natgillin/translations-raw huggingface dataset:
General Galvus is not a substitute for insulin in insulin-requiring patients.
Splošno Zdravilo Galvus ne more nadomestiti zdravljenja z insulinom pri bolnikih, ki potrebujejo insulin.
Renal impairment There is limited experience in patients with moderate to severe renal impairment or in patients with ESRD on haemodialysis.
Okvara ledvic Pri bolnikih z zmerno do hudo okvaro ledvic oziroma pri bolnikih s končno ledvično odpovedjo na hemodializi so izkušnje omejene.
Therefore, the use of Galvus is not recommended in these patients.
Zato uporaba zdravila Galvus pri teh bolnikih ni priporočena.
Hepatic impairment Galvus should not be used in patients with hepatic impairment, including patients with pre-treatment ALT or AST > 3x ULN.
Okvara jeter Zdravilo Galvus se ne sme uporabljati pri bolnikih z okvaro jeter, vključno z bolniki, ki imajo pred zdravljenjem vrednosti ALT ali AST nad 3- kratno zgornjo mejo normalnih vrednosti.
Liver enzyme monitoring Rare cases of hepatic dysfunction (including hepatitis) have been reported.
Spremljanje jetrnih encimov Poročali so o redkih primerih motenega delovanja jeter (vključno s hepatitisom).
Liver function tests should be performed prior to the initiation of treatment with Galvus in order to know the patient’ s baseline value.
Pred začetkom zdravljenja z zdravilom Galvus je treba opraviti pregled jetrnih testov za določitev bolnikovih izhodiščnih vrednosti.
Patients who develop increased transaminase levels should be monitored with a second liver function evaluation to confirm the finding and be followed thereafter with frequent liver function tests until the abnormality(ies) return(s) to normal.
Bolnikom, pri katerih pride do zvišanja vrednosti aminotransferaz, je treba za potrditev opraviti še drugo preiskavo delovanja jeter, nato pa jih je treba spremljati s pogostimi pregledi jetrnih testov, dokler se nenormalni izvid( i) ne normalizira( jo).
Should an increase in AST or ALT of 3x ULN or greater persist, withdrawal of Galvus therapy is recommended.
Če zvišanje AST ali ALT na ali nad 3- kratno zgornjo mejo normalnih vrednosti vztraja, je priporočena prekinitev zdravljenja z zdravilom Galvus.
3 Cardiac failure Experience with vildagliptin therapy in patients with congestive heart failure of New York Heart Association (NYHA) functional class I-II is limited and therefore vildagliptin should be used cautiously in these patients.
3 Srčno popuščanje Pri bolnikih s kongestivnim srčnim popuščanjem funkcijskih razredov I- II po klasifikaciji Združenja za srce iz New Yorka (New York Heart Association - NYHA) so izkušnje z uporabo vildagliptina omejene, zato je potrebna previdnost pri uporabi vildagliptina pri teh bolnikih.
Skin disorders Skin lesions, including blistering and ulceration have been reported in extremities of monkeys in non- clinical toxicology studies (see section 5.3).
Kožne spremembe V nekliničnih toksikoloških študijah so poročali o kožnih spremembah, med drugim o mehurčastem izpuščaju in razjedah na okončinah opic (glejte poglavje 5. 3).
Excipients The tablets contain lactose.
Pomožne snovi Tablete vsebujejo laktozo.
Combination with pioglitazone, metformin and glyburide Results from studies conducted with these oral antidiabetics have shown no clinically relevant pharmacokinetic interactions.
Kombinacija s pioglitazonom, metforminom in gliburidom Rezultati študij s temi peroralnimi antidiabetiki niso pokazali nobenih klinično pomembnih farmakokinetičnih interakcij.
Digoxin (Pgp substrate), warfarin (CYP2C9 substrate) Clinical studies performed with healthy subjects have shown no clinically relevant pharmacokinetic interactions.
Digoksin (substrat P- glikoproteina), varfarin (substrat CYP2C9) Klinične študije na zdravih prostovoljcih niso pokazale nobenih klinično pomembnih farmakokinetičnih interakcij.
Combination with amlodipine, ramipril, valsartan or simvastatin Drug-drug interaction studies in healthy subjects were conducted with amlodipine, ramipril, valsartan and simvastatin.
Kombinacija z amlodipinom, ramiprilom, valsartanom ali simvastatinom Na zdravih prostovoljcih so izvajali klinične študije medsebojnega delovanja z amlodipinom, ramiprilom, valsartanom in simvastatinom.
It is not known whether vildagliptin is excreted in human breast milk.
Ni znano, ali se vildagliptin izloča v materino mleko pri človeku.
Galvus should not be used during lactation.
Zdravila Galvus se v obdobju dojenja ne sme uporabljati.
Patients who experience dizziness as an undesirable effect should avoid driving vehicles or using machines.
Bolniki, pri katerih prihaja do neželenega učinka v obliki omotičnosti, naj se izogibajo vožnji ali upravljanju s stroji.
Safety data were obtained from a total of 3,784 patients exposed to vildagliptin at a daily dose of 50 mg (once daily) or 100 mg (50 mg twice daily or 100 mg once daily) in controlled trials of at least 12 weeks duration.
Podatki o varnosti so pridobljeni iz kontroliranih preskušanj, ki so trajala vsaj 12 tednov, zajemala pa so skupno 3. 784 bolnikov, ki so prejemali vildagliptin v dnevnem odmerku 50 mg (enkrat dnevno) ali 100 mg (50 mg dvakrat dnevno ali 100 mg enkrat dnevno).
Of these patients, 2,264 patients received vildagliptin as monotherapy and 1,520 patients received vildagliptin in combination with another medicinal product.
Od teh bolnikov jih je 2. 264 prejemalo vildagliptin kot monoterapijo, 1. 520 bolnikov pa je prejemalo vildagliptin v kombinaciji z drugim zdravilom.
2,682 patients were treated with vildagliptin 100 mg daily (either 50 mg twice daily or 100 mg once daily) and 1,102 patients were treated with vildagliptin 50 mg once daily.
2. 682 bolnikov je prejemalo vildagliptin v odmerku 100 mg dnevno (bodisi 50 mg dvakrat dnevno ali 100 mg enkrat dnevno), 1. 102 bolnika pa sta prejemala vildagliptin v odmerku 50 mg dnevno.
Frequencies are defined as very common (≥ 1/ 10), common (≥ 1/ 100, < 1/ 10), uncommon (≥ 1/ 1,000, < 1/ 100), rare (≥ 1/ 10,000 to < 1/ 1,000), very rare (< 1/ 10,000), not known (cannot be estimated from the available data).
Pogostnosti so definirane kot: zelo pogosti (≥1/ 10), pogosti (≥1/ 100 do < 1/ 10), občasni (≥1/ 1. 000 do < 1/ 100), redki (≥1/ 10. 000 do < 1/ 1. 000), zelo redki (< 1/ 10. 000), neznana pogostnost (ni mogoče oceniti iz razpoložljivih podatkov).
Combination with metformin In controlled clinical trials with the combination of vildagliptin 100 mg daily + metformin, no withdrawal due to adverse reactions was reported in either the vildagliptin 100 mg daily + metformin or the placebo + metformin treatment groups.
Kombinacija z metforminom V kontroliranih kliničnih preskušanjih s kombinacijo 100 mg vildagliptina dnevno in metformina niso poročali o nobenem izstopu iz preskušanja zaradi neželenih učinkov niti v skupini, ki je skupaj z metforminom prejemala 100 mg vildagliptina dnevno, niti v skupini, ki je skupaj z metforminom prejemala placebo.
In clinical trials, the incidence of hypoglycaemia was common in patients receiving vildagliptin 100 mg daily in combination with metformin (1%) and uncommon in patients receiving placebo + metformin (0.4%).
V kliničnih preskušanjih je do hipoglikemije prišlo pogosto: pri 1% bolnikov, ki so prejemali 100 mg vildagliptina dnevno v kombinaciji z metforminom, in občasno: pri 0, 4% bolnikov, ki so prejemali placebo in metformin.
In clinical trials, weight did not change from baseline when vildagliptin 100 mg daily was added to metformin (+0.2 kg and -1.0 kg for vildagliptin and placebo, respectively).
Telesna masa se v kliničnih preskušanjih ni bistveno spremenila od izhodiščne: pri dodajanju 100 mg vildagliptina metforminu se je zvečala za 0, 2 kg, pri kombinaciji metformina s placebom pa se je zmanjšala za 1, 0 kg.
5 Table 1
5 Preglednica 1
Adverse reactions reported in patients who received Galvus 100 mg daily in combination with metformin in double-blind studies (N=208)
Neželeni učinki, o katerih so poročali pri bolnikih, ki so prejemali zdravilo Galvus v odmerku 100 mg dnevno v kombinaciji z metforminom v dvojno slepih študijah (N=208)
Combination with a sulphonylurea In controlled clinical trials with the combination of vildagliptin 50 mg + a sulphonylurea, the overall incidence of withdrawals due to adverse reactions was 0.6% in the vildagliptin 50 mg + sulphonylurea vs 0% in the placebo + sulphonylurea treatment group.
Kombinacija s sulfonilureo V kontroliranih kliničnih preskušanjih s kombinacijo 50 mg vildagliptina in sulfoniluree je bila skupna incidenca izstopov iz preskušanja zaradi neželenih učinkov 0, 6% v skupini, ki je prejemala 50 mg vildagliptina s sulfonilureo, v primerjavi z 0% v skupini, ki je skupaj s sulfonilureo prejemala placebo.
In clinical trials, the incidence of hypoglycaemia when vildagliptin 50 mg once daily was added to glimepiride was 1.2% versus 0.6% for placebo + glimepiride.
V kliničnih preskušanjih je bila incidenca hipoglikemije 1, 2%, če so 50 mg vildagliptina enkrat dnevno dodali zdravljenju z glimepiridom, v primerjavi z 0, 6% pri zdravljenju z glimepiridom in placebom.
In clinical trials, weight did not change from baseline when vildagliptin 50 mg daily was added to glimepiride (-0.1 kg and -0.4 kg for vildagliptin and placebo, respectively).
Telesna masa se v kliničnih preskušanjih ni bistveno spremenila od izhodiščne: pri dodajanju 50 mg vildagliptina glimepiridu se je zmanjšala za 0, 1 kg, pri kombinaciji glimepirida s placebom pa se je zmanjšala za 0, 4 kg.
Adverse reactions reported in patients who received Galvus 50 mg in combination with a sulphonylurea in double-blind studies (N=170)
Neželeni učinki, o katerih so poročali pri bolnikih, ki so prejemali zdravilo Galvus v odmerku 50 mg dnevno v kombinaciji s sulfonilureo v dvojno slepih študijah (N=170)
Combination with a thiazolidinedione In controlled clinical trials with the combination of vildagliptin 100 mg daily+ a thiazolidinedione, no withdrawal due to adverse reactions was reported in either the vildagliptin 100 mg daily + thiazolidinedione or the placebo + thiazolidinedione treatment groups.
Kombinacija s tiazolidindionom V kontroliranih kliničnih preskušanjih s kombinacijo 100 mg vildagliptina dnevno in tiazolidindiona niso poročali o nobenem izstopu iz preskušanja zaradi neželenih učinkov niti v skupini, ki je skupaj s tiazolidindionom prejemala 100 mg vildagliptina dnevno, niti v skupini, ki je skupaj s tiazolidindionom prejemala placebo.
In clinical trials, the incidence of hypoglycaemia was uncommon in patients receiving vildagliptin + pioglitazone (0.6%) but common in patients receiving placebo + pioglitazone (1.9%).
V kliničnih preskušanjih je do hipoglikemije prišlo občasno (0, 6%) pri bolnikih, ki so prejemali vildagliptin in pioglitazon, pogosto (1, 9%) pa pri bolnikih, ki so prejemali placebo in pioglitazon.
In the pioglitazone add-on study, the absolute weight increases with placebo, Galvus 100 mg daily were 1.4 and 2.7 kg, respectively.
6 V študiji s pioglitazonom in dodanim zdravilom je prišlo do povečanja telesne mase in sicer pri placebu za 1, 4 kg, pri zdravilu Galvus v odmerku 100 mg dnevno pa za 2, 7 kg.
The incidence of peripheral oedema when vildagliptin 100 mg daily was added to a maximum dose of background pioglitazone (45 mg once daily) was 7.0%, compared to 2.5% for background pioglitazone alone.
Incidenca perifernih edemov pri dodatku 100 mg vildagliptina dnevno k osnovnemu zdravljenju z največjim odmerkom pioglitazona (45 mg enkrat dnevno) je bila 7, 0% v primerjavi z 2, 5% pri zdravljenju samo s pioglitazonom.
6 Table 3
Preglednica 3
Adverse reactions reported in patients who received Galvus 100 mg daily in combination with a thiazolidinedione in double-blind studies (N=158)
Neželeni učinki, o katerih so poročali pri bolnikih, ki so prejemali zdravilo Galvus v odmerku 100 mg dnevno v kombinaciji s tiazolidindionom v dvojno slepih študijah (N=158)
Headache Asthenia
glavobol astenija
Metabolism and nutrition disorders
Presnovne in prehranske motnje Žilne
Common Uncommon
pogosti občasni bolezni pogosti
Weight increase Hypoglycaemia
zvečanje telesne mase hipoglikemija periferni edemi
In addition, in controlled monotherapy trials with vildagliptin the overall incidence of withdrawals due to adverse reactions was no greater for patients treated with vildagliptin at doses of 100 mg daily (0.3%) than for placebo (0.6%) or comparators (0.5%).
Poleg navedenega skupna incidenca izstopov iz preskušanja zaradi neželenih učinkov, v kontroliranih preskušanjih z vildagliptinom v monoterapiji, pri bolnikih, ki so prejemali 100 mg vildagliptina dnevno, ni bila večja (0, 3%) kot pri bolnikih, ki so prejemali placebo (0, 6%) ali primerjalna zdravila (0, 5%).
In clinical trials, weight did not change from baseline when vildagliptin 100 mg daily was administered as monotherapy (-0.3 kg and -1.3 kg for vildagliptin and placebo, respectively).
Telesna masa se v kliničnih preskušanjih ni bistveno spremenila od izhodiščne: pri jemanju 100 mg vildagliptina v monoterapiji se je zmanjšala za 0, 3 kg, pri placebu pa se je zmanjšala za 1, 3 kg.
Adverse reactions reported in patients who received Galvus 100 mg daily as monotherapy in double-blind studies (N=1,855)
Neželeni učinki, o katerih so poročali pri bolnikih, ki so prejemali zdravilo Galvus v odmerku 100 mg dnevno kot monoterapijo v dvojno slepih študijah (N=1. 855)
Vascular disorders
4. 9 Preveliko odmerjanje
Information on the likely symptoms of overdose was taken from a rising dose tolerability study in healthy subjects given Galvus for 10 days.
7 Podatki o verjetnih simptomih prevelikega odmerjanja temeljijo na študiji prenašanja naraščajočih odmerkov, izvedeni na zdravih osebah, ki so prejemale zdravilo Galvus 10 dni.
At 600 mg, one subject experienced oedema of the feet and hands, and increases in creatine phosphokinase (CPK), aspartate aminotransferase (AST), C-reactive protein (CRP) and myoglobin levels.
Pri 600 mg je pri eni osebi prišlo do otekanja rok in stopal ter zvišanja koncentracij kreatin- kinaze (CK), aspartat - aminotransferaze (AST), C- reaktivnega proteina (CRP) in mioglobina.
7 Management In the event of an overdose, supportive management is recommended.
Obravnava V primeru zaužitja prevelikega odmerka je priporočeno podporno zdravljenje.
However, the major hydrolysis metabolite (LAY 151) can be removed by haemodialysis.
Vildagliptina se ne da odstaniti s hemodializo, vendar je s hemodializo mogoče odstraniti glavni hidrolizni metabolit (LAY 151).
Dipeptidyl peptidase 4 (DPP-4) inhibitors, ATC code:
Farmakoterapevtska skupina: zaviralci dipeptidil peptidaze 4 (DPP- 4), oznaka ATC:
Vildagliptin, a member of the islet enhancer class, is a potent and selective DPP-4 inhibitor.
Vildagliptin iz skupine spodbujevalcev Langerhansovih otočkov je močan in selektiven zaviralec DPP- 4.
The administration of vildagliptin results in a rapid and complete inhibition of DPP-4 activity, resulting in increased fasting and postprandial endogenous levels of the incretin hormones GLP-1 (glucagon-like peptide 1) and GIP (glucose-dependent insulinotropic polypeptide).
Uporaba vildagliptina povzroči hitro in popolno zaviranje delovanja DPP- 4, kar povzroča zvišanje endogenih koncentracij hormonov inkretinov GLP- 1 (glukagonu podoben peptid 1; glucagon- like peptide 1) in GIP (od glukoze odvisni insulinotropni polipeptid; glucose- dependent insulinotropic polypeptide) na tešče in po obroku.
Treatment with vildagliptin 50-100 mg daily in patients with type 2 diabetes significantly improved 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.
Zdravljenje z vildagliptinom v odmerkih 50- 100 mg dnevno je pri bolnikih s sladkorno boleznijo tipa 2 pomembno izboljšalo vrednosti kazalcev delovanja beta celic, vključno z modelom ocene homeostaze HOMA- β (Homeostasis Model Assessment- β), razmerjem med proinsulinom in insulinom ter merjenjem odzivnosti beta celic po obroku s pogostim vzorčenjem.
The enhanced increase in the insulin/ glucagon ratio during hyperglycaemia due to increased incretin hormone levels results in a decrease in fasting and postprandial hepatic glucose production, leading to reduced glycaemia.
Pri hiperglikemiji zaradi zvišanih koncentracij hormonov inkretinov pride do dodatnega zvišanja razmerja insulin/ glukagon, kar povzroči zmanjšanje tvorbe glukoze v jetrih na tešče in po obroku, to pa zniža koncentracije glukoze v krvi.
A total of 5,759 patients with type 2 diabetes participated in 13 double-blind placebo- or active- controlled clinical trials of at least 12-weeks’ treatment duration.
V 13 dvojno slepih kontroliranih kliničnih preskušanjih s placebom ali s primerjalnim zdravilom, ki so trajala vsaj po 12 tednov, je bilo vključenih skupno 5. 759 bolnikov.
In these studies, vildagliptin was administered to 3,784 patients at daily doses of 50 mg once daily (N=1,102), 50 mg twice daily (N=2,027) or 100 mg once daily (N=655).
V teh študijah je vildagliptin prejemalo 3. 784 bolnikov in sicer v dnevnem odmerku 50 mg enkrat dnevno (N=1. 102), 50 mg dvakrat dnevno (N=2. 027) ali 100 mg enkrat dnevno (N=655).
The number of male and female patients receiving vildagliptin 50 mg once daily or 100 mg daily was 2,069 and 1,715, respectively.
Odmerke 50 mg vildagliptina enkrat dnevno ali 100 mg dnevno je prejemalo 2. 069 moških in 1. 715 žensk.
The number of patients receiving vildagliptin 50 mg once daily or 100 mg daily who were ≥ 65 years of age was 664 and 121 of the patients were ≥ 75 years of age.
Odmerke 50 mg vildagliptina enkrat dnevno ali 100 mg dnevno je prejemalo 664 bolnikov, starih 65 let ali več, 121 od teh jih je bilo starih 75 let ali več.
In these trials, vildagliptin was administered as monotherapy in drug-naïve patients with type 2 diabetes or in combination in patients not adequately controlled by other antidiabetic medicinal products.
V teh preskušanjih so vildagliptin v monoterapiji prejemali bolniki s sladkorno boleznijo tipa 2, ki prej še niso prejemali nobenih zdravil za sladkorno bolezen, v kombinaciji z
Overall, vildagliptin improved glycaemic control when given as monotherapy or when used in combination with metformin, a sulphonylurea, and a thiazolidinedione, as measured by clinically relevant reductions in HbA1c from baseline at study endpoint (see Table 5).
V celoti je vildagliptin bodisi v monoterapiji bodisi v kombinaciji z metforminom, s sulfonilureo ali s tiazolidindionom izboljšal urejenost glukoze v krvi, kar se je pokazalo kot klinično pomembno znižanje vrednosti HbA1c od izhodišča do časa opazovanja v študiji (glejte preglednico 5).
In a 52-week double-blind controlled trial, vildagliptin (50 mg twice daily) reduced baseline HbA1c by -1% compared to -1.6% for metformin (titrated to 2 g/ day) statistical non-inferiority was not achieved.
V 52- tedenskem dvojno slepem kontroliranem preskušanju je vildagliptin (50 mg dvakrat dnevno) znižal vrednost izhodiščnega HbA1c za 1% v primerjavi z znižanjem za 1, 6% pri metforminu (titriranem do 2 g/ dan), pri tem pa statistično ni bilo mogoče potrditi, da vildagliptin ni manj učinkovit od metformina (ne- inferiornost).
8 Patients treated with vildagliptin reported significantly lower incidences of gastrointestinal adverse reactions versus those treated with metformin.
Pri bolnikih, ki so prejemali vildagliptin, so poročali o pomembno nižji incidenci gastrointestinalnih neželenih učinkov v primerjavi s tistimi, ki so prejemali metformin.
In a 24-week double-blind controlled trial, vildagliptin (50 mg twice daily) was compared to rosiglitazone (8 mg once daily).
V 24- tedenskem dvojno slepem kontroliranem preskušanju so primerjali vildagliptin (50 mg dvakrat dnevno) z rosiglitazonom (8 mg enkrat dnevno).
Mean reductions were -1.20% with vildagliptin and -1.48% with rosiglitazone in patients with mean baseline HbA1c of 8.7%.
Pri bolnikih s povprečno izhodiščno vrednostjo HbA1c 8, 7% je pri vildagliptinu prišlo do povprečnega znižanja za 1, 20%, pri rosiglitazonu pa za 1, 48%.
Patients receiving rosiglitazone experienced a mean increase in weight (+1.6 kg) while those receiving vildagliptin experienced no weight gain (-0.3 kg).
Pri bolnikih, ki so prejemali rosiglitazon, je v povprečju prišlo do povečanja telesne mase za 1, 6 kg v nasprotju s tistimi, ki so prejemali vildagliptin, pri katerih ni prišlo do povečanja telesne mase (- 0, 3 kg).
4.1% respectively).
Incidenca perifernih edemov je bila nižja v skupini z vildagliptinom v primerjavi s skupino z rosiglitazonom (2, 1% v primerjavi s 4, 1%).
Key efficacy results of vildagliptin in placebo-controlled monotherapy trials and in add-on combination therapy trials (primary efficacy ITT population)
Kjučni rezultati učinkovitosti vildagliptina v preskušanjih, kontroliranih s placebom, in sicer z monoterapijo oziroma s kombinacijo z dodanim zdravilom (primarna ITT populacija za oceno učinkovitosti)
Monotherapy placebo
Povprečna Povprečna
Mean
Povprečna
Mean change
izhodiščna
Placebo-
sprememba
controlled studies
sprememba
baseline
vrednost
from baseline in
vrednosti HbA1c
corrected mean
vrednosti HbA1c
HbA1c (%) at week 24
po 24 tednih,
change in HbA1c (%) at week 24 (95%CI)
24 tednih (%)
Study 2301:
korigirana glede na vrednosti pri
Vildagliptin 50 mg twice daily (N=90)
placebu (% (95% IZ)) študija 2301: vildagliptin 50 mg dvakrat dnevno (N=90)
Vildagliptin 50 mg twice daily (N=79)
študija 2384: vildagliptin 50 mg dvakrat dnevno (N=79)
* p < 0.05 for comparison versus placebo Add-on / Combination studies Vildagliptin 50 mg twice daily + metformin (N=143)
* p < 0, 05 za primerjavo s placebom Študije z dodanim zdravilom / s kombinacijami zdravil vildagliptin 50 mg dvakrat dnevno + metformin (N=143)
* p < 0.05 for comparison versus placebo + comparator
* p < 0, 05 za primerjavo s placebom + primerjalnim zdravilom
Absorption Following oral administration in the fasting state, vildagliptin is rapidly absorbed, with peak plasma concentrations observed at 1.7 hours.
Absorpcija Po peroralni aplikaciji na tešče se vildagliptin hitro absorbira in doseže najvišje koncentracije v plazmi po 1, 7 ure.
However, the magnitude of change is not clinically significant, so that Galvus can be given with or without food.
Zaradi uživanja vildagliptina skupaj s hrano se je znižala Cmax (19%), vendar velikost te spremembe ni klinično pomembna, zato se lahko zdravilo Galvus uživa s hrano ali brez nje.
Biotransformation Metabolism is the major elimination pathway for vildagliptin in humans, accounting for 69% of the dose.
Biotransformacija Glavna pot izločanja vildagliptina pri človeku je njegova presnova, ki odstrani 69% odmerka.
The major metabolite (LAY 151) is pharmacologically inactive and is the hydrolysis product of the cyano moiety, accounting for 57% of the dose, followed by the amide hydrolysis product (4% of dose).
Glavni metabolit (LAY 151) nima farmakološkega učinka in nastane s hidrolizo ciano skupine ter predstavlja 57% odmerka, sledi pa mu produkt hidrolize amida (4% odmerka).
Accordingly, the metabolic clearance of vildagliptin is not anticipated to be affected by co-medications that are CYP 9 450 inhibitors and/ or inducers.
Glede na to ni pričakovati, da bi na presnovni očistek vildagliptina vplivala sočasna uporaba zdravil, ki so zaviralci in/ ali induktorji encimov CYP 450.
In vitro studies demonstrated that vildagliptin does not inhibit/ induce CYP 450 enzymes.
In vitro študije so pokazale, da vildagliptin ne zavira/ inducira encimov CYP 450.
Therefore, vildagliptin is not likely to affect metabolic clearance of co-medications metabolised by CYP 1A2, CYP 2C8, CYP 2C9, CYP 2C19, CYP 2D6, CYP 2E1 or CYP 3A4/ 5.
Zato ni verjetno, da bi vildagliptin vplival na presnovni očistek sočasno uporabljanih zdravil, ki se presnavljajo z encimi CYP 1A2, CYP 2C8, CYP 2C9, CYP 2C19, CYP 2D6, CYP 2E1 ali CYP 3A4/ 5.
Elimination Following oral administration of [14C] vildagliptin, approximately 85% of the dose was excreted into the urine and 15% of the dose is recovered in the faeces.
Izločanje Po peroralni aplikaciji s 14C označenega vildagliptina se je približno 85% odmerka izločilo z urinom, 15% odmerka pa so našli v blatu.