Gleevec 100mg Tablets

Imatinib is a small molecule tyrosine kinase inhibitor that selectively inhibits the Bcr-Abl tyrosine kinase, which is the oncogenic driver in Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL). It also inhibits the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-Kit, which are involved in the pathogenesis of gastrointestinal stromal tumors (GIST) and other diseases.

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of infection: fever, chills, severe sore throat, ear or sinus pain, cough, increased or changed sputum production, painful urination, mouth sores, or a wound that won't heal.
Signs of bleeding: vomiting or coughing up blood, coffee ground-like vomit, blood in the urine, black, red, or tarry stools, bleeding gums, abnormal vaginal bleeding, unexplained bruises or bruises that get bigger, or uncontrollable bleeding.
Signs of electrolyte problems: mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance changes, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting.
Signs of kidney problems: inability to urinate, changes in urine production, blood in the urine, or significant weight gain.
Chest pain or pressure.
Abnormal burning, numbness, or tingling sensations.
Changes in vision, eye pain, or severe eye irritation.
Depression.
Bone pain.

Fluid Retention and Heart Failure

This medication may cause fluid retention, leading to swelling and weight gain. If you experience swelling, weight gain, or breathing difficulties, inform your doctor. Heart failure has been reported in patients taking this medication, including those with pre-existing heart disease. If you have heart disease, notify your doctor. Seek immediate medical attention if you experience shortness of breath, significant weight gain, abnormal heartbeat, or new or worsening swelling in your arms or legs.

Liver Problems and Tumor Lysis Syndrome

Severe and potentially life-threatening liver problems have been associated with this medication. If you notice signs of liver problems, such as dark urine, fatigue, decreased appetite, nausea, stomach pain, light-colored stools, vomiting, or yellow skin and eyes, contact your doctor immediately. Patients with cancer taking this medication may be at increased risk of developing tumor lysis syndrome (TLS), a potentially life-threatening condition. If you experience a rapid or abnormal heartbeat, fainting, difficulty urinating, muscle weakness or cramps, nausea, vomiting, diarrhea, or loss of appetite, seek medical attention right away.

Severe Skin Reactions

This medication may cause severe skin reactions, including Stevens-Johnson syndrome (SJS) and other serious conditions that can affect internal organs and be life-threatening. If you experience signs such as red, swollen, blistered, or peeling skin, red or irritated eyes, sores in your mouth, throat, nose, eyes, genitals, or skin, fever, chills, body aches, shortness of breath, or swollen glands, seek medical help immediately.

Other Side Effects

Most medications can cause side effects, but many people experience none or only mild effects. If you encounter any of the following side effects or any other symptoms that bother you or don't go away, contact your doctor:

Hair loss.
Muscle spasms.
Dizziness, drowsiness, fatigue, or weakness.
Sleep disturbances.
Gas.
Headaches.
Dry skin.
Watery eyes.
Changes in taste.
Nose or throat irritation.
Back, muscle, joint, arm, or leg pain.
Weight gain.
Night sweats.
Anxiety.
Stomach pain or heartburn.
Constipation, diarrhea, nausea, vomiting, and decreased appetite are common side effects. If you experience these, discuss ways to manage them with your doctor. If these effects bother you, don't improve, or are severe, seek medical attention.

Reporting Side Effects

These are not all possible side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you are currently taking warfarin.
If you are taking any of the following medications: carbamazepine, dexamethasone, phenobarbital, phenytoin, rifabutin, rifampin, or St. John's wort.
If you are breastfeeding. Note that you should not breastfeed while taking this medication or for 1 month after your last dose.

This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require alertness or clear vision, such as driving, wait until you understand how this drug affects you.

Regular blood tests and other laboratory evaluations should be performed as directed by your doctor. Additionally, avoid consuming grapefruit and grapefruit juice, as they may interact with this medication. This drug can potentially suppress the bone marrow's ability to produce necessary blood cells, leading to an increased risk of bleeding problems, infections, or anemia. If you have concerns, discuss them with your doctor.

You may be more susceptible to infections; therefore, practice good hygiene by washing your hands frequently and avoiding close contact with individuals who have infections, colds, or flu. Furthermore, this medication can increase your risk of bleeding easily, so exercise caution to prevent injuries. Use a soft-bristled toothbrush and an electric razor to minimize the risk of bleeding. If you have had your thyroid removed, consult your doctor about the need for more frequent blood tests.

Before receiving any vaccinations, consult your doctor, as certain vaccines may not be effective or may increase the risk of infection when taken with this medication. You may also be more prone to sunburn; thus, limit your exposure to the sun, sunlamps, and tanning beds, and use protective measures such as sunscreen, clothing, and eyewear.

There is a risk of severe and potentially life-threatening gastrointestinal tract perforation associated with this drug. Discuss this risk with your doctor. If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

In some cases, this drug may affect growth in children and adolescents, and regular growth checks may be necessary. Discuss this with your doctor. This medication can cause harm to an unborn baby. A pregnancy test will be conducted before initiating treatment to confirm that you are not pregnant. If you may become pregnant, use effective birth control during treatment and for at least 2 weeks after your last dose. If you become pregnant, notify your doctor immediately.

• Strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital, St. John's Wort): May significantly decrease imatinib plasma concentrations, leading to loss of efficacy.
• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, grapefruit juice): May significantly increase imatinib plasma concentrations, increasing risk of toxicity.
• Warfarin: Imatinib may increase anticoagulant effect of warfarin due to inhibition of CYP2C9 and CYP2D6.

• CYP3A4 substrates with narrow therapeutic index (e.g., cyclosporine, pimozide, ergot alkaloids, triazolobenzodiazepines): Imatinib may increase their concentrations.
• Other TKIs: Potential for additive toxicities or altered pharmacokinetics.
• Paracetamol (acetaminophen): Potential for increased hepatotoxicity with high doses or prolonged use of imatinib.

• Proton Pump Inhibitors (PPIs) and H2-receptor antagonists: May slightly decrease imatinib absorption due to pH elevation, but generally not clinically significant for standard dosing.

• Fatigue
• Nausea
• Vomiting
• Diarrhea
• Muscle cramps
• Rash
• Edema (swelling, especially around eyes or ankles)
• Weight gain
• Fever
• Unusual bleeding or bruising
• Shortness of breath
• Chest pain
• Yellowing of skin or eyes (jaundice)
• Dark urine
• Abdominal pain

Imatinib can cause fetal harm when administered to a pregnant woman. Based on animal studies and its mechanism of action, imatinib is expected to cause fetal harm. Advise pregnant women of the potential risk to the fetus. Advise females of reproductive potential to use effective contraception during treatment and for at least 14 days after the last dose. Advise males with female partners of reproductive potential to use effective contraception during treatment and for at least 14 days after the last dose.

Imatinib and its active metabolite are excreted into human milk. Due to the potential for serious adverse reactions in the breastfed infant, advise women not to breastfeed during treatment with imatinib and for at least 14 days after the last dose.

Dosing is established for pediatric patients with CML and Ph+ ALL. Safety and efficacy in other indications have not been established. Monitor growth and development in pediatric patients receiving long-term treatment.

No specific dose adjustment is required based on age. However, elderly patients may be more susceptible to certain adverse effects such as fluid retention and myelosuppression. Monitor closely for adverse reactions.

• Always take imatinib with a meal and a large glass of water to minimize gastrointestinal irritation and improve absorption.
• Monitor patients closely for fluid retention (edema, pleural effusion, ascites, pericardial effusion), especially in the first year of treatment. Promptly manage with diuretics or other supportive measures.
• Regular monitoring of CBC and LFTs is crucial due to the risk of myelosuppression and hepatotoxicity.
• Imatinib is a substrate and inhibitor of CYP3A4; significant drug interactions can occur with strong CYP3A4 inducers or inhibitors. Review concomitant medications carefully.
• Patients should be advised to report any signs of infection, unusual bleeding/bruising, or severe muscle cramps/pain.
• For patients with difficulty swallowing, tablets can be dispersed in a large glass of water or apple juice (for 100mg tablets, 50mL; for 400mg tablets, 200mL). Stir until completely dispersed and drink immediately.

• Dasatinib (Sprycel)
• Nilotinib (Tasigna)
• Bosutinib (Bosulif)
• Ponatinib (Iclusig)
• Omacetaxine (Synribo) - for CML
• Chemotherapy (for ALL, MDS/MPD)
• Surgery (for GIST, DFSP)

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.