QT time prolongation
Adverse drug events
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Explanations of the substances for patients
We have no additional warnings for the combination of lumateperon and abarelix. Please also consult the relevant specialist information.
The reported changes in exposure correspond to the changes in the plasma concentration-time curve [ AUC ]. We do not expect any change in exposure for lumateperon, when combined with abarelix (100%). We do not expect any change in exposure for abarelix, when combined with lumateperon (100%).
The pharmacokinetic parameters of the average population are used as the starting point for calculating the individual changes in exposure due to the interactions.
Lumateperon has a low oral bioavailability [ F ] of 4%, which is why the maximum plasma level [Cmax] tends to change strongly with an interaction. The terminal half-life [ t12 ] is 18 hours and constant plasma levels [ Css ] are reached after approximately 72 hours. The protein binding [ Pb ] is 97.4% strong. which is why, with a mean hepatic extraction rate of 0.31, both liver blood flow [Q] and a change in protein binding [Pb] are relevant. The metabolism takes place via CYP1A2, CYP2C8 and CYP3A4, among others and the active transport takes place partly via UGT1A1 and UGT1A4.
The bioavailability of abarelix is unknown. The terminal half-life [ t12 ] is rather long at 316.8 hours and constant plasma levels [ Css ] are only reached after more than 1267.2 hours. The protein binding [ Pb ] is 97.5% strong. The metabolism via cytochromes is currently still being worked on.
|Serotonergic Effects a||0||Ø||Ø|
Rating: According to our knowledge, neither lumateperon nor abarelix increase serotonergic activity.
|Kiesel & Durán b||0||Ø||Ø|
Rating: According to our knowledge, neither lumateperon nor abarelix increase anticholinergic activity.
QT time prolongation
Rating: In combination, lumateperon and abarelix can potentially trigger ventricular arrhythmias of the torsades de pointes type.
General adverse effects
|Side effects||∑ frequency||lum||aba|
|Elevated creatine kinase||4.0 %||4.0||n.a.|
|Elevated transaminases||1.0 %||+||n.a.|
|Orthostatic hypotension||0.7 %||0.7||n.a.|
Neuroleptic malignant syndrome: lumateperon
Tardive dyskinesia: lumateperon
Based on your answers and scientific information, we assess the individual risk of undesirable side effects. These recommendations are intended to advise professionals and are not a substitute for consultation with a doctor. In the restricted test version (alpha), the risk of all substances has not yet been conclusively assessed.
No literature information available.