Onglisa: ndemanga pakugwiritsa ntchito mankhwalawa, malangizo

Onglisa ndi mankhwala a odwala matenda ashuga, chophatikiza chomwe ndi saxagliptin. Saxagliptin ndi mankhwala wovomerezeka pochizira matenda amishuga a 2.

Pasanathe maola 24 mutakhazikitsa, amalepheretsa enzyme DPP-4. Kulepheretsa kwa enzyme mukamayanjana ndi glucose kumawonjezeka ndi 2P3 kuchuluka kwa glucagon-ngati peptide-1 (apa GLP-1) ndi shuga wodalira glucose-HIP, kumachepetsa kuchuluka kwa glucagon ndikuthandizira kuyankha kwa maselo a beta.

Zotsatira zake, zomwe zimakhala ndi insulin ndi C-peptide m'thupi zimakulanso. Insulin itatulutsidwa ndi ma cell a beta a kapamba ndi glucagon kuchokera ku maselo a alpha, glycemia wothamanga ndi glycemia wa postprandial amachepetsa kwambiri.

Kugwiritsa ntchito bwino kwa saxagliptin mu Mlingo wosiyanasiyana komwe kwaphunziridwa mosamala bwino m'maphunziro asanu ndi amodzi olamulidwa ndi placebo, omwe adakhudza odwala 4148 omwe adapezeka ndi mtundu wachiwiri wa matenda a shuga.

M'maphunzirowa, kusintha kwamphamvu kwa glycated hemoglobin, kusala kwamadzi am'magazi komanso glucose wa postprandial adadziwika. Odwala omwe saxagliptin monoprint sanabweretse zotsatira zomwe akuyembekezeredwa adapangidwanso mankhwala monga metformin, glibenclamide ndi thiazolidinediones.

Umboni wa odwala ndi madokotala: masabata 4 pambuyo pa kuyamba kwa mankhwalawa, saxagliptin yokha, kuchuluka kwa hemoglobin ya glycated kunachepa, ndipo kuchuluka kwa glucose kosala kudya kunatsika pambuyo pa masabata awiri.

Zizindikiro zomwezo zidalembedwa mu gulu la odwala omwe adalembedwa mankhwala ophatikiza ndi kuwonjezeredwa kwa metformin, glibenclamide ndi thiazolidinediones; analogues amagwira ntchito momwemo.

M'nthawi zonsezi, kuwonjezeka kwa odwala sikunachitike.

Mukamagwiritsa ntchito ongliza

Mankhwala amathandizidwa ndi odwala omwe ali ndi matenda amtundu wa 2 matenda ngati awa:

Ndi monotherapy ndi mankhwalawa limodzi ndi zolimbitsa thupi komanso zakudya,
Ndi mankhwala othandizira osakanikirana ndi metformin,
Palibe mphamvu ya monotherapy ndi metformin, mankhwala a sulfonylurea, thiazolidinediones ngati mankhwala ena.

Ngakhale kuti mankhwala osokoneza bongo akhala akupanga kafukufuku ndi mayeso angapo, kuwunika za izi ndizabwino kwambiri, chithandizo chokhacho chitha kuyamba kuyang'aniridwa ndi dokotala.

Contraindative pa ntchito yopanda tanthauzo

Popeza mankhwalawa amakhudza magwiridwe antchito a beta ndi ma alpha, amalimbikitsa kwambiri ntchito yawo, sangathe kugwiritsidwa ntchito nthawi zonse. Mankhwala okhazikika:

Pa nthawi yoyembekezera, pobereka komanso mkaka wa m'mawere.
Achinyamata osakwana zaka 18.
Odwala omwe ali ndi mtundu woyamba wa matenda a shuga (machitidwe osaphunziridwa).
Ndi mankhwala a insulin.
Ndi matenda ashuga ketoacidosis.
Odwala wobadwa nawo galactose tsankho.
Ndi chidwi cha aliyense pazinthu zilizonse za mankhwala.

Palibe chifukwa chomwe malangizo a mankhwalawo anganyalanyazidwe. Ngati mukukayika za chitetezo chazogwiritsidwa ntchito, ma analog inhibitors kapena njira ina yothandizira ayenera kusankhidwa.

Mlingo Wovomerezeka ndi Kachitidwe

Onglisa amatumizidwa pakamwa, osatchula chakudya. Pafupifupi tsiku lililonse mankhwala ndi 5 mg.

Ngati mankhwala ophatikiza aphatikizidwa, mlingo wa saxagliptin sunasinthike, Mlingo wa metformin ndi zotumphukira za sulfonylurea umatsimikiziridwa mosiyana.

Kumayambiriro kwa kuphatikiza mankhwalawa pogwiritsa ntchito metformin, mlingo wa mankhwalawa ukhale motere:

Onglisa - 5 mg patsiku,
Metformin - 500 mg patsiku.

Ngati zochita zosakwanira zadziwika, mlingo wa metformin uyenera kusintha, umachulukitsidwa.

Ngati, pazifukwa zilizonse, nthawi yakumwa mankhwalawo idasemphana, wodwalayo amwe mapiritsi ake mwachangu. Sikoyenera kuwirikiza kawiri mlingo wa tsiku ndi tsiku.

Kwa odwala omwe ali ndi matenda opatsika pang'ono aimpso, ndikofunikira kuti musinthe mwanjira ina. Ndi kusokonezeka kwa impso kwamitundu yozama komanso yozama ya owlis ayenera kumwedwa m'magawo ang'onoang'ono - 2,5 mg kamodzi patsiku.

Ngati hemodialysis ichitika, onglisa amatengedwa kumapeto kwa gawo. Zotsatira za saxagliptin pa odwala omwe akudwala peritoneal dialysis sizinafufuzidwebe. Chifukwa chake, musanayambe mankhwala ndi mankhwalawa, kuyenera kuchitika kwa impso kuyenera kuchitidwa.

Ndi vuto la chiwindi, kupezeka mwachindunji muyezo wake muyezo - 5 mg patsiku. Zochizira odwala okalamba, zachidziwitso zimagwiritsidwanso ntchito chimodzimodzi. Koma tikumbukire kuti chiopsezo chokhala ndi kulephera kwa aimpso m'gulu lino la odwala matenda ashuga ndiwambiri.

Palibe ndemanga kapena kafukufuku wapadera wazomwe zimachitika chifukwa cha mankhwalawa kwa odwala ochepera zaka 18. Chifukwa chake, kwa achinyamata omwe ali ndi matenda a shuga a mtundu wachiwiri, ma fanizo omwe ali ndi chinthu china chogwira ntchito amasankhidwa.

Kuthandiza mulingo woyenera wofunikanso ndikofunikira ngati mankhwalawo adapangidwira pamodzi ndi mankhwala ochepetsa mphamvu. Izi ndi:

ketoconazole,
madalin,
atazanavir
indinavir
igraconazole
nelfinavir
ritonavir
saquinavir ndi telithromycin.

Chifukwa chake, mlingo woyenera tsiku ndi tsiku ndi 2,5 mg.

Zambiri za chithandizo cha amayi apakati komanso zoyipa

Sizinaphunziridwe momwe mankhwalawa amakhudzira nthawi ya kubereka, komanso ngati amatha kulowa mkaka wa m'mawere, chifukwa chake, mankhwalawa sanalembedwe panthawi yakubala ndi kudyetsa mwana. Ndikulimbikitsidwa kugwiritsa ntchito ma analogu ena kapena kusiya kuyamwitsa.

Nthawi zambiri, kutsatira kuchuluka ndi malingaliro a mankhwala ophatikiza, mankhwalawa amalekeredwa bwino, kawirikawiri, monga ndemanga zimatsimikizira, zotsatirazi zingaoneke:

Kubweza
Gastroenteritis,
Mutu
Mapangidwe matenda opatsirana a chapamwamba kupuma thirakiti,
Matenda opatsirana a genitourinary system.

Ngati pali chizindikiro chimodzi kapena zingapo, muyenera kuyimitsa mankhwalawo kapena kusintha mankhwalawo.

Malinga ndi ndemanga, ngakhale patakhala kuti zosafunikira zimagwiritsidwa ntchito kwa nthawi yayitali mu milingo yopitilira 80, palibe chizindikiro chakupha. Kuchotsa mankhwalawa m'thupi ngati muledzera, njira ya geomdialysis imagwiritsidwa ntchito.

Zina zomwe muyenera kudziwa

Onglis sanalembedwe ndi insulin kapena mankhwala patatu ndi metformin ndi thiazolididones, popeza maphunziro a kuyanjana kwawo sanachitike. Ngati wodwala akudwala pang'ono komanso wamphamvu kulephera kwa impso, mlingo wa tsiku ndi tsiku uyenera kuchepetsedwa. Anthu odwala matenda ashuga omwe ali ndi vuto lofooka laimpso amafunikira kuwunika momwe impso ikuthandizira.

Zinakhazikitsidwa kuti zotumphukira za sulfanilurea zimatha kupangitsa hypoglycemia. Kuti mupewe chiopsezo cha hypoglycemia, mlingo wa sulfanilurea osakanikirana ndi chithandizo cha mankhwala osafunikira uyenera kusinthidwa. Ndiye kuti, kuchepetsedwa.

Ngati wodwala ali ndi mbiri ya hypersensitivity kwa zoletsa zilizonse zofanana za DPP-4, saxagliptin sichosankhidwa. Ponena za chitetezo ndi kuyenera kwa chithandizo cha odwala okalamba (opitilira zaka 6) ndi mankhwalawa, palibe machenjezo pankhaniyi. Onglisa amalekeredwa ndipo amachita chimodzimodzi ndi odwala achinyamata.

Popeza mankhwalawa ali ndi lactose, sioyenera kwa iwo omwe ali ndi vuto lodana ndi chinthuchi, kuperewera kwa lactose, glucose-galactose malabsorption.

Mphamvu ya mankhwalawa pa kuyendetsa magalimoto ndi zida zina zofunikira kwambiri kuti adziyang'anitsitse sizinaphunzire konse.

Palibe zotsutsana mwachindunji poyendetsa galimoto, koma ziyenera kukumbukiridwa kuti pakati pazotsatira zoyipa ndi kupweteka kwa mutu kumadziwika.

Kuchita ndi mankhwala ena

Malinga ndi kafukufuku wazachipatala, chiopsezo cholumikizana pakati pa oslises ndi mankhwala ena, ngati agwiritsidwanso chimodzimodzi, ndi ochepa kwambiri.

Asayansi sanakhazikitse momwe kusuta, kuledzera, kugwiritsa ntchito mankhwala ofooketsa, kapena chakudya chamagulu kumakhudza zotsatira za mankhwalawa, chifukwa cha kusowa kwa kafukufuku m'derali.

Kutulutsa mawonekedwe ndi kapangidwe kake

Mtundu wa kutulutsidwa kwa Onglis ndi mapiritsi okhala ndi mafilimu: ozungulira, biconvex, zolembedwazo zimayikidwa ndi utoto wabuluu, 2.5 mg iliyonse - kuchokera pakuwala mpaka kutalika chikasu, mawu olembedwa "2,5" mbali imodzi, ndi "" 4214 ", 5 mg iliyonse - pinki, mbali ina zolembedwa" 5 ", mbali inayo -" 4215 "(ma PC 10. M'matumba, pamatoni a makatoni 3 matuza).

Piritsi 1:

yogwira mankhwala: saxagliptin (munthawi ya saxagliptin hydrochloride) - 2,5 kapena 5 mg,
othandizira zigawo: lactose monohydrate - 99 mg, cellcrystalline cellulose - 90 mg, croscarmellose sodium - 10 mg, magnesium stearate - 1 mg, 1M yankho la hydrochloric acid - mokwanira,
chipolopolo: Opadry II yoyera (mowa wa polyvinyl - 40%, titaniyumu - 25%, macrogol - 20.2%, talc - 14.8%) - 26 mg, Opadry II wachikasu (mapiritsi 2.5 mg) mowa wa polyvinyl - 40%, titanium dioxide - 24.25%, macrogol - 20.2%, talc - 14.8%, utoto wachitsulo wachikasu (E172) - 0,75% - 7 mg, Opadry II pinki (mapiritsi a 5 mg) mowa wa polyvinyl - 40%, titanium dioxide - 24.25%, macrogol - 20.2%, talc - 14.8%, utoto wa iron utoto wa okosijeni (E172) - 0,75% - 7 mg,
ink: Opacode buluu - (45% shellac mu ethyl mowa - 55.4%, FD&C Blue # 2 / indigo carmine aluminium pigment - 16%, n-butyl mowa - 15%, propylene glycol - 10,5%, isopropyl mowa - 3% , 28% ammonium hydroxide - 0,1% - - zokwanira.

Mankhwala

Saxagliptin ndi njira yosinthira masinthidwe obwezeretsanso a dipeptidyl peptidase-4 (DPP-4). Mtundu wachiwiri wa matenda ashuga, makulidwe ake amatsogolera ku kuponderezedwa kwa ntchito ya DPP-4 kwa maola 24. Pambuyo pakulowetsa shuga, kuletsa kwa DPP-4 kumapangitsa kuti chiwonetsero cha glucose-insulinotropic polypeptide (HIP) cha glucose komanso glucagon chizindikirike, zomwe zimayambitsa kuchuluka kwa glucagon C-peptide ndi insulin.

Kuchepetsa kumasulidwa kwa glucagon ku maselo a pancreatic alpha ndikutulutsa kwa insulin ndi maselo a pancreatic beta kumabweretsa kuchepa kwa kusala kwa postprandial glycemia ndi glycemia.

Zotsatira zamaphunziro oyendetsedwa ndi placebo, zidapezeka kuti kutenga Onglisa akupitiliza kusinthasintha kwakuchuluka kwa plasma glucose (GPN), glycosylated hemoglobin (HbA)_1c) ndi postprandial glucose (BCP) plasma yamagazi poyerekeza ndi kuwongolera.

Odwala omwe sanathe kukwaniritsa cholinga cha glycemic pamene akutenga saxagliptin monga monotherapy amadziwikanso ngati metformin, thiazolidinediones kapena glibenclamide. Mukamamwa 5 mg ya saxagliptin, kuchepa kwa HbA_1c adadziwika pambuyo pa masabata 4, GPN - atatha masabata awiri. Kwa odwala omwe adalandira saxagliptin kuphatikiza ndi metformin, thiazolidinediones kapena glibenclamide, kuchepa kofananako kunawonedwa.

Poyerekeza ndi kumbuyo kwa kutenga Onglisa, kuwonjezeka kwa thupi sikudziwika. Zotsatira za saxagliptin pa lipid mbiri ndizofanana ndi za placebo.

Pharmacokinetics

Mwa odzipereka athanzi komanso odwala omwe ali ndi matenda ashuga a 2, pharmacokinetics yofanana ya saxagliptin ndi metabolite yake yayikulu imawonedwa.

Zinthu pambuyo pakamwa pakamwa yopanda kanthu zimatengedwa mwachangu. Kukwaniritsa C_max (kuchuluka kwa zinthu) saxagliptin ndi metabolite yayikulu m'madzi a m'magazi amapezeka 2 maola ndi maola 4, motero. Ndi kuchuluka kwa mlingo, kuchuluka kwa C_max ndi AUC (dera lomwe lili munthawi yopondera nthawi) ya thunthu ndi metabolite yake yayikulu. Patatha mlingo umodzi wa 5 mg wa saxagliptin ndi anthu odzipereka athanzi, mphamvu ya C_max saxagliptin ndi metabolite yake yayikulu mu plasma inali 24 ng / ml ndi 47 ng / ml, mfundo za AUC zinali 78 ng × h / ml ndi 214 ng × h / ml, motsatana.

Kutalika kwapakati pa T yomaliza_1/2 (theka-moyo) ya saxagliptin ndipo metabolite yake yayikulu ndi maola 2.5 ndi maola 3.1, motere, mtengo wapakati wa zoletsa T_1/2 Plasma DPP-4 - maola 26.9 Kuletsa kwa ntchito ya plasma DPP-4 kwa maola osachepera 24 mutatha saxagliptin kumalumikizidwa ndi mgwirizano wake wapamwamba wa DPP-4 ndipo umakhalapo kwa nthawi yayitali. Kuwerengedwa kowoneka kwazinthu ndi metabolite yake yayitali pakapita nthawi yayitali ndi kuwongolera nthawi 1 patsiku sikuwonetsedwa. Kudalira kwa chilolezo cha saxagliptin ndi metabolite yake yayikulu patsiku tsiku lililonse ndi nthawi yayitali ya mankhwalawa pomwa mankhwalawa 1 nthawi tsiku lililonse muyezo wa 2.5-400 mg kwa masiku 14 sanapezeka.

Pambuyo pakamwa, osachepera 75% ya mankhwalawa amatengedwa. Kudya pa pharmacokinetics ya saxagliptin sikukhudzidwa kwambiri. Zakudya zamafuta kwambiri zimakhudza C_max ilibe chinthu, koma AUC imayerekeza poyerekeza ndi kusala kosala ndi 27%. Mukamamwa mankhwalawo ndi chakudya, kuyerekeza ndi kusala kudya, nthawi yofikira C imawonjezeka pafupifupi mphindi 30_max. Zosintha izi zilibe tanthauzo lakuchipatala.

Saxagliptin ndi metabolite yake yayikulu imamangiriza mapuloteni a seramu pang'ono. Pankhaniyi, titha kuganiza kuti kusintha kwa mapangidwe a seramu yamagazi omwe amawoneka kuti aimpso kapena kwa chiwindi, kugawa kwa saxagliptin sikusintha kwambiri.

Thupi limapukusidwa makamaka ndi gawo la cytochrome P450 3A4 / 5 isoenzymes (CYP 3A4 / 5). Pankhaniyi, metabolite yayikulu imapangidwa, mphamvu yotsitsa yomwe motsutsana ndi DPP-4 imakhala yofooka kawiri kuposa saxagliptin.

Saxagliptin ndi bile ndi mkodzo umachotsedwa. The wamba aimpso chilolezo cha chinthu pafupifupi 230 ml / min, pafupifupi glomerular kusefera ndi pafupi 120 ml / min. Kuvomerezeka kwa metabolite yayikulu ndikufanizira ndi kuchuluka kwa kusefera kwa glomerular.

Mtengo wa AUC wa saxagliptin ndi metabolite yake yofunikira kwambiri yolephera kupweteka kwaimpso ndi 1.2 ndi 1.7 nthawi, motero, kuposa odwala omwe ali ndi vuto laimpso. Kukula kwa mfundo za AUC sikofunikira mwanjira iliyonse, ndipo kusintha kwa mankhwalawa sikuyenera kuchitika.

Kulephera kwapakati / kwambiri kwa aimpso, komanso kwa odwala omwe ali ndi hemodialysis, mfundo za AUC za thunthu ndi metabolite yake yayikulu ndi 2.1 ndi 4.5 pafupipafupi, motsatana. Pankhaniyi, tsiku lililonse mlingo wa gululi la odwala sayenera kupitirira 2,5 mg mu 1 mlingo. Mu vuto la chiwopsezo cha hepatic, kusintha kwakukulu mu pharmacokinetics ya saxagliptin sikunazindikiridwe ndipo, kusintha kwa mankhwalawa sikofunikira.

Kusiyana kwakukulu mu pharmacokinetics ya saxagliptin mu odwala a zaka 65-80 zaka poyerekeza ndi odwala aang'ono sanazindikiridwe. Ngakhale kuti kusintha kwa mankhwalawa sikofunikira pa gulu ili la odwala, ndikofunikira kuti muganizire za kuchepa kwa impso.

Zizindikiro zogwiritsidwa ntchito

Onglisa adalembedwa kuti athandize odwala matenda a shuga 2 ngati njira yowonjezera yochitira masewera olimbitsa thupi komanso zakudya kuti akwaniritse kusintha kwa glycemic.

Mankhwala atha kutumikiridwa motere:

monotherapy
kuyamba kuphatikiza mankhwala ndi metformin,
kuphatikiza pa monotherapy ndi thiazolidatediones, metformin, sulfonylurea zotumphukira milandu ngati akusowa yoyenera glycemic pa chithandizo.

Malangizo ogwiritsira ntchito Onglises: njira ndi mlingo

Onglisa amatengedwa pakamwa, ngakhale chakudya chotani.

Mlingo woyenera ndi 5 mg mu 1 mlingo.

Popanga mankhwala ophatikiza, Onglisa amagwiritsidwa ntchito ndi metformin, sulfonylureas kapena thiazolidinediones.

Mukayamba kuphatikiza mankhwala ndi metformin, mlingo wake woyamba wa tsiku lililonse ndi 500 mg. Pankhani ya yankho losakwanira, iwonjezeke.

Ngati mlingo wa Onglisa wasowa, uyenera kumwedwa mwachangu, komabe, imwani kawiri pasanathe maola 24 sayenera kutero.

Mlingo wa tsiku ndi tsiku wa odwala omwe ali ndi kuchepa kwapakati / kupweteka kwambiri aimpso (omwe ali ndi creatinine chilolezo cha 50 ml / min), komanso kwa odwala omwe ali ndi hemodialysis, ndi 2.5 mg mu mlingo umodzi. Ongliz ayenera kumwedwa atatha gawo la hemodialysis. Kugwiritsa ntchito mankhwalawa kwa odwala pa peritoneal dialysis sikunaphunzire. Musanayambe / munthawi ya chithandizo, tikulimbikitsidwa kuwunika ntchito yaimpso.

Mlingo watsiku ndi tsiku wa Onglisa akaphatikizidwa ndi indinavir, nefazodone, ketoconazole, atazanavir, ritonavir, clarithromycin, itraconazole, nelfinavir, saquinavir, telithromycin ndi zoletsa zina zamphamvu za CYP 3A4 / 5 ndi 2.5 mg.