Amathebulethi e-Yanumet ohlobo 2 sikashukela

Amathebhulethi aseYanumet okusetshenziselwa kuwo abhekisela emithini ye-hypoglycemic esetshenziselwa ukunxenxa isifo sikashukela sohlobo 2. Ukusebenza kwawo kuqiniswa ukwakheka okuhlukile komkhiqizo. Ngabe ilungele bani nokuthi ungayisebenzisa kanjani ngokufanele?

Imvamisa kunqunywa uma ukuguqulwa kwendlela yokuphila ne-monotherapy yangaphambilini ye-metotherin noma ukwelashwa okuyinkimbinkimbi akuzange kulethe imiphumela elindelekile. Kwesinye isikhathi kubhekelwa kubantu abazibandakanya nezemidlalo ukuze balawule iphrofayili yabo ye-glycemic. Ngaphezu kokujwayelana okuningiliziwe nemiyalo, ngaphambi kokusetshenziswa esimweni ngasinye, ukubonisana nodokotela kuyimpoqo.

I-Yanumet: ukwakheka nezimpawu

Isithako esisebenzayo esiyisisekelo kwifomula yi-metformin hydrochloride. Umuthi ufakelwe ku-500 mg, 850 mg noma ku-1000 mg kuthebhulethi eyi-1. I-Sitagliptin isiza isithako esiyinhloko, kwikhophu eyodwa kuzoba ngu-50 mg kunoma yiliphi ithamo le-metformin. Kukhona okutholwayo kwifomula engeyona inzalo ngokuya ngamakhono okwelapha.

Amaphilisi we-convex we-Elatedated avikelekile kumafakethi ngombhalo "575", "515" noma "577", ngokuya ngomthamo. Iphakheji ngalinye lekhadibhodi liqukethe amapuleti amabili noma amane ezincezu eziyi-14. Umuthi kadokotela uyachithwa.

Ibhokisi libuye likhombisa impilo yeshelufu yemithi - iminyaka emi-2. Umuthi ophelelwe yisikhathi kumele ulahlwe. Izidingo zezimo zesitoreji zisezingeni elifanele: indawo eyomile ayifinyeleleki elangeni kanye nezingane ezinokushisa okufika ku-25 degrees.

Amathuba wemithi

I-Yanumet iyinhlanganisela ecatshangelwe yemithi emibili eyehlisa ushukela enezimpawu ezihambisanayo (ezihambisanayo): i-metformin hydrochloride, okuyiqembu lama-Biguanides, kanye nesgliptin, i-inhibitor ye-DPP-4.

I-Synagliptin

Ingxenye yenzelwe ukusetshenziswa komlomo. Indlela yokusebenza ye-sitagliptin isuselwa ekuvuseleleni kwama-incretins. Lapho i-DPP-4 ivinjelwe, izinga le-GLP-1 ne-HIP peptides, elilawula i-glucose homeostasis, liyanda. Uma ukusebenza kwayo kujwayelekile, ama -retretin enza kusebenze ukukhiqizwa kwe-insulin kusetshenziswa β-cell. I-GLP-1 nayo ivimbela ukukhiqizwa kwe-glucagon ngama-cy-cell esibindi. Le algorithm ayifani nomgomo wokuchayeka emithini yeklasi ye-sulfonylurea (SM) ekhulisa ukukhiqizwa kwe-insulin kunoma yiliphi izinga le-glucose.

Umsebenzi onjalo ungadala i-hypoglycemia hhayi kuma-diabetes kuphela, kodwa futhi nakwivolontiya elinempilo.

I-DPP-4 enzyme inhibitor kwimithamo enconyiwe ayivimbi umsebenzi wama-enzyme we-PPP-8 noma PPP-9. Ku-pharmacology, i-sitagliptin ayifani ne-analogues yayo: I-GLP-1, insulin, i-SM derivatives, i-meglitinide, i-biguanides, i-α-glycosidase inhibitors, i-γ-receptor agonists, i-amylin.

I-Metformin

Ngenxa ye-metformin, ukubekezelela ushukela ohlotsheni 2 sikashukela kuyanda: ukugxilisa ingqondo kwabo kuyancipha (kokubini kwe-postprandial ne-basal), ukumelana kwe-insulin kunciphisa. I-algorithm yomphumela wesidakamizwa ihlukile kuzinkambiso zomsebenzi wamanye amakhambi okwehlisa ushukela. Ukuvimbela ukukhiqizwa kwe-glucogen yisibindi, i-metformin yehlisa ukungena kwayo ngezindonga zamathumbu, inciphise ukumelana ne-insulin, ithuthukise ukuthathwa kwe-peripheral.

Ngokungafani nezidakamizwa ze-SM, i-metformin ayivusi ukuhlaselwa kwe-hyperinsulinemia ne-hypoglycemia noma kwabanesifo sikashukela abanesifo sohlobo 2, noma eqenjini elilawulayo. Ngesikhathi sokwelashwa nge-metformin, ukukhiqizwa kwe-insulin kuhlala kwelinye izinga elifanayo, kepha ukushesha kwalo kanye namazinga wansuku zonke kuvame ukuncipha.

Izici ze-Pharmacokinetic

Umuthi ohlanganisiwe uYanumen une-bioequivalent ekutholeni okuhlukile komthamo owanele weJanuvia neMetformin.

Ukuhlelwa

I-bioavailability ye-sitagliptin ingama-87%. Ukusetshenziswa okufanayo kokudla okunamafutha nangama-khalori amaningi akuthinti isilinganiso sokutholwa. Izinga eliphakeme lesithako egazini liqondiswa emahoreni angama-1-4 ngemuva kokutholwa emgudwini we-gastrointestinal.

I-bioavailability ye-metformin esiswini esingenalutho ifinyelela ku-60% ku-500 mg. Ngomthamo owodwa wemithamo emikhulu (kufika ku-2550 mg), umgomo wokulingana wephulwa, ngenxa yokufakwa kancane. IMetformin iqala ukusebenza ngemuva kwamahora amabili nesigamu. Izinga layo lifinyelela ku-60%. Izinga eliphakeme le-metformin liqoshwa ngemuva kosuku noma ezimbili. Ngesikhathi sokudla, ukusebenza kahle komuthi kuyancipha.

Ukusatshalaliswa

Umthamo wokusatshalaliswa kwe-sinagliptin ngokusetshenziswa okukodwa kwe-1 mg yeqembu lokulawula lababambe iqhaza kulolu cwaningo kwakungu-198 l. Izinga lokubopha kumaprotheni egazi lincane - 38%.

Ekuhlolweni okufanayo ne-metformin, iqembu elilawulayo lanikezwa umuthi ngenani lama-850 mg, ivolumu yokusabalalisa ngasikhathi sinye yaba yisilinganiso samalitha angama-506.

Uma siqhathanisa nezidakamizwa zekilasi le-SM, i-metformin empeleni ayibophele amaprotheni, okwesikhashana ingxenye encane yayo itholakala kumaseli abomvu egazi.

Uma uthatha umuthi ngendlela evamile, umuthi ufinyelela ezingeni elifanele (<1 μg / ml) egazini ngosuku noma ezimbili. Ngokwemiphumela yokuhlolwa, noma ngokuya ngemikhawulo evamile, inani eliphakeme lokuqukethwe kwezidakamizwa egazini alizange lidlule ku-5 μg / ml.

Isiphetho

Kufika ku-80% wezidakamizwa ezidonswa yizinso, i-metformin ayenziwa umzimba emzimbeni, eqenjini lokulawula cishe yonke ingxenye esele kwesimo sayo sokuqala ngosuku. I-Hepatic metabolism kanye ne-excretion ku-ducts ye-bile ayikho ngokuphelele. ISinagliptin ikhishwa ngendlela efanayo (kufinyelela ku-79%) nge-metabolism encane. Uma kwenzeka ezinkingeni zezinso, kumele kuchazwe umthamo weYanumet. Ngama-pathologies e-hepatic, izimo ezikhethekile zokwelashwa azidingeki.

I-Pharmacokinetics yezigaba ezikhethekile zeziguli

1. Isifo sikashukela esinesifo sohlobo 2. Indlela yokufakwa kanye nokusatshalaliswa kwe-sitagliptin iyefana nezinqubo emzimbeni onempilo. Uma izinso zivamile, umehluko kumingcele ye-pharmacokinetic lapho kusetshenziswa imithamo emibili ye-metformin ku-diabetesics kanye namavolontiya anempilo awabonwa. Ukuqedwa kwesidakamizwa ngokuhambisana nezinqubo akulungisiwe.
2. Ngokuhluleka kwezinso, iJanumet ayinqunyelwe, ngoba umuthi ucishe ucishwe ngokuphelele yizinso, okwenza umthwalo ophindwe kabili kuleso sitho esibaluleke kangaka.
3. Kwi-pathologies yesibindi yobuchopho obukhulu nobulinganiselayo, umthamo owodwa we-sitagliptin awuzange uveze umehluko omkhulu ekutholweni nasekuhanjisweni. Akukho datha emiphumeleni yokuphuza umuthi wezifo ezinzima zesibindi, kodwa ukubikezela kuleli cala akukuhle. Ngokusho kwe-metformin, imiphumela yokuhlolwa okufanayo ayizange ishicilelwe.
4. Izazi zesifo sikashukela sokudala. Ukwehluka okuhlobene nobudala kuhlobene nokungasebenzi kahle kwinso, ngemuva kweminyaka engama-80, akuboniswanga uJanumet (ngaphandle kwabanesifo sikashukela ngokuvunyelwa okujwayelekile kwe-cretatinin).

Kuboniswa bani futhi kabukhonjiswanga kuYanumet

Umuthi wenzelwe ukulawula isifo sikashukela sohlobo 2. Kunqunywe emacaleni athile.

1. Njengokwengezwa kokuguqulwa kwendlela yokuphila ukuze kuthuthukiswe iphrofayili ye-glycemic yesifo sikashukela, uma i-metformin monotherapy inganikeli mphumela we-100%.
2. I-Yanumet isetshenziswa ekwelapheni inhlanganisela nokutholakala kwe-SM, uma ukhetho "umuthi we-metformin + weqembu le-SM + ukudla okuphansi kwe-carb nomthwalo wemisipha" belungasebenzi ngokwanele.
3. Umuthi uhlanganiswe, uma kunesidingo, nama-gamma receptor agonists.
4. Uma imijovo ye-insulin inganikeli isinxephezelo esiphelele sikashukela, i-Yanumet inqunywe ngokufana.

Ukuxhumana phakathi kwemiyalo kungokulandelayo:

• Hypersensitivity kuzithako zefomula;
• I-Coma (isifo sikashukela);
• I-Pathology yezinso;
• Izifo ezithathelwanayo;
• Ukufakwa kwezidakamizwa nge-iodine (iv);
• Izimo ezishaqisayo;
• Izifo ezidala ukuntuleka komoya-mpilo kwezicubu;
• Ukungasebenzi kwesibindi, ubuthi, ukusetshenziswa kabi kotshwala;
• Ukuncelisa;
• Thayipha isifo sikashukela sokuqala.

Imiphumela emibi

Ngaphambi kokusebenzisa, udinga ukutadisha uhlu lwemiphumela emibi nezimpawu zazo ukuze wazise udokotela ngesikhathi mayelana nokusabela komzimba ukulungisa inqubo yokwelashwa. Phakathi kwemiphumela ejwayelekile engafuneki:

• Ukukhwehlela iziphonso;
• Ukuphazamiseka kwe-dyspeptic;
• Ubuhlungu bekhanda njenge-migraine;
• Ukuphazamiseka kwesigqi sokuhamba kwamathumbu;
• Izifo zamapheshana wokuphefumula;
• Ukwehla kwekhwalithi yokulala;
• Ukwanda kwe-pancreatitis namanye ama-pathologies we-pancreas;
• Ukuvuvukala;
• Ukwehla kwesisindo, i-anorexia;
• Ukutheleleka kwesikhunta esikhunjeni.

Izehlakalo zemiphumela emibi zingalinganiswa ngesilinganiso se-WHO:

• Kaningi (> 1 / 0,1);
• Imvamisa (> 0.001, <0.1);
• Kaningi (> 0.001, <0.01).

Imininingwane yezibalo zezokwelapha yethulwe etafuleni.

Ungasifaka kanjani isicelo

Isandulelo "sahlangana" egameni lomuthi sikhombisa ubukhona be-metformin ekwakhiweni kwayo, kepha umuthi uphathwa ngendlela efanayo nalapho kunqunywa uJanuvia, umuthi osuselwe ku-sitagliptin ngaphandle kwe-metformin.

Udokotela ubala umthamo, aphuze amaphilisi ekuseni nakusihlwa ngokudla.

Kwezinye izimo, umuntu kufanele aqaphele kakhulu ekwelapheni kweYanumet.

1. I-pancreatitis ye-acute. ISitagliptin iyakwazi ukuthuthukisa izimpawu zayo. Udokotela kufanele axwayise isiguli: uma kukhona izinhlungu esiswini noma i-hypochondrium yangakwesokudla, kufanele uyeke ukuthatha umuthi lowo.
2. I-Lactic acidosis. Lesi simo esingathi sína futhi esingajwayelekile kangako siyingozi ngemiphumela ebulalayo, futhi ukwelashwa kuyaphazamiseka lapho kuvela izimpawu. Ingabonakala ngokufushane komoya, nobuhlungu be-epigastric, ukubanda, ushintsho ekwakhekeni kwegazi, imisipha yemisipha, i-asthenia, nokuphazamiseka kwendlela yokuhamba kwesisu.
3. I-Hypoglycemia Ngaphansi kwezimo ezijwayelekile, uma kuqhathaniswa nesizinda seYanumet, asikhuli. Kungacasulwa ukuzikhandla ngokweqile komzimba, i-calorie ephansi (kuze kufike ku-1000 kcal / ngosuku), izinkinga ngezindlala ze-adrenal kanye ne-pituitary gland, udakwa, nokusetshenziswa kwe-β-blockers. Kwandisa amathuba okuba ne-hypoglycemia ekwelapheni okufanayo ne-insulin.
4. Izifo zezitho zomzimba. Ingozi yokuthola i-lactic acidosis inyuka ngesifo sezinso, ngakho-ke kubaluleke kakhulu ukubheka i-creatinine. Lokhu kuyiqiniso ikakhulukazi kwabanesifo sikashukela esivuthiwe, ngoba ukuphazamiseka kwabo ngokwezinso kungenzeka kube yi-asymptomatic.
5. I-Hypersensitivity. Uma umzimba uhlangana nezimpawu zokwaliwa, umuthi uyakhanselwa.
6. Ukungenelela kokuhlinzwa. Uma isifo sikashukela sisebenza ngokuhlinzwa okuhleliwe, ezinsukwini ezimbili ngaphambi kwaso, uJanumet uyakhanselwa bese isiguli sidluliselwa ku-insulin.
7. Imikhiqizo equkethe i-iodine. Uma i-ejenti esekwe iodine ingeniswa ngeYanumet, lokhu kungavusa isifo sezinso.

Umphumela weYanumet kwabesifazane abakhulelwe wafundwa kuphela kubameli bezilwane zezilwane. Kwabesifazane abakhulelwe, ukuphazamiseka kokukhula kwengane akuzange kubhalwe phansi lapho kuthathwa i-metformin. Kepha iziphetho ezinje azanele ukunquma umuthi kwabesifazane abakhulelwe. Shintshela ku-insulin esigabeni sokuhlela ukukhulelwa.

IMetformin ibuye idlulele obisini lwebele, ngakho-ke, iJanumet ayinqunyelwe ukukhishwa kwesibeletho.

I-Metformin ayiphazamisi izimoto zokushayela noma izindlela eziyinkimbinkimbi, futhi i-sinagliptin ingadala ubuthakathaka kanye nokubola, ngakho-ke, iJanuvia ayisetshenziswanga uma ukusabela okusheshayo kanye nokunaka okukhulu kokudingeka kuyadingeka.

Imiphumela yokweqisa kwemithi

Ukugwema ukweqisa kwe-metformin, awukwazi ukuyisebenzisa ngaphezu kweYanumet. I-drug overdose iyingozi nge-lactic acidosis, ikakhulukazi ngokweqile kwe-metformin. Lapho kuvela izimpawu zokweqisa kwezezidakamizwa, kusetshenziswa ukwelashwa okubonisa izimpawu ezidambisa ukudakwa.

Kungani uthuthukisa ama-Metformin complexes ne-Yanuvia, Galvus, Onglyza, Glybyuryd, uma ungasebenzisa amathuluzi afanayo ekwelapheni okuyinkimbinkimbi ngokuhlukile? Ukuhlolwa kwesayensi kukhombisile ukuthi nganoma yiluphi uhlobo lwesikimu sokulawula isifo sikashukela sohlobo 2, iMetformin ikhona (noma ngabe ishintshela ku-insulin). Ngaphezu kwalokho, lapho usebenzisa izinto ezimbili ezisebenzayo ngomshini ohlukile wokusebenza, ukusebenza kahle kwezidakamizwa kuyanda futhi ungakwenza ngamaphilisi ngomthamo ophansi.

Kubalulekile kuphela ukulawula umthamo we-metformin ephaketheni (500 mg, 850 mg noma we-1000 mg) ukuze ugweme izimpawu zokugcwala ngokweqile. Ezigulini ezikhohlwa ukuphuza zonke izinhlobo zephilisi ngesikhathi, ithuba lokuthatha konke elikudingayo ngasikhathi sinye inzuzo enhle ethinta kakhulu ukuphepha nemiphumela yokwelashwa.

Ukusebenzelana kwezidakamizwa

Amathuba we-metformin ancishiswa ama-diuretics, i-glucagon, ama-corticosteroids, ama-hormone we-thyroid, ama-phenothiazines, izindlela zokuvimbela inzalo zomlomo ezibhebheni, i-phenytoin, i-nicotinic acid, i-audiathomimetics, i-calcium antagonists, isoniazid. Kokuhlolwa, umthamo owodwa we-nifedipine wandise ukumuncwa kwe-metformin kubahlanganyeli abanempilo ocwaningweni, isikhathi sokufika ezingeni lokuphakama kanti nengxenye yempilo yahlala ifana.

Izici ze-hypoglycemic zizothuthukiswa yi-insulin, izidakamizwa zeqembu le-sulfonylurea, i-acarbose, i-MAO ne-ACE inhibitors, ama-NSAIDs, ama-oxytetracycline, ama-clofibrate derivatives, cyclophosphamide, β-blockers. Ukusetshenziswa okukodwa kwe-furosemide ngabahlanganyeli abanempilo ekuhlolweni kukhuphule ukumuncwa nokusatshalaliswa kwe-metformin ngo-22% no-15%, ngokulandelana. Amanani wokuqalwa kwezinso awashintshanga kangako. Akunamininingwane yokwelashwa okuhlala isikhathi eside okuhlanganisiwe nge-furosemide ne-metformin.

Imithi esetshenziselwa ukuvikela izithambiso zezokuthutha, ngakho-ke uma isetshenziswa isikhathi eside ingakhuphula izinga lokuqina le-metformin ngo-60%.

I-Cimetidine ivimbela ukumbiwa kwe-metformin, ukunqwabelana kwezidakamizwa egazini kungakhipha i-acidosis.

I-Yanumet nayo ayihambisani notshwala, nayo ekhulisa amathuba we-acidosis.

Lapho sifunda ukusabela kwemithi kwamanye amaqembu (i-metformin, i-simvastatin, i-glibenclamide, i-warfarin, i-rosiglitazone, inzalo), i-sinagliptin yayingasebenzi kakhulu. Ukuqoqwa kwe-plasma kwe-digoxin kukhuphuke ngo-18% lapho kuthathwa kanyekanye ne-sitagliptin.

Ukuhlaziywa kwemiphumela yabahlanganyeli abanempilo abangama-858 ocwaningweni abathathe izinhlobo ezingama-83 zemithi ehambisanayo, u-50% wayo owachitha izinso, awubanga nomthelela obonakalayo ekufakweni nasekuhanjisweni kwe-sitagliptin.

Analogs kanye namanani

I-Yanumet iwumuthi obiza kakhulu: ngokwesilinganiso, inani entweni ekhemisi lisuka ema-ruble amabili nengxenye liye ezinkulungwaneni ezintathu ngebhokisi ngamapuleti we-1-7 (amaphilisi ayi-14 ku-blister eyodwa). Bakhiqiza umuthi wokuqala eSpain, eSwitzerland, eNetherlands, e-USA, ePuerto Rico. Phakathi kokufana, i-Velmetia kuphela efanele ngokuphelele ukwakheka. Ukusebenza kanye nekhodi yemithi ye-ATC kuyafana:

• I-Douglimax;
• I-Glibomet;
• I-Tripride;
• Avandamet.

I-Glibomet ifaka i-metformin ne-glibenclamide, eyinikeza ngamakhono we-hypoglycemic kanye ne-hypolipidemic.Izinkomba zokusetshenziswa ziyafana nezincomo zeYanumet. I-Douglimax isuselwe kwi-metformin ne-glimepiride. Indlela yokuvezwa nezinkomba ifana kakhulu neYanumet. I-Tripride ine-glimepiride ne-pioglitazone, enomphumela we-antidiabetesic kanye nezinkomba ezifanayo. I-Avandamet, okuyinhlanganisela ye-metformin + rosiglitazone, nayo inezakhiwo ze-hypoglycemic.

Uma uYanumet engafanele

Izizathu zokubuyisela umuthi zingahluka: kwabanye, umuthi umane awusizi ngezinga elifanele, kwabanye ubangela umphumela ophikelelayo noma umane ungasakwazi ukuwubiza.

Lapho ukusetshenziswa komuthi kungahlanganisi ngokuphelele ushukela, kuthathelwa indawo imijovo ye-insulin. Amanye amaphilisi kuleli cala awasebenzi. Okungenzeka ukuthi, kusukela ekwelashweni kwezidakamizwa okunolaka, ama-pancreas ayesebenza, futhi uhlobo oluphambili lwesifo sikashukela sohlobo 2 lwedlulisela kuhlobo 1 sikashukela.

Ngisho namaphilisi wesimanje kakhulu ngeke asebenze uma ungazinaki izincomo ze-endocrinologist ngokudla okuphansi kwe-carb nemithwalo ebekiwe.

Imiphumela emibi ivame ukucasulwa yi-metformin, i-sitagliptin kulokhu ayinangozi. Ngokwamandla ayo ekhemisi, iMetformin ingumuthi oyingqayizivele, ngaphambi kokuyifunela enye, kufanelekile ukwenza imizamo ephezulu yokuvumelana nezimo. Ukuphazamiseka kwe-dyspeptic kuzodlula isikhathi, futhi i-metformin izogcina ushukela uvamile ngaphandle kokubhubhisa ama-pancreas nezinso. Imiphumela emincane engathandeki inikezwa ngokuthatha uJanumet hhayi ngaphambi noma ngemuva kokudla, kodwa ngesikhathi sokudla.

Ukuze wonge imali, ungafaka uJanumet noma uJanuvia kuphela nge-metformin emsulwa. Kwinethiwekhi yamakhemisi, kungcono ukhethe uphawu lweGlyukofazh noma lweSiofor esikhundleni sabakhiqizi basekhaya.

Isifo sikashukela nodokotela ngeYanumet

Mayelana nomuthi uJanumet, ukubuyekezwa kodokotela kuyavumelana. Odokotela bathi: inzuzo ebalulekile yezakhi zayo (ikakhulukazi i-sitagliptin) ukuthi azikhuphi i-hypoglycemia. Uma ungaphuli ngokweqile irejimeni ebekiwe bese ulandela izincomo zokudla okunempilo nokwakha umzimba, izinkomba zamamitha zizobe ziphansi kakhulu. Uma kunokungakhululeki ku-epigastrium neminye imiphumela engathandeki, kubalulekile ukuhlukanisa umthamo wansuku zonke emithanjeni emi-2 ukunciphisa umthwalo emzimbeni. Ngemuva kokuzivumelanisa nezimo, ungaphindela embusweni wangaphambilini, uma ushukela uphakeme kunamanani okuhlosiwe, ukulungiswa kwamthamo ngudokotela obonakalayo kungenzeka.

Mayelana neYanumet, ukubuyekezwa kweziguli kuyimpikiswano, ngoba lesi sifo kuwo wonke umuntu sihlukile. Ngaphezu kwakho konke, iziguli ezindala zikhononda ngemiphumela emibi, ngoba izinso, nomzimba wonke, sezivele zincishiswa yizifo ezihambisana nawo.

I-Endocrinologists inesaga esithandwayo: "Ezemidlalo nokudla - ukugoma ukulwa noshukela." Noma ngubani ofuna iphilisi eliyisimangaliso, futhi akholelwe ngokuqinile ukuthi amaphilisi amasha, elinye iphakethe lokuphromotha noma itiye le-herbal lizoselapha unomphela isifo sikashukela ngaphandle komzamo omkhulu, kufanele akhumbule njalo.