Leha ho na le khetho e kholo ea lithethefatsi tse fokotsang tsoekere, sesebelisoa se hantle sa ho laola glycemia ha se e-so fumanoe. Vildagliptin ke e 'ngoe ea lithethefatsi tsa mehleng ena tsa antidiabetes. Ha e na litla-morao tse fokolang feela: ha e bake boima ba 'mele le hypoglycemia, ha e senye ts'ebetso ea pelo, sebete le liphio, empa e boetse e eketsa bokhoni ba lisele tsa beta ho hlahisa insulin.
Vildagliptin ke sesebelisoa se eketsang nako ea bophelo ea li-insretin - lihormone tsa tlhaho tsa mokokotlo. Ho ea ka lingaka, ntho ena e ka sebelisoa ka katleho le lefu la tsoekere le nako e telele methating ea pele ea lefu lena, ho kenyelletsa le karolo ea kalafo e kopaneng.
Mokhoa oa vildagliptin o fumanoe joang
Tlhahisoleseling ea pele mabapi le li-insretin e hlahile lilemo tse fetang 100 tse fetileng, morao koana ka 1902. Maemo a ne a arotsoe ho tsoa mpeng ea mala le ho bitsoa li-secretins. Joale bokhoni ba bona ba ho susumetsa ho lokolloa ha li-enzyme ho tsoa makhophong a hlokahalang bakeng sa ho sila lijo bo ile ba fumanoa. Lilemo tse 'maloa hamorao, ho bile le litlhahiso tsa hore li-secretions li ka ama le ts'ebetso ea li-hormone tsa tšoelesa. Ho ile ha fumaneha hore ho bakuli ba nang le "glucosuria", ha ba nka karolo ea "insretin" ea pele, tekanyo ea tsoekere ka har'a urine e fokotseha haholo, molumo oa moroto oa fokotseha, 'me bophelo bo botle boa ntlafala.
Ka 1932, hormone e ile ea fumana lebitso la eona la sejoale - glucose-insulinotropic polypeptide (HIP). E ile ea fumaneha hore e hlophisitsoe ka har'a lisele tsa mucosa tsa duodenum le jejunum. Ka 1983, li-peptides tse peli tse tsoekere (glucagon-peptides (GLPs)) li ne li qheletsoe ka thoko Ho ile ha fumaneha hore GLP-1 e baka secretion ea insulin ha e arabela ts'ebeliso ea tsoekere, mme secretion ea eona e fokotsehile ho batho ba lefu la tsoekere.
Ketso ea GLP-1:
Lefu la tsoekere le khatello e matla e tla ba ntho ea khale
- Ts'oarelo ea tsoekere -95%
- Ho felisoa ha vein thrombosis - 70%
- Ho felisa ho otla ha pelo e matla -90%
- Ho tlosa khatello e phahameng ea mali - 92%
- Keketseho ea matla mots'eare, ho ntlafatsa boroko bosiu -97%
- e susumetsa ho lokolloa ha insulin ho bakuli ba nang le lefu la tsoekere;
- e lelefatsa boteng ba lijo ka mpeng;
- e fokotsa tlhokeho ea lijo, e thusa ho fokotsa boima ba 'mele;
- e na le phello e ntle pelong le methapong ea mali;
- e fokotsa tlhahiso ea "glucagon" makhophong - hormone e fokotsang ketso ea insulin.
E petsoha kahare ho enzyme DPP-4, e teng ka har'a endothelium ea capillaries e kenang ka har'a mucosa ea mala, kaha sena se nka metsotso e 2.
Tšebeliso ea bongaka ea liphumano tsena e qalile ka 1995 ke k'hamphani ea meriana e bitsoang Novartis. Bo-rasaense ba ile ba khona ho khetholla lintho tse sitisang mosebetsi oa enzyme ea DPP-4, ke ka lebaka leo nako ea bophelo ea GLP-1 le HIP e ileng ea eketseha ka makhetlo a 'maloa, mme tlhahiso ea insulin le eona e ile ea eketseha. Ntho ea pele e tsitsitseng ea lik'hemik'hale e nang le mochini oa ts'ebetso o fetisitseng tlhahlobo ea polokeho e ne e le vildagliptin. Lebitso lena le amohetse leseli le lengata: mona ke sehlopha se secha sa li-hypoglycemic agents "glyptin" le karolo ea lebitso la moetsi oa eona Willhower, le sesupo sa bokhoni ba lithethefatsi ho fokotsa glycemia "gly" esita le poleloana ea "e", kapa dipeptidylamino-peptidase, enzyme haholo DPP -4.
Ketso ea vildagliptin
Qalo ea mehla ea li-incretin kalafo ea lefu la tsoekere e nkoa e le selemo sa 2000, ha monyetla oa ho thibela DPP-4 o bonts'oa pele ho Congress of Endocrinologists. Ka nako e khuts'oane, vildagliptin e fumane boemo bo matla litekanyetsong tsa kalafo ea lefu la tsoekere linaheng tse ngata tsa lefats'e. Russia, ntho ena e ngolisitsoe ka 2008. Hona joale vildagliptin e kenngoa lenaneng la meriana ea bohlokoa kamehla.
Katleho e potlakileng joalo e bakiloe ke thepa e ikhethang ea vildagliptin, e netefalitsoeng ke litholoana tsa lithuto tse fetang 130 tsa machabeng.
Le lefu la tsoekere, sethethefatsi se u lumella ho:
- Ntlafatsa taolo ea glycemic. Vildagliptin ka tekanyetso ea letsatsi le letsatsi ea 50 mg e thusa ho fokotsa tsoekere ka mor'a ho ja ka karolelano ea 0,9 mmol / L. Glycated hemoglobin e fokotseha ka karolelano ea 1%.
- Etsa hore khaba ea glucose e be bonolo ka ho felisa litlhoro. Glycemia e phahameng ea postprandial e fokotseha ka hoo e ka bang 0,6 mmol / L.
- Tšepahala fokotsa khatello ea mali ea mots'eare le bosiu ka likhoeli tse tšeletseng tsa kalafo.
- Ntlafatsa metabolism ea lipid haholo ka ho fokotsa khatello ea methapo ea methapo ea methapo. Bo-rasaense ba nka phello ena e le e eketsang, e sa amaneng le ntlafatso ea matšeliso a lefu la tsoekere.
- Fokotsa boima le thekeng ho bakuli ba batenya haholo.
- Vildagliptin e tšoauoa ka mamello e ntle le polokeho e kholo. Likarolo tsa hypoglycemia nakong ea ts'ebeliso ea eona li fumaneha seoelo: kotsi e ka makhetlo a 14 ho feta ha u nka litlatsetso tsa setso tsa sulfonylurea.
- Setlhare se tsamaea hantle le metformin. Ho bakuli ba nkang metformin, ho eketsoa ha 50 mg ea vildagliptin kalafong ho ka fokotsa le ho feta GH ka 0,7%, 100 mg ka 1.1%.
Ho ea ka litaelo, ketso ea Galvus, lebitso la khoebo la vildagliptin, ka kotloloho e ipapisitse le matla a lisele tsa pancreatic beta le maemo a tsoekere. Mofuteng oa pele oa lefu la tsoekere le mofuteng oa 2 oa lefu la tsoekere le karolo e kholo ea lisele tse senyehileng tsa beta, vildagliptin ha e na matla. Bathong ba phetseng hantle le ho diabetes ba nang le tsoekere e tloaelehileng, e ke ke ea baka boemo ba hypoglycemic.
Hona joale, vildagliptin le li-analogues tsa eona li nkoa e le lithethefatsi tsa mola oa bobeli kamora metformin. Li ka atleha ho khutlisa tse tsoang teng tse atileng haholo sulfonylurea, le tsona li matlafatsang motsoako oa insulin, empa li sa bolokehe haholo.
Pharmacokinetics ea lithethefatsi
Matšoao a Pharmacokinetic a vildagliptin ho tsoa litaelo tse tla sebelisoa:
| Letšoao | Boholo ba tšebeliso | |
| Bioavailability,% | 85 | |
| Nako e hlokahalang ho fihlela tlhoro ea tlhoro e maling, min. | ho itima lijo | 105 |
| kamora ho ja | 150 | |
| Mekhoa ea ho tlosa 'meleng,% vildagliptin le metabolites ea eona | liphio | 85, ho kenyelletsa 23% e sa fetoheng |
| mala | 15 | |
| Phetoho e fokotsang tsoekere phokotsong ea sebete,% | bonolo | -20 |
| tekano | -8 | |
| boima | +22 | |
| Fetoha ho nka khato haeba mosebetsi o sa sebetseng oa renal,% | E matlafatsoa ke 8-66%, ha e ea its'etleha ka tlolo ea tlolo ea molao. | |
| Pharmacokinetics ho batho ba tsofetseng ba tsoekere | Keketseho ea vildagliptin e nyolohela ho 32%, phello ea lithethefatsi ha e fetohe. | |
| Tšusumetso ea lijo ho monkeloeng le katleho ea litafole | e lahlehile | |
| Matla a boima, bong, morabe ho katleho ea sethethefatsi | e lahlehile | |
| Half-life | 180, ha ea itšetleha ka lijo | |
Lithethefatsi tse nang le vildagliptin
Litokelo tsohle tsa vildagliptin li entsoe ka nepo ke Novartis, e tsetileng boikitlaetso le chelete e ngata ho nts'etsopele le ho hlahisa sehlahisoa 'marakeng. Matlapa a etsoa Switzerland, Spain, Jeremane. Haufinyane, ho lebelletsoe ho phatlalatsoa ha mohala Russia lekaleng la Novartis Neva. Motsoako oa litlhare, e leng vildagliptin ka boeona, o tsoa feela Switzerland.
Vildagliptin e na le lihlahisoa tse 2 tsa Novartis: Galvus le Galvus Met. Ntho e sebetsang ea Galvus ke vildagliptin feela. Matlapa a na le litekanyetso tse le 'ngoe tsa 50 mg.
Galvus Met ke motsoako oa metformin le vildagliptin matlapeng a le mong. Likhetho tsa litekanyetso tse fumanehang: 50/500 (mg sildagliptin / mg metformin), 50/850, 50/100. Khetho ena e u lumella ho nahana ka likarolo tsa lefu la tsoekere ho mokuli ea itseng ebe u khetha lethal dose le nepahetseng la meriana.
Ho latela litsebi tsa lefu la tsoekere, ho nka Galvus le metformin matlapeng a arohaneng ho theko e tlase: theko ea Galvus e ka ba li-ruble tse 750, metformin (Glucophage) ke li-ruble tse 120, Galvus Meta e batla e le li-ruble tse 1600. Leha ho le joalo, kalafo e kopaneng le Galvus Metom e ile ea amoheloa e le e sebetsang haholoanyane ebile e le bonolo.
Galvus ha e na analogues Russia e nang le vildagliptin, kaha ntho ena e ka tlisoa ke thibelo e sebetsang. Hajoale, ha e thibetsoe feela tlhahiso ea lithethefatsi leha e le life tse nang le vildagliptin, empa le nts'etsopele ea ntho ka boeona. Mohato ona o lumella moetsi hore a phete litšenyehelo tsa lithuto tse ngata tse hlokahalang ho ngolisa moriana leha e le ofe o mocha.
Matšoao a ho amoheloa
Vildagliptin e bontšoa feela lefu la tsoekere la mofuta oa 2. Ho latela litaelo, matlapa a ka khethoa:
- Ntle le metformin, haeba tekanyetso ea eona e lekaneng e sa lekana ho laola lefu la tsoekere.
- Ho nkela litokisetso tsa sulfonylurea (PSM) ho batho ba nang le lefu la tsoekere ka kotsi e eketsehileng ea hypoglycemia. Lebaka e kanna ea ba botsofe, likarolo tsa lijo, lipapali le mesebetsi e meng ea 'mele, neuropathy, ts'ebetso ea sebete e senyehileng le lits'ebetso tsa tšilo ea lijo.
- Litsebi tsa lefu la tsoekere le ho kula ho sehlopha sa PSM.
- Sebakeng sa sulfonylurea, haeba mokuli a batla ho lieha ho qala kalafo ea insulin kamoo ho ka khonehang.
- Joalo ka monotherapy (ke vildagliptin feela), haeba ho nka Metformin ho kopantsoe kapa ho sa khonehe ka lebaka la litlamorao tse mpe.
Ho amohela vildagliptin ntle le phoso ho lokela ho kopantsoe le lijo tsa lefu la tsoekere le thuto ea 'mele. Khanyetso e phahameng ea insulin ka lebaka la khatello e tlase ea khatello ea maikutlo le ho ja lijo tse sa laoleheng tsa lik'habohaedreite e ka fetoha tšitiso e ke keng ea lekanngoa ea ho fumana matšeliso bakeng sa lefu la tsoekere. Taeo e u lumella ho kopanya vildagliptin le metformin, PSM, glitazones, insulin.
Tekanyetso e khothalletsoang ea lithethefatsi ke 50 kapa 100 mg. Ho latela botebo ba lefu la tsoekere. Setlhare haholo se ama gypcemia ea postprandial, ka hona ho bohlokoa hore o noe tekanyetso ea 50 mg hoseng. Li-100 mg li arotsoe ka mokhoa o tšoanang li-reception tsa hoseng le tsa mantsiboea.
Khafetsa liketso tse sa batleheng
Monyetla o ka sehloohong oa vildagliptin ke litla-morao tse tlase tsa litlamorao nakong ea ts'ebeliso ea eona. Bothata bo ka sehloohong ho batho ba nang le lefu la tsoekere ba sebelisa PSM le insulin ke hypoglycemia. Leha e le hore khafetsa li feta ka mokhoa o bobebe, marotholi a tsoekere a kotsi ts'ebetsong ea methapo, ka hona a leka ho a qoba ka hohle kamoo a ka khonang. Litaelo tsa tšebeliso li tsebisa hore kotsi ea hypoglycemia ha u nka vildagliptin ke 0.3-0.5%. Bakeng sa papiso, sehlopheng sa taolo se sa sebeliseng sethethefatsi, kotsi ena e hakantsoe ho 0,2%.
Tšireletseho e phahameng ea vildagliptin e boetse e netefatsoa ke taba ea hore nakong ea lipatlisiso, ha ho lefu la tsoekere le hlokang ho tlosoa ha moriana ka lebaka la litla-morao tsa ona, joalo ka ha ho pakoa ke palo e tšoanang ea ho hana kalafo lihlopheng tse nkang vildagliptin le placebo.
Bakoa ba ka tlase ho 10% ba ile ba tletleba ka ho hlonepha habohloko, mme ba ka tlase ho 1% ba tletleba ka ho sokela, ho opeloa ke hlooho le ho ruruha hoa makhulo. Ho fumanoe hore tšebeliso ea nako e telele ea vildagliptin ha e lebise ho eketseheng ha litla-morao tsa litlamorao tsa eona.
Ho latela litaelo, likhokahano tsa ho sebelisa sethethefatsi sena ke hypersensitivity feela ho vildagliptin, bongoana, ho ima le ho nyeka. Galvus e na le lactose e le karolo e thusang, ka hona, ha e sa mamellehe, matlapa ana a haneloa. Galvus Met e lumelloa, kaha ha ho na lactose sebopeho sa eona.
Bongata
Liphetho tse ka bang teng ka lebaka la overdose ea vildagliptin ho latela litaelo:
| Motsoako, mg / letsatsi | Tlolo ea molao |
| ho fihla ho 200 | E mamelloa hantle, ha ho na matšoao. Kotsi ea hypoglycemia ha e eketsehe. |
| 400 | Bohloko ba mesifa Khafetsa - maikutlo a tukang kapa ho fifala letlalong, feberu, edema ea pherekano. |
| 600 | Ntle le tlolo ea molao e boletsoeng kaholimo, liphetoho tsa sebopeho sa mali lia khoneha: kholo ea popeho ea kinine, protheine ea C-reactive, AlAT, myoglobin. Matšoao a laboratori a fetoha butle butle ka mor'a ho tlohela moriana. |
| tse fetang 600 | Litlamorao tsa 'mele ha li e-so ithutoe. |
Haeba ho hlokahala hore motho a sebelise moriti o mongata, ho itlhoekisa ka mpeng le kalafo ea matšoao. Li-metabolites tsa Vildagliptin li hlahisoa ke hemodialysis.
Ka kopo hlokomela: overdose ea metformin, e 'ngoe ea likarolo tsa Galvus Meta, e eketsa kotsi ea lactic acidosis, e' ngoe ea mathata a kotsi a lefu la tsoekere.
Vildagliptin analogues
Kamora vildagliptin, ho fumanoe lintho tse ling tse 'maloa tse ka thibelang DPP-4. Kaofela ha tsona ke lipapatso:
- Saksagliptin, lebitso la khoebo Onglisa, mohlahisi Astra Zeneka. Motsoako oa saxagliptin le metformin o bitsoa Comboglize;
- Sitagliptin e fumaneha litokisetsong tsa Januvius ho tsoa k'hamphaning Merck, Xelevia ea Berlin-Chemie. Sitagliptin e nang le metformin - lintho tse sebetsang tsa matlapa a likarolo tse peli Janumet, analog ea Galvus Meta;
- Linagliptin e na le lebitso la khoebo Trazhenta. Moriana ona ke "brainchild" ea k'hamphani ea Jeremane Beringer Ingelheim. Linagliptin plus metformin ka har'a letlapa le le leng le bitsoa Gentadueto;
- Alogliptin ke karolo e sebetsang ea matlapa a Vipidia, a entsoeng USA le Japane ke Takeda Pharmaceuticals. Motsoako oa alogliptin le metformin o etsoa tlas'a letšoao la Vipdomet;
- Gozogliptin ke eona feela analogue ea lapeng ea vildagliptin. Ho reriloe ho e lokolla ke Satereks LLC. Potoloho e felletseng ea tlhahiso, ho kenyelletsa le ntho ea pharmacological, e tla etsoa seterekeng sa Moscow. Ho latela liphetho tsa liteko tsa tleliniking, polokeho le katleho ea gozogliptin e ne e le haufi le vildagliptin.
Ka lifekthering tsa Russia, o ka reka Ongliz (theko ea thupelo ea khoeli le khoeli e ka ba li-ruble tse 1800), Combogliz (ho tloha li-ruble tse 3200), Januvius (li-ruble tse 1500), Kselevia (li-ruble tse 1500), Yanumet (ho tloha 1800), Trazhent ( 1700 rub.), Vipidia (ho tloha ho 900 rub.). Ho latela palo ea litekolo, ho ka pheha khang ea hore maikutlo a tsebahalang ka ho fetisisa a Galvus ke Januvius.
Lingaka li hlahloba ka vildagliptin
Lingaka li nka vildagliptin haholo. Ba bitsa melemo ea moriana ona ka tlhaho ea ts'ebetso ea bona, mamello e ntle, phello e phehellang ea hypoglycemic, kotsi e tlase ea hypoglycemia, melemo e eketsehileng ka mokhoa oa ho hatella nts'etsopele ea microangiopathy le ho ntlafatsa maemo a marako a likepe tse kholo.
Vildagliptin, ehlile e phahamisa theko ea kalafo haholo, empa maemong a mang (khafetsa hypoglycemia) ha ho na mokhoa o mong o loketseng. Tšusumetso ea lithethefatsi e nkuoa e lekana le metformin le PSM, ha nako e ntse e feta, matšoao a metabolism ea carbohydrate a ntlafala hanyane.
Hape bala sena:
- Matlapa a Glyclazide MV ke lithethefatsi tse tsebahalang haholo ho batho ba lefu la tsoekere.
- Matlapa a Dibicor - melemo ea ona ke efe ho bakuli ba nang le lefu la tsoekere (melemo ea bareki)
