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Imatinib (Gleevec®

 

Warning:  Gleevec is associated with a number of Warnings and Precautions which require medical supervision throughout the treatment. Severe fluid retention has occurred in certain cancer patients. When Gleevec is combined with certain chemotherapy drugs liver toxicity and liver failure can also occur. Monitoring of liver function is recommended during the treatment.

 

Clinical cases of hypothyroidism (the thyroid gland does not make enough thyroid hormone) have been reported in a specific group of patients during treatment with Gleevec. If you have thyroid problem, it is very important that you talk to your oncologist before taking this medication.

 

Indications: Children and adults who are battling certain types of leukemia and cancer such as gastrointestinal stromal tumors, chronic myeloid leukemia, Philadelphia chromosome positive, relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia, and myelodysplastic/myelodyproliferative diseases are prescribed this drug.  Imatinib is a kinase inhibitor and stops the proteins found in cancer cells from giving the cells the nourishment they need to grow.  While protein is found in all human cells, it is found in greater numbers in cancer cells and is one of the factors that lead to cancer cells being able to multiply faster than normal cells.  Medical study shows that this drug actually helps slow down and destroy cancer cells.

The side effects for this drug include headaches, vomiting, loss of appetite, swelling of arms and legs, nausea, diarrhea, muscular pain, itchiness, fluid retention, dizziness, and even a rash.  More serious side effects include loss of platelets, lower counts in white or red blood cells, bleeding in the intestines/stomach/brain, fluid in the lungs, infections, reduced liver functioning, and heart failure.  If you are experiencing fever, persistent sore throat, or other signs of an infection, call your doctor immediately.

 

Dosage: Imatinib comes as a tablet to be taken by mouth . Most patients on the medication take it as a tablet and the dosage can range between 300mg and 800 mg, depending on the disease or cancer being treated.  If you have problems with swallowing, you can put the tablet into juice or water so that it can dissolve.  This drug should always be taken with food or water and it is important to read all of the directions that come with the prescription. 

The dosage you are recommended to take varies depending on your body surface area (BSA), general state of your health, whether you are taking other drugs or not, and the type of cancer being treated. Regardless of dosage indicated, it is necessary to take the medication as prescribed by your health care provider.  

Storage:  storeImatinib at room temperature (15-25 ° C), away from heat above 40 ° C, light and moisture. Keep the medication out of the reach of children. Imatinib and other drugs should not be used beyond the expiration date printed on the container.  

Overdose:  Imatinib overdose can cause life threatening problems. Chemotherapy drugs including Imatinib tend to damage the bone marrow, and lead to a decrease in white blood cells and platelets, which can cause serious infections in some patients. If you take a Imatinib overdose, contact your doctor or the poison control center nearest you immediately.  

Missing dose: take Imatinib and all medications as prescribed.  In case you forget to take a dose, take the missed one as soon as you remember it. However, if it is almost time for your next dose,  do not double the next dose to recover the missing; it can be dangerous. Contact your doctor or wait to go back to your regular schedule. This applies not only to Imatinib  but also any other drug.

Mechanism of action (MOA): Imatinib is an anticancer drug belongs to the family of tyrosine kinase inhibitors. It works by preventing the development, and selectively inducing cancer cell death. 

Interactions:   If you are taking Imatinib, you need to avoid drinking grapefruit juice as it can increase the level of side effects that you experience.  Your doctor should have a complete listing of all herbs, prescription drugs, and non-prescription drugs that you are taking.  Some drugs are known to interfere with this drug’s effectiveness on cancer cells and patients have experienced blood concentration drops or rises.  Drugs that are known to affect this drug include St. John’s Wort, Zocor, Phenobarbital, Viracept, Primidone, Norvir, Crixivan, Sporanox, Reyataz, and Invirase.

 

Contradindications:  Imatinib can hurt fetuses so it is important to notify your doctor if you are pregnant or intending to become pregnant.  Nursing mothers should also not use this drug as it can be passed to the baby through breast milk.  Your doctor should be made aware to any previous health conditions such as bleeding problems, heart problems, kidney issues, and liver problems.

 

Side effects: while attacking cancer cells,Imatinib also affects healthy cells, which lead to development of adverse effects in most patients; most common Imatinib side effects include

  • hair loss
  • fatigue
  • headache
  • muscle cramps and pain
  • nausea and vomiting
  • decreased appetite
  • weight loss
  • mouth blistering
  • drying or darkening of the skin or nails
  • joint pain
  • night sweats
  • teary eyes
  • Bowel disorders (diarrhea, indigestion, constipation and diarrhea).  

You need to see a medical spcialist as soon as you can if you develop any of these adverse reactions:

  • fever
  • chills
  • dizziness
  • shortness of breath
  • puffy face
  • fainting
  • chest pain
  • weight gain
  • blood in the stool
  • severe depression symptoms

 

  • yellowing of the skin or eyes
  • swelling of the hands, feet, ankles, or lower legs
  • fast or irregular heartbeat
  • difficulty falling asleep or staying asleep
  • persistent coughing associated with bloody mucus
  • urgent need to urinate, especially at night
  • unusual bruising or bleeding
  • Excessive tiredness or weakness 
  • skin problems such as rash or blisters

 

 

References:

http://www.fda.gov/Safety/MedWatch/SafetyInformation/Safety-RelatedDrugLabelingChanges/ucm122980 .htm