I-Insulin analogues: esikhundleni sehlobo lomuthi

Ukuqeda ushukela emisebenzini yezokwelapha, kuyisiko ukusebenzisa ama-insulin analogues.

Ngokuhamba kwesikhathi, izidakamizwa ezinjalo ziye zaziwa kakhulu odokotela nasezigulini zabo.

Isimo esifanayo singachazwa:

• ukusebenza kahle okwanele kwe-insulin ekukhiqizweni kwezimboni;
• iphrofayili yezokuphepha ephezulu;
• ukusetshenziswa kalula;
• amandla okuvumelanisa umjovo womuthi nokufihlwa kwawo kwehomoni.

Ngemuva kwesikhashana, iziguli ezinesifo sikashukela sohlobo lwesibili ziphoqelelwa ukuba zishintshe zisuka kumathebhulethi anciphisa ushukela egazini zijovwe kumijovo ye-insulin ye-hormone. Ngakho-ke, umbuzo wokukhetha umuthi ofanele kubo uyinto ebaluleke kakhulu.

Izici ze-insulin yesimanje

Kunemikhawulo ethile ekusetshenzisweni kwe-insulin yomuntu, ngokwesibonelo, ukuqala kancane kokuvezwa (isifo sikashukela kufanele sinikeze umjovo imizuzu engama-30 kuya kwangaphambi kokudla) kanye nesikhathi eside kakhulu (kufika emahoreni ayi-12), esingaba yisidingo sokulibala kwe-hypoglycemia.

Ekupheleni kwekhulu leminyaka eledlule, kwavela isidingo sokuqhakambisa ama-insulin analogues okungahle kube nalawo maphutha. Ama-insulin asebenza ngokufishane aqala ukukhiqizwa ngokuncishiswa okuphezulu kwengxenye yempilo.

Lokhu kubasondeze kakhulu ezimeni ze-insulin zomdabu, ezingavunyelwa ngemuva kwemizuzu engu-4-5 ngemuva kokungena egazini.

Ukwahluka okungenantambo kwe-insulin kungahlanganiswa ngokulingene futhi ngokushelela kusuka kumanoni angaphansi kwe-subcutaneous hhayi ukuvusa i-hypoglycemia yangemuva.

Eminyakeni yamuva nje, kube noshintsho obalulekile ku-pharmacology, ngoba kuphawuliwe:

• ukushintshwa kusuka kwezixazululo ze-acidic kuya kokungathathi hlangothi;
• ukuthola i-insulin yabantu kusetshenziswa ubuchwepheshe be-DNA esebenza kabusha;
• ukwakhiwa kwezindawo ezisezingeni eliphakeme ze-insulin ezinezakhiwo ezintsha ze-pharmacological.

Ama-anulin we-insulin aguqula ubude besikhathi se-hormone yomuntu ukuhlinzeka indlela yomuntu siqu yokwelashwa nokwenzelela okukhulu koshukela.

Le mishanguzo yenza kube nokwenzeka ukufeza ibhalansi efanelekile phakathi kwezingozi zokuncipha koshukela wegazi nokufezekiswa kwe-glycemia okuhlosiwe.

Ama-analogues anamuhla we-insulin ngokwesikhathi sokwenza kwawo ahlala ahlukaniswe:

1. i-ultrashort (Humalog, Apidra, Novorapid Penfill);
2. isikhathi eside (uLantus, Levemir Penfill).

Ngaphezu kwalokho, kunezidakamizwa ezihlanganisiwe zokufaka esikhundleni, okuyingxube ye-ultrashort kanye ne-hormone ende esikalini esithile: I-Penfill, Humalog mix 25.

Isi-Humalog (lispro)

Esakhiweni sale insulin, isikhundla se-proline ne-lysine sashintshwa. Umehluko phakathi kwesidakamizwa esisetshenziselwa i-insulin ne-insulin yabantu ukungabonakali okubuthakathaka kwezinhlangano ezihlangana ndawonye. Ngenxa yalokhu, i-lispro ingangenwa masinyane egazini likashukela.

Uma ufaka izidakamizwa ku-dosage efanayo futhi ngasikhathi sinye, i-Humalog izonikeza inani eliphakeme izikhathi ezi-2 ngokushesha. Le hormone isuswa ngokushesha okukhulu futhi ngemuva kwamahora ama-4 ukuhlushwa kwayo kufinyelele ezingeni layo lasekuqaleni. Ukuhlushwa kwe-insulin elula yabantu kuzonakekelwa kungakapheli amahora ayi-6.

Uma siqhathanisa i-lispro ne-insulin elula esebenza ngokushesha, singasho ukuthi okwedlule kungavimbela ukukhiqizwa kwe-glucose yisibindi ngokuqina.

Kukhona enye inzuzo yesidakamizwa seHumalog - ingabhekeka ngaphezulu futhi ingahambisa isikhathi sokulungiswa komthamo emithanjeni yokudla okunempilo. Kuboniswa ukungabikho kwezinguquko esikhathini sokuvezwa kusuka ekukhuleni kwevolumu yento yokufaka.

Usebenzisa i-insulin elula yabantu, isikhathi somsebenzi wakhe ingahluka kuye ngethamo. Kungalesi sikhathi lapho kuvela khona isikhathi esijwayelekile samahora ayisithupha kuya kwayi-12.

Ngokukhula komthamo we-insulin Humalog, isikhathi somsebenzi waso sigcina sisezingeni elifanayo futhi sizoba amahora angama-5.

Kulandela ukuthi ngokunyuka komthamo we-lispro, ubungozi be-hypoglycemia obambezelayo abunyuki.

I-Aspart (i-Novorapid Penfill)

Le analogue ye-insulin ingalingisa ngokuphelele ukuphendula okwanele kwe-insulin ekudleni kokudla. Isikhathi saso esifushane sibangela umphumela obuthakathaka phakathi kokudla, okwenza sikwazi ukulawula ngokuphelele ushukela wegazi.

Uma siqhathanisa imiphumela yokwelashwa ne-insulin analogues ne-insulin ejwayelekile esebenza njenge-insulin, kuzokwaziwa ukwanda okukhulu kwekhwalithi yokuphathwa kwamazinga kashukela wegazi ngemuva.

Ukwelashwa okuhlanganisiwe noDetemir no-Aspart kunika ithuba:

• cishe i-100% yenza ngokwejwayelekile iphrofayili ye-insulin yansuku zonke;
• ukwenza ngokufanelekile amazinga we-glycosylated hemoglobin;
• kunciphisa kakhulu amathuba okukhula kwezimo ze-hypoglycemic;
• banciphise ukuqina kanye nenani eliphakeme likashukela egazini likashukela.

Kuyaphawuleka ukuthi ngesikhathi sokwelashwa nge-basal-bolus insulin analogues, ukwanda okuyisisindo somzimba kwakuphansi kakhulu kunesikhathi sonke sokubuka okunamandla.

Glulisin (Apidra)

I-anidulin ye-insulin yomuntu umuthi umuthi wokuvezwa osendaweni emfishane. Ngokwe-pharmacokinetic yayo, izici ze-pharmacodynamic kanye ne-bioavailability, iGlulisin ilingana neHumalog. Emsebenzini wayo we-mitogenic and metabolic, i-hormone ayihlukile kwe-insulin elula yabantu. Ngenxa yalokhu, kungenzeka ukuyisebenzisa isikhathi eside, futhi kuphephile ngokuphelele.

Njengomthetho, i-Apidra kufanele isetshenziswe ngokuhambisana ne:

1. ukudalulwa kwe-insulin yesikhathi eside komuntu;
2. i-basal insulin analogue.

Ngaphezu kwalokho, umuthi ubonakala ngokuqala komsebenzi okusheshayo kanye nesikhathi sawo esifushane kune-hormone yomuntu ejwayelekile. Ivumela iziguli ezinesifo sikashukela ukukhombisa ukuguquguquka okukhulu ekusebenziseni ngokudla kunama-hormone abantu. I-insulin iqala ukusebenza ngokushesha kwayo ngemuva kokuphathwa, futhi izinga likashukela wegazi lehla imizuzu eli-10 ukuya kwengama-20 ngemuva kokuba i-Apidra ilimale ngaphandle kokukhubazeka.

Ukugwema i-hypoglycemia ezigulini esezikhulile, odokotela batusa ukuthi kungeniswe umuthi ngokushesha ngemuva kokudla noma ngasikhathi sinye. Isikhathi esincishisiwe se-hormone sisiza ukugwema umphumela okuthiwa "ukunqwabelana", owenza ukuthi kuvikeleke i-hypoglycemia.

I-Glulisin ingaba ngempumelelo kulabo abakhuluphele, ngoba ukusetshenziswa kwayo akubangeli ukuqhubeka kwesisindo. Umuthi ubonakala ngokuqala okusheshayo kokuhlungwa okuphezulu ngokuqhathaniswa nezinye izinhlobo zamahomoni, ejwayelekile ne-lispro.

I-Apidra ilungele kahle amazinga ahlukahlukene ngokweqile ngenxa yokuguquguquka kwayo okuphezulu kokusebenzisa. Ehlobo lokukhuluphala kohlobo lwe-visceral, isilinganiso sokumunca somuthi sinokuhluka, okwenza kube nzima ukulawulwa kwe-prandial glycemic.

I-Detemir (Levemir Penfill)

I-Levemir Penfill iyi-analogue ye-insulin yabantu. Inesikhathi sokusebenza esilinganiselwe futhi ayinazo iziqongo. Lokhu kusiza ukuqinisekisa ukulawulwa kwe-basal glycemic phakathi nosuku, kepha kuncike ekusetshenzisweni kabili.

Lapho ihanjiswa ngokungaziphathi kahle, i-Detemir yakha izinto ezihlangana ne-serum albhamuin ku-fluid yangaphakathi. Ngemuva kokudluliselwa odongeni lwe-capillary, i-insulin ibopha futhi i-albhamuin esegazini.

Ekulungiseleleni, yingxenye kuphela yamahhala esebenza ngokusebenza. Ngakho-ke, ukubopha i-albhamuin kanye nokubola kwayo kancane kunikeza ukusebenza isikhathi eside futhi okungenamkhawulo.

U-Levemir Penfill insulin usebenza ogulayo onesifo sikashukela futhi aphindise isidingo sakhe esiphelele se-insal insulin. Akuhlinzeki ukuqhaqhazela ngaphambi kokuphatha okufushane.

I-Glargin (i-Lantus)

Ukufakwa esikhundleni kwe-insulin ye-Glargin kushesha kakhulu. Lesi sidakamizwa singaba lula futhi singanyibiliki ngokuphelele endaweni ene-acidic encane, futhi endaweni engathathi hlangothi (emafutheni angamakhompiyutha) asincibiliki kahle.

Ngokushesha nje emva kokuphathwa kwe-subcutaneous, i-Glargin ingena ekuphenduleni kokungathathi hlangothi nokwakhiwa kwe-microprecipitation, okudingeka ukukhululwa okuqhubekayo kwe-hexamers yezidakamizwa kanye nokuhlukaniswa kwabo ku-monulin ye-insulin nama-dimers.

Ngenxa yokugeleza ngokushelelayo nangokuhamba kancane kweLantus ukungena egazini lesiguli esinesifo sikashukela, ukujikeleza kwakhe esiteshini kwenzeka kungakapheli amahora angama-24. Lokhu kwenza ukuthi sikwazi ukujova ama-insulin analogue kanye ngosuku.

Lapho kufakwa inani elincane le-zinc, i-insulin Lantus ikhala ngezicubu ezingaphansi, ezibuye zandise isikhathi sayo sokufaka. Impela zonke lezi zinhlobo zalesi sidakamizwa ziqinisekisa iphrofayili yaso ebushelelezi nethe thuli ngokuphelele.

I-Glargin iqala ukusebenza imizuzu engama-60 ngemuva kokujova ngokunqenqemeni. Ukuqina kwayo okuqinile ku-plasma yegazi lesiguli kungabukwa ngemuva kwamahora angama-2-2 kusuka lapho kukhishwe umthamo wokuqala.

Kungakhathalekile ukuthi yisiphi isikhathi sokulimala ngqo salo muthi we-ultrafast (ekuseni noma kusihlwa) nendawo yomjovo osheshayo (isisu, ingalo, umlenze), isikhathi sokuchayeka emzimbeni sizoba:

• isilinganiso - amahora angama-24;
• isilinganiso - amahora angama-29.

Ukufakwa esikhundleni kwe-insulin Glargin kungahambisana ngokuphelele ne-hormone yokwakheka komzimba ekusebenzeni kwayo okuphezulu, ngoba umuthi:

1. kufanelekile ukuvuselela ukusetshenziswa koshukela yizicubu zomzimba ezibhekela i-insulin (ikakhulukazi okunamafutha nomsipha);
2. ivimbela i-gluconeogeneis (yehlisa ushukela wegazi).

Ngaphezu kwalokho, umuthi uvimbela kakhulu ukuwohloka kwezicubu ze-adipose (lipolysis), ukubola kwamaprotheni (proteinolysis), ngenkathi kuthuthukisa ukwenziwa kwezicubu zomzimba.

Izifundo zezokwelapha ze-pharmacokinetics zikaGlargin zikhombisile ukuthi ukusatshalaliswa okungenanhlonipho kwalesi sidakamizwa kwenza ukuthi sikwazi ukucishe sibe yi-100% ukulingisa ukukhiqizwa kwe-basal kwe-endo native hormone insulin kungakapheli amahora angama-24. Ngasikhathi sinye, amathuba okukhula kwezimo ze-hypoglycemic kanye nokugxuma okubukhali emazingeni kashukela wegazi ancishiswa kakhulu.

Hlanganisa u-25

Lesi sidakamizwa siyingxube equkethe:

• Ukumiswa okungamaphesenti angama-75 kwe-hormone lispro;
• I-25% insulin Humalog.

Lokhu namanye ama-insulin analogue nawo ahlanganiswe ngokwendlela yawo yokukhulula. Isikhathi esihle somuthi siqinisekiswa ukuthi sibonga umphumela wokumiswa okunamahlwili we-lyspro ye-hormone, okwenza sikwazi ukuphinda ukukhiqizwa kwe-basal kwe-hormone.

Ama-25% asele we-inspro insulin ayingxenye yesikhathi sokuvezwa okufushane kakhulu, onomphumela omuhle kwi-glycemia ngemuva kokudla.

Kuyaphawuleka ukuthi i-Humalog ekwakhiweni kwengxube ithinta umzimba ngokushesha okukhulu ngokuqhathaniswa ne-hormone emfushane. Inikeza ukulawulwa okuphezulu kwe-gypcemia ye-postpradial ngakho-ke iphrofayli yayo iphilile ngokwenyama uma uyiqhathanisa ne-insulin efushane.

Ama-insulin ahlanganisiwe anconywa kakhulu kubantu abanesifo sikashukela sohlobo 2. Leli qembu lifaka iziguli esezikhulile ezithi, njengomthetho, zinenkinga yememori. Kungakho ukwethulwa kwe-hormone ngaphambi kokudla noma ngokushesha nje ngemuva kokusiza kakhulu ekuthuthukiseni izinga lempilo yeziguli ezinjalo.

Ucwaningo lwesimo sempilo sabanesifo sikashukela eqenjini labaneminyaka engama-60 kuye kwengama-80 sisebenzisa isidakamizwa uHusalog 25 sakhombisa ukuthi bakwazile ukuthola isinxephezelo esihle kakhulu se-carbohydrate metabolism. Kwindlela yokulawulwa kwama-hormone ngaphambi nangemva kokudla, odokotela bakwazile ukuthola isisindo esincane kanye nenani eliphansi kakhulu le-hypoglycemia.

Yikuphi okungcono i-insulin?

Uma siqhathanisa ne-pharmacokinetics yezidakamizwa ezibhekwayo, khona-ke ukuqokwa kwabo ngudokotela ovumayo kufanelekile uma kwenzeka kunesifo sikashukela, zombili izinhlobo zokuqala nezesibili. Umehluko omkhulu phakathi kwalawa ma-insulin ukungabikho kokukhuphuka kwesisindo somzimba ngesikhathi sokwelashwa kanye nokwehla kwesibalo sezinguquko zobusuku ekugxambeni kwe-glucose egazini.

Ngaphezu kwalokho, kubalulekile ukuqaphela isidingo somjovo owodwa kuphela phakathi nosuku, okulungele kakhulu iziguli. Ngokuphakeme kakhulu ukusebenza kwe-analogue ye-insulin Glargin yabantu ngokuhlanganiswa ne-metformin yeziguli ezinohlobo lwesibili sikashukela. Ucwaningo lukhombise ukwehla okukhulu kwe-spikes ebusuku ekuhlushwa ushukela. Lokhu kusiza ngokweqiniso ukuguquguqula i-glycemia yansuku zonke.

Ukuhlanganiswa kweLantus nemithi yomlomo ukwehlisa ushukela wegazi kwafundwa kulezo ziguli ezingakwazi ukunxephezela isifo sikashukela.

Badinga ukunikezwa i-Glargin ngokushesha okukhulu. Lesi sidakamizwa sinconyelwa ukwelashwa nodokotela we-endocrinologist nodokotela ojwayelekile.

Ukwelashwa okujulile ngeLantus kwenza sikwazi ukuthuthukisa kakhulu ukulawulwa kwe-glycemic kuwo wonke amaqembu eziguli ezinesifo sikashukela.