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imatinib imatinib

 
  Trade/other name(s)
Gleevec, Glivec, STI 571, STI-571, imatinib mesylate
 
  Pronunciation: im-mat-uh-nib  
  Why would this drug be used?
This drug is used to treat some types of leukemia (especially chronic myelogenous leukemia, or CML), as well as gastrointestinal stromal tumors (GISTs). It is also being studied for use against a number of other cancers and non-cancerous conditions.
 
  How does this drug work?
Imatinib is a type of targeted therapy known as a tyrosine kinase inhibitor. Its targets include tyrosine kinase proteins called BCR-ABL and c-kit. These abnormal proteins are found on or near the surface on some cancer cells. They are always "turned on", sending constant messages telling the cells to divide and stay alive. By blocking these messages, imatinib stops the cancer cells from making more cells and causes them to die.
 
  Before taking this medicine

Tell your doctor:
 
 
  • If you are allergic to any medicines, dyes, additives, or foods.
  • If you have any type of liver disease (including hepatitis). This drug is cleared from the body mainly by the liver. Reduced liver function might result in more drug than expected staying in the body, which could lead to unwanted side effects. Your doctor may need to adjust your dose accordingly.
  • If you have congestive heart failure. Some early reports have suggested that this drug may contribute to heart failure or make existing conditions worse.
  • If you have any other medical conditions such as kidney disease, heart disease, diabetes, gout, or infections. These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you are taking the blood-thinning medicine warfarin (Coumadin) - see interactions below.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. This drug can cause problems with the fetus if taken at the time of conception or during pregnancy. If you're sexually active while taking this drug, you should use some kind of birth control. It is important to check with your doctor about what kinds of birth control can be used with this medicine. In pregnant women, treatment with this drug should be used only if the potential benefit to the mother outweighs the risk to the fetus.
  • If you are breast-feeding. While no studies have been done, this drug may pass into breast milk and affect the baby. Breast-feeding is not recommended during treatment with this drug.
  • If you think you might want to have children in the future. This drug may affect fertility. Talk with your doctor about the possible risk with this drug and the options that may preserve your ability to have children.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs.
 
  Interactions with other drugs
Imatinib can interact with a number of drugs and supplements, which may either raise or lower the level of imatinib in your blood. Tell your doctor if you are taking any of the following: rifampin, phenytoin, phenobarbital, St. John’s wort, carbamazepine, itraconazole, ketoconazole, dexamethasone, nefazodone, erythromycin, clarithromycin, ritonavir (or other drugs for HIV or AIDS). Other medicines may also have this effect.

Imatinib can alter the blood levels of other drugs, including acetaminophen (Tylenol), birth control pills, cyclosporin, some calcium channel blockers (amlodipine, nifedipine) and some cholesterol-lowering drugs (simvastatin, pravastatin, atorvastatin, etc.). Tell your doctor if you are taking any of these medicines.

Imatinib can also change the blood levels of warfarin (Coumadin). If you are taking this drug to help prevent blood clots, your doctor may need to switch you to another medicine during treatment with imatinib.

Check with your doctor, nurse, or pharmacist about any other medicines, herbs, and supplements you are taking, and whether alcohol can cause problems with this medicine.

 
  Interactions with foods
Grapefruit or grapefruit juice may change the level of imatinib in your blood. Check with your doctor, nurse, or pharmacist about whether these or other foods may be a problem.
 
 
Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.


 
  How is this drug taken or given?
Imatinib is a capsule taken by mouth. It is usually taken once a day. At higher doses, you may be asked to split the dose in half, taking it once in the morning and once later in the day. It can cause stomach irritation if taken on an empty stomach, so it should be taken with a meal and a full glass of water. The dose depends on the reason you are taking it and on other factors such as your liver function and blood counts.

Store the medicine in a tightly closed container away from heat and moisture and out of the reach of children and pets.

 
  Precautions
This drug may interact with a number of other drugs or supplements in the body, especially warfarin (Coumadin). See interactions above. Be sure your doctor is aware of all drugs and supplements you are taking.

You may have nausea and vomiting on the day you receive this drug or in the first few days afterward. Your doctor may give you medicine before your treatment to help prevent nausea and vomiting. You may also get a prescription for an anti-nausea medicine that you can take at home. It is important to have these medicines on hand and to take them as prescribed by your doctor.

This drug may cause diarrhea. If left unchecked, this could lead to dehydration and chemical imbalances in the body. Your doctor will likely prescribe medicine to help prevent or control this side effect. It is very important that you take this medicine as prescribed. Make sure you get the medicine right away, so that you will have it at home when you need it.

Imatinib may cause fluid buildup in the chest or abdomen and swelling around the eyes or in the hands or feet (edema). Some early reports have suggested this may be due the effects of this drug on the heart. Tell your doctor or nurse right away if you are gaining weight, develop swelling around your eyes or in your hands or feet, notice swelling in your abdomen, or have trouble breathing (shortness of breath).

Imatinib may affect your liver, which could increase liver enzyme levels in your blood. Your doctor will likely check your liver function with blood tests on a regular basis. The drug may need to be stopped or the dose changed if the effects are severe. If you have liver problems before starting treatment, the doctor may need to monitor you more carefully.

While taking this medicine, and a few days afterward, there is a small chance of a serious skin reaction. Symptoms often start as a skin rash with redness or blistering in the mouth, nose, or eyes, along with fever and body aches. If this happens, call your doctor right away.

Your doctor will likely test your blood throughout your treatment, looking for possible effects of the drug on blood counts or on blood chemistry levels. Based on the test results, you may be given medicines to help treat any effects. Your doctor may also need to reduce or delay your next dose of this drug, or even stop it altogether.

This drug can lower your white blood cell count, especially in the weeks after the drug is given. This can increase your chance of getting an infection. Be sure to let your doctor or nurse know right away if you have any signs of infection, such as fever, chills, pain when passing urine, new onset of cough, or bringing up sputum.

This drug may lower your platelet count in the weeks after it is given, which can increase your risk of bleeding. Speak with your doctor before taking any drugs or supplements that might affect your body's ability to stop bleeding, such as aspirin or aspirin-containing medicines, warfarin (Coumadin), or vitamin E. Tell your doctor right away if you have unusual bruising, or bleeding such as nosebleeds, bleeding gums when you brush your teeth, or black, tarry stools.

Do not get any immunizations (vaccinations), either during or after treatment with this drug, without your doctor's OK. This drug may affect your immune system, which could make vaccinations ineffective, or could even lead to serious infections. Try to avoid contact with people who have recently received a live virus vaccine, such as the oral polio vaccine or smallpox vaccine.

 
 
Possible side effects
 
  Common
  • nausea*
  • vomiting*
  • swelling around the eyes or feet (edema)*
  • weight gain
  • diarrhea*
  • muscle aches and pains
  • skin rash
  • tiredness (fatigue)
  • headache
  • joint and bone pain
  • abdominal pain
 
  Less common
  • low platelet count with increased risk for bleeding*
  • low white blood cell count with increased risk for infection*
  • fluid buildup in the lining of the lungs (pleural effusion), heart (pericardial effusion), or abdomen (ascites)*
  • heartburn
  • itching
  • shortness of breath
  • constipation
  • low blood level of potassium
 
  Rare
  • abnormal blood tests which suggest that the drug is affecting the liver (Your doctor will discuss the importance of this finding, if any.)*
  • serious skin reactions*
  • low red blood cell count
  • congestive heart failure (can cause shortness of breath or swelling in hands or feet)

*See "Precautions" section for more detailed information.

 
 
There are other side effects not listed above that can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.
 
 
 
  FDA approval
Yes - first approved in 2001.
 
 
 
  Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.  


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