I-pioglitazone - umuthi wohlobo lwesifo sikashukela 2

IPioglitazone isidakamizwa esinciphisa ushukela esisha; yaqalwa ukusebenza ngemithi yezempilo ngo-1996. Umuthi ungokwesigaba se-thiazolidinediones, indlela yokwenza okukhona kuyo ukwandisa ukuzwela kwezicubu zomzimba namafutha ku-insulin. I-pioglitazone ayithinti ngokuqondile izinga lokucashelwa kwe-hormone. Umuthi ubekezelelwa kahle, awubangeli i-hypoglycemia, unomphumela omuhle kuma-lipid metabolism. Ibonisa umphumela omuhle kakhulu we-hypoglycemic kuma-diabetesics ngokweqile.

Umshini wesenzo se-pioglitazone

Ukunciphisa ukuzwela kwe-insulin kungenye yezimbangela eziyisisekelo zokubonakaliswa kwesifo sikashukela. I-pioglitazone inganciphisa ukumelana ne-insulin, okuholela ekucindezelweni kwe-gluconeogenesis esibindini, ukuncipha kokuxineka kwamafutha acid egazini, kanye nokwanda kokusetshenziswa kweglucose yizicubu zemisipha. Ngesikhathi esifanayo, i-glycemia iyancipha, i-lipids yegazi ijwayelekile, futhi i-protein glycation inciphisa ijubane. Ngokusho kocwaningo, iPioglitazone ingakhuphula ukuthathwa koshukela izicubu izikhathi ezi-2,5.

Ngokwesiko, i-metformin isetshenziselwe ukunciphisa ukumelana ne-insulin. Le nto ikhulisa ukuzwela kwama-hormone ikakhulukazi esibindini. Ezicubu zemisipha kanye ne-adipose, umphumela wayo umenyezelwa kancane. I-pioglitazone inciphisa ukumelana emafutheni nasemisipha, kudlula amandla e-metformin. Kunqunywa njengesidakamizwa solayini lwesibili lapho umphumela we-metformin unganele (imvamisa ukukhuluphala kakhulu nokuhamba okuphansi) noma ungabekezelelwa kahle yisifo sikashukela.

Emuva kokwelashwa ngePioglitazone, umthelela onobuthi we-glucose nama-lipid kumaseli we-beta nezicubu ezixakile uyancipha, ngakho-ke umsebenzi wamaseli we-beta uya ngokuya ukhula, inqubo yabo yokufa iyancipha, inqubo ye-insulin iyathuthuka.

Emiyalweni yokusetshenziswa, umphumela omuhle wePioglitazone kwizimbangela zokuphazamiseka kwesifo sikashukela senhliziyo kuyaphawulwa. Ngemuva kweminyaka emithathu yokuphatha, izinga le-triglycerides lehla ngokwesilinganiso ngamaphesenti ayi-13, "cholesterol" enhle "inyuka ngo-9%. Ingozi yokuhlaselwa yisifo sohlangothi nokushaya kwenhliziyo incipha ngo-16%. Kwafakazelwa ngokokuhlola ukuthi, ngokumelene ingemuva kokusetshenziswa kwePioglitazone, ukushuba kwezindonga zemithambo yegazi kuvamile, kuyilapho ingozi yokuwohloka kwesifo sikashukela nayo incipha.

Isifo sikashukela nokucindezela kuzoba yinto yesikhathi esedlule

• Ukwehlela ushukela -95%
• Ukuqedwa kwe-vein thrombosis - 70%
• Ukuqedwa kokushaya kwenhliziyo okuqinile -90%
• Ukuqeda umfutho wegazi ophakeme - 92%
• Ukwanda kwamandla ngesikhathi sosuku, ngcono ukulala ebusuku -97%

I-pioglitazone ayifaki sandla ekuzuzeni okunamandla kwesisindo, njengezidakamizwa ezithinta ukwakheka kwe-insulin. Ngokuphambene nalokho, ezigulini ezinesifo sikashukela kukhona ukwehla kwesimo sesisu ngenxa yokwehla kwethamo lamafutha e-visceral.

I-Pharmacokinetics yePioglitazone ngokwemiyalo: Ngemuva kokuphathwa ngomlomo, into ingena egazini ngemuva kwengxenye yehora. Ukugxila kwethanga kwenzeka emahoreni ama-2 uma amaphilisi edakiwe esiswini esingenalutho, futhi ngamahora angama-3.5 uma aphuzwa nokudla. Isenzo ngemuva komthamo owodwa sigcinwa okungenani ngosuku. Kufika kuma-30% wePioglitazone kanye nama-metabolites ayo akhishwa emchameni, amanye aqukethe indle.

Amalungiselelo we-pioglitazone

Umuthi wokuqala wasePioglitazone uthathwa njenge-Aktos okhiqizwa yinkampani yezokwelapha iMelika u-Eli Lilly. Into esebenzayo kumathebulethi yiPioglitazone hydrochloride, futhi izakhi ezisizayo ziyi-cellulose, i-magnesium stearate ne-lactose. Umuthi uyatholakala kumthamo we-15, 30, 45 mg. Manje ukubhaliswa kwe-Aktos eRussia sekuphelelwe yisikhathi, umuthi awukabhaliswa kabusha, ngakho-ke awunakuthenga kumakhemisi. Lapho u-oda usuka eYurophu, intengo yesishuqulu sama-Aktos izoba cishe ngama-ruble angama-3300. iphakethe ngalinye lamathebulethi angama-28.

Ama-Analogs eRussia azobiza kakhulu. Isibonelo, inani lentengo lePioglar licishe libe ngama-ruble angama-400. amaphilisi angu-30 ama-30 mg. Lokhu kulungiswa okulandelayo kwePioglitazone kubhalisiwe ebhukwini lombuso:

Zonke lezi zidakamizwa ziyi-analogues ephelele ye-Aktos, okungukuthi, ziphinda ngokuphelele umphumela we-pharmacological wesidakamizwa sokuqala. Ukusebenza okulinganayo kuqinisekiswa izifundo zomtholampilo. Kodwa ukubuyekezwa kwabanesifo sikashukela akuhambisani ngaso sonke isikhathi nabo, abantu bathembela i-Aktos ngaphezulu.

Izinkomba zokwamukelwa

I-pioglitazone isetshenziselwa ukunciphisa i-glycemia kuphela kuhlobo 2 sikashukela. Njengamanye ama-ejenti omlomo we-antidiabetic, uPioglitazone akakwazi ukuthinta ngempumelelo ushukela wegazi uma onesifo sikashukela engazange alungise indlela yakhe yokuphila. Okungenani, udinga ukunciphisa inani lama-carbohydrate asetshenzisiwe, futhi ngesisindo ngokweqile - nama-kilojoule, faka izivivinyo zakho zokuvivinya umzimba nsuku zonke. Ukuze uthuthukise i-glycemia ye-postprandial, udinga ukukhipha ukudla nge-GI ephezulu ekudleni, usabalalise ama-carbohydrate ngokulinganayo kukho konke ukudla.

I-pioglitazone iyasebenza futhi njenge-monotherapy, kepha imvamisa ichazwa njengengxenye yokwelashwa okuhlanganiswayo okubandakanya ama-hypoglycemic agents amaningana. Imiyalo yokusebenzisa ikuvumela ukuthi usebenzise i-Pioglitazone ngokuhlangana ne-metformin, i-sulfonylureas, ne-insulin.

Izinkomba zokuqokwa kwamathebhulethi:

1. Sisanda kuthola isifo sikashukela kwiziguli ezikhuluphele, uma onesifo sikashukela esene-contraindication yokusetshenziswa (ukuhluleka kwe-renal) noma ukubekezelela okungahambi kahle (ukuhlanza, isifo sohudo) se-metformin.
2. Ngokubambisana ne-metformin kuma-diabetics angama-feta uma i-metformin monotherapy ayanele ukwenza ushukela ube ngokwejwayelekile.
3. Ngokuhambisana namalungiselelo we-sulfonylurea, uma kunesizathu sokukholelwa ukuthi isiguli saqala ukuwohloka ukwakheka kwe-insulin yaso.
4. Isifo sikashukela esincike ku-insulin, uma isiguli sidinga imithamo ephezulu ye-insulin ngenxa yokuzwela okuphansi kwezicubu kuso.

Contraindication

Umyalo wenqabela ukuthatha iPioglitazone kulezi zimo ezilandelayo:

• uma i-hypersensitivity okungenani kwenye yezakhi zomuthi itholakele. Ukusabela okungezwani komzimba ngendlela yokumiswa noma ukuqubuka akudingi ukuyekwa komuthi;
• ngohlobo lwe-1 sikashukela mellitus, noma isiguli singamelana ne-insulin;
• ezinganeni ezinesifo sikashukela;
• ngesikhathi sokukhulelwa kanye ne-HB. Ucwaningo kula maqembu eziguli ezinesifo sikashukela alwenziwe, ngakho akwaziwa ukuthi ngabe uPioglitazone weqa umgoqo we-placental ungene kubisi. Izibhebhe zikhanselwa ngokushesha lapho nje ukukhulelwa sekuqaliwe;
• ukwehluleka kwenhliziyo okukhulu;
• ezimweni ezibucayi ezidinga ukwelashwa kwe-insulin (ukulimala okungathi sína, izifo nokuhlinzwa, i-ketoacidosis), wonke ama-ejenti we-tablet hypoglycemic akhanselwa okwesikhashana.

Umyalo utusa ukuthatha lo muthi ngokuqapha uma kwenzeka une-edema, i-anemia. Akukona ukweqa umthetho, kepha ukwehluleka kwesibindi kudinga ukubhekwa okwengeziwe kwezokwelapha. Nge-nephropathy, iPioglitazone ingasetshenziswa ngenkuthalo kune-metformin, ngoba le nto ayivezi kangako ezincekelweni zezinso.

Ukunakwa ikakhulukazi kudinga ukuqokwa kwePioglitazone yanoma yisiphi isifo senhliziyo. I-analogue yeqembu layo eliseduze kakhulu, i-rosiglitazone, iveze ingozi eyengeziwe yokuqunjelwa kwe-myocardial nokufa kusuka kwezinye izifo zenhliziyo. I-pioglitazone ayizange ibe nomphumela omubi kangako, kepha izindlela zokuqapha ezingeziwe lapho zizithatha ngeke zisaphazamisa. Ngokusho kodokotela, bazama ukuyidlala ephephile futhi abayikhiphi iPioglitazone engcupheni encane yokwehluleka kwenhliziyo.

Ukusebenzelana kwezidakamizwa

Ngokusetshenziswa okuhlangene kwePioglitazone nezinye izidakamizwa, ushintsho ekusebenzeni kwazo kungenzeka:

Kwezinye izidakamizwa, akukho ukusebenzisana nePioglitazone okutholakele.

Imithetho yokuthatha iPioglitazone

Akunandaba nomthamo, uPioglitazone udakwa kanye ngosuku ushukela. Ukubopha ukudla akudingeki.

Inqubo yokukhetha umthamo:

1. Njengomuthi wokuqala, phuza i-15 noma i-30 mg. Kwabanesifo sikashukela esikhuluphele, imiyalo incoma ukuqala kokwelashwa nge-30 mg. Ngokusho kokubuyekezwa, ngethamo elihlangene ne-metformin, i-15 mg yePioglitazone ngosuku yanele kwabaningi.
2. Umuthi unciphisa kancane kancane ukumelana ne-insulin, ngakho-ke kunzima ukuhlola ukusebenza kwawo ngemitha yeglucose yasekhaya. Isifo sikashukela sidinga ukuqashwa kwamakota kwe-hemoglobin ye-glycated. Umthamo wePioglitazone unyuka ngo-15 mg uma, ngemuva kwezinyanga ezi-3 zokuthatha i-GH, uhlala ngaphezulu kwe-7%.
3. Uma iPioglitazone isetshenziswa ndawonye ne-sulfonylurea noma i-insulin, i-hypoglycemia ingaqhamuka neziguli ezinesifo sikashukela. Kulokhu, udinga ukunciphisa umthamo wezidakamizwa ezengeziwe, umthamo wePioglitazone ushiywe ungashintshiwe. Ukubuyekezwa kweziguli eziphikisana ne-insulin kukhombisa ukuthi umuthi unganciphisa inani le-insulin esetshenziswa cishe ikota.
4. Umthamo omkhulu ovunyelwe yimiyalo yesifo sikashukela ngu-45 mg nge-monotherapy, i-30 mg uma isetshenziswa ngokubambisana nezinye izidakamizwa ezinciphisa ushukela. Uma ngemuva kwezinyanga ezi-3 zokuphuza iPioglitazone ngethamo elikhulu, i-GH ayibuyelanga kwesejwayelekile, esinye isiguli sinqunywe umuthi ukulawula i-glycemia.

Imiphumela emibi

Ukuqokwa kwePioglitazone ekusebenzeni ngokomtholampilo kukhawulelwe yimiphumela engathandeki yento, eminingi ikhula ngokusetshenziswa isikhathi eside:

1. Ezinyangeni zokuqala eziyisithupha, kuma-5% abantu abanesifo sikashukela, ukwelashwa nePioglitazone kuhlangana ne-sulfonylurea noma i-insulin kuhambisana nokwanda kwesisindo esifinyelela kuma-3.7 kg, bese le nqubo izinza. Uma uthathwa nge-metformin, isisindo somzimba asikhuphuki. Ku-mellitus yesifo sikashukela, lo mphumela ongathandeki ubalulekile, ngoba iziguli eziningi zikhuluphele. Ekuvikeleni umuthi, kufanele kuthiwe isisindo sikhuphuka ikakhulu ngenxa yamafutha angaphansi, futhi nethamo lamafutha e-visceral ayingozi kakhulu, ngokuhlukile, ayancipha. Okusho ukuthi, ngaphandle kokuthola isisindo, iPioglitazone ayifaki sandla ekuthuthukisweni kwezinkinga zesifo sikashukela.
2. Ezinye iziguli zibona ukugcinwa kwamanzi emzimbeni. Imiyalo esetshenzisiwe yazisa ukuthi imvamisa yokutholwa kwe-edema nge-pioglitazone monotherapy ingu-5%, kanye ne-insulin - 15%. Ukugcinwa kwamanzi kuhambisana nokwenyuka kwevolumu yegazi kanye noketshezi olungaphandle kwegazi. Kungenxa yalomphumela oseceleni lapho amacala wokuhluleka kwenhliziyo ehlotshaniswa nokuphathwa kwePioglitazone.
3. Ukwelashwa kungahle kuhambisane nokuncipha okuncane kwe-hemoglobin ne-hematocrit. Isizathu ukuthi kubuye kugcinwe uketshezi, akukho miphumela enobuthi ezinqubweni zokwenziwa kwegazi etholakele kulo muthi.
4. Ngokusebenzisa isikhathi eside i-rosiglitazone, i-analogue yePioglitazone, ukwehla kobuningi bethambo kanye nengozi eyengeziwe yokuqhekeka kwatholakala. NgePioglitazone, ayikho idatha enjalo.
5. Ku-0.25% yeziguli ezinesifo sikashukela i-mellitus, kunyuswe inani eliphindwe kathathu kumazinga e-ALT. Ezimweni ezingazodwa, kwatholakala ukuthi i-hepatitis iyatholakala.

Ukulawulwa kwempilo

Ukusetshenziswa kwePioglitazone kudinga ukubhekwa okwengeziwe kwesimo sempilo sikashukela:

Ungayifaka kanjani esikhundleni sePioglitazone

Kwizinto eziseqenjini le-thiazolidinedione, yi-rosiglitazone kuphela ebhaliswe eRussia ngaphandle kwePioglitazone. Iyingxenye yezidakamizwa iRoglit, Avandia, Avandamet, Avandaglim. Ucwaningo luye lwabonisa ukuthi ukwelashwa isikhathi eside nge-rosiglitazone kukhulisa ubungozi bokwehluleka kwenhliziyo, ukufa okuvela ekuqhekekeni kwe-myocardial, ngenxa yalokho, kunqunywa kuphela lapho kungekho okunye okungahlukile.

Ngaphezu kwePioglitazone, izidakamizwa ezakhiwe nge-metformin zinciphisa ukumelana ne-insulin. Ukwenza ngcono ukubekezelelwa kwalolutho, kudalwe amaphilisi wokukhishwa aguquliwe - Kukhiqizwe i-Glucofage Long nama-analogues.

Zombili i-rosiglitazone ne-metformin zinokuphikisana okuningi, ngakho-ke zingabekwa udokotela wakho kuphela.

Ukubuyekezwa kodokotela neziguli

Ama-endocrinologists anquma i-pioglitazone kuyaqabukela. Isizathu sokungawuthandi kwabo lo muthi isidingo sokulawulwa okwengeziwe kwe-hemoglobin nemisebenzi yesibindi, ingozi enkulu yokunquma umuthi wokwelashwa kwe-angiopathy kanye neziguli esezikhulile, ezakha iningi leziguli. Imvamisa, odokotela babheka iPioglitazone njengenye indlela ye-metformin lapho kungenakwenzeka ukuyisebenzisa, hhayi njenge-hypoglycemic ezimele.

Esikhathini sikashukela, iPioglitazone nayo ayithandwa. Isithiyo esikhulu ekusetshenzisweni kwaso yintengo ephezulu yesidakamizwa, ukungakwazi ukusithola mahhala. Umuthi awutholakali kuwo wonke amakhemisi, nawo ongangezi ukuthandwa kwawo. Imiphumela emibi yomuthi, ikakhulukazi isisindo, kanye nokuvela ngezikhathi ezithile mayelana nengozi yesifo senhliziyo uma uthatha ama-glitazones yiziguli ezesabekayo ezinesifo sikashukela.

Izibhebhe zoqobo zazilinganiswa yiziguli njengezisebenza kakhulu neziphephe kunazo zonke. Bathembela ama-generics amancane, bakhetha ukwelashwa ngezindlela zendabuko: metformin ne-sulfonylureas.