ILiraglutide ingesinye sezidakamizwa ezintsha kakhulu esinciphisa ngempumelelo ushukela wegazi emikhunjini enesifo sikashukela. Umuthi unomphumela we-multifactorial: unyusa ukukhiqizwa kwe-insulin, uvimbela ukwakheka kwe-glucagon, wehlise iphango, futhi wehlise ukumuncwa kwe-glucose ekudleni. Eminyakeni embalwa edlule, iLiraglutide yavunyelwa njengendlela yokunciphisa umzimba ezigulini ngaphandle kwesifo sikashukela, kodwa ngokukhuluphala ngokweqile. Ukubuyekezwa kwalabo abanciphisa isisindo kukhombisa ukuthi umuthi omusha ungafinyelela imiphumela ehlaba umxhwele kubantu asebevele belahlekelwe yithemba lesisindo esijwayelekile. Ekhuluma ngeLiraglutida, umuntu ngeke ehluleke ukusho ukushiyeka kwayo: intengo ephezulu, ukungakwazi ukuthatha amaphilisi ngendlela evamile, ulwazi olwanele olusetshenziswayo.
Uhlobo nokwakheka kwalo muthi
Amathumbu ethu, kukhiqizwa ama-hormone ama-incretin, phakathi kwawo lapho i-glucagon enjenge-peptide ye-gluc-1 idlala indima eholayo ekuqinisekiseni ushukela wegazi ojwayelekile. ILiraglutide iyi-analogue eyenziwe ngobuhlakani ye-GLP-1. Ukwakheka nokulandelana kwama-amino acid kule molekyuli yeLyraglutide iphinda i-97% ye-peptide yemvelo.
Ngenxa yalokhu kufana, lapho kungena ukungena kwegazi, into iqala ukusebenza njenge-hormone yemvelo: ukuphendula ukwanda koshukela, kuvimbela ukukhishwa kwe-glucagon futhi kusebenze ukucubungula kwe-insulin. Uma ushukela ujwayelekile, isenzo se-liraglutide siyamiswa, ngenxa yalokho, i-hypoglycemia ayisongeli abantu abanesifo sikashukela. Umphumela owengeziwe womuthi ukuvimbela ukukhiqizwa kwe-hydrochloric acid, ukwenza buthaka kwe-motility yesisu, ukucindezela indlala. Lo mphumela we-liraglutide esiswini nakuhlelo lwezinzwa uyakuvumela ukuthi usetshenziselwe ukwelapha ukukhuluphala.
Imvelo ye-GLP-1 ihlukana ngokushesha. Kungakapheli nemizuzu emi-2 ngemuva kokukhishwa, ingxenye ye-peptide ihlala egazini. I-Artificial GLP-1 isemzimbeni isikhathi eside, okungenani ngosuku.
ILiraglutide ayikwazi ukuthathwa ngomlomo ngesimo samathebulethi, ngoba emgodini wokugaya ukudla izolahlekelwa umsebenzi wayo. Ngakho-ke, umuthi uyatholakala ngesimo sesisombululo nge-ntho esebenzayo ye-6 mg / ml. Ukuze kube lula ukuyisebenzisa, ama-cartridge wesisombululo abekwa emapeni wesirinji. Ngosizo lwabo, ungayikhetha kalula umthamo oyifunayo bese wenza umjovo endaweni engafanelekile yalokhu.
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%
Izimpawu Zentengiso
ILiraglutid yathuthukiswa yinkampani yaseDenmark iNovoNordisk. Ngaphansi kwegama lokuhweba elithi Viktoza, selithengisiwe eYurophu naseMelika kusukela ngo-2009, eRussia kusukela ngo-2010. Ngo-2015, i-Liraglutide yavunywa njengesidakamizwa ekwelapheni ukukhuluphala kakhulu. Imithamo enconyiwe yokunciphisa isisindo yehlukile, ngakho-ke ithuluzi laqala ukukhishwa ngumenzi ngaphansi kwegama elihlukile - iSaxenda. IViktoza neSaksenda ziyizichazi ezishintshashintshayo; zinento efanayo esebenzayo nokuxazululwa kwezisombululo. Ukwakheka kwama-excipients kuyafana futhi: i-sodium hydrogen phosphate, propylene glycol, phenol.
Victoza
Ephaketheni lomuthi kukhona amapeni amabili wesirinji, ngalinye linama-18 mg e-liraglutide. Iziguli ezinesifo sikashukela ziyelulekwa ukuthi zingasebenzisi ngaphezu kwe-1.8 mg ngosuku. Isilinganiso esilinganiselwe sokunxephezela isifo sikashukela kwiziguli eziningi singu-1,2 mg. Uma uthatha lo muthi, iphakethe leVictoza lanele inyanga eyi-1. Intengo yokufaka imayelana nama-ruble angama-9500.
Saxenda
Ukwehla kwesisindo, kuthathwa imithamo ephakeme ye-liraglutide kunoshukela ojwayelekile. Iningi lezifundo, lo myalezo uncoma ukuthatha u-3 mg wesidakamizwa ngosuku. Kwiphakheji leSaksenda kunezinhlayiya ezi-5 zesirinji ezingama-18 mg zezithako ezisebenzayo kokukodwa, ingqikithi ye-90 mg ye-Liragludide - impela yezifundo zenyanga. Intengo ephakathi kumakhemisi ngama-ruble angama-25,700. Izindleko zokwelashwa ngeSaksenda ziphakeme kancane kunezakwabo, i-1 mg yeLyraglutide eSaksend ibiza ama-ruble angama-286, eViktoz - ama-ruble angama-264.
Ngabe iLiraglutid isebenza kanjani?
Isifo sikashukela mellitus sibonakala nge-polymorbidity. Lokhu kusho ukuthi wonke umuntu onesifo sikashukela unezifo eziningana ezingamahlalakhona ezinezimbangela ezivamile - ukuphazamiseka kwe-metabolic. Iziguli zivame ukutholakala zinomfutho wegazi ophakeme, isifo sokuqina kwemithambo yegazi, izifo zamahomoni, ezingaphezu kwezi-80% yeziguli zikhuluphele. Ngezinga eliphakeme le-insulin, ukunciphisa isisindo kunzima impela ngenxa yemizwa engapheli yendlala. Isifo sikashukela sidinga amandla amakhulu ukuze silandele ukudla okuphansi kwe-carb. I-Liraglutide ayigcini nje ukunciphisa ushukela, kodwa futhi inqoba izifiso zamaswidi.
Imiphumela yokuphuza umuthi ngocwaningo:
- Ukwehla okujwayelekile kwe-hemoglobin ye-glycated ku-diabetesics ukuthatha i-1,2 mg yeLyraglutide ngosuku kungu-1.5%. Ngalesi sikhombisi, umuthi uphakeme hhayi kuphela ngokutholakala ku-sulfonylurea, kodwa futhi ne-sitagliptin (amaphilisi kaJanuvia). Ukusetshenziswa kwe-liraglutide kuphela kungakunxephezela isifo sikashukela kuma-56% eziguli. Ukungezwa kwamacwecwe wokulwa ne-insulin (Metformin) kukhulisa kakhulu ukusebenza kwakwelashwa.
- Ukushesha ushukela kwehla ngo-2 mmol / L ngaphezulu.
- Umuthi ukhuthaza ukunciphisa umzimba. Ngemuva konyaka wokuphatha, isisindo kuma-60% eziguli sehlile ngamaphesenti angaphezu kwama-5, ku-31% - ngo-10%. Uma iziguli zinamathela ekudleni, ukunciphisa umzimba kuphezulu kakhulu. Ukwehla kwesisindo kuhloswe ikakhulukazi ukunciphisa inani lamafutha e-visceral, imiphumela emihle ibonwa esinqeni.
- I-Liraglutide inciphisa ukumelana ne-insulin, ngenxa yokuthi i-glucose eqala ukushiya izikebhe ngokwengeziwe, isidingo se-insulin siyancipha.
- Umuthi usebenza isikhungo sokugcotshwa esisendaweni ye-hypothalamus, ngaleyo ndlela sicindezela umuzwa wokulamba. Ngenxa yalokhu, okuqukethwe ikhalori yansuku zonke yokudla kunciphisa ngokuzenzakalela ngo-200 kcal.
- ILiraglutide ithinta kancane ingcindezi: ngokwesilinganiso, yehla ngo-2-6 mm Hg. Ososayensi bathi lo mphumela ungumthelela omuhle wesidakamizwa ekusebenzeni kwezindonga zemithambo yegazi.
- Umuthi unezici ze-cardioprotective, unomphumela omuhle kuma-lipids egazi, wehlisa i-cholesterol ne-triglycerides.
Ngokusho kodokotela, i-Liraglutid isebenza kakhulu ezigabeni zokuqala zesifo sikashukela. Ukuqokwa okuhle: umuntu onesifo sikashukela ethatha amaphilisi eMetformin endaweni ephezulu, ehola impilo esebenzayo, elandela ukudla. Uma lesi sifo singafakelwa isinxephezelo, i-sulfonylurea ngokwesiko yengezwa kunhlobo yokwelashwa, okuholela ekuholeleni ekuqhubekeni kwesifo sikashukela. Ukufaka la mathebhulethi ne-Liraglutide kugwema umphumela omubi kumaseli we-beta, futhi kuvimbele ukonakala kwangaphambilini kwamanyikwe. Ukuhlanganiswa kwe-insulin akwehli ngokuhamba kwesikhathi, umphumela wesidakamizwa uhlala uhlala njalo, okwandisa umthamo awudingeki.
Lapho eqokwa
Ngokusho kwemiyalo, iLiraglutid imiselwe ukuxazulula imisebenzi elandelayo:
- isinxephezelo sikashukela. Umuthi ungathathwa kanyekanye ngamaphilisi e-insulin angafakelwa kanye ne-hypoglycemic aqhamuka emakilasini we-Biguanides, glitazones, sulfonylureas. Ngokuya ngezincomo zomhlaba wonke, i-Ligalutid yesifo sikashukela isetshenziswa njengomuthi wezintambo ezi-2. Izikhundla zokuqala ziyaqhubeka nokuphathwa ngamacwecwe eMetformin. I-Liraglutide njengomuthi kuphela onqunyelwe kuphela ngokungabekezeleli iMetformin. Ukwelashwa empeleni kunesekelwa ukusebenza komzimba nokudla okuphansi kwe-carb;
- ubungozi obuncishisiwe bokushaywa unhlangothi kanye nokushaywa yinhliziyo kubantu abanesifo sikashukela abanezifo zenhliziyo. ILiraglutide ichazwe njengekhambi elingeziwe, ingahlanganiswa nama-statins;
- ngokulungiswa kokukhuluphala kweziguli ngaphandle kwesifo sikashukela esine-BMI ngaphezulu kwama-30;
- sokuncipha kwesisindo ezigulini ezine-BMI ngenhla ezingama-27, uma kutholakale ukuthi okungenani zinesifo esisodwa esihambisana nokuphazamiseka kwe-metabolic.
Umphumela we-liraglutide kwesisindo uhluka kakhulu ezigulini. Uma kuqhathaniswa nokubuyekezwa kokuncipha kwesisindo, abanye balahlekelwa amashumi amakhilogremu, kanti abanye banemiphumela emincane kakhulu, engakapheli ama-5 kg. Hlola ukusebenza kweSaksenda othathwe ngokwemiphumela yokwelashwa izinyanga ezi-4. Uma ngalesi sikhathi ngaphansi kwesilinganiso se-4% sesisindo sesilahlekile, ukulahleka kwesisindo okuzinzile kulesi siguli kungenzeka kakhulu ukuthi kungenzeki, umuthi uyamiswa.
Amanani aphakathi wokunciphisa isisindo ngokwemiphumela yokuhlolwa konyaka anikezwa kwimiyalo yokusetshenziswa kweSaksenda:
Study No. | Isigaba seziguli | Ukwehla kwesisindo okuyisilinganiso,% | |
ILiraglutide | placebo | ||
1 | Obese. | 8 | 2,6 |
2 | Ngokukhuluphala kanye noshukela. | 5,9 | 2 |
3 | U-Obese no-Apnea. | 5,7 | 1,6 |
4 | Ngokukhuluphala, okungenani i-5% yesisindo yehle ngokuzimela ngaphambi kokuthatha iLiraglutide. | 6,3 | 0,2 |
Uma unikezwe umjovo nokuthi umuthi ubiza malini, ukwehla kwesisindo okunjalo akukhona ukuhlaba umxhwele. I-Lyraglutidu nemiphumela yayo emvamisa emgudwini wokugaya ukudla awufaki ukuthandwa.
Imiphumela emibi
Iningi lemiphumela emibi ihlobene ngqo nomshini wesidakamizwa. Ngenxa yokuncipha kokugaya ukudla emasontweni okuqala okwelashwa ngeLyraglutide, kuvela imiphumela engemihle yesisu: ukuqunjelwa, isifo sohudo, ukwanda kwerhasi, ukubopha, izinhlungu ngenxa yokuqhuma, isicanucanu. Ngokusho kokubuyekezwa, ikota yeziguli izizwa icanusea ngezigaba ezahlukahlukene. Ukuphila kahle kuvama ukuthuthuka ngokuhamba kwesikhathi. Ngemuva kwezinyanga eziyisithupha zokudla ejwayelekile, zingama-2% kuphela iziguli ezikhalaza ngokuhlaselwa kwenhliziyo.
Ukunciphisa le miphumela emibi, umzimba unikezwa isikhathi sokujwayela i-Liraglutid: ukwelashwa kuqalwa ngo-0,6 mg, umthamo uyakhuphuka kancane kancane uvuseleleke. Isicanucanu akusithinti kabi isimo sezitho zomzimba ezihlanzekile. Kwezifo ezithathelwanayo zepheshana esiswini, ukuphathwa kwe-liraglutide akuvunyelwe.
Imiphumela emibi emibi yesidakamizwa echazwe kwimiyalo yokusebenzisa:
Imicimbi Emibi | Imvamisa yokwenzeka,% |
I-pancreatitis | ngaphansi kuka-1 |
Ukungezwani komzimba kwizakhi ze-liraglutide | ngaphansi kuka-0,1 |
Ukwehla komzimba njengendlela yokusabela ekunciphiseni ukumuncwa kwamanzi emgodini wokugaya ukudla kanye nokwehla kwesifiso sokudla | ngaphansi kuka-1 |
Insomnia | 1-10 |
I-Hypoglycemia ngenhlanganisela ye-liraglutide enamacwecwe e-sulfonylurea ne-insulin | 1-10 |
Ukuphazamiseka ukunambitheka, isiyezi ezinyangeni ezi-3 zokuqala zokwelashwa | 1-10 |
I-tachycardia emnyama | ngaphansi kuka-1 |
I-Cholecystitis | ngaphansi kuka-1 |
Isifo se-Gallstone | 1-10 |
Umsebenzi wezinso ongasebenzi kahle | ngaphansi kuka-0,1 |
Ezigulini ezinesifo se-yegilo, umphumela ongemuhle wesidakamizwa kulesi sitho waphawulwa. Manje uLiraglutid wenza olunye uvivinyo lokufaka ngaphandle ukuxhumeka kokuthatha umuthi ngomdlavuza we-thyroid. Amathuba okusebenzisa i-liraglutide ezinganeni nawo ayafundwa.
Umthamo
Isonto lokuqala le-liraglutide liphathwa ngethamo lika-0,6 mg. Uma umuthi ubekezelelwa kahle, ngemuva kwesonto umthamo uphindwe kabili. Uma kwenzeka imiphumela emibi iqhubeka, iqhubeka nokujova i-0.6 mg isikhashana ize izizwe ingcono.
Izinga lokuphakanyiswa komthamo olinconywayo ngu-0.6 mg ngeviki. Ku-mellitus yesifo sikashukela, umthamo ophelele ngu-1,2 mg, okuphezulu - 1,8 mg. Lapho usebenzisa i-Liraglutide kusuka ekukhuluphweni, umthamo uguqulwa ube ngu-3 mg kungakapheli amasonto ayi-5. Kuleli nani, iLyraglutide injekelwa izinyanga ezingama-4 kuya ku-12.
Ungawenza kanjani umjovo
Ngokusho kwemiyalo, imijovo yenziwa ngokungena esiswini, engxenyeni engaphandle yethanga, nengalo engenhla. Indawo yomjovo ingashintshwa ngaphandle kokunciphisa umphumela womuthi. ILyraglutide injekiwe ngasikhathi sinye. Uma isikhathi sokuphatha siphuthelwe, umjovo ungenziwa kungakapheli amahora ayi-12. Uma kudlule okuningi, lo mjovo ulahlekile.
ILiraglutide ifakwe ipeni yesirinji, elula kakhulu ukuyisebenzisa. Umthamo owuthandayo ungavele usethwe kwisisabalalisi esakhelwe ngaphakathi.
Ungawenza kanjani umjovo:
- khipha ifilimu evikela inaliti;
- khipha cap kusukela isibambo;
- faka inaliti esibambweni ngokusiguqula ngokwezikhathi;
- khipha cap inaliti;
- jikisa isondo (ungaphenduka kuzinhlangothi zombili) zokukhethwa komthamo ekugcineni kwesibambo uye endaweni oyifunayo (umthamo uzokhonjiswa efasiteleni eliphikisayo);
- faka inaliti ngaphansi kwesikhumba, isibambo sime mpo;
- cindezela inkinobho uyibambe kuze kuvele u-0 ewindini;
- khipha inaliti.
Analogs of Liraglutida
Ukuvikelwa kobunikazi kweLiraglutide kuphelelwa yisikhathi ngo-2022, kuze kube manje asikufanele ukulindela ukuvela kwama-analogues ashibhile eRussia. Njengamanje, inkampani yakwa-Israyeli iTeva izama ukubhalisa isidakamizwa ngento efanayo esebenzayo, ekhiqizwa ubuchwepheshe bayo. Kodwa-ke, iNovoNordisk iyakuphikisa ngentshiseko ukubukeka kohlobo oluthile. Le nkampani ithi inqubo yokukhiqiza iyinkimbinkimbi kakhulu kangangokuba kuzoba nzima ukuthola izilinganiso ezifanayo. Lokho wukuthi, kungahle kube umuthi onamandla ahluke ngokuphelele noma ngokujwayelekile ngokuntuleka kwezindawo ezidingekayo.