Mercaptopurine

Uses	Acute Lymphoblastic Leukaemia
Therapy	Anti-Neoplastic
Side Effects	Low Blood Counts, Nausea, Liver Problems, Mouth Ulcers

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Molecule Description

Mercaptopurine is an anticancer medicine in a group of drugs called nucleoside metabolic inhibitors, also known as purine analogues. It is used along with other medicines to treat Acute Lymphoblastic Leukaemia (ALL). Mercaptopurine is converted inside the body into active forms that interfere with DNA and RNA production of cancer cells, stopping the cells from dividing and causing them to die. Mercaptopurine is taken by mouth as prescribed by your doctor It can affect the bone marrow, lowering white blood cells, red blood cells, and platelets, which raises the risk of infection, anaemia, and bleeding. It can also affect the liver, so your doctor will check your blood counts and liver function regularly, both before starting and throughout treatment. Before starting Mercaptopurine, tell your doctor about any kidney or liver problems, any recent or planned vaccinations, TPMT and/or NUDT15 enzyme deficiency and whether you are pregnant, planning a pregnancy, or breastfeeding.

Uses

It is used in the management of Acute Lymphoblastic Leukaemia (ALL).

Contraindications

When should one not use Mercaptopurine

If you have a known hypersensitivity or severe allergic reaction to mercaptopurine or any of the inactive ingredients.

Side effects

Common side effects of this drug are:

Low platelet count (increases bruising or bleeding risk)
Low white blood cell count (increases infection risk)
Low red blood cell count (anaemia)
Loss of appetite
Nausea and vomiting
Diarrhoea, feeling generally unwell (malaise)
Rash
Hives (urticaria)
Mouth sores resembling thrush
Raised liver enzymes
Yellowing of the skin or eyes (jaundice)
Skin darkening
Infections
Pancreatitis
Fever, sore throat, or signs of infection
Cuts or wounds that are red, swollen, or draining
Any unusual bleeding
Tiredness or weakness, shortness of breath (possible anaemia)
Yellowing of the skin or eyes, loss of appetite, diarrhoea, nausea or vomiting, or abdominal swelling or pain, which may indicate liver injury or other serious complications
Severe or persistent abdominal pain, especially with nausea or vomiting, which may indicate pancreatitis
Severe weakness, dizziness, or other symptoms associated with very low blood counts
Low blood sugar, particularly in young children

Precautions and Warnings

Pregnancy

Mercaptopurine may harm an unborn baby and should be used during pregnancy only when clearly necessary and under specialist medical supervision. Women who can become pregnant should use effective contraception during treatment and for the period advised by their doctor. Men with partners who can become pregnant should also discuss contraception with their doctor.

Breast Feeding

Breastfeeding is not recommended during treatment as it may pass through breast milk and harm the nursing baby. Discuss with your doctor when you can safely resume breastfeeding.

Driving

Mercaptopurine is not known to affect your ability to drive or operate machinery, but if you feel unwell, tired, or unsteady, avoid driving or using machinery until you feel better.

Alcohol

There is no known specific alcohol interaction, but alcohol can add strain to a liver that is already being closely monitored during treatment. Discuss alcohol use with your doctor.

Other General Warnings

Talk to your doctor if

You have kidney or liver problems.
You have a known deficiency of the TPMT or NUDT15 enzyme.
You have phenylketonuria (PKU).
You have recently had, or are planning to have, a vaccination.
You notice signs of infection, unusual bleeding, or symptoms of a liver problem.
You are concerned about your future fertility, as this medicine may affect fertility in both men and women.
You develop severe abdominal pain, particularly if accompanied by nausea or vomiting, because this may indicate pancreatitis.

Mode of Action

How Does It Work?

Mercaptopurine belongs to a class of medicines called nucleoside metabolic inhibitors (purine analogues). Once inside the body, Mercaptopurine is incorporated into the DNA and RNA of rapidly dividing leukaemia cells. This disrupts normal cell division and leads to the death of the cancer cells.

Interactions

Interactions with other medicines

Allopurinol can raise Mercaptopurine levels in the body; your doctor will usually reduce your Mercaptopurine dose if the two are used together.
Mercaptopurine may reduce the blood-thinning effect of warfarin; your doctor may need to monitor your INR more closely.
Using Mercaptopurine with other medicines that affect the bone marrow (such as co-trimoxazole) or the liver can increase the risk of side effects.
Aminosalicylates (such as mesalamine, olsalazine, or sulfasalazine) can increase the risk of bone marrow side effects when combined with Mercaptopurine.
Methotrexate may affect mercaptopurine exposure or toxicity; your doctor will consider this interaction when both medicines are used together.
Live vaccines are not recommended during treatment; discuss any vaccination plans with your doctor.
Always tell your doctor about every prescription medicine, over-the-counter medicine, vitamin, and herbal or dietary supplement you are taking.

Interactions with food items

You can take mercaptopurine with or without food, but take it consistently in the same way each day. Maintain a balanced diet and stay well-hydrated throughout your treatment course. Avoid excessive alcohol consumption, as it may increase the risk of liver problems.

Dosage

Overdose

If an overdose is suspected, seek immediate medical intervention in a hospital setting. Symptoms of an overdose can include severe nausea, vomiting, profound bone marrow suppression, and signs of liver damage. Management involves supportive hospital care, monitoring of blood counts, and close clinical observation.

Missed a Dose

If you miss a dose, do not take a double dose to make up for it. Take your next dose at the regular scheduled time. Contact your doctor or clinic if you are unsure about your dosing instructions.

Frequently Asked Questions (FAQs)

This medication can suppress your bone marrow, reducing the production of white blood cells, red blood cells, and platelets. Frequent blood tests allow your doctor to ensure these counts are safe; your dose may need to be adjusted or temporarily paused based on these results to prevent severe infections or bleeding.

Dosage is individualized based on factors such as your treatment regimen, blood counts, response to treatment, and how your body processes the medicine. TPMT and NUDT15 testing may be considered in patients with severe or repeated myelosuppression.

Allopurinol significantly increases mercaptopurine levels in your body and increases the risk of toxicity. Always tell your doctor if you are prescribed allopurinol (or other gout medications) before starting or while taking mercaptopurine, as your dose will need to be reduced significantly.

Watch for yellowing of the skin or the whites of your eyes (jaundice), dark-coloured urine, light-coloured stools, or persistent upper-right abdominal pain. If you notice any of these, contact your doctor immediately.

Treatment length depends on your diagnosis and treatment regimen. For acute leukaemia, mercaptopurine is commonly used as part of combination chemotherapy, including maintenance therapy for ALL

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