Imatinib belongs to a family of medications called protein tyrosine kinase inhibitors. It is used to treat adults and children who have been newly diagnosed with Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase. It works by affecting enzymes that play a role in certain cancer cells.
It is also used to treat adults with Ph+ CML in blast crisis (sudden attack), accelerated phase (fast growth), or chronic phase (long-term illness) after the failure of interferon-alpha therapy.
It is used to treat adults who have been newly diagnosed with certain types of acute lymphoblastic leukemia (Philadelphia-positive – Ph+ ALL). It is also used to treat Ph+ ALL that have not responded to other medications. Imatinib is also used to treat dermatofibrosarcoma protuberans (DFSP), a cancer where tissue under the skin grows out of control, when it cannot be removed by surgery or it is spreading to other parts of the body.
Other types of cancers can also be treated with imatinib. Imatinib may be used to treat certain types of gastrointestinal stromal tumours (GIST), a cancer of the stomach and bowels. Imatinib may also be used to treat some types of myelodysplastic/myeloproliferative diseases (MDS/MPD), aggressive systemic mastocytosis (ASM), hypereosinophilic syndrome (HES), and chronic eosinophilic leukemia (CEL). In these conditions, different types of blood cells start growing out of control.
This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.
Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.
Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.
Each dark-yellow-to-brownish-orange, round, film-coated tablet, debossed with "IT" and "1" divided by the score line on one side, contains 100 mg of imatinib (as mesylate). Nonmedicinal ingredients: anhydrous dibasic calcium phosphate, crospovidone, magnesium stearate; coating: iron oxide yellow, iron oxide red, macrogol, polyvinyl alcohol, talc, and titanium dioxide.
Each dark-yellow-to-brownish-orange, oblong, film-coated tablet debossed with "IT" and "4" divided by the score line on one side, contains 400 mg of imatinib (as mesylate). Nonmedicinal ingredients: anhydrous dibasic calcium phosphate, crospovidone, magnesium stearate; coating: iron oxide yellow, iron oxide red, macrogol, polyvinyl alcohol, talc, and titanium dioxide.
Treatment with imatinib should be started under the direct supervision of a physician experienced in the treatment of the conditions for which this medication is being used.
Doses for children are based on body size and will be calculated by your child’s doctor.
For newly diagnosed chronic myeloid leukemia (CML) or chronic phase CML, the usual adult dose of imatinib is 400 mg daily. The usual adult dose in accelerated phase or blast crisis CML is 600 mg daily. Depending on how you respond to the treatment and on the side effects you experience, you doctor may increase your dose to 800 mg daily.
For cancerous gastrointestinal stromal tumours (GIST), the usual adult dose ranges from 400 mg to 600 mg daily. Dose adjustments may be required depending on your response and on the side effects you experience. The usual dose for adults at intermediate to high risk of relapse of GIST is 400 mg taken once daily.
For Ph+ ALL, the usual adult dose is 600 mg daily.
For MDS/MPD in adult patients, the starting dose is 400 mg daily.
For some types of ASM, HES, or CEL, the starting dose is 100 mg daily. Depending on how you respond to the treatment and on the side effects you experience, you doctor may increase your dose to 400 mg daily.
For DFSP in adult patients, imatinib is taken as 800 mg daily. Doses of 800 mg should be taken as 400 mg twice a day, in the morning and evening.
Imatinib should be taken by mouth, with a meal and a large glass of water. Avoid drinking grapefruit juice while you are taking imatinib. Swallow the tablets whole.
If you are not able to swallow the tablet(s) whole, the tablet(s) may be dissolved in a glass of water or apple juice. Stir with a spoon to completely disintegrate. This liquid must be swallowed immediately. Rinse the glass with the same fluid and drink this as well.
Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.
It is important that this medication be taken exactly as prescribed by your doctor. If you miss a dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one. If you are not sure what to do after missing a dose, contact your doctor or pharmacist for advice. If you vomit after taking a dose, do not take a replacement dose. Take your next dose at the usual time.
Store this medication at room temperature, in its original package, protect it from light and moisture, and keep it out of the reach of children.
Do not dispose of medications in wastewater (e.g. down the sink or in the toilet) or in household garbage. Ask your pharmacist how to dispose of medications that are no longer needed or have expired.
Do not take this medication if you are allergic to imatinib or any ingredients of the medication.
This medication should not be used except under direct supervision by an experienced physician.
Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.
The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.
The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.
Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.
Although most of the side effects listed below don’t happen very often, they could lead to serious problems if you do not check with your doctor or seek medical attention.
Check with your doctor as soon as possible if any of the following side effects occur:
Stop taking the medication and seek immediate medical attention if any of the following occur:
Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.
Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.
Anemia: Imatinib may cause low levels of red blood cells. If you experience symptoms of reduced red blood cell count (anemia) such as shortness of breath, feeling unusually tired, or pale skin, contact your doctor as soon as possible.
Your doctor will do blood tests regularly to monitor the number of specific types of blood cells, including red blood cells, in your blood.
Bleeding: Imatinib may cause a reduced number of platelets in the blood, which can make it difficult to stop cuts from bleeding. If you notice any signs of bleeding, such as frequent nosebleeds, unexplained bruising, or black and tarry stools, notify your doctor as soon as possible. Your doctor will order routine blood tests to make sure potential problems are caught early.
Drowsiness/reduced alertness: This medication is not expected to make you drowsy and impair your ability to drive or use machinery. However, it may make some people feel weak. Do not drive or use machinery until you know how this medication affects you.
Fluid retention: This medication can cause serious fluid retention. If you experience unexpected rapid weight gain or swelling in your feet, ankles, lower legs, or hands, contact your doctor immediately. Your doctor will weigh and monitor you regularly for signs of fluid retention while you are taking this medication.
Grapefruit juice: Grapefruit juice affects how imatinib is removed from the body and may cause too much of the medication to build up in the body. Do not drink grapefruit juice while taking this medication.
Heart problems and heart failure: Rarely, heart problems including heart failure, have been reported with the use of imatinib. If you are at risk for heart problems such as heart failure (e.g., people with high blood pressure, diabetes, and coronary artery disease), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Contact your doctor immediately if you have symptoms of heart failure such as leg swelling, chest pain, or shortness of breath.
Hepatitis B: People who have hepatitis B or have had hepatitis B infection are at risk of the infection returning when they are taking imatinib or after stopping the medication. If you have a history of hepatitis B infection, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Infection: As well as killing cancer cells, imatinib can reduce the number of cells that fight infection in the body (white blood cells). If possible, avoid contact with people with contagious infections. Tell your doctor immediately if you notice signs of an infection, such as fever or chills, severe diarrhea, shortness of breath, prolonged dizziness, headache, stiff neck, weight loss, or listlessness. Your doctor will do blood tests regularly to monitor the number of specific types of blood cells in your blood.
Kidney function: Decreased kidney function or kidney disease may cause this medication to build up in the body, causing side effects. If you have kidney problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.
Liver function: Imatinib may affect liver function. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function with blood tests regularly while you are taking this medication.
If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.
Male fertility: There is evidence that men who take imatinib may experience decreased fertility. If this is a concern, speak to your doctor about fertility preservation.
Muscle effects: In rare cases, serious muscle damage has been associated with the use of this medication. Report any unexplained muscle pain, tenderness, weakness or cramps, or any brown or discoloured urine to your doctor immediately, particularly if you are also experiencing malaise (a general feeling of being unwell) or fever.
Stomach problems: Imatinib may cause stomach irritation or bleeding. To reduce stomach irritation, take this medication with food and a large glass of water. If you experience signs of stomach bleeding (e.g., severe stomach pain, black stools, vomiting blood, dizziness), get immediate medical attention.
Thyroid: If you have hypothyroidism due to removal of thyroid gland, you may need closer monitoring of your thyroid levels. Let your doctor know if you are experiencing unusual tiredness, weight gain, hair loss, unusually dry skin, mood changes, and intolerance to cold temperatures.
Tumour lysis syndrome: Imatinib, like many other cancer medications, causes many cancer cells to be suddenly killed when treatment is first started. This can overwhelm the body with waste products from the cells. As a result, the body may not be able to keep up with getting rid of all the waste. When this happens, you may experience nausea and shortness of breath, and notice cloudy urine or joint pain. This is called tumour lysis syndrome. Your doctor may prescribe some medications to help your body get rid of the waste products. Make sure you understand how to use these medications and report any of these signs or symptoms to your doctor immediately.
Pregnancy: This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. Women of childbearing age who are taking imatinib should use an effective method of birth control during treatment.
Breast-feeding: This medication passes into breast milk. If you are a breast-feeding mother and are taking imatinib, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.
Children: The safety and effectiveness of using this medication have not been established for children less than 2 years of age. Growth may be slowed in children and adolescents that take this medication.
Seniors: Seniors have a greater risk of fluid retention than younger patients. Contact your doctor if you experience a sudden increase in weight or swelling of the ankles, lower legs, or hands. Your doctor will weigh and monitor you closely.
There may be an interaction between imatinib and any of the following:
If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:
An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.
Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications that you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.
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