Ngaphandle kokukhethwa okukhulu kwemithi enciphisa ushukela, ithuluzi elifanele lokulawula i-glycemia alikatholakali. I-Vildagliptin ingenye yezidakamizwa zesimanje zokulwa namagciwane. Akugcini nje ngokuba nemiphumela emibi engezansi: akubangeli ukwanda kwesisindo kanye ne-hypoglycemia, akukuphazamisi ukusebenza kwenhliziyo, isibindi nezinso, kepha futhi kwandisa amandla amaseli we-beta ukukhiqiza i-insulin.
IVildagliptin iyithuluzi elikhulisa isikhathi sokuphila kwama-incretins - ama-hormone emvelo emgudu wesisu. Ngokusho kodokotela, lo muthi ungasetshenziswa ngempumelelo nge-mellitus yesikhathi eside yesifo sikashukela nasezigabeni zokuqala zesifo, kufaka phakathi njengengxenye yokwelashwa okuhlanganisayo.
Itholwe kanjani i-vildagliptin
Imininingwane yokuqala yama -retretin yavela ngaphezu kweminyaka eyi-100 eyedlule, emuva ngo-1902. Izinto zazihlukaniswe ngamathumbu esibeletho futhi zabizwa ngokuthi ama-secretins. Lapho-ke amandla abo okuvusa ukukhishwa kwama-enzyme aphuma kumanyikwe adingekayo wokugaya ukudla atholakala. Eminyakeni embalwa kamuva, kwaba neziphakamiso zokuthi ama-secretions angathinta nomsebenzi we-hormonal we-gland. Kwavela ukuthi ezigulini ezine-glucosuria, lapho kuthatha i-incretin precursor, inani ushukela kumchamo liyancipha kakhulu, umthamo womchamo uyancipha, futhi nempilo iba ngcono.
Ngo-1932, i-hormone yaba negama layo lesimanje - i-insulinotropic polypeptide (HIP) esekela glucose. Kwavela ukuthi ihlanganiswe kumaseli we-mucosa we-duodenum nejejunum. Ngo-1983, ama-peptides ama-2 glucagon anjenge-glucagon (GLPs) ahlukaniswa Kwavela ukuthi i-GLP-1 ibangela ukugcinwa kwe-insulin ukuphendula ukuthathwa kwe-glucose, futhi ukugcinwa kwayo kuncishiswe kwabanesifo sikashukela.
Isenzo se-GLP-1:
Isifo sikashukela nokucindezela kuzoba yinto yesikhathi esedlule
- Ukwehlela ushukela -95%
- Ukuqedwa kwe-vein thrombosis - 70%
- Ukuqedwa kokushaya kwenhliziyo okuqinile -90%
- Ukuqeda umfutho wegazi ophakeme - 92%
- Ukwanda kwamandla ngesikhathi sosuku, ngcono ukulala ebusuku -97%
- ivuselela ukukhishwa kwe-insulin ezigulini ezinesifo sikashukela;
- kwandisa ubukhona bokudla esiswini;
- kunciphisa isidingo sokudla, kunomthelela ekwehliseni isisindo;
- kunomthelela omuhle enhliziyweni nasemithanjeni yegazi;
- kwehlisa ukukhiqizwa kwe-glucagon kuma-pancreas - i-hormone eyenza buthaka isenzo se-insulin.
Ifafaza ama-incretin nge-enzyme DPP-4, ekhona kwi-endothelium yama-capillaries angena mucosa wamathumbu, ngoba lokhu kuthatha imizuzu emi-2.
Ukusetshenziswa kwemitholampilo kwalokhu okutholakele kwaqala ngo-1995 yinkampani yezokwelapha i-Novartis. Ososayensi bakwazile ukwahlukanisa izinto eziphazamisa umsebenzi we-enzyme ye-DPP-4, yingakho isikhathi sokuphila kwe-GLP-1 ne-HIP sikhuphuke kaninginingi, kanti nokuqanjwa kwe-insulin nakho kwandile. Into yokuqala ezinzile ngamakhemikhali enendlela yokwenza enjalo edlulise isheke lokuphepha kwakuyi-vildagliptin. Leli gama lifake imininingwane eminingi: nansi isigaba esisha sabenzeli be-hypoglycemic "glyptin" nengxenye yegama lomenzi waso uWillhower, kanye nophawu lwekhono lomuthi ukunciphisa i-glycemia "gly" kanye nesifinyezo esithi "yebo", noma dipeptidylamino-peptidase, yona kanye inzalo ye-DPP -4.
Isenzo se-vildagliptin
Ukuqala kwenkathi yama-incretin ekwelashweni kwesifo sikashukela kubhekwa njengonyaka we-2000, lapho ithuba lokuvimbela i-DPP-4 liboniswa okokuqala okokuqala kwiCongress of Endocrinologists. Esikhathini esifushane, i-vildagliptin ithole isikhundla esiqinile ezindinganisweni zokwelapha isifo sikashukela emazweni amaningi omhlaba. E-Russia, le nto yabhaliswa ngonyaka we-2008. Manje i-vildagliptin ifakwa minyaka yonke ohlwini lwemithi ebalulekile.
Impumelelo esheshayo enjalo ingenxa yezakhiwo ezihlukile ze-vildagliptin, eziqinisekiswe ngemiphumela yezifundo zomhlaba wonke ezingaphezu kwe-130.
Isifo sikashukela, umuthi ukuvumela ukuthi:
- Thuthukisa ukulawulwa kwe-glycemic. IVildagliptin kumthamo wansuku zonke we-50 mg isiza ukunciphisa ushukela ngemuva kokudla ngesilinganiso esingu-0.9 mmol / L. I-hemoglobin ye-Glycated incishiswa ngesilinganiso esingu-1%.
- Yenza i-glucose ijika ibe bushelelezi ngokuqeda iziqongo. I-glycemia ephezulu ye-postprandial yehla cishe ngo-0.6 mmol / L.
- Ngokuthembekile yehlisa umfutho wegazi imini nobusuku ezinyangeni eziyisithupha zokuqala zokwelashwa.
- Thuthukisa i-lipid metabolism ikakhulukazi ngokunciphisa ukuqoqwa kwama-lipoprotein aphansi kwabantu. Ososayensi babheka lo mphumela njengento eyengeziwe, engahlobene nokuphuculwa kwesinxephezelo sikashukela.
- Yehlisa isisindo okhalweni kwiziguli ezikhuluphele.
- IVildagliptin ibonakala ngokubekezelela okuhle nokuphepha okuphezulu. Iziqephu ze-hypoglycemia ngesikhathi sokusetshenziswa kwazo azivamile kakhulu: ubungozi bungaphansi kwezikhathi eziyi-14 kunalokho lapho kuthathwa okususwayo kwendabuko kwe-sulfonylurea.
- Umuthi uhambe kahle nge-metformin. Ezigulini ezithatha i-metformin, ukwengezwa kwe-50 mg ye-vildagliptin ekwelashweni kungaphinde kunciphise i-GH nge-0.7%, 100 mg ngo-1.1%.
Ngokwemiyalo, isenzo seGalvus, igama lokuhweba le-vildagliptin, ngokuqondile kuncike ekusebenzeni kwamaseli we-pancreatic beta namazinga kashukela. Ohlelweni lokuqala lwesifo sikashukela nohlobo 2 sikashukela esinamaphesenti amaningi amaseli we-beta onakele, i-vildagliptin ayinamandla. Ebantwini abaphilile nabanesifo sikashukela esine-glucose ejwayelekile, ngeke sibangele isimo se-hypoglycemic.
Njengamanje, i-vildagliptin kanye nama-analogues ayo kubhekwa njengezidakamizwa zomugqa wesi-2 ngemuva kwe-metformin. Bangakwazi ukubuyisa ngempumelelo ukuphuma kokunye okuvame kakhulu kwe-sulfonylurea, futhi okuthuthukisa ukwakheka kwe-insulin, kepha kuphephe kakhulu.
I-Pharmacokinetics yesidakamizwa
Izinkomba ze-Pharmacokinetic ze-vildagliptin ezivela emiyalweni yokusetshenziswa:
| Isikhombi | Izici zesilinganiso | |
| I-Bioavailability,% | 85 | |
| Isikhathi esidingekayo ukuze sifinyelele ekuphakameni kwethonya egazini, min. | ukuzila ukudla | 105 |
| ngemuva kokudla | 150 | |
| Izindlela zokususa emzimbeni, i-% vildagliptin nama-metabolites ayo | izinso | 85, kufaka phakathi u-23% ongashintshiwe |
| amathumbu | 15 | |
| Shintsha kumphumela wehlisela ushukela ekuhlulekeni kwesibindi,% | mnene | -20 |
| ngokulinganiselayo | -8 | |
| esindayo | +22 | |
| Shintsha isenzo uma kwenzeka umsebenzi wezinso ongasebenzi kahle,% | Iqinisa ngo-8-66%, akuxhomeki kulokho ukwephulwa kwezinga. | |
| I-Pharmacokinetics in diabetesics asebekhulile | Ukuhlushwa kwe-vildagliptin kukhuphukela kuma-32%, umphumela wesidakamizwa awushintshi. | |
| Umphumela wokudla kokufakwa kanye nokusebenza kahle kwamathebulethi | ulahlekile | |
| Umphumela wesisindo, ubulili, ubuhlanga ekusetshenzisweni kwesidakamizwa | ulahlekile | |
| Half-life, min | I-180, ayixhomekile ekudleni | |
Izidakamizwa ezine-vildagliptin
Wonke amalungelo e-vildagliptin aphethwe ngokufanele yiNovartis, ebeke imali eningi nomzamo nemali ekuthuthukiseni nasekuqaliseni lesi sidakamizwa emakethe. Amacwecwe enziwa eSwitzerland, Spain, Germany. Kungekudala, kulindeleke ukuthi kwethulwe umugqa eRussia egatsheni likaNovartis Neva. Umuthi wemithi, okuyi-vildagliptin uqobo, unomsuka waseSwitzerland kuphela.
IVildagliptin iqukethe imikhiqizo emi-2 yeNovartis: iGalvus neGalvus Met. Into esebenzayo yeGalvus yi-vildagliptin kuphela. Amathebulethi anomthamo owodwa wama-50 mg.
IGalvus Met iyinhlanganisela ye-metformin ne-vildagliptin kwithebhulethi eyodwa. Izinketho zemithamo etholakalayo: 50/500 (mg sildagliptin / mg metformin), 50/850, 50/100. Lokhu kukhetha kukuvumela ukuthi unake izici zesifo sikashukela esigulini esithile bese ukhetha ngokunembile umthamo ofanele wemithi.
Ngokusho kwesifo sikashukela, ukuthatha i-Galvus ne-metformin kumathebhulethi ahlukile kushibhile: inani lentengo leGalvus licishe libe ngama-ruble angama-750, i-metformin (Glucophage) lingama-ruble ayi-120, uGalvus Meta ucishe abe ngama-ruble ayi-1600. Kodwa-ke, ukwelashwa okuhlanganisiwe kweGalvus Metom kwaqashelwa njengokusebenza ngempumelelo nokulula.
UGalvus awunazo izifaniso eRussia eziqukethe i-vildagliptin, ngoba into leyo ingaphansi kokuvinjelwa okusebenzayo. Njengamanje, akuvinjelwe kuphela ukukhiqizwa kwanoma yiziphi izidakamizwa ezine-vildagliptin, kodwa futhi nokuthuthukiswa kwento uqobo. Lesi silinganiso sivumela umenzi ukuthi abize izindleko zezifundo eziningi ezidingekayo ukubhalisa noma yimuphi umuthi omusha.
Izinkomba zokwamukelwa
IVildagliptin ikhonjiswa kuphela isifo sikashukela sohlobo 2. Ngokusho kwemiyalo, amaphilisi angabekwa:
- Ngaphezu kwe-metformin, uma umthamo wayo ofanele unganele ukulawula ushukela.
- Ukushintsha amalungiselelo we-sulfonylurea (PSM) kwabanesifo sikashukela ngengozi eyandayo ye-hypoglycemia. Isizathu kungaba ukuguga, izici zokudla, ezemidlalo neminye imisebenzi engokomzimba, i-neuropathy, umsebenzi wesibindi okhubazekile nezinqubo zokugaya.
- Abanesifo sikashukela abanokungezwani neqembu lePSM.
- Esikhundleni se-sulfonylurea, uma isiguli sifuna ukubambezela ukuqala kokwelashwa kwe-insulin ngangokunokwenzeka.
- Njenge-monotherapy (i-vildagliptin kuphela), uma ukuthatha iMetformin kuphambene noma akunakwenzeka ngenxa yemiphumela emibi kakhulu.
Ukwemukela i-vildagliptin nakanjani kufanele kuhlanganiswe nokudla kwesifo sikashukela nemfundo yomzimba. Ukumelana ne-insulin ephezulu ngenxa yamazinga aphansi okucindezela kanye nokudla okungalawulwa kwama-carbohydrate kungaba yisithiyo esingenakunqotshwa sokuthola isinxephezelo sikashukela. Umyalo ukuvumela ukuthi uhlanganise i-vildagliptin ne-metformin, i-PSM, i-glitazones, ne-insulin.
Umthamo ophakanyisiwe wesidakamizwa ngu-50 noma 100 mg. Kuya ngobucayi besifo sikashukela. Umuthi uthinta ikakhulukazi i-postprandial glycemia, ngakho-ke kuyalulekwa ukuphuza umthamo ka-50 mg ekuseni. I-100 mg ihlukaniswe ngokulinganayo ekwamukelweni kwasekuseni nakusihlwa.
Imvamisa yezenzo ezingafuneki
Inzuzo enkulu ye-vildagliptin imvamisa ephansi yemiphumela emibi ngesikhathi sokusetshenziswa kwayo. Inkinga enkulu kubantu abanesifo sikashukela besebenzisa i-PSM ne-insulin yi-hypoglycemia. Naphezu kweqiniso lokuthi esikhathini esiningi badlula ngendlela emnene, amaconsi kashukela ayingozi ohlelweni lwezinzwa, ngakho-ke bazama ukuwagwema ngangokunokwenzeka. Imiyalo esetshenzisiwe yazisa ukuthi ubungozi be-hypoglycemia lapho uthatha i-vildagliptin ingu-0.3-0.5%. Ukuqhathanisa, eqenjini elilawulayo elingathathi lo muthi, le ngozi ibalwe ku-0,2%.
Ukuphepha okuphezulu kwe-vildagliptin nakho kufakazelwa ukuthi ngesikhathi kuqhubeka lolu cwaningo, akekho umuntu onesifo sikashukela odinga ukuthi ahoxiswe umuthi ngenxa yemiphumela yawo emibi, njengoba kufakazelwa yinani elifanayo lokwenqaba ukwelashwa emaqenjini athatha i-vildagliptin ne-placebo.
Ngaphansi kwe-10% yeziguli zikhononda ngokungahambi kahle, futhi abangaphansi kuka-1% bakhala ngokuqunjelwa, ikhanda, nokuvuvukala kwemikhawulo. Kwatholakala ukuthi ukusetshenziswa isikhathi eside kwe-vildagliptin akuholeli ekwandeni kwemvamisa yemiphumela yayo emibi.
Ngokusho kwemiyalo, ukwephulwa kokuphuza umuthi kungukuqonda kuphela i-vildagliptin, ingane, ukukhulelwa nokukhulelwa. IGalvus iqukethe i-lactose njengengxenye yokusiza, ngakho-ke, uma ingabekezeleli, lezi zibhebhe zenqatshelwe. IGalvus Met ivunyelwe, njengoba kungekho lactose ekwakhiweni kwayo.
Ukweqisa
Imiphumela engaba khona ye-overdose ye-vildagliptin ngokwemiyalo:
| Umthamo, mg / usuku | Ukwephulwa |
| kufika ku-200 | Kubekezelelwa kahle, azikho izimpawu. Ingozi ye-hypoglycemia ayikhuphuki. |
| 400 | Ubuhlungu bemisipha Akuvamile - umuzwa ovuthayo noma ukudonsa esikhunjeni, umkhuhlane, i-edema yangaphakathi. |
| 600 | Ngaphezu kokwephulwa okungenhla, izinguquko ekubunjweni kwegazi zingenzeka: ukukhula kwe-creatine kinase, amaprotheni e-C-reactive, i-AlAT, i-myoglobin. Izinkomba zaselebhu kancane kancane zijwayelekile ngemuva kokuyekiswa komuthi. |
| ngaphezulu kwama-600 | Imiphumela emzimbeni ayifundwanga. |
Uma kwenzeka kuba ne-overdose, ukuhlanza esiswini nokwelashwa okubonakalayo kuyadingeka. Ama-metabolite e-Vildagliptin adalulwa yi-hemodialysis.
Uyacelwa ukuthi uqaphele: okweqile kwe-metformin, okungenye yezingxenye zeGalvus Meta, kwandisa ingozi ye-lactic acidosis, enye yezinkinga eziyingozi kakhulu zesifo sikashukela.
Izithonjana zeVildagliptin
Ngemuva kwe-vildagliptin, ezinye izinto eziningi zitholakele ezingavimba i-DPP-4. Zonke ziyizichazi:
- ISaksagliptin, igama lokuhweba u-Onglisa, umkhiqizi u-Astra Zeneka. Ukuhlanganiswa kwe-saxagliptin ne-metformin ibizwa ngokuthi yi-Comboglize;
- ISitagliptin itholakala kumalungiselelo kaJanuvius avela enkampanini iMerck, eXelevia evela eBerlin-Chemie. I-Sitagliptin ene-metformin - izinto ezisebenzayo zamathebulethi ezinxenye ezimbili uJanumet, i-analog kaGalvus Meta;
- ILinagliptin inegama lokuhweba iTrazhenta. Umuthi lo yi-brainchild yenkampani yaseJalimane iBeringer Ingelheim. ILinagliptin plus metformin kwithebhulethi elilodwa ibizwa ngokuthi iGentadueto;
- I-Alogliptin iyisakhi esisebenzayo samathebhulethi eVipidia, enziwa eMelika naseJapan ngabakwaTakeda Pharmaceuticals. Ukuhlanganiswa kwe-alogliptin ne-metformin kwenziwa ngaphansi kophawu lwentengiso Vipdomet;
- I-Gozogliptin ukuphela kwe-analogue yasekhaya ye-vildagliptin. Kuhlelelwe ukuyikhipha ngabakwaSatereks LLC. Umjikelezo ophelele wokukhiqiza, kufaka phakathi umuthi we-pharmacological, uzokwenziwa esifundeni saseMoscow. Ngokwemiphumela yokuhlolwa kwezempilo emtholampilo, ukuphepha kanye nokusebenza ngempumelelo kwe-gozogliptin yayiseduze kwe-vildagliptin.
Kumakhemisi aseRussia, njengamanje ungathenga i-Ongliza (intengo yezifundo zanyanga zonke icishe ibe ngama-ruble ayi-1800), iCombogliz (kusuka kuma-ruble angama-3200), iJanuvius (1500 ruble), Kselevia (1500 ruble), Yanumet (kusuka 1800), Trazhentu ( 1700 rub.), Vipidia (kusuka kuma-900 rub.). Ngokwezibalo zokubuyekezwa, kungaphikiswa ukuthi okuthandwa kakhulu kwama-analogues kaGalvus nguJanuvius.
Odokotela babuyekeza nge-vildagliptin
Odokotela bayazisa kakhulu i-vildagliptin. Babiza izinzuzo zalo muthi isimo semvelo sesenzo saso, ukubekezelela okuhle, umphumela ophikelelayo we-hypoglycemic, ubungozi obuphansi be-hypoglycemia, izinzuzo ezengeziwe ngendlela yokucindezela ukuthuthukiswa kwe-microangiopathy kanye nokwenza ngcono isimo sezindonga zemikhumbi emikhulu.
IVildagliptin, empeleni, inyusa kakhulu intengo yokwelashwa, kepha kwezinye izimo (i-hypoglycemia ejwayelekile) ayikho enye indlela efanelekile kuyo. Umphumela wesidakamizwa ubhekwa njengelingana ne-metformin ne-PSM, ngokuhamba kwesikhathi, izinkomba ze-carbohydrate metabolism ngcono kancane.
Futhi funda lokhu:
- Amathebulethi we-Glyclazide MV ayisidakamizwa esidume kakhulu kubantu abanesifo sikashukela.
- Amathebhulethi e-Dibicor - yini izinzuzo zawo ezigulini ezinesifo sikashukela (izinzuzo zabathengi)
