Analogues na maganin insulin degludec * (insulin degludec *)

Alurar riga kafi 100 U / ml

1 ml na bayani ya ƙunshi

abu mai aiki - insulin degludec * - 100 PIECES (3.66 MG),

magabata: phenol, metacresol, glycerol, zinc, hydrochloric acid / sodium hydroxide (don gyaran pH), ruwa don allura.

* wanda aka samar da shi ta hanyar kimiyyar halittar DNA ta hanyar amfani da iri Sadaukarwacerevisiae

Cartayan katako ɗaya ya ƙunshi 3 ml na bayani, daidai yake da 300 PIECES.

M m bayani.

Kayan magunguna

Pharmacokinetics

Bayan allurar subcutaneous, samuwar insulin degludec multhexamers mai narkewa mai narkewa, wanda ke haifar da ɗibar insulin a cikin ƙananan ƙwayar tsoka mai ƙonewa. Heaƙƙarfan ƙwayoyi suna rarrabewa, da sakin ƙwararrun insulin degludec, wanda ke haifar da jinkirin ci gaba da ƙwayar magunguna zuwa jini.

An daidaita daidaituwar Tresiba® a cikin plasma bayan kwanaki 2-3 na amfanin yau da kullun.

Ayyukan insulin degludec na tsawon sa'o'i 24 tare da gudanarwa ta yau da kullun a rana ana rarraba su tsakanin tsaka-tsakin farko da na biyu na 12-awa (AUCGIR, 0-12h, SS / AUCGIR, τ, SS = 0.5).

Haɗin insulin degludec insulin na albumin yayi daidai da ƙarfin ɗaukar ƙwayar plasma> kashi 99% cikin jini na mutum.

Rashin layi

Tare da gudanarwa na subcutaneous, jimlar yawan plasma sun kasance daidai gwargwado ga adadin da aka gudanar a cikin kewayon allurai na warkewa.

Groupsungiyoyin haƙuri na musamman

Tsofaffi marasa lafiya, marasa lafiya na kabilu daban-daban, marasa lafiya na jinsi daban-daban, marasa lafiya da ke fama da rauni ko aikin hanta

Babu wani bambance-bambance na asibiti mai mahimmanci a cikin magungunan Tresiba Penfill® tsakanin tsofaffi da matasa marasa lafiya, tsakanin marasa lafiya na kabilu daban-daban, tsakanin marasa lafiya da ke fama da rauni ko aikin hepatic da marasa lafiya masu lafiya.

Har ila yau, babu bambance-bambance a cikin kayyakin magani na magunguna dangane da jinsi na haƙuri.

Yara da matasa

Abubuwan da ke cikin pharmacokinetic na Tresiba Penfill® a cikin wani binciken a cikin yara (shekaru 1 - 11) da matasa (12-18 years old) tare da nau'in ciwon sukari na 1 na mellitus sun yi daidai da waɗanda ke cikin tsofaffi marasa lafiya tare da allura guda.

Gabaɗaya yawan kashi na insulin degludec a cikin yara da matasa yana da girma idan aka kwatanta da wannan a cikin manya marasa lafiya da tsarin kulawa guda ɗaya na magani ga marasa lafiya da masu ciwon sukari na 1.

Pharmacodynamics

Tresiba® Penfill® kwatanci ne na insulin aiki na mutum-mutum wanda aka samar ta hanyar ilimin halittar halittar jikin halittar DNA ta hanyar amfani da irin wannan kwayar cutar Saccharomyces cerevisiae.

Tyariba® Penfill® ita ce daidaitaccen tsarin aikin insulin na ɗan adam. Bayan allurar subcutaneous, kayan kwalliyar ƙwayar cuta (insulin degludec) yana samar da mai narkewa mai yawa a cikin subpotaneous depot, daga wanda akwai ci gaba mai saurin kwararar insulin degludec cikin wurare dabam dabam, yana samar da ɗakunan bayanin martaba na aiki da kuma tsayayyen sakamako na maganin.

A cikin sa'o'i 24 na saiti na tasirin hypoglycemic na miyagun ƙwayoyi a cikin marasa lafiya wanda aka kula da sashin degludec insulin sau ɗaya a rana, maganin Tresiba Penfill®, ya bambanta da glargine na insulin, ya nuna ƙimar rarraba suttura tsakanin ayyukan a cikin lokaci na farko da na biyu na sa'o'i 12 (AUCGIR, 0-12h, SS / AUCGIR, jimla, SS = 0.5)

Hoto 1. Matsakaicin matsakaiciyar matsakaiciyar matsakaitan glucose na sa'o'i 24 - daidaita daidaituwa insulinbutum degludec insulin na 100 PIECES / ml 0.6 PIECES / kg (1987 binciken)

Tsawon lokacin da miyagun ƙwayoyi Tresiba Penfill® ya fi awanni 42 a cikin kewayon maganin warkewa. An sami daidaituwa game da ƙwayar cuta a cikin jini na plasma ana samun kwanaki 2-3 bayan gudanar da maganin.

Insulin degludec a cikin daidaitawa yana nuna ƙarancin raguwa (sau 4) idan aka kwatanta da insulin glargin yau da kullun bambancin ayyukan hypoglycemic, wanda aka ƙididdige shi da ƙimar coefficient na canji (CV) don nazarin tasirin hypoglycemic na miyagun ƙwayoyi akan tazara tazara daga 0 zuwa 24 hours ( AUCGIR, τ, SS) kuma a tsakanin lokacin tsakanin daga 2 zuwa 24 hours (AUCGIR, 2-24h, SS) (Tebur 1).

Tab. 1. Bambancin bayanan martaba na yau da kullun na tasirin hypoglycemic na miyagun ƙwayoyi Tresiba da insulin glargine a cikin daidaitattun ma'aunin marasa lafiya a cikin marasa lafiya da nau'in 1 ciwon sukari mellitus.

Canjin yanayin bayanan yau da kullun na aikin hypoglycemic yayin ɗaukar tazara guda (AUCGIR, τ, SS)

Canjin bayanan bayanan yau da kullun na aikin hypoglycemic a cikin lokacin tazara daga sa'o'i 2 zuwa 24 (AUCGIR, 2-24 h, SS)

CV: ikon magana da bayanai na musayar bayanai cikin%

SS: maida hankali a cikin magunguna

AUCGIR, 2-24h: sakamako na rayuwa a cikin awanni 22 na ƙarshe na tazara tazara (in ba haka ba, babu wani tasiri akan sa na insulin cikin ciki yayin nazarin gabatar da kara)

An tabbatar da alaƙar layin tsakanin karuwa a cikin yawan ƙwayoyin Tresiba Penfill® da tasirin hypoglycemic gaba ɗaya.

Karatun bai bayyana bambancin asibiti ba a cikin magungunan Tresiba na miyagun ƙwayoyi tsakanin tsofaffi marasa lafiya da tsofaffi marassa lafiya.

Ingantaccen Asibiti da Aminci

An gudanar da gwaje-gwaje na asibiti 11 na kasa da kasa a cikin regimen "Jiyya ga makasudin" wanda zai kasance makonni 26 da 52, wanda aka gudanar a cikin ƙungiyoyi a layi daya, wanda ya haɗa da marasa lafiya 4275 masu ciwon sukari na mellitus (1102 masu fama da ciwon sukari na 1 da marasa lafiya 3173 masu fama da ciwon sukari nau'in ciwon sukari guda 2) tare da Tresiba®.

An yi nazarin ingancin Tresiba® a cikin marasa lafiya da ke da nau'in ciwon sukari na 1 na 1 (Table 3), a cikin marasa lafiya da nau'in ciwon sukari na 2 wanda bai sami insulin ba kafin (farawa daga cikin insulin, Table 4), kuma wanda ya karbi maganin insulin (ƙaruwa a cikin insulin, Table 5 ) a cikin tsayayyen tsari ko sassauya allurar rigakafin magungunan Tresiba® (Table 6).

Rashin girman kwatancen kwatancen kwatancen (insulin detemir da insulin glargine) akan maganin Tresiba dangane da raguwar cutar haemoglobin (HbA1c) daga lokacin hadawa har zuwa karshen binciken. Wani banbanci shine sitagliptin na miyagun ƙwayoyi, yayin kwatancen da maganin Tresiba® miyagun ƙwayoyi ya nuna mahimmancin ƙididdigar ƙididdigar su dangane da raguwar ƙididdigar HbA1c (Table 5).

Sakamakon bincike na meta mai zurfi na bayanan da aka samo yayin gwaje-gwaje na asibiti 7 da aka shirya kan ka'idar “Jiyya zuwa makasudin” tare da halartar marasa lafiya da ke da nau'in 1 da nau'in ciwon sukari na 2 wanda ya nuna alfanun maganin Tresiba dangane da ƙananan idan aka kwatanta da insulin glargine therapy , yawan ci gaba a cikin marasa lafiya da sassan abubuwa da aka tabbatar da rashin ƙarfi a cikin jini (Table 2). Rage yawan abin da ke faruwa a cikin jini yayin maganin Tresiba® an cimma shi tare da ƙaramin matsakaicin azumi na jini tare da insulin glargine.

Tebur 2. Meta-analysis na labarin data yawan haila

Fasali pamincewakishiyawan hailadaamma

An kiyasta Ratio Ratsi

(insulin degludec / insulin glargine)

Gaba ɗaya

Dares

Type 1 ciwon sukari mellitus + ciwon sukari na 2 2 (babban bayanan)

Bayanin maganin

Insulin degarinec * (Insulin degarinec *) - Magungunan Insulin degludec * (Insulin degludec *) ® Penfill ® - insulin da ɗan adam yakeyi wanda yake samarwa ta hanyar ilimin halittar halittar DNA ta hanyar amfani da ƙwaƙwalwar Saccharomyces cerevisiae.

Insulin degludec takamaiman yana ɗaure wa mai karɓar inshinin halittar ɗan adam kuma, yin ma'amala dashi, yasan tasirin magungunansa masu kama da tasirin insulin ɗan adam.

Tasirin hypoglycemic na insulin degludec shine saboda karuwar amfani da glucose ta hanyar kyallen takarda bayan an danganta insulin zuwa tsoka da mai karban kwayar halitta da kuma raguwa a lokaci guda a cikin yawan samarwar glucose ta hanta.

Magungunan Tresiba Penfill® shine kwatankwacin asali na insulin na mutum na tsawon lokaci, bayan allurar subcutaneous yana samar da narkewa mai yawa a cikin subpotaneous depot, daga wanda ake samun ci gaba da tsawaita insulin na insulin degludec zuwa cikin jini, wanda ke samar da cikakken tsari mai zurfi, yanayin kwanciyar hankali wanda yake aiki da kuma tsayayyen sakamako na maganin. A cikin sa'o'i 24 na saiti na tasirin hypoglycemic na miyagun ƙwayoyi a cikin marasa lafiya wanda aka kula da sashin degludec insulin sau ɗaya a rana, maganin Tresiba Penfill®, sabanin glargine na insulin, ya nuna ƙarar rarraba suttura tsakanin ayyukan a cikin lokaci na farko da na biyu na sa'o'i 12 Auc_{GiR, 0-12h, SS}/ Auc_{GiR, jimla, SS} = 0.5).

Tsawon lokacin da miyagun ƙwayoyi Tresiba Penfill® ya fi awanni 42 a cikin kewayon maganin warkewa. An sami daidaituwa game da ƙwayar cuta a cikin jini na plasma ana samun kwanaki 2-3 bayan gudanar da maganin.

Insulin degludec a cikin daidaitawa yana nuna ƙarancin raguwa (4 sau) idan aka kwatanta da insulin glargin yau da kullun bambancin ayyukan hypoglycemic, wanda aka ƙididdige shi da ƙimar da ke tattare da rarrabuwa (CV) don nazarin sakamakon cutar yawan ƙwayoyi yayin ɗaukar tazara guda (AUC_{GiR, t, SS}) kuma a tsakanin tsawon lokacin 2 zuwa 24 (AUC)_{GiR, 2-24h, SS}), duba Table 1.

Tebur 1. Bambancin bayanan martaba na yau da kullun na tasirin hypoglycemic na miyagun ƙwayoyi Tresiba da insulin glargine a cikin daidaitattun ma'aunin marasa lafiya a cikin marasa lafiya da nau'in 1 ciwon sukari mellitus.

CV shine bayanin ikon bambance-bambancen karatu cikin%,

SS shine taro na miyagun ƙwayoyi a ma'auni,

Auc_{GiR, 2-24h, SS} - Tasirin sakamako na rayuwa a cikin sa'o'i 22 na ƙarshe na tazara tazara (wato, babu wani tasiri akan sa na cikin insulin cikin allura yayin gabatarwar lokacin karatun).

An tabbatar da alaƙar layin tsakanin karuwa a cikin yawan ƙwayoyin Tresiba Penfill® da tasirin hypoglycemic gaba ɗaya.

Karatun bai bayyana bambancin asibiti ba a cikin magungunan Tresib® na miyagun ƙwayoyi tsakanin tsofaffi marasa lafiya da matasa marasa lafiya.

Ingantaccen Asibiti da Aminci

An gudanar da gwaje-gwaje na 11 na kasa da kasa na bude gwaji game da Tsira-da-Target ("warkar da makasudin" dabarun) tsawon makonni 26 da 52, wanda aka gudanar a kungiyoyi masu daidaituwa, wanda ya hada da jimlar masu cutar 4275 (marasa lafiya 1102 da ke dauke da cutar 1 guda 1 da 3173) haƙuri tare da nau'in ciwon sukari na 2 na sukari) wanda aka bi da Tresiba®.

An yi nazarin ingancin Tresiba® a cikin marasa lafiya da masu ciwon sukari na 1 na sukari wanda basu karɓi insulin kafin ba, kuma tare da nau'in ciwon sukari na 2 wanda ya sami maganin insulin, a cikin ajali mai ƙayyadadden tsari ko sassauya don Tresiba®. Rashin ingancin kwatancin kwatancen kwayoyi (insulin detemir da insulin glargia) akan Tresiba® dangane da raguwar alamarin HbA_1C daga lokacin hadawa har zuwa karshen karatun Banda ya kasance sitagliptin, lokacin da Tresiba® ya nuna mahimmancin ƙididdiga na rage HbA_1C.

Sakamakon binciken asibiti ("bi da makasudin" manufa) don farawa da maganin insulin a cikin marasa lafiya da ke da nau'in ciwon sukari na 2 na kashi 2 ya nuna raguwar 36% a cikin abubuwan da suka faru na tabbatar da cutar sankarar tsokar jini (wanda aka ayyana shi a matsayin cututtukan cututtukan zuciya wanda ya faru tsakanin sa'oin sa'o'i da ƙarfe shida na safe) an tabbatar dashi ta hanyar auna yawan glucose din plasma b0.84*0.68* Tsofaffi marasa lafiya ≥ 65 shekara0.820.65* Type 1 ciwon sukari1.10.83 Lokacin kula da allurai b1.020.75* Type 2 ciwon sukari0.83*0.68* Lokacin kula da allurai b0.75*0.62* Kawai maganin basal a cikin marasa lafiya a baya baya karbar insulin0.83*0.64*

* ƙididdiga ta mahimmanci
a - g-tabbatar hypoglycemia wani lamari ne na hypoglycemia, wanda aka tabbatar dashi ta hanyar ma'aunin plasma glucose b - kashi na hypoglycemia bayan mako na 16 na maganin.

Babu wani gagarumin aikin samarda magungunan kariya zuwa insulin bayan magani tare da Tresiba Penfill® na tsawan lokaci.

Generation na gaba Mai daukar aiki insulin

Ga masu ciwon sukari, ana samun insulin NPH na mutum da dogon aikin analogues. Tebur da ke ƙasa yana nuna manyan bambance-bambance tsakanin waɗannan magunguna.

A watan Satumbar 2015, an gabatar da sabon aikin insha na Abasaglar, wanda kusan yake daidai yake da Lantus mai nagarta.

Insulin aiki mai tsawo

Gudanar da Abinci da Magunguna (FDA, FDA ta Amurka) - Wani ma'aikacin gwamnati wanda ke ƙarƙashin Sashin Lafiya na Amurka a cikin 2016 ya amince duk da haka analog ɗin anarol-insulin na yau da kullun, Toujeo. Ana samun wannan samfurin a kasuwannin gida kuma yana tabbatar da fa'idarsa a cikin maganin cutar sikari.

NPH insulin (NPH Tsakanin Protamine Tsattsauran Hageorn)

Wannan wani nau'in insulin na roba ne wanda aka kera shi a ƙirar insulin ɗan adam, amma ya wadatar da protamine (furotin na kifi) don rage tasirin sa. NPH yana da gajimare. Sabili da haka, kafin gudanarwa, ya kamata a juya shi a hankali don haɗawa da kyau.

NPH shine mafi ƙarancin nau'in insulin aiki na tsawon lokaci. Abin takaici, yana ɗaukar haɗarin hauhawar jini da hauhawar nauyi, tunda yana da ƙarfin magana a cikin aiki (kodayake tasirinsa a hankali kuma ba shi da sauri kamar insulin a cikin bolus).

Marasa lafiya da ke dauke da ciwon sukari na 1 ana yawanci ba su kashi biyu na NPH insulin kowace rana. Kuma masu haƙuri da ke da nau'in ciwon sukari na 2 na iya yin allura sau ɗaya a rana. Dukkanta ya dogara da matakin glucose a cikin jini da kuma shawarwarin likita.

Analogs Insulin na tsawon lokaci

Insulin, abubuwan sunadarai wadanda ake canza su har suke rage jinkiri da tasirin maganin, ana daukar su ne a matsayin kwayar kwayar halittar dan adam.

Lantus, Abasaglar, Tujeo da Tresiba suna da fasalin gama gari - tsawon lokaci na aiki da ƙarancin rawar da aka ambata fiye da NPH. A wannan batun, cin abincin nasu yana rage haɗarin hauhawar jini da hauhawar nauyi. Koyaya, farashin analogues yafi girma.

Abasaglar, Lantus, da Tresiba insulin ana ɗaukar su sau ɗaya a rana. Wasu marasa lafiya kuma suna amfani da Levemir sau ɗaya a rana. Wannan bai shafi nau'in masu ciwon sukari guda 1 ba wanda aikin miyagun ƙwayoyi ya kasa da sa'o'i 24.

Tresiba shine sabon kuma a halin yanzu shine mafi tsada irin insulin da ake samu a kasuwa. Koyaya, yana da muhimmiyar fa'ida - haɗarin hauhawar jini, musamman da daddare, shine mafi ƙasƙanci.

Yaya tsawon lokacin insulin zai wuce

Matsayin insulin da ke aiki tsawon lokaci shine wakiltar babban ɓarin insulin ta cikin farji. Don haka, ana samun daidaitaccen matakin wannan hormone a cikin jini a duk tsawon aikinsa. Wannan yana bawa sel jikin mu damar amfani da glucose da ke narkar da jini a cikin tsawan awa 24.

Yadda ake allurar insulin

Dukkanin abubuwan insulins na dogon lokaci ana allura a karkashin fata zuwa wuraren da akwai matattakakken mai. Wani gefen gefen cinya ya fi dacewa da waɗannan manufofin. Wannan wurin yana ba da damar jinkirin shan magunguna. Ya danganta da alƙawarin endocrinologist, kuna buƙatar yin allura ɗaya ko biyu kowace rana.

Mitar allura

Idan makasudin ku shine ku kiyaye allurar insulin kamar yadda zai yiwu, to yi amfani da Abasaglar, Lantus, Toujeo ko Tresiba analogues. Jectionaya daga cikin allura (safe ko maraice, amma koyaushe a lokaci guda na rana) na iya samar da matakan insulin a kusa da agogo.

Kuna iya buƙatar allura biyu a kowace rana don kula da ingantaccen matakan hormone jini lokacin zabar NPH. Wannan, koyaya, yana baka damar daidaita sashi gwargwadon lokacin rana da aiki - mafi girma yayin rana da ƙasa da lokacin kwanciya.

Rashin haɗarin hauhawar jini a cikin amfani da insulin basal

An tabbatar da cewa analogues na insulin analogues ba su da wataƙila zai iya haifar da rashin lafiyar hypoglycemia (musamman tsananin rashin ƙarfi a cikin dare) idan aka kwatanta da NPH. Lokacin amfani da su, ƙimar abubuwan haemoglobin HbA1c mai yiwuwa ana iya cimma su.

Hakanan akwai tabbaci cewa yin amfani da insulin analogues na dogon lokaci idan aka kwatanta da isoflan NPH yana haifar da raguwa a cikin nauyin jiki (kuma, sakamakon haka, raguwar juriya da magunguna da kuma buƙatar gaba ɗaya na miyagun ƙwayoyi).

Dogon aiki insulin don irin nau'in ciwon sukari

Idan kun sha wahala daga kamuwa da ciwon sukari na 1, ƙwayar kumburinku ba ta iya samar da isasshen insulin ba. Sabili da haka, bayan kowane abinci, yakamata kuyi amfani da wani magani mai amfani wanda zaiyi kwatancin asirin insulin ta hanyar beta. Idan ka rasa allura, to akwai hadarin kamuwa da cutar ketoacidosis.

Lokacin zabar tsakanin Abasaglar, Lantus, Levemir da Tresiba, kuna buƙatar sanin wasu fasalolin insulin.

• Lantus da Abasaglar suna da bayanin martaba kaɗan fiye da Levemir, kuma ga mafi yawan marasa lafiya, suna da aiki awanni 24.
• Levemir na iya buƙatar ɗauka sau biyu kowace rana.
• Amfani da Levemir, ana iya lissafta allurai gwargwadon lokacin rana, don haka rage haɗarin cutar rashin ƙwaƙwalwa ta hanji da haɓaka kulawar rana.
• Toujeo, magungunan Tresibia sun fi dacewa rage alamun da ke sama idan aka kwatanta da Lantus.
• Hakanan ya kamata kuyi la’akari da tasirin magunguna kamar su fitsari. Waɗannan halayen suna da ɗan wuya, amma suna iya faruwa.
• Idan kana buƙatar canzawa daga analogues insulin analogues zuwa NPH, ka tuna cewa kashi bayan cin abinci mai yiwuwa ana buƙatar rage shi.

Dogon aiki insulin don ciwon sukari na II

Jiyya don ciwon sukari na II yawanci yana farawa da gabatarwar ingantaccen tsarin abinci da magunguna na baka (Metformin, Siofor, Diabeton, da dai sauransu ..). Koyaya, akwai yanayi yayin da aka tilasta likitoci suyi amfani da maganin insulin.

Mafi na kowa ana jera su a ƙasa:

• Rashin tasirin magungunan baka, rashin iya maganin glycemia na al'ada da haemoglobin glycated
• Contraindications don maganin baka
• Binciken cutar sankara tare da yawan ƙwayar glycemic, ƙara yawan alamun bayyanar cututtuka
• Myocardial infarction, na jijiyoyin zuciya, angiography, bugun jini, m kamuwa da cuta, hanyoyin tiyata
• Ciki

Bayanin insulin mai aiki da dogon lokaci

Maganin farko shine yawanci raka'a 0.2 / kilogiram na jiki. Wannan lissafin yana da amfani ga mutane ba tare da juriya na insulin ba, tare da aikin hanta da koda na koda. An tsara sashin insulin ne kawai daga likitanka (!)

Baya ga tsawon lokacin aiki (mafi tsawo shine degludec, mafi guntu shine asalin injinin inuwa na insulin-isophan), wadannan kwayoyi ma sun banbanta da bayyanar. A batun insulin NPH, ana rarraba kololuwar yanayi tsawon lokaci kuma yana faruwa tsakanin awanni 4 zuwa 14 bayan allura. Alamar aiki insulin ta yin aiki tsawon lokaci tana kai kololuwa tsakanin awanni 6 zuwa 8 bayan allurar, amma ya fi ƙanƙanta da rashin ƙarfi.

Saboda haka ake kira insulin glargine saboda haka ake kira 'insulin basal'. Hankalinsa a cikin jini ya ragu sosai, saboda haka hadarin cutar ƙwacewar jini ya ragu sosai.

Jerin analogues

Visitoraya daga cikin baƙo ya ba da rahoton yawan cin abincin yau da kullun