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Gleevec (imatinib mesylate) is a protein tyrosine kinase inhibitor use for treatment in cases of chronic-phase. Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in both children and adults. It may also be utilize for those with Ph+ CML that is in the accelerated phase. Or in blast crisis if prior treatment with interferon-alpha has proven to be unsuccessful. Additional uses of Gleevec include treating other variations of leukemia as well as skin cancer, stomach and other digestive tumors, and bone marrow disorders.

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Patients taking Gleevec should consume the medication orally either once daily.  (for the lower doses of 400 mg or 600 mg) Or twice daily for those who are require to take two doses of 400 mg to reach a total dosage of 800 mg daily. It should be consume with a meal as well as plenty of water. This medication should not be use on an empty stomach.

Individuals who experience difficulty with swallowing the tablets have the option of dispersing the medication in a glass of apple juice or water. For those who use this method of breaking down their medication for easier consumption. The Gleevec tablets should be stirred into either the water or apple juice until fully dissolve. The patient should immediately consume the suspension once prepared. The recommended ratio of liquid to medication is 2 oz/100 mg tablet or 7 oz/400 mg tablet.

Patients may expect a dose increase in instances of insufficient treatment results after multiple months of treatment, a reduction in results or improvement of their condition after having previously shown improvement with Gleevec, or a progression of their condition.

People taking a dose of 800 mg of Gleevec or more per day, depending on the severity of their condition, are often recommended to achieve this dosage using the 400 mg tablets of the medication to reduce iron exposure. Patients should not attempt to take eight of the 100 mg tablets of Gleevec to achieve the 800 mg dosage due to the coating on the tablets containing iron which may result in adverse effects from consuming too much of the mineral.

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Gleevec tablets should be stored between temperatures of 68°F (20°C) to 77°F (25°C). This medication may be exposed to temperatures as low as 59°F (15°C) and as high as 86°F (30°C) in some circumstances. However, exposure to temperatures outside of the recommended range is not suggested and may impact the integrity of the medication.

Keep this medication out of the reach of pets and children at all times.

Gleevec tablets should not be crushed, and all individuals should avoid contact with any tablets that have been crush as the medication may be dangerous when exposure occurs to one’s skin as well as the eyes, nose, or mouth. This includes breathing in any dust from crushed Gleevec tablets. Individuals that come into contact with crushed Gleevec tablets should wash the expose areas thoroughly.

Uses

Gleevec is prescribed for a variety of conditions, including but not limited to:

Acute lymphoblastic disorder.
Aggressive systemic mastocytosis.
Chronic eosinophilic leukemia.
Chronic myelogenous leukemia.
Dermatofibrosarcoma protuberans
Hypereosinophilic syndrome.
Leukemia.
Multiple myeloma.
Myelodysplastic disease.
Myeloproliferative disorder
Polycythemia vera.
Thrombocythemia

How Does Gleevec Work?

Gleevec functions as a protein tyrosine kinase inhibitor by blocking tyrosine kinase enzymes, which are responsible for cell growth, division, and communication. By inhibiting these particular enzymes, Gleevec is able to slow or halt the growth and spread of cancerous cells.

The main enzymes targeted by Gleevec include those associates with the KIT protein, SCF (stem cell factor), PDGF (platelet-derived growth factor), and BCR-ABL protein. These proteins are those most commonly associated with conditions such as acute lymphoblastic leukemia (ALL), gastrointestinal stromal tumors, chronic myelogenous leukemia (CML), and certain skin cancers.

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Gleevec is available in two different strengths:

100 mg tablets (film-coated)
400 mg tablets (film-coated)

Most individuals of adult age with CML in its chronic phase are prescribe a dosage of 400 mg per day, whereas patients with CML in blast crisis or its accelerating phase will often be requires to take 600 mg per day. Adults using Gleevec for the treatment of Ph+ ALL that is refractory or in relapse will generally be prescribe a daily dose of 600 mg.

Adult patients who are prescribed Gleevec for myelodysplastic or myeloproliferative disorders are most commonly prescribed a dose of 400 mg per day for treatment.

The recommended daily dose of Gleevec for adult patients with hypereosinophilic syndrome or chronic eosinophilic leukemia is 400 mg per day. Those with FIP1L1-PDGFR? fusion kinase will typically start treatment with Gleevec at a lower dose of 100 mg per day that may be increased as needed.

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Patients with aggressive systemic mastocytosis will typically be prescribed a dose of 400 mg per day for both those who have not had a sufficient response to prior therapy options as well as those without the D816V c-Kit mutation. A daily dose of 100 mg per day is recommended for those who have ASM that is linked to eosinophilia or that have hematological conditions associated with the fusion kinase FIP1L1-PDGFR?. These individuals may also have their dosage increased to 400 mg per day if they show sufficient tolerance to Gleevec in regard to adverse reactions along with the need for a higher dose of the medication to achieve a positive response.

Adult patients with dermatofibrosarcoma protuberans most commonly are treated with a daily dose of 800 mg of Gleevec per day.

Patients with gastrointestinal stromal tumors are typically prescribed a daily dose of 400 mg of Gleevec when the condition is adjuvant. When metastatic or unresectable, the prescribed dosage of Gleevec may vary between 400 mg per day up to 800 mg per day (taken as a twice-daily dose of the 400 mg tablets) when required based on the progression of the disease as well as a decent tolerance for any adverse side effects.

Pediatric patients with a new diagnosis of Ph+ CML should not exceed 600 mg of Gleevec per day. The best dosage for this age group is 340 mg/m2/day, and it may be administers once per day in a single dose or split into two doses taken once in the morning and once in the evening.

Overdose

Individuals who have overdosed on Gleevec or suspect they may have taken too much of the medication should seek emergency medical attention immediately or call their local Poison Control Center.

A single dose of 8 g to 10 g of Gleevec has been reported to result in gastrointestinal pain and vomiting.

A patient who ingested a single dose of 6,400 mg experienced abdominal pain, facial swelling, a decrease in neutrophil count, nausea, pyrexia, vomiting, and an increase in transaminases.

Prolonge overdosage of Gleevec (such as 1,800 mg to 3,200 mg of Gleevec ingest for a period of six days) has been shown to result in gastrointestinal pain, an increase in bilirubin, an increase in CPK, myalgia, and weakness.

A duration of one to ten days with ingestion of overdose levels of 1,200 mg to 1,600 mg of Gleevec has been shown to result in symptoms such as abdominal pain, a decrease in appetite, fatigue, edema, headache, muscle spasms, diarrhea, nausea, swelling, vomiting, pancytopenia, and thrombocytopenia.

Side Effects

The most common side effects of taking Gleevec are as follows:

Abdominal pain
Blurred vision.
Diarrhea
Dizziness.
Fatigue or unusual tiredness
Fluid retention.
Gas
Hair loss
Joint pain
Muscle pain.
Nausea
Rash.
Sinus pain.
Stuffy nose
Vomiting.

Some of the eye-related side effects associated with Gleevec use include the following:

Bleeding in the eye
Cataract development.
Eye irritation
Dryness of the eyes.
Blurry vision.
Glaucoma
Infections (e.g., pink eye).
A red spot developing on the sclera.

Please contact your doctor for further information if you experience any of the following additional side effects. Also,  have any concerns, as the following symptoms are considers serious and may impact treatment with this medication:

Bloody or black stools.
Dark-colored urine
Easy bleeding or bruising.
Extreme fatigue
Fluid-filled blisters.
Flu-like symptoms that are severe
Gastrointestinal bleeding.
Headaches that are notably severe.
Jaundice (yellowing of the eyes or skin).
Rapid heart rate.
Rashes with severe blistering.
Severe rashes on the skin.
Shortness of breath.
Swelling around the eyes.
Swelling of the lower legs
Symptoms of impaired immunity.
Unusual or sudden weight gain.
Vomit that resembles coffee grounds.
Weakness.

If you experience any of the following symptoms of an allergic reaction. Stop taking Gleevec immediately and seek out emergency medical care:

Swelling of the tongue, mouth, lips, or throat.
Difficulty breathing.
Swelling under the skin of the hands, feet, or eyelids.
Itching.
Rash
Skin flushing.

Due to some of the potential side effects of taking Gleevec, patients are advise to avoid exposure to individuals who have infections or are otherwise sick. Avoid any activities that may have an increased risk of causing injury or bleeding. So, exercise caution when operating a motor vehicle or any other equipment before knowing how Gleevec will impair their ability to concentrate and perform such tasks.

Patients are also advise to exercise caution when using marijuana or consuming alcohol due to the dizziness. And drowsiness that already occurs with Gleevec. The use of alcohol while taking this medication should be limited. So,  patients should discuss any prior or ongoing cannabis or alcohol use when being prescribed Gleevec.

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