Litokisetso tsa Thiazolidinedione - litšobotsi le likarolo tsa ts'ebeliso

Meriana ea sejoale-joale e sebelisa sehlopha se fapaneng sa lithethefatsi ho phekola lefu la tsoekere la mofuta oa 2.

E 'ngoe ea lihlopha tsena ke thiazolidinediones, e nang le phello e ts'oanang le metformin.

Ho lumeloa hore, ha ho bapisoa le ntho e sebetsang ka holimo, li-thiazolidinediones li sireletsehile.

Phekolo ee e tšoaroa joang?

Phekolo ea sejoale-joale ea lefu la tsoekere ke mekhoa e mengata.

Mehato ea kalafo e kenyelletsa thupelo ea bongaka, ho latela lijo tse thata, kalafo ea 'mele, kalafo e seng lithethefatsi le ts'ebeliso ea litlhare tsa setso tsa setso.

Phekolo ea lefu la tsoekere e kenyelletsa tšebeliso ea meriana e khethehileng ho fihlela sepheo se itseng sa kalafo.

Lipheo tsa phekolo ke:

• ho boloka palo ea insulin ea "hormone" maemong a hlokahalang,
• Sekhahla sa glucose e maling,
• tšitiso ea ho ntšetsa pele tšebetso ea methapo ea kutlo,
• ho se nke lehlakore ha lipontšo tsa mathata le litlamorao tse mpe.

Tlhahlobo ea kalafo e kenyelletsa tšebeliso ea lihlopha tse latelang tsa lithethefatsi:

1. Litokisetso tsa Sulfonylurea, tse etsang liperesente tse mashome a robong tsa lithethefatsi tsohle tse theolelang tsoekere. Matlapa a joalo a etsa hantle ho hanyetsa insulin.
2. Biguanides ke lithethefatsi tse nang le ntho e sebetsang e kang metformin. Karolo ena e na le phello e molemo ho theoleng boima ba 'mele, hape e thusa ho fokotsa tsoekere ea mali. Ha e le molao, ha e sebelisoe ha mosebetsi o sa sebetseng oa liphio le sebete, kaha o bokellana ka potlako litho tsena.
3. Li-inhibitors tsa alpha-glycosidase li sebelisoa prophylactically ho thibela nts'etsopele ea lefu la tsoekere la mofuta oa 2. Monyetla o ka sehloohong oa lithethefatsi tsa sehlopha sena ke hore ha li lebise ponahalong ea hypoglycemia. Lithethefatsi tse khabisitsoeng li na le phello e molemo ho ho fetoleng ha boima ba 'mele, haholo ha phekolo ea lijo e lateloa.
4. Li-Thiazolidcediones li ka sebelisoa e le lithethefatsi tse ka sehloohong bakeng sa kalafo ea methapo kapa hammoho le lithethefatsi tse ling tse theolelang tsoekere. Kameho e kholo ea matlapa ke ho eketsa kutloisiso ea lithane ho insulin, ka ho etsa joalo ho hanyetsa ho hanyetsa. Lithethefatsi tsena ha li sebelisoe ho nts'etsopele mofuta oa lefu la tsoekere la mofuta oa 1, hobane li ka sebetsa feela ho na le insulin, e hlahisoang ke manyeme.

Ntle le moo, ho sebelisoa meglitinides - meriana e eketsang secretion ea insulin, ka hona e ama lisele tsa pancreatic beta.

Phokotseho ea litekanyetso tsa tsoekere e bonoa e se e le metsotso e leshome le metso e mehlano ka mor'a ho nka pilisi.

Polokeho

Thiazolidinediones e hlahisa litlamorao ka ho fokotsa ho hanyetsa ha insulin. Ho na le li-thiazolidinediones tse fumanehang 'marakeng - rosiglitazone (Avandia) le pioglitazone (Actos). Troglitazone e bile ea pele sehlopheng sa eona, empa e ile ea hlakoloa hobane e baka ts'ebetso ea sebete sa hae. Lithethefatsi li ka sebelisoa ka bobeli e le monotherapy, hammoho le lithethefatsi tse ling.

Mokhoa oa ketso. Li-Thiazolidinediones li eketsa kutloisiso ea insulin ka ho etsa lintho ka sesepa sa adipose, mesifa le sebete, moo li eketsang tšebeliso ea tsoekere le ho fokotsa sebopeho sa eona (1,2). Mokhoa oa ts'ebetso ha o utloisisoe ka botlalo. Li kenya mofuta o le mong kapa tse 'maloa tsa li-receptor tse etsang hore matla a fetele pele ho feta (RAPP) a sebetsang ka tsela e atisang ho ata, ao ka nako eo, a laolang polelo ea liphatsa tsa lefutso (3).

Ho sebetsa hantle Li-pioglitazone le rosiglitazone li na le ts'ebetso e ts'oanang kapa katleho e nyane joaloka basebelisi ba bang ba hypoglycemic. Boleng bo bohareng ba hemoglobin ea glycosylated ha e nka rosiglitazone e fokotseha ka 1,2-1,5%, mme khatello ea lipoprotein e phahameng le e tlase e eketseha. Ho ipapisitsoe le datha, ho ka nahanoa hore kalafo ka thiazolidatediones ha e tlase ho katleho ea phekolo ea metformin, empa ka lebaka la theko e phahameng le litlamorao, meriana ena ha e sebelisoe kalafo ea pele ea lefu la tsoekere.

Matla a tlisoang ke thiazolidinediones tsamaisong ea pelo le pelo. Lithethefatsi sehlopheng sena li ka ba le ts'ebetso ea anti-inflammatory, antithrombotic, and anti-atherogenic, empa leha ho le joalo, tlhaiso-leseling e bonts'ang kotsi e fokolitsoeng ea lefu la pelo ha e khahlise, 'me palo ea litlamorao e ea tšosa (4,5,6,7). Liphetho tsa tlhahlobo ea meta li bonts'a tlhokeho ea tlhokomeliso ts'ebelisong ea thiazolidatediones le rosiglitazone ka ho khetheha, ho fihlela data e ncha e tiisa kapa e hana data e mabapi le cardiotoxicity. Ho feta moo, hoa hlokahala ho nahana ka monyetla oa ho holofala ha pelo. Boemong bona, ha ho kgothaletswe ho sebelisa rosiglitazone haeba ho khonahala ho sebelisa lithethefatsi tse sireletsehileng (metformin, sulfonylureas, insulin).

Lipids. Nakong ea phekolo e nang le pioglitazone, khatello ea lipids-low-density lipids e lula e sa fetohe, mme ka kalafo ka rosiglitazone, keketseho ea khatello ea karolo ena ea lipids e bonoa ke karolelano ea 8-16%. (3)

Tsamaiso ea polokeho |Likarolo tsa thiazolidinediones

Thiazolidinediones, ka mantsoe a mang glitazones, ke sehlopha sa lithethefatsi tse theolelang tsoekere tse ikemiselitseng ho eketsa phello ea tlhaho ea insulin. Bakeng sa kalafo ea lefu la tsoekere mellitus e qalile ho sebelisoa haufinyane - ho tloha ka 1996. Li fanoa ka tieo ho latela lengolo la ngaka.

Glitazones, ntle le ts'ebetso ea hypoglycemic, e na le phello e ntle tsamaisong ea pelo le pelo. Ketsahalo e latelang e ile ea bonoa: antithrombotic, antiatherogenic, anti-inflammatory. Ha u nka thiazolidinediones, boemo ba hemoglobin ea glycated bo fokotseha ka karolelano ka 1.5%, mme boemo ba HDL bo eketseha.

Kalafo e nang le lithethefatsi tsa sehlopha sena ha e sebetse ho feta kalafo e nang le Metformin. Empa ha e sebelisoe sethaleng sa pele ka lefu la tsoekere la mofuta oa 2. Sena se bakoa ke ho teba ha litlamorao le theko e phahameng. Kajeno, glitazones e sebelisoa ho theola glycemia e nang le sulfonylurea derivatives le metformin. Li ka fanoa ka bobeli ka thoko le lithethefatsi ka bomong, le hammoho.

Melemo le likotsi

Har'a likarolo tsa lithethefatsi ho na le tse ntle le tse mpe:

• eketsa boima ba 'mele ka 2 kg ka kakaretso,
• Lenane le leholo la litlamorao
• Ntlafatsa profil ea lipid
• Ka katleho ama ho hanyetsa insulin
• ts'ebetso e tlase ea ho fokotsa tsoekere ha e bapisoa le metformin, lisebelisoa tse tsoang sulfonylurea,
• khatello ea mali e tlase
• fokotsa lintho tse amang nts'etsopele ea atherosulinosis,
• boloka metsi, 'me ka lebaka leo, menyetla ea ho nyekeloa ke pelo e eketseha,
• fokotsa masapo a masapo, ho eketsa kotsi ea ho robeha,
• hepatotoxicity.

Mokhoa oa ketso

Thiazolidinediones e sebetsa ho li-receptors, tse ntlafatsang ho ajoa le ho bokelloa ha tsoekere ke lisele. Ketso ea lihormone ka har'a sebete, adipose tishu le mesifa ea ntlafala. Ho feta moo, tšusumetso ho boemo ba matšoao a mabeli a ho qetela e phahame haholo.

Li-glitazones ha li khothalletse tlhahiso ea insulin ke lisele tsa "pancreatic". Phokotso ea ts'ebetso e fihlelleha ka ho fokotsa ho hanyetsa ha insulin ea lisele tsa pherekano le ts'ebeliso e matla ea tsoekere ke linama. Phello e theolelang tsoekere, joalo ka molao, e etsahala butle butle. Tekanyo ea "glucose" e potlakileng haholo e bonoa feela ka mor'a ho qeta likhoeli tse peli. Phekolo e tsamaisana le ho nona.

Ho na le ntlafatso taolong ea metabolic ka ho theola tsoekere ea mali. Ha e kopantsoe le metformin le sulfonylurea derivatives, taolo ea glycemic e ntlafatsoa ho bakuli ba nang le lefu la tsoekere la 2, hammoho le maemo a bohlokoa a lihormone tsa plasma. Glitazones e sebetsa feela boteng ba insulin.

Litekanyetso tsa Pharmacokinetic li ka fapana ho ea ka moriana. Se ke oa ba ama bong le lilemo tsa mokuli. Ka tšenyo ea sebete ho bakuli, e fetola li-pharmacokinetics.

Matšoao le contraindication

Li-Thiazolidinediones li laeloa lefu la tsoekere le sa ts'epheng insulin (lefu la tsoekere la 2):

• joalo ka monotherapy ho bakuli ba laolang boemo ba glycemia ntle le meriana (lijo le ho ikoetlisa),
• e le pheko e kopanetsoeng hammoho le litokisetso tsa sulfonylurea,
• e le kalafo e kopanetsoeng le metformin bakeng sa taolo e lekaneng ea glycemic,
• joalo ka kalafo e potlakileng ea "glitazone + metformin + sulfonylurea",
• motswako le insulin
• motswako le insulin le metformin.

Har'a lintho tse hanyetsanang mabapi le ho sebelisa meriana:

• motho ka mong,
• boimana / ho nyeka
• lilemo tse 18
• ho hloleha ha sebete - ho teba le ho teba ha matla,
• lefu la pelo le matla
• ho se sebetse hantle haholo ke matla.

Puo ea video mabapi le litokisetso tsa sehlopha sa thiazolidatedione:

Litlamorao

Tse ling tsa litlamorao ka mor'a ho nka thiazolidinediones ke:

• ho basali - ho hloka molao ho ea khoeling,
• ho hloleha ha pelo,
• tlolo ea boemo ba lihormone,
• ho eketseha ha li-enzyme tsa sebete,
• phokolo ea mali
• hypoglycemia,
• hypercholesterolemia,
• hlooho e bohloko le ho tsekela,
• boima ba 'mele
• takatso e matla ea lijo
• bohloko ba ka mpeng, ho hlonama,
• matlalo a letlalo, haholo-holo urticaria,
• ho ruruha
• ho tepella ho eketsehileng
• ho sitisoa hoa pono
• benign formations - polyps le cysts,
• tšoaetso e phahameng ea phepelo ea pampiri.

Nakong ea phekolo, boima le matšoao li hlahlojoa tse bontšang ho boloka metsi. Tlhokomelo ea ts'ebetso ea sebete e boetse e etsoa. Tšebeliso ea lino tse tahang ha e ame taolo ea glycemic haholo.

Tekanyetso, mokhoa oa tsamaiso

Li-glitazones li nkuoa ntle le lijo. Phetoho ea litekanyetso bakeng sa batho ba tsofetseng e nang le ho kheloha hanyane ka har'a sebete / liphio ha e etsoe. Mokhahlelo oa ho qetela oa bakuli o fuoe tšebeliso e tlase ea lithethefatsi letsatsi le letsatsi. Litekanyetso li beoa ke ngaka ka bonngoe.

Ho qala ha kalafo ho qala ka tekanyetso e tlase. Haeba ho hlokahala, e eketseha ka likhakanyo ho latela moriana. Ha e kopantsoe le insulin, litekanyetso tsa eona li lula li sa fetoha kapa li fokotseha ka litlaleho tsa maemo a hypoglycemic.

Lenane la Lithethefatsi la Thiazolidinedione

Baemeli ba babeli ba glitazone ba fumaneha 'marakeng oa litlhare kajeno - rosiglitazone le pioglitazone. Ea pele sehlopheng sena e ne e le troglitazone - e ile ea hlakoloa haufinyane ka lebaka la nts'etsopele ea ts'enyo e matla ea sebete.

Lithethefatsi tse thehiloeng ho rosiglitazone li kenyeletsa tse latelang:

• 4 mg avandia - Spain,
• DIgnitazone 4 mg - Ukraine,
• Roglit ho 2 mg le 4 mg - Hungary.

Lithethefatsi tse thehiloeng ho piogitazone li kenyelletsa:

• Glutazone 15 mg, 30 mg, 45 mg - Ukraine,
• Nilgar 15 mg, 30 mg - India,
• Dropia-Sanovel 15 mg, 30 mg - Turkey,
• Pioglar 15 mg, 30 mg - India,
• Pyosis 15 mg le 30 mg - India.

Ho sebelisana le meriana e meng

1. Rosiglitazone. Tšebeliso ea joala ha e ame taolo ea glycemic. Ha ho na tšebelisano ea bohlokoa le lithibela-pelehi tsa litafole, Nifedipine, Digoxin, Warfarin.
2. Peoglitazone. Ha e kopantsoe le rifampicin, phello ea pioglitazone e ea fokotsoa. Mohlomong ho fokotseha hanyane ho katleho ea bokhoni ba thibelo ea bokhachane ha u ntse u sebelisa lithibela-mafu. Ha o sebelisa ketoconazole, taolo ea glycemic hangata e hlokahala.

Li-Thiazolidinediones ha li fokotse maemo a tsoekere feela, empa hape li ama tsamaiso ea methapo ea pelo. Ntle le melemo, ba na le likarolo tse 'maloa tse mpe, tse atileng haholo ke nts'etsopele ea ho nyekeloa ke pelo le ho fokotseha ha masapo a masapo.

Li sebelisoa ka mafolofolo kalafong e rarahaneng, ts'ebeliso ea thiazolidatediones bakeng sa thibelo ea kholo ea lefu e hloka ho ithuta ho eketsehileng.

Melao ea kopano

1. Lithethefatsi tsa pele tse khethiloeng tsa lefu la tsoekere la mofuta oa 2 ho bakuli ba fetang boima ba 'mele ke metformin kapa lithethefatsi tse tsoang sehlopheng sa thiazolidinediones.
   
2. Bakeng sa bakuli ba nang le boima ba 'mele bo tloaelehileng, ho khethoa ho litokisetso tsa sulfonylurea kapa meglitinides.
   
3. Ka ho se sebetse hantle ha u sebelisa pilara e le 'ngoe, e le molao, ho kopantsoe litlhare tse peli (tse sa atiseng ho ba tse tharo). Motsoako o sebelisoang khafetsa:
   
   • sulfonylurea + metformin,
   • metformin + thiazolidatedione,
   • metformin + thiazolidinedione + sulfonylurea.
     

Litokisetso tsa Sulfonylurea

Tse tummeng haholo ke lithethefatsi tse amanang le litlamorao tsa sulfonylurea (ho fihlela ho 90% ea lithethefatsi tsohle tse fokotsang tsoekere). Ho lumeloa hore keketseho ea secretion ea insulin ke lithethefatsi tsa sehlopha sena hoa hlokahala ho hlola khanyetso ea insulin.

Litokisetso tsa skulonylurea ea bobeli li kenyeletsa:

• Gliclazide - e na le phello e phatlalalitsoeng mabapi le ho ts'oaroa ha methapo ea mali, phallo ea mali, e na le phello e molemo litlamong tsa lefu la tsoekere.
• Glibenclamide - e na le phello e matla ka ho fetisisa ea hypoglycemic. Hajoale, ho na le likhatiso tse ling tse ngata tse buang ka litlamorao tse mpe tsa sethethefatsi sena nakong ea mafu a pelo.
• Glipizide - e na le ts'ebetso e fokotsang tsoekere, empa nako ea ts'ebetso e khuts'oane ho feta ea glibenclamide.
• Glycidone - setlhare se le seng se tsoang sehlopheng sena, se laetsoeng bakuli ba nang le bothata ba ho leka-lekanya lefu la mmele. E na le nako e khuts'oane haholo ea ketso.

Litokisetso tsa skulonylurea ea boraro ea selemo li fanoa Glimeprimide:

• e qala ho nka khato pejana mme e ba le nako e telele ea ho pepeseha (ho fihlela lihora tse 24) ka tekanyetso e tlase,
• Monyetla oa ho nka moriana o le mong feela ka letsatsi,
• ha e fokotse secretion ka insulin nakong ea boikoetliso,
• e baka ho nts'oa ha insulin kapele ka lebaka la takatso ea lijo,
• e ka sebelisoa bakeng sa ho hloleha ha renal hantle,
• o na le kotsi e tlase ea hypoglycemia ha e bapisoa le lithethefatsi tse ling sehlopheng sena.

Bokhabane bo boholo ba litokisetso tsa sulfonylurea bo bonoa ho bakuli ba nang le lefu la tsoekere la mofuta oa 2, empa ka boima ba 'mele bo tloaelehileng.

Fana ka litlhare tsa sulfonylurea bakeng sa lefu la tsoekere la mofuta oa 2, ha lijo le ho ikoetlisa khafetsa li sa thusa.

Litokisetso tsa Sulfonylurea li hanyetsanoa: ho bakuli ba nang le lefu la tsoekere la mofuta oa 1, baimana le nakong ea lebele, ba nang le lefu le matla la sebete le liphio, ba nang le lefu la tsoekere. Tlhokomelo e khethehileng e lokela ho nkuoa haeba ho na le leqeba la ka mpeng, hammoho le ho bakuli ba febrile ba lemaletseng joala bo sa feleng.

Ho latela lipalo-palo, ka bomalimabe, ke karolo ea boraro feela ea bakuli e fumanang matšeliso a nepahetseng bakeng sa lefu la tsoekere ka ts'ebeliso ea sulfonylureas. Bakuli ba bang ba khothalletsoa ho kopanya lithethefatsi tsena le lithethefatsi tse ling tse kentsoeng, kapa ba fetohela kalafo ea insulin.

Motsoako o mong feela sehlopheng sena ke metformin, e liehisang tlhahiso le ho lokolloa ha tsoekere maling, e ntlafatsa tšebeliso ea tsoekere ka lithishu tse nang le moea, e ntlafatsa phallo ea mali, 'me e nolofatsa metabolism ea lipid. Matla a hypoglycemic a hlaha matsatsi a 2-3 kamora hore moriana a qale.Ka nako e ts'oanang, boemo ba glycemia bo potlakileng boa fokotseha, 'me takatso ea lijo ea fokotseha.

Karolo e khethollang ea metformin ke ho tsitsa, esita le ho theola boima ba 'mele - ha ho le ea mong oa baemeli ba bang ba hypoglycemic ea nang le sena.

Matšoao a ts'ebeliso ea metformin ke a mofuta oa "mellitus" ea 2 lefu la tsoekere ho bakuli ba nang le boima ba 'mele, prediabetes, ho se mamelle litokisetso tsa sulfonylurea.

Metformin e hanyetsanoa: ho bakuli ba nang le lefu la tsoekere la mofuta oa 1, baimana le nakong ea ho fepa, ba nang le lefu le matla la sebete le liphio, le mathata a lefu la tsoekere, a nang le tšoaetso e matla, le mafu afe kapa afe a tsamaeang le phepelo e lekaneng ea oksijene ho litho.

Alpha Glycosidase Inhibitors

Lithethefatsi tsa sehlopha sena li kenyeletsa acarbose le miglitol, e fokotsang ho phatloha ha lik'habohaedreite ka mala, e leng se tiisang ho kenngoa ha tsoekere butle butle maling. Ka lebaka lena, ho phahama ha tsoekere ea mali nakong ea ho ja ho felisoa, ha ho na kotsi ea hypoglycemia.

Tšobotsi ea lithethefatsi tsena ke katleho ea tsona ea ho ja limatlafatsi tse ngata tsa nama ea kolobe. Haeba lik'habohaedreite tse bonolo li ata lijong tsa mokuli, kalafo e nang le alpha-glycosidase inhibitors ha e fane ka phello e ntle. Mokhoa o boletsoeng oa ts'ebetso o etsa hore meriana ea sehlopha sena e sebetse hantle bakeng sa glycemia e potlakileng ea ho itima lijo le ho phahama ka sekhahla ka mor'a ho ja. Hape, lithethefatsi tsena ha li eketse boima ba 'mele.

Alpha-glycosidase inhibitors e bontšoa ho bakuli ba nang le lefu la tsoekere la mofuta oa 2 ka lijo le ho se sebetse hantle ka boiphihlelo ba hyperglycemia kamora ho ja.

Contraindication bakeng sa ts'ebeliso ea li-alpha-glycosidase inhibitors ke: lefu la tsoekere la ketoacidosis, cirrhosis, ho ruruha le ho sa foleng ha mala ka mpeng, ho kenella ka popelong ka mpeng ka ho eketseha ha khase, ho ruruha ha lesapo la mokokotlo, mokokotlo oa mokokotlo, hernias e kholo, ts'ebetso e mpe ea renal.

Thiazolidinediones (glitazones)

Lithethefatsi tse sehlopha sena li kenyeletsa pioglitazone, rosiglitazone, troglitazonetse fokotsang ho hanyetsa insulin, ho fokotsa ho ntšoa ha tsoekere maling, ho boloka tšebetso ea lisele tse hlahisang insulin.

Ketso ea lithethefatsi tsena e tšoana le ketso ea metformin, empa e amohuoa litšoaneleho tsa eona tse mpe - ntle le ho fokotsa khatello ea insulin, lithethefatsi tsa sehlopha sena li khona ho liehisa nts'etsopele ea mathata a renal le khatello ea methapo ea methapo, li ama metabolism e ntle ea lipid. Empa, ka lehlakoreng le leng, ha o nka glitazones, o lokela ho lekola ts'ebetso ea sebete ka linako tsohle. Hajoale, ho na le bopaki ba hore tšebeliso ea rosiglitazone e ka eketsa kotsi ea infyo ea myocardial le ho hloleha ha pelo le pelo.

Glitazones e bontšoa ho bakuli ba nang le lefu la tsoekere la mofuta oa 2 maemong a ho se sebetse hantle ha 'mele le ho ikoetlisa ka boits'oaro ba insulin.

Contraindication ke: mofuta oa lefu la tsoekere 1 mellitus, lefu la tsoekere, ho ima le ho nyeka, lefu le matla la sebete, ho se sebetse hantle ha pelo.

Meglitinides

Lithethefatsi tse sehlopha sena li kenyeletsa repaglinide le nateglinideho ba le phello e khuts'oanyane ea tsoekere. Meglitinides e laola boemo ba glucose kamora ho ja, e etsang hore ho se lumellane le lijo tse thata, hobane moriana o sebelisoa kapele pele ho lijo.

Karolo e khethollang ea meglitinides ke ho fokotseha ho phahameng ha tsoekere: ka mpeng e se nang letho ka 4 mmol / l, kamora ho ja - ka 6 mmol / l. Khokahano ea hemoglobin HbA1c ea glycated e fokotsehile ka 2%. Ka tšebeliso ea nako e telele ha u bake boima ba 'mele ebile ha u hloke khetho ea lethal dose. Keketseho ea phello ea hypoglycemic e bonoa ha u ntse u sebelisa joala le lithethefatsi tse ling.

Letšoao bakeng sa ts'ebeliso ea li-meglitinides ke mofuta oa tsoekere ea 2 maemong a khaello ea ho ja le ho ikoetlisa.

Miglitinides e hanyetsanoa: ho bakuli ba nang le mofuta oa 1 lefu la tsoekere, le lefu la tsoekere la ketoacidosis, basali baimana le ba anyesa, ka kutloisiso e eketsehileng ea lithethefatsi.

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Hypoglycemic kapa lithethefatsi tsa antidiabetesic ke meriana e fokotsang tsoekere ea mali mme e sebelisetsoa ho phekola lefu la tsoekere.

Hammoho le insulin, litokisetso tsa eona li loketse feela tšebeliso ea batsoali, ho na le metsoako e mengata ea maiketsetso e nang le phello ea hypoglycemic mme e sebetsa hantle ha e nkuoa ka molomo. Sesebelisoa se ka sehloohong sa lithethefatsi tsena ke mofuta oa lefu la tsoekere la mofuta oa 2.

Li-oral hypoglycemic (hypoglycemic) li ka khethoa ka tsela e latelang:

— sulfonylurea derivatives (glibenclamide, glycidone, glyclazide, glimepiride, glipizide, chlorpropamide),

— meglitinides (nateglinide, repaglinide),

— biguanides (buformin, metformin, phenformin),

— thiazolione (pioglitazone, rosiglitazone, ciglitazone, englitazone, troglitazone),

— alpha glucosidase inhibitors (acarbose, miglitol),

Melemo ea Hypoglycemic e tsoang ho sulfonylurea e fumanoe ka tšohanyetso. Bokhoni ba metsoako ea sehlopha sena ho fana ka phello ea hypoglycemic e fumanoe ho 50s, ha ho fokotseha ha tsoekere ea mali ho fumanoe ho bakuli ba fumanang lithethefatsi tsa antibacterial sulfonamide bakeng sa kalafo ea mafu a tšoaetsanoang. Mabapi le taba ena, patlo e ile ea qala ho fumana litokollo tsa sulfonamides tse nang le phello e boletsoeng ea hypoglycemic lilemong tsa 50s. Mokhoa oa pele o tsoang litlamong tsa sulfonylurea tse ka sebelisoang ho phekola lefu la tsoekere o ile oa etsoa. Lithethefatsi tsa pele tse joalo e ne e le carbutamide (Jeremane, 1955) le tolbutamide (USA, 1956). Mathoasong a bo-50. li-derivatives tsena tsa sulfonylurea li se li qalile ho sebelisoa tloaelong ea bongaka. Ka 60-70s. sulfonylureas ea moloko oa bobeli e hlahile. Moemeli oa pele oa litokisetso tsa sulfonylurea ea moloko oa bobeli, glibenclamide, o ile a qala ho sebelisoa ho phekola lefu la tsoekere ka 1969, ka 1970 glibornuride e ile ea qala ho sebelisoa, mme ka 1972, glipizide. Gliclazide le glycidone li hlahile hoo e ka bang ka nako e tšoanang.

Ka 1997, repaglinide (sehlopha sa meglitinides) e ile ea amoheloa bakeng sa kalafo ea lefu la tsoekere.

Nalane ea ts'ebeliso ea li-biguanides e qalile morao Mehleng e Bohareng, ha semela se ne se sebelisetsoa ho phekola lefu la tsoekere Galega officinalis (likhahla tsa french).

Thiazolidinediones (glitazones) o ile a kenella ts'ebetsong ea bongaka ka 1997. Setlhare sa pele se neng se lumeletsoe ho sebelisoa e le moemeli oa hypoglycemic e ne e le troglitazone, empa ka 2000 ts'ebeliso ea eona e ile ea thibeloa ka lebaka la hepatotoxicity e phahameng. Ho fihla joale, lithethefatsi tse peli tse tsoang sehlopheng sena li sebelisitsoe - pioglitazone le rosiglitazone.

Ketso sulfonylureas haholo-holo e amanang le ho hlohlona ha lisele tsa pancreatic beta, e tsamaeang le ts'usumetso le keketseho e kholo ea tlhahiso ea insulin.

Ka kalafo ea nako e telele le lihlahisoa tsa sulfonylurea, tšusumetso ea bona ea pele e matlafatsang ea secretion e nyamela. Ho lumeloa hore sena se bakoa ke ho fokotseha ha palo ea li-receptor liseleng tsa beta. Kamora ho phomola kalafong, karabelo ea lisele tsa beta ho ho sebelisa lithethefatsi tsa sehlopha sena ea khutlisoa.

Li-sulfonylureas tse ling le tsona li na le litlamorao tse eketsehileng. Litlamorao tsa extrapancreatic ha li na bohlokoa bo boholo ba kliniki, li kenyelletsa keketseho ea kutlo ea lisele tse itšetlehileng ka insulin ho kenya insulin le ho fokotseha ha sebopeho sa tsoekere maling. Mochine oa nts'etsopele ea litlamorao tsena o bakoa ke taba ea hore lithethefatsi tsena (haholo-holo glimepiride) li eketsa palo ea li-insulin tse amohelang insulin liseleng tsa sepheo, li ntlafatsa tšebelisano ea insulin-receptor, le ho khutlisa phetisetso ea lets'oao la postreceptor.

Ntle le moo, ho na le bopaki ba hore prizvodnye sulfonylureas e hlohlelletsa ho nts'oa ha somatostatin ebe ka tsela eo e thibela ho bolokoa ha glucagon.

Moloko oa ka: tolbutamide, carbamide, tolazamide, acetohexamide, chlorpropamide.

Moloko oa II: glibenclamide, glisoxepide, glibornuril, glycidone, glyclazide, glipizide.

Moloko oa III: glimepiride.

Hajoale, Russia, litokisetso tsa sulfonylurea tsa moloko oa pele ha li sebelisoe.

Phapang e kholo lipakeng tsa lithethefatsi tsa moloko oa bobeli le lintho tse tsoang molemong oa pele ke tšebetso e kholo (makhetlo a 50-100), e li lumellang hore li sebelisoe ka tekanyetso e tlase mme, ka hona, e fokotsa monyetla oa litlamorao. Baemeli ba ikemetseng ba li-sogonylureas tsa moloko oa 1 le oa 2 li fapana ka ts'ebetso le mamello. Kahoo, litekanyetso tsa letsatsi le letsatsi tsa lithethefatsi tsa molala oa pele - tolbutamide le chlorpropamide - 2 le 0,75 g, ka ho latellana, le lithethefatsi tsa moloko oa bobeli - glibenclamide - 0,02 g, glycvidone - 0,06-0.12 g. .

Litokisetso tsa Sulfonylurea li na le botebo le nako e fapaneng ea ts'ebetso, e khethang khetho ea lithethefatsi ha e laetsoe. Glibenclamide e na le phello e tsebahalang ka ho fetisisa ea hypoglycemic ho tsohle tse tsoang ho sulfonylurea. E sebelisoa e le mokhoa oa ho hlahloba phello ea hypoglycemic ea lithethefatsi tse sa tsoa etsoa. Tšusumetso e matla ea hypoglycemic ea glibenclamide e bakoa ke taba ea hore e na le tumellano e phahameng ka ho fetisisa bakeng sa liteishene tsa potasiamo tse itšetlehileng ka ATP tsa lisele tsa pancreatic beta. Hona joale, glibenclamide e hlahisoa ka bobeli ka sebopeho sa foromo ea litekanyetso tsa setso le sebopeho sa sebopeho sa micronized - sebopeho se hlophisitsoeng ka mokhoa o ikhethang oa glibenclamide se fanang ka profil e ntle ea profacokinetic le pharmacodynamic ka lebaka la ho kenella ka potlako le ka botlalo (bioavailability e ka bang 100%) mme e etsa hore ho khonehe ho sebelisa lithethefatsi ho litekanyetso tse nyane.

Gliclazide ke moemeli oa bobeli o atileng haholo oa molomo oa hypoglycemic ka mor'a glibenclamide. Ntle le taba ea hore gliclazide e na le phello ea hypoglycemic, e ntlafatsa methapo ea hematological, mali a rheological, e na le phello e ntle ho sisteme ea heestatic le microcirculation, mme e thibela nts'etsopele ea microvasculitis, ho kenyelletsa Tšenyo ea mokokotlo oa mokokotlo oa mokokotlo oa retina, e sitisa ho kopanngoa ha liplatelete, e eketsa haholo index ea ho se lumellane, e eketsa ts'ebetso ea heparin le fibrinolytic, e eketsa mamello ea heparin hape e bonts'a thepa ea antioxidant.

Glycvidone ke lithethefatsi tse ka laeloang ho bakuli ba nang le bothata ba ho hlaphoheloa ha renal hantle ke 5% feela ea metabolites e epeloang lipelong, tse ling (95%) - ka mala.

Glipizide, e nang le phello e boletsoeng, e beha kotsi e nyane haholo mabapi le karabelo ea hypoglycemic, kaha ha e phatsime ebile ha e na metabolites e sebetsang.

Lithethefatsi tsa molomo tsa antidiabetic ke lithethefatsi tse ka sehloohong bakeng sa kalafo ea mofuta oa tsoekere ea mofuta oa 2 lefu la tsoekere (e sa itšetlehang ka insulin) mme hangata li fuoe bakuli ba lilemo tse fetang 35 ntle le ketoacidosis, khaello ea phepo e nepahetseng, mathata kapa mafu a kopaneng a hlokang kalafo ea insulin kapele.

Litokisetso tsa sehlopha sa sulfonylurea ha li khothalletsoe ho bakuli bao, ka lijo tse nepahetseng, tlhoko ea letsatsi le letsatsi ea insulin e fetang li-unit tse 40. Hape, ha e ngoletsoe bakuli ba nang le mefuta e matla ea lefu la tsoekere mellitus (e nang le ho fokola haholo ha beta-cell), ba nang le nalane ea ketosis kapa lefu la tsoekere, ba nang le hyperglycemia ka holimo ho 13.9 mmol / L (250 mg%) ka mpeng e se nang letho le glucosuria e ngata nakong ea phekolo ea lijo.

Phetisetso ho kalafo ka lithethefatsi tsa sulfonylurea bakeng sa bakuli ba nang le lefu la tsoekere ba leng kalafo ea insulin ho ka khoneha haeba mathata a metabolism ea carbohydrate a lefisoa bakeng sa litekanyetso tsa insulin tsa likarolo tse ka tlase ho 40 / ka letsatsi. Ka tekanyetso ea insulin ho fihlela li-unit tse 10 / ka letsatsi, o ka fetohela hanghang kalafong ka lintho tse tsoang ho sulfonylurea.

Tšebeliso ea nako e telele ea lihlahisoa tsa sulfonylurea e ka baka nts'etsopele ea ho hanyetsa, e ka felisoang ka phekolo ea ho kopanya le litokisetso tsa insulin. Ho mofuta oa 1 lefu la tsoekere mellitus, ho kopana ha litokisetso tsa insulin le lintho tse tsoang ho sulfonylurea ho etsa hore ho khonehe ho fokotsa tlhokahalo ea letsatsi le letsatsi ea insulin mme ho thusa ho ntlafatsa boemo ba lefu lena, ho kenyelletsa le ho liehisa tsoelo-pele ea retinopathy, eo ka tsela e itseng e amanang le ts'ebetso ea angioprotective ea litokollo tsa sulfonylurea (haholo-holo moloko oa II). Ka nako e ts'oanang, ho na le matšoao a matla a bona a katleho ea atherogenic.

Ho feta moo, litlamorao tsa sulfonylurea li kopantsoe le insulin (motsoako o joalo o nkuoa o loketse haeba boemo ba mokuli bo sa ntlafale le IU e fetang 100 ea insulin ka letsatsi), ka linako tse ling li kopantsoe le biguanides le acarbose.

Ha u sebelisa lithethefatsi tsa sulfonamide hypoglycemic, ho lokela ho hopoloa hore li-antibacterial sulfonamides, li-anticoagulants tse sa tobang, butadion, salicylates, ethionamide, tetracyclines, chloramphenicol, cyclophosphamide e sitisa metabolism ea eona le ho eketsa katleho (hypoglycemia e ka hlaha). Ha lits'oants'o tsa sulfonylurea li kopantsoe le thiazide diuretics (hydrochlorothiazide, jj.) Le BKK (nifedipine, diltiazem, jj.), Ho qhekella ho etsahala ka litekanyetso tse kholo - li-thiazides li kena-kenana le phello ea lits'oaetso tsa sulfonylurea, mme lisele tsa BKK li sitisa phallo ea phallo ea calcium. litsoelesa.

Liphetho tsa sulfonylureas li matlafatsa phello le ho se mamelle joala, mohlomong ka lebaka la ho lieha ha oxidation ea acetaldehyde. Liphetoho tse kang tsa Antabuse li ka etsahala.

Lithethefatsi tsohle tsa sulfonamide hypoglycemic li khothalletsoa ho nooa hora e le 'ngoe pele ho lijo, e leng se etsang hore ho be le phokotseho e phahameng ea "postprandial" (kamora ho ja) glycemia. Tabeng ea ho teba ho matla ha dyspeptic phenomena, ho khothalletsoa ho sebelisa lithethefatsi tsena ka mor'a ho ja.

Litlamorao tse sa rateheng tsa litokollo tsa sulfonylurea, ho ekelletsa ho hypoglycemia, ke mathata a ho ferekanya kelello (ho kenyelletsa ho nyekeloa, ho hlatsa, lets'ollo), jaundice ea cholestatic, boima ba 'mele, ho khutla hoa leopopenia, thrombocytopenia, agranulocytosis, anemia ea methapo ea mokokotlo le lefu la mokokotlo la mmele. ho hlohlona, ​​erythema, dermatitis).

Ts'ebeliso ea litokisetso tsa sulfonylurea nakong ea kemolo ha e khothalletsoe, hobane boholo ba bona ke ba sehlopha sa C ho latela FDA (Tsamaiso ea Lijo le Lithethefatsi), kalafo ea insulin e laetsoe moo.

Bakuli ba tsofetseng ha ba khothalletsoe ho sebelisa lithethefatsi tse nkang nako e telele (glibenclamide) ka lebaka la kotsi e eketsehang ea hypoglycemia. Lekhetlong lena, ho loketse ho sebelisa li-derivatives tse khutšoanyane - gliclazide, glycidone.

Meglitinides - batsamaisi ba prandial (repaglinide, nateglinide).

Repaglinide ke derivative ea benzoic acid. Leha ho na le phapang ea sebopeho sa lik'hemik'hale ho tsoa litsing tsa sulfonylurea, e boetse e thibela lik'homphieutha tsa potasiamo tse itšetlehileng ka ATP ka har'a li-membrane tsa lisele tse sebetsang tse sebetsang tsa beta ea lisebelisoa tsa islet pancreatic, li baka ho putlama ha tsona le ho buloa ha liteishene tsa khalsiamo, ka ho etsa joalo ho tsosa phaello ea insulin. Karabelo ea insulinotropic lijong e ba teng ka nako ea metsotso e 30 kamora kopo mme e tsamaisoa le ho fokotseha ha tsoekere ea mali nakong ea lijo (khatello ea insulin pakeng tsa lijo ha e eketsehe). Joaloka lintho tse tsoang sulfonylurea, sephetho se ka sehloohong ke hypoglycemia. Ka hlokolosi, repaglinide e fuoe bakuli ba nang le ho hloleha hoa hepatic le / kapa renal.

Nateglinide ke derivative ea D-phenylalanine.Ho fapana le baemeli ba bang ba hypoglycemic ea molomo, phello ea nateglinide ho secretion ea insulin e potlakile, empa ha e phehelle. Nateglinide e sebelisoa haholo ho fokotsa tsoekere ea postprandial hyperglycemia ho lefu la tsoekere la mofuta oa 2.

Biguanides, e qalileng ho sebelisoa ho phekola lefu la tsoekere la mofuta oa 2 lilemong tsa 70, u se ke oa tsosa secretion ea insulin ka lisele tsa pancreatic beta. Phello ea bona e haholo-holo e emisoa ke thibelo ea gluconeogeneis ka har'a sebete (ho kenyeletsoa le glycogenolysis) le ts'ebeliso e matla ea glucose ke lithane tsa peripheral. E boetse e thibela ho kenella ha insulin le ho ntlafatsa ho tlama ha eona li-insulin receptor (hona ho eketsa ho monya ha tsoekere le metabolism ea eona).

Biguanides (ho fapana le litlamorao tsa sulfonylurea) ha e fokotse tsoekere ea mali ho batho ba phetseng hantle le ho bakuli ba nang le lefu la tsoekere la mofuta oa 2 kamora ho bolaoa ke tlala bosiu, empa e le fokotsa haholo keketseho ea lona kamora ho ja, ntle le ho baka hypoglycemia.

Hypoglycemic biguanides - metformin le ba bang - le tsona li sebelisoa bakeng sa mofuta oa "mellitus" oa tsoekere. Ntle le phello e fokotsang tsoekere, li-biguanides, ka tšebeliso ea nako e telele, li na le phello e ntle ho metabolism ea lipid. Lithethefatsi tsa sehlopha sena li inhibit lipogenesis (ts'ebetso eo ka eona tsoekere le lintho tse ling li fetoleloang mafura 'meleng), li hlahisang lipolysis (mokhoa oa ho arola lipids, haholo-holo li-triglycerides tse fumanehang mafura, ho li-acid tsa tsona tse mafura ka ketso ea enzyme ea lipase). ho theola boima ba 'mele. Maemong a mang, ts'ebeliso ea bona e tsamaisana le ho fokotseha ha litaba tsa triglycerides, cholesterol le LDL (e behiloeng ka mpeng e se nang letho) ka serum ea mali. Mofuteng oa 2 oa lefu la tsoekere, mathata a amanang le 'mele ea carbohydrate a kopantsoe le liphetoho tse boletsoeng metabolism ea lipid. Kahoo, bakuli ba nang le lefu la tsoekere la mofuta oa 85% ba na le boima ba 'mele bo eketsehileng. Ka hona, ka motsoako oa mofuta oa 2 lefu la tsoekere le boima bo feteletseng, lithethefatsi tse tloaelehileng tsa lipid metabolism lia bontšoa.

Letšoao bakeng sa tsamaiso ea li-biguanides ke mofuta oa lefu la tsoekere la 2 (haholo maemong a tsamaeang le botenya) ka ho se sebetse hantle hoa kalafo ea ho ja, hammoho le ho se sebetse hantle ha litokisetso tsa sulfonylurea.

Ha ho na le insulin, phello ea biguanides ha e hlahe.

Biguanides e ka sebelisoa hammoho le insulin ha e le teng ea ho e loantša. Motsoako oa lithethefatsi tsena tse tsoang ho sulfonamide derivatives o bontšoa maemong ao ho a latelang a sa faneng ka khalemelo e felletseng ea mathata a metabolic. Biguanides e ka baka nts'etsopele ea lactic acidosis (lactic acidosis), e thibelang ts'ebeliso ea lithethefatsi sehlopheng sena.

Biguanides e ka sebelisoa hammoho le insulin ha e le teng ea ho e loantša. Motsoako oa lithethefatsi tsena tse tsoang ho sulfonamide derivatives o bontšoa maemong ao ho a latelang a sa faneng ka khalemelo e felletseng ea mathata a metabolic. Biguanides e ka baka nts'etsopele ea lactic acidosis (lactic acidosis), e thibelang ts'ebeliso ea lithethefatsi tse ling sehlopheng sena.

Li-Biguanides li hanyetsitsoe boteng ba acidosis le tšekamelo ea eona (ho hlohlelletsa le ho eketsa ho bokellana ha lactate), maemong a tsamaeang le hypoxia (ho kenyelletsa le pelo le ho hloleha ho phefumoloha, karolo e mpe ea infyoction ea myocardial, khaello ea phepo ea methapo ea methapo, anemia).

Litla-morao tsa li-biguanides li bonoa khafetsa ho feta tse tsoang ho sulfonylurea (20% bapisoa le 4%), pele ho tsohle, litla-morao tsa litla-morao: tatso ea tšepe molomong, matšoao a dyspeptic, jj. Ho fapana le sulfonylurea derivatives, hypoglycemia ha u sebelisa biguanides (e.g metformin ) etsahala ka seoelo.

Lactic acidosis, eo ka linako tse ling e hlahang ha ho nkuoa metformin, e nkuoa e le bothata bo tebileng, ka hona, metformin ha ea lokela ho laeloa bakeng sa ho se sebetse hantle ha mokokotlo le maemo a lekang nts'etsopele ea lona - ho senyeha ha renal le / kapa ho sebetsa ha sebete, ho nyekeloa ke pelo, lefu la pelo.

Biguanides ha ea lokela ho laeloa ka nako e le 'ngoe le cimetidine, kaha ba qothisana lehlokoa ha ba ntse ba sebetsana le sechu la tubular ka liphio, e leng se ka lebisang ho cumulation ea biguanides, ho feta moo, cimetidine e fokotsa biotransformation ea biguanides ka har'a sebete.

Ho kopana ha glibenclamide (derivative of sulfonylurea ea moloko oa bobeli) le metformin (biguanide) e kopanya thepa ea bona hantle, e o lumella ho fihlela sephetho se lakatsehang sa hypoglycemic ka lethal dose le tlase la e 'ngoe le e' ngoe ea lithethefatsi ebe ka tsela eo o fokotsa kotsi ea litlamorao.

Ho tloha ka 1997, o ile a kenella ts'ebetsong ea bongaka thiazolidinediones (glitazones), motheo oa sebopeho sa lik'hemik'hale seo e leng selikalikoe sa thiazolidine. Sehlopha sena se secha sa li-antidiabetesic agents se kenyelletsa pioglitazone le rosiglitazone. Lithethefatsi tsa sehlopha sena li phahamisa kutloisiso ea li-tishu tse lebisitsoeng (mesifa, lithaelese tsa adipose, sebete) ho insulin, synthes ea lipid e ka tlase liseleng tsa mesifa le mafura. Li-Thiazolidinediones ke li-agonists tse ikhethileng tsa li-receptors tsa nyutlelie PPARγ (peroxisome proliferator-activated receptor-gamma). Ho batho, li-receptor tsena li fumaneha ho "li-tishu" tse etselitsoeng "tse bohlokoa bakeng sa ts'ebetso ea insulin: lithong tsa adipose, mesifa ea skeletal le sebete. Li-receptor tsa nyutlelie tsa PPARγ li laola phetisetso ea liphatsa tsa lefutso tse arabelang ka insulin tse amanang le taolo ea tlhahiso ea tsoekere, ho tsamaisa le ts'ebeliso. Ntle le moo, liphatsa tsa lefutso tse amanang le PPARγ li kentse letsoho ho metabolism ea mafura acid.

E le hore thiazolidinediones e fane ka phello ea eona, boteng ba insulin boa hlokahala. Lithethefatsi tsena li fokotsa khatello ea "insulin" le "sebete", li eketsa tšebeliso ea tsoekere e thehiloeng ho "insulin" hape li fokotsa phallo ea tsoekere maling, li-triglycerides tse tlase, li eketsa khatello ea "HDL" le cholesterol, hape li thibela hyperglycemia ka mor'a ho ja, le hemoglobin glycosylation.

Alpha Glucosidase Inhibitors (acarbose, miglitol) e thibela ho phatloha ha poly- le oligosaccharides, e theolang sebopeho le ho monya ha tsoekere ka mpeng ebe ka tsela eo e thibela nts'etsopele ea hypprobial hyperglycemia. Lik'habohaedreite tse nooang le lijo tse sa fetoloang li kena likarolong tse ka tlase tsa mala a manyane le a maholo, ha ho kenngoa ha li-monosaccharides nako e telele ho feta lihora tse 3-4. Ho fapana le li-agents tsa sulfonamide hypoglycemic, ha li eketse ho lokolloa ha insulin mme, ka hona, ha li bake hypoglycemia.

Ho ile ha bontšoa hore phekolo ea nako e telele ea acarbose e tsamaisana le phokotso e kholo ea menyetla ea ho ba le mathata a pelo le tlholeho ea atherosranceotic. Alfa glucosidase inhibitors e sebelisoa e le monotherapy kapa hammoho le li-agents tse ling tsa molomo tsa hypoglycemic. Motsoako oa pele ke 25-50 mg hang hang kapa nakong ea lijo, 'me ka morao ho moo o ka eketseha butle-butle (boholo ba letsatsi le letsatsi ke 600 mg).

Matšoao a ts'ebeliso ea li-alpha-glucosidase inhibitors ke mofuta oa tsoekere ea lefu la tsoekere le ho se sebetse hantle ha 'mele (e leng nako eo bonyane e ka bang likhoeli tse 6), hammoho le mofuta oa 1 lefu la tsoekere (joalo ka karolo ea phekolo ea motsoako).

Lithethefatsi tsa sehlopha sena li ka baka dyspeptic liketsahalo tse bakoang ke tlolo ea tšilo ea lijo le ho monya nama ea nama ea nama ea kolobe, e kenngoeng ka koloneng ka ho etsoa ha li-acid tse ngata, khabone le hydrogen. Ka hona, ha u fana ka alpha-glucosidase inhibitors, ho latela ka tieo lijo tse nang le lik'habohaedreite tse rarahaneng, ho kenyeletsoa le sucrose.

Acarbose e ka kopanngoa le lingaka tse ling tsa antidiabetes. Neomycin le colestyramine li matlafatsa phello ea acarbose, ha khafetsa le ho teba ha litlamorao ho tsoa mpeng ea mpa ea mpa. Ha e kopantsoe le li-antacids, adsorbents le enzymes tse ntlafatsang tšilo ea lijo, katleho ea acarbose ea fokotseha.

Hajoale, ho hlahile sehlopha se secha sa li-hypoglycemic - incretinomimetics. Keketseho ke lihormone tse patiloeng ke mefuta e meng ea lisele tse nyane tsa mala ho arabela kenyelletsong ea lijo le ho tsosa secretion ea insulin. Lihormone tse peli li ile tsa aroloa: glucagon-polypeptide (GLP-1) le glucose-insulinotropic polypeptide (HIP).

Ho incretinomimetics e kenyelletsa lihlopha tsa 2 tsa lithethefatsi:

- Lintho tse etsisang phello ea GLP-1 - liphatlalatso tsa GLP-1 (liraglutide, exenatide, lixisenatide),

- dintho tse holisang ketso ya endo native GLP-1 ka lebaka la thibelo ya dipeptidyl peptidase-4 (DPP-4) - enzyme e senyang GLP-1 - DPP-4 inhibitors (sitagliptin, vildagliptin, saxagliptin, linagliptin, alogliptin).

Kahoo, sehlopha sa baemeli ba hypoglycemic se kenyelletsa lithethefatsi tse 'maloa tse sebetsang. Li na le mochine o fapaneng oa ts'ebetso, li fapana ka litekanyetso tsa pharmacokinetic le pharmacodynamic. Tsebo ea likarolo tsena e lumella ngaka ho etsa khetho e nepahetseng ka ho fetisisa ea bongaka.

Contraindication

• 1. Mofuta oa 1 lefu la tsoekere.
• 2. Lefu la tsoekere ketoacidosis (boemo bo fetelletseng maling a 'mele ea ketone), komisi.
• 3. Bokhachane le pelehi.
• 4. Mafu a sa foleng le a hlobaetsang a sebete a nang le ts'ebetso e sa sebetseng.
• 5. Ho nyekeloa ke pelo.
• 6. Hypersensitivity ho lithethefatsi.

Litokisetso tsa Thiazolidinedione

Troglitazone (Rezulin) e ne e le lithethefatsi molokong oa pele oa sehlopha sena. O ile a hopoloa ho tloha thekisong, kaha phello ea hae e ne e bonahala hampe ho sebete.

Rosiglitazone (Avandia) ke setlhare sa meloko ea boraro sehlopheng sena. E khaolitse ho sebelisoa ka 2010 (e thibetsoe European Union) kamora hore ho netefatsoe hore e eketsa kotsi ea lefu la pelo.

Tšusumetso ea ts'ebeliso

Ntle le moo, ho netefalitsoe hore moriana o na le litlamorao tse ling tse thusang:

• E fokotsa khatello ea mali
• E ama boemo ba cholesterol (e eketsa boteng ba "cholesterol e ntle", ke hore, HDL, mme ha e eketse "cholesterol e mpe" - LDL),
• E thibela ho thehwa le kholo ea atherosulinosis,
• Fokotsa kotsi ea lefu la pelo (jk., Lefu la pelo, stroke).

Bala haholoanyane: Jardins o tla sireletsa pelo

Ho boleloa mang pioglitazone

Pioglitazone e ka sebelisoa e le sethethefatsi se le seng, i.e. monotherapy. Hape, haeba o na le mofuta oa lefu la tsoekere la mofuta oa 2 lefu la tsoekere, liphetoho tseo u li etsang bophelong ha li fane ka litholoana tse lebelletsoeng mme ho na le li-contraindication ho metformin, ho mamella ha eona hampe le litlamorao tse ka bang teng.

Ts'ebeliso ea pioglitazone e khonahala hammoho le lithethefatsi tse ling tsa antidiabetes (mohlala, acarbose) le metformin haeba liketso tse ling li sa tlise katleho

Pioglitazone e ka sebelisoa le insulin, haholo bathong bao 'mele oa bona o kenang hampe ho metformin.

Bala haholoanyane: Mokhoa oa ho nka metformin

Mokhoa oa ho nka pioglitazone

Moriana o lokela ho nooa hang ka letsatsi, ka molomo, ka nako e behiloeng. Sena se ka etsoa pele le ka mor'a lijo, kaha lijo ha li ame ho fufuleloa ha moriana. Hangata, kalafo e qala ka tekanyetso e tlase. Maemong moo phello ea kalafo e sa khotsofatseng, e ka eketseha butle-butle.

Ho sebetsa ha moriana ho bonoa maemong ao ho hlokahalang ho phekola lefu la tsoekere la mofuta oa 2, empa metformin e ke ke ea sebelisoa, monotherapy ka sethethefatsi se le seng ha e lumelloe.

Ntle le taba ea hore pioglitazone e fokotsa gypcemia ea postprandial, glucose ea plasma mme e tsitsisa hemoglobin ea glycated, e boetse e na le phello e ntle ea khatello ea mali le cholesterol ea mali. Ntle le moo, ha e bake liphapang.

Litokisetso tsa Thiazolidinedione

Thiazolidinediones (TZD) - sehlopha se secha sa lithethefatsi tsa antidiabetesic bakeng sa tšebeliso ea molomo. Lithethefatsi tsa Thiazolidinedione (pioglitazone, rosiglitazone) li kene ts'ebetsong ea bongaka feela lilemong tsa morao tjena. Joalo ka li-biguanides, lithethefatsi tsena ha li tsose secretion ea insulin, empa li eketsa kutloisiso ea lithane tsa pherekano ho eona. Likhakanyo tsa sehlopha sena li sebetsa e le li-agonists tsa li-receptor tsa nyutlelie tsa PPAR-y (peroxisome proliferator-activated receptor). Li-receptor tsena li fumanoa liseleng tse mafura, mesifa le sebete. Ho kenngwa tshebetsong ha li-receptor tsa PPAR-y ho fetolela phetiso ea mefuta e 'maloa e amanang le phetiso ea litlamorao tsa insulin bakeng sa ho kenella ha tsoekere le lipids ho lisele. Ntle le ho theola boemo ba glycemia, ho ntlafatsa methapo ea kutlo ea lisele ho insulin ho ama hantle boemo ba lipid (boemo ba lipoprotein bo phahameng bo eketseha, litaba tsa triglycerides lia fokotseha). Ka lebaka la hore lithethefatsi tsena li sebetsa ka ho khothaletsa mongolo oa liphatsa tsa lefutso, ho nka ho isa ho likhoeli tse 2-3 ho fumana sephetho se phahameng. Lithutong tsa bongaka, meriana ena e fanne ka ho fokotseha hoa boemo ba HbAc ka monotherapy ka 0,5 ho isa ho 2%.

Lithethefatsi tsa sehlopha sena li ka sebelisoa hammoho le PSM, insulin kapa metformin. Motsoako le metformin o na le mabaka a 'nete hobane ketso ea biguanides e etselitsoe haholo ho hatella gluconeogeneis,' me ketso ea thiazolidinediones e etselitsoe ho eketsa tšebeliso ea glucose e eketsehileng. Ha li hlile ha li bake hypoglycemia (empa, joalo ka li-greatuanides, li ka eketsa khafetsa ha hypoglycemia hammoho le lithethefatsi tse hlohlelletsang insulin secretion. Phello e ka sehloohong ke ts'ebeliso ea tsoekere e pherimeng le phokotso ea glycogeneis ka ts'ebetso ea mefuta ea methapo e amanang le insulin (ho fokotseha ha insulin ho hanyetsa). Thiazolidinediones e le lithethefatsi tse felisang ho loants'oa ha "insulin", sesosa se ka sehloohong sa nts'etsopele ea lefu la tsoekere la mofuta oa 2, ke sehlopha se ts'episang haholo sa lithethefatsi bakeng sa thibelo ea lefu la tsoekere la 2. Phello ea ts'ireletso ea thiazolidinediones e phehella likhoeli tse fetang tse 8 kamora ho itokolla. Ho na le monahano oa hore glitazones e khona ho lokisa ka botlalo bofokoli ba lefutso la tsoekere, bo sa lumelle feela ho liehisa nts'etsopele ea lefu la tsoekere la mofuta oa 2, empa hape le ho felisa nts'etsopele ea lona ka botlalo.

Leha ho le joalo, ho fihlela joale sena ke tšusumetso feela.

Ts'ebeliso ea thiazolidinediones ho bakuli ba lefu la tsoekere la mofuta oa 2 e bula menyetla ea ho thibela mathata a pelo, mokhoa oa nts'etsopele o bakoang haholo ke ho hanyetsa insulin. Lintlha tsa pele mabapi le phello ea li-thiazolidinediones li se li fumanoe lithutong tse ling tsa liteko. Lithuto tse tšoanang tsa kliniki ha li e-so tšoaroe.

Ho na le meloko e meraro ea thiazolidinediones lefatšeng:
- "litloholo tsa pele" lithethefatsi - troglitazone (e bontsitse phello e phatlalalitsoeng ea hepatotoxic le cardiotoxic, mabapi le moo e neng e thibetsoe ho sebelisoa),
- sethethefatsi sa "moloko oa bobeli" - pioglitazone,
- "Moloko oa boraro" lithethefatsi - rosiglitazone.

Hajoale, sethethefatsi se tsoang molokong oa bobeli oa thiazolidinediones - actos (pioglitazone hydrochloride) ho Eli Lilly (USA) le moloko oa boraro - avandium (rosiglitazone) se ngolisitsoe Russia. Actos e fumaneha ka mokhoa oa matlapa a nang le 15.30 le 45 mg ea ntho e sebetsang ea pioglitazone hydrochloride, hang ka letsatsi, ho sa tsotelloe lijo tse ngata.

Sekhahla sa letsatsi le letsatsi ke 30-45 mg. Glaxo SmithKJine (GSK) avandium e fumaneha ka foromo ea letlhare e nang le 4 le 8 mg ea ntho e sebetsang ea rosiglitazone, hanngoe kapa habeli ka letsatsi, ho sa tsotelehe tlhahiso ea lijo. Tekanyetso ea letsatsi le letsatsi ea 8 mg. Ho reriloe ho lokolla sethethefatsi se kopaneng ke k'hamphani e le 'ngoe - Avandamet (motsoako oa avandia le metformin).

Li-Thiazolidinediones li sebelisoa e le monotherapy, empa ho molemo hammoho le li-biguanides, acarbose, PSM, insulin ho bakuli ba nang le lefu la tsoekere la 2. Tšebeliso e lekanyelitsoeng ea sehlopha sena sa lithethefatsi e bakiloe ke litšenyehelo tsa bona tse phahameng haholo.Setlhare sena, e leng karolo ea moloko oa bobeli oa thiazolidinediones, ha se a ka a hlahisa phello ea hepatotoxic. Pioglitazone ha e kenngoe ka har'a sebete, e theha li-metabolites tse sebetsang, tse pepesitsoeng haholo-holo ka bile. E 'ngoe ea litlamorao e ka ba ponahalo ea edema, hammoho le phaello ea boima ba' mele. Khahlano le semelo sa kalafo, ho khothaletsoa ho laola boemo ba alanine le aspartic aminotransferase le ho emisa ho sebelisa lithethefatsi ka tekanyo ea "enzyme" e tloaelehileng ka makhetlo a mabeli. Ho khothalletsoa ho lekola phello ea sethethefatsi ka kalafo ea nako e telele (ea likhoeli tse 3). Contraindication:
- mofuta oa 1 lefu la tsoekere
- ketoacidosis le mofuta ofe kapa ofe oa lefu la tsoekere,
- moimana, ho nyeka,
- feteletseng tloaelo ea phetisetso ea alanine makhetlo a 3,
- bongata ba vaerase e matla, e chefo hepatitis,
- hepatitis e sa foleng.

Thibelo ea lefu la tsoekere la Mofuta oa 2

Teko ea bongaka ea DREAM e bonts'itse kotsi e fokotsehileng ea ho ba le lefu la tsoekere ho bakuli ba nang le mamello ea tsoekere e eketsehileng le khatello e matla ea ho itima lijo ha tsoekere ho bakuli ba nkang rosiglitazone (11, hape le 12). Phuputso ena e bontšitse hore nts'etsopele ea lefu la tsoekere e ka lieha ka lilemo tse 1.5, empa menyetla ea nts'etsopele e eketseha ebe e ts'oana le sehlopheng sa placebo.