natgillin/translations-raw huggingface dataset:
Samtidig er
Rimonabant is metabolized by both CYP3A and amidohydrolase (predominantly hepatic) pathways in no
administration af CYP3A4 hæmmere vil føre til forøget optagelse af rimonabant.
Concomitant administration of CYP3A4 inhibitors will lead to increased exposure of rimonabant.
Samtidig administration af CYP3A4 fremmere forventes at føre til reduceret optagelse af rimonabant. ng
Concomitant administration of CYP3A4 inducers is expected to reduce the exposure of rimonabant. ct
Potentiale for andre lægemidler for påvirkning af rimonabant: læ
Potential for other medicinal products to affect rimonabant:
Samtidig administration af ketoconazol (en potent CYP3A4 hæmmer) forøgede AUC for rimonabant med 104% (95% confidensinterval:
by 104% (95% prediction interval:
En tilsvarende forøgelse i optagelse er forventet med andre potente CYP3A4- hæmmere.
A similar increase in exposure is expected with other potent CYP3A4 inhibitors.
Forsigtighed anbefales under samtidig anvendelse af ACOMPLIA og potente CYP3A4 hæmmere (f. eks. ketoconazol, itraconazol, ritonavir, telithromycin, ke
Caution is advised during concomitant use of ACOMPLIA and potent CYP3A4 inhibitors (e. g. ketoconazole, itraconazole, ritonavir, telithromycin, clarithromycin, nefazodone). ro
Selvom samtidig administration med CYP3A4 fremmere (f. eks. rifampicin, phenytoin, phenobarbital, r ik
Although concomitant administration of CYP3A4 inducers (e. g. rifampicin, phenytoin, phenobarbital, carbamazepine, St John’ s wort) has not been studied, it is expected that concomitant administration of potent CYP3A4 inducers may reduce the plasma concentration of rimonabant and may result in loss of lp
carbamazepine, Hyperikum Perforatum) ikke er undersøgt, forventes det, at samtidig administration af potente CYP3A4 fremmere kan reducere plasmakoncentrationen af rimonabant og kan resultatere i tab af effekt. te
efficacy.
Samtidig administration af orlistat, ethanol eller lorazepam havde ingen signifikant effekt på plasmaniveauet af rimonabant. dle
Concomitant administration of orlistat, ethanol or lorazepam had no significant effect on the plasma ina
Dog havde rimonabant in vitro en mildt mi
However, in vitro, rimonabant had a dic
hæmmende effekt på CYP2C8.
mild inhibitory effect on CYP2C8.
Rimonabant hæmmer eller fremmer ikke andre CYPenzymer eller P- glycoprotein (P- gp) in vitro. ge
Rimonabant does not inhibit or induce other CYP enzymes or P-glycoprotein (P-gp) in vitro.
Dette blev bekræftet klinisk med specifikke forsøg med midazolam (CYP3A4 substrat) og warfarin (CYP2C9 substrat) og digoxin (et P- gp substrat).
This was confirmed clinically with specific probe studies using midazolam (CYP 3A4 substrate) and warfarin (CYP 2C9 substrate) and digoxin (a P-gp substrate).
Steady- state farmakokinetikken af ethinyl estradiol/ levonorgestrel kombination oralt kontraceptiv blev ikke signifikant ændret ved samtidig administration af rimonabant.
The steady-state pharmacokinetics of an ethinyl estradiol/ levonorgestrel combination oral contraceptive were not significantly altered by concomitant administration of rimonabant.
4 4. 6 Graviditet og amning
4 4.6 Pregnancy and lactation
Der er ingen tilstrækkelige eller velkontrollerede forsøg med gravide.
Animal data are inconclusive but
5. 3).
d suggest possible deleterious effects on embryonal/ foetal development (see section 5.3).
Anvendelse under graviditet anbefales derfor
Use in pregnancy is, therefore, not recommended.
Patienter bør informere deres læge, hvis de bliver gravide under behandling med ACOMPLIA.
ise their physician if they become pregnant during treatment with ACOMPLIA.
s Det vides ikke, om rimonabant udskilles i human mælk.
It is not known if rimonabant is excreted in human milk.
ACOMPLIA er kontraindiceret under amning (se pkt.
ACOMPLIA is contraindicated during
4. 3).
or breast-feeding (see section 4.3).
til 4. 7 Virkninger på evnen til at føre motorkøretøj eller betjene maskiner
4.7 Effects on ability to drive and use machines
et Der er ikke foretaget undersøgelser af virkningen på evnen til at føre motorkøretøj eller betjene
uth No studies on the effects on the ability to drive and use machines have been performed.
Kognitive undersøgelser i klinisk farmakologiske forsøg viste, at rimonabant er blottet for kognitiv
Cognitive investigations in clinical pharmacology studies demonstrated that rimonabant is devoid of any significant cognitive or sedative effect.
ris eller sedativ effekt.
ra 4.8 Undesirable effects
Sikkerheden for ACOMPLIA 20 mg er blevet undersøgt hos ca.
ACOMPLIA 20 mg has been evaluated for safety in approximately 2500 patients enrolled in studies
3800 patienter i andre indikationer.
ge that examined the metabolic and weight loss effects in overweight and obese patients and in approximately 3800 patients in other indications.
I placebokontrollerede forsøg var frekvensen af afbrudt behandling, pga. bivirkninger, 15, 7% for patienter, der fik rimonabant.
In placebo-controlled studies, the discontinuation rate due to adverse reactions was 15.7% for patients receiving rimonabant.
symptomer, depressive sygdomme, uro og svimmelhed. ng
The most common adverse lon reactions resulting in discontinuation were: nausea, mood alteration with depressive symptoms, depressive disorders, anxiety and dizziness.
Depressive sygdomme blev rapporteret hos 3, 2% af obese patienter, eller overvægtige patienter med associerede risikofaktor( er) i behandling med rimonabant 20 mg.
Depressive disorders were reported in 3.2% of obese patients, or overweight patients with associated risk factor(s) treated with rimonabant 20 mg.
Disse var sædvanligvis milde eller læ
These were usually mild or moderate in severity and no
Korrektiv behandling eller afbrydelse af rimonabant resulterede i helbredelse i alle tilfælde og behandlingen udviste ingen forskelle sammenlignet med tilfælde rapporteret i kontrolgruppen.
resulted in recovery in all cases either after corrective treatment or discontinuation of rimonabant and did not exhibit any differentiating characteristics compared to cases reported in the control groups.
Den følgende tabel (Tabel 1) viser alle behandlingsrelaterede bivirkninger fra placebokontrollerede ke
The following table (table 1) shows all treatment-emergent adverse reactions from placebo-controlled ct
forsøg med patienter, som blev behandlet for vægttab og relaterede metaboliske sygdomme, når forekomsten var statistisk signifikant større end den tilsvarende placebofrekvens (for tilfælde ≥ 1%) r ik
studies in patients treated for weight loss and related metabolic disorders when these incidences were statistically significantly greater than the corresponding placebo rate (for events ≥ 1%) or considered clinically relevant (for events < 1%). du
Klassifikation af forventede frekvenser af bivirkninger: te
Classification of expected frequencies of undesirable effects:
Meget almindelig (≥ 10%); Almindelig (≥ 1, < 10%); Usædvanlig (≥ 0, 1, < 1%); Sjælden (≥ 0, 01, < 0, 1%); Meget sjælden (< 0, 01%), ikke kendt (kan ikke estimeres ud fra de forhåndenværende data). dle
Very common (≥ 10%); Common (≥ 1, < 10%); Uncommon (≥ 0.1, < 1%); Rare (≥ 0.01, < 0.1%); Very ro
Inden for hver enkelt frekvensgruppe skal bivirkningerne opstilles efter, hvor alvorlige de er.
rare (< 0.01%), Not known (cannot be estimated from the available data). lp ina dic Me
De alvorligste bivirkninger skal anføres først. mi ge Læ
5 Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.
5 Tabel 1:
Table 1:
Meget almindelig Infektioner i det øvre åndedrætssystem
d
Almindelig Gastroenteritis
System Organ Class
Sjælden
Common
Metabolisme og
Uncommon
Hypoglykæmi *
Rare
alg ernæring Psykiske forstyrrelser
ise
Depressive sygdomme
Infections infestations Metabolism and
Paniksymptomer Hallucinationer Vrede
and Upper respiratory Gastroenteritis tract infection
s
Hypoglycaemia*
Humørsvingninger med depressive
or nutrition disorders
Dysphoria Følelses -
Psychiatric disorders
til
Depressive disorders
symptomer Angst
Panic symptoms Anger
forstyrrelser Selvmordstanker
Hallucinations
et
uth Mood alterations Dysphoria
Irritabilitet Nervøsitet
with depressive symptoms Anxiety
Aggressivitet Aggressiv
Emotional disorder Suicidal ideation
er
ra
Søvnforstyrrelser Søvnløshed
Irritability Nervousness Sleep disorders Insomnia
ris Parasomni Nervesystemet
Aggressiveness Aggressive behaviour
Hukommelsestab
ge Parasomnias
Apati
Nervous system disorders
Svimmelhed Hypoaesthesia Ischias ea Paræstesi
Memory loss Dizziness lon Hypoaesthesia Sciatica Paresthesia
Tremor
Lethargy Tremor
Vaskulære sygdomme
Vascular disorders Respiratory,
Rødme
no
Luftveje, thorax og
Hot flush
mediastinum Mave- tarmkanalen
thoracic and mediastinal disorders
Kvalme
Gastrointestinal
ng
Nausea ct
Opkastning Hud og subkutane væv
disorders
læ
du
Hyperhidrosis Knogler, led, muskler og bindevæv
Hyperhidrosis
ke
Musculoskeletal and ro
Tendonitis Muskelkramper
Tendonitis Muscle cramp
Muskelspasmer Almene symptomer
connective tissue disorders lp
r ik
Muscle spasms
Slaphed/ træthed Influenza
Asthenia/ fatigue Influenza
Traumer, forgiftninger og behandlingskomplikatio te
Injury, Poisoning and procedural ina
Fald Blå mærker Ledforstuvning
complications
ner * frekvens er kun baseret på rapporter på obese eller overvægtige personer. dle
*frequency is based only on reports in obese or overweight diabetic patients.
I kliniske forsøg for andre indikationer, blev følgende, yderligere bivirkninger rapporteret som almindelige: mi
In clinical studies for other indications, the following additional adverse reactions were commonly dic
- Infektioner og parasitære sygdomme: sinusitis
reported: − infections and infestations: sinusitis − metabolism and nutrition disorders: anorexia, decreased appetite, Me
- Metabolisme og ernæring: anoreksi, nedsat appetit,
− gastrointestinal disorders: stomach discomfort, dry mouth.
6 Efter markedsføring Følgende bivirkninger er yderligere rapporteret efter markedsføring (hyppighed ikke kendt):
6 Post-Marketing In addition the following adverse reactions were reported during postmarketing (frequency not known):
- Psykiske forstyrrelser: psykotiske tilstande inklusive hallucinationer, vrangforestillinger
d − Psychiatric disorder: psychotic disorders including hallucinations, delusion and paranoia. − Skin and subcutaneous tissue disorders: rash.
- Nervesystemet: kramper, koncentrationsforstyrrelser, hovedpine.
ise − Nervous disorders: convulsions, disturbance in attention, headache. − gastrointestinal disorders: abdominal pain.
- Mave- tarm kanalen: mavesmerter.
Laboratory adverse events
s Laboratorie bivirkninger ACOMPLIA har ikke vist påvirkning af laboratorietestværdier.
or ACOMPLIA has not been shown to alter laboratory test values.
til 4. 9 Overdosering
4.9 Overdose
et Erfaring med overdosering af rimonabant er begrænset.
uth Experience with rimonabant in overdosage is limited.
Ved forsøget blev der rapporteret svage symptomer.
In a single-dose tolerability study, doses up to 300 mg were administered to a limited number of subjects with only minor symptoms reported.
Den farmakokinetiske profil
The pharmacokinetic profile demonstrates that a
ris viser et plateau i optagelse ved 180 mg.
ra plateau in exposures is reached at 180 mg.
Behandling bør bestå
Treatment should consist of the general measures employed in the management of overdoses, such as keeping airways
FARMAKOLOGISKE EGENSKABER
ge unobstructed, monitoring cardiovascular function and general symptomatic and supportive measures.
5. 1 Farmakodynamiske egenskaber er
PHARMACOLOGICAL PROPERTIES lon 5.1 Pharmacodynamic properties
Farmakoterapeutisk klassifikation:
Pharmaco-therapeutic group:
Antiobesitas middel ng
Anti obesity agent ATC code:
A08AX01 læ
A08AX01 no
Rimonabant er en selektiv cannabinoid- 1 receptor (CB1) antagonist som hæmmer den farmakologiske effekt af cannabinoid agonister in vitro og in vivo.
Rimonabant is a selective cannabinoid-1 receptor (CB1) antagonist that inhibits the pharmacological effects of cannabinoid agonists in vitro and in vivo.
Det endocannabinoide system er et fysiologisk system som er placeret i hjernen og de perifere væv (inklusive adiposytter).
The endocannabinoid system is a physiological system present in brain and peripheral tissues ct
Systemet befinder sig ligeledes i neuroner i det mesolimbiske system som modulerer indtagelse af meget velsmagende ting, slik og fed mad. r ik
(including adipocytes) that affects energy balance, glucose and lipid metabolism and body weight, and in neurons of the mesolimbic system modulates the intake of highly palatable, sweet or fatty foods. du
Resultater i kliniske forsøg te
Clinical study results
Vægtstyring
Weight Management ro
Patienterne inkluderet i dle
The patients included in the phase 3 trials followed a restrictive diet during the trial prescribed by a dietician and lp
fase 3 forsøgene fulgte en restriktiv diæt under forsøget ordineret af en diætist og de blev rådet til at forøge deres fysiske aktivitet.
they were advised to increase their physical activity.
Patienterne havde et BMI ≥ 30 kg/ m2 eller BMI > 27 kg/ m2 med hypertension og/ eller dyslipaedimia ved inklusionen.
Patients had a BMI ≥ 30 kg/ m² or BMI > 27 kg/ m² with hypertension and/ or dyslipidemia at inclusion.
Cirka 80% af populationen var kvinder, 87% mi
Approximately 80% of the population were women, 87% Caucasian and 9% Black.
Erfaring med patienter over 75 år og orientalere/ asiater er begrænset. ge
Experience in patients over 75 years and ina
Et middel vægttab på 6, 5 kg fra baseline til et år blev vist for ACOMPLIA 20 mg versus et middelvægttab på 1, 6 kg for placebo Læ
A mean weight loss of 6.5 kg dic
(forskel - 4, 9 kg CI95% - 5, 3; - 4, 4, p < 0, 001).
from baseline to one year was shown for ACOMPLIA 20 mg versus a mean weight loss of 1.6 kg for placebo (Difference -4.9 kg CI95% -5.3; -4.4, p < 0.001).
Procentdelen af patienter som tabte 5% og 10% af deres baseline kropsvægt efter 1 års behandling er vist i Tabel 2:
Me
7 Tabel 2
7 Table 2:
Ikke- diabetesforsøg
Non-diabetic studies
Diabetesforsøg
Placebo ACOMPLIA
alg Vægt ved baseline (kg)
Weight at baseline (kg)
101 101
101
s Personer med 5% vægtreduktion
Subjects with a 5%
til Forskel (CI 95%)
Difference (CI 95%)
et Personer med 10%
Subjects with a 10% 7.8% weight reduction
ris uto Det meste af den observerede vægtreduktion blev set inden for de første 9 måneders behandling.
ra Most of the observed weight reduction was obtained within the first nine months of treatment.
Vægttab ved 2 år var 5, 1 kg for patienter, der fik ACOMPLIA 20 mg og 1, 2 kg for placebo (forskel – 3, 8 kg; CI95 - 4, 4, - 3, 3; p < 0, 001). ea Rimonabant 20 mg reducerede risikoen for vægtforøgelse.
ge was 5.1 kg for patients who received ACOMPLIA 20 mg and 1.2 kg for placebo (Difference -3.8 kg; CI95% -4.4, -3.3; p < 0.001).
Patienter, der fik ACOMPLIA 20 mg, blev re- randomiseret til at få ACOMPLIA 20 mg eller placebo.
Patients who received ACOMPLIA 20 mg for one year were re-randomized to ACOMPLIA 20 mg or placebo.
Ved 2 år havde patienter, der fortsatte på er
At two years, patients continuing on rimonabant had a mean total weight loss of 7.5 kg over 2 years whereas patients re-randomized to placebo group during the second year had a mean total weight loss of 3.1 kg over 2 years.
rimonabant, et gennemsnitlig totalt vægttab på 7, 5 kg over de 2 år, mens patienter, der blev re - randomiseret til placebogruppen i det andet år, havde et gennemsnitligt totalt vægttab på 3, 1 kg over ng
At two years, the difference in total weight loss between ACOMPLIA and placebo was -4.2 kg (CI95% -5.0; - no
de 2 år.
3.4, p < 0.001).
Behandling med rimonabant var associeret med en signifikant reduktion i livsmål, en kendt markør for intra- abdominalt fedt. ke
Treatment with rimonabant was associated with significant reductions in waist circumference, a known marker of intra-abdominal fat. ct
Vægttabet i det begrænsede antal af negroide patienter var mindre udtalt (middelforskel til placebo - 2, 9 kg).
In the limited number of Black patients weight loss was less pronounced (mean difference to placebo -2.9 kg).
Der kan ikke drages r ik
No du
nogle konklusioner vedrørende effekt for patienter over 75 år eller for asiater/ orientalere p. g. a. af det lave antal patienter. te
conclusions can be drawn with regard to effects in patients over 75 years or in Asian/ Oriental patients due to the low number of patients. ro
I ikke- diabetesforsøgene med en blandet population af personer med/ uden (behandlet) dyslipidemia dle
For lp
Forskellen var statistisk signifikant mi
HDL-C an average increase of 16.4% was seen under rimonabant 20 mg (baseline HDL-C 1.24 mmol/ l) compared to an increase of 8.9% for placebo (baseline HDL-C 1.21 mmol/ l).
(forskel 7, 9% CI95 6, 6%; 9, 2%, p < 0, 001).
The difference was statistically significant (Difference 7.9% CI95% 6.6%; 9.2%, p < 0.001).
For triglycerider blev der set et middelfald på 6, 9% ved rimonabant 20 mg (baseline TG 1, 62 mmol/ l) sammenlignet med en forøgelse på 5, 8% for placebo ge
For the ina
(baseline TG 1, 65 mmol/ l).
triglycerides an average decrease of 6.9% was seen under rimonabant 20 mg (baseline TG 1.62 mmol/ l) compared to an increase of 5.8% for placebo (baseline TG 1.65 mmol/ l).
Forskellen var statistisk signifikant (forskel - 13, 3% CI95 – 16, 5; - 10, 2% p < 0, 001).
The difference was statistically significant (Difference -13.3% CI95% -16.5; -10.2% p < 0.001).
Læ
rimonabant 20 mg was beyond that expected from weight loss alone.
ACOMPLIA 20 mg havde generelt ingen signifikant effekt på Total- C eller LDL- C niveauer.
Generally ACOMPLIA 20 mg had no significant effect on Total-C or LDL-C levels.
8 Der blev observeret forbedringer i HbA1c og kropsvægt i forsøget med type 2 diabetes patienter (RIO - Diabetes) behandlet med metformin eller sulfonylurea, som var overvægtige eller obese.
metformin or sulfonylurea improvements in HbA1c and body weight were observed.
Den absolutte ændring i HbA1c ved et år var - 0, 6 for rimonabant 20 mg (baseline 7, 3%) og +0, 1 for placebo (baseline 7, 2%).
The absolute change in HbA1c at one year was -0.6 for rimonabant 20 mg (baseline 7.3%) and +0.1 on placebo (baseline 7.2%).
Forskellen var statistisk signifikant (forskel - 0, 7%, CI95% - 0, 80; - 0, 5, p < 0, 001).
Differences were statistically significant (Difference -0.7%, CI95% -0.80; -0.5, p < 0.001).
alg 1, 4 kg (forskel - 3, 9 kg CI95% - 4, 6; - 3, 3, p < 0, 001).
8 At one year a mean weight loss of 5.3 kg was shown for ACOMPLIA 20 mg versus a loss on placebo of 1.4 kg (Difference – 3.9 kg CI95% -4.6; -3.3 p < 0.001).
Procentdelen af patienter, som tabte 5% og 10% af deres kropsvægt ved baseline efter 1 års behandling, er vist i tabel 2.
The percentage of patients who lost 5% and 10% of their baseline body weight after 1 year of treatment are given in the table 2.
s ændring i HbA1c ved 6 måneder - 0, 8 for rimonabant 20 mg og - 0, 3 for placebo (baseline for begge grupper:
d In a second trial in treatment naïve type 2 diabetic obese patients (Serenade), the absolute change in HbA1c (with a baseline of 7.9% for both groups) at six months was -0.8 for rimonabant 20 mg and
Procentdelen af patienter, som opnåede
ise -0.3 under placebo (Difference -0.51 CI95% -0.78, -0.24 p < 0.001).
til HbA1c < 7,% var 51% i rimonabant- gruppen og 35% i placebo- gruppen.
The percentage of patients reaching HbA1c < 7% was 51% in the rimonabant group and 35% in the placebo group.
Forskellen mellem 20 mg - og placebo- gruppen, i den gennemsnitlige ændring af kropsvægt, var 3, 8 kg (CI95% - 5, 0, - 2, 6 p <
The difference in mean body weight change between the 20 mg and placebo groups was 3.8 kg (CI95% -5.0, -2.6 p < 0.001).
Ændringer i HDL- C og TG i denne population svarede til dem i ikke- diabetespopulationen.
Changes in HDL-C and TG in this population were similar to that of the non-diabetic population.
er estimeres, at ca. halvdelen af middelforbedringen i HbA1c hos patienter, der fik rimonabant 20 mg var ud over den forventede effekt på vægttabet alene.
or estimated that approximately half of the mean improvement in HbA1c in patients receiving rimonabant 20 mg was beyond that expected from weight loss alone.
ris 5. 2 Farmakokinetiske egenskaber
uth 5.2 Pharmacokinetic properties
uto Farmakokinetikken for rimonabant er forholdsvis proportional op til 20 mg.
Rimonabant pharmacokinetics are fairly dose proportional up to about 20 mg.
Absorption:
ra Absorption:
Rimonabant viser høj in vitro permeabilitet og er ikke et substrat af P- glycoprotein.
Rimonabant displays high in vitro permeability and is not a substrate of P-glycoprotein.
Efter mange doser af 20 mg givet en gang dagligt til er
Following multiple once-daily doses of 20 mg
2 timer med et steady state plasmaniveau opnået efter 13 dage (Cmax = 196 + 28, 1 ng/ ml; Cmin = 91, 6 + 14, 1 ng/ ml; ng
ge to healthy subjects in the fasted state, maximum plasma concentrations of rimonabant are achieved in approximately 2 hours with steady state plasma levels achieved within 13 days (Cmax = 196 ± 28.1 ng/ ml; Ctrough = 91.6 ± 14.1 ng/ ml; AUC0-24 = 2960 ± 268 ng. h/ ml).
Steady state rimonabant eksponering er 3, 3 gange højere end det observerede efter første dosis.
Steady state rimonabant lon exposures are 3.3-fold higher than those observed after the first dose.
min. plasmakoncentration, men ingen forskel i steady state AUC, som vægten øges.
Population pharmacokinetic analysis demonstrated less fluctuation in peak to trough plasma concentration but no differences in steady state AUC as weight increases.
Som vægten forøges fra 65 kg til 200 kg, forventes Cmax at falde 24% og Cmin forventes at forøges med 5%.
As weight increases from 65 to 200 kg, Cmax is expected to decrease 24% and Ctrough is expected to increase by 5%.
Farmakokinetiske populationsanalyser indikerer, at ke
Population no
rimonabants farmakokinetik er den samme for sunde, ikke- rygende personer og patienter som ryger. r ik
pharmacokinetic analysis indicated that rimonabant pharmacokinetics are similar between healthy non-smoking subjects and patients who smoke.
Effekt af mad:
Effect of food: ct
Administration af rimonabant til sunde fastende personer eller med et meget fedt måltid, viste at Cmax og AUC forøgedes henholdsvis 67% og 48% ved fedt måltid.
Administration of rimonabant to healthy subjects in the fasted state or with a high fat meal demonstrated that Cmax and AUC were increased 67% and 48% respectively, under fed conditions.
ACOMPLIA 20 mg blev taget om te
In clinical studies, ACOMPLIA 20 mg was taken in the morning usually before breakfast. du
Distribution: dle
Distribution:
In vitro human plasmaproteinbinding af rimonabant er høj (> 99, 9%) og ikke- mættet over et stort koncentrationsområde.
The in vitro human plasma protein binding of rimonabant is high (> 99.9%) and non-saturable over a ro
normal vægt. ge
wide concentration range.
Biotransformation:
Biotransformation:
Rimonabant metaboliseres via både CYP3A og amidohydrolase (primært hepatiske) veje in vitro.
Rimonabant is metabolized by both CYP3A and amidohydrolase (predominantly hepatic) pathways in ina
Læ
Circulating metabolites do not contribute to its pharmacologic activity.
9 Elimination:
Elimination:
Rimonabant bliver hovedsageligt elimeneret via metabolisme og efterfølgende udskillelse af metabolitter via galden.
Only dic
Kun omkring 3% af rimonabant- dosis bliver elimineret via urinen, mens omkring 86% af dosis udskilles i fæces som uomdannet stof og metabolitter.
an approximate 3% of the dose of rimonabant is eliminated in the urine, while approximately 86% of the dose is excreted in the faeces as unchanged drug and metabolites.
9 dage) p. g. a. af et
Me
s Race:
9 Special Populations Race:
I enkelt - og gentagen- dosisforsøg var Cmax og AUC for rimonabant ens hos sunde japanske og
In single- and repeat-dose studies, the Cmax and AUC of rimonabant were similar in healthy Japanese
9 dage).
d and Caucasian subjects, whereas elimination half-life was shorter in Japanese subjects (3-4 days) compared to Caucasian subjects (about 9 days).
Forskellen i halveringstiden skyldtes forskellen i
The difference in half-life was due to differences in
et det perifere distributionsvolume som konsekvens af lavere vægt hos japanske personer.
ise peripheral volume of distribution as a consequence of lower weight in Japanese subjects.