Izinkampani zemithi ezaziwayo zihlala zakha amathuluzi amasha wokulawula i-glycemic. Umuthi owodwa onjalo yi-dapagliflozin. Umuthi waba ngummeleli wokuqala weqembu le-inhibitors ye-SGLT2. Akuthinti ngqo noma iziphi izimbangela zesifo sikashukela; umphumela wazo ukukhipha ushukela ngokweqile egazini ungene kumchamo. Umphumela omuhle we-dapagliflozin on ngokweqile kanye nomfutho wegazi nawo watholakala. Umuzwa wokusebenzisa lo muthi eRussia awudluli iminyaka emi-5, ngakho-ke ama-endocrinologists amaningi akhetha izidakamizwa ezindala ezifakazelwe, esaba imiphumela emibi yesikhathi eside.
Ukulungiselela kwe-Dapagliflozin
Igama lokuhweba le-Dapagliflozin lithi I-Forsyga. Inkampani yaseBrithani i-AstraZeneca ikhiqiza amaphilisi ngokubambisana ne-American Bristol-Myers. Ukuze usebenzise kalula, umuthi unemithamo emi-2 - 5 no-10 mg. Umkhiqizo woqobo kulula ukuwuhlukanisa kumkhohlisi. Amacwecwe weForig 5 mg anejamo eliyindilinga futhi okubhaliwe okukhishwe "5" no "1427"; I-10 mg - imise okwamadayimane, abhalwe "10" no "1428". Ithebhulethi yomibili imithamo iphuzi.
Ngokwemiyalo, i-Forsigu ingagcinwa iminyaka emi-3. Ngenyanga yokwelashwa, iphakethe elilodwa liyadingeka, intengo yalo icishe abe ngama-ruble angama-2500. Ithiyori, kwisifo sikashukela i-mellitus, i-Forsigu kufanele ichazwe mahhala, ngoba iDapagliflozin ifakiwe ohlwini lwemithi ebalulekile. Ngokusho kokubuyekezwa, kuyaqabukela kakhulu ukuthola isidakamizwa. IForig inqunyiwe uma kukhona ukungqubuzana nokuthatha i-metformin noma i-sulfonylurea, futhi nangezinye izindlela akunakwenzeka ukufeza ushukela ojwayelekile.
U-Forsigi akanazo i-analogues ephelele, ngoba ukuvikela kwe-patent kusasebenza ku-Dapagliflozin. Ama-analogues eqembu abhekwa njenge-Invocana (aqukethe i-canagliflozin SGLT2 inhibitor) noJardins (empagliflozin). Intengo yokwelashwa ngalezi zidakamizwa ivela kuma-ruble angama-2800. ngenyanga.
Isenzo sezidakamizwa
Izinso zethu zibamba iqhaza kakhulu ekugcineni amazinga kashukela egazini. Ebantwini abaphilile, kufinyelela ku-180 g we-glucose ohlungwayo nsuku zonke kumchamo oyinhloko, cishe wonke uyabuyiselwa futhi ubuyiselwe egazini. Lapho i-glucose emikhunjini ikhuphuka ku-mellitus yesifo sikashukela, ukuhlunga kwayo ku-glomeruli ye-renal nakho kuyanda. Lapho ifinyelela ezingeni elithile (cishe ama-10 mmol / l ezinhlokodweni ezinesifo sikashukela ezinso ezinempilo), izinso ziyeka ukuphinda zibambe lonke ushukela bese ziqala ukususa ngokweqile kumchamo.
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-glucose ayinakungena ngaphakathi kolwelwesi ngokwayo, ngakho-ke, abathuthi be-sodium-glucose babamba iqhaza ezinhlelweni zayo zokubuyiselwa emuva. Inhlobo eyodwa, i-SGLT2, itholakala kuphela kuleyo ngxenye yezithonjana lapho ingxenye enkulu yeglucose iphinde yenziwa kabusha. Kwezinye izitho zomzimba, i-SGLT2 ayitholakalanga. Isenzo se-Dapagliflozin sisuselwa ekuvinjelweni (kokuvinjelweni) komsebenzi walento yokudlulisa. Isebenza kuphela ku-SGLT2, ayithinti abathutha be-analog, futhi ngenxa yalokho ayiphazamisi i-carbohydrate metabolism ejwayelekile.
I-Dapagliflozin iphazamisa umsebenzi wezinso wezinso kuphela. Ngemuva kokuphuza iphilisi, ushukela ophinda abambe ushukela uyaqina futhi uqala ukuthululwa emchameni ngevolumu enkulu kunangaphambili. I-Glycemia iyancishiswa. Umuthi awuthinti ushukela ojwayelekile, ngakho-ke ukuwuthatha akubangeli i-hypoglycemia.
Ucwaningo luye lwabonisa ukuthi umuthi awugcini nje ngokunciphisa ushukela, kodwa futhi uthinta ezinye izici zokwenziwa kwezinkinga zesifo sikashukela:
- I-Normalization ye-glycemia iholela ekunciphiseni kokumelana ne-insulin, ngemuva kwengxenye yenyanga yokuthatha inkomba incipha ngokwesilinganiso se-18%.
- Ngemuva kokunciphisa imiphumela enobuthi ye-glucose kumaseli e-beta, ukubuyiselwa kwemisebenzi yabo kuqala, i-insulin synthesis inyuka kancane.
- I-Excretion ye-glucose iholela ekulahlekelweni kwama-kilojoule. Imiyalo ikhombisa ukuthi uma usebenzisa i-Forsigi 10 mg ngosuku, cishe u-70 g we-glucose ukhishwa, ohambelana nama-280 kilocalories. Ngaphezu kweminyaka emi-2 yokwamukelwa, ukulindeka kwesisindo okungamakhilogremu ayi-4,5 kungalindelwa, kuthi ama-2.8 - ngenxa yamafutha.
- E-diabetesics ekuqaleni kwegazi eliphezulu, ukuncipha kwayo kuyabonakala (i-systolic yehla cishe ngu-14 mmHg). Ukuqashelwa kwenziwa iminyaka engu-4, umphumela waphikelela sonke lesi sikhathi. Lo mphumela we-Dapagliflozin uhlotshaniswa nomphumela wawo ongasho lutho we-diuretic (umchamo more ukhishwa kanyekanye noshukela) kanye nokwehla kwesisindo lapho usebenzisa umuthi.
I-Pharmacokinetics
IDapagliflozin igxishwe ngokuphelele kusuka emgudwini wesisu, i-bioavailability yesidakamizwa icishe ibe yi-80%. Ukuqunjelwa okuphezulu kwento esegazini kubonwa ngemuva kwamahora ama-2 uma amaphilisi edakiwe esiswini esingenalutho. Lapho isetshenziswa ngasikhathi sinye ngokudla, inani eliphakeme lokuhlushwa lifinyelelwa kamuva, ngemuva kwamahora amathathu. Ngasikhathi sinye, ukusebenza kokwehlisa ushukela akushintshi, ngakho-ke amaphilisi angadakwa ngokungakhathalekile isikhathi sokudla.
Isilinganiso sokuphila esisusa amahora ayi-13; yonke i-Dapagliflozin ikhishwa isikhathi esingaphezu kosuku. Cishe ama-60% ento ayenziwa umzimba, okunye kuphuma kungashintshiwe. Indlela ekhethiwe yokuphuma ku-excretion izinso. Umchamo, ama-75% we-Dapagliflozin kanye nama-metabolites awo atholakala, ezindlekeni - ama-21%.
Izici ze-pharmacokinetics emaqenjini ahlukahlukene kashukela, kuboniswe kwimiyalo esetshenziswayo:
- ukusebenza kuncipha ngomsebenzi wokuphazamiseka wezinso. Ngokuhluleka okwezinso okuncane, cishe i-52 g yeglucose iyakhululwa ngosuku, ngokwehluleka okunamandla kwezinso, kungabi ngaphezu kwe-11 g;
- isibindi siyabandakanyeka kumetabolism ye-Dapagliflozin, ngakho-ke ukungatholakali kahle kwayo kuholela ekwandeni kokuqoqwa kwento ngo-12%, okuyisilinganiso esiphakathi - ngama-36%. Ukukhula okunjalo akubhekwa njengokubalulekile ngokomtholampilo futhi akudingi ushintsho kumthamo;
- kwabesifazane, ukusebenza kahle kwezidakamizwa kuphezulu kancane kunakubesilisa;
- kwizifo zikashukela ezikhuluphele, umphumela wezidakamizwa mubi kakhulu.
Izinkomba zokuqokwa
IDapagliflozin ihloselwe abanesifo sikashukela sohlobo 2. Izidingo eziphoqelekile - ukwehla kwenani lama-carbohydrate ekudleni, umsebenzi ojwayelekile womzimba wokuqina okuphakathi.
Ngokusho kwemiyalo, umuthi ungasetshenziswa:
- Njengoba i-monotherapy. Ngokusho kodokotela, ukuqokwa kukaForigi kuphela kwenziwa kakhulu.
- Ngaphezu kwe-metformin, uma inganikeli ukwehla okwanele kweshukela, futhi azikho izinkomba zokuqokwa kwamacwecwe akhuthaza ukwenziwa kwe-insulin.
- Njengengxenye yokwelashwa okuphelele ukwenza ngcono isinxephezelo sikashukela.
Contraindication
Uhlu lwe-contraindication ekwelapheni nge-Dapagliflozin ngokusho komkhiqizi:
| Amaqembu esifo sikashukela | Isizathu sokuvinjelwa |
| Hypersensitivity to the drug, lactose ukungabekezeleli. | Ukuphendula kohlobo lwe-anaphylactic kungenzeka. Ngaphezu kwe-Dapagliflozin, i-Forsigi iqukethe i-lactose, i-silicon dioxide, iselula, kanye nodayi. |
| I-ketoacidosis. | Lokhu kwephula umthetho kudinga ukuqedwa kwanoma imaphi amaphilisi anciphisa ushukela kanye nokuguqukela ekwelashweni kwe-insulin kuze kube yilapho isimo sizinza. |
| Ukwehluleka kwangempela | Kusukela esigabeni esiphakathi (i-GFR <60), ukukhuphuka kwengcindezi ezinsweni kuyinto engathandeki. |
| Ukukhulelwa, HB, iminyaka yezingane. | Umenzi akanayo imininingwane ngokuphepha komuthi kulawa maqembu ezinesifo sikashukela, ngakho-ke umyalo wenqabela ukuwuthatha. |
| Ukwemukelwa kwe-loop diuretics. | Ukusetshenziswa okuhlanganisiwe kuthuthukisa i-diuresis, kungaholela ekuphepheni komzimba nokwehla kwengcindezi. |
| Isifo sikashukela esidala kuneminyaka engama-75. | Umuthi okuleli qembu uvame ukubanga imiphumela emibi. Kunesizathu sokukholelwa ukuthi i-Dapagliflozin izosuswa ngokudlulele futhi ingasebenzi kahle ekwehliseni ushukela ngenxa yokulimazeka ngokomzimba komsebenzi wezinso. |
| 1 uhlobo lwesifo sikashukela. | Ingozi ye-hypoglycemia enzima, ukungakwazi ukubala umthamo owanele we-insulin. |
Ukukhetha umthamo
Umthamo ojwayelekile wansuku zonke we-Dapagliflozin ngu-10 mg. Kunqunyelwe uma ukwelashwa kunqunywa kuphela nalesi sidakamizwa, noma ngokuhlanganiswa neMetformin. Umthamo wokuqala we-metformin ngu-500 mg, khona-ke uyandiswa kuze kube yilapho kunxephezelwa ushukela. Umthamo we-Dapagliflozin lapho usetshenziswa namanye amaphilisi we-antidiabetic unqunywa ngudokotela oya khona. Ngokusho kokubuyekezwa, zonke iziguli zinqunywe i-10 mg ye-Dapagliflozin, futhi ushukela wegazi ulawulwa ngokushintsha imithamo yamanye amaphilisi.
Ekwehlulekeni kwesibindi okunzima, imiyalo yokusebenzisa itusa ukunciphisa isilinganiso somuthi kuya ku-5 mg. Ukwehluleka kwezinso okuncane akudingi ukulungiswa komthamo, ngokuphulwa okungathi sína, umuthi uvunyelwe.
Umuthi udakwa kanye ngosuku, kungakhathalekile isikhathi nesikhathi okwakhiwa ngaso.
Umphumela Omubi we-Dapagliflozin
Ukwelashwa nge-Dapagliflozin, njenganoma yisiphi esinye isidakamizwa, kuhlotshaniswa nengozi ethile yemiphumela emibi. Ngokuvamile, iphrofayili yokuphepha kwezidakamizwa ilinganiswe njengethandekayo. Uhlu lwemiyalo yonke imiphumela kungenzeka, imvamisa yabo kunqunywa:
- Ukutheleleka nge-genitourinary kungumphumela othize we-Dapagliflosin nama-analogues ayo. Kuhlobene ngqo nomgomo wokusebenza kwomuthi - ukukhishwa kwe-glucose kumchamo. Ingozi yezifo ilinganiselwa ku-5.7%, eqenjini elilawulayo - 3.7%. Ngokuvamile, izinkinga zenzeka kubantu besifazane ekuqaleni kokwelashwa. Izifo eziningi zazinobunzima obukhulu futhi zingaqedi kahle ngezindlela ezijwayelekile. Amathuba we-pyelonephritis awukhulisi umuthi.
- Ngaphansi kwe-10% yeziguli, umthamo womchamo uyakhuphuka. Ukukhula okumaphakathi kungama-375 ml. Ukungasebenzi kwe-Urinary akuvamile.
- Ngaphansi kwe-1% yabanesifo sikashukela ababone ukuqunjelwa, izinhlungu emuva, ukujuluka. Ingozi efanayo yokwandisa i-creatinine noma i-urea egazini.
Ukubuyekezwa mayelana nomuthi
Ama-Endocrinologists ngamathuba we-Dapagliflozin aphendula kahle, abaningi bathi umthamo ojwayelekile ukuvumela ukuthi unciphise i-glycated hemoglobin nge-1% noma ngaphezulu. Ukuntuleka kwemithi bacubungula isikhathi esifushane sokusetshenziswa kwaso, inani elincane lezifundo zangemva kokumaketha. I-Forsigu icishe ingabekwa njengomuthi kuphela. Odokotela bakhetha i-metformin, glimepiride ne-gliclazide, ngoba le mishanguzo ayibizi, ifundwe kahle futhi iqeda ukuphazamiseka kwengqondo okuphathelene nesifo sikashukela i-mellitus, futhi hhayi nje ukususa ushukela, njenge-Forsyga.
Isifo sikashukela futhi asigcini ngokuthatha umuthi omusha, ngokwesaba ukutheleleka ngegciwane le-genitourinary sphere. Ingozi yalezi zifo sikashukela iphakeme. Abesifazane baqaphela ukuthi ngokwanda kwesifo sikashukela, inani le-vaginitis ne-cystitis liyakhuphuka, futhi besaba ukuthuthukisa ukubukeka kwabo ne-Dapagliflozin. Okubaluleke kakhulu ezigulini inani lentengo eliphakeme le-Forsigi kanye nokuntuleka kwama-analogues ashibhile.
