Onglisa: mankhwala a shuga, ndemanga ndi mapiritsi a mapiritsi

Tsambali limapereka mndandanda wazofanizira zonse za Ongliz mwa kapangidwe kake ndi chisonyezo chogwiritsa ntchito. Mndandanda wama analogi otsika mtengo, mutha kuyerekezeranso mitengo muma pharmacies.

• Analogue wotsika mtengo kwambiri wa Ongliz:Trazenta
• Analogue otchuka kwambiri a Ongliz:Vipidia
• Gulu la ATX: Saxagliptin
• Zosakaniza / yogwira: saxagliptin
  

Mukamawerengera mtengo wake zotupa za Ongliz mtengo wocheperako womwe umapezeka mumndandanda wamapulogalamu omwe amaperekedwa ndi ma pharmacies adaganiziridwa

Popeza mndandanda wamankhwala osokoneza bongo kutengera manambala a mankhwala omwe apemphedwa kwambiri

Analogs mwa chisonyezo ndi njira yogwiritsira ntchito

Kuphatikizika kosiyanasiyana, kungagwirizane mukuwonetsa komanso momwe mungagwiritsire ntchito

Kodi mungapeze bwanji analogue yotsika mtengo ya mankhwala okwera mtengo?

Kuti mupeze chiwonetsero chotsika mtengo cha mankhwala, chofananira kapena chofanana, choyambirira timalimbikitsa kulabadira kapangidwe kake, zomwe ndi zinthu zomwezo zomwe zikugwiritsidwa ntchito ndikuwonetsa. Zomwe zimagwiritsidwanso mosiyanasiyana ndi mankhwalawa zimawonetsa kuti mankhwalawo ndi ofanana ndi mankhwalawo, monga mankhwala ena kapena mitundu ina. Komabe, musaiwale za zovuta zomwe zimagwiritsidwa ntchito ndi mankhwala ofanana, omwe angakhudze chitetezo ndi kugwiranso ntchito. Musaiwale za malangizo a madotolo, kudzipereka nokha kungawononge thanzi lanu, chifukwa chake onani dokotala wanu musanagwiritse ntchito mankhwala.

Malangizo a Onglisa

MALANGIZO
pa kugwiritsa ntchito mankhwalawa
Onglisa

Kutulutsa Fomu
Mapiritsi okhala ndi mafilimu.

Kupanga
Saxagliptin 2.5 ndi 5 mg,
Omwe amathandizira: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, 1 M hydrochloric acid kapena sodium hydroxide solution 1 M, Opadray II yoyera (polyvinyl mowa, titanium dioxide, macrogol (PEG 3350), talc), Opadray wachikasu (mowa polyvinyl, titanium dioxide, macrogol (PEG 3350), talc, utoto wachikasu wachikasu oxide (E172), inki Opacode buluu (chipolopolo mu mowa wa ethyl, FD&C Blue # 2 / indigo carmine aluminium pigment (E132), mowa wa n-butyl, propylene glycol, mowa wa isopropyl, 28% ammonium roksid).

Kulongedza
Mu phukusi la mapiritsi 30.

Zotsatira za pharmacological
ONGLISA - saxagliptin - chosankha champhamvu chopikisana chosinthika cha dipeptidyl peptidase-4 (DPP-4).
Odwala omwe ali ndi mtundu wachiwiri wa matenda ashuga, kuperekera kwa saxagliptin kumachepetsa mphamvu ya enzyme ya DPP-4 pasanathe maola 24. Pambuyo kuyamwa kwa shuga mkamwa, kuyimitsidwa kwa DPP-4 kumapangitsa kuti chiwonetsero cha glucagon-peptide-1 chiziwonjezeke. polypeptide (HIP), kuchepa kwa kuchuluka kwa glucagon ndikuwonjezereka kwa mayankho omvera a shuga a maselo a beta, zomwe zimapangitsa kuti chiwopsezo cha insulin ndi C-peptide chiwonjezeke.
Kutulutsidwa kwa insulin ndi masamba a pancreatic beta ndi kuchepa kwa kutulutsidwa kwa glucagon kuchokera ku maselo a pancreatic alpha kumabweretsa kuchepa kwa glycemia ndi postprandial glycemia.
Kuchita bwino ndi chitetezo cha saxagliptin mutatengedwa mu Mlingo wa 2,5 mg, 5 mg ndi 10 mg 1 nthawi / adawerengera maphunziro asanu ndi awiri akhungu, owongoleredwa ndi placebo mwa odwala 4148 omwe ali ndi matenda a shuga a 2.Kumwa mankhwalawo limodzi ndi kuwongolera kwakukulu mu glycosylated hemoglobin (HbA1c), glucose ofulumira (GPN) ndi postprandial glucose (PPG) plasma wamagazi poyerekeza ndi kuwongolera.
Odwala omwe mulingo wa glycemic womwe sakanatha kutero sukwaniritsidwa ndi saxagliptin monga monotherapy adapangidwanso mankhwala a metformin, glibenclamide kapena thiazolidinedione. Mukamamwa saxagliptin pa mlingo wa 5 mg, kuchepa kwa HbA1c kumawonedwa patatha milungu 4 ndi GPN pambuyo masabata awiri. Pagulu la odwala omwe amalandila saxagliptin osakanikirana ndi metformin, glibenclamide kapena thiazolidinediones, kuchepa kwa HbA1c kumawonedwanso pambuyo pa masabata 4 ndi GPN pambuyo pa masabata awiri.
Zotsatira za saxagliptin pa lipid mbiri ndizofanana ndi za placebo. Pa mankhwala ndi saxagliptin palibe kuwonjezeka kwa thupi kunadziwika.

Onglisa, zikugwiritsira ntchito
Type 2 shuga mellitus kuwonjezera pa zakudya ndi masewera olimbitsa thupi kuti muthe kuyendetsa bwino glycemic control:
- monotherapy,
- kuyambitsa kuphatikiza mankhwala ndi metformin,
- zowonjezera pa monotherapy ndi metformin, thiazolidinediones, sulfonylurea, zotumphukira, pakalibe chitetezo chokwanira cha glycemic mu mankhwalawa.

Contraindication
- lembani matenda ashuga 1 (musawerenge)
- gwiritsani ndi insulin (yophunziridwa),
- matenda ashuga ketoacidosis,
- kobadwa nako galactose tsankho, lactase akusowa ndi shuga-galactose malabsorption,
- mimba
- kuyamwa,
- wazaka mpaka 18 (chitetezo ndi zomwe sizinawerenge),
- kuchuluka kwa chidwi chamtundu uliwonse wa mankhwala.

Mlingo ndi makonzedwe
Mankhwala ndi mankhwala pakamwa, ngakhale kudya zakudya.
Ndi monotherapy, mlingo woyenera wa saxagliptin ndi 5 mg 1 nthawi / tsiku.
Kuphatikiza mankhwala, muyezo wa saxagliptin ndi 5 mg 1 nthawi / tsiku limodzi ndi metformin, thiazolidinediones kapena sulfonylureas.
Mukayamba kuphatikiza mankhwala ndi metformin, muyezo wa saxagliptin ndi 5 mg 1 nthawi / tsiku, mlingo woyambirira wa metformin ndi 500 mg / tsiku. Potha kuyankha kosakwanira, mlingo wa metformin ungathe kuchuluka.
Ngati mungadumphe kumwa Ongliz ®, muyenera kumwa piritsi lomwe linasowa mukangokumbukira izi, koma musamwe mankhwalawa tsiku limodzi.
Kwa odwala omwe ali ndi vuto lochepa la impso (CC> 50 ml / min), kusintha kwa mlingo sikofunikira. Kwa odwala omwe ali ndi kuchepa kwapakati kapena kwambiri aimpso (CC ≤ 50 ml / min), komanso kwa omwe ali ndi hemodialysis, mlingo wolimbikitsidwa wa Ongliz® ndi 2.5 mg 1 nthawi / tsiku. Mankhwala ayenera kumwedwa kumapeto kwa gawo la hemodialysis. Kugwiritsa ntchito saxagliptin mwa odwala omwe akupanga peritoneal dialysis sikunaphunzire. Musanayambe chithandizo ndi saxagliptin komanso munthawi ya chithandizo, tikulimbikitsidwa kuwunika ntchito yaimpso.
Pankhani ya chiwindi ntchito, kufatsa, wowerengeka komanso wamphamvu mlingo sayenera.
Kusintha kwa Mlingo kwa okalamba sikofunikira. Komabe, posankha mlingo, muyenera kukumbukira kuti m'gulu lino la odwala, kuchepa kwa impso kumachitika.
Chitetezo ndi kufunika kwa mankhwalawa kwa odwala ochepera zaka 18 sizinaphunzire.
Mukamagwiritsidwa ntchito ndi CYP 3A4 / 5 zoletsa zamphamvu, monga ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir ndi telithromycin, mlingo woyenera wa Ongliz® ndi 2.5 mg 1 nthawi / tsiku

Mimba komanso kuyamwa
Chifukwa chakuti kugwiritsidwa ntchito kwa saxagliptin pa nthawi yomwe ali ndi pakati sikunaphunzire, mankhwalawa sayenera kulembedwa panthawiyi.
Sizikudziwika ngati saxagliptin idutsa mkaka wa m'mawere.Chifukwa chakuti kuthekera kwa kulowa kwa saxagliptin mkaka wa m'mawere sikunathetsedwe, kuyamwitsa kuyenera kuyimitsidwa kwa nthawi yopereka chithandizo ndi saxagliptin kapena chithandizo chamankhwala ziyenera kusiyidwa, poganizira kuchuluka kwa chiwopsezo cha mwana komanso phindu la mayi.

Zotsatira zoyipa
Matenda opumira kwambiri a m'mapapo
Matenda amitsempha
Gastroenteritis
Sinusitis
Kubweza
Mutu.

Malangizo apadera
Kugwiritsa ntchito kwa mankhwala Onglisa® osakanikirana ndi insulin, komanso mankhwalawa patatu ndi metformin ndi thiazolidinediones kapena metformin ndi zotumphukira za sulfonylurea, sizinaphunzire.
Odwala ndi mkhutu aimpso ntchito.
Kusintha kwa Mlingo kumalimbikitsidwa kwa odwala omwe ali ndi pakati komanso aimpso kwambiri, komanso odwala hemodialysis. Musanayambe mankhwala ndipo munthawi ya chithandizo ndi mankhwalawa, tikulimbikitsidwa kuyesa ntchito yaimpso.
Gwiritsani ntchito limodzi ndi mankhwala omwe angayambitse hypoglycemia.
Zotsatira za sulfonylureas zimatha kuyambitsa hypoglycemia, motero, kuchepetsa chiopsezo cha hypoglycemia pogwiritsa ntchito Ongliz®, kuchepetsa kwa sulfonylureas kungafunike.
Hypersensitivity zimachitika.
Mankhwalawa sayenera kutumizidwa kwa odwala omwe ali ndi vuto lalikulu la hypersensitivity akamagwiritsa ntchito zina za DPP-4 zoletsa.
Odwala okalamba.
Malinga ndi kafukufuku wa zamankhwala, zothandiza komanso zodzitetezera mwa odwala omwe ali ndi zaka 65 ndi akulu sanasiyane ndi zofananira zomwezo mwa odwala omwe ali ndi zaka zochepa. Komabe, chidwi chowonjezeka cha saxagliptin mwa odwala ena okalamba sichingaletsedwe.
Saxagliptin ndi metabolite yayikulu imachotsedwa pang'ono ndi impso, choncho ziyenera kukumbukiridwa kuti odwala okalamba, kuchepa kwa impso ndizotheka. Onglisa® ili ndi lactose. Odwala obadwa nawo galactose tsankho, lactase akusowa ndi shuga-galactose malabsorption sayenera kumwa mankhwala.

Kukopa pa kuyendetsa magalimoto ndi kayendedwe kazinthu.
Kafukufuku wokhudzana ndi saxagliptin pakutha kuyendetsa magalimoto ndi kayendedwe ka kayendedwe sanachitike. Kumbukirani kuti saxagliptin ikhoza kuyambitsa chizungulire.

Kuyanjana kwa mankhwala osokoneza bongo
Kusanthula kwa zidziwitso zamankhwala azachipatala kumawonetsa kuti chiopsezo cha kugwirana kwakukulu kwa saxagliptin ndi mankhwala ena akagwiritsidwa ntchito palimodzi ndizochepa.
Metabolism ya Saxagliptin imayang'aniridwa makamaka ndi cytochrome P450 3A4 / 5 isoenzyme system (CYP3A4 / 5). Kafukufuku wa in vitro awonetsa kuti saxagliptin ndi metabolite yake yayikulu sikuletsa CYP 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 ndi 3A4 isoenzymes ndipo osalimbikitsa CYP 1A2, 2B6, 2C9, ndi 3A4 isoenzymes. Kafukufuku wokhudzana ndi odzipereka athanzi, magawo a pharmacokinetic a saxagliptin ndi metabolite yake yayikulu sanasinthe kwambiri motsogozedwa ndi metformin, glibenclamide, pioglitazone, digoxin, simvastatin, diltiazem, ketoconazole, omeprazole, kuphatikiza kwa aluminium hydroxide, ndi magnesium hydroxide, Saxagliptin sasintha kwambiri magawo a pharmacokinetic a metformin, glibenclamide, pioglitazone, digoxin, simvastatin, diltiazem kapena ketoconazole.
Zotsatira za ma CYP 3A4 / 5 isoenzymes pa pharmacokinetics ya saxagliptin sizinaphunzire. Komabe, kuphatikiza kwa saxagliptin ndi ma inducers a CYP 3A4 / 5 isoenzymes, monga carbamazepine, dexamethasone, phenobarbital, phenytoin ndi rifampicin, kungayambitse kuchepa kwa kuchuluka kwa saxagliptin mu plasma ndikuwonjezera kuchuluka kwa metabolite yake yayikulu.Kafukufuku wazomwe zimachitika pakusuta, zakudya, mankhwala owonjezera azakumwa, ndi kumwa mowa pa saxagliptin sanaphunzirepo.

Bongo
Zizindikiro za kuledzera sizinafotokozeredwe kwa nthawi yayitali kugwiritsa ntchito mankhwalawa mpaka mpaka 80 kuposa momwe analimbikitsira.
Chithandizo: cha bongo, mankhwala a chithandizo ayenera kugwiritsidwa ntchito. Saxagliptin ndi metabolite yake yayikulu imapukusidwa ndi hemodialysis (kuchuluka kwa excretion: 23% ya mlingo mu maola 4).

Malo osungira
Kutentha kopitilira 30 ° C

Onglisa: malangizo ogwiritsira ntchito, ndemanga, kuchuluka kwake

Ndi kupitilira kwa matenda a shuga a 2, endocrinologist ayenera kusankha mankhwalawa. Amakulolani kuti muchepetse kuchuluka kwa shuga m'magazi. Chimodzi mwa zida izi ndi Onglisa. Musanagule, ndikofunika kuti odwala adziwe zofunikira za mankhwalawa. Malangizo ogwiritsira ntchito Onglises, analogues, ndemanga ndi mtengo - odwala matenda ashuga ayenera kukhala ndi chidwi ndi chilichonse.

Kuphatikizika kwa malonda ndi mawonekedwe omasulidwa

Gawo lothandiza kwambiri la Onglisa ndi saxagliptin hydrochloride. Ichi ndi mankhwala a hypoglycemic: dipeptidyl peptidase-4 inhibitor (DPP-4).

Chogulitsacho chimapezeka monga mawonekedwe a mapiritsi, omwe amaphatikizidwa ndi filimu. Pogulitsa mutha kupeza "Onglizu" ndi mlingo wa mankhwala 2,5 ndi 5 mg. Mapiritsiwa amadzaza matuza, amadzagulitsidwa m'mapaketi: chilichonse chimakhala ndi matuza atatu.

Mankhwalawa amadziwika pansi pa INN (dzina lopanda tanthauzo) la saxagliptin.

Zotsatira zamatsenga

Mukamamwa othandizira a hypoglycemic, ntchito ya enzyme DDP-4 imapanikizika kwa maola 24. Mukamamwa shuga, kuchuluka kwa GLP-1 ndi GUI kumawonjezeka katatu. Nthawi yomweyo, kuchuluka kwa glucagon kumachepa, kuyankha kochokera m'magazi a beta kumawonjezeka. Chifukwa cha machitidwe awa, kuchuluka kwa C-peptide ndi insulin kumawonjezeka.

Insulin ikamasulidwa ku kapamba (maselo ake apadera a beta), ndikuchepetsa njira yotulutsidwa kwa glucagon kuchokera ku maselo a alpha, kumachepa kudya glycemia atatha kudya.

Chitetezo ndi mphamvu ya saxagliptin adayesedwa m'maphunziro 6 olamulidwa ndi placebo mwa odwala omwe ali ndi matenda a shuga a 2. Opirally, zidapezeka kuti glycated hemoglobin, kusala magazi ndimminye ndikatha kudya zakudya zonse zimasintha.

Saxaliptin pambuyo makonzedwe mofulumira odzipereka mu m'mimba thirakiti, pazipita ndende zimawonedwa pambuyo 2 mawola (waukulu metabolite - 4) pambuyo makonzedwe. Kuposa 75% ya mlingo wotengedwa umamwa. Yogwira ntchito imachotsedwa ndi ndulu ndi mkodzo.

Mndandanda wazisonyezo

Chida "Onglisa" chitha kulembedwera matenda ashuga, omwe amapangidwa molingana ndi mtundu 2. Mankhwala amatchulidwa ngati cholumikizira glycemic control pomwe mukudya komanso kuchita masewera olimbitsa thupi.

Lembani mapiritsi awa:

• ngati njira yoperekera chithandizo chamankhwala,
• monga chowonjezera cha monotherapy ndi zotumphukira za sulfonylurea, metformin, thiazolidinediones,
• poyambira kuphatikiza mankhwalawa kuphatikiza ndi metformin.

Ndi zoletsedwa kuyamba kumwa mankhwalawo popanda mankhwala a dokotala.

"Onglizu" imagwiritsidwa ntchito ngati njira yowonjezera kuphatikiza ndimankhwala ena, malinga ngati mankhwalawa omwe amachepetsa shuga sangathe kukwaniritsa bwino glycemic control.

Kusankha kwa Mlingo, njira yogwiritsira ntchito

The endocrinologist ayenera kupereka mankhwala, kutengera momwe wodwalayo alili.

Ndi "Onglise" monotherapy, chisankhocho nthawi zambiri chimapangidwa mokomera mapiritsi a 5 mg. Amatengedwa kamodzi patsiku.

Pogwiritsa ntchito njira zophatikizira zamankhwala, tikulimbikitsidwa kumwa saxagliptin mu 5 mg molumikizana ndi zotumphukira za sulfonylurea, mankhwala a thiazolidinedione, metformin.

Popeza ndaganiza zoyamba kuphatikiza mankhwalawa ndi metformin ndi saxagliptin, ndikofunikira kusankha mankhwalawo kuti chinthu choyamba chimalowa mthupi mu 500 mg, chachiwiri - 5 mg patsiku. Palibe yankho lokwanira, onjezani mlingo wa metformin.

Ngati piritsi lotsatira la Ongliza lasowa, ndiye kuti muyenera kumwa nthawi yomweyo wodwala matenda ashuwalawo akamakumbukira. Koma simungathe kumwa mapiritsi 2 patsiku.

Mlingo wa odwala omwe matenda ashuga amakumana ndi matenda amtunduwu amasankhidwa mosiyana:

• Ndi kulephera kwamphuno, mankhwalawa sasinthidwa,
• Kulephera kwapakati komanso mwamphamvu kwa impso, "Ongliza" imalembedwa 2,5 mg (mapiritsi omwewo akulimbikitsidwa kwa odwala omwe ali ndi hemodialysis),
• kukanika kwa chiwindi sikufuna kusintha kwa mlingo,
• Okalamba odwala ndi yachibadwa impso ntchito, mankhwala zotchulidwa muyezo Mlingo.

Musanamwe mankhwala omwe amapangidwa pamaziko a saxagliptin, muyenera kuyang'ana impso, kuwunika ntchito yawo.

Contraindication

Asanapereke chithandizo cha Onglisa, adotolo ayenera kudziwa mbiri yachipatala ya wodwalayo ndikupeza ngati angamwe mankhwalawa.

Mndandanda wa contraindication umaphatikizapo izi:

• kumvetsetsa kwazigawo zilizonse za malonda,
• galactose tsankho, apezeka shuga-galactose malabsorption kapena kuchepa kwa lactase,
• matenda ashuga ketoacidosis,
• nthawi ya pakati komanso yoyamwitsa.

Mankhwalawa saikidwa kwa odwala omwe ali ndi matenda a shuga 1 omwe amadalira insulin komanso odwala omwe amagwiritsa ntchito insulin pochizira ngakhale T2DM. Muzochitika izi, kugwiritsa ntchito saxagliptin sikunaphunzire.

Pa chifukwa chomwechi, sikulimbikitsidwa kupereka mapiritsi awa kwaana.

Kuphatikiza ndi kukonzekera kwa zotumphukira za sulfonylurea, mankhwalawa amagwiritsidwa ntchito mosamala.

Komanso, vutoli liyenera kuyang'aniridwa ndi odwala omwe ali ndi vuto la aimpso (okhala ndi mawonekedwe ochepa komanso owopsa), anthu okalamba.

Kugwiritsa ntchito mankhwalawa panthawi yapakati sikunaphunzire. Sizikudziwikanso ngati mankhwalawo amadutsa mkaka wa m'mawere. Chifukwa chake, panthawi yamankhwala, madokotala amalimbikitsa kusiya kudya kapena kukana chithandizo ndi saxagliptin.

Zotsatira zoyipa

Odwala ena amakumana ndi zovuta pamene akumwa Onglisa.

Kodi pamakhala ngozi yayikulu ikadzachitika? Ngati wodwala wazindikira mavuto aliwonse, ndiye kuti kufunsira kwa dokotala kuyenera kuwunika momwe aliri ndikuwunika momwe mankhwalawo alili.

Ngakhale pakapita maphunziro oyesera, zotsatirazi zidakhazikitsidwa. Zomwe zimachitika pazochitika zoyipa m'maphunziro omwe amatenga saxogliptin zikufanana ndi zomwe zimachitika mwa odwala omwe adatenga placebo.

Nthawi yomweyo, panalibe kusiyana kwakukulu pakati pa kumwa mankhwalawo monga njira ya monotherapy komanso ndi mankhwala ophatikiza.

Nthawi zambiri zotsatirapo zoyipa izi:

• matenda opatsirana thirakiti (kumtunda),
• matenda a kwamkodzo thirakiti
• sinusitis
• gastroenteritis
• kusanza
• mutu.

Kafukufukuyu adapeza kuti pa sabata la 24 la mankhwala, odwala ena anali ndi vuto la hypersensitivity: 1.5% ya anthu omwe amatenga Onglizu ndi 0.4% ya anthu omwe akutenga placebo. Koma zotengera za hypersensitivity zomwe zimayamba nthawi ya zoyesazi sizinawononge moyo wa odwala ndipo sizinafune chithandizo.

Ndi mankhwala ophatikiza, zotsatirazi zinaonedwa.

Kugwiritsa ntchito saxagliptin kuphatikiza ndi glibenclamide kunayambitsa hypoglycemia mu 0.8% ya milandu, pagulu lolamulira (likuchitika placebo) - mu 0.7%. Zomwe zimachitika mu hypoglycemia ndi kugwiritsa ntchito pamodzi kwa metformin ndi thiazolidinediones zikufanana ndi zochitika za hypoglycemia pagulu la odwala omwe adapatsidwa placebo.

Ndi kuphatikiza kwa saxagliptin ndi thiazolidinediones, zotumphukira edema zinachitika mu 8.1% ya milandu, pagulu lolamulira - 4,3%.Koma chotupa chomwe chinali chifukwa chake chinali chofatsa kapena chochepa, kusiya kwa chithandizo sikunafunikire. Ndi monotherapy ndi kuphatikiza kwina, kuphatikizika uku kunachitika mu 1.7%, pomwe mukuchitika placebo mu 2.4%, motsatana.

Kugwiritsidwa ntchito mosiyanasiyana kwa mankhwala a Onglisa ndi metformin kungayambitse nasopharyngitis ndi mutu. Nasopharyngitis idapezeka mu 6.9% ya odwala: ndi metformin monotherapy - 4%, saxagliptin - mu 4,2% ya odwala. 7.5% idadandaula za kupweteka kwa mutu: ndi metformin monotherapy - 5.2%, saxagliptin - 6.3% ya odwala.

Palibe kusintha kooneka mu magawo a labotale komwe kunawonedwa pa maphunziro a saxagliptin. Kutsika pang'ono kwa chiwerengero cha ma lymphocyte ndikotheka, koma chiwerengero chawo chimakhalabe chokhazikika.

Milandu yambiri

Opanga mankhwala opangidwa ndi saxagliptin, kuphatikizapo Onglises, salimbikitsa kudya mapiritsi awiri a mankhwalawa tsiku lomwelo mukadumpha mlingo wotsatira. Koma mukamamwa mankhwalawa kwa nthawi yayitali mu Mlingo womwe umaposa mpaka nthawi 80, zizindikiro za kuledzera sizinachitike.

Koma malangizo ogwiritsira ntchito akunena kuti ndi mankhwala osokoneza bongo, mankhwalawa ayenera kuperekedwa ndi hemodialysis. Kwa maola 4, 23% ya mankhwalawa amachotsedwa.

Kuyanjana kwa mankhwala osokoneza bongo

Popereka mankhwala a Onglisa, madokotala safuna kudziwa mtundu wa mankhwala omwe mumagwiritsabe ntchito. Kupatula apo, chiwopsezo cha kuyanjana kwakukulu kwa mankhwalawa ndimankhwala ena ndizochepa kwambiri.

Kuphatikizika kwa metabolite yayikulu ya saxagliptin kumatha kuchepa pogwiritsa ntchito CYP 3A4 / 5 isoenzymes (monga Phenobarbital, Carbamazepine, Phenytoin, Dexamethasone, Rifampicin).

Mukaphatikizidwa ndi mankhwala a sulfonylurea, muyenera kusamala: hypoglycemia ikhoza kuyamba. Mutha kuchepetsa chiwopsezo pochepetsa kukonzekera kwa sulfonylurea.

Malangizo apadera

Kawuniwuni wamomwe njira ya "Ongliza" imakhudzira kuthekera koyendetsa magalimoto ndi njira zoyendetsera sizinachitike. Sizikudziwikanso kuti kumwa mowa, kusuta fodya komanso kugwiritsa ntchito mankhwala azitsamba kumakhudza bwanji.

Ngati odwala kale anali ndi vuto la hypersensitivity akamagwiritsa ntchito D1111-4 inhibitors, ndiye kuti Ongliz sayenera kutumizidwa.

Mitengo ndi kusankha kwa analogues

Mutha kugula mankhwalawa m'mafakitala ambiri. Koma mtengo wake ndi wokwera kwambiri: kuti phukusi la mapiritsi 30 a 5 mg, ma ruble 1881 ayenera kuperekedwa. Mankhwalawa sanaphatikizidwe pamndandanda wazokonda zomwe zimaperekedwa kwa wodwala yemwe ali ndi matenda a shuga a 2 mwa kulandira kwaulere.

Odwala ali ndi ufulu wofunsa endocrinologist kuti akupatseni mankhwala kuti atulutsidwe mwaulere njira ina yomwe ingalowe m'malo mwa Onglisa. Komanso, zofunikira m'malo mwake ndizofunikira ngati wodwalayo akulekerera saxagliptin.

Mbale zophatikizira monga mankhwala ochepetsa shuga:

• "Galvus" - yogwira ntchito vildagliptin,
• "Januvia" - sitagliptin,
• "Vipidia" - alogliptin,
• "Trazhenta" - linagliptin,
• "Glucovans" - glibenclamide, metformin hydrochloride,
• Glucophage ndi Metformin hydrochloride.

Koma okhawo opezeka mu endocrinologist ndi omwe amasankha fanizo la "Onglisa" la matenda ashuga.

Pakati pa mndandanda womwe wafotokozedwatuwo palibe mankhwala omwe ndi chilolezo cha Unduna wa Zaumoyo, omwe angathe kuperekedwa mwaulere. Mtengo wazofanizira izi sungatchedwenso wotsika.

Phukusi la mapiritsi 28 a 50 mg a Galvus, muyenera kulipira ma ruble 810.

"Januvia" idzadula odwala ma ruble 1650. - 28 tabu. 100 mg aliyense.

"Vipidia" m'mafakisi amawononga ma ruble a 1288. - 28 tabu. 25 mg aliyense.

"Trazhenta" imawononga ma ruble 1785. - mapiritsi 30 5 mg aliyense.

Koma mankhwala opangidwa ndi metformin ndi otsika mtengo. Glucophage imawononga ma ruble 114. (Ma PC 30. 500 mg iliyonse), "Glucovans" 277 rubles. 30 tabu. 500 / 2,5 mg ya metformin ndi glibenclamide, motero.

Ndemanga za Odwala

Asanapeze mankhwala okwera mtengo ngati amenewa, ambiri amafuna kudziwa kuti ndi othandiza bwanji komanso ngati amathandiza odwala ena.Koma chidwi cha anthu odwala matenda ashuga kupita ku mankhwala a saxagliptin sichimodzimodzi: kwa odwala ena mankhwalawa amakhala panacea, pomwe ena amadandaula chifukwa chosakwanira.

Koma kuwunika kwa odwala kumapereka mpata wothana ndi machitidwe a mankhwalawa. Ngakhale malingaliro a anthu ena, odwala matenda ashuga ayenera kuwongoleredwa ndi malingaliro awo omwe amathandizira endocrinologist. Ngati samukhulupirira, ndiye kuti ndiyenera kuyesa kusintha adokotala.

Odwala ena amadandaula kuti Onglisa samatulutsa zotsatira zomwe amayembekeza. Mwa ena, kuchuluka kwa shuga kumachulukanso ngakhale mukumwa mankhwalawo. Madokotala amapereka "Ongliz" ambiri ngati njira yowonjezeramo mankhwala a "Siofor", "Diabeteson".

Koma odwala matenda ashuga ambiri, ngakhale ndi monotherapy yokhala ndi saxagliptin, amatha kukwanitsa bwino komanso kuwongolera glycemia. Phindu la mankhwalawa, ambiri amati amatha kumwa mapiritsi nthawi iliyonse, mosasamala kanthu za kudya.

Ena amanenanso kuti kuphatikiza ndi metformin kumathandizira kuti zizikhala bwino. Koma kuti mukwaniritse zotsatira zomwe mukufuna, chithandizo cha nthawi yayitali chimafunikira. Ndipo izi ndizosangalatsa kwa ambiri. Ndi regimen yodziwika bwino, mapiritsi akukwana pamwezi.

Koma odwala ambiri amayenera kumwa mankhwala ena kuti achepetse shuga.
Ngati dokotala akuwonetsa "Ongliza", ndiye muyenera kuyesa mankhwala ndi mankhwalawa. Chinthu chachikulu chomwe muyenera kukumbukira ndikufunika kotsatira zakudya komanso kugwiritsa ntchito mphamvu zolimbitsa thupi.

Ngati mupuma ndikumwa mapiritsi okhawo, ndiye kuti simungathe kusintha momwe ziliri.

Mankhwala a Onglisa - malangizo ndi malangizo oti mugwiritse ntchito

Mwa mankhwala omwe amagwiritsidwa ntchito pochiza matenda ashuga, mankhwala omwe amatchedwa Onglisa amadziwika.

Ndikofunikira kuphunzira malangizo a mankhwalawa, kuzindikira mawonekedwe ake ndi zabwino zake, komanso kudziwa zomwe zingakuthandizeni kupewa kukulitsa zotsatira zoyipa chifukwa chogwiritsa ntchito molakwika.

Zambiri, kapangidwe ndi mawonekedwe ake amasulidwe

Mankhwala a shuga amapezeka ku United States. Amapangidwa kuti azionera odwala omwe ali ndi shuga. Ili ndi vuto la hypoglycemic. Gwiritsani ntchito kuyenera kuvomerezeka ndi dokotala, kuti musavulaze thanzi lanu. Ichi ndichifukwa chake mutha kugula Ongliz kokha ndi mankhwala.

Maziko a mankhwalawa ndi mankhwala a Saksagliptin. Imagwira ntchito yayikulu mu mankhwalawa. Gawolo limagwiritsidwa ntchito pothandiza kutsika kwa hyperglycemia pochepetsa kuchuluka kwa shuga m'magazi.

Ngati wodwalayo aphwanya malangizo azachipatala, ndiye kuti mankhwalawo amatha kuyambitsa zovuta komanso zovuta.

Zomwe akuphatikizidwazo zimaphatikizapo zinthu zothandiza:

• lactose monohydrate,
• croscarmellose sodium
• hydrochloric acid
• olimbitsa magnesium.

Kuphatikiza apo, mankhwalawa amakhala ndi utoto wocheperako, womwe umafunikira kuti apange filimu yophimba miyala (mankhwalawo ali ndi mawonekedwe a piritsi).

Amatha kukhala achikasu kapena ofiira okhala ndi zojambula zamtambo. Pogulitsa, mutha kupeza mapiritsi okhala ndi muyeso wa 2,5 ndi 5 mg. Onsewa amagulitsidwa m'matumba amtundu wa ma PC 10.

Mapaketi atatu oterewa amayikidwa mu paketi.

Zofunika m'malo mwa mapiritsi a Ongliz

Analogue ndiotsika mtengo kuchokera ku ma ruble 981.

Galvus imapangidwanso mtundu wa matenda ashuga a 2, koma wotsika mtengo kwambiri ndipo amasiyana ndi Ongliz pazomwe zimagwira. 50 mg vildagliptin imagwiritsidwa ntchito pano. Pali zosiyana mu contraindication, musanayambe chithandizo, werengani malangizo.

Vipidia (mapiritsi) Kukala: 28 Pamwamba

Analogue ndiyotsika mtengo kuchokera ku ruble 799.

Vipidia imasiyananso pakapangidwe, koma ili mgulu lofanana la mankhwala monga mankhwala omwe ali pamwambapa. Amagwiritsidwanso ntchito ngati mtundu wa 2 shuga mellitus ngati monotherapy komanso kuphatikiza ena othandizira pakamwa kapena hypulin.

Pharmacology ndi pharmacokinetics

Zotsatira za mankhwalawa pa odwala matenda ashuga zimachitika chifukwa cha zomwe zimachitika. Ikalowa mthupi, saxagliptin imalepheretsa enzyme DPP-4. Zotsatira zake, maselo a pancreatic beta amathandizira kaphatikizidwe ka insulin. Kuchuluka kwa glucagon panthawiyi kumachepa.

Chifukwa cha izi, kuchuluka kwa shuga m'magazi a wodwalayo kumachepetsedwa, zomwe zimapangitsa kuti zinthu zikhale bwino (pokhapokha mlingo wake umatsika mpaka pamavuto). Chofunikira kwambiri pazinthu zomwe zikufunsidwa ndizoperewera pa thupi la wodwalayo. Odwala omwe amagwiritsa ntchito Ongliza samonda.

Kuchepetsa kwa saxagliptin kumachitika mwachangu ngati mumwa mankhwalawa musanadye. Nthawi yomweyo, gawo lalikulu la chinthu chogwira ntchito limamwa.

Saksagliptin alibe chizolowezi cholowa m'mapuloteni amwazi - mawonekedwe a maubwenzi awa amakhudza gawo laling'ono la chinthucho. Kuchuluka kwa mankhwalawa kumatheka mu maola pafupifupi awiri (ziwalo zamunthu zimakhudza izi). Zimatenga pafupifupi maola atatu kuti muchepetse theka la Saxagliptin lomwe likubwera.

Zizindikiro ndi contraindication

Ndikofunika kwambiri kutsatira malangizo okhudzana ndi zofunikira zoika mankhwalawo. Kugwiritsa ntchito Onglisa mosavomerezeka kumabweretsa chiopsezo ku thanzi ndi moyo. Mankhwala okhala ndi vuto la hypoglycemic ayenera kugwiritsidwa ntchito kokha kwa anthu omwe ali ndi kuchuluka kwa shuga, chifukwa kwa ena chithandizo ichi ndi chovulaza.

Izi zikutanthauza kuti chizindikiritso cha mankhwalawa ndi mtundu 2 shuga. Chidachi chimagwiritsidwa ntchito ngati kudya komanso kuchita masewera olimbitsa thupi kulibe vuto pakukhudzidwa kwa shuga.

Mungathe kugwiritsidwa ntchito mwanjira ina komanso mosiyanasiyana ndi mankhwala ena (Metformin, sulfonylurea derivatives, etc.).

Mankhwala ali ndi zotsutsana:

• mtundu 1 shuga
• mimba
• kudya kwachilengedwe
• matupi awo sagwirizana ndi mankhwala
• kuchepa kwa lactase
• shuga ketoacidosis
• galactose tsankho.

Kukhalapo kwa chinthu chimodzi kuchokera pamndandanda ndi chifukwa chokana kugwiritsa ntchito mapiritsi.

Gawaninso magulu aanthu omwe amaloledwa kugwiritsa ntchito Onglisa, koma amayang'aniridwa mosamala ndi madokotala. Izi zimaphatikizapo okalamba, komanso odwala omwe amalephera impso.

Malangizo ogwiritsira ntchito

Gwiritsani ntchito mankhwalawa malinga ndi malamulo. Ngati dotolo sanatchule mlingo wina, ndiye kuti wodwalayo ayenera kugwiritsa ntchito 5 mg ya mankhwalawa patsiku. Mlingo wofanana umalimbikitsidwa ndikuphatikizidwa kwa Onglisa ndi Metformin (kutumikiridwa kwa Metformin tsiku lililonse ndi 500 mg).

Kugwiritsa ntchito mankhwalawa kumangokhala mkati. Ponena za kudya, palibe zisonyezo, mutha kumwa mapiritsi musanadye komanso mutatha kudya. Cholinga chokha ndikugwiritsa ntchito mankhwalawa pawotchi.

Mukadumpha mlingo wotsatira, simuyenera kudikirira nthawi yokhayo yoti mumwe mankhwalawa. M'pofunika kumwa mankhwalawa mwachizolowezi wodwala akangomukumbukira.

Zotsatira zoyipa ndi bongo

Kupezeka kwa mavuto obwera chifukwa chogwiritsidwa ntchito ndi Onglisa sikugwirizana nthawi zonse ndi kusalolera kwake. Nthawi zina amayamba chifukwa chamoyo chomwe sichinabatizidwe. Komabe, ngati atapezeka, tikulimbikitsidwa kudziwitsa adotolo za iwo.

Malangizo a mankhwalawa amawonetsa mavuto monga:

• matenda a kwamkodzo thirakiti
• mutu
• nseru
• kupweteka m'mimba
• sinusitis
• nasopharyngitis (munthawi yomweyo kugwiritsa ntchito ndi metformin).

Chithandizo cha Syndrome chimagwiritsidwa ntchito pochotsa mavuto awa. Nthawi zina, dokotala amachotsa mankhwalawo.

Palibe chidziwitso chokhudza mankhwala osokoneza bongo omwe ali ndi mankhwalawa. Ngati zichitika, chithandizo chamankhwala ndichofunikira.

Maganizo a odwala

Taphunzira za mankhwalawa za mankhwala a Onglisa, titha kunena kuti mankhwalawa amachepetsa shuga wamagazi, koma siabwino kwa aliyense ndipo amafunikira njira yolankhulirana payekha.

Zotsatira za mankhwalawa ndi zabwino kwambiri. Shuga wanga wakhazikika tsopano, kunalibe zotsatirapo zake ndipo ayi. Kuphatikiza apo, ndizosavuta kugwiritsa ntchito.

Dmitry, wazaka 44

Mankhwala a Ongliz amandiwona ngati ofooka. Mlingo wa shuga sunasinthe, kuwonjezera apo, ndinazunzidwa ndi mutu wokhazikika - mwachionekere, zotsatira zoyipa. Ndinatenga mwezi ndipo sindimatha kupirira, ndimayenera kupempha mankhwala ena.

Alexander, wazaka 36

Ndakhala ndikugwiritsa ntchito Onglise kwa zaka zitatu. Kwa ine, ichi ndiye chida chabwino kwambiri. Asanamwe mankhwala osiyanasiyana, koma zotsatira zake zinali zochepa kwambiri, kapena adazunzidwa ndi zovuta. Tsopano palibe vuto lotere.

kusonkhanitsa kwa mankhwala atsopano pa matenda a shuga:

Mankhwalawa ndi amodzi mwa okwera mtengo - mtengo uliwonse ndi 30 ma PC. pafupifupi 1700-2000 rub. Kuti mupeze ndalama, muyenera kulandira mankhwala.

Adalimbikitsa Zolemba Zina Zogwirizana

Onglisa - mapiritsi a shuga

Ngati matenda amtundu wa 2 akayamba, dokotala yemwe akupezekapo ayenera kupereka mankhwala kwa odwala.

Chimodzi mwazomwe zimasankhidwa nthawi zambiri chimadziwika kuti ndi Onglisa.

Musanagwiritse ntchito, tikulimbikitsidwa kuti muphunzire malangizo ogwiritsira ntchito, kuwunikira (pali zoopsa pambuyo pakugwiritsa ntchito), analogues ndi mtengo.

Zizindikiro zogwiritsidwa ntchito

Mtundu wachiwiri wa matenda ashuga, chiwopsezo cha maselo ku glucose amachepetsa kwambiri. Pakadali pano, pali kuchedwa mu gawo loyamba la kuphatikiza kwa mahomoni.

Mtsogolomo, gawo lachiwiri limatayika chifukwa chosowa ma insretin. Kuchepetsa kwa chiwonetsero cha enzyme DPP 4, ma insretin amakhala nthawi yayitali m'magazi, insulin yambiri imapangidwa. Glycemia pamimba yopanda kanthu komanso yodzaza imakonzedwa, kugwira ntchito kwa kapamba kumabwezeretsedwa. Chifukwa chake, Onglisa amawonjezera ntchito ya mahomoni awoawo, amawonjezera zomwe ali.

Mankhwala Onglisa okhala ndi matenda a shuga a 2 (kuwonjezera pa zakudya zoyenera ndi masewera) amasonyezedwa monga:

• mankhwala oyamba ndimankhwala angapo, limodzi ndi metformin,
• mankhwala othandizira ndi metformin, insulin, zotumphukira za sulfonylurea,
• monotherapy.

Kugwiritsa ntchito Onglises kumapangitsa kuti glycemic control.

Kutulutsa Fomu

Dziko loyambira - USA, koma mapiritsi okonzedwa okonzeka akhoza kuikidwa mu UK kapena Italy.

Amapangidwa mwanjira ya mapiritsi ozungulira, ma convex mbali zonse ziwiri, mbali yakunja ndi yokutira. Piritsi lililonse lili ndi manambala amtambo. Mtundu wa Onglisa umatengera kuchuluka kwa zinthu zomwe zimagwira: 2.5 mg iliyonse ndi maso achikasu achikasu ("2,5" amalembedwa mbali imodzi, "4214" amalembedwa mbali inayo), ndipo 5 mg iliyonse ndi yapinki (manambala “5” ndi “4215 ").

Mapiritsiwo amakhala m'matumba opangidwa ndi zojambulazo: m'matumba amodzi 3 matuza a zidutswa 10. Chodzaza chilichonse chimakhala ndi mafuta omwe amagawa magawo 10 (mwa kuchuluka kwa mapiritsi). Katemera wa makatoni amatetezedwa kuti asasokonekera ndi zomata zowoneka bwino zomwe zimawonetsa mauna achikasu.

Mwazi wamagazi nthawi zonse umakhala 3,8 mmol / L

Momwe mungasungire shuga kukhala wabwinobwino mu 2019

Mutha kugula mankhwala a shuga Onglizu m'masitolo ogulitsa. Mankhwala omwe akupezeka, koma si onse azachipatala omwe amatsata lamuloli. Mu 2015, mankhwalawo adaphatikizidwa pamndandanda wazofunikira, kotero ngati wodwala matenda ashuga adalembetsa, akhoza kuupeza kwaulere.

Pafupipafupi, mtengo wokumangira mapiritsi 30 ndi pafupifupi 1800 rubles. Sungani mankhwalawo pa kutentha kosachepera 30 madigiri kutali ndi ana. Kusungirako sikuyenera kupitirira zaka zitatu.

Chomwe chimagwira ndi saxagliptin hydrochloride (2,5 kapena 5 mg). Uwu ndi woyimira wa inhibitor wamakono wa DPP-4.

Othandizira ndi:

• MCC
• lactose monohydrate,
• sodium croscarmellose,
• magnesium wakuba,
• hydrochloric acid
• utoto.

Gawo lakunja la piritsi limakhala ndi utoto wa OpadryII.

Zolemba ntchito

Pa gawo loyamba la kusintha kwa impso, palibe chifukwa chosinthira.Pamavuto akulu kwambiri, hemodialysis, mlingo woyenera wa mankhwala a Ongliza ndi 2.5 mg patsiku. Mankhwalawa amalimbikitsidwa kuti aperekedwe njira yakuyeretsa magazi ikatha. Pamaso pathu ndi chithandizo, ndikofunikira kuwunika momwe impso zimayambira.

Zotsatira za Onglises pa thupi ndi njira yodziwira kuyeretsa magazi sizinafufuzidwe.

Kusintha kwa ntchito ya chiwindi, mosasamala za kuopsa, sikofunikira kusintha kamodzi.

Zotsatira zakugwiritsa ntchito kwa Onglisa mu odwala matenda ashuga oposa 65 ndizofanana ndi zomwe zimachitika kwa odwala achichepere. Mukakalamba, muyenera kumwa nthawi zonse. Ndikofunikira kukumbukira kuti pa nthawi iyi ya chitukuko, kugwira ntchito kwa impso kumachepa, gawo lomwe likugwira ntchito mokwanira linawatulukira.

Palibe chidziwitso chazakuwopsa ndi zotsatira zoyipa za Onglisa osakwanitsa zaka 18.

Kugwirizana kwa Onglisa ndi insulin panthawi yamankhwala sikunafufuzidwe. Palibe deta pazomwe zimagwiritsa ntchito mankhwalawa poyendetsa komanso zochitika ndi makina osinthika. Chizungulire zitha kuchitika pambuyo kumwa mankhwalawo.

Zokhudza zomwe zimagwira thupi la mayi wapakati komanso mkaka wake sizinaphunzire.

Palibe chidziwitso kuti ngati chinthu chomwe chikugwiracho chikutha kulowa m'chiberekero ndi kupita mkaka wa m'mawere, ndiye kuti mankhwalawa sanalembedwe nthawi ino.

Ngati sikotheka kupewa kugwiritsa ntchito Onglisa, panthawi yomwe mumamwa mankhwalawa, kuyamwitsa kumayima. Pankhaniyi, kuopsa kwa mwana komanso zovuta zomwe zingachitike kwa mayi zimaganiziridwa.

Sulfonylurea zotumphukira kwambiri amachepetsa shuga. Kupewa matenda amtunduwu limodzi ndi Onglisa, ndikofunikira kuti muchepetse mlingo wa sulfonylurea kapena insulin.

Pokhala ndi mbiri yakuwunika kwakukulu kwa odwala matenda ashuga (kuphatikizapo momwe thupi limagwirira ndi Quincke's edema), Ongliza sagwiritsidwa ntchito pakugwiritsa ntchito zoletsa zina za DPP-4. Ndikofunikira kuzindikira zomwe zimayambitsa hypersensitivity ndikuwonetsa njira zina zochizira (analogues za mankhwala Onglisa).

Pali umboni wa kapamba pachimake ndi kugwiritsa ntchito mankhwalawa. Odwala ayenera kudziwitsidwa zamtunduwu popereka Onglisa. Ngati mukuwoneka kuti mukuwonetsedwa kwa zizindikiro zoyambirira za kapamba, mankhwalawa amachotsedwa.

Mapiritsiwo ali ndi lactose, chifukwa chake, odwala matenda ashuga okhala ndi chibadwa cha galactose tsankho, kuchepa kwa lactase sikungatenge Onglisa.

Kuchita ndi mankhwala ena

Chithandizo choyambirira ndi metformin pakufunika kwa kusintha kwa moyo. Ngati chithandizo chotere sichikubweretsa zotsatira zoyembekezeredwa, mankhwala ena ovomerezeka amayamba.

Kafukufuku wachitika omwe akuwonetsa kuti pali chiopsezo chochepa cha kuphatikiza kwa saxagliptin ndi mankhwala ena.

Kugwiritsa ntchito palimodzi ndi ma inducers a CYP 3A4 / 5 isoenzymes kumathandiza kuchepetsa zomwe zili mu saxagliptin metabolic product.

Kutenga mankhwala a sulfonylurea kumachepetsa kwambiri kuchuluka kwa shuga m'magazi. Kuti mupewe chiopsezo chotere, ndikofunikira kuti muchepetse mlingo wa mankhwala Onglisa.

Palibe maphunziro omwe adachitika pazotsatira za kusuta, kudya, kapena kumwa mowa pa saxagliptin.

Njira zopewera

Onglisa ndi mankhwala otetezeka, zotsatira zosakonzekera sizimachitika. Pali zinthu zambiri zoyipa zomwe zimachitika ndi saxagliptin monga chithandizo cha placebo.

Kugwiritsa ntchito Onglises ndizoletsedwa pomwe:

• mtundu 1 shuga
• mogwirizana ndi insulin
• kuchepa kwa mkaka,
• matenda ashuga ketoacidosis,
• mimba
• yoyamwitsa
• wosakwana zaka 18
• kusalolera kwa chimodzi mwazigawo za mankhwala.

Ndikofunikira kuti odwala azigwiritsa ntchito:

• akuvutika kwambiri ndi vuto laimpso kapena chifuwa chachikulu m'mbuyomu,
• okalamba
• kugwiritsa ntchito munthawi yomweyo ndi sulfonylureas.

Mu chithandizo cha Onglisa, pamakhala zovuta zina:

• matenda a kwamkodzo thirakiti
• chapamwamba kupuma thirakiti matenda
• kutupa kwa sinus mucosa,
• kutupa kwam'mimba ndi matumbo aang'ono,
• akukumbutsa
• pachimake kapamba
• migraines.

Ndi mankhwala osakanikirana ndi metformin, nasopharyngitis imadziwonekera nthawi zina.

Hypersensitivity idadziwika mu 1.5% yamilandu, sinaopseze moyo, ndipo kuchipatala sikunafunike.

Mukamayikidwa limodzi ndi thiazolidinediones, kuweruza ndi kuwunika kwa Onglise, kupezeka kwa edema yofowoka kapena yapakati kunadziwika, komwe sikunafunike kutha kwa chithandizo.

Zovuta za hypoglycemia panthawi ya chithandizo ndi Ongliza zinali zogwirizana ndi zotsatira zake ndi placebo.

Bongo

Pogwiritsa ntchito mankhwalawa kwa nthawi yayitali, zizindikiro za poizoni sizifotokozedwa. Pankhani ya bongo, Zizindikiro ziyenera kutsitsimuka. The yogwira thunthu ndi kagayidwe kachakudya mankhwala amuchotsa ndi hemodialysis.

Analogs Onglises okhala ndi zinthu zomwezi omwe mulibe. Ili ndiye mankhwala okhawo omwe ali ndi saxagliptin. Zofanana pa thupi zimaphatikizidwa ndi Nesin, Trigueent, Galvus. Sizoletsedwa kugwiritsa ntchito analogi za Ongliz popanda chilolezo cha adokotala.

Mankhwala a shuga a Onglis amathandizira kuti magazi a shuga aziwongolera. Mapiritsi ndiosavuta kutenga. Ndikutha kuwona mwayi womwe sindinawone zotsatira zoyipa. Mwa maminiti, nditha kutchula mayina ochulukirachulukira.

Ndimakonda mankhwala Onglisa, pali malangizo omveka bwino ogwiritsa ntchito, ndi osavuta kugwiritsa ntchito. Nthawi zina mutu wochepa. Ndikupangira mankhwalawa.

Chithandizo cha Ongliza ndikuyimira gulu latsopano la mankhwala ochepetsa shuga. Ili ndi njira yosinthira mosiyanasiyana, koma mwanjira yofananira imafanana ndi mankhwala achikhalidwe, ndipo pachitetezo imapambana. Mankhwalawa ali ndi zotsatira zabwino pa matenda oyanjana, amalepheretsa kukula kwa shuga komanso zovuta zina.

Ubwino wosakayikiridwa ndi kusapezeka kwa chiwopsezo cha hypoglycemia, zimakhudza kulemera kwa wodwala komanso mwayi wogwiritsa ntchito mankhwala ena ochepetsa shuga. M'tsogolomu, asayansi akufuna kupanga mankhwala omwe adzabwezeretsenso chida cha pancreatic kwa nthawi yayitali.

Matenda a shuga nthawi zonse amayambitsa zovuta zakupha. Mwazi wamagazi ochulukirapo ndi woopsa kwambiri.

Lyudmila Antonova mu Disembala 2018 adafotokoza mwatsatanetsatane za chithandizo cha matenda ashuga. Werengani kwathunthu

Kodi nkhaniyo inali yothandiza?

Mankhwala Onglisa wochokera ku matenda osokoneza bongo - malangizo tsatanetsatane kuti mugwiritse ntchito

Matendawa masiku ano amakhudza anthu 9% padziko lapansi. Makampani opanga mankhwala ndi machitidwe azachipatala a mayiko otsogola padziko lonse lapansi akuika ndalama mabiliyoni ambiri, ndipo matenda ashuga akuyenda mozungulira dziko lapansi, kuyamba kukhala achichepere, ndikuyamba kukhala ankhanza.

Vutoli likufika pamlingo womwe sunkayembekezeredwa: pofika chaka cha 2020, theka la odwala biliyoni omwe ali ndi matenda a shuga a 2 akunenedweratu, ndipo madokotala sanaphunzire momwe angapewere matendawa moyenera.

Ngati ndi matenda amtundu wa 1 shuga, omwe amakhudza osakwana 10% ya onse odwala matenda ashuga, zonse ndizosavuta: muchepetse kuchuluka kwa glucose m'magazi mwa kubaya insulini (palibe chomwe chingaperekedwe pamenepo) ndipo zonse zikhala bwino (lero, kwa odwala otere, adapanganso kapamba wochita kupanga) ), ndiye ndi matenda a shuga 2, ukadaulo wapamwamba sugwira ntchito.

Mwa fanizo, la matenda ashuga amtundu wa 2, shuga adanenedwa kukhala mdani wamkulu, kudzaza msika ndi mankhwala ochepetsa shuga. Mankhwala a odwala matenda ashuga mothandizidwa ndi mapiramidi othandizira amalimbikitsidwa, mankhwala ena akapaka mankhwala amodzi, ndiye kuti mankhwala ena achitatu amawonjezeredwa ku zovuta izi kufikira nthawi ya insulin itafika.

Kwa zaka 20 zapitazi, madokotala akhala akulimbana ndi shuga, koma zotsatira zake zimakhala zotsika, chifukwa zovuta komanso zovuta kuchokera ku mankhwala nthawi zambiri zimapambana, makamaka ngati simumatsatira mlingo, musaganizire kuti mankhwalawo ndiabwino komanso ndani osachita.

Chimodzi mwa ziwalo zomwe tikufuna ndi mtima ndi mtsempha wamagazi. Zimatsimikiziridwa kuti chithandizo chachikulu cha matenda ashuga chimayambitsa zosiyana ndipo zimapangitsa kufa kwa mitsempha. Shuga ndi chizindikiro chabe cha matenda amtundu wa 2; matendawa amatengera metabolic syndrome.

Mankhwala a m'badwo watsopano Onglisa, opangidwa ndi asayansi aku Britain ndi ku Italy, sikuti amangothandiza odwala, komanso luso la mtima. Mankhwala a mndandanda wa maretretin, omwe akuphatikizapo Onglisa, ndi zomwe zapezeka pamunda wa matenda ashuga. Amagwira ntchito kuti achepetse kusadya komanso kuwonda - chimodzi mwazifukwa zazikuluzakhazikitsira matenda a shuga 2.

Kuphatikiza apo, incretinomimetics silipiritsa hypoglycemia, amathandizira kuchepetsa kuthamanga kwa magazi, komanso kuteteza maselo a pancreatic. Mtengo wokwera komanso kusowa kwa chithandizo chachipatala chifukwa chakugwiritsa ntchito mankhwalawa kungachitike chifukwa cha zovuta za Onglisa, koma izi ndizofunikanso nthawi.

Kupanga ndi mawonekedwe a kumasulidwa

Piritsi iliyonse ya Onglisa, chithunzi chake chomwe chaperekedwa m'gawoli, chili ndi 2.5 kapena 5 mg ya saxagliptin hydrochloride mu chipolopolo. Fomuloli idathandizidwa ndi ma excipients: cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate ndi Opadray utoto (woyera, wachikasu ndi wabuluu mapiritsi a 2.5 mg ndi oyera, apinki ndi abuluu pamtundu wa 5 mg).

Mankhwalawa amatha kuzindikiridwa ndi mawonekedwe (mapiritsi a biconvex okhala ndi chikasu chachikasu ndikuwonetsa 2,5 / 4214 ndi pinki wolemba 5/4215). Zolemba zake zimasindikizidwa mbali iliyonse ndi inki wabuluu.

Mutha kugula mankhwala omwe mumalandira. Kwa mapiritsi a Ongliz, mtengo wake suchokera pagulu la bajeti: 30 ma PC. 5 mg ku Moscow muyenera kulipira ma ruble 1700. Wopanga adatsimikiza moyo wamashelefu pazaka zitatu. Malo osungira mankhwalawa ndi muyezo.

Zotsatira za pharmacological

Chofunikira chachikulu cha Onglisa ndi saxagliptin. Pasanathe tsiku limodzi atalowa m'mimba, zimalepheretsa ntchito ya DPP-4 peptide. Mukakumana ndi glucose, kuponderezedwa kwa enzyme modabwitsa (katatu) kumathandizira kubisalira kwa glucagon-ngati peptide-1 (GLP-1) ndi glucose-wodalira insulinotropic polypeptide (HIP).

Nthawi yomweyo, kuchuluka kwa glucagon mu b-cell kumachepa, ntchito ya ma b-cell omwe amachititsa kuti ma cell a insulin achuluke. Zotsatira zake, zizindikiro za kusala ndi postprandial glycemia zimachepetsedwa kwambiri.

Chitetezo ndikuyenda bwino kwa mankhwalawa adaphunziridwa poyesa 6, momwe amodzi odzipereka a 4148 omwe adatenga nawo matenda amtundu wa 2 adatenga nawo gawo.

Onse ogwira nawo ntchito adawonetsa kusintha kwa glycated hemoglobin, shuga yokhala ndi njala ndi glycemia pambuyo ponyamula katundu.

Mankhwala owonjezera, monga thiazolidinediones, metformin, glibenclamide, adawerengedwa kwa omwe atenga nawo gawo omwe sanakwaniritse 100% glycemic control.

About Onglis, kuwunika kwa odzipereka omwe adachita nawo zofufuza zofanana ndi placebo kukuwonetsa kuti, pamiyeso yosiyanasiyana, hemoglobin wa glycated ndi kapangidwe ka magazi zimayenda bwino patatha milungu iwiri.

Odwala omwe ali ndi mankhwala owonjezera a antiidiabetes amawonetsa zotsatira zofananazo. Kulemera kwa onse omwe atenga nawo mayesowa kunakhazikika.

Oral hypoglycemic mankhwala

Zotsatira za pharmacological

Saxagliptin ndi njira yosinthira mwatsopano yosinthira yopikisana ndi dipeptidyl peptidase-4 (DPP-4).

Odwala omwe ali ndi vuto la matenda a shuga 2, makonzedwe a saxagliptin amatsogolera pakuwapanikizika kwa ntchito ya enzyme DPP-4 kwa maola 24.

Pambuyo pakulowetsa shuga, kuletsa kwa DPP-4 kumapangitsa kuti chiwopsezo cha glucagon-peptide-1 (GLP-1) komanso kuchuluka kwa glucose amadalira glucagon chikuwonjezere, zomwe zimatsogolera pakuwonjezeka kwa kuyamwa kwa cell ya cell glucose. insulin ndi C-peptide.

Kutulutsidwa kwa insulin ndi masamba a pancreatic beta ndi kuchepa kwa kutulutsidwa kwa glucagon kuchokera ku maselo a pancreatic alpha kumabweretsa kuchepa kwa glycemia ndi postprandial glycemia.

Kuchita bwino ndi chitetezo cha saxagliptin mutatengedwa mu Mlingo wa 2,5 mg, 5 mg ndi 10 mg 1 nthawi / tsiku amaphunziridwa m'maphunziro asanu ndi limodzi amaso, owongoleredwa ndi placebo okhudza odwala 4148 omwe ali ndi matenda a shuga a mtundu 2.

Kumwa mankhwalawo limodzi ndi kuwongolera kwakukulu mu glycosylated hemoglobin (HbA1c), glucose ofulumira (GPN) ndi postprandial glucose (PPG) plasma wamagazi poyerekeza ndi kuwongolera.

Odwala omwe mulingo wa glycemic womwe sakanatha kutero sukwaniritsidwa ndi saxagliptin monga monotherapy adapangidwanso mankhwala a metformin, glibenclamide kapena thiazolidinedione.

Mukamamwa saxagliptin pa mlingo wa 5 mg, kuchepa kwa HbA1c kumawonedwa patatha milungu 4 ndi GPN pambuyo masabata awiri.

Pagulu la odwala omwe amalandila saxagliptin osakanikirana ndi metformin, glibenclamide kapena thiazolidinediones, kuchepa kwa HbA1c kumawonedwanso pambuyo pa masabata 4 ndi GPN pambuyo pa masabata awiri.

Zotsatira za saxagliptin pa lipid mbiri ndizofanana ndi za placebo. Pa mankhwala ndi saxagliptin palibe kuwonjezeka kwa thupi kunadziwika.

Pharmacokinetics

Odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga komanso anthu odzipereka omwe ali ndi thanzi labwino, ma pharmacokinetics ofanana a saxagliptin ndi metabolite yake yayikulu adadziwika.

Saxagliptin imatengedwa mwachangu pambuyo pakumeza pamimba yopanda kanthu ndikwaniritsa Cmax ya saxagliptin ndi metabolite yayikulu mu plasma kwa maola 2 ndi maola 4, motero.

Ndi kuchuluka kwa saxagliptin, kuchuluka kwa Cmax ndi AUC ya saxagliptin ndipo metabolite yake yayikulu idadziwika.

Pambuyo pakukonzekera kamlomo kamodzi kwa saxagliptin pa mlingo wa 5 mg ndi odzipereka athanzi, odwala AOL amagwira saxagliptin ndi metabolite yake yayikulu anali 78 ng × h / ml ndi 214 ng × h / ml, ndipo ma plma a Cmax anali 24 ng / ml ndi 47 ng / ml, motsatana .

Kutalika kwapakati pa T1 / 2 yomaliza ya saxagliptin ndipo metabolite yake yayikulu inali maola 2,5 ndi maola 3.1, motsatana, ndipo choletsa chachikulu cha plasma T1 / 2 cha DPP-4 chinali maola 26.9.

Kuletsa kwa ntchito ya plasma DPP-4 kwa maola osachepera 24 mutatenga saxagliptin ndi chifukwa chogwirizana kwambiri ndi DPP-4 komanso kumangiriza kwa nthawi yayitali. Kuchulukitsa kwakukulu kwa saxagliptin ndi metabolite yake yayitali pogwiritsa ntchito nthawi yayitali 1 nthawi / tsiku silinawonedwe.

Panalibe kudalira kwachindunji kwa saxagliptin ndi metabolite yake yayikulu pakumwa mankhwala ndi nthawi yayitali pakumwa saxagliptin 1 nthawi / tsiku mu Mlingo kuyambira 2,5 mg mpaka 400 mg kwa masiku 14.

Pambuyo pakukonzekera pakamwa, osachepera 75% ya muyezo wa saxagliptin. Kudya sizinakhudze kwambiri pharmacokinetics ya saxagliptin mwa odzipereka athanzi.

Zakudya zamafuta kwambiri sizinakhudze Cmax ya saxagliptin, pomwe AUC inakwera ndi 27% poyerekeza ndi kusala kudya. Nthawi yofikira Cmax ya saxagliptin inakula ndi pafupifupi 0.

Maola 5 mukamamwa mankhwala ndi chakudya poyerekeza ndi kusala. Komabe, zosinthazi sizofunikira pakadwala.

Kumangidwa kwa saxagliptin ndi metabolite yake yayikulu m'mapuloteni a seramu sikofunikira, chifukwa chake, titha kulingaliridwa kuti kugawa kwa saxagliptin ndikusintha kwa kapangidwe ka mapuloteni a seramu yamagazi omwe amawonekera mu hepatic kapena aimpso kulephera sikungasinthe.

Saxagliptin imapangidwa makamaka ndi kutengapo gawo kwa ma isoenzymes a cytochrome P450 3A4 / 5 (CYP 3A4 / 5) ndi mapangidwe a metabolite yogwira, mphamvu ya inhibitory yomwe motsutsana ndi DPP-4 ndi yofooka nthawi 2 kuposa saxagliptin.

Saxagliptin amamuchotsa mkodzo ndi bile. Pambuyo pa gawo limodzi la 50 mg yolembedwa 14C-saxagliptin, 24% ya mankhwalawa idachotsedwa ndi impso ngati saxagliptin yosasinthika ndi 36% monga metabolite yayikulu ya saxagliptin.

Ma radioactivine omwe apezeka mumkodzo amafanana ndi 75% ya mlingo womwe unatengedwa.Chilolezo chapakati cha saxagliptin chinali pafupifupi 230 ml / mphindi, kuchuluka kwa kusefera kwa glomerular kunali pafupifupi 120 ml / mphindi.

Pa metabolite yayikulu, chilolezo cha impso chinali chofanana ndi tanthauzo la kusefera kwa glomerular.

Pafupifupi 22% ya ma radioacaction athu onse adapezeka mu ndowe.

Pharmacokinetics mu milandu yapadera yamankhwala

Odwala omwe ali ndi vuto lochepetsa aimpso, AUC amagwira saxagliptin ndi metabolite yake yayikulu anali 1,2 ndi 1,7, motero, kuposa omwe ali ndi vuto laimpso. Kukula kwa mfundo za AUC sikofunikira mwakuthupi, chifukwa chake kusintha kwa mankhwalawa sikofunikira.

Odwala omwe ali ndi kuchepa kwambiri kwaimpso, komanso odwala hemodialysis, mfundo za AUC za saxagliptin ndi metabolite yake yayikulu anali 2.1 ndi 4, motero.

Kutalika kokwanira kuposa zofanana mwa anthu omwe ali ndi vuto laimpso.

Kwa odwala omwe ali ndi vuto laimpso lokwanira komanso lovuta, komanso odwala hemodialysis, mlingo wa saxagliptin uyenera kukhala 2,5 mg 1 nthawi / tsiku.

Odwala omwe ali ndi vuto lochepa kwambiri, loletsa komanso la hepatic kwambiri, panalibe kusintha kwakukulu pama pharmacokinetics a saxagliptin, kotero kusintha kwa mlingo kwa odwala kotere sikofunikira.

Odwala a zaka zapakati pa 65-80, panalibe kusiyana kwakukulu mu pharmacokinetics ya saxagliptin poyerekeza ndi odwala aang'ono (zaka 18 mpaka 40), motero, kusintha kwa mlingo kwa odwala okalamba sikofunikira. Komabe, ziyenera kukumbukiridwa kuti m'gulu ili la odwala, kuchepa kwa impso ndizotheka kwambiri.

Type 2 shuga mellitus kuwonjezera pa zakudya ndi masewera olimbitsa thupi kuti muthe kuyendetsa bwino glycemic control:

- kuyambitsa kuphatikiza mankhwala ndi metformin,

- zowonjezera pa monotherapy ndi metformin, thiazolidinediones, sulfonylurea, zotumphukira, pakalibe chitetezo chokwanira cha glycemic mu mankhwalawa.

Mankhwala ndi mankhwala pakamwa, ngakhale kudya zakudya.

At monotherapy Mlingo woyenera wa saxagliptin ndi 5 mg 1 nthawi / tsiku.

At kuphatikiza mankhwala Mlingo wovomerezeka wa saxagliptin ndi 5 mg 1 nthawi / tsiku limodzi ndi metformin, thiazolidinediones kapena sulfonylurea.

At kuyambira kuphatikiza mankhwala ndi metformin Mlingo woyenera wa saxagliptin ndi 5 mg 1 nthawi / tsiku, mlingo woyambirira wa metformin ndi 500 mg / tsiku. Potha kuyankha kosakwanira, mlingo wa metformin ungathe kuchuluka.

At pochitika kumwa mankhwala Ongliza adaphonya piritsi liyenera kumwedwa nthawi yomweyo wodwalayo akakumbukira izi, musamamwe kawiri pa mankhwalawa tsiku limodzi.

Chifukwa odwala ndi wofatsa aimpso kulephera (KK> 50 ml / mphindia) kusintha kwa mlingo sikofunikira.

Chifukwa odwala ndi olimbitsa kapena aimpso kulephera (KK ≤50 ml / mphindi), komanso hemodialysis odwala Mlingo woyenera wa Ongliza ndi 2.5 mg 1 nthawi / tsiku. Mankhwala ayenera kumwedwa kumapeto kwa gawo la hemodialysis.

Kugwiritsa ntchito saxagliptin mwa odwala omwe akupanga peritoneal dialysis sikunaphunzire. Musanayambe chithandizo ndi saxagliptin komanso munthawi ya chithandizo, tikulimbikitsidwa kuwunika ntchito yaimpso.

At chiwindi chosokoneza ntchito wodekha, wofatsa komanso wowopsa kusintha kwa mlingo sikofunikira.

Mlingo kusintha odwala okalamba osafunikira. Komabe, posankha mlingo, muyenera kukumbukira kuti m'gulu lino la odwala, kuchepa kwa impso kumachitika.

Chitetezo ndi kufunika kwa mankhwalawa mu odwala osakwana zaka 18 osati kuphunzira.

At Kugwiritsa ntchito limodzi ndi zoletsa zamphamvu za CYP 3A4 / 5monga ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir ndi telithromycin, mlingo wovomerezeka wa Ongliza ndi 2.5 mg 1 nthawi / tsiku.

Pafupipafupi zochitika zolakwika mutamwa Ongliza 5 mg mu monotherapy ndi njira yowonjezerapo chithandizo ndi metformin, thiazolidinedione kapena glibenclamide anali ofanana ndi omwe anali mgulu la placebo.

Kukula kwa mayendedwe azovuta: nthawi zambiri (≥1 / 10), nthawi zambiri (≥1 / 100,

Onglisa: mankhwala a shuga, ndemanga ndi mapiritsi a mapiritsi

Ndi kukula kwa shuga osadalira insulin, odwala satha nthawi zonse kuwongolera kuchuluka kwa glycemia pogwiritsa ntchito zakudya zapadera komanso masewera olimbitsa thupi. Onglisa ndi mankhwala ochepetsa shuga omwe amagwiritsidwa ntchito mwanjira imeneyi kukhazikitsa kuchuluka kwa shuga m'magazi.

Monga mankhwala aliwonse, Onglisa ali ndi zotsutsana, zochita zoyipa, komanso mawonekedwe ogwiritsira ntchito. Chifukwa chake, musanagwiritse ntchito mankhwalawa, muyenera kudziwa zambiri za mankhwalawo.

Onglisa (mu lat. Onglyza) ndi mankhwala odziwika bwino omwe amagwiritsidwa ntchito padziko lonse lapansi matenda ashuga a 2. Dzinalo losafunikira ladziko lonse (INN) la mankhwalawa ndi Saxagliptin.

Wopanga wothandizila wa hypoglycemic ndi kampani yaku America ya mankhwala a Bristol-Myers squibb. Gawo lalikulu - saxagliptin amadziwika kuti ndi imodzi mwazosankha zamphamvu kwambiri zosakanikirana za dipeptidyl peptidase-4 (DPP-4). Izi zikutanthauza kuti mankhwalawa akamwa pakamwa, chinthu chachikulu chimachepetsa mphamvu ya enzyme ya DPP-4 masana.

Kuphatikiza pa saxagliptin, mapiritsi a Onglis ali ndi zochepa zowonjezera - lactose monohydrate, croscarmellose sodium, microcrystalline cellulose, macrogol, talc, titanium dioxide, magnesium stearate ndi ena ambiri. Kutengera mtundu wa kumasulidwa, piritsi limodzi la mankhwalawa limatha kukhala ndi 2.5 kapena 5 mg ya chinthu chomwe chikugwira ntchito.

Kodi wothandizila wodwala matenda a shuga Akuma amatha bwanji atalowa m'thupi la munthu? Saxagliptin imalowa mwachangu m'mimba, zomwe zimapezeka kwambiri m'madzi a m'magazi zimawonedwa patatha maola 2-4 mutatha kuzigwiritsa ntchito. Mankhwala ali ndi zotsatirazi:

1. Kuchulukitsa mulingo wa ISU ndi GLP-1.
2. Amachepetsa zomwe zili ndi glucagon, komanso zimathandizira momwe maselo a beta, omwe amaphatikizira kuwonjezeka kwa C-peptides ndi insulin.
3. Zimakwiyitsa kumasulidwa kwa timadzi totsitsa-shuga ndi ma cell a beta omwe amapezeka m'matumbo.
4. Imaletsa kumasulidwa kwa glucagon ku ma alpha cell a islets a Langerhans.

Pakuwonjezera njira zomwe zili pamwambapa, mankhwala a Onglis amasintha mphamvu za glycated hemoglobin (HbA1c), zizindikiro za shuga pamimba yopanda kanthu ndikatha kudya. Madokotala amatha kupereka mankhwalawa limodzi ndi othandizira ena a hypoglycemic (metformin, glibenclamide kapena thiazolidinediones).

Chidacho chimachotsedwa m'thupi m'njira yosasinthika komanso mawonekedwe a metabolite ndi bile ndi mkodzo.

Pafupipafupi, chiwonetsero cha impso cha saxagliptin ndi 230 ml pamphindi, ndipo kuchuluka kwa kusefedwa kwa glomerular (GFR) ndi 120 ml pamphindi.

Asanayambe kumwa mankhwalawa, wodwalayo ayenera kufunsa odziwa ntchito yake yazaumoyo omwe angadziwe kuchuluka kwake malinga ndi shuga. Pogula mankhwalawa Onglisa, malangizo ogwiritsira ntchito ayenera kuwerengedwa mosamala ndipo ngati muli ndi mafunso mufunse adokotala.

Mapiritsi amagwiritsidwa ntchito mosasamala nthawi yakudya, osambitsidwa ndi kapu yamadzi. Ngati mankhwalawa amatengedwa ngati monotherapy, ndiye kuti tsiku lililonse mlingo 5 mg. Ngati dokotala atakupatsani mankhwala othandizira, ndiye kuti tsiku limaloledwa kugwiritsa ntchito Onglisa amatanthauza 5 mg ndi metformin, thiazolidinediones ndi mankhwala ena a hypoglycemic.

Kuphatikiza Onglisa ndi metformin, muyenera kutsatira mlingo woyambirira wa 5 mg ndi 500 mg, motsatana. Ndi zoletsedwa kumwa mitundu iwiri panthawi yomwe wodwalayo atayiwala kumwa mankhwalawa panthawi. Akakumbukira izi, ayenera kumwa piritsi limodzi.

Makamaka makamaka ndi odwala omwe ali ndi vuto la impso. Ndi mawonekedwe ofatsa aimpso, sikofunikira kusintha mlingo wa mankhwalawa. Odwala omwe ali ndi kuchepa kwapakati kapena kwambiri aimpso, komanso omwe akudwala hemodialysis, mlingo wa tsiku ndi tsiku ndi 2.5 mg. Kuphatikiza apo, mukamagwiritsa ntchito CYP 3A4 / 5 zoletsa, mlingo wa mankhwala a Onglis uyenera kukhala wochepa (2,5 mg).

Wopanga akuwonetsa pa phukusi tsiku lotha ntchito, lomwe nthawi zambiri limakhala zaka zitatu. Mankhwalawa amasungidwa kutali ndi ana aang'ono pa kutentha kosaposa 30 digiri.

Mapiritsi okhala ndi mafilimu kuchokera ku chikaso chonyezimira chikongoletsa chikaso chowoneka bwino, chozungulira, biconvex, cholembedwa "2,5" mbali ina ndi "4214" mbali inayo, yokutira ndi utoto wabuluu.

Omwe amathandizira: lactose monohydrate - 99 mg *, cellcrystalline cellulose - 90 mg, croscarmellose sodium - 10 mg, magnesium stearate - 1 mg **, hydrochloric acid 1 M kapena sodium hydroxide solution 1 M - kuchuluka kofunikira, Opadry II yoyera (% kulemera / kulemera) - 26 mg (polyvinyl mowa 40%, titanium dioxide 25%, macrogol (PEG 3350) 20.2%, talc 14.8%), Opadry II chikasu (% kulemera / kulemera) - 7 mg (polyvinyl mowa 40%, titanium dioxide 24.25%, macrogol (PEG 3350) 20.2%, talc 14.8%, utoto wachitsulo wamakilidwe achikasu (E172) 0,75%), inki Opacode buluu *** - kuchuluka kofunikira.

Ma PC 10 - mabuloni a aluminium zojambulazo (3) - mapaketi a katoni.

* Kuchuluka kwa lactose kumatha kusiyanasiyana kutengera kuchuluka kwa ma magnesium stearate omwe agwiritsidwa ntchito.
** Kuchuluka kwa kunenepa kwa magnesium kumasiyana pakati pa 0,5-2 mg. Mulingo woyenera kwambiri wa 1 mg.
*** Ink analemba Opacode buluu (% kulemera / kulemera): shellac 45% mu ethyl mowa 55.4%, FD&C Blue # 2 / indigo carmine aluminium pigment (Е132) 16%, n-butyl mowa 15%, propylene glycol 10,5%, isopropyl mowa 3%, 28% ammonium hydroxide 0.1%. Zida zochepa kwambiri za shellac ndi FD&C Blue # 2 / indigo carmine aluminium zimangokhala pamapiritsi pomwe zilembo. Zosungunulira zomwe zimaphatikizidwa ndi inki zimachotsedwa pakupanga.

Mapiritsi okhala ndi mafilimu pinki, yozungulira, biconvex, yolembedwa "5" mbali imodzi ndi "4215" mbali inayo, utoto wa utoto wabuluu.

Omwe amathandizira: lactose monohydrate - 99 mg *, cellcrystalline cellulose - 90 mg, croscarmellose sodium - 10 mg, magnesium stearate - 1 mg **, hydrochloric acid 1 M kapena sodium hydroxide solution 1 M - kuchuluka kofunikira, Opadry II yoyera (% kulemera / kulemera) - 26 mg (polyvinyl mowa 40%, titanium dioxide 25%, macrogol (PEG 3350) 20.2%, talc 14.8%), Opadry pink pink (% kulemera / kulemera) - 7 mg (polyvinyl mowa 40%, titanium dioxide 24.25%, macrogol (PEG 3350) 20.2%, talc 14.8%, utoto wachitsulo utoto wofiira (E172) 0,75%), inki Opacode buluu *** - kuchuluka kofunikira.

Ma PC 10 - mabuloni a aluminium zojambulazo (3) - mapaketi a katoni.

* Kuchuluka kwa lactose kumatha kusiyanasiyana kutengera kuchuluka kwa ma magnesium stearate omwe agwiritsidwa ntchito.
** Kuchuluka kwa kunenepa kwa magnesium kumasiyana pakati pa 0,5-2 mg. Mulingo woyenera kwambiri wa 1 mg.
*** Ink analemba Opacode buluu (% kulemera / kulemera): shellac 45% mu ethyl mowa 55.4%, FD&C Blue # 2 / indigo carmine aluminium pigment (Е132) 16%, n-butyl mowa 15%, propylene glycol 10,5%, isopropyl mowa 3%, 28% ammonium hydroxide 0.1%. Zida zochepa kwambiri za shellac ndi FD&C Blue # 2 / indigo carmine aluminium zimangokhala pamapiritsi pomwe zilembo. Zosungunulira zomwe zimaphatikizidwa ndi inki zimachotsedwa pakupanga.

Saxagliptin ndi njira yosinthira mwatsopano yosinthira yopikisana ndi dipeptidyl peptidase-4 (DPP-4).

Odwala omwe ali ndi mtundu wachiwiri wa matenda ashuga, kuperekera kwa saxagliptin kumachepetsa mphamvu ya enzyme ya DPP-4 pasanathe maola 24. Pambuyo kuyamwa kwa shuga mkamwa, kuyimitsidwa kwa DPP-4 kumapangitsa kuti chiwonetsero cha glucagon-peptide-1 chiziwonjezeke. polypeptide (HIP), kuchepa kwa kuchuluka kwa glucagon ndikuwonjezereka kwa mayankho omvera a shuga a maselo a beta, zomwe zimapangitsa kuti chiwopsezo cha insulin ndi C-peptide chiwonjezeke.

Kutulutsidwa kwa insulin ndi masamba a pancreatic beta ndi kuchepa kwa kutulutsidwa kwa glucagon kuchokera ku maselo a pancreatic alpha kumabweretsa kuchepa kwa glycemia ndi postprandial glycemia.

Kuchita bwino ndi chitetezo cha saxagliptin mutatengedwa mu Mlingo wa 2,5 mg, 5 mg ndi 10 mg 1 nthawi / tsiku amaphunziridwa m'maphunziro asanu ndi limodzi amaso, owongoleredwa ndi placebo okhudza odwala 4148 omwe ali ndi matenda a shuga a mtundu 2. Kumwa mankhwalawo limodzi ndi kuwongolera kwakukulu mu glycated hemoglobin (HbA_1c), kuthamanga kwa plasma glucose (GPN) ndi magazi a m'magazi a postprandial (PPG) poyerekeza ndi kuwongolera.

Odwala omwe mulingo wa glycemic womwe sakanatha kutero sukwaniritsidwa ndi saxagliptin monga monotherapy adapangidwanso mankhwala a metformin, glibenclamide kapena thiazolidinedione. Mukamamwa saxagliptin pa mlingo wa 5 mg, kuchepa kwa HbA_1c idadziwika pambuyo pa masabata anayi ndi GPN - atatha masabata awiri. Pagulu la odwala omwe amalandila saxagliptin limodzi ndi metformin, glibenclamide kapena thiazolidinediones, kuchepa kwa HbA_1c adanenanso pambuyo pa masabata anayi ndi GPN - atatha masabata awiri.

Zotsatira za saxagliptin pa lipid mbiri ndizofanana ndi za placebo. Pa mankhwala ndi saxagliptin palibe kuwonjezeka kwa thupi kunadziwika.

Odwala omwe ali ndi mtundu wachiwiri wa matenda a shuga komanso anthu odzipereka omwe ali ndi thanzi labwino, ma pharmacokinetics ofanana a saxagliptin ndi metabolite yake yayikulu adadziwika.

Saxagliptin imatengedwa mwachangu pambuyo pomenyedwa pamimba yopanda kanthu ndikupanga C_max saxagliptin ndi metabolite yayikulu mu plasma kwa maola 2 ndi maola 4, motero. Ndi kuchuluka kwa saxagliptin mlingo, kuchuluka kwa C kunadziwika_max ndi AUC ya saxagliptin ndi metabolite yake yayikulu. Pambuyo pakukonzekera kamlomo kamodzi kwa saxagliptin pa mlingo wa 5 mg ndi odzipereka athanzi labwino, pafupifupi AUC mfundo za saxagliptin ndi metabolite yake yayikulu 78 ng × h / ml ndi 214 ng × h / ml, ndi C_max mu plasma - 24 ng / ml ndi 47 ng / ml, motsatana.

Kutalika kwapakati pa T yomaliza_1/2 saxagliptin ndi metabolite yake yayikulu inali maola a 2,5 ndi maola 3.1, motsatana, komanso kuchuluka kwa zoletsa T_1/2 Plasma DPP-4 - maola 26.9 Kuletsa kwa ntchito ya plasma DPP-4 kwa maola osachepera 24 pambuyo pa kuperekedwa kwa saxagliptin ndi chifukwa chogwirizana kwambiri ndi DPP-4 ndipo idakhalapo kwa nthawi yayitali. Kuchulukitsa kwakukulu kwa saxagliptin ndi metabolite yake yayitali pogwiritsa ntchito nthawi yayitali 1 nthawi / tsiku silinawonedwe. Panalibe kudalira kwachindunji kwa saxagliptin ndi metabolite yake yayikulu pakumwa mankhwala ndi nthawi yayitali pakumwa saxagliptin 1 nthawi / tsiku mu Mlingo kuyambira 2,5 mg mpaka 400 mg kwa masiku 14.

Pambuyo pakukonzekera pakamwa, osachepera 75% ya muyezo wa saxagliptin. Kudya sizinakhudze kwambiri pharmacokinetics ya saxagliptin mwa odzipereka athanzi. Zakudya zamafuta kwambiri sizinakhudze C_max saxagliptin, pomwe AUC idakula ndi 27% poyerekeza ndi kusala. Nthawi yoti mufikire C_max saxagliptin kuchuluka ndi pafupifupi 0,5 maola kumwa mankhwala poyerekeza ndi kusala. Komabe, zosinthazi sizofunikira pakadwala.

Kumangidwa kwa saxagliptin ndi metabolite yake yayikulu m'mapuloteni a seramu sikofunikira, chifukwa chake, titha kulingaliridwa kuti kugawa kwa saxagliptin ndikusintha kwa kapangidwe ka mapuloteni a seramu yamagazi omwe amawonekera mu hepatic kapena aimpso kulephera sikungasinthe.

Saxagliptin imapangidwa makamaka ndi kutengapo gawo kwa ma isoenzymes a cytochrome P450 3A4 / 5 (CYP 3A4 / 5) ndi mapangidwe a metabolite yogwira, mphamvu ya inhibitory yomwe motsutsana ndi DPP-4 ndi yofooka nthawi 2 kuposa saxagliptin.

Saxagliptin amamuchotsa mkodzo ndi bile. Mlingo umodzi wa 50 mg wolembedwa 14 C-saxagliptin, 24% ya mankhwalawa idachotsedwa ndi impso ngati saxagliptin wosasinthika ndi 36% monga metabolite yayikulu ya saxagliptin. Ma radioactivine omwe apezeka mumkodzo amafanana ndi 75% ya mlingo womwe unatengedwa.Chilolezo chapakati cha saxagliptin chinali pafupifupi 230 ml / mphindi, kuchuluka kwa kusefera kwa glomerular kunali pafupifupi 120 ml / mphindi. Pa metabolite yayikulu, chilolezo cha impso chinali chofanana ndi tanthauzo la kusefera kwa glomerular.

Pafupifupi 22% ya ma radioacaction athu onse adapezeka mu ndowe.

Pharmacokinetics mu milandu yapadera yamankhwala

Odwala omwe ali ndi vuto lochepetsa aimpso, AUC amagwira saxagliptin ndi metabolite yake yayikulu anali 1,2 ndi 1,7, motero, kuposa omwe ali ndi vuto laimpso. Kukula kwa mfundo za AUC sikofunikira mwakuthupi, chifukwa chake kusintha kwa mankhwalawa sikofunikira.

Odwala omwe ali ndi kuchepa kwapakati komanso mwamphamvu aimpso, komanso odwala hemodialysis, mfundo za AUC za saxagliptin ndi metabolite yake yayikulu anali 2.1 ndi 4.5 kuposa, motero, kuposa omwe ali ndi anthu omwe ali ndi vuto laimpso. Kwa odwala omwe ali ndi vuto laimpso lokwanira komanso lovuta, komanso odwala hemodialysis, mlingo wa saxagliptin uyenera kukhala 2,5 mg 1 nthawi / tsiku.

Odwala omwe ali ndi vuto lochepa kwambiri, loletsa komanso la hepatic kwambiri, panalibe kusintha kwakukulu pama pharmacokinetics a saxagliptin, kotero kusintha kwa mlingo kwa odwala kotere sikofunikira.

Odwala a zaka zapakati pa 65-80, panalibe kusiyana kwakukulu mu pharmacokinetics ya saxagliptin poyerekeza ndi odwala aang'ono (zaka 18 mpaka 40), motero, kusintha kwa mlingo kwa odwala okalamba sikofunikira. Komabe, ziyenera kukumbukiridwa kuti m'gulu ili la odwala, kuchepa kwa impso ndizotheka kwambiri.

Type 2 shuga mellitus kuwonjezera pa zakudya ndi masewera olimbitsa thupi kuti muthe kuyendetsa bwino glycemic control:

- kuyambitsa kuphatikiza mankhwala ndi metformin,

- zowonjezera pa monotherapy ndi metformin, thiazolidinediones, sulfonylurea, zotumphukira, pakalibe chitetezo chokwanira cha glycemic mu mankhwalawa.

- lembani matenda ashuga 1 (musawerenge)

- gwiritsani ndi insulin (yophunziridwa),