid arthritis, it has been studied for its potential use in treating these conditions 345. However, more research is needed to determine its efficacy and safety for these purposes.

Here are some references that provide more information about mercaptopurine:

  1. American Cancer Society: Treating Acute Lymphocytic Leukemia (ALL)
  2. DrugBank Online: Mercaptopurine
  3. Frontiers in Immunology: Preclinical Autoimmune Disease: a Comparison of Rheumatoid Arthritis, Systemic Lupus Erythematosus, Multiple Sclerosis and Type 1 Diabetes
  4. Proceedings of UCLA Healthcare: ABATACEPT-induced Lupus Erythematosus Panniculitis in a Patient with Rheumatoid Arthritis
  5. SpringerLink: Cytokine profile in systemic lupus erythematosus, rheumatoid arthritis and other rheumatic diseases

Other Forms of Cancer

Sometimes doctors use mercaptopurine along, with cancer fighting drugs to treat solid tumors.

Pediatric Crohn’s Disease

Pediatricians sometimes use Mercaptopurine to alleviate the symptoms associated with Crohn's disease in children.

V. Dosage and Administration

Standard Dosage

The recommended daily dosage ranges from 60 to 115 mg per meter for all conditions. In the case of Chronic Myeloid Leukemia (CML), the suggested dosage is between 1.5 and 2.5 mg per kilogram per day. For Inflammatory Bowel Disease, it is advised to take between 1 and 1.5 mg per kilogram daily.

Route of Administration

Oral tablets and liquid formulations are frequently utilized in practice.

Administration to Specific Populations

Administration to Elderly

It is crucial to proceed cautiously when adjusting the dosage to prevent any effects on the bone marrow and liver function.

Administration to Pregnant Women and Nursing Mothers

Mercaptopurine falls into Pregnancy Category D. It Should not be used by pregnant or breastfeeding women.

Administration to Children

Dosages, for children, are typically determined based on their body surface area and necessitate careful monitoring.

VI. Side Effects of Mercaptopurine

Common Side Effects

Gastrointestinal Issues

  • Nausea
  • Vomiting
  • Abdominal pain

Hematologic Effects

  • Leucopenia
  • Anemia
  • Thrombocytopenia

Liver Function Alterations

Elevated liver enzymes have been observed.

Less Common Side Effects

Skin Reactions

  • Urticaria
  • Rash

Central Nervous System Effects

  • Dizziness
  • Malaise

Pancreatic Complications

Acute pancreatitis has been reported, although it is not an occurrence.

VII. Important Precautions

Pre-Treatment Tests

Preliminary blood counts and liver function tests are essential.

Monitoring During Treatment

Regular monitoring of blood parameters and occasional liver function tests should be included as part of the treatment plan.

Steps for Dose Adjustments

Immediate adjustments to the dosage are necessary if there is a decrease in the count of blood cells or any indication of liver toxicity.

VIII. Drug Interactions

Interaction with Allopurinol

When Mercaptopurine is combined with Allopurinol, it can amplify the effects of Mercaptopurine, which may require adjustments to the dosage. Allopurinol inhibits xanthine oxidase, an enzyme that affects how Mercaptopurine is metabolized. As a result, there is an increased risk of experiencing toxicity. It is essential to modify the dosage and closely monitor the situation to ensure safety.

Interaction with Blood Thinners

When Mercaptopurine and anticoagulants, like warfarin, are taken together, the anticoagulant effects may become more muscular. This can lead to an increased risk of bleeding. To manage this, it is advised to monitor the prothrombin time or international normalized ratio (INR).

Interaction with Live Vaccines

Administering vaccines to patients taking Mercaptopurine can lead to severe and potentially life-threatening infections because the drug weakens the immune system. As a result, patients become more vulnerable to conditions. Therefore, it is generally recommended to avoid administering vaccines in such cases.

IX. Warnings and Contraindications

General Warnings

Risk of Secondary Neoplasms

People who are prescribed Mercaptopurine may have a risk of developing additional types of cancer, specifically skin cancers and lymphomas.

Bone Marrow Suppression

One of the serious negative consequences of Mercaptopurine is its tendency to cause myelosuppression, which is a reduction in the production of blood cells. It is essential to monitor blood counts to ensure the safety and well-being of patients taking this medication.

Hepatotoxicity Risks

Mercaptopurine carries a probability of causing liver problems, which is emphasized by the possibility of increased liver enzyme levels.

Contraindications

Known Hypersensitivity

Individuals with a known sensitivity or allergy to the drug should not use mercaptopurine.

Severe Liver or Kidney Dysfunction

Individuals with liver or kidney problems should avoid taking Mercaptopurine because it can be more toxic for this group of patients.

X. Careful Administration

Guidelines for Safe Handling

Make sure to wear protective equipment (PPE) when handling tablets. Ensure your hands are dry before touching them. Be careful not to crush or break the tablet.

Patient Education Points

The significance of taking medication as prescribed and following the recommended schedule Identifying the indications of toxicity at an early stage Taking necessary precautions in terms of dietary habits and choices

Provider Responsibility

We need to keep an eye on the patient's progress, provide them with guidance and support, and make any necessary changes, to their medication dosage if required.

XI. Overdosage

Signs and Symptoms

Experiencing an amount of Mercaptopurine can result in intense feelings of nausea, throwing up, and abnormalities in the blood, among other symptoms.

Emergency Management

You should seek medical attention and consider having your stomach flushed if necessary. If required, hemodialysis may also be considered.

Supportive Measures

Administering fluids through a vein, Providing support for blood needs, observing and tracking essential indicators.

XII. Storage and Handling Precautions

Optimal Storage Conditions

You should keep mercaptopurine in a place where it's not too hot or humid and away from sunlight.

Shelf Life

Usually, Mercaptopurine can last for around 36 months if stored properly.

Disposal Guidelines

It is important to follow both state regulations when disposing of medication. It is crucial to avoid throwing away medication, in household waste, or flushing it down the toilet.

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