Examples of using Netupitant in English and their translations into German
{-}
-
Colloquial
-
Official
-
Ecclesiastic
-
Medicine
-
Financial
-
Ecclesiastic
-
Political
-
Computer
-
Programming
-
Official/political
-
Political
Netupitant is not mutagenic.
The active substances are palonosetron and netupitant.
Netupitant is not a substrate for P-gp.
Renal excretion for netupitant is negligible.
Netupitant and combination with palonosetron.
In vitro data show that netupitant is a P-gp inhibitor.
Netupitant is a selective antagonist of human substance P/neurokinin 1(NK1) receptors.
Akynzeo contains the active substances netupitant and palonosetron.
Neither netupitant nor palonosetron have been evaluated in patients with end-stage renal disease.
It is unknown whether palonosetron or netupitant are excreted in human milk.
Netupitant doses up to 600 mg and palonosetron doses up to 6 mg have been used in clinical studies without any safety concerns.
In vitro data suggests that netupitant inhibits the efflux of transporter BCRP.
No consistent effect was seen with cyclophosphamide after netupitant co- administration.
At a dose of 300 mg in humans, netupitant is a substrate and moderate inhibitor of CYP3A4.
The ratios were time dependent with values decreasing gradually beyond 24 h post-dose,indicating that netupitant is being rapidly metabolized.
In vitro data shows that netupitant inhibits UGT2B7, the magnitude of such an effect in the clinical setting is not established.
No specific studies were performed to evaluate netupitant in patients with renal impairment.
Furthermore, netupitant may also affect the efficacy of chemotherapeutic agents that need activation by CYP3A4 metabolism.
However, due to the large volume of distribution of palonosetron and netupitant, dialysis is unlikely to be an effective treatment for overdose.
Netupitant is mainly metabolized by CYP3A4; therefore, co-administration with medicinal products that inhibit or induce CYP3A4 activity may influence plasma concentrations of netupitant.
Because of the antiemetic activity of netupitant and palonosetron, emesis induced by a medicinal product may not be effective.
Administration of theCYP3A4 inducer rifampicin with Akynzeo alone decreased the AUC of netupitant 5.2 fold and Cmax 2.6 fold.
Reproductive studies in animals with netupitant do not indicate direct or indirect harmful effects with respect to fertility, parturition or postnatal development.
Administration of the CYP3A4 inhibitor ketoconazole with Akynzeo increased the AUC of netupitant fold and Cmax 1.3 fold when compared to the administration of Akynzeo alone.
Absolute netupitant bioavailability data are not available in humans; based on data from two studies with intravenous netupitant, the bioavailability in humans is estimated to be greater than 60.
The medicines in Akynzeo attach to the receptors in the nervous systemthrough which serotonin and substance P work: netupitant(an NK1 receptor antagonist) blocks the receptors for substance P, and palonosetron(a 5- HT3 receptor antagonist) blocks certain receptors for serotonin.
The pharmacokinetics of palonosetron or netupitant has not been studied in subjects with end-stage renal disease requiring hemodialysis and no data on the effectiveness or safety of Akynzeo in these patients are available.
Following administration of a single dose of Akynzeo, netupitant is eliminated from the body in a multi-exponential fashion, with an apparent mean elimination half-life of 88 hours in cancer patients.
Co-administration of a single dose of 300 mg netupitant with a dexamethasone regimen(20 mg on Day 1, followed by 8 mg twice daily from Day 2 to Day 4) significantly increased the exposure to dexamethasone in a time and dose dependent manner.
Non-clinical studies indicate that netupitant and its metabolites and the combination with palonosetron only at very high concentrations may block ion channels involved in ventricular de- and re- polarisation and prolong action potential duration.