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Drug Interactions between imatinib and rivaroxaban

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

imatinib rivaroxaban

Applies to: imatinib and rivaroxaban

MONITOR: Coadministration with moderate or potent inhibitors of CYP450 3A4 may increase the plasma concentrations of rivaroxaban, which is a substrate of the isoenzyme. This interaction is not expected to be clinically significant in patients with normal renal function, but may be important in patients with renal impairment. When a single dose of rivaroxaban was coadministered with the moderate CYP450 3A4 inhibitor, fluconazole, rivaroxaban peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 30% and 40%, respectively. These increases are within the magnitude of the normal variability of Cmax and AUC and are not considered clinically relevant. However, the magnitude of interaction may be greater in patients with renal impairment. Even in the absence of concomitant CYP450 3A4 inhibitors, rivaroxaban AUC was increased 1.4-, 1.5- and 1.6 fold in individuals with mild (CrCl 50 to 80 mL/min), moderate (CrCl 30 to 49 mL/min) and severe (CrCl 15 to 29 mL/min) renal impairment, respectively, compared to healthy subjects with normal renal function (CrCl 80 mL/min or greater). Overall inhibition of factor Xa activity increased by a factor of 1.5, 1.9 and 2.0, and prolongation of PT was similarly increased by a factor of 1.3, 2.2 and 2.4, respectively. There are no data in patients with CrCl below 15 mL/min.

MANAGEMENT: In patients with significant renal impairment (e.g., CrCl between 15 to 50 mL/min), the use of rivaroxaban with moderate or potent inhibitors of CYP450 3A4 should be approached with caution. Patients should be routinely evaluated for signs and symptoms suggesting blood loss such as a drop in hemoglobin and/or hematocrit, hypotension, or fetal distress (in pregnant women). Renal function should also be assessed periodically, and treatment with rivaroxaban discontinued if acute renal failure develops. Due to the lack of clinical data, rivaroxaban is not recommended in patients with CrCl below 30 mL/min when used for the prophylaxis of deep vein thrombosis and in patients with CrCl below 15 mL/min when used for reducing the risk of stroke and systemic embolism in nonvalvular atrial fibrillation.

References (3)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. Cerner Multum, Inc. "Australian Product Information."
  3. (2008) "Product Information. Xarelto (rivaroxaban)." Bayer Inc

Drug and food interactions

Moderate

imatinib food

Applies to: imatinib

GENERALLY AVOID: Coadministration of imatinib with strong CYP450 3A4 inhibitors such as grapefruit juice, may significantly increase the plasma concentrations of imatinib, a known substrate of CYP450 3A4. The proposed mechanism is inhibition of CYP450 3A4-mediated metabolism of imatinib by certain compounds present in grapefruits. Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability). In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition. Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict. In a single-dose study, coadministration of imatinib with ketoconazole (a strong CYP450 3A4 inhibitor) increased imatinib peak plasma concentration (Cmax) and systemic exposure (AUC) by 26% and 40%, respectively.

MANAGEMENT: Patients treated with imatinib should preferably avoid the consumption of grapefruit or grapefruit juice. If coadministration is unavoidable, monitor for prolonged and/or increased pharmacologic effects of imatinib, including edema, hematologic toxicity and immunosuppression.

References (3)
  1. (2022) "Product Information. Gleevec (imatinib)." Novartis Pharmaceuticals
  2. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  3. Cerner Multum, Inc. "Australian Product Information."

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

See also

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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