Imatinib drug interactions

Patients are placed on imatinib at the time of diagnosis. Patients should be monitored for a dose-dependent myelo-suppression, Cl intolerance, edema, and rash. Drug interactions with CYP450 3A4 inducers are clinically important and should be monitored. 

Haouala A et al (2011) Drug interactions with the tyrosine kinase inhibitors imatinib, dasatinib, and nilotinib. Blood 117 e75-e87... 

Sheth SR, Hicks K, Ippoliti C, Giralt, Champlin RE, Anderlini P, Safety, tolerability, and drug interactions of adjuvant imatinib mesylate (Gleevec) within the first 100 days following stem cell transplantation (SCT) in patients with Ph+ CML and PH+ ALL at high risk for recurrence. Blood Q.002) 100, Abstract 2500,... 

Drug-drug interactions Imatinib Peripheral neuropathy is uncommon in imatinib-treated patients and has previously been reported only during combination therapy with cytotoxic agents that affect microtubule function, such as vinca alkaloids and taxanes. A suspected adverse interaction with amlodipine has been reported, with a temporal association between amlodipine and symptoms of imatinib toxicity [21 ]. 

Extraction recovery >90%. The method can be routinely used in pharmacokinetic and drug interaction studies. An LC-MS-MS method used in a pharmacokinetic study where imatinib mesylate (Glivec) and its main metabohte (CGP74588) were measured in blood samples of a patient with end-stage renal disease on hemodialysis and compared with... 

Numerous drugs may interact with imatinib, discuss with prescriber... 

Sunirinib (Sutent) [Kinase Inhibitor] Uses Advanced GI stromal tumor refractory/intolerant of imatinib advanced RCC Action Kinase inhibitor Dose Adults. 50 mg PO daily x 4 wk, followed by 2 wk holiday = 1 cycle 4- to 37.5 mg w/ CYP3A4 inhibitors (Table VI-8), to T 87.5 mg w/ CYP3A4 inducers Contra w/ atazanavir Caution [D, -] Multiple interactions require dose modification (eg, St. John s wort) Disp Caps SE -l WBC pit, bleeding, T BP, -l ejection fraction, T QT interval, pancreatitis, DVT, Sz, adrenal insuff, N/V/D, skin discoloration, oral ulcers, taste perversion, hypothyroidism Interactions Multiple interactions require dose modification (eg, St. John s wort) EMS Monitor ECG for T QT interval grapefruit juice may T adverse effects may affect potassium level (hypo-/hyperkalemia) monitor for S/Sxs of heart failure drug can 4- ejection fraction OD May cause abd pain, muscle weakness, and chills symptomatic and supportive... 

E Itraconazole. Imatinib is primarily metabolized by the CYP3A4 hepatic enzyme system. Drugs that may inhibit this enzyme (such as ketoconazole, itraconazole, erythromycin, clarithromycin, etc.) may impair clearance of imatinib and result in increased toxicity. Imatinib itself is also a fairly potent inhibitor of the CYP3A4 enzyme and may result in toxicity due to other drugs that are substrates for this enzyme (such as simvastatin, warfarin, benzodiazepines, etc.). The other medications iisted are uniikeiy to affect the function of 0 P3A4 or interact adversely with imatinib. 

The UK manufacturer of aprepitant recommends caution when it is used with antineoplastics that are metabolised by CYP3A4, particularly irinotecan, because of the possibility of increased toxicity with this drug. They also mention that etoposide, vinoreibine, docetaxel, paclitaxel, ifosfamide, imatinib, vinblastine and vincristine, were given without dosage adjustment for potential interactions, but as this was not a formal interaction study they recommend caution. However, with intravenous docetaxel, it appears that no important changes in pharmacokinetics occur, and therefore dosage adjustments are unlikely to be needed for this drug,... 

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