I-Linagliptin yi-ejenti yomlomo ye-hypoglycemic ekwazi ukuvimba i-enzyme dipeptidylpetitase-4. Le enzyme ibamba iqhaza ku-inactivation yama-hormone we-incretin.
Ama-hormone anjalo emzimbeni womuntu yi-glucapeptide-1 ne-glucose-insulinotropic polypeptide. Lezi zingxube ze-bioactive zonakaliswa ngokushesha yi-enzyme.
Zombili lezi zinhlobo zama-incretin ziqinisekisa ukuqina kwezinqubo ezibhekene nokugcina izinga le-glucose ezingeni eliqinisekisa ukusebenza okujwayelekile komzimba wonke.
Ukwakheka kanye nomthamo womuthi
Isidakamizwa esithandwa kakhulu esiqukethe i-linagliptin isidakamizwa segama elifanayo.
Ukwakheka kwalesi sidakamizwa kufaka phakathi into esemqoka esebenzayo - i-linagliptin. Umthamo owodwa wesidakamizwa uqukethe i-5 mg yento esebenzayo.
Ngaphezu kwesithako esikhulu esisebenzayo, umuthi uqukethe izinto ezengeziwe.
Izinto ezisizayo ekwakhiweni kwalo muthi zimi ngalendlela elandelayo:
- IMannitolum.
- Isitashi pregelatinized.
- Isitashi sombila.
- Colovidone.
- Magnesium stearate.
Umuthi uyicwecwe elihlanganiswe nokuhlanganiswa okukhethekile kwefilimu.
Ukwakheka kwengubo ekhethekile yethebhulethi ngayinye kufaka phakathi okulandelayo:
- I-opadra pink;
- i-hypromellose;
- titanium dioxide;
- i-talc;
- macrogol 6000;
- i-iron oxide ibomvu.
Umuthi uyatholakala ngesimo samaphilisi anesimo esiyindilinga. Izibhebhe zidluliselwe emaphethelweni ifilimu ihlanganiswa. Igobolondo lethebhulethi linombala wokukhanya obomvu. Igobolondo liqoshwe ngophawu lwenkampani ekhiqiza i-BI endaweni eyodwa ne-D5 kwelinye.
Amathebhulethi ayatholakala emaphaketheni okulimaza izingcezu eziyi-10 inye. Amabhola agcwele ebhokisini lekhadibhodi. Iphakethe ngalinye liqukethe 3 amabhulashi. Qiniseka ukuthi ufaka imiyalo yokusebenzisa umuthi kwiphakethe ngalinye lomuthi.
Ukugcinwa komuthi kufanele kwenziwe endaweni emnyama emazingeni okushisa angaphansi kwama-25 degrees Celsius.
Indawo yokubeka umuthi akufanele ifinyeleleke ezinganeni. Impilo yeshalofu yesidakamizwa yiminyaka emithathu.
I-Pharmacodynamics ne-pharmacokinetics yesidakamizwa
Ngemuva kokuphathwa komlomo emzimbeni, uLinagliptin ubopha ngokuqinile ku-dipeptidyl peptidase-4.
Isibopho esiyinkimbinkimbi esiholelayo siyaphenduka. Ukuhlanganiswa kwe-enzyme ene-linagliptin kuholela ekwandeni kokuxineka kwama-incretins emzimbeni futhi kusiza ukugcina umsebenzi wabo isikhathi eside.
Umphumela womuthi ukwehla kokukhiqizwa kwe-glucagon kanye nokwanda kokuqunjelwa kwe-insulin, futhi lokhu, kuqinisekisa ukwenzeka okujwayelekile kwezinga le-glucose emzimbeni womuntu.
Lapho usebenzisa i-Linagliptin, ukwehla kwe-glucose hemoglobin kanye nokwehla kwe-glucose ku-plasma yegazi kwasungulwa ngokuthembekile.
Ngemuva kokuthatha umuthi, udonswa ngokushesha. Iqoqo eliphezulu lomuthi ku-plasma litholakala emahoreni angama-1.5 ngemuva kokuphathwa.
Ukwehla kokuqukethwe kwe-linagliptin kwenzeka ngezigaba ezimbili. Ukuqedwa kwesigamu sempilo kukude futhi kungamahora ayi-100. Lokhu kungenxa yokuthi umuthi wakheka isakhiwo esizinzile nge-enzyme DPP-4. Ngenxa yokuthi ukuxhumana ne-enzyme kuwukuqongelela kabusha komuthi emzimbeni akwenzeki.
Endabeni yokusebenzisa i-Linagliptin ekuhlakazweni kwe-5 mg ngosuku, ukuqina okuzinzile kwesikhathi esisodwa sento esebenza ngomuthi kutholakala emzimbeni wesiguli ngemuva kokuphuza imithamo emithathu yomuthi.
I-bioavailability ephelele yesidakamizwa icishe ibe ngama-30%. Uma i-linagliptin ithathwa ngasikhathi sinye njengokudla okugcwele amanoni, khona-ke ukudla okunjalo akukuthinti kakhulu ukufakwa komuthi.
Ukukhishwa komuthi emzimbeni kwenziwa ikakhulu emathunjini. Cishe ama-5% akhishwa ngohlelo lokuchama yizinso.
Izinkomba kanye ne-contraindication yokusebenzisa umuthi
Inkomba yokusetshenziswa kwe-linagliptin ubukhona besifo sikashukela sohlobo II esigulini.
Ngesikhathi se-monotherapy, i-linagliptin isetshenziswa ezigulini ezinokulawulwa okunganele kwezinga le-glycemia emzimbeni ngosizo lokudla nokuzivocavoca umzimba.
Ukusetshenziswa kwomuthi kuyanconywa uma isiguli sinokungabekezeleleki kwe-metformin noma uma kukhona ukuphikisana nokusetshenziswa kwe-metformin ngenxa yokuthuthukiswa kokuhluleka kwe-renal esigulini.
Umuthi unconyelwa ukwelashwa okwenziwa izingxenye ezimbili kuhlanganiswa ne-metformin, i-sulfonylurea derivatives noma i-thiazolidinedione, uma kwenzeka ukuthi ukusetshenziswa kwezindlela zokudla, ukuvivinya umzimba kanye ne-monotherapy ngezidakamizwa ezikhonjisiwe kutholakala kungasebenzi.
Kunengqondo ukusebenzisa i-Linagliptin njengengxenye yokwelashwa okwenziwa izingxenye ezintathu, uma ukudla, ukuzivocavoca, ukwelashwa nge-monotherapy noma ukwelashwa okwenziwa izingxenye ezimbili akunikezanga umphumela omuhle.
Kungenzeka ukusebenzisa umuthi ngokuhambisana ne-insulin, lapho wenza ukwelashwa okuxubile ngesifo sikashukela i-mellitus, lapho ungekho khona umphumela wokusetshenziswa kokudla kokuzivocavoca umzimba kanye nokwelashwa kwamahhala kwe-insulin
Izimpawu eziphikisayo ezisetshenziselwa umkhiqizo wezokwelapha yilezi:
- ukuba khona komzimba wesiguli sohlobo lwe-1 isifo sikashukela;
- ukuthuthukiswa kwe-ketoacidosis yesifo sikashukela;
- isikhathi sokukhulelwa nokukhulelwa;
- iminyaka yesiguli ingaphansi kweminyaka eyi-18;
- ukuba khona kwe-hypersensitivity esenzweni emzimbeni wanoma iziphi izingxenye zezidakamizwa.
ILingliptin iyenqatshelwe ngokuphelele ukusebenzisa ngesikhathi sokukhulelwa nokuqunjelwa. Lokhu kungenxa yokuthi into esebenzayo, lapho ingena egazini lesiguli, iyakwazi ukuwela isithintelo se-placental, futhi iyakwazi ukungena kubisi lwebele ngesikhathi sokubeletha.
Uma kudingekile ngokuphelele ukusebenzisa umuthi ngesikhathi sokukhulelwa, ukuncelisa ibele kufanele kumiswe ngokushesha.
Imiyalo yokusebenzisa umuthi
Imiyalo yokusebenzisa umuthi ikhombisa ukuthi i-Linagliptin isetshenziswa ekwelapheni uhlobo 2 lwesifo sikashukela emthanjeni we-5 mg kanye ngosuku, okuyipilisi elilodwa. Umuthi uphuzwa ngomlomo.
Uma uphuthelwa isikhathi sokuphuza umuthi, kufanele uwuphuze masisha lapho isiguli sikhumbula lokhu. Umthamo ophindwe kabili womuthi awunqatshelwe.
Lapho uthatha umuthi, ngokuya ngezici ngazinye, imiphumela emibi ingahle ivele.
Imiphumela emibi eyenzeka emzimbeni wesiguli ingathinta:
- Amasosha omzimba.
- Izitho zokuphefumula.
- Uhlelo lwamapheshana esiswini.
Ngaphezu kwalokho, kungenzeka ukuthuthukisa izifo ezithathelwanayo emzimbeni, njenge-nasopharyngitis.
Lapho usebenzisa i-Linagliptin kuhlangene ne-Metformin, imiphumela emibi elandelayo ingenzeka:
- ukubonakala kwe-hypersensitivity;
- ukuvela kwesikhwehlela;
- ukuthuthukiswa kwe-pancreatitis
- ukubonakala kwezifo ezithathelwanayo.
Endabeni yokusebenzisa umuthi ngokuhambisana ne-sulfonylureas yesizukulwane sakamuva, kungenzeka ukuthi umzimba uthuthuke ukuphazamiseka okuhlobene nokusebenza:
- Amasosha omzimba.
- Izinqubo ze-Metabolic.
- Uhlelo lokuphefumula.
- Izitho zesisu.
Endabeni yokusebenzisa iLinagptin ngokuhlangana nePioglipazone, ukuthuthukiswa kwezifo ezilandelayo kungabonakala:
- ukubonakala kwe-hypersensitivity;
- i-hyperlipidemia kushukela;
- ukuvela kwesikhwehlela;
- i-pancreatitis
- izifo ezithathelwanayo;
- isisindo somzimba.
Lapho usebenzisa i-Linagliptin ehambisana ne-insulin ngesikhathi sokwelashwa, imiphumela emibi elandelayo ingaqhamuka emzimbeni wesiguli:
- Ukuthuthukiswa kwe-hypersensitivity emzimbeni.
- Ukubonakala kokukhwehlela nokuphazamiseka ohlelweni lokuphefumula.
- Ukusuka ohlelweni lokugaya ukudla, ukubonakala kwe-pancreatitis nokuqunjelwa kungenzeka.
- Izifo ezithathelwanayo zingavela.
Endabeni yokusetshenziswa kweLinagliptin yohlobo lwesibili lokwelashwa kwe-mellitus yesifo sikashukela kuhlangene ne-Metformin ne-sulfonylurea derivatives, hypersensitivity, hypoglycemia, ukubukeka kokhwehlela, ukubonakala kwezimpawu pancreatitis kanye nokwanda kwesisindo somzimba kungenzeka.
Ngaphezu kwale miphumela emibi, ukubonakala kanye nokukhula kwe-angioedema, i-urticaria, i-pancreatitis eshubile, ukuqubuka kwesikhumba emzimbeni wesiguli kungenzeka.
Uma kwenzeka i-overdose, izindlela ezijwayelekile okuhloswe ngazo ukugcina umzimba kufanele zisetshenziswe.
Izinyathelo ezinjalo ukususwa kwalo muthi emzimbeni nasekwelashweni kwezimpawu.
Ukuxhumana kwe-linagliptin nezinye izidakamizwa
Ngokuphathwa kanyekanye kweMetformin 850 ngeLinagliptin, ukwehla okuphawulekayo kwezinga loshukela emzimbeni wesiguli kwenzeka.
I-pharmacokinetics yesidakamizwa uma isetshenziswa ndawonye ne-sulfonylurea derivatives yesizukulwane sakamuva alunalo ushintsho olukhulu.
Lapho kusetshenziswa ekwelapheni okuyinkimbinkimbi kwe-thiazolidinediones, akukho ushintsho olubalulekile kuma-pharmacokinetics. Lokhu kuphakamisa ukuthi i-linagliptin akuyona i-inhibitor ye-CYP2C8.
Ukusetshenziswa kwe-ritonavir ekwelashweni okuyinkimbinkimbi akuholeli kuguquko olubalulekile emtholampilo kanye ne-pharmacokinetics ye-linagliptin.
Ngokusetshenziswa okuphindaphindiwe kweLinagliptin kanye neRifampicin kuholela ekunciphiseni okuningana komsebenzi wesidakamizwa
ILinagliptin iphikisiwe ekwelapheni uhlobo lwesifo sikashukela sohlobo 1 noma ekwelapheni isifo sikashukela.
Imvamisa yokuthuthuka kwesimo se-hypoglycemia emzimbeni wesiguli ngesikhathi se-monotherapy icishe ibe mincane.
Amathuba okukhula kwe-hyperglycemia akhuphuka uma iLinagliptin isetshenziswa ngokubambisana nezidakamizwa ezitholakala kwe-sulfonylureas yesizukulwane sakamuva. Ngalesi sizathu, ukunakekelwa okukhethekile kufanele kuthathwe ngokuphathwa okuyinkimbinkimbi.
Uma kunesidingo, umthamo wemithi ezothathwa kufanele uguqulwe ukuvikela ukuthuthukiswa kwezimpawu ze-hypoglycemia.
Ukusetshenziswa kwe-linagliptin akuthinti amathuba ezinkinga zomsebenzi wohlelo lwethambo nenhliziyo.
I-Linagliptin ingasetshenziswa ekwelapheni isifo sikashukela ezigulini ezihluleka kakhulu yizinso.
Lapho usebenzisa i-Linagliptin, kunikezwa ukwehla okukhulu kokuqukethwe kwe-glycosylated hemoglobin kanye ne-glucose esheshayo.
Uma kwenzeka izinsolo zokuqalwa kokukhula kwepancreatitis emzimbeni, ukusetshenziswa komuthi kufanele kumiswe ngokushesha.
Ukubuyekezwa mayelana nomuthi, ukufana kwawo nezindleko
Umuthi, kubandakanya i-linagliptin, unegama lokuhweba lakwamanye amazwe iTrazhenta.
Umenzi walo muthi yiBeringer Ingelheim Roxane Inc., etholakala e-United States. Ngaphezu kwalokho, lo muthi ukhiqizwa yi-Austria. Umuthi uhanjiswa emakhemisi ngesibopho sencwadi ebekiwe ngudokotela oholayo.
Ukubuyekezwa kweziguli mayelana nomuthi uvame ukuba muhle kakhulu. Ukubuyekezwa okungalungile kuvame ukuhlotshaniswa nokusetshenziswa komuthi kwephula imiyalo yokusetshenziswa, okubangela ukweqisa noma ukubonakala kwemiphumela emibi eshiwo.
Izindleko zomuthi zinenani elihlukile ngokuya ngomkhiqizi, umakethi, kanye nesifunda lapho kuthengiswa khona umuthi eRussia.
ILinagliptin 5 mg No. 30 eyenziwe nguBeringer Ingelheim Roxane Inc., e-USA eRussia inezindleko eziphakathi esifundeni sama-ruble ayi-1760.
ILinagliptin kumathebhulethi ayi-5 mg kwiphakeji lezingcezu ezingama-30 ezenziwe e-Austria eRussia Federation inezindleko ezimaphakathi ebangeni ukusuka ku-1648 kuya ku-1724 ruble.
Izifanekiso zomuthi iTrazhenta, equkethe i-linagliptin, yiJanuvia, Onglisa noGalvus. Le mishanguzo iqukethe izithako ezahlukahlukene ezisebenzayo, kepha umphumela wazo emzimbeni uyefana nalowo iTrazhenta onawo emzimbeni.
Funda kabanzi ngezidakamizwa zesifo sikashukela kuvidiyo kule ndatshana.
