I-Glibenclamide - imiyalo yokuthi iyingozi nokungena ngakuphi

I-Glibenclamide iyindawo etholakala kakhulu futhi isetshenziswa kabanzi nge-sulfonylurea enezakhiwo ezinokwehlisa ushukela. Ngo-2010, waklonyeliswa ngomklomelo ohlonishwayo weKreutzfeld, onikezwa impumelelo yemithi. Umuthi uhambisana ngokuphelele nenqubo eqinile ebekwe yikomidi lokukhetha, ukusebenza kwalo kuqinisekiswa ngeminyaka eminingi yocwaningo nokuzilolongela ngemitholampilo.

Zimbalwa izidakamizwa ezingazigabisa ngeminyaka engama-20 yokubukwa kanye nokutadisha ngokucophelela imiphumela eyephuzile yokusetshenziswa kwayo. Intengo ephansi yamaphilisi inciphisa kakhulu izindleko zizonke zokwelapha isifo sikashukela. Ngokwendlela yokubiza eshibhile nokusebenza kahle, i-glibenclamide ifakiwe ohlwini lwezidakamizwa ezibalulekile ezisetshenziselwa ushukela. Ngaphandle kwakhe, iMetformin ne-insulin kuphela ezinikezwe udumo olunjalo.

Izinkomba zokuqokwa

Uhlobo lwesibili sikashukela yisifo esiqhubekayo esidinga ukwelashwa okuqhubekayo. Noma ngaphansi kwezimo zokulawulwa okuhle kwe-glycemic, ukusebenza kwamaseli we-beta kuya ngokuya kukhula ezigulini futhi inani lokukhiqizwa kwe-insulin kuzo liyancipha. Ngoshukela ophakanyisiwe oqhubekayo, izinqubo zokubhujiswa kwamaseli ziyasheshiswa. Izinguquko zokuqala secretion ye-insulin zingabonakala ngesikhathi sokuxilongwa. Kwezinye iziguli, alithinti kakhulu izinga likashukela, futhi ukunxephezela isifo sikashukela, umsoco ofanele kuphela, i-metformin kanye nemfundo yomzimba yanele.

Isifo sikashukela, lapho amaseli e-beta enempilo angakwazi ukuzisebenzela futhi nabafowethu abafile, kufanele banikeze imfihlo yomfihlo. Zivusa ukwakheka kwe-insulin, okwenza amaseli asebenze ngokwengeziwe.

Lapho i-glibenclamide inqunyelwe:

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%

1. Umuthi ubhekwa njengenye yezimfihlo ezinamandla kakhulu, ngakho-ke kukhonjiswa ezigulini ezinesifo sikashukela esinokuncipha okunciphisiwe kwe-insulin yazo, njengoba kufakazelwa yi-glycemia ephezulu kakhulu ngesikhathi sokuxilongwa. Nge-mellitus ebunjiwe yesifo sikashukela, ukuthuthuka akwenzeki ngokushesha, kancane kancane ushukela uphela cishe amasonto amabili. Isifo sikashukela esine-hyperglycemia encane asikuniki imishanguzo ngokushesha ngemuva kokuxilongwa kwesifo sikashukela.
2. I-Glibenclamide iboniswa ukuqinisa ukwelashwa ngaphezu kwamanye ama-ejenti. Sekuyisikhathi eside kufakazelwa ukuthi izidakamizwa ezimbalwa ezinciphisa ushukela ezithinta izimbangela ze-hyperglycemia ezivela ezinhlangothini ezihlukene zisebenza kakhulu kunoyedwa. Ukwenza ngcono ukulawulwa kwe-metabolic, i-glibenclamide ingahlanganiswa ne-insulin kanye namanye amaphilisi okwehlisa ushukela, ngaphandle kwe-PSM nobumba.

Lapho unquma umuthi, kufanele kukhunjulwe ukuthi kufaka amaseli we-beta ukusebenza ngamandla amakhulu. Ngokusho kocwaningo, ukukhuthaza okunjalo kuholela ekunciphiseni okuncane kwesikhathi sabo sempilo. Njengoba i-glibenclamide inamandla eqenjini layo, lo mphumela ongathandeki udalulwa kakhulu kuwo kune-PSM yanamuhla. Uma umuntu onesifo sikashukela efuna ukugcina ukwakheka kwe-insulin isikhathi eside ngangokunokwenzeka, ukwelashwa nge-glibenclamide kufanele kuhlehliswe kuze kube yilapho izidakamizwa ezibuthakathaka ziyeka ukulawula isifo sikashukela.

Indlela i-glibenclamide esebenza ngayo

Indlela yokusebenza ye-glibenclamide iqondakala kahle futhi ichazwa ngokuningiliziwe emiyalweni yomuthi. Umuthi uvimba iziteshi ze-KatiF ezitholakala kungqimba yamangqamuzana e-beta, okuholela ekunqanyelweni kwe-potassium kumaseli, okwenza buthaka ukuhlukaniswa kolwelwesi kanye nokungena kwe-calcium ion. Ukwanda kokuxinzekwa kwe-calcium esitokisini kuvuselela inqubo yokukhishwa kwe-insulin kuyo kuyiwe ku-infellular fluid, bese kungena egazini. I-glucose iyancipha ngenxa yekhono le-insulin yokuyihambisa emithanjeni yegazi iye kwezicubu. I-Glibenclamide ikhuthele kakhulu kunezinye i-PSM ezibopha kuma-beta-cell receptors, ngakho-ke inomphumela omuhle kakhulu wehlisela ushukela.

Amandla omuthi akhuphuka ngomthamo owandayo. Umphumela we-glibenclamide awuxhomekile ku-glycemia, umuthi usebenza ngokweqile kwe-glucose nangongenele, ngakho-ke lapho uwuthatha, kudingeka uqaphele ngangokunokwenzeka futhi ulinganise ushukela lapho kuvela noma yiziphi izimpawu ezifana ne-hypoglycemic.

Ngaphezu kwe-hypoglycemic enkulu, umphumela owengeziwe we-peripheral ubonakala kuyo yonke i-PSM. Ngokusho kwemiyalo, i-glibenclamide inciphisa kancane ukumelana kwe-insulin kwamangqamuzana emisipha namafutha, okufaka isandla ekwehlelweni okwengeziwe kweglucose.

Imiphumela yemizwa yesidakamizwa yafundwa eceleni. Kwavela ukuthi i-glibenclamide iyakwazi ukuvimba iziteshi ze-KatiF hhayi kuphela kumaseli we-beta, kodwa nakumaseli ezinhliziyo - i-cardiomyocyte. Ngokwe-theory, isenzo esinjalo singaba sibi kakhulu imiphumela yokuhlaselwa yisifo senhliziyo kwabanesifo sikashukela. Kwivivinyo lomtholampilo, lo mphumela wecala awukaqinisekiswa. Ngaphezu kwalokho, kutholakale umphumela we-antiarrhythmic ku-glibenclamide, okunciphisa ukufa kwabantu esikhathini esibi se-ischemia. Ngokusho kodokotela, iningi labo liyasaba ukunquma umuthi i-Glibenclamide nganoma yisiphi isifo senhliziyo esitholakele, naphezu kwedatha yocwaningo.

Amalungiselelo we-Glibenclamide

Iningi labanesifo sikashukela bajwayelana ne-glibenclamide ngomuthi iManinil, okhiqizwa eJalimane yiBerlin-Chemie. Lo muthi ungowokuqala, ngokubamba iqhaza kwawo inani elikhulu kakhulu locwaningo lwenziwe olufunde ukusebenza ngempumelelo nokuphepha kwe-glibenclamide. IManinil inezinketho ezintathu zomthamo. Ezibhebheni ze-1.75 kanye ne-3.5 mg, into esebenzayo isefomini elikhethekile elinemikghoni, elivumela ukunciphisa i-glycemia ngethamo eliphansi lomuthi. I-5 mg maninyl iqukethe i-classic glibenclamide.

Analogs eRussia yile:

• IStiglin esivela kuFarmasintez-Tyumen noGlibenclamide abavela enkampanini yase-Ozon (irejista. Isitifiketi ngesika-Atoll LLC). Le mishanguzo inemithamo efanayo, kodwa abakhiqizi abatshelanga ubukhona be-glibenclamide enemicrosoft kunoma yikuphi ukukhetha.
• Amathebulethi eGlibenclamide akhiqizwa nguMoskhimpharmpreparaty, Pharmaceard-Leksredstva, Biosynthesis, uValenta Pharmaceuticals anomthamo owodwa we-5 mg. Zingahlukaniswa ukuze zithole umthamo onguhafu ka-2,5 mg.

Kuhle ukuqaphela ukuthi zingama-analogues asekhaya kuphela, ngoba amabhizinisi athenga i-glibenclamide phesheya, ikakhulukazi eNdiya. Okuwukuphela kwento eyodwa yi-Statiglin, ebhaliswe ngo-2017. IGlibenclamide ngoba ikhiqizwa eRussia ebhizinisini leBratskKhimSintez.

Zonke izikhombisi zeManinil zivivinyelwa i-bioequivalence futhi zibe nokwakheka okufanayo. Ukubuyekezwa kweziguli kukhombisa ukuthi le mishanguzo isebenza ngokulingene, kepha abashukela abanesifo sikashukela bancamela ukuthenga umuthi wokuqala, ngenxa yedumela lawo elikhulu nentengo ephansi.

Ngokuqhathanisa nokubuyekezwa, inhlanganisela ye-glibenclamide ne-metformin nayo ithandwa kakhulu. Lezi zinto zombili ziyingxenye yezidakamizwa eziqukethe izingxenye ezimbili i-Glucovans, Glimecomb, Gluconorm. Metglib, Glibomet nabanye.

Imiyalo yokusebenzisa

Umyalo wokusetshenziswa uncoma ukunquma isidingo se-glibenclamide ngawodwana esigulini ngasinye:

1. Umthamo wokuphepha ophephile ungaphezu kuka-2,5 mg, onobunzima obukhulu be-hyperglycemia - 5 mg. Kuvunyelwe ukuqala ukwelashwa nge-glibenclamide kuphela uma ukulawulwa okujwayelekile kwe-glycemic kungenzeka futhi kuphela njengoba kuyalelwe nangaphansi kokuqondisa kukadokotela. Akumele sikhohlwe ukuthi umuthi ungadala i-hypoglycemia, kubandakanya kakhulu. Umuthi osezingeni elincane udakwa kanye ngosuku, imizuzu engama-20 ngaphambi kokudla kwasekuseni. I-Microsized glibenclamide ithathwa ngaphambi kokudla.
2. Uma amazinga kashukela engabuyanga ejwayelekile phakathi nesonto, umthamo uyakhuphuka kancane kancane, unezela u-1.75-2.5 mg kanye ngesonto. Ngomthamo ofinyelela ku-10 mg, i-glibenclamide idakiwe ekuseni. Uma kudingeka umthamo omkhulu ukunxephezela ushukela, umuthi udakwa ngaphambi kokudla kwasekuseni nangaphambi kokudla. Ukuthatha i-glibenclamide ngaphambi kokulala kunqatshelwe yimiyalo, ngoba kungaholela ku-hypoglycemia yasesikhathini.
3. Umthamo omkhulu ngamathebulethi ama-3 we-5 mg. Ababili babo baphuza ekuseni, omunye ngaphambi kokudla.

Imiphumela emibi

Imvamisa yemiphumela engathandeki ekwelashweni ne-Glibenclamide iphansi. Ngomthamo ofanele nokuhambisana nemiyalo yokusetshenziswa, imiphumela emibi itholakala cishe ku-1% yabanesifo sikashukela, esibonisa ukuphepha okuphezulu komuthi.

I-Hypoglycemia kanye nokuthola isisindo kuwumphumela wokungondleki kanye ne-overdose ye-glibenclamide. Ngokusho kwesifo sikashukela, uma ulungiselela ukudla okudlayo, ubale inani lama-carbohydrate ekudleni ngakunye, ungakweqi ukudla, hlela ukudla okulula ngenkathi uzivocavoca isikhathi eside, ubungozi bale miphumela mibi bungancishiswa kakhulu.

Ukwemukelwa kubani?

Umyalo wethula ukuvinjelwa kokuthatha amaphilisi we-Glibenclamide kulezi zimo ezilandelayo:

• uma umuthi noma izifanekisimo zawo ngaphambilini zinokungezwani komzimba;
• lapho ishukela likashukela lingenawo ama-beta cell (uhlobo 1 sikashukela, resection pancreatic);
• esimweni sokuwohloka okukhulu kwesifo sikashukela i-mellitus nge-ketoacidosis noma engcupheni enkulu yokuhoxa ngenxa yokulimala okubi nezifo;
• ngokulimala okunamandla kwe-renal kanye ne-hepatic;
• uma kwenzeka ukungabekezelelani kwe-lactose, okuqukethwe kulo muthi njengento yokusiza;
• ngesikhathi sokukhulelwa, ukukhulelwa;
• ezinganeni ezinesifo sikashukela.

Ngokuqapha ngokweqile, kuyadingeka ukwenza ukwelashwa kokuphazamiseka kwe-hormonal, uphuzo oludakayo, izifo zokugaya ukudla, ukuguga, ekushiseni okuphezulu.

Ukweqisa

I-overdose ihlala iholela ku-hypoglycemia. Esigabeni sokuqala, kungaqedwa ukuphathwa okwengeziwe komlomo kwe-glucose. Uma i-hypoglycemia ikhuphukile, imiyalo incoma ukuphathwa kwe-glucagon kwe-subcutaneous. Ngesikhathi esifanayo, isifo sikashukela sidinga ukunakekelwa okuphuthumayo kwezokwelapha. Ngomthamo omubi wesidakamizwa i-Glibenclamide, ushukela wehla kaninginingi phakathi nosuku, ngakho-ke isiguli sifakwa ngekhambi le-glucose ngaphakathi futhi siqaphe isimo sakhe.

Ama-analog we-Glibenclamide kanye nokufakwa esikhundleni

Ama-analogues asondele kakhulu we-glibenclamide ezinye izinto eziphuma ku-sulfonylureas. Njengamanje, i-glyclazide, i-glimepiride isetshenziswa kabanzi, kuvame kakhulu i-glycidone.

Indawo ebiza kakhulu ye-glibenclamide

Ama-Gliptins, futhi avuselela ukuhlanganiswa kwe-insulin, abiza kakhulu ama-glibenclamide analogues. Ama-Gliptins ayingxenye kaJanuvii, Ongliza, Xelevia, Galvus, Trazhenty, izindleko zawo zokwelapha zibiza okungenani ama-ruble ayi-1,500. ngenyanga. Le mishanguzo ayibangeli i-hypoglycemia, ayifaki sandla ekubhujisweni kwamaseli we-beta, kepha unganciphisi ushukela ngokushesha njenge-glibenclamide. Ngokusho kokubuyekezwa, ama-glyptins anikeza imiphumela engcono nge-glycemia ephezulu kakhulu.

Inani lentengo emakhemisi

I-Maninil equkethe i-glibenclamide enemicrosoft ibiza ama-ruble ayi-130-160. iphakethe ngalinye elinamathebulethi ayi-120. IManinil 5 mg izoba eshibhile, intengo yepakethe ingama-ruble ayi-120. Izindleko zama-analogues ezifuywayo ziphansi ngisho: kusuka kuma-ruble angama-26. amaphilisi angu-50 noma ama-ruble angama-92. amaphilisi angu-120. Ngakho-ke, noma umthamo ophelele, intengo yokwelashwa ayidluli ama-ruble ayi-100. ngenyanga.

Umuthi iGlibenclamide ungatholwa mahhala kunoma yisiphi isifunda saseRussia, uma isiguli sinesifo sikashukela, futhi sibhaliswa nodokotela oyisidakamizwa.

Ukubuyekezwa kwesifo sikashukela