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 lofexidine 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 lofexidine, when combined with abarelix (100%). We do not expect any change in exposure for abarelix, when combined with lofexidine (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.
Lofexidine has a mean oral bioavailability [ F ] of 72%, which is why the maximum plasma levels [Cmax] tend to change with an interaction. The terminal half-life [ t12 ] is 12 hours and constant plasma levels [ Css ] are reached after approximately 48 hours. The protein binding [ Pb ] is rather weak at 55%. Since the substance has a low hepatic extraction rate of 0.16, displacement from protein binding [Pb] in the context of an interaction can lead to increased exposure. The metabolism mainly takes place via CYP2D6.
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 lofexidine nor abarelix increase serotonergic activity.
|Kiesel & Durán b||0||Ø||Ø|
Rating: According to our knowledge, neither lofexidine nor abarelix increase anticholinergic activity.
QT time prolongation
Rating: In combination, lofexidine and abarelix can potentially trigger ventricular arrhythmias of the torsades de pointes type.
General adverse effects
|Side effects||∑ frequency||lof||aba|
|Orthostatic hypotension||35.5 %||35.5||n.a.|
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.
Abstract: No Abstract available