Mankhwala Atsopano a shuga a Generation

Saxagliptin ndi mankhwala a hypoglycemic omwe amagwiritsidwa ntchito kuchipatala pochiza matenda osokoneza bongo omwe amadalira insulin. M'nkhaniyi tikambirana za saxagliptin - malangizo ogwiritsira ntchito.

Yang'anani! Mu gulu la anatomical-achire-kemikali (ATX), saxagliptin akuwonetsedwa ndi code A10BH03. Dzina Lopanda tanthauzo Lapadziko Lonse (Latin): Saxagliptin.

Kutulutsa Fomu

Saxagliptin (С18Н25N3O2, Mg = 315.41 g / mol) ili ndi mankhwala omwe amapezeka ngati oyera oyera a crystalline ufa, omwe amangosungunuka pang'ono m'madzi. Mankhwala amapezeka mu mawonekedwe a mapiritsi okhala ndi filimu ya 2,5 mg ndi 5 mg. Dzina la mankhwala ogulitsa: "Ongliza".

Pharmacodynamics ndi pharmacokinetics: malongosoledwe

Saxagliptin ndiye gliptin yachitatu yomwe ivomerezedwa ku Russia. Ma glisitins amasankha ma inhibitors a nembanemba. DPP-4 ndiyo imayambitsa kuchepa kwa ma insretins. Ma incretins amapangidwa m'maselo a endocrine a m'matumbo, chofunikira kwambiri ndi glucagon-peptide-1 (GLP-1) ndi glucose-insulinotropic polypeptide (HIP). Ma polypeptides amasungidwa atatha kudya, zomwe zimabweretsa kukondoweza kwa insulin komanso kuletsa kupanga kwa glucagon. Saxagliptin ali ndi vuto lodziletsa. Tiyenera kudziwa kuti DPP-4 imathandizira osati kuwonongeka kwa ma protein, komanso ma cytokines ndi ma peptides ena.

Pambuyo pakukonzekera pakamwa, saxagliptin imatengedwa mwachangu: misempha ya peas ya plasma imafikiridwa pambuyo 2 maola. Oral bioavailability pafupifupi 70%. Mankhwalawa amakonzedwa kudzera mu CYP3A4 ndi CYP3A5 kwa gulu lothandizira - 5-hydroxysaxagliptin (M2) - komanso ma metabolites osafunikira kwenikweni. M2 ili ndi pafupifupi theka la zochitika zamankhwala. The plasma theka-moyo ndi pafupifupi 2½ maola, ndipo M2 pafupifupi maola atatu. Mankhwalawa amachotsedwa m'thupi osasinthika (70%) komanso mkodzo (30%). Chifukwa chake, kinetics sikusintha ndi kuchepa kwa chiwindi.

Zizindikiro ndi contraindication

Kuchita bwino ndi kulolera kwa mankhwalawa kunaphunziridwa mu maphunziro 6 osindikizidwa momwe chinthu chatsopano chimayesedwa ngati monotherapy kapena adjuential therapy. Maphunzirowa sanawerenge zomwe zimapangitsa kuti pakhale kuvulala komanso kufa. Mankhwalawa sanayerekezedwe ndi ma glyptin ena.

Pakufufuza kwamaso kawiri, odwala matenda ashuga adalandira mitundu yambiri ya saxagliptin kapena placebo. Odwala sanamwe mankhwala ena a antiidiabetes. Pamalo omwe anthu amalandira "zochepa" tsiku lililonse, anthu 282 ankalandira chithandizo kwa milungu 12. Kuchiza kwa placebo kunayambitsa kuchepa pang'ono kwa HbA1c. Kutsika kwakukulu kwakukulu kunatheka m'magulu onse omwe adamwa mankhwalawa ndi saxagliptin. Zotsatira zabwino kwambiri zidaperekedwa mu tsiku la 5 mg ya saxagliptin.

Kafukufuku wachiwiri, omwe anthu 265 adakhalapo, adatenga milungu 24. Mlingo wachitatu wa mankhwalawa ndi gulu la placebo anayerekeza. Ngakhale mtengo wa HbA1c wapakati umakwera pang'ono ndi placebo, mtengo wake unatsika ndimankhwala. Kuyambira 35% mpaka 41% ya ogwiritsa ntchito anali ndi HbA1c ochepera 7%. Kuphatikiza apo, kuchuluka kwa glucose m'magazi (asanafike komanso atatha kudya 2) anali kutsika kwambiri akamagwiritsa ntchito mankhwalawa kuposa ndi placebo.

Kafukufuku wamasabata 24 adagwiritsa ntchito glibenclamide pa mlingo wa 7.5-15 mg / tsiku poyerekeza. Pakakhala vuto losakwanira, metformin idaperekedwa kwa odwala. Kafukufukuyu adakhudza anthu 768 okhala ndi mfundo zoyambirira za HbA1c kuyambira 7,5 mpaka 10%. Kuphatikiza ndi sulfonylurea, muyezo wa 2.5 mg wa saxagliptin amangochepetsa pang'ono glycated hemoglobin.

Pakafukufuku wina, odwala 565 omwe ali ndi matenda a shuga adalandira mankhwala kapena placebo kuwonjezera pa njira yokhazikika yokhazikika ndi glitazone. Phunziroli nthawi zambiri linadziwitsidwa pakuphunzira luso la pioglitazone. Phunziroli, kusintha kwakukulu kwa metabolic kumatheka patadutsa milungu 24 pogwiritsa ntchito kuphatikiza kwa zinthu.

Mwa ana ndi achinyamata ochepera zaka 18, mankhwalawa sanaphunzire. Saxagliptin ndi bwinonso kuti musamapereke mankhwala kwa amayi apakati pa nthawi yobereka.

Zotsatira zoyipa

5% ya odwala adakumana ndi kupweteka kwa mutu, kupumira kwam'mimba komanso matenda amkodzo. Zotsatira zoyipa izi zinali zofanana mu maphunziro a placebo. Sinusitis, kupweteka kwam'mimba, gastroenteritis, kapena kusanza zanenedwa zoposa 2% ya omwe amathandizidwa ndi mankhwalawa. Chiwerengero chonse cha ma lymphocyte akamagwiritsa ntchito mankhwalawa. Wodwala m'modzi anali ndi lymphocytopenia, koma kenako asayansi adazindikira kuti akupatsidwa chithandizo cha radiation.

Thupi lawo siligwirizana (urticaria, kutupa kwa nkhope) zinaonedwa mu 1.5% ya odwala omwe amalandila saxagliptin. Hypoglycemia pafupifupi nthawi zambiri amapezeka pa kuphatikiza mankhwala ndi sulfonylurea. Mwambiri, saxagliptin siyambitsa kulemera. Komabe, zotumphukira edema nthawi zambiri zimawonedwa pogwiritsa ntchito mankhwala a 5 mg patsiku. Malinga ndi kafukufuku wina, mankhwalawa amatha kuyambitsa pancreatitis yayikulu.

Mlingo ndi bongo

Mankhwalawa amavomerezedwa ngati amathandizira odwala omwe ali ndi shuga omwe amadalira insulin tsiku lililonse. Kuphatikiza ndi insulin sikulimbikitsidwa. Mu vuto la impso, mulingo wapamwamba ndi 2,5 mg / tsiku. Asanaikidwe koyamba, ndikofunikira kuyang'ana kuchuluka kwa plasma creatinine.

Kuchita

Ma inhibitors amphamvu a CYP3A4 / 5 - ketoconazole - angapangitse kuwonjezeka kwakukulu kwa milingo ya plasma ya saxagliptin. Ngati mogwirizana ndi ketoconazole afunika, tsiku lililonse mlingo sayenera upambana 2.5 mg. Ma Weaker CYP3A4 / 5 zoletsa, monga diltiazem, safuna kuchepetsa mlingo. Malinga ndi chidziwitso cha nthawi yayitali, mankhwalawa samakhudza kinetics wa mankhwala ena.

Saksagliptin - ma fanizo ndi cholowa mmalo:

Maganizo a odwala matenda ashuga komanso odwala matenda ashuga okhudza mankhwalawa.

Glyptins amagwiritsidwa ntchito kokha pochizira matenda a shuga 2. Mankhwala a gululi angayambitse hypoglycemia mu mlingo waukulu, choncho muyenera kusamala. Mwambiri, mankhwala amakhala ndi mbiri yotetezeka ya kusinthaku ndikuchita bwino.

Stanislav Alexandrovich, katswiri wa matenda ashuga

Amayika shuga pachaka chapitacho. Ndidayesa kusintha zakudya poyamba, ndimachita masewera olimbitsa thupi, koma sizinaphule kanthu. Dotolo adalemba mankhwala angapo omwe sanathandize. Ndakhala ndikumwa saxagliptin kwa miyezi itatu. Sindikumva zovuta zilizonse, koma glycemia idabwezeretsa.

Mtengo (mu Russian Federation)

Mtengo wa mankhwalawa, mosasamala ndi mlingo, ndi ma ruble 2200 pamwezi. Mankhwalawa ndi okwera mtengo kuposa vildagliptin (ma ruble 1200 pamwezi). Komabe, ngati Mlingo wolimbikitsidwa ndi wofanana sizikudziwika. Metformin ndi imodzi mwamankhwala otsika mtengo komanso othandiza kwambiri: mtengo wake ndi ma ruble 100.

Uphungu! Musanagwiritse ntchito, ndikulimbikitsidwa kukaonana ndi dokotala. Mankhwalawa amaperekedwa mosamalitsa ndi mankhwala.

Limagwirira a zochita za saxagliptin pa thupi shuga

Pochizira mafupa, owerenga athu adagwiritsa ntchito DiabeNot bwino. Kuwona kutchuka kwa malonda, tidaganiza zoperekera chidwi chanu.

Kukula kwa matenda ashuga amtundu wa 2 padziko lapansi ukukula, izi zikuchitika chifukwa cha chikhalidwe cha anthu komanso chakudya chamagulu ambiri. Komabe, pharmacology siyimayima, ndikupanga zinthu zatsopano zochizira matenda ashuga.

Chimodzi mwazinthu zatsopano za zinthu zoterezi ndi ma incretin mimetics, omwe amaphatikizapo saxagliptin.

Limagwirira a zochita za ma impretins

Ma insretins ndi mahomoni amunthu omwe amapangidwa ndi m'mimba thirakiti chakudya chikamalowa. Chifukwa cha zomwe amachita, kupanga insulini kumachulukana, komwe kumathandiza kuti glucose ayamwa, omwe amamasulidwa panthawi yokugaya.

Mpaka pano, mitundu iwiri ya ma insretins yapezeka:

• GLP-1 (glucone-monga peptide-1),
• ISU (insulinotropic polypeptide).

Ma receptor oyamba ali m'magulu osiyanasiyana, zomwe zimamupatsa mwayi wowonetsa bwino. Yachiwiri imayendetsedwa ndi ma pancreatic β-cell receptors.

Mwa zina mwazofunikira zochita:

• kuchuluka katulutsidwe wa mankhwala a insulin ndi ma cell a pancreatic,
• Kuchepetsa m'matumbo,
• kuchepetsa kupezeka kwa glucagon,
• kudya kwakachepera ndi kumva kuti mwakhuta,
• kusintha kwa mtima ndi mitsempha yamagazi, zimathandiza mu ubongo.

Pakuwonjezereka kwa kupanga kwa insulini, shuga amaphatikizidwa bwino, koma ngati zili zabwinobwino, ndiye kuti njira yobisalira imasiya ndipo munthuyo sakhala pachiwopsezo cha hypoglycemia Kutsika kwa kuchuluka kwa glucagon, wotsutsana ndi insulin, kumabweretsa kuchepetsedwa kwa kudya kwa chiwindi glycogen ndi kumasulidwa kwa shuga wamagulu, pomwe munthawi yomweyo kumathandizira kuwonjezeka kwa kumwa kwa glycogen m'misempha. Zotsatira zake, shuga imagwiritsidwa ntchito nthawi yomweyo pamalo opangira, osalowa m'magazi.

Kutulutsa kwam'mimba kuchepa, chakudya chimalowa m'matumbo m'magawo ang'onoang'ono, zomwe zimachepetsa kuyamwa kwa magazi m'magazi ndipo, chifukwa chake, kuchuluka kwake. Kuchita zinthu zing'onozing'ono, kumalowa mosavuta m'thupi. Potere, kuchepa kwa chakudya kumachepetsa kudya kwambiri.

Zowononga dongosolo la kufalikira kwazinthu za pakadali pano zadziwika kale, koma osaphunzira. Zinapezeka kuti ma insretins amathandizira β-cell ya kapamba amachira msanga.

Ndizosatheka kupeza mahomoni mu mawonekedwe awo oyera mokwanira, chifukwa chake asayansi apanga ma analogu omwe amagwira ntchito zofanana:

• kukonzanso zochita za glucone-peptide-1,
• Kuchepetsa mphamvu za ma enzyme owononga, motero kukulitsa moyo wa mahomoni.

Saxagliptin ndi wa gulu lachiwiri.

Kutulutsa Mafomu

Saxagliptin ndi gawo limodzi la mankhwala a Akulisa, omwe amagwira ntchito ngati choletsa DPP-4. Chida ichi sichiri pamndandanda wabungwe la chithandizo chamankhwala, koma chingaperekedwe kwa odwala omwe ali ndi matenda osokoneza bongo pomalizira bajeti yakomweko.

Mankhwalawa amapezeka mwa mapiritsi okhala ndi chipolopolo chachikasu, chokhala ndi 2.5 mg ya saxagliptin kapena 5 mg ya hydrochloride yake. Kuphatikizikako kumaphatikizanso magawo omwe amakhathamiritsa mphamvu ya ntchito. Mapiritsiwa alembedwa kuti awonetsetse ake.

Mapiritsi amadzaza paketi yonyamula zidutswa 10 ndi kabokosi.

Malangizo ogwiritsira ntchito

Mapiritsi amatengedwa pakamwa mosaganizira zakudya. Kapholo kam'meza lonse ndikusambitsidwa ndi madzi pang'ono. Mlingo umatengera mtundu wa chithandizo komanso thanzi la wodwala.

Pogwiritsa ntchito mosiyanasiyana, saxagliptin tikulimbikitsidwa kutenga 5 mg kamodzi patsiku.

Kuphatikiza mankhwala ndi mankhwala ena a shuga, mlingo ndi 5 mg patsiku, zomwezo zimagwiritsidwa ntchito pophatikiza omwe amagwiritsidwa ntchito kale ndi othandizira a hypoglycemic ndi saxagliptin.

Pakumayambiriro kogwiritsa ntchito chinthucho ndi metformin, mulingo wa saxagliptin ndi mamiligalamu 5, ndipo metformin ndi 500 milligrams patsiku.

Kwa odwala omwe ali ndi matenda a impso, mlingo umachepetsedwa kukhala 2,5 mg patsiku. Ngati hemodialysis imagwiritsidwa ntchito, mankhwalawa amamwa atamaliza. Zotsatira za mankhwalawa pa peritoneal dialysis sizinafufuzidwe. Mulimonsemo, asanalembe mankhwala, akatswiri amalangizidwa kuti ayesetse impso za wodwalayo.

Kwa odwala omwe ali ndi vuto la chiwindi ntchito, kusintha kwa mankhwalawa sikofunikira. Kuchiza kumachitika malinga ndi malingaliro onse. Izi zikugwiranso ntchito kwa okalamba, ngati alibe mavuto a impso.

Kafukufuku wokhudzana ndi mphamvu ya mankhwalawa pa mwana wosabadwayo mwa amayi apakati ndi ana aang'ono sichinachitike. Chifukwa chake, ndizovuta kulosera zamtsogolo. Kwa odwala awa, njira zina zotsimikiziridwa zimagwiritsidwa ntchito. Ngati mayi amatenga saxacgliptin panthawi yoyamwitsa, ayenera kukana kudyetsa.

Pankhani ya munthawi yomweyo makonzedwe othandizira a CYP3A4 / 5, mlingo wa tsiku lililonse wa mankhwalawa umachepa.

Awa ndi mankhwala awa:

• Ketoconazole,
• Clarithromycin
• Atazanavir
• Indinavir
• Nefazodon,
• Itraconazole
• Ritonavir
• Telithromycin,
• Nelfinavir
• Saquinavir ndi ena.

Mukumwa mankhwala a saxagliptin, wodwalayo amapitiliza kukhazikitsa malangizo a gulu pazakudya, amayeserera masewera olimbitsa thupi ndikuwunikira momwe munthu akumvera.

Chingalowe m'malo ndi saxagliptin ndi chiyani?

Kugwiritsa ntchito saxagliptin monga gawo lalikulu limapangidwa mu mankhwala a Onglise, ngati wodwalayo ali ndi zovuta, ayenera kugwiritsa ntchito analogues, yomwe imaphatikizapo zoletsa zina za enzyme ya DPP-4:

1. Januvia - Chimodzi mwa zida zoyambirira zamtunduwu, zopangidwa ku United States. Imazindikira mu Mlingo wa 25, 50 ndi 100 mg. Zomwe zimachitika tsiku lililonse zimakhala pafupifupi 100 mg. Zotsatira za mankhwalawa zimatha pafupifupi tsiku limodzi. Nthawi zina amapangidwa pansi pa mtundu wa YanuMet, womwe umaphatikizanso ndi metformin.
2. Galvus - mankhwala omwe amapangidwa ku Switzerland, amagwiritsidwa ntchito pa mlingo wa 50 mg tsiku lililonse kapena kupitilira apo, amagwiritsidwa ntchito limodzi ndi insulin.
3. Nesina - wopangidwa ku Ireland, kutengera apolgiptin benzoate ndi mlingo wa 12,5 kapena 25 mg. Piritsi limodzi amatengedwa kamodzi patsiku.
4. Vipidia - chinthu chachikulu cha mankhwala a alogliptin, omwe ali ndi vuto lofananalo, amatengedwa kamodzi patsiku pa mlingo wa 25 mg.
5. Trazhenta - chida chochokera linagliptin, chimadziwika ngati mapiritsi 5 mg omwe amamwa pakamwa.

Ma analogu ena amagwiritsidwa ntchito omwe ali ndi mawonekedwe osiyana, koma mawonekedwe ofanana. Mtengo wa mankhwalawa umasiyana malinga ndi dziko lakapangidwe ake komanso kapangidwe kake ka mankhwalawo.

Mtengo wa mankhwalawa Onglisa, wophatikiza saxagliptin, kuyambira 1700 mpaka 1900 rubles.

Mtundu watsopano wamankhwala umakupatsani mwayi wambiri komanso wosavuta wothana ndimatenda a shuga mwa odwala matenda ashuga.

Pomwe mndandanda wawo sunali waukulu kwambiri, ndi mankhwala amodzi okha omwe amapangidwa pamaziko a saxagliptin, omwe ali ndi zotsatira zabwino pothandizira matenda a shuga ndipo sayambitsa chikhalidwe cha hypoglycemia. Nthawi yomweyo, pali ma fanizo okhala ndi chinthu china chosiyana, koma ndimankhwala ofanana.

Lemberani mankhwala a shuga atatu

• Mitundu 1 yamankhwala
  • 1.1 Mndandanda wa mankhwala omwe amachepetsa shuga mu shuga yachiwiri
  • 1.2 Mapiritsi omwe amachititsa chidwi cha maselo ku insulin
    • 1,2.1 Thiazolidinediones
  • 1.3 Oyang'anira olamulira
  • 1.4 cy-glucosidase zoletsa
    • 1.4.1 Kuchepetsa kukana kwa insulin
  • 1.5 Mankhwala atsopano
  • 1.6 Mankhwala ena
• 2 Kodi zotsutsana ndi ziti?

Mankhwala amakono a matenda a shuga a 2 amapangitsa miyoyo ya odwala kukhala yodzaza. Amadziwika kuti shuga mellitus ndi matenda omwe amafotokozedwa mu insulin yokwanira m'thupi la munthu, zomwe zimayambitsa kusokonezeka kwa kagayidwe kazakudya.Matendawa sangathe kuchiritsidwa, monga mphuno kapena mutu. Ndikovuta kuthetsa zizindikiro za vutoli, chifukwa chake cholinga chachikulu chothandizira matenda a shuga ndikusunga momwe wodwalayo alili.

Mitundu ya mankhwala

Mapiritsi onse a shuga 2, ngakhale amagwira ntchito yayikulu yochepetsa shuga, amaphatikiza zowonjezera za odwala matenda ashuga. Mu msika, zonse zakale komanso mankhwala omwe amapezeka kale antidiabetic amafunanso chimodzimodzi. Mankhwala atsopano a shuga amagawika m'magulu angapo kutengera zikhalidwe zina. Komabe, ziyenera kukumbukiridwa kuti mankhwala a insulin am'badwo uliwonse omwe amachepetsa shuga ya magazi sangathetse vutoli. Ndikofunikira kuwunika zakudya (kupewa kunenepa kwambiri), zolimbitsa thupi, ndipo koposa zonse, kuyezetsa mayeso muzipatala nthawi yake.

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Mndandanda wamankhwala omwe amachepetsa shuga mu shuga yachiwiri

Kugwiritsa ntchito mankhwalawa chifukwa cha matendawa kumaphatikizapo kugwiritsa ntchito mankhwala ochepetsa shuga. Mapiritsi onse a shuga a 2 amawagawa m'magulu awa:

• mankhwala a greatuanide,
• dipeptidyl peptidase zoletsa - IV,
• zochokera sulfonylurea,
• incretinomimetic mankhwala,
• α-glucosidase zoletsa,
• glitazones.

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Thimang

Pioglar imakulitsa chidwi cha maselo kuti apange insulin.

Mankhwala amakono ogwirira matenda a shuga a 2 mwa achikulire ndi achinyamata, omwe amawerengera poyankha maselo ku mahomoni, amatchedwa thiazolidinediones. Mankhwala angapo awa samakhudza kugwira ntchito kwa kapamba, koma amawonjezera chiwopsezo cha maselo a cell ndi zimakhala kuti apange insulin, pomwe akusintha mbiri ya lipid. Zotsatira za hypoglycemic zachokera ku 0.5% mpaka 2%. Mwa zolakwa za chithandizo chotere, kusokonezeka kwa dongosolo la m'mimba ndikusiyanitsidwa, mankhwalawa amadziwikanso m'magulu oopsa monga aimpso kapena mtima. Njira zabwino kwambiri zothandizira mgulu lino:

Pochizira mafupa, owerenga athu adagwiritsa ntchito DiabeNot bwino. Kuwona kutchuka kwa malonda, tidaganiza zoperekera chidwi chanu.

• Piroglar
• "Diagnitazone".

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Oyang'anira Pandial

Njira zamakono zochizira matenda ashuga zimaphatikizanso kugwiritsa ntchito dongo. Gulu la mankhwalawa lili ndi nthawi yochepa, pomwe likuchepetsa kuchuluka kwa shuga chifukwa chakuchulukitsa kwa insulin. Mankhwala a Prandial a shuga amayamba kugwira ntchito atangodya, zomwe zimakhudza kapamba. Mtundu wamba:

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Α-glucosidase zoletsa

Acarbose amatseka ma enzyme ena omwe amachititsa kuti mafuta asawonongeka, omwe amalepheretsa shuga kulowa mwachangu m'magazi.

Chithandizo cha matenda amtundu wa 2 chimaphatikizanso kugwiritsa ntchito mankhwala omwewo. Mphamvu ya mankhwalawa imachitika chifukwa chakuthawa kwa zakudya zamagetsi poyimitsa ntchito ya ma enzyme omwe amachititsa kuti pakhale chakudya chamagulu ambiri. Nthawi zambiri, amapereka mankhwala okhawo omwe amapezeka mgululi, omwe amatchedwa "Acarbose". Kuchuluka kwa chakudya, mukamwa mankhwalawa, sikunasinthidwe, koma njira yothetsera imachulukirachulukira, zomwe zimachepetsa kuthekera kwa kudumpha kwa glucose.

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Kuchepetsa kukana kwa insulin

Chithandizo cha matenda amtundu wa 2 chimaphatikizaponso mankhwala othandiza omwe amachepetsa thupi kukana insulin. Mndandandandawu umaphatikizapo magome othandiza kwambiri kuchokera ku gulu la thiazolidinediones ndi biguanides. Magulu onse awiriwa ochepetsa shuga ali ndi zabwino zingapo pochiza matenda amtundu wa 2. Chifukwa choyamba chomwe zinthu zotere zimayamikiridwa ndi chiopsezo chochepa kwambiri cha hypoglycemia. Izi ndi zabwino mwanjira yochepetsera cholesterol ndipo, chifukwa chake, kuchepetsa chiopsezo cha myocardial infarction ndi zina pathologies zamtima. Komabe, mukamamwa mankhwalawa, mutha kukumana ndi zovuta kuchokera m'matumbo am'mimba.

Ngakhale mankhwala omwe amagwiritsidwa ntchito kwambiri antipyretic sangagwiritsidwe ntchito popanda mankhwala a dokotala. Kuopsa kwa matenda ashuga osakakumana ndi katswiri.

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Mankhwala atsopano

Galvus ili m'gulu lamankhwala angapo am'badwo watsopano.

Mankhwala amakono a mtundu wachiwiri wa shuga adakwanitsa kale kuti apange mbiri yabwino pamsika wa mankhwala azachipatala. Mankhwalawa amatengedwa kuti asunge glucagon ndi peptide-1 kuchokera kuzowonongeka zosawonongeka za enzyme DPP-4. Kuphatikiza apo mankhwalawa amachepetsa shuga, amakhudzanso kukula kwa glucagon, komwe, kumapangitsa kuti insulini ipangidwe. Ngakhale mapiritsi ochepetsera shuga samalimbikitsa phindu lochulukirapo, amakhala ndi zovuta zingapo. Chifukwa chake, ngati wodwalayo ali ndi mavuto ndi chiwindi, ndibwino kukana kumwa mankhwalawa. Jakisoni watsopano wa matenda a shuga a 2 (Victoza, Baeta) amagwira ntchito tsiku lonse, chifukwa chake amafunikira odwala kwambiri. Njira yatsopano yothana ndi matendawa (mndandanda):

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Mankhwala ena

Kwina konse, zotsatira zabwino zimawonekera pambuyo pa chithandizo ndi Diabeteson.

Mankhwala osokoneza bongo a matenda amtundu wa 2 amalola kugwiritsa ntchito mankhwala ena. Makamaka, kuphatikiza pazakudya zothandizira monga "Diabeteson" mu protocol ya chithandizo kwachitika kale. Mankhwala abwino aku America amenewa amakhala ngati ntchito kapamba, pomwe insulin imapangidwa bwino, ndipo chiopsezo cha hypoglycemia chimachepa. Malangizowo amamuwonetsa wodwalayo kuti ngati mumwa mapiritsi molondola, ndiye kuti zotsatira zake zabwino sizingokuyembekezerani. Komabe, kwenikweni izi sizabwino. Njira yolandirayi siiyi yayikulu ndipo siyimitsa njira yovomerezeka yochiritsira. Mulimonsemo, wina sayenera kutengeka ndi njira zosadziwika, ngati mukukayikira ndikofunikira kukaonana ndi dokotala.

Bwererani ku tebulo la zamkati

Ndi mankhwala ati omwe akuphwanya?

Mankhwala aliwonse omwe amachititsa odwala matenda a shuga kukhala ndi madigiri 2 amakhala ndi mavuto osiyanasiyana mthupi. Koma kuphatikiza pa izi, muyenera kusamala ndikumwa mankhwala ena. Ndi shuga wowonjezereka, ndizowopsa kutenga ma pinkiller amphamvu, osokoneza bongo, chifukwa momwe zochita zawo zimapangitsira kulumpha kowopsa m'magazi a magazi. Ndikofunika kuphunzira malangizo mosamala musanamwe mankhwalawo, werengani za zovuta ndi contraindication.

Mankhwala 2 a shuga a mellitus: mndandanda wa mankhwala

Mu shuga mellitus wamtundu wachiwiri, dokotala, monga lamulo, samapereka mankhwala othandizira, zochitika zolimbitsa thupi, komanso othandizira ena apadera a hypoglycemic mu mapiritsi, omwe amalola kukhalabe kwa shuga m'magazi. Mankhwala amasankhidwa molingana ndi momwe thupi la wodwalayo limakhalira, shuga m'magazi ndi mkodzo, mawonekedwe a matendawa komanso kupezeka kwa matenda ang'onoang'ono.

Masiku ano m'masitolo apadera mungapeze mndandanda waukulu wamankhwala atsopano omwe amamwa mtundu wa matenda ashuga a 2. Pakadali pano, ndikofunikira kusankha mankhwala ochepetsa shuga pokhapokha mukaonana ndi dokotala, chifukwa ndikofunikira kuti musangoganizira zonse zomwe zimapezeka ndi matendawa, contraindication, komanso mlingo woyenera. Kugwiritsa ntchito mosagwiritsa ntchito popanda upangiri wa zamankhwala kungakhale kovulaza thanzi lanu.

Ndikofunikira kudziwa kuti mankhwalawa sagwiritsidwa ntchito pochiza matenda amtundu wa 1 ana ndipo amasankhidwa payekhapayekha kwa amayi apakati.

Othandizira ochepetsa shuga a m'badwo wakale ndi watsopano agawidwa m'mitundu itatu, amasiyana mu kapangidwe ka mankhwala komanso momwe amakhudzira thupi.

Mankhwala a Sulfonamide

• Othandizanso a hypoglycemic omwe ali ndi shuga amathandizira kupanga kwambiri ndikupanga insulin m'magazi.
• Komanso, mankhwalawa amalimbikitsa chidwi cha minyewa ya ziwalo, chomwe chimakupatsani mwayi wambiri wa insulin.
• Sulfanilamides amachulukitsa kuchuluka kwa insulin zolandilira pama cell.
• Mankhwala ochepetsa shuga amathandiza kugwetsa ndikuchepetsa mapangidwe a shuga m'chiwindi.

Kwa nthawi yayitali, odwala matenda ashuga amagwiritsa ntchito mankhwala a m'badwo woyamba. Kuti apange chithandizo chanthawi zonse chamankhwala, odwala amafunika kutenga 0,5 mpaka 2 gm ya sulfonamides, womwe ndi mulingo wokwanira. Masiku ano, mankhwala azigawo zam'tsogolo amapangidwa omwe ndi othandiza kwambiri.

Mlingo wawo ndi wocheperako, zomwe zimabweretsa zotsatira zoyipa zochepa.

Monga lamulo, mankhwalawa amakhudza thupi kwa maola 6-12. Amamwa mapiritsi 0,5 musanadye kapena pambuyo chakudya kawiri pa tsiku.

Nthawi zina, dokotala amakupatsani mankhwala katatu patsiku kuti muchepetse magazi.

Kupatula kuti amachepetsa shuga m'magazi, mankhwalawa amakhala ndi phindu pamitsempha yamagazi, amasintha kayendedwe ka magazi awo ndikuletsa kuwonongeka kwa ziwiya zazing'ono. Kuphatikiza mapiritsi ochepetsa shuga am'badwo wachiwiri, amachotsedwa mwachangu mthupi ndipo samakakamiza impso, kuteteza ziwalo zamkati pakukula kwa zovuta chifukwa cha matenda ashuga amtundu wa 2.

Pakadali pano, othandizira a hypoglycemic awa monga sulfanilamides ali ndi zovuta zina:

1. Mankhwalawa mwina sangakhale oyenera kwa odwala onse.
2. Amayesetsa kuti asamapereke kwa achikulire, omwe amachotsa pang'onopang'ono mankhwala m'thupi. Kupanda kutero, mankhwalawa amatha kudziunjikira m'thupi, zomwe nthawi zambiri zimayambitsa matenda a hypoglycemic and coma.
3. Sulfanilamides amatha kukhala osokoneza bongo patapita kanthawi chifukwa chakuti zaka zisanu atagwiritsa ntchito mankhwalawa, chidwi cha zolandilira minofu pazotsatira zawo chimachepa. Zotsatira zake, ma receptor amasiya kugwira ntchito.

Kuphatikiza pazovuta za mankhwalawa ndikuti ma sulfonamides amachepetsa kwambiri shuga wamagazi, omwe angayambitse zotsatira za hypoglycemic. Mitundu yayikulu ya hypoglycemia imayamba chifukwa cha mankhwala a magulu a chlorpropamide ndi glibenclamide. Pachifukwa ichi, Mlingo wofotokozedwa ndi adotolo uyenera kuyang'aniridwa mosasamala.

Ndikofunika kukumbukira kuti glycemia imatha kubweretsa njala yambiri, kugwiritsa ntchito zakumwa zoledzeretsa, kulimbitsa thupi mwamphamvu, komanso aspirin. Chifukwa chake, musanayambe kugwiritsa ntchito mankhwalawa, muyenera kufunsa dokotala za kukhalapo kwa contraindication.

Ndani amasonyezedwa kuti amamwa mankhwala a sulfa?

Mankhwala ochepetsa shuga amtunduwu amadziwika motere:

• Mankhwalawa matenda a shuga a mtundu woyamba, ngati chithandizo chamankhwala sichilola kuti achepetse kuchuluka kwa shuga m'magazi, ndipo wodwala samadwala chifukwa chambiri.
• Ndi matenda a shuga a mtundu woyamba, ngati wodwalayo ali ndi kunenepa kwambiri.
• Ndi matenda osakhazikika a shuga a mtundu woyamba.
• Ngati wodwala samva mphamvu ya mankhwala a insulin 1 a matenda a shuga.

Nthawi zina, sulfonamides amaperekedwa limodzi ndi insulin. Izi ndizofunikira kuti muchepetse kusintha kwa insulin thupi ndikumasulira shuga yosakhazikika mu mawonekedwe okhazikika.

M'badwo woyamba sulfanilamides angathe kumwedwa musanadye chakudya. Pankhaniyi, mlingo umayikidwa payekha. Musanayambe kumwa mankhwalawa, muyenera kuphunzira malangizo mosamala.

Amamwa mankhwala ochepetsa shuga amtunduwu mosamala kwambiri muyezo wokhazikika, popeza kumwa mankhwala olakwika kungayambitse kuchepa kwamphamvu kwa magazi, chifuwa, nseru, kusanza, kusokonezeka kwa m'mimba ndi chiwindi, ndikuchepa kwa chiwerengero cha leukocytes ndi hemoglobin.

Chithandizo cha Biguanide

Mankhwala ofanana ndi omwe amachepetsa shuga amathandizanso thupi, chifukwa chomwe shuga amatha kumizidwa mwachangu ndi minofu ya minofu. Kuwonetsedwa kwa biguanides kumayenderana ndi zomwe zimapangitsa ma cell receptors, omwe amasintha kupanga kwa insulin komanso amathandizira shuga m'magazi.

Mankhwala ochepetsa shuga amenewa ali ndi zabwino zambiri:

1. Kutsika kwamwazi wamagazi.
2. Kuchepetsa shuga m'matumbo ndi kumasulidwa kwake ku chiwindi.
3. Mankhwala salola kuti glucose apangidwe m'chiwindi.
4. Mankhwala amawonjezera kuchuluka kwa zolandilira zomwe zimakhudza insulin.
5. Mankhwala osokoneza bongo amathandizira kuthana ndi kutentha mafuta osafunikira amthupi.
6. Mothandizidwa ndi mankhwalawa, zakumwa zamagazi.
7. Chilako cha wodwalayo chimachepa, chomwe chimakupatsani kuchepa thupi.

Biguanides sichikhudza kupanga insulin, imathandizira kugwiritsidwa ntchito kwa glucose mu minofu, kuwonjezera mphamvu ya insulin yomwe idayambitsidwa kapena ilipo m'thupi. Izi zimadzetsa kuti ma cell sachotsa zomwe asunga.

Chifukwa cha kuphatikiza kwa insulin mwa wodwala, kulakalaka kwambiri kumachepetsedwa, komwe kumathandiza kwambiri odwala matenda ashuga komanso anthu onenepa kapena onenepa kwambiri. Chifukwa kuchepa kwa mayamwidwe a shuga m'matumbo, mulingo wa zigawo zam'magazi m'magazi amatulutsa, zomwe zimalepheretsa kukula kwa atherosulinosis.

Komabe, Biguanides ali ndi vuto. Mankhwalawa amalola zinthu za asidi kudzikundikira m'thupi, zomwe zimapangitsa minofu hypoxia kapena kufa ndi mpweya.

Mankhwalawa ayenera kugwiritsidwa ntchito mosamala ndi matenda osokoneza bongo okalamba komanso anthu omwe ali ndi matenda am'mapapo, chiwindi ndi mtima. Kupanda kutero, odwala amatha kusanza, kusanza, kutulutsa tulo, kupweteka kwam'mimba, komanso chifuwa.

Biguanides aletsedwa kugwiritsa ntchito:

• Odwala opitilira 60
• pamaso pa mtundu uliwonse wa hypoxia,
• matenda a chiwindi ndi impso,
• Pamaso pa opaleshoni yayikulu, yotupa ndi yotupa.

Biguanides amalembedwa makamaka kwa odwala omwe ali ndi matenda a shuga a 2, okhala ndi kulemera kwakuthupi komanso osakonda kutopa ketoacidosis. Komanso, mankhwalawa amagwiritsidwa ntchito pochiza odwala matenda ashuga, omwe thupi lawo sililekerera sulfonamides kapena osokoneza bongo.

Biguanides, yemwe ali ndi dzina loti "retard" muzina, amakhudza thupi kwakutali kuposa mankhwala wamba. Muyenera kumwa mankhwalawa mukatha kudya, chinthu chosavuta - katatu patsiku, kuchita nthawi yayitali - kawiri patsiku, m'mawa ndi madzulo.

Mankhwala amtunduwu amaphatikizapo mankhwala monga adebit ndi glyformin. Komanso mankhwalawa amagwiritsidwa ntchito ndi anthu athanzi kuti achepetse kuchuluka kwa thupi.

Makhalidwe a chinthu Saksagliptin

Wothandizira hypoglycemic pakugwiritsa ntchito pakamwa ndi DPP-4 inhibitor.

Saxagliptin monohydrate ndi ufa wamakristali kuyambira kuyera kumtundu wowala wachikaso kapena wonyezimira wowoneka bwino, wopanda hygroscopic. Pang'onopang'ono sungunuka m'madzi pa kutentha kwa (24 ± 3) ° C, sungunuka pang'ono mu ethyl acetate, sungunuka mu methanol, ethanol, isopropyl mowa, acetonitrile, acetone ndi polyethylene glycol 400 (PEG 400). Kulemera molekyu ndi 333.43.

Pharmacology

Saxagliptin ndi choletsa chosankha chosinthira kusintha chopikisana cha DPP-4. Odwala omwe ali ndi matenda a shuga 2 a mellitus (DM2), makonzedwe a saxagliptin amachepetsa ntchito ya DPP-4 enzyme kwa maola 24. Atatha kuyamwa kwa glucose, kuletsa kwa DPP-4 kumapangitsa kuti chiwonetsero cha GLP-1 ndi HIP chichepe kwambiri, kuchepa kwa anthu ambiri glucagon komanso kuchuluka kwama cell a beta omwe amadalira shuga, zomwe zimabweretsa chiwopsezo cha insulin ndi C-peptide.Kutulutsidwa kwa insulin ndi maselo a beta a kapamba ndi kuchepa kwa kutulutsa kwa glucagon kuchokera ku maselo a pancreatic alpha kumabweretsa kuchepa kwa glycemia wofulumira ndi postprandial glycemia.

Kuchita Mwachipatala ndi Chitetezo

M'maso awiri akhungu, osasankhidwa, mayesero azachipatala, mankhwala a saxagliptin adalandiridwa ndi oposa 17,000 odwala T2DM.

Kuchita bwino ndi chitetezo cha saxagliptin mutatengedwa mu Mlingo wa 2,5, 5 ndi 10 mg kamodzi patsiku amaphunziridwa m'maphunziro asanu ndi limodzi amaso, owongoleredwa ndi placebo okhudza odwala 4148 omwe ali ndi matenda amtundu wa 2. Saxagliptin anali 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.

Saxagliptin adawonetsedwa ngati monotherapy kapena mankhwala ophatikiza. Kuphatikiza mankhwala omwe ali ndi saxagliptin adawonjezedwanso kwa odwala omwe samalipiridwa panthawi ya monotherapy ndi metformin, glibenclamide, thiazolidinediones kapena insulin, kapena monga poyambira kuphatikiza ndi metformin kwa odwala omwe sanapatsidwe zakudya komanso zolimbitsa thupi. Mukamamwa saxagliptin pa mlingo wa 5 mg, kuchepa kwa HbA_1s 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_1s adanenanso pambuyo pa masabata anayi ndi GPN - atatha masabata awiri.

Kafukufuku wokhudzana ndi mankhwala ophatikizika ndi saxagliptin ndi insulin (kuphatikiza ndi metformin) okhudza odwala 455 omwe ali ndi T2DM adawonetsa kuchepa kwakukulu kwa HbA_1s ndi BCP poyerekeza ndi placebo.

Kafukufuku wa mankhwala a saxagliptin osakanikirana ndi mankhwala a metformin ndi sulfonylurea mu 257 odwala omwe ali ndi T2DM adawonetsa kuchepa kwakukulu kwa HbA_lc ndi PPG poyerekeza ndi placebo kuphatikiza ndi metformin ndi zotumphukira za sulfonylurea.

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

Pakuyerekeza mwachindunji kwa odwala 858 omwe ali ndi matenda a shuga a 2, kuwonjezeredwa kwa saxagliptin 5 mg kwa metformin poyerekeza ndi kuwonjezera kwa glipizide ku metformin kuwonetsa kuchepa kwakukulu kwa HbA_1c, komabe, adalumikizidwa ndi ziwerengero zochepa kwambiri za episode za hypoglycemia - 3% ya milandu poyerekeza ndi 36.3% ndi kuwonjezera kwa glipizide, komanso kusowa kwa kuwonjezeka kwa kulemera kwa odwala omwe amalandila saxagliptin chithandizo (−1.1 makilogalamu kuchokera pamlingo woyamba mu gulu la saxagliptin, +1.1 makilogalamu m'gulu la glipizide).

Pofika sabata la 104 la mankhwala, gawo limodzi la hypoglycemia limapezeka mu 3.5% ya odwala mu saxagliptin ndi gulu la metformin ndipo mu 38.4% mu gulu la glipizide ndi metformin, kusintha kwa kulemera kwa thupi kuchokera pamlingo woyamba anali −1.5 kg ndi + 1,3 kg, motero.

Mukuwerenga WOPULUMUTSA (Kuwunika kwa zotsatira zamtima mwa odwala omwe ali ndi matenda ashuga omwe amatenga saxagliptin), zotsatira za mtima zimaphunziridwa mwa odwala 16,492 omwe ali ndi matenda a shuga 2 (12,959 odwala omwe ali ndi vuto la mtima (CVD), odwala 3,533 omwe ali ndi chiopsezo chambiri chifukwa cha zovuta zamtima) zofunikira za 6.5% ≤HbA_lc CHF, angina wosakhazikika, kapena kusinthanso kwamitsempha yama coronary poyerekeza ndi placebo (RR: 1.02, 95% CI: 0.94, 1.11). Kufa kwathunthu kunali kofanana ndi magulu a saxagliptin ndi a placebo (RR: 1.11, 95% CI: 0.96, 1.27).

Kafukufukuyu akuwonetsa kuwonjezeka kwa pafupipafupi kwa kuchipatala chifukwa cha kulephera kwa mtima mu gulu la saxagliptin (3.5%, odwala 289) poyerekeza ndi gulu la placebo (2.8%, odwala 228) okhala ndi tanthauzo lofunikira lamaumbidwe (i.e., popanda kusintha angapo malekezero) (RR: 1.27, 95% CI: 1.07, 1.51, P = 0.007). Odwala omwe ali ndi vuto la mtima kapena aimpso omwe amalandila saxagliptin analibe chiwopsezo chachikulu chokhala ndi vuto lalikulu, kuwonongeka kwachiwiri, komanso kufa kwathunthu poyerekeza ndi gulu la placebo.

Mu gulu la saxagliptin, mphamvu za HbA_lc idatchuka kwambiri, komanso kuchuluka kwa odwala omwe amafikira phindu la HbA_lcanali okwera kwambiri kuposa gulu la placebo. Nthawi yomweyo, kukulitsa kwa hypoglycemic Therapy kapena kuwonjezera kwa insulin m'gulu la saxagliptin pamafunika odwala ochepa mphamvu kuposa omwe ali mgulu la placebo.

Odwala omwe ali ndi matenda a shuga a 2 komanso odzipereka athanzi adawonetsa pharmacokinetics yofanana ya saxagliptin ndi metabolite yake yayikulu. Saxagliptin adalumikizidwa mwachangu pambuyo pakubaya pamimba yopanda kanthu ndikupanga C_max saxagliptin ndi metabolite yayikulu mu plasma kwa 2 ndi maola 4, motero. Ndi kuchuluka kwa saxagliptin mlingo, kuchuluka kwa C kunadziwika_max ndi AUC mtengo wa saxagliptin ndi metabolite yake yayikulu. Pambuyo pakukonzekera kamlomo kamodzi kwa saxagliptin pa mlingo wa 5 mg ndi odzipereka athanzi, avareji ya AUC ya saxagliptin ndi metabolite yake yayikulu inali 78 ndi 214 ng · h / ml, ndi mfundo za C_max mu plasma - 24 ndi 47 ng / ml, motsatana.

Kutalika kwapakati pa T yomaliza_1/2 saxagliptin ndi metabolite yake yayikulu inali maola 2.5 ndi 3.1, motsatana, komanso mtengo wapakati wa T_1/2 kuletsa kwa plasma DPP-4 - maola 27. Kuletsa kwa plasma DPP-4 ntchito kwa maola osachepera 24 mutatenga saxagliptin ndi chifukwa chogwirizana kwambiri ndi DPP-4 ndikumangika kwa nthawi yayitali. Kuwerengetsa kwakukulu kwa saxagliptin ndi metabolite yake yayitali pogwiritsa ntchito nthawi yayitali 1 patsiku sizinawoneke. Panalibe kudalira kwa chilolezo cha saxagliptin ndi metabolite yake yayikulu pakumwa ndi nthawi yayitali pakumwa saxagliptin 1 nthawi patsiku la 2,5 mpaka 400 mg kwa masiku 14.

Pambuyo pakukonzekera pakamwa, osachepera 75% ya muyezo wa saxagliptin unamwa. Kudya sizinakhudze kwambiri pharmacokinetics ya saxagliptin mwa odzipereka athanzi. Zakudya zamafuta kwambiri sizinakhudze C_max saxagliptin, pomwe AUC idakula ndi 27% poyerekeza ndi kusala. T_max saxagliptin ukuwonjezeka ndi pafupifupi maola 0.5 mukamamwa 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 pogwiritsa ntchito CYP3A4 / 5 isoenzymes ya cytochrome P450 ndikupanga metabolite yogwira, yomwe mphamvu yake ya DPP-4 imakhala yodziwika kawiri 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 atapezeka mumkodzo amafanana ndi 75% ya mlingo wovomerezeka wa saxagliptin. Chilolezo chapakati cha saxagliptin chinali pafupifupi 230 ml / mphindi, mtengo wa CF wamba unali pafupifupi 120 ml / mphindi. Pa metabolite yayikulu, chilolezo cha impso chinali chofanana ndi tanthauzo la CF.

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

Magulu apadera a odwala

Matenda aimpso. Odwala omwe ali ndi vuto lochepa la impso, 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 sikofunika mwakuthupi, chifukwa chake kusintha kwa mankhwalawa sikofunikira.

Odwala omwe ali ndi vuto lochepa kwambiri la impso, 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, muyezo wa saxagliptin uyenera kukhala 2.5 mg kamodzi patsiku (onani "Precautions").

Kuwonongeka kwa chiwindi. Odwala omwe ali ndi vuto lochepa kwambiri, lochepa komanso lowopsa kwa hepatic, panalibe kusintha kwakukulu pama pharmacokinetics a saxagliptin, kotero kusintha kwa mankhwalawa kwa odwala sikofunikira.

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

BMI Kusintha kwa mulingo sikulimbikitsidwa malinga ndi BMI, yomwe sinadziwike kuti ndi covariate yofunika pakuwonekera kwa saxagliptin kapena metabolite yogwira pakukhudzana ndi kuchuluka kwa anthu a pharmacokinetic.

Paulo Kusintha kwa Mlingo wotsatira jenda sikufunika. Palibe kusiyana komwe kunapezeka mu pharmacokinetics ya saxagliptin pakati pa amuna ndi akazi. Zowoneka bwino za metabolite yogwira ndizokwera 25% mwa akazi poyerekeza ndi amuna, koma kusiyana kumeneku sikungakhale kwofunikira m'chipatala. Kutengera kawerengeredwe ka anthu okhala mu pharmacokinetic, jenda sanazindikiridwe ngati covariate yofunika pakuwonekera kwa saxagliptin ndi metabolite yogwira.

Mtundu ndi fuko. Kusintha kwa Mlingo wampikisano sikulimbikitsidwa. Malinga ndi kuchuluka kwa anthu omwe amapanga pharmacokinetic, poyerekeza pharmacokinetics ya saxagliptin ndi metabolite yogwira nawo mu 309 omwe amatenga nawo mpikisano wa Caucasian komanso maphunziro ena a mitundu si a 17 omwe sanali a ku Europe (kuphatikiza mitundu isanu ndi umodzi), panalibe kusiyana kwakukulu mu pharmacokinetics ya saxagliptin ndi metabolite yogwira pakati pa anthu awiriwa.

Kugwiritsa ntchito thundu Saksagliptin

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, kuphatikizapo kuphatikiza ndi metformin posakhalitsa pakulamulira kwa glycemic kokwanira mu mankhwalawa.

- zowonjezera kuphatikiza kwa metformin ndi sulfonylurea zotumphukira popanda kupezeka koyenera kwa glycemic mu mankhwalawa.

Contraindication

Kuchulukitsa kwa chidwi cha munthu payekha, kusintha kwakukulu kwa hypersensitivity (anaphylaxis kapena angioedema) kwa DPP-4 inhibitors, lembani 1 shuga mellitus (musanaphunzire), matenda ashuga a ketoacidosis, kutenga pakati, msambo, zaka zosakwana 18 (chitetezo ndi kuchita bwino osaphunziridwa).

Mimba komanso kuyamwa

Chifukwa chakuti kugwiritsa ntchito saxagliptin panthawi yophunzira sikunaphunzire, sikuyenera kutumikiridwa panthawi yomwe muli ndi pakati.

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 kuchira kuyenera kuyimitsidwa, poganizira chiopsezo cha mwana komanso phindu la mayi.

FDA Fetal Action Gulu - B.

Kafukufuku wokwanira komanso wowongolera mosamala za kugwiritsa ntchito saxagliptin mwa amayi apakati sanachitike. Kugwiritsa ntchito pa nthawi ya pakati ndikotheka pokhapokha ngati pakufunika.

Saxagliptin imasungidwa mkaka wotsekemera makoswe pafupifupi 1: 1 ndi kuchuluka kwake m'magazi a plasma. Sizikudziwika ngati saxagliptin imasungidwa mkaka wa m'mawere wa anthu. Popeza mankhwala ambiri amatulutsidwa mkaka wa m'mawere, kusamala kuyenera kugwiritsidwa ntchito mukamagwiritsa ntchito saxagliptin mwa amayi oyamwitsa.

Mankhwala omwe amasokoneza mayamwidwe a shuga m'matumbo

Masiku ano, mankhwalawa siofala ku Russia, chifukwa amakhala ndi mtengo wokwera. Pakadali pano, mankhwalawa akutchuka kwambiri pakati pa odwala matenda ashuga chifukwa chogwira ntchito kwambiri. Wodziwika kwambiri ndi mankhwala a glucobai.

Glucobai kapena acarbose, imakuthandizani kuti muchepetse kuyamwa kwa shuga m'matumbo ndi kulowa kwake m'mitsempha yamagazi. Izi zimathandiza kutsitsa shuga m'magulu onse a shuga. Komanso, mankhwalawa amachepetsa kuchuluka kwa triglycerides m'magazi, omwe amayamba kudalira insulin kwa odwala omwe ali ndi mtundu wa 2 matenda a shuga, omwe nthawi zambiri amatsogolera ku atherosulinosis.

Nthawi zambiri, glucobai amalembedwa mtundu 2 shuga mellitus ngati chithandizo chachikulu kapena chowonjezera chophatikiza ndi sulfonamides. Mtundu wa shuga 1, mankhwalawa amagwiritsidwa ntchito molumikizana ndi kukhazikitsidwa kwa insulin m'thupi. Pankhaniyi, mlingo wa insulin womwe umayendetsedwa umachepetsedwa.

Popeza mankhwalawa samayambitsa hypoglycemic reaction, glucobai nthawi zambiri imalembedwa kwa okalamba. Pakalipano, mankhwalawa atha kukhala ndi zovuta, monga zotulutsa zotulutsa komanso kuphuka.

Glucobai sayenera kutengedwa ndi odwala osakwanitsa zaka 18, omwe ali ndi matenda am'mimba, nthawi yapakati kapena yoyamwitsa. Kuphatikiza mankhwala osavomerezeka kuti agwiritsidwe ntchito mu gastroparesis yoyambitsidwa ndi matenda amitsempha ya m'mimba.

Kugwiritsa ntchito mankhwala osokoneza bongo kumachitika m'masiku oyambirira a 0,55 magalamu katatu patsiku. Ngati ndi kotheka, mlingo umawonjezeka mpaka 0,2, 0,2 kapena 0,3 magalamu katatu patsiku. Mankhwala ambiri ali osavomerezeka. Mlingo uyenera kuwonjezeka pang'onopang'ono, m'njira imodzi mpaka milungu iwiri.

Glucobay imangotengedwa musanadye zakudya popanda kutafuna. Mankhwalawa ayenera kutsukidwa ndi madzi ochepa. Zochita za mankhwala zimayamba atangolowa m'mimba.

Momwe mungamwe mankhwala ochepetsa shuga

Mankhwala ngati Manilin a shuga amatengedwa theka la ola musanadye. Glucobai imangotengedwa musanadye, imatha kudyedwa ndi chakudya choyamba. Ngati wodwalayo adayiwala kumwa mankhwalawo musanadye, amaloledwa kumwa mankhwalawo pambuyo podyera, koma pasanathe mphindi 15 pambuyo pake.

Mulimonsemo, wodwalayo akaiwala kumwa mankhwala ochepetsa shuga, amaletsedwa kuwonjezera mlingo wa mankhwalawo mtsogolo. Muyenera kumwa mlingo wokhawo womwe mankhwala omwe dokotala amakupatsani.

Kumwa mankhwala ochepetsa shuga panthawi yoyembekezera

Pa nthawi ya pakati, kugwiritsa ntchito mankhwala ochepetsa shuga kumapangidwa, chifukwa amatha kulowa m'chiberekero cha mwana ndipo amakhala ndi vuto pa mwana wosabadwa. Pachifukwa ichi, shuga kwa amayi apakati amathandizidwa ndikupereka insulin ndikugwiritsa ntchito mankhwala othandizira.

Ngati mayi ali ndi matenda a shuga a 2 ndipo m'mbuyomu adalandira chithandizo cha mankhwala a hypoglycemic, amapitilira insulin. Nthawi yomweyo, dokotala amayang'anira wodwalayo mosamala; kuyesa magazi ndi mkodzo kumachitika pafupipafupi. Insulin imafotokozedwa kuti muyezo womwe mankhwalawa amachepetsa shuga.

Komabe, chithandizo chachikulu ndicho kutsogoza zakudya ndikusintha menyu.

Mayi woyembekezera yemwe wapezeka ndi matenda ashuga sayenera kudya zopitilira 35 kilogalamu imodzi patsiku. Kuchuluka kwa mapuloteni tsiku lililonse pa kilogalamu yolemera kumatha kukhala magalamu awiri, chakudya - 200-240 magalamu. Mafuta - 60-70 magalamu.

Ndikofunikira kusiya kotheratu zakudya zamafuta am'mimba othamanga, zomwe zimaphatikizapo zinthu za ufa, semolina, confectionery, maswiti.M'malo mwake, muyenera kudya zakudya zokhala ndi mavitamini A, B, C, D, E, michere ndi ulusi wazomera.

Bongo

Zizindikiro za kuledzera sizinafotokozeredwe kwa nthawi yayitali kugwiritsa ntchito saxagliptin mu Mlingo mpaka 80 nthawi yayikulu kuposa momwe analimbikitsira.

Chithandizo: vuto la mankhwala osokoneza bongo ayenera kugwiritsidwa ntchito ngati mankhwala. Saxagliptin ndi metabolite yake yayikulu imapukusidwa ndi hemodialysis (kuchuluka kwa excretion: 23% ya mlingo mu maola 4).

M'mayeso azachipatala olamulidwa, pamene anthu athanzi amatenga saxagliptin pakamwa kamodzi pa tsiku pa mlingo wa mpaka 400 mg / tsiku kwa masabata awiri (80 kuchulukirapo kuposa MPD), panalibe zovuta zotsatiridwa ndi madokotala komanso sizinawakhudze kwambiri pakubwera kwa QTc kapena mtima.

Chenjezo la saxagliptin

Kugwiritsa ntchito saxagliptin monga gawo limodzi la mankhwala apatatu ndi metformin ndi thiazolidinediones sikunaphunzire.

Gwiritsani ntchito limodzi ndi mankhwala omwe angayambitse hypoglycemia. Zotsatira za sulfonylureas ndi insulin zingayambitse hypoglycemia, motero, kuchepetsa chiopsezo cha hypoglycemia pogwiritsa ntchito saxagliptin, kuchepetsa mlingo wa zotumphukira za sulfonylureas kapena insulin kungafunike.

Hypersensitivity zimachitika. Zovuta zazikulu za hypersensitivity, kuphatikizapo anaphylaxis ndi angioedema, zanenedwa pakugulitsa ntchito saxagliptin. Ndi kukula kwa vuto lalikulu la hypersensitivity, muyenera kusiya kugwiritsa ntchito saxagliptin, kuwunika zina zomwe zingayambitse chitukuko, ndikuti mupatseni mankhwala ena a shuga a matenda a shuga (onani "Contraindication" ndi "Zotsatira Zowopsa").

Pancreatitis Pogwiritsa ntchito saxagliptin atangogulitsa, zalandiridwa mwadzidzidzi za milandu yamatenda owononga pancreatitis. Odwala omwe akutenga saxagliptin ayenera kudziwitsidwa za chizindikiro cha pancreatitis yayikulu - yayitali, kupweteka kwambiri pamimba. Ngati mukukayikira kupezeka kwa kapamba, muyenera kusiya kumwa saxagliptin (onani "Malingaliro pazogwiritsa ntchito" ndi "Zotsatira zoyipa").

Zomwe zimachitika pancreatitis mu kafukufukuyu WOPULUMUTSAzomwe zatsimikiziridwa malinga ndi ndondomeko yophunzirira inali 0.3% mu saxagliptin ndi magulu a placebo pagulu la odwala onse osakhazikika.

Pancreatitis Pakufufuza zotsatira za mtima wazomwe ophunzira akuchita nawo omwe ali ndi CVDs yotsimikizika kapena zoopsa zingapo za ma atherosselotic CVD (mayeso WOPULUMUTSAa) milandu yovuta kwambiri ya kapamba imatsimikiziridwa mu 17 mwa 8240 (0,2%) odwala omwe amalandila saxagliptin, poyerekeza ndi 9 mwa 8173 (0.1%) odwala omwe akulandira placebo. Zovuta za preexisting pancreatitis zimapezeka mu 88% (15/17) ya odwala omwe amalandila saxagliptin, ndi 100% (9/9) mwa omwe amalandira placebo.

Pambuyo poyambitsa makonzedwe a saxagliptin, ndikofunikira kuwunika odwala kuti azindikire zizindikiro ndi zizindikiro za kapamba. Ngati pancreatitis ikukayikira, saxagliptin iyenera kusiyidwa pomwepo ndipo njira zoyenera zitenge. Sizikudziwika ngati odwala omwe ali ndi mbiri ya pancreatitis ali pachiwopsezo chowonjezereka cha kapamba akamagwiritsa ntchito saxagliptin.

Kulephera kwa mtima. Mukuwerenga WOPULUMUTSA panali kuchuluka kwa zipatala kaamba ka kulephera kwa mtima mu gulu la saxagliptin poyerekeza ndi gulu la placebo, ngakhale kuti ubale wa causal sunakhazikitsidwe. Muyenera kusamala mukamagwiritsa ntchito saxagliptin mwa odwala omwe ali pachiwopsezo chogonekedwa kuchipatala chifukwa cha kulephera kwa mtima, monga kuchepa kwambiri kwaimpso kapena mbiri yolephera kwapakati. Odwala ayenera kudziwitsidwa ndi zomwe zimachitika chifukwa cha kulephera kwa mtima ndi kufunika kofotokozera mwadzidzidzi zinthu ngati izi (onani Pharmacodynamics).

Kulephera kwa mtima. Pakufufuza zotsatira za mtima wazomwe ophunzira akuchita nawo omwe ali ndi CVDs yotsimikizika kapena zoopsa zingapo za ma atherosselotic CVD (mayeso WOPULUMUTSA) ambiri odwala omwe adasankhidwa mwachisawawa ku gulu la mankhwala a saxagliptin (289/8280, 3.5%) adagonekedwa m'chipatala chifukwa cha kulephera kwa mtima poyerekeza ndi odwala omwe adapangidwa ndi gulu la placebo (228/8212, 2.8%). Mukamasanthula nthawi isanachitike chochitika choyamba, chiopsezo chogonekedwa m'chipatala chifukwa cha kulephera kwa mtima chinali chachikulu mu gulu la saxagliptin (RR: 1.27, 95% CI: 1.07, 1.51). Odwala omwe ali ndi vuto la mtima asanachitike komanso odwala omwe ali ndi vuto la impso anali ndi chiopsezo chachikulu cha kuchipatala chifukwa cha kulephera kwa mtima, mosasamala kanthu za mankhwalawa.

Kuopsa komanso phindu la mankhwala ziyenera kuganiziridwa kwa odwala omwe ali ndi chiopsezo chowonjezeka cha kulephera kwa mtima musanatenge saxagliptin. Odwala ayenera kuyang'aniridwa kuti azindikire ndi zizindikiro za kulephera kwa mtima panthawi yamankhwala. Odwala ayenera kudziwitsidwa ndi zomwe zimachitika chifukwa cha kulephera kwa mtima ndikuti afotokozereni mwansanga. Ndi chitukuko cha kulephera kwa mtima, munthu akuyenera kutsogoleredwa ndi miyezo yapano ya chisamaliro chachipatala ndikuwona mwayi woletsa kugwiritsa ntchito saxagliptin.

Arthralgia. Mauthenga otsatsa malonda amafotokoza ululu wolumikizana, kuphatikizapo olimba mukamagwiritsa ntchito DPP-4 zoletsa. Odwala, mpumulo wazizindikiro unawonedwa atayimitsa kukonzanso kwa saxagliptin, ndipo mwa wodwala payekhapayekha chizindikiro chimawonedwanso poyambanso kugwiritsa ntchito chimodzimodzi kapena inhibitor ina ya DPP-4. Kuyamba kwa zizindikiro mutayamba kugwiritsa ntchito mankhwalawa kumatha kufulumira kapena kuchitika nthawi yayitali. Ndi kukula kwa ululu wolumikizika kwambiri, kayendetsedwe ka saxagliptin paliponse payenera kuyesedwa.

Macrovascular zovuta. Palibe kafukufuku wazachipatala omwe adachitidwa kuti apeze umboni wotsimikizika wochepetsera chiopsezo cha zovuta zazikulu pakuchita kwa mankhwalawa saxagliptin kapena mankhwala ena aliwonse odana ndi matenda ashuga.

Gwiritsani ntchito m'magulu a odwala odwala mwapadera

Odwala ndi mkhutu aimpso ntchito. Kwa odwala omwe ali ndi vuto lochepa la impso (creatinine Cl> 50 ml / min), kusintha kwa mlingo sikofunikira. Kwa odwala omwe ali ndi kuchepa kwapakati kapena kwambiri aimpso (Cl creatinine ≤50 ml / min), komanso kwa odwala a hemodialysis, kusintha kwa mlingo kumalimbikitsidwa.

Kugwiritsa ntchito saxagliptin mwa odwala pa peritoneal dialysis sikunaphunzire.

Musanayambe chithandizo ndi saxagliptin komanso munthawi ya chithandizo, tikulimbikitsidwa kuwunika ntchito yaimpso.

Odwala omwe ali ndi vuto la chiwindi. Pankhani ya chiwindi ntchito, kufatsa, wowerengeka komanso wamphamvu mlingo sayenera.

Odwala okalamba. Mwa odwala 16,492 omwe adasinthiratu kafukufukuyu. WOPULUMUTSA, Odwala 8561 (51.9%) anali azaka 65 kapena kupitirira, ndipo odwala 2330 (14.1%) anali azaka 75 kapena kupitirira. Mwa awa, odwala 4290 azaka zapakati pa 65 ndi akulu ndi 1169 odwala wazaka 75 ndi akulu omwe adalandira saxagliptin. Malinga ndi kafukufuku wazachipatala, zothandiza komanso zodzitetezera mwa odwala azaka zapakati pa 65 ndi kupitirira, zaka 75 ndi akulu sizinasiyane ndi zofananira zomwezo mwa odwala omwe ali ndi zaka zochepa. Kusintha kwa Mlingo kwa okalamba sikofunikira. Komabe, posankha mlingo, muyenera kukumbukira kuti m'gulu lino la odwala, kuchepa kwa impso kumachitika.

Ana. Chitetezo ndikuwonetsetsa kwa odwala osaposa zaka 18 sizinaphunzire.

Kugwiritsa ntchito mogwirizana ndi zoletsa zamphamvu za CYP3A4 / 5

Mukamagwiritsidwa ntchito ndi CYP3A4 / 5 zoletsa monga ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir ndi telithromycin, mlingo wovomerezeka ndi 2.5 mg kamodzi patsiku.

Kukopa pa kuyendetsa magalimoto ndi kayendedwe kazinthu. Kafukufuku wofufuza momwe mphamvu ya saxagliptin ikuyendera magalimoto ndi kayendedwe ka zinthu sizinachitike.

Kumbukirani kuti saxagliptin ikhoza kuyambitsa chizungulire.