Thiazolidinedione npaj - cov yam ntxwv thiab daim ntawv thov nta

Cov tshuaj niaj hnub siv ntau hom tshuaj los kho hom 2 ntshav qab zib.

Ib ntawm cov pab pawg no yog thiazolidinediones, uas muaj qhov zoo sib xws nrog metformin.

Nws ntseeg tau tias, piv nrog cov tshuaj yeeb yam saum toj no, thiazolidinediones muaj kev nyab xeeb dua.

Yuav kho tus mob pathology li cas?

Cov kev kho mob ntshav qab zib niaj hnub yog qhov ntsuas nyuaj kawg.

Cov txheej txheem kho mob suav nrog kev kawm kho mob, kev noj zaub mov nruj, kev kho lub cev, kev kho mob tsis muaj tshuaj thiab kev siv cov tshuaj suav tshuaj.

Kev kho mob ntshav qab zib koom nrog kev siv cov tshuaj tshwj xeeb kom ua tiav qee lub hom phiaj kho.

Cov hom phiaj kho yog:

• tswj qhov nyiaj ntawm cov tshuaj hormone insulin nyob rau theem xav tau,
• normalization ntawm tus nqi ntawm cov piam thaj nyob rau hauv cov ntshav,
• ib qho kev khuam siab rau kev txhim kho ntxiv ntawm txheej txheem pathological,
• neutralization ntawm kev tshwm sim ntawm cov teeb meem thiab qhov tshwm sim tsis zoo.

Kho chav kawm koom nrog kev siv cov hauv qab no pab pawg ntawm cov tshuaj:

1. Sulfonylurea kev npaj, uas ua rau kwv yees li cuaj caum feem pua ​​ntawm tag nrho cov tshuaj qab zib. Xws li cov ntsiav tshuaj zoo neutralize manifested insulin tsis kam.
2. Biguanides yog cov tshuaj uas muaj cov tshuaj yeeb tshuaj xws li metformin. Lub txheej txheem muaj cov txiaj ntsig zoo rau kev poob phaus, thiab kuj pab txo cov ntshav qab zib. Raws li txoj cai, nws tsis siv rau thaum muaj teeb meem lub raum thiab lub siab ua haujlwm, vim nws sai sai nyob rau hauv cov kabmob no.
3. Alpha-glycosidase inhibitors tau siv prophylactically los tiv thaiv kev txhim kho ntshav qab zib hom 2. Qhov tseem ceeb tseem ceeb ntawm cov tshuaj ntawm cov pab pawg no yog qhov lawv tsis ua rau cov tsos mob ntawm cov ntshav qab zib. Cov tshuaj noj pab pawg muaj cov txiaj ntsig zoo ntawm kev rov ua kom yuag, tshwj xeeb yog kev qhia txog kev noj zaub mov.
4. Thiazolidinediones tuaj yeem siv los ua cov tshuaj tseem ceeb rau kev kho mob ntawm tus kab mob pathology lossis ua ke nrog lwm cov tshuaj txo suab thaj. Lub luag haujlwm tseem ceeb ntawm cov ntsiav tshuaj yog ua kom cov nqaij mos zoo rhiab rau insulin, yog li ua kom tsis txhob muaj kev cuam tshuam. Cov tshuaj tsis yog siv rau hauv kev txhim kho ntawm hom 1 mob ntshav qab zib mellitus, txij li lawv tuaj yeem tsuas ua nyob rau hauv muaj cov kua dej, uas yog tsim los ntawm cov txiav.

Tsis tas li ntawd, meglitinides yog siv - cov tshuaj uas ua rau cov insulin ntau dua, yog li cuam tshuam cov pancreatic beta hlwb.

Kev txo qis hauv qabzib tau pom tias twb dhau sijhawm kaum tsib feeb tom qab noj cov ntsiav tshuaj.

Kev Nyab Xeeb

Thiazolidinediones sib cuam tshuam los ntawm kev txo qis cov tshuaj insulin. Muaj 2 thiazolidinediones muaj nyob rau ntawm kev ua lag luam - rosiglitazone (Avandia) thiab pioglitazone (Actos). Troglitazone yog thawj zaug hauv nws chav kawm, tab sis tau muab tso tseg vim tias nws ua rau lub siab ua haujlwm tsis zoo. Cov tshuaj tuaj yeem siv ob qho tib si li monotherapy, thiab ua ke nrog lwm cov tshuaj.

Mechanism ntawm kev ua. Thiazolidinediones nce insulin rhiab heev los ntawm kev ua yeeb yam rau cov ntaub so ntswg adipose, cov leeg thiab cov nplooj siab, qhov uas lawv nce siab siv cov piam thaj thiab txo nws cov tshuaj synthesis (1,2). Tus txheej txheem ntawm kev ua tsis tau to taub tag nrho. Lawv qhib ib lossis ntau hom ntawm receptors uas qhib peroxisome proliferation (RAPP) Receptors uas qhib peroxisome proliferation, uas, nyeg, tswj cov noob qhia (3).

Qhov Txiab Pioglitazone thiab rosiglitazone muaj tib qho kev ua haujlwm lossis txo qis me ntsis zoo li lwm yam kab mob hypoglycemic. Tus nqi nruab nrab ntawm glycosylated hemoglobin thaum noj rosiglitazone poob qis los ntawm 1.2-1.5%, thiab cov ntsiab lus ntawm lipoproteins ntau thiab tsawg ntom nce. Raws li cov ntaub ntawv, nws tuaj yeem xav tias kev kho mob nrog thiazolidinediones tsis qis dua qhov ua tau zoo ntawm kev siv tshuaj metformin, tab sis vim yog tus nqi siab thiab phiv, cov tshuaj no tsis siv rau kev kho mob ntshav qab zib thaum pib.

Cov nyhuv ntawm thiazolidinediones rau ntawm cov hlab plawv. Cov tshuaj hauv cov pab pawg no yuav muaj kev tawm tsam, antithrombotic, thiab tshuaj tiv thaiv atherogenic, tab sis txawm tias qhov no, cov ntaub ntawv uas qhia tias txo qis kev pheej hmoo ntawm cov kab mob plawv tsis txaus, thiab tus naj npawb ntawm cov kev mob tshwm sim yog ib qho ceeb toom (4,5,6,7). Cov txiaj ntsig ntawm kev ntsuas meta-tshuaj ntsuam pom tau hais tias yuav tsum tau ceev faj hauv kev siv thiazolidinediones thiab rosiglitazone tshwj xeeb, thaum cov ntaub ntawv tshiab tsis lees paub lossis tsis lees txais cov ntaub ntawv cardiotoxicity. Ntxiv mus, nws yog qhov yuav tsum xav txog qhov ua tau ntawm kev mob plawv nres. Hauv qhov xwm txheej no, nws tsis pom zoo kom siv cov rosiglitazone yog tias nws muaj peev xwm siv cov tshuaj muaj kev nyab xeeb (metformin, sulfonylureas, insulin).

Lipids. Thaum lub sij hawm kho nrog pioglitazone, qhov tseem ceeb ntawm cov lipids uas tsis muaj qhov hnyav tseem tsis hloov, thiab nrog kev kho nrog rosiglitazone, kev nce siab ntawm cov kab mob lipid feem tau pom los ntawm qhov nruab nrab ntawm 8-16%. (3)

Kev ruaj ntseg hloov |Nta ntawm thiazolidinediones

Thiazolidinediones, hauv lwm lo lus glitazones, yog ib pawg ntawm cov tshuaj qab zib uas muaj lub hom phiaj txhawm rau nce cov kev lom neeg ntawm cov tshuaj insulin. Txog kev kho mob ntshav qab zib mellitus tau pib siv tsis ntev los no - txij li xyoo 1996 los. Tau coj tawm nruj raws li kws kho mob hais.

Glitazones, ntxiv rau kev txiav txim siab hypoglycemic, muaj cov txiaj ntsig zoo ntawm lub plawv hlab plawv. Cov kev ua hauv qab no tau pom: antithrombotic, antiatherogenic, tiv thaiv. Thaum noj thiazolidinediones, qib ntawm glycated hemoglobin poob qis rau nruab nrab li 1.5%, thiab qib ntawm HDL nce.

Kev kho mob nrog cov tshuaj ntawm chav kawm no tsis muaj tsawg dua li kev kho nrog Metformin. Tab sis lawv tsis siv nyob rau theem pib nrog hom 2 mob ntshav qab zib. Qhov no yog vim qhov loj heev ntawm kev phiv thiab tus nqi siab. Niaj hnub no, glitazones raug siv los txo qis glycemia nrog sulfonylurea derivatives thiab metformin. Lawv tuaj yeem raug sau ob leeg sib cais nrog txhua cov tshuaj, thiab sib xyaw.

Qhov zoo thiab qhov tsis zoo

Ntawm cov yam ntxwv ntawm cov tshuaj muaj qhov zoo thiab tsis zoo:

• nce lub cev hnyav los ntawm 2 kg ntawm qhov nruab nrab,
• Cov npe loj ntawm cov kev mob tshwm sim
• Txhim kho lipid profile
• Kev cuam tshuam zoo rau insulin tsis kam
• txo qis kev ua haujlwm qis dua piv rau metformin, sulfonylurea derivatives,
• txo cov ntshav siab
• txo cov xwm txheej cuam tshuam rau kev txhim kho atherosclerosis,
• khaws cov kua dej, thiab raws li qhov tshwm sim, kev pheej hmoo ntawm lub plawv tsis tuaj yeem nce,
• txo qhov ceev cov pob txha, nce qhov kev pheej hmoo ntawm pob txha lov,
• hepatotoxicity.

Mechanism ntawm kev ua

Thiazolidinediones ua rau cov receptors, uas ua kom qhov kev faib tawm thiab kom muaj zog ntawm cov piam thaj los ntawm hlwb. Kev ua ntawm cov tshuaj hormones hauv lub siab, adipose cov nqaij thiab cov leeg txhim kho. Ntxiv mus, qhov cuam tshuam rau theem ntawm ob lub cim kawg tseem muaj ntau dua.

Glitazones tsis txhawb kev tsim cov tshuaj insulin los ntawm pancreatic cells-hlwb. Qhov kev txo qis hauv kev ua tiav yog ua tiav los ntawm kev txo qis cov tshuaj insulin ntawm cov ntaub so ntswg thiab kev siv cov kua nplaum ntau los ntawm cov ntaub so ntswg. Cov piam thaj-ua kom qis dua, raws li txoj cai, tshwm sim maj. Kev noj cov ntshav qabzib tsawg kawg yog pom tsuas yog tom qab ob lub hlis twg. Kev kho nrog nrog qhov hnyav nce.

Muaj kev txhim kho hauv kev tswj cov zom zaub mov kom muaj ntshav qab zib kom tsawg. Thaum ua ke nrog metformin thiab sulfonylurea derivatives, glycemic tswj tau txhim kho hauv cov neeg mob ntshav qab zib hom 2, nrog rau cov tseem ceeb hauv cov ntshav plasma hormone ntau ntau. Glitazones ua dab tsi tsuas yog muaj cov tshuaj insulin.

Cov tshuaj Pharmacokinetic yuav txawv nyob ntawm cov tshuaj. Tsis txhob cuam tshuam rau lawv tus tub los ntxhais thiab hnub nyoog ntawm tus neeg mob. Nrog rau daim siab puas hauv cov neeg mob, nws hloov cov chaw muag tshuaj.

Kev taw qhia thiab contraindications

Thiazolidinediones yog kho rau cov ntshav qab zib tsis yog insulin-mob ntshav qab zib (ntshav qab zib hom 2):

• raws li kev kho mob rau cov neeg mob uas tswj cov qib glycemia tsis siv tshuaj (noj zaub mov thiab ua si lub cev),
• raws li kev kho ob yam nyob rau hauv nrog sulfonylurea npaj,
• raws li kev kho mob dual nrog metformin rau kev tswj glycemic txaus,
• raws li triple kev kho mob ntawm "glitazone + metformin + sulfonylurea",
• ua ke nrog tshuaj insulin
• ua ke nrog cov tshuaj insulin thiab metformin.

Ntawm cov contraindications kom noj tshuaj:

• ib tug neeg intolerance,
• cev xeeb tub / lactation,
• hnub nyoog txog 18 xyoo
• daim siab ua haujlwm - mob hnyav thiab mob nyhav,
• lub plawv dhia tsis zoo
• lub raum tsis ua haujlwm yog mob hnyav.

Video qhuab qhia ntawm kev npaj ntawm thiazolidinedione pab pawg:

Sab sij huam

Ntawm cov kev mob tshwm sim tom qab noj thiazolidinediones yog:

• rau cov poj niam - coj khaub ncaws tsis xwm yeem,
• kev txhim kho lub plawv tsis ua haujlwm,
• ua txhaum cai ntawm qhov xwm txheej hormonal,
• nce qib ntawm daim siab enzymes,
• anemia
• ntshav qab zib,
• hypercholesterolemia,
• mob taub hau thiab kiv taub hau,
• hnyav
• nce qab los noj mov
• mob plab, kiv,
• daim tawv nqaij ua pob, tshwj xeeb, urticaria,
• o tuaj
• muaj zog rog ntau zuj zus
• pom kev pom
• benign formations - polyps thiab hlwv,
• sab sauv ntawm txoj hlab ua pa tuaj.

Hauv chav kawm ntawm kev kho mob, qhov hnyav thiab cov paib tau raug saib xyuas uas qhia tau hais tias muaj kua dej tawm. Kev kuaj xyuas lub siab ua haujlwm. Tau haus ntau hauv cov cawv cov cawv tsis cuam tshuam dab tsi rau kev tswj glycemic.

Tsuas tshuaj, txoj kev ntawm kev coj

Glitazones raug coj tawm yam tsis hais txog zaub mov. Dosage kev kho rau cov neeg laus nrog kev sib txawv me me hauv daim siab / ob lub raum tsis tau nqa tawm. Cov ntawv tom kawg ntawm cov neeg mob tau sau tseg kom tsawg dua ntawm cov tshuaj txhua hnub. Cov koob tshuaj yog txiav txim los ntawm tus kws kho mob ib leeg zuj zus.

Lub sijhawm pib ntawm kev kho mob pib nrog qhov txhaj tshuaj tsawg. Yog tias tsim nyog, nws yog nce nyob rau hauv ntau ntau nyob ntawm cov tshuaj. Thaum ua ke nrog cov tshuaj insulin, nws txoj kev noj tshuaj tsis hloov pauv lossis txo qis nrog cov lus ceeb toom ntawm kev mob hypoglycemic.

Thiazolidinedione Cov Npe Tshuaj

Ob tus neeg sawv cev ntawm glitazone muaj nyob rau ntawm cov chaw muag tshuaj hnub no - rosiglitazone thiab pioglitazone. Thawj thawj hauv cov pab pawg yog troglitazone - nws tau sai sai vim tias kev txhim kho ntawm daim siab ua rau lub siab hnyav.

Cov tshuaj raws rosiglitazone suav nrog cov hauv qab no:

• 4 mg avandia - Spain,
• 4 mg Diagnitazone - Ukraine,
• Roglit ntawm 2 mg thiab 4 mg - Hungary.

Piogitazone-based tshuaj muaj xws li:

• Glutazone 15 mg, 30 mg, 45 mg - Ukraine,
• Nilgar 15 mg, 30 mg - Is Nrias teb,
• Dropia-Sanovel 15 mg, 30 mg - Qaib Cov Txwv,
• Pioglar 15 mg, 30 mg - Is Nrias teb,
• Pyosis 15 mg thiab 30 mg - Is Nrias teb.

Kev cuam tshuam nrog lwm yam tshuaj

1. RosiglitazoneCov. Kev haus cawv tsis cuam tshuam rau kev tswj glycemic. Tsis muaj qhov cuam tshuam loj nrog cov ntsiav tshuaj tiv thaiv kab mob, Nifedipine, Digoxin, Warfarin.
2. PioglitazoneCov. Thaum ua ke nrog rifampicin, cov nyhuv ntawm pioglitazone tsawg dua. Tej zaum qhov poob qis hauv kev ua haujlwm zoo thaum siv tshuaj ntsiav. Thaum siv ketoconazole, glycemic tswj feem ntau tsim nyog.

Thiazolidinediones tsis tsuas txo cov ntshav qab zib, tab sis kuj tseem cuam tshuam rau cov kab mob plawv. Ntxiv rau qhov zoo, lawv muaj ib tug xov tooj ntawm qhov tsis zoo, feem ntau ntawm cov uas yog kev txhim kho lub plawv tsis ua hauj lwm thiab txo pob txha lub cev.

Lawv nquag siv hauv kev kho nyuaj, siv cov thiazolidinediones rau kev tiv thaiv kev txhim kho tus kab mob yuav tsum muaj kev kawm ntxiv.

Cov cai teem caij

1. Qhov xaiv thawj cov tshuaj rau cov ntshav qab zib hom 2 hauv cov neeg mob nyhav dhau los yog metformin lossis tshuaj los ntawm pawg thiazolidinediones.
   
2. Hauv cov neeg mob uas muaj lub cev nyhav, qhov kev xaiv yog muab rau sulfonylurea kev npaj lossis meglitinides.
   
3. Nrog rau qhov tsis muaj txiaj ntsig ntawm kev siv ib ntsiav tshuaj, raws li txoj cai, kev sib xyaw ntawm ob (tsawg dua peb) tshuaj yog tshuaj. Feem ntau siv ua ke:
   
   • sulfonylurea + metformin,
   • metformin + thiazolidinedione,
   • metformin + thiazolidinedione + sulfonylurea.
     

Sulfonylurea npaj

Cov tshuaj uas nrov tshaj plaws yog cov tshuaj cuam tshuam nrog sulfonylurea derivatives (txog 90% ntawm tag nrho cov tshuaj txo suab thaj). Nws ntseeg tau hais tias kev nce ntxiv hauv insulin secretion los ntawm cov tshuaj hauv chav kawm no yog qhov tsim nyog kom kov yeej cov tshuaj tiv thaiv insulin ntawm kev cuam tshuam insulin.

Thib 2 tiam sulfonylurea npaj muaj:

• Gliclazide - muaj cov lus tshaj tawm zoo rau microcirculation, ntshav ntws, muaj cov txiaj ntsig zoo rau microvascular cov teeb meem ntshav qab zib.
• Glibenclamide - muaj cov nyhuv hypoglycemic feem ntau. Tam sim no, muaj ntau ntau thiab ntau tshaj tawm kev hais lus txog qhov tsis zoo ntawm cov tshuaj no ntawm chav kawm ntawm cov kab mob plawv.
• Glipizide - muaj cov suab thaj txo qis tshaj plaws, tab sis lub sijhawm ua haujlwm tau luv dua li ntawm glibenclamide.
• Glycidone - tsuas yog cov tshuaj los ntawm pab pawg no, uas yog tau sau ntawv rau cov neeg mob uas mob raum. Nws muaj lub sijhawm luv tshaj ntawm kev ua.

Cov koob thib 3 tiam sulfonylurea npaj tau nthuav tawm Glimeprimide:

• pib ua thaum ntxov thiab muaj lub sijhawm ntev dua (txog li 24 teev) ntawm kev noj tshuaj tsawg dua,
• cov kev muaj peev xwm noj cov tshuaj tsuas yog 1 zaug hauv ib hnub,
• tsis txo qis insulin secretion thaum qoj ib ce,
• ua rau kev tso tawm sai sai ntawm cov tshuaj insulin rau hauv kev tau txais khoom noj,
• yuav siv tau rau mob raum tsis ua hauj lwm,
• muaj kev pheej hmoo qis ntawm hypoglycemia piv nrog lwm cov tshuaj hauv chav kawm no.

Qhov ua tau zoo tshaj plaws ntawm sulfonylurea npaj tau pom nyob hauv cov neeg mob ntshav qab zib hom 2, tab sis nrog lub cev qhov hnyav.

Qhia cov tshuaj sulfonylurea rau cov ntshav qab zib hom 2, thaum kev noj zaub mov zoo thiab kev tawm dag zog tsis pab.

Sulfonylurea kev npaj yog contraindicated: rau cov neeg mob uas muaj ntshav qab zib hom 1, cev xeeb tub thiab lub sijhawm lactation, nrog cov kab mob hnyav ntawm daim siab thiab lub raum, nrog cov mob caj dab mob ntshav qab zib. Kev saib xyuas tshwj xeeb yuav tsum tau saib xyuas thaum muaj mob rwj thiab mob plab hnyuv, nrog rau thaum muaj mob febrile nyob hauv cov cawv cawv ntev.

Raws li kev txheeb cais, hmoov tsis, tsuas yog ib feem peb ntawm cov neeg mob ua tiav tau them nyiaj rau kev mob ntshav qab zib mellitus nrog kev siv sulfonylureas. Lwm tus neeg mob tau raug pom zoo kom muab cov tshuaj no nrog lwm cov tshuaj kho mob, lossis hloov mus rau kev kho tshuaj insulin.

Cov tshuaj ib leeg hauv pawg no metformin, uas ua kom qis qis dua ntawm kev tsim tawm thiab tso tawm cov piam thaj hauv lub siab, txhim kho kev siv cov kua nplaum los ntawm cov ntaub so ntswg, txhim kho cov ntshav khiav, thiab normalizes lipid metabolism. Cov nyhuv hypoglycemic tshwm sim 2-3 hnub tom qab pib siv tshuaj.Nyob rau tib lub sijhawm, theem ntawm kev yoo glycemia poob qis, thiab lub siab poob qis.

Ib qhov tshwj xeeb ntawm metformin yog kev ua kom ruaj khov, thiab txawm tias poob phaus - tsis muaj lwm yam ntawm cov ntshav nruab nrog cev muaj cov nyhuv no.

Kev qhia txog kev siv tshuaj metformin yog: hom 2 mob ntshav qab zib mellitus hauv cov neeg mob rog rog, ntshav qab zib, ua tsis haum rau sulfonylurea npaj.

Metformin yog contraindicated rau cov neeg mob uas muaj hom 1 mob ntshav qab zib mellitus, cev xeeb tub thiab thaum lactation, nrog cov kab mob hnyav ntawm lub siab thiab lub raum, nrog cov mob hnyav ntawm ntshav qab zib, nrog rau mob hnyav, thiab ib yam kab mob nrog los ntawm kev tsis txaus cov kabmob nrog cov pa.

Alpha Glycosidase Cov Tshuaj Hauv Chaw

Cov tshuaj ntawm pab pawg no muaj xws li acarbose thiab miglitol, uas ua kom qeeb ntawm qhov kev zom zom ntawm carbohydrates hauv txoj hnyuv, uas ua kom lub ntsej muag nqus qis dua ntawm cov piam thaj hauv cov ntshav. Vim qhov no, qhov nce ntawm cov ntshav qab zib thaum lub sijhawm noj mov yog smoothed tawm, tsis muaj kev pheej hmoo ntawm kev mob ntshav qab zib.

Ib qho tshwj xeeb ntawm cov tshuaj no yog lawv qhov kev ua tau zoo hauv kev noj cov khoom noj loj ntawm cov carbohydrates. Yog tias cov carbohydrates yooj yim yeej nyob hauv tus neeg mob cov zaub mov noj, kev kho mob alpha-glycosidase inhibitors tsis muaj txiaj ntsig zoo. Lub tshuab tshwj xeeb ntawm kev txiav txim siab ua rau cov tshuaj ntawm pawg no ua hauj lwm zoo tshaj plaws rau kev yoo mov glycemia thiab nce siab tom qab noj mov. Tsis tas li, cov tshuaj no xyaum tsis ua rau lub cev hnyav.

Alpha-glycosidase inhibitors qhia rau cov neeg mob ntshav qab zib hom 2 mob ntshav qab zib nrog kev noj zaub mov noj thiab qoj ib ce tsis muaj txiaj ntsig nrog kev cia siab ntawm hyperglycemia tom qab noj mov.

Cov tshuaj tiv thaiv tsis haum rau kev siv alpha-glycosidase inhibitors yog: mob ntshav qab zib ketoacidosis, mob ntsws, mob hnyav thiab mob plab hnyuv, mob plab hnyuv plab nrog txoj kev ua kom muaj roj, ua kom mob plab, mob plab hnyuv, mob hnyuv loj, mob raum tsis zoo, kev xeeb tub thiab lactation.

Thiazolidinediones (glitazones)

Cov tshuaj hauv pawg no suav nrog pioglitazone, rosiglitazone, troglitazoneuas txo cov kab mob insulin, txo qis tso tawm cov piam thaj hauv lub siab, tswj kev ua haujlwm ntawm cov kua dej hauv insulin.

Qhov kev txiav txim ntawm cov tshuaj no zoo ib yam nrog kev ua ntawm metformin, tab sis lawv tsis kam ua nws qhov tsis zoo - ntxiv rau kev txo qis cov tshuaj insulin, cov tshuaj ntawm cov pab pawg no muaj peev xwm ua kom qeeb ntawm kev tsim kho cov teeb meem lub raum thiab kev mob ntshav siab, ntxim nyiam cuam tshuam lipid metabolism. Tab sis ntawm qhov tod tes, thaum noj glitazones, koj yuav tsum tau saib xyuas lub siab kom ua haujlwm tas li. Tam sim no, muaj cov ntawv pov thawj uas siv cov rosiglitazone tuaj yeem ua rau muaj kev pheej hmoo ntawm myocardial infarction thiab lub plawv tsis ua haujlwm.

Glitazones tau qhia rau cov neeg mob ntshav qab zib hom 2 hauv rooj plaub ntawm kev noj zaub mov tsis ua hauj lwm thiab kev tawm dag zog nrog lub zog ntawm kev tiv thaiv cov tshuaj insulin.

Cov txheej txheem tiv thaiv yog: hom 1 mob ntshav qab zib mellitus, mob ntshav qab zib ketoacidosis, cev xeeb tub thiab lactation, mob siab mob siab, mob plawv tsis ua haujlwm.

Meglitinides

Cov tshuaj hauv pawg no suav nrog kwv huam thiab nawb kev pabmuaj lub sij hawm luv luv-qab zib cov nyhuv. Meglitinides tswj hwm theem ntawm cov piam thaj tom qab noj mov, uas ua rau nws tsis tuaj yeem ua raws li cov zaub mov nruj, vim tias cov tshuaj yog siv tam sim ua ntej noj mov.

Qhov tshwj xeeb sib txawv ntawm meglitinides yog qhov nce siab ntawm cov piam thaj: ntawm lub plab tsis muaj 4 mmol / l, tom qab noj mov - los ntawm 6 mmol / l. Qhov siab ntawm glycated hemoglobin HbA1c yog txo 2%. Nrog rau siv ntev tsis ua rau hnyav nce thiab tsis tas yuav xaiv cov koob tshuaj. Kev nce hauv hypoglycemic cov nyhuv yog pom thaum noj cawv thiab qee cov tshuaj.

Kev qhia txog kev siv meglitinides yog hom 2 mob ntshav qab zib yog thaum muaj kev noj zaub mov tsis zoo thiab ua haujlwm lub cev.

Miglitinides yog contraindicated: rau cov neeg mob uas muaj hom 1 mob ntshav qab zib mellitus, nrog cov mob ntshav qab zib ketoacidosis, cov poj niam cev xeeb tub thiab pub niam mis, nrog rau kev nkag siab ntau dua rau cov tshuaj.

XAUS! Cov ntaub ntawv muab los ntawm lub xaib DIABET-GIPERTONIA.RU yog rau siv xwb. Lub chaw tswj hwm txoj haujlwm tsis yog lub luag haujlwm yog qhov tshwm sim tsis zoo yog tias koj noj tshuaj lossis cov txheej txheem yam tsis muaj kev teem caij ntsib kws kho mob!

Kev siv tshuaj hypoglycemic lossis antidiabetic yog cov tshuaj uas txo cov ntshav qabzib thiab siv los kho ntshav qab zib.

Nrog rau cov tshuaj insulin, cov kev npaj ntawm cov uas haum rau kev siv niam txiv nkaus xwb, muaj ntau cov hluavtaws sib xyaw uas muaj cov nyhuv hauv lub cev tsis muaj zog thiab muaj txiaj ntsig thaum noj ntawm qhov ncauj. Kev siv cov tshuaj tseem ceeb nyob hauv ntshav qab zib hom 2.

Cov neeg sawv cev ntawm tus ncauj ntshav hypoglycemic (hypoglycemic) tuaj yeem muab cais raws li hauv qab no:

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

— meglitinides (pab pawg, cov pab pawg),

— lojmuas (buformin, metformin, phenformin),

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

— alpha glucosidase inhibitors (acarbose, miglitol),

Kev muaj ntshav qab zib nyob hauv sulfonylurea derivatives tau tshawb pom los ntawm lub caij nyoog. Lub peev xwm ntawm cov sib txuas ntawm cov pab pawg no ua rau muaj qhov ua rau lub ntsej muag hypoglycemic tau pom nyob rau hauv 50s, thaum cov ntshav qabzib tsawg dua tau sau tseg nyob hauv cov neeg mob tau txais cov tshuaj tua kab mob sulfonamide rau kev kho mob kis mob. Hauv qhov no, ib qho kev tshawb nrhiav tau pib rau cov neeg nyiam ntawm sulfonamides nrog lub suab tshaj lij hypoglycemic hauv 50s. Kev sib txuas ntawm thawj sulfonylurea derivatives uas tuaj yeem siv los kho ntshav qab zib mellitus tau ua tiav. Thawj cov tshuaj no yog carbutamide (Lub Tebchaws Yelemees, 1955) thiab tolbutamide (Tebchaws USA, 1956). Hauv 50 thaum ntxov. cov sulfonylurea derivatives tau pib siv rau hauv kev coj ua. Hauv 60-70. thib ob-tiam sulfonylureas tshwm sim. Thawj tus sawv cev ntawm kev npaj sulfonylurea thib ob, glibenclamide, tau pib siv los kho ntshav qab zib hauv xyoo 1969, xyoo 1970 glibornuride pib siv, thiab xyoo 1972, glipizide. Gliclazide thiab glycidone tshwm sim yuav luag ib txhij.

Xyoo 1997, repaglinide (ib pawg meglitinides) tau pom zoo rau kev kho mob ntshav qab zib.

Keeb kwm ntawm kev siv cov khoom loj los tsim nyob rau Hnub nyoog Nruab Nrab, thaum siv ib tsob nroj los kho ntshav qab zib Galega officinalis (french Lily).

Thiazolidinediones (glitazones) nkag mus rau kev kho mob hauv xyoo 1997. Thawj cov tshuaj pom zoo rau kev siv raws li tus neeg sawv cev hypoglycemic yog troglitazone, tab sis xyoo 2000 nws siv tau txwv vim tias muaj cov hepatotoxicity siab. Txog rau hnub no, ob qho tshuaj los ntawm pab pawg no yog siv - pioglitazone thiab rosiglitazone.

Nkaus sulfonylureas feem ntau cuam tshuam nrog kev tsim kho ntawm pancreatic beta hlwb, nrog kev npaj thiab nce tawm ntawm cov tshuaj insulin endogenous.

Nrog rau kev kho mob ntev nrog sulfonylurea derivatives, lawv qhov pib cuam tshuam rau insulin secretion ploj mus. Nws ntseeg tau tias qhov no yog vim muaj qhov txo qis ntawm tus naj npawb ntawm receptors ntawm beta hlwb. Tom qab so kho mob, kev tawm tsam ntawm beta hlwb rau kev siv tshuaj ntawm pab pawg no tau rov qab los.

Qee qhov sulfonylureas tseem muaj cov teebmeem ntxiv-pancreatic. Cov kev tiv thaiv sab nrauv tsis yog qhov tseem ceeb hauv cov chaw kho mob, lawv suav nrog kev nce siab ntawm cov insulin-cov nqaij ua kom cov insulin endogenous thiab txo qis hauv kev tsim cov piam thaj hauv lub siab. Lub tshuab kev txhim kho ntawm cov kev cuam tshuam no vim yog qhov tseeb tias cov tshuaj no (tshwj xeeb yog glimepiride) nce cov insulin-rhiab receptors ntawm cov phiaj hlwb, txhim kho insulin-receptor kev sib cuam tshuam, thiab rov qab kev sib hloov ntawm cov teeb liab postreceptor.

Tsis tas li ntawd, muaj pov thawj pom tias prizvodnye sulfonylureas txhawb kev tso tawm somatostatin thiab yog li inhibit qhov tso pa tawm ntawm glucagon.

Kuv tiam: tolbutamide, carbamide, tolazamide, acetohexamide, chlorpropamide.

II tiam: glibenclamide, glisoxepide, glibornuril, glycidone, glyclazide, glipizide.

III tiam: glimepiride.

Tam sim no, hauv Russia, sulfonylurea kev npaj ntawm thawj tiam yog xyaum tsis siv.

Lub ntsiab sib txawv ntawm cov tshuaj thib ob thiab sulfonylurea derivatives ntawm thawj tiam yog ntau dua kev ua haujlwm (50-100 zaug), uas tso cai rau lawv siv rau hauv cov koob tshuaj qis dua thiab, raws li, txo qhov ntxim nyiam ntawm cov kev mob tshwm sim. Cov tib neeg sawv cev ntawm cov hypoglycemic derivatives ntawm sulfonylureas ntawm 1st thiab 2nd tiam sib txawv hauv kev ua thiab kev ua siab ntev. Yog li, cov tshuaj txhua hnub ntawm thawj cov tshuaj - tolbutamide thiab chlorpropamide - 2 thiab 0.75 g, ntsig txog, thiab cov tshuaj thib ob - glibenclamide - 0.02 g, glycvidone - 0.06-0.12 g. Cov tshuaj thib ob feem ntau zoo dua rau cov neeg mob Cov.

Kev npaj Sulfonylurea muaj qhov sib txawv thiab lub sijhawm ua haujlwm, uas txiav txim siab xaiv cov tshuaj thaum kws kho mob hais. Glibenclamide muaj qhov tseem ceeb tshaj plaws ntawm qhov kev xav ntawm txhua qhov sulfonylurea derivatives. Nws yog siv los siv rau kev soj ntsuam cov nyhuv hypoglycemic ntawm cov tshuaj tshiab synthesized. Qhov ua tau zoo hypoglycemic ntawm glibenclamide yog vim qhov tseeb tias nws muaj qhov sib txuam zoo tshaj plaws rau ATP-dependant potassium ntawm cov roj ntsha pancreatic beta hlwb. Lub sijhawm tam sim no, glibenclamide tsim tawm ob qho tib si ntawm kev siv tshuaj ib txwm muaj thiab hauv kev siv tshuaj micronized - daim ntawv tshwj xeeb glibenclamide uas muab qhov zoo tshaj plaws pharmacokinetic thiab pharmacodynamic profile vim los ntawm kev nqus sai thiab ua tiav (bioavailability yog li 100%) thiab ua rau nws siv tau cov tshuaj hauv me koob tshuaj.

Gliclazide yog qhov ncauj ntau tshaj plaws ntawm qhov ncauj hypoglycemic tus neeg sawv cev tom qab glibenclamide. Ntxiv rau qhov tseeb tias gliclazide muaj cov nyhuv hypoglycemic, nws txhim kho hematological tsis, rheological zog ntawm cov ntshav, muaj cov txiaj ntsig zoo ntawm cov kab mob hemostatic thiab microcirculation, thiab tiv thaiv kev txhim kho microvasculitis, suav nrog kev puas tsuaj rau retina, inhibits platelet sib sau ua ke, nce ntau qhov txheeb cais kev sib cais, ua rau muaj kev ua haujlwm heparin thiab fibrinolytic, nce siab rau heparin, thiab tseem ua kom pom cov khoom antioxidant.

Glycvidone yog ib qho tshuaj uas tuaj yeem kho cov neeg mob uas mob raum tsis txaus, vim tias tsuas yog 5% ntawm cov tshuaj metabolites raug tawm los ntawm ob lub raum, so (95%) - dhau los ntawm txoj hnyuv.

Glipizide, muaj cov lus tshaj tawm, ua rau muaj kev phom sij tsawg kawg hauv kev hais txog kev tiv thaiv hypoglycemic, vim tias nws tsis ceev thiab tsis muaj cov metabolites.

Cov tshuaj tiv thaiv kab mob hauv lub qhov ncauj yog cov tshuaj tseem ceeb rau kev kho mob hom 2 mob ntshav qab zib mellitus (tsis-insulin-dependant) thiab feem ntau yog kho rau cov neeg mob hnub nyoog qis dua 35 xyoo uas tsis muaj ketoacidosis, kev noj zaub mov tsis zoo, muaj teeb meem lossis cov kab mob uas xav tau kev kho mob insulin tam sim ntawd.

Kev npaj ntawm sulfonylurea pab pawg tsis pom zoo rau cov neeg mob hauv leej twg, nrog kev noj zaub mov kom zoo, kev xav tau txhua hnub rau insulin ntau dua 40 units. Tsis tas li ntawd, lawv tsis raug sau tseg rau cov neeg mob uas muaj mob ntshav qab zib mellitus ntau ntau (muaj qhov tsis txaus beta-cell tsis txaus), muaj keeb kwm ntawm ketosis lossis mob ntshav qab zib tsis nco qab, nrog hyperglycemia saum toj no 13.9 mmol / L (250 mg%) ntawm lub plab thiab lub siab glucosuria thaum noj tshuaj.

Hloov mus rau kev kho mob nrog sulfonylurea tshuaj rau cov neeg mob ntshav qab zib uas nyob rau hauv kev kho mob insulin yog ua tau yog tias cov khoom noj tsis haum rau carbohydrate metabolism tau raug them rau ntawm kev noj tshuaj insulin tsawg dua 40 units / hnub. Ntawm kev noj tshuaj ntawm cov insulin txog 10 units / hnub, koj tuaj yeem hloov mus rau kev kho mob nrog sulfonylurea derivatives.

Kev siv ntev ntawm sulfonylurea derivatives tuaj yeem ua rau kev txhim kho ntawm kev tsis kam, uas tuaj yeem kov yeej los ntawm kev sib xyaw nrog kev kho nrog insulin npaj. Hauv hom 1 mob ntshav qab zib mellitus, kev sib xyaw ua ke ntawm insulin npaj nrog sulfonylurea derivatives ua rau nws txo qis txhua hnub xav tau cov tshuaj insulin thiab pab txhim kho cov chav kawm ntawm tus kabmob, suav nrog kev txo qis ntawm kev hloov kho ntawm retinopathy, uas yog qee yam cuam tshuam nrog cov kev ua haujlwm angioprotective ntawm sulfonylurea derivatives (tshwj xeeb tshaj yog tiam II). Nyob rau tib lub sijhawm, muaj qhov ntsuas ntawm lawv lub peev xwm atherogenic ua tau.

Tsis tas li ntawd, sulfonylurea derivatives yog ua ke nrog cov tshuaj insulin (xws li kev sib koom ua ke yog suav tias tsim nyog yog tias tus neeg mob tus mob tsis txhim kho thaum sau ntau dua 100 IU ntawm cov tshuaj insulin ib hnub), qee zaum lawv tau ua ke nrog biguanides thiab acarbose.

Thaum siv sulfonamide hypoglycemic tshuaj, nws yuav tsum tau yug los rau hauv lub siab tias cov tshuaj tua kab mob sulfonamides, cov kabmob anticoagulants, indadion, salicylates, ethionamide, tetracyclines, chloramphenicol, cyclophosphamide inhibit lawv cov metabolism thiab nce kev ua haujlwm (hypoglycemia yuav loj hlob). Thaum sulfonylurea derivatives yog ua ke nrog thiazide diuretics (hydrochlorothiazide, thiab lwm yam) thiab BKK (nifedipine, diltiazem, thiab lwm yam), antagonism tshwm sim hauv cov tshuaj loj - thiazides cuam tshuam nrog kev cuam tshuam ntawm sulfonylurea derivatives vim yog qhib cov poov tshuaj raws, thiab BKK cuam tshuam cov kev khiav ntawm calcium ions mus rau hauv cov qog.

Derivatives ntawm sulfonylureas txhim kho cov nyhuv thiab intolerance ntawm cawv, tej zaum vim los ntawm qeeb hauv oxidation ntawm acetaldehyde. Antabuse zoo li cov tshuaj tiv thaiv tuaj yeem siv tau.

Txhua cov tshuaj sulfonamide hypoglycemic pom zoo kom noj 1 teev ua ntej noj mov, uas ua rau muaj kev tawm suab ntau ntxiv hauv postprandial (tom qab noj mov) glycemia. Thaum muaj qhov ua txhaum hnyav los ntawm dyspeptic tshwm sim, nws raug nquahu kom siv cov tshuaj no tom qab noj mov.

Cov teebmeem tsis tsim nyog ntawm sulfonylurea derivatives, ntxiv rau hypoglycemia, yog dyspeptic cuam tshuam (suav nrog xeev ntuav, ntuav, raws plab), mob cholestatic jaundice, hnyav nce, thim rov qab leukopenia, thrombocytopenia, agranulocytosis, aplastic thiab hemolytic anemia, kev tsis haum tshuaj khaus, erythema, dermatitis).

Kev siv cov sulfonylurea npaj thaum cev xeeb tub tsis pom zoo, vim tias feem ntau ntawm lawv zwm rau chav kawm C raws li FDA (Kev Tswj Xyuas Khoom Noj thiab Tshuaj), kev kho tshuaj insulin yog yam hloov pauv.

Cov neeg mob hnub nyoog siab tsis pom zoo siv cov tshuaj ntev ntev (glibenclamide) vim tias qhov pheej hmoo ntawm cov ntshav nce siab yuav nce. Thaum muaj lub hnub nyoog no, nws yog qhov zoo dua los siv luv-ntau yam kev kawm - gliclazide, glycidone.

Meglitinides - muaj kev pom zoo rau cov neeg tswj hwm (repaglinide, nateglinide).

Repaglinide yog ib qho kev sib txuas ntawm benzoic acid. Txawm hais tias qhov sib txawv hauv cov qauv hauv tshuaj los ntawm sulfonylurea derivatives, nws tseem thaiv ATP-nyob hauv cov pa roj carbon monoxide raws rau hauv cov qog ua haujlwm ntawm cov kab mob ntawm tes dej num hauv lub islet pancreatic apparatus, ua rau lawv cov depolarization thiab qhib cov calcium calcium, yog li ua kom muaj insulin ntau ntxiv. Kev siv tshuaj insulinotropic rau ib pluas noj muaj kev noj qab haus huv tsis pub dhau 30 feeb tom qab thov thiab muaj nrog cov ntshav qabzib tsawg dua thaum noj mov (qhov tsis haum ntawm insulin ntawm cov zaub mov tsis nce ntxiv). Zoo li sulfonylurea derivatives, lub ntsiab cuam tshuam yog hypoglycemia. Nrog kev ceev faj, repaglinide yog kho rau cov neeg mob uas mob rau daim siab thiab / lossis lub raum tsis ua haujlwm.

Nateglinide yog ib qho kev sib txuas ntawm D-phenylalanine.Tsis zoo li lwm tus kab mob hauv qhov ncauj hypoglycemic, cov nyhuv ntawm nateglinide ntawm cov tshuaj insulin tso tawm sai dua, tab sis tsis tshua pheej ua. Nateglinide siv feem ntau los txo qis tom qab hyperglycemia hauv ntshav qab zib hom 2.

Kev Loj Loj, uas pib siv los kho tus mob ntshav qab zib hom 2 hauv xyoo 70, tsis txhob siv tshuaj tua cov ntshav los ntawm kev mob ntshav qab zib. Lawv cov nyhuv yog tsuas yog txiav txim siab los ntawm kev cuam tshuam ntawm gluconeogenesis hauv daim siab (suav nrog glycogenolysis) thiab kev siv cov piam thaj ntau ntxiv los ntawm cov ntaub so ntswg peripheral. Lawv kuj inhibit qhov ua tsis tiav ntawm insulin thiab txhim kho nws txoj kev khi rau cov insulin receptors (qhov no nce ntawm kev nqus ntawm cov piam thaj thiab nws cov metabolism hauv).

Biguanides (tsis zoo li sulfonylurea derivatives) tsis txo cov ntshav qabzib hauv cov neeg muaj kev noj qab haus huv thiab hauv cov neeg mob uas muaj ntshav qab zib hom 2 tom qab lub hnub tsaus ntuj tsis zoo, tab sis tseem ceeb txwv nws nce ntxiv tom qab noj mov, tsis tas yuav ua rau muaj ntshav qab zib tsawg.

Hypoglycemic biguanides - metformin thiab lwm tus - kuj tseem siv rau hom 2 mob ntshav qab zib mellitus Ntxiv rau qhov ua kom cov suab thaj txo qis, loj kho, nrog kev siv lub sijhawm ntev, muaj qhov zoo ntawm lipid metabolism. Cov tshuaj ntawm cov pab pawg no inhibit lipogenesis (cov txheej txheem uas cov piam thaj thiab lwm yam tshuaj hloov mus rau hauv cov roj ntsha hauv lub cev), ua kom lipolysis (cov txheej txheem ntawm kev sib cais lipids, tshwj xeeb tshaj yog triglycerides muaj nyob hauv cov rog, rau hauv lawv cov roj ntsha los ntawm kev ua ntawm lipase enzyme), txo kev qab los noj mov, thiab txhawb nqa poob phaus. Qee qhov xwm txheej, lawv txoj kev siv yog nrog los txo qis cov ntsiab lus ntawm triglycerides, roj cholesterol thiab LDL (txiav txim siab hauv lub plab khoob) hauv cov ntshav cov ntshav. Ntawm cov ntshav qab zib mellitus hom 2, kev cuam tshuam ntawm cov metabolism carbohydrate yog ua ke nrog cov suab pauv hauv lipid metabolism. Yog li, 85-90% ntawm cov neeg mob uas mob ntshav qab zib hom 2 tau nce hauv lub cev hnyav. Yog li ntawd, nrog kev sib xyaw ntawm hom 2 mob ntshav qab zib mellitus nrog cov rog dhau, cov tshuaj normalizing lipid metabolism yog qhia.

Qhov qhia tau rau kev tswj hwm ntawm biguanides yog hom 2 mob ntshav qab zib mellitus (tshwj xeeb tshaj yog nyob rau hauv cov neeg mob nrog rog) nrog qhov tsis muaj txiaj ntsig ntawm kev noj zaub mov, nrog rau kev ua tsis tau zoo ntawm sulfonylurea npaj.

Thaum tsis muaj cov tshuaj insulin, cov nyhuv ntawm biguanides tsis tshwm.

Biguanides tuaj yeem siv ua ke nrog cov tshuaj insulin nyob rau hauv qhov chaw tiv thaiv nws. Kev sib xyaw ntawm cov tshuaj no nrog sulfonamide derivatives yog qhia nyob rau hauv cov xwm txheej uas tom kawg tsis muab kev txhim kho tiav ntawm kev tsis txaus siab ntawm metabolic. Biguanides tuaj yeem ua rau kev txhim kho ntawm cov kab mob lactic acidosis (kab mob lactic acidosis), uas txwv tsis pub siv tshuaj nyob hauv pab pawg no.

Biguanides tuaj yeem siv ua ke nrog cov tshuaj insulin nyob rau hauv qhov chaw tiv thaiv nws. Kev sib xyaw ntawm cov tshuaj no nrog sulfonamide derivatives yog qhia nyob rau hauv cov xwm txheej uas tom kawg tsis muab kev txhim kho tiav ntawm kev tsis txaus siab ntawm metabolic. Biguanides tuaj yeem ua rau kev txhim kho ntawm cov kab mob lactic acidosis (lactic acidosis), uas txwv kev siv qee yam tshuaj hauv pawg no.

Biguanides yog contraindicated nyob rau hauv muaj acidosis thiab ib tug nyiam rau nws (provoke thiab nce tsub zuj zuj ntawm lactate), nyob rau hauv tej yam kev mob nrog hypoxia (nrog rau lub plawv thiab ua pa tsis ua hauj lwm, mob theem ntawm myocardial infarction, mob cerebrovascular tsis txaus, anemia), thiab lwm yam.

Cov kev mob tshwm sim ntawm biguanides tau sau tseg ntau dua li sulfonylurea derivatives (20% tiv thaiv 4%), ua ntej txhua yam, mob plab hnyuv phiv: cov xim hlau hauv lub qhov ncauj, cov tsos mob dyspeptic, etc. Tsis zoo li sulfonylurea derivatives, hypoglycemia thaum siv biguanides (xws li metformin ) tshwm sim tsawg kawg.

Cov kab mob lactic acidosis, uas qee zaus zoo li thaum noj cov tshuaj metformin, suav tias yog ib qho kev mob hnyav, yog li metformin yuav tsum tsis txhob ua rau lub raum tsis ua haujlwm thiab cov mob uas cuam tshuam rau nws txoj kev txhim kho - lub raum tsis ua haujlwm thiab / lossis lub siab ua haujlwm, lub plawv tsis ua haujlwm, lub ntsws pathology.

Biguanides yuav tsum tsis txhob muab cov tshuaj ib txhij nrog cimetidine, txij li thaum lawv sib tw nrog kev sib tw hauv cov txheej txheem ntawm cov leeg tso zis rau hauv lub raum, uas tuaj yeem ua rau kom muaj kev nkag siab ntawm biguanides, ntxiv rau, cimetidine txo cov biotransformation ntawm biguanides hauv lub siab.

Kev sib xyaw ntawm glibenclamide (ib qho kev sib txuas ntawm sulfonylurea ntawm lub cim thib ob) thiab metformin (biguanide) tau ua kom zoo rau lawv lub zog, tso cai rau koj kom ua tiav cov kev xav txog hypoglycemic nrog rau kev txo qis ntawm txhua cov tshuaj thiab yog li txo qhov kev pheej hmoo ntawm kev phiv.

Txij li thaum xyoo 1997, nkag mus rau hauv kev xyaum kho mob thiazolidinediones (glitazones), lub hauv paus ntawm cov qauv hauv tshuaj lom neeg ntawm uas yog lub nplhaib thiazolidine. Pab pawg tiv thaiv kabmob tshiab no suav nrog pioglitazone thiab rosiglitazone. Cov tshuaj ntawm pab pawg no nce qhov rhiab ntawm cov nqaij mos lub hom phiaj (nqaij, adipose ntaub so ntswg, nplooj siab) rau insulin, qis lipid synthesis hauv cov leeg nqaij thiab cov rog. Thiazolidinediones yog cov xaiv cov agonists ntawm cov tshuaj tiv thaiv nuclear PPARγ (peroxisome proliferator-activated receptor-gamma). Hauv tib neeg, cov receptors no nyob rau hauv “lub hom phiaj cov ntaub so ntswg” uas yog qhov tseem ceeb rau ua cov insulin: hauv cov ntaub so ntswg adipose, hauv cov leeg pob txha thiab lub siab. PPARγ lub zog txais kev tswj cov transmissions ntawm insulin-teb cov noob koom nrog kev tswj hwm cov kua nplaum tsim khoom, thauj thiab siv. Ntxiv rau, PPARγ-rhiab cov noob koom tes nrog cov metabolism hauv kev ua kom muaj roj.

Txhawm rau thiazolidinediones siv lawv cov nyhuv, qhov yuav tsum muaj insulin yog qhov tsim nyog. Cov tshuaj no txo ​​cov insulin tsis kam ntawm peripheral cov ntaub so ntswg thiab lub siab, nce kev noj ntawm insulin-nyob rau hauv qabzib thiab txo cov kua qabzib tawm los ntawm daim siab, qis qis nruab nrab triglycerides, nce qhov nce ntawm HDL thiab cov cholesterol, thiab tiv thaiv hyperglycemia tom qab noj, nrog rau hemoglobin glycosylation.

Alpha Glucosidase Inhibitors (acarbose, miglitol) inhibit qhov tawg ntawm poly- thiab oligosaccharides, txo qhov tsim thiab nqus ntawm cov piam thaj hauv txoj hnyuv thiab thiaj li tiv thaiv kev txhim kho ntawm postprandial hyperglycemia. Carbohydrates noj nrog zaub mov tsis hloov pauv nkag mus rau qhov qis ntawm qhov me me thiab cov hnyuv, thaum lub sijhawm nqus cov monosaccharides ntev ntev txog 3-4 teev. Tsis zoo li sulfonamide hypoglycemic tus neeg sawv cev, lawv tsis nce insulin tso tawm thiab, yog li ntawd, tsis txhob ua rau muaj ntshav qab zib tsawg.

Nws tau pom tias kev kho mob acarbose ntev yog nrog kev txo qis txaus ntshai ntawm kev pheej hmoo ntawm kev txhim kho mob plawv ntawm cov mob atherosclerotic. Alpha glucosidase inhibitors yog siv los ua kev kho mob lossis siv nrog lwm tus neeg hauv lub qhov ncauj qog ntshav. Thawj koob tshuaj yog 25–50 mg tam sim ntawd ua ntej lossis thaum noj mov, thiab tom qab ntawd tuaj yeem maj mam nce ntxiv (qhov koob tshuaj txhua hnub yog 600 mg).

Cov lus qhia rau kev siv alpha-glucosidase inhibitors yog hom 2 mob ntshav qab zib mellitus nrog kev kho mob tsis muaj txiaj ntsig (qhov kev kawm uas yuav tsum yog tsawg kawg 6 lub hlis), nrog rau hom 1 mob ntshav qab zib mellitus (ua ib feem ntawm kev sib xyaw ua ke).

Cov tshuaj ntawm cov pab pawg no tuaj yeem ua rau dyspeptic tshwm sim los ntawm kev ua txhaum ntawm kev zom thiab nqus ntawm cov carbohydrates, uas yog metabolized hauv txoj hnyuv nrog kev tsim cov roj, carbon dioxide thiab hydrogen. Yog li no, thaum kho mob alpha-glucosidase inhibitors, nruj ua raws li kev noj zaub mov nrog cov ntsiab lus tsawg tsawg ntawm cov kev ua kom muaj roj, nrog rau sucrose.

Acarbose tuaj yeem ua ke nrog lwm cov tshuaj tiv thaiv kab mob siab. Neomycin thiab colestyramine txhim kho cov nyhuv ntawm acarbose, thaum lub zaus thiab mob ntawm cov kev mob tshwm sim los ntawm lub plab zom mov nce ntxiv. Thaum ua ke nrog antacids, adsorbents thiab enzymes uas txhim kho kev zom zaub mov, cov txiaj ntsig ntawm acarbose txo qis.

Tam sim no, chav kawm tshiab ntawm cov kab mob hypoglycemic tau tshwm sim - ncetinomimetics. Cov tshuaj muaj ntau yog cov tshuaj hormones uas ua zais los ntawm qee yam mob me me hauv cov hnyuv hauv kev teb rau kev noj zaub mov thiab ua rau muaj cov kua dej hauv lub cev. Ob qho tshuaj hormones tau raug cais tawm: glucagon-zoo li polypeptide (GLP-1) thiab glucose-nyob insulinotropic polypeptide (HIP).

Txhawm rau nce zuj zus suav nrog 2 pawg tshuaj:

- cov yeeb yaj kiab uas qog tau qhov tshwm sim ntawm GLP-1 - analogues ntawm GLP-1 (liraglutide, exenatide, lixisenatide),

- cov tshuaj ncua ntev rau qhov kev txiav txim ntawm endogenous GLP-1 vim qhov thaiv ntawm dipeptidyl peptidase-4 (DPP-4) - ib qho enzyme uas txav GLP-1 - DPP-4 inhibitors (sitagliptin, vildagliptin, saxagliptin, linagliptin, alogliptin).

Yog li, pab pawg ntawm hypoglycemic tus neeg sawv cev suav nrog tus naj npawb ntawm cov tshuaj zoo. Lawv muaj cov txheej txheem sib txawv ntawm kev txiav txim, txawv hauv pharmacokinetic thiab pharmacodynamic tsis. Kev paub txog cov yam ntxwv no tso cai rau tus kws kho mob ua qhov kev xaiv ntau tshaj plaws thiab kho kom raug.

Cov Yuav Tsum Muaj

• 1. Hom 1 mob ntshav qab zib.
• 2. Mob ntshav qab zib ketoacidosis (ib qho dhau ntawm cov ntshav ntawm ketone lub cev), tsis xeev plab.
• 3. Cev xeeb tub thiab lactation.
• 4. Kab mob siab thiab mob siab uas muaj qhov ua haujlwm tsis zoo.
• 5. Lub plawv tsis ua haujlwm.
• 6. Hypersensitivity rau cov tshuaj.

Thiazolidinedione npaj

Troglitazone (Rezulin) yog cov tshuaj ntawm thawj tiam ntawm pab pawg no. Nws tau rov qab los ntawm qhov muag, vim nws cov nyhuv cuam tshuam tsis zoo rau daim siab.

Rosiglitazone (Avandia) yog hom tshuaj thib peb hauv pab pawg no. Nws tsis kam siv hauv xyoo 2010 (txwv tsis pub nyob hauv European Union) tom qab tau muaj pov thawj tias nws ua rau muaj kev pheej hmoo ntawm cov kab mob plawv.

Daim ntawv thov nyhuv

Tsis tas li ntawd, nws tau raug pov thawj tias cov tshuaj muaj qee cov txiaj ntsig zoo ntxiv:

• Lowers ntshav siab
• Cuam tshuam rau theem ntawm cov roj (txhaws qhov nce ntawm "cov roj (cholesterol)" zoo, uas yog, HDL, thiab tsis nce "cov roj (cholesterol) phem" - LDL),
• Nws inhibits qhov tsim thiab loj hlob ntawm atherosclerosis,
• Txo txo ​​txoj kev pheej hmoo mob plawv (piv txwv li, mob plawv nres, mob stroke).

Nyeem ntxiv: Jardins yuav tiv thaiv lub siab

Rau leej twg pioglitazone yog kws kho

Pioglitazone tuaj yeem siv los ua ib qho yeeb tshuaj, i.e. tshuaj mob hlwb. Tsis tas li, yog tias koj muaj hom 2 mob ntshav qab zib mellitus, koj cov kev hloov pauv hauv kev ua neej tsis muab cov txiaj ntsig kev cia siab thiab muaj contraindications rau metformin, nws qhov tsis ua siab ntev thiab muaj kev phiv

Kev siv ntawm pioglitazone yog ua tau nrog kev sib xyaw nrog lwm cov tshuaj tiv thaiv kab mob (piv txwv li, acarbose) thiab metformin yog tias lwm cov kev coj ua tsis coj ua tiav

Pioglitazone tseem tuaj yeem siv nrog cov kua dej insulin, tshwj xeeb tshaj yog rau cov tib neeg uas lawv lub cev cuam tshuam rau metformin tsis zoo.

Nyeem ntxiv: Yuav noj cov tshuaj metformin li cas

Yuav ua li cas noj pioglitazone

Cov tshuaj yuav tsum noj ib hnub ib zaug, hais ntawm ncauj, thaum lub sijhawm lav. Qhov no tuaj yeem ua tau ob qho ua ntej thiab tom qab noj mov, vim tias cov zaub mov tsis cuam tshuam rau kev nqus ntawm cov tshuaj. Kev kho mob feem ntau yog pib nrog qhov qis dua. Hauv qhov xwm txheej uas qhov tshwm sim ntawm kev kho tsis zoo, nws tuaj yeem maj mam dhau los.

Qhov ua tau zoo ntawm cov tshuaj pom nyob rau hauv rooj plaub uas yuav tsum tau kho mob ntshav qab zib hom 2, tab sis siv tsis tau metformin, kev kho mob monotherapy nrog rau ib qho tshuaj tsis raug tso cai.

Ntxiv rau qhov tseeb tias pioglitazone txo qis postprandial glycemia, ntshav qabzib thiab khov kho glycated hemoglobin, nws kuj tseem muaj cov txiaj ntsig zoo ntxiv ntawm cov ntshav siab thiab ntshav cov roj. Tsis tas li ntawd, nws tsis ua kev tsis haum.

Thiazolidinedione npaj

Thiazolidinediones (TZD) - chav kawm tshiab ntawm cov tshuaj tiv thaiv kab mob rau kev siv ncauj. Thiazolidinedione tshuaj (pioglitazone, rosiglitazone) tau nkag mus hauv tsev kho mob kev coj ua hauv xyoo tas los no xwb. Zoo li biguanides, cov tshuaj no tsis txhawb kev tsim txom cov tshuaj insulin, tab sis nce siab rhiab ntawm cov ntaub so ntswg txuas rau nws. Cov sib xyaw ntawm cov chav kawm no ua cov agonists ntawm nuclear PPAR-y receptors (peroxisome proliferator-activated receptor). Cov receptors no muaj nyob hauv cov rog, nqaij thiab lub siab. Kev ua kom zoo ntawm PPAR-y receptors hloov kho cov kev sib hloov ntawm ntau cov noob cuam tshuam nrog kev sib kis ntawm cov teebmeem ntawm insulin rau kev nkag mus ntawm cov piam thaj thiab lipids mus rau hauv cov hlwb. Ntxiv rau qhov qis dua ntawm qib glycemia, txhim kho qhov rhiab ntawm cov ntaub so ntswg mus rau insulin haum rau lipid profile (qib ntawm lipoproteins ntau ntom nce, cov ntsiab lus ntawm triglycerides txo). Muab hais tias cov tshuaj no ua los ntawm kev txhawb cov noob hloov ntaub ntawv, nws yuav siv sijhawm ntev txog 2-3 lub hlis kom tau txais cov txiaj ntsig siab. Hauv cov kev tshawb fawb soj ntsuam, cov tshuaj no muab txo qis hauv HbAc nrog kev kho mob monotherapy txog li 0.5 txog 2%.

Cov tshuaj hauv cov hoob kawm no tuaj yeem siv ua ke nrog PSM, insulin lossis metformin. Kev sib xyaw nrog metformin tsuas yog txiav txim siab vim qhov tseeb tias kev nqis tes ntawm biguanides feem ntau yog tsom kwm ntawm kev tiv thaiv gluconeogenesis, thiab qhov kev nqis tes ntawm thiazolidinediones yog txhawm rau nce kev siv peripheral qabzib. Lawv xyaum ua tsis tau rau kev mob ntshav qab zib (tab sis, zoo li biguanides, lawv tuaj yeem nce ntau zaus ntawm cov ntshav qog ntshav qis nyob rau hauv kev sib xyaw nrog cov tshuaj uas txhawb cov tshuaj insulin secretion). Lub txiaj ntsig tseem ceeb yog kev siv cov peripheral glucose thiab txo cov glycogenesis los ntawm kev ua kom muaj zog ntawm cov insulin-rhiab noob (txo qis hauv insulin tsis kam). Thiazolidinediones ua cov tshuaj uas tshem tawm cov tshuaj tiv thaiv insulin, ua rau muaj kev txhim kho ntshav qab zib hom 2 yog cov pab pawg zoo tshaj plaws rau kev tiv thaiv tus kab mob ntshav qab zib hom 2. Qhov kev tiv thaiv ntawm thiazolidinediones tseem muaj ntau dua 8 lub hlis tom qab nws tshem tawm. Muaj kev xav tias glitazones muaj peev xwm ua kom tiav qhov kev tshuaj ntsuam caj ces ntawm cov metabolism hauv qabzib, uas tso cai tsis tsuas yog ncua kev txhim kho ntawm cov ntshav qab zib hom 2, tab sis kuj yuav tshem tawm nws txoj kev txhim kho kom tiav.

Txawm li cas los xij, kom txog rau qhov no tsuas yog ib qho kev xav.

Kev siv ntawm thiazolidinediones hauv cov neeg mob uas muaj ntshav qab zib hom 2 qhib kev cia siab rau kev tiv thaiv kev mob plawv, qhov kev txhim kho ntawm qhov uas feem ntau yog vim muaj cov tshuaj tiv thaiv insulin tam sim no. Cov ntawv qhia ua ntej hais txog cov nyhuv angioprotective ntawm thiazolidinediones twb tau los ntawm qee cov kev tshawb nrhiav sim. Cov kev tshawb fawb tshawb fawb zoo sib xws tseem tsis tau ua.

Muaj peb tiam ntawm thiazolidinediones hauv lub ntiaj teb:
- "thawj tiam" yeeb tshuaj - troglitazone (tsom qhia cov kab mob hepatotoxic thiab cardiotoxic effect, txuas nrog uas nws tau txwv rau kev siv),
- cov tshuaj ntawm "tiam thib ob" - pioglitazone,
- "thib peb tiam" tshuaj - rosiglitazone.

Tam sim no, ib hom tshuaj los ntawm thiazolidinediones tiam thib ob - actos (pioglitazone hydrochloride) los ntawm Eli Lilly (USA) thiab lub cim thib peb - ​​avandium (rosiglitazone) tau sau npe nyob hauv Russia. Actos muaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj muaj 15,30 thiab 45 mg ntawm cov tshuaj nquag pioglitazone hydrochloride, ib hnub ib zaug, tsis hais txog kev noj zaub mov.

Cov koob tshuaj txhua hnub yog 30-45 mg. Glaxo SmithKJine Avandia (GSK) muaj nyob rau hauv cov ntsiav tshuaj ntawv uas muaj 4 thiab 8 mg ntawm cov tshuaj nquag ntawm rosiglitazone, ib zaug lossis ob zaug ib hnub, tsis hais txog ntawm cov zaub mov noj. Txhua hnub koob tshuaj 8 mg. Nws tau npaj los tso cov tshuaj sib xyaw los ntawm tib lub tuam txhab - Avandamet (kev sib xyaw ntawm avandia thiab metformin).

Thiazolidinediones siv los ua kev kho mob, tab sis zoo dua los ntawm kev sib xyaw nrog biguanides, acarbose, PSM, insulin hauv cov neeg mob ntshav qab zib hom 2. Kev siv tshuaj tsawg ntawm cov pab pawg no vim lawv tus nqi ntau heev.Cov tshuaj, uas belongs rau lub cim thib ob ntawm thiazolidinediones, pom tsis muaj cov tshuaj hepatotoxic. Pioglitazone tsis ua haujlwm nyob rau hauv daim siab, ua rau lub cev cov khoom noj nquag, ua rau lub cev ntuag nrog cov kua tsib. Ib qho ntawm cov kev mob tshwm sim tuaj yeem yog cov tsos ntawm edema, ntxiv rau qhov hnyav ntxiv. Tawm tsam ntawm keeb kwm ntawm kev kho mob, nws raug nquahu kom tswj cov theem ntawm alanine thiab aspartic aminotransferase thiab tsum tsis txhob noj cov tshuaj ntawm ib qho enzyme uas yog ob zaug ntawm kev coj ua. Nws raug nquahu kom soj ntsuam cov nyhuv ntawm cov tshuaj nrog kev kho ntev (3-hlis). Cov Tshuaj Tiv Thaiv:
- hom ntshav qab zib 1
- ketoacidosis nrog rau ib hom ntshav qab zib,
- cev xeeb tub, lactation,
- dhau ntawm qhov kev hloov pauv ntawm alanine transferase 3 zaug,
- mob khaub thuas, kis mob siab,
- mob siab dhia mob siab.

Kev Tiv Thaiv Ntawm Ntshav Qab Zib Hom 2

DREAM kev kuaj mob pom tias muaj kev pheej hmoo txhim kho cov ntshav qab zib hauv cov neeg mob uas tsis txaus siab cov ntshav qabzib thiab nce siab sai nyob rau hauv cov neeg mob noj rosiglitazone (11, kuj pom 12). Txoj kev tshawb no qhia tau hais tias kev txhim kho ntshav qab zib tuaj yeem ncua sijhawm 1.5 xyoo, tab sis tom qab ntawd txoj kev pheej hmoo ntawm kev loj hlob nce thiab ua tib yam li cov pab pawg placebo.