Cov tshuaj Xelevia: cov lus qhia rau kev siv > Kev khomob thiab kev tiv thaiv

Muaj nyob rau hauv cov yeeb yaj kiab-coated ntsiav tshuaj. Cov ntsiav tshuaj pleev xim, nyob rau saum npoo ntawm cov zaj duab xis ntawm ib sab yog sau rau “277”, ntawm sab nraud lawv yog kom du.

Lub ntsiab nquag ua haujlwm yog sitagliptin phosphate monohydrate hauv kev siv tshuaj ntawm 128,5 mg. Cov tshuaj ntxiv: microcrystalline cellulose, calcium hydrogen phosphate, croscarmellose sodium, magnesium stearate, magnesium stearyl fumarate. Cov txheej txheej ua yeeb yaj kiab muaj cov dej cawv polyvinyl, titanium dioxide, polyethylene glycol, talc, daj thiab liab hlau oxide.

Cov tshuaj muaj nyob hauv hlwv rau 14 ntsiav tshuaj. Hauv ib pob ntawv ntawm cardboard muaj 2 cov hlwv thiab cov lus qhia rau kev siv.

Qhov twg thiab yuav ua li cas txhaj tshuaj insulin hauv ntshav qab zib mellitus - nyeem hauv kab lus no.

Pharmacological kev txiav txim

Npaj rau kev kho mob ntshav qab zib hauv hom ob. Lub tshuab kev ua haujlwm yog ua raws li kev txwv tsis pub tawm ntawm enzyme DPP-4. Cov tshuaj nquag muaj qhov sib txawv hauv kev txiav txim los ntawm insulin thiab lwm yam kev tiv thaiv antiglycemic. Cov concentration ntawm cov piam thaj hauv insulinotropic cov tshuaj hormones ntau dua.

Muaj kev tsuj ntawm kev zais cia ntawm glucagon los ntawm pancreatic cells. Qhov no pab txo cov synthesis ntawm cov piam thaj hauv daim siab, ua rau cov tsos mob ntawm cov ntshav qog ntshav qis. Qhov kev nqis tes ntawm sitagliptin yog tsom rau thaiv cov hydrolysis ntawm pancreatic enzymes. Glucagon tso pa tawm yuav txo qis, yog li txhawb kev tso tawm ntawm cov kua dej. Hauv qhov no, glycosylated insulin index thiab qhov concentration ntawm cov piam thaj hauv cov ntshav yuav txo qis.

Xelevia yog tsim los kho hom 2 ntshav qab zib.

Cov Tshuaj Pharmacokinetics

Tom qab noj tshuaj hauv ncoo sab hauv, cov tshuaj nquag yuav nqus tawm sai sai ntawm lub plab zom mov. Noj mov cuam tshuam nrog kev nqus. Nws qhov siab tshaj plaws hauv cov ntshav tau txiav txim siab tom qab ob peb teev. Bioavailability yog siab, tab sis muaj peev xwm khi rau cov qauv protein muaj tsawg. Kev mob plab zom mov tshwm sim hauv lub siab. Cov tshuaj tawm hauv lub cev tawm hauv lub cev nrog rau cov zis los ntawm lub raum lim ob qho tib si tsis hloov thiab hauv hom kev sib xyaw ua ke.

Kev ntsuas rau siv

Muaj ntau tus lej ntawm qhov taw qhia ncaj qha rau kev siv tshuaj kho mob no:

monotherapy los txhim kho glycemic metabolism hauv cov neeg mob uas muaj ntshav qab zib hom 2,
pib txoj kev kho nrog tshuaj metformin yam 2 mob ntshav qab zib pathology,
kev kho mob ntshav qab zib hom 2, thaum kev noj haus thiab kev tawm dag zog tsis ua haujlwm,
tshuaj insulin
txhawm rau txhim kho glycemic tswj nrog sulfonylurea derivatives,
kev sib xyaw kho mob ntshav qab zib ntawm yam thib ob nrog thiazolidinediones.

Cov Yuav Tsum Muaj

Kev ntsuas ncaj qha rau kev siv tshuaj, uas tau qhia hauv cov lus qhia rau kev siv, yog:

muaj lub cev tsis haum rau lub tshuaj,
cev xeeb tub thiab lactation
hnub nyoog txog 18 xyoo
mob ketoacidosis,
ntshav qab zib hom 1
lub raum tsis ua haujlwm.

Xelevia yog siv rau hauv kev kho mob ntshav qab zib hom 2, thaum kev noj zaub mov noj thiab kev tawm dag zog tsis ua haujlwm.

Nrog kev saib xyuas zoo, Xelevia yog kho rau cov neeg muaj mob raum tsis zoo thiab mob raum, cov neeg mob uas muaj keeb kwm ua ntej.

Yuav ua li cas noj Xelevia?

Tsuas tshuaj thiab lub sijhawm rau kev kho mob ncaj qha nyob ntawm qhov mob hnyav ntawm tus mob.

Thaum ua kev kho mob monotherapy, cov tshuaj raug muab rau hauv thawj zaug pib 100 mg ib hnub twg. Kev haus dej tib yam yog pom thaum siv cov tshuaj ua ke nrog metformin, insulin thiab sulfonylureas. Thaum ua txoj kev kho cov nyom, nws raug nquahu kom txo cov koob tshuaj insulin kom tsis txhob muaj kev txhim kho ntawm hypoglycemia.

Tsis txhob noj ob zaug ntawm cov tshuaj hauv ib hnub. Nrog rau qhov kev hloov pauv rau hauv kev noj qab haus huv dav dav, yuav tsum tau txhaj koob tshuaj. Qee qhov xwm txheej, ib nrab lossis plaub hlis ntsiav tshuaj yog kws kho, uas feem ntau tsuas yog muaj cov nyhuv placebo. Cov koob tshuaj txhua hnub tuaj yeem hloov mus rau hauv tus account qhov tshwm sim ntawm cov teeb meem ntawm tus kab mob thiab kev ua haujlwm ntawm kev siv cov tshuaj no.

Sab Sij Huam Xelevia

Thaum noj Xelevia, cov kev mob tshwm sim tom qab no tuaj yeem tshwm sim:

kev fab tshuaj tsis haum
tsis qab los noj mov
cem quav
cramps
tachycardia
insomnia
paresthesia
kev xav tsis txaus ntseeg.

Muaj qee zaus, mob exorerbation ntawm hemorrhoids yog tau. Txoj kev kho yog mob. Hauv cov mob nyhav, nrog rau cov leeg noj nrog cev, mob ntshav khov kho.

Siv rau lub sijhawm qub

Feem ntau, cov neeg mob laus tsis tas yuav tsum tau kho ntau npaum li cas. Tab sis yog hais tias tus mob hnyav zuj zus lossis kev kho mob tsis muab qhov tshwm sim uas xav tau, ces nws zoo dua kom tsis txhob noj tshuaj lossis kho qhov ntau npaum li qhov txo qis.

Cov neeg mob laus tsis tas yuav tshuaj kho Xelevia.

Siv thaum cev xeeb tub thiab lactation

Tsis muaj ib qho tseeb ntawm cov txiaj ntsig ntawm kev muab tshuaj nquag ntawm tus me nyuam hauv plab. Yog li, kev siv cov tshuaj no thaum xeeb tub yog txwv tsis pub.

Txij li thaum tsis muaj cov ntaub ntawv txaus ntseeg ntawm seb cov tshuaj hloov mus rau leej niam mis, nws yog qhov zoo dua rau tso tseg rau kev pub niam mis yog tias tsim nyog kho.

Daim ntawv thov rau lub raum khiav tsis zoo

Cov tshuaj ntawm lub tshuaj yuav vam khom rau creatinine tshem tawm. Qhov ntau nws yog, qhov qis dua cov tshuaj tau hais tseg. Yog tias qhov ua haujlwm tsis zoo hauv lub raum, qhov pib txhaj yuav tuaj yeem hloov kho rau 50 mg rau ib hnub. Yog tias kev kho mob tsis muab qhov kev xav ua kom zoo, koj yuav tsum tshem tawm cov tshuaj.

Daim ntawv thov rau lub siab ua haujlwm tsis zoo

Nrog kev qog ua kom lub raum tsis ua haujlwm, kev hloov kho tshuaj tsis tas yuav tsum muaj. Qhov koob tshuaj txhua hnub hauv qhov no yuav tsum yog 100 mg. Tsuas yog nrog kev mob siab rau daim siab hnyav, kho nrog cov tshuaj no tsis ua tiav.

Nrog txoj kev mob siab hnyav rau daim siab, Xelevia tsis raug kho.

Noj tshuaj ntau ntawm Xelevia

Muaj qee yam tsis muaj kev kis ntau tshaj plaws. Ib lub xeev ntawm kev haus yeeb tshuaj loj heev tuaj yeem tshwm sim thaum noj ib koob tshuaj ntau tshaj 800 mg. Hauv qhov no, cov tsos mob ntawm cov kev mob tshwm sim yog exacerbated.

Kev kho mob suav nrog kev mob plab, ntxiv kev tshem tawm thiab kho kev kho. Nws yuav muaj peev xwm tshem tawm cov co toxins tawm ntawm lub cev siv ntev lim ntshav, vim tias tus qauv mob hemodialysis zoo rau kev muaj mob me ntawm kev noj ntau tshaj.

Kev cuam tshuam nrog lwm yam tshuaj

Cov tshuaj tuaj yeem ua ke nrog metformin, warfarin, qee qhov kev tswj kom tsis txhob mob. Cov chaw muag tshuaj ntawm cov tshuaj nquag tsis hloov nrog kev kho ua ke nrog ACE inhibitors, cov tshuaj tiv thaiv kab mob, tshuaj lipid-txo qis, beta-blockers thiab calcium channel blockers.

Qhov no kuj suav nrog cov tshuaj uas tsis yog tshuaj steroidal los tiv thaiv, tshuaj tua kab mob, tshuaj tiv thaiv antihistamines, proton twj tso kua mis inhibitors thiab qee cov tshuaj kom tshem tawm erectile kawg.

Thaum ua ke nrog Digoxin thiab Cyclosporine, qhov kev nce siab me ntsis ntawm cov khoom ua kom nquag plias hauv cov ntshav ntshav tau pom.

Cawv tau zoo

Koj tsis tuaj yeem siv cov tshuaj no nrog cawv. Cov nyhuv ntawm cov tshuaj yog txo, thiab cov tsos mob dyspeptic tsuas yog nce.

Cov tshuaj no muaj cov lej ntawm cov qauv tshuaj tiv thaiv zoo ib yam li nws ntawm cov tshuaj nquag thiab cov nyhuv uas nws muaj. Feem ntau ntawm lawv yog:

Sitagliptin,
Sitagliptin phosphate monohydrate,
Januvius
Yasitara.

Chaw tsim tshuaj paus

Lub tuam txhab tsim khoom: Berlin-Chemie, Lub teb chaws Yelemees.

Khaws Xelevia kom deb ntawm cov menyuam yaus.

Mikhail, 42 xyoo, Bryansk

Tus kws kho mob qhia kom noj Xelevia ua cov kev kho mob tseem ceeb. Tom qab ib hlis ntawm kev siv, yoo qab zib sai me ntsis nce, ua ntej nws yog nyob rau hauv 5, tam sim no nws nce mus txog 6-6.5. Kev hloov pauv ntawm lub cev mus rau kev ua haujlwm ntawm lub cev kuj tau hloov. Ua ntej lawm, tom qab taug kev lossis ua kis las ncaws pob, qab zib poob qis, thiab pom meej, qhov ntsuas yog kwv yees 3. Thaum noj Xelevia, qab zib tom qab kev qoj ib ce poob qis, maj mam, thiab tom qab ntawd nws rov qab zoo. Nws pib zoo siab dua. Yog li kuv xav cov tshuaj.

Alina, 38 xyoo, Smolensk

Kuv txais Xelevia ua qhov tsim nyog ntxiv rau insulin. Kuv tau mob ntshav qab zib tau ntau xyoo thiab tau sim ntau yam tshuaj noj thiab sib xyaw. Kuv nyiam tus no tshaj. Cov tshuaj tsuas yog ua rau cov suab thaj siab. Yog tias nws tau qis tam sim no, tom qab ntawd cov tshuaj yuav tsis "kov" nws thiab tsa nws siab. Ua ntu zus. Tsis muaj spikes hauv qab zib thaum nruab hnub. Muaj lwm qhov txiaj ntsig zoo, uas tsis tau piav qhia hauv cov lus qhia rau kev siv: hloov khoom noj. Qab los noj mov yog txo los ntawm yuav luag ib nrab. Qhov no yog qhov zoo.

Cim, 54 xyoo, Irkutsk

Cov tshuaj tuaj tam sim ntawd. Ua ntej ntawd, nws tau siv Januvia. Tom qab nws, nws tsis zoo. Tom qab ntau lub hlis ntawm kev noj Xelevia, tsis tsuas qab zib theem rov qab mus rau qhov qub, tab sis kuj noj qab haus huv tag nrho. Kuv xav tias nquag ntau dua, tsis tas yuav tsum tau khoom txom ncauj tas li. Kuv yuav luag tsis nco qab tias lub qog ntshav qab zib yog dab tsi. Cov piam thaj tsis dhia, nws nqus thiab nce thiab maj mam thiab maj mam, kom lub cev teb zoo.

Tso tawm daim ntawv thiab muaj pes tsawg leeg

Daim ntawv noj cov tshuaj Xelevia yog cov ntsiav tshuaj zaj duab xis: beige, biconvex, puag ncig, du rau ntawm ib sab, sau tus "277" (hauv cov duab los qhia 2 lub ntsej muag uas muaj 14 ntsiav tshuaj txhua) thiab cov lus qhia rau kev siv Xelevia.

Composition 1 ntsiav tshuaj:

cov tshuaj nquag: sitagliptin phosphate monohydrate - 128,5 mg (sib raug rau cov ntsiab lus ntawm sitagliptin - 100 mg),
Cov khoom siv pabcuam: sodium stearyl fumarate - 12 mg, magnesium stearate - 4 mg, croscarmellose sodium - 8 mg, tsis siv tshuaj calcium calcium phosphate - 123.8 mg, microcrystalline cellulose - 123.8 mg,
zaj duab xis txheej: Opadry II beige 85F17438 hlau oxide liab (E 172) - 0.37%, hlau oxide daj (E 172) - 3.07%, talc - 14.8%, polyethylene glycol (macrogol 3350) - 20.2% titanium dioxide (E 171) - 21.56%, cawv polyvinyl - 40% - 16 mg.

Cov Tshuaj Hauv Tshuaj

Xelevia yog qhov muaj kev xaiv tshwj xeeb rau lub enzyme DPP-4, uas yog nquag thaum noj ntawm qhov ncauj thiab tau npaj rau kev kho mob hom 2 ntshav qab zib mellitus.

Cov tshuaj muaj zog ntawm Xelevia (sitagliptin) los ntawm analogues ntawm glucagon-zoo li peptide-1 (GLP-1) thiab amylin, α-glucosidase inhibitors, γ-receptor agonists uas ua haujlwm los ntawm cov peroxisome proliferator (PPAR-γ), insulin, sulfonylurea derivatives thiab cov qauv loj ua rau muaj qhov sib txawv. thiab pharmacological kev txiav txim. Los ntawm inhibiting DPP-4, sitagliptin tsub kom qhov siab ntxiv ntawm ob cov tshuaj hormones ntawm tsev neeg incretin - GLP-1 thiab glucose-nyob insulinotropic polypeptide (HIP).

Cov tshuaj hormones ntawm tsev neeg no tau muab zais rau hauv txoj hnyuv li 24 teev, teb rau cov khoom noj, lawv cov kev xav ntau ntxiv. Tus incretins yog ib feem ntawm cov txheej txheem kho mob sab hauv lub zog rau kev tswj hwm cov ntshav qabzib homeostasis. Tawm tsam keeb kwm yav dhau los ntawm ib txwm los sis nce ntshav qabzib, cov tshuaj hormones ntawm tsev neeg muaj ntau ntxiv ua rau muaj cov insulin ntau zog thiab nws txoj kev zais cia los ntawm pancreatic cells-hlwb los ntawm kev taw qhia rau intracellular mechanisms cuam tshuam nrog cyclic adenosine monophosphate (AMP).

Kuj, GLP-1 suppresses nce tsis pub lwm tus ntawm glucagon los ntawm pancreatic α-hlwb. Kev poob qis hauv glucagon concentration nrog kev nce ntxiv ntawm cov tshuaj insulin ua rau cov piam thaj ntau zuj zus los ntawm lub siab, uas thaum kawg ua rau glycemia txo qis. Qhov kev ua haujlwm ntawm kev txiav txim no txawv ntawm qhov muaj feem rau sulfonylurea derivatives, uas, txawm tias muaj cov ntshav qabzib tsawg cov ntsiab lus, txhawb kev tso tawm ntawm insulin. Qhov no ua rau muaj qhov tshwm sim ntawm sulfone-kev tsim cov hypoglycemia tsis yog hauv cov neeg mob uas muaj yam mob ntshav qab zib 2 mob ntshav qab zib, tab sis kuj tseem muaj cov neeg noj qab nyob zoo.

Thaum lub siab tsis zoo ntawm cov piam thaj hauv cov ntshav, cov txiaj ntsig tau teev tseg ntawm incretins ntawm kev txo qis hauv glucagon tso pa tawm thiab insulin tso tawm tsis pom. HIP thiab GLP-1 tsis cuam tshuam rau glucagon tso tawm rau hauv kev teb rau hypoglycemia. Cov kev ua ntawm incretins nyob rau hauv physiological tej yam kev mob yog txwv los ntawm lub enzyme DPP-4, uas sai sai hydrolyzes lawv nrog kev tsim cov khoom tsis ua haujlwm. Sitagliptin tiv thaiv cov txheej txheem no, vim tias cov plasma ntau ntau ntawm cov ntawv nquag ntawm HIP thiab GLP-1 nce.

Los ntawm kev ua kom cov ntsiab lus nce ntxiv, Xelevia nce cov piam thaj hauv kev tso tawm ntawm cov kua dej thiab pab txo qis ntawm glucagon. Hauv cov neeg mob uas muaj ntshav qab zib hom 2 nrog hyperglycemia, cov kev hloov pauv hauv kev zais ntawm glucagon thiab insulin pub rau kom txo qis qhov glycated hemoglobin HbA _1C thiab qhov txo qis piam thaj hauv ntshav ntshav, txiav txim siab ntawm lub plab khoob thiab tom qab kev ntsuas kev ntxhov siab.

Kev noj ib zaug ntawm Xelevia hauv hom 2 mob ntshav qab zib mellitus ua rau kev txwv tsis pub muaj kev ua haujlwm ntawm DPP-4 enzyme rau 24 teev, uas ua haujlwm pab txo cov ntshav qabzib ntau, nrog rau tom qab qabzib lossis zaub mov thauj khoom, txo cov concentration ntawm glucagon hauv ntshav plasma, nce ntshav plasma concentration ntawm insulin thiab C- peptide, nce qhov siab ntawm kev xa mus zuj zus GLT-1 thiab ISU hauv 2 lossis 3 zaug.

Tsis hlauv

Txoj kev kawm qhib ntawm sitagliptin nyob rau hauv ib koob tshuaj txhua hnub ntawm 50 mg tau ua qhov kev kawm los tshawb cov pharmacokinetics rau qhov sib txawv ntawm qhov mob ntawm cov mob raum tsis ua haujlwm. Cov neeg ua haujlwm pab dawb nyob hauv qhov kev tshawb fawb tau muab faib ua cov pab hauv qab no:

cov neeg mob uas mob raum tsis zoo: kev tshem tawm (creatinine tshem tawm) (CC) 50-80 ml hauv 1 feeb,
cov neeg mob uas mob raum tsis ua haujlwm: CC 30–50 ml rau 1 feeb,
cov neeg mob uas lub raum tsis ua haujlwm: CC 9 cov ntsiab lus) tsis tuaj. Txawm li cas los xij, muab hais tias cov tshuaj feem ntau yog ua rau lub raum, ib qho yuav tsum tsis txhob xav tias yuav muaj kev hloov pauv tseem ceeb hauv nws cov khw muag tshuaj hauv cov xwm txheej zoo li no.

Laus lub caij nyoog

Lub hnub nyoog ntawm cov neeg mob tsis muaj kev cuam tshuam los ntawm kev kho mob rau tus cwj pwm pharmacokinetic ntawm cov tshuaj. Piv nrog rau cov neeg mob hluas, qhov concentration ntawm sitagliptin hauv cov neeg laus (hnub nyoog 65 txog 80 xyoo) yog siab dua kwv yees li 19%. Nyob ntawm seb muaj hnub nyoog li cas, kev kho tshuaj ntawm Xelevia tsis yog nqa tawm.

Xelevia, cov lus qhia rau kev siv: txoj kev thiab ntau npaum li cas

Cov ntsiav tshuaj tau noj ntawm qhov ncauj, tsis hais zaub mov dab tsi. Cov koob tshuaj pom zoo ntawm cov tshuaj yog 1 ntsiav tshuaj (100 mg) ib hnub ib zaug. Xelevia yog siv rau hauv kev saib xyuas mob, ib txhij nrog metformin / sulfonylurea derivatives / PPAR-agonists, lossis nrog metformin thiab sulfonylurea derivatives / metformin thiab PPAR-γ agonists / insulin (tsis muaj lossis nrog metformin).

Qhov ntau npaum ntawm kev noj tshuaj ntawm cov tshuaj siv ib txhij nrog Xelevia yog xaiv raws li kev pom zoo koob tshuaj rau cov tshuaj no.

Tawm tsam cov keeb kwm yav dhau los ntawm kev kho mob sib xyaw nrog Xelevia nrog cov insulin lossis sulfonylurea derivatives, nws raug nquahu kom txo qis cov tshuaj tua kab mob ib txwm muaj ntawm cov tshuaj insulin thiab sulfonylurea derivatives kom txo tau qhov muaj peev xwm ntawm insulin los yog sulfone-hob cov ntshav qab zib tsawg.

Thaum hla cov ntsiav tshuaj, nws raug nquahu kom coj lawv sai li sai tau tom qab tus neeg mob nco qab qhov tshuaj uas ploj lawm. Nws yuav tsum tau yug nyob rau hauv lub siab hais tias kev siv tshuaj ntawm ob zaug tshuaj ntawm tib hnub yog tsis tsim nyog.

Kev hloov kho ntawm koob tshuaj rau kev mob raum tsis zoo (CC ≥ 50 ml ib 1 min, kwv yees sib luag rau qhov kev tsim cov tshuaj lom neeg ≤ 1.5 mg rau 1 dL hauv cov poj niam thiab ≤ 1.7 mg rau 1 dL hauv txiv neej) tsis tas yuav.

Hauv cov neeg mob uas mob raum mus rau lub raum tsis ua haujlwm, yuav tsum tau kho cov tshuaj sitagliptin kom haum.Txij li thaum tsis muaj ib qho kev sib cais sib txawv ntawm cov ntsiav tshuaj ntawm Xelevia thiab lawv tsis tso tawm ntawm qhov ntau npaum li 25 lossis 50 mg (tab sis tsuas yog ntawm 100 mg), nws tseem tsis tuaj yeem ua kom muaj peev xwm ntau npaum li cas hauv cov tshuaj no. Hauv kev hais txog qhov no, cov tshuaj nyob rau hauv pawg no ntawm cov neeg mob tsis tau sau tseg.

Kev siv cov sitagliptin tiv thaiv cov keeb kwm yav dhau los ntawm lub raum tsis ua haujlwm yuav tsum muaj kev ntsuam xyuas ntawm lub raum kev ua haujlwm ua ntej pib kho thiab tsis tseg thaum siv.

Hauv cov mob me mus txog qib qeeb ntawm daim siab ua haujlwm, nrog rau cov neeg laus, cov koob tshuaj tsis raug hloov kho. Kev siv Xelevia tawm tsam keeb kwm yav dhau los ntawm kev mob siab ua haujlwm tsis tau soj ntsuam.

Thaum xub thawj ua ke kev kho nrog metformin

Lub sijhawm 24-lub hlis tshuaj placebo tau tshawb xyuas los ntawm kev pib ua ke kev kho ntawm sitagliptin nyob rau hauv ib koob tshuaj 100 mg thiab metformin nyob rau hauv ib koob tshuaj txhua hnub ntawm 1000 lossis 2000 mg (50 mg ntawm sitagliptin + 500 lossis 1000 mg ntawm metformin 2 zaug hauv ib hnub). Raws li cov ntaub ntawv tau, cov xwm txheej tsis zoo cuam tshuam nrog kev noj tshuaj tau pom ntau dua (nrog zaus ntawm ≥ 1%) hauv pawg tau txais sitagliptin + metformin dua li nrog metformin monotherapy. Qhov tshwm sim ntawm cov kev mob tshwm sim hauv cov pawg ntawm sitagliptin + metformin thiab metformin hauv monotherapy yog (feem):

raws plab - 3.5 thiab 3.3%,
ntuav - 1.1 thiab 0.3%,
mob taub hau - 1.3 thiab 1.1%,
dyspepsia - 1.3 thiab 1.1%,
hypoglycemia - 1.1 thiab 0.5%,
flatulence - 1.3 thiab 0.5%.

Kev siv yooj yim nrog sulfonylurea derivatives lossis sulfonylurea derivatives thiab metformin

Hauv 24-lub lis piam, kev kawm tshuaj placebo ntawm kev siv ua ke ntawm 100 mg ntawm sitagliptin ib hnub nrog glimepiride lossis glimepiride thiab metformin, ntau zaus (nrog rau zaus ntawm ≥ 1%) kev soj ntsuam hypoglycemia tau muab piv nrog cov pab pawg tau txais cov placebo nrog glimepiride los yog glimepiride thiab metformin. Qhov zaus ntawm nws txoj kev loj hlob yog 9.5 / 0.9%, feem.

Pib kev kho ua ke nrog PPAR-γ agonists

Thaum ua qhov kev tshawb nrhiav 24-lub lim tiam ntawm kev pib ua ke nrog kev kho mob nrog sitagliptin hauv ib koob tshuaj 100 mg thiab pioglitazone hauv ib koob tshuaj 30 mg txhua hnub hauv cov pawg tau txais sitagliptin hauv kev sib xyaw, cov kev mob tshwm sim tau pom ntau dua (nrog rau zaus ntawm ≥ 1%) dua li hauv cov pawg tau txais pioglitazone hauv kev kho mob monotherapy Cov. Qhov tshwm sim ntawm cov xwm txheej tsis zoo hauv cov pawg ntawm sitagliptin + pioglitazone thiab pioglitazone hauv kev kho mob monotherapy yog (feem):

Cov tsos mob hypoglycemia: 0.4 thiab 0.8%,
asymptomatic txo cov ntshav qabzib hauv siab: 1.1 thiab 0%.

Kev sib xyaw ua ke nrog metformin thiab PPAR-y agonists

Ib qho kev soj ntsuam tshuaj placebo tau siv 100 mg ntawm sitagliptin ib hnub ib txhij nrog rosiglitazone thiab metformin nrog kev koom ua ke ntawm ob pawg - cov neeg mob tau txais kev sib xyaw nrog kev kawm tshuaj, thiab cov neeg tau txais kev sib xyaw nrog cov placebo. Raws li cov ntaub ntawv tau txais, kev phiv tshuaj tiv thaiv tau pom ntau dua (nrog zaus ntawm ≥ 1%) hauv pawg tau txais sitagliptin ntau dua li cov pab pawg uas tau txais cov placebo.

Hauv 18 lub lim tiam ntawm kev soj ntsuam hauv cov pab pawg no, cov kev mob tshwm sim tau sau tseg nrog cov zaus hauv qab no:

ntuav - 1.2 thiab 0%,
mob taub hau - 2.4 thiab 0%,
hypoglycemia - 1.2 thiab 0%,
xeev siab - 1.2 thiab 1.1%,
raws plab - 1.8 thiab 1.1%.

Nyob rau 54th lub lim tiam ntawm kev soj ntsuam hauv cov pab pawg no, muaj ntau qhov tshwm sim ntawm cov kev mob tshwm sim nrog cov zaus hauv qab no:

peripheral edema - 1.2 thiab 0%,
mob taub hau - 2.4 thiab 0%,
xeev siab - 1.2 thiab 1.1%,
fungal kis ntawm daim tawv nqaij - 1.2 thiab 0%,
hnoos - 1.2 thiab 0%,
hypoglycemia - 2.4 thiab 0%,
sab qaum cov kab mob ua pa - 1.8 thiab 0%,
ntuav - 1.2 thiab 0%.

Kev sib xyaw ua ke nrog cov tshuaj insulin

Hauv 24 lub lis piam placebo-tswj kev kawm txog kev siv ua ke 100 mg ntawm sitagliptin ib hnub thiab ib qho tshuaj insulin tsis tu ncua (tsis muaj los yog nrog metformin), cov kev mob tshwm sim tau pom ntau zaus (nrog ntau zaus ntawm ≥ 1%) hauv cov pab pawg tau txais sitagliptin nrog insulin (tsis muaj lossis nrog metformin) ) dua li hauv cov placebo pawg nrog insulin (tsis muaj lossis nrog metformin). Qhov xwm txheej ntawm cov nyom cov xwm txheej yog (feem):

mob taub hau - 1.2 / 0%,
mob npaws - 1.2 / 0.3%,
cov tshuaj tiv thaiv ntshav qab zib - 9.6 / 5.3%.

Lwm qhov kev tshawb nrhiav 24-lub lim tiam, hauv uas sitagliptin tau siv los ua cov khoom siv ntxiv rau kev kho insulin (tsis muaj lossis nrog metformin), tsis tau qhia txog cov kev mob tshwm sim uas cuam tshuam nrog kev noj tshuaj.

Kev mob caj dab

Kev tsom xam dav dav ntawm 19 ob qhov muag tsis pom, kev tshawb xyuas qhov tseeb ntawm kev siv tshuaj sitagliptin hauv ib koob tshuaj 100 mg txhua hnub los yog cov tshuaj tiv thaiv sib cuam tshuam (nquag lossis cov placebo) tau qhia tias qhov tshwm sim ntawm qhov tsis lees paub tseeb txog kev mob ntsig txog pancreatitis yog 0.1 tus neeg ntawm 100 tus neeg mob-xyoo ntawm txoj kev kho hauv txhua pawg.

Clinically qhov teeb meem sib txawv hauv cov cim tseem ceeb lossis electrocardiograms, suav nrog lub sijhawm ntawm QTc luv, tsis pom nrog sitagliptin.

Kev Soj Ntsuam Kev Ntsuas Ntshav plawv Ntsuas Kev Nyab Xeeb (TECOS)

TECOS suav nrog 7332 cov neeg mob uas tau txais 100 mg ntawm sitagliptin ib hnub (lossis 50 mg rau ib hnub yog tias lub hauv paus kwv yees tus nqi glomerular npaum li cas yog ≥ 30 thiab 2), thiab 7339 cov neeg mob uas tau txais cov placebo nyob rau hauv cov pejxeem ib txwm ntawm cov neeg uas tau muab haujlwm. kev kho

Cov tshuaj lossis cov placebo tau ntxiv rau hauv kev kho mob kom raws li cov qauv hauv tebchaws uas twb muaj lawm rau kev xaiv lub hom phiaj ntawm HbA_1C thiab tswj cov kab mob plawv txaus ntshai. Tag nrho ntawm 2004 tus neeg mob txij li lub hnub nyoog ntawm 75 xyoo tau suav nrog hauv kev soj ntsuam, uas 970 tau txais sitagliptin, thiab 1034 tau txais cov placebo. Cov teeb meem tag nrho ntawm cov kev mob tshwm sim loj heev hauv ob pab pawg no zoo ib yam. Kev ntsuam xyuas ntawm cov teeb meem cuam tshuam nrog cov ntshav qab zib mellitus, uas tau qhia ua ntej rau kev saib xyuas, qhia tawm qhov sib piv ntawm cov kev mob tshwm sim tsis zoo ntawm cov pab pawg thaum noj cov sitagliptin / placebo, suav nrog kev ua haujlwm tsis zoo hauv lub raum (1.4 / 1.5%) thiab kis (18, 4 / 17.7%). Cov kev mob tshwm sim rau cov neeg mob hnub nyoog 75 xyoos thiab laus dua ntawd feem ntau zoo ib yam rau cov pej xeem.

Qhov xwm txheej ntawm kev mob ntshav qab zib ntau hauv cov pej xeem ntawm cov neeg mob uas tau kho "kev npaj siab kho" kev kho mob thiab tus uas tau txais kev kho mob sulfonylurea thiab / lossis insulin kho thaum noj cov tshuaj sitagliptin / placebo yog 2.7 / 2.5%, feem. Ntxiv mus, hauv cov neeg mob uas thaum xub thawj tsis noj sulfonylurea thiab / los yog cov tshuaj insulin npaj, qhov zaus no yog 1 / 0.7%, feem. Thaum lub sij hawm tshuaj ntsuam, qhov tshwm sim ntawm cov paub tseeb tias muaj mob pancreatitis thaum noj cov tshuaj / placebo yog 0.3 / 0.2%, thiab malignant neoplasms - 3.7 / 4%, feem.

Kev soj ntsuam tom qab cuv npe tas

Kev cuv npe tom qab kev saib xyuas ntawm kev siv cov sitagliptin hauv kev kho mob monotherapy thiab / lossis kev sib xyaw nrog lwm cov tshuaj hypoglycemic qhia ntxiv cov kev mob tshwm sim. Vim tias cov ntaub ntawv no tau txais los ntawm cov pej xeem ntawm cov lej tsis tau txiav txim siab, qhov ntau zaus thiab kev sib raug zoo nrog kev kho cov xwm txheej no tsis tuaj yeem tsim.

Cov no suav nrog:

angioedema,
kev tsis haum qhov ua haujlwm, suav nrog anaphylaxis,
mob caj dab / ua pob liab, urticaria, pemphigoid, tawv nqaij vasculitis, tawv nqaij ua rau lub cev tawv nqaij, nrog rau Stevens-Johnson syndrome,
mob pancreatitis, suav nrog hemorrhagic thiab necrotic cov ntaub ntawv nrog / tsis muaj kev ploj tuag,
lub raum tsis ua hauj lwm zoo, suav nrog mob raum tsis ua haujlwm (qee qhov, yuav tsum raug lim ntshav),
sab sauv ntawm txoj hlab ua pa tuaj
nasopharyngitis,
ntuav, cem quav,
mob taub hau
arthralgia, myalgia,
mob hauv cov nqua, nraub qaum.

Kev hloov pauv hauv tsev kho mob

Hauv kev tshawb fawb feem ntau, muaj qhov nce me ntsis ntawm leukocyte suav hauv cov neeg mob tau txais sitagliptin (100 mg ib hnub) piv nrog cov placebo pawg (200 μl ntawm qhov nruab nrab, thaum pib ntawm txoj kev kho qhov ntsuas yog 6600 μl), uas yog vim muaj qhov nce ntawm neutrophils.

Qhov nce me ntsis hauv cov ntsiab lus uric acid (los ntawm 0.2 mg rau 1 dl) tau tshawb pom nrog 100 thiab 200 mg ntawm sitagliptin ib hnub piv nrog cov placebo. Ua ntej pib kev kho mob, tus nqi nruab nrab yog 5-5.5 mg rau 1 dL. Tsis muaj cov tshaj tawm ntawm gout tau tshaj tawm.

Kuj tseem muaj qhov txo qis me ntsis ntawm tag nrho cov alkaline phosphatase hauv cov pab pawg tau txais cov tshuaj, piv nrog cov pawg placebo (yuav luag 5 IU ib 1 liter, ntawm qhov nruab nrab, ua ntej pib kho, qhov siab yog 56 rau 62 IU ib 1 liter), uas cuam tshuam nrog ib qho me me txo cov pob txha muaj nuj nqi ntawm qhov enzyme.

Cov kev hloov hauv chav ntsuas tsis pom qhov tseem ceeb hauv chaw kho mob.

Kev ntshav siab

Raws li kev soj ntsuam los ntawm kev soj ntsuam, qhov tshwm sim ntawm hypoglycemia thaum lub sij hawm monotherapy nrog sitagliptin lossis nws cov kev kho mob ib txhij nrog cov tshuaj tsis ua rau muaj cov kab mob no (pioglitazone, metformin) zoo ib yam li ntawd hauv cov pab pawg placebo. Ib yam li nrog rau lwm cov tshuaj hypoglycemic, hypoglycemia tshwm sim thaum lub sijhawm tswj hwm Xelevia ua ke nrog sulfonylurea derivatives lossis insulin. Txhawm rau txo qhov zoo li ntawm sulfon-hob hypoglycemia, ntau npaum ntawm cov sulfonylurea derivative tau txo.

Kev Kho Mob Hauv Cov Neeg Laus

Kev nyab xeeb thiab kev ua tau zoo ntawm Xelevia hauv kev soj ntsuam hauv cov neeg mob laus (409 tus neeg mob) uas muaj hnub nyoog 65 xyoos ntau dua piv rau cov pab pawg hauv hnub nyoog 65 xyoos. Hauv qhov no, kho kom haum cov tshuaj ntau ntxiv nyob ntawm lub hnub nyoog ntawm tus neeg mob tsis tas yuav tsum tau ua. Nws yuav tsum tau nyob rau hauv lub siab tias cov neeg laus cov neeg mob ua rau muaj kev tshwm sim ntawm lub raum tsis ua haujlwm ntau dua. Yog li no, nyob rau hauv qhov muaj qhov tsis zoo nyob tsis zoo hauv cov pab pawg hnub nyoog no, zoo li hauv lwm qhov, kev noj cov tshuaj sitagliptin yog kho tau.

Hauv kev kawm txog TECOS, cov neeg ua haujlwm pab dawb tau txais sitagliptin ntawm koob tshuaj 100 mg txhua hnub (lossis 50 mg rau ib hnub nrog tus nqi pib ntawm kev kwv yees glomerular pom kev nqi ≥ 30 thiab 2) lossis cov placebo. Lawv tau ntxiv rau hauv kev kho mob raws li cov qauv hauv tebchaws muaj txiaj ntsig rau kev txiav txim siab cov hom phiaj HbA._1C thiab tswj cov kab mob plawv txaus ntshai. Thaum kawg ntawm lub sijhawm kawm nruab nrab (3 xyoo) hauv cov neeg mob ntshav qab zib hom 2, noj cov tshuaj ntxiv rau kev kho mob tsis ua rau muaj feem tau mus pw hauv tsev kho mob vim lub plawv tsis ua hauj lwm (feem phom sij - 1, 95% kev ntseeg siab ib ncua - ntawm 0.83 rau 1.2, p = 0.98 rau qhov sib txawv ntawm cov zaus ntawm kev pheej hmoo) lossis kev pheej hmoo ntawm kev phiv loj heev los ntawm cov hlab plawv (qhov sib piv ntawm cov leeg - 0.98, 95% kev ntseeg siab nyob nruab nrab - los ntawm 0.89 txog 1.08, p CYP 2C8, CYP 2C9 thiab CYP 3 A 4. Raws li hauv cov ntaub ntawv hauv vitro , nws kuj tsis inhibit CYP 1A2, CYP 2B6, CYP 2C19 thiab CYP 2 D 6 isoenzymes thiab tsis ntxias CYP 3 A 4 isoenzyme.

Nrog rau kev siv ntau yam ua ke ntawm metformin nrog sitagliptin, qhov kev hloov pauv tseem ceeb ntawm qhov pharmacokinetic cov thib ob tsis tau pom hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus.

Cov ntaub ntawv tau los ntawm cov pej xeem pharmacokinetic tsom xam ntawm cov neeg mob uas muaj ntshav qab zib hom 2 qhia tau hais tias kev kho mob concomitant tsis muaj kev cuam tshuam loj hauv kev kho mob ntawm pharmacokinetics ntawm cov tshuaj. Txoj kev tshawb fawb no tau tshuaj xyuas cov tshuaj uas feem ntau tau siv rau ntshav qab zib hom 2, suav nrog cov hauv qab no:

β-blockers
lipid-tej tshuaj (xws li ezetimibe, fibrates, statins),
Cov tshuaj tiv thaiv kab mob (xws li sertraline, fluoxetine, bupropion),
cov tshuaj tiv thaiv kab mob hauv lub cev (piv txwv li clopidogrel),
antihistamines (piv txwv li cetirizine),
tshuaj rau kev kho mob ntawm kev kho erectile kawg (piv txwv li sildenafil),
tshuaj tsis-tshuaj steroidal (xws li celecoxib, diclofenac, naproxen),
proton twj tso kua mis inhibitors (xws li lansoprazole, omeprazole),
antihypertensive tshuaj (xws li hydrochlorothiazide, qeeb calcium calcium blockers, angiotensin II receptor antagonists, angiotensin hloov mus rau enzyme inhibitors).

Kev nce me ntsis hauv AUC thiab C _m_ah digoxin (los ntawm 11 thiab 18%, feem) tau sau tseg nrog nws siv ua ke nrog sitagliptin. Qhov nce no tsis yog qhov tseem ceeb hauv tsev kho mob. Nrog kev sib koom tes, kev hloov pauv cov tshuaj tsis pom zoo.

Nce AUC thiab C _m_ah Sitagliptin (29 thiab 68%, feem) tau pom thaum siv nws ntawm 100 koob ntawm mg rau qhov sib xyaw nrog ib koob tshuaj cyclosporine (lub zog txwv ntawm P-glycoprotein) rau kev tswj hwm qhov ncauj ntawm ib koob ntawm 600 mg. Cov kev pauv hloov uas tau pom tshwm sim hauv cov qauv tshuaj pharmacokinetic tsis suav pom tias tseem ceeb hauv lub tsev kho mob. Thaum siv cov tshuaj sib tov nrog cyclosporine lossis lwm tus P-glycoprotein inhibitor (piv txwv, ketoconazole), nws tsis pom zoo kom hloov cov tshuaj Xelevia.

Raws li cov pej xeem pharmacokinetic tsom xam ntawm cov neeg mob thiab cov neeg ua haujlwm noj qab haus huv (N = 858) rau ntau yam tshuaj tsis sib xws (N = 83, yuav luag ib nrab ntawm cov tshuaj tawm hauv ob lub raum), cov tshuaj no tsis muaj kev cuam tshuam loj rau lub pharmacokinetics ntawm sitagliptin.

Cov cim ntawm Xelevia yog Yasitara, Sitagliptin phosphate monohydrate, Januvia.

Kev taw qhia thiab contraindications

Kev qhia rau kev siv "Xelevia" yog:

tsis tshua rhiab ntawm cov ntshav qab zib mus rau hypoglycemia nyob rau hauv tus ntawm neuropathy lossis lwm yam teebmeem kev noj qab haus huv,
predisposition rau sib ntau ntawm hypoglycemia thaum hmo ntuj,
laus lawm
qhov xav tau kom muaj kev mloog zoo ntxiv thaum tsav tsheb lossis ua haujlwm nrog cov txheej txheem cov nyom,
nquag tawm tsam ntshav qog ntshav thaum noj sulfonylurea.

Ua ntej noj nws, nws yog ib qho tseem ceeb heev kom paub koj tus kheej nrog cov contraindications. Cov no suav nrog:

coj menyuam, lactation,
ntshav qab zib hom 1
ketoacidosis uas mob ntshav qab zib, hnub nyoog qis dua 18 xyoo,
raum tsis ua hauj lwm ntawm cov qauv hnyav los sis hnyav.

Vim tias tsis muaj cov kev tshawb fawb tswj tau hais txog kev ua tau zoo thiab kev nyab xeeb ntawm cov tshuaj rau cov poj niam cev xeeb tub, Xelevia tsis pom zoo siv thaum cev xeeb tub. Tsis tas li, muaj peev xwm ntawm nws txoj kev nthuav dav nrog rau niam cov kua mis tsis tau kawm, yog li ntawd, nrog lactation, nws yog contraindicated.

Tsuas tshuaj thiab tshaj

Cov koob tshuaj pom zoo ntawm cov tshuaj yog 100 mg 1 zaug nyob rau ib hnub. Nws yog noj ntawm qhov ncauj raws li cov tshuaj tseem ceeb lossis nrog ntxiv nrog metformin lossis tshuaj nrog lwm cov tshuaj sib xyaw. Noj tshuaj tsis muaj feem rau khoom noj. Qhov ntau npaum ntawm "Xelevia" thiab cov tshuaj ntxiv, lawv qhov sib piv yog tsim los ntawm tus kws kho mob mus koom nrog hauv qhov kev xav ntawm cov lus qhia

Yog tias koj plam ntsiav tshuaj, nws raug nquahu kom koj noj sai li sai tau tom qab tus neeg nco qab qhov no. Hauv ib hnub nws raug txwv tsis pub noj ob zaug ntawm cov tshuaj.

Hauv kev sim tshuaj rau cov neeg tuaj yeem noj qab haus huv, cov tshuaj ntau kawg nkaus 800 mg rau cov neeg mob ntshav qab zib tau txais txiaj ntsig zoo. Yam tsawg kawg hloov ntawm qhov ntsuas tsis tseem ceeb. Dosages saum 800 mg tsis tau kawm. Kev phiv tshuaj thaum noj 400 mg ntawm "Xelevia" rau 4 lub lis piam tsis pom pom.

Tab sis, yog tias kev haus ib qho rau ib qho laj thawj twg tau tshwm sim, tus neeg mob tsis xav tias nyob tsis tau, tom qab ntawd lub koom txoos ntawm cov xwm txheej no yuav tsum muaj:

hle cov tshuaj tsis tau tawm ntawm lub plab zom mov,
tshuaj xyuas cov ntsuas, nrog rau saib xyuas kev ua haujlwm ntawm lub siab los ntawm ECG,
nqa tawm kev kho mob.

Cov tshuaj active sitagliptin tsis zoo lim ntshav. Tsuas yog 13,5% raug zam tawm thaum lub sijhawm 4-teev ntawm cov txheej txheem. Nws tau raug tsa los ua qhov chaw kawg nkaus.

Txoj hauv kev loj tshaj plaws kom tshem tawm cov tshuaj ntawm lub cev yog los ntawm lub raum tsis ua haujlwm. Rau cov neeg mob uas muaj cov kab mob zoo li no ntawm lub raum, qhov ntau npaum li cas tau tsim los nruab nrab, tab sis tus yam ntxwv ntawm cov teeb meem hauv lub raum, nws txo qis:

sim ua hauj lwm nruab nrab los yog tsis ua hauj lwm hnyav
davhlau ya nyob twg theem ntawm lub raum tsis ua hauj lwm.

Xaus

Ua raws li kev piav qhia ntawm cov tshuaj thiab tshuaj xyuas txog nws, peb tuaj yeem xaus tias nws ua haujlwm tau zoo thiab muaj lub txiaj ntsig zoo rau kev saib xyuas zoo ntawm cov neeg mob. Ib qho zoo dua indisputable yog qhov yuav luag tiav ntawm kev phiv los ntawm lub cev. Lawm, ib tug neeg yuav tsis muaj peev xwm xaiv cov ntau npaum, thiab ntau dua qhov tsim nyog ua ke nrog lwm cov tshuaj, tsis muaj kev phom sij rau nws kev noj qab haus huv. Txhawm rau ua qhov no, koj yuav tsum hu rau tus kws kho qhov mob endocrinologist, thiab tsis txhob ua tus kheej kev noj tshuaj.

Kev Sib Sau thiab daim ntawv ntawm kev tso tawm

Ntsiav tshuaj - 1 ntsiav tshuaj:

Cov khoom siv nquag: sitagliptin phosphate monohydrate - 128,5 mg, uas sib haum rau cov ntsiab lus ntawm sitagliptin - 100 mg,
Cov tub ntxhais: cov microcrystalline cellulose - 123.8 mg, tsis siv tshuaj calcium calcium phosphate - 123,8 mg, croscarmellose sodium - 8 mg, magnesium stearate - 4 mg, sodium stearyl fumarate - 12 mg,
muaj pes tsawg leeg: opadry II beige, 85F17438 - 16 mg (polyvinyl cawv - 40%, titanium dioxide (E171) - 21.56%, macrogol 3350 (polyethylene glycol) - 20.2%, talc - 14.8%, daj hlau oxide (E172) - 3.07% , hlau oxide liab (E172) - 0.37%).

14 pcs. - hlwv (2) - pob khoom los ntawm cardboard.

Cov ntsiav tshuaj, coated nrog beige zaj duab xis plhaub, yog puag ncig, biconvex, nrog engraving "277" ntawm ib sab thiab du ntawm lwm yam.

Cov tshuaj Xelevia (sitagliptin) yog qhov ncauj tsis zoo, xaiv tau ntau yam tshuaj tiv thaiv kab mob enzyme dipeptidyl peptidase-4 (DPP-4), npaj rau kev kho mob hom 2 ntshav qab zib mellitus. Sitagliptin sib txawv hauv cov qauv tshuaj thiab cov tshuaj pharmacological los ntawm analogues ntawm glucagon-zoo li peptide-1 (GLP-1), insulin, sulfonylurea derivatives, biguanides, gamma receptor agonists ua kom los ntawm peroxisome proliferator (PPAR-γ), alpha-glucosidase inhibitors, amylin analogues. Los ntawm inhibiting DPP-4, sitagliptin tsub kom qhov siab ntxiv ntawm ob cov tshuaj hormones ntawm tsev neeg incretin: GLP-1 thiab glucose-nyob insulinotropic polypeptide (HIP). Cov tshuaj hormones ntawm tsev neeg incretin yog zais hauv cov hnyuv nruab hnub, lawv qhov kev nce siab hauv cov lus teb ntxiv rau kev noj zaub mov. Tus incretins yog ib feem ntawm cov txheej txheem kho mob sab hauv lub zog rau kev tswj hwm cov ntshav qabzib homeostasis. Thaum lub cev ntshav lossis ntshav qabzib muaj ntau ntxiv, cov tshuaj hormones ntawm tsev neeg muaj ntau ntxiv los ua rau muaj insulin hluavtaws ntau ntxiv, nrog rau nws qhov zais cia los ntawm pancreatic beta hlwb vim kev taw qhia rau intracellular mechanisms cuam tshuam nrog cyclic adenosine monophosphate (AMP).

GLP-1 kuj tseem pab txhawb ntxiv kom muaj kev zais ntawm glucagon los ntawm alpha cell. Kev poob qis hauv glucagon concentration tiv thaiv tom qab ntawm qhov nce ntawm insulin concentration pab txo cov piam thaj hauv qab los ntawm daim siab, uas thaum kawg ua rau txo qis glycemia. Qhov kev ua haujlwm ntawm qhov kev sib txawv no txawv ntawm cov txheej txheem ntawm kev ua ntawm sulfonylurea derivatives, uas txhawb kev tso tawm ntawm insulin txawm tias ntawm cov ntshav qabzib tsawg nyob rau hauv cov ntshav, uas yog fraught nrog txoj kev loj hlob ntawm sulfone-hus hypoglycemia tsis yog hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, tab sis kuj nyob rau hauv cov neeg noj qab haus huv.

Thaum lub siab tsis zoo ntawm cov piam thaj hauv cov ntshav, cov txiaj ntsig tau teev ntawm incretins ntawm insulin tso tawm thiab qhov txo qis hauv glucagon zais cia tsis pom. GLP-1 thiab HIP tsis cuam tshuam rau qhov glucagon tso tawm rau hauv kev teb rau hauv lub ntsej muag hypoglycemia. Nyob rau hauv cov kev mob tshwm sim hauv lub cev, kev ua si ntawm incretins raug txwv los ntawm enzyme DPP-4, uas tau nrawm hydrolyzes nce nrog kev tsim cov khoom tsis muaj zog.

Sitagliptin txwv tsis pub cov hydrolysis ntawm incretins los ntawm enzyme DPP-4, yog li ua kom cov ntshav ntau dua ntawm cov nquag cov ntaub ntawv ntawm GLP-1 thiab HIP. Los ntawm nce qhov kev mloog ntxiv ntawm incretins, sitagliptin tsub kom cov piam thaj-tso tawm ntawm cov kua dej thiab pab txo qis kev ua haujlwm ntawm glucagon. Hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus nrog hyperglycemia, cov kev hloov pauv hauv kev zais ntawm insulin thiab glucagon ua rau txo qis ntawm cov ntshav glycosylated hemoglobin HbA1C thiab txo qis hauv plasma concentration ntawm cov piam thaj, txiav txim siab ntawm lub plab tsis muaj zog thiab tom qab kev ntsuam xyuas mob.

Hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, noj ib koob ntawm Xelevia ua rau kev cuam tshuam ntawm kev ua si ntawm enzyme DPP-4 rau 24 teev, uas ua rau muaj kev nce siab ntau ntxiv ntawm cov ntshav nce ntxiv GLP-1 thiab HIP los ntawm qhov tseem ceeb ntawm 2-3, kev nce ntshav ntau ntxiv ntawm insulin thiab C peptide, qhov kev txo qis hauv cov concentration ntawm glucagon nyob rau hauv cov ntshav ntshav, txo qis ntawm cov piam thaj, nrog rau kev txo qis glycemia tom qab cov piam thaj los yog zaub mov noj.

Cov pharmacokinetics ntawm sitagliptin tau piav qhia ntau yam hauv cov neeg muaj kev noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2. Hauv cov neeg muaj kev noj qab haus huv, tom qab qhov ncauj tswj hwm 100 mg ntawm sitagliptin, kev nqus tshuaj sai yog pom nrog lub siab tshaj plaws (Cmax) hauv thaj tsam li 1 mus rau 4 teev txij li lub sijhawm saib xyuas. Thaj chaw hauv qab qhov nkhaus-sijhawm nkhaus (AUC) nce raws qib koob tshuaj thiab cov ntsiab lus noj qab haus huv yog 8.52 μmol / L * teev thaum noj 100 mg ntawm qhov ncauj, Cmax yog 950 nmol / L. Lub plasma AUC ntawm sitagliptin nce ntxiv kwv yees li 14% tom qab kev noj tshuaj ntxiv ntawm 100 mg ntawm tshuaj los ua kom tiav qhov sib luag ntawm lub xeev tom qab siv thawj zaug. Nyob rau hauv- thiab kev sib tshuam hloov sib tshooj ntawm sitagliptin AUC tsis tau zoo.

Qhov tsis ncaj ncees ntawm bioavailability ntawm sitagliptin yog kwv yees li 87%. Txij li thaum ua kev sib xyaw ua ke ntawm sitagliptin thiab cov zaub mov muaj roj tsis muaj kev cuam tshuam rau cov pharmacokinetics, cov tshuaj Xelevia tuaj yeem yog tshuaj tsis hais cov zaub mov noj.

Qhov ntim nruab nrab ntawm kev faib tawm hauv qhov sib luag tom qab ib koob nkaus xwb ntawm 100 mg ntawm sitagliptin hauv cov neeg tuaj yeem noj qab haus huv yog kwv yees li 198 l. Tus zauv seem ntawm sitagliptin uas khi rau cov ntshav muaj protein tsawg nyob ntawm 38%.

Kwv yees li 79% ntawm cov sitagliptin yog cov tsis hloov pauv los ntawm lub raum. Tsuas yog ib feem me me ntawm cov tshuaj tau txais hauv lub cev yog metabolized.

Tom qab kev tswj hwm ntawm 14C-daim ntawv lo ntawm sitagliptin sab hauv, kwv yees li 16% ntawm cov xov tooj cua sitagliptin raug tshem tawm raws li nws cov metabolites. Kab ntawm 6 metabolites ntawm sitagliptin raug kuaj pom, tej zaum tsis muaj DPP-4 inhibitory kev ua si. Hauv cov kev tshawb fawb hauv vitro tau qhia tias thawj cov isoenzymes koom nrog cov metabolism tsis txaus ntawm sitagliptin yog CYP3A4 thiab CYP2C8.

Tom qab tswj hwm ntawm 14C-daim ntawv lo sitagliptin rau hauv cov neeg ua haujlwm noj qab haus huv, kwv yees li 100% ntawm cov tshuaj sitagliptin raug tso tawm: 13% los ntawm txoj hnyuv, 87% los ntawm lub raum hauv ib lub lis piam tom qab noj cov tshuaj. Qhov kev tshem tawm txhais tau tias ib nrab ntawm lub neej ntawm sitagliptin los ntawm kev tswj hwm qhov ncauj ntawm 100 mg yog kwv yees li 12.4 teev; lub raum tshem tau yog kwv yees li 330 ml / min.

Kev nthuav dav ntawm sitagliptin yog nqa tawm feem ntau los ntawm kev tawm los ntawm lub raum los ntawm kev ua haujlwm ntawm cov tubular muaj kev zais cia. Sitagliptin yog lub hauv paus rau qhov thauj cov organic tib neeg anions ntawm hom thib peb (hOAT-3), uas tuaj yeem cuam tshuam txog kev zam ntawm sitagliptin los ntawm lub raum. Clinically, kev koom tes ntawm hOAT-3 hauv kev thauj khoom ntawm sitagliptin tseem tsis tau kawm. Sitagliptin kuj tseem yog cov p-glycoprotein, uas tuaj yeem cuam tshuam nrog kev zam ntawm sitagliptin los ntawm lub raum. Txawm li cas los xij, cyclosporin, ib qho inhibitor ntawm p-glycoprotein, tsis txo qis kev tshem tawm ntawm sitagliptin.

Pharmacokinetics hauv cov neeg mob ib leeg:

Cov neeg mob raum tsis ua haujlwm:

Txoj kev kawm qhib ntawm sitagliptin ntawm kev noj tshuaj ntawm 50 mg ib hnub twg tau tshawb nrhiav nws cov tshuaj pharmacokinetics hauv cov neeg mob uas muaj qib sib txawv ntawm qhov mob ntawm lub raum tsis ua haujlwm. Cov neeg mob suav nrog kev tshawb fawb tau muab faib ua pab pawg ntawm cov neeg mob uas lub raum tsis ua haujlwm me me (creatinine tshem tawm los ntawm 50 txog 80 ml / min), mob nruab nrab (creatinine tshem tawm ntawm 30 txog 50 ml / min) thiab mob raum tsis zoo (creatinine tshem tawm tsawg dua 30 ml / min) , nrog rau lub davhlau ya nyob twg ib theem ntawm lub raum tsis ua hauj lwm uas yuav tsum tau lim ntshav.

Hauv cov neeg mob uas tsis ua haujlwm hauv lub raum me me, tsis muaj kev hloov pauv tseem ceeb hauv plasma concentration ntawm sitagliptin piv nrog pawg tswj hwm ntawm cov neeg ua haujlwm noj qab haus huv.

Kev nce ob npaug ntawm sitagliptin AUC piv nrog pab pawg tswj tau pom nyob hauv cov neeg mob uas mob raum tsis txaus, kwv yees li ntawm plaub feem pua ntawm AUC raug pom hauv cov neeg mob uas mob raum tsis ua haujlwm loj, thiab ntxiv rau cov neeg mob raum tsis mob lub raum tsis ua haujlwm piv nrog pawg tswj hwm. Sitagliptin tau raug tshem tawm me ntsis los ntawm hemodialysis: tsuas yog 13.5% ntawm cov koob tshuaj tau raug tshem tawm ntawm lub cev thaum lub sijhawm 3-4 teev lim ntshav lim ntshav.

Yog li, txhawm rau kom ua tiav kev kho kom haum xeeb ntawm sitagliptin hauv ntshav ntshav (zoo ib yam li cov neeg mob uas lub raum ua haujlwm) hauv cov neeg mob uas tsis tshua mob plab mus rau lub raum tsis ua haujlwm, yuav tsum tau txhaj tshuaj.

Cov neeg mob mob siab tsis ua haujlwm:

Hauv cov neeg mob uas muaj mob hepatic tsis txaus (7-9 cov ntsiab lus ntawm Child-Pugh nplai), qhov nruab nrab ntawm AUC thiab Cmax ntawm sitagliptin nrog ib koob tshuaj 100 mg nce ntxiv kwv yees 21% thiab 13%, feem. Yog li, kev hloov kho rau tshuaj rau me me mus rau daim siab tsis ua haujlwm tsis tas yuav tsum.

Tsis muaj cov ntaub ntawv tshawb fawb txog kev siv cov sitagliptin hauv cov neeg mob uas tsis muaj peev xwm rau hepatic txaus (ntau dua li 9 ntsiab lus ntawm Cov Ntawv Qhia Me-Pugh). Txawm li cas los xij, vim tias qhov tseeb tias sitagliptin feem ntau ua rau lub raum ua haujlwm, ib qho yuav tsum tsis txhob cia siab tias muaj kev hloov pauv tseem ceeb ntawm pharmacokinetics ntawm sitagliptin hauv cov neeg mob uas muaj mob tsis txaus hnyav hnyav.

Lub hnub nyoog ntawm cov neeg mob tsis muaj kev cuam tshuam los ntawm kev kho mob tseem ceeb ntawm cov tshuaj pharmacokinetic ntawm sitagliptin. Piv nrog cov neeg mob yau, cov neeg mob laus (65-80 xyoo) muaj cov sitagliptin concentration ntawm kwv yees li 19% siab dua. Tsis tas yuav tsum kho qhov koob tshuaj raws li lub hnub nyoog.

Tshuaj qhov ncauj hypoglycemic.

Xelevia Sab Sij Huam

Sitagliptin feem ntau ua tau zoo rau ob qho tib si hauv monotherapy thiab hauv kev sib xyaw nrog lwm cov tshuaj hypoglycemic. Hauv kev sim tshuaj, tag nrho cov tshwm sim ntawm qhov tshwm sim tsis zoo, nrog rau lub caij nyoog ntawm kev tshem tawm cov tshuaj vim muaj cov xwm txheej tsis zoo, zoo ib yam li cov uas muaj cov placebo.

Raws li 4 cov kev tshawb fawb tshuaj (ntev ntev 18-24 lub lis piam) ntawm sitagliptin nyob rau hauv ib koob tshuaj txhua hnub ntawm 100-200 mg li mono- lossis kev sib koom ua ke nrog kev kho mob nrog metformin lossis pioglitazone, tsis muaj qhov tsis zoo uas cuam tshuam nrog kev kawm txog tshuaj tau tshawb pom, qhov ntau zaus uas dhau 1% hauv pawg neeg mob noj sitagliptin. Cov ntaub ntawv kev nyab xeeb ntawm kev txhaj tshuaj txhua hnub ntawm 200 mg tau piv nrog daim ntawv qhia kev nyab xeeb ntawm kev txhaj tshuaj txhua hnub ntawm 100 mg.

Kev tsom xam ntawm cov ntaub ntawv tau txais thaum cov kev sim kho mob saum toj no pom tau hais tias tag nrho kev muaj qog ntshav qab zib hauv cov neeg mob noj sitagliptin zoo ib yam li cov placebo (sitagliptin 100 mg-1.2%, sitagliptin 200 mg-0.9%, placebo - 0.9%). Qhov ntau zaus ntawm kev soj ntsuam lub plab cov nyom tsis zoo thaum noj cov tshuaj sitagliptin nyob rau hauv ob zaug tau zoo ib yam li ntawd thaum noj cov placebo (tshwj tsis yog tias muaj kev pheej hmoo ntau tshaj thaum noj sitagliptin ntawm koob tshuaj 200 mg ib hnub): mob plab (sitagliptin 100 mg - 2 , 3%, sitagliptin 200 mg - 1.3%, tso tshuaj - 2.1%), xeev siab (1.4%, 2.9%, 0.6%), ntuav (0.8%, 0.7% , 0.9%), raws plab (3.0%, 2.6%, 2.3%).

Hauv txhua qhov kev tshawb fawb, qhov tshwm sim tsis zoo nyob rau hauv daim ntawv ntawm hypoglycemia tau sau tseg los ntawm txhua daim ntawv tshaj tawm ntawm cov kws kho mob qhia tias cov tsos mob hypoglycemia, kev ntsuas cov ntshav qabzib hauv lub siab tsis xav tau.

Pib txoj kev kho ua ke nrog metformin:

Hauv 24-lub lis piam, cov tshuaj placebo-soj ntsuam qhov tseeb ntawm kev pib ua ke nrog kev kho mob nrog sitagliptin hauv ib koob tshuaj 100 mg thiab metformin hauv ib koob tshuaj 1000 mg lossis 2000 mg (sitagliptin 50 mg + metformin 500 mg lossis 1000 mg x 2 zaug hauv ib hnub) hauv pawg kho mob sib xyaw Piv nrog metformin monotherapy pab pawg, cov kev coj ua tsis zoo hauv qab no tau pom:

Kev phiv tshuaj txuam nrog kev noj cov tshuaj tau pom nrog ntau zaus & gt1% hauv pawg kho mob sitagliptin thiab ntau dua li ntau dua ntawm cov pab pawg kho mob metformin hauv kev kho mob monotherapy: raws plab (sitagliptin + metformin - 3.5%, metformin - 3.3%), dyspepsia (1, 3%, 1.1%), mob taub hau (1.3%, 1.1%), pom tsis tau (1.3%, 0.5%), mob ntshav qab zib (1.1%, 0.5%), ntuav (1.1%, 0.3%).

Ua ke nrog sulfonylurea derivatives los yog sulfonylurea derivatives thiab metformin:

Hauv 24 lub lis piam placebo-tswj kev kawm ua ke nrog kev kho mob sib xyaw nrog sitagliptin (koob tshuaj txhua hnub 100 mg) thiab glimepiride lossis glimepiride thiab metformin, cov xwm txheej tsis zoo hauv qab no tau pom nyob hauv pawg tshuaj kawm piv rau pab pawg ntawm cov neeg mob noj placebo thiab glimepiride lossis glimepiride thiab metformin:

Kev phiv tshuaj uas cuam tshuam nrog kev noj cov tshuaj tau pom nrog ntau zaus & gt1% hauv pawg kho mob nrog sitagliptin thiab ntau zaus ntau dua li ntawm kev kho ua ke nrog cov placebo: hypoglycemia (sitagliptin - 9,5%, placebo - 0.9%).

Pib kev kho ua ke nrog PPAR-γ agonists:

Hauv kev tshawb nrhiav 24 lub lim tiam ntawm kev pib ua ke nrog kev kho mob nrog sitagliptin hauv ib koob tshuaj 100 mg thiab pioglitazone hauv ib koob tshuaj 30 mg txhua hnub, cov xwm txheej tsis zoo hauv qab no tau pom nyob hauv pawg kho mob sib piv piv rau pioglitazone monotherapy:

Cov kev tsis haum siab cuam tshuam nrog kev noj tshuaj tau pom tias muaj ntau zaus & gt1% hauv pawg kho mob ntawm sitagliptin thiab ntau zaus ntau dua li pawg kho mob ntawm pioglitazone hauv kev kho mob monotherapy: asymptomatic txo hauv cov ntshav qabzib concentration (sitagliptin + pioglitazone - 1.1%, pioglitazone - 0.0%) cov tsos mob tus mob hypoglycemia (0.4%, 0.8%).

Ua ke nrog PPAR-y agonists thiab metformin:

Raws li kev tshawb pom cov tshuaj placebo hauv kev kho cov sitagliptin (koob tshuaj txhua hnub ntawm 100 mg) hauv kev sib xyaw nrog rosiglitazone thiab metformin hauv pab pawg tshuaj, cov xwm txheej tsis zoo hauv qab no tau pom hauv kev sib piv nrog pab pawg ntawm cov neeg mob noj placebo srosiglitazone thiab metformin:

Thaum 18 lub lim tiam ntawm kev soj ntsuam:

Kev phiv tshuaj los cuam tshuam nrog kev noj cov tshuaj tau pom nrog ntau zaus & gt1% hauv pawg kho mob nrog sitagliptin thiab ntau zaus ntau dua li ntawm kev kho ua ke nrog placebo: mob taub hau (sitagliptin - 2.4%, placebo - 0.0%), raws plab (1.8 %, 1.1%), xeev siab (1.2%, 1.1%), mob ntshav qab zib (1.2%, 0.0%), ntuav (1.2%, 0.0%).

Ntawm 54 lub lim tiam ntawm kev soj ntsuam:

Kev phiv tshuaj los cuam tshuam nrog kev noj cov tshuaj tau pom nrog ntau zaus & gt1% hauv pawg kho mob nrog sitagliptin thiab ntau zaus ntau dua li kev kho mob sib xyaw nrog cov tshuaj placebo: mob taub hau (sitagliptin - 2.4%, placebo - 0.0%), ntshav qab zib ntshav qab zib (2.4) %, 0.0%), cov kab mob ua pa siab (1.8%, 0.0%), xeev siab (1.2%, 1.1%), hnoos (1.2%, 0.0%), fungal kis ntawm daim tawv nqaij (1.2%, 0.0%), peripheral edema (1.2%, 0.0%), ntuav (1.2%, 0.0%).

Ua ke nrog cov tshuaj insulin:

Hauv 24-lub lis piam placebo-tswj kev kawm txog kev sib xyaw ua ke nrog sitagliptin (hauv ib koob tshuaj 100 mg txhua hnub) thiab cov tshuaj insulin tsis tu ncua (nrog lossis tsis muaj metformin) hauv kev kawm tshuaj pab pawg piv nrog pab pawg ntawm cov neeg mob noj placebo thiab insulin (nrog lossis tsis muaj metformin), tom qab phiv kev tshwm sim:

Cov kev tsis haum tshuaj cuam tshuam nrog kev noj tshuaj tau pom nrog ntau zaus & gt1% hauv pawg kho mob sitagliptin thiab ntau dua li ntau dua pawg pawg kho mob insulin (nrog lossis tsis muaj metformin): hypoglycemia (sitagliptin + insulin (nrog lossis tsis muaj metformin) - 9.6%, placebo + cov tshuaj insulin (nrog lossis tsis muaj metformin) - 5.3%), mob khaub thuas (1.2%, 0.3%), mob taub hau (1.2%, 0.0%).

Lwm qhov kev tshawb nrhiav 24-lub lim tiam, hauv cov neeg mob tau txais sitagliptin ua kev kho ntxiv rau kev kho mob insulin (nrog lossis tsis muaj metformin), tsis muaj qhov tshwm sim tsis zoo uas cuam tshuam nrog kev siv tshuaj nrog rau zaus & gt1% hauv pawg kho mob ntawm sitagliptin (ntawm 100 koob tshuaj ), thiab ntau zaus dua nyob rau hauv pawg placebo.

Hauv qhov kev ntsuam xyuas dav dav ntawm 19 ob lub qhov muag tsis pom kev tshawb nrhiav qhov tseeb ntawm kev siv cov sitagliptin hauv ib koob tshuaj 100 mg txhua hnub los yog cov tshuaj tiv thaiv sib cuam tshuam (nquag lossis cov placebo), qhov tshwm sim ntawm qhov tsis lees paub tseeb txog tus mob pancreatitis yog 0.1 tus neeg ntawm 100 tus neeg mob-xyoo ntawm kev kho mob hauv txhua pawg.

Tsis muaj qhov sib txawv hauv tsev kho mob hauv cov cim tseem ceeb lossis ECG (suav nrog lub sijhawm QTc ntu nruab nrab) tau pom thaum kho nrog sitagliptin.

Kev Tshawb Xyuas Kev Tshawb Xyuas Kev Ntshav Ntshav Hauv Kev Tshawb Fawb (TECOS):

Txoj kev tshawb fawb txog kev mob plawv ntawm sitagliptin (TECOS) suav nrog 7332 cov neeg mob uas siv cov tshuaj sitagliptin 100 mg rau ib hnub (lossis 50 mg rau ib hnub yog tias lub hauv paus kwv yees tus nqi glomerular filtration rate (eGFR) yog & gt30 thiab & lt50 ml / min / 1, 73 m), thiab 7339 cov neeg mob noj cov placebo nyob rau hauv cov pej xeem feem ntau ntawm cov neeg mob uas tau raug tshuaj kho. Txoj kev tshawb no tshuaj (sitagliptin lossis placebo) tau ntxiv rau hauv kev kho mob raws li cov qauv hauv tebchaws uas twb muaj lawm rau kev xaiv cov hom phiaj ntawm HbA1C thiab kev tswj hwm ntawm cov kab mob plawv. Txoj kev tshawb no suav tag nrho ntawm 2004 cov neeg mob hnub nyoog 75 xyoo thiab laus dua (970 coj sitagliptin thiab 1034 coj tshuaj placebo). Cov xwm txheej dav dav muaj qhov tshwm sim tsis zoo hauv cov neeg mob noj sitagliptin yog tib yam li hauv cov neeg mob noj cov placebo. Kev soj ntsuam txog cov teeb meem yav dhau los cuam tshuam nrog cov ntshav qab zib tau qhia tias muaj kev sib piv ntawm qhov tshwm sim tsis zoo ntawm cov pab pawg, suav nrog kev kis mob (18.4% hauv cov neeg mob noj sitagliptin thiab 17.7% hauv cov neeg mob noj cov placebo) thiab lub raum tsis ua haujlwm ( 1.4% hauv cov neeg mob noj cov tshuaj sitagliptin thiab 1.5% hauv cov neeg mob noj cov placebo). Lub profile ntawm cov xwm txheej tsis zoo hauv cov neeg mob hnub nyoog 75 xyoo thiab laus dua feem ntau zoo ib yam li cov neeg ntawd.

Hauv cov pej xeem ntawm cov neeg mob uas tau kho mob ("kev npaj siab-rau-kho"), ntawm cov neeg uas tau txais kev kho mob insulin thiab / los yog sulfonylureas, qhov tshwm sim ntawm kev mob ntshav qab zib tsawg kawg yog 2.7% hauv cov neeg mob noj sitagliptin, thiab 2, 5% hauv cov neeg mob noj cov placebo. Ntawm cov neeg mob uas tsis tau txhaj tshuaj insulin thiab / los yog sulfonylurea, qhov teeb meem ntawm lub qog ntshav qab zib hnyav yog 1.0% rau cov neeg mob noj cov tshuaj sitagliptin thiab 0.7% hauv cov neeg mob noj cov placebo. Qhov tshwm sim ntawm cov mob pancreatitis-paub tseeb yog 0.3% hauv cov neeg mob noj sitagliptin thiab 0.2% hauv cov neeg mob noj cov placebo. Qhov tshwm sim ntawm cov neeg mob qog hais tias mob cancer ntawm neoplasms yog 3.7% hauv cov neeg mob noj sitagliptin thiab 4.0% hauv cov neeg mob noj cov placebo.

Thaum lub sijhawm sau npe tom qab kuaj xyuas kev siv cov sitagliptin hauv kev kho mob monotherapy thiab / lossis kev sib txuam nrog kev kho mob nrog lwm tus neeg hypoglycemic, ntxiv cov kev tshwm sim tsis zoo tau pom. Vim tias cov ntaub ntawv no tau txais zoo los ntawm cov pejxeem uas tsis muaj qhov loj me, qhov ntau zaus thiab kev sib raug zoo nrog kev kho ntawm cov xwm txheej tsis zoo no tsis tuaj yeem txiav txim siab. Cov no suav nrog:

Cov tshuaj tiv thaiv kev tsis haum tshuaj, nrog rau kev mob siab, mob hlwb, pob khaus, urticaria, tawv nqaij vasculitis, ua kom mob tawv nqaij, nrog rau mob Stevens-Johnson mob, mob txha cajqaum, suav nrog cov mob hemorrhagic thiab necrotic nrog rau kev ua kom tuag taus thiab tsis mob, ua rau lub raum tsis ua haujlwm, nrog rau lub raum tsis ua haujlwm kev tsis txaus (qee qhov raug tso ntshav qee zaus yuav tsum tau), mob ua pa ntawm lub caj pas, nasopharyngitis, cem quav, ntuav, mob taub hau, mob caj dab, mob myalgia, nqua, mob nraub qaum, khaus, pemphigoid.

Hloov cov ntsuas ntsuas:

Cov zaus sib txawv ntawm kev kuaj ntsuas hauv pawg kho mob ntawm sitagliptin (hauv koob tshuaj 100 mg txhua hnub) tau muab piv nrog cov zaus hauv cov placebo pawg. Feem ntau, tab sis tsis yog txhua qhov kev sim tshuaj, muaj qhov nce ntawm leukocyte suav (kwv yees 200 / comparedl piv nrog cov placebo, cov ntsiab lus nruab nrab thaum pib kho yog 6600 / )l), vim tias nce neutrophils ntau.

Kev tsom xam ntawm cov ntaub ntawv tshawb fawb soj ntsuam ntawm cov tshuaj pom tias muaj zog me ntsis ntawm cov tshuaj uric acid (kwv yees 0.2 mg / dl piv rau cov placebo, qhov nruab nrab concentration ua ntej kev kho mob yog 5-5.5 mg / dl) hauv cov neeg mob tau txais sitagliptin ntawm koob tshuaj 100 thiab 200 mg hnub. Tsis muaj cov kev tshwm sim ntawm gout. Muaj qhov txo qis me ntsis hauv kev saib xyuas ntawm tag nrho cov alkaline phosphatase (kwv yees li 5 IU / L piv nrog cov placebo, qhov nruab nrab concentration ua ntej kev kho mob yog 56-62 IU / L), qee feem cuam tshuam nrog me ntsis ntawm cov pob txha feem ntawm alkaline phosphatase.

Cov pauv hloov hauv chav ntsuas tsis pom tias yog tseem ceeb hauv chaw kho mob.

Hauv kev tshawb fawb txog kev cuam tshuam nrog lwm cov tshuaj, sitagliptin tsis muaj kev cuam tshuam loj rau lub pharmacokinetics ntawm cov tshuaj hauv qab no: metformin, rosiglitazone, glibenclamide, simvastatin, warfarin, qhov ncauj tawm tsam. Raws li cov ntaub ntawv no, sitagliptin tsis inhibit CYP3A4, 2C8, lossis 2C9 isoenzymes. Raws li cov ntaub ntawv hauv vitro, sitagliptin kuj tseem tsis tiv thaiv CYP2D6, 1A2, 2C19 thiab 2B6 isoenzymes thiab tsis ntxias CYP3A4 isoenzyme. Kev rov ua dua ntawm cov tshuaj metformin hauv kev sib xyaw nrog sitagliptin tsis cuam tshuam qhov pharmacokinetic ntau ntawm sitagliptin hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus.

Raws li cov pej xeem pharmacokinetic tsom xam ntawm cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, kev kho mob concomitant tsis muaj kev cuam tshuam loj hauv kev kho mob ntawm pharmacokinetics ntawm sitagliptin. Txoj kev tshawb nrhiav tau soj ntsuam ntau yam tshuaj uas feem ntau siv los ntawm cov neeg mob uas muaj tus mob ntshav qab zib hom 2, nrog rau: cov tshuaj lipid-txo qis (statins, fibrates, ezetimibe), tshuaj antiplatelet (clopidogrel), tshuaj tiv thaiv kab mob ntshav (ACE inhibitors, angiotensin II receptor antagonists, beta-blockers, blockers) Cov kab mob "qeeb" calcium, hydrochlorothiazide), cov tshuaj tiv thaiv tsis muaj tshuaj steroidal (naproxen, diclofenac, celecoxib), antidepressants (bupropion, fluoxetine, sertraline), antihistamines (cetiri zine), proton twj tso kua mis inhibitors (omeprazole, lansoprazole) thiab tshuaj rau kev kho mob erectile kawg (sildenafil).

Muaj kev nce me ntsis hauv AUC (11%), ntxiv rau qhov nruab nrab Cmax (18%) ntawm digoxin thaum sib xyaw nrog sitagliptin. Qhov nce no tsis yog qhov tseem ceeb hauv tsev kho mob. Nws tsis pom zoo kom hloov cov koob tshuaj ntawm digoxin lossis sitagliptin thaum siv ua ke.

Kev nce ntawm AUC thiab Cmax ntawm sitagliptin tau sau tseg los ntawm 29% thiab 68%, feem ntau, hauv cov neeg mob nrog kev siv sib xyaw ntawm ib leeg qhov ncauj ntawm 100 mg ntawm sitagliptin thiab ib qho ncauj ntawm 600 mg ntawm cyclosporin, lub zog ua kom muaj zog ntawm p-glycoprotein. Cov kev pauv hloov uas pom muaj hauv cov qauv pharmacokinetic ntawm sitagliptin tsis suav tias yog kev kho mob tseem ceeb. Hloov cov koob tshuaj ntawm Xelevia tsis pom zoo thaum sib xyaw nrog cyclosporine thiab lwm yam p-glycoprotein inhibitors (e.g. ketoconazole).

Ib tug pej xeem-based pharmacokinetic tsom xam ntawm cov neeg mob thiab cov neeg ua haujlwm noj qab haus huv (N = 858) rau ntau yam tshuaj tsis sib haum (N = 83, kwv yees li ib nrab ntawm cov uas tau tawm los ntawm lub raum) tsis qhia txog qhov kev cuam tshuam los ntawm cov tshuaj no rau hauv pharmacokinetics ntawm sitagliptin.

Xelevia ntau npaum

Cov koob tshuaj pom zoo ntawm Xelevia yog 100 mg ib hnub ib zaug li qhov ncauj li tshuaj tua kab mob, lossis hauv kev sib xyaw nrog metformin, lossis sulfonylurea derivatives, lossis PPAR-γ agonists (thiazolidinediones), lossis insulin (nrog lossis tsis muaj metformin), lossis kev sib xyaw nrog metformin thiab ib qho sulfonylurea derivative, los yog metformin thiab PPAR-γ agonists.

Xelevia noj tau yam tsis xav noj dab tsi. Kev noj tshuaj ntawm cov tshuaj metformin, sulfonylurea derivatives thiab PPAR-γ agonists yuav tsum xaiv raws li kev pom zoo koob tshuaj rau cov tshuaj no.

Thaum muab cov Xelevia nrog sulfonylurea derivatives los yog nrog insulin, nws raug nquahu kom txo qis cov tshuaj ib txwm pom zoo ntawm sulfonylurea lossis insulin derivative txhawm rau txo cov kev pheej hmoo ntawm kev tsim muaj sulfone-ntxias los yog insulin-hob hypoglycemia.

Yog tias tus neeg mob tsis nco qab noj cov tshuaj Xelevia, cov tshuaj yuav tsum ua kom sai li sai tau tom qab tus neeg mob nco qab txog cov tshuaj uas ploj lawm.

Nws tsis tuaj yeem lees txais rau xoom tshuaj ob zaug ntawm Xelevia nyob rau tib hnub.

Cov neeg mob raum tsis ua haujlwm:

Cov neeg mob uas tsis tshua muaj lub raum tsis txaus (creatinine tshem tawm (CC) & gt50 ml / min, kwv yees sib luag rau qhov kev tsim kom muaj cov tshuaj loog ntawm & lt1.7 mg / dl hauv cov txiv neej thiab & lt1.5 mg / dl hauv cov poj niam) tsis xav tau kev kho kom haum ntawm Xelevia.

Vim tias qhov xav tau kho qhov tshuaj ntawm cov tshuaj sitagliptin hauv cov neeg mob uas tsis tshua txaus rau lub raum tsis txaus, kev siv Xelevia tsis tau muaj nyob hauv pawg no ntawm cov neeg mob (qhov tsis muaj kev pheej hmoo ntawm ib ntsiav tshuaj 100 mg thiab qhov tsis muaj 25 mg thiab 50 mg koob tshuaj tsis pub rau nws cov tshuaj ntau dua hauv cov neeg mob raum. tsis muaj txhij txhua ntawm muaj mob nrab thiab mob hnyav).

Vim yog qhov xav tau hloov tshuaj, nws raug nquahu kom cov neeg mob lub raum tsis ua haujlwm ntsuam xyuas lub raum ua ntej pib kho nrog sitagliptin thiab tsis tseg thaum kho.

Cov neeg mob mob siab tsis ua haujlwm:

Tsis tas yuav hno tshuaj ntawm Xelevia hauv cov neeg mob uas tsis tshua mob me me mus rau mob siab rau hepatic. Cov tshuaj tsis tau kawm hauv cov neeg mob uas muaj lub siab ua haujlwm tsis zoo.

Cov neeg laus cov neeg mob yuav tsum tsis txhob txhaj tshuaj Xelevia.

Thaum lub sijhawm sim kho mob hauv cov neeg tuaj yeem pab dawb noj qab haus huv, ib koob tshuaj 800 mg ntawm sitagliptin feem ntau pom zoo ua tau zoo. Tsawg hloov me me hauv QTc luv, tsis suav tias yog kev kho mob tseem ceeb, tau pom nyob hauv ib txoj kev tshawb fawb ntawm sitagliptin ntawm koob tshuaj 800 mg rau ib hnub. Qhov koob tshuaj ntau tshaj 800 mg toj ib hnub hauv tib neeg tsis tau kawm.

Hauv thawj theem ntawm kev sim tshuaj, ntau koob tshuaj ntawm kev tsis haum tshuaj nrog kev kho nrog sitagliptin tsis tau pom thaum noj cov tshuaj hauv ib hnub ib zaug txog li 400 mg rau 28 hnub.

Yog tias muaj kev noj ntau dhau, nws yog ib qho tsim nyog yuav tsum pib ua tus qauv kev txhawb nqa: tshem tawm cov tshuaj tsis tuaj yeem los ntawm lub plab zom mov, soj ntsuam cov cim tseem ceeb, suav nrog ECG, nrog rau kev teem caij kho kev kho mob, yog tias tsim nyog.

Sitagliptin tsis zoo lim ntshav. Hauv cov kev tshawb fawb soj ntsuam, tsuas yog 13.5% ntawm cov koob tshuaj tau raug tshem tawm ntawm lub cev thaum lub sijhawm 3-4 teev lim piam ua haujlwm. Kev lim ntshav ntev yuav tsim tawm yog tsim nyog. Tsis muaj pov thawj qhia txog kev ua haujlwm ntawm peritoneal dialysis rau sitagliptin.

Lub ntsiab txoj kev ntawm kev zam ntawm sitagliptin los ntawm lub cev yog kev tsim kho raum. Yuav kom ua tiav cov ntshav plasma ntau xws li nyob hauv cov neeg mob uas muaj lub cev tsis ua haujlwm zoo ntawm lub raum, cov neeg mob uas tsis tshua mob raum mus rau lub raum tsis txaus, nrog rau cov neeg mob uas mob raum tsis ua haujlwm sai uas yuav tsum tau mob hemodialysis lossis peritoneal lim ntshav, yuav tsum tau txhaj tshuaj kho Xelevia. Cov.

Muaj cov ntaub ntawv tshaj tawm txog kev txhim kho ntawm tus mob ua paug, nrog rau hemorrhagic lossis necrotic nrog rau kev ua rau neeg tuag taus thiab tsis ua rau tuag taus, hauv cov neeg mob noj sitagliptin. Cov neeg mob yuav tsum tau qhia txog cov yam ntxwv ntawm tus yam ntxwv ntawm tus mob pancreatitis: mob hnyav, mob plab heev. Soj ntsuam qhov tseeb ntawm pancreatitis ploj tom qab tsis mus kev ntawm sitagliptin. Yog hais tias xav tias tsam tus mob pancreatitis, nws yog ib qho tsim nyog yuav tsum tsis txhob noj Xelevia thiab lwm yam tshuaj muaj feem txaus ntshai.

Raws li kev soj ntsuam kev sim ntawm sitagliptin, qhov tshwm sim ntawm kev mob ntshav qab zib thaum lub sij hawm monotherapy lossis kev sib txuas ua ke nrog cov tshuaj uas tsis ua rau cov ntshav qog ntshav (metformin, pioglitazone) tau piv nrog qhov tshwm sim ntawm hypoglycemia hauv pawg placebo. Ib yam li nrog lwm cov tshuaj tiv thaiv ntshav qab zib, hypoglycemia tau pom nrog sitagliptin hauv kev sib xyaw nrog insulin lossis sulfonylurea derivatives. Txhawm rau kom txo qis kev pheej hmoo ntawm kev tsim muaj sulfone-hleem hypoglycemia, qhov koob tshuaj sulfonylurea derivative yuav tsum raug txo kom tsawg.

Siv rau cov neeg laus:

Hauv cov kev tshawb fawb soj ntsuam, qhov ua tau zoo thiab kev nyab xeeb ntawm sitagliptin rau cov neeg mob laus (? 65 xyoo, 409 tus neeg mob) piv rau cov neeg mob uas muaj hnub nyoog qis dua 65 xyoos. Koob tshuaj hloov raws li cov hnub nyoog tsis muaj qhov xav tau. Cov neeg laus yog cov neeg lub raum tsis zoo. Raws li, ib yam li lwm pab pawg hnub nyoog, yuav tau kho kom haum cov neeg mob lub raum tsis ua hauj lwm zoo.

Kev Tshawb Xyuas Kev Tshawb Xyuas Kev Ntshav Ntshav Hauv Kev Tshawb Fawb (TECOS):

Tso tawm daim ntawv, muaj pes tsawg leeg thiab ntim khoom

Nws yog tsim nyob rau hauv daim ntawv ntawm beige, biconvex ntsiav tshuaj nyob rau hauv zaj duab xis txheej. Muaj pes tsawg leeg:

sitagliptin phosphate monohydrate (100 mg sitagliptin),
calcium hydrogen phosphate tsis muaj,
microcrystalline cellulose,
sodium stearyl fumarate
croscarmellose sodium,
magnesium stearate.

14 ntsiav tshuaj yog pob nyob rau hauv lub hlwv (2 nyob rau hauv lub thawv.

Yeeb tshuaj sib cuam tshuam

Tsis muaj kev cuam tshuam loj hauv lwm qhov chaw kho mob los ntawm lwm tus neeg sawv cev ntawm cov txiaj ntsig ntawm Xelevia tau pom. Yog li no, cov xwm txheej no tsis tas yuav muaj kev hloov pauv hauv lawv cov ntau npaum. Qhov zam tshwj xeeb yog sulfonylurea thiab tshuaj insulin.

Sitagliptin tsis cuam tshuam rau cov txiaj ntsig ntawm kev siv tshuaj ntxiv. Tsis muaj kev cuam tshuam loj heev nyob rau hauv cov txheej txheem ntawm kev sib txuas ua ke nrog lwm tus neeg sawv cev.

Txawm li cas los xij, kom tsis txhob muaj kev phom sij txog kev noj qab haus huv, thaum sau tshuaj kho mob, cov kws tshwj xeeb yuav tsum paub txog qhov tseeb ntawm kev noj lwm yam tshuaj.

Cov lus qhia tshwj xeeb

Txhawm rau kom tsis txhob muaj qog ntshav qab zib, nws raug nquahu kom txo qis cov tshuaj noj rau lwm qhov kev tiv thaiv kabmob hypoglycemic hauv kev sib koom tes kho.

Nws yog ib qho tseem ceeb rau cov neeg laus dua 65 xyoos los saib xyuas cov mob ntawm ob lub raum, vim tias qhov khoom no ua rau muaj kev cuam tshuam ntau. Cov neeg mob zoo li no muaj feem ntau yuav tsum muaj ntshav qab zib tsawg lub sijhawm kho nrog lwm cov tshuaj zoo sib xws.

Tsis muaj dab tsi cuam tshuam rau ntawm cov hlab plawv cov ntshav.

Cov tshuaj nquag nws tus kheej tsis cuam tshuam rau lub peev xwm tsav lub tshuab lossis ua haujlwm nrog cov tshuab. Txawm li cas los xij, hauv kev sib txuam ua ke, qhov kev mob tshwm sim no muaj ntau heev. Yog li no, hauv qhov no, nws zoo dua rau kev tso tseg kev tsav tsheb.

Nws yog tso rau cov tshuaj noj!

Piv nrog analogues

Januvius. Ib qho tshuaj raws li sitagliptin. Ua cov tuam txhab "Merck Sharp", lub Netherlands. Tus nqi rau kev ntim khoom yuav yog 1600 rubles thiab siab dua. Qhov kev nqis tes ua los ntawm cov cuab yeej zoo ib yam li Xelevia. Qhov no yog ib qho zuj zus ntxiv, uas cuam tshuam rau cov ntshav qab zib thiab txuas ntxiv qhov ua kom qab los ntawm cov ntshav qab zib. Yog li, nws tau nquag muaj rau cov neeg muaj rog rog raws li kev mob tshwm sim. Ntawm cov minuses - tus nqi. Qhov no yog ua tiav analogue.

Yasitara. Cov ntsiav tshuaj nrog sitagliptin hauv qhov muaj pes tsawg leeg. Cov chaw tsim khoom yog Pharmasintez, Russia. Raug tshuaj analogue ntawm cov tshuaj, uas muaj ib qho zoo sib xws thiab kev teeb tsa ntawm contraindications.Tus nqi rau tus nqi no. Nws yooj yim dua rau kev muab tshuaj kho, vim nws muaj peb qhov ntau thiab tsawg ntawm cov khoom sib txuam - 25, 50 thiab 100 mg ntawm sitagliptin. Txawm li cas los txwv tsis pub rau cov poj niam cev xeeb tub thiab cov menyuam yaus. Ntawm cov minuses - feem ntau ua rau cov ntshav qis.

Vipidia. Nws kuj yog ib qho incretin mimetic, tab sis muaj apogliptin. Muaj nyob hauv daim ntawv ntawm cov ntsiav tshuaj ntawm 12.5 thiab 25 mg. Nqe - los ntawm 800 txog 1150 rubles, nyob ntawm seb ntau npaum li cas. Tsim los ntawm Takeda GmbH, Nyiv. Nws qhov kev txiav txim yog qhov zoo sib xws, tab sis muaj txiaj ntsig zoo dua. Tsis txhob xaj rau cov menyuam yaus thiab cov pojniam xeeb tub vim tias tsis muaj cov ntaub ntawv tshawb fawb. Cov qauv kev tiv thaiv kab mob thiab daim ntawv teev cov kev mob tshwm sim.

Ua tub rog. Canagliflozin raws li cov ntsiav tshuaj. Ua cov tuam txhab Italian Janssen-Silag. Tus nqi nce siab: ntawm 2600 rubles rau 100 daim. Nws yog siv rau hauv kev kho mob ntshav qab zib nrog kev tsis muaj txiaj ntsig ntawm metformin thiab kev noj haus. Txawm li cas los xij, txoj kev kho yuav tsum yog sib xyaw nrog txoj kev noj haus uas xaiv los ntawm kws kho mob. Cov tshuaj tiv thaiv yog tus qauv.

Galvus Met. Qhov no yog qhov sib xyaw daws rau cov ntshav qab zib, thaum cov txiaj ntsig ntawm ib qho quav lawm tsis tau zoo txaus. Sau ua ke ntawm metformin thiab vildagliptin. Cov ntsiav tshuaj yog tsim los ntawm lub tuam txhab Swiss Novartis. Nqe - los ntawm 1500 rubles thiab sab saud. Cov nyhuv ntev, ntev li 24 teev. Nws tuaj yeem siv tsis tau los kho menyuam yaus, cev xeeb tub thiab poj niam menyuam yaus. Hauv cov laus, nws yog siv nrog ceev faj. Tsis haum ua ib qho hloov pauv rau cov tshuaj insulin.

Trazenta. Cov tshuaj no muaj cov tshuaj linagliptin, uas tseem yog ib qho inhibitor ntawm DPP-4. Yog li ntawd, nws txoj haujlwm yog zoo li Xelevia. Nws yog qhov zoo dua hauv qhov nws tau tas tsuas yog los ntawm txoj hnyuv, uas yog, kev ntxhov siab tsawg dua yog tsim rau ntawm ob lub raum. Nws tuaj yeem siv nrog lwm cov tshuaj. Kev txwv tsis pub nkag mus yog ib qho zoo ib yam. Tseem muaj ntau phiv. Tus nqi - los ntawm 1500 rubles. Tsim cov tuam txhab "Beringer Ingelheim Pharma" nyob hauv lub teb chaws Yelemees thiab Asmeskas.

Hloov mus rau lwm cov tshuaj tsuas yog ua los ntawm tus kws kho mob nkaus xwb. Kev noj tshuaj rau tus kheej tsis tuaj yeem lees txais!

Feem ntau, cov neeg mob ntshav qab zib hais tau zoo txog cov tshuaj no. Nws cov high efficiency thiab yooj yim ntawm kev txais tos yog sau tseg. Rau qee leej, qhov kev hais daws no tsis haum.

Valery: “Kuv tau coj Galvus, Kuv nyiam nws heev. Tab sis tom qab ntawd lawv tsum tsis muab nws txiaj ntsig rau kuv lub tsev kho mob, thiab tus kws kho mob qhia kuv hloov mus rau Xelevia. Kuv tsis tau pom qhov txawv. Lawv ua hauj lwm hauv kev zoo sib xws, raws li kws kho mob tau piav qhia. Qab zib yog qhov qub, Kuv tsis saib leaps. Lub sijhawm kho, "kev mob tshwm sim" tsis tshwm sim. Kuv txaus siab nrog cov tshuaj no. "

Alla: “Tus kws kho mob kuj tseem ntxiv Xelevia rau cov tshuaj insulin, vim qhov qub tsis dhau los daws cov piam thaj hauv kev coj ua. Tom qab ib lub hlis txo nws cov tshuaj ntau npaum li cas, Kuv pib hnov cov nyhuv rau lub zog. Qhov ntsuas tsis tau dhia, qhov kev ntsuam xyuas tau zoo, nrog rau kev noj qab haus huv txhua lub xeev. Kuv tseem pom tias kuv xav noj tsawg dua. Tus kws kho mob tau piav qhia tias txhua yam tshuaj ntawm hom kev ua no yog ua haujlwm. Zoo, uas yog ib qho ntxiv lawm. "