Mapiritsi a Vipidia - malangizo ogwiritsira ntchito ndi analog mankhwala

Mtundu wa kutulutsidwa kwa Vipidia ndi mapiritsi okhala ndi mafilimu: biconvex, oval, 12.5 mg aliyense - wachikasu, mbali imodzi amalembedwa inki ndi zolembedwa "ALG-12.5" ndi "TAK", 25 mg iliyonse - yofiyira, "ALG-25" ndi "TAK" akulembera inki mbali imodzi (7 m'matumba, matuza 4 m'bokosi lamatoni).

Piritsi 1:

• yogwira mankhwala: alogliptin - 12,5 kapena 25 mg (alogliptin benzoate - 17 kapena 34 mg),
• othandizira zigawo (12,5 / 25 mg): mannitol - 96.7 / 79.7 mg, magnesium stearate - 1.8 / 1.8 mg, croscarmellose sodium - 7.5 / 7.5 mg, microcrystalline cellulose - 22 5 / 22,5 mg, hyprolose - 4.5 / 4.5 mg,
• utoto wa makanema: hypromellose 2910 - 5.34 mg, utoto wa okusayidi wachikasu - 0,06 mg, titaniyamu - 0,6 mg, macrogol 8000 - otsata kuchuluka, inki ya imvi F1 (shellac - 26%, utoto wa ayoni wakuda - 10%, ethanol - 26%, butanol - 38%) - amatengera kuchuluka.

Mankhwala

Alogliptin ndi choletsa kusankha kwambiri cha DPP (dipeptidyl peptidase) -4 kwambiri. Kusankha kwake kwa DPP-4 kuli pafupifupi ma 10,000 kuchulukirapo kuposa momwe zimakhudzira ma enzymes ena okhudzana, makamaka DPP-8 ndi DPP-9. DPP-4 ndiye puloteni yayikulu yomwe ikukhudzidwa pakuwonongeka kwachangu kwa mahomoni a banja la apretin: glucose-insulinotropic polypeptide (HIP) komanso glucagon-peptide-1 (HIP-1). Mahomoni a banja la incretin amapangidwa m'matumbo, ndipo kuwonjezeka kwa msambo wawo kumagwirizana mwachindunji ndi chakudya. HIP ndi GLP-1 yambitsa kuphatikizika kwa insulin kapangidwe kake ndi maselo a beta omwe atulutsidwa m'ziphuphu. GLP-1 imathandizanso kupanga shuga wa glucagon komanso imalepheretsa kaphatikizidwe ka shuga.

Pachifukwa ichi, alogliptin samangowonjezera zomwe zimapangidwa, koma zimathandizanso kuphatikizira kwa glucose, ndipo amalepheretsa kubisalira kwa glucagon ndi kuchuluka kwa shuga m'magazi. Odwala omwe ali ndi matenda a shuga a mtundu wachiwiri omwe amayenda ndi hyperglycemia, kusintha kwa kaphatikizidwe ka glucagon ndi insulin kumachepetsa kuchuluka kwa hemoglobin HbA_1c ndi kuchepa kwa shuga m'magazi am'magazi utatengedwa pamimba yopanda kanthu, komanso ndende ya gluprose ya postprandial.

Pharmacokinetics

Ma pharmacokinetics a alogliptin ndi ofanana mwa anthu athanzi komanso odwala omwe ali ndi mtundu wa 2 matenda a shuga. Mtheradi bioavailability wa yogwira mankhwala pafupifupi 100%. Dongosolo la munthawi yomweyo la alogliptin lomwe lili ndi mafuta omwe amakhala ndi mafuta okwanira sizikhudza malo omwe ali munthawi yogundana (AUC), kotero Vipidia imatha kutengedwa nthawi iliyonse, mosasamala kanthu za kudya.

A pakamwa limodzi alogliptin muyezo wa 800 mg ndi anthu wathanzi kumabweretsa mayamwidwe mwachangu, momwe ambiri pazipita ndende zimatheka pambuyo 1-2 mawola kuchokera nthawi ya kukonzekera. Pambuyo mobwerezabwereza makonzedwe, kuphatikizidwa kwakukulu kwa alogliptin sikunawonedwe ngakhale kwa odwala omwe ali ndi mtundu wa 2 matenda a shuga kapena odzipereka athanzi.

AUC ya alogliptin imawonetsa kudalira kolunjika mwachindunji pamtundu wa mankhwalawa, ndikukula ndi muyeso umodzi wa Vipidia muzochitika zochizira za 6.25-100 mg. Kusintha kofananira kwa chizindikiro ichi cha pharmacokinetic pakati pa odwala ndi kochepa komanso kofanana ndi 17%.

Ndi muyezo umodzi wa AUC (0-inf), alogliptin amafanana ndi AUC (0-24) atamwa mlingo womwewo 1 nthawi patsiku kwa masiku 6. Izi zimatsimikizira kusowa kwa kudalira kwa mankhwala mu pharmacokinetics ya mankhwala atatha kubwereza.

Pambuyo kamodzi kukonzanso kwa yogwira mankhwala Vipidia pa mlingo wa 12,5 mg odzipereka athanzi, kuchuluka kwa magawo mu terminal anali 417 l, zomwe zikuwonetsa kugawa bwino kwa alogliptin mu minofu. Mlingo womangidwa kumapuloteni a plasma pafupifupi 20-30%.

Alogliptin sakukhudzidwa ndi magawo a metabolism kwambiri, chifukwa chake 60-70% ya zinthu zomwe zimapezeka mu dokotala amatulutsidwa mosasinthika mkodzo.

Ndi kukhazikitsidwa kwa 14 C-cholembedwa alogliptin mkati, kukhalapo kwa ma metabolites awiri akuluakulu adatsimikiziridwa: N-demethylated alogliptin, M-I (ochepera 1% pazinthu zoyambira) ndi N-acetylated alogliptin, M-II (zosakwana 6% pazinthu zoyambira). M-I ndi metabolite wogwira ntchito wowonetsera kwambiri zosankha zoletsa motsutsana ndi DPP-4, zofanana mu kuchitira mwachindunji alogliptin. Kwa M-II, ntchito ya inhibitory motsutsana ndi DPP-4 kapena ma enzyme ena a DPP sikuchita nawo.

Kafukufuku wa in vitro amatsimikizira kuti CYP3A4 ndi CYP2D6 amathandizira kagayidwe kochepa ka alogliptin. Zotsatira zawo zikuwonetsanso kuti chinthu chogwira ntchito cha Vipidia sichimayambitsa CYP2B6, CYP2C9, CYP1A2 ndi cholepheretsa CYP3A4, CYP1A2, CYP2D6, CYP2B6, CYP2C19, CYP2C8 kapena CYP2C9 omwe atsimikiza kuti akutsatira. Mu vrogen, alogliptin itha kuyambitsa CYP3A4 pang'ono, koma muzochitika za vivo, mawonekedwe ake osawoneka samayenderana ndi isoenzyme iyi.

Mu thupi la munthu, alogliptin si choletsa aimpso onyamula a organic cations a chachiwiri ndi aimpso onyamula organic anions a mitundu yoyamba ndi yachitatu.

Alogliptin imakhalapo makamaka mu mtundu wa (R) -enantiomer (woposa 99%) ndipo yaying'ono ngakhalenso mu vivo kapena ayi konse mukuchita nawo kusintha kwa chiral mu (S) -enantiomer. Yotsirizira satsimikiza mutatenga Vipidia mu Mlingo wothandizira.

Ndi mkamwa makonzedwe a 14 C olembedwa kuti alogliptin, zimatsimikiziridwa kuti 76% ya mankhwalawa amatengedwa kuti amkatuluka mkodzo, ndipo 13% ndi ndowe. The wamba aimpso chilolezo cha mankhwala ndi 170 ml / mphindi ndipo amapitilira muyeso kuchuluka kwa kusefera madzi pafupifupi 120 l / min, yomwe imalola kuperewera kwa alogliptin kudzera mu mphamvu ya aimpso. Pafupifupi, theka lamoyo la gawo la Vipidia ili pafupifupi maola 21.

Odwala omwe akudwala matenda a impso amalephera kusinthasintha kosiyanasiyana, kafukufuku adachitika chifukwa cha zotsatira za alogliptin atamwa tsiku lililonse 50 mg. Odwala omwe akuphatikizidwa ndi phunziroli adagawika m'magulu anayi malinga ndi njira ya Cockcroft - Gault, potengera kulephera kwa impso ndi QC (kuvomerezedwa kwa creatinine), ndikupeza zotsatirazi:

• Gulu I (kulephera kupweteka kwapakati, CC 50-80 ml / min): AUC ya alogliptin inakulitsidwa pafupifupi nthawi 1.7 poyerekeza ndi gulu loyendetsa. Komabe, kuwonjezeka kumeneku kwa AUC kudakhalabe pakati pololera gulu lolamulira,
• Gulu Lachiwiri (kulephera kwapakati paimpso, CC 30-50 ml / min): kuwonjezeka kwapafupipafupi kwa 2 AOL ya alogliptin kumawonedwa poyerekeza ndi gulu loyang'anira.
• Gulu III ndi IV (kulephera kwambiri kwaimpso, CC zosakwana 30 ml / min, ndi gawo logona la kulephera kwa impso ngati kuli kotheka, njira ya hemodialysis): AUC inachulukitsa pafupifupi kanayi poyerekeza ndi gulu lolamulira. Odwala omwe ali ndi vuto loti aimpso amatha kutenga nawo mbali mu hemodialysis atangomaliza kumwa Vipidia. Pa maola atatu a dialysis gawo, pafupifupi 7% ya mlingo wa alogliptin adachotsedwa m'thupi.

Pazifukwa izi, pagulu I, palibe chifukwa chosinthira mlingo. Odwala omwe ali ndi vuto la aimpso wolephera, kuti akwaniritse kuchuluka kwa yogwira magazi m'magazi am'magazi, pafupi ndi omwe odwala omwe ali ndi vuto laimpso, muyenera kusintha kwa mlingo wa Vipidia. Alogliptin siyikulimbikitsidwa kuti azichulukana kwambiri, komanso odwala omwe ali ndi vuto loti amalephera, nthawi zonse amakumana ndi hemodialysis.

Odwala omwe ali ndi chiwindi chosakwanira, AUC ndi kuchuluka kwambiri kwa alogliptin amachepetsa pafupifupi 10% ndi 8%, motero, poyerekeza ndi odwala omwe ali ndi chiwindi chogwira ntchito, koma izi sizimaonedwa kuti ndizofunika kwambiri. Chifukwa chake, kusintha kwa mlingo kwa Vipidia kwaofatsa pang'ono pang'ono kwa chiwindi (5- 9 point malinga ndi kukula kwa Mwana) sikufunika. Palibe zambiri zamankhwala pakugwiritsa ntchito alogliptin mwa odwala omwe ali ndi vuto loopsa la hepatic (oposa 9 mfundo).

Kulemera kwa thupi, zaka (kuphatikizapo zaka zapakati pa 65-81), mtundu ndi jenda ya odwalawa sizinawakhudze kwambiri matendawa a mankhwala, i.e. panalibe chifukwa chosinthira mlingo. Ma pharmacokinetics a alogliptin mwa odwala ochepera zaka 18 sanaphunzire.

Contraindication

• mtundu 1 shuga
• kulephera kwamphamvu kwa chiwindi (maulendo oposa 9 pamiyeso ya Mwana-Pugh, chifukwa cha kusowa kwa chidziwitso chachipatala pakuchita bwino / chitetezo chazogwiritsira ntchito),
• matenda ashuga ketoacidosis,
• aakulu mtima kulephera (FC NYHA kalasi III - IV),
• kulephera kwambiri kwaimpso
• zaka mpaka zaka 18 (chifukwa cha kusowa kwa chidziwitso pakuyenda bwino / chitetezo cha mankhwala m'gululi)
• Mimba ndi mkaka wa m`mawere (chifukwa cha kusowa kwa chidziwitso pakuyenda bwino / chitetezo cha kugwiritsa ntchito Vipidia m'gululi)
• kusalolera kwa zigawo za Vipidia, zambiri zowonjezera pamalingaliro azovuta za hypersensitivity ku inhibitor iliyonse ya DPP-4, kuphatikizapo mawonekedwe anaphylactic, angioedema ndi anaphylactic.

Achibale (matenda / mikhalidwe momwe mapiritsi a Vipidia amayenera kugwiritsidwa ntchito mosamala):

• mbiri yolemetsa yamatenda owopsa a kapamba,
• kulephera kwapakati paimpso,
• kuphatikiza kwamatsenga ndi thiazolidinedione ndi metformin,
• kuphatikiza ntchito ndi insulin kapena zotumphukira za sulfonylurea.

Malangizo ogwiritsira ntchito Vipidia: njira ndi mlingo

Mapiritsi a Vipidia amatengedwa pakamwa, mosasamala chakudyacho, kumeza lonse, osafuna kutafuna ndi kumwa ndi madzi.

Mlingo wovomerezeka tsiku lililonse ndi 25 mg mu 1 mlingo. Mankhwalawa amatengedwa okha, osakanikirana ndi metformin, thiazolidinedione, sulfonylurea zotumphukira kapena insulin, kapena monga kaphatikizidwe kamitundu itatu ndi metformin, insulin kapena thiazolidinedione.

Ngati mwaphonya piritsi mwangozi, muyenera kumwa mwachangu. Imwani kawiri mu tsiku limodzi ndizosatheka.

Vipidia ikamayikidwa, kuwonjezera pa thiazolidinedione kapena metformin, dongosolo lawo la masinthidwe sasintha.

Kuchepetsa mwayi wa hypoglycemia akaphatikizidwa ndi sulfonylurea yotengedwa kapena insulin, tikulimbikitsidwa kuti mlingo wawo ukhale wotsika.

Kukhazikitsidwa kwa kuphatikiza kwapazinthu zitatu ndi thiazolidinedione ndi metformin kumafuna kusamala (kophatikizidwa ndi chiwopsezo cha hypoglycemia, kusintha kwa mankhwalawa kwa mankhwala kungafunike).

Ngati aimpso kulephera, tikulimbikitsidwa kuyesa magwiridwe antchito ya impso musanayambe chithandizo, kenaka munthawi yamankhwala. Mlingo wa tsiku ndi tsiku kwa odwala omwe amalephera kupweteka aimpso (ndi kulephera kwa creatinine kuyambira from 30 mpaka ≤ 50 ml / min) ndi 12,5 mg. Mokulira / kudwala kwamatenda aimpso kulephera, Vipidia sichosankhidwa.

Ndemanga pa Vipidia

Nthawi zambiri, pali ndemanga zabwino za Vipidia ngati mankhwala omwe amachepetsa shuga ndikukhazikitsa kuchuluka kwamagazi. Odwala amati mphamvu ya mankhwalawa imapitirira tsiku limodzi, pomwe samakulitsa chilakolako chofuna kudya, komanso ngati gawo limodzi la mankhwala ophatikizika a hypoglycemic, amathandiza kuchepetsa kunenepa komanso amachepetsa ululu wamiyendo. Komanso, odwala amakonda mawonekedwe a Vipidia: amatha kumwa nthawi iliyonse masana.

Komabe, palinso ndemanga yoyipa yokhudza kusagwira ntchito kwa mankhwalawo komanso kuthekera kwa tsankho kwa alogliptin.

Akatswiri amachenjeza za kugwiritsa ntchito mosavomerezeka kwa Vipidia pakuchepetsa thupi.

Zambiri zamankhwala

Chida ichi chikunena za zomwe zachitika posachedwa pa shuga. Ndizoyenera kwa anthu omwe ali ndi matenda a shuga a 2. Vipidia ikhoza kugwiritsidwa ntchito yokhayokha komanso molumikizana ndi mankhwala ena a gululi.

Muyenera kumvetsetsa kuti kugwiritsa ntchito mankhwalawa mosasamala kumatha kudwalitsa wodwalayo, chifukwa chake muyenera kutsatira malangizo a dokotala. Simungagwiritse ntchito mankhwalawa osaneneka, makamaka mukamamwa mankhwala ena.

Dzinali lomwe limagulitsidwa mankhwalawa ndi Vipidia. Padziko lonse lapansi, dzina loti Alogliptin limagwiritsidwa ntchito, lomwe limachokera ku chinthu chachikulu chomwe chimapanga.

Choyimiracho chikuyimiriridwa ndi mapiritsi okhala ndi mawonekedwe owonera filimu. Amatha kukhala achikasu kapena ofiira owala (zimatengera mlingo). Phukusi limaphatikizapo 28 ma PC. - Malonda 2 mapiritsi 14.

Zotsatira za pharmacological

Chida ichi ndichotengera Alogliptin. Ichi ndi chimodzi mwazinthu zatsopano zomwe zimagwiritsidwa ntchito kuwongolera shuga. Ndi gawo la kuchuluka kwa hypoglycemic, ili ndi mphamvu.

Mukamagwiritsa ntchito, pali kuwonjezeka kwa katemera wa shuga yemwe amadalira glucose pomwe amachepetsa kupanga shuga.

Ndi matenda a shuga a 2, omwe amaphatikizidwa ndi hyperglycemia, mawonekedwe awa a Vipidia amathandizira kusintha kotere monga:

• kutsika kwa kuchuluka kwa hemoglobin ya glycated (НbА1С),
• kutsitsa shuga.

Izi zimapangitsa chida ichi kukhala chothandiza pochiza matenda ashuga.

Zizindikiro ndi contraindication

Mankhwala omwe amadziwika ndi kuchitapo kanthu mwamphamvu amafunikira kusamala kuti mugwiritse ntchito. Malangizo a iwo akuyenera kuwunikidwa mosamala, m'malo mwake amapindulitsa thupi la odwala. Chifukwa chake, mutha kugwiritsa ntchito Vipidia pokhapokha akutsimikizirani katswiri mosamalitsa pazotsatira.

Chipangizocho chikuvomerezedwa kuti chizigwiritsidwa ntchito ndi matenda a shuga a 2. Imakhala ndi malamulo a kuchuluka kwa glucose pokhapokha ngati chithandizo cha mankhwala sichigwiritsidwa ntchito ndipo zolimbitsa thupi sizofunikira. Gwiritsani ntchito bwino mankhwala a monotherapy. Amaloledwanso kugwiritsidwa ntchito kwake pamodzi ndi mankhwala ena omwe amathandizira kuchepetsa shuga.

Kusamala mukamagwiritsa ntchito mankhwalawa amayamba chifukwa cha kuponderezedwa. Ngati sangalandiridwe, chithandizo sichingagwire ntchito ndipo chingayambitse zovuta.

Vipidia saloledwa pamilandu yotsatirayi:

• tsankho limodzi ndi zigawo za mankhwala,
• mtundu 1 shuga
• kulephera kwamtima kwambiri
• matenda a chiwindi
• kuvulala kwambiri kwa impso
• Mimba ndi kuyamwa
• kukula kwa ketoacidosis yoyambitsidwa ndi matenda ashuga,
• zaka wodwala zafika 18.

Zophwanya izi ndizotsutsana kwambiri pakugwiritsa ntchito.

Palinso mayiko omwe mankhwalawa amalembedwa mosamala:

• kapamba
• aimpso kulephera zolimbitsa.

Kuphatikiza apo, chisamaliro chimayenera kuthandizidwa popereka Vipidia limodzi ndi mankhwala ena kuti azitha kuyendetsa shuga.

Zotsatira zoyipa

Pochiza ndi mankhwalawa, nthawi zina zizindikiro zosagwirizana ndi zotsatira za mankhwalawa zimachitika:

• mutu
• matenda a ziwalo kupuma
• nasopharyngitis,
• kupweteka m'mimba
• kuyabwa
• zotupa pakhungu,
• pachimake kapamba
• urticaria
• Kukula kwa chiwindi kulephera.

Zotsatira zoyipa zikachitika, pitani kuchipatala. Ngati kupezeka kwawo sikuwononga thanzi la wodwalayo, komanso kulimba kwake sikukula, chithandizo cha Vipidia chitha kupitilizidwa. Vuto lalikulu la wodwalayo limafuna kuchotsedwa kwa mankhwalawo mwachangu.

Mlingo ndi makonzedwe

Mankhwalawa amapangidwira pakamwa. Mlingo amawerengedwa payekha, molingana ndi kuopsa kwa matendawa, zaka za wodwalayo, matenda ofanana ndi zina.

Pafupifupi, amayenera kutenga piritsi limodzi lokhala ndi 25 mg ya mankhwala othandizira. Mukamagwiritsa ntchito Vipidia mu mlingo wa 12,5 mg, kuchuluka kwa tsiku ndi tsiku ndi mapiritsi awiri.

Ndikulimbikitsidwa kumwa mankhwalawa kamodzi patsiku. Mapiritsi ayenera kuledzera kwathunthu osafuna kutafuna. Ndikofunika kumwa iwo ndi madzi owiritsa. Ch phwando chololedwa chovomerezeka musanadye komanso pambuyo chakudya.

Osagwiritsa ntchito mankhwalawa pawiri ngati mankhwala atasowa - izi zitha kuyipa. Muyenera kumwa mankhwala mwachizolowezi posachedwa.

Malangizo apadera ndi kugwiritsa ntchito mankhwala osokoneza bongo

Kugwiritsa ntchito mankhwalawa, tikulimbikitsidwa kuganizira zina mwazinthu zina kuti mupewe mavuto:

1. Panthawi yobala mwana, Vipidia imatsutsana. Kafukufuku wokhudza momwe mankhwalawa amakhudzira mwana wosabadwayo sanachitike. Koma madokotala amakonda kuti asazigwiritse ntchito, kuti asachititse kuti pakhale pathupi pang'onopang'ono kapena kukula kwa zoperewera mwa mwana. Zomwezo zimapitilira kuyamwitsa.
2. Mankhwalawa sagwiritsidwa ntchito pochiza ana, chifukwa palibe chidziwitso chokwanira chokhudza thupi la ana.
3. Ukalamba wa odwala si chifukwa chosiya mankhwalawa. Koma kutenga Vipidia pankhaniyi kumafuna kuwunika madokotala. Odwala azaka zopitilira 65 ali ndi chiopsezo chowonjezereka cha matenda a impso, chifukwa chake kusamala ndikofunikira posankha mlingo.
4. Pazowonongeka zazing'onoting'ono, odwala amapatsidwa mlingo wa 12,5 mg tsiku lililonse.
5. Chifukwa choopseza kukhala ndi pancreatitis mukamagwiritsa ntchito mankhwalawa, odwala ayenera kudziwa bwino zizindikiro zazikulu za matenda awa. Akawonekera, ndikofunikira kusiya mankhwala ndi Vipidia.
6. Kumwa mankhwalawa sikuwononga kuthekera kwakukhudzidwa. Chifukwa chake, mukamagwiritsa ntchito, mutha kuyendetsa galimoto ndikuchita nawo zinthu zomwe zimafunikira chidwi. Komabe, hypoglycemia ikhoza kuyambitsa zovuta m'derali, chifukwa chake kusamala ndikofunikira.
7. Mankhwalawa amatha kusokoneza ntchito ya chiwindi. Chifukwa chake, asanaikidwe, kuyesedwa kwa thupi kuyenera.
8. Ngati Vipidia yakonzekera kugwiritsidwa ntchito limodzi ndi mankhwala ena kuti achepetse kuchuluka kwa shuga, mulingo wawo uyenera kusinthidwa.
9. Kafukufuku wokhudzana ndi momwe mankhwalawa amagwiritsidwira ntchito ndi mankhwala ena sanawonetse kusintha kwakukulu.

Zinthuzi zikazikumbukiridwa, chithandizo chitha kuthandizidwa kwambiri komanso motetezeka.

Zochita zamankhwala

Alogliptin ali ndi tanthauzo losankha zoletsa ma enzyme ena, kuphatikizapo dipeptidyl peptidase-4. Ichi ndiye puloteni yofunika kwambiri yomwe imachitapo kanthu kuwonongeka msanga kwa mahomoni mu mawonekedwe a shuga-wodalira insulinotropic polypeptide. Amapezeka m'matumbo ndipo nthawi yakudya imapangitsa kuti insulin ipange.

Peptide yokhala ndi glucone, imachepetsa kuchuluka kwa glucagon ndikulepheretsa kupanga kwa glucose m'chiwindi. Ndi kuwonjezeka pang'ono kapena kwakukulu pamlingo wa ma insretins, gawo lalikulu la mankhwala Vipidia 25, alogliptin imayamba kuwonjezera kupanga kwa insulin ndikuchepetsa glucagon ndikuwonjezera kuchuluka kwa shuga m'magazi. Zonsezi zimabweretsa kuchepa kwa hemoglobin mwa odwala omwe ali ndi matenda a shuga a mtundu wachiwiri.

Vipidia 25 kapena 12.5 mapiritsi a shuga amaloledwa kugulitsidwa m'masitolo okha mwa mankhwala.

Zizindikiro zogwiritsidwa ntchito

Vipidia 25 imasonyezedwa matenda a shuga mellitus molumikizana ndi mankhwala ena okhala ndi insulin. Mankhwalawa ndi hypoglycemic. mankhwala amkamwa, akuwonetsedwa pochiza matenda amishuga amitundu iwiri pofuna kuthana ndi matenda a glucose chifukwa chakudya komanso masewera olimbitsa thupi.

Mlingo

12,5 mg ndi 25 mg mapiritsi okhala ndi mafilimu

Piritsi limodzi lili

yogwira mankhwala: alogliptin benzoate 17 mg (wofanana ndi 12.5 mg wa alogliptin) ndi 34 mg (wofanana ndi 25 mg wa alogliptin)

Core: mannitol, cellcrystalline cellulose, hydroxypropyl cellulose, croscarmellose sodium, magnesium stearate

Zomwe zimapangidwa ndi membrane wa filimuyi: hypromellose 2910, titanium dioxide (E 171), iron oxide chikasu (E 172), iron oxide ofiira (E 172), polyethylene glycol 8000, inki ya imvi F1

Mapiritsi a Oval biconvex, opakidwa utoto wamafuta wachikaso, olembedwa "TAK" ndi "ALG-12.5" mbali imodzi ya piritsi (pamlingo wa 12.5 mg),

Mapiritsi a Oval biconvex, ophatikizidwa ndi utoto wofiirira wopepuka, wolembedwa kuti "TAK" ndi "ALG-25" kumbali imodzi ya piritsi (pamlingo wa 25 mg).

Mankhwala

Ma pharmacokinetics a alogliptin adawerengeredwa m'maphunziro omwe akukhudza onse odzipereka athanzi komanso odwala matenda a shuga a mtundu wachiwiri. Mwa odzipereka athanzi, pakapita pakamwa kamodzi mpaka 800 mg ya alogliptin, kuyamwa mwachangu kwa mankhwalawa kumawonedwa ndi kuchuluka kwa plasma kwa ola limodzi mpaka awiri kuchokera pa nthawi ya makonzedwe (a Tmax). Mutatenga mlingo wokwanira wodwala wowonjezera wa mankhwalawa (25 mg), theka lomaliza la moyo (T1 / 2) pafupifupi maola 21.

Pambuyo poyang'anira mobwerezabwereza mpaka 400 mg kwa masiku 14 kwa odwala omwe ali ndi matenda a shuga a 2, kuchuluka kwambiri kwa alogliptin kunawonedwa ndi kuwonjezeka kwa malo omwe ali pansi pa pharmacokinetic curve (AUC) komanso pazambiri za plasma ndende (Cmax) ndi 34% ndi 9%, motero. Ndi mulingo wambiri komanso zingapo za alogliptin, AUC ndi Cmax zimachulukana molingana ndi kuchuluka kwa mlingo kuchokera 25 mg mpaka 400 mg. Kuthekera kosiyanasiyana kwa AUC ya alogliptin pakati pa odwala ndi kochepa (17%).

Mtheradi bioavailability wa alogliptin pafupifupi 100%. Popeza mukamamwa alogliptin ndi chakudya chamafuta ambiri, osakhudzidwa ndi AUC ndi Cmax, mankhwalawa amatha kutengedwa mosasamala zakudya.

Pambuyo pakuwongolera kamodzi kwa alogliptin pa mlingo wa 12,5 mg mu odzipereka athanzi labwino, kuchuluka kwa magawo mu terminal anali 417 L, zomwe zikuwonetsa kuti alogliptin imagawidwa bwino mu minofu.

Kuyankhulana ndi mapuloteni a plasma ndi 20%.

Alogliptin sathanidwa ndi kagayidwe kakakulu, chifukwa chomwe 60% mpaka 71% ya mlingo womwe umayendetsedwa sichimasinthidwa mumkodzo. Pambuyo pakukonzekera kwa 14C-olembedwa alogliptin, ma metabolites ang'onoang'ono anali otsimikiza: N-demethylated alogliptin M-I (˂ osakwana 1% pazinthu zoyambira) ndi N-acetylated alogliptin M-II (˂ ochepera 6% pazinthu zoyambira). M-I ndi metabolite wogwira komanso wosankha wa DPP-4, wofanana ndi alogliptin, M-II samawonetsa zochitika zoletsa DPP-4 kapena ma enzyme ena a DPP. Kafukufuku wa in vitro awulula kuti CYP2D6 ndi CYP3A4 zimathandizira kagayidwe kochepa ka alogliptin. Alogliptin ilipo makamaka mwa mtundu wa (R) enantiomer (> woposa 99%) ndipo imasinthidwa ndi kusintha kwa chiral kukhala (S) kwakukulu mu vivo. (S) -enantiomer sazindikira pamene akumwa alogliptin mu Mlingo wa achire (25 mg).

Mutatenga 14C yolembedwa ndi alogliptin, 76% ya ma radioac yonse amatsitsidwa ndi impso ndi 13% kudzera m'matumbo, mpaka kufika pa 89%

Mlingo wothandizidwa ndi wailesi. Chilolezo cha alogliptin (9,6 L / h) chikuwonetsa kubisala kwa impso. Chilolezocho ndi 14.0 l / h.

Pharmacokinetics m'magulu apadera odwala: mkhutu waimpso

AUC ya alogliptin odwala omwe ali ndi vuto laimpso kuwonda kwambiri (60≤ creatinine chilolezo (CrCl)

Zotsatira zoyipa

Popeza mayesero azachipatala adachitika m'mikhalidwe yosiyana kwambiri, sizingatheke kuyerekeza pafupipafupi kuchuluka kwa zoyipa zomwe zimachitika pazochitika zamankhwala zomwe zimayesedwa pakamayesedwe ka mankhwala ena, ndipo pafupipafupi izi sizingasonyeze momwe mankhwalawo amagwiritsidwira ntchito.

Pakufufuza kophatikizidwa kwa mayesero 14 a chipatala olamulidwa, zochitika zonse zovuta zinali 73% mwa odwala omwe amalandila alogliptin 25 mg, 75% mu gulu la placebo, ndi 70% pagululi ndi ena. Pafupifupi, kugwiritsidwa ntchito kwa discrinuation chifukwa cha zovuta zoyipa kunali 6.8% m'gulu la 25 mg alogliptin, 8.4% mu gulu la placebo, kapena 6.2% pagululi ndi njira inanso yofananira.

Pakhala lipoti la zovuta zoyipa zopitilira 4% mwa odwala omwe adalandira alogliptin: nasopharyngitis, kupweteka kwa mutu, matenda am'mimba opatsirana.

Zotsatira zotsatirazi zikufotokozedwa mu gawo la Maupangiri apadera:

- Zokhudza chiwindi

Milandu ya hypoglycemia yanenedwa potengera kuchuluka kwa shuga wamagazi ndi / kapena zizindikiro zamankhwala ndi zizindikiro za hypoglycemia. Pakafukufuku wa monotherapy, zochitika za hypoglycemia zinaonedwa mu 1.5% ndi 1.6% ya odwala omwe ali m'magulu a alogliptin ndi placebo, motero. Kugwiritsidwa ntchito kwa alogliptin monga cholumikizira kuthandizira kwa glyburide kapena insulin sikumakulitsa chiwopsezo cha hypoglycemia poyerekeza ndi placebo. Mu kafukufuku wa monotherapy poyerekeza alogliptin ndi sulfonylureas mwa odwala okalamba, zochitika za hypoglycemia zinali 5.4% ndi 26% m'magulu a alogliptin ndi glipizide.

Zotsatira zotsatirazi zotsatirazi zidadziwika panthawi yomwe akugulitsa ntchito alogliptin - hypersensitivity (anaphylaxis, edema ya Quincke, totupa, urticaria), zotsatira zoyipa za khungu (kuphatikizapo Stevens-Johnson syndrome), ma enzymes okwera a chiwindi, kufooka kwathunthu kwa chiwindi, arthralgia yayikulu komanso yolumala. ndi pachimake kapamba, kutsegula m'mimba, kudzimbidwa, mseru, ndi matumbo.

Popeza zoyipa izi zidanenedwa mwakufuna mwa kuchuluka kwakukulu, sikungatheke kuyerekeza kuchuluka kwawo, motero kusinthaku kumawerengedwa kuti sikudziwika.

Zochita zamankhwala osokoneza bongo

Vipidium imapangidwa makamaka ndi impso ndipo imapangidwa pang'ono ndi dongosolo la enzyme ya cytochrome (CYP) P450. Mukufufuza, ayi

kulumikizana kwakukulu ndi ma substrates kapena cytochrome inhibitors kapena ndi mankhwala ena omwe amatsitsidwa kudzera mu impso.

Mu vitro kugwiritsa ntchito mankhwala

Kafukufuku wa in vitro akuwonetsa kuti alogliptin sakulowetsa CYP1A2, CYP2B6, CYP2C9, CYP2C19 ndi CYP3A4, komanso sateteza CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP3A4 ndi CYP3A4.

Mu vivo kuyanjana kwa mankhwala osokoneza bongo

Zotsatira za alogliptin pa mankhwala ena

M'mayesero azachipatala, zotsatira za alogliptin pama paracokinetic magawo a mankhwala omwe amakonzedwa ndi CYP isoenzymes kapena chowonjezera chosasinthika sichinaululidwe. Kutengera ndi zotsatira za kafukufuku wa pharmacokinetic wofotokozedwa, kusintha kwa mlingo wa Vipidia ™ sikulimbikitsidwa.

Zotsatira zamankhwala ena pa pharmacokinetics of alogliptin Palibe kusintha kwakukulu pamankhwala komwe kumachitika mu pharmacokinetics mukamagwiritsa ntchito alogliptin mogwirizana ndi metformin, cimetidine gemfibrozil (CYP2C8 / 9), pioglitazone (CYP2C8), fluconazole (CYP2C9CazCazPaz4azCazPazCaz4azcineCazPazCaz4azacazacazacazacazcazacazacazaconascazcazcazcazcazcazcazcazcazacazacaccaccazacahcaccacion.com; digoxin.

Bongo

Mlingo wapamwamba wa alogliptin m'mayesero azachipatala anali 800 mg kamodzi mwa odzipereka athanzi ndi 400 mg kamodzi patsiku kwa masiku 14 kwa odwala omwe ali ndi matenda a shuga a 2, omwe ali 32 ndi 16 kuposa nthawi yayikulu yovomerezeka ya 25 mg. Palibe zovuta zoyipa zomwe zidawonetsedwa ndi awa.

Pankhani ya mankhwala osokoneza bongo a Vipidia ™, ndikofunikira kuchotsa chinthu chosasinthika pamtunda wam'mimba ndikupereka kuyang'aniridwa kwazomwe zikufunika, komanso ndi chithandizo chamankhwala. Pambuyo pa maola atatu a hemodialysis, pafupifupi 7% ya alogliptin imatha kuchotsedwa. Chifukwa chake, kuthekera kwa hemodialysis chifukwa cha bongo ndi kosatheka. Palibe deta pakachotsa alogliptin mwa peritoneal dialysis.

Zolemba zogwiritsira ntchito

Vipidia sagwiritsidwa ntchito pochiza matenda ashuga pakati pa ana ndi achinyamata. Maupangiri ogwiritsira ntchito sakhala ndi chidziwitso pakuyesa mayeso kuchipatala m'gulu ili la odwala. Zikatero, madokotala amagwiritsa ntchito analogi.

Zochizira gulu la odwala okalamba, mankhwalawa amadziwitsa mankhwala. Kuthandizira okalamba, mlingo wa tsiku ndi tsiku umagwiritsidwa ntchito, womwe suyenera kusintha. Ngakhale simuyenera kuyiwala kuti alogliptin, yomwe yalowa m'thupi, imatha kukhudza kugwira ntchito kwa chiwindi ndi impso.

Kuchita ndi mankhwala ena

Ndi chithandizo chanthawi imodzi ndi Vipidia ndi mankhwala ena odana ndi matenda a shuga, ndikofunikira kuwerengetsa ndikusintha Mlingo kuti muchepetse kuyambika kwa hypoglycemia.

Kafukufuku sanawonetse kusintha kulikonse pakuphatikizidwa kwa alogliptin ndi magawo ena a mankhwala a shuga.

Mphamvu yamankhwala yokhudza thupi idadziwika, yomwe imaletsa kumwa mowa. Ndi zoletsedwa kugwiritsa ntchito mankhwalawa panthawi yakubala ndikudyetsa mwana chifukwa cha zovuta zake. Kafukufuku awonetsa kuti mankhwalawa samayambitsa kugona kapena kusokoneza, sangathe kusokoneza, ndikuvomerezedwa kuti azigwiritsa ntchito oyendetsa.

Timapereka kuchotsera kwa owerenga tsamba lathu!

Kukonzekera kofananako

Ngakhale palibe mankhwala omwe angakhale ndi mawonekedwe omwewo ndi zotsatira zake. Koma pali mankhwala omwe ali ofanana pamtengo, koma opangidwa kuchokera ku zinthu zina zomwe zingagwire ntchito ngati analogues a Vipidia.

Izi zikuphatikiza:

1. Januvia. Mankhwalawa amalimbikitsidwa kuti muchepetse magazi. Chosakaniza chophatikizacho ndi sitagliptin. Amatchulidwa mu milandu yomweyo Vipidia.
2. Galvus. Mankhwalawa amachokera ku Vildagliptin. Katunduyu ndi analog wa Alogliptin ndipo ali ndi katundu yemweyo.
3. Janumet. Ichi ndi mankhwala ophatikiza ndi hypoglycemic effect. Zofunikira zake ndi Metformin ndi Sitagliptin.

Ma pharmacist amathanso kupereka mankhwala ena kuti asinthe Vipidia. Chifukwa chake, sikofunikira kubisala kwa dokotala kusintha kwakuthupi komwe kumachitika chifukwa cha kudya.

Malangizo apadera ndi kulumikizana

Vitidia wa mankhwalawa sichikhudza ntchito yomwe imakhudzana ndi chidwi chowonjezeka, pomwe kuyendetsa galimoto kumaloledwa panthawi ya chithandizo. Ntchito mogwirizana ndi ena hypoglycemic mankhwala ayenera yoyang'aniridwa ndi adotolo, chifukwa pangafunike kusintha njira yochiritsirayo ndikuchepetsa. Izi zimagwirizanitsidwa ndi chiopsezo chokhala ndi vuto la hypoglycemic.

Asanapereke mapiritsi kwa odwala omwe ali ndi vuto laimpso, owonjezera amafufuzidwa kuti adziwe momwe wodwalayo akumvera mankhwalawo.

Ngati kwambiri ntchito kuwonongeka kwa impso Mankhwala amasiya, ndipo amafananizidwa. Ndi matenda ochepa a matenda, mlingo umachepetsedwa kukhala 12,5 mg. Chofunikira chachikulu cha alogliptin chimatha kupweteka pachiwindi, chomwe chimayang'aniridwa ndi matenda am'mimba.

Zizindikiro zowopsa zidzakhala mawonekedwe a zilonda pamimba ndi irradiation kumbuyo.

Ndi zizindikiro zofanana, mankhwalawa amathetsedwa.Kuchira kwa nthawi yayitali ndi Vipidia kumatha kubweretsa kuwonongeka kwa impso, koma kusintha kwa mankhwalawa sikofunikira ndi yankho lachilendo lachipatala.

Mtengo ndi fanizo

Mankhwala Vapidia - mtengo m'masitolo ogulitsa mankhwala ku Moscow amayamba pa ruble 800. Mtengo wapakati zimasiyanasiyana kuchokera ku ruble 1000 kupita ku ruble 1500.

Mndandanda wa mankhwala Vipidia: