natgillin/translations-raw huggingface dataset:
In clinical studies, approximately 13.5% of the dose was removed over a 3- to 4-hour haemodialysis session.
V kliničnih študijah so približno 13, 5% odmerka odstranili s 3 - do 4- urno hemodializo.
It is not known if sitagliptin is dialyzable by peritoneal dialysis.
Ni znano, ali se sitagliptin dializira s peritonealno dializo.
In the event of an overdose, it is reasonable to employ the usual supportive measures, e. g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required.
Pri prevelikem odmerjanju je smiselno uporabiti običajne podporne ukrepe, na primer odstranitev neabsorbiranega zdravila iz prebavil, uvedbo kliničnega nadzora (vključno s spremljanjem elektrokardiograma) in po potrebi uvedbo podpornega zdravljenja.
Combinations of oral blood glucose lowering drugs, ATC code:
Farmakoterapevtska skupina: kombinacije peroralnih antidiabetikov, oznaka ATC:
Efficib combines two antihyperglycaemic agents with complementary mechanisms of action to improve glycaemic control in patients with type 2 diabetes: sitagliptin phosphate, a dipeptidyl peptidase 4 (DPP-4) inhibitor, and metformin hydrochloride, a member of the biguanide class.
Vsebuje sitagliptinijev fosfat, ki je zaviralec dipeptidil- peptidaze 4 (DPP- 4), in metforminijev klorid, ki spada med bigvanide.
9 Sitagliptin Sitagliptin phosphate is an orally-active, potent, and highly selective inhibitor of the dipeptidyl peptidase 4 (DPP-4) enzyme for the treatment of type 2 diabetes.
Sitagliptin Sitagliptinijev fosfat je peroralno aktivni, močan in zelo selektiven zaviralec encima dipeptidil - peptidaze 4 (DPP- 4) in se uporablja za zdravljenje sladkorne bolezni tipa 2.
The DPP-4 inhibitors are a class of agents that act as incretin enhancers.
Zaviralci DPP so učinkovine, ki delujejo kot spodbujevalci inkretina.
By inhibiting the DPP-4 enzyme, sitagliptin increases the levels of two known active incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).
Z zaviranjem encima DPP- 4 sitagliptin zviša raven dveh znanih inkretinskih hormonov, glukagonu podobnega peptida- 1 (GLP- 1; » glucagon- like peptide - 1 «) in od glukoze odvisnega insulinotropnega polipeptida (GIP; » glucose- dependent insulinotropic
When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells.
Kadar so koncentracije glukoze v krvi normalne ali zvišane, GLP- 1 in GIP povečata sintezo insulina in njegovo sproščanje iz celic beta trebušne slinavke.
GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production.
GLP- 1 tudi zmanjša izločanje glukagona iz celic alfa trebušne slinavke, kar povzroči zmanjšano nastajanje glukoze v jetrih.
When blood glucose levels are low, insulin release is not enhanced and glucagon secretion is not suppressed.
Kadar so ravni glukoze nizke, se izločanje insulina ne spodbudi in sekrecija glukagona se ne zavira.
Sitagliptin is a potent and highly selective inhibitor of the enzyme DPP-4 and does not inhibit the closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations.
Sitagliptin je močan in zelo selektiven zaviralec encima DPP- 4 ter pri terapevtskih koncentracijah ne zavira sorodnih encimov DPP- 8 ali DPP- 9.
Sitagliptin differs in chemical structure and pharmacological action from GLP-1 analogues, insulin, sulphonylureas or meglitinides, biguanides, peroxisome proliferator-activated receptor gamma (PPARγ) agonists, alpha- glucosidase inhibitors, and amylin analogues.
Sitagliptin se po kemijski strukturi in farmakološkem delovanju razlikuje od analogov GLP- 1, insulina, slulfonilsečnin ali meglitinidov, bigvanidov, agonistov receptorjev gama, aktiviranih s peroksisomskim proliferatorjem (PPARγ – peroxisome proliferator- activated receptor gamma), zaviralcev alfa- glukozidaze in analogov amilina.
Overall, sitagliptin improved glycaemic control when used in combination with metformin (as initial or add-on therapy) and in combination with a sulphonylurea and metformin, as measured by clinically relevant reductions in HbA1c from baseline at study endpoint (see Table 3).
To so ugotovili s klinično pomembnim zmanjšanjem vrednosti HbA1c od izhodišča pri opazovanem študijskem dogodku (glejte tabelo 3).
Reduction in fasting plasma glucose (FPG) was observed at 3 weeks, the first time point at which FPG was measured.
Znižanje glukoze v plazmi na tešče (FPG – fasting plasma glucose) so opazili po 3 tednih, ko so prvič merili FPG.
Body weight did not increase from baseline with sitagliptin therapy.
Telesna masa se v primerjavi z izhodiščno vrednostjo ni povečala.
Improvements in surrogate markers of beta cell function, including HOMA-β (Homeostasis Model Assessment-β), proinsulin to insulin ratio, and measures of beta cell responsiveness from the frequently-sampled meal tolerance test were observed.
Opazili so izboljšanje surogatnih markerjev funkcije celic beta, vključno s HOMA– β (Homeostasis Model Assessment– β), razmerjem proinsulin/ insulin in meritvami odzivnosti celic beta po pogosto izvedenem tolerančnem testu s hrano.
Studies of sitagliptin in combination with metformin In a 24-week, placebo-controlled clinical study to evaluate the efficacy and safety of the addition of sitagliptin 100 mg once daily to ongoing metformin, sitagliptin provided significant improvements in glycaemic parameters compared with placebo.
Študije sitagliptina v kombinaciji z metforminom V 24- tedenski s placebom nadzorovani študiji, v kateri so vrednotili učinkovitost in varnost sitagliptina (100 mg enkrat na dan), če so ga dodali potekajočemu zdravljenju z metforminom, je sitagliptin pomembno izboljšal glikemične parametre v primerjavi s placebom.
Change from baseline in body weight was similar for patients treated with sitagliptin relative to placebo.
Glede na izhodiščno vrednost je bila sprememba telesne mase pri bolnikih, ki so prejemali sitagliptin, podobna kot pri bolnikih, ki so prejemali placebo.
In a 24-week placebo-controlled factorial study of initial therapy, sitagliptin 50 mg twice daily in combination with metformin (500 mg or 1000 mg twice daily) provided significant improvements in glycaemic parameters compared with either monotherapy.
V 24- tedenski s placebom nadzorovani študiji začetnega zdravljenja je sitagliptin v odmerku 50 mg dvakrat na dan v kombinaciji z metforminom (500 mg ali 1. 000 mg dvakrat na dan) pomembno izboljšal glikemične parametre v primerjavi z zdravljenjem z vsakim zdravilom posebej.
The decrease in body weight with the combination of sitagliptin and metformin was similar to that observed with metformin alone or placebo; there was no change from baseline for patients on sitagliptin alone.
Zmanjšanje telesne mase je bilo pri uporabi kombinacije sitagliptina in metformina podobno kot pri uporabi metformina samega ali placeba; telesna masa se v primerjavi z izhodiščno vrednostjo ni spremenila.
The incidence of hypoglycaemia was similar across treatment groups.
Pogostnost hipoglikemije je bila podobna v vseh skupinah.
Study of sitagliptin in combination with metformin and a sulphonylurea A 24-week placebo-controlled study was designed to evaluate the efficacy and safety of sitagliptin (100 mg once daily) added to glimepiride (alone or in combination with metformin).
Študija sitagliptina v kombinaciji z metforminom in s sulfonilsečnino Zasnovana je bila 24- tedenska s placebom nadzorovana študija, v kateri so vrednotili učinkovitost in varnost sitagliptina (100 mg enkrat na dan), če so ga dodali glimepiridu (samemu ali v kombinaciji z metforminom).
The addition of sitagliptin to glimepiride and metformin provided significant improvements in glycaemic parameters.
V primerjavi s placebom so se pri dodatku sitagliptina glimepiridu samemu ali glimepiridu in metforminu glikemični parametri pomembno izboljšali.
Patients treated with sitagliptin had a modest increase in body weight (+1.1 kg) compared to those given placebo.
Bolnikom, ki so prejemali sitagliptin, se je telesna masa v primerjavi z bolniki, ki so prejemali placebo, zmerno povečala (+1, 1 kg).
10 Table 3:
10 Tabela 3:
HbA1c results in placebo-controlled combination therapy studies of sitagliptin and metformin*
Vrednosti HbA1c v s placebom nadzorovanih študijah kombiniranega zdravljenja s sitagliptinom in metforminom *
Mean baseline
Povprečna S placebom korigirana Povprečna sprememba povprečna sprememba vrednosti izhodiščna vrednosti HbA1c od Študija HbA1c (%) v 24. tednu † vrednost izhodišča (%) v Sitagliptin 100 mg enkrat na dan, dodan k že
in HbA1c (%) at Week 24†
24.
at Week 24†
tednu †
-0.7
(95- odstotni IZ) – 0, 7 ‡
-0.7‡
– 0, 7
(-0.8, -0.5)
(– 0, 8, – 0, 5) – 0, 9 ‡
added to ongoing glimepiride + metformin therapy (N=115) Initial Therapy (twice daily):
glimepiridom in metforminom (N = 115) Začetno zdravljenje (dvakrat na dan):
-0.6
– 0, 6
-0.9‡ (-1.1, -0.7)
(– 1, 1, – 0, 7) – 1, 6 ‡
Sitagliptin 50 mg + metformin 500 mg (N=183) Initial Therapy (twice daily):
sitagliptin 50 mg + metformin 500 mg (N = 183) Začetno zdravljenje (dvakrat na dan):
-1.4
– 1, 4
-1.6‡ (-1.8, -1.3)
(– 1, 8, – 1, 3) – 2, 1 ‡
Sitagliptin 50 mg + metformin 1000 mg (N=178)
sitagliptin 50 mg + metformin 1. 000 mg (N = 178)
-1.9
– 1, 9
-2.1‡ (-2.3, -1.8)
(– 2, 3 – 1, 8)
* All Patients Treated Population (an intention-to-treat analysis). † Least squares means adjusted for prior antihyperglycaemic therapy status and baseline value. ‡ p < 0.001 compared to placebo or placebo + combination treatment.
p < 0, 001 v primerjavi s placebom ali placebom + kombiniranim zdravljenjem ‡
In a 52-week study, comparing the efficacy and safety of the addition of sitagliptin 100 mg once daily or glipizide (a sulphonylurea agent) in patients with inadequate glycaemic control on metformin monotherapy, sitagliptin was similar to glipizide in reducing HbA1c (-0.7% mean change from baselines at week 52, with baseline HbA1c of approximately 7.5% in both groups).
V 52- tedenski študiji, v kateri so primerjali učinkovitost in varnost sitagliptina v odmerku 100 mg enkrat na dan in glipizida (pripravek sulfonilsečnine) pri bolnikih z neustrezno urejenostjo glikemije s samostojnim zdravljenjem z metforminom, je bil sitagliptin pri zmanjševanju HbA1c podoben glipizidu (– 0, 7- odstotna povprečna sprememba glede na izhodiščno vrednost po 52 tednih, pri vrednosti HbA1c približno 7, 5% v obeh skupinah).
The mean glipizide dose used in the comparator group was 10 mg per day with approximately 40% of patients requiring a glipizide dose of ≤ 5 mg/ day throughout the study.
Povprečni odmerek glipizida, ki so ga uporabili v primerjalni skupini, je bil 10 mg na dan, pri čemer je ves čas trajanja študije približno 40% bolnikov potrebovalo odmerek glipizida ≤ 5 mg/ dan.
Patients treated with sitagliptin exhibited a significant mean decrease from baseline in body weight (-1.5 kg) compared to a significant weight gain in patients administered glipizide (+1.1 kg).
Pri bolnikih, ki so prejemali sitagliptin, so opazili pomembno povprečno zmanjšanje telesne mase glede na izhodiščno vrednost (– 1, 5 kg) v primerjavi z bolniki, ki so prejemali glipizid (+1, 1 kg).
In this study, the proinsulin to insulin ratio, a marker of efficiency of insulin synthesis and release, improved with sitagliptin and deteriorated with glipizide treatment.
V tej študiji se je razmerje proinsulin/ insulin, ki je označevalec učinkovitosti sinteze insulina, pri zdravljenju s sitagliptinom izboljšalo, pri zdravljenju z glipizidom pa poslabšalo.
The incidence of hypoglycaemia in the sitagliptin group (4.9%) was significantly lower than that in the glipizide group (32.0%).
Pojavnost hipoglikemije je bila v skupini, ki je prejemala sitagliptin (4, 9%), pomembno manjša, kot v skupini, ki je prejemala glipizid (32, 0%).
Metformin Metformin is a biguanide with antihyperglycaemic effects, lowering both basal and postprandial plasma glucose.
Metformin Metformin je bigvanid z antihiperglikemičnimi učinki in znižuje koncentracijo glukoze v plazmi na tešče in po obroku.
- by reduction of hepatic glucose production by inhibiting gluconeogenesis and glycogenolysis
- z zaviranjem glukoneogeneze in glikogenolize zmanjšuje nastajanje glukoze v jetrih;
Metformin stimulates intracellular glycogen synthesis by acting on glycogen synthase.
11 Metformin stimulira znotrajcelično sintezo glikogena tako, da deluje na glikogen- sintazo.
Metformin increases the transport capacity of specific types of membrane glucose transporters (GLUT-1 and GLUT-4).
Metformin povečuje transportno zmožnost specifičnih tipov membranskih prenašalcev za glukozo (GLUT- 1 in GLUT- 4).
This has been shown at therapeutic doses in controlled, medium-term or long-term clinical studies: metformin reduces total cholesterol, LDLc and triglyceride levels.
Slednje je bilo dokazano v kontroliranih, srednje dolgih ali dolgotrajnejših kliničnih študijah z uporabo terapevtskih odmerkov: metformin znižuje skupni holesterol, LDL- holesterol in raven trigliceridov.
11 The prospective randomised (UKPDS) study has established the long-term benefit of intensive blood glucose control in type 2 diabetes.
V prospektivni randomizirani študiji (UKPDS) so ugotovili dolgoročno korist intenzivne urejenosti glukoze v krvi pri sladkorni bolezni tipa 2.
- a significant reduction of the absolute risk of any diabetes-related complication in the metformin
- pomembno zmanjšanje absolutnega tveganja za katerikoli s sladkorno boleznijo povezani zaplet
group (29.8 events/ 1,000 patient-years) versus diet alone (43.3 events/ 1,000 patient-years), p=0.0023, and versus the combined sulphonylurea and insulin monotherapy groups (40.1 events/ 1,000 patient-years), p=0.0034
v skupini bolnikov, ki so se zdravili z metforminom (29, 8 primerov/ 1. 000 bolnik - let), v primerjavi s skupino bolnikov, ki je imela predpisano samo dieto (43, 3 primerov/ 1. 000 bolnik - let), p = 0, 0023, ter v primerjavi s skupino, ki je prejemala še sulfonilsečnino, in skupino, ki je jemala samo insulin (40, 1 primerov/ 1. 000 bolnik - let), p = 0, 0034;
- a significant reduction of the absolute risk of any diabetes-related mortality: metformin
- pomembno zmanjšanje absolutnega tveganja za umrljivost, povezano s sladkorno boleznijo:
7.5 events/ 1,000 patient-years, diet alone 12.7 events/ 1,000 patient-years, p=0.017
metformin – 7, 5 primerov/ 1. 000 bolnik - let, samo dieta – 12, 7 primerov/ 1. 000 bolnik - let, p = 0, 017;
- a significant reduction of the absolute risk of overall mortality: metformin
- pomembno zmanjšanje absolutnega tveganja za skupno umrljivost: metformin –
13.5 events/ 1,000 patient-years versus diet alone 20.6 events/ 1,000 patient-years, (p=0.011), and versus the combined sulphonylurea and insulin monotherapy groups 18.9 events/ 1,000 patient-years (p=0.021)
13, 5 primerov/ 1. 000 bolnik - let, samo dieta – 20, 6 primerov/ 1. 000 bolnik - let (p = 0, 011), skupaj s sulfonilsečnino in monoterapijo z insulinom – 18, 9 primerov/ 1. 000 bolnik - let (p = 0, 021);
- a significant reduction in the absolute risk of myocardial infarction: metformin
- pomembno zmanjšanje absolutnega tveganja za miokardni infarkt: metformin –
11 events/ 1,000 patient-years, diet alone 18 events/ 1,000 patient-years, (p=0.01).
11 primerov/ 1. 000 bolnik - let, samo dieta – 18 primerov/ 1. 000 bolnik - let, (p = 0, 01).
Efficib A bioequivalence study in healthy subjects demonstrated that the Efficib (sitagliptin/ metformin hydrochloride) combination tablets are bioequivalent to co-administration of sitagliptin phosphate and metformin hydrochloride as individual tablets.
V bioekvivalenčni študiji pri zdravih osebah so pokazali, da so kombinirane tablete Efficib (sitagliptin/ metforminijev klorid) bioekvivalentne sočasni uporabi sitagliptinijevega fosfata in metforminijevega klorida v obliki posameznih tablet.
Sitagliptin Absorption Following oral administration of a 100-mg dose to healthy subjects, sitagliptin was rapidly absorbed, with peak plasma concentrations (median Tmax) occurring 1 to 4 hours post-dose, mean plasma AUC of sitagliptin was 8.52 μ M• hr, Cmax was 950 nM.
Absorpcija Po peroralni uporabi 100- miligramskega odmerka pri zdravih osebah se je sitagliptin hitro absorbiral; največje koncentracije v plazmi (srednja Tmax) so se pojavile v 1 do 4 urah po odmerku, povprečna vrednost AUC sitagliptina v plazmi je bila 8, 52 μM• hr, vrednost Cmax je bila 950 nM.
The absolute bioavailability of sitagliptin is approximately 87%.
Absolutna biološka uporabnost sitagliptina je približno 87%.
Dose-proportionality was not established for Cmax and C24hr (Cmax increased in a greater than dose-proportional manner and C24hr increased in a less than dose-proportional manner).
Za vrednosti Cmax in C24hr niso ugotovili sorazmernega povečanja z odmerkom (vrednost Cmax se je povečala bolj kot sorazmerno, vrednost C24hr pa se je povečala manj kot sorazmerno).
Distribution The mean volume of distribution at steady state following a single 100-mg intravenous dose of sitagliptin to healthy subjects is approximately 198 litres.
Porazdelitev Pri zdravih osebah je povprečni volumen porazdelitve v stanju dinamičnega ravnovesja po enkratnem 100- miligramskem intravenskem odmerku približno 198 litrov.
The fraction of sitagliptin reversibly bound to plasma proteins is low (38%).
Delež sitagliptina, vezanega na beljakovine v plazmi, je majhen (38%).
Metabolism Sitagliptin is primarily eliminated unchanged in urine, and metabolism is a minor pathway.
12 Presnova Sitagliptin se primarno izloča z urinom v nespremenjeni obliki, presnova pa je manj pomemben način izločanja.
Approximately 79% of sitagliptin is excreted unchanged in the urine.
Približno 79% sitagliptina se izloči z urinom v nespremenjeni obliki.
Following a [14C]sitagliptin oral dose, approximately 16% of the radioactivity was excreted as metabolites of sitagliptin.
Po peroralnem odmerku [14C] sitagliptina se je približno 16% radioaktivnosti izločilo v obliki presnovkov sitagliptina.
Six metabolites were detected at trace levels and are not expected to contribute to the plasma DPP-4 inhibitory activity of sitagliptin.
Šest presnovkov je bilo odkritih v sledeh, zanje pa se ne pričakuje, da sodelujejo pri zaviralnem delovanju sitagliptina na DPP- 4 v plazmi.
In vitro data showed that sitagliptin is not an inhibitor of CYP isoenzymes CYP3A4, 2C8, 2C9, 2D6, 1A2, 2C19 or 2B6, and is not an inducer of CYP3A4 and CYP1A2.
Podatki, pridobljeni in vitro, kažejo, da sitagliptin ni zaviralec izoencimov CYP CYP3A4, 2C8, 2C9, 2D6, 1A2, 2C19 ali 2B6 ter ni induktor CYP3A4 in CYP1A2.
12 Elimination Following administration of an oral [14C]sitagliptin dose to healthy subjects, approximately 100% of the administered radioactivity was eliminated in faeces (13%) or urine (87%) within one week of dosing.
Izločanje Po dajanju peroralnega odmerka [14C] sitagliptina zdravim osebam se je v enem tednu po prejemu odmerka približno 100% prejete radioaktivnosti izločilo z blatom (13%) ali urinom (87%).
The apparent terminal t½ following a 100-mg oral dose of sitagliptin was approximately 12.4 hours.
Po prejemu 100 mg peroralnega odmerka sitagliptina je navidezni končni t1/ 2 znašal približno 12, 4 ure.
Sitagliptin accumulates only minimally with multiple doses.
Kopičenje sitagliptina po večkratnih odmerkih je majhno.
The renal clearance was approximately 350 ml/ min.
Ledvični očistek je bil približno 350 ml/ min.
Sitagliptin is a substrate for human organic anion transporter-3 (hOAT-3), which may be involved in the renal elimination of sitagliptin.
Sitagliptin je substrat za humani organski anionski prenašalec- 3 (hOAT- 3; » human organic anion transporter- 3 «), ki bi bil lahko vključen v izločanje sitagliptina skozi ledvice.
The clinical relevance of hOAT-3 in sitagliptin transport has not been established.
Klinični pomen hOAT- 3 pri transportu sitagliptina ni bil ugotovljen.
However, cyclosporine, a p-glycoprotein inhibitor, did not reduce the renal clearance of sitagliptin.
Sitagliptin je tudi substrat za p- glikoprotein, ki je prav tako lahko vključen pri izločanju sitagliptina prek ledvic, vendar pa ciklosporin, zaviralec p- glikoproteina, ni zmanjšal ledvičnega očistka sitagliptina.
Sitagliptin is not a substrate for OCT2 or OAT1 or PEPT1/ 2 transporters.
Sitagliptin ni substrat za prenašalce OCT2 ali OAT1 ali PEPT1/ 2.
In vitro, sitagliptin did not inhibit OAT3 (IC50=160 μ M) or p-glycoprotein (up to 250 μ M) mediated transport at therapeutically relevant plasma concentrations.
Sitagliptin in vitro pri terapevtsko pomembnih plazemskih koncentracijah ni zaviral prenosa z OAT3 (IC50=160 μM) ali p- glikoproteina (do 250 μM).
In a clinical study sitagliptin had a small effect on plasma digoxin concentrations indicating that sitagliptin may be a mild inhibitor of p-glycoprotein.
V klinični študiji je sitagliptin imel majhen učinek na koncentracijo digoksina v plazmi, kar kaže, da je sitagliptin lahko blagi zaviralec p - glikoproteina.
Characteristics in patients The pharmacokinetics of sitagliptin were generally similar in healthy subjects and in patients with type 2 diabetes.
Značilnosti pri bolnikih Pri zdravih osebah in bolnikih s sladkorno boleznijo tipa 2 je farmakokinetika sitagliptina na splošno podobna.
Renal insufficiency A single-dose, open-label study was conducted to evaluate the pharmacokinetics of a reduced dose of sitagliptin (50 mg) in patients with varying degrees of chronic renal insufficiency compared to normal healthy control subjects.
Ledvična insuficienca Opravljena je bila odprta študija z enim samim odmerkom, v kateri so ovrednotili farmakokinetiko zmanjšanega odmerka sitagliptina (50 mg) pri bolnikih z različnimi stopnjami kronične ledvične insuficience v primerjavi z zdravimi kontrolnimi osebami.
The study included patients with renal insufficiency classified on the basis of creatinine clearance as mild (50 to < 80 ml/ min), moderate (30 to < 50 ml/ min), and severe (< 30 ml/ min), as well as patients with end-stage renal disease (ESRD) on haemodialysis.
V študiji so sodelovali bolniki z ledvično insuficienco, ki je bila na podlagi kreatininskega očistka ocenjena kot blaga (50 do < 80 ml/ min), zmerna (30 do < 50 ml/ min) ali huda (< 30 ml/ min), in bolniki s končno ledvično odpovedjo, ki so se zdravili s hemodializo.
Patients with mild renal insufficiency did not have a clinically meaningful increase in the plasma concentration of sitagliptin as compared to normal healthy control subjects.
V primerjavi z zdravimi kontrolnimi osebami pri bolnikih z blago ledvično insuficienco plazemske koncentracije sitagliptina niso bile klinično pomembno povečane.
An approximately 2-fold increase in the plasma AUC of sitagliptin was observed in patients with moderate renal insufficiency, and an approximately 4-fold increase was observed in patients with severe renal insufficiency and in patients with ESRD on haemodialysis, as compared to normal healthy control subjects.
Pri bolnikih z zmerno ledvično insuficienco so bile opažene približno 2- krat večje vrednosti plazemske AUC sitagliptina kot pri zdravih kontrolnih osebah, pri bolnikih s hudo ledvično insuficienco in pri bolnikih s končno ledvično odpovedjo, ki so se zdravili s hemodializo, pa so bile opažene približno 4- krat večje vrednosti plazemske AUC sitagliptina kot pri zdravih kontrolnih osebah.
Sitagliptin was modestly removed by haemodialysis (13.5% over a 3- to 4-hour haemodialysis session starting 4 hours post-dose).
Sitagliptin se zmerno odstrani s hemodializo (13, 5% pri 3 - do 4- urni hemodializi, ki se začne 4 ure po odmerku).
Sitagliptin is not recommended for use in patients with moderate or severe renal insufficiency including those with ESRD since experience in these patients is too limited (see section 4.2).
Ker je izkušenj pri bolnikih z zmerno ali s hudo ledvično insuficienco, vključno z bolniki s končno ledvično odpovedjo, premalo, uporabe zdravila sitagliptina pri teh bolnikih ne priporočamo (glejte poglavje 4. 2).
Hepatic insufficiency No dose adjustment for sitagliptin is necessary for patients with mild or moderate hepatic insufficiency (Child-Pugh score ≤ 9).
Jetrna insuficienca Pri bolnikih z blago ali zmerno jetrno insuficienco (Child- Pughova lestvica ≤ 9) odmerka ni treba prilagajati.