Thiazolidinediones: malangizo ogwiritsira ntchito ndi kagwiritsidwe ntchito kake

Mankhwala amakono amagwiritsa ntchito mitundu yosiyanasiyana ya mankhwala kuchiza matenda amtundu wa 2.

Limodzi mwa maguluwa ndi thiazolidinediones, omwe ali ndi vuto lofanananso ndi metformin.

Amakhulupirira kuti, poyerekeza ndi chinthu chomwe chatchulidwa pamwambapa, thiazolidatediones ndi otetezeka.

Kodi matendawa amathandizidwa bwanji?

Chithandizo chamakono cha matenda ashuga ndi njira zingapo.

Njira zochizira zimaphatikizapo maphunziro azachipatala, kutsatira zakudya zokhwima, kulimbitsa thupi, kugwiritsa ntchito mankhwala osokoneza bongo komanso kugwiritsa ntchito maphikidwe achire.

Kuthandiza odwala matenda ashuga kumaphatikizapo kugwiritsa ntchito mankhwala apadera kuti mukwaniritse zina mwa njira zochizira.

Zolinga zamankhwala awa ndi:

kukhalabe kuchuluka kwa insulin ya mahomoni pamlingo wofunikira,
kuchuluka kwa shuga m'magazi,
cholepheretsa kupititsa patsogolo kwa njira ya pathological,
kulowererapo kwa mawonekedwe a zovuta ndi zotsatira zoyipa.

Njira ya achire imaphatikizanso kugwiritsa ntchito magulu otsatirawa a mankhwala:

Kukonzekera kwa Sulfonylurea, komwe kumakhala pafupifupi magawo makumi asanu ndi anayi a zana onse a mankhwala ochepetsa shuga. Mapiritsi oterewa amathandizira mawonekedwe a insulin kukana.
Biguanides ndi mankhwala okhala ndi chinthu monga metformin. Gawo lake limakhala ndi phindu pa kuwonda, komanso limathandizira kuchepetsa shuga. Monga lamulo, sagwiritsidwa ntchito ngati vuto la impso ndi chiwindi, chifukwa limakhazikika mu ziwalo izi.
Alpha-glycosidase inhibitors amagwiritsidwa ntchito prophylactically kuteteza kukula kwa matenda ashuga a 2. Ubwino waukulu wa mankhwala a gululi ndikuti sotsogolera ku chiwonetsero cha hypoglycemia. Mankhwala okhala ndiwothandiza amathandizanso pakukula kwa kulemera, makamaka ngati mankhwala azakudya amatsatiridwa.
Thiazolidinediones angagwiritsidwe ntchito ngati mankhwala akuluakulu ochizira matenda am'mimba kapena pamodzi ndi mankhwala ena ochepetsa shuga. Choyambitsa chachikulu cha mapiritsi ndikuwonjezera chidwi cha insulin, motero zimapangitsa kukana. Mankhwalawa sagwiritsidwa ntchito popanga mtundu wa matenda a shuga 1, chifukwa amatha kuchita zokha pamaso pa insulin, yomwe imapangidwa ndi kapamba.

Kuphatikiza apo, meglitinides amagwiritsidwa ntchito - mankhwala omwe amachulukitsa katemera wa insulin, motero akukhudza maselo a pancreatic beta.

Kutsika kwa glucose kumawonedwa patatha mphindi khumi ndi zisanu mutamwa mapiritsi.

Chitetezo

Thiazolidinediones imapereka zotsatira zake mwakuchepetsa kukana kwa insulin. Pali ma 2 thiazolidinediones omwe amapezeka pamsika - rosiglitazone (Avandia) ndi pioglitazone (Actos). Troglitazone anali woyamba m'gulu lawo, koma adathetsedwa chifukwa adayambitsa chiwindi ntchito. Mankhwalawa amatha kugwiritsidwa ntchito ngati monotherapy, komanso kuphatikiza mankhwala ena.

Njira yamachitidwe. Thiazolidinediones imakulitsa chidwi cha insulin pochita monga minofu ya adipose, minofu ndi chiwindi, komwe zimakulitsa kugwiritsidwa ntchito kwa glucose ndikuchepetsa kaphatikizidwe kake (1,2). Njira zomwe amagwirira ntchito sizomveka bwino. Amayambitsa mtundu umodzi kapena zingapo za ma receptor omwe amachititsa kuti peroxisome proliferation (RAPP) Receptors imayambitsa kuchuluka kwa peroxisome, yomwe, imayang'anira mawonekedwe a gene (3).

Kuchita bwino Pioglitazone ndi rosiglitazone amagwiranso ntchito mofananamo kapena pang'ono pang'onopang'ono monga othandizira ena a hypoglycemic. Mtengo wapakati wa hemoglobin wa glycosylated mukamatenga rosiglitazone amatsika ndi 1,2-1,5%, ndipo kuchuluka kwa lipoproteins okwera komanso otsika kumawonjezeka. Kutengera ndi kafukufukuyu, zitha kuganiziridwa kuti chithandizo chamankhwala okhala ndi thiazolidatediones sichiri chotsika pakuthana ndi chithandizo cha metformin, koma chifukwa cha mtengo wokwera ndi zotsatirapo zake, mankhwalawa sagwiritsidwa ntchito pochiza matenda ashuga.

Zotsatira za thiazolidinediones pamtima pamtima. Mankhwala osokoneza bongo omwe ali mgululi amatha kukhala ndi anti-yotupa, antithrombotic, ndi anti-atherogenic, koma ngakhale izi, deta yomwe imawonetsa kuchepa kwa matenda amtima sichodabwitsa, ndipo kuchuluka kwa zotsatira zake ndizowopsa (4,5,6,7). Zotsatira za kusanthula kwa meta zikuwonetsa kufunikira kwa kusamala pakugwiritsa ntchito thiazolidinediones ndi rosiglitazone, pomwe deta yatsopano sikutsimikizira kapena kukana deta ya cardiotoxicity. Kuphatikiza apo, ndikofunikira kulingalira za mwayi wokhala ndi vuto la mtima. Panthawi imeneyi, sikulimbikitsidwa kugwiritsa ntchito rosiglitazone ngati nkotheka kugwiritsa ntchito mankhwala otetezeka (metformin, sulfonylureas, insulin).

Lipids. Pa mankhwalawa pioglitazone, kuchuluka kwa osachulukitsa lipids kumakhalabe kosasinthika, ndipo ndi chithandizo cha rosiglitazone, kuwonjezereka kwa kuchuluka kwa lipids kumawonedwa ndi pafupifupi 8-16%. (3)

Security edit |Mawonekedwe a thiazolidinediones

Thiazolidinediones, mwa kuyankhula kwina, glitazones, ndi gulu la mankhwala ochepetsa shuga omwe amafunitsitsa kukulitsa zotsatira za kubereka. Zochizira matenda a shuga zayamba kugwiritsidwa ntchito posachedwa - kuyambira 1996. Amaperekedwa mosamalitsa monga mankhwala.

Glitazones, kuwonjezera pa hypoglycemic action, imathandizira mtima wamtima. Ntchito yotsatirayi idawonedwa: antithrombotic, antiatherogenic, anti-kutupa. Mukamatenga thiazolidinediones, kuchuluka kwa hemoglobin ya glycated kumachepera pafupifupi 1.5%, ndipo mulingo wa HDL umakulanso.

Chithandizo cha mankhwala a mkalasi lino sichothandiza kwenikweni kuposa kuchiritsa ndi Metformin. Koma sizigwiritsidwa ntchito poyambira ndi 2 shuga. Izi ndichifukwa cha zovuta zoyipa komanso mtengo wokwera. Masiku ano, glitazones amagwiritsidwa ntchito kutsitsa glycemia wokhala ndi zotumphukira za sulfonylurea ndi metformin. Zitha kutumikiridwa padera ndi iliyonse ya mankhwalawo, komanso kuphatikiza.

Ubwino ndi zoyipa

Mwa zina mwa mankhwalawa pali zabwino komanso zoyipa:

onjezani thupi ndi 2 kg pafupifupi,
Mndandanda waukulu wazotsatira zoyipa
Sinthani mbiri ya lipid
Momwe zimakhudzira insulin kukana
ntchito yochepetsera shuga poyerekeza ndi metformin, zotumphukira za sulfonylurea,
kuthamanga kwa magazi
sinthani zinthu zomwe zikukhudza chitukuko cha atherosulinosis,
kusunga madzi, ndipo chifukwa chake, ngozi zakulephera kwamtima zimawonjezeka,
muchepetse kufooka kwa mafupa, ndikuchulukitsa chiopsezo cha
hepatotoxicity.

Njira yamachitidwe

Thiazolidinediones amachita ma receptors, omwe amathandizira kugawa ndikupeza shuga ndi ma cell. Zochita za mahomoni m'chiwindi, minofu ya adipose ndi minofu zimayenda bwino. Kuphatikiza apo, zovuta pamlingo wazizindikiro ziwiri zomaliza ndizapamwamba kwambiri.

Glitazones simalimbikitsa kupanga insulin ndi ma pancreatic β-cell. Kuchepetsa magwiridwe antchito kumatheka chifukwa chotsitsa insulin kukokana ndi zotumphukira ndikuonjezera kugwiritsidwa ntchito kwa glucose ndi minofu. Kutsitsa kwa shuga, monga lamulo, kumachitika pang'onopang'ono. Mlingo wocheperako wama glucose umawonedwa pokhapokha pakatha miyezi iwiri. Mankhwalawa amathandizidwa ndi kunenepa kwambiri.

Pali kusintha kwa kagayidwe kachakudya pochepetsa shuga la magazi. Akaphatikizidwa ndi metformin ndi sulfonylurea, zotumphukira zamkati zimasintha mwa odwala omwe ali ndi matenda amtundu wa 2, komanso kuchuluka kwam mahomoni a plasma. Glitazones amachita okha pamaso pa insulin.

Magawo a Pharmacokinetic amatha kusiyanasiyana kutengera mankhwalawo. Osawakhudza amuna ndi akazi komanso zaka. Ndi kuwonongeka kwa chiwindi mwa odwala, amasintha pharmacokinetics.

Zizindikiro ndi contraindication

Thiazolidinediones amapatsidwa mankhwala osokoneza bongo omwe amadalira shuga (mtundu 2 shuga):

monga monotherapy kwa odwala omwe amawongolera kuchuluka kwa glycemia popanda mankhwala (zakudya ndi zolimbitsa thupi),
Monga njira ziwiri zophatikizira limodzi ndi kukonzekera kwa sulfonylurea,
Monga chithandizo chachiwiri ndi metformin yoyang'anira mokwanira glycemic,
ngati katatu chithandizo cha "glitazone + metformin + sulfonylurea",
kuphatikiza ndi insulin
kuphatikiza ndi insulin ndi metformin.

Zina mwazopinga zomwe amamwa mankhwala:

tsankho
mimba / mkaka wa m`mawere
wazaka 18
Kulephera kwa chiwindi - kuuma koopsa komanso koyenera,
kulephera kwamtima kwambiri
Kulephera kwa aimpso ndikovuta.

Nkhani yavidiyo pakukonzekera kwa gulu la thiazolidinedione:

Zotsatira zoyipa

Zina mwazotsatira zoyipa pambuyo pakupeza thiazolidinediones ndi:

mwa azimayi - kusamba kwamiseche,
kulephera kwamtima,
kuphwanya ufulu wamagulu,
kuchuluka kwa michere ya chiwindi,
kuchepa magazi
achina,
hypercholesterolemia,
mutu ndi chizungulire,
kunenepa
kulakalaka
kupweteka pamimba, kukwiya,
zotupa pakhungu, makamaka urticaria,
kutupa
kutopa kwambiri
kuwonongeka kwamawonekedwe
mawonekedwe a benign - ma polyps ndi ma cysts,
chapamwamba kupuma thirakiti matenda.

Munthawi ya chithandizo, kulemera ndi zizindikiritso zimayang'aniridwa zomwe zimawonetsa kusungunuka kwa madzi. Kuwunika ntchito ya chiwindi kumachitidwanso. Kumwa pakamwa moledzera sikukhudza kwambiri glycemic control.

Mlingo, njira yoyendetsera

Glitazones amatengedwa mosasamala chakudya. Kusintha kwa magazi kwa okalamba omwe amapatuka pang'ono m'chiwindi / impso sikuchitika. Omaliza omaliza a odwala ndi omwe amatsitsa kumwa ochepa tsiku lililonse. Mlingo umatsimikiziridwa ndi dokotala payekhapayekha.

Kuyamba kwa mankhwalawa kumayamba ndi mlingo wochepa. Ngati ndi kotheka, imachulukidwa m'maganizo kutengera mankhwala. Akaphatikizidwa ndi insulin, mlingo wake umakhalabe wosasinthika kapena umachepetsa ndi malipoti a machitidwe a hypoglycemic.

Mndandanda wa Mankhwala Osokoneza Thuzi

Oimira awiri a glitazone akupezeka pamsika wamankhwala masiku ano - rosiglitazone ndi pioglitazone. Woyamba m'gululi anali troglitazone - posakhalitsa idathetsedwa chifukwa chopanga chiwindi choopsa.

Mankhwala motengera rosiglitazone akuphatikiza:

4 mg avandia - Spain,
4 mg Diagnitazone - Ukraine,
Kuthamanga pa 2 mg ndi 4 mg - Hungary.

Mankhwala okhala ndi piogitazone akuphatikiza:

Glutazone 15 mg, 30 mg, 45 mg - Ukraine,
Nilgar 15 mg, 30 mg - India,
Dropia-Sanovel 15 mg, 30 mg - Turkey,
Pioglar 15 mg, 30 mg - India,
Pyosis 15 mg ndi 30 mg - India.

Kuchita ndi mankhwala ena

Rosiglitazone. Kuledzera sikukhudza kuwongolera glycemic. Palibe kuyanjana kwakukulu ndi njira zolerera za piritsi, Nifedipine, Digoxin, Warfarin.
Pagogazone. Akaphatikizidwa ndi rifampicin, mphamvu ya pioglitazone imachepetsedwa. Mwina kuchepa pang'ono mu mphamvu ya kulera pomwe mukumwa mankhwala apiritsi. Mukamagwiritsa ntchito ketoconazole, kuyang'anira glycemic nthawi zambiri ndikofunikira.

Thiazolidinediones samangochepetsa kuchuluka kwa shuga, komanso zimakhudza dongosolo lamtima. Kuphatikiza pazopindulitsa, ali ndi zinthu zingapo zoyipa, zomwe zimakonda kwambiri ndikutukuka kwa mtima komanso kuchepa kwa mafupa.

Amagwiritsidwa ntchito mwachangu mu zovuta mankhwala, kugwiritsa ntchito thiazolidatediones popewa kukula kwa matendawa kumafunikanso kuphunzira.

Malamulo okasankhidwa

Mankhwala oyamba osankha mtundu wa matenda ashuga a 2 omwe ali m'magulu onenepa kwambiri ndi metformin kapena mankhwala ochokera ku gulu la thiazolidinediones.
Odwala omwe ali ndi thupi labwino, amakonda kukonzekera kwa sulfonylurea kapena meglitinides.
Ndi kusakwaniritsidwa kugwiritsa ntchito piritsi limodzi, monga lamulo, kuphatikiza kwa mitundu iwiri (yocheperapo katatu) imayikidwa. Kuphatikiza komwe kumagwiritsidwa ntchito kwambiri:
- sulfonylurea + metformin,
- metformin + thiazolidinedione,
- metformin + thiazolidinedione + sulfonylurea.

Kukonzekera kwa Sulfonylurea

Odziwika kwambiri ndi mankhwala okhudzana ndi mankhwala a sulfonylurea (mpaka 90% ya mankhwala onse ochepetsa shuga). Amakhulupirira kuti kuwonjezeka kwa insulin katulutsidwe ndi mankhwala a mkalasi imeneyi ndikofunikira kuthana ndi insulin ya insulin.

Kukonzekera kwachiwiri sulfonylurea ndi monga:

Gliclazide - ili ndi tanthauzo labwino pa kukoka kwa magazi, kuthamanga kwa magazi, kumakhala ndi phindu pa zovuta za shuga.
Glibenclamide - ili ndi mphamvu kwambiri pa hypoglycemic. Pakadali pano, pali zofalitsa zambiri zomwe zikuyankhula za zoyipa za mankhwalawa pamatenda a mtima.
Glipizide - ili ndi mphamvu yochepetsa shuga, koma kutalika kwa zochita kumakhala kochepa kwambiri kuposa kuja kwa glibenclamide.
Glycidone - mankhwala okhawo a gululi, omwe amaperekedwa kwa odwala omwe ali ndi vuto laimpso. Ili ndi nthawi yayifupi kwambiri yochitapo kanthu.

3 mibadwo ya 3 sulfonylurea kukonzekera kumayambitsidwa Glimeprimide:

imayamba kuchita kale ndipo imakhala nthawi yayitali (mpaka maola 24) pamlingo wotsika,
Kutheka kumwa mankhwalawa kamodzi kokha patsiku,
samachepetsa katulutsidwe ka insulin panthawi yochita masewera olimbitsa thupi,
imayambitsa kutulutsa insulin mwachangu chifukwa chakudya,
itha kugwiritsidwa ntchito pakulephera kwapakati paimpso,
ali ndi chiopsezo chochepa cha hypoglycemia poyerekeza ndi mankhwala ena mkalasiyi.

Kuchita kwakukulu kwa kukonzekera kwa sulfonylurea kumawonedwa mwa odwala omwe ali ndi matenda a shuga a 2, koma ndi thupi labwinobwino.

Fotokozerani mankhwala a sulfonylurea a matenda a shuga a 2, pamene kudya ndi kuchita zolimbitsa thupi sizithandiza.

Kukonzekera kwa Sulfonylurea ndi kotsutsana: kwa odwala omwe ali ndi matenda a shuga 1, omwe ali ndi pakati komanso nthawi yotsira, ali ndi matenda oopsa a chiwindi ndi impso, omwe ali ndi matenda osokoneza bongo. Kusamalidwa makamaka kuyenera kuchitika ngati zilonda zam'mimba komanso zam'mimba, komanso kwa odwala omwe ali ndi vuto laukali.

Malinga ndi ziwerengero, mwatsoka, gawo limodzi lokha la odwala ndi omwe amalipirira chindapusa cha matenda a shuga ogwiritsira ntchito sulfonylureas. Odwala ena amalimbikitsidwa kuphatikiza mankhwalawa ndi ena mwa matebulo ena, kapena kusinthira ku chithandizo cha insulin.

Mankhwala okhawo m'gululi metformin, yomwe imachepetsa kupanga ndi kutulutsa shuga mu chiwindi, imasintha magwiritsidwe ake a shuga ndi zotumphukira zake, imasintha kayendedwe ka magazi, komanso imapangitsa matenda a lipid metabolism. Mphamvu ya hypoglycemic imayamba patatha masiku awiri ndi atatu atayamba kumwa mankhwalawa.Nthawi yomweyo, kuchuluka kwa kudya kwamphamvu kwa glycemia kumachepa, ndipo njala imachepa.

Mbali yodziwika bwino ya metformin ndikukhazikika, komanso kuwonda - palibe amodzi anzeru a hypoglycemic omwe ali ndi izi.

Zisonyezero zakugwiritsa ntchito metformin ndi awa: mtundu wachiwiri wa shuga wambiri mwa odwala onenepa kwambiri, prediabetes, tsankho la kukonzekera kwa sulfonylurea.

Metformin imatsutsana: odwala omwe ali ndi vuto la matenda a shuga 1, oyembekezera komanso akamadyetsa, ali ndi matenda oopsa a chiwindi ndi impso, omwe ali ndi zovuta za matenda ashuga, omwe ali ndi matenda owopsa, omwe ali ndi matenda aliwonse omwe amaphatikizidwa ndi kuperewera kwa okosijeni ku ziwalo.

Alpha Glycosidase Inhibitors

Mankhwala a gululi amaphatikizapo acarbose ndi miglitol, zomwe zimachepetsa kuwonongeka kwa mafuta m'matumbo, zomwe zimapangitsa kuti shuga azikhala pang'ono m'magazi. Chifukwa cha izi, kukwera kwa shuga m'magazi pakudya kumatha, palibe chiopsezo cha hypoglycemia.

Chimodzi mwa mankhwalawa ndikuyenda bwino kwawo pakudya chakudya chamafuta ambiri. Ngati mafuta osavuta amapezeka m'zakudya za wodwalayo, chithandizo cha alpha-glycosidase inhibitors sichimapereka phindu. Kapangidwe kamene kamathandizidwe kamapangitsa mankhwala a gululi kukhala othandiza kwambiri pakudya mwachangu kwa glycemia komanso kuwuka kwakuthwa pambuyo chakudya. Komanso, mankhwalawa sikuti amachulukitsa thupi.

Alfa glycosidase zoletsa akuwonetsa odwala 2 mtundu wa shuga ndi zakudya ndi zolimbitsa thupi atatha kudya hyperglycemia atatha kudya.

Contraindication ntchito alpha-glycosidase zoletsa ndi: matenda ashuga ketoacidosis, cirrhosis, pachimake ndi matenda m'matumbo kutupa, m'mimba matenda, kuchuluka kwa kupangidwe kwa mpweya, zilonda zam'mimba, m'mimba, kutsekeka, hernias yayikulu, kuvulala kwambiri kwaimpso.

Pangamira (glitazones)

Mankhwala omwe ali mgululi akuphatikizapo pioglitazone, rosiglitazone, troglitazoneomwe amachepetsa kukana insulini, amachepetsa kutulutsa shuga mu chiwindi, amasunga ntchito ya maselo opanga insulin.

Kuchita kwa mankhwalawa ndi ofanana ndi zochita za metformin, koma amakanidwa chifukwa cha machitidwe ake osayenera - kuwonjezera pakuchepetsa insulin, mankhwala a gululi amatha kuchepetsera kukula kwa zovuta za aimpso komanso matenda oopsa a m'magazi, zimakhudza metabolid ya lipid. Koma, kumbali yake, mukamatenga glitazones, muyenera kuyang'anira ntchito ya chiwindi nthawi zonse. Pakadali pano, pali umboni kuti kugwiritsa ntchito rosiglitazone kuonjezera mwayi wa kulowerera kwamtima ndi mtima Kulephera.

Glitazones akuwonetsedwa kwa odwala omwe ali ndi matenda amtundu wa 2 matenda ovutika kudya komanso kuchita masewera olimbitsa thupi chifukwa chokhala ndi insulin.

Contraindication ndi: mtundu 1 shuga mellitus, matenda ashuga ketoacidosis, pakati ndi mkaka wa m`mawere, chiwindi matenda, kulephera kwamtima.

Meglitinides

Mankhwala omwe ali mgululi akuphatikizapo kubwezera ndi nateglinidekukhala ndi nthawi yochepa yochepetsera shuga. Meglitinides imayang'anira kuchuluka kwa glucose mukatha kudya, zomwe zimapangitsa kuti asamatsatire zakudya zowonjezera, chifukwa Mankhwala amagwiritsidwa ntchito musanadye.

Gawo lodziwika bwino la meglitinides ndi kuchepa kwakukulu kwa shuga: pamimba yopanda kanthu ndi 4 mmol / l, mutatha kudya - ndi 6 mmol / l. Mafuta a glycated hemoglobin HbA1c amachepetsa 2%. Kugwiritsa ntchito nthawi yayitali sikuti kumapangitsa kuti muchepetse kunenepa komanso sikutanthauza kusankha mankhwalawa. Kuwonjezeka kwa zotsatira za hypoglycemic kumawonedwa pakumwa mowa komanso mankhwala ena.

Chizindikiro chogwiritsidwa ntchito ndi meglitinides ndi mtundu wa 2 shuga mukadwala.

Miglitinides amatsutsana: odwala omwe ali ndi matenda a shuga 1, omwe ali ndi matenda ashuga a ketoacidosis, azimayi oyembekezera komanso oyamwitsa, amawonjezera chidwi cha mankhwalawa.

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Hypoglycemic kapena antidiabetesic mankhwala ndi mankhwala omwe amachepetsa shuga ya magazi ndipo amagwiritsidwa ntchito pochiza matenda ashuga.

Pamodzi ndi insulin, makonzedwe ake omwe ndi oyenera kungogwiritsa ntchito makolo, pali zinthu zingapo zomwe zimapangidwa zomwe zimakhala ndi vuto la hypoglycemic ndipo zimagwira ntchito mukamamwa. Kugwiritsa ntchito kwakukulu kwa mankhwalawa ndi mtundu wa 2 shuga.

Ma oral hypoglycemic (hypoglycemic) amatha kufotokozedwa motere:

— zochokera sulfonylurea (glibenclamide, glycidone, glyclazide, glimepiride, glipizide, chlorpropamide),

— meglitinides (nateglinide, repaglinide),

— khwawa (buformin, metformin, phenformin),

— kachikachiyama (pioglitazone, rosiglitazone, ciglitazone, englitazone, troglitazone),

— alpha glucosidase zoletsa (acarbose, miglitol),

Hypoglycemic katundu mu sulfonylurea zotumphukira adapezeka mwangozi. Kuthekera kwa mankhwala opanga gululi kukhala ndi vuto la hypoglycemic kunapezeka mu 50s, mwa odwala omwe amalandila antibacterial sulfonamide mankhwala ochizira matenda opatsirana, kuchepa kwa shuga m'magazi kunadziwika. Pankhaniyi, kusaka kunayamba kuchokera kwa sulfonamides okhala ndi tanthauzo la hypoglycemic mu 50s. Kuphatikizika kwa mankhwala oyamba a sulfonylurea omwe angagwiritsidwe ntchito pochiza matenda a shuga kunachitika. Mankhwala oyamba oterewa anali carbutamide (Germany, 1955) ndi tolbutamide (USA, 1956). M'zaka 50 zoyambirira. zotumphukira za sulfonylurea tsopano zayamba kugwiritsidwa ntchito pakuchipatala. Mu 60-70s. sulfonylureas wa m'badwo wachiwiri adawonekera. Woimira woyamba wa m'badwo wachiwiri wa sulfonylurea kukonzekera - glibenclamide - adayamba kugwiritsidwa ntchito pochiza matenda ashuga mu 1969, mu 1970 adayamba kugwiritsa ntchito glibornuride, kuyambira 1972 - glipizide. Gliclazide ndi glycidone adawoneka pafupifupi nthawi yomweyo.

Mu 1997, repaglinide (gulu la meglitinides) idavomerezeka pochiza matenda ashuga.

Mbiri yakagwiritsidwe ntchito ka nkhokwe zazikulu imayambika ku Middle Ages, pomwe chomera chimagwiritsidwa ntchito pochiza matenda ashuga Galega officinalis (kakombo wa ku french).

Thiazolidinediones (glitazones) adalowa mchitidwe wakuchipatala mu 1997. Mankhwala oyamba ovomerezeka kuti agwiritsidwe ntchito ngati hypoglycemic othandizira anali troglitazone, koma mu 2000 kugwiritsidwa ntchito kwake kunaletsedwa chifukwa cha hepatotoxicity yayikulu. Mpaka pano, mankhwala awiri ochokera pagululi amagwiritsidwa ntchito - pioglitazone ndi rosiglitazone.

Machitidwe sulfonylureas makamaka omwe amakhudzidwa ndi kukondoweza kwa maselo a pancreatic beta, limodzi ndi kusuntha komanso kuwonjezeka kwa kutulutsa kwa insulin.

Ndi chithandizo cha nthawi yayitali ndi zotumphukira za sulfonylurea, mphamvu zawo zoyambirira za kutulutsa insulin zimatha. Amakhulupirira kuti izi zimachitika chifukwa cha kuchepa kwa chiwerengero cha ma cell a beta. Pambuyo pakupuma kwa mankhwalawa, momwe maselo a beta amamwa mankhwalawa amabwezeretsedwa.

Ma sulfonylureas ena amakhalanso ndi zowonjezera-pancreatic. Zotsatira za extrapancreatic sizofunika kwambiri pakukhudzika, zimaphatikizira kuwonjezeka kwa minyewa yodalira insulin kuti ithetse insulin komanso kuchepa kwa mapangidwe a shuga m'chiwindi. Kupanga kwa chitukuko cha zotsatirazi kumachitika chifukwa chakuti mankhwalawa (makamaka glimepiride) amawonjezera kuchuluka kwa zolandilira zomwe zimapangitsa chidwi cha insulin pama cell azisulo, kusintha insulin-receptor mogwirizana, ndikubwezeretsa kutulutsa kwa chizindikiro cha postreceptor.

Kuphatikiza apo, pali umboni kuti prizvodnye sulfonylureas imalimbikitsa kutulutsidwa kwa somatostatin ndipo potero amalepheretsa kubisalira kwa glucagon.

Mbadwo: tolbutamide, carbamide, tolazamide, acetohexamide, chlorpropamide.

M'badwo wachiwiri: glibenclamide, glisoxepide, glibornuril, glycidone, glyclazide, glipizide.

M'badwo wachitatu: glimepiride.

Pakadali pano, ku Russia, kukonzekera kwa m'badwo woyamba sikugwiritsidwa ntchito.

Kusiyanitsa kwakukulu pakati pa mankhwala a m'badwo wachiwiri ndi mankhwala a sulfonylurea a m'badwo woyamba ndi ntchito yayikulu (nthawi 50-100), yomwe imawathandiza kugwiritsidwa ntchito Mlingo wochepa, motero, imachepetsa mwayi wokhala ndi zotsatirapo zoyipa. Oimira pawokha a hypoglycemic ofanana a sulfonylureas a 1st ndi 2nd m'badwo amasiyana muzochitika ndi kulolerana. Chifukwa chake, mankhwalawa a mankhwala a mibadwo yoyamba - tolbutamide ndi chlorpropamide - 2 ndi 0,75 g, motero, ndi mankhwala a m'badwo wachiwiri - glibenclamide - 0,02 g, glycvidone - 0,06-0.12 g. .

Kukonzekera kwa Sulfonylurea kumakhala kosiyanasiyana komanso nthawi yayitali, yomwe imasankha kusankha kwa mankhwala akaperekedwa. Glibenclamide ili ndi zotchulidwa kwambiri za hypoglycemic zomwe zimachokera ku sulfonylurea. Amagwiritsidwa ntchito ngati cholozera pakuwona zotsatira za hypoglycemic ya mankhwala omwe apangidwa kumene. Mphamvu ya hypoglycemic yamphamvu kwambiri ya glibenclamide imachitika chifukwa chakuti imakhala ndi mgwirizano wapamwamba kwambiri pa njira zotengera potaziyamu za ATP zotengera maselo a pancreatic beta. Pakadali pano, glibenclamide imapangidwa zonse ngati mawonekedwe a miyeso yachikhalidwe komanso mawonekedwe ojambula - mawonekedwe apadera a glibenclamide omwe amapereka chidziwitso choyenera cha pharmacokinetic ndi pharmacodynamic chifukwa cha kuthira mwachangu komanso kwathunthu (bioavailability ndi pafupifupi 100%) ndikupanga kugwiritsa ntchito mankhwala mu Mlingo wocheperako.

Gliclazide ndi wachiwiri wofala kwambiri pamlomo wa hypoglycemic pambuyo pa glibenclamide. Kuphatikiza pa mfundo yoti gliclazide ili ndi vuto la hypoglycemic, imasintha magawo a hematological, magazi a magazi, imakhudzanso dongosolo la heestatic ndi microcirculation, imalepheretsa kukula kwa microvasculitis, kuphatikiza kuwonongeka kwa retina, tikulephera kuphatikizika kwa kupatsidwa zinthu za m'magazi, kumachulukitsa kalozera wosagwirizana, kumawonjezera ntchito ya heparin ndi fibrinolytic, kumawonjezera kulolerana kwa heparin, ndikuwonetsanso katundu wa antioxidant.

Glycvidone ndi mankhwala omwe angagwiritsidwe ntchito kwa odwala omwe ali ndi kuchepa kwa aimpso, chifukwa 5% yokha ya metabolites omwe amuchotsa kudzera mu impso, ena onse (95%) - kudzera m'matumbo.

Glipizide, wokhala ndi mphamvu yotchulidwa, imakhala ndi chiopsezo chochepa kwambiri poyerekeza ndi hypoglycemic reaction, popeza sichipanga ndipo ilibe metabolites yogwira.

Mankhwala othandizira pakamwa ndi mankhwala akuluakulu othandizira odwala matenda a shuga 2 a mellitus (osagwirizana ndi insulin) ndipo nthawi zambiri amalembedwa kwa odwala omwe ali ndi zaka zopitilira 35 popanda ketoacidosis, kuperewera kwa zakudya, zovuta kapena zovuta zokhudzana ndi matenda omwe amafunikira insulin.

Kukonzekera kwa gulu la sulfonylurea sikulimbikitsidwa kwa odwala omwe, pakudya koyenera, tsiku lililonse insulin imaposa 40 mayunitsi. Komanso, samalembedwa kwa odwala omwe ali ndi mitundu yayikulu ya matenda osokoneza bongo a mellitus (omwe ali ndi vuto lalikulu la beta-cell), omwe ali ndi mbiri ya ketosis kapena matenda ashuga, omwe ali ndi hyperglycemia pamtunda wa 13.9 mmol / L (250 mg%) pamimba yopanda kanthu komanso glucosuria wamkulu pazakudya.

Kusamutsa chithandizo ndi sulfonylurea kukonzekera kwa odwala matenda a shuga omwe ali pa insulin chithandizo ndikotheka ngati zovuta za carbohydrate metabolism zidzalipiridwa pa insulin Mlingo wochepera 40 mayunitsi / tsiku. Pa Mlingo wa insulin mpaka 10 mayunitsi / tsiku, mutha kusinthira ku mankhwalawa ndi mankhwala a sulfonylurea.

Kugwiritsa ntchito kwa nthawi yayitali mankhwala a sulfonylurea kungayambitse kukana, komwe kumatha kugonjetsedwa ndi kuphatikiza mankhwala ndi insulin. Mtundu woyamba wa matenda a shuga 1, kuphatikiza kwa insulin kukonzekera ndi zotumphukira za sulfonylurea kumapangitsa kuti kuchepetsedwa kusowa kwa insulin tsiku ndi tsiku ndikuthandizanso kusintha njira ya matendawa, kuphatikizapo kufupikitsa kuchepa kwa retinopathy, komwe kumalumikizana ndi ntchito ya angioprotective ya zotumphukira za sulfonylurea (makamaka m'badwo Wachiwiri). Nthawi yomweyo, pali zisonyezo za kuthekera kwawo kwa ma atherogenic.

Kuphatikiza apo, mankhwala a sulfonylurea amaphatikizidwa ndi insulin (kuphatikiza koteroko kumawoneka koyenera ngati vuto la wodwalayo silikuyenda bwino ndi 100 IU ya insulin patsiku), nthawi zina amaphatikizidwa ndi biguanides ndi acarbose.

Mukamagwiritsa ntchito mankhwala a sulfonamide hypoglycemic, ziyenera kukumbukiridwa kuti antibacterial sulfonamides, anticoagulants, butadion, salicylates, ethionamide, tetracyclines, chloramphenicol, cyclophosphamide imalepheretsa kagayidwe kake ndikuwonjezera mphamvu (hypoglycemia ikhoza kukhala). Pamene zotumphukira za sulfonylurea zimaphatikizidwa ndi thiazide diuretics (hydrochlorothiazide, etc.) ndi BKK (nifedipine, diltiazem, etc.), kukokomeza kumachitika mumagulu akulu - thiazides amasokoneza zotsatira za zotumphukira za potaziyamu, ndipo maselo a BKK akusokoneza kayendedwe ka pot. zotupa.

Zomwe zimachokera ku sulfonylureas zimapangitsa kuti pakhale zovuta komanso kulekerera mowa, mwina chifukwa cha kuchedwa kwa oxidation a acetaldehyde. Zomwe zimachitika ngati antabuse.

Mankhwala onse a sulfonamide hypoglycemic amalimbikitsidwa kuti atenge ola limodzi musanadye chakudya, zomwe zimapangitsa kuchepa kwambiri kwa matenda a postprandial (atatha kudya) glycemia. Pankhani ya zovuta za dyspeptic phenomena, tikulimbikitsidwa kugwiritsa ntchito mankhwalawa mutatha kudya.

Zotsatira zosafunikira za sulfonylurea zotumphukira, kuwonjezera pa hypoglycemia, ndizovuta zamisala (kuphatikizapo mseru, kusanza, kutsegula m'mimba, kuchepa kwa thupi, kusinthika kwa leukopenia, thrombocytopenia, agranulocytosis, aplastic ndi hemolytic anemia) kuyabwa, erythema, dermatitis).

Kugwiritsa ntchito sulfonylurea kukonzekera panthawi yoyembekezera sikulimbikitsidwa, chifukwa ambiri aiwo ali mgulu la C malinga ndi FDA (Food and Drug Administration), mankhwala a insulin ndi omwe amaperekedwa m'malo mwake.

Odwala okalamba salimbikitsidwa kugwiritsa ntchito mankhwala omwe atenga nthawi yayitali (glibenclamide) chifukwa chowonjezera chiopsezo cha hypoglycemia. Pakadali pano, ndikofunikira kugwiritsa ntchito njira zazifupi - gliclazide, glycidone.

Meglitinides - owongolera prandial (repaglinide, nateglinide).

Repaglinide ndi yochokera ku benzoic acid. Ngakhale pali kusiyana kwamapangidwe amakanidwe amthupi kuchokera ku sulfonylurea yomwe imachokera, imalephereranso njira za ATP zotengera potaziyamu zomwe zimagwira ntchito m'maselo a beta, zomwe zimayambitsa kupatsirana ndikutsegulidwa kwa njira za calcium, potero kulimbikitsa insulin kukulira. Kuyankha kwa insulinotropic pakudya kumayamba pakadutsa mphindi 30 kuchokera nthawi yofunsira ndipo kumayendetsedwa ndi kuchepa kwa glucose wamagazi panthawi ya chakudya (kuchuluka kwa insulin pakati pa chakudya sikukula). Monga zotumphukira za sulfonylurea, zotsatira zoyipa kwambiri ndi hypoglycemia. Mosamala, repaglinide imalembedwa kwa odwala omwe ali ndi hepatic komanso / kapena aimpso.

Nateglinide ndi yotengera D-phenylalanine.Mosiyana ndi othandizira ena am'magazi a hypoglycemic, zotsatira za nateglinide pa insulin secretion zimachitika mwachangu, koma osalimbikira. Nateglinide imagwiritsidwa ntchito makamaka kuchepetsa matenda a postprandial hyperglycemia a 2 mtundu.

Biguanides, yomwe idayamba kugwiritsidwa ntchito pochiza matenda amishuga amtundu wa 2 mu 70s, musalimbikitse kubisalira kwa insulin mwa maselo a pancreatic beta. Zotsatira zake zimatsimikiziridwa makamaka ndi chopinga cha gluconeogeneis mu chiwindi (kuphatikizapo glycogenolysis) ndikuwonjezera kugwiritsidwa ntchito kwa glucose ndi zotumphukira zimakhala. Zimalepheretsanso kuwonjezereka kwa insulini ndikuwongolera kugwirizanitsa kwake ndi insulin receptors (izi zimapangitsa kuyamwa kwa glucose ndi metabolism yake).

Biguanides (mosiyana ndi mankhwala a sulfonylurea) samachepetsa shuga wamagazi mwa anthu athanzi komanso odwala omwe ali ndi matenda a shuga 2 atatha kufa ndi njala usiku, koma amachepetsa kwambiri kuchuluka kwake mutatha kudya, osayambitsa hypoglycemia.

Hypoglycemic biguanides - metformin ndi ena - amagwiritsidwanso ntchito ngati mtundu wa shuga 2. Kuphatikiza pa kutsika kwa shuga, biguanides, wogwiritsa ntchito nthawi yayitali, amakhala ndi zotsatira zabwino pa metabolid ya lipid. Mankhwala a gululi amalepheretsa lipogenesis (njira yomwe shuga ndi zinthu zina zimasinthidwira kukhala ma acid m'thupi), amathandizira lipolysis (njira yogawa lipids, makamaka triglycerides yomwe ili ndi mafuta, mu ma acid omwe amapezeka mothandizidwa ndi lipase enzyme), kuchepetsa chilimbikitso, ndi kulimbikitsa kuwonda. Nthawi zina, kugwiritsidwa ntchito kwawo kumayendetsedwa ndi kuchepa kwa zomwe zili triglycerides, cholesterol ndi LDL (zotchulidwa pamimba yopanda kanthu) mu seramu yamagazi. Mu matenda a shuga a mellitus 2, zovuta zama kagayidwe kazakudya zimaphatikizidwa ndi kusintha kwamawu a lipid metabolism. Chifukwa chake, 85-90% ya odwala omwe ali ndi matenda a shuga a 2 amakhala ndi thupi lochulukirapo. Chifukwa chake, kuphatikiza kwa mtundu 2 wa shuga ndi mafuta onenepa kwambiri, mankhwala osokoneza bongo a lipid amawonetsedwa.

Chizindikiro cha kuperekera kwa gluuanides ndi mtundu wachiwiri wa matenda ashuga (makamaka pamavuto a kunenepa kwambiri) ndi kusachita bwino kwa mankhwala othandizira, komanso kusachita bwino kwa kukonzekera kwa sulfonylurea.

Popanda insulini, zotsatira za Biguanides sizimawoneka.

Biguanides angagwiritsidwe ntchito limodzi ndi insulin pamaso pokana izo. Kuphatikiza kwa mankhwalawa ndi sulfonamide zotumphukira kumasonyezedwa pokhapokha ngati omaliza sapereka kukonzanso kwathunthu kwa matenda a metabolic. Biguanides angayambitse kukula kwa lactic acidosis (lactic acidosis), yomwe imaletsa kugwiritsa ntchito mankhwala m'gululi.

Biguanides amatsutsana pamaso pa acidosis komanso chizolowezi chake (kumakweza ndikuwonjezera kuchuluka kwa lactate), mumikhalidwe yomwe imayendetsedwa ndi hypoxia (kuphatikizapo mtima ndi kupuma, kulephera kwa pachimake kwa myocardial infarction, kuchepa kwa magazi m'thupi pachimake, kuchepa kwa magazi m'thupi, zina.

Zotsatira zoyipa za biguanides zimadziwika nthawi zambiri kuposa zochokera ku sulfonylurea (20% motsutsana 4%), choyambirira, zotsatira zoyipa zam'mimba: kutsekemera kwazitsulo mkamwa, zizindikiro za dyspeptic, etc. Mosiyana ndi sulfonylurea zotumphukira, hypoglycemia mukamagwiritsa ntchito Biguanides (mwachitsanzo metformin ) zimachitika kawirikawiri.

Lactic acidosis, yomwe nthawi zina imawoneka ngati imatenga metformin, imawoneka ngati yovuta kwambiri, kotero metformin sayenera kufotokozedwa chifukwa cha kulephera kwa impso ndi mikhalidwe yomwe imatsutsana ndi kukula kwake - aimpso ndi / kapena ntchito ya chiwindi, kulephera kwa mtima, mapapu

Biguanides sayenera kutumikiridwa nthawi imodzi ndi cimetidine, chifukwa amapikisana wina ndi mnzake momwe amapangira secretion wa tubular mu impso, zomwe zingayambitse kuwerengera kwa Biguanides, Kuphatikiza apo, cimetidine amachepetsa biotransfform ya biguanides m'chiwindi.

Kuphatikizidwa kwa glibenclamide (kotengera sulfonylurea ya m'badwo wachiwiri) ndi metformin (biguanide) kuphatikiza zomwe ali nazo, ndikukulolani kuti mukwaniritse zotsatira za hypoglycemic ndi mlingo wotsika wa lirilonse la mankhwalawa ndipo potero mumachepetsa chiopsezo cha mavuto.

Kuyambira 1997, adalowa m'chipatala kachikachiyama (glitazones), maziko a kapangidwe kazomwe zimapangidwa ndi mphete ya thiazolidine. Gulu latsopanoli la othandizira odwala matenda ashuga limaphatikizapo pioglitazone ndi rosiglitazone. Mankhwala osokoneza bongo a gululi amalimbikitsa chidwi cha minofu yolimbana ndi minofu (minofu, minofu ya adipose, chiwindi) ku insulin, kaphatikizidwe kam'munsi ka lipid m'maselo am'mimba ndi mafuta. Thiazolidinediones ndiosankha agonists a nyukiliya receptors PPARγ (peroxisome proliferator-activated receptor-gamma). Mwa anthu, ma receptor awa amapezeka mu "minofu yotsogoza" yomwe ndiyofunikira kuti insulini ichite: mu minofu ya adipose, minofu yamatumbo ndi chiwindi. PPARγ receptors nyukiliya imayang'anira kusindikiza kwa majini amtundu wa insulin omwe amayendetsedwa ndikuwongolera kupanga kwa shuga, kayendedwe ndi kagwiritsidwe ntchito. Kuphatikiza apo, majini amtundu wa PPARγ amakhudzidwa ndi metabolism yamafuta acid.

Kuti thiazolidatediones apereke mphamvu zawo, kupezeka kwa insulin ndikofunikira. Mankhwalawa amachepetsa kukana kwa insulin kwa chiwindi ndi chiwindi, kuonjezera kudya kwa glucose wodalira insulin ndikuchepetsa kutulutsa shuga m'magazi, kuchepetsa ma triglycerides, kuonjezera kuchuluka kwa HDL ndi cholesterol, ndikuletsa kusala kudya kwa hyperglycemia mutatha kudya, komanso hemoglobin glycosylation.

Alpha Glucosidase Inhibitors (acarbose, miglitol) amalepheretsa kuwonongeka kwa poly- ndi oligosaccharides, kuchepetsa mapangidwe ndi kupatsidwa kwa shuga m'matumbo ndikulepheretsa kukula kwa postprandial hyperglycemia. Mafuta omwe amamwetsedwa ndi chakudya osasinthika amalowa m'matumbo ang'ono ndi akulu, pomwe kuyamwa kwa monosaccharides kumatenga maola 3-4. Mosiyana ndi othandizira a sogonamide hypoglycemic, samakulitsa kutulutsidwa kwa insulin ndipo, chifukwa chake, samayambitsa hypoglycemia.

Zinawonetsedwa kuti chithandizo cha acarbose cha nthawi yayitali chimaphatikizidwa ndi kuchepetsedwa kwakukulu kwa chiopsezo chokhala ndi mtima wamtima wamakhalidwe a atherosranceotic. Ma alpha glucosidase inhibitors amagwiritsidwa ntchito ngati monotherapy kapena kuphatikiza ndi ena omwe amakamwa a hypoglycemic. Mlingo woyambirira ndi 25-50 mg yomweyo musanadye kapena nthawi ya chakudya, ndipo pang'onopang'ono utha kuwonjezeka pang'onopang'ono (mlingo waukulu wa tsiku ndi tsiku ndi 600 mg).

Zisonyezero zakugwiritsa ntchito alpha-glucosidase zoletsa ndi mitundu yachiwiri ya shuga ndi matenda osakwanira (njira yomwe iyenera kukhala osachepera miyezi 6) komanso mtundu wa 1 shuga mellitus (monga gawo la mankhwala othandizira).

Mankhwala osokoneza bongo a gululi amatha kuyambitsa zochitika zosokoneza bongo zomwe zimayambitsidwa ndi kuphwanya kwa chimbudzi komanso kuyamwa kwa chakudya, zomwe zimapangidwa m'matumbo ndikupanga mafuta acids, kaboni dayoksidi ndi hydrogen. Chifukwa chake, popereka mankhwala a alpha-glucosidase inhibitors, kutsatira kwambiri zakudya zomwe zili ndi zopatsa mphamvu zophatikiza ndi chakudya, kuphatikiza sucrose.

Acarbose akhoza kuphatikizidwa ndi othandizira ena odwala matenda ashuga. Neomycin ndi colestyramine amalimbikitsa mphamvu ya acarbose, pomwe pafupipafupi komanso kuopsa kwa zovuta kuchokera m'mimba thirakiti kumakulirakulira. Akaphatikizidwa ndi maantacid, ma adsorbents ndi ma enzyme omwe amasintha chimbudzi, mphamvu ya acarbose imachepetsedwa.

Pakadali pano, gulu latsopano laophunzira ma hypoglycemic laoneka - incretinomimetics. Kuchulukitsa ndi mahomoni omwe amasungidwa ndi mitundu ina ya maselo am'matumbo ang'onoang'ono poyankha kudya komanso kumapangitsa kuti insulin itulutsidwe. Mahomoni awiri adalekanitsidwa: glucagon-polypeptide (GLP-1) ndi glucose-insulinotropic polypeptide (HIP) ya glucose.

Kuti incretinomimetics imaphatikizapo magulu awiri a mankhwala:

- zinthu zomwe zimatsutsana ndi zotsatira za GLP-1 - fanizo la GLP-1 (liraglutide, exenatide, lixisenatide),

-zinthu zomwe zimakulitsa kuchitapo kanthu kwa endo native GLP-1 chifukwa cha blockade ya dipeptidyl peptidase-4 (DPP-4) - enzyme yomwe imawononga GLP-1 - DPP-4 inhibitors (sitagliptin, vildagliptin, saxagliptin, linagliptin, alogliptin).

Chifukwa chake, gulu la othandizira a hypoglycemic limaphatikizapo mankhwala angapo ogwira mtima. Ali ndi magwiritsidwe osiyanasiyana, osiyana magawo a pharmacokinetic ndi pharmacodynamic. Kudziwa zinthu izi kumathandizira adotolo kusankha mwanzeru komanso moyenera pa chithandizo chamankhwala.

Contraindication

1. Type 1 shuga.
2. Matenda a shuga a ketoacidosis (kuchuluka kwambiri m'magazi a matupi a ketone), chikomokere.
3. Mimba komanso kuyamwa.
4. Matenda a chiwindi ndi pachimake komanso opuwala.
5. Kulephera kwa mtima.
6. Hypersensitivity mankhwala.

Kukonzekera kwa Thiazolidinedione

Troglitazone (Rezulin) anali mankhwala a m'badwo woyamba wa gululi. Adakumbukiridwa kuchokera kugulitsa, popeza momwe amawonekera adawonetsa molakwika pachiwindi.

Rosiglitazone (Avandia) ndi mankhwala m'badwo wachitatu m'gululi. Inaleka kugwiritsidwa ntchito mu 2010 (yoletsedwa ku European Union) zitadziwika kuti zimawonjezera chiopsezo cha matenda amtima.

Dzinalo lantchito yogwira	Zitsanzo Zamalonda	Mlingo piritsi limodzi Mg
Pagogazone	Pioglitazone Bioton	15 30 45

Kugwiritsa ntchito

Kuphatikiza apo, zatsimikiziridwa kuti mankhwalawa ali ndi zina zowonjezera zopindulitsa:

Amachepetsa kuthamanga kwa magazi
Zimakhudzanso cholesterol (imawonjezera kupezeka kwa "cholesterol yabwino", ndiye kuti, HDL, ndipo sichulukitsa "cholesterol yoyipa" - LDL),
Imalepheretsa mapangidwe ndi kukula kwa atherosulinosis,
Amachepetsa chiopsezo cha matenda a mtima (mwachitsanzo, kugunda kwa mtima, sitiroko).

Werengani zambiri: Jardins amateteza mtima

Kwa omwe pioglitazone adalembedwa

Pioglitazone ikhoza kugwiritsidwa ntchito ngati mankhwala amodzi, i.e. monotherapy. Komanso, ngati muli ndi mtundu wachiwiri wa matenda ashuga, kusintha kwanu pa moyo sikupereka zotsatira zomwe zikuyembekezeka ndipo pali zotsutsana ndi metformin, kulekerera kwake kosavomerezeka komanso zoyipa zake zomwe zingachitike

Kugwiritsa ntchito pioglitazone ndikotheka ndikuphatikiza ndi mankhwala ena othandizira (mwachitsanzo, acarbose) ndi metformin ngati zochita zina sizibweretsa bwino

Pioglitazone itha kugwiritsidwanso ntchito ndi insulin, makamaka kwa anthu omwe thupi lawo limachita mosavomerezeka ndi metformin.

Werengani zambiri: Momwe mungatenge metformin

Momwe mungatenge pioglitazone

Mankhwalawa amayenera kumwa kamodzi patsiku, pakamwa, panthawi yokhazikika. Izi zitha kuchitika musanadye komanso pambuyo chakudya, popeza chakudya sichikhudza mayamwidwe a mankhwalawo. Nthawi zambiri, chithandizo chimayamba ndi mlingo wotsika. Panthawi yomwe chithandizo cha mankhwalawa sichikhutiritsa, chitha kuchepa.

Kugwiritsa ntchito bwino kwa mankhwalawa kumawonedwa pakachitika matenda a 2 odwala, koma Metformin sangathe kugwiritsidwa ntchito, monotherapy yokhala ndi mankhwala amodzi saloledwa.

Kuphatikiza apo pioglitazone imachepetsa postprandial glycemia, plasma glucose ndipo imakhazikitsa hemoglobin ya glycated, imakhalanso ndi chiwopsezo chowonjezeka cha kuthamanga kwa magazi ndi cholesterol yamagazi. Kuphatikiza apo, sizimayambitsa zosankha.

Kukonzekera kwa Thiazolidinedione

Thiazolidinediones (TZD) - kalasi yatsopano ya mankhwala othandizira kuti asagwiritsidwe ntchito pakamwa. Mankhwala a Thiazolidinedione (pioglitazone, rosiglitazone) adangolowa mchitidwe wazachipatala muzaka zaposachedwa. Monga biguanides, mankhwalawa samalimbikitsa kubisalira kwa insulin, koma amathandizira chidwi cha zotumphukira zake. Zophatikizira za gululi zimagwira ngati agonists a PPAR-y receptors (peroxisome proliferator-activated receptor). Ma receptor awa amapezeka m'maselo amafuta, minofu ndi chiwindi. Kutsegula kwa ma PPAR-y receptors modulates mayendedwe angapo amitundu yomwe imakhudzana ndi kufalikira kwa zotsatira za insulin kuti ilowe mkati mwa glucose ndi lipids m'maselo. Kuphatikiza kuchepetsa kutsika kwa glycemia, kukonza chidwi cha zimakhala kuti insulin ikukhudza bwino mawonekedwe a lipid (kuchuluka kwa osalimba a lipoproteins kumawonjezereka, zomwe zili triglycerides zimachepa). Popeza kuti mankhwalawa amagwira ntchito polimbikitsa kusintha kwa majini, zimatenga miyezi iwiri kuti mupeze zotsatira zabwino. M'maphunziro azachipatala, mankhwalawa adapereka kuchepa kwa HbAc ndi monotherapy ndi 0,5 mpaka 2%.

Mankhwala osokoneza bongo a gululi amatha kugwiritsidwa ntchito limodzi ndi PSM, insulin kapena metformin. Kuphatikizidwa ndi metformin ndikoyenera chifukwa chochitika cha biguanides makamaka cholinga chake kuponderezera gluconeogenesis, ndipo zochita za thiazolidinediones cholinga chake ndikuwonjezera kugwiritsidwa ntchito kwa glucose. Sizomwe zimayambitsa hypoglycemia (koma, monga biguanides, zimatha kuwonjezera kuchuluka kwa hypoglycemia kuphatikiza ndi mankhwala omwe amachititsa insulin secretion. Chochita chachikulu ndikugwiritsira ntchito mpweya wophatikizika ndi kuchepetsedwa kwa glycogeneis kudzera mu kukhazikitsa kwa majini amisala a insulin (kuchepa kwa insulin kukaniza). Thiazolidinediones ngati mankhwala omwe amachotsa kukana kwa insulin, omwe amayambitsa kukula kwa matenda a shuga a 2, ndiye gulu labwino kwambiri la mankhwala othandizira kupewa matenda a shuga a mtundu wa 2. Kubwezeretsa kwa thiazolidinediones kumapitilira miyezi yopitilira 8 itachotsedwa. Pali lingaliro kuti glitazones amatha kukonza kuwonongeka kwa majini a glucose metabolism, omwe amalola kuti asangolekezera kukula kwa matenda a shuga a 2, komanso kuti athetse kwathunthu chitukuko.

Komabe, pakadali pano ndikungoganizira chabe.

Kugwiritsira ntchito thiazolidinediones kwa odwala omwe ali ndi matenda a shuga a 2 kumatsegula mwayi wopewera zovuta zamtima, njira ya chitukuko yomwe imachitika makamaka chifukwa cha kukana insulini. Zambiri zam'mbuyo zokhudzana ndi zotsatira za angioprotective za thiazolidinediones zapezeka kale mu maphunziro ena oyesera. Maphunziro azachipatala ofananawa sanachitike.

Pali mibadwo itatu ya thiazolidinediones padziko lapansi:
- mankhwala a "m'badwo woyamba" - troglitazone (adawonetsa kutchulidwa kwa hepatotoxic ndi cardiotoxic effect, mogwirizana ndi momwe adaletsedwera kuti agwiritse ntchito),
- mankhwala a "m'badwo wachiwiri" - pioglitazone,
- "m'badwo wachitatu" mankhwala - rosiglitazone.

Pakadali pano, mankhwala ochokera ku m'badwo wachiwiri wa thiazolidinediones - actos (pioglitazone hydrochloride) ochokera ku Eli Lilly (USA) ndi m'badwo wachitatu - avandium (rosiglitazone) walembedwa ku Russia. Actos amapezeka mu mawonekedwe a mapiritsi okhala ndi 15.30 ndi 45 mg ya yogwira pioglitazone hydrochloride, kamodzi patsiku, mosasamala kanthu za kudya.

Mlingo watsiku ndi tsiku ndi 30-45 mg. Glaxo SmithKJine (GSK) avandium imapezeka mu piritsi la 4 ndi 8 mg yogwira ya rosiglitazone, kamodzi kapena kawiri tsiku lililonse, mosasamala za kudya. Tsiku mlingo wa 8 mg. Amakonzekera kutulutsa mankhwala ophatikizidwa ndi kampani yomweyo - Avandamet (kuphatikiza kwa avandia ndi metformin).

Thiazolidinediones amagwiritsidwa ntchito ngati monotherapy, koma ndi bwino kuphatikiza ndi biguanides, acarbose, PSM, insulin odwala omwe ali ndi matenda a shuga a mtundu wa 2. Kugwiritsira ntchito kochepa kwa gulu ili chifukwa cha mtengo wawo wokwera kwambiri.Mankhwala, omwe ndi a m'badwo wachiwiri wa thiazolidatediones, sanawonetse ngati hepatotoxic. Pioglitazone sichinapangidwe mu chiwindi, kupanga metabolites yogwira, yomwe imapukusidwa makamaka ndi bile. Chimodzi mwazotsatira zoyipa zimatha kukhala mawonekedwe a edema, komanso kulemera. Poyerekeza ndi momwe mankhwalawo amathandizira, tikulimbikitsidwa kuwongolera kuchuluka kwa alanine ndi aspartic aminotransferase ndikusiya kumwa mankhwalawa panthawi ya enzyme yomwe imakhala yofala kawiri. Ndikofunika kuwunika momwe mankhwalawa amathandizira pakanthawi (3-mwezi) mankhwala. Zoyipa:
- lembani matenda ashuga 1
- ketoacidosis ndi mtundu uliwonse wa matenda ashuga,
- mimba, kuyamwa,
- owonjezera muyezo wa alanine transferase katatu,
- mavairasi owopsa a hepatitis,
- Matenda oopsa a chiwindi.

Kupewa kwa matenda a shuga a Type 2

Mayeso azachipatala a DREAM adawonetsa chiopsezo chochepetsa shuga kwa odwala omwe ali ndi vuto la glucose komanso kuwonjezeka kwa glucose kosalekeza kwa odwala omwe akutenga rosiglitazone (11, onaninso 12). Kafukufukuyu adawonetsa kuti chitukuko cha matenda ashuga chimatha kuchepetsedwa ndi zaka 1.5, koma ndiye kuti chiwopsezo cha chitukuko chikuwonjezeka ndikukhala chimodzimodzi mu gulu la placebo.