Vildagliptin - malangizo, analogi ndi ndemanga za odwala

Ngakhale pali kusankha kwakukulu kwa mankhwala ochepetsa shuga, chida choyenera chogwiritsira ntchito glycemia sichinapezekebe. Vildagliptin ndi imodzi mwamankhwala osokoneza bongo amakono kwambiri. Sikuti imangokhala ndi zoyipa zochepa: sizimapangitsa kuchuluka kwa thupi ndi hypoglycemia, sizimangokhala ntchito za mtima, chiwindi ndi impso, komanso zimakulitsa kuthekera kwa maselo a beta kuti apange insulin.

Vildagliptin ndi chida chomwe chimawonjezera moyo wa ma insretins - mahomoni achilengedwe am'mimba. Malinga ndi madotolo, mankhwalawa amatha kugwiritsidwa ntchito bwino ndi matenda a shuga a nthawi yayitali komanso m'magawo oyamba a matendawa, kuphatikiza ngati gawo la chithandizo chophatikiza.

Momwe vildagliptin idapezeka

Zambiri zokhudzana ndi maretretin zidawoneka zaka zoposa 100 zapitazo, mmbuyo mu 1902. Zinthu zinalekanitsidwa ndi matumbo a nthumbu ndipo zimatchedwa kuti makande. Kenako kuthekera kwawo kolimbikitsa kutulutsa kwa ma enzymes kuchokera ku kapamba ofunikira kugaya chakudya kunapezeka. Zaka zingapo pambuyo pake, panali malingaliro omwe mawonekedwe a minyewa ingakhudzirenso ntchito ya mahomoni. Zinapezeka kuti odwala omwe ali ndi glucosuria, akamamwa mankhwala ampretin, kuchuluka kwa shuga mu mkodzo kumachepa kwambiri, kuchuluka kwa mkodzo kumachepa, ndipo thanzi limayenda bwino.

Mu 1932, mahomoni adakhala ndi dzina lamakono - glucose-insulinotropic polypeptide (HIP). Zinapezeka kuti zimapangidwa m'maselo a mucosa a duodenum ndi jejunum. Pofika 1983, ma peptides awiri ngati glucagon (GLPs) anali atadzipatula. Zinapezeka kuti GLP-1 imayambitsa kutulutsa kwa insulini poyankha kuchuluka kwa shuga, ndipo katulutsidwe kake kamachepetsedwa mu odwala matenda ashuga.

Zochita za GLP-1:

Matenda a shuga ndi kupsinjika kudzakhala chinthu chakale

• Matenda a shuga -95%
• Kuthetsa kwa mitsempha thrombosis - 70%
• Kuthetsa kwa kugunda kwamtima kwamphamvu -90%
• Kuthana ndi kuthamanga kwa magazi - 92%
• Kuwonjezeka kwa mphamvu masana, kukonza kugona usiku -97%

• imalimbikitsa kumasulidwa kwa insulin mwa odwala matenda a shuga;
• imachulukitsa kupezeka kwa chakudya m'mimba;
• amachepetsa kufunika kwa chakudya, amathandizira kuchepetsa thupi;
• imakhudzanso mtima ndi mitsempha ya magazi;
• amachepetsa kupanga glucagon mu kapamba - timadzi timene timafooketsa insulin.

Imagawikana ndi ma enzyme DPP-4, omwe amapezeka pa endothelium ya capillaries yomwe imalowa m'matumbo, chifukwa izi zimatenga mphindi ziwiri.

Kugwiritsa ntchito zamankhwala pazotsatira izi kunayamba mu 1995 ndi kampani yopanga zamankhwala Novartis. Asayansi adatha kudzipatula pazinthu zomwe zimasokoneza ntchito ya enzyme ya DPP-4, ndichifukwa chake njira yamoyo ya GLP-1 ndi HIP inachuluka kangapo, ndipo kuphatikiza kwa insulin kumakulanso. Pulogalamu yoyamba yokhazikika pamapangidwe othandizira omwe amapititsa cheke cha chitetezo chinali vildagliptin. Dzinali lapeza zambiri: apa pali gulu latsopano la hypoglycemic othandizira "glyptin" ndi gawo la dzina la wopanga wake Willhower, komanso chidziwitso chazomwe angathe kugwiritsa ntchito mankhwalawa kuti achepetse glycemia "gly" komanso ngakhale chidule "inde", kapena dipeptidylamino-peptidase, enzyme DPP -4.

Zochita za vildagliptin

Kuyamba kwa nthawi ya ma incretin pothandizira odwala matenda ashuga kumayesedwa ngati chaka cha 2000, pamene mwayi woletsa DPP-4 unawonetsedwa koyamba ku Congress of Endocrinologists. Munthawi yochepa, vildagliptin yatenga malo okhazikika machitidwe a mankhwala othandizira odwala matenda a shuga m'maiko ambiri padziko lapansi. Ku Russia, chinthucho chidalembetsedwa mu 2008. Tsopano vildagliptin imaphatikizidwa pachaka mndandanda wazithandizo zofunika.

Kupambana mwachangu kumeneku kumachitika chifukwa cha zida zapadera za vildagliptin, zomwe zatsimikiziridwa ndi zotsatira za maphunziro oposa 130 apadziko lonse lapansi.

Ndi matenda a shuga, mankhwalawa amakulolani:

1. Sinthani kayendedwe ka glycemic. Vildagliptin mu tsiku lililonse 50 mg amathandizira kuchepetsa shuga atatha kudya ndi pafupifupi 0,9 mmol / L. Glycated hemoglobin imachepetsedwa ndi 1%.
2. Pangani kupindika kwa glucose pothana ndi nsonga. Mlingo wapamwamba wa postprandial glycemia umachepa pafupifupi 0,6 mmol / L.
3. Molondola muchepetsani kuthamanga kwa magazi masana ndi usiku m'miyezi isanu ndi umodzi yoyambirira.
4. Sinthani kagayidwe ka lipid makamaka pochepetsa kuchuluka kwa lipoproteins otsika. Asayansi amawona kuti izi ndizowonjezera, sizikugwirizana ndi kuwongolera kwa shuga.
5. Chepetsani kunenepa komanso m'chiuno mwa odwala onenepa kwambiri.
6. Vildagliptin imadziwika ndi kulolerana kwabwino komanso chitetezo chachikulu. Ma epicode a hypoglycemia pa nthawi yomwe amagwiritsidwa ntchito ndi osowa kwambiri: chiwopsezo ndi chotsika kwambiri kuposa nthawi yomwe mumatenga zotengera za sulfonylurea.
7. Mankhwala amapita bwino ndi metformin. Odwala omwe atenga metformin, kuwonjezeredwa kwa 50 mg ya vildagliptin ku mankhwalawa kumathandizanso kuchepetsa GH ndi 0.7%, 100 mg ndi 1.1%.

Malinga ndi malangizo, machitidwe a Galvus, dzina lamalonda la vildagliptin, zimatengera mwachindunji kutukukira kwa maselo a pancreatic beta komanso kuchuluka kwa shuga. Mtundu woyamba wa matenda ashuga komanso amitundu iwiri ya ashuga okhala ndi kuchuluka kwa maselo a beta owonongeka, vildagliptin ilibe mphamvu. Mwa anthu athanzi komanso odwala matenda ashuga okhala ndi shuga wamba, sizingayambitse vuto la hypoglycemic.

Pakadali pano, vildagliptin ndi mawonekedwe ake amawonetsedwa ngati mankhwala a mzere wachiwiri pambuyo pa metformin. Amatha kusintha m'malo mwazomwe zimapezeka pompopompo sulfonylurea, zomwe zimapangitsanso kaphatikizidwe ka insulin, koma ndiotetezeka kwambiri.

Pharmacokinetics wa mankhwala

Zisonyezo za pharmacokinetic za vildagliptin kuchokera kuzomwe mungagwiritse ntchito:

Mankhwala osokoneza bongo omwe ali ndi vildagliptin

Maumwini onse a vildagliptin ali ndi ufulu wokhala ndi a Novartis, omwe adayika kuyesetsa ndi ndalama zambiri pakukonzekera ndikuyambitsa mankhwalawa pamsika. Mapiritsi amapangidwa ku Switzerland, Spain, Germany. Posachedwa, kukhazikitsidwa kwa mzere ku Russia kunthambi ya Novartis Neva kuyembekezeredwa. Mankhwala, omwe ndi vildagliptin palokha, ali ndi mbiri yaku Switzerland yokha.

Vildagliptin ili ndi zinthu za 2 Novartis: Galvus ndi Galvus Met. Zomwe zimagwiritsidwa ntchito ku Galvus ndi vildagliptin chokha. Mapiritsi ali ndi gawo limodzi la 50 mg.

Galvus Met ndi kuphatikiza kwa metformin ndi vildagliptin piritsi limodzi. Zosankha zamitengo yomwe ilipo: 50/500 (mg sildagliptin / mg metformin), 50/850, 50/100. Kusankha kumeneku kumakupatsani mwayi woganizira mawonekedwe a shuga mwa wodwala wina ndikusankha moyenera mankhwalawa.

Malinga ndi odwala matenda ashuga, kutenga Galvus ndi metformin piritsi zosiyana ndi zotsika mtengo: mtengo wa Galvus ndi pafupifupi rubles 750, metformin (Glucophage) ndi ma ruble 120, Galvus Meta pafupifupi 1600 rubles. Komabe, chithandizo chophatikizidwa ndi Galvus Metom chinadziwika kuti chinali chothandiza komanso chosavuta.

Galvus ilibe fanizo ku Russia yokhala ndi vildagliptin, popeza mankhwalawa ali oletsedwa. Pakadali pano, ndizoletsedwa kupangira mankhwala aliwonse okhala ndi vildagliptin, komanso chitukuko cha chinthucho. Kuchita kumeneku kumapangitsa wopanga kubwezeretsanso mtengo wa maphunziro angapo ofunikira kulembetsa mankhwala atsopano.

Chizindikiro chovomerezeka

Vildagliptin imangowonetsa mtundu wa shuga wachiwiri. Malinga ndi malangizo, mapiritsi akhoza kulembedwa:

1. Kuphatikiza pa metformin, ngati mulingo woyenera mulibe matenda okwanira a shuga.
2. M'malo mwake kukonzekera kwa sulfonylurea (PSM) mu odwala matenda ashuga ndi chiopsezo cha hypoglycemia. Chifukwa chake chimatha kukhala kukalamba, mawonekedwe a kadyedwe, masewera ndi zina zolimbitsa thupi, kuchepa kwa mitsempha, kuwonongeka kwa chiwindi ndi njira ya chimbudzi.
3. Anthu odwala matenda ashuga omwe ali ndi chifuwa ku gulu la PSM.
4. M'malo mwa sulfonylurea, ngati wodwalayo akufuna kuti achedwetse kuyamba kwa mankhwala a insulin momwe angathere.
5. Monga monotherapy (pokhapokha vildagliptin), ngati mutenga Metformin ndi yolakwika kapena yosatheka chifukwa cha zovuta zoyipa.

Kulandila vildagliptin mosakayikira kuyenera kuphatikizidwa ndi zakudya za anthu odwala matenda ashuga komanso maphunziro akuthupi. Kukana kwambiri kwa insulin chifukwa cha kuchuluka kwa ntchito komanso kudya kosagwiritsidwa ntchito m'thupi kumatha kukhala cholepheretsa kubwezeretsa chiphuphu cha shuga. Malangizowa amakupatsitsani kuphatikiza vildagliptin ndi metformin, PSM, glitazones, insulin.

Mlingo woyenera wa mankhwalawa ndi 50 kapena 100 mg. Zimatengera kuopsa kwa matenda ashuga. Mankhwalawa amakhudza kwambiri glycemia ya postprandial, motero m`pofunika kumwa mlingo wa 50 mg m'mawa. 100 mg amagawidwa chimodzimodzi m'maphwando a m'mawa ndi madzulo.

Pafupipafupi pazinthu zosafunika

Ubwino wawukulu wa vildagliptin ndizovuta zochepa pamagwiritsidwe ake. Vuto lalikulu mu odwala matenda ashuga omwe amagwiritsa ntchito PSM ndi insulin ndi hypoglycemia. Ngakhale kuti nthawi zambiri zimadutsa mofatsa, madontho a shuga amakhala owopsa mumitsempha yamitsempha, chifukwa chake amayesa kuzipewa momwe angathere. Malangizo ogwiritsira ntchito amadziwitsa kuti chiopsezo cha hypoglycemia mutatenga vildagliptin ndi 0.3-0.5%. Poyerekeza, pagulu lolamulira lomwe silimamwa mankhwalawa, chiwopsezo ichi chidapatsidwa 0,2%.

Kutetezedwa kwakukulu kwa vildagliptin kumatsimikiziridwanso ndikuti nthawi yamaphunziroli, palibe munthu wodwala matenda ashuga amene amayenera kuchoka pamankhwala chifukwa chotsatira zake zoyipa, monga zikuwonetsedwera ndi chiwerengero chomwecho cha kukana chithandizo m'magulu omwe atenga vildagliptin ndi placebo.

Ochepera ochepera 10% adadandaula za kupepuka, ndipo osachepera 1% adadandaula za kudzimbidwa, kupweteka kwa mutu, ndi kufalikira kwa malekezero. Zinapezeka kuti kugwiritsa ntchito nthawi yayitali kwa vildagliptin sikuti kumawonjezera pafupipafupi zotsatira zake zoyipa.

Malinga ndi malangizo, contraindication kumwa mankhwalawa ndi hypersensitivity vildagliptin, ubwana, pakati ndi mkaka wa m`mawere. Galvus imakhala ndi lactose monga gawo lothandizira, chifukwa chake, pakakhala zovuta, mapiritsi awa ndi oletsedwa. Galvus Met imaloledwa, popeza palibe lactose pakapangidwe kake.

Bongo

Zotheka kuzipezeka chifukwa cha kuchuluka kwa vildagliptin malinga ndi malangizo:

Pankhani ya bongo, kuyeretsa kwam'mimba ndi chithandizo chamankhwala ndikofunikira. Vildagliptin metabolites amathandizidwa ndi hemodialysis.

Vildagliptin analogues

Pambuyo pa vildagliptin, zinthu zingapo zapezeka zomwe zitha kuletsa DPP-4. Onsewa ndi fanizo:

• Saksagliptin, dzina lamalonda Onglisa, wopanga Astra Zeneka. Kuphatikizika kwa saxagliptin ndi metformin kumatchedwa Comboglize;
• Sitagliptin ilipo mu kukonzekera kwa Januvius kuchokera ku kampani Merck, Xelevia wochokera ku Berlin-Chemie. Sitagliptin ndi metformin - zinthu zomwe zimagwiritsa ntchito mapiritsi awiri a Janumet, analog ya Galvus Meta;
• Linagliptin ali ndi dzina lamalonda Trazhenta. Mankhwalawa ndi ubongo wa kampani ya ku Germany Beringer Ingelheim. Linagliptin kuphatikiza metformin piritsi limodzi limatchedwa Gentadueto;
• Alogliptin ndi gawo limodzi la mapiritsi a Vipidia, omwe amapangidwa ku USA ndi Japan ndi Takeda Pharmaceuticals. Kuphatikiza kwa alogliptin ndi metformin kumapangidwa pansi pa amalonda Vipdomet;
• Gozogliptin ndiye mndandanda wokha wa vildagliptin. Adalinganiza kuti amasule ndi Satereks LLC. Kutulutsa kokwanira, kuphatikiza mankhwala, kudzachitika m'chigawo cha Moscow. Malinga ndi zotsatira za mayeso azachipatala, chitetezo ndi kugwira ntchito kwa gozogliptin kunali pafupi ndi vildagliptin.

M'magawo ogulitsa ku Russia, mutha kugula Ongliz (mtengo wamaphunziro a pamwezi ndi pafupifupi ruble 1800), Combogliz (kuchokera ma ruble 3200), Januvius (1500 rubles), Kselevia (1500 rubles), Yanumet (kuchokera 1800), Trazhent ( 1700 rub.), Vipidia (kuchokera 900 rub.). Malinga ndi kuchuluka kwa zowunikira, titha kunena kuti odziwika bwino kwambiri pa fanizo la Galvus ndi Januvius.

Madokotala amakambirana za vildagliptin

Madokotala amayamikira kwambiri vildagliptin. Amatchulanso zabwino za mankhwalawa kuti ndizachilengedwe monga momwe zimakhalira, kulekerera bwino, kupitiriza kwa hypoglycemic kwenikweni, chiopsezo chochepa cha hypoglycemia, maubwino ena owonjezera m'njira yoponderezera kukula kwa microangiopathy ndikuwongolera mkhalidwe wamakoma azombo zazikulu.

Vildagliptin, ndithudi, imachulukitsa mtengo wamankhwala, koma nthawi zina (pafupipafupi hypoglycemia) palibenso njira ina yabwino. Zotsatira za mankhwalawa zimawerengedwa kuti ndizofanana ndi metformin ndi PSM, pakupita nthawi, zizindikiro za metabolism za carbohydrate zimasintha pang'ono.

Komanso werengani izi:

• Mapiritsi a Glyclazide MV ndi mankhwala otchuka kwambiri kwa odwala matenda ashuga.
• Mapiritsi a Dibicor - zabwino zake ndi chiyani kwa odwala omwe ali ndi matenda ashuga (phindu la ogula)