Amaryl® (4 mg) Glimepiride

Kev piav qhia ntawm daim ntawv tshuaj

Amaryl ® 1 mg: ntsiav tshuaj ntawm cov xim liab, oblong, tiaj tus nrog txoj kab sib faib ntawm ob sab. Kos rau "NMK" thiab stylized "xyob h"Ntawm ob sab.

Amaryl ® 2 mg: cov ntsiav tshuaj ntsuab, oblong, tiaj tus nrog txoj kab sib faib ntawm ob sab. Engraved "NMM" thiab stylized "xyob h"Ntawm ob sab.

Amaryl ® 3 mg: ntsiav tshuaj daj ntseg daj, oblong, tiaj tus nrog txoj kab sib faib ntawm ob sab. Sau "NMN" thiab "stylized"xyob h"Ntawm ob sab.

Amaryl ® 4 mg: cov ntsiav tshuaj xiav, oblong, tiaj tus nrog cov kab sib faib ntawm ob tog. Engraved "NMO" thiab stylized "xyob h"Ntawm ob sab.

Cov Tshuaj Hauv Tshuaj

Glimepiride txo qis cov ntsiab lus ntawm cov piam thaj hauv cov ntshav, feem ntau vim yog kev tsa los ntawm kev tso tawm ntawm cov kua dej los ntawm beta hlwb ntawm cov txiav. Nws cov nyhuv yog feem ntau cuam tshuam nrog kev txhim kho nyob rau hauv lub peev xwm ntawm pancreatic beta hlwb los teb rau lub zog kev xav nrog cov piam thaj. Piv nrog rau glibenclamide, kev noj cov tshuaj glimepiride tsawg ua rau muaj cov insulin tsawg dua thaum ua tiav ntawm cov kwv yees li qub hauv cov ntshav qabzib. Qhov tseeb no ua tim khawv nyob rau hauv kev pom zoo ntawm muaj cov kab mob ntxiv ntawm cov qog ntshav hypoglycemic nyob rau hauv glimepiride (nce rhiab heev ntawm cov ntaub so ntswg mus rau insulin thiab cov nyhuv insulin-mimetic).

Cov tshuaj insulin zais cia. Zoo li txhua lwm yam sulfonylurea derivatives, glimepiride tswj hwm cov kua dej los ntawm kev sib koom tes nrog ATP-nkag siab poov tshuaj raws ntawm beta-cell daim nyias nyias. Tsis zoo li lwm cov sulfonylurea derivatives, glimepiride xaiv khi rau cov protein nrog cov molecular phaus ntawm 65 kilodaltons (kDa) nyob rau hauv cov qog ua rau ntawm pancreatic beta hlwb. Qhov no sib cuam tshuam ntawm glimepiride nrog cov protein sib khi ua kom nws tswj qhov qhib lossis kaw ntawm ATP-nkag mus poov tshuaj raws.

Glimepiride kaw cov kab xo potassium. Qhov no ua rau depolarization ntawm beta hlwb thiab coj mus rau qhov qhib ntawm voltage-rhiab calcium channel thiab qhov khiav ntawm calcium tuaj rau hauv lub cell. Raws li qhov tshwm sim, ib qho kev nce ntxiv hauv cov tshuaj calcium uas muaj siab tshaj yuav ua rau cov insulin secretion los ntawm exocytosis.

Glimepiride ua tau nrawm dua thiab yog li thiaj li nkag los rau hauv kev sib cuag thiab raug tso tawm los ntawm daim ntawv cog lus nrog cov protein uas khi rau nws dua li glibenclamide. Nws tau kwv yees tias cov cuab yeej no ntawm kev hloov pauv siab ntawm glimepiride nrog cov protein khi rau nws txiav txim siab nws cov lus tshaj tawm ntawm kev nkag siab ntawm cov hlwb hlwb rau cov piam thaj thiab lawv cov kev tiv thaiv tiv thaiv desensitization thiab ntxov ntxov.

Cov nyhuv ntawm nce zuj zus cov ntaub so ntswg mus rau insulin. Glimepiride ua rau kev cuam tshuam zoo ntawm insulin rau ntawm qhov nqus ntawm cov piam thaj los ntawm cov ntaub so ntswg peripheral.

Cov tshuaj Insulinomimetic. Glimepiride muaj cov teebmeem zoo ib yam li cov tshuaj insulin rau ntawm qhov nqus ntawm cov piam thaj los ntawm cov ntaub so ntswg thiab kev tso tawm cov piam thaj los ntawm lub siab.

Peripheral cov ntaub so ntswg qabzib yog nqus tau los ntawm kev thauj nws mus rau hauv cov leeg nqaij thiab adipocytes. Glimepiride ncaj qha nce tus naj npawb ntawm cov lwg me nyuam thauj cov piam thaj hauv plasma cov leeg ntawm cov leeg nqaij thiab adipocytes. Kev nce ntxiv ntawm kev noj cov ntshav qabzib ua rau kev ua haujlwm ntawm glycosylphosphatidylinositol-phospholipase C. Yog li ntawd, cov tshuaj calcium calcium uas tsis txaus siab poob qis, ua rau muaj kev cuam tshuam ntawm cov dej num ntawm protein kinase A, uas ua rau lub ntsej muag ua rau lub zog ntawm cov metabolism glucose.

Glimepiride inhibits kev tso tawm ntawm qabzib los ntawm lub siab los ntawm kev nce lub siab ntawm fructose-2,6-bisphosphate, uas inhibits gluconeogenesis.

Ntxim rau platelet aggregation. Glimepiride txo cov platelet sib sau ua ke hauv vitro thiab hauv vivo Cov. Cov nyhuv no zoo li cuam tshuam nrog kev xaiv inhibition ntawm COX, uas yog lub luag haujlwm rau kev tsim ntawm thromboxane A, ib qho tseem ceeb endogenous platelet aggregation factor.

Antiatherogenic nyhuv ntawm cov tshuaj. Glimepiride pab txhawb rau kev kho lipid cov ntsiab lus, txo cov ntsiab lus ntawm malondialdehyde hauv cov ntshav, uas ua rau txo qis lipid peroxidation. Hauv cov tsiaj txhu, glimepiride ua rau muaj qhov txo qis hauv kev tsim ntawm atherosclerotic plaques.

Txo oxidative kev ntxhov siab, uas yog tas li nyob rau hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus. Glimepiride nce cov ntsiab lus ntawm endogenous to-tocopherol, cov haujlwm ntawm catalase, glutathione peroxidase thiab superoxide dismutase.

Kev mob plawv. Los ntawm ATP-nkag siab cov potassium (saib saud), sulfonylurea derivatives kuj cuam tshuam rau CCC. Piv rau cov tshuaj sulfonylurea derivatives, glimepiride muaj cov txiaj ntsig qis dua ntawm CCC, uas tuaj yeem piav qhia los ntawm qhov xwm txheej tshwj xeeb ntawm nws cov kev cuam tshuam nrog cov protein txuas ntawm ATP-nkag siab poov tshuaj raws.

Hauv cov neeg ua haujlwm noj qab haus huv, cov tshuaj txhaj tsawg kawg ntawm glimepiride yog 0.6 mg. Cov nyhuv ntawm glimepiride yog koob tshuaj thiab rov ua dua tshiab. Lub cev muaj zog teb rau kev ua lub cev (txo qis insulin qis) nrog glimepiride yog tswj.

Tsis muaj qhov sib txawv ntawm cov nyhuv, nyob ntawm seb cov tshuaj tau noj 30 feeb ua ntej noj mov lossis ua ntej noj mov. Hauv cov neeg mob ntshav qab zib, kev tswj kev zom zaub mov txaus tuaj yeem ua tiav nyob hauv 24 teev nrog tib lub tshuaj. Ntxiv mus, hauv kev soj ntsuam mob, 12 ntawm 16 cov neeg mob raum tsis ua haujlwm (Cl creatinine 4–79 ml / min) kuj ua tiav cov kev tswj cov zom zaub mov txaus.

Kev sib xyaw ua ke nrog metformin. Hauv cov neeg mob uas lub cev tsis txaus tswj kev tiv thaiv thaum siv ntau tshaj plaws ntawm glimepiride, kev sib txuas ua ke nrog glimepiride thiab metformin tuaj yeem pib ua. Hauv ob txoj kev tshawb nrhiav, thaum ua cov kev kho mob sib xyaw ua ke, nws tau ua pov thawj tias kev tswj cov metabolism yog qhov zoo dua li ntawm kev kho mob ntawm txhua yam ntawm cov tshuaj cais tawm.

Kev sib xyaw ua ke nrog cov tshuaj insulin. Hauv cov neeg mob uas tsis muaj cov tswj kev noj zaub mov kom tsis txaus, kev kho tshuaj insulin ib txhij tuaj yeem pib muaj qhov siab tshaj plaws ntawm glimepiride. Raws li cov txiaj ntsig ntawm ob txoj kev tshawb nrhiav, nrog kev siv ntawm kev sib xyaw ua ke no, tib txoj kev tswj kev noj zaub mov zoo yog ua tiav nrog kev siv ntawm ib qho tshuaj insulin, txawm li cas los xij, kev kho mob sib xyaw ua ke xav tau qis dua cov tshuaj insulin.

Siv rau menyuam yaus. Muaj cov ntaub ntawv tsis txaus ntawm kev ua haujlwm ntev thiab kev nyab xeeb ntawm cov tshuaj rau menyuam yaus.

Cov Tshuaj Pharmacokinetics

Nrog kev siv tas li ntawm glimepiride hauv ib koob tshuaj txhua hnub ntawm 4 mg C_max hauv cov dej ntshiab tau mus txog tom qab li 2,5 teev thiab yog 309 ng / ml. Muaj txoj kab sib txuas ntawm koob tshuaj thiab C_max glimepiride nyob rau hauv ntshav, ntxiv rau ntawm koob thiab AUC. Thaum noj cov glimepiride nws qhov kev qhia tseeb txog kev noj qab haus huv tau ua tiav. Noj mov tsis muaj kev cuam tshuam loj ntawm kev nqus, nrog rau kev zam ntawm kev ua kom qeeb me ntsis hauv nws qhov ceev. Glimepiride yog tus cwj pwm los ntawm V qis heev_d (li ntawm 8.8 L), kwv yees li V_d albumin, qhov kev kawm siab ntawm kev muab khi rau cov ntshav plasma protein (ntau dua li 99%) thiab tsis pom tseeb (li 48 ml / min). Nruab Nrab T_1/2 , txiav txim siab los ntawm ntshav siab ntau nyob rau hauv cov kev mob ntawm kev rov ua dua ntawm cov tshuaj, yog kwv yees li 5-8 teev. Tom qab noj ntau, muaj qhov nce siab hauv T_1/2 .

Tom qab txhaj ib koob tshuaj glimepiride, 58% koob tshuaj yog tawm los ntawm ob lub raum thiab 35% ntawm cov koob tshuaj los ntawm txoj hnyuv. Kev hloov pauv glimepiride nyob rau hauv cov zis tsis kuaj.

Hauv cov zis thiab cov quav, ob hom metabolites tau txheeb xyuas uas tau tsim los ntawm cov metabolism hauv lub siab (feem ntau nrog kev pab los ntawm CYP2C9), ib qho ntawm lawv yog hydroxy derivative, thiab lwm qhov carboxy derivative. Tom qab noj ntawm glimepiride, lub davhlau ya nyob twg T_1/2 ntawm cov metabolites yog 3-5 thiab 5-6 h, ntsig txog.

Glimepiride ua haujlwm tawm hauv cov kua mis thiab hla tus qib placental.

Kev sib piv ntawm ib qho thiab ntau yam (ib zaug ib hnub) kev tswj hwm glimepiride tsis qhia tawm qhov sib txawv tseem ceeb hauv cov chaw muag tshuaj, lawv qhov kev hloov pauv ntawm cov neeg mob sib txawv. Tsis muaj qhov tseem ceeb tsub zuj zuj ntawm cov tshuaj.

Pharmacokinetic cov cim muaj qhov zoo sib xws hauv cov neeg mob sib txawv thiab pawg hnub nyoog sib txawv. Hauv cov neeg mob uas tsis zoo lub raum (nrog rau qhov tsis muaj creatinine tsawg), muaj qhov nyiam ua kom lub qhov txhaws ntau ntxiv thiab txo qis hauv nws cov ntsiab lus nruab nrab hauv cov ntshav cov ntshav, uas, txhua qhov yuav tshwm sim, vim sai dua cov tshuaj vim qhov cuam tshuam ntawm cov protein tsawg. Yog li, hauv pawg no ntawm tus neeg mob tsis muaj kev pheej hmoo ntxiv los khaws cov tshuaj.

Cov Yuav Tsum Muaj

hypersensitivity rau glimepiride lossis rau ib yam dab tsi pabcuam ntawm cov tshuaj, lwm yam sulfonylurea derivatives lossis sulfonamide tshuaj (muaj kev pheej hmoo ntawm hypersensitivity tshua),

ntshav qab zib hom 1

ketoacidosis, mob ntshav qab zib precoma thiab coma,

mob ua rau daim siab mob hnyav (tsis muaj kev tshawb nrhiav hauv chaw kuaj mob),

mob raum tsis zoo, suav nrog nyob rau hauv cov neeg mob ntawm mob hemodialysis (tsis muaj kev kuaj mob hauv chaw kho mob),

tsis tshua muaj cov kab mob xws li galactose intolerance, lactase deficiency lossis glucose-galactose malabsorption,

cov menyuam yaus hnub nyoog (tsis muaj kev paub hauv chaw kuaj mob).

hauv thawj lub lis piam ntawm kev kho mob (muaj kev pheej hmoo ntshav siab qog ntshav). Yog tias muaj kev pheej hmoo txaus rau kev txhim kho hypoglycemia (saib Ntu "Cov Lus Qhia Tshwj Xeeb"), yuav tsum tau txhaj koob tshuaj glimepiride lossis kev kho txhua yam,

nrog cov kabmob sib kis thaum kho lossis nrog kev hloov pauv ntawm lub neej ntawm cov neeg mob (hloov hauv kev noj zaub mov thiab lub sijhawm noj mov, nce lossis txo qis rau kev tawm dag zog),

nrog piam thaj-6-phosphate dehydrogenase tsis muaj peev xwm,

nrog malabsorption ntawm cov zaub mov thiab tshuaj hauv plab zom mov (mob hnyuv, mob plab hnyuv).

Yam 1 ntshav qab zib. - Tus kab mob ntshav qab zib ketoacidosis, mob ntshav qab zib precoma thiab coma. - Cov tshuaj tiv thaiv tsis haum rau glimepiride lossis rau ib yam dab tsi pabcuam ntawm cov tshuaj, rau lwm tus sulfonylurea derivatives lossis rau lwm yam sulfanilamide npaj (kev pheej hmoo ntawm kev tiv thaiv hypersensitivity). - Kev ua rau lub siab ua haujlwm tsis zoo (tsis muaj kev tshawb nrhiav hauv lub sijhawm). - Kev cuam tshuam ntawm lub raum tsis zoo, suav nrog cov neeg mob kho mob hemodialysis (tsis muaj kev sim kho mob). - Cev xeeb tub thiab lactation. - Cov menyuam yaus lub hnub nyoog (tsis muaj kev ntsuam xyuas mob). - Cov kab mob tsis tshua muaj mob xws li galactose intolerance, lactase deficiency lossis glucose-galactose malabsorption tsis txaus.

Cev xeeb tub thiab lactation

Glimepiride yog sib xyaw rau cov poj niam cev xeeb tub. Kev xeeb menyuam hauv plab lossis thaum pib cev xeeb tub, tus pojniam yuav tsum pauv mus rau kev kho mob insulin.

Glimepiride kis mus rau hauv niam mis, yog li nws tsis tuaj yeem siv thaum lactation. Hauv qhov no, koj yuav tsum hloov mus rau kev siv tshuaj insulin lossis txwv kev pub niam mis.

Sab sij huam

Qhov ntau zaus ntawm cov kev mob tshwm sim tau txiav txim siab raws li WHO kev faib tawm: feem ntau (≥10%), feem ntau (≥1%, ® hypoglycemia yuav loj hlob tuaj, uas, zoo li lwm yam sulfonylurea derivatives, tuaj yeem siv sijhawm ntev.

Cov tsos mob ntawm tus mob hypoglycemia yog: mob taub hau, tshaib plab, xeev siab, ntuav, hnov ​​nkees, tsaug zog, pw tsaug zog, ntxhov siab vim, txhoj puab heev, tsis meej pem thiab mob hlwb psychomotor tshua, kev nyuaj siab, tsis meej pem, hais lus tsis meej, tsis meej pem, pom kev tsis meej, tshee tshee, paresis, hnov ​​lub siab tsis sib xws, kiv taub hau, ploj ntawm kev tswj tus kheej, tsis paub pab, delirium, lub hlwb txhaws, tsis ntseeg thiab tsis nco qab, mus txog thaum tsis nco qab, ua pa nyuaj, bradycardia.

Tsis tas li ntawd, tej zaum yuav muaj cov tsos mob ntawm adrenergic counterregulation nyob rau hauv kev teb rau kev txhim kho cov ntshav qab zib, xws li nce hws, txias thiab ntub ntawm daim tawv nqaij, nce kev ntxhov siab, tachycardia, nce ntshav siab, angina pectoris, palpitations thiab mob plawv mob siab.

Cov lus qhia soj ntsuam ntawm cov ntshav khov qis yuav zoo ib yam li mob hlab ntsha tawg. Cov tsos mob ntawm hypoglycemia yuav luag ploj tom qab nws tshem tawm.

Qhov hnyav nce. Thaum noj glimepiride, zoo li lwm yam sulfonylurea derivatives, qhov nce hauv lub cev qhov hnyav yog ua tau (ntau zaus tsis paub).

Los ntawm sab ntawm cov khoom ntawm lub zeem muag: lub sijhawm kho (tshwj xeeb thaum pib), qhov pom kev tsis pom kev zoo vim muaj qhov hloov pauv hauv cov ntshav qabzib hauv lub siab yuav pom. Lawv qhov ua rau yog ib ntus hloov ntawm qhov lo ntsiab muag o, nyob ntawm kev mloog ntawm cov piam thaj hauv cov ntshav, thiab vim qhov no, qhov hloov pauv ntawm qhov lo ntsiab muag ntawm lub lo ntsiab muag.

Los ntawm cov hnyuv: tsis tshua muaj - xeev siab, ntuav, zoo nkaus li hnyav lossis txia ntawm thaj chaw epigastric, mob plab, raws plab.

Nyob rau ib feem ntawm daim siab thiab kais plab: hauv qee kis, kab mob siab, ua haujlwm nce siab ntawm daim siab enzymes thiab / lossis cholestasis thiab daj ntseg, uas tuaj yeem ua rau lub siab ua rau lub siab tsis ua haujlwm, tab sis yuav dhau los ua kev thim rov qab thaum cov tshuaj txiav tawm.

Ntawm ib feem ntawm cov ntshav thiab cov lymphatic system: tsis tshua muaj thrombocytopenia, nyob rau qee kis - leukopenia, hemolytic anemia, erythrocytopenia, granulocytopenia, agranulocytosis thiab pancytopenia. Hauv kev tshaj tawm txog kev siv tshuaj, cov teeb meem loj ntawm thrombocytopenia nrog lub platelet suav tsawg dua 10,000 / μl thiab thrombocytopenic purpura (zaus tsis paub) tau qhia.

Los ntawm lub nruab zog: tsis tshua muaj - ua xua thiab pseudo-kev tawm tsam tsis haum, xws li mob pruritus, urticaria, tawv nqaij ua pob. Cov kev xav zoo li no yuav luag tas li muaj mob me, tab sis tuaj yeem nkag mus rau qhov kev tsis haum nrog ua pa luv, txo qis ntshav siab, uas qee zaum nce mus rau qhov kev poob siab anaphylactic. Yog tias cov tsos mob ntawm tus mob urticaria tshwm sim, sab laj nrog tus kws kho mob tam sim ntawd. Kev phiv khaub thuas muaj peev xwm ua tau nrog lwm cov sulfonylurea derivatives, sulfonamides lossis cov khoom sib xws, qee qhov muaj kev tsis haum tshuaj vasculitis.

Ntawm ib feem ntawm daim tawv nqaij thiab cov nqaij mos subcutaneous: hauv qee kis - photosensitivity, qhov tsawg tsis paub - alopecia.

Kuaj thiab ntsuas cov ntaub ntawv: hauv qee kis - hyponatremia.

Kev sib txuam

Glimepiride yog metabolized los ntawm cytochrome P4502C9 (CYP2C9), uas yuav tsum tau coj mus rau hauv tus account thaum siv ib txhij nrog cov inducers (piv txwv li rifampicin) lossis inhibitors (e.g. fluconazole) CYP2C9.

Potentiation ntawm hypoglycemic kev txiav txim siab thiab, nyob rau qee kis, kev loj hlob tau ntawm hypoglycemia cuam tshuam nrog nws tej zaum yuav pom thaum ua ke nrog ib qho ntawm cov tshuaj hauv qab no: insulin thiab lwm yam kab mob hypoglycemic rau kev tswj hwm qhov ncauj, ACE inhibitors, anabolic steroids thiab txiv neej pw ua ke, chloramphenicol, coumarin derivatives, cyclophosphamide, disopyramide, fenfluramine, pheniramidol, fibrates, fluoxetine, guanethide MAO inhibitors, fluconazole, para-aminosalicylic acid, pentoxifylline (siab ntau koob tshuaj), phenylbutazone, azapropazone, oxyphenbutazone, probenecid, quinolones, salicylates, sulfinpyrazone, clarithromycin n, sulfonamides, tetracyclines, tritocqualin, trophosphamide.

Cov qaug zog ntawm kev ua haujlwm ntawm hypoglycemic thiab qhov nce ntxiv hauv cov ntshav qabzib concentration tuaj yeem pom thaum ua ke nrog ib qho ntawm cov tshuaj hauv qab no: acetazolamide, barbiturates, GCS, diazoxide, diuretics, epinephrine thiab lwm yam tshuaj sympathomimetic, glucagon, laxatives (nrog rau siv ntev), nicotinic acid (hauv kev txhaj tshuaj ntau), estrogens thiab progestogens, phenothiazines, phenytoin, rifampicin, iodine-muaj cov thyroid hormones.

Cov Thaiv Khoom N₂histamine receptors, beta-blockers, clonidine thiab reserpine muaj peev xwm txhim kho ob qho tib si thiab ua kom tsis muaj zog ntawm cov nyhuv hypoglycemic ntawm glimepiride. Hauv qab ntawm cov neeg mob sympatholytic, xws li beta-blockers, clonidine, guanethidine thiab reserpine, cov cim ntawm adrenergic counterregulation nyob rau hauv teb rau hypoglycemia tej zaum yuav raug txo lossis ploj.

Tawm tsam keeb kwm yav dhau los ntawm kev noj glimepiride, ib qho kev nce los yog qaug zog ntawm kev nqis tes ua ntawm coumarin derivatives tuaj yeem pom.

Kev haus cawv ib leeg lossis mob cawv tuaj yeem txhim kho ob qho tib si thiab ua kom tsis muaj zog ntawm cov nyhuv hypoglycemic ntawm glimepiride.

Sequestrants ntawm cov kua tsib kua qaub rau cov chafer khi rau glimepiride thiab txo qhov nqus ntawm glimepiride tsawg kawg 4 teev ua ntej noj cov chafer, tsis muaj kev cuam tshuam pom. Yog li no, glimepiride yuav tsum tau noj tsawg kawg 4 teev ua ntej coj log log.

Tsuas tshuaj thiab tswj hwm

Noj Amaril ®

Sab hauv tsis tas yuav zom, ntxau kom muaj kua txaus (li 0.5 khob). Yog tias tsim nyog, ntsiav tshuaj ntawm Amaril ® tuaj yeem muab faib raws cov kev pheej hmoo ua 2 qhov sib luag.

Raws li txoj cai, koob tshuaj ntawm Amaril ® yog txiav txim los ntawm lub hom phiaj concentration ntawm cov piam thaj hauv cov ntshav. Qhov tshuaj tiv thaiv qis qis txaus kom ua tiav qhov kev tswj hwm metabolic tsim nyog yuav tsum tau siv.

Thaum kho nrog Amaril ®, nws yog ib qho tsim nyog yuav tsum tau txiav txim siab tsis tu ncua cov ntsiab lus ntawm cov piam thaj hauv cov ntshav. Tsis tas li ntawd, kev soj ntsuam tas li ntawm glycosylated hemoglobin qib raug pom zoo.

Qhov tsis zoo ntawm kev siv tshuaj, piv txwv li, hla kev siv tshuaj ntxiv, yuav tsum tsis txhob ntxiv los ntawm kev noj tshuaj ntxiv tom qab ntawm qhov siab dua.

Tus neeg mob cov kev coj ua thaum muaj qhov yuam kev thaum noj cov tshuaj (tshwj xeeb, thaum tsis txhaj koob tshuaj ntxiv lossis noj zaub mov noj) lossis cov xwm txheej tsis tuaj yeem siv tshuaj, yuav tsum tau tham nrog tus neeg mob thiab tus kws kho mob ua ntej.

Pib xaiv koob thiab koob tshuaj

Thawj qhov tshuaj yog 1 mg ntawm glimepiride 1 zaug ib hnub.

Yog tias tsim nyog, cov koob tshuaj txhua hnub tuaj yeem hloov maj mam zuj zus (ntawm ntu li 1-2 lub lis piam). Nws raug nquahu tias qhov kev nce ntxiv yuav raug saib xyuas hauv kev saib xyuas cov ntshav qabzib hauv siab thiab kom raws li cov qib nce ntxiv hauv qab no: 1 mg - 2 mg - 3 mg - 4 mg - 6 mg (−8 mg).

Cov koob tshuaj ntau hauv cov neeg mob uas muaj ntshav qab zib ua tau zoo

Feem ntau, ib koob tshuaj txhua hnub hauv cov neeg mob uas muaj ntshav qab zib kom zoo yog 1-4 mg glimepiride. Kev noj tshuaj txhua hnub ntau dua 6 mg yuav zoo dua hauv qee tus neeg tsawg xwb.

Lub sijhawm ntawm kev noj tshuaj thiab faib tawm ntawm cov tshuaj thoob plaws hauv lub hnub txiav txim siab los ntawm tus kws kho mob, nyob ntawm tus neeg mob txoj kev ua neej nyob rau lub sijhawm (noj mov, lub sijhawm ntawm kev siv lub cev).

Feem ntau, ib koob tshuaj ib zaug ntawm cov tshuaj thaum nruab hnub yog txaus. Nws raug nquahu tias qhov no, tag nrho cov tshuaj ntawm cov tshuaj yuav tsum tau noj tam sim ntawd ua ntej noj tshais tag nrho lossis, yog tias nws tsis noj thaum lub sijhawm ntawd, tam sim ntawd ua ntej thawj pluas noj. Nws yog ib qho tseem ceeb heev kom tsis txhob noj mov tom qab noj cov ntsiav tshuaj.

Txij li kev txhim kho metabolic tswj yog txuam nrog kev nce insulin rhiab heev, qhov xav tau rau glimepiride tuaj yeem txo qis thaum kho. Txhawm rau kom tsis txhob muaj kev txhim kho hypoglycemia, nws yog ib qho tsim nyog yuav tsum txo kom tsis txhob noj lub sijhawm lossis tsis noj tshuaj Amaril ®.

Cov mob uas yuav tau txhaj tshuaj kho qhov mob glimepiride:

- txo lub cev qhov hnyav ntawm tus neeg mob,

- kev hloov pauv ntawm tus neeg mob txoj kev ua neej (pauv kev noj haus, lub sijhawm noj mov, qhov khoom siv lub cev),

- kev tshwm sim ntawm lwm yam uas ua rau muaj kev cuam tshuam ua ntej rau kev txhim kho hypoglycemia lossis hyperglycemia (saib ntu "Cov lus qhia tshwj xeeb").

Glimepiride kho mob feem ntau yog ua rau lub sijhawm ntev.

Hloov chaw ntawm tus neeg mob los ntawm lwm tus neeg sawv cev hypoglycemic rau qhov ncauj tswj hwm rau Amaryl l

Tsis muaj kev sib raug zoo ntawm cov koob tshuaj ntawm Amaril ® thiab lwm yam kev tiv thaiv hypoglycemic rau kev tswj hwm qhov ncauj. Thaum lwm tus neeg sawv cev hypoglycemic rau kev tswj hwm qhov ncauj tau hloov nrog Amaril ®, nws raug pom zoo tias cov txheej txheem rau nws txoj kev tswj hwm yog tib yam li nrog kev pib ua thawj coj ntawm Amaril ®, i.e. kev kho mob yuav tsum pib nrog ib koob tshuaj tsawg kawg ntawm 1 mg (txawm tias tus neeg mob hloov mus rau Amaryl ® nrog qhov siab tshaj plaws ntawm lwm qhov tshuaj hypoglycemic rau kev tswj hwm qhov ncauj). Qhov koob tshuaj nce ntxiv yuav tsum tau nqa tawm hauv theem, suav txog qhov lus teb rau glimepiride raws li cov lus pom zoo saum toj no.

Nws yog ib qho tsim nyog yuav tsum coj mus rau hauv lub zog thiab lub sijhawm ntawm cov nyhuv ntawm yav dhau los hypoglycemic tus neeg sawv cev rau kev tswj hwm qhov ncauj. Kev cuam tshuam kev kho mob tej zaum yuav tsum kom tsis txhob muaj kev sib tham ntawm cov teebmeem uas yuav ua rau muaj kev pheej hmoo ntawm ntshav qab zib.

Siv ua ke nrog metformin

Hauv cov neeg mob uas tsis muaj peev xwm tswj tau tus mob ntshav qab zib mellitus, thaum noj ntau tshaj plaws txhua hnub ntawm ob qho tshuaj glimepiride lossis metformin, kev kho mob nrog kev sib xyaw ntawm ob hom tshuaj no tuaj yeem pib ua. Hauv qhov no, kev kho yav dhau los nrog rau glimepiride lossis metformin txuas ntxiv nyob rau tib theem li qub, thiab cov koob tshuaj ntxiv ntawm metformin lossis glimepiride pib nrog kev txhaj tshuaj qis, uas yog tom qab ntawv suav nyob ntawm lub hom phiaj theem ntawm kev tswj metabolic mus txog qhov siab tshaj plaws txhua hnub. Kev sib koom ua ke yuav tsum tau pib hauv kev saib xyuas mob nkeeg zoo.

Siv ua ke nrog cov tshuaj insulin

Hauv cov neeg mob uas tsis muaj peev xwm tswj tau tus mob ntshav qab zib mellitus, insulin tuaj yeem muab rau tib lub sijhawm thaum noj ntau tshaj plaws txhua hnub ntawm glimepiride. Hauv qhov no, koob tshuaj kawg ntawm glimepiride qhia rau tus neeg mob tseem tsis hloov pauv. Hauv qhov no, kev kho tshuaj insulin pib nrog kev siv tshuaj tsawg, uas maj mam nce ntxiv ntawm kev tswj hwm qhov kev tswj hwm ntawm cov piam thaj hauv cov ntshav. Kev kho mob sib xyaw ua ke yuav tsum muaj kev saib xyuas mob nkeeg.

Siv rau hauv cov neeg mob lub raum tsis ua haujlwm. Tsuas muaj lus qhia tsawg ntawm kev siv cov tshuaj rau cov neeg mob uas lub raum tsis ua haujlwm. Cov neeg mob uas lub raum tsis ua haujlwm yuav nkag siab zoo rau lub ntsej muag hypoglycemic ntawm glimepiride (saib ntu "Pharmacokinetics", "Contraindications").

Siv rau hauv cov neeg mob mob siab tsis ua haujlwm. Muaj qee qhov lus qhia ntawm kev siv tshuaj yeeb rau cov nplooj siab ua tsis ua haujlwm (saib Ntu "Kev Tshawb Xyuas Tsis Txaus").

Siv rau menyuam yaus. Cov ntaub ntawv hais txog kev siv cov tshuaj nyob hauv menyuam yaus tsis txaus.

Noj ntau dhau

Cov tsos mob kev siv tshuaj ntau dhau, nrog rau kev kho mob ntev ntev nrog rau kev noj ntshav ntau dua ntawm glimepiride, tuaj yeem ua rau muaj kev phom sij heev rau lub neej ntshav qab zib.

Kev Kho Mob: sai li sai tau pom ib qho kev noj tshuaj ntau dhau lawm, koj yuav tsum qhia koj tus kws kho mob sai. Kev mob ntshav qab zib yog ib txwm muaj peev xwm nres tau sai sai los ntawm kev noj zaubmov sai (cov piam thaj lossis ib qho piam thaj, kua txiv qab zib lossis tshuaj yej). Hauv qhov no, tus neeg mob yuav tsum tau muaj tsawg kawg 20 g piam thaj (4 daim piam thaj). Cov khoom qab zib yog qhov tsis muaj txiaj ntsig hauv kev kho mob ntawm hypoglycemia.

Txog thaum tus kws kho mob txiav txim siab tias tus neeg mob tsis muaj kev phom sij, tus neeg mob yuav tsum tau ua tib zoo saib xyuas mob. Nws yuav tsum nco ntsoov tias hypoglycemia tuaj yeem rov ua haujlwm tom qab kev pib kho thawj zaug ntawm cov concentration ntawm cov piam thaj hauv cov ntshav.

Yog tias ib tug neeg mob uas mob ntshav qab zib tau txais kev kho mob los ntawm cov kws kho mob sib txawv (piv txwv li, thaum nyob hauv tsev kho mob tom qab muaj xwm txheej, nrog mob thaum hnub so), nws yuav tsum qhia lawv txog nws kev mob nkeeg thiab kev kho mob dhau los.

Qee lub sij hawm yuav tsum tau pw hauv tsev kho mob ntawm tus neeg mob, txawm tias tsuas yog kev ceev faj ua ntej. Cov kev noj tshuaj ntau tshaj thiab muaj kev txhaum loj heev nrog cov kev mob tshwm sim xws li tsis nco qab lossis lwm cov mob loj ntawm cov mob paj hlwb yog qhov mob sai sai thiab xav tau kev kho mob sai sai thiab mus pw hauv tsev kho mob.

Yog tias thaum tus neeg mob tsis nco qab lawm, kev txhaj tshuaj ntxhiv ntawm cov tshuaj dextrose (qabzib) yog tsim nyog (rau cov neeg laus, pib nrog 40 ml ntawm 20% kev daws). Raws li lwm txoj hauv kev rau cov neeg laus, tso cov tshuaj, subcutaneous lossis intramuscular thawj coj ntawm glucagon yog ua tau, piv txwv li, ntawm ib koob ntawm 0.5-1 mg.

Hauv kev kho mob ntawm hypoglycemia vim los ntawm kev tswj hwm kev sib tsoo ntawm Amaril ® los ntawm cov menyuam mos lossis menyuam yaus, cov tshuaj dextrose tau noj yuav tsum tau ua tib zoo kho nyob rau hauv kev muaj peev xwm txaus ntshai hyperglycemia, thiab kev tswj hwm ntawm dextrose yuav tsum tau ua nyob rau hauv tas li saib xyuas cov ntshav qabzib hauv siab.

Yog tias muaj kev noj tshuaj ntau dhau ntawm Amaril ®, lub plab zom mov thiab kev nqus cov pa hluav taws muaj qhov xav tau.

Tom qab kev kho kom sai ntawm kev saib xyuas ntawm cov piam thaj hauv cov ntshav, txoj hlab ntshav ntawm dextrose tov ntawm qhov qis qis yog qhov tsim nyog los tiv thaiv kev rov ua haujlwm ntawm hypoglycemia. Qhov siab ntawm cov piam thaj hauv cov ntshav hauv cov neeg mob ntawd yuav tsum tau saib xyuas tsis tu ncua li 24 teev.

Cov lus qhia tshwj xeeb

Hauv cov chaw muaj kev ntxhov siab tshwj xeeb, xws li kev mob nyhav, kev phais mob, kev kis mob nrog kub taub hau febrile, kev tswj cov teeb meem hauv lub cev yuav ua rau cov neeg mob ntshav qab zib mellitus ploj mus ib ntus, thiab tej zaum lawv yuav tsum tau hloov mus rau kev kho mob insulin ib ntus kom tswj tau cov kev tswj lub cev kom txaus.

Hauv thawj lub lis piam ntawm kev kho mob, qhov kev pheej hmoo ntawm kev muaj ntshav qab zib tsawg zuj zus tuaj, thiab yog li ntawd, tshwj xeeb yog saib xyuas tshwj xeeb ntawm kev saib xyuas cov ntshav qabzib hauv cov ntshav yuav tsum tau nyob rau lub sijhawm no.

Qhov tseem ceeb uas yuav ua rau muaj kev pheej hmoo ntawm lub qog ntshav qab zib muaj xws li:

- kev tsis tuaj yeem lossis tsis muaj peev xwm ntawm tus neeg mob (feem ntau pom tau hauv cov neeg mob laus) kom koom tes nrog tus kws kho mob,

- noj tsis txaus, tsis noj mov los yog yoo mov noj,

- tsis txaus ntawm kev qoj ib ce thiab kev ua kom yuag,

- kev haus dej haus cawv, tshwj xeeb tshaj yog ua ke nrog kev tshem tawm cov zaub mov,

- Lub raum khiav tsis zoo,

- Lub siab ua rau lub siab ua haujlwm zoo (hauv cov neeg mob uas lub siab ua rau lub siab ua haujlwm tsis txaus, hloov mus rau kev kho tshuaj insulin yog qhov tsawg, tsawg kawg kom txog thaum tswj kev zom zaub mov tiav),,

- qee qhov decompensated endocrine cuam tshuam uas ua rau cov pluas noj tsis txaus lossis ua kom tsis qab los ua rau lub cev muaj tshuaj tiv thaiv kab mob ntshav qab zib (piv txwv li, qee qhov kev ua haujlwm ntawm cov thyroid caj pas thiab lub caj qaum ua pa, adrenal tsis txaus),

- tau txais ib co tshuaj (ua ke nrog "sib cuam tshuam"),

- txais tos ntawm glimepiride thaum tsis muaj kev ntsuas rau nws kev txais tos.

Kev kho mob nrog sulfonylurea derivatives, uas suav nrog glimepiride, tuaj yeem ua rau muaj kev loj hlob ntawm hemolytic anemia, yog li ntawd, cov neeg mob uas muaj ntshav qabzib-6-phosphate dehydrogenase yuav tsum tau tshwj xeeb tshaj yog thaum sau ntawv rau glimepiride thiab nws zoo dua yog siv cov tshuaj hypoglycemic uas tsis yog sulfonylurea derivatives.

Nyob rau ntawm qhov muaj cov kev pheej hmoo saum toj no rau kev txhim kho hypoglycemia, koob tshuaj kho glimepiride lossis kev kho tag nrho yuav raug xav tau. Qhov no kuj tseem siv rau qhov tshwm sim ntawm cov kabmob sib kis thaum kho lossis hloov pauv ntawm cov neeg mob lub neej.

Cov tsos mob ntawm tus mob ntshav qab zib tsawg uas ua rau muaj kev tiv thaiv lub cev hauv lub cev hauv kev teb rau hypoglycemia (saib "Cov Kev Mob Rau Sab Nraud") tej zaum yuav mob sib khuav lossis tsis tuaj yeem dhau ntawm kev txhim kho hypoglycemia, hauv cov neeg mob laus, cov neeg mob uas muaj lub hlwb tsis zoo ntawm lub hlwb, lossis cov neeg mob uas tau txais beta adrenoblockers, clonidine, reserpine, guanethidine thiab lwm tus neeg siv sympatholytic.

Kev mob ntshav qab zib tsawg tuaj yeem raug tshem tawm sai sai nrog kev noj sai ntawm kev zom cov zaub mov sai sai (qabzib lossis sucrose).

Ib yam li lwm yam sulfonylurea derivatives, txawm hais tias thawj zaug kev vam meej ntawm kev txo qis ntawm hypoglycemia, hypoglycemia yuav rov pib dua. Yog li, cov neeg mob yuav tsum nyob twj ywm nrog kev saib xyuas tas mus li.

Hauv kev mob ntshav nce siab ntau, yuav tsum tau txais kev kho mob sai thiab kev saib xyuas mob, thiab qee kis, yuav tsum tau pw hauv tsev kho mob.

Thaum kho nrog glimepiride, yuav tsum soj ntsuam daim siab ua haujlwm thiab daim duab txhav ntshav (tshwj xeeb cov leukocytes thiab platelets).

Txij li thaum muaj qee yam kev mob tshwm sim, xws li mob ntshav qab zib ntau ntau, hloov pauv loj heev hauv daim duab ntshav, kev tsis haum tshuaj loj, lub siab tsis ua haujlwm, tuaj yeem ua rau muaj kev phom sij rau lub neej, nyob rau hauv kev txhim kho tsis xav ua lossis tsis haum, tus neeg mob yuav tsum qhia tus kws kho mob tam sim ntawd nyob rau hauv txhua rooj plaub, tsis txhob txuas ntxiv noj cov tshuaj yam tsis tau txais kev pom zoo.

Cuam tshuam rau kev muaj peev xwm tsav tsheb thiab lwm yam txheej txheem. Cov xwm txheej ntawm kev txhim kho hypoglycemia lossis hyperglycemia, tshwj xeeb tshaj yog thaum pib kho lossis tom qab hloov txoj kev kho, lossis thaum cov tshuaj tsis noj tsis tu ncua, txo qis thiab ceev ceev ntawm cov kev xav psychomotor yog tau. Qhov no yuav ua rau tus neeg mob lub peev xwm tsav lub tsheb lossis lwm yam txheej txheem.

Daim ntawv tso tawm

Cov ntsiav tshuaj, 1 mg, 2 mg, 3 mg, 4 mg.

Rau qhov ntau npaum ntawm 1 mg

30 ntsiav tshuaj nyob rau hauv cov hlwv ntawm PVC / aluminium ntawv ci. 1, 2, 3 lossis 4 bl. muab tso rau hauv lub thawv ntawv thawv.

Rau cov tshuaj ntawm 2 mg, 3 mg, 4 mg

15 tab. nyob rau hauv cov hlwv ntawm PVC / aluminium ntawv ci. Rau 2, 4, 6 lossis 8 bl. muab tso rau hauv lub thawv ntawv thawv.

Chaw tsim tshuaj paus

Sanofi S.p.A., Ltalis. Stabilimento di Scoppito, Strada Statale 17, km 22, I-67019 Scoppito (L'Aquilla), Ltalis.

Cov koomhaum muaj txoj cai lij choj nyob rau hauv lawv lub npe sau npe rau daim ntawv pov thawj yog muab. Sanofi-Aventis Deutschland GmbH, Lub Teb Chaws Yelemees

Kev thov cov neeg tau txais kev pabcuam yuav tsum xa mus rau qhov chaw nyob hauv Lavxias. 125009, Moscow, st. Tverskaya, 22.

Xov Tooj: (495) 721-14-00, fev: (495) 721-14-11.

Dosage daim ntawv

Ib qho 4 mg ntsiav tshuaj muaj

cov tshuaj nquag - glimepiride 4 mg

zam txim: lactose monohydrate, sodium hmoov txhuv nplej siab glycolate (hom A), povidone 25000, microcrystalline cellulose, magnesium stearate, indigo carmine txhuas cov kua roj vanish (E 132).

Cov ntsiav tshuaj, oblong nyob rau hauv cov duab, nrog ib tug ca saum npoo ntawm ob sab, lub teeb xiav nyob rau hauv cov xim nrog lub kab txhaum ntawm ob sab thiab NMO npav / tuam txhab logo lossis tuam txhab logo / NMO.

Amaril ntsiav tshuaj 4 mg muaj peev xwm muab faib ua cov koob tshuaj sib npaug.

Cov chaw muag tshuaj

Cov Tshuaj Pharmacokinetics

Glimepiride yog tus cwj pwm los ntawm kev ua tiav bioavailability tom qab kev tswj hwm qhov ncauj. Noj mov tsis muaj qhov cuam tshuam tseem ceeb ntawm kev nqus ntawm cov tshuaj, nrog nws tus kheej tsuas yog txo qis ntawm qhov nqus ntawm qhov nqus. Qhov siab kawg ntawm cov ntshav ntau (Cmax) tau tiav kwv yees li 2.5 teev tom qab kev tswj hwm ntawm qhov ncauj (nruab nrab 0.3 μg / ml nrog ntau qhov koob tshuaj 4 mg ib hnub twg), qhia txog txoj kev sib raug zoo ntawm koob tshuaj thiab Cmax thiab AUC nqi ( thaj chaw hauv qab qhov concentration piv rau lub sijhawm nkhaus).

Glimepiride muaj tsawg kawg ntawm cov khoom faib (kwv yees li 8,8 litres), kwv yees sib xws rau qhov chaw ntawm faib albumin, qhov siab ntawm cov protein khi (> 99%) thiab tsis tshua pom tseeb (kwv yees li 48 ml / min.). Hauv cov kev tshawb fawb preclinical, glimepiride ua tawm hauv cov kua mis. Glimepiride tuaj yeem hla dhau ntawm qhov tso ntshav. Cov neeg kawm tiav ntawm kev nkag los ntawm cov ntshav-lub hlwb lub cev yog tsawg.

Biotransformation thiab excretion

Qhov nruab nrab qhov tseem ceeb ib nrab-lub neej ntawm qhov tseem ceeb rau ntshav dej ntau ntau hauv qab kev siv ntau yog kwv yees li 5-8 teev. Tom qab noj cov tshuaj hauv qhov siab kawg, ntev me ntsis ib nrab-lub neej tau sau tseg. Tom qab ib koob tshuaj hluav taws xob isotope-daim ntawv lo glimepiride, 58% ntawm xov tooj cua tau kuaj pom hauv cov zis thiab 35% hauv cov quav. Cov tshuaj tsis raug hloov nyob rau hauv cov zis tsis tau kuaj pom. Ob lub cev siv tau muaj qhia nyob rau hauv cov zis thiab cov quav, feem ntau yuav yog cov khoom lag luam ntawm hepatic metabolism (qhov tseem ceeb enzyme CYP2C9): hydroxy derivative thiab carboxy derivative. Tom qab qhov ncauj tswj hwm ntawm glimepiride, lub davhlau ya nyob twg tshem tawm ib nrab-lub neej ntawm cov metabolites tau 3-6 thiab 5-6 teev, feem.

Kev sib piv ntawm cov txiaj ntsig tau nrog rau ib qho thiab tau txais kev tso cai ntau dua hauv cov kev cai ib zaug tsis qhia tawm qhov sib txawv tseem ceeb hauv cov chaw muag tshuaj tsis sib haum, muaj cov cim ntawm qhov tsis tshua pom kev txawv txav ntawm qhov tseem ceeb. Tsis pom zoo ua ke ntawm glimepiride.

Cov khoom lag luam pharmacokinetic zoo sib xws hauv cov txiv neej thiab poj niam, zoo li hauv cov hluas thiab cov laus (laus dua 65 xyoos) cov neeg mob. Hauv cov neeg mob uas tsis muaj qhov tsis txaus creatinine, muaj qhov nyiam ua rau glimepiride tshem tawm thiab tsawg dua qhov nruab nrab ntawm cov ntshav, feem ntau yuav yog vim muaj qhov zam sai dua vim muaj qis ntawm cov protein ntau. Tsis tas li ntawd, ib qho kev txo qis hauv lub raum ua haujlwm ntawm ob qhov tseem ceeb tshuaj tiv thaiv kab mob. Feem ntau, ib qho kev pheej hmoo ntxiv ntawm kev sib txuam tshuaj nyob hauv cov neeg mob no tsis xav pom.

Cov chaw muab tshuaj rau hauv tsib cov neeg mob ntshav qab zib tom qab kev phais mob ntawm cov kua tsib lub plab tau zoo li cov uas tau pom hauv cov neeg noj qab nyob zoo.

Ib txoj kev tshawb nrhiav tshuaj pharmacokinetics, kev nyab xeeb, thiab kev mob siab rau ntawm glimepiride noj ib zaug ntawm 1 koob tshuaj rau 30 cov neeg mob (4 cov menyuam hnub nyoog 10-12 xyoo thiab 26 cov menyuam hnub nyoog 12-17 xyoo) uas muaj ntshav qab zib hom 2 qhia pom nruab nrab AUC qhov tseem ceeb (0 -last.), Cmax thiab t1 / 2, zoo ib yam li cov uas tau pom yav tas los rau hauv cov neeg laus.

Cov Tshuaj Hauv Tshuaj

Glimepiride yog lub qhov ncauj hypoglycemic nquag nyob rau hauv sulfonylurea derivatives pab pawg. Nws tuaj yeem siv rau cov ntshav qab zib uas tsis-insulin-mellitus.

Qhov kev nqis tes ntawm glimepiride yog feem ntau hauv kev ua kom muaj kev zais ntawm cov kua dej los ntawm cov qe hlwb ntawm cov txiav.

Ib yam li nrog lwm cov sulfonylurea derivatives, cov nyhuv no yog nce raws li qhov nce ntawm cov lus teb ntawm pancreatic beta hlwb ua rau kev voos nrog physiological glucose qib. Tsis tas li ntawd, glimepiride, pom meej, muaj cov lus tshaj tawm ntawm cov nyhuv ntxiv, tseem muaj cov yam ntxwv ntawm lwm cov sulfonylurea derivatives.

Sulfonylurea derivatives tswj kev tsim tshuaj insulin zais los ntawm kev kaw ATP-rhiab poov tshuaj raws ntawm beta-cell daim nyias nyias. Kaw cov poov tshuaj channel ua rau depolarization ntawm beta hlwb thiab los ntawm kev qhib cov calcium calcium uas ua rau kev nce calcium ntau ntxiv rau hauv cov hlwb. Qhov no ua rau kev tso tawm cov tshuaj insulin los ntawm exocytosis.

Glimepiride nrog rau qhov hloov pauv siab tau muab khi rau cov protein ntawm cov cell cell ntawm beta hlwb, uas cuam tshuam nrog ATP-nkag siab poov tshuaj raws, tab sis txawv ntawm qhov chaw khi ntawm sulfonylurea li niaj zaus.

Extrapancreatic cov teebmeem muaj xws li, txhim kho qhov rhiab heev ntawm cov ntaub so ntswg mus rau insulin thiab txo qis ntawm cov ntshav insulin los ntawm daim siab.

Qhov nqus ntawm cov piam thaj los ntawm cov ntshav los ntawm cov leeg thiab cov nqaij rog ua rau muaj qhov tshwm sim vim muaj cov protein tshwj xeeb thauj nyob hauv cov cell. Cov kua nplaum nyob hauv cov ntaub so ntswg no yog cov kauj ruam qhia txog kev siv cov kua nplaum ntau los ntawm cov ntaub so ntswg. Glimepiride nrawm heev ntxiv cov naj npawb ntawm cov piam thaj transporter molecules hauv cov cell ua rau ntawm cov leeg nqaij thiab cov roj ntsha, uas ua rau lub ntsej muag ua kom qabzib.

Glimepiride ua rau cov kev ua si tshwj xeeb glycosyl phosphatidylinositol phospholipase C, uas tuaj yeem cuam tshuam nrog cov tshuaj lipogenesis thiab glycogenesis hauv cov rog thiab cov leeg nqaij. Glimepiride inhibits glucose ntau lawm hauv lub siab los ntawm kev ua rau muaj ntau yam ntawm intuctose-2,6-bisphosphate, uas, nyeg, inhibits gluconeogenesis.

Hauv cov tib neeg muaj kev noj qab haus huv, qhov tshuaj kho qhov ncauj tsawg kawg nkaus yog kwv yees li 0.6 mg. Glimepiride yog tus cwj pwm los ntawm qhov tsis siv tshuaj ntau ntxiv thiab ua qhov txuas ntxiv. Lub cev muaj zog teb rau kev tawm dag zog lub cev, qhov txo qis hauv insulin secretion, tseem nyob nrog kev siv glimepiride.

Qhov sib txawv sib txawv ntawm qhov xwm ntawm kev nqis tes thaum noj cov tshuaj 30 feeb thiab tam sim ntawd ua ntej noj mov tsis tau pom. Hauv cov neeg mob uas mob ntshav qab zib mellitus, kev tswj hwm metabolic txaus hauv 24 teev yuav ua tiav nrog kev siv cov tshuaj ib hnub ib zaug.

Lub hydroxymetabolite ntawm glimepiride, txawm hais tias nws ua rau me me tab sis tseem ceeb txo cov ntshav qabzib hauv cov neeg noj qab nyob zoo, yog lub luag haujlwm tsuas yog ib feem me me ntawm cov nyhuv tag nrho ntawm cov tshuaj.

Kev Kho Mob Los Sib Ntxiv nrog Metformin

Hauv ib txoj kev tshawb nrhiav, cov neeg mob uas tsis txaus tswj ntawm metformin ntawm cov koob tshuaj ntau tshaj plaws nrog kev siv cov tshuaj glimepiride qhia tau hais tias muaj kev txhim kho hauv kev tswj metabolic piv nrog metformin monotherapy.

Kev sib xyaw ua ke nrog cov tshuaj insulin

Lub sijhawm no, muaj cov ntaub ntawv tsis tshua muaj neeg ntawm kev kho mob sib xyaw ua ke nrog kev siv tshuaj insulin. Cov neeg mob uas tsis tuaj yeem tswj hwm tus kabmob tsis txaus ntawm qhov ntau tshaj plaws ntawm glimepiride tuaj yeem yog tus kws kho mob ua cov tshuaj insulin. Hauv ob txoj kev tshawb nrhiav, kev sib txuas ua ke tau nrog kev txhim kho hauv kev tswj lub cev zoo ib yam li kev pom nrog insulin monotherapy, tab sis kev sib xyaw ua ke yuav tsum siv cov tshuaj insulin qis dua.

Kev tshawb nrhiav 24-lub lim tiam tau ua nrog kev tswj hwm (glimepiride hauv koob tshuaj ntau txog 8 mg rau ib hnub lossis metformin hauv koob tshuaj ntau txog 2,000 mg ib hnub) hauv 285 cov menyuam (hnub nyoog 8-17 xyoo) uas muaj ntshav qab zib hom 2.

Txais tos ntawm glimepiride thiab metformin tau nrog ua kom poob qis hauv HbA1c piv nrog qib pib (glimepiride - 0.95 (СО 0.41), metformin -1.39 (СО 0.40)). Txawm li cas los xij, tus nqi nruab nrab ntawm kev hloov pauv hauv HbA1c piv rau qib pib hauv pawg glimepiride tsis tau ua tiav cov qauv kev ua tau zoo uas tsis qis dua rau metformin. Qhov sib txawv ntawm cov pawg kho mob yog 0.44% txaus siab ntawm metformin. Kev txwv siab dua (1.05) ntawm 95% kev ntseeg siab ntawm lub sijhawm sib txawv ntawm qhov sib txawv yog qhov siab dua 0.3% ntawm qhov txwv tsis muaj tsawg dua kev ua haujlwm.

Tawm tsam keeb kwm ntawm kev kho cov tshuaj glimepiride hauv cov menyuam yaus, tsis muaj lub cim ntawm cov kev phiv tshuaj tshiab piv nrog cov pom nyob hauv cov neeg laus cov neeg mob ntshav qab zib hom 2 ntshav qab zib. Cov ntaub ntawv hais txog kev ua tau zoo thiab kev nyab xeeb ntawm kev siv lub sijhawm ntev hauv cov tshuaj hauv cov menyuam yaus mob yog tsis muaj.