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Kisqali FeMara Co-Pack(Ribociclib And Letrozole Tablets)(七十)
2017-08-12 06:51:49 来源: 作者: 【 】 浏览:31852次 评论:0
The systemic exposure of suvorexant may be increased during concurrent use resulting in an increase in treatment-related adverse reactions.
Tacrolimus: (Major) Avoid coadministration of ribociclib with tacrolimus due to an increased risk for QT prolongation and torsade de pointes (TdP). Systemic exposure of tacrolimus may also be increased resulting in an increase in tacrolimus-related adverse reactions. Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. Tacrolimus has also been associated with QT prolongation. Concomitant use may increase the risk for QT prolongation. Ribociclib is also a moderate CYP3A4 inhibitor and tacrolimus is a sensitive CYP3A4 substrate with a narrow therapeutic window.
Tadalafil: (Moderate) Use caution if ribociclib is coadministered with tadalafil, as the systemic exposure of tadalafil may be increased resulting in adverse events such as hypotension, syncope, visual changes, and prolonged erection. Ribociclib is a moderate CYP3A4 inhibitor, and tadalafil is a CYP3A4 substrate. Administration with a strong CYP3A4 inhibitor increased the AUC and Cmax after a single dose of tadalafil 10 mg by 107% and 15%, respectively; the AUC and Cmax after a 20 mg dose of tadalafil increased by 312% and 22%, respectively. Moderate CYP3A4 inhibitors may also increase tadalafil exposure.
Tamoxifen: (Major) Avoid coadministration of tamoxifen with ribociclib due to an increased risk of QT prolongation; reduced tamoxifen efficacy and/or increased tamoxifen toxicity is also possible. If coadministration is unavoidable, monitor for altered tamoxifen efficacy, increased tamoxifen-related adverse effects, and evidence of QT prolongation. Tamoxifen has been reported to prolong the QT interval, usually in overdose or when used in high doses. Rare case reports of QT prolongation have also been described when tamoxifen is used at lower doses. Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. These ECG changes occurred within the first four weeks of treatment and were reversible with dose interruption. Ribociclib may reduce the conversion of tamoxifen to other potent active metabolites via inhibition of CYP3A4. (Major) Letrozole should not be given concurrently with tamoxifen; when administered together, there is an average 38% reduction in letrozole plasma concentrations. Letrozole therapy after the completion of standard tamoxifen treatment is not associated with impaired effects of letrozole.
Tamsulosin: (Moderate) Use caution if coadministration of ribociclib with tamsulosin is necessary, especially at a tamsulosin dose higher than 0.4 mg, as the systemic exposure of tamsulosin may be increased resulting in increase in treatment-related adverse reactions including hypotension, dizziness, and vertigo. Ribociclib is a moderate CYP3A4 inhibitor and tamsulosin is a CYP3A4 substrate. The effect of concomitant use of a moderate CYP3A4 inhibitor with tamsulosin has not been eva luated; however, administration with a strong CYP3A4 inhibitor significantly increased the AUC and Cmax of tamsulosin.
Tasimelteon: (Moderate) Use caution if coadministration of ribociclib with tasimelteon is necessary, as the systemic exposure of tasimelteon may be increased resulting in increase in treatment-related adverse reactions. Ribociclib is a moderate CYP3A4 inhibitor and tasimelteon is a CYP3A4 substrate. Administration with a strong CYP3A4 inhibitor increased the AU
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