Ukusebenza kwesenzo se-saxagliptin emzimbeni kushukela

Ukudlanga kwesifo sikashukela sohlobo 2 emhlabeni kuyakhula, lokhu kungenxa yendlela yokuphila yabantu nokudla okunempilo. Kodwa-ke, i-pharmacology ayimile, ithuthukisa izinto ezintsha zokwelapha isifo sikashukela.

Enye yamakilasi amasha ezinto ezinjalo ama-incretin mimetics, ahlanganisa i-saxagliptin (saxagliptin).

Umshini wokusebenza kwama-incretins

Ama-incretin angama-hormone omuntu akhiqizwa yipheshana lesisu lapho ukudla kungena khona. Ngenxa yesenzo sabo, ukukhiqizwa kwe-insulin kuyanda, okusiza ukuthi ushukela ukhunjulwe, okhishwa ngesikhathi kugaywa.

Kuze kube manje, izinhlobo ezimbili zama-insretin zitholakele:

• I-GLP-1 (i-peptide-1 ye-glucone-1);
• I-ISU (insulinotropic polypeptide).

Ama-receptors okuqala asezitho ezihlukile, okumvumela ukuthi abonise umphumela obanzi. Okwesibili kulawulwa ama-pancreatic β-cell receptors.

Ezinye zezindlela eziyinhloko zesenzo sabo yilezi:

• ukukhushulwa okuthe xaxa kwe-insulin ye-hormone ngamaseli e-pancreatic;
• ukunciphisa ijubane esiswini;
• ukuncishiswa ekukhiqizeni ushukela;
• ukwehla kokudla kanye nomuzwa wokugcwala;
• ukuthuthuka kwenhliziyo nemithambo yegazi, umphumela omuhle ohlelweni lwezinzwa.

Ngokwanda kokukhiqizwa kwe-insulin, ushukela udonswa kangcono, kepha uma kuyinto evamile, inqubo yokufihla iyama futhi umuntu angabi sengozini ye-hypoglycemia. Ukwehla kwenani le-glucagon, umphikisi we-insulin, kuholela ekunciphiseni kokusetshenziswa kwe-glycogen yesibindi kanye nokukhululwa kweglucose yamahhala, ngenkathi ngakolunye uhlangothi kube nomthelela ekwandeni kokusetshenziswa kwe-glycogen emisipha. Ngenxa yalokhu, ushukela usetshenziswa ngokushesha endaweni yokukhiqiza, ngaphandle kokungena egazini.

Lapho ukukhishwa kwesisu kuncishisiwe, ukudla kungena amathumbu ngezingxenye ezincane, okunciphisa inani lokufakwa kweglucke egazini futhi ngenxa yalokho, kukhuphuka kokuhlushwa kwalo. Ukwenza ibhendi emincane, imunwa kalula ngumzimba. Kulokhu, ukwehla kokudla kunganciphisa ngokweqile.

Umphumela ohlelweni lokujikeleza kwegazi okwamanje ubonakalisiwe kuphela, kepha awufundwanga. Kutholakale ukuthi ama-incretin asiza ama-pancreatic β-cell alulame ngokushesha.

Akunakwenzeka ukuthola ama-hormone ngendlela yabo emsulwa ngamanani anele, ngakho-ke, ososayensi bahlakulele ama-analogues enza imisebenzi efanayo:

• ukuphinda uqalise ukusebenza kwe-peptide-1 ye-glucone-1;
• ukunciphisa imiphumela yama-enzyme abhubhisayo, ngaleyo ndlela kwandise impilo yama-hormone.

ISaxagliptin ingeyeqembu lesibili.

Khipha amafomu

ISaxagliptin iyingxenye yesidakamizwa u-Onglisa, esebenza njenge-inhibitor ye-DPP-4. Leli thuluzi alikho ohlwini lwenhlangano yemithi ekhethekile, kepha lunganikezwa iziguli ezinesifo sikashukela ngokuxhasa isabelomali sendawo.

Umuthi uyatholakala ngesimo sezibhebhe ezinegobolondo eliphuzi, equkethe i-2,5 mg ye-saxagliptin noma i-5 mg ye-hydrochloride yayo. Ukuqanjwa kubandakanya futhi izakhi ezandisa umphumela wento esebenzayo. Amacwecwe abhalwe ukuthi akhombisa umthamo wawo.

Amatafula agcwele iphakethe elinezinto eziyishumi kanye nebhokisi lekhadibhodi.

Izinkomba kanye ne-contraindication

Amalungiselelo asuselwa ku-Saxagliptin anconyelwe ukusetshenziswa ne:

1. Isigaba pre-sikashukela, lapho izinyathelo zendabuko, kufaka phakathi ukudla, ukuzivocavoca nezinye izincomo azisizi. Ithuluzi likuvumela ukuthi uyeke ukubhujiswa kwama-β-cell bese unqande ukuthuthukiswa kwesifo sikashukela sohlobo 2;
2. Ukuba khona kwesifo esitholakele. Kulokhu, ithuluzi lingasetshenziswa njengomuthi ozimele noma lihlanganiswe nezinye izidakamizwa:
   • I-Metformin;
   • insulin;
   • izinto ezithathwe kuma-sulfonylurea;
   • nguyenkungu.

Ukuxhumana kokuphuza umuthi yilezi:

• thayipha i-1 isifo sikashukela;
• ukuthambekele ngokweqile kunoma yiziphi izingxenye zomuthi;
• ukuzwela okuphezulu kuma-inhibitors e-DPP-4;
• ukuba khona kwe-ketoacidosis yesifo sikashukela;
• i-indigestibility ye-lactose kanye nokushoda kwe-lactase, ukuzalwa kwe-glucose-galactose malabsorption;
• isikhathi sokukhulelwa nokuqunjelwa;
• iminyaka emincane.

Kulezi zimo, izifaniso zomuthi ziyasetshenziswa noma imali enesakhiwo esehlukile iyakhethwa.

Ukusebenza kokuqala kwe-saxagliptin + metformin

Imiyalo yokusebenzisa

Ithebhulethi zithathwa ngomlomo ngaphandle kokubheka ukudla. I-capsule igwinyiwe igcwele igezwe ngenani elincane lamanzi. Umthamo uncike ohlotsheni lokwelashwa nenhlala kahle yesiguli.

Ngokusetshenziswa okuhlukile, i-saxagliptin inconywa ukuthatha i-5 mg kanye ngosuku.

Ekwelashweni okuhlanganisiwe nezinye izidakamizwa zesifo sikashukela, umthamo ngu-5 mg ngosuku, okufanayo kusebenza ekuhlanganiseni kokuhlanganiswa okusetshenzisiwe kwama-hypoglycemic agents nge-saxagliptin

Esigabeni sokuqala sokusetshenziswa kwento ene-metformin, umthamo we-saxagliptin ungama-milligram angama-5, kuthi i-metformin ngama-milligram angama-500 ngosuku.

Ezigulini ezine-pathology yezinso, umthamo wehliselwa ku-2,5 mg ngosuku. Uma i-hemodialysis isetshenziswa, umuthi udakwa ngemuva kokuphothulwa kwawo. Umphumela womuthi ngenkathi kwenziwa i-peritoneal dialysis awukaphenywa. Kunoma ikuphi, ngaphambi kokunquma umuthi, ochwepheshe beluleka ukuthi bahlole isiguli.

Ezigulini ezine-pathologies yesibindi yokusebenza, ukulungiswa kwamthamo akudingekile. Ukwelashwa kwenziwa ngokuya ngezincomo ezijwayelekile. Lokhu kuyasebenza nasezigulini esezikhulile, uma nje zingenazo izinkinga zezinso.

Ucwaningo lwethonya lomuthi ku-fetus kwabesifazane abakhulelwe nezingane ezisencane alukenziwa. Ngakho-ke, kunzima ukubikezela imiphumela yako. Kulezi ziguli, ezinye i-ejenti ezifakazelwe zivame ukusetshenziswa. Uma owesifazana ethatha i-saxacgliptin ngesikhathi sokuncelisa, kufanele anqabe ukondla.

Esimweni sokuphatha kanyekanye ngama-inhibitors e-CYP3A4 / 5 asebenzayo, isilinganiso semithi yansuku zonke sinqanyuliwe.

Le yimithi elandelayo:

• I-Ketoconazole;
• Clarithromycin;
• Atazanavir;
• Indinavir;
• Nefazodon;
• I-Itraconazole;
• I-Ritonavir;
• I-Telithromycin;
• INelfinavir;
• Saquinavir nabanye.

Lapho uthatha i-saxagliptin, isiguli siyaqhubeka nokusebenzisa izincomo ezijwayelekile enhlanganweni yokudla, sikhiphe izivivinyo zomzimba futhi siqaphe isimo sengqondo.

Imiphumela emibi kanye ne-overdose

Umuthi awunayo imiphumela emibi. Inzuzo yayo eyinhloko ukuntuleka kwengozi ye-hypoglycemia.

Kodwa-ke, njenganoma yisiphi isidakamizwa sokwenza, sithinta izinqubo zomzimba womzimba, ezinegalelo ekuguqukeni kwabo, okungaholela ku:

• ukuthuthukiswa kwezifo ezithathelwanayo zohlelo lokuphefumula;
• ukuphazamiseka kwe-dyspeptic;
• i-sinusitis
• ukubonakala kwekhanda;
• i-gastroenteritis;
• ukuthuthukiswa kokuvuvukala ohlelweni lwezitho zofuzo.

Lapho ubheka noma yiziphi zalezi zimpawu, kufanele ukhononde kudokotela ozobe esekhetha umthamo ofanele womuthi noma awushintshe kwamanye amaphilisi.

I-overdose esivivinyweni somtholampilo ayitholakalanga, ngenkathi ukugxila kwezikhathi ezingama-80 eziphakeme kunalezo ezinconyiwe kwakusetshenziswa. Uma kwenzeka kuba nezimpawu ze-overdose (isicanucanu, ukuhlanza, isifo sohudo, ikhanda, ubuthakathaka, njll.), Ukwelashwa kwenziwa ngokwezimpawu ngokususwa ngokushesha komuthi emzimbeni, okulula ukukwenza ngokusebenzisa i-hemodialysis.

Lapho kuhlanganiswa nezinye izidakamizwa, ukuphambuka okumenyezelwe akuzange kutholakale. Kodwa-ke, ukusetshenziswa okufanayo kanye ne-metformin ne-thiazolidinediones akufundwanga.

Ividiyo evela kusazi:

Yini engathatha isikhundla saxagliptin?

Ukusetshenziswa kwe-saxagliptin njengengxenye eyinhloko kuthuthukiswa kuphela kumuthi we-Onglise, uma isiguli sinemiphumela emibi, kuzodingeka sisebenzise i-analogues, efaka nezinye izinto ezivimbela i-enzyme ye-DPP-4:

1. UJanuvia - Elinye lamathuluzi okuqala alolu hlobo, athuthukiswe e-United States. Kuyabonakala kumthamo ka-25, 50 no-100 mg. Isimo semihla ngemihla simayelana ne-100 mg. Umphumela wesidakamizwa uhlala cishe usuku. Kwesinye isikhathi kukhiqizwa ngaphansi komkhiqizo weYanuMet, okungezelela ukuthi uqukethe i-metformin.
2. UGalvus - umuthi okhiqizwa eSwitzerland, usetshenziswa kumthamo ka-50 mg ngosuku noma ngaphezulu, uvame ukusetshenziswa ngokubambisana ne-insulin.
3. INesina - ekhiqizwa e-Ireland, isuselwa ku-apolgiptin benzoate ngomthamo ka-12,5 noma 25 mg. Ithebhulethi eli-1 lithathwa kanye ngosuku.
4. I-Vipidia - into esemqoka ye-alogliptin yezidakamizwa, enomphumela ofanayo, ithathwa kanye ngosuku umthamo we-25 mg.
5. I-Trazhenta - ithuluzi elususelwe kwe-linagliptin, itholakala ngesimo samaphilisi ayi-5 mg athathwe ngomlomo.

Amanye ama-analogues asetshenziswa anokwakheka okuhlukile, kepha inqubo efanayo yokwenza. Izindleko zezidakamizwa ziyehluka ngokuya ngezwe lokukhiqizwa nokwakheka kwale mishanguzo.

Intengo yesidakamizwa u-Onglisa, okubandakanya i-saxagliptin, kusuka ku-1700 kuya ku-1900 ruble.

Isizukulwane esisha sezidakamizwa senza sikwazi ukuxazulula ngokushesha futhi kalula izinkinga zokuthathwa koshukela ezigulini ezinesifo sikashukela.

Ngenkathi uhlu lwabo lungakabi banzi kakhulu, kukhiqizwa isidakamizwa esisodwa kuphela ngesisekelo se-saxagliptin, esinomthelela omuhle ekwelashweni kwesifo sikashukela futhi akubangeli isimo se-hypoglycemia. Ngasikhathi sinye, kukhona ama-analogu aqukethe into ehlukile esebenzayo, kepha ngomphumela ofanayo wokwelapha.