I-Thiazolidinediones yiqembu elisha lemithi yomlomo ye-antidiabetic. Njengama-greatuanides, awaligcwalisi i-pancreas, avuselela ukukhiqizwa kwe-insulin endulin, kepha amane anciphise ukumelana kwamangqamuzana kwi-hormone.
Ngaphezu kokushintsha i-glycemia ejwayelekile, izidakamizwa futhi zithuthukisa i-lipid spectrum: ukugcwala kwe-HDL kuyanda, izinga le-triglycerol liyancipha. Njengoba umphumela wezidakamizwa uncike ekuvuseleleni okubhalwe ku-gene, umphumela ofanele ophuma ekwelashweni ungalindelwa ezinyangeni ezingama-2-3. Ezilingweni zemitholampilo, i-monotherapy ene-thiazolidinediones yanciphisa i-glycated hemoglobin yaba ngu-2%.
Imithi yaleli qembu ihlanganiswe ngokuphelele namanye ama-antidiabetesic agents - metformin, insulin, sulfonylurea derivatives. Ukuhlanganiswa ne-metformin kungenzeka ngenxa yendlela ehlukile yokusebenza: i-biguanides inhibit glucogenesis, futhi i-thiazolidinediones ikhulisa ukusetshenziswa kwe-glucose.
Ababuye bavuse umphumela we-hypoglycemic nge-monotherapy, kepha, njenge-metformin, ekwelapheni okuyinkimbinkimbi ngemithi ye-hypoglycemic kungadala imiphumela enjalo.
Njengoba izidakamizwa ezandisa ukuzwela kwama-receptors ku-insulin, ama-thiazolidatediones aphakathi kwezidakamizwa ezethembisa kakhulu zokuphatha isifo sikashukela sohlobo 2. Umphumela wokuvimbela ngemuva kokuthatha umuthi uthatha izinyanga ezi-8 ngemuva kokuphela kwekhosi.
Kukhona umbono wokuthi izidakamizwa zalesi sigaba zingalungisa isici sofuzo se-metabolic syndrome, sibambezele ukuqhubeka kwesifo sikashukela sohlobo 2 kuze kube yilapho sinqoba ngokuphelele lesi sifo.
Kuma-thiazolidinediones, umuthi wesizukulwane wesibili we-Aktos wenkampani yemithi "Eli Lilly" (USA) ubhalisiwe emakethe yaseRussia namuhla. Ukusetshenziswa kwaso kuvula amathuba amasha hhayi ku-diabetesology kuphela, kodwa naku-cardiology, lapho umuthi usetshenziselwa ukuvikela i-pathologies yenhliziyo nemithambo yegazi, ikakhulukazi ngenxa yokumelana ne-insulin.
Ifomu lomthamo nokwakheka kwePioglitazone
Isakhi esiyisisekelo salo muthi yi-pioglitazone hydrochloride. Kwithebhulethi elilodwa, inani laso lincike kumthamo - 15 noma 30 mg. Ikhompiyutha esebenzayo ekwakhiweni ifakiwe lactose monohydrate, hydroxypropyl cellulose, calcium carboxymethyl cellulose, magnesium stearate.
Amathebulethi amhlophe angokoqobo angakhonjwa ngesimo se-round convex nokuqopha u- "15" noma "30".
Kwipuleti elilodwa amatafula ayi-10, ebhokisini - amapuleti anjalo ayi-3-10. Impilo yeshalofu yesidakamizwa yiminyaka emi-2. Kwi-pioglitazone, intengo incike hhayi kuphela kumthamo wezidakamizwa, kepha futhi nakumenzi ojwayelekile: Amathebulethi angama-30 e-Indian Pioglar 30 mg ngalinye lingathengwa ngama-ruble ayi-1083, amaphilisi angama-28 e-Ireland Actos 30 mg lilinye - ngama-ruble ayi-3000.
Izici ze-Pharmacological
I-pioglitazone umuthi we-hypoglycemic womlomo wesigaba se-thiazolidinedione. Umsebenzi wesidakamizwa uhlotshaniswa nokuba khona kwe-insulin: ukwehlisa umkhawulo wokuzwela kwesibindi nezicubu ku-hormone, kukhulisa izindleko ze-glucose futhi kunciphise ukukhiqizwa kwawo esibindini. Uma kuqhathaniswa nezidakamizwa ze-sulfonylurea, i-pioglitazone ayivuseleli amaseli we-b abhekene nokukhiqizwa kwe-insulin futhi akusheshisi ukuguga kwayo necrosis.
Ukwehla kokumelana ne-insulin ngohlobo 2 sikashukela kusiza ukuguqulela iphrofayili ye-glycemic kanye nama-glycated hemoglobin. Ngokuphazamiseka kwe-metabolic, umuthi unesandla ekukhuphukeni kwamazinga e-HDL kanye nokwehla kwamazinga e-triglycerol. Okuqukethwe kwe-cholesterol ephelele ne-LDL kuhlala kungashintshiwe.
Uma ungena emgudwini wokugaya ukudla, umuthi udonswa ngentshiseko, ufinyelela kumanani wokulinganisa egazini ngemuva kwamahora ama-2 une-bioavailability ka-80%. Ukwanda okulingene kokuhlatshwa kwezidakamizwa egazini kwaqoshwa ngemithamo ukusuka ku-2 kuye ku-60 mg. Umphumela ozinzile uyatholakala ngemuva kokuthatha amaphilisi ezinsukwini zokuqala ezingama-4-7.
Ukusetshenziswa okuphindaphindwayo akukuphazamisi ukunqwabelana kwalo muthi. Izinga lokufakwa alincike esikhathini sokutholwa kwezakhi zomzimba.
IPioglitazone isuswa ngamalongwe (55%) nomchamo (45%). Umuthi, obizwa ngefomu elingashintshiwe, unempilo eyihafu yamahora ama-5-6, kuma-metabolites awo, amahora ayi-16-23.
Iminyaka yesifo sikashukela ayithinti i-pharmacokinetics yomuthi. Nge-dysfunctions ye-renal, okuqukethwe kwe-glitazone kanye nama-metabolites ayo kuzokwehla, kepha ukucaca kuzolingana, ngakho-ke ukugcwala komuthi wamahhala kugcinwa.
Ngokuhluleka kwesibindi, izinga eliphelele lomuthi osegazini lihlala njalo, ngokwanda kwevolumu yokusabalalisa, imvume izoncishiswa, futhi nengxenye yezidakamizwa zamahhala izonyuswa.
Izinkomba zokusetshenziswa
I-pioglitazone isetshenziselwa ukulawula isifo sikashukela sohlobo lwe-2 kokubili njenge-monotherapy kanye nasekwelapheni okuyinkimbinkimbi, uma ukuguqulwa kwendlela yokuphila (umsoco ophansi we-carbohydrate, umsebenzi owanele womzimba, ukulawulwa kwesimo somoya) musa ukubuyisana ngokuphelele ne-glycemia.
Ekwelashweni okuyinkimbinkimbi, ama-regimens aphindwe kabili nge-metformin asetshenziswa (ikakhulukazi ukukhuluphala), uma i-monotherapy ene-metformin emithini yokwelapha inganikeli i-100% glycemic control. Uma kwenzeka kuphulwa i-metformin, i-pioglitazone ihlanganiswe nezidakamizwa ze-sulfonylurea, uma ukusetshenziswa kwe-monotherapy kunganikeli ngomphumela oyifunayo.
Ukuhlanganiswa kwe-pioglitazone kanye nokuhlanganiswa okuphindwe kathathu nge-metformin ne-sulfonylurea ukulungiselela kungenzeka, ikakhulukazi kwiziguli ezikhuluphele, uma amacebo wangaphambilini anganikeli iphrofayili ye-glycemic evamile.
Amathebulethi nawo alungele uhlobo lwe-2 yesifo sikashukela esincike ku-insulin, uma imijovo ye-insulin ingalawulwa ngokwanele ushukela, futhi i-metformin iphikisiwe noma ingabekezelelwa yisiguli.
Contraindication
Ngaphezu kwe-hypersensitivity kuzithako zefomula, i-pioglitazone ayinconywa:
- Iziguli ezinesifo sohlobo 1;
- Nge-ketoacidosis yesifo sikashukela;
- Iziguli ezinenkinga yokuqina kwesibindi;
- Uma ku-anamnesis - ama-pathologies enhliziyo yobuciko. Mina - IV NYHA;
- Ngama-macroscopic hematuria we-etiology engaqinisekile;
- Isifo sikashukela nge-oncology (umdlavuza wesinye).
Ukusebenzelana kwezidakamizwa
Ukusetshenziswa okuhlangene kwe-pioglitazone nge-digoxin, i-warfarin, i-fenprocoumone kanye ne-metformin akushintshi amandla abo e-pharmacological. Ayithinti i-pharmacokinetics kanye nokusetshenziswa kwe-glitazone ene-sulfonylurea derivatives.
Ucwaningo oluphathelene nokusebenzisana kwe-pioglitazone ngezindlela zokuvimbela inzalo ngomlomo, ama-calcium blockers, ama-cyclosporine nama-HMCA-CoA reductase inhibitors awazange aveze ushintsho ezimweni zawo.
Ukusetshenziswa okubonakalayo kwe-pioglitazone ne-gemfibrozil kukhuthaza ukwanda kwe-AUC ye-glitazone, egcizelela ukuthembela kokuhlushwa isikhathi, izikhathi ezi-3. Isimo esinjalo sandisa amathuba okuvela kwemiphumela engathandeki yokuxhomekeka kumthamo, ngakho-ke, umthamo we-pioglitazone kufanele ulungiswe lapho uhlanganiswa ne-inhibitor.
Izinga le-pioglitazone lenyuka lapho i-rifampicin isetshenziswa ndawonye. Ukuqapha i-glycemia kuyimpoqo.
Incomo ngokusetshenziswa kwePioglitazonum
Imiyalo ye-pioglitazone yokusetshenziswa itusa ukuthi abanesifo sikashukela basebenzise 1 kk / Usuku. Ithebhulethi ligwinywe lonke ngamanzi, udokotela ukhetha umthamo uthatha ukwelashwa okwedlule, iminyaka, isigaba sesifo, i-concomitant pathologies, ukusabela komzimba.
Ngokulashwa okuyinkimbinkimbi nge-insulin, umthamo wokugcina ulungiswa ngokuya ngokufundwa kwe-glucometer nezici zokudla.
Kwabashukela asebekhulile, asikho isidingo sokushintsha umthamo, baqala ngesilinganiso esiphansi, banda kancane, ikakhulukazi ngezinhlelo ezihlangene- lokhu kwenza lula ukuzivumelanisa nezimo futhi kunciphisa umsebenzi wemiphumela emibi.
Ngokudalwa kwe-renal (imvume ye-creatinine enkulu kune-4 ml / min.), I-Glitazone ichazwe njengokujwayelekile, ayikhonjiswa kwiziguli ze-hemodialysis, kanye nokwehluleka kwesibindi.
Izincomo ezingeziwe
Ukusebenza kahle kwerejimeni ekhethiwe kuhlolwa njalo ezinyangeni ezi-3 kusetshenziswa ama-glycated hemoglobin assows. Uma kungekho ukusabela okwanele, yeka ukuthatha lo muthi. Ukusetshenziswa isikhathi eside kwe-pioglitazone kuthwala ubungozi obukhona, ngakho-ke, udokotela kufanele aqaphele iphrofayili yokuphepha yomuthi.
Umuthi uyakwazi ukugcina uketshezi emzimbeni futhi wenze isimo sibe nzima ngokwenhliziyo. Uma isifo sikashukela sinezici zobungozi ngendlela yokuba mdala, isifo senhliziyo noma isifo senhliziyo, umthamo wokuqala kufanele ube omncane.
Ukudluliswa kwamandla kungenzeka ngezimo ezinhle. Lesi sigaba sabanesifo sikashukela sidinga ukubhekwa njalo kwesimo sabo sempilo (isisindo, ukuvuvukala, izimpawu zesifo senhliziyo), ikakhulukazi ngenqolobane ephansi ye-diastolic.
Ukugxila ikakhulukazi lapho kunqunywa umuthi kufanele kunikezwe abanesifo sikashukela besikhathi esivuthiwe (kusuka eminyakeni engama-75), ngoba akukho okuhlangenwe nakho ngokusetshenziswa kwezidakamizwa kwalesi sigaba. Ngokuhlanganiswa kwe-pioglitazone nge-insulin, ama-pathologies enhliziyo angathuthukiswa. Kulesi sikhathi, ingozi yomdlavuza, i-fractures iyanda, ngakho-ke lapho unquma umuthi, kubalulekile ukuhlola izinzuzo zangempela kanye nomonakalo ongaba khona.
Izivivinyo zomtholampilo ziqinisekisa amathuba okuba nomdlavuza wesinye ngemuva kokudla i-pioglitzone. Ngaphandle kwengozi ephansi (0.06% qhathanisa ne-0,02% eqenjini lokulawula), zonke izinto ezikhuthaza umdlavuza (ukubhema, ukukhiqiza okulimazayo, i-pelvic irradiation, iminyaka) kufanele ihlolwe.
Ngaphambi kokuqokwa komuthi, ama-enzyme wesibindi ayahlolwa. Ngokukhuphuka kwe-ALT ngezikhathi ezingama-2,5 kanye nokwehluleka kwesibindi okunamandla, umuthi uphethwe i-contraindication. Ngokuqina okulinganiselayo kwama-pathologies wesibindi, i-pioglitazone ithathwa ngokuqapha.
Ngezimpawu zokulimazeleka kwe-hepatic (ukuphazamiseka kwengqondo), ubuhlungu be-epigastric, i-anorexia, ukukhathala okungapheli), ama-enzyme esibindi ayahlolwa. Ukudlula okujwayelekile ngezikhathi ezi-3, kanye nokuvela kwe-hepatitis, kufanele kube yisizathu sokuhoxiswa kwezidakamizwa.
Ngokuncipha kokumelana ne-insulin, kusatshalaliswa kabusha amafutha kwenzeka: kuyancipha i-visceral, kanye nokwenyuka kwesisu okungeziwe. Uma ukuzuza kwesisindo kuhlotshaniswa ne-edema, kubalulekile ukulawula ukusebenza kwenhliziyo kanye nokudla kakhulu ikhalori.
Ngenxa yethamo legazi elikhulayo, i-hemoglobin ingancipha ngesilinganiso se-4%. Izinguquko ezifanayo ziyaqapheleka lapho kuthathwa ezinye izidakamizwa ze-antidiabetic (ze-metformin - 3-4%, amalungiselelo we-sulfonylurea - 1-2%).
Ekuhlanganisweni okubili nokuphindwe kathathu nge-pioglitazone, i-insulin ne-sulfonylurea, ingozi ye-hypoglycemia iyanda. Ngokulapha okuyinkimbinkimbi, ukufakwa kwesithamo okufika ngesikhathi komthamo kubalulekile.
I-Thiazolidinediones ingasiza ekubonakaleni kokukhubazeka nokudumba. Lapho uthinta i-ophthalmologist, kubalulekile ukucabanga ngamathuba we-macular edema nge-pioglitazone. Kukhona ubungozi bokuqhekeka kwamathambo.
Ngenxa yesisekelo sobufakazi obunganele bokusebenza okusebenzayo nokuphepha maqondana nokukhulelwa nokuqunjelwa, abesifazane ababekelwanga i-polyglitazone ngalezi zikhathi. Umuthi uphambaniswe ebuntwaneni.
Lapho ushayela izimoto noma izindlela eziyinkimbinkimbi, kungenzeka ukuthi kubhekwe imiphumela emibi ngemuva kokusebenzisa i-glitazone.
Imiphumela yokusetshenziswa ngokweqile nemiphumela engathandeki
Ngama-monotherapy nasezinhlelweni eziyinkimbinkimbi, kuqoshwa izinto ezingathandeki:
- I-edema ye-Macular, ukungaboni kahle;
- I-Anemia
- I-Hypersthesia, ikhanda;
- Ukutheleleka kohlelo lokuphefumula, i-sinusitis ne-pharyngitis;
- I-allergy, anaphylaxis, hypersensitivity, angioedema;
- Ukwehla kwekhwalithi yokulala;
- Ama-tumors emvelo ehlukahlukene: ama-polyps, ama-cysts, umdlavuza;
- Amaqabunga nobuhlungu emikhawulweni;
- Isiphithiphithi sesigqi;
- Ukungasebenzi kwe-Erectile;
I-Hypoglycemia, isifiso sokungalawulwa;- I-Hypesthesia, ukuhlangana okungahambi kahle;
- UVertigo;
- Isisindo sokukhula nokukhula kwe-ALT;
- I-Glucosuria, i-proteinuria.
I-Hypoglycemia, isifiso sokungalawulwa;Izifundo zivivinye ukuphepha komthamo we-120 mg, okwathi ngokuzithandela kwathatha izinsuku ezi-4, kwathi ezinye izinsuku eziyi-7 kwaba ngu-180 mg. Azikho izimpawu ze-overdose ezitholakele.
Izimo ze-Hypoglycemic zingenzeka ngohlobo oluyinkimbinkimbi ngamalungiselelo e-insulin kanye ne-sulfonylurea. Ukwelapha kunguphawu futhi kuyasekela.
I-pioglitazone - analogues
Emakethe yaseMelika yezidambisigciwane, enye enkulu kunazo zonke emhlabeni, i-pioglitazone ithola ingxenye efana ne-metformin. Nge-contraindication noma ukubekezelela okungekuhle, i-pioglitazone ingathathelwa indawo yi-Avandia noma i-Roglit - ama-analogues asuselwa ku-rosiglitazone - umuthi wesigaba esifanayo se-thiazolidinediones, noma kunjalo, izibikezelo zesikhathi eside kuleli qembu ziyadumaza.
Yehlisa ukumelana ne-insulin nama-biguanides. Kulokhu, i-pyoglizatone ingathathelwa indawo yiGlucophage, Siofor, Bagomet, NovoFormin neminye imithi esekwe nge-metformin.
Kusukela engxenyeni yesabelomali sezidakamizwa ze-hypoglycemic, ama-analogues aseRussia athandwa kakhulu: UDab-ejwayelekile, iDiaglitazone, i-Astrozone. Ngenxa yohlu oluqinile lwe-contraindication, inani lakhona elanda ngokwelashwa okuyinkimbinkimbi, umuntu kufanele aqaphele ekukhetheni kwama-analogues.
Ukuhlolwa Komthengi
Mayelana ne-pioglitazone, ukubuyekezwa kwabanesifo sikashukela kuxutshwe. Labo abathathe izidakamizwa zokuqala babona ukusebenza okuphezulu kanye nemiphumela emincane.
Isiphetho asiqiniseki: umuthi wehlisa ngempela izinga le-glycemia, i-glycated hemoglobin futhi nesidingo se-insulin (ikakhulukazi ngokwelashwa okuyinkimbinkimbi). Kepha awulungele wonke umuntu, ngakho-ke akufanele uzame impilo, uthole umuthi kwizeluleko zabangani. Uchwepheshe kuphela okwazi ukunquma ukuthi kungenzeka yini ukwelashwa okunjalo kanye ne-algorithm yokuthola i-pioglitazone.
Ungafunda kabanzi ngokusetshenziswa kwama-thiazolidinediones ekusebenzeni ngokomtholampilo kusuka kuvidiyo:
