natgillin/translations-raw huggingface dataset:
Infections Common: influenza like symptoms, respiratory tract infection (e. g bronchitis), urinary tract infection Uncommon: candidiasis, ear infection, herpes simplex, tooth infection
Redke: kandidiaza, infekcije ušes, herpes simpleks, okužbe zob.
Blood and lymphatic system disorders Uncommon: anaemia Rare: pancytopenia, neutropenia, leucopenia
Redke: pancitopenija, nevtropenija, levkopenija.
Nervous system disorders Common: dizziness, headache Uncommon: syncope, hypoaesthesia, migraine, paraesthesia, dysgeusia, vertigo, tinnitus
Redke: sinkopa, hipestezija, migrena, parestezije, disgevzija, vrtoglavica, tinitus.
Eye disorders Uncommon: conjunctivitis, dry eye, visual disturbance (e. g. blurred vision) Rare: keratitis
Redka: keratitis.
Cardiac disorders Uncommon: palpitations, myocardial infarction* Rare: cardiac failure, atrioventricular block of first degree Vascular disorders Uncommon: venous insufficiency, hypotension, cerebrovascular accident*
Žilne bolezni Občasne: venska insuficienca, hipotenzija, cerebrovaskularni incident *.
Respiratory disorders Common: cough, pharyngitis Uncommon: dyspnoea, epistaxis, rhinitis, sinus congestion, asthma
Občasne: dispneja, epistaksa, rinitis, kongestija sinusov, astma.
14 Gastrointestinal disorders Common: abdominal pain, constipation, diarrhoea, dyspepsia, nausea, vomiting, flatulence Uncommon: gastroduodenal ulcer, gastroduodenitis, oesophagitis, abdominal distension, aphthous stomatitis, dry mouth, dysphagia, epigastric discomfort, eructation, gastrooesophageal reflux disease, gingivitis, hyperacidity, toothache Rare: gastrointestinal haemorrhage
Redka: gastrointestinalna krvavitev.
Skin and subcutaneous tissue disorders Uncommon: contusion, exanthem, pruritus, rash, urticaria Rare: angioedema
Redka: angioedem.
Musculoskeletal disorders Uncommon: joint swelling, muscle cramps, arthralgia
Bolezni mišično- skeletnega sistema Občasne: otekanje sklepov, mišični krči, artralgija.
Renal and urinary disorders Uncommon: dysuria, urinary frequency, cystitis Rare: chromaturia, renal failure
Redki: kromaturija, ledvična odpoved.
General disorders Common: fatigue, oedema (e. g lower limb) Uncommon: appetite increased or decreased, chest pain, rigors, thirst Rare: anaphylaxis
Redka: anafilaksija.
Investigations Uncommon: alanine aminotransferase increased, aspartate aminotransferase increased, blood creatinine increased, blood urea increased, gamma-glutamyltransferase increased, weight increased.
Preiskave Občasne: zvišana alanin aminotransferaza, zvišana aspartat aminotransferaza, zvišan kreatinin v krvi, zvišana sečnina v krvi, zvišana gama- glutamiltransferaza, zvečana telesna teža.
* Based on analyses of long-term placebo and active controlled clinical trials, some selective COX-2 inhibitors have been associated with an increased risk of serious thrombotic arterial events, including myocardial infarction and stroke.
* Glede na rezultate dolgoročnih, s placebom in drugim zdravilom primerjanih kliničnih raziskav so bili nekateri selektivni zaviralci COX- 2 povezani s povečanim tveganjem za resne trombotične dogodke v arterijah, vključno z miokardnim infarktom in možgansko kapjo.
The absolute risk increase for such events is unlikely to exceed 1% per year based on existing data (uncommon).
Glede na obstoječe podatke je malo verjetno, da absolutno povečanje tveganja teh dogodkov preseže 1% na leto (občasni).
Approximately 1,100 patients were treated with lumiracoxib in analgesia clinical studies (post-surgical dental pain, primary dysmenorrhea, and post-orthopedic surgery pain).
Približno 1. 100 bolnikov so zdravili z lumirakoksibom v kliničnih študijah analgezije (bolečine po operaciji zob, primarne dismenoreje in bolečine po ortopedskih operacijah).
The following rare serious undesirable effects have been reported in association with the use of NSAIDs and cannot be ruled out for lumiracoxib: nephrotoxicity including interstitial nephritis and nephrotic syndrome and renal failure; hepatotoxicity including hepatic failure and jaundice; cutaneo- mucosal adverse effects and severe skin reactions.
15 sindromom in ledvično odpovedjo; hepatotoksičnost vključno z odpovedjo jeter in zlatenico; kožnosluznični neželeni učinki in hude kožne reakcije.
15 There is no clinical experience of overdose.
S prevelikim odmerjanjem ni nobenih kliničnih izkušenj.
Multiple doses of lumiracoxib 1,200 mg once daily have been administered to patients with rheumatoid arthritis for 4 weeks without clinically significant adverse effects.
Bolnikom z revmatoidnim artritisom so 4 tedne dolgo dajali večkratne odmerke lumirakoksiba po 1. 200 mg enkrat na dan brez klinično pomembnih neželenih učinkov.
In the event of suspected overdose, appropriate supportive medical care should be provided e. g. by eliminating the gastric contents, clinical supervision and, if necessary, the institution of symptomatic treatment.
V primeru suma na prevelik odmerek je treba nuditi ustrezno podporno medicinsko oskrbo, na primer odstranitev želodčne vsebine, klinični nadzor, po potrebi pa tudi uvesti simptomatsko zdravljenje.
Anti-inflammatory and antirheumatic products, non-steroids, coxibs, ATC code:
Nesteroidna protivnetna in protirevmatična zdravila, koksibi, Oznaka ATC:
M01 AH 06
M01 AH 06.
Mode of Action Lumiracoxib is an orally active, selective cyclooxygenase-2 (COX-2) inhibitor within the clinical dose range.
Način delovanja Lumirakoksib je znotraj območja kliničnih odmerkov peroralni selektivni zaviralec ciklooksigenaze- 2 (COX- 2).
Two isoforms, COX-1 and COX-2 have been identified.
Identificirali so dve izoobliki, COX- 1 in COX- 2.
COX-2 is the isoform of the enzyme that has been shown to be induced by pro- inflammatory stimuli and has been postulated to be primarily responsible for the synthesis of prostanoid mediators of pain, inflammation, and fever.
COX- 2 predstavlja izoobliko encima, za katero so je pokazalo, da jo inducirajo provnetni dražljaji in za katerega domnevajo, da je odgovoren predvsem za sintezo prostanoidnih mediatorjev bolečine, vnetja in vročine.
COX-2 is also involved in ovulation, implantation and closure of the ductus arteriosus, regulation of renal function, and central nervous system functions (fever induction, pain perception and cognitive function).
COX- 2 ima vlogo tudi pri ovulaciji, vgnezdenje zarodka in zaprtju duktusa arteriozusa, regulaciji ledvične funkcije ter funkcije v centralnem živčnem sistemu (indukcija vročine, dojemanje bolečine in kognitivna funkcija).
COX-2 has been identified in tissue around gastric ulcers in man but its relevance to ulcer healing has not been established.
COX- 2 so odkrili v tkivu okrog želodčnih razjed pri ljudeh, vendar njenega pomena celjenje razjed še niso dokazali.
The difference in antiplatelet activity between some COX-1 inhibiting NSAIDs and COX-2 selective inhibitors may be of clinical significance in patients at risk of thrombo-embolic reactions.
Razlika v antiagregacijski aktivnosti med nekaterimi NSAR- i, ki zavirajo COX- 1, in selektivnimi zaviralci COX- 2 je lahko klinično pomembna pri bolnikih s tveganjem za tromboembolične reakcije.
COX-2 selective inhibitors reduce the formation of systemic (and therefore possibly endothelial) prostacyclin without affecting platelet thromboxane.
Selektivni zaviralci COX- 2 zmanjšajo nastajanje sistemskega (in zato možno endotelijskega) prostaciklina, ne da bi vplivali na trombocitni tromboksan.
Across clinical pharmacology studies, lumiracoxib produced dose-dependent inhibition of COX-2 in plasma without inhibition of COX-1.
V kliničnofarmakoloških študijah je lumirakoksib povzročal od odmerka odvisno inhibicijo COX- 2 v plazmi, brez inhibicije COX- 1.
Selective inhibition of COX-2 by lumiracoxib provides anti-inflammatory and analgesic effects.
Selektivna inhibicija COX- 2 z lumirakoksibom povzroča protivnetne in analgetične učinke.
Administration of 100 mg, 200 mg or 400 mg once daily leads to > 90% peak inhibition of COX-2.
Uporaba 100 mg, 200 mg ali 400 mg enkrat na dan povzroči > 90% največje inhibicije COX- 2.
There is no significant inhibition of COX-1 (assessed as ex vivo inhibition of thromboxane B2) up to 800 mg in healthy volunteers.
Pri zdravih prostovoljcih do odmerka 800 mg ni signifikantne inhibicije COX- 1 (ocenjene kot ex vivo inhibicija tromboksana B2).
Efficacy In patients with osteoarthritis, lumiracoxib doses up to 200 mg once daily provided significant improvements in pain, stiffness, function, and patient assessments of disease status.
Učinkovitost Pri bolnikih z osteoartrozo je lumirakoksib v odmerkih do 200 mg enkrat na dan signifikantno izboljšal bolečine, otrdelost, funkcijo in bolnikovo oceno stanja bolezni.
In clinical studies, lumiracoxib 400 mg relieved pain in acute analgesic models of post-operative dental pain, post-orthopaedic surgical pain, and primary dysmenorrhea.
16 V kliničnih raziskavah je lumirakoksib v odmerku 400 mg olajšal bolečine v akutnih analgetičnih modelih postoperativnega zobobola, bolečine po ortopedskih operacijah in primarne dismenoreje.
16 TARGET, a 12-month, double-blind, phase III study included 18,325 OA patients randomized to lumiracoxib 400 mg once daily (two to four times the recommended OA dose), naproxen 500 mg twice daily or ibuprofen 800 mg three times daily.
Varnost Preskus Terapevtska raziskava artritisa in gastrointestinalnih dogodkov (TARGET) Študija TARGET, 12- mesečna dvojno slepa študija III. faze, je zajela 18. 325 bolnikov z OA, randomiziranih na lumirakoksib 400 mg enkrat na dan (ta odmerek je dvakrat do štirikrat večji od priporočenega odmerka pri OA), naproksen 500 mg dvakrat na dan ali ibuprofen 800 mg trikrat na dan.
TARGET included patients taking low-dose ASA (75-100 mg daily) for primary or secondary prevention of coronary heart disease.
TARGET je zajel bolnike, ki so jemali ASA v majhnih odmerkih (75- 100 mg na dan) za primarno ali sekundarno preventivo koronarne bolezni srca.
Randomization was stratified by low-dose ASA use (24% of patients in the overall study population) and age.
Randomizacija je bila stratificirana po uporabi ASA v majhnih odmerkih (24% bolnikov v celotni populaciji študije) in po starosti.
Gastrointestinal Effect in TARGET (12-month study) The primary endpoint was time to event distribution of definite or probable upper gastrointestinal tract ulcer (UGIT) complications (POBs).
Gastrointestinalni učinki v študiji TARGET (12- mesečna študija) Primarno končno stanje je bil čas do dogodkovne distribucije definitivnih ali verjetnih komplikacij (POB) ulkusa zgornjih prebavil (UGIT).
- In the population not using low-dose aspirin, the incidence of POBs was 14/ 6950 patients
- Pri populaciji, ki ni jemala aspirina v majhnih odmerkih, je bila incidenca POB
(0.2%) for lumiracoxib versus 64/ 6968 patients (0.92%) for NSAIDs, with a hazard ratio (HR) of 0.21 [95% CI 0.12-0.37] p < 0.0001.
14/ 6950 bolnikov (0, 2%) za lumirakoksib proti 64/ 6968 bolnikov (0, 92%) za NSAR, s kvocientom tveganja (HR) 0, 21 [95% CI 0, 12- 0, 37] p < 0, 0001.
- In the low dose ASA group the incidence of POBs was 15/ 2167 patients (0.69%) for
- V skupini z ASA v majhnih odmerkih je bila incidenca POB 15/ 2167 bolnikov (0, 69%) za
lumiracoxib versus 19/ 2159 patients (0.88%) for NSAIDs, with a HR of 0.79 [95% CI 0.40- 1.55] (not statistically significant).
lumirakoksib proti 19/ 2159 bolnikov (0, 88%) za NSAR, HR 0, 79 [95% CI 0, 40- 1, 55] (statistično nesignifikantno).
- In the overall population, the incidence of POBs was 29/ 9117 patients (0.32%) for lumiracoxib
- V celotni populaciji je bila incidenca POB 29/ 9117 bolnikov (0, 32%) za lumirakoksib proti
versus 83/ 9127 patients (0.91%) for NSAIDs, with a HR of 0.34 [95% CI 0.22-0.52] p < 0.0001.
83/ 9127 bolnikov (0, 91%) za NSAR, s HR 0, 34 [95% CI 0, 22- 0, 52] p < 0, 0001.
Cardiovascular Effect in TARGET (12-month study) The primary cardiovascular (CV) endpoint studied was the Antiplatelet Trialists’ Collaboration (APTC) endpoint: confirmed or probable myocardial infarction (clinical or silent), stroke (ischemic or haemorrhagic) and CV death.
Kardiovaskularni učinki v študiji TARGET (12- mesečna študija) Primarno kardiovaskularno (CV) končno stanje, ki so ga proučevali, je bilo končno stanje po Antiplatelet Trialists ’ Collaboration (APTC): potrjen ali verjeten miokardni infarkt (klinični in tihi), možganska kap (ishemična ali hemoragična) in CV smrt.
- In the population not using low-dose aspirin, the incidence of APTC events was
- V skupini, ki ni jemala aspirina v majhnih odmerkih, je bila incidenca APTC dogodkov
35/ 6950 patients (0.50%) for lumiracoxib versus 27/ 6968 patients (0.39%) for NSAIDs, with a HR of 1.22 [95% CI 0.74-2.02] p=0.4343.
35/ 6950 bolnikov (0, 50%) za lumirakoksib proti 27/ 6968 bolnikov (0, 39%) za NSAR, s HR 1, 22 [95% CI 0, 74- 2, 02] p=0, 4343.
When compared separately to ibuprofen and naproxen, the HR were 0.94 [95% CI 0.44-2.04] p=0.8842 and 1.49 [95% CI 0.76-2.92] p=0.2417, respectively.
Ko so ga ločeno primerjali z ibuprofenom in naproksenom, je bil HR 0, 94 [95% CI 0, 44- 2, 04] p=0, 8842 oziroma 1, 49 [95% CI 0, 76- 2, 92] p=0, 2417.
- In the low-dose ASA group, the incidence of APTC events was 24/ 2167 patients (1.11%) for
- V skupini z ASA v majhnih odmerkih je bila incidenca APTC dogodkov 24/ 2167 bolnikov
lumiracoxib versus 23/ 2159 patients (1.07%) for NSAIDs, with a hazard ratio (HR) of 1.04 [95% CI 0.59-1.84] p=0.8918.
(1, 11%) za lumirakoksib proti 23/ 2159 bolnikov (1, 07%) za NSAR, s kvocientom tveganja (HR) 1, 04 [95% CI 0, 59- 1, 84] p=0, 8918.
When compared separately to ibuprofen and naproxen, the HR were 0.56 [95% CI 0.20-1.54] p=0.2603 and 1.42 [95% CI 0.70-2.90] p=0.3368, respectively.
Ko so ga ločeno primerjali z ibuprofenom in naproksenom, je bil HR 0, 56 [95% CI 0, 20- 1, 54] p=0, 2603 oziroma 1, 42 [95% CI 0, 70- 2, 90] p=0, 3368.
- In the overall population, the incidence of APTC events was 59/ 9117 patients (0.65%) for
- V celotni populaciji je bila incidenca APTC dogodkov 59/ 9117 bolnikov (0, 65%) za
lumiracoxib versus 50/ 9127 patients (0.55%) for NSAIDs, with a HR of 1.14 [95% CI 0.78- 1.66] p=0.5074.
lumirakoksib proti 50/ 9127 bolnikov (0, 55%) za NSAR, s HR 1, 14 [95% CI 0, 78- 1, 66] p=0, 5074.
When compared separately to ibuprofen and naproxen, the HR were 0.76 [95% CI 0.41-1.40] p=0.3775 and 1.46 [95% CI 0.89-2.37] p=0.1313, respectively.
Ko so ga ločeno primerjali z ibuprofenom in naproksenom, je bil HR 0, 76 [95% CI 0, 41- 1, 40] p=0, 3775 oziroma 1, 46 [95% CI 0, 89- 2, 37] p=0, 1313.
MI events in TARGET (12-month study) There was no statistically significant difference between lumiracoxib and NSAIDs for incidence of MI (clinical MI and silent MI).
MI dogodki v študiji TARGET (12- mesečna študija) Med lumirakoksibom in NSAR glede incidence MI (klinični MI in tihi MI) ni bilo statistično signifikantne razlike.
- In the population not using low-dose aspirin, the incidence of MI events was 14/ 6950 patients
- V skupini, ki ni jemala aspirina v majhnih odmerkih, je bila incidenca MI dogodkov
(0.20%) for lumiracoxib versus 9/ 6968 patients (0.13%) for NSAIDs, with a HR of 1.47 [95% CI 0.63-3.39] p=0.3706.
14/ 6950 bolnikov (0, 20%) za lumirakoksib proti 9/ 6968 bolnikov (0, 13%) za NSAR, s HR 1, 47 [95% CI 0, 63- 3, 39] p=0, 3706.
When compared separately to ibuprofen and naproxen, the HR were 0.75 [95% CI 0.20-2.79] p=0.6669 and 2.37 [95% CI 0.74-7.55] p=0.1454, respectively.
Ko so ga ločeno primerjali z ibuprofenom in naproksenom, je bil HR 0, 75 [95% CI 0, 20- 2, 79] p=0, 6669 oziroma 2, 37 [95% CI 0, 74- 7, 55] p=0, 1454.
- In the low-dose ASA group, the incidence of MI events was 9/ 2167 patients (0.42%) for
- V skupini z ASA v majhnih odmerkih je bila incidenca MI dogodkov 9/ 2167 bolnikov (0, 42%)
lumiracoxib versus 8/ 2159 patients (0.37%) for NSAIDs, with a HR of 1.14 [95% CI 0.44-2.95] p=0.7899.
za lumirakoksib proti 8/ 2159 bolnikov (0, 37%) za NSAR, s HR 1, 14 [95% CI 0, 44- 2, 95]
When compared separately to ibuprofen and naproxen, the HR were 0.47 [95% CI 0.04-5.14] p=0.5328 and 1.36 [95% CI 0.47-3.93] p=0.5658, respectively.
Ko so ga ločeno primerjali z ibuprofenom in naproksenom, je bil HR 0, 47 [95% CI 0, 04- 5, 14] p=0, 5328 in 1, 36 [95% CI 0, 47- 3, 93] p=0, 5658.
- In the overall population, the incidence of MIs was 23/ 9117 patients (0.25%) for lumiracoxib
- V celotni populaciji je bila incidenca MI 23/ 9117 bolnikov (0, 25%) za lumirakoksib proti
versus 17/ 9127 patients (0.19%) for NSAIDs, with a HR of 1.31 [95% CI 0.70-2.45] p=0.4012.
17/ 9127 bolnikov (0, 19%) za NSAR, s HR 1, 31 [95% CI 0, 70- 2, 45] p=0, 4012.
When compared separately to ibuprofen and naproxen, the HR were 0.66 [95% CI 0.21-2.09] p=0.4833 and 1.77 [95% CI 0.82-3.84] p=0.1471, respectively.
Ko so ga ločeno primerjali z ibuprofenom in naproksenom, je bil HR 0, 66 [95% CI 0, 21- 2, 09] p=0, 4833 oziroma 1, 77 [95% CI 0, 82- 3, 84] p=0, 1471.
17 For systolic blood pressure, mean change from baseline were +0.4 mmHg for lumiracoxib and +2.1 mmHg for NSAIDs (p < 0.0001).
Kardiorenalni učinki v študiji TARGET (12- mesečna študija) Za sistolični krvni tlak je bila povprečna sprememba od izhodne vrednosti +0, 4 mmHg pri lumirakoksibu in +2, 1 mmHg pri NSAR (p < 0, 0001).
For diastolic blood pressure, mean change from baseline were - 0.1 mmHg for lumiracoxib and +0.5 mmHg for NSAIDs (p < 0.0001).
Za diastolični krvni tlak je bila povprečna sprememba od izhodne vrednosti - 0, 1 mmHg pri lumirakoksibu in +0, 5 mmHg pri NSAR (p < 0, 0001).
Absorption Lumiracoxib is rapidly absorbed following oral administration.
Absorpcija Lumirakoksib se po peroralni uporabi hitro absorbira.
At 15 minutes post 400 mg dose, the plasma concentration reached 0.6 µg/ ml, which is sufficiently high to achieve over 90% inhibition of COX-2.
15 minut po 400- miligramskem odmerku je plazemska koncentracija dosegla 0, 6 µg/ ml, ki zadostuje za preko 90- odstotno inhibicijo COX- 2.
Following 400 mg once daily dosing, Cmax was about 9 µg/ ml and AUC was about 31 µg h/ ml.
Po odmerjanju 400 mg enkrat na dan je bila Cmax okrog 9 µg/ ml, AUC pa okrog 31 µg h/ ml.
The absolute bioavailability of lumiracoxib is approximately 74%.
Absolutna biološka uporabnost lumirakoksiba je približno 74%.
Food had no significant effect on either Cmax or AUC of lumiracoxib when either 200 mg or 400 mg film-coated tablets of {Invented Name} were taken with a high-fat meal.
Hrana ni pomembno vplivala niti na Cmax niti na AUC lumirakoksiba, če so jemali bodisi 200- miligramske bodisi 400- miligramske filmsko obložene tablete zdravila {IZMIŠLJENO IME} z mastnim obrokom.
{Invented Name} film- coated tablets can be administered without regard to timing of meals.
{IZMIŠLJENO IME} filmsko obložene tablete se lahko jemljejo brez ozira na čas obrokov.
Distribution Lumiracoxib is highly bound to plasma proteins, (≥ 98%), and binding is independent of concentration over a range of 0.1 to 100 µg/ mL.
Porazdelitev Lumirakoksib se v veliki meri veže na plazemske beljakovine (≥98%), vezava pa je v mejah med 0, 1 in 100 µg/ ml neodvisna od koncentracije.
By about 5 hour post dose, concentrations of lumiracoxib in human synovial fluid of rheumatoid arthritis patients were higher than plasma and remained substantially higher for the remainder of the dose interval (AUC12-24 in synovial fluid was 2.6 times higher than that for plasma).
Približno 5 ur po odmerku so bile koncentracije lumirakoksiba v človeški sinovialni tekočini bolnikov z revmatoidnim artritisom višje kot v plazmi in so ostale znatno višje v času do naslednjega odmerka (AUC12- 24 v sinovialni tekočini je bila 2, 6- krat višja kot v plazmi).
One hour after oral administration of 14[C]-labeled lumiracoxib in a rat model of inflammation, the ratio of radioactivity detected at the site of inflammation versus that detected in the blood was 2:1, and was 8:1 four hours post dose.
Eno uro po peroralni aplikaciji lumirakoksiba, označenega s 14[ C], v podganjem modelu vnetja je bilo razmerje radioaktivnosti, izmerjene na mestu vnetja, in tiste, izmerjene v krvi, 2: 1, štiri ure po odmerku pa 8: 1.
This indicates lumiracoxib and/ or its metabolites are preferentially distributed and retained in inflamed tissue.
To kaže, da se lumirakoksib in/ ali njegovi presnovki prednostno porazdeljujejo in zadržujejo v vnetem tkivu.
Biotransformation In humans, lumiracoxib undergoes extensive hepatic metabolism.
Biotransformacija Pri ljudeh se lumirakoksib intenzivno presnavlja v jetrih.
The oxidative metabolism of lumiracoxib is mainly CYP2C9 mediated.
Oksidativno presnovo lumirakoksiba večinoma posreduje CYP2C9.
Three major metabolites were identified in plasma:
V plazmi so identificirali tri glavne presnovke:
4’ -hydroxy-lumiracoxib, 5-carboxy-lumiracoxib and 4’ - hydroxy-5-carboxy-lumiracoxib.
4 ’ - hidroksi- lumirakoksib, 5- karboksi -
In addition various conjugates (glucuronides and sulfates) of these metabolites are formed.
Poleg tega nastajajo različni konjugati (glukuronidi in sulfati) teh presnovkov.
The 4’ -hydroxy metabolite has similar potency and COX-2 selectivity to lumiracoxib.
4 ’ - hidroksi presnovek ima podobno potenco in selektivnost za COX- 2 kot lumirakoksib.
The concentration of 4’ -hydroxy metabolite in plasma and synovial fluid is low, thus it is unlikely to contribute to efficacy.
Koncentracija 4 ’ - hidroksi presnovka v plazmi in sinovialni tekočini je nizka, zato ni verjetno, da bi ta presnovek prispeval k učinkovitosti zdravila.
Other metabolites are not active as COX-1 or COX-2 inhibitors.
Drugi presnovki niso aktivni kot zaviralci COX- 1 ali COX- 2.
Elimination Lumiracoxib is eliminated predominantly via hepatic metabolism.
Odstranjevanje iz telesa Lumirakoksib se odstranjuje iz telesa pretežno s presnovo v jetrih.
After administration of a single dose of lumiracoxib 400 mg to healthy subjects, 54% of drug-related material was excreted in urine
Po aplikaciji posameznega 400- miligramskega odmerka lumirakoksiba zdravim osebam se je 54% z zdravilom povezanih snovi izločilo v urinu in 43% v blatu.
Only about 5% of the administered dose was recovered in excreta as unchanged lumiracoxib.
Le okrog 5% danega odmerka so prestregli iz izločkov v obliki nespremenjenega lumirakoksiba.
Plasma clearance is 7.7 L/ h.
Plazemski očistek je 7, 7 l/ h.
There is no difference in exposure of lumiracoxib in men and women.
Pri moških in ženskah se izpostavljenost lumirakoksibu ne razlikuje.
In elderly subjects (over 65 years old), a 15% increase in AUC was observed as compared to younger subjects.
Pri starejših osebah (starejših od 65 let) so opazili 15- odstotno zvečanje AUC v primerjavi z mlajšimi osebami.
The pharmacokinetics of lumiracoxib are similar in Asians, Blacks and Caucasians.
Farmakokinetika lumirakoksiba je pri pripadnikih rumene, črne in bele rase podobna.
Compared to healthy subjects, exposure to lumiracoxib was not changed in patients with moderate hepatic impairment (Child-Pugh score 7-8).
V primerjavi z zdravimi osebami se izpostavljenost lumirakoksibu ni spremenila pri bolnikih z zmernimi okvarami jeter (ocena 7- 8 po Child- Pughovi lestvici).
The pharmacokinetics of lumiracoxib have not been studied in patients with severe hepatic impairment (Child-Pugh > 9).
Pri bolnikih s hudim obolenjem jeter ocena > 9 po Child- Pughovi lestvici) farmakokinetike lumirakoksiba niso proučevali.
Renal Insufficiency:
19 Insuficienca ledvic:
When lumiracoxib was administered to patients with end-stage renal disease, a 33% decrease in lumiracoxib Cmax and a 27% decrease in AUC were observed compared to healthy subjects.
Ko so lumirakoksib dali bolnikom z boleznijo ledvic v končnem stadiju, so ugotovili 33- odstotno znižanje Cmax lumirakoksiba in 27- odstotno zmanjšanje AUC v primerjavi z zdravimi osebami.
Mean exposure to the active 4'-hydroxy-lumiracoxib metabolite was largely unaffected.
Povprečna izpostavljenost aktivnemu presnovku 4 '- hidroksi- lumirakoksibu je bila večinoma nespremenjena.