natgillin/translations-raw huggingface dataset:
In 2 randomised, double-blind studies encompassing a total of 1,094 patients receiving chemotherapy that included cisplatin ≥ 70 mg/ m2, aprepitant in combination with an ondansetron/ dexamethasone regimen (see section 4.2) was compared with a standard regimen (placebo plus ondansetron 32 mg intravenously administered on Day 1 plus dexamethasone 20 mg orally on Day 1 and 8 mg orally twice daily on Days 2 to 4).
V 2 randomiziranih, dvojno slepih študijah, ki sta skupaj zajeli 1. 094 bolnikov na kemoterapiji, ki je vključevala cisplatin ≥ 70 mg/ m2, so primerjali aprepitant v kombinaciji z ondansetronom/ deksametazonom (glejte poglavje 4. 2) in standardno terapijo (placebo in ondansetron 32 mg intravensko prvi dan ter deksametazon 20 mg peroralno prvi dan in 8 mg peroralno dvakrat na dan od drugega do četrtega dne).
The results were evaluated for each individual study and for the 2 studies combined.
Rezultate so ovrednotili za vsako posamezno študijio ter za kombinacijo obeh študij.
A summary of the key study results from the combined analysis is shown in Table 1.
Povzetek ključnih rezultatov kombinirane analize je prikazan v Preglednici 1.
18 Table 1 Percent of Patients Receiving Highly Emetogenic Chemotherapy Responding by Treatment Group and Phase — Cycle 1
Preglednica 1 Odstotek bolnikov, ki so prejemali zelo emetogeno kemoterapijo, z odzivom po zdravljenih skupinah in fazi – 1. ciklus
Standard Therapy
Aprepitant
Differences*
Običajno
(N= 524) †%
zdravljenje (N = 524) †
(95% CI)
% (95% IZ)
Complete Response (no emesis and no
Popoln odziv (brez bruhanja in brez rešilnega zdravljenja)
rescue therapy)
Skupaj (0 – 120 ur) 0 – 24 ur 25 – 120 ur
INDIVIDUAL MEASURES No Emesis (no emetic episodes regardless of use of rescue therapy)
POSAMEZNI MERILI Brez bruhanja (brez bruhanja ne glede na rešilno zdravljenje)
Overall (0-120 hours) 0-24 hours 25-120 hours
Skupaj (0 – 120 ur) 0 – 24 ur 25 – 120 ur
No Significant Nausea (maximum VAS < 25 mm on a scale of 0-100 mm)
Brez pomembne navzee (največja ocena < 25 mm na vizualni analogni lestvici 0 – 100 mm) 18
Overall (0-120 hours) 25-120 hours
Skupaj (0– 120 ur) 25– 120 ur
* The confidence intervals were calculated with no adjustment for gender and concomitant chemotherapy, which were included in the primary analysis of odds ratios and logistic models. † One patient in the Aprepitant Regimen only had data in the acute phase and was excluded from the overall and delayed phase analyses; one patient in the Standard Regimen only had data in the delayed phase and was excluded from the overall and acute phase analyses.
Oceno časa do prvega bruhanja v kombinirani analizi prikazuje Kaplan- Meierjeva krivulja na Sliki 1.
The estimated time to first emesis in the combined analysis is depicted by the Kaplan-Meier plot in Figure 1.
Slika 1
Figure 1 Percent of Patients Receiving Highly Emetogenic Chemotherapy Who Remain Emesis Free Over Time – Cycle 1
Odstotek bolnikov, ki so prejemali zelo emetogeno kemoterapijo, pri katerih se bruhanje ne pojavi, glede na čas – 1. ciklus
Aprepitant Regimen (N=520) Standard Therapy (N=523)
Aprepitant Regimen Standard Therapy (N=523)
80%
80% Odstotek bolnikov
Time (hours)
Time( ure) Čas (hours)
In the same 2 clinical studies, 851 patients continued into the Multiple-Cycle extension for up to 5 additional cycles of chemotherapy.
851 bolnikov iz teh dveh študij je zdravljenje nadaljevalo v podaljšku z več ciklusi, in sicer so prejeli do 5 dodatnih ciklusov kemoterapije.
19 In a randomised, double-blind study in a total of 866 patients (864 females, 2 males) receiving chemotherapy that included cyclophosphamide 750-1500 mg/ m2; or cyclophosphamide 500- 1500 mg/ m2 and doxorubicin (< 60 mg/ m2) or epirubicin (< 100 mg/ m2), aprepitant in combination with an ondansetron/ dexamethasone regimen (see section 4.2) was compared with standard therapy (placebo plus ondansetron 8 mg orally (twice on Day 1, and every 12 hours on Days 2 and 3) plus dexamethasone 20 mg orally on Day 1).
V randomizirani, dvojno slepi študiji, ki je skupaj zajela 866 bolnikov (864 žensk, 2 moška), ki so dobivali kemoterapijo s ciklofosfamidom 750– 1500 mg/ m2 ali ciklofosfamidom 500– 1500 mg/ m2 in doksorubicinom (≤60 mg/ m2) ali epirubicinom (≤100 mg/ m2), so primerjali aprepitant v kombinaciji z ondansetronom in deksametazonom (glejte 4. 2) ter standardno terapijo (placebo in ondansetron 8 mg peroralno (dvakrat 1. dan ter na 12 ur 2. in 3. dan) ter deksametazon 20 mg peroralno 1. dan).
Table 2 Percent of Patients Responding by Treatment Group and Phase — Cycle 1 Moderately Emetogenic Chemotherapy
Preglednica 2 Odstotek bolnikov z odzivom po zdravljenih skupinah in fazi – 1. ciklus Zmerno emetogena kemoterapija
Aprepitant Regimen
Razlike *
(N= 433) †%
(N = 433) †% 19
(N= 424)%%
zdravljenje (N = 424)%
Complete Response (no emesis and no rescue therapy)
Popoln odziv (brez bruhanja
Overall (0-120 hours) 0-24 hours 25-120 hours
Skupaj (0– 120 ur) 0– 24 ur 25– 120 ur
50.8 75.7 55.4
50, 8 42, 5 75, 7 69, 0 55, 4 49, 1
(1.6, 15.0) (0.7, 12.7) (-0.4, 13.0)
(1, 6; 15, 0) (0, 7; 12, 7) (- 0, 4; 13, 0)
INDIVIDUAL MEASURES No Emesis (no emetic episodes regardless of use of rescue therapy)
Brez bruhanja (brez bruhanja ne glede na rešilno zdravljenje)
No Significant Nausea (maximum VAS < 25 mm on a scale of 0-100 mm)
Brez pomembne navzee (največja ocena < 25 mm na vizualni analogni lestvici 0 – 100 mm)
* The confidence intervals were calculated with no adjustment for age category (< 55 years, ≥ 55 years) and investigator group, which were included in the primary analysis of odds ratios and logistic models. † One patient in the Aprepitant Regimen only had data in the acute phase and was excluded from the overall and delayed phase analyses.
* Intervali zaupanja so bili izračunani brez prilagoditve glede na starost (< 55 let, ≥55 let) in preiskovano skupino, ki sta bili vključeni v primarno analizo razmerij obetov in logističnih modelov. † Za enega bolnika, ki je prejemal aprepitant, so na voljo le podatki iz akutne faze zdravljenja in je bil izključen iz celotne analize in analize podaljšane faze.
20 The estimated time to first emesis in the study is depicted by the Kaplan-Meier plot in Figure 2.
Oceno časa do prvega bruhanja v kombinirani analizi prikazuje Kaplan- Meierjeva krivulja na sliki 2.
Figure 2 Percent of Patients Receiving Moderately Emetogenic Chemotherapy Who Remain Emesis Free Over Time – Cycle 1
Slika 2 Odstotek bolnikov, ki so prejemali zmerno emetogeno kemoterapijo, pri katerih se bruhanje ne pojavi, glede na čas – 1. ciklus
48
48 Time
60
60 (hours)
In the same clinical study, 744 patients continued into the Multiple-Cycle extension for up to 3 additional cycles of chemotherapy.
V isti klinični študiji je 744 bolnikov nadaljevalo v podaljšku z več ciklusov, in sicer so prejeli do 3 dodatne cikluse kemoterapije.
The mean peak plasma concentration (Cmax) of aprepitant occurred at approximately 4 hours (tmax).
Povprečno najvišjo plazemsko koncentracijo (Cmax) je aprepitant dosegel
Oral administration of the capsule with an approximately 800 Kcal standard breakfast resulted in an up to 40% increase in AUC of aprepitant.
Po peroralnem zaužitju kapsule skupaj z običajnim zajtrkom z 800 kcal se je AUC aprepitanta povečal za največ 40%.
In healthy young adults, the increase in AUC0-∞ was 26% greater than dose proportional between 80 mg and 125 mg single doses administered in the fed state.
Pri zdravih mladih preiskovancih je bilo povečanje AUC0– ∞ za 26% višje od razmerja odmerkov med posameznima 80 mg in 125 mg odmerkoma, ki so ju preiskovanci prejeli siti.
Following oral administration of a single 125 mg dose of EMEND on Day 1 and 80 mg once daily on Days 2 and 3, the AUC0-24hr (mean±SD) was 19.6±2.5 microgram x h/ ml and 21.2±6.3 microgram x h/ ml on Days 1 and 3, respectively.
Po peroralnem zaužitju enega 125 mg odmerka zdravila EMEND prvi dan ter 80 mg enkrat na dan drugi in tretji dan je AUC0– 24 ur (povprečje ±SD) znašal 19, 6 ± 2, 5 μg × h/ ml prvi dan ter 21, 2 ± 6, 3 μg × h/ ml tretji dan.
Cmax was 1.6±0.36 microgram/ ml and 1.4±0.22 microgram/ ml on Days 1 and 3, respectively.
Cmax je znašala 1, 6 ± 0, 36 μg/ ml prvi dan ter 1, 4 ± 0, 22 μg/ ml tretji dan.
21 Metabolism Aprepitant undergoes extensive metabolism.
Presnova Aprepitant se v veliki meri presnavlja.
Elimination Aprepitant is not excreted unchanged in urine.
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.
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 ranged from approximately 9 to 13 hours.
Srednja terminalna razpolovna doba je znašala v razponu od približno 9 do 13 ur.
Pharmacokinetics in special populations Elderly:
Farmakokinetika pri posebnih skupinah bolnikov Starostniki:
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- Plough- 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- Plough- 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 (razred C po Child - Plough- ovi klasifikaciji) ni.
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.
21 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.
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 zdravila v primerjavi z zdravimi preiskovanci ni bistveno spremenil.
22 Relationship between concentration and effect 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 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.
However, it should be noted that systemic exposure in rodents was similar or even lower than therapeutic exposure in humans at the 125 mg/ 80 mg dose.
Vendar je treba opozoriti, da je bila sistemska izpostavljenost pri glodalcih podobna ali celo manjša od terapevtske izpostavljenosti pri človeku pri odmerku 125 mg/ 80 mg.
Capsule shell Gelatin Sodium laurilsulfate and silica colloidal anhydrous may be used Titanium dioxide (E 171)
Ovojnica kapsule želatina uporabita se lahko natrijev lavrilsulfat in brezvodni, koloidni silicijev dioksidtitanov dioksid (E171)
6.4 Special precautions for storage
4 leta 22 6. 4 Posebna navodila za shranjevanje
23 6.6 Special precautions for disposal
6 Posebni varnostni ukrepi za odstranjevanje
EMEND 125 mg hard capsules
EMEND 125 mg trde kapsule
Each capsule contains 125 mg of aprepitant.
Ena 125 mg kapsula vsebuje 125 mg aprepitanta.
125 mg sucrose.
125 mg saharoze.
Capsules are opaque with a white body and pink cap with “ 462” and “ 125 mg” printed radially in black ink on the body.
125 mg kapsule so neprozorne; telo je bele barve, pokrovček je rožnate barve; na sredini imajo oznaki "462" in "125 mg" v črni barvi.
EMEND 125 mg is given as part of combination therapy (see section 4.2).
Zdravilo EMEND 125 mg se daje v sklopu kombiniranega zdravljenja (glejte poglavje 4. 2).
25 Highly Emetogenic Chemotherapy Regimen
Zelo emetogena kemoterapija
mg PO 8 mg PO none none
80 mg PO 8 mg POs brez
8
brez 8 mg PO brez
Moderately Emetogenic Chemotherapy Regimen
24 Zmerno emetogena kemoterapija
Efficacy data on combination with other corticosteroids and 5-HT3 antagonists are limited.
Podatkov o učinkovitosti pri kombiniranju z drugimi kortikosteroidi in antagonisti 5- HT3 ni dovolj.
For additional information on the co-administration with corticosteroids, see section 4.5.
Za dodatne podatke o sočasnem jemanju skupaj s kortikosteroidi glejte poglavje 4. 5.
Please refer to the Summary of Product Characteristics of co-administered antiemetic agents.
Glejte tudi Povzetek glavnih značilnosti zdravila za antiemetike, ki jih jemljete sočasno.
(see section 4.5).
Sočasno jemanje s pimozidom, terfenadinom, z astemizolom ali s cisapridom (glejte poglavje 4. 5).
Co-administration of EMEND with ergot alkaloid derivatives, which are CYP3A4 substrates, may result in elevated plasma concentrations of these active substances.
25 Pri sočasni uporabi zdravila EMEND z alkaloidi rženega rožička (ergot alkaloidi), ki so substrat za CYP3A4, se lahko zviša plazemska raven teh zdravilnih učinkovin.
John’ s Wort (Hypericum perforatum) is not recommended.
Sočasna uporaba zdravila EMEND in zeliščnih pripravkov, ki vsebujejo šentjanževko (Hypericum perforatum), ni priporočljiva.
27 Induction As a moderate inducer of CYP2C9 and a mild inducer of CYP3A4 and glucuronidation, aprepitant can decrease plasma concentrations of substrates eliminated by these routes.
Indukcija Kot zmeren induktor CYP2C9 in blag induktor CYP3A4 in glukuronidacije, lahko aprepitant zniža plazemske koncentracije substratov, ki se izločajo po teh poteh.
Data are lacking regarding effects on CYP2C8 and CYP2C19.
V tem obdobju
Caution is advised when warfarin, acenocoumarol, tolbutamide, phenytoin or other active substance that are known to be metabolised by CYP2C9 are administered during this time period.
26 svetujemo previdnost pri dajanju varfarina, acenokumarola, tolbutamida, fenitoina in drugih zdravilnih učinkovin, ki se presnavljajo s CYP2C9.
The dose of dexamethasone in chemotherapy induced nausea and vomiting clinical trials was chosen to account foractive substance interactions (see section 4.2).
Odmerek deksametazona je bil v kliničnih študijah navzee in bruhanja zaradi kemoterapije določen z upoštevanjem medsebojnega delovanja zdravilnih učinkovin (glejte poglavje 4. 2).
Because the effect of EMEND on the pharmacokinetics of orally administered CYP3A4 substrates is greater than the effect of EMEND on the pharmacokinetics of intravenously administered CYP3A4 substrates, an interaction with orally administered chemotherapeutic agents metabolised primarily or in part by CYP3A4 (e. g. etoposide, vinorelbine) cannot be excluded.
Ker je učinek zdravila EMEND na farmakokinetko substratov za CYP3A4, če so dani peroralno, večji kot če so dani inravensko, interakcije s peroralno danimi kemoterapevtiki, ki se predvsem ali delno presnavljajo s CYP3A4 (npr. etopozid, vinorelbin), ne moremo izključiti.
28 In a third study with intravenous and oral administration of midazolam, EMEND was given as 125 mg on Day 1 and 80 mg/ day on Days 2 and 3, together with ondansetron 32 mg Day 1, dexamethasone 12 mg Day 1 and 8 mg Days 2-4.
V tretji študiji z intravenskim in s peroralnim odmerjanjem midazolama so EMEND dajali po shemi 125 mg prvi dan ter 80 mg/ dan drugi in tretji dan, skupaj z ondansentronom 32 mg prvi dan in deksametazonom 12 mg prvi dan ter 8 mg drugi do četrti dan.
Intravenous 2 mg midazolam was given 1 hour after oral administration of a single dose of EMEND 125 mg.
27 125 mg peroralnega odmerka zdravila EMEND.
This effect was not considered clinically important.
Ta učinek nima kliničnega pomena.
Aprepitant does not seem to interact with the P-glycoprotein transporter, as suggested by the lack of interaction of EMEND with digoxin.
EMEND nima medsebojnega vpliva z digoksinom, zato verjetno ne intereagira s P- glikoproteinskim prenašalcem.
When a single 375 mg dose of aprepitant was administered on Day 9 of a 14-day regimen of 600 mg/ day of rifampicin, a strong CYP3A4 inducer, the AUC of aprepitant decreased 91% and the mean terminal half-life decreased 68%.
Pri enkratnem odmerku 375 mg aprepitanta 9. dan 14- dnevnega zdravljenja z rifampicinom (ki je močan induktor CYP3A4) 600 mg na dan, se je AUC aprepitanta zmanjšal za 91%, srednja terminalna razpolovna doba aprepitanta pa se je skrajšala za 68%.
4.6 Pregnancy and lactation
28 4. 6 Nosečnost in dojenje
ALT increased, AST increased
zvišanje ALT, zvišanje AST zvišanje alkalne fosfataze, hiperglikemija, mikrohematurija, hiponatriemija, zmanjšanje telesne mase
Bradycardia febrile neutropenia, anaemia
limfatičnega anemija, febrilna nevtropenija
uncommon uncommon
občasne
headache, dizziness
glavobol, omotica
dream abnormality, cognitive disorder
neobičajne sanje, motnje mišljenja
Tinnitus hiccups
tinitus
uncommon common
občasne
uncommon uncommon
občasne občasne
uncommon uncommon common
občasne občasne pogoste
31 One case of angioedema and urticaria was reported as a serious adverse event in a patient receiving aprepitant in a non-CINV/ non-PONV study.
Poročali so o enem primeru angioedema in urtikarije kot o resnem neželenem dogodku, vendar pa ne v študiji CINV (Chemotherapy Induced Nausea and Vomiting) / PONV.
4.9 Overdose
30 4. 9 Preveliko odmerjanje
32 Table 1 Percent of Patients Receiving Highly Emetogenic Chemotherapy Responding by Treatment Group and Phase — Cycle 1
Preglednica 1 Odstotek bolnikov, ki so prejemali zelo emetogeno kemoterapijo, z odzivom po zdravljenih skupinah in fazi – 1. ciklus
(N= 524) †%
zdravljenje (N = 524) †%
Overall (0-120 hours) 25-120 hours
Skupaj (0– 120 ur)
72.1 74.0
(1, 6; 12, 8)
64.9 66.9
25– 120 ur
7.2 7.1
66, 9
(1.6, 12.8) (1.5, 12.6)
(1, 5; 12, 6)
33 In a randomised, double-blind study in a total of 866 patients (864 females, 2 males) receiving chemotherapy that included cyclophosphamide 750-1500 mg/ m2; or cyclophosphamide 500- 1500 mg/ m2 and doxorubicin (< 60 mg/ m2) or epirubicin (< 100 mg/ m2), aprepitant in combination with an ondansetron/ dexamethasone regimen (see section 4.2) was compared with standard therapy (placebo plus ondansetron 8 mg orally (twice on Day 1, and every 12 hours on Days 2 and 3) plus dexamethasone 20 mg orally on Day 1).
V randomizirani, dvojno slepi študiji, ki je skupaj zajela 866 bolnikov (864 žensk, 2 moška), ki so dobivali kemoterapijo s ciklofosfamidom 750– 1500 mg/ m2 ali ciklofosfamidom 500– 1500 mg/ m2 in doksorubicinom (≤60 mg/ m2) ali epirubicinom (≤100 mg/ m2), so primerjali aprepitant v kombinaciji z ondansetronom in deksametazonom (glejte 4. 2) ter standardno terapijo (placebo in ondansetron 8 mg peroralno (dvakrat 1. dan ter na 12 ur 2. in 3. dan) ter deksametazon 20 mg peroralno 1. dan).
Complete Response (no emesis and no rescue therapy)
32 Popoln odziv (brez bruhanja in brez rešilnega zdravljenja)
34 The estimated time to first emesis in the study is depicted by the Kaplan-Meier plot in Figure 2.
Oceno časa do prvega bruhanja v kombinirani analizi prikazuje Kaplan- Meierjeva krivulja na sliki 2.
35 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.
Following oral administration of a single 125 mg dose ofaprepitant, 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.
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.
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 (razred C po Child - Pugh- ovi klasifikaciji) ni.
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.
34 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.
Relationship between concentration and effect 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.
36 5.3 Pre-clinical safety data
5. 3 Predklinični podatki o varnosti
Capsule shell Gelatin Sodium laurilsulfate and silica colloidal anhydrous may be used Titanium dioxide (E 171) Yellow iron oxide (E 172) Red iron oxide (E 172)
Ovojnica kapsule želatina uporabita se lahko natrijev lavrilsulfat in brezvodni, koloidni silicijev dioksid titanov dioksid (E171) rdeči železov oksid (E172) rumeni železov oksid (E172)
6.3 Shelf-life
35 6. 3 Rok uporabnosti
125 mg sucrose (in the 125 mg capsule).
125 mg saharoze (v 125 mg kapsuli).
80 mg sucrose (in the 80 mg capsule).
80 mg saharoze (v 80 mg kapsuli).
The 125 mg capsule is opaque with a white body and pink cap with “ 462” and “ 125 mg” printed radially in black ink on the body.
125 mg kapsule so neprozorne; telo je bele barve, pokrovček je rožnate barve; na sredini imajo oznako "462" in "125 mg" v črni barvi.
The 80 mg 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 oznako "461" in "80 mg" v črni barvi.
EMEND 125 mg/ 80 mg is given as part of combination therapy (see section 4.2).
Zdravilo EMEND 125 mg/ 80 mg se daje v sklopu kombiniranega zdravljenja (glejte poglavje 4. 2).
39 Highly Emetogenic Chemotherapy Regimen
Zelo emetogena kemoterapija
80 mg PO 80 mg PO
EMEND deksametazon
12 mg PO 32 mg IV
125 mg PO 12 mg PO
8
80 mg PO 8 mg PO
mg PO 8 mg PO none none
80 mg PO 8 mg PO
8
brez 8 mg PO
mg PO none
32 mg iv.
Dexamethasone was administered 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 to 4.
37 Deksametazon so bolniki prvi dan dobili 30 minut pred kemoterapijo, od drugega do četrtega dne pa zjutraj.
EMENDwas 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.
Please refer to the Summary of Product Characteristics of co-administered antiemetics.
Glejte tudi Povzetek glavnih značilnosti zdravila za antiemetike, ki jih jemljete sočasno.