Mu tizilombo toyambitsa matenda amtundu wa 2, njira zitatu zazikuluzikulu zimasiyanitsidwa:
- Minofu insulin kukana;
- Kusokonezeka kwa kapangidwe ka insulin;
- Kuchuluka kwa shuga kwa chiwindi.
Udindo wakukula kwa nthenda yotsimikizika yotereyi imakhala ndi ma cell a c ndi ma canc. Otsatirawa amatulutsa timadzi tomwe timapangitsa kuti shuga asandulike kukhala mphamvu ya minofu ndi ubongo. Ngati kupangira kwake kumachepa, izi zimakwiyitsa hyperglycemia.
Ma B-cell ndi omwe amapangitsa kuti shuga azikhala ndi glucagon, kuchuluka kwake kumapangitsa kuti zinthu ziziwayika kwambiri m'magazi. Glucagon owonjezera komanso kusowa kwa insulini kumapereka zofunikira pakuchulukana kwa glucose wosagonjetseka m'magazi.
Kuwongolera moyenera matenda a shuga a 2 sikungatheke popanda kukhazikika komanso kwanthawi yayitali (kwanthawi yonse ya matendawa) kuwongolera kwa metabolism ya carbohydrate. Mayesero ambiri apadziko lonse lapansi amatsimikizira kuti shuga yokhayo yomwe imapereka ndi njira zopewera zovuta komanso kuwonjezera nthawi yodwala matenda ashuga.
Ngakhale ali ndi mitundu yosiyanasiyana ya mankhwala antidiabetic, si odwala onse omwe amakwanitsa kulipira chakudya chokwanira cha carbohydrate ndi thandizo lawo. Malinga ndi kafukufuku wanthawi zonse wa UKPDS, 45% ya anthu odwala matenda ashuga alandila chindapusa 100% popewa kuyambitsidwa kwa microangiopathy patatha zaka zitatu, ndipo 30% yokha itatha zaka 6.
Mavuto awa amawonetsa kufunika kokhala ndi mtundu watsopano wamankhwala omwe sangathandizire kuthetsa mavuto a metabolic, komanso kusunga kapamba, zomwe zimapangitsa kuti thupi likhale ndi kayendedwe ka insulin komanso glycemia.
Mankhwala amtundu wa incretin omwe amatha kuthana ndi matenda a shuga a 2 popanda kukondoweza, kusintha kwadzidzidzi kwa glycemia, chiopsezo cha hypoglycemia ndizatsopano zomwe apanga madokotala.
The inhibitor ya enzyme GLP-4 Sitagliptin imathandizira wodwala matenda ashuga kuthana ndi chilakolako cha thupi ndi kulimbitsa thupi, kupatsa thupi mwayi wodziimira pawokha pothana ndi vuto la kuchuluka kwa shuga.
Kutulutsa mawonekedwe ndi kapangidwe kake
Mankhwala omwe amachokera ku sitagliptin okhala ndi dzina la malonda a Januvia amapangidwa ngati mapiritsi ozungulira ndi pinki kapena beige hue ndipo amalembedwa "227" pa 100 mg, "112" pa 50 mg, "221" pa 25 mg. Mapiritsiwo amadzaza m'mabokosi apulasitiki kapena pensulo. Pakhoza kukhala ma mbale angapo m'bokosi.
Pulogalamu yogwira yogwira ya sitagliptin phosphate hydrate imaphatikizidwa ndi croscarmellose sodium, magnesium stearate, cellulose, sodium stearyl fumarate, chosakwaniritsidwa cha calcium hydrogen phosphate.
Kwa sildagliptin, mtengo umadalira ma CD, makamaka mapiritsi 28 omwe muyenera kulipira rubles 1,596-1724. Mankhwala othandizira amaperekedwa, moyo wa alumali ndi chaka chimodzi. Mankhwalawa safuna mikhalidwe yapadera kuti asungidwe. Ma CD otseguka amasungidwa pakhomo la firiji kwa mwezi umodzi.
Pharmacology Sitagliptinum
Ma mahomoni amenewa amapangidwa ndi mucosa wamatumbo, ndipo kupanga ma insretin kumawonjezeka ndi mphamvu ya michere. Ngati kuchuluka kwa glucose ndikwabwinobwino komanso kokulirapo, mahomoni amakula mpaka 80% yopanga insulini komanso chinsinsi chake ndi maselo a β-cell chifukwa cha ma signature a ma cell mu ma cell. GLP-1 amalepheretsa katulutsidwe wambiri wa timadzi ta glucagon ndi ma cell a B.
Kuchepa kwa kuchuluka kwa glucagon poyang'ana kumbuyo kwa kuchuluka kwa insulini kumatsimikizira kuchepetsedwa kwa katulutsidwe ka shuga mu chiwindi. Njira izi ndikuwonetsetsa kuti glycemia ikhale yofanana. Zochita za ma insretins zimachepetsedwa ndi mtundu wina wazamoyo, makamaka ndi hypoglycemia, sizimakhudza kaphatikizidwe ka glucagon ndi insulin.
Pogwiritsa ntchito DPP-4, ma insretins ndi hydrolyzed kuti apange ma inert metabolites. Polekerera zomwe zimachitika mu enzyme iyi, sitagliptin imachulukitsa zomwe zili ndi ma insretin ndi insulin, zimachepetsa kupanga glucagon.
Ndi hyperglycemia, chimodzi mwazizindikiro zazikulu za matenda amitundu iwiri, njira iyi yothandizira imachepetsa kuchepa kwa hemoglobin wa glycated, shuga wanjala ndi glucose pambuyo ponyamula katundu. Mlingo umodzi wa sitagliptin umatha kuletsa kugwira ntchito kwa DPP-4 kwa tsiku, ndikuwonjezera kuchuluka kwa ma insretin m'magazi ndi katatu.
Pharmacokinetics a sitagliptin
Kuyamwa kwa mankhwalawa kumachitika msanga, ndi bioavailability wa 87%. Kuchuluka kwa mayamwa sikudalira nthawi yakudya komanso kapangidwe kake ka chakudya, makamaka, zakudya zamafuta sizisintha magawo a pharmacokinetic magawo a incretin mimetic.
Pofanana, kugwiritsa ntchito piritsi la 100 mg kumachulukitsa dera lomwe lili pansi pa AUC pamapindikira, komwe kumakhala kofanana ndi kudalirana kwa magawo nthawi, ndi 14%. Mlingo umodzi wa mapiritsi a 100 mg umatsimikizira kuchuluka kwa magawo a 198 l.
Gawo laling'ono la incretin mimetic limapangidwa. Ma metabolites 6 adadziwika kuti alibe luso lolepheretsa DPP-4. Chilolezo cha Renal (QC) - 350 ml / min. Gawo lalikulu la mankhwalawo limachotsedwa ndi impso (79% mu mawonekedwe osasinthika ndi 13% mu mawonekedwe a metabolites), ena onse amatsitsidwa ndi matumbo.
Poona kulemera kwakukulu kwa impso mu odwala matenda ashuga omwe ali ndi mawonekedwe osakhazikika (CC - 50-80 ml / min.), Zizindikiro ndizofanana, ndi CC 30-50 ml / min. kuphatikiza kwapawiri kwa mfundo za AUC kumawonedwa, ndi CC pansi 30 ml / min. - kanayi. Zinthu zoterezi zimapereka lingaliro lokonzekera.
Ndi hepatic pathologies ya zolimbitsa zolimbitsa, Cmax ndi AUC kuchuluka ndi 13% ndi 21%. Mitundu yayikulu, ma pharmacokinetics a sitagliptin sasintha kwambiri, chifukwa mankhwalawa amachotsedwa ndi impso.
Ndani akuwonetsedwa incretinomimetic
Mankhwalawa amalembera mtundu wa matenda a shuga a 2 kuwonjezera pa zakudya zamafuta ochepa komanso minyewa yokwanira.
Amagwiritsidwa ntchito ngati mankhwala amodzi komanso mankhwala ophatikizidwa ndi metformin, sulfonylurea kukonzekera kapena thiazolidinediones. Ndikothekanso kugwiritsa ntchito ma reginens a insulin ngati njirayi ikuthandizira kuthana ndi vuto la insulin.
Contraindication ya sitagliptin
Osakupatsani mankhwala:
Ndi chidwi chapamwamba chamunthu;- Anthu odwala matenda ashuga omwe ali ndi matenda amtundu 1;
- Amayi oyembekezera komanso oyamwitsa;
- Mu matenda a diabetes ketoacidosis;
- Kwa ana.
Ndi chidwi chapamwamba chamunthu;Anthu odwala matenda ashuga omwe ali ndi mawonekedwe a aimpso amafunikira chisamaliro chapadera.
Momwe angatenge
Kwa sitagliptin, malangizo omwe angagwiritsidwe ntchito amalimbikitsa kumwa mankhwalawa musanadye. Mlingo wofanana ndiwofanana ndi mtundu uliwonse wa mankhwala - 100 mg / tsiku. Ngati dongosolo la kuvomerezedwa lathyoledwa, piritsi liyenera kumamwa nthawi iliyonse, kuwirikiza kawiri mlingo sikovomerezeka.
Zochitika Zosiyanasiyana
Poyerekeza ndi ndemanga, ambiri a odwala matenda ashuga onse amakhala ndi nkhawa chifukwa cha kukomoka, kukhumudwa. Mu mayeso a labotale, hyperuricemia, kuchepa kwa mphamvu ya chithokomiro, komanso leukocytosis amadziwika.
Zina mwazinthu zina zomwe sizinachitike (chiyanjano ndi incretin mimetic sichinatsimikizidwe) - matenda opumira, arthralgia, migraine, nasopharyngitis). Zowopsa za hypoglycemia ndizofanana ndi zotsatira za gulu loyang'anira malo.
Kuthandiza ndi bongo
Ngati bongo wambiri, mankhwala osagwiritsidwa ntchito mopitilira muyeso amachotsedwa pamimba, magawo onse ofunikira (kuphatikiza ECG) amayang'aniridwa. Zizindikiro zothandizira komanso zothandizira zimawonetsedwa, kuphatikizapo hemodialysis yokhala ndi mphamvu yayitali (13.5 ya mankhwalawa amachotsedwa mu maola 3-4).
Zotsatira Zogwiritsa Ntchito Mankhwala
Ndi munthawi yomweyo kugwiritsa ntchito sitagliptin ndi metformin, rosiglitazone, kulera pakamwa, glibenclamide, warfarin, simvastatin, pharmacokinetics yamagulu awa a mankhwalawa sasintha.
Yomwe imayendetsedwa ndi sitagliptin ndi digoxin sizitanthauza kusintha kwa mankhwalawa. Malangizo ofanana amaperekedwa ndi malangizo komanso mogwirizana ndi sitagliptin ndi cyclosporin, ketoconazole.
Sildagliptin - analogues
Sitagliptin ndi dzina lapadziko lonse la mankhwalawa; dzina lake la malonda ndi Januvius. Analogue imatha kuganiziridwa ngati mankhwala a Yanumet ophatikizidwa, omwe amaphatikizapo sitagliptin ndi metformin. Galvus ndi m'gulu la DPP-4 inhibitors (Novartis Pharma AG, Switzerland) yokhala ndi gawo la vildagliptin, mtengo 800 rubles.
Mankhwala a Hypoglycemic ndiwofunikanso pa code ya ATX ya mulingo 4:
- Nesina (Takeda Pharmaceuticals, USA, kutengera alogliptin);
- Onglisa (Bristol-Myers squibb Company, kutengera saxagliptin, mtengo - 1800 rubles);
- Trazhenta (Bristol-Myers squibb Company, Italy, Britain, ndi yogwira mankhwala linagliptin), mtengo - 1700 rubles.
Mankhwalawa ophatikizidwa sakuphatikizidwa pamndandanda wamankhwala okondera; kodi nkoyenera kuyesa pachiwopsezo chanu ndikuwopseza bajeti ndi thanzi lanu?
Sitagliptin - ndemanga
Poyerekeza ndi malipoti pamisonkhano yamatenda, Januvius nthawi zambiri amalembedwa kuti azikhala ndi matenda ashuga koyambirira kwa matendawa. About sitagliptin, kuwunika kwa madokotala ndi odwala kukuwonetsa kuti kugwiritsa ntchito incretinomimetic kumakhala ndi malingaliro ambiri.
Januvia ndi mankhwala atsopano ndipo si madokotala onse amene apeza chida chokwanira chogwiritsira ntchito. Mpaka posachedwa, metformin inali mankhwala oyambira; tsopano, Januvia amadziwikanso ngati monotherapy. Ngati kuthekera kwake ndikokwanira, kuonjezerapo ndi metformin ndi mankhwala ena sikofunikira.
Odwala matenda ashuga amadandaula kuti mankhwalawa samakwaniritsa zomwe zanenedwa, pakapita nthawi ntchito yake imachepa. Vuto pano silikuzolowera mapiritsi, koma mikhalidwe ya matendawa: matenda a shuga a 2 ndi njira yokhazikika.
Ndemanga zonse zimabweretsa mawu akuti kuyambitsidwa kwachipatala cha sitagliptin, komwe ndi gulu latsopano lamankhwala, kumapereka mwayi wowongolera matenda amtundu wa 2 shuga nthawi iliyonse, kuyambira prediabetes mpaka mankhwala owonjezera, osakhala ndi zotsatira zosagwirizana ndi njira zoperekera chipukutiro chachikhalidwe.
Nkhani ya Pulofesa A.S. Ametov, endocrinologist-diabetesologist ponena za chiphunzitso ndi chizolowezi chogwiritsa ntchito sitagliptin - pa kanema.
