Vildagliptin - umarnin, analogues da sake dubawa na haƙuri

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Duk da tarin zaɓuɓɓukan magungunan rage ƙwayar sukari, har yanzu ba a samo kayan aikin da ya dace don sarrafa glycemia ba. Vildagliptin ɗayan magungunan antidiabetic ne na zamani. Ba wai kawai yana da ƙananan tasirin sakamako ba: ba ya haifar da hauhawar nauyi da hauhawar jini, ba ya lalata aikin zuciya, hanta da ƙodan, amma kuma yana tsawan ikon ƙwayoyin beta don samar da insulin.

Vildagliptin kayan aiki ne wanda ke haɓaka rayuwar al'amuran - jijiyoyin halittar jiki na hanji. A cewar likitocin, ana iya yin amfani da wannan kayan cikin nasara tare da cutar sankarar ƙwayar cutar sankara na dogon lokaci da kuma a farkon matakan cutar, ciki har da wani ɓangare na magani hade.

Yadda aka gano vildagliptin

Bayanai na farko game da abubuwan banmamaki sun bayyana ne sama da shekaru 100 da suka gabata, a cikin shekarar 1902. Abubuwan sun kasance daga kewayen hanji kuma ana kira asirin. Sa'annan kuma an gano ikon su ta hanzarin sakin enzymes daga cututtukan farji da suka wajaba don narkewar abinci. Bayan 'yan shekaru bayan haka, akwai shawarwari da ke nuna cewa asirin na iya shafar ayyukan hormonal na gland shine yake. Ya juya cewa a cikin marasa lafiya tare da glucosuria, lokacin ɗaukar madaidaicin abubuwa, yawan sukari a cikin fitsari yana raguwa, yawan fitsari yana raguwa, kuma lafiyar ta inganta.

A cikin 1932, hormone ya sami suna na zamani - polypeptide glucose-dogara insulinotropic polypeptide (HIP). Ya juya cewa an haɗa shi cikin sel na mucosa na duodenum da jejunum. Zuwa 1983, ƙwayoyin glucagon guda 2 (GLPs) sun kasance ware. Ya juya cewa GLP-1 yana haifar da ɓoye insulin a cikin martaba ga cin abinci na glucose, kuma an rage yawan ɓoyewar shi a cikin masu ciwon sukari.

Ayyukan GLP-1:

Ciwon sukari da hauhawar jini zai zama abin da ya wuce

  • Normalization na sukari -95%
  • Cirewa kan jijiyoyin mara wuya - 70%
  • Cire zuciyar mai karfin zuciya -90%
  • Rabu da cutar hawan jini - 92%
  • Increasearuwar kuzarin rana, inganta bacci da dare -97%
  • yana ƙarfafa sakin insulin a cikin marasa lafiya da ciwon sukari;
  • yana tsawan kasancewar abinci a cikin ciki;
  • rage bukatar abinci, yana taimakawa rage nauyi;
  • yana da tasirin gaske a zuciya da jijiyoyin jini;
  • yana rage haɓakar glucagon a cikin ƙwayar ƙwayar cuta - homonin da ke raunana aikin insulin.

Ya fashe incretins tare da enzyme DPP-4, wanda ya kasance akan endothelium na capillaries wanda ya shiga cikin mucosa na hanji, don wannan yana ɗaukar minti 2.

Amfani da wannan binciken ya fara ne a 1995 daga kamfanin magunguna na Novartis. Masana kimiyya sun sami damar ware abubuwan da ke hana aikin enzyme na DPP-4, wanda shine dalilin da yasa rayuwar GLP-1 da HIP ta karu sau da yawa, kuma aikin insulin ya karu. Abu na farko da ke tattare da keɓaɓɓiyar ƙwayar cuta tare da irin wannan hanyar aiwatarwa wanda ta wuce ƙimar aminci shine vildagliptin. Wannan sunan yana ɗaukar bayanai da yawa: a nan ne sabon rukuni na wakilai na hypoglycemic "glyptin" da kuma wani ɓangare na sunan mahaliccinsa Willhower, kuma alama ce ta ikon da miyagun ƙwayoyi don rage glycemia "gly" har ma da raguwa "ee", ko dipeptidylamino-peptidase, the enzyme sosai -4.

Ayyukan vildagliptin

Farkon lokacin da ake ciki game da magance cututtukan cututtukan ƙwayar cuta ana yin la'akari da hukuma a shekara ta 2000, lokacin da aka fara nuna yiwuwar hana DPP-4 a Majalisa na Endocrinologists. A cikin dan kankanin lokaci, vildagliptin ya sami matsayi mai ƙarfi a cikin ka'idojin maganin cutar sukari a cikin ƙasashe da yawa na duniya. A Rasha, an yi rajista da kayan a cikin 2008. Yanzu ana haɗa vildagliptin a cikin jerin magunguna masu mahimmanci.

Irin wannan nasarar ta hanzari ta faru ne saboda halayen musamman na vildagliptin, waɗanda aka tabbatar da sakamakon binciken sama da ƙasa na 130.

Tare da ciwon sukari, ƙwayar ta ba ka damar:

  1. Inganta sarrafa glycemic. Vildagliptin a cikin kashi 50 na yau da kullun na 50 na taimaka wajan rage sukari bayan cin abinci da kimanin 0.9 mmol / L. Glycated haemoglobin an rage shi da matsakaitan 1%.
  2. Sanya murfin glucose ya zama mai sauki ta hanyar kawar da kololuwa. Matsakaicin ƙwayar cuta ta glycemia ta ragu da kimanin 0.6 mmol / L.
  3. Dogara rage jini da rana dare da rana a cikin farkon watanni shida na jiyya.
  4. Metabolara haɓakar ƙwayar lipid da rage rage yawan ƙwayoyin lipoproteins mai yawa. Masana kimiyya suna ɗaukar wannan sakamako a matsayin ƙarin, ba da alaƙa da haɓaka diyya na masu cutar siga ba.
  5. Rage nauyi da kugu a cikin masu fama da kiba.
  6. An san Vildagliptin ta hanyar haƙuri mai kyau da aminci mai kyau. Abubuwa na cututtukan hypoglycemia yayin amfani dashi suna da matuƙar wuya: haɗarin ya ragu sau 14 fiye da lokacin da ake ɗaukar asalin abubuwan da ake amfani da su na gargajiya.
  7. Magungunan suna tafiya lafiya tare da metformin. A cikin marasa lafiya suna shan metformin, ƙari na 50 MG na vildagliptin zuwa jiyya na iya kara rage GH ta 0.7%, 100 MG ta 1.1%.

Dangane da umarnin, aikin Galvus, sunan cinikayyar don vildagliptin, kai tsaye ya dogara da yiwuwar ƙwayar ƙwayar ƙwayar cutar ƙwayar cuta da matakan glucose. A cikin nau'in farko na ciwon sukari da kuma nau'in masu ciwon sukari na 2 tare da adadi mai yawa na sel da aka lalace, vildagliptin ba shi da ƙarfi. A cikin mutane masu lafiya da masu ciwon sukari tare da glucose na al'ada, ba zai haifar da yanayin hypoglycemic ba.

A halin yanzu, ana ɗaukar vildagliptin da analogues su magunguna ne na layin na biyu bayan metformin. Zasu iya samun nasarar maye gurbin abubuwan da ake amfani dasu na yau da kullun na yau da kullun, wanda kuma suna haɓaka aikin insulin, amma basu da haɗari.

Pharmacokinetics na miyagun ƙwayoyi

Magungunan Pharmacokinetic na vildagliptin daga umarnin don amfani:

Mai nunawaAlamar ƙididdiga
Bioavailability,%85
Lokacin da ake buƙata don isa taro mafi girma a cikin jini, min.azumi105
bayan cin abinci150
Hanyoyi don cirewa daga jiki,% vildagliptin da metaboliteskodan85, ciki har da 23% canzawa
hanji15
Canza tasirin rage sukari a cikin gazawar hanta,%m-20
matsakaici-8
nauyi+22
Canji a aiki idan akwai makaɗaɗan aiki na keɓaɓɓiyar aiki,%Ngarfafawa da kashi 8-66%, baya dogaro da matakin ƙeta doka.
Pharmacokinetics a cikin tsofaffi masu ciwon sukariHankalin vildagliptin yana ƙaruwa zuwa 32%, sakamakon maganin ba ya canzawa.
Sakamakon abinci a cikin ɗaukar abinci da tasirin allunanya ɓace
Sakamakon nauyi, jinsi, tsere akan tasirin maganinya ɓace
Rabin-rabin, min180, bai dogara da abinci ba

Magunguna tare da vildagliptin

Duk haƙƙin don vildagliptin mallakar mallakar Novartis ne, wanda ya ba da himma da ƙoƙari da yawa don haɓaka da ƙaddamar da miyagun ƙwayoyi a kasuwa. Allunan an yi su ne a Switzerland, Spain, Jamus. Ba da daɗewa ba, ana tsammanin ƙaddamar da layin a Rasha a reshen Novartis Neva. Magungunan magani, shine vildagliptin kanta, yana da asalin asalin Switzerland kawai.

Vildagliptin ya ƙunshi samfuran 2 na Novartis: Galvus da Galvus Met. Abubuwan da ke aiki da Galvus shine kawai vildagliptin. Allunan suna da sashi guda 50 na mg.

Galvus Met shine haɗin metformin da vildagliptin a cikin kwamfutar hannu ɗaya. Zaɓuɓɓukan sashi na zaɓin magani: 50/500 (mg sildagliptin / mg metformin), 50/850, 50/100. Wannan zaɓin yana ba ku damar yin la’akari da fasalulluka na cututtukan ƙwayar cuta a cikin wani haƙuri kuma ku zaɓi madaidaicin maganin.

A cewar masu ciwon sukari, shan Galvus da metformin a cikin allunan daban yana da rahusa: farashin Galvus kusan 750 rubles ne, metformin (Glucophage) shine 120 rubles, Galvus Meta kusan 1600 rubles ne. Koyaya, lura tare da haɗa Galvus Metom an gane shi mafi inganci da dacewa.

Galvus ba shi da analogues a Rasha wanda ke dauke da vildagliptin, tunda abu yana ƙarƙashin haramtacciyar dakatarwa. A halin yanzu, an haramta shi ba kawai samar da kowace kwayoyi tare da vildagliptin ba, har ma da haɓaka kayan da kanta. Wannan ma'aunin yana bawa mai masana'antar damar dawo da farashin karatun da yawa da suka wajaba don yin rajistar kowane sabon magani.

Alamu don shigowa

Ana nuna Vildagliptin don ciwon sukari na 2 kawai. Dangane da umarnin, za'a iya ba da allunan:

  1. Baya ga metformin, idan ingantaccen kashi bai isa ya sarrafa ciwon sukari ba.
  2. Don maye gurbin shirye-shiryen sulfonylurea (PSM) a cikin masu ciwon sukari tare da haɓakar haɗarin hypoglycemia. Dalilin na iya zama tsufa, fasalin kayan abinci, wasanni da sauran ayyukan jiki, neuropathy, aikin hanta mai rauni da kuma tsarin narkewa.
  3. Masu ciwon sukari tare da rashin lafiyan ƙungiyar PSM.
  4. Madadin maganin sulfonylurea, idan mai haƙuri ya nemi jinkirta farawar insulin gwargwadon ƙarfinsa.
  5. Kamar yadda monotherapy (kawai vildagliptin), idan shan Metformin yana contraindicated ko ba zai yiwu ba saboda mummunan sakamako masu illa.

Karɓar vildagliptin ba tare da gazawa ba ya kamata a haɗe shi tare da rage cin abinci mai ciwon sukari da ilimin jiki. Babban jurewar insulin saboda karancin damuwa da karancin karuwar kwayoyi na iya zama babban cikas ga cikar biyan diyya ga masu ciwon suga. Umarni yana ba ku damar haɗaka vildagliptin tare da metformin, PSM, glitazones, insulin.

Shawarar da aka ba da shawarar maganin shine 50 ko 100 MG. Ya dogara da tsananin ciwon sukari. Magungunan sun fi shafar postprandial glycemia, saboda haka yana da kyau a sha kashi 50 na safe da safe. Ana rarraba 100 MG daidai da liyafar maraice da maraice.

Akai-akai na ayyukan da ba'a so

Babban amfanin vildagliptin shine ƙarancin tasirin sakamako masu illa yayin amfani. Babban matsala a cikin masu ciwon sukari ta amfani da PSM da insulin shine hypoglycemia. Duk da gaskiyar cewa galibi suna wucewa a cikin tsari mai sauƙi, saukad da sukari suna da haɗari ga tsarin juyayi, don haka suna ƙoƙarin guje musu gwargwadon iko. Umarnin don amfani yana sanar da cewa haɗarin hypoglycemia lokacin ɗaukar vildagliptin shine 0.3-0.5%. Don kwatantawa, a cikin ƙungiyar kulawa ba shan kwayoyi, an ƙaddara wannan haɗarin a 0.2%.

Hakanan an tabbatar da babban amincin vildagliptin ta hanyar gaskiyar cewa yayin gudanar da binciken, babu masu ciwon sukari da ake buƙatar cire maganin saboda cututtukan da ke tattare da ita, kamar yadda aka tabbatar ta hanyar yawan adadin ƙi na magani a cikin rukunin shan vildagliptin da placebo.

Kasa da 10% na marasa lafiya sun koka da rashin walwala, kuma ƙasa da 1% sun koka da maƙarƙashiya, ciwon kai, da kumburin ƙarshen hancin. An gano cewa yawan amfani da vildagliptin baya haifar da karuwa da yawaitar tasirin sakamako.

Dangane da umarnin, contraindications don shan miyagun ƙwayoyi sune kawai maganin rashin lafiyar zuwa vildagliptin, yara, ciki da lactation. Galvus ya ƙunshi lactose a matsayin kayan taimako, sabili da haka, lokacin da ya zama mai haƙuri, waɗannan allunan an haramta. An yarda da Galvus Met, saboda babu lactose a cikin kayan sa.

Yawan damuwa

Sakamakon mai yiwuwa na yawan yawan zubar da jini na vildagliptin bisa ga umarnin:

Sashi, mg / ranaRikici
har zuwa 200An yarda da shi sosai, babu alamun cutar. Rashin haɗarin hypoglycemia ba ya ƙaruwa.
400Ciwon ciki Da wuya - abin motsa rai ko firgita kan fata, zazzabi, farji na waje.
600Baya ga cin zarafin da aka ambata a sama, canje-canje a cikin abubuwan da ke cikin jini yana yiwuwa: haɓakar halittar kinase, C-reactive protein, AlAT, myoglobin. Manuniya na dakin gwaje-gwaje a hankali sun daidaita bayan dakatar da maganin.
fiye da 600Ba a yi nazarin tasirin jiki ba.

Game da yawan abin sama da ya kamata, yin tsabtace ciki da kuma maganin alamomin ya zama dole. Vildagliptin metabolites an cire shi ta hanyar hemodialysis.

Da fatan za a kula: doarfewar metformin, ɗayan abubuwan Galvus Meta, yana ƙaruwa da haɗarin lactic acidosis, ɗayan haɗari mafi haɗari na ciwon sukari.

Vildagliptin analogues

Bayan vildagliptin, an gano ƙarin abubuwa da yawa waɗanda zasu iya hana DPP-4. Dukkansu analog ne:

  • Saksagliptin, sunan kasuwanci Onglisa, mai samarwa Astra Zeneka. Haɗin saxagliptin da metformin ana kiranta Comboglize;
  • Sitagliptin yana cikin shirye-shiryen Januvius daga kamfanin Merck, Xelevia daga Berlin-Chemie. Sitagliptin tare da metformin - abubuwa masu aiki na allunan biyu Janumet, analog na Galvus Meta;
  • Linagliptin yana da sunan kasuwanci Trazhenta. Magungunan shine ƙwaƙwalwar ƙwaƙwalwar kamfanin kamfanin Beringer Ingelheim. Linagliptin da metformin a cikin kwamfutar hannu guda daya ana kiranta Gentadueto;
  • Alogliptin wani bangare ne mai aiki na allunan Vipidia, wanda aka kera shi a Amurka da Japan ta Takeda Pharmaceuticals. Haɗin haɗarin alogliptin da metformin an sanya su a ƙarƙashin alamar kasuwanci ta Vipdomet;
  • Gozogliptin shine kawai analog na gida na vildagliptin. An shirya don sakin shi ta Satereks LLC. Za a gudanar da cikakken zagayen samarwa, gami da kayan aikin magunguna a cikin yankin Moscow. Dangane da sakamakon gwaji na asibiti, aminci da tasiri na gozogliptin ya kasance kusa da vildagliptin.

A cikin kantin magunguna na Rasha, a halin yanzu zaku iya sayan Ongliza (farashin don kwatancin wata ya kusan 1800 rubles), Combogliz (daga 3200 rubles), Januvius (1500 rubles), Kselevia (1500 rubles), Yanumet (daga 1800), Trazhentu ( 1700 rub.), Vipidia (daga 900 rub.). Dangane da yawan sake dubawa, ana iya yin jayayya cewa mafi mashahuri na analogues na Galvus shine Janavius.

Nazarin likitan

Likitoci suna da darajar vildagliptin sosai. Suna kiran alfanun wannan magani yanayin dabi'ar aikinsa, haƙuri mai kyau, m sakamako mai ƙarfi, ƙarancin haɗarin hypoglycemia, ƙarin fa'idodi ta hanyar hana ci gaban microangiopathy da inganta yanayin ganuwar manyan tasoshin.

Farfesa A.S. Ametov ya yi imanin cewa magungunan da ke amfani da tasirin sakamako suna ba da gudummawa ga maido da ayyukan haɗin gwiwa a cikin ƙwayoyin ƙwayoyin ƙwayoyin cuta. Don inganta rayuwar rayuwar masu ciwon sukari, sai ya ba da shawarar abokan aiki su kara himma wajen aiwatar da nasarorin kimiyyar zamani a aikace.
Masu koyarwa a Jami'ar Sechenovskiy suna kula da babban ingancin haɗuwa da metformin da vildagliptin. Abubuwan amfanin wannan magani an nuna su a yawancin karatun asibiti.
Likitan magunguna MD A.L. Vertkin ya lura cewa ana iya amfani da vildagliptin cikin nasara don murƙushe hanyoyin atherosclerotic na halayyar ciwon sukari mellitus. Babu ƙarancin mahimmanci shine tasirin cutar zuciya.
Nazarin marasa kyau na vildagliptin suna da wuya sosai. Ofayansu yana nufin 2011. Ph.D. Kaminsky A.V. sunyi jayayya cewa vildagliptin da analogues suna da "inganci mai sauƙi" kuma suna da tsada sosai, saboda haka ba za su iya yin gasa da insulin da PSM ba. Yana fata.

Vildagliptin, hakika, yana ƙaruwa da farashin jiyya, amma a wasu halaye (m hygglycemia) babu wani madadin cancanta a ciki. Ana ganin tasirin maganin yana daidai da metformin da PSM, a tsawon lokaci, alamomin metabolism na metabolism suna inganta kaɗan.

Kuma karanta wannan:

  • Allunan magungunan Glyclazide MV sune magungunan da suka shahara ga masu ciwon sukari.
  • Allunan Dibicor - menene amfaninta ga marasa lafiya da ke dauke da cutar siga (fa'idodin masu amfani)

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