SITAGLIPTIN - COV LUS QHIA RAU KEV SIV, NQE, XYUAS THIAB ANALOGUES

Send

Hauv pathogenesis ntawm ntshav qab zib hom 2, peb cov txheej txheem tseem ceeb yog qhov txawv:

Ntaub so ntswg insulin kuj;
Kev tsis sib haum hauv kev tsim cov tshuaj insulin endogenous;
Ntau cov synthesis ntawm qabzib los ntawm lub siab.

Lub luag haujlwm rau kev txhim kho ntawm cov kab mob insidious no nyob nrog b thiab c hlwb ntawm lub txiav. Qhov tom kawg kuj tsim cov tshuaj hormone uas txhawb kev hloov pauv ntawm cov piam thaj rau lub zog rau cov leeg thiab lub hlwb. Yog hais tias tus nqi ntawm nws cov khoom lag luam qis qis, qhov no provokes hyperglycemia.

B-cov hlwb yog lub luag haujlwm rau kev tsim cov khoom ntawm glucagon, nws dhau mus tsim kev tsim nyog rau kev zais cia ntau dhau ntawm cov piam thaj los ntawm nplooj siab. Tshaj ntawm glucagon thiab tsis muaj cov tshuaj insulin muab cov zwj ceeb rau kev txuam nrog cov piam thaj hauv kev ntshav.

Kev tswj tau zoo ntawm tus mob ntshav qab zib hom 2 tsis tuaj yeem ua tsis tau yam tsis muaj kev ruaj khov thiab lub sijhawm ntev (rau tag nrho lub sijhawm ntawm tus kabmob) tswj kev noj cov zaub mov carbohydrate. Ntau cov kev sim thoob ntiaj teb lees paub tias tsuas yog nyiaj qab zib thiaj li ua kom muaj kev tiv thaiv ntawm cov teeb meem thiab ua kom lub neej muaj hnub nyoog ntev dua ntawm tus mob ntshav qab zib.

Txawm hais tias tag nrho ntau yam tshuaj tiv thaiv kev tiv thaiv kab mob, tsis yog txhua tus neeg mob tswj kom ua tiav kev them nyiaj ruaj khov ntawm carbohydrates nrog lawv pab. Raws li kev tshawb pom muaj tseeb UKPDS txoj kev tshawb nrhiav, 45% ntawm cov neeg mob ntshav qab zib tau txais 100% kev them nyiaj rau kev tiv thaiv microangiopathy tom qab 3 xyoos, thiab tsuas yog 30% tom qab 6 xyoo.

Cov teeb meem no sau qhov kev xav tau los tsim kho cov kev kawm tshiab ntawm cov tshuaj uas yuav tsis tsuas yog pab tshem tawm cov teeb meem metabolic, tab sis kuj tswj cov txiav, ua kom lub cev muaj zog los tswj cov tshuaj insulin ntau lawm thiab glycemia.

Cov tshuaj ntau ntxiv uas tuaj yeem tswj hwm tus mob ntshav qab zib hom 2 yam tsis muaj kev ua rau lub siab, kev hloov pauv sai ntawm glycemia, qhov kev pheej hmoo ntawm hypoglycemia yog qhov kev tsim tawm tshiab los ntawm cov kws tshuaj.

Lub inhibitor ntawm cov enzyme GLP-4 Sitagliptin pab cov neeg mob ntshav qab zib kom tswj tau lub siab thiab lub cev qhov hnyav, muab lub cev kom muaj peev xwm ywj pheej kov yeej qhov teeb meem ntawm cov piam thaj.

Tso tawm daim ntawv thiab muaj pes tsawg leeg

Cov tshuaj raws li sitagliptin nrog lub npe lag luam Januvia yog tsim nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj puag ncig nrog cov xim liab lossis beige hue thiab cim "227" rau 100 mg, "112" rau 50 mg, "221" rau 25 mg. Cov ntsiav tshuaj yog ntim rau hauv lub thawv yas lossis tus cwj mem qhuav. Muaj peev xwm muaj ntau lub phaj ntim hauv ib lub thawv.

Cov khoom ua yeeb yam tseem ceeb sitagliptin phosphate hydrate yog ntxiv nrog croscarmellose sodium, magnesium stearate, cellulose, sodium stearyl fumarate, tsis muaj tshuaj calcium calcium phosphate.

Rau sildagliptin, tus nqi nyob ntawm qhov ntim, tshwj xeeb rau 28 ntsiav tshuaj koj yuav tsum them 1,596-1724 rubles. Daim ntawv muab tshuaj muab rau, cov khoom txee lub neej yog 1 xyoos. Cov tshuaj tsis tas yuav tshwj xeeb rau kev khaws cia. Qhib ntim tau khaws cia rau ntawm lub qhov rooj tub yees rau ib hlis.

Kws tshuaj Sitagliptinum

Sitagliptin txawv ntawm lwm cov tshuaj tiv thaiv kab mob hauv nws cov tshuab ntawm kev ua thiab nws cov qauv. Kev txwv tsis pub muaj peev xwm ntawm DPP-4 enzyme, qhov inhibitor nce cov ntsiab lus ntawm incretins HIP thiab GLP-1, uas tswj cov kua nplaum hauv tsev.

Cov tshuaj hormones no yog tsim tawm los ntawm cov hnyuv hauv plab, thiab ua kom muaj cov nce zuj zus ntxiv nrog rau kev noj zaub mov hauv lub cev. Yog tias cov piam thaj nyob hauv lub cev thiab cov siab dua, cov tshuaj hormones nce ntxiv txog 80% ntawm kev tsim tawm ntawm cov tshuaj insulin thiab nws txoj kev tso tawm los ntawm β-cov hlwb vim muaj cov paib qhia hauv cov hlwb. GLP-1 inhibits qhov kev tso siab zoo ntawm glucagon hormone los ntawm b-hlwb.

Qhov kev txo qis hauv glucagon cov ntsiab lus tawm tsam tom qab ntawm qhov nce ntawm insulin ntau yuav ua rau muaj kev txo cov ntshav qabzib tawm hauv lub siab. Cov txheej txheem no thiab ua kom paub tseeb tias qhov muaj teeb meem ntawm glycemia. Cov kev ua ntawm incretins raug txwv los ntawm qee yam keeb kwm ntawm physiological, tshwj xeeb nrog hypoglycemia, lawv tsis cuam tshuam rau cov synthesis ntawm glucagon thiab insulin.

Siv DPP-4, cov incretins yog hydrolyzed los ua inert metabolites. Txhawb nqa kev ua haujlwm ntawm cov enzyme no, sitagliptin tsub kom cov ntsiab lus ntawm incretins thiab insulin, txo cov khoom ntawm glucagon.

Nrog hyperglycemia, ib qho ntawm cov cim tseem ceeb ntawm cov ntshav qab zib hom 2, qhov kev ua haujlwm ntawm kev ua no yuav pab txo qis qib glycated hemoglobin, suab thaj tshaib plab thiab qabzib tom qab muaj cov teeb meem carbohydrate. Ib koob tshuaj sitagliptin tuaj yeem thaiv kev ua haujlwm ntawm DPP-4 rau ib hnub, nce kev ncig ntawm cov khoom ntxiv nyob rau hauv cov ntshav txaus los ntawm 2-3 zaug.

Pharmacokinetics ntawm sitagliptin

Qhov nqus ntawm cov tshuaj tshwm sim sai sai, nrog kev ntsuas kev noj qab haus huv ntawm 87%. Qhov nqus ntshav tsis yog nyob ntawm lub sijhawm ntawm kev nkag thiab cov khoom noj ntawm cov zaub mov, tshwj xeeb, cov khoom noj muaj roj tsis hloov pauv pharmacokinetic ntawm qhov ua kom ntau ntxiv.

Qhov tshuaj tiv thaiv ncav cuag nws cov qib siab kawg (950 nmol) hauv 1-4 teev .AUC nyob ntawm qhov koob tshuaj, qhov txawv txav ntawm ntau pawg sib txawv ntawm cov ntshav qab zib muaj tsawg.

Hauv kev sib npaug, kev siv ntxiv ntawm 100 mg ntsiav tshuaj tsub kom thaj tsam hauv qab AUC nkhaus, uas yog qhov cim ntawm kev tos ntawm cov khoom faib kom ncav sijhawm, los ntawm 14%. Ib koob tshuaj ntawm 100 mg ntsiav tshuaj tuaj yeem lav qhov muab faib tawm ntawm 198 l.

Ib feem me me ntawm incretin mimetic yog metabolized. 6 metabolites tau qhia tias tsis muaj peev xwm inhibit DPP-4. Kev hlais tawm (QC) - 350 ml / min. Lub ntsiab tseem ceeb ntawm cov tshuaj yog tshem tawm los ntawm lub raum (79% nyob rau hauv daim ntawv tsis hloov pauv thiab 13% hauv daim ntawv tshuaj tiv thaiv kab mob), qhov seem yog dhau los ntawm txoj hnyuv.

Txhawm rau saib xyuas lub nra hnyav rau lub raum hauv cov neeg mob ntshav qab zib nrog daim ntawv ntev (CC - 50-80 ml / min.), Qhov ntsuas yog zoo ib yam, nrog CC 30-50 ml / min. ob npaug ntawm AUC qhov tseem ceeb tau pom, nrog CC hauv qab 30 ml / min. - plaub zaug. Cov xwm txheej zoo li no qhia kom muaj feem kaum koob tshuaj.

Nrog tus kab mob hepatic pathologies ntawm kev mob nyhav ib nrab, Cmax thiab AUC nce li ntawm 13% thiab 21%. Hauv cov ntawv loj, cov pharmacokinetics ntawm sitagliptin tsis hloov pauv ntau, vim tias cov tshuaj feem ntau yog tawm los ntawm lub raum.

Hauv cov neeg mob ntshav qab zib ntawm lub hnub nyoog loj (65-80 xyoo), qhov tsis muaj txiaj ntsig ntawm cov tshuaj ntxiv los ntawm 19%. Xws li qhov tseem ceeb tsis yog qhov tseem ceeb hauv kev kho mob, yog li ntawd kev ua haujlwm txauv ntawm cov cai tsis tas yuav tsum ua.

Leej twg muaj qhia incretinomimetic

Cov tshuaj yog tawm rau cov ntshav qab zib hom 2 ntxiv rau kev noj zaub mov kom tsawg thiab muaj cov leeg ua haujlwm txaus.

Nws yog siv los ua ib qho yeeb tshuaj thiab ua ke nrog kev kho mob nrog metformin, sulfonylurea kev npaj lossis thiazolidinediones. Nws kuj tseem siv tau qhov kev txhaj tshuaj insulin yog tias qhov kev xaiv no pab daws qhov teeb meem ntawm kev tiv thaiv insulin.

Cov tshuaj tiv thaiv rau sitagliptin

Tsis txhob xaj tshuaj rau:

Nrog tus neeg rhiab heev;
Tus mob ntshav qab zib nrog hom 1;
Cev xeeb tub thiab pub mis;
Hauv lub xeev muaj ketoacidosis uas mob ntshav qab zib;
Rau cov me nyuam.

Tus mob ntshav qab zib uas mob ntev li kab mob ntsws raum yuav tsum tau saib xyuas tshwj xeeb.

Yuav noj li cas

Txog sitagliptin, cov lus qhia rau kev siv pom zoo kom haus tshuaj ua ntej noj mov. Cov qauv muab tshuaj yog ib yam rau txhua qhov kev kho mob - 100 mg / hnub. Yog hais tias cov sij hawm ntawm kev pub nkag yog tawg, cov ntsiav tshuaj yuav tsum haus ib lub sijhawm twg, ob zaug koob tshuaj tsis tuaj yeem lees txais.

Nrog CC 30-50 ml / min. qhov pib siv tshuaj yuav yog 2 zaug qis dua - 50 mg / hnub., nrog CC hauv qab 30 ml / min. - 4 zaug - 25 mg / hnub. (ib-zaug). Lub sijhawm ntawm hemodialysis tsis cuam tshuam rau kev kho sitagliptin txoj kev kho kom zoo.

Phiv Txheej Xwm

Kev txiav txim los ntawm kev txheeb xyuas, feem ntau ntawm txhua tus neeg mob ntshav qab zib tau txhawj xeeb txog mob dyspepsia, mob plab. Hauv chav kuaj, hyperuricemia, txo qis kev ua haujlwm ntawm lub qog ua haujlwm lub qog, thiab leukocytosis tau sau tseg.

Ntawm lwm cov teebmeem uas tsis tuaj yeem ua tiav (ib qho sib txuas nrog incretin mimetic tsis tau muaj pov thawj) - ua mob ua pa, mob caj pas, mob pob txha taub hau, mob hlab pas). Qhov xwm txheej ntawm cov ntshav qog ntshav qab zib zoo ib yam li cov txiaj ntsig hauv cov placebo tswj pab pawg.

Pab nrog overdose

Yog tias muaj kev noj ntau dhau, dhau ntawm ib qho tshuaj uas tsis tuaj yeem tshem tawm ntawm txoj hnyuv, txhua qhov tseem ceeb (suav nrog ECG) raug saib xyuas. Cov tsos mob thiab txhawb kev tiv thaiv tau qhia, suav nrog kev kho mob hemodialysis nrog lub peev xwm ntev (13.5 koob tshuaj tau raug tshem tawm hauv 3-4 teev).

Qhia Txog Kev Sib Koom Tes Nrog Tshuaj

Nrog rau kev siv sib npaug ntawm sitagliptin nrog metformin, rosiglitazone, qhov ncauj qhov kev tiv thaiv, glibenclamide, warfarin, simvastatin, lub chaw muag tshuaj ntawm cov tshuaj no tsis hloov.

Concurrent coj ntawm sitagliptin nrog digoxin tsis cuam tshuam qhov hloov pauv ntawm kev noj tshuaj. Cov ntsiab lus zoo ib yam yog muab los ntawm kev qhia thiab ntawm kev cuam tshuam ntawm sitagliptin thiab cyclosporin, ketoconazole.

Sildagliptin - analogues

Sitagliptin yog lub npe tshuaj thoob ntiaj teb rau nws cov yeeb tshuaj; nws lub npe lag luam yog Januvius. Ib qho tshuaj yeeb yaj kiab tuaj yeem suav tau tias yog qhov sib xyaw ua ke tshuaj Yanumet, uas suav nrog sitagliptin thiab metformin. Galvus belongs rau cov pab pawg ntawm DPP-4 inhibitors (Novartis Pharma AG, Switzerland) nrog cov nquag vildagliptin, tus nqi 800 rubles.

Kev siv tshuaj Hypoglycemic tseem tsim nyog rau ATX code ntawm qib 4:

Nesina (Takeda Cov Tshuaj, Tebchaws Asmeskas, raws li alogliptin);
Onglisa (Bristol-Myers Squibb Tuam Txhab, raws li saxagliptin, tus nqi - 1800 rubles);
Trazhenta (Bristol-Myers Squibb Tuam Txhab, Ltalis, Tebchaws Askiv, nrog rau cov khoom muaj txiaj ntsig linagliptin), tus nqi - 1700 rubles.

Cov tshuaj txhaum loj no tsis suav nrog hauv cov tshuaj tshwj xeeb; nws puas tsim nyog sim ntawm koj tus kheej qhov kev pheej hmoo thiab pheej hmoo nrog koj pob nyiaj thiab kev noj qab haus huv?

Sitagliptin - kev txheeb xyuas

Kev txiav txim los ntawm cov lus ceeb toom ntawm cov ntsiab lus sib tham, Januvius feem ntau yog kho rau cov neeg mob ntshav qab zib nyob rau theem pib ntawm tus kab mob. Txog sitagliptin, kev tshuaj xyuas ntawm cov kws kho mob thiab cov neeg mob qhia tias kev siv ntawm incretinomimetic muaj ntau yam nuances.

Januvia yog kev tsim yeeb tshuaj tshiab thiab tsis yog txhua tus kws kho mob tau txais kev paub txaus siv nws. Txog thaum nyuam qhuav, metformin yog thawj cov tshuaj kab; tam sim no, Januvia kuj tseem raug kho raws li kev kho mob monotherapy. Yog tias nws lub peev xwm tau txaus, ntxiv nws nrog metformin thiab lwm yam tshuaj tsis pom zoo.

Tus mob ntshav qab zib yws tias cov tshuaj tsis tas ua raws li cov lus teev tseg, dhau sij hawm nws cov hauj lwm txo qis. Qhov teeb meem ntawm no tsis yog nyob rau hauv tau txais siv rau cov ntsiav tshuaj, tab sis nyob rau hauv cov yam ntxwv ntawm tus kabmob: hom 2 mob ntshav qab zib yog mob ntev, kev vam meej pathology.

Eugene, Lipetsk. Thaum kawg kuv tus kws kho mob tau tawm mus so. Kuv tau saib kuv phau ntawv khaws cov piam thaj, hais txog kab mob kebabs. Qhov tsom xam tau tsis phem, thiab nws tau hais tias kuv hloov Diabeton MV nrog Yanuvia. Kuv tus kws kuaj mob endocrinologist tau ntsib dhau los, nws yeej ceeb toom txog txhua yam khoom tshiab. Dab tsi yog nws kom zoo dua, dua li tus nqi (6 siab dua!), Kuv tseem tsis nkag siab. Kuv haus Januvia lub tshuaj ntsiav rau ib hlis thaum sawv ntxov, 3 ntau dua Siofora 500 thaum nruab hnub. Tsog tsis muaj piam thaj tam sim no tsis tshaj 7 mmol / l, thiab nws sai sai rov qab los rau tom qab noj mov. Sij hawm dhau los, tom qab kev qhia ua kis las hauv chaw dhia ua si, qab zib poob ntau heev. Tam sim no nws ncav cuag qhov kev cai (5.5 mmol / l) thiab maj mam nce siab ntxiv. Hauv nruab nrab, Kuv muaj cov cim zoo sib xws ua ntej, tab sis cov piam thaj hauv qab zib muaj qhov poob qis. Kuv tsis tuaj yeem hais dab tsi txog cov kev mob tshwm sim - Kuv tau siv ib hlis calmly.

Tag nrho cov lus pom ua rau qhov xaus hais tias kev qhia ntawm sitagliptin mus rau kev xyaum siv, uas sawv cev rau cov chav kawm tshiab ntawm cov tshuaj, muab lub sijhawm txaus rau kev tswj cov ntshav qab zib hom 2 ntawm txhua theem, los ntawm kev mob ntshav qab zib mus rau kev kho ntxiv, nrog cov txiaj ntsig tsis txaus ntseeg los ntawm kev siv cov tshuaj kho mob ntawm cov tshuaj kho mob glycemic.

Daim ntawv qhia los ntawm cov xibfwb A.S. Ametov, endocrinologist-diabetologist txog qhov kev xav thiab kev coj ua ntawm siv sitagliptin - hauv video.

Send