Vildagliptin analogues

Matenda a shuga ndi matenda ofala. Mankhwala ambiri apangidwa kuti athandizidwe. Kuti muchepetse mlozera wama shuga, chinthu chochita Vildagliptin chimasungidwa.

Koma sioyenera kwa wodwala aliyense, chifukwa chake makampani azachipatala amasiyanitsa malo ena, ofanana pakuwoneka. Werengani malangizo oti agwiritse ntchito, mitengo ndi malingaliro pamitengo yotsika mtengo ya Vildagliptin.

Malangizo ogwiritsira ntchito

Vildagliptin ndi chinthu cha hypoglycemic. Mankhwala ndi a gulu la zolimbikitsa za islet pancreatic zida.

Mankhwalawa amatha kuperekedwa mosasamala kanthu za m'mimba zathunthu kapena zopanda kanthu. Kukhalapo kwa chakudya sikukhudza njira yolerera.

Mankhwalawa amalimbikitsidwa ndi adotolo kuti amuchiritse pamayeso omwe achitidwa komanso zotsatira zomwe zimapezeka povuta kwa matenda omwe akupitiliza. Mlingo umaperekedwa kwa wodwala aliyense, motero, zomwe zimaperekedwa mwachizolowezi zimaperekedwa kuti zidziwike ponse ponse.

Popanga mankhwala pogwiritsa ntchito mankhwala amodzi okhawo omwe mumagwiritsa ntchito mankhwala awiri, Mlingo sayenera kupitirira 50 ndi 100 mg kamodzi patsiku.

Chithandizo cha magawo awiri chimaphatikizanso mankhwala:

Mlingo wofanana, monga mankhwala ophatikiza, muyezo wa 100 mg, amafunikira pakukhazikitsa kwa mankhwala othandizira atatu - Metformin + Vildagliptin + sulfonylurea.

Kulowetsa 50 mg m'thupi - kuchitidwa kamodzi patsiku (m'mawa kapena madzulo). Ndi muyezo wofunikira wa 100 mg - kugwiritsa ntchito ma dragees kumachitika kawiri patsiku, mutadzuka komanso musanakagone.

Mankhwala Amangolembera mankhwalawa odwala omwe ali ndi matenda a shuga 2. Mankhwalawa amagwiritsidwa ntchito ngati mankhwala odziyimira pawokha kapena monga gawo la mankhwala.

Kuti muchiritse matenda operewera, pamafunika zinthu ziwiri zofunika. Pankhaniyi, mankhwala ena owonjezera amadziwika:

  • Insulin
  • Mankhwala aliwonse omwe amachepetsa shuga ya plasma.

Vildagliptin ndicho chophatikiza chophatikizika chomwe chimagwiritsidwa ntchito popanga mankhwala omwe amadziwika kuti Galvus. Yotsirizirayi imapezeka mu mawonekedwe a dragee yoyera, yoyera bwino, yokhala ndi zolemba zosiyanasiyana mbali imodzi.

The yogwira thunthu mu dragee ndi - 50 mg. Kuphatikiza apo, anactrous lactose ndi magnesium stearate amagwiritsidwa ntchito. Pang'ono pang'ono wowuma wa sodium carboxymethyl.

Zomwe zimagwira zimagwira ngati gawo lalikulu la Galvus ndipo zimakhala ndi mphamvu. Mankhwala mumadera osiyanasiyana amagulitsa mankhwalawo mtengo wake kuyambira 1150 mpaka 1300 rubles.

Vildagliptin ili ndi mitundu yofananira yopangidwa ndi makampani azachipatala aku Russia ndi achilendo. Mkhalidwe wamankhwala kuchokera ku mtundu wa wopanga sasintha, chifukwa chake chimagulidwa nthawi zambiri, chinthu chomwe chimakhala chotsika mtengo.

Zofananira zonse za vildagliptin ndi mankhwala a hypoglycemic. Iwo ali zimakhudza thupi la munthu, kutsitsa ma shuga a plasma. Chifukwa chake, zotsutsana zawo ndi zoyipa zimakhala pafupi.

Ndi zoletsedwa kugwiritsa ntchito anthu pazinthu:

  • Makamaka chidwi chophatikizika,
  • Kutsatira kwa glucose,
  • Ana osakwana zaka 18,
  • Ketoacidosis
  • Mtundu I shuga
  • Nthawi yobala mwana,
  • Nthawi yakudyetsa mwana,
  • Insulin
  • Kulephera kwina.

Zotsatira zoyipa zimachitika ndikulowa kolakwika mu:

  • Mutu, chizungulire,
  • Thupi lawo siligwirizana,
  • Khansa ya m'mimba, kudzimbidwa,
  • Kugona
  • Hypoglycemia.

Nthawi zina Mankhwala ena akaperekedwa, zotsatira zotsatirazi zimakwiya:

  • Galvus Met - kugwedezeka ndi chisangalalo,
  • Trazhenta, Onglisa - nasopharyngitis, kapamba,
  • Glucovans, Gluconorm - lactic acidosis, kupweteka m'mimba, kusowa kwa chilimbikitso,
  • Janumet - kugona, kamwa yowuma, zotumphukira edema, kapamba,
  • Amaril M - ulesi, kulumala, kusokonezeka kwa chikumbumtima, kukhumudwa,
  • Gliformin - atatha kuyambitsa khomo lamkamwa, kutseka kwachitsulo kumawonekera, dongosolo logaya chakudya.

Mankhwala ena samawonetsa zotsatira zoyipa, kapena ndizogwirizana kwathunthu ndi zomwe zikupezeka zizindikiritso.

Russian

Ma analogi a Vildagliptin opangidwa ndi makampani opanga mankhwala ophatikizira mankhwala akuphatikizapo mndandanda wocheperako - Diabefarm, Formmetin, Glformin, Gliclazide, Glidiab, Glimecomb. Mankhwala otsalawo amapangidwa kunja.

Vildagliptin sagwiritsidwa ntchito palokha mwazinthu zilizonse zomwe zaperekedwa. Amasinthidwa ndi zinthu zofananira zomwe zimayambitsa chiwonetsero chazinthu komanso mtundu wa kuwonekera kwa thupi la munthu.

Zinthu zazikulu zomwe zimayikidwa pazokha za Vildagliptin:

  • Metformin - Glformin, Formetin,
  • Glyclazide - Diabefarm, Glidiab, Glyclazide,
  • Glyclazide + Metformin - Glimecomb.

Pali zinthu ziwiri zokha zomwe zimapezeka zomwe zimaletsa shuga wambiri m'thupi. Ngati aliyense sangathe kupirira payekhapayekha, mankhwalawa amaphatikizidwa limodzi ndi mankhwala osakaniza (Glimecomb).

Ndi mtengo, opanga aku Russia ali kutsalira kwakunja. Anzake akunja anakula mtengo, atakhala oposa ruble 1000.

Foretin (ma ruble 119), Diabefarm (ma ruble 130), Glidiab (ma ruble 140) ndi Gliclazide (147 rubles) ndiwo mankhwala otsika mtengo kwambiri ku Russia. Gliformin ndiokwera mtengo kwambiri - 202 ma ruble. pafupifupi mapiritsi 28. Wotsika mtengo kwambiri ndi Glimecomb - rubles 440.

Zowonjezera

Mankhwala ochepetsa chiwonetsero cha matenda ashuga, opangidwa m'maiko ena, amapezeka ochulukirapo kuposa olowa m'malo.

Mankhwalawa otsatirawa amasiyanitsidwa, omwe amatha kuthetsa kuchuluka kwa shuga m'magazi mwa anthu.

  • USA - Trazhenta, Januvia, Combogliz Prolong, Nesina, Yanumet,
  • Netherlands - Onglisa,
  • Germany - Galvus Met, Glibomet,
  • France - Amaril M, Glucovans,
  • Malawi - Vipidia,
  • Spain - Avandamet,
  • India - Gluconorm.

Mankhwala achilendo akuphatikizapo Galvus, yokhala ndi Vildagliptin. Kutulutsidwa kwake kudakhazikitsidwa ku Switzerland. Masinthidwe amtheradi sanapangidwe.

Posinthana mumapatsidwa mankhwala ofanana, koma osakaniza ndi ena. Zomwe zimagwirira ntchito limodzi ndikupanga zigawo ziwiri zimasiyanitsidwa:

  • Linagliptin - Trazhenta,
  • Sitagliptin - Onglisa,
  • Saxagliptin - Januvius,
  • Alogliptin benzoate - Vipidia, Nesina,
  • Rosiglitazone + Metformin - Avandamet,
  • Saksagliptin + Metformin - Comboglyz Prolong,
  • Glibenclamide + Metformin - Gluconorm, Glucovans, Glibomet,
  • Sitagliptin + Metformin - Yanumet,
  • Glimepiride + Metformin - Amaril M.

Mankhwala achilendo amakhala ndi mtengo wokwera. Chifukwa chake Gluconorm - ma ruble 176, Avandamet - ma ruble 210 ndi a Glukovans - ma ruble 267 ndiotsika mtengo kwambiri. Pamtengo wokwera pang'ono - Glibomet ndi Glimecomb - 309 ndi 440 rubles. motero.

Gawo lamtengo wapakati ndi Amaril M (773 rubles) Mtengo kuchokera ku ma ruble 1000. amapanga mankhwala:

  • Vipidia - 1239 rub.,
  • Galvus Met - 1499 rub.,
  • Onglisa - ma ruble 1592.,
  • Trazhenta - 1719 rubles.,
  • Januvia - 1965 rub.

Otsika kwambiri ndi Combogliz Prolong (2941 rubles) ndi Yanumet (2825 rubles).

Chifukwa chake, Galvus, yomwe ili ndi mankhwala othandizira Vildagliptin, si mankhwala okwera mtengo kwambiri. Amalembedwa m'gulu la mitengo yapakatikati, poganizira mankhwala onse akunja.

Mapiritsi a Galvus

Galvus ndi mankhwala a hypoglycemic omwe amapangidwa kuti azilamulira shuga m'magazi omwe ali ndi matenda a shuga a 2. Zomwe zimagwira ndi vildagliptin. Chifukwa cha mankhwalawa, kuwongolera kwa glucagon ndi insulin metabolism kumachitika. Malinga ndi European Antidiabetesic Association, kugwiritsa ntchito mankhwalawa monotherapy pokhapokha ngati pali zotsutsana ndi metformin. Werengani mosamala malangizo ogwiritsira ntchito mapiritsi a Galvus ndi mndandanda wazoletsa.

INN, opanga, mtengo

Galvus ndi dzina lodziwika lamankhwala. INN (dzina losavomerezeka padziko lonse lapansi) - vildagliptin. Amapangidwa ku Spain (Novartis Pharmaceutica) komanso ku Switzerland (Novartis Pharma).

Mutha kugula mankhwala kumalo ena aliwonse malinga ndi mankhwala a dokotala. Mtengo wa paketi yamapiritsi 28 umachokera ku 724 mpaka 956 rubles.

Zotsatira za pharmacological

Vildagliptin ndi gulu lapadera la mankhwala omwe amapangitsa kuti azitha kugwiritsa ntchito kapangidwe kake ka kapamba, kamene kamayambitsa zoletsa DPP-4. Izi zimawonjezera kukondoweza kwa kapangidwe ka glucagon ngati mtundu woyamba, komanso insulinotropic yodalira shuga wa polypeptide. Pamene michere ilowa m'matumbo, mahomoni amtundu wa incretin amapangidwa ndipo amathandizira kupanga insulin m'thupi. Vutoli linapezeka mu 1960 atapeza njira yoyezera kuchuluka kwa insulin m'madzi a m'magazi.

GLP-1 (glucagon-ngati peptide-1) amadziwika kuti ndiye wodziwika kwambiri, chifukwa motsutsana ndi mtundu wa shuga II matenda a mellitus ndimomwe ndimachepera omwe amachepera pomwepo. Ponena za ma Dhib-4 ma inhibitors, amachulukitsa kwambiri kuchuluka kwa mahomoni, ndikuletsa kuwonongeka kwawo kwina.

Zofunika! Pogwiritsa ntchito vildagliptin kwa masabata 12-52, kuchuluka kwa glucose ndi hemoglobin m'magazi pamimba yopanda kanthu kumachepetsedwa kwambiri.

Pharmacokinetics

Vildagliptin mthupi imalowetsedwa mwachangu, kutsimikizika kwamtundu wa bioavailability kumafika 85%. Mukamamwa mankhwalawa pamimba yopanda kanthu, magazi ambiri amalembedwa pasanathe maola awiri. Kubwera ndi chakudya, mankhwalawa amamwa 19% pang'onopang'ono, pafupifupi maola awiri ndi theka.

Kugawa kwa mankhwalawa kumachitika chimodzimodzi pakati pa maselo ofiira am'magazi ndi madzi a m'magazi. Njira yayikulu yopatula vildagliptin imawerengedwa kuti biotransfform. 85% ya chinthucho imapukutidwa ndi impso, 15% yotsalayi - kudzera m'matumbo.

Ndikulimbikitsidwa kugwiritsa ntchito "Galvus" pothandizira matenda ashuga komanso kusunga zakudya zoyenera ndi masewera olimbitsa thupi. Zisonyezo zogwiritsa ntchito mankhwalawa ndi:

  • mankhwala oyamba a odwala omwe alibe mphamvu yothandizira pakudya ndi olimbitsa thupi kuphatikiza ndi metformin,
  • monga monotherapy - kwa odwala matenda ashuga omwe sayenera kumwa metformin, kapena pali zosintha zabwino kuchokera pakudya ndi masewera olimbitsa thupi,
  • chithandizo cha magawo awiri ndi thiazolidinedione ndi metformin, insulin, ngati palibe zotsatira kuchokera ku monotherapy,
  • kuphatikiza katatu ndi mankhwala a sulfonylurea ndi zotumphukira za metformin,
  • mankhwala othandizira patatu ndi insulin ndi metformin, ngati palibe kuwongolera kwenikweni kwa glycemia ndi njira zonsezi.

Mlingo, kumene, nthawi ya maphunzirowa amasankhidwa ndi dokotala.

Contraindication

Monga mankhwala onse, Galvus ali ndi zoletsa zingapo zofunika pakugwiritsa ntchito, zomwe wodwala aliyense ayenera kudziwa.
Kuletsa Malire:

Ndi kusamala kwapadera, mankhwalawa amatchulidwa motsutsana ndi maziko a pancreatitis pachimake, gawo lochepetsa matenda a impso ndi mtima wachitatu.

Zotsatira zoyipa

Kukula kwa angioedema kumatha kuchitika mukamamwa vildagliptin osakanikirana ndi angiotensin-kutembenuza ma enzyme zoletsa. Vutoli ndi lovuta kwambiri, nthawi zambiri limangodziyimira lokha. Nthawi zina, chiwindi chimatha kukhudzana ndi mankhwalawa. Kuwonetsa kuti kuwonetsa kwa izi sikufuna mankhwala owonjezera, ndikwanira kusiya kulandira.

Monotherapy, ndikuwonetsa kuchuluka kwa 50 mg kawiri patsiku, kumayambitsa zopweteka monga:

  • mutu
  • chizungulire
  • kudzimbidwa
  • nseru
  • kufalikira kwamphepo,
  • nasopharyngitis.

Mankhwala ophatikizidwa pamodzi ndi metformin, zizindikiro zofanananso zimawonedwa.
Chithandizo chokwanira ndi insulin chitha kutsagana ndi kuzizira, hypoglycemia, flatulence, gastroesophageal Reflux. Matenda otopa kwambiri nthawi zina amawonekera.
Kuphatikiza pazomwe tafotokozazi, maphunziro omwe adalembedwa pambuyo polembetsedwa olembedwa mwa odwala monga chiwindi, urticaria, arthralgia ndi myalgia, kapamba, komanso kuwonongeka pakhungu.

Bongo

Mlingo wa chinthu chogwira mpaka 200 mg umaloledwa ndi odwala. Kulera mpaka mayunitsi 400 kumatha kupweteka kwa minofu, kuchepa kawirikawiri, paresthesia, kuchuluka kwa ndende ya lipase ndi malungo. Kulandila oposa 600 mg a vildagliptin kumayambitsa kuchuluka kwa ALT ndi CPK, myoglobin, komanso mapuloteni a C-reactive. Kuyimitsa mankhwalawa kumathandizira kuthetsa zizindikiro. Sizotheka kuchotsa "Galvus" m'thupi la wodwala pogwiritsa ntchito dialysis, koma mutha kugwiritsa ntchito njira ya hemodialysis.

Kuyanjana kwa mankhwala osokoneza bongo

Poyerekeza ndi maziko a chithandizo chophatikiza, zotsatira za kuyanjana ndi mankhwala monga digoxin, warfarin, ramipril ndi metformin, pioglitazone, amlodipine ndi simvastatin, valsartan ndi glibenclamide sizinapezeke.

Ngati mutenga "Galvus" ndi glucocorticosteroids, thiazides, sympathomimetics, komanso mankhwala a mahomoni, ntchito ya hypoglycemic ya vildagliptin imachepetsedwa kwambiri. Panthawi ya makonzedwe apakati ndi angiotensin otembenuza enzyme zoletsa, angioedema angayambe. Izi sizitanthauza kuti mankhwalawa athetsedwe, chizindikirocho chizingochita pakokha.

Malangizo apadera

Galvus ndi mankhwala othandizira odwala matenda ashuga, koma osafanana ndi insulin. Poyerekeza ndi momwe amagwiritsidwira ntchito, ndikofunikira kuyang'anira ntchito ya chiwindi pafupipafupi, chifukwa ntchito yogwira ntchito imathandizira aminotransferase. Izi sizikuwonetsedwa ndi zizindikiro zenizeni, koma pali chiopsezo chotenga chiwindi. Pankhani ya kupweteka kwambiri pamimba, ndikofunikira kusiya, chifukwa izi zingasonyeze kukula kwa kapamba am'mimba.

Zokumana nazo zamavuto, kupsinjika kungachepetse zotsatira za kumwa mankhwalawa.

Ngati mukukumana ndi vuto la mseru komanso kugwiritsidwa ntchito bwino, sikulimbikitsidwa kuyendetsa magalimoto kapena kugwira ntchito yowopsa kapena yovuta.

Musanayese mayeso azachipatala, ndikofunikira kusiya kugwiritsa ntchito mankhwalawa kwa masiku awiri: ayodini onse omwe amagwiritsidwa ntchito podziwitsa, ayodini amapezeka. Amakhudzana ndi vildagliptin, yomwe imathandizira kuti pakhale kupsinjika kwa chiwindi ndi impso, yodzala ndi kukula kwa lactic acidosis.

Mimba komanso kuyamwa

Kafukufuku wowonetsa akuwonetsa kuti kuchuluka kwa mankhwalawa kwa mankhwalawa sikukhudza mbali yoyipa ya mluza. Panalibe zofooka zazikazi zomwe zimapezeka. Kafukufuku ochulukirapo sanachitikebe, chifukwa chake, musatayenso chiwopsezo cha mayi ndi mwana. Ndikofunika kukumbukira kuti ngati pali kuphwanya kwa kagayidwe ka shuga m'magazi, pamakhala chiopsezo cha kubadwa kwa fetalital, ndipo chiopsezo cha kufa ndi vuto la Neonatal limachulukirachulukira.

Gwiritsani ntchito muubwana ndi ukalamba

Palibe chidziwitso chokhudza kumwa mapiritsi pakati pa odwala osakwana zaka 18, chifukwa chake sichikulimbikitsidwa kuti muwaphatikizire pochiritsa.

Anthu opitilira zaka zopitilira 65 safuna kusintha kwapadera kwa mankhwalawa, koma musanagwiritse ntchito, muyenera kuonana ndi endocrinologist, kuyang'anira chiwindi ndi impso, ndikuwunika kuchuluka kwa shuga m'magazi.

Fananizani ndi fanizo

Mapiritsi a Galvus ali ndi ma fanizo ambiri, tiyeni tiyesetse kumvetsetsa zabwino ndi zovuta zawo.

Dzina lamankhwalaMapindu akeZoyipaMtengo, pakani.
JanuviaImalepheretsa enzyme DPP-4 kwa maola 24, imachepetsa chilimbikitso, imachulukitsa zochita zamahomoni a incretin.

Mtengo wokwera.1400
VipidiaZovomerezeka patsiku, sizikukondweretsa. Mofulumira komanso moyenera amachepetsa shuga m'magazi.Zotsatira zoyipa zakumbuyo za tsankho la munthu pakapangidwe.875
DiabetesMatenda a shuga amasintha kwakanthawi kochepa, amalepheretsa mapangidwe magazi. Amapereka bata. Zochepa zoyipa zimachitika.Zimatsutsa kufa kwa maselo omwe amatsimikizira kapangidwe ka insulin. Zitha kupangitsa kuti shuga asakhale mtundu woyamba. Imathandizira kukana insulin. Pamafunika kudya mosamalitsa.310
MetforminAmachepetsa kuchuluka kwa shuga wopezeka m'mankhwala ambiri a hypoglycemic.
Kukula kwa mavuto am'matumbo, chiopsezo cha matenda a anorexia, zotsekemera zakumwa zimatha kusintha.
Kukula kwa mavuto am'matumbo, chiopsezo cha matenda a anorexia, zotsekemera zakumwa zimatha kusintha.290
JanumetKuphatikizikako kuli ndi metformin. Kulekerera kwabwino kwa mankhwalawo.Milandu yambiri ndi zoyipa, mtengo wokwera.1800-2800
ForsygaZabwino zimawonedwa ngakhale ndi kuwonongeka kwa kapamba. Kuchepa kwa glucose kumachitika kale koyamba kugwiritsa ntchito mankhwalawa.Mtengo wokwera.2000-2700
GlucophageNthawi yomweyo imayimitsa zizindikiro za hyperglycemia. Zimathandizira kukhazikika pang'onopang'ono m'magulu a shuga.Chiwerengero chachikulu cha contraindication, chiopsezo chachikulu cha mavuto.315
GlibometWothandizira hypoglycemic wozikidwa pa glibenclamide ndi metformin hydrochloride. Mphamvu ya hypolipidemic imawonedwa. Amapereka chithandizo mwachangu komanso chothandiza. Mphamvu zabwino zitha kuchitika pakuphatikiza mankhwala.Zotsatira zoyipa.345
SioforZomwe zimagwiritsidwa ntchito ndi metformin hydrochloride. Imakhala ndi zochizira. Zimathandizira kuchepetsa kulemera, kumenyana ndi cholesterol "choyipa".Chiwerengero chachikulu chotsutsana.390
TrazentaKulekerera kwabwino kwambiri komanso zotsatira zake mwachangu. Imatsimikizira mtundu wa shuga, imatsuka magazi.Mtengo wokwera.1600
AmarilZimakhalabe ndi shuga pamene mukudya ndikuchita masewera olimbitsa thupi apadera. Kuchita bwino kwambiri ndi mulingo woyenera.Kuthamanga kwa mawonekedwe ndi kuzindikira kumachepetsedwa, ndikosayenera kuyendetsa magalimoto. Mtengo uli pamwamba pa avareji.355-800
ManinilYoyenera monotherapy ndi kuphatikiza mankhwala. Amapereka khola la shuga la magazi kukhala labwinobwino.Sikuti aliyense amathandizira, angathandizire kuwonetsa zizindikiro zam'mbali. Pali zotsutsana zambiri.170
OnglisaZomwe zimagwiritsidwa ntchito ndi saxagliptin. Kuchepetsa msanga magazi, kusintha kagayidwe, kumathandiza kuchepetsa thupi.Mtengo wokwera.1900

Chithandizo cha antiidiabetesic "Galvus" chotchuka pakati pa odwala, pali ndemanga zambiri zabwino.

Vladimir, wazaka 43: “Ndimatenga 50 mg ndi Metformin 500 mg m'mawa uliwonse ndi madzulo kwa zaka ziwiri. Pambuyo pa miyezi isanu ndi umodzi yogwiritsidwa ntchito mwadongosolo potsatira zakudya, kuchuluka kwa shuga kunatsikira ku 4.5. Kuphatikiza apo, zinali zotheka kuchepetsa thupi. Ngati m'mbuyomu ndidalemera makilogalamu 123, tsopano zolemetsa zimachokera ku 93-95 kg ndikukula kwa 178 cm. "

Karina, wazaka 32: “Ngakhale kuti ambiri adandipatsa chithandizo chambiri, sindinayamikire. Nthawi zambiri ndimakhala ndikumva chizungulire, kufooka komanso kupweteka m'mimba ndikugwiritsa ntchito, motero ndinayenera kusiya mankhwalawo. "

Svetlana, wazaka 56: "M'mbuyomu, adotolo adamuuza Maninil, koma sanabwere, sanataye shuga, thanzi lake lidayamba kuwipira. Kuphatikiza apo, ndimakumana ndi mavuto ndi mtima komanso mitsempha yamagazi. Kenako adotolo adandiuza kuti ndiyese Galvus. Ndikofunikira kutenga, ingomwa piritsi limodzi patsiku. Chifukwa cha machitidwe ake, shuga amachepetsa bwino ndipo pang'onopang'ono, osati kwambiri, chifukwa chake zinthu zomwe sizikukula zikuwonjezeka. Tsopano ndikusangalala, ndimatha kusangalala ndi moyo komanso kugwira ntchito. ”

Pofupikitsa, titha kudziwa kuti Galvus ndi imodzi mwamankhwala otetezeka kwambiri komanso othandiza kwambiri pa hypoglycemic omwe amapezeka pamsika wa pharmacological. Mankhwalawa ndi oyenera kuthandizira mtundu wa 2 matenda a shuga, angagwiritsidwe ntchito ngati mankhwala, kuphatikizapo masewera olimbitsa thupi komanso zakudya zapadera.

INN
Vildagliptin
Mlingo
mapiritsi
Zotsatira za pharmacological

Wothandizirana ndi hypoglycemic, wopatsa mphamvu pulogalamu ya kapamba, kapenanso kosankha zolembera za pulotidyl peptidase-4 (DPP-4).

Kuletsa mwachangu komanso kwathunthu kwa zochitika za DPP-4 (zopitilira 90%) kumayambitsa kuwonjezeka kwa zonse zoyambira komanso zosasinthika (kudya zakudya) zotsekemera za mtundu wa 1 glucagon ngati peptide ndi glucose-insulinotropic polypeptide kuchokera m'matumbo kulowa kutsekemera kwazinthu tsiku lonse.

Powonjezera kuchuluka kwa glucagon ngati mtundu 1 peptide komanso glucose wodalira insulinotropic polypeptide, vildagliptin imawonjezera chidwi cha maselo a pancreatic beta ku glucose, zomwe zimapangitsa kuti pakhale kusintha kwa insulin yotengera shuga.

Mukamagwiritsa ntchito mlingo wa 50-100 mg wa patsiku kwa odwala omwe ali ndi matenda a shuga 2, kusintha kwa ntchito ya maselo oteteza khungu la beta kumadziwika.

Kuchulukitsa kwa magwiridwe antchito a maselo a beta kumadalira kuchuluka kwa kuwonongeka kwawo koyamba, kotero mwa anthu omwe alibe matenda a shuga mellitus (omwe ali ndi kuchuluka kwa shuga m'magazi am'magazi), mankhwalawa samalimbikitsa kutulutsa kwa insulin ndipo samachepetsa kuchuluka kwa shuga.

Mwakulitsa kuchuluka kwa glucagon wamkati wama protein 1, vildagliptin imawonjezera mphamvu ya maselo a alpha ku glucose, zomwe zimabweretsa kusintha kwa shuga wodalira glucagon secretion.

Kuchepa kwa kuchuluka kwa glucagon owonjezera pakudya, kumapangitsa kuchepa kwa insulin.

Kuwonjezeka kwa kuchuluka kwa insulin / glucagon motsutsana ndi maziko a hyperglycemia, chifukwa cha kuwonjezeka kwa kuchuluka kwa glucagon ngati peptide ya mtundu 1 ndi insulinotropic polypeptide, kumapangitsa kuchepa kwa kupanga kwa shuga ndi chiwindi (munthawi ya prandial komanso chakudya), komwe kumapangitsa kutsika kwa magazi.

Pogwiritsa ntchito vildagliptin, kuchepa kwa kuchuluka kwa lipids m'madzi am'magazi kumadziwika, komabe, izi sizimakhudzana ndi mphamvu yake peptide yofanana ndi glucagon polypeptide ndi kusintha kwa magawo a cell pancreatic beta.

Kuwonjezeka kwa kuchuluka kwa glucagon ngati peptide ya mtundu 1 kungapangitse kuti m'mimba muchepetse, komabe, motsutsana ndi kugwiritsidwa ntchito kwa vildagliptin, izi sizikuwoneka.

Mukamagwiritsa ntchito vildagliptin monga monotherapy kapena kuphatikiza ndi metformin, zotumphukira za sulfonylurea, thiazolidinedione, kapena insulin, kuchepa kwakukulu kwa nthawi yayitali kwa glycosylated Hb ndikuwonjezera shuga wamagazi.
Pharmacokinetics

AUC imagwirizana mwachindunji ndi kuchuluka kwa mankhwalawa.

Mukamamwa ndi chakudya, kuchuluka kwa mayamwidwe kumachepa pang'ono, Cmax imachepa ndi 19%, TCmax imakwera mpaka maola 2,5, kuchuluka kwa mayamwidwe ndi AUC sikusintha.

Kuyankhulana ndi mapuloteni ndizochepa - 9.3%. Imagawidwa chimodzimodzi pakati pa plasma ndi maselo ofiira amwazi. Kugawa voliyumu (koyambira / koyambira) - 71 l.

Kugawa ndi kopitilira muyeso.

Njira yayikulu yotsitsira mafuta ndi kusanja mitundu.

69% ya mlingo wa mankhwalawa amapita kutembenuka. Metabolite yayikulu - lay151 (57% ya mlingo) imagwira ntchito pamankhwala ndipo ndi chida cha hydrolysis cha gawo la cyano. Pafupifupi 4% ya mankhwalawa amapezeka amide hydrolysis.

Zotsatira zabwino za DPP-4 pa hydrolysis yamankhwala zimadziwika.

Vildagliptin sapangidwa kuti akhale ndi ma cytochrome P450 isoenzymes ndipo si gawo lawo, siyimawaletsa kapena kuwalimbikitsa.

T1 / 2 - 3h. Imafufutidwa ndi impso - 85% (kuphatikiza 23% yosasinthika), m'matumbo - 15%.

Pankhani yolephera kufinya kwa chiwindi (maulendo a 606 malingana ndi Child-Pyug) ndi digiri yolimbitsa thupi (mfundo 6 - 10 malinga ndi Child-Pyug) atagwiritsidwa ntchito kamodzi pamankhwala, bioavailability imachepetsedwa ndi 20% ndi 8%, motero.

Kulephera kwambiri kwa chiwindi (mfundo 12 malinga ndi kufalitsa kwa ana-Pyug) kumachuluka ndi 22%. Kuwonjezeka kapena kuchepa kwa kuchuluka kwa bioavailability, osapitirira 30%, sikofunika kuchipatala.

Panalibe kulumikizana pakati pa kuwonongeka kwa chiwindi chovuta ndi kukhudzana kwa mankhwalawa.

Odwala omwe ali ndi vuto lochepa kwambiri, lochita kuchepa, komanso aimpso kwambiri, omwe ali ndi vuto la kumapeto kwa CRF (pa hemodialysis), akuwonjezeka Cmax ya 8% -66% ndi AUC ndi 32% -134%, omwe sagwirizana ndi kutha kwa vutoli, komanso kuwonjezeka kwa AUC ya metabolite yolimba. Lay151 1.6-6.7 nthawi, kutengera kuzunza kwa kuphwanya. T1 / 2 sasintha.

Kuchuluka kwambiri kwa bioavailability ndi 32% ndi max ndi 18% (odwala azaka zopitilira 70) sikofunika kuchipatala ndipo sikukhudza kuletsa kwa DPP-4.
Zizindikiro zogwiritsidwa ntchito

Type 2 shuga mellitus: monotherapy (kuphatikiza mankhwala othandizira pakudya ndi masewera olimbitsa thupi) komanso kuphatikiza mankhwala (osakanikirana ndi metformin, zotumphukira za sulfonylurea, thiazolidinedione, insulin) ngati mankhwala osagwiritsa ntchito bwino, kuchita masewera olimbitsa thupi komanso monotherapy ya mankhwalawa.
Contraindication

Hypersensitivity, kwambiri hepatic kuwonongeka (kuwonjezeka kwa ALT ndi AST ntchito 2,5 kuchulukitsa kuposa malire apamwamba), kuchepa kwapakati kapena kupweteka kwambiri kwaimpso (kuphatikizapo kumapeto kwa CRF pa hemodialysis), kutenga pakati, kuyamwa, kubwana (mpaka zaka 18).

Kwa Lf yomwe ili ndi lactose (posankha): galactose tsankho, kuperewera kwa lactase kapena malabsorption a glucose-galactose.
Mlingo

Mkati, mosasamala kanthu za kudya, mankhwala a monotherapy kapena othandizira awiri othandizira ndi metformin, thiazolidinedione kapena insulin - 50 mg / tsiku (m'mawa) kapena 100 mg / tsiku (50 mg m'mawa ndi madzulo), pogwiritsa ntchito mankhwala awiri othandizira omwe amapezeka ndi sulfonylurea - 50 mg / tsiku (m'mawa), wokhala ndi matenda oopsa a shuga, odwala omwe amalandira chithandizo cha insulin - 100 mg / tsiku.

Ndi osakwanira kliniki chifukwa mukumwa mankhwala a 100 mg / tsiku, mankhwala ena a hypoglycemic omwe ali ndi zotheka: metformin, zotumphukira za sulfonylurea, thiazolidinedione kapena insulin.

Pamene zotchulidwa limodzi ndi sulfonylurea zotumphukira, mphamvu ya mankhwala pa 100 mg / tsiku anali ofanana ndi mlingo wa 50 mg / tsiku.
Zotsatira zoyipa

Maulendo pafupipafupi: Nthawi zambiri (1/10 kapena kupitirirapo), nthawi zambiri (kupitirira 1/100 ndi ochepera 1/10), nthawi zina (zopitilira 1/1000 ndi ochepera 1/100), kawirikawiri (kuposa 1/10000 komanso zosakwana 1/1000) kawirikawiri kwambiri (zosakwana 1/10000).

Ndi monotherapy: mbali yamanjenje - nthawi zambiri - chizungulire, nthawi zina - kupweteka kwa mutu.

Kuchokera pamimba yogaya: nthawi zina - kudzimbidwa.

Kuchokera ku CCC: nthawi zina - zotumphukira edema.

Mukamagwiritsa ntchito mlingo wa 50 mg (kawiri pa tsiku) limodzi ndi metformin: mbali yamanjenje - nthawi zambiri - chizungulire, kupweteka kwa mutu, kugwedezeka.

Mukamagwiritsa ntchito mlingo wa 50 mg / tsiku osakanikirana ndi mankhwala a sulfonylurea: kuchokera ku mantha amthupi - nthawi zambiri - chizungulire, kupweteka mutu, asthenia, kugwedezeka.

Mukamagwiritsa ntchito mlingo wa 50 mg 1-2 kawiri pa tsiku limodzi ndi thiazolidatedione: kuchokera ku CCC - nthawi zambiri - zotumphukira edema.

Zina: nthawi zambiri - kuwonjezeka kwa thupi.

Mukamagwiritsa ntchito mlingo wa 50 mg 2 kawiri pa tsiku limodzi ndi insulin: kuchokera ku mantha amthupi - nthawi zambiri - mutu.

Kuchokera pamimba yogaya chakudya: Nthawi zambiri - nseru, kugonthetsa, matenda a gastroesophageal Reflux.

Kuchokera kumbali ya kagayidwe: kawirikawiri - hypoglycemia.

Panthawi ya monotherapy kapena kuphatikiza mankhwala ena, zovuta zoyipa sizinali zofatsa, zosakhalitsa, ndipo sizinkafuna kuti mankhwala atuluke. Zomwe zimachitika ndi angioedema (kawirikawiri - zoposa 1/10000 komanso zosakwana 1/1000) zinali zofanana ndi zomwe zili pagulu lolamulira. Nthawi zambiri, angioedema imawonedwa ikaphatikizidwa ndi ACE zoletsa, inali yofatsa ndipo imazimiririka ndi mankhwala.

Hepatic ntchito kuwonongeka (kuphatikizapo hepatitis) ya asymptomatic kumene sikanachitike kawirikawiri, yomwe nthawi zambiri imadzimasulira payekha atasiya kumwa mankhwala.
Bongo

Zizindikiro: myalgia, chosakhalitsa paresthesia, malungo, edema (kuphatikiza zotumphukira), kuchuluka kwa pang'onopang'ono pantchito ya lipase (2 kutalika kuposa malire apamwamba), kuchuluka kwa ntchito ya CPK, ALT, protein-m-protein komanso myoglobin.

Chithandizo: kusiya kwa mankhwalawa, dialysis (kuchotsedwa kwa mankhwalawa ndizokayikitsa, komabe, hydrolysis metabolite yayikulu ya vildagliptin (lay 151) imatha kuchotsedwa ndi hemodialysis.
Kuchita

Ili ndi mwayi wotsika wogwirizana ndi mankhwala. Vildagliptin si gawo lapansi la cytochrome P450 isoenzymes, sichiletsa kapena kukopa ma enzymes amenewa, momwe amagwiritsidwira ntchito ndi mankhwala omwe ali am'munsi, zoletsa kapena oyambitsa cytochrome P450 ndiwokayikitsa.

Kugwiritsa ntchito nthawi yomweyo vildagliptin sikukhudza kagayidwe ka mankhwala omwe ali magawo a isoenzymes CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 ndi CYP3A4 / 5.

Zochulukirapo zamankhwala ndi mankhwala omwe amagwiritsidwa ntchito nthawi zambiri pochiza matenda amishuga 2 mellitus (glibenclamide, pioglitazone, metformin) kapena yoperewera pamankhwala ena (amlodipine, digoxin, ramipril, simvastatin, valsartan, warfarin) sanakhazikitsidwe.
Malangizo apadera

Nthawi zina, mukamagwiritsa ntchito vildagliptin, kuwonjezeka kwa zochitika za aminotransferase kumadziwika (nthawi zambiri popanda mawonekedwe a chipatala). Musanalembe mankhwala ndi chaka choyamba chamankhwala (1 nthawi mu miyezi 3), tikulimbikitsidwa kudziwa magawo amomwe amachititsa chiwindi kugwira ntchito.

Ndi kuwonjezeka kwa ntchito za aminotransferases, zotsatira zake ziyenera kutsimikiziridwa ndi kafukufuku wobwerezabwereza, ndipo nthawi ndi nthawi muzitsimikizira magawo a michere ya chiwindi mpaka atasintha.

Ngati zochulukirapo za AST kapena ALT ndizokwera katatu poyerekeza ndi malire omwe amapezeka zimatsimikiziridwa ndi kafukufuku wachiwiri, ndikulimbikitsidwa kuti muthane ndi mankhwalawo.

Ndi chitukuko cha jaundice kapena zizindikiro zina zokhudzana ndi chiwindi ntchito, mankhwalawa amayenera kuyimitsidwa nthawi yomweyo osayambitsanso pambuyo pazomwe zimayambitsa matenda a chiwindi.

Ngati chithandizo cha insulin chikufunika, vildagliptin imagwiritsidwa ntchito limodzi ndi insulin.

Mankhwala sayenera kugwiritsidwa ntchito ngati matenda a shuga 1 kapena mankhwalawa a matenda ashuga a ketoacidosis.

Munthawi yamankhwala (ndi chizungulire), ndikofunikira kupewa magalimoto oyendetsa galimoto ndikuchita zinthu zoopsa zomwe zimafuna kuti anthu azisamalira komanso azithamanga kwambiri.

Kufotokozera za chinthu yogwira Vildagliptin / Vildagliptin.

Fomula C17H25N3O2, dzina lamakemikolo: (S) -1-N- (3-hydroxy-1-adamantyl) glycylpyrrolidine-2-carbonitrile
Gulu lamagulu: metabolites / hypoglycemic kapangidwe ndi othandizira ena.
Machitidwe hypoglycemic.

Mankhwala

Vildagliptin imalimbikitsa pulogalamu ya kapamba, kaphatikizidwe kenakake kamene kamaletsa dipeptidyl peptidase-4. Kuletsa kwathunthu komanso mwachangu kwa ntchito ya dipeptidyl peptidase-4 kumabweretsa kuwonjezeka kwa basal ndikusinthidwa kwa glucose amadalira insulinotropic polypeptide ndi glucagon-ngati mtundu 1 peptide kulowa kozungulira kwa dongosolo kuchokera tsiku lamatumbo tsiku lonse.Mwa kukulitsa zomwe zili glucose-wodwala insulinotropic polypeptide ndikulemba mtundu 1 glucagon-peptide, vildagliptin imawonjezera chidwi cha glucose maselo a pancreatic beta, zomwe zimapangitsa kuti pakhale kusintha kwa insulin yotengera shuga. Kuchulukitsa kwa magwiridwe antchito a maselo a beta kutengera kuchuluka kwa kuwonongeka kwawo koyamba; mwa anthu opanda matenda a shuga (okhala ndi glucose wabwinobwino mu seramu yamagazi), vildagliptin simalimbikitsa kutulutsa kwa insulin komanso sikuchepetsa kuchuluka kwa shuga. Mwa kukulitsa zomwe zili ndi mtundu wa glucagon wamkati wam'mimba, vildagliptin imawonjezera chidwi cha maselo a alpha ku glucose, izi zimapangitsa kuti pakhale kusintha kwamalamulo a shuga a glucagon. Kuchepa kwa glucagon okwera kwambiri pakudya kumapangitsa kuchepa kwa insulin. Kuwonjezeka kwa kuchuluka kwa insulin / glucagon mu hyperglycemia, komwe kumachitika chifukwa cha kuchuluka kwa glucose-insulinotropic polypeptide ndi mtundu wa 1 glucagon ngati peptide, kumabweretsa kuchepa kwa kupanga kwa glucose ndi chiwindi chonse munthawi ya prandial komanso pambuyo podya, zomwe zimapangitsa kutsika kwa magazi m'thupi. Komanso, mukamagwiritsa ntchito vildagliptin, mawonekedwe a serum lipid amachepetsa, koma zotsatira zake sizikugwirizana ndi zotsatira za vildagliptin pa insulinotropic polypeptide yokhazikitsidwa ndi glucagon komanso mtundu wa glucagon ngati mtundu 1 peptide ndikuwongolera magwiridwe antchito a ma cell a pancreatic beta.
Vildagliptin akaperekedwa pakamwa imatengedwa mwachangu, bioavailability kwathunthu ndi 85%. Kuchulukitsa kwa kuchuluka kwa vildagliptin mu seramu ndi malo ogwiririra ntchito nthawi yotsala kuli pafupi mwachindunji kukuwonjezeka kwa mlingo wa vildagliptin. Kuzindikira kwakukulu pakumwa mankhwala mkati mopanda kanthu kumafikira pambuyo pa ola limodzi ndi mphindi 45. Mukamamwa mankhwala ndi chakudya, kuchuluka kwa mayamwidwe a vildagliptin kumachepa pang'ono: kumachepa kwambiri pazomwe zimachitika ndi 19% komanso kuwonjezeka kwa nthawi yomwe amafika maola 2,5. Koma zomwe zimakhudza kuchuluka kwa mayamwidwe ndi malo omwe amapangidwira nthawi yopondera alibe chakudya. Vildagliptin okhala ndi mapuloteni a plasma samanga bwino (9,3%). Vildagliptin imagawidwa chimodzimodzi pakati pa maselo ofiira am'magazi ndi madzi a m'magazi. Mwina kugawa kwa mankhwalawa kumachitika mopitilira muyeso, motsatana, voliyumu yogawa pambuyo pokonzekera makonzedwe ake ndi malita 71. Mu thupi la munthu, vildagliptin ndi biotransformed 69%. Metabolite yayikulu ndi kuphatikizika kwa mankhwala 155 (57% ya mlingo), womwe umapangidwa nthawi ya hydrolysis ya gawo la cyano. Pafupifupi 4% amakumana ndi amide hydrolysis. Vildagliptin yomwe amatenga nawo gawo la cytochrome P450 isoenzymes siinapangidwe. Vildagliptin simalimbikitsa kapena kuletsa cytochrome CYP450 isoenzymes ndipo si gawo limodzi la P (CYP) 450 isoenzymes. Pakumeza, pafupifupi 85% ya mankhwalawa imachotsedwa impso, 15% imachotseredwa m'matumbo, osasinthika (23%) ya vildagliptin imachotsedwa impso. Kutha kwa theka-moyo kuli pafupifupi maola atatu ndipo sizimatengera mlingo. Gender, fuko, komanso kuchuluka kwamthupi sikukhudza ma pharmacokinetics a vildagliptin. Odwala omwe ali ndi vuto la chiwindi osachepera limodzi ndi mankhwala, kuchepa kwa bioavailability kwa vildagliptin kumadziwika ndi 20% ndi 8%, motero. Odwala omwe ali ndi vuto lalikulu la kuchepa kwa magazi kwa chiwindi, bioavailability wa vildagliptin ukuwonjezeka ndi 22%. Kutsika kapena kuchuluka kwa bioavailability wa vildagliptin, komwe sikupitirira 30%, sikutanthauza kuchipatala. Odwala ofooka pang'ono, olimbitsa komanso owopsa aimpso kulephera, hemodialysis kumawonjezera pazipita ndende ya vildagliptin ndi 8 - 66% ndi malo omwe ali munthawi yoponderezedwa ndi 32 - 134%, omwe sagwirizana ndi kuwonongeka kwa kuphwanya. zinchito boma la impso, komanso kuwonjezeka m'dera pansi pa ndende nthawi yogwira metabolite lof151 mu 1.6 - 6.7 zina, zomwe zimatengera kuzunza kwawomwe ukuchita. Pankhaniyi, theka la moyo wa vildagliptin sasintha. Mwa odwala omwe ali ndi zaka zopitilira 70, mankhwalawa a bioavailability ndiwonjezereka wa 32% (kuchuluka kwa plasma ndende ya 18%), komwe sikutanthauza kuchipatala ndipo sikumakhudza zoletsa za dipeptidyl peptidase-4. Ma pharmacokinetics a vildagliptin mwa odwala osakwana zaka 18 sanakhazikitsidwe.

Type 2 shuga mellitus monga gawo la monotherapy kapena mankhwala ophatikiza.

Njira yogwiritsira ntchito vildagliptin ndi mlingo

Vildagliptin amatengedwa pakamwa, ngakhale zakudya. Mlingo wa mankhwalawa amasankhidwa ndi dokotala payekha, kutengera kulolera komanso kuchita bwino.
Mukamagwiritsa ntchito vildagliptin, kuwonjezereka kwa ntchito za aminotransferases ndikotheka (kawirikawiri popanda mawonekedwe a chipatala), tikulimbikitsidwa kudziwa magawo amomwe amathandizira a chiwindi asanaikidwe, komanso pafupipafupi pachaka choyamba chamankhwala. Ngati wodwalayo ali ndi zochitika zambiri za aminotransferases, ndiye kuti izi ziyenera kutsimikiziridwa ndi kafukufuku wachiwiri, kenaka kudziwa magwiridwe antchito a chiwindi mpaka atasintha. Ngati ntchito ya aminotransferases idaposa katatu kupitirira malirewo komanso kutsimikiziridwa ndi kafukufuku wachiwiri, ndiye kuti vildagliptin iyenera kuletsedwa. Ndikupanga kwa jaundice kapena zizindikiro zina zakulephera kwa chiwindi, vildagliptin iyenera kuyimitsidwa nthawi yomweyo. Ndi matenda a chiwongola dzanja, vildagliptin sangathe kuyambiranso. Vildagliptin sayenera kugwiritsidwa ntchito mwa odwala omwe ali ndi matenda a shuga 1 komanso mankhwalawa a matenda ashuga a ketoacidosis. Ndi kukula kwa chizungulire ndikutenga vildagliptin, odwala sayenera kugwira ntchito ndi zida kapena magalimoto oyendetsa.

Mimba komanso kuyamwa

Poyeserera, mukamamwa vildagliptin mu Mlingo womwe ndi wowonjezereka 200 kuposa momwe analimbikitsira, mankhwalawo sanayambitse kukula koyambirira kwa mwana wosabadwa, kupatsa mphamvu chonde ndipo sanapatse mphamvu mwana wosabadwayo. Palibe deta yokwanira yogwiritsira ntchito vildagliptin mwa amayi apakati, chifukwa chake sayenera kugwiritsidwa ntchito panthawi yapakati. Sizikudziwika ngati vildagliptin idutsa mkaka wa m'mawere, chifukwa chake siyiyenera kugwiritsidwa ntchito mkaka wa mkaka.

Malangizo a Galvus

Kupanga
1 tabu. Muli vildagliptin 50 mg,
zotuluka: MCC, anactrous lactose, sodium carboxymethyl starch, magnesium stearate,

Kulongedza
mu phukusi la ma 14, 28, 56, 84, 112 ndi 168 ma PC.

Zotsatira za pharmacological
GALVUS - vildagliptin - nthumwi ya kalasi ya zopititsa patsogolo ziwiya za kapamba, mosaloledwa zimalepheretsa pulotidyl peptidase-4 (DPP-4) ya enzyme. Kulepheretsa mwachangu komanso kwathunthu kwa ntchito ya DPP-4 (> 90%) kumayambitsa kuwonjezeka kwa kubisa komanso kokhala ndi chakudya komwe kumapangitsa mtundu wa 1 glucagon-peptide (GLP-1) ndi glucose-wodalira insulinotropic polypeptide (HIP) kuchokera kumatumbo kulowa kutsekemera kwazinthu tsiku lonse.
Kuchulukitsa milingo ya GLP-1 ndi HIP, vildagliptin kumayambitsa kukhudzika kwa pancreatic? Maselo ku glucose, zomwe zimabweretsa kusintha kwa secretion ya shuga. Mukamagwiritsa ntchito vildagliptin pa mlingo wa 50-100 mg / odwala omwe ali ndi vuto lachiwiri la matenda a shuga, kusintha kwa kapangidwe ka mankhwala kapamba kumadziwika. Kuchuluka kwa kusintha kwa ntchito? -Cell imatengera kuchuluka kwa kuwonongeka kwawo koyambirira, kotero, mwa anthu omwe alibe matenda a shuga (chifukwa cha shuga wamagazi), vildagliptin simalimbikitsa kutulutsa kwa insulin ndipo sikuchepetsa shuga.
Potukula miyezo ya am'kati mwa GLP-1, vildagliptin imawonjezera chidwi cha cells-cell ku glucose, zomwe zimapangitsa kuti pakhale kusintha kwamphamvu kwa shuga wa glucagon. Kutsika kwa glucagon ochulukirapo panthawi ya chakudya, kumayambitsa kuchepa kwa insulin.
Kuwonjezeka kwa kuchuluka kwa insulin / glucagon motsutsana ndi maziko a hyperglycemia, chifukwa cha kuchuluka kwa GLP-1 ndi HIP, kumayambitsa kuchepa kwa kupanga kwa chiwindi ndi chiwindi nthawi yonse ya chakudya ndikatha kudya, zomwe zimayambitsa kuchepa kwa shuga m'magazi.
Kuphatikiza apo, motsutsana ndi kagwiritsidwe ntchito ka vildagliptin, kuchepa kwa milomo ya lipids m'magazi amwazi kumadziwika, komabe, izi sizikugwirizana ndi zotsatira zake ku GLP-1 kapena HIP komanso kusintha kwa magwiridwe antchito a pancreatic?
Amadziwika kuti kuwonjezeka kwa GLP-1 kumatha kuchepetsa m'mimba, koma izi sizikuwoneka ndi kugwiritsa ntchito vildagliptin.
Mukamagwiritsa ntchito vildagliptin mu 5795 odwala omwe ali ndi mtundu wa 2 shuga mellitus kwa masabata 12 mpaka 52 monga monotherapy kapena osakanikirana ndi metformin, zotumphukira za sulfonylurea, thiazolidinedione, kapena insulin, kuchepa kwakukulu kwakanthawi kwakanthawi kwa kuchuluka kwa glycated hemoglobin (HbA1c) komanso kusala glucose.

Galvus, zikugwiritsa ntchito
Type 2 matenda a shuga:
- monga monotherapy kuphatikiza mankhwala ochizira komanso masewera olimbitsa thupi,
- monga gawo limodzi la magawo awiri ophatikizira mankhwala ndi metformin, zotumphukira za sulfonylurea, thiazolidinedione kapena insulini pang'onopang'ono chifukwa cha kusakwanira kwa mankhwala othandizira, kuchita masewera olimbitsa thupi komanso monotherapy ndi mankhwalawa.

Contraindication
Hypersensitivity to vildagliptin ndi zina zilizonse za Galvus,
ana ochepera zaka 18 (mphamvu ndi chitetezo sizinakhazikitsidwe).
Ndi chisamaliro:
kuphwanya kwambiri chiwindi, kuphatikiza odwala omwe ali ndi zochitika zambiri za michere ya chiwindi (ALT kapena AST> 2,5 nthawi zambiri kuposa malire apamwamba - 2,5 × VGN),
kuwonongeka kwakanthawi kapena kupweteka kwambiri kwa impso (kuphatikiza CRF yotsitsa pa hemodialysis) - luso logwiritsira ntchito ndilochepa, mankhwalawa saloledwa pagulu la odwala.
matenda abwinobwino obadwa nawo - galactose tsankho, kuchepa kwa lactase kapena malabsorption a shuga-galactose.

Mlingo ndi makonzedwe
Galvus amatengedwa pakamwa, ngakhale atakhala chakudya chotani.
Mlingo wa mankhwalawa wa mankhwalawa uyenera kusankhidwa payekha kutengera momwe umagwirira ntchito komanso kulolera.
Mlingo wovomerezeka wa mankhwalawa panthawi ya monotherapy kapena ngati gawo limodzi la mankhwala ophatikizika awiri, metazin, thiazolidinedione kapena insulin ndi 50 kapena 100 mg kamodzi patsiku. Odwala omwe ali ndi matenda oopsa a 2 omwe alandila chithandizo cha insulin, Galvus amalimbikitsidwa pa 100 mg / tsiku.
Mlingo wa 50 mg / tsiku uyenera kutumikiridwa mu 1 mg m'mawa, mlingo wa 100 mg / tsiku - 50 mg kawiri pa tsiku m'mawa ndi madzulo.

Mimba komanso kuyamwa
Mu kafukufuku woyesera, atalembedwa muyezo Mlingo 200% kuposa momwe analimbikitsira, mankhwalawa sanayambitse chonde ndikukula koyambirira kwa mwana wosabadwayo ndipo sanatanthauze mwana wosabadwayo. Palibe deta yokwanira yogwiritsira ntchito mankhwalawa Galvus mwa amayi apakati, chifukwa chake mankhwalawa sayenera kugwiritsidwa ntchito panthawi yoyembekezera. Milandu ya vuto logaya shuga mwa amayi apakati, pamakhala chiwopsezo chodzala ndi vuto lobadwa nalo, komanso kufalikira kwamatenda a kubadwa kwa neonatal.
Popeza sizikudziwika ngati vildagliptin yokhala ndi mkaka wa m'mawere idachotsedwa mwa anthu, Galvus sayenera kugwiritsidwa ntchito pa mkaka wa mkaka.

Zotsatira zoyipa
Mukamagwiritsa ntchito Galvus ngati monotherapy kapena kuphatikiza mankhwala ena, zovuta zambiri sizinali zofatsa, zosakhalitsa, ndipo sizinafune kusiya chithandizo. Palibe kulumikizana komwe kunapezeka pakati pa pafupipafupi pazochitika zoyipa (AE) ndi zaka, jenda, mtundu, nthawi yogwiritsira ntchito, kapena mtundu wa dosing. Zomwe zimachitika ndi edema ya angioneurotic pa nthawi ya mankhwala ndi Galvus inali ≥1 / 10,000. Poyerekeza ndi chithandizo cha mankhwala ndi Galvus, chiwopsezo cha hepatic (kuphatikizapo hepatitis) komanso kuchepa kwa asymptomatic sichinawone. Nthawi zambiri, izi kuphwanya ndi kupatuka kwa chiwindi ntchito indices kuchokera munthawi zonse anakambirana popanda zovuta pambuyo kusiya ntchito mankhwala. Mukamagwiritsa ntchito Gal Gal mankhwala mu 50 mg 1 kapena 2 pa tsiku, pafupipafupi kuchuluka kwa michere ya chiwindi (ALT kapena AST ≥3 × VGN) inali 0,2 kapena 0,3%, motero (poyerekeza ndi 0,2% pagulu lolamulira) . Kuwonjezeka kwa ntchito ya ma enzymes a chiwindi nthawi zambiri anali asymptomatic, sanapite patsogolo, ndipo sanali limodzi ndi kusintha kwa cholestatic kapena jaundice.

Malangizo apadera
Nthawi zina, mukamagwiritsa ntchito vildagliptin, kuwonjezeka kwa zochitika za aminotransferase kumadziwika (nthawi zambiri popanda mawonekedwe a chipatala). Musanalembe mankhwala ndi chaka choyamba chamankhwala (1 nthawi mu miyezi 3), tikulimbikitsidwa kudziwa magawo amomwe amachititsa chiwindi kugwira ntchito. Ndi kuwonjezeka kwa ntchito za aminotransferases, zotsatira zake ziyenera kutsimikiziridwa ndi kafukufuku wobwerezabwereza, ndipo nthawi ndi nthawi muzitsimikizira magawo a michere ya chiwindi mpaka atasintha. Ngati zochulukirapo za AST kapena ALT ndizokwera katatu poyerekeza ndi malire omwe amapezeka zimatsimikiziridwa ndi kafukufuku wachiwiri, ndikulimbikitsidwa kuti muthane ndi mankhwalawo. Ndi chitukuko cha jaundice kapena zizindikiro zina zokhudzana ndi chiwindi ntchito, mankhwalawa amayenera kuyimitsidwa nthawi yomweyo osayambitsanso pambuyo pazomwe zimayambitsa matenda a chiwindi. Ngati chithandizo cha insulin chikufunika, vildagliptin imagwiritsidwa ntchito limodzi ndi insulin. Mankhwala sayenera kugwiritsidwa ntchito ngati matenda a shuga 1 kapena mankhwalawa a matenda ashuga a ketoacidosis. Munthawi yamankhwala (ndi chizungulire), ndikofunikira kupewa magalimoto oyendetsa galimoto ndikuchita zinthu zoopsa zomwe zimafuna kuti anthu azisamalira komanso azithamanga kwambiri.

Kuyanjana kwa mankhwala osokoneza bongo
Galvus ali ndi mwayi wotsika wolumikizana ndi mankhwala. Popeza Galvus si gawo laling'ono la ma enzymes a cytochrome P450, komanso sikulepheretsa kapena kuyambitsa ma enzyme awa, kuyanjana kwa Galvus ndi mankhwala omwe ali apansi, zoletsa, kapena inducers a P450 sizokayikitsa. Kugwiritsa ntchito pamodzi kwa vildagliptin sikukhudzanso kuchuluka kwa kagayidwe kazakudya kamene kamakhala mu ma enzyme: CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 ndi CYP3A4 / 5.

Bongo
Zizindikiro mukamagwiritsa ntchito mankhwala a 400 mg /, kupweteka kwa minofu kumatha kuchitika, kawirikawiri, mapapo ndi kuchepa kwapakati paresthesia, kutentha thupi, edema komanso kuwonjezeka kwapang'onopang'ono kwa ndende ya lipase (2 times kuposa VGN). Ndi kuwonjezeka kwa mlingo wa Galvus mpaka 600 mg /, chitukuko cha edema cha malekezero okhala ndi paresthesias ndi kuwonjezeka kwa kuchuluka kwa CPK, ALT, protein-m-protein komanso myoglobin ndizotheka. Zizindikiro zonse za mankhwala osokoneza bongo komanso kusintha kwa magawo a ma laboratite amatha pambuyo pakutha kwa mankhwalawa.
Chithandizo: Kutha kwa mankhwala kuchokera mthupi kudzera mu dialysis ndizokayikitsa. Komabe, hydrolytic metabolite yayikulu ya vildagliptin (lay151) imatha kuchotsedwa m'thupi ndi hemodialysis.

Malo osungira
Pamalo amdima pakutentha kosaposa 25 ° C.

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