Onglisa: sake dubawa game da amfani da miyagun ƙwayoyi, umarnin

Onglisa magani ne ga masu ciwon sukari, sinadari mai aiki wanda shine saxagliptin. Saxagliptin magani ne wanda aka sanya shi don warkar da ciwon sukari na 2.

A cikin sa'o'i 24 bayan gudanarwa, yana hana aikin enzyme DPP-4. Haramcin enzyme lokacin hulɗa tare da glucose yana ƙaruwa sau 2-3 matakin glucagon-kamar peptide-1 (a nan GLP-1) da glucose-polypeptide-insulinotropic polypeptide (HIP), yana rage yawan glucagon kuma yana ƙarfafa amsawar sel sel.

Sakamakon haka, abun cikin insulin da C-peptide a cikin jiki yana ƙaruwa. Bayan an fitar da insulin ta hanyar sel beta na pancreas da glucagon daga ƙwayoyin alpha, glycemia na azumi da kuma glycemia na postprandial suna ragu sosai.

Ta yaya aminci da tasiri ga amfanin saxagliptin a cikin magunguna daban-daban an yi nazari a hankali a cikin karatun shida da aka sarrafa sau biyu, waɗanda suka haɗa da marasa lafiya 4148 waɗanda suka kamu da cutar sukari na 2 na mellitus.

Yayin nazarin, an lura da babban ci gaba a cikin haemoglobin mai narkewa, glucose plasma azumi da kuma glucose postprandial. Marasa lafiya waɗanda a cikin tsarin mulkin kamalat ɗin saxagliptin bai kawo sakamakon da ake tsammanin ba an kuma haɗa su da magunguna kamar haka metformin, glibenclamide da thiazolidinediones.

Shaidar marasa lafiya da likitoci: 4 makonni bayan farawar rashin lafiya, kawai saxagliptin, matakin glycated hemoglobin ya ragu, kuma matakin glucose din plasma mai azumi ya zama ƙasa bayan makonni 2.

An rubuta waɗannan alamomi guda ɗaya a cikin rukuni na marasa lafiya waɗanda aka rubuta su tare da ƙari na metformin, glibenclamide da thiazolidinediones; analogues sunyi aiki a cikin rawar guda.

A cikin dukkan halayen, ba a lura da karuwa a cikin nauyin jikin marasa lafiya ba.

Lokacin amfani da ongliza

An wajabta magunguna ga marasa lafiya da ke dauke da cutar sukari irin ta 2 a cikin irin waɗannan halaye:

Tare da monotherapy tare da wannan magani a hade tare da aiki na jiki da kuma maganin abinci,
Tare da haɗin gwiwa a hade tare da metformin,
A cikin rashin ingancin monotherapy tare da metformin, abubuwan da suka samo asali na sulfonylurea, thiazolidinediones a matsayin ƙarin magunguna.

Duk da gaskiyar cewa maganin onglise ya halarta karatu da gwaje-gwaje da yawa, sake dubawa game da shi galibi tabbatacce ne, za'a iya fara amfani da magani a ƙarƙashin kulawar likita.

Contraindications wa yin amfani da onglise

Tun da miyagun ƙwayoyi suna tasiri sosai akan aikin beta da ƙwayoyin alpha, suna ƙarfafa aikin su sosai, koyaushe ba za'a iya amfani dashi ba. Magungunan yana contraindicated:

A lokacin haihuwa, haihuwa da lactation.
Matasa 'yan kasa da shekara 18.
Marasa lafiya tare da nau'in 1 na sukari mellitus (aikin ba a yi nazari ba).
Tare da insulin far.
Tare da ketoacidosis mai ciwon sukari.
Marasa lafiya tare da rashin haƙuri na galactose.
Tare da hankalin mutum ga kowane ɓangaren magungunan.

A cikin akwati bai kamata a yi watsi da umarnin magani ba. Idan akwai shakku game da amincin amfanin sa, to sai a zaɓi hanyoyin hana analog ko kuma wata hanyar magani.

Siyarda da shawarar

Ana gudanar da Onglisa a baki, ba tare da ambaton abinci ba. Matsakaicin da aka ba da shawarar maganin yau da kullun shine 5 MG.

Idan ana aiwatar da maganin haɗin gwiwa, ana amfani da maganin yau da kullun na saxagliptin, sashi na matakan metformin da abubuwan da ke haifar da maganin sulfonylurea dabam.

A farkon haɗuwa da magani ta amfani da metformin, sashi na magungunan zai zama kamar haka:

Onglisa - 5 MG kowace rana,
Metformin - 500 MG kowace rana.

Idan an lura da rashin dacewar yanayin, ya kamata a daidaita sashi na metformin, yana ƙaruwa.

Idan, saboda kowane dalili, an rasa lokacin shan maganin, mai haƙuri yakamata ya ɗauki kwaya da wuri-wuri. Ba shi da mahimmanci a ninka sau biyu a rana sau biyu.

Ga marasa lafiya waɗanda ke da rauni na koda game da shi azaman cuta mai haɗari, ba lallai ba ne don daidaita sashi na onglise. Tare da dysfunction na koda na matsakaici kuma mai tsanani na onglis ya kamata a ɗauka a cikin adadi kaɗan - 2.5 mg sau ɗaya a rana.

Idan anyi hemodialysis, ana shan onglisa bayan karshen zaman. Har yanzu ba a bincika sakamakon saxagliptin ba a cikin marasa lafiyar da ke fama da ciwon dijital ba. Saboda haka, kafin fara magani tare da wannan magani, yakamata a gudanar da cikakken kima akan aikin koda.

Tare da gazawar hanta, za'a iya samarda onglise lafiya a cikin matsakaiciyar maganin da aka nuna - 5 MG kowace rana. Don maganin tsofaffi marasa lafiya, ana amfani da onglise iri ɗaya. Amma ya kamata a tuna cewa hadarin haɓaka ƙarancin haɓaka a cikin wannan rukuni na masu ciwon sukari ya fi hakan yawa.

Babu sake dubawa ko nazarin hukuma game da tasirin maganin a kan marasa lafiya da ke ƙasa da shekaru 18. Sabili da haka, ga matasa masu fama da ciwon sukari na 2, an zaɓi analogues tare da wani sashi mai aiki.

Ana buƙatar rage ƙwayar ƙwayar onglise idan an sanya magani a lokaci guda tare da masu hanawa. Wannan shi ne:

ketoconazole,
Sankasari,
atazanavir
indinavir
igraconazole
nelfinavir
ritonavir
saquinavir da telithromycin.

Don haka, matsakaicin yawan maganin yau da kullun shine 2.5 MG.

Siffofin lura da mata masu juna biyu da tasirinsu

Ba a yi nazarin yadda miyagun ƙwayoyi ke shafar lokacin daukar ciki ba, kuma ko yana iya shiga cikin madarar nono, saboda haka, ba a sanya maganin ba lokacin haihuwar da ciyar da jariri. An ba da shawarar yin amfani da wasu analogues ko don dakatar da shayarwa.

Yawancin lokaci, bin sigogi da shawarwari na maganin hadewar, ana yarda da maganin sosai, a cikin mafi yawan lokuta, kamar yadda sake dubawa suka tabbatar, ana iya lura da masu zuwa:

Amai
Ciwon ciki,
Ciwon kai
Samuwar cututtukan cututtukan cututtuka na hanji na sama,
Cututtukan cututtukan cututtukan ƙwayar cuta.

Idan akwai alamun guda ɗaya ko fiye, ya kamata ku dakatar da maganin ko kuma daidaita sashi.

Dangane da sake dubawa, ko da an yi amfani da onglise na dogon lokaci a cikin adadin da ya wuce lokacin da aka ba da shawarar sau 80, ba a lura da alamun guba ba. Don cire miyagun ƙwayoyi daga jiki idan akwai yiwuwar maye, ana amfani da hanyar geomdialysis.

Me kuma ya kamata sani

Ba a sanya Onglis da insulin ko a cikin sau uku na maganin tare da metformin da thiazolididones, tunda ba a gudanar da nazarin hulɗar su ba. Idan mai haƙuri yana shan wahala daga matsakaici zuwa gazawar ƙididdigar tazara, ya kamata a rage sashi na yau da kullun. Masu ciwon sukari da ke fama da rashin lafiyar koda suna buƙatar kulawa da kulawa koyaushe game da yanayin kodan yayin jiyya.

An kafa shi ne cewa abubuwan da ke haifar da sulfanilurea na iya tsokani yawan zubar jini. Don hana haɗarin hypoglycemia, sashi na sulfanilurea a hade tare da maganin onglise ya kamata a daidaita. Wato, an rage.

Idan mai haƙuri yana da tarihin rashin damuwa ga kowane iri mai kama da DPP-4 inhibitors, ba a sanya takagliptin ba. Amma game da aminci da tasirin magani na tsofaffi marasa lafiya (fiye da shekaru 6) tare da wannan magani, babu gargadi a wannan yanayin. Onglisa an yarda da shi kuma yana aiki kamar yadda yake a cikin marasa lafiya matasa.

Tunda samfurin ya ƙunshi lactose, bai dace ba ga waɗanda ke da rashin haƙuri a cikin wannan abun, rashi lactose, glucose-galactose malabsorption.

Sakamakon magani a cikin ikon tuki motocin da sauran kayan aiki waɗanda ke buƙatar jan hankali da yawa ba a yi nazarin su ba.

Babu contraindications kai tsaye zuwa tuki mota, amma ya kamata a tuna cewa daga cikin sakamako masu illa da ciwon kai lura.

Yin hulɗa tare da wasu kwayoyi

Dangane da bincike na asibiti, haɗarin hulɗa tsakanin onglises da wasu kwayoyi, idan an ɗauka lokaci guda, ƙanƙane ne.

Masana kimiyya ba su kafa yadda shan sigari, shan giya, amfani da magungunan homeopathic, ko abincin abinci ke shafar tasirin maganin ba, saboda karancin bincike a wannan fannin.

Formaddamar da tsari da abun da ke ciki

Hanyar sakin sakin Onglis shine allunan da aka sanya a fim: zagaye, biconvex, ana amfani da rubutaccen zane tare da fenti mai launin shuɗi, 2.5 MG kowane - daga haske zuwa launin rawaya, rubutu "2.5" a gefe guda, da kuma “ 4214 ", 5 MG kowane - ruwan hoda, a gefe ɗaya rubutun" 5 ", a gefe guda -" 4215 "(inji mai kwakwalwa 10. A cikin blisters, a cikin kwali na kwali 3 blisters).

Abun ciki 1 kwamfutar hannu:

abu mai aiki: saxagliptin (a cikin nau'in saxagliptin hydrochloride) - 2.5 ko 5 mg,
abubuwan taimako: lactose monohydrate - 99 mg, microcrystalline cellulose - 90 mg, croscarmellose sodium - 10 mg, magnesium stearate - 1 mg, 1M bayani na hydrochloric acid - a wadatacce mai yawa,
harsashi: Opadry II fari (polyvinyl barasa - 40%, titanium dioxide - 25%, macrogol - 20,2%, talc - 14.8%) - 26 MG, Opadry II rawaya (don Allunan 2.5 MG) barasa polyvinyl - 40%, titanium dioxide - 24.25%, macrogol - 20,2%, talc - 14.8%, farar baƙin ƙarfe oxide yellow (E172) - 0.75% - 7 MG, Opadry II ruwan hoda (don Allunan 5 MG) polyvinyl barasa - 40%, titanium dioxide - 24.25%, macrogol - 20,2%, talc - 14.8%, baƙin ƙarfe baƙin ƙarfe jan (E172) - 0.75% - 7 mg,
tawada: Opacode shudi - (45% shellac a cikin ethyl barasa - 55.4%, FD&C Blue # 2 / indigo carmine aluminum pigment - 16%, n-butyl barasa - 15%, propylene glycol - 10.5%, isopropyl barasa - 3% , 28% ammonium hydroxide - 0.1%) - a cikin wadataccen adadi.

Pharmacodynamics

Saxagliptin mai ƙarfi ne mai zaɓar mai sauya dipeptidyl peptidase-4 (DPP-4) mai hanawa. A cikin nau'in 2 na ciwon sukari na mellitus, gudanarwarsa yana haifar da dakatar da ayyukan aikin enzyme DPP-4 na tsawon awanni 24. Bayan shiga glucose, hanawar DPP-4 yana haifar da karuwa sau biyu a cikin polypeptide glucose-dogara insulinotropic polypeptide (HIP) da glucagon-kamar peptide-1 (GLP-1), karuwar amsawar kwayar glucose-dogara da kwayar glucagon, wanda ke haifar da karuwar taro C-peptide da insulin.

Rage ƙaddamar da glucagon daga ƙwayoyin ƙwayar ƙwayar tsoka da ƙaddamar da insulin ta hanyar ƙwayoyin beta na pancreatic yana haifar da raguwa a cikin azumin postprandial na glycemia da glycemia.

Sakamakon binciken da aka sarrafa mutum-wuri, an gano cewa shan Onglisa ya ci gaba tare da wani babban ci gaba na ilimin jini na jini (GPN), hawan jini na jini (HbA)_1c) da plasma na jini bayan jini (BCP) jini idan aka kwatanta da sarrafawa.

Marasa lafiya waɗanda ba su sami damar cimma matakin glycemic matakin lokacin shan saxagliptin kamar yadda monotherapy an kuma haɗu da metformin, thiazolidinediones ko glibenclamide. Lokacin ɗaukar 5 MG na saxagliptin, raguwa a cikin HbA_1c lura bayan makonni 4, GPN - bayan makonni 2. A cikin marasa lafiyar da suka karɓi saxagliptin a hade tare da metformin, thiazolidinediones ko glibenclamide, an lura da raguwa iri ɗaya.

A bango daga ɗaukar Onglisa, ba a kula da karuwa a cikin nauyin jikin mutum ba. Tasirin saxagliptin akan bayanan lipid yayi kama da na placebo.

Pharmacokinetics

A cikin masu ba da agaji da lafiya da kuma a cikin marasa lafiya da ke da nau'in ciwon sukari na 2, ana lura da irin wannan magunguna na likagliptin da babban metabolite.

Abun bayan sarrafawar bakin a kan komai a ciki yana cikin hanzari. Nasara C_max (matsakaici mafi yawa na abu) na saxagliptin da babban metabolite a cikin plasma yana faruwa awanni 2 da 4 hours, bi da bi. Tare da karuwa na kashi, karuwa gwargwado a C_max da kuma AUC (yanki a ƙarƙashin ɓoye lokaci-lokaci) na duka abu da babban metabolite. Bayan kashi ɗaya na 5 MG na saxagliptin ta masu hidimar lafiya, matsakaicin ƙimar C_max saxagliptin da babban metabolite a cikin plasma sun kasance 24 ng / ml da 47 ng / ml, ƙimar AUC sun kasance 78 ng × h / ml da 214 ng × h / ml, bi da bi.

Matsakaicin tsayi na ƙarshe na T_1/2 (rabin rayuwa) na saxagliptin kuma babban aikin shi shine tsawan awa 2.5 da awoyi 3.1, bi da bi, matsakaicin darajar hanawar T_1/2 Plasma DPP-4 - 26,9,26. Haramcin aikin plasma DPP-4 na aƙalla awanni 24 bayan ɗaukar saxagliptin yana da alaƙa da babban kusancinta na DPP-4 da ɗaukar madaidaiciya zuwa gare ta. M cumlation na abu da babban metabolite a cikin dogon hanya tare da mita na gudanar da 1 lokaci a rana ba a lura. Dogarowar warwarewar saxagliptin da babban metabolite dinsa a kullun da tsawon lokacin jiyya lokacin shan magani 1 lokaci kowace rana a cikin kewayon kashi na 2.5-400 mg na kwanaki 14.

Bayan gudanarwar baka, kasa da kashi 75% na kashin da aka dauka yana shanshi. Cin abinci a kan pharmacokinetics na saxagliptin ba shi da tasiri sosai. Manyan abinci mai mai yawa suna tasiri ga C_max ba shi da wani abu, amma ƙimar AUC idan aka kwatanta da yin azumin ƙaruwa da kashi 27%. Lokacin shan miyagun ƙwayoyi tare da abinci, idan aka kwatanta da azumi, lokacin isa zuwa C yana ƙaruwa game da minti 30_max. Wadannan canje-canjen ba su da mahimmancin asibiti.

Saxagliptin da babban metabolite dinsu suna ɗaure sunadarai na dan kadan. A wannan batun, ana iya ɗauka cewa tare da canje-canje a cikin tsarin furotin na ƙwayoyin jini wanda aka lura da shi a cikin renal ko hepatic insufficiency, rarraba saxagliptin ba zai sami canje-canje masu mahimmanci ba.

Abun yana metabolized galibi tare da halartar cytochrome P450 3A4 / 5 isoenzymes (CYP 3A4 / 5). A wannan yanayin, an kafa babban metabolite mai aiki, sakamako mai hanawa wanda ya dace da DPP-4 ya zama sau 2 mafi rauni fiye da na saxagliptin.

Saxagliptin da bile da fitsari an keɓe su. Matsakaicin tsabtace dan asalin abu shine kusan 230 ml / min, matsakaiciyar matattarar duniya shine kusan 120 ml / min. Enaladdamar da hukunci don babban metabolite yana daidai da matsakaiciyar ƙimar ƙirar ƙasa.

AUimar AUC ta saxagliptin da babban metabolite tare da gazawar ƙarancin ƙarancin wucin gadi shine 1.2 da 1.7 sau mafi girma, bi da bi, fiye da marasa lafiya da keɓaɓɓen aikin renal. Wannan ƙaruwa a cikin ƙimar AUC ba shi da mahimmanci a asibiti, kuma ba za a yi gyaran fuska ba.

A cikin gazawar matsakaici / mummunan lalacewa, har ma a cikin marasa lafiya da ke fama da cutar sankara, ƙimar AUC na kayan da babban metabolite ya kasance 2.1 da 4.5 sau mafi girma, bi da bi. A wannan batun, kashi na yau da kullun don wannan rukuni na marasa lafiya kada ya wuce 2.5 MG a cikin kashi 1. A cikin yanayin rashin aiki mara nauyi, ba a gano mahimman canje-canje na asibiti a cikin magunguna na saxagliptin kuma, saboda haka, daidaita sashi ba lallai ba ne.

Musamman bambance-bambance a cikin pharmacokinetics na saxagliptin a cikin marasa lafiya 65-80 shekara idan aka kwatanta da marasa lafiya na ƙaramin shekaru ba a gano. Duk da gaskiyar cewa ba a buƙatar daidaita sashi na adadin wannan rukuni na marasa lafiya, yana da mahimmanci a la'akari da babban yiwuwar raguwa a aikin renal.

Alamu don amfani

An wajabta Onglisa don magance nau'in ciwon sukari na 2 na mellitus a matsayin ƙarin hanyoyin motsa jiki da abinci don inganta sarrafa glycemic.

Ana iya tsara maganin kamar haka:

monotherapy
fara hadewar jiyya tare da metformin,
ban da monotherapy tare da thiazolidinediones, metformin, abubuwan asali na sulfonylurea a cikin yanayin rashin isasshen kulawar glycemic yayin irin wannan jiyya.

Umarnin don amfani da Onglises: hanya da sashi

Onglisa ya sha ta baki, ba tare da la'akari da cin abincin ba.

Ganin da aka bada shawarar shine 5 MG a cikin kashi 1.

Lokacin gudanar da aikin haɗin gwiwa, ana amfani da Onglisa tare da metformin, sulfonylureas ko thiazolidinediones.

Lokacin fara maganin haɗin gwiwa tare da metformin, farkon maganin yau da kullun shine 500 MG. A yanayin rashin isasshen amsa, ana iya ƙara girma.

Idan an rasa kashi na Onglisa, dole ne a ɗauka da wuri-wuri, koyaya, bai kamata a ɗauki kashi biyu cikin awa 24 ba.

Matsayi na yau da kullun ga marasa lafiya da matsakaici / lalacewa na kasawa mai lalacewa (tare da keɓantaccen keɓaɓɓen ≤ 50 ml / min), da kuma ga marasa lafiya akan maganin hemodialysis, shine 2.5 MG a cikin kashi 1. Ya kamata a dauki Ongliz bayan ƙarshen zaman hemodialysis. Ba a yi amfani da maganin ba a cikin marasa lafiya akan maganin tsinkaye na ciki. Kafin farawa / lokacin jiyya, ana bada shawara don kimanta aikin koda.

Yawan shawarar da aka bayar na Onglisa yau da kullun lokacin da aka haɗu tare da indinavir, nefazodone, ketoconazole, atazanavir, ritonavir, clarithromycin, itraconazole, nelfinavir, saquinavir, telithromycin da sauran masu hana CYP 3A4 / 5 inhibitors shine 2.5 mg.