natgillin/translations-raw huggingface dataset:
Graden af interaktion med andre OATP- hæmmere (visse HMG CoA- reduktasehæmmere, f. eks. atorvastatin, proteasehæmmere, f. eks. ritonavir, tuberkulostatika, f. eks. rifamycin) er ikke kendt, men kan resultere i en stigning i sitaxentans plasmakoncentration.
The extent of interaction with other OATP inhibitors (some HMG CoA reductase inhibitors eg, atorvastatin, protease inhibitors eg, ritonavir, tuberculostatics eg, rifamycin) is unknown but could result in raised plasma levels of sitaxentan.
Derudover resulterede kliniske interaktionsforsøg med nelfinavir, en moderat potent OATP- hæmmer, og pravastatin, en OATP- hæmmer med lav affinitet, ikke i klinisk signifikante ændringer i sitaxentans plasmakoncentration.
Moreover, Clinical interaction studies with nelfinavir, a moderately potent OATP inhibitor, and pravastatin, a low affinity OATP inhibitor, did not result in clinically significant changes in sitaxentan plasma levels.
Fluconazol (CYP2C19 - og CYP2C9 -, og CYP3A4/ 5- hæmmer):
Fluconazole (inhibitor of CYP2C19, CYP2C9 and CYP3A4/ 5):
Samtidig administration af Thelin og fluconazol havde ingen effekt på clearance af sitaxentannatrium.
Co-administration of Thelin and fluconazole had no effect on the clearance of sitaxentan sodium.
Ketoconazol (CYP3A4/ 5- substrat og - hæmmer):
Ketoconazole (substrate and inhibitor of CYP3A4/ 5):
Samtidig administration af Thelin og ketoconazol forårsagede ikke en klinisk siginifikant ændring af hverken sitaxentannatriums eller ketoconazols clearance.
Co-administration with Thelin did not cause a clinically significant change in the clearance of either sitaxentan sodium or ketoconazole.
Nelfinavir (CYP2C19 - og CYP3A4/ 5- substrat):
Nelfinavir (substrate of CYP3A4/ 5, CYP2C19):
Samtidig administration af Thelin og nelfinavir forårsagede ikke en klinisk signifikant ændring i clearance af sitaxentannatrium eller af nelfinavir.
Co-administration with Thelin did not cause a clinically significant change in the clearance of either sitaxentan sodium or nelfinavir.
Warfarin (vitamin K- antagonist, CYP2C9- substrat):
5 Effects of Thelin on other medicinal products
Samtidig behandling med sitaxentannatrium resulterede i en forøgelse af S- warfarins eksponering på 2, 4 gange.
Concomitant treatment with sitaxentan sodium resulted in a 2.4 fold increase in S-warfarin exposure.
Patienter, som får warfarin, opnår terapeutisk antikoagulation (International normaliseret ratio (INR) mål) med lavere doser af
Subjects receiving warfarin achieve therapeutic anticoagulation (International Normalised Ratio [INR] target) with lower doses of the anticoagulant in the presence of sitaxentan sodium.
Ved indledning af behandling med vitamin K- antagonister hos patienter, som tager sitaxentannatrium, anbefales det at begynde ved den lavest mulige dosis af vitamin K - antagonisten.
When initiating vitamin K antagonist therapy in a patient taking sitaxenten sodium, it is recommended to start at the lowest available dose.
Hos patienter, som allerede tager en vitamin K- antagonist, anbefales det, at dosis af vitamin K- antagonisten reduceres ved indledning af sitaxentannatrium- behandling.
In patients already taking a vitamin K antagonist, it is recommended that the dose of the vitamin K antagonist be reduced when starting sitaxentan sodium.
Stigning i dosis af vitamin K- antagonisten skal foretages lidt efter lidt for at nå et passende mål- INR.
Increases in the vitamin K antagonist dose should be done in small increments to reach an appropriate target INR.
Hvis INR ikke monitoreres omhyggeligt, og stigning i dosis af vitamin K- antagonister forbliver uopdaget, kan der opstå alvorlige eller livstruende blødningstilfælde.
If INR is not properly monitored and increased exposure to vitamin K antagonists remains undetected, severe or life-threatening bleeding episodes may occur.
Orale kontraceptiva (CYP3A4/ 5- substrat):
Oral contraceptives (substrate of CYP3A4/ 5):
Samtidig administration af Thelin og Ortho- Novum 1/ 35 (1 mg norethindron / 0, 035 mg ethinylestradiol) resulterede i stigning i eksponering for ethinylestradiol (CYP3A4/ 5- substrat) og norethindron (CYP3A4/ 5) på henholdsvist 59% og 47%.
Concomitant administration of Thelin and Ortho- Novum 1/ 35 (1 mg norethindrone/ 0.035 mg ethinyl estradiol) resulted in increases in exposure to ethinyl estradiol (substrate of CYP3A4/ 5) and norethindrone (CYP3A4/ 5) of 59% and 47%, respectively.
4. 4).
However, sitaxentan sodium did not affect the anti-ovulatory activity of the oral contraceptive as assessed by the plasma concentrations of follicle stimulating hormone (FSH), luteinising hormone (LH), and progesterone (see section 4.4).
Sildenafil (CYP3A4- substrat):
Sildenafil (substrate of CYP3A4):
En enkeltdosis af sildenafil på 100 mg indgivet samtidig med Thelin øgede sildenafils Cmax og AUC∞ med henholdsvist 18% og 28%.
A single dose of sildenafil 100 mg coadministered with Thelin increased Cmax and AUC∞ of sildenafil by 18% and 28%, respectively.
Der var ingen ændring i Cmax eller AUC for den aktive metabolit n- desmethylsildenafil.
There was no change in Cmax or AUC for the active metabolite, n-desmethylsildenafil.
Nifedipin (CYP3A4/ 5- substrat):
Nifedipine (substrate of CYP3A4/ 5):
Nifedipins clearance var ikke klinisk signifikant ændret ved indgivelse samtidig med Thelin.
The clearance of nifedipine was not clinically significantly changed when given concomitantly with Thelin.
Omeprazol (CYP2C19- substrat):
Omeprazole (substrate of CYP2C19):
Samtidig administration af Thelin og omeprazol øgede omeprazols AUC0- 24 med 30%; Cmax var uændret.
Concomitant administration of Thelin with omeprazole increased the omeprazole AUC0-24 by 30%; Cmax was unchanged.
Digoxin (p- glykoprotein- substrat):
Digoxin (substrate of p-Glycoprotein):
Samtidig administration af Thelin ændrede ikke digoxins farmakokinetik, hvilket indikerer, at der ingen indvirkning var på p- glykoprotein- transportstof.
Concomitant administration of Thelin did not alter the pharmacokinetics of digoxin indicating no effect on the p-glycoprotein transporter
Der er ikke udført kliniske interaktionsforsøg med et CYP2C8- substrat.
No clinical interaction study was performed with a substrate of CYP 2C8.
Der er ingen humane data for anvendelse af sitaxentannatrium under graviditet.
Pregnancy There are no human data regarding the use of sitaxentan sodium during pregnancy.
5. 3).
Sitaxentan sodium caused teratogenicity in rats (see section 5.3).
Amning; Sitaxentannatrium blev påvist i plasma fra rotteunger, som havde diet hos hunrotter behandlet med sitaxentannatrium, hvilket indikerer, at sitaxentannatrium var til stede i brystmælken.
Lactation Sitaxentan sodium was detected in the plasma of breast fed pups from female rats treated with sitaxentan sodium, indicating that sitaxentan sodium was present in the breast milk.
Pga. mulig teratogenicitet må behandling ikke påbegyndes hos kvinder i den fertile alder, medmindre de anvender sikker kontraception.
6 Women of child-bearing potential Treatment must not be initiated in women of child-bearing potential unless they practice reliable contraception, due to possible teratogenicity.
Thelins sikkerhed er vurderet i kliniske forsøg med mere end 1200 patienter med PAH, såvel som i sikkerhedsdata efter markedsføring.
General description Safety of Thelin has been evaluated in clinical trials of more than 1200 patients with PAH, as well as post-marketing safety data.
I placebo- kontrollerede forsøg af PAH med den anbefalede dosis var den mest almindelige bivirkning, som blev vurderet til muligvis at være relateret til Thelin, hovedpine hos 15% af patienterne, og perifert ødem og nasal kongestion, hver hos 9% af patienterne.
At the recommended dose during placebo-controlled trials in pulmonary arterial hypertension PAH, the most common adverse drug reactions considered to be at least possibly related to Thelin treatment were headache in 15% of patients, and peripheral oedema and nasal congestion, each in 9% of patients.
Hyppighederne er rapporteret som meget almindelig (≥1/ 10), almindelig (≥1/ 100 til < 1/ 10), ikke almindelig (≥1/ 1. 000 til ≤1/ 100), sjælden (≥1/ 10. 000 til < 1/ 1. 000) og meget sjælden (< 1/ 10. 000).
Frequencies are reported as very common (≥ 1/ 10), common (> 1/ 100 ,< 1/10), uncommon (> 1/ 1,000, ≤ 1/ 100), rare (> 1/ 10,000, ≤ 1/ 1,000), and very rare (≤ 1/ 10,000).
System organklasse / Bivirkninger Blod og lymfesystem
System Organ Class / Adverse reaction Blood and lymphatic system disorders
Nervesystemet Hovedpine Insomni, svimmelhed
Nervous system disorders Headache Insomnia, dizziness
Vaskulære sygdomme Gingival blødning, rødmen
Vascular disorders Gingival bleeding, flushing
Mave- tarmkanalen Kvalme, obstipation, øvre abdominalsmerter, opkastning, dyspepsi og diarré
Gastrointestinal disorders Nausea, constipation, upper abdominal pain, vomiting, dyspepsia and diarrhoea
Lever og galdeveje Stigninger i lever- aminotransferase, stigning i bilirubin (forbundet med lever- aminotransferase)
Hepatobiliary disorders Liver aminotransferases increase, bilirubin increase (associated with liver aminotransferase increase)
Hud og subkutane væv Udslæt (forskellige former)
7 Skin and subcutaneous tissue Rash (various types and presentations)
7 Knogler, led, muskler og bindevæv Muskelkramper
Musculoskeletal and connective tissue disorders Muscle cramp
Undersøgelsers Stigning i INR (ved samtidig behandling med vitamin K- antagonist).
Investigations INR increase (with concomitant vitamin K antagonist therapy).
Stigning i protrombintid (PT) (ved samtidig behandling med vitamin K - antagonist).
Prothrombin time (PT) increase (with concomitant vitamin K antagonist therapy).
Forhøjet ASAT og/ eller ALAT er forbundet med sitaxentannatrium.
Increased Liver Aminotransferases (see section 4.4) Elevations of AST and/ or ALT are associated with sitaxentan sodium.
I fase 2 og 3 orale forsøg hos patienter med PAH blev forhøjelse af ALAT og/ eller ASAT > 3 ULN observeret hos 5% af patienterne, der blev behandlet med placebo (N=155) og hos 7% af patienterne behandlet med Thelin 100 mg (N=887).
In phase 2 and 3 oral studies in patients with PAH, elevations in ALT and/ or AST > 3 ULN were observed in 5% of placebo-treated patients (N = 155) and 7% of Thelin 100 mg-treated patients (N = 887).
Forhøjelserne i ALAT- værdierne > 5 ULN var 4% (36/ 887) for sitaxentan 100 mg én gang dagligt og 0, 6% i placebogruppen (1/ 155).
Elevations in ALT values > 5 ULN were 4% (36/ 887) for sitaxentan 100 mg QD and 0.6% in the placebo group (1/ 155).
Sitaxentanpopulationen omfattede også patienter (N=53), hvor behandling med en anden endothelinreceptor- antagonist var seponeret pga. leverfunktionsabnormiteter.
The Sitaxentan population also included patients (N = 53) who had discontinued another endothelin receptor antagonist due to liver function abnormalities.
Dette tyder på, at der bør udvises forsigtighed, når sitaxentan initieres i denne population.
This specific group had a higher risk (19%; N = 10/ 53) of developing elevations in ALT and/ or AST > 3 x ULN indicating that appropriate care should be exercised when initiating sitaxentan in this patient population.
Det samlede gennemsnitlige fald i hæmoglobinkoncentration var 0, 5 g/ dl (ændring fra start til behandlingsafslutning) for patienter behandlet med Thelin.
Decreased Haemoglobin (see section 4.4) The overall mean decrease in haemoglobin concentration for Thelin -treated patients was 0.5 g/ dl (change to end of treatment).
I placebo- kontrollerede undersøgelser blev markerede fald i hæmoglobin (> 15% fald fra baseline med værdi < nedre normalgrænse) observeret i 7% af patienter behandlet med Thelin (N = 149) og 3% af patienter behandlet med placebo (N = 155).
In placebo-controlled studies, marked decreases in haemoglobin (> 15% decrease from baseline with value < lower limit of normal) were observed in 7% of patients treated with Thelin (N = 149) and 3% of placebo-treated patients (N = 155).
Et fald i hæmoglobinkoncentration med mindst 1 g/ dl blev observeret i 60% af patienter behandlet med Thelin sammenlignet med i 32% af patienter behandlet med placebo.
A decrease in haemoglobin concentration by at least 1 g/ dl was observed in 60% of patients treated with Thelin as compared to 32% of placebo-treated patients.
Disse bivirkninger er de samme som dem, der blev rapporteret i de kliniske forsøg.
Post marketing experience Adverse events reported during the post-marketing period to date have been similar to those reported in clinical trials.
I de kliniske forsøg blev Thelin givet som en daglig oral dosis på 1. 000 mg i 7 dage til raske frivillige.
During clinical trials, Thelin was given as a daily oral dose of 1000 mg/ day for 7 days to healthy volunteers.
I et åbent PAH- forsøg blev der rapporteret om et fatalt tilfælde af leversvigt efter kronisk dosering af 600 mg sitaxentan dagligt givet som 300 mg 2 gange dagligt.
8 In an open-label PAH study, one fatal case of hepatic failure has been reported after chronic dosing of sitaxentan at 600 mg/ day administered as 300 mg bid.
Andre antihypertensiver, ATC- kode:
Other antihypertensives, ATC code:
Det kan desuden fremme fibrose, celleproliferation, hjertehypertrofi og remodellering og er pro- inflammatorisk.
Mechanism of action Endothelin-1 (ET-1) is a potent vascular paracrine and autocrine peptide in the lung, and can also promote fibrosis, cell proliferation, cardiac hypertrophy, and remodelling and is pro-inflammatory.
Dette angiver, at ET- 1 spiller en patologisk rolle i disse sygdomme.
ET-1 concentrations are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension, as well as other cardiovascular disorders and connective tissue diseases, including scleroderma, acute and chronic heart failure, myocardial ischaemia, systemic hypertension, and atherosclerosis, suggesting a pathogenic role of ET-1 in these diseases.
I pulmonal arteriel hypertension og hjertesvigt er forhøjede ET- 1 koncentrationer ved fraværet af endothelinreceptor - antagonisme stærkt korreleret med sværhedsgraden af og prognosen for disse sygdomme.
In pulmonary arterial hypertension and heart failure, in the absence of endothelin receptor antagonism, elevated ET-1 concentrations are strongly correlated with the severity and prognosis of these diseases.
Endvidere er pulmonal arteriel hypertension ligeledes karakteriseret ved reduceret dinitrogenoxidaktivitet.
Additionally, pulmonary arterial hypertension also is characterized by reduced nitric oxide activity.
ET- 1’ s virkning medieres gennem endothelin A- receptorer (ETA) på celler i glatte muskelceller og endothelin B- receptorer (ETB) på endotelceller.
ET-1 actions are mediated through endothelin A receptors (ETA), present on smooth muscle cells, and endothelin B receptors (ETB), present on endothelial cells.
Dette skyldes til dels frigivelse af dinitrogenoxid og prostacyclin.
Predominant actions of ET-1 binding to ETA are vasoconstriction and vascular remodelling, while binding to ETB results in ET-1 clearance, and vasodilatory/ antiproliferative effects due in part to nitric oxide and prostacyclin release.
Thelin er en potent (Ki 0, 35 nM) og yderst selektiv ETA- antagonist (omkring 6. 500 gange mere selektiv for ETA sammenlignet med ETB).
Thelin is a potent (Ki 0.35 nM) and highly selective ETA antagonist (approximately 6,500-fold more selective for ETA as compared to ETB).
To randomiserede, dobbelt- blinde, multicenter, placebo- kontrollerede forsøg blev foretaget for at påvise effekten.
Efficacy Two randomized, double-blind, multi-centre, placebo-controlled trials were conducted to demonstrate efficacy.
STRIDE- 1, som omfattede 178 patienter, sammenlignede 2 orale doser af Thelin (100 mg én gang dagligt og 300 mg én gang dagligt) med placebo under 12 ugers behandling.
STRIDE-1, which included 178 patients, compared 2 oral doses of Thelin (100 mg once daily and 300 mg once daily) with placebo during 12 weeks of treatment.
STRIDE- 2 - forsøget på 18 uger foretaget med 246 patienter omfattede 4 behandlingsarme: placebo én gang dagligt; Thelin 50 mg én gang dagligt, Thelin 100 mg én gang dagligt, og åbent bosentan to gange dagligt (effekten vurderet blindet, indgivet i henhold til godkendt indlægsseddel).
The 18 week STRIDE-2 trial, conducted in 246 patients, included 4 treatment arms: placebo once daily, Thelin 50 mg once daily, Thelin 100 mg once daily, and open-label bosentan twice daily (efficacy-rater blinded, administered according to the approved package insert).
Patienterne havde moderat til svær (NYHA/ WHO - funktionsklasse I- IV) PAH som et resultat af idiopatisk PAH (IPAH, også betegnet primær pulmonal hypertension), bindevævssygdom (CTD) eller medfødt hjertesygdom (CHD).
Patients had moderate to severe (NYHA/ WHO functional class II-IV) pulmonary arterial hypertension resulting from idiopathic pulmonary arterial hypertension (IPAH, also known as primary pulmonary hypertension), connective tissue disease (CTD), or congenital heart disease (CHD).
I disse forsøg blev forsøgsmedicinen føjet til patientens aktuelle behandling, som kunne have inkluderet en kombination af digoxin, antikoagulantia, diuretika, ilt og vasodilatorer (f. eks. kalciumkanalblokkere, ACE- hæmmere).
In these studies, the study medicine was added to patients’ current therapy, which could have included a combination of digoxin, anticoagulants, diuretics, oxygen, and vasodilators (eg, calcium channel blockers, ACE inhibitors).
Patienter med præeksisterende leversygdom og patienter, som fik ikke- konventionelle PAH- behandlinger (f. eks. iloprost), var ekskluderede.
Patients with pre-existent hepatic disease and patients using non- conventional PAH treatments (eg, iloprost) were excluded.
Nedsat fysisk funktionsevne blev bedømt ved at måle den distance, patienten kunne gå på 6 minutter (6 min. gangtest) efter 12 uger for STRIDE- 1 og 18 uger for STRIDE- 2.
Sub-maximal exercise capacity was assessed by measuring distance walked in 6 minutes (6-minute walk test) at 12 weeks for STRIDE-1 and 18 weeks for STRIDE-2.
I begge undersøgelser resulterede behandling med Thelin i betydelig forøgelse af fysisk funktionsevne.
In both trials, treatment with Thelin resulted in a significant increase in exercise capacity.
De placebo - korrigerede forøgelser i gangdistance sammenlignet med baseline var henholdsvis 35 meter (p=0, 006; ANCOVA) og 31 meter (p < 0, 05; ANCOVA).
The placebo-corrected increases in walk distance compared to baseline were 35 metres (p = 0.006; ANCOVA) and 31 metres (p < 0.05; ANCOVA), respectively.
Blandt patienter med CTD blev der observeret en statistisk signifikant forskel versus placebo (37, 73 meter, p < 0, 05).
Among patients with CTD, a statistically significant difference versus placebo was observed (37.73 metres, p < 0.05).
En reduktion i symptomer på PAH blev observeret med Thelin- behandling.
A reduction in symptoms of pulmonary arterial hypertension was observed with Thelin treatment.
I STRIDE- 1 - forsøget blev 59 (33%) af de 178 patienter klassificerede ved baseline som NYHA- funktionsklasse II (gennemsnitlig baseline 6- min. - gangdistance 451 meter) og 117 (66%) som funktionsklasse III (gennemsnitlig baseline 6- min. - gangdistance 372 meter).
9 II (mean baseline 6 minute walk distance 451 meters) and 117 (66%) as functional class III (mean baseline 6 minute walk distance 372 meters).
I STRIDE- 2 -
Treatment with Thelin led to net improvement in NYHA functional class in 25% of patients (placebo 8%, p < 0.05).
9 forsøget blev 93 (38%) af de 246 patienter ved baseline klassificerede som NYHA- funktionsklasse II (gennemsnitlig baseline 6- min. - gangdistance 370 meter) og 144 (59%) som funktionsklasse III (gennemsnitlig baseline 6- min. - gangdistance 322 meter).
In the STRIDE-2 trial 93 (38%) of the 246 patients were classified at baseline as NYHA functional class II (mean baseline 6 minute walk distance 370 meters) and 144 (59%) as functional class III (mean baseline 6 minute walk distance 322 meters).
Behandling med Thelin førte til en nettoforbedring i WHO- funktionsklasse hos 12% af patienterne (placebo - 3%, p < 0, 05).
Treatment with Thelin led to net improvement in WHO functional class in 12% of patients (placebo -3%, p < 0.05).
Hæmodynamiske parametre blev bedømt i STRIDE- 1.
Haemodynamic parameters were assessed in STRIDE-1.
Sammenlignet med placebo- behandling resulterede Thelin i en forbedring (p < 0, 05) af hjerteindekset på +0, 3 l/ min/ m2 (13%), af lungekarmodstand på - 221 dyn* sek. / cm5 (22%), og af systemisk karmodstand på - 276 dyn* sek. / cm5 (16%) efter 12- uger behandling.
Compared with placebo treatment, Thelin resulted in improvement (p < 0.05) in cardiac index of +0.3 L/ min/ m2 (13%), in pulmonary vascular resistance of-221 dynes*sec/ cm5 (22%), and in systemic vascular resistance of -276 dynes*sec/ cm5 (16%) after 12 weeks of treatment.
Reduktionen i gennemsnitlig lungearterietryk på 3 mmHg (6%) var ikke statistisk signifikant.
The reduction in mean pulmonary artery pressure of 3 mmHg (6%) was not statistically significant.
Virkningen af Thelin på resultatet af sygdommen kendes ikke.
The effect of Thelin on the outcome of the disease is unknown.
Der er ingen forsøg til at påvise gunstig virkning på overlevelse ved behandling med sitaxentannatrium.
Long-term Data There are no studies to demonstrate beneficial effects on survival of treatment with sitaxentan sodium.
Patienter, som fuldførte STRIDE- 2, var dog kvalificerede til at tilmelde sig STRIDE- 2X, som er et 1- årigt åbent forsøg af Thelin 100 mg.
However, patients completing STRIDE-2 were eligible to enrol in STRIDE-2X, a 1-year open-label study of Thelin 100 mg.
I alt 145 patienter blev behandlet med 100 mg Thelin.
A total of 145 patients were treated with Thelin 100 mg.
I denne samlede population var Kaplan- Meier skønnet for overlevelse 96% for patienter efter 1- års behandling med Thelin.
In this total population, Kaplan-Meier estimates of survival were 96% for patients after 1 year of therapy with sitaxentan sodium.
Et- årige overlevelsesskøn var tilsvarende i undergruppen af patienter med PAH sekundært til bindevævssygdom for gruppen behandlet med Thelin (98%).
One-year survival estimates were similar in the subgroup of patients with PAH secondary to connective tissue disease for the Thelin treated group (98%).
Skønnene kan være påvirket af indledningen af nye eller supplerende PAH- behandlinger, som forekom i 24% af patienter.
The estimates may have been influenced by the initiation of new or additional PAH therapies, which occurred in 24% of patients.
Sitaxentannatrium absorberes hurtigt efter oral indgivelse.
Absorption Sitaxentan sodium is rapidly absorbed following oral administration.
Hos PAH patienter blev den maksimale plasmakoncentration sædvanligvist opnået inden for 1- 4 timer.
In PAH patients, peak plasma concentrations are generally achieved within 1-4 hours.
Den absolutte biotilgængelighed af Thelin er mellem 70 og 100%.
The absolute bioavailability of Thelin is between 70 and 100%.
Ved indgivelse med et måltid rigt på fedt blev absorptionshastigheden (Cmax) af Thelin reduceret med 43% og Tmax forsinket (dobbelt forøgelse) sammenlignet med fastende tilstand, men graden af absorption var den samme.
When administered with a high fat meal, the rate of absorption (Cmax) of Thelin was decreased by 43% and the Tmax delayed (2-fold increase) compared to fasted conditions, but the extent of absorption was the same.
Sitaxentannatrium er mere end 99% proteinbundet til plasmaproteiner, hovedsagligt til albumin.
Distribution Sitaxentan sodium is more than 99% protein bound to plasma proteins, predominantly albumin.
Sitaxentannatrium penetrerer ikke ind i erythrocytter og lader ikke til at krydse blod- hjerne- barrieren.
Sitaxentan sodium does not penetrate into erythrocytes and does not appear to cross the blood-brain barrier.
Sitaxentannatrium er yderst omsætteligt efter oral indgivelse til raske frivillige.
Metabolism and Elimination Following oral administration to healthy volunteers, sitaxentan sodium is highly metabolised.
De mest almindelige metaboliske produkter er mindst 10 gange mindre potente som ETA- antagonister end sitaxentannatrium i en standard in vitro- aktivitetstest.
The most common metabolic products are at least 10 times less potent as ETA antagonists than sitaxentan sodium in a standard in vitro test of activity.