I-TRAGENT - IMIYALO ESETSHENZISWAYO, INTENGO, UKUBUYEKEZWA KANYE NAMA-ANALOGUES

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I-Trazhenta (igama lomhlaba wonke elithi Trajenta) yisigaba esisha semithi ye-antidiabetesic. Ama-inhibitors e-DPP-4 anendlela yomlomo yokuphatha asetshenziswe ngempumelelo ukulawula isifo sikashukela sohlobo 2; isisekelo esikhulu sobufakazi siqongelelwe ukusebenza kwawo ngempumelelo.

Isakhi esisebenzayo somuthi yi-linagliptin. Okunconywe kakhulu ngezinzuzo zayo abakwa-diabetes onesifo sezinso, ngoba umuthi awunawo umthwalo owengeziwe kubo.

I-Trazhenta - ukwakheka nefomu lomthamo

Abakhiqizi, i-BOEHRINGER INGELHEIM PHARMA (Germany) ne-BOEHRINGER INGELHEIM ROXANE (USA), bakhipha umuthi ngendlela yamacwecwe abomvu ejikelezayo. Isimboli somenzi esivikela umuthi ezifuyweni sibhalwe ngakolunye uhlangothi, bese kuthi uphawu lwe-“D5” lubhalwe kolunye.

Ngayinye yayo iqukethe i-5 mg yesithako esisebenzayo se-linagliptin kanye nezinye izihlungi ezifana nesitashi, udayi, i-hypromellose, i-magnesium stearate, i-copovidone, i-macrogol.

I-aluminium blister ngayinye ipakisha amaphilisi ayi-7 noma ayi-10 wesidakamizwa iTrazhenta, isithombe saso esingabonakala kulesi sigaba. Ebhokisini bangaba inombolo ehlukile - kusuka kumapuleti amabili kuya kwayisishiyagalombili. Uma ngabe kunamaseli ayi-10 anamathebhulethi ku-blister, kuzoba khona amapuleti amathathu ebhokisini.

Ikhemisi

Amathuba wesidakamizwa atholakala ngempumelelo ngenxa yokuvinjwa komsebenzi we-dipeptidyl peptidase (DPP-4). Le enzyme iyabhubhisa

kuma-HIP we-hormonal kanye ne-GLP-1, edlala indima enkulu ekugcineni i-glucose ibhalansi. Ama-incretins athuthukisa ukukhiqizwa kwe-insulin, asiza ukulawula i-glycemia, futhi avimbele ukucasheka kwe-glucagon. Umsebenzi wabo uphila isikhashana; kamuva, i-HIP ne-GLP-1 zidiliza ama-enzyme. I-Trazhenta ihlotshaniswa kabusha ne-DPP-4, lokhu kukuvumela ukuthi ulondoloze impilo yama-incretins futhi ukwenyuse izinga labo lokusebenza kahle.

Indlela yethonya leTrazhenty ifana nemigomo yokusebenza kwamanye ama-analogues - uJanuvius, uGalvus, u-Ongliza. I-HIP ne-GLP-1 kukhiqizwa lapho izakhamzimba zingena emzimbeni. Ukusebenza kahle kwesidakamizwa akuhlotshaniswa nokukhuthaza ukukhiqizwa kwawo, umuthi umane wandisa isikhathi sokuvezwa kwawo. Ngenxa yalezi zimpawu, iTrazhenta, njengamanye ama-incretinomimetics, ayicasuli ukuthuthukiswa kwe-hypoglycemia futhi lokhu kuyinzuzo enkulu ngaphezu kwezinye izigaba zemithi ye-hypoglycemic.

Uma izinga likashukela lingangeqi ngokweqile, ama-insretin asiza ukukhuphula ukukhiqizwa kwe-insulin endulin ngama-β-cell. I-hormone i-GLP-1, enohlu olubaluleke kakhulu lwamathuba ngokuqhathaniswa ne-GUI, ivimba ukwakheka kwe-glucagon kumaseli wesibindi. Zonke lezi zinqubo zisiza ukugcina kahle i-glycemia isezingeni elifanele - ukunciphisa i-glycosylated hemoglobin, ushukela osheshayo kanye namazinga kashukela ngemuva kokuzivocavoca isikhathi sokuphumula amahora amabili. Ekwelashweni okuyinkimbinkimbi nge-metformin kanye ne-sulfonylurea amalungiselelo, amapharamitha we-glycemic ayathuthuka ngaphandle kokuthola isisindo esibucayi.

Kubalulekile ukuthi i-linagliptin ingakhuphi ubungozi bethambo nenhliziyo (amathuba wokuhlaselwa yinhliziyo ngomphumela obulalayo).

I-Pharmacokinetics

Ngemuva kokungena emgodini wokugaya ukudla, umuthi udonswa ngokushesha, i-Cmax ibonwa ngemuva kwehora nesigamu. Ukuhlushwa kwehla ngezigaba ezimbili.

Ukusetshenziswa kwamathebulethi ngokudla noma ngokwehlukana kuma-pharmacokinetics wesidakamizwa akuthinti. I-bioavailability yesidakamizwa ingafika kuma-30%. Amaphesenti amancane ancishisiwe, ama-5% akhishwe yizinso, angama-85% athulwe indle. Noma yikuphi i-pathology yezinso akudingi ukuhoxiswa kwezidakamizwa noma ukuguqulwa komthamo. Izici ze-pharmacokinetics ebuntwaneni azizange zifundwe.

Ubani umuthi

I-Trazent ichazwa njengomuthi womugqa wokuqala noma uhlangana neminye imithi yokwehlisa ushukela.

I-Monotherapy. Uma umuntu onesifo sikashukela engazibekezeleli izidakamizwa zesigaba se-bigudins ezifana ne-metformin (ngokwesibonelo, nge-renal pathologies noma ukungabekezelelani komuntu ngamunye kwizakhi zayo), kanye nokuguqulwa kwendlela yokuphila akulethi imiphumela efiselekayo.
Isifunda esiyizingxenye ezimbili. I-Trazent ichazwe kanye namalungiselelo we-sulfonylurea, metformin, thiazolidinediones. Uma isiguli siku-insulin, i-incretinomimetic ingayengezela.
Inketho enezingxenye ezintathu. Uma ama-algorithms okwelashwa wangaphambilini engasebenzi ngokwanele, iTrazhenta ihlanganiswa ne-insulin nohlobo oluthile lomuthi we-antidiabetic ngenqubo ehlukile yokusebenza.

Ongabelwe iTrazhent

ILinagliptin ivunyelwe emikhakheni enjalo yesifo sikashukela:

Uhlobo 1 sikashukela;
I-Ketoacidosis icasulwe yisifo sikashukela;
Ikhulelwe futhi iletha;
Izingane nobusha;
Hypersensitivity kuzithako zefomula.

Ezinsukwini ezi-2 ngaphambi kokuhlinzwa, umuntu onesifo sikashukela udluliswa kusuka kumanxusa omlomo awathole kuyi-insulin, imijovo ikhanselwa ezinsukwini ezi-2 ngemuva kokuhlinzwa ngempumelelo.

Imiphumela engathandeki

Emuva kokuthatha i-linagliptin, imiphumela emibi ingahle ibe khona:

I-Nasopharyngitis (isifo semvelo esithathelwanayo);
Ukukhwehlela iziphonso;
I-Hypersensitivity;
I-pancreatitis
Ukwanda kwe-triglycerol (uma ihlanganiswa nezidakamizwa zekilasi le-sulfonylurea);
Amanani we-LDL andayo (ngokuphathwa kanyekanye kwe-pioglitazone);
Ukukhula kwesisindo somzimba;
Izimpawu ze-Hypoglycemic (ngokumelene nesizinda sokwelashwa kwezingxenye ezimbili nezinthathu).

Imvamisa nenombolo yemiphumela emibi eba khona ngemuva kokudla iTrazhenta iyafana nenani lemiphumela emibi ngemuva kokusebenzisa i-placebo. Imvamisa, imiphumela emibi ibonakaliswa ekwelashweni okuphindwe kathathu kweTrazhenta nge-metformin ne-sulfonylurea.

Umuthi ungadala ukuphazamiseka kokuxhumana, lokhu kubalulekile ukucubungula lapho ushayela izimoto nezinqubo eziyinkimbinkimbi.

Ukweqisa

Ababambe iqhaza banikezwa amaphilisi ayi-120 (600 mg) ngasikhathi. I-overdose eyodwa ayizange ithinte isimo sezempilo samavolontiya avela eqenjini lokulawula elinempilo. Phakathi kwabanesifo sikashukela, amacala okweqa awazange abhalwe izibalo zezokwelapha. Futhi nokho, uma kwenzeka kusetshenziswa ingozi ngamabomu noma ngamabomu imithamo eminingana ngasikhathi sinye, isisulu sidinga ukukuhlanza isisu namathumbu ukuze kususwe ingxenye yemithi enganambitheki, inikeze izangoma nezinye izidakamizwa ngokuya nezimpawu, khombisa udokotela.

Ungawuthatha kanjani umuthi

Ukudepha ngokuhambisana nemiyalo yokusetshenziswa kufanele kuthathwe kathathu ngosuku, 1 ithebhulethi (5 mg). Uma umuthi usetshenziswa ekwelapheni okuyinkimbinkimbi ngokufana ne-metformin, khona-ke umthamo wokugcina ugcinwa.

Abantu abanesifo sikashukela abanokulimala kwe-renal noma i-hepatic abadingi ukulungiswa kwamthamo. Izimo azihlukile ezigulini zobudala ezivuthiwe. E-senile (kusuka eminyakeni engama-80) yobudala, iTrazhent ayinqunyelwe ngenxa yokuntuleka kwesipiliyoni somtholampilo kulesi sigaba sobudala.

Uma isikhathi sokuphuza umuthi sishoda, kufanele uphuze iphilisi ngokushesha okukhulu. Akunakwenzeka ukuphinda okujwayelekile. Ukusetshenziswa kwomuthi akuboshelwe esikhathini sokudla.

Ithonya le-trazhenti ekukhulelweni nasekukhulelwe

Imiphumela yokusetshenziswa kwesidakamizwa ngabesifazane abakhulelwe ayishicilelwa. Kuze kube manje, ucwaningo selwenziwe ezilwaneni kuphela, futhi akukho zimpawu zobuthi bokuzala ezirekhodiwe. Futhi noma kunjalo, ngesikhathi sokukhulelwa, abesifazane abayinikeziwe umuthi.

Ekuhlolweni kwezilwane, kwatholakala ukuthi umuthi uyakwazi ukungena ubisi lukamama lowesifazane. Ngakho-ke, ngesikhathi sokudla kwabesifazane, iTrazhent ayinqunyelwe. Uma isimo sezempilo sidinga ukwelashwa okunjalo, ingane idluliselwa kokudla okungenamsoco.

Ukuhlolwa kwethonya lomuthi ekhonweni lokukhulelwa ingane akwenziwe. Ukuhlolwa okufanayo kwezilwane akuzange kuveze ingozi kulolu hlangothi.

Ukusebenzelana kwezidakamizwa

Ukusetshenziswa kanyekanye kweTrazhenta neMetformin, noma ngabe umthamo wawuphezulu kunokwejwayelekile, akuholelanga umehluko omkhulu kuma-pharmacokinetics wezidakamizwa.

Ukusetshenziswa okufanayo kwePioglitazone nakho akuguquki amandla e-pharmacokinetic yazo zombili lezi zidakamizwa.

Ukwelashwa okuyinkimbinkimbi ne-Glibenclamide akuyona ingozi kuTrazhenta, ngoba eyokugcina, i-Cmax iyancipha kancane (ngo-14%).

Umphumela ofanayo wokusebenzisana uboniswa ezinye izidakamizwa zesigaba se-sulfonylurea.

Ukuhlanganiswa kwe-ritonavir + linagliptin kukhulisa i-Cmax izikhathi ezi-3, ushintsho olunjalo aludingi ukulungiswa komthamo.

Ukuhlanganiswa neRifampicin kuvusa ukwehla kwe-Cmax Trazenti. Ngokwengxenye, izici zokwelashwa zigcinwa, kepha umuthi awusebenzi u-100%.

Akuyona ingozi ukunquma i-Digoxin ngasikhathi sinye ne-lynagliptin: ama-pharmacokinetics ayo womabili la makhambi awashintshi.

I-Trazhent ayithinti amandla e-Varfavin.

Ushintsho oluncane lubonwa ngokusetshenziswa okufanayo kwe-linagliptin ene-simvastatin, kepha i-incretin mimetic ayizithinti kakhulu izici zayo.

Ngokuphikisana nesizinda sokwelashwa neTrazhenta, izindlela zokuvimbela inzalo ngomlomo zingasetshenziswa ngokukhululekile.

Izincomo ezingeziwe

I-Trazent ayinqunyelwe uhlobo lwe-1 yesifo sikashukela ne-ketoacidosis, okuyi-complication yesifo sikashukela.

Ukwanda kwezimo ze-hypoglycemic ngemuva kokwelashwa nge-linagliptin, esetshenziswa njenge-monotherapy, kwanele inani lamacala anjalo nge-placebo.

Ukuhlolwa kwemitholampilo kukhombisile ukuthi imvamisa yokuvela kwe-hypoglycemia lapho usebenzisa iTrezhenta ekwelashweni okuhlanganisiwe ayibhekeki, ngoba isimo esibucayi asibangeli linagliptin, kepha i-metformin nezidakamizwa zeqembu le-thiazolidinedione.

Ukuqapha kufanele kuqashelwe lapho kuqokwa iTrazhenta ngokuhambisana nezidakamizwa zesigaba se-sulfonylurea, ngoba kudala i-hypoglycemia. Ngobungozi obukhulu, kuyadingeka ukulungisa umthamo wemithi yeqembu le-sulfonylurea.

ILinagliptin ayithinti amathuba okuthuthuka kwezifo zenhliziyo nemithambo yegazi.

Ekwelashweni okuhlanganisiwe, iTrazhent ingasetshenziswa ngisho nangomsebenzi oqinile we-renal.

Ezigulini zabantu abadala (ngaphezu kweminyaka engama-70), ukwelashwa kukaTrezenta kubonise imiphumela emihle ye-HbA1c: i-hemoglobin yokuqala ye-glycosylated yayingu-7.8%, owokugcina - u-7.2%.

Umuthi awukhuphi ukwanda kwengozi ye-inhliziyo. Umugqa oyisisekelo obonisa imvamisa nesikhathi sokufika, ukufa kwenhliziyo, unhlangothi, i-angina pectoris engadingi ukwedinga ukulaliswa esibhedlela, abanesifo sikashukela abathathe i-linagliptin babevame kakhulu futhi kamuva kunabazinikeli beqembu elilawulayo abathola izidakamizwa ze-placebo noma zokuqhathanisa.

Kwezinye izimo, ukusetshenziswa kwe-linagliptin kuvuse ukuhlaselwa kwe-pancreatitis e-acute.

Uma kunezimpawu zalokho (ubuhlungu obukhulu ku-epigastrium, ukuphazamiseka kwengqondo, ubuthakathaka obujwayelekile), umuthi kufanele umiswe bese uthintana nodokotela wakho.

Ucwaningo ngethonya leTrazhenta lekhono lokushayela izimoto nezinqubo eziyinkimbinkimbi alwenziwe, kepha ngenxa yokuhlangana okungalungile, thatha umuthi uma kunesidingo, ugxile kakhulu futhi usheshe usabele ngokuqapha.

Ama-analog kanye nezindleko zemithi

Kwe-Trazhenta yezidakamizwa, intengo isukela kuma-ruble ayi-1500-1800 wamathebulethi angama-30 ngomthamo ongu-5 mg. Uyakhishwa umuthi kadokotela.

Izithasiselo zesigaba esifanayo se-DPP-4 inhibitors zifaka i-Januvia esekelwe kwisinagliptin, i-Onglizu ngokusekelwe ku-saxagliptin neGalvus enesakhi esisebenzayo se-vildagliptin. Le mithi ifana nekhodi ye-ATX level 4.

Umphumela ofanayo ukhishwa yizidakamizwa iSitagliptin, i-Alogliptin, iSaksagliptin, iVildagliptin.

Azikho izimo ezikhethekile zokugcinwa kweTrazenti emiyalweni. Iminyaka emithathu (ngokuya ngosuku lokuphelelwa yisikhathi), amaphilisi agcinwa ekushiseni kwegumbi (afinyelela ku-+25 degrees) endaweni emnyama ngaphandle kokutholwa yizingane. Imithi ephelelwe yisikhathi ayikwazi ukusetshenziswa, kumele ichithwe.

Isifo sikashukela nodokotela mayelana neTrazhent

Ukusebenza okuphezulu kweTrazenti ekuhlanganisweni okuhlukahlukene kwaqinisekiswa ngezifundo zamazwe omhlaba kanye nokwenza umsebenzi wezokwelapha. Ama-endocrinologists akhetha ukusebenzisa i-linagliptin njengomuthi wolayini wokuqala noma ekwelashweni okuhlanganisiwe. Ngokuthambekela kwe-hypoglycemia (ukuzikhandla okusindayo ngokomzimba, ukungondleki kahle), esikhundleni somuthi wekilasi we-sulfonylurea, anikezwa abakwaTrazent, kunokubuyekezwa mayelana nokunikezwa komuthi wokumelana ne-insulin nokukhuluphala. Abaningi besifo sikashukela bathola umuthi njengengxenye yokwelashwa okuyinkimbinkimbi, ngakho-ke kunzima ukuhlola ukusebenza kwawo, kepha ngokuvamile, wonke umuntu ujabule ngomphumela.

U-Alina, uRyazan, oneminyaka engama-32 “Sekuphele inyanga ngiphuza iTrazhent. Ngize kulawa mapilisi ngemuva kokuhlolwa isikhathi eside nokungaphumeleli ngempilo. Ngemuva kokubeletha, ngathola isisindo esiningi. Ngemuva kwezinyanga eziyisithupha, isigaxa sami senyongo sasuswa kwaqalwa nokudla. Phambilini, ngabe ngilahlekele ngokushesha emzimbeni ngokudla okunjalo, kepha ngabe sengilulama, yize ingane yami yayingabekezeleleki. Udokotela uphakamise ukuthi ngihlole ushukela. Ngemuva kokuhlolwa kokubekezelela kwe-glucose kwembula ukumelana ne-insulin. Isazi se-endocrinologist sithe ngokuhlaziya okunjalo akusizi ngalutho ukuzihlukumeza ngendlala, waqoka uTrazhent. Kwaphela inyanga, kanye nokudla namaphilisi, ngilahlekelwe ama-4 kg. Lokhu ngumphumela omuhle kimi. Ngakho-ke ngincoma ukuthi noma ngubani onenkinga enkulu ngokweqile aqale ngokuhlolwa, hhayi ngokudla. ”

UTatyana, Belgorod “Umyeni wami wayenenkinga efanayo nesisindo. Ngemuva kwengozi, walala isikhathi eside ngomlenze ophukile, wabe ehamba ngezinduku. Ngenkathi umthwalo usencane, ngithole ama-32 kg wesisindo ngokweqile. Lapho nje elulama, waqala ukulwa nokukhuluphala, kepha kwakungekho mqondo. I-endocrinologist yaxhumana ekugcineni. Ngiyabonga uNkulunkulu, akanaso isifo sikashukela, kepha isizinda sehomoni sihle ukuthi okungenani iklabishi elilodwa limondle ngokunciphisa umzimba. Ingozi, imithi, izinguquko ngendlela ejwayelekile yokuphila - konke kudlale indima. Waqala ukuthatha iTrazhenta futhi waya ejimini. Isisindo siqale ukuhamba - 15 kg ezinyangeni ezi-2. Basho ukuthi akunakwenzeka ukwehlisa isisindo ngendlela ebukhali, kepha ubengasakwazi ukuhlala nakho. Kuhle ukuthi sinokwelashwa kwethemu: inani lentengo yokulunywa yiTrazhenta, ngokuvuma njalo, kuzofanela ngithathe ama-analog wesabelomali. ”

U-Anatoly Ivanovich, oneminyaka engama-55 ubudala, uNaberezhnye Chelny “Ngiphuza isifo sikashukela ekuseni, kanye nethebhulethi kaTrazhenta ebusuku. Ushukela usebangeni le-6 kuye ku-8 mmol / L. Kumuntu onesifo sikashukela onamava, lokhu kungumphumela omuhle. Ngenkathi uthatha iDiabeteson kuphela, i-glycated hemoglobin yayingu-9.2%, futhi manje ingu-6.5%. Ngine-pyelonephritis, kepha umuthi usebenza kahle ezinso. Intengo, empeleni, ayisiyabo abahola impesheni, kodwa amaphilisi ayabiza imali yawo. ”

UNina Petrovna, oneminyaka engama-67, uVoskresensk “Ekuseni ngiphuza isibhebhe saseTrazhenta futhi kabili ngosuku - iGlucofage. Bengilokhu ngisebenzisa ukuqokwa kwami okusha izinyanga ezi-4, ngaphambi, uSiofor wakuthatha, futhi konke bekuhamba kahle ngami kwaze kwaba yilapho izinga le-creatinine ne-urea ekuhlolweni kwegazi likhuphuka, futhi nomchamo - amaprotheni. Isazi se-endocrinologist sathi ngokumelene nesizinda seswekile, ngiba nengxaki - nephropathy. Ubeke ithebhulethi elilodwa kuTreazent. Elula kakhulu - ngiphuza ekuseni futhi angicabangi ngokwelashwa usuku lonke. Ngizwa kahle, kodwa okusemqoka ukuthi izivivinyo sezithuthukile futhi ayikho imiphumela emibi, ngaze ngancipha nesisindo esincane. ”

Ama-Dhib-4 ama-inhibitors, okungelawo iTrazhenta, ahlukaniswa hhayi kuphela ngamakhono antidiabetes, kodwa futhi nangezinga eliphephile lokuphepha, ngoba awavuseleli umphumela we-hypoglycemic, awafaki sandla ekuzuzeni isisindo, futhi awenzi ukuba ukwehluleka kwe-renal kungasebenzi. Kuze kube manje, lesi sigaba sezidakamizwa sithathwa njengesinye esithembisa kakhulu ukuphathwa kukashukela wohlobo 2.

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