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Imatinib is a small molecule kinase inhibitor. Imatinib film-coated tablets contain equivalent amounts of imatinib mesylate. Imatinib doses are available in mg and mg. Its structural formula is
z Functional Therapy Editor
Gleevec is an indication approved by the Mainland Food and Drug Administration for the treatment of the accelerated chronic phase or blast phase of Philadelphia chromosome-positive chronic myelogenous leukemia (h+). . For the treatment of chronic phase accelerated or blast phase of Philadelphia chromosome-positive chronic myelogenous leukemia (h+)
For the treatment of adult patients with unresectable and/or metastatic malignant gastrointestinal stromal tumors for the following The safety and effectiveness information of the indications mainly comes from foreign research data. The Chinese population data are limited. It is used to treat adults with relapsed or refractory Philadelphia chromosome-positive acute lymphoblastic leukemia (h+). For the treatment of adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia associated with h-fusion kinase. Imatinib mesylate is the world's first approved inhibitor of tumorigenesis-related signaling for chronic myelogenous leukemia gastrointestinal stromal tumors. Treatment should be initiated initially by a physician experienced in treating chronic myelogenous leukemia. The recommended dose of imatinib mesylate for patients in blast phase and accelerated phase is /day. For patients in chronic phase who have failed interferon therapy, the recommended dose is once daily. It should be taken orally with a meal and drink a large glass of water. If effective, you should continue to take it. If the blood picture permits and there are no serious adverse drug reactions, the dose may be considered to be increased from / day to / day or from / day to / day (orally)
z Usage and dosage editing
Starting dose for chronic granuloma The recommended dose of imatinib mesylate for patients in the blast phase and accelerated phase of leukemia is/day. The recommended dose for patients in the chronic phase who have failed interferon therapy and for patients with malignant gastrointestinal stromal tumors that cannot be surgically removed or metastasized is/day. The average daily dose is 2 times a day. It should be taken orally with a meal and a large glass of water. It should be continued as long as it is effective.
If the blood picture permits and there are no serious adverse drug reactions, the dose may be considered to be increased from / day to / day or from / day to / day (taken in divided doses) if the disease progresses and treatment fails to be satisfactory after at least one month. The hematological response that had been achieved disappeared again.
In the following circumstances, the dose must be adjusted. If serious non-hematological adverse reactions (such as severe water retention) occur during treatment, the drug should be discontinued until the adverse reactions disappear, and then the dose should be adjusted according to the severity of the adverse reactions.
Dosage adjustments should be made in cases of severe liver toxicity and side effects, such as bilirubin elevation exceeding the upper limit of the normal range or transaminase elevation exceeding the upper limit of the normal range. It is advisable to discontinue the drug until the above indicators drop to or below the upper limit of the normal range respectively. .
Dose adjustment during neutropenia or thrombocytopenia During accelerated phase or blast crisis If severe neutropenia and thrombocytopenia occur (neutrophils less than ./ and/or platelets less than ./ or platelets less than ./ it is recommended that the dose be reduced to Day. If the blood cells continue to decrease for weeks, the dose should be further reduced to / day. If the blood cells continue to decrease for weeks, it is advisable to discontinue the drug until neutrophils / and platelets /. The dose for re-use is / day.
h After the failure of interferon treatment For patients in the chronic phase, when the neutrophil count is less than ./ and/or the platelet count is less than/, it is advisable to stop taking the drug only when the neutrophil count is less than ./ and the platelet count is . When resuming the drug, the dose is reduced to /day.
Dosage in patients with hepatic failure The plasma concentration of imatinib mesylate may increase in patients with hepatic impairment. Therefore, caution should be exercised when using this drug in these patients. Clinical data on the use of imatinib mesylate in patients with hepatic impairment do not allow for dose adjustment recommendations.
Dosage in patients with renal failure and elderly patients It is known that creatinine clearance decreases with age and age has a negative effect on imatinib mesylate. There is no significant effect on the pharmacokinetics of imatinib acid. Since clinical trials have not been conducted in patients with renal impairment, no dosage adjustment recommendations can be made