natgillin/translations-raw huggingface dataset:
Celecoxib is well absorbed reaching peak plasma concentrations after approximately 2-3 hours.
Celekoksib se dobro absorbira in doseže največjo koncentracijo v plazmi po približno 2- 3 urah.
Dosing with food (high fat meal) delays absorption by about 1 hour with an increase in total absorption (AUC) of 10 to 20%.
Zaužitje s hrano (zelo masten obrok) upočasni absorpcijo za približno 1 uro, celotna absorpcija (AUC) pa se zveča za 10 do 20%.
Less than 1% of the dose is excreted unchanged in urine.
Manj kot 1% odmerka se nespremenjenega izloči v urin.
The inter-subject variability in the exposure of celecoxib is about 10-fold.
Interindividualna variabilnost izpostavljenosti celekoksibu je približno 10- kratna.
Plasma protein binding is about 97% at therapeutic plasma concentrations and celecoxib is not preferentially bound to erythrocytes.
Pri terapevtskih plazemskih koncentracijah je vezava na beljakovine v plazmi približno 97- odstotna; celekoksib se ne veže prednostno na eritrocite.
Elimination half-life is 8-12 hours.
Razpolovna doba izločanja je 8- 12 ur.
The main metabolites found in the circulation have no detectable COX-1 or COX-2 activity.
Glavni presnovki v obtoku nimajo ugotovljive aktivnosti na COX- 1 ali COX- 2.
Three metabolites, inactive as COX-1 or COX-2 inhibitors, have been identified in human plasma i. e., a primary alcohol, the corresponding carboxylic acid and its glucuronide conjugate.
Pri človeku so v plazmi našli tri presnovke: primarni alkohol, ustrezno karboksilno kislino in njen glukuronidni konjugat; vsi ti presnovki so kot zaviralci COX- 1 ali COX- 2 neaktivni.
Cytochrome P450 CYP2C9 activity is reduced in individuals with genetic polymorphisms that lead to reduced enzyme activity, such as those homozygous for the CYP2C9*3 polymorphism.
Aktivnost citokroma P450 CYP 2C9 je manjša pri posameznikih z genetskim polimorfizmom, ki zmanjšuje aktivnost encima, npr. pri tistih s homozigotnostjo za polimorfizem CYP2C9* 3.
11 In a pharmacokinetic study of celecoxib 200 mg administered once daily in healthy volunteers, genotyped as either CYP2C9*1/ *1, CYP2C9*1/ *3, or CYP2C9*3/ *3, the median Cmax and AUC 0-24 of celecoxib on day 7 were approximately 4-fold and 7-fold, respectively, in subjects genotyped as CYP2C9*3/ *3 compared to other genotypes.
V farmakokinetični študiji celekoksiba 200 mg enkrat na dan pri zdravih prostovoljcih, genotipiziranih kot CYP2C9* 1 / * 1, CYP2C9* 1 / * 3 ali CYP2C9* 3 / * 3, je bila pri preiskovancih, genotipiziranih kot CYP2C9* 3 / * 3, sedmi dan mediana Cmax celekoksiba 4- krat tolikšna, njegova mediana AUC 0- 24 pa 7 - krat tolikšna kot pri drugih genotipih.
In three separate single dose studies, involving a total of 5 subjects genotyped as CYP2C9*3/ *3, single-dose AUC 0-24 increased by approximately 3-fold compared to normal metabolizers.
V treh ločenih študijah posamičnih odmerkov, ki so zajele 5 preiskovancev, genotipiziranih kot CYP2C9* 3 / * 3, je bila AUC 0- 24 po posamičnem odmerku približno 3- krat tolikšna kot pri bolnikih, ki normalno presnavljajo.
It is estimated that the frequency of the homozygous *3/ *3 genotype is 0.3-1.0% among different ethnic groups.
Ocenjena pogostnost homozigotnosti genotipa * 3 / * 3 je v različnih etničnih skupinah od 0, 3 do 1, 0%.
Patients who are known or suspected to be CYP2C9 poor metabolizers based on previous history/ experience with other CYP2C9 substrates should be administered celecoxib with caution (see Section 4.2).
Celekoksib morate previdno uporabljati pri bolnikih, za katere na podlagi anamneze ali izkušenj z drugimi substrati CYP2C9 veste ali sumite, da slabo presnavljajo s CYP2C9 (glejte poglavje 4. 2).
The plasma concentration of celecoxib is approximately 100% increased in elderly women (> 65 years).
Pri starejših ženskah (> 65 let) je koncentracija celekoksiba v plazmi za približno 100% večja.
Compared to subjects with normal hepatic function, patients with mild hepatic impairment had a mean increase in Cmax of 53% and in AUC of 26% of celecoxib.
Pri bolnikih z blago jetrno okvaro je bila Cmax celekoksiba v povprečju za 53% večja, AUC pa za 26% večja kot pri preiskovancih z normalnim delovanjem jeter.
When dosed at 200 mg per day the corresponding values in patients with moderate hepatic impairment were 41% and 146% respectively.
Ob odmerku 200 mg na dan je bila Cmax pri bolnikih z zmerno jetrno okvaro 41% in AUC 146%.
In FAP patients with moderate hepatic impairment (serum albumin of 25-35 g/ l), the daily recommended dose of celecoxib should be reduced by 50%.
Pri bolnikih s FAP, ki imajo zmerno jetrno okvaro (albumin v serumu od 25 do 35 g/ l), je treba priporočeni dnevni odmerek celekoksiba zmanjšati za 50%.
Patients with severe hepatic impairment (serum albumin < 25 g/ l) have not been studied and celecoxib is contraindicated in this patient group.
Študij pri bolnikih s hudo jetrno okvaro (albumin v serumu < 25 g/ l) niso izvedli, zato je celekoksib pri teh bolnikih kontraindiciran.
The pharmacokinetics of celecoxib has not been studied in patients with renal impairment but is unlikely to be markedly changed in these patients since it is mainly eliminated by hepatic metabolism.
Izkušenj s
There is little experience of celecoxib in renal impairment and therefore caution is advised when treating patients with renal impairment.
12 celekoksibom pri bolnikih z ledvično okvaro je malo, zato je pri zdravljenju takšnih bolnikov potrebna previdnost.
Conventional embryo-foetal toxicity studies resulted in dose dependent occurrences of diaphragmatic hernia in rat foetuses and of cardiovascular malformations in rabbit foetuses at systemic exposures to free celecoxib approximately 3 times (rat) and 2 times (rabbit) higher than those achieved at the recommended daily human dose (800 mg).
2- krat večja (kunci) od izpostavljenosti, dosežene s priporočenim dnevnim odmerkom za človeka (800 mg).
Diaphragmatic hernia was also seen in a peri-post natal toxicity study in rats, which included exposure during the organogenetic period.
Diafragmalno hernijo so ugotovili tudi v peri - / postnatalni študiji toksičnih učinkov na podganah, v kateri so bile živali izpostavljene zdravilu tudi med obdobjem organogeneze.
In the latter study, at the lowest systemic exposure where this anomaly occurred in a single animal, the estimated margin relative to the recommended daily human dose was 2 times more than the recommended daily human dose (800 mg).
V tej zadnji študiji, je bila ob najmanjši sistemski izpostavljenosti (pri kateri se je ta anomalija pojavila pri eni sami živali) ocenjeno, da je bil mejni odmerek glede na priporočeni dnevni odmerek za človeka 2- krat večji od priporočenega dnevnega odmerka za človeka (800 mg).
In a peri-post natal study in rats, pup toxicity was observed.
Med peri - / postnatalno študijo na podganah so opažali toksične učinke pri mladičih.
Capsules contain: lactose monohydrate sodium lauryl sulphate povidone K30 croscarmellose sodium
Kapsule vsebujejo: laktozo monohidrat natrijev lavrilsulfat povidon K30 premreženi natrijev karmelozat magnezijev stearat
Clear or opaque PVC/ Aclar/ Aluminium foil blisters.
Prozorni ali motni pretisni omoti iz PVC/ aclar/ aluminijske folije.
17 October 2003
17. oktober 2003
Excipients:
Pomožne snovi: laktoza monohidrat 99, 6 mg.
Lactose Monohydrate 99.6 mgFor a full list of excipients, see section 6.1.
Za celoten seznam pomožnih snovi glejte poglavje 6. 1.
White, opaque capsules with two gold bands marked 7767 and 400.
Bele, neprozorne kapsule z dvema zelenima črtama in oznakama 7767 in 400.
The recommended oral dose is one 400 mg capsule twice per day, taken with food (see section 5.2).
Priporočeni peroralni odmerek je ena 400 mg kapsula dvakrat na dan zaužita s hrano (glejte poglavje 5. 2).
4.3 Contraindications
15 4. 3 Kontraindikacije
14 • Hypersensitivity to the active substance or to any of the excipients (see section 6.1). • Known hypersensitivity to sulphonamides. • Active peptic ulceration or gastrointestinal (GI) bleeding. • Patients who have experienced asthma, acute rhinitis, nasal polyps, angioneurotic oedema, urticaria or other allergic-type reactions after taking acetylsalicylic acid or non steroidal anti-inflammatory drugs (NSAIDs) including COX-2 (cyclooxigenase-2) selective inhibitors. • In pregnancy and in women who can become pregnant unless using an effective method of contraception (see sections 4.5, 4.6 and 5.3) • Breast feeding (see sections 4.6 and 5.3) • Severe hepatic dysfunction (serum albumin< 25 g/l or Child-Pugh score > 10) (Class C). • Patients with renal insufficiency with estimated creatinine clearance < 30 ml/ min. • Inflammatory bowel disease. • Congestive heart failure (NYHA II-IV). • Established ischaemic heart disease, peripheral arterial disease and/or cerebrovascular disease
• Preobčutljivost za zdravilno učinkovino ali katerokoli pomožno snov (glejte poglavje 6. 1). • Znana preobčutljivost za sulfonamide. • Aktiven peptični ulkus ali krvavitev v prebavilih. • Bolniki, ki so po jemanju acetilsalicilne kisline ali nesteroidnih protivnetnih zdravil (NSAID – „ non steroidal antiinflammatory drugs “), vključno s selektivnimi zaviralci COX- 2 (ciklooksigenaze- 2), kdaj imeli astmo, akutni rinitis, nosne polipe, angionevrotični edem, urtikarijo ali kakšno drugo alergijsko reakcijo. • V nosečnosti in pri ženskah, ki lahko zanosijo, če ne uporabljajo učinkovite kontracepcijske zaščite (glejte poglavja 4. 5, 4. 6 in 5. 3) • Dojenje (glejte poglavji 4. 6 in 5. 3). • Hudo poslabšano delovanje jeter (albumin v serumu < 25 g/ l ali ocena po Child- Pughu > 10) (stopnja C) • Bolniki z ledvično insuficienco z ocenjenim očistkom kreatinina < 30 ml/ min. • Vnetna črevesna bolezen. • Kongestivno srčno popuščanje (NYHA II- IV). • Potrjena ishemična bolezen srca, bolezen perifernih arterij in/ ali cerebrovaskularna bolezen
NSAIDs + acetylsalicylic acid has not been demonstrated in long-term clinical trials (see 5.1).
Glede varnosti za prebavila v dolgoročnih kliničnih preskušanjih niso ugotovili pomembne razlike med uporabo selektivnih zaviralcev COX- 2 in acetilsalicilne kisline v primerjavi z uporabo nesteroidnih protivnetnih zdravil in acetilsalicilne kisline (glejte poglavje 5. 1).
The concomitant use of celecoxib and a non-aspirin NSAID should be avoided.
Celekoksiba ne uporabljajte sočasno z ne- aspirinskimi nesteroidnimi protivnetnimi zdravili.
As the cardiovascular risks of celecoxib were increased with the 400 mg twice daily dose in the APC trial (section 5.1), the response of the FAP patient to celecoxib should be re-examined periodically in order to avoid unnecessary exposure in FAP patients for whom celecoxib is not effective (sections 4.2, 4.3, 4.8 and 5.1).
Zato je treba odziv bolnikov s FAP na celekoksib redno preverjati, da bi preprečili nepotrebno izpostavljanje zdravilu pri bolnikih s FAP, pri katerih celekoksib ni učinkovit (glejte poglavja 4. 2, 4. 3, 4. 8 in 5. 1).
15 COX-2 selective inhibitors are not a substitute for acetylsalicylic acid for prophylaxis of cardiovascular thrombo-embolic diseases because of their lack of antiplatelet effect.
Ker selektivni zaviralci COX- 2 nimajo antiagregacijskega delovanja, niso nadomestilo za acetilsalicilno kislino v profilaksi kardiovaskularnih trombemboličnih bolezni.
Skin Reactions Serious skin reactions, some of them fatal, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, have been reported very rarely in association with the use of celecoxib (see section 4.8).
Kožne reakcije Pri uporabi celekoksiba so zelo redko poročali o resnih kožnih reakcijah, nekatere od njih so bile smrtne, vključno z eksfoliacijskim dermatitisom, Stevens- Johnsonovim sindromom in toksično epidermalno nekrolizo (glejte poglavje 4. 8).
Celecoxib may mask fever and other signs of inflammation.
17 Celekoksib lahko prikrije zvišano telesno temperaturo in druge znake vnetja.
Onsenal 400 mg capsules contain lactose (99.6 mg).
Kapsule Onsenal 400 mg vsebujejo laktozo (99, 6 mg).
17 In patients with rheumatoid arthritis celecoxib had no statistically significant effect on the pharmacokinetics (plasma or renal clearance) of methotrexate (in rheumatologic doses).
Pri bolnikih z revmatoidnim artritisom celekoksib ni statistično značilno vplival na farmakokinetiko (plazemski ali ledvični očistek) metotreksata (v revmatoloških odmerkih).
In individuals who are CYP2C9 poor metabolisers and demonstrate increased systemic exposure to celecoxib, concomitant treatment with CYP2C9 inhibitors could result in further increases in celecoxib exposure.
Pri posameznikih, ki slabo presnavljajo s CYP2C9 in imajo večjo sistemsko izpostavljenost celekoksibu, lahko sočasno zdravljenje z zaviralci CYP2C9 dodatno poveča izpostavljenost celekoksibu.
Such combinations should be avoided in known CYP2C9 poor metabolisers (see sections 4.2 and 5.2).
Pri bolnikih, za katere je znano, da slabo presnavljajo s CYP2C9, ne uporabljajte takšnih kombinacij (glejte poglavji 4. 2 in 5. 2).
4.8 Undesirable effects Adverse reactions are listed by system organ class and ranked by frequency in Table 1, reflecting data from the following sources:
Podatki so iz naslednjih virov:
which an estimated > 70 million patients were treated with celecoxib (various doses, durations, and indications).
katerim je celekoksib po ocenah dobivalo > 70 milijonov bolnikov (različni odmerki, trajanje in indikacije).
Because not all adverse drug reactions are reported to the MAH and included in the safety database, the frequencies of these reactions cannot be reliably determined.
Zato pogostnosti teh učinkov ni mogoče zanesljivo ugotoviti.
18
Redki
Common
(≥ 1/ 100 do <
Uncommon
(≥ 1/ 1000 do < 1/ 100)
Rare
(≥ 1/ 10. 000 do <
Frequency Not Known
znana
(≥ 1/ 100 to < 1/ 10)
Infekcijske in
(≥ 1/ 1000 to < 1/ 100)
1/ 10) sinuzitis, okužba
(≥ 1/ 10,000 to < 1/ 1000)
1/ 1000)
Leucopenia, thrombocytopeni a
levkopenija, trombocitopenija
Vascular
20 palpitacije, tahikardija
Hypertension, hypertension aggravate d
Žilne bolezni
Gastrointestinal
faringitis, rinitis,
Abdominal pain, diarrhoea, dyspepsia, flatulence
dispneja
Constipation, eructation, gastritis, stomatitis, vomiting, aggravation of gastrointestinal inflammation
bronhospazem
Duodenal, gastric, Nausea, acute oesophageal, pancreatitis, intestinal, and gastrointestinal colonic ulceration; haemorrhage, dysphagia, colitis/ colitis aggravated intestinal perforation; oesophagitis, melaena; pancreatitis
prsnega koša in kašelj mediastinalnega prostora Bolezni prebavil bolečine v
Hepatobiliary
zaprtje, riganje, gastritis razjeda na
Abnormal hepatic function, increased SGOT and SGPT
navzea, akutni
Elevation of Hepatitis, hepatic failure hepatic enzymes jaundice
trebuhu, driska, stomatitis, bruhanje, dispepsija, poslabšanje flatulenca gastrointestinalnega vnetja
19
dvanajstniku, želodcu pankreatitis, požiralniku, tankem ingastrointestinalna debelem črevesu, krvavitev, disfagija, perforacija kolitis/ poslabšanje črevesa, ezofagitis, kolitisa melena, pankreatitis
Skin and subcutaneous
Bolezni jeter,
Rash, pruritus
nenormalno delovanje zvišanje jetrnih
Urticaria
hepatitis, jetrna
Alopecia, photosensitivity
žolčnika in žolčevodov
Musculoskeletal and connective
jeter, zvišana SGOT in encimov SGPT
Leg cramps
odpoved, zlatenica
Arthralgia, myositis
Bolezni kože in izpuščaj, srbenje urtikarija podkožja
Renal and urinary
alopecija, fotosenzitivnost
Increased creatinine, BUN increased
ekhimoze, bulozen izpuščaj, eksfoliativni dermatitis, multiformni eritem, Stevens- Johnsonov sindrom, toksična epidermalna nekroliza, angioedem
Acute renal failure, interstitial nephritis, hyponatraemia
krči v nogah Bolezni mišično - skeletnega sistema in vezivnega tkiva
Reproductive and breast
artralgija, miozitis
Menstrual disorder
zvišan kreatinin, Bolezni sečil
1
akutna odpoved
General
zvišana sečnina Motnje reprodukcije in dojk Splošne težave gripi podobni simptomi, periferni edemi/ zastajanje tekočine 1
Flu-like symptoms, peripheral oedema/ fluid retention
ledvic, intersticijski nefritis, hiponatriemija menstruacijske motnje
The additional adverse reactions listed by system organ class and ranked by frequency in Table 2 were reported at incidence rates greater than placebo for subjects treated with celecoxib 400 mg to 800 mg daily in long-term polyp prevention trials of duration up to 3 years (the APC and PreSAP trials; see Section 5.1, Pharmacodynamic properties:
21 400 do 800 mg na dan v dolgoročnih preskušanjih preprečevanja polipov, ki so trajala do 3 leta (preskušanji APC in PreSAP; glejte poglavje 5. 1, Farmakodinamične lastnosti:
Infections and infestations
okužba ušesa, glivična okužba okužba s Helicobactrom, herpes Infekcijske in parazitske bolezni
Ear infection, fungal infection (fungal infections were primarily nonsystemic)
zoster, šen, okužba rane, okužbe
Helicobacter infection, herpes zoster, erysipelas, wound infection, gingival infection, labrynthitis, bacterial infection
Neoplazme Psihiatrične motnje Bolezni živčevja Očesne bolezni Ušesne bolezni, vključno z motnjami labirinta
Neoplasms Psychiatric Nervous system Eye
predvsem nesistemske)
Lipoma Sleep disorder Cerebral infarction Vitreous floaters; conjunctival hemorrhage
dlesni, labirintitis, bakterijska okužba lipom motnja spanja cerebralni infarkt delci v steklovini, veznična krvavitev hipakuza
Ear and labyrinth
angina pektoris, miokardni
Hypoacusis
nestabilna angina pektoris,
Cardiac
infarkt
Angina unstable, aortic valve incompetence, coronary artery atherosclerosis, sinus bradycardia, ventricular hypertropy
insuficienca aortne zaklopke, ateroskleroza koronarnih arterij, sinusna bradikardija, prekatna hipertrofija
Respiratory, thoracic,
Bolezni dihal, prsnega koša in mediastinalnega prostora
and
Bolezni prebavil
mediastinal
driska *
Gastrointestinal
navzea, gastroezofagealna
Diarrhoea*
hemoroidalna krvavitev, pogosto
Nausea, gastroesophageal reflux disease, diverticulum, vomiting, * dysphagia, irritable bowel syndrome
refluksna bolezen, divertikel, iztrebljanje, razjeda v ustih, bruhanje, * disfagija, sindrom stomatitis razdražljivega črevesa alergijski dermatitis Bolezni kože in podkožja Bolezni mišično - skeletnega sistema in vezivnega tkiva
Haemorrhoidal haemorrhage, frequent bowel movements, mouth ulceration, stomatitis
spazmi mišic
Skin and subcutaneous
ganglion
Dermatitis allergic
Bolezni sečil
Musculoskeletal and connective
nefrolitiaza, zvišanje kreatinina v krvi
Muscle spasms
nikturija
Ganglion
Motnje reprodukcije
Renal and urinary
benigna hipertrofija prostate,
Nephrolithiasis, blood creatinine increased
krvavitev iz nožnice, občutljivost
Nocturia
in dojk
Reproductive and breast General and administrative site
prostatitis, zvišanje za
Benign prostatic hyperplasia, prostatitis, prostatic specific antigen increased Edema
dojk, dismenoreja, cista jajčnika,
Vaginal haemorrhage, breast tenderness, dysmenorrhea, ovarian cyst, menopausal symptoms
Splošne težave in spremembe na mestu aplikacije
Investigations
prostato specifičnega antigena edemi
Foot fracture, lower limb fracture, epicondylitis, tendon rupture, fracture
Zvišanje kalija, natrija, hemoglobina v krvi Znižanje hematokrita, testosterona v krvi zlom stopala, zlom spodnje okončine, epikondilitis, pretrganje tetive, zlom
In final data (adjudicated) from the APC trial in patients treated with celecoxib 800 mg daily for up to 3 years, the excess rates over placebo were 11 events per 1000 patients for myocardial infarction (common); and 5 events per 1000 patients for stroke (uncommon; types of stroke not differentiated).
22 Po oceni končnih podatkov preskušanj APC in PreSAP pri bolnikih, zdravljenih z 800 mg celekoksiba na dan do 3 leta, je bil presežni delež miokardnih infarktov v primerjavi s placebom 11 dogodkov na 1000 bolnikov (pogosto) in možganskih kapi 5 dogodkov na 1000 bolnikov (občasno; kapi nerazvrščene po tipu).
Single doses up to 1400 mg and multiple doses up to 1400 mg twice daily have been administered to healthy subjects for nine days without clinically significant adverse events.
Zdravi preiskovanci so devet dni dobivali posamične odmerke do 1. 400 mg in večkratne odmerke do 1. 400 mg dvakrat na dan brez klinično pomembnih neželenih učinkov.
Celecoxib is an oral, selective cyclooxygenase-2 (COX-2) inhibitor.
Celekoksib je peroralen, selektiven zaviralec ciklooksigenaze- 2 (COX- 2).
21 Cyclooxygenase is responsible for generation of prostaglandins.
Ciklooksigenaza je odgovorna za nastajanje prostaglandinov.
Celecoxib inhibits tumour formation in preclinical models of colon cancer, which overexpress COX-2, whether induced by chemical (rat AOM model) or genetic (MIN mouse model) mutation.
23 V predkliničnih modelih karcinoma na kolonu s prekomerno izraženo COX- 2 celekoksib zavira nastanek tumorjev, izzvanih s kemično (model podgan AOM) ali genetsko (model miši MIN) mutacijo.
The long-term cardiovascular toxicity in children exposed to celecoxib has not been evaluated and it is unknown if the long-term risk may be similar to that seen in adults exposed to celecoxib or other COX-2 selective and non-selective NSAIDs (see section 4.4; cardiovascular effects).
Tako ni znano, ali je dolgoročno tveganje morda podobno, kot je ugotovljeno pri odraslih osebah, izpostavljenih celekoksibu ali drugim COX- 2 selektivnim in neselektivnim nesteroidnim protivnetnim zdravilom (glejte poglavje 4. 4, Srčnožilni učinki).
Cardiovascular Safety – Long-Term Studies Involving Subjects With Sporadic Adenomatous Polyps:
Srčnožilna varnost – dolgoročne študije preiskovancev s sporadičnimi adenomatoznimi polipi:
22 death, myocardial infarction, or stroke (adjudicated) with celecoxib compared to placebo over 3 years of treatment.
V preskušanju APC so med 3- letnim zdravljenjem pri celekoksibu v primerjavi s placebom ugotovili z odmerkom povezan porast sestavljenega opazovanega dogodka srčnožilne smrti, miokardnega infarkta ali možganske kapi (presojeno).
The relative risk compared to placebo for a similar composite endpoint (CV death, MI, stroke) was 1.14 (95% CI 0.61 - 2.12) with celecoxib 200 mg twice daily.
Relativno tveganje za podoben sestavljeni opazovani dogodek (srčnožilna smrt, miokardni infarkt, možganska kap) je bilo za celekoksib 200 mg dvakrat na dan v
Cytochrome P450 2C9 activity is reduced in individuals with genetic polymorphisms that lead to reduced enzyme activity, such as those homozygous for the CYP2C9*3 polymorphism.
Aktivnost citokroma P450 CYP 2C9 je manjša pri posameznikih z genetskim polimorfizmom, ki zmanjšuje aktivnost encima, npr. pri tistih s homozigotnostjo za polimorfizem CYP2C9* 3.
In a pharmacokinetic study of celecoxib 400 mg administered once daily in healthy volunteers, genotyped as either CYP2C9*1/ *1, CYP2C9*1/ *3, or CYP2C9*3/ *3, the median Cmax and AUC 0-24 of celecoxib on day 7 were approximately 4-fold and 7-fold, respectively, in subjects genotyped as CYP2C9*3/ *3 compared to other genotypes.
V farmakokinetični študiji celekoksiba 200 mg enkrat na dan pri zdravih prostovoljcih, genotipiziranih kot CYP2C9* 1 / * 1, CYP2C9* 1 / * 3 ali CYP2C9* 3 / * 3, je bila pri preiskovancih, genotipiziranih kot CYP2C9* 3 / * 3, sedmi dan mediana Cmax celekoksiba 4- krat tolikšna, njegova mediana AUC 0- 24 pa 7- krat tolikšna kot pri drugih genotipih.
In three separate single dose studies, involving a total of 5 subjects genotyped as
V treh ločenih študijah posamičnih odmerkov, ki so zajele 5 preiskovancev, genotipiziranih kot CYP2C9* 3 / * 3, je bila AUC 0- 24 po posamičnem odmerku približno 3- krat tolikšna kot pri bolnikih, ki normalno presnavljajo.
23 CYP2C9*3/ *3, single-dose AUC 0-24 increased by approximately 3-fold compared to normal metabolizers.
Ocenjena pogostnost homozigotnosti genotipa * 3 / * 3 je v različnih etničnih skupinah od 0, 3 do 1, 0%.
The pharmacokinetics of celecoxib has not been studied in patients with renal impairment but is unlikely to be markedly changed in these patients since it is mainly eliminated by hepatic metabolism.
25 Farmakokinetika celekoksiba pri bolnikih z ledvično okvaro niso raziskali, vendar ni verjetno, da bi bila bistveno spremenjena, ker se zdravilo izloča predvsem s presnovo v jetrih.
24 Printing ink contains: shellac propylene glycol iron oxide (E172)
Črnilo vsebuje: šelak propilenglikol železov oksid (E172) modro FCF (E133)
Opaque PVC/ Aclar/ Aluminium foil blisters.
Motni pretisni omoti iz PVC/ aluminijske folije.