Примери за използване на Rolapitant на Английски и техните преводи на Български
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Complete Response Rolapitant.
Rolapitant is a moderate CYP2D6 inhibitor.
The active substance is rolapitant.
Rolapitant is an inhibitor of P-glycoprotein(P-gp).
There are no data on the presence of rolapitant in human milk.
Rolapitant is eliminated primarily through the hepatobiliary route.
Varuby contains the active substance rolapitant.
Unchanged rolapitant or M19 were not found in pooled urine sample.
There are no available data on rolapitant use in pregnant women.
Rolapitant was highly protein bound to human plasma(99.8%).
The exposure ratio of M19 to rolapitant was approximately 50% in plasma.
Rolapitant is metabolised by CYP3A4 to form a major active metabolite, M19.
In vitro studies suggest that rolapitant is not an inhibitor of CYP2E1.
Rolapitant is slowly eliminated with a mean terminal half-life of approximately 7 days.
The active substance in Varuby, rolapitant, works by blocking neurokinin-1(NK1) receptors.
Rolapitant did not affect the fertility or general reproductive performance of male rats.
In a population pharmacokinetic analysis of rolapitant, the Vd/F was 387 L in cancer patients.
Rolapitant is an inhibitor of Breast-Cancer-Resistance Protein(BCRP).
Because of the antiemetic activity of rolapitant, emesis induced by a medicinal product may not be effective.
Rolapitant doses up to 720 mg have been used in clinical studies without any safety concerns.
There is no medicinal product interaction between rolapitant and dexamethasone, so no dosage adjustment for dexamethasone is required.
Rolapitant is eliminated mainly through the hepatobiliary route, with minor contributions from renal elimination.
In a population pharmacokinetic analysis the apparent total clearance(CL/F) of rolapitant was 0.96 L/hour in cancer patients.
In vivo, rolapitant is not expected to exhibit any inhibitory or inducing effect on CYP3A4.
No clinically significant effect was seen on the pharmacokinetics of rolapitant when ketoconazole, a strong CYP3A4 inhibitor was administered with rolapitant.
Rolapitant displays linear PK with exposures increased in a dose-proportional manner.
Concomitant administration of rifampicin,a strong enzyme inducer significantly decreased the systemic exposure to rolapitant and to its active metabolite.
The safety and efficacy of rolapitant in children and adolescents below 18 years of age has not yet been established.
Drug metabolising enzymes(and drug transporters)other than CYP3A4 involved in rolapitant hepatobiliary elimination remain to be elucidated.
In pooled samples collected over 2 weeks, 8.3% of the dose was recovered in the urine primarily as metabolites and37.8% of the dose was recovered in the feces primarily as unchanged rolapitant.