reactions. Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. Maprotiline has been reported to prolong the QT interval, particularly in overdose or with higher-dose prescription therapy (elevated serum concentrations). Cases of long QT syndrome and TdP tachycardia have been described with maprotiline use, but rarely occur when the drug is used alone in normal prescribed doses and in the absence of other known risk factors for QT prolongation. Limited data are available regarding the safety of maprotiline in combination with other QT-prolonging drugs. Concomitant use may increase the risk for QT prolongation. Ribociclib is also a moderate CYP3A4 inhibitor and maprotiline is a CYP3A4 substrate.
Maraviroc: (Moderate) Use caution if coadministration of ribociclib with maraviroc is necessary, as the systemic exposure of maraviroc may be increased resulting in increase in treatment-related adverse reactions. Ribociclib is a moderate CYP3A4 inhibitor and maraviroc is a CYP3A4 substrate.
Medroxyprogesterone: (Moderate) Use caution if coadministration of ribociclib with medroxyprogesterone is necessary, as the systemic exposure of medroxyprogesterone may be increased resulting in an increase in treatment-related adverse reactions. Ribociclib is a moderate CYP3A4 inhibitor. Medroxyprogesterone is metabolized primarily by hydroxylation via a CYP3A4.
Mefloquine: (Major) Avoid coadministration of ribociclib with mefloquine due to an increased risk for QT prolongation. Systemic exposure of mefloquine may also be increased resulting in increase in treatment-related adverse reactions. Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. There is evidence that the use of halofantrine after mefloquine causes a significant lengthening of the QTc interval. Mefloquine alone has not been reported to cause QT prolongation. However, due to the lack of clinical data, mefloquine should be used with caution in patients receiving drugs that prolong the QT interval. Ribociclib is also a moderate CYP3A4 inhibitor and mefloquine is a CYP3A4 substrate.
Meperidine; Promethazine: (Major) Avoid coadministration of ribociclib with promethazine due to an increased risk for QT prolongation. Ribociclib has been shown to prolong the QT interval in a concentration-dependent manner. Promethazine, a phenothiazine, is associated with a possible risk for QT prolongation. Concomitant use may increase the risk for QT prolongation.
Mephobarbital: (Major) Avoid coadministration of ribociclib with mephobarbital, as the systemic exposure of ribociclib may be decreased resulting in decreased efficacy; consider an alternative treatment with less potential to induce CYP3A. Ribociclib is extensively metabolized by CYP3A4. Mephobarbital is metabolized to phenobarbital, a strong CYP3A4 inducer.
Metaproterenol: (Minor) Coadministration may result in additive effects on the QT interval. Beta-agonists may be associated with adverse cardiovascular effects including QT interval prolongation, usually at higher doses, when associated with hypokalemia, or when used with other drugs known to prolong the QT interval such as ribociclib. This risk may be more clinically significant with long-acting beta-agonists as compared to short-acting beta-agonists.
Metformin; Pioglitazone: (Moderate) Coadminister ribociclib and pioglitazone with caution, as the systemic exposure of pioglitazone may be inc |
