MERCAPTOPURINE
Background and Date of Approval
Mercaptopurine is an anticancer medicine belonging to the purine antagonist class. The U.S. FDA approved it on 28th April 2014 for treating acute lymphoblastic leukaemia.
Uses
Mercaptopurine is used in the treatment of acute lymphoblastic leukaemia.
How is it administered?
Mercaptopurine is to be administered orally. Swallow the whole tablet with water. If you forgot to take the tablet, simply take your next dose at the scheduled time. Do not take a double dose to make up for a forgotten dose. You must take these tablets at least 1 hour before or 2 hours after having milk or dairy products.
Side Effects
The common side effects that are likely to occur while you are on the treatment with mercaptopurine are nausea, vomiting, anaemia, fever or infection (sore throat, sore mouth, or urinary problems), unexplained bruising or bleeding, low white blood cell and platelet count. If you experience any allergic or unusual reactions after taking this medicine, report to your doctor immediately.
Warnings
If you are going to have a vaccination, speak to your doctor or nurse before you have it. When you take this drug, you should not have a live vaccine (like polio, measles, mumps and rubella.) until advised it is safe to do so by your doctor. This is because some vaccines may give you an infection if you have them while you are taking this drug. Do not get vaccinated with yellow fever vaccine while you are taking this drug because it may lead to serious illness. Your doctor may also ask for other blood and urine tests to monitor how your kidneys are working and to measure uric acid levels. Uric acid is a natural substance made in your body and levels of uric acid can rise while you are taking this drug. High levels of uric acid may damage your kidneys, so your doctor may sometimes change your dose of the drug as a result of these tests. It is probably advisable to start with lower doses 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.
Precautions
This drug is not recommended during pregnancy as it causes harm to the unborn baby. Tell your healthcare provider before beginning this treatment if you are pregnant or planning to have a baby. It is advised for both men and women to follow proper contraceptive methods during and for 3 months after the last dose of Mercaptopurine. During the treatment, your doctor may periodically monitor your white blood cell counts, platelets, blood sugar, electrolytes and kidney parameters to prevent serious complications. Inform to the doctor if you have been diagnosed with liver disorders, heart failure, high blood cholesterol levels, or hypertension before starting this treatment.This medicine has the potential to cause liver problems, so your doctor will carry out weekly liver function tests when you are taking this drug. Report to your doctor if you experience any hypersensitive reactions like itchy skin or rashes, while taking this medicine. This tablet contains lactose as an inactive ingredient in which the body is unable to digest lactose, a sugar found in milk and dairy products. It can cause symptoms such as bloating, and abdominal pain. If you have lactose intolerance, inform your doctor before starting this therapy.
Word of Advice
Consult your physician if you experience fever, sore throat, jaundice, nausea, vomiting, signs of local infection, bleeding from any site, or symptoms suggestive of anaemia. Women of childbearing potential should avoid becoming pregnant. This medicine is not recommended for pregnant women as it may cause fetal harm. Consult your doctor if you are pregnant or planning for pregnancy during treatment. This medicine passes into breast milk; breastfeeding is not recommended during treatment. Limit alcohol intake or avoid it altogether during treatment. While taking this drug, you are more sensitive to the sun and UV light. Limit your exposure to sunlight and UV light, wear protective clothing, and use a sun cream with a high sun protection factor (SPF). Low blood sugar (sweating more than usual, nausea, dizziness, confusion, etc.) has sometimes been observed in children, mainly in children under the age of six or with a low body mass index. Inform your child's doctor if this occurs.
References
Aspen Pharma Trading Limited, Electronic medicines compendium (EMC), [ Revised on August 2019] (Accessed: April 6, 2023), https://www.medicines.org.uk/emc/files/pil.4655.pdf Purinethol® (mercaptopurine) 50-mg scored tablets caution. Available at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/009053s032lbl.pdf (Accessed: April 6, 2023). Goodman & Gilmanâs, The Pharmacological Basis of Therapeutics, Cytotoxic agents, 12th edition, 2011, 1701 - 1702. KD Tripathi, Essentials of Medical Pharmacology, Anticancer drugs, 7th edition, 2013, 863.
Frequently Asked Questions
What happens if you take Mercaptopurine with milk?
Taking Mercaptopurine with milk may decrease the absorption and effectiveness of the medication. This is because the calcium in milk can bind to mercaptopurine, forming an insoluble complex that reduces the amount of the drug that can be absorbed by the body.
Can I drink alcohol while taking Mercaptopurine?
It is generally advised to avoid drinking alcohol while taking Mercaptopurine , as alcohol can increase the risk of liver damage.
What is the complication of Mercaptopurine?
Mercaptopurine can also cause more serious complications, such as bone marrow suppression, which can lead to decreased production of blood cells and an increased risk of infections, bleeding, and anaemia.
Which enzyme is responsible for metabolism of Mercaptopurine?
The metabolism of Mercaptopurine involves several enzymes, including thiopurine S-methyltransferase (TPMT), and xanthine oxidase (XO). Among these enzymes, TPMT is primarily responsible for the metabolism of mercaptopurine. TPMT converts mercaptopurine into 6-methylmercaptopurine, which is then further metabolised into inactive compounds that are excreted from the body.
What is the recommended dose of this drug?
For the treatment of acute lymphoblastic leukaemia (ALL), the recommended dose for adults and children is approximately 1.5 to 2.5 milligrams per kilogram of body weight taken orally once a day, usually in combination with other chemotherapy medications.
What you should know while taking Mercaptopurine ?
You should have caution while taking this Mercaptopurine , it can cause liver problems like jaundice, hepatomegaly and anorexia.