natgillin/translations-raw huggingface dataset:
In 2 multicenter, randomized, double-blind, active comparator-controlled, parallel-group phase III clinical studies, aprepitant was compared with ondansetron for the prevention of postoperative nausea and vomiting in 1,658 patients undergoing open abdominal surgery.
V 2 multicentričnih, randomiziranih, dvojno slepih, z učinkovino nadzorovanih kliničnih študijah paralelnih skupin faze III, so pri preprečevanju pooperacijske navzee in bruhanja aprepitant primerjali z ondansetronom pri 1. 658 bolnikih z operacijo na odprti trebušni votlini.
The majority of patients were women (> 90%), mainly undergoing gynaecological surgery.
Večina bolnikov je bila žensk (> 90%), pretežno po prestanih ginekoloških operativnih posegih.
Patients were randomized to receive 40 mg aprepitant, 125 mg aprepitant, or 4 mg ondansetron.
Bolniki so bili ramdominizirani tako, da so prejeli bodisi 40 mg aprepitanta, 125 mg aprepitanta ali 4 mg ondansetrona.
Aprepitant was given orally (PO) with 50 ml of water 1 to 3 hours before anesthesia.
Aprepitant so prejeli peroralno (PO) s 50 ml vode 1 do 3 ure pred anestezijo.
Ondansetron was given intravenously immediately before induction of anesthesia.
Ondansetron so prejeli intravensko neposredno pred uvodom v anestezijo.
The results show that a higher percentage of post-surgical patients experienced complete response (no emesis and no use of rescue) with aprepitant 40 mg than with ondansetron 4 mg (lower bound of C. I. is 0.0 indicating borderline significance) as described in Table 1.
6 Rezultati, prikazani v preglednici 1 kažejo, da je imelo popoln odziv (brez bruhanja in brez rešilnega zdravljenja) večji odstotek post- operativnih bolnikov v skupini, ki je prejemala aprepitant 40 mg, kot v skupini, ki je prejemala ondansetron 4 mg (spodnja meja intervala zaupanja (IZ) je 0, 0 kar kaže na mejno signifikantnost):
6 Table 1 Percent of Post-Operative Patients Responding by Treatment Group Combined Results from 2 Phase III Trials
Preglednica 1 Odstotek bolnikov z odzivom po operaciji glede na skupino zdravljenja Kombinirani rezultati dveh študij faze III
Aprepitant 40 mg PO (N=541)
Aprepitant 40 mg p. o (N=541)
Ondansetron 4 mg IV (N=526)
Ondansetron 4 mg i. v (N=526)
Percentage Point Difference (%) § and 95% C. I. #
Razlika v odstotkih (%) § in 95% IZ #
95% C. I.
95% IZ
Complete Response (0-24 hours) † †
Popoln odziv (0- 24 ur) †
258/ 526
298/ 541 (55, 1) 258/ 526 (49, 0)
Complete Response:
† Popoln odziv:
No emesis and no use of rescue § Difference (%) calculated as Aprepitant 40 mg minus Ondansetron 4 mg # Difference (%) and 95% C. I. calculated using stratified Miettinen-Nurminen method using Cochran-Mantel- Haenszel weights
Brez bruhanja in brez rešilnega zdravljenja § Razlika (%) izračunana kot aprepitant 40 mg minus ondansetron 4 mg # Razlika (%) in 95% IZ izračunan z uporabo stratificirane Miettinen- Nurminen metode in Cochran- Mantel- Haeszel mer
The reduction in risk for a vomiting episode over the 0 to 24 hour period with aprepitant 40 mg relative to ondansetron 4 mg was 53.3% (95% C. I.:
53, 3% (95% IZ:
35.3 to 66.3) in an analysis that censors patients at the time of rescue use.
35, 3 do 66, 3) v analizi, ki nadzoruje bolnike v času rešilnega zdravljenja.
Absorption The mean absolute oral bioavailability of aprepitant is 67% for the 80 mg capsule and 59% for the 125 mg capsule.
Absorpcija Povprečna absolutna biološka uporabnost po peroralnem zaužitju 80 mg kapsule aprepitanta je 67%, pri 125 mg kapsuli pa 59%.
Following oral administration of a single 40 mg dose of EMEND in the fasted state, the AUC0-∞ (mean ± SD) was 8.0 ± 2.1 microgram x h/ ml and the Cmax was 0.7 ± 0.24 microgram/ ml.
Po peroralnem dajanju enkratnega 40 mg odmerka zdravila EMEND na tešče je bila AUC0- ∞ (povprečje±SD) 8, 0±2, 1 mikrogramov x h/ ml, Cmax pa 0, 7±0, 24 mikrogramov/ ml.
The median tmax was 3.0 hours.
Srednji Tmax je bil 3, 0 ure.
Concomitant intake of a 40 mg dose with a standard breakfast decreased the aprepitant Cmax by 18% but did not affect AUC.
Pri jemanju 40 mg odmerka skupaj z običajnim zajtrkom se zmanjša le Cmax aprepitanta za 18%, AUC pa se ne spremeni.
This is not considered to be clinically important.
Menimo, da ta vpliv nima kliničnega pomena.
Distribution Aprepitant is highly protein bound, with a mean of 97%.
Porazdelitev Aprepitant se močno veže na beljakovine, povprečno 97- odstotno.
The geometric mean apparent volume of distribution at steady state (Vdss) is approximately 66 l in humans.
Geometrični srednji navidezni volumen porazdelitve v stanju dinamičnega ravnovesja (Vdss) je pri ljudeh približno 66 l.
Metabolism Aprepitant undergoes extensive metabolism.
Presnova Aprepitant se v veliki meri presnavlja.
In healthy young adults, aprepitant accounts for approximately 19% of the radioactivity in plasma over 72 hours following a single intravenous administration 100 mg dose of [14C]-fosaprepitant, a prodrug for aprepitant, indicating a substantial presence of metabolites in the plasma.
Pri zdravih mladih preiskovancih je, 72 ur po eni intravenski infuziji 100 mg odmerka [14C] fosaprepitanta, predzdravila aprepitanta, približno 19% radioaktivnosti v plazmi prispeval aprepitant, kar kaže na znatno prisotnost presnovkov v plazmi.
Elimination Aprepitant is not excreted unchanged in urine.
7 Izločanje Aprepitant se ne izloča nespremenjen z urinom.
Following a single intravenously administered 100 mg dose of [14C]-fosaprepitant, a prodrug for aprepitant to healthy subjects, 57% of the radioactivity was recovered in urine and 45% in faeces.
Pri zdravih preiskovancih se je po enem intravenskem odmerku fosaprepitanta 100 mg, predzdravila [14C] aprepitanta, 57% radioaktivnosti izločilo v urinu, 45% pa v blatu.
7 The plasma clearance of aprepitant is dose-dependent, decreasing with increased dose and ranged from approximately 60 to 72 ml/ min in the therapeutic dose range.
V območju terapevtskih odmerkov znaša od približno 60 do 72 ml/ min.
The terminal half-life is approximately 9 hours after administration of a single 40 mg dose.
Terminalni razpolovni čas je znašal približno 9 ur po zaužitju enkratnega 40 mg odmerka.
Pharmacokinetics in special populations Elderly:
Starostniki:
Following oral administration of a single 125 mg dose of aprepitant on Day 1 and 80 mg once daily on Days 2 through 5, the AUC0-24hr of aprepitant was 21% higher on Day 1 and 36% higher on Day 5 in elderly (≥ 65 years) relative to younger adults.
Po enem peroralnem odmerku 125 mg aprepitanta prvi dan ter 80 mg enkrat na dan od drugega do petega dne je bil AUC0– 24 h aprepitanta pri starejših preiskovancih (≥ 65 let) višji kot pri mlajših odraslih preiskovancih, in sicer prvi dan za 21%, peti dan pa za 36%.
The Cmax was 10% higher on Day 1 and 24% higher on Day 5 in elderly relative to younger adults.
Cmax je bila pri starejših preiskovancih prvi dan za 10% višja, 5. dan pa za 24% višja kot pri mlajših odraslih preiskovancih.
These differences are not considered clinically meaningful.
Menimo, da te razlike nimajo kliničnega pomena.
No dosage adjustment for EMEND is necessary in elderly patients.
Odmerka zdravila EMEND pri starostnikih ni treba prilagoditi.
Following oral administration of a single 125 mg dose of aprepitant, the Cmax for aprepitant is 16% higher in females as compared with males.
Po enem peroralnem odmerku 125 mg aprepitanta je Cmax aprepitanta pri ženskah za 16% višja kot pri moških.
The half-life of aprepitant is 25% lower in females as compared with males and its tmax occurs at approximately the same time.
Razpolovna doba aprepitanta je pri ženskah za 25% nižja kot pri moških, tmax pa je približno enak.
These differences are not considered clinically meaningful.
Velja ocena, da te razlike nimajo kliničnega pomena.
No dosage adjustment for EMEND is necessary based on gender.
Odmerka zdravila EMEND ni treba prilagoditi glede na spol.
Mild hepatic impairment (Child-Pugh class A) does not affect the pharmacokinetics of aprepitant to a clinically relevant extent.
Blaga okvara jeter (razred A po Child- Pugh- ovi klasifikaciji) na farmakokinetiko aprepitanta ne vpliva v tolikšni meri, da bi bilo to klinično pomembno.
Conclusions regarding the influence of moderate hepatic impairment (Child-Pugh class B) on aprepitant pharmacokinetics cannot be drawn from available data.
Iz razpoložljivih podatkov ni mogoče sklepati, kakšen je vpliv zmerne okvare jeter (razred B po Child- Pugh- ovi klasifikaciji) na farmakokinetiko aprepitanta.
There are no clinical or pharmacokinetic data in patients with severe hepatic impairment (Child-Pugh class C).
Kliničnih podatkov o farmakokinetiki aprepitanta pri bolnikih s hudo okvaro jeter (razdred C po Child- Pugh- ovi klasifikaciji) ni.
A single 240 mg dose of aprepitant was administered to patients with severe renal impairment (CrCl < 30 ml/ min) and to patients with end stage renal disease (ESRD) requiring haemodialysis.
Bolnikom s hudo okvaro ledvic (očistek kreatinina < 30 ml/ min) ter bolnikom s končno odpovedjo ledvic, ki se zdravijo s hemodializo, so dali po en sam odmerek 240 mg aprepitanta.
In patients with severe renal impairment, the AUC0-∞ of total aprepitant (unbound and protein bound) decreased by 21% and Cmax decreased by 32%, relative to healthy subjects.
Pri bolnikih s hudo okvaro ledvic je bil AUC0– ∞ celokupnega aprepitanta (nevezanega in vezanega na beljakovine) za 21% manjši, Cmax pa je bila za 32% nižja kot pri zdravih preiskovancih.
In patients with ESRD undergoing haemodialysis, the AUC0-∞ of total aprepitant decreased by 42% and Cmax decreased by 32%.
Pri bolnikih s končno odpovedjo ledvic, ki se zdravijo s hemodializo, je bil AUC0– ∞ celokupnega aprepitanta za 42% manjši, Cmax pa je bila za 32% nižja.
Due to modest decreases in protein binding of aprepitant in patients with renal disease, the AUC of pharmacologically active unbound aprepitant was not significantly affected in patients with renal impairment compared with healthy subjects.
Zaradi nekoliko manjše vezave aprepitanta na beljakovine pri bolnikih z okvaro ledvic, se AUC farmakološko aktivnega nevezanega aprepitanta v primerjavi z zdravimi preiskovanci ni bistveno spremenil.
Haemodialysis conducted 4 or 48 hours after dosing had no significant effect on the pharmacokinetics of aprepitant; less than 0.2% of the dose was recovered in the dialysate.
Hemodializa, opravljena 4 ali 48 ur po odmerjanju, ni pomembno vplivala na farmakokinetiko aprepitanta; v dializatu se je izločilo manj kot 0, 2% odmerka.
No dose adjustment for EMEND is necessary for patients with renal impairment or for patients with ESRD undergoing haemodialysis.
Pri bolnikih z okvaro ledvic in pri bolnikih s končno odpovedjo ledvic, ki se zdravijo s hemodializo, odmerka ni treba prilagoditi.
Relationship between concentration and effect (PK/ PD) Using a highly specific NK1-receptor tracer, positron emission tomography (PET) studies in healthy young men have shown that aprepitant penetrates into the brain and occupies NK1 receptors in a dose- and plasma-concentration-dependent manner.
Razmerje med koncentracijo in učinkom (PK/ PD) S študijami pozitronske emisijske tomografije (PET) pri mladih odraslih moških so z uporabo visoko specifičnega označevalca receptorjev NK1 ugotovili, da aprepitant prodre v možgane in zasede receptorje NK1, pri čemer je stopnja zasedenosti odvisna od odmerka in plazemske koncentracije.
Aprepitant plasma concentrations achieved with the 3- day regimen of EMEND are predicted to provide greater than 95% occupancy of brain NK1 receptors.
Predvidevajo, da plazemske koncentracije aprepitanta, ki jih dosežemo s 3 dni trajajočim zdravljenjem z zdravilom EMEND, zagotavljajo več kot 95- odstotno zasedenost možganskih receptorjev NK1.
Pre-clinical data reveal no special hazard for humans based on conventional studies of single and repeated dose toxicity, genotoxicity, carcinogenic potential, and toxicity to reproduction.
Predklinični podatki na osnovi običajnih študij toksičnosti pri enkratnem in ponavljajočih se odmerkih, genotoksičnosti, kancerogenega potenciala in vpliva na sposobnost razmnoževanja ne kažejo posebnega tveganja za človeka.
Consequently, no adequate assessment of potential effects on male fertility in rats can be made.
Treba je opozoriti, da je bila pri samcih podgan sistemska 8 izpostavljenost manjša od terapevtske izpostavljenosti pri človeku, dosežene s 40 mg odmerkom, zato ni moč ustrezno oceniti učinka na fertilnost samcev podgan.
However, in a 9 month study in dogs, no organ weight changes nor gross or histomorphologic findings were present in male reproductive organs at systemic exposures 35-fold above the therapeutic exposure in humans at 40 mg.
Vendar pa v 9 mesečni študiji pri psih pri sistemski izpostavljenosti, ki je 35- krat presegala terapevtsko izpostavljenost človeka pri 40 mg odmerku, ni bilo sprememb v teži organov niti histomorfoloških ali makroskopskih sprememb v moških reproduktivnih organih.
Although no adverse effects were noted in reproduction studies when female animals were exposed 3.5- to 4-fold above the therapeutic exposure in humans at 40 mg, the potential effects on reproduction of alterations in neurokinin regulation are unknown.
Neželenih vplivov na sposobnost razmnoževanja pri sistemski izpostavljenosti samic, ki je bila 3, 5 - do 4- krat večja od izpostavljenosti človeka pri 40 mg odmerku niso opazili, vendar pa možni vplivi na sposobnost razmnoževanja zaradi sprememb v nevrokininski regulaciji niso znani.
Capsule content Sucrose Microcrystalline cellulose (E 460) Hydroxypropyl cellulose (E 463) Sodium laurilsulfate
Vsebina kapsule saharoza mikrokristalna celuloza (E460) hidroksipropilceluloza (E463) natrijev lavrilsulfat
Capsule shell Gelatin Titanium dioxide (E 171) Yellow iron oxide (E 172) Sodium laurilsulfate and silica colloidal anhydrous may be used
Ovojnica kapsule želatina titanov dioksid (E171) rumeni železov oksid (E172) uporabita se lahko natrijev lavrilsulfat in brezvodni, koloidni silicijev dioksid
Printing ink Shellac Potassium hydroxide Black iron oxide (E 172)
Črnilo za tisk šelak kalijev hidroksid črni železov oksid (E172)
6.6 Special precautions for disposal
6 Posebni varnostni ukrepi za odstranjevanje
9 8.
9 Merck Sharp & Dohme Ltd.
11 November 2003 Date of latest renewal:
11. november 2003 Datum zadnje obnove:
Detailed information on this medicinal product is available on the website of the European Medicines Agency (EMEA) http: / /www. emea. europa. eu/.
Podrobne informacije o zdravilu so objavljene na spletni strani Evropske agencije za zdravila (EMEA) http: // www. emea. europa. eu.
EMEND 80 mg hard capsules
EMEND 80 mg trde kapsule
Each capsule contains 80 mg of aprepitant.
Ena 80 mg kapsula vsebuje 80 mg aprepitanta.
80 mg sucrose.
80 mg saharoze.
Capsules are opaque with a white body and cap with “ 461” and “ 80 mg” printed radially in black ink on the body.
80 mg kapsule so neprozorne; telo je bele barve, pokrovček je bele barve; na sredini imajo oznaki "461" in "80 mg" v črni barvi.
Prevention of acute and delayed nausea and vomiting associated with highly emetogenic cisplatin- based cancer chemotherapy in adults.
Preprečevanje akutne in zapoznele navzee in bruhanja, povezanih z zelo emetogeno kemoterapijo raka s cisplatinom pri odraslih.
EMEND 80 mg is given as part of combination therapy (see section 4.2).
Zdravilo EMEND 80 mg se daje v sklopu kombiniranega zdravljenja (glejte poglavje 4. 2).
Posology EMEND is given for 3 days as part of a regimen that includes a corticosteroid and a 5-HT3 antagonist.
Odmerjanje EMEND se daje 3 dni po shemi zdravljenja, ki vključuje kortikosteroid in antagonist 5- HT3.
The recommended posology of EMEND is 125 mg orally (PO) once daily one hour before start of chemotherapy on Day 1 and 80 mg PO once daily on Days 2 and 3.
Priporočeno odmerjanje zdravila EMEND je 125 mg peroralno (PO) enkrat dnevno pred pričetkom kemoterapije prvi dan ter 80 mg (PO) enkrat na dan drugi in tretji dan.
Please refer to the Summary of Product Characteristics for fosaprepitant.
Fosaprepitant 115 mg, liofilizirano predzdravilo aprepitanta v obliki 15- minutne infuzije, lahko prvi dan, 30 minut pred kemoterapijo za preprečevanje s kemoterapijo povzročene navzee in bruhanja (CINV; “ chemotherapy induced nausea and vomiting ”) nadomesti uporabo zdravila EMEND (125 mg).
In clinical studies with EMEND, the following regimens were used for the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy:
V kliničnih študijah z zdravilom EMEND so za preprečevanje navzee in bruhanja pri emetogeni kemoterapiji raka bolnike zdravili po naslednjih shemah:
11 Highly Emetogenic Chemotherapy Regimen
Zelo emetogena kemoterapija
Dexamethasone Ondansetron
EMEND deksametazon ondansetron
12 mg PO 32 mg IV
125 mg PO 12 mg PO 32 mg iv.
8
80 mg PO 8 mg PO brez
mg PO 8 mg PO none none
80 mg PO 8 mg PO brez
8
Brez PO 8 mg PO brez
EMEND was administered orally 1 hour prior to chemotherapy treatment on Day 1 and in the morning on Days 2 and 3.
EMEND so bolniki prejemali peroralno, in sicer prvi dan zdravljenja 1 uro pred kemoterapijo, drugi in tretji dan pa zjutraj.
Dexamethasone was administered 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 to 4.
Deksametazon so bolniki prvi dan dobili 30 minut pred kemoterapijo, od drugega do četrtega dne pa zjutraj.
The dose of dexamethasone was chosen to account for active substance interactions.
Odmerek deksametazona je bil določen z upoštevanjem medsebojnega delovanja zdravilnih učinkovin.
Ondansetron was administered intravenously 30 minutes prior to chemotherapy treatment on Day 1.
Ondansetron so bolniki dobili intravensko, in sicer samo prvi dan 30 minut pred kemoterapijo.
Moderately Emetogenic Chemotherapy Regimen
11 Zmerno emetogena kemoterapija
EMEND
EMEND Deksametazon Ondansetron
125 mg PO
125 mg PO 12 mg PO 2 x 8 mg PO
80 mg PO
80 mg PO brez brez
Dexamethasone was administered 30 minutes prior to chemotherapy treatment on Day 1.
Deksametazon so bolniki prvi dan dobili 30 minut pred kemoterapijo.
One 8 mg capsule of ondansetron was administered 30 to 60 minutes prior to chemotherapy treatment and one 8 mg capsule was administered 8 hours after first dose on Day 1.
Prvi dan so bolniki dobili eno 8 mg kapsulo ondansetrona 30 do 60 minut pred kemoterapijo, še eno 8 mg kapsulo pa 8 ur za tem.
Efficacy data on combination with other corticosteroids and 5-HT3 antagonists are limited.
Za dodatne podatke o sočasnem jemanju skupaj s kortikosteroidi glejte poglavje 4. 5.
For additional information on the co-administration with corticosteroids, see section 4.5. Please refer to the Summary of Product Characteristics co-administered antiemetics.
Glejte tudi Povzetek glavnih značilnosti zdravila za antiemetike, ki jih jemljete sočasno.
Elderly (≥ 65 years) No dose adjustment is necessary for the elderly (see section 5.2).
Starostniki (≥65 let) Pri starostnikih odmerka ni treba prilagajati (glejte poglavje 5. 2).
Method of administration The hard capsule should be swallowed whole.
Način uporabe Trdo kapsulo je treba pogoltniti celo.
Co-administration with pimozide, terfenadine, astemizole or cisapride (see section 4.5).
Sočasna uporaba s pimozidom, terfenadinom, z astemizolom ali s cisapridom (glejte poglavje 4. 5).
EMEND should be used with caution in patients receiving concomitant orally administered active substances that are metabolised primarily through CYP3A4 (see section 4.5).
Zdravilo EMEND je treba uporabljati previdno pri bolnikih, ki sočasno jemljejo peroralne zdravilne učinkovine, ki se primarno presnavljajo s CYP3A4 (glejte poglavje 4. 5).
Additionally, concomitant administration with irinotecan should be approached with particular caution as the combination might result in increased toxicity.
Previdnost je še posebej potrebna pri sočasnem dajanju irinotekana, saj lahko kombinacija poveča toksični učinek.
Co-administration of EMEND with ergot alkaloid derivatives, which are CYP3A4 substrates, may result in elevated plasma concentrations of these active substances.
12 Pri sočasni uporabi zdravila EMEND z alkaloidi rženega rožička (ergot alkaloidi), ki so substrat za CYP3A4, se lahko zviša plazemska raven teh zdravilnih učinkovin.
Therefore, caution is advised due to the potential risk of ergot-related toxicity.
Zaradi morebitnega tveganja za pojav z ergot alkaloidi povezanih toksičnih učinkov svetujemo previdnost.
Co-administration of EMEND with warfarin results in decreased prothrombin time, reported as International Normalised Ratio (INR).
Sočasna uporaba zdravila EMEND z varfarinom zmanjša protrombinski čas, izražen kot INR (International Normalised Ratio).
In patients on chronic warfarin therapy, the INR should be monitored closely during treatment with EMEND and for 2 weeks following each 3-day course of EMEND for chemotherapy induced nausea and vomiting (see section 4.5).
Pri bolnikih, ki se kontinuirano zdravijo z varfarinom, je treba INR skrbno spremljati med zdravljenjem z zdravilom EMEND in še 2 tedna po vsakem 3- dnevnem ciklusu zdravljenja navzee in bruhanja zaradi kemoterapije z zdravilom EMEND (glejte poglavje 4. 5).
The efficacy of hormonal contraceptives may be reduced during and for 28 days after administration of EMEND.
Med jemanjem zdravila EMEND in še 28 dni po koncu jemanja zdravila EMEND, se lahko zmanjša učinkovitost hormonskih kontraceptivov.
Alternative or back-up methods of contraception should be used during treatment with EMEND and for 2 months following the last dose of EMEND (see section 4.5).
Med zdravljenjem z zdravilom EMEND in 2 meseca po zadnjem odmerku zdravila EMEND je treba uporabljati alternativno ali dodatno kontracepcijsko metodo (glejte poglavje 4. 5).
Concomitant administration of EMEND with active substances that inhibit CYP3A4 activity (e. g. ritonavir, ketoconazole, clarithromycin, telithromycin) should be approached cautiously as the combination results in increased plasma concentrations of aprepitant (see section 4.5).
Potrebna je previdnost pri sočasni uporabi zdravila EMEND in zdravilnih učinkovin, ki zavirajo aktivnost CYP3A4 (npr. ritonavir, ketokonazol, klaritromicin, telitromicin), ker kombinacija povzroči zvišanje plazemskih koncentracij aprepitanta (glejte poglavje 4. 5).
Aprepitant (125 mg/ 80 mg) is a substrate, a moderate inhibitor, and an inducer of CYP3A4.
Aprepitant (125 mg / 80 mg) je substrat, zmerni zaviralec in induktor CYP3A4.
During treatment with EMEND, CYP3A4 is inhibited.
Med zdravljenjem z zdravilom EMEND se CYP3A4 inhibira.
After the end of treatment, EMEND causes a transient moderate induction of CYP2C9 and a transient mild induction of CYP3A4 and glucuronidation.
Po koncu zdravljenja EMEND povzroči prehodno zmerno indukcijo CYP2C9 ter blago prehodno indukcijo CYP3A4 in glukuronidacijo.
Effect of CYP3A4 inhibition by aprepitant on the pharmacokinetics of other active substances As a moderate inhibitor of CYP3A4, aprepitant (125 mg/ 80 mg) can increase plasma concentrations of co-administered active substances that are metabolised through CYP3A4.
Učinek aprepitanta preko inhibicije CYP3A4 na farmakokinetiko drugih zdravilnih učinkovin Kot zmerni zaviralec CYP3A4 lahko aprepitant (125 mg/ 80 mg) zviša plazemske koncentracije sočasno uporabljenih peroralnih zdravilnih učinkovin, ki se presnavljajo s CYP3A4.
The area under the curve (AUC) of orally administered CYP3A4 substrates may increase up to approximately 3-fold during the 3-day treatment with EMEND; the effect of aprepitant on the plasma concentrations of intravenously administered CYP3A4 substrates is expected to be smaller.
Pričakuje se manjši vpliv aprepitanta na plazemske koncentracije intravensko uporabljenih substratov za CYP3A4.
Caution is advised during concomitant administration of EMEND and CYP3A4 substrates.
Pri sočasnem dajanju substratov za CYP3A4 in zdravila EMEND svetujemo previdnost.
EMEND must not be used concurrently with pimozide, terfenadine, astemizole, or cisapride (see section 4.3).
Zdravila EMEND se ne sme uporabljati skupaj s pimozidom, terfenadinom, z astemizolom ali s cisapridom (glejte poglavje 4. 3).