Synthetic antidiabetic tus neeg sawv cev > Kev khomob thiab kev tiv thaiv

Synthetic antidiabetic tus neeg sawv cev (hluavtaws hypoglycemic cov neeg sawv cev, qhov ncauj hypoglycemic cov neeg sawv cev) - cov tshuaj uas txo cov ntshav piam thaj thiab siv los kho ntshav qab zib. Txhua yam tshuaj tua kab mob muaj nyob rau hauv cov foos.

Lub pathogenesis ntawm ntshav qab zib mellitus yog ua raws li cov insulin tsis txaus, uas tej zaum yuav yog vim muaj cov insulin tsis txaus los ntawm β-hlwb ntawm cov islets ntawm Langerhans (insulin-dependent ntshav qab zib mellitus lossis hom I mob ntshav qab zib mellitus), lossis cov tshuaj insulin tsis txaus (tsis muaj ntshav qab zib-tiv thaiv ntshav qab zib mellitus lossis hom II mob ntshav qab zib mellitus). Raws li qhov no, cov tshuaj hypoglycemic tau muab faib ua cov tshuaj uas yuav tsim cov insulin ntau ntxiv los ntawm β-hlwb ntawm cov islets ntawm Langerhans, thiab cov tshuaj uas ua rau muaj kev cuam tshuam cov ntaub so ntswg mus rau insulin.

Amino Acid Derivatives

Mechanism ntawm kev ua: txhawb cov insulin zais zis los ntawm β-hlwb ntawm islets ntawm Langerhans. Nquag, nrog nce ntxiv nyob rau thaj chaw piam thaj, piam thaj mus rau β-hlwb ntawm cov islets ntawm Langerhans yog tsa. Los ntawm kev qhia txoj kev tsis haum txaus siv qhov tshwj xeeb thauj khoom (GLUT-2), cov piam thaj nkag mus rau hauv β-hlwb thiab phosphorylates, uas ua rau muaj kev nce ntxiv hauv kev tsim cov txheej txheem ATP lwg me, uas txwv ATP-dependant K + channels (K_ATPraws). Nrog thaiv K_ATP-chaw raws, K + tawm ntawm lub cell yog cuam tshuam, thiab depolarization ntawm cell cell tsim. Nrog depolarization ntawm cell cell, muaj peev xwm tso Ca 2+ raws qhib, thiab qib Ca 2+ hauv cytoplasm ntawm β-hlwb nce. Ca 2+ ions ua kom muaj kev sib cog lus microfilaments thiab txhawb kev txav ntawm cov granules nrog insulin rau lub cell cell, kev koom ua ke ntawm granules hauv daim nyias nyias, thiab insulin exocytosis.

Sulfonylurea derivatives ua raws li cov kev txais ntawm hom 1 (SUR1) K_ATP-yog raws thiab thaiv cov kev raws. Hauv qhov no, depolarization ntawm lub cell membrane tshwm sim, voltage-depend Ca 2+ raws kev ua haujlwm, thiab Ca 2+ nkag rau hauv β cov hlwb nce. Nrog kev nce qib ntawm Ca 2+ hauv cells-hlwb, kev txav ntawm cov granules nrog insulin mus rau lub plasma membrane, kev suav nrog cov granules hauv daim nyias nyias thiab cov tshuaj insulin exocytosis yog ua kom rov ua haujlwm.

Nws tseem ntseeg tias sulfonylurea derivatives ua rau nce rhiab ntawm cov ntaub so ntswg mus rau insulin thiab txo cov piam thaj ntau hauv cov nplooj siab.

Kev ua haujlwm hypoglycemic ntawm sulfonylurea derivatives tsis yog nyob ntawm qib ntawm cov piam thaj hauv cov ntshav (txiav tawm qhov kev sib txuas ntawm cov piam thaj thiab insulin secretion). Yog li no, thaum siv sulfonylurea derivatives, hypoglycemia yog ua tau.

Sulfonylurea derivatives yog siv rau hom II mob ntshav qab zib mellitus (kev tsim tawm hauv insulin tsis txaus, txo qis cov ntaub so ntswg rhiab rau insulin). Hauv hom I mob ntshav qab zib mellitus txuam nrog kev rhuav tshem β-hlwb, cov tshuaj no tsis ua hauj lwm zoo.

Cov tsim tawm ntawm sulfonylureas ntawm thawj tiam - chlorpropamide, tolbutamide (butamide) raug kho nyob rau hauv cov koob tshuaj loj, ua rau luv luv.

Cov tsim tawm ntawm sulfonylureas ntawm lub cim thib ob - glibenclamide, glycidone, glycoslide, glimepiride, glipizide - tau raug tshaj tawm nyob rau hauv ntau dua cov koob tshuaj, lawv siv sijhawm ntev, lawv cov kev mob tshwm sim tsawg dua li hais tawm. Txawm li cas los xij, vim tias siv lub sijhawm ntev (12-24 teev), cov tshuaj no muaj qhov txaus ntshai ntau dua li qhov ua tau ntawm kev ua kom tsis muaj ntshav qab zib. Tam sim no, tsuas yog sulfonylurea npaj ntawm lub cim thib ob tau siv. Sulfonylurea derivatives tau muab tshuaj noj 30 feeb ua ntej noj mov.

Phiv los ntawm sulfonylurea derivatives:

Kev ntshav siab
Xeev siab ntuag, nws yog xim hlau saj ntawm lub qhov ncauj, hnov mob hauv plab
Qhov hnyav nce
Hypersensitivity rau kev haus cawv
Kev Hyponatremia
Kev fab tshuaj, photodermatosis
Lub siab ua haujlwm tsis zoo
Leukopenia

Amino Acid Derivatives

Nateglinide yog ib qho phenylalanine derivative. Nws muaj lub zog ceev thim rov qab inhibitory nyhuv ntawm K_ATP-chaw ntawm β-hlwb ntawm cov islet apparatus. Rov qab tso cov tshuaj insulin thaum ntxov ua rau kev txhim kho los ntawm cov piam thaj (tsis mob ntshav qab zib hom II). Nws ua rau muaj cim zais cia ntawm insulin hauv thawj 15 feeb ntawm kev noj mov. Hauv 3-4 teev tom ntej, cov theem ntawm cov tshuaj insulin rov mus rau qhov qub. Nateglinide stimulates insulin secretion nyob ntawm seb cov piam thaj. Hauv cov ntshav qabzib tsawg, nateglinide muaj cov nyhuv me ntsis ntawm kev nqus insulin. Kev zais ntshis ntawm insulin tshwm sim los ntawm nateglinide txo nrog qhov txo qis hauv qabzib, yog li hypoglycemia tsis tshwm sim nrog kev siv cov tshuaj no.

2. Lub tswv yim ntawm cov txheej txheem ntawm cov tshuaj tiv thaiv kev ua ntawm t-activin, interferon, BCG, levamisole

Raws li cov tshuaj tiv thaiv kabmob, cov tshuaj biogenic (npaj ntawm thymus, interferons, interleukin-2, BCG) thiab cov khoom siv hluavtaws (piv txwv, levamisole) yog siv. Hauv kev kho mob, ntau tus thymus npaj tau siv uas muaj cov tshuaj tiv thaiv kabmob (thymalin, tactivin, thiab lwm yam). Lawv cuam tshuam nrog polypeptides lossis cov protein. Tactivin (T-activin) normalizes tus lej thiab kev ua haujlwm ntawm T-lymphocytes (hauv cov tshuaj tiv thaiv kab mob hauv lub xeev), txhawb kev tsim cov cytokines, rov tsim cov tshuaj tua kom muaj zog ntawm T-killers thiab feem ntau ua rau lub nro ntawm lub cev tiv thaiv kab mob. Nws yog siv hauv cov tshuaj tiv thaiv kab mob (tom qab kho hluav taws xob thiab kev kho tshuaj hauv cov neeg mob qog nqaij hlav, nrog rau kev ua kom huv thiab mob tshwm sim, thiab lwm yam), lymphogranulomatosis, lymphocytic leukemia, ntau yam sclerosis. Cov tshuaj interferons nyob rau hauv pab pawg cytokines muaj cov tshuaj tiv thaiv kab mob, tiv thaiv kabmob thiab tiv thaiv kabmob. A, b thiab y-interferons raug rho tawm. Tshaj tawm cov kev cai tshaj tawm rau kev tiv thaiv kab mob yog interferon-y. Qhov ua rau cov tshuaj tiv thaiv kab mob cuam tshuam los ntawm kev cuam tshuam yog pom hauv kev ua kom cov macrophages, T-lymphocytes thiab lub hlwb tua neeg. Ua cov kev npaj ntawm ntuj interferon tau los ntawm tib neeg cov ntshav pub (interferon, interlock), thiab ntxiv tawm cov tshuaj interferons (reaferon, intron A, betaferon). Lawv siv rau hauv kev kho mob ntawm ntau tus kabmob kis (piv txwv li, mob ua npaws, mob siab), nrog rau qee cov kab mob qog (nrog myeloma, lymphoma los ntawm B hlwb). Tsis tas li ntawd, thiaj li hu ua interferonogens (piv txwv li ib nrab-seev cev, prodigiosan), uas nce ntau lawm ntawm cov tshuaj tiv thaiv endogenous interferons, qee zaum siv los ua tshuaj tiv thaiv kabmob (immunostimulants). Qee cov tshuaj tiv thaiv interleukins, piv txwv li, tso tawm tshuaj interleukin-2, kuj tau raug sau ua tshuaj tiv thaiv kabmob (immunostimulants). BCG yog siv rau kev txhaj tshuaj tiv thaiv kab mob ntsws. Tam sim no, BCG qee zaum siv nyob rau hauv txoj kev kho mob ntawm ntau tus hlav qog ua hlav. BCG stimulates macrophages thiab, qhov tseeb, T-lymphocytes. Qee qhov muaj txiaj ntsig zoo tau sau tseg nyob rau hauv mob myeloid leukemia, qee hom qog ntshav (tsis hais txog Hodgkin's lymphoma), mob cancer ntawm txoj hnyuv thiab mis, thiab mob cancer ntawm lub zais zis. Ib qho ntawm cov tshuaj hluavtaws yog levamisole (decaris). Nws yog siv nyob rau hauv daim ntawv ntawm hydrochloride. Nws muaj cov haujlwm ua anthelmintic tshaj tawm, nrog rau tshuaj tiv thaiv immunostimulating. Tus txheej txheem ntawm tus tom kawg tsis meej txaus. Muaj pov thawj tias levamisole muaj cov nyhuv hom mob zoo rau macrophages thiab T-lymphocytes. Nws tsis hloov pauv ntawm cov tshuaj tiv thaiv. Yog li ntawd, cov nyhuv tseem ceeb ntawm levamisole yog pom nyob rau hauv qhov ua haujlwm ntawm kev tiv thaiv cellular. Nws yog siv rau kev txhaj tshuaj tiv thaiv kab mob, qee yam mob mus ntev, mob caj dab, thiab cov hlav hlav. IRS-19, ribomunil, interferon gamma, aldesleukin, thymogen, tiloron npaj ntawm echinacea, azathioprine, methotrexate, cyclosporin, basiliximab.

Cov Neeg Tsim Khoom

Lub chaw tsim tshuaj rau cov yeeb tshuaj Beat yog lub tuam txhab tshuaj Eli Lilly thiab tuam txhab tshuaj, tsim tsa thaum xyoo 1876 hauv Indianapolis (Tebchaws Asmeskas, Indiana).

Nov yog thawj lub tuam txhab kev lag luam pib ua haujlwm cov tshuaj insulin hauv xyoo 1923.

Lub tuam txhab txhim kho thiab tsim cov tshuaj rau cov neeg uas tau muag zoo hauv ntau tshaj ib puas lub teb chaws, thiab hauv 13 lub xeev muaj cov chaw ua haujlwm rau lawv cov khoom lag luam.

Qhov kev coj thib ob ntawm lub tuam txhab yog kev tsim cov tshuaj rau cov kev xav tau ntawm cov tshuaj veterinary.

Lilly thiab Tuam Txhab tau nyob hauv Moscow ntau tshaj nees nkaum xyoo. Lub hauv paus ntawm nws txoj kev lag luam hauv Lavxias yog cov tshuaj kho mob rau kev kho mob ntshav qab zib, tab sis muaj lwm yam tshwj xeeb: kev mob hlwb, kev puas hlwb, oncology.

Tus neeg sawv cev nquag ntawm cov tshuaj yog 250 micrograms ntawm exenatide.

Ntxiv yog sodium acetate trihydrate, glacial acetic acid, mannitol, metacresol thiab dej rau kev txhaj tshuaj.

Baeta yog muaj nyob rau hauv daim ntawv ntawm cov phwj yeeb yaj kiab uas siv cov kua tshuaj uas muaj cov tshuaj tsis haum rau kev txhaj tshuaj hauv qab daim tawv nqaij 60 feeb ua ntej noj thaum sawv ntxov thiab yav tsaus ntuj.

Baeta raug pom zoo nyob rau hauv kev kho mob ntawm qhov tsis yog-insulin-mob ntshav qab zib mellitus (hom II) txhawm rau txhawm rau txhawm rau tswj glycemic:

nyob rau hauv daim ntawv ntawm monotherapy - tawm tsam keeb kwm ntawm ib tug nruj tsawg carb noj cov zaub mov thiab ua haujlwm lub cev,
ua ke nrog kev kho:
- ua ib qho ntxiv rau txo cov tshuaj qab zib (metformin, thiazolidinedione, sulfonylurea derivatives),
- rau kev siv nrog metformin thiab basal insulin.

Hauv qhov no, sulfonylurea derivatives yuav tsum tau txo tshuaj ntau npaum li cas. Thaum siv Byeta, koj tuaj yeem tam sim ntawd txo qis ib txwm li 20% thiab kho nws hauv qab tswj kav glycemia.

Rau lwm yam tshuaj, kev pib hloov pauv tsis tuaj yeem hloov pauv.

Kev tshaj tawm, ntxiv cov tshuaj rau hauv chav kawm tau pom zoo kom muab coj los ua ke nrog lwm cov kab mob hypoglycemic los txhim kho lawv qhov kev txiav txim siab thiab ncua sij hawm teem tshuaj insulin.

Kev siv exenatide tsis yog qhia rau:

Ib tug neeg ntxim rau cov tshuaj uas muaj cov tshuaj,
mob ntshav qab zib insulin-hom mob ntshav qab zib hom (hom I),
decompensated lub raum lossis lub siab ua haujlwm,
cov kab mob ntawm lub plab zom mov, nrog cov paresis (txo qis kev cog lus) ntawm lub plab,
cev xeeb tub thiab pub niam mis,
mob hnyav ua ntej lossis mob hlwb ua ntej.

Tsis txhob muab tshuaj rau cov menyuam yaus kom txog thaum lawv loj tiav.

Ceev faj yuav tsum tau siv nrog kev siv ua ke nrog kev siv exenatide thiab qhov ncauj npaj uas yuav tsum tau nqus sai los ntawm cov hnyuv: lawv yuav tsum noj tsis pub dhau ib teev ua ntej Bayet kev txhaj tshuaj lossis hauv cov zaub mov uas tsis cuam tshuam nrog nws cov thawj coj.

Qhov ntau zaus ntawm cov xwm txheej tsis zoo thaum siv Byet yog los ntawm 10 txog 40%, lawv tsuas yog hais qhia txog kev hloov pauv qhov ntuav thiab ntuav thaum pib kho. Qee zaum cov tshuaj tiv thaiv hauv zos tuaj yeem tshwm sim ntawm qhov chaw txhaj tshuaj.

Analogues ntawm cov tshuaj

Ntshav qab zib yog ntshai ntawm cov tshuaj no, zoo li hluav taws!

Koj tsuas yog xav tau thov ...

Cov lus nug ntawm hloov Bayet nrog lwm txoj kev kho, raws li txoj cai, tuaj yeem tshwm sim hauv qab no:

cov tshuaj tsis txo cov ntshav qabzib,
kev mob tshwm sim yog hnov mob heev,
Tus nqi yog siab dhau.

Cov tshuaj Baeta generics - cov tshuaj uas muaj pov thawj kho thiab lom sib npaug - tsis haum.

Nws tag nrho cov analogues nyob rau hauv daim ntawv tso cai los ntawm Lilly thiab Tuam Txhab yog tsim los ntawm Bristol-Myers Squibb Co (BMS) thiab AstraZeneca.

Qee lub teb chaws kev lag luam Byetu nyob rau hauv Bydureon cov tshuaj lag luam.

Baeta Long yog ib tus neeg sawv cev hypoglycemic nrog tib tus neeg sawv cev nquag (exenatide), tsuas yog ua ntev ntev. Tus tsis yeem pev txwv ntawm Baeta. Txoj kev siv - ib qho txhaj tshuaj subcutaneous txhua 7 hnub.

Cov pab pawg ntawm cov tshuaj ntau zuj zus ntxiv kuj muaj xws li Victoza (Denmark) - cov tshuaj txo suab thaj, cov tshuaj yeeb dej caw yog tshuaj muaj liraglutide. Los ntawm kev kho cov yam ntxwv, ntsuas thiab contraindications, nws zoo ib yam li Baete.

Incretin agonists muaj tsuas yog ib daim ntawv tshuaj rau tshuaj - txhaj tshuaj.

Qhov pab pawg thib ob ntawm cov chav kawm ntawm cov tshuaj incretin yog sawv cev los ntawm cov tshuaj uas txwv qhov tsim tawm ntawm enzyme dipeptidyl peptidase (DPP-4). Lawv muaj ntau yam qauv tsim tsa thiab muaj cov qauv pharmacological.

DPP-4 cov tshuaj tiv thaiv kab mob suav nrog Januvia (Netherlands), Galvus (Switzerland), Transgenta (Lub Tebchaws Yelemees), Ongliza (USA).

Zoo li Baeta thiab Victoza, lawv nce insulin ntau ntau los ntawm kev ua kom ntev dua ntawm cov tshuaj incretins, inhibit glucagon ntau lawm thiab txhawb kev tsim kho pancreatic cell.

Tsuas yog tsis cuam tshuam rau tus nqi ntawm tso tawm ntawm lub plab thiab tsis pab txhawb rau qhov poob phaus.

Kev qhia txog kev siv cov tshuaj pab pawg no tseem yog cov ntshav qab zib tsis yog insulin-tiv thaiv mob ntshav qab zib mellitus (hom II) hauv kev kho mob monotherapy lossis hauv kev sib xyaw nrog lwm cov tshuaj txo cov ntshav qab zib.

Noj tshuaj rau qhov tsis yog ua rau poob ntshav qab zib, vim tias thaum nws qhov ntsuas lub cev tau dhau mus, qhov kev tsuj ntawm glucagon nres.

Ib qho ntawm qhov zoo yog lawv daim ntawv tshuaj rau hauv cov qauv ntawm cov ntsiav tshuaj rau qhov ncauj kev tswj hwm, uas tso cai rau koj nkag mus rau cov tshuaj rau hauv lub cev tsis muaj qhov xa mus rau kev txhaj tshuaj.

Dosage daim ntawv

Kev daws rau subcutaneous thawj coj.

1 ml ntawm cov tshuaj muaj:

cov tshuaj nquag: exenatide 250 mcg,

tus zam: sodium acetate trihydrate 1.59 mg, acetic acid 1.10 mg, mannitol 43.0 mg, metacresol 2.20 mg, dej rau kev txhaj tshuaj q.s. txog li 1 ml.

Cov xim tsis muaj pob tshab.

Cov chaw muag tshuaj

Exenatide (Exendin-4) yog glucagon zoo li polypeptide receptor agonist thiab yog 39-amino acid amidopeptide. Cov ntau zuj zus, xws li glucagon-zoo li peptide-1 (GLP-1), txhim kho cov kua dej tsis txaus rau cov kua dej, txhim kho beta ntawm tes ua haujlwm, txwv tsis pub muaj ntshav qabzib ntau thiab ua rau lub plab zom mov tom qab lawv nkag mus rau hauv cov ntshav tawm ntawm txoj hnyuv. Exenatide yog lub zog loj zuj zus uas ua rau cov ntshav qabzib-insulin muaj peev xwm ua rau muaj cov ntshav qabzib ntau yam thiab muaj lwm yam teebmeem ntshav qabzib ntau ntxiv rau cov neeg mob ntshav qab zib hom 2.

Cov amino acid sib lawv liag ntawm exenatide ib feem sib raug rau ntu ntawm tib neeg GLP-1, los ntawm qhov uas nws khi thiab ua rau GLP-1 cov neeg txais kev pabcuam hauv tib neeg, uas ua rau muaj kev sib txuas ntxiv rau cov ntshav qabzib thiab kev tso ntshav ntawm insulin los ntawm pancreatic beta hlwb nrog kev koom tes ntawm cyclic AMP thiab / lossis lwm yam kev cuam tshuam ntawm lub cev. txoj kev. Exenatide txhawb kev tso tawm ntawm insulin los ntawm beta hlwb nyob ib puag ncig muaj kev nce siab ntxiv ntawm cov piam thaj. Exenatide sib txawv hauv cov qauv tshuaj thiab cov tshuaj pharmacological los ntawm insulin, sulfonylurea derivatives, D-phenylalanine derivatives thiab meglitinides, biguanides, thiazolidinediones thiab alpha-glucosidase inhibitors.

Exenatide txhim kho glycemic tswj nyob rau hauv cov neeg mob uas muaj ntshav qab zib hom 2 vim yog cov haujlwm hauv qab no.

Cov qabzib-insulin secretion: hauv hyperglycemic tej yam kev mob, exenatide ua rau cov piam thaj tsis muaj peev xwm tso cov kua dej ntawm cov kua dej los ntawm pancreatic beta hlwb. Qhov insulin secretion tso tseg thaum cov concentration ntawm cov piam thaj hauv cov ntshav txo qis thiab nws nce mus rau qhov qub, yog li txo cov kev pheej hmoo ntawm cov ntshav qog ntshav qab zib.

Thawj theem ntawm cov tshuaj insulin: Kev siv tshuaj insulin thaum thawj 10 feeb, hu ua "thawj theem ntawm cov tshuaj insulin", tsis tuaj rau cov neeg mob ntshav qab zib hom 2. Tsis tas li ntawd xwb, qhov poob ntawm thawj theem ntawm cov tshuaj insulin yog ib qho kev ua haujlwm thaum ntxov ntawm beta cell ua haujlwm hauv hom 2 ntshav qab zib. Kev tswj hwm ntawm exenatide rov qab los yog hloov kho tau zoo ntau theem ntawm thawj thiab theem ob ntawm cov tshuaj insulin hauv cov neeg mob uas muaj ntshav qab zib hom 2.

Glucagon tso pa tawm: nyob rau hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus tawm tsam keeb kwm ntawm hyperglycemia, kev tswj hwm ntawm exenatide suppresses zais cia ntau dhau ntawm glucagon.Txawm li cas los xij, exenatide tsis cuam tshuam rau lub cev glucagon teb li cas rau kev mob ntshav qab zib.

Kev nrhiav zaub mov: kev tswj hwm ntawm exenatide ua rau muaj kev poob qab los noj mov thiab txo qis hauv kev noj zaub mov.

Phaj plab muab nchuav: nws tau pom tias kev tswj hwm ntawm exenatide inhibits lub plab zom mov, uas ua rau nws qeeb. Hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, kev kho mob exenatide hauv kev kho mob monotherapy thiab nyob rau hauv kev sib xyaw nrog metformin thiab / lossis sulfonylurea kev npaj ua rau txo qis ntawm cov ntshav qabzib concentration, postprandial ntshav qabzib concentration, thiab HbA1c, yog li txhim kho glycemic tswj hauv cov neeg mob no.

Cov Tshuaj Pharmacokinetics

Tom qab ua haujlwm subcutaneous rau cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus, exenatide nrawm nrawm thiab nce mus txog qhov nruab nrab ntshav siab tshaj plaws tom qab 2.1 teev. Qhov nruab nrab siab tshaj plaws (Cmax) yog 211 pg / ml thiab tag nrho thaj tsam hauv qab cov phiaj xwm qhov siab-sijhawm (AUC)_{0-rau cov}) yog 1036 pg x h / ml tom qab subcutaneous tswj hwm ntawm ib koob tshuaj 10 exg exenatide. Thaum tso tawm rau exenatide, AUC nce rau hauv kev faib ua feem rau cov koob tshuaj nce ntxiv los ntawm 5 μg txog 10 μg, thaum tsis muaj qhov sib npaug ntawm Cmax. Tib cov txiaj ntsig tau pom nrog kev coj ua subcutaneous ntawm exenatide hauv plab, ncej puab lossis xub pwg.

Qhov ntim ntawm kev faib tawm ntawm exenatide tom qab subcutaneous tswj hwm yog 28.3 litres.

Kev ntsuas phoo thiab nthuav tawm

Exenatide yog feem ntau raug ntog los ntawm glomerular pom ua raws los ntawm kev kho mob proteolytic kev ua haujlwm. Exenatide tshem tawm yog 9.1 l / teev thiab qhov kawg ib nrab-lub neej yog 2.4 teev. Cov ntsej muag pharmacokinetic ntawm exenatide yog koob tshuaj ywj siab. Ntsuas qhov ntau ntawm exenatide raug txiav txim kwv yees li 10 teev tom qab noj tshuaj.

Cov pab pawg neeg tshwj xeeb

Cov neeg mob uas lub raum tsis ua hauj lwm zoo

Hauv cov neeg mob uas muaj mob me me los yog ua rau lub raum tsis ua haujlwm (kev tsim kho lub peev xwm ntawm 30-80 ml / min), exenatide tshem tawm tsis txawv ntau ntawm kev tshem tawm hauv cov ncauj lus nrog lub raum kev ua haujlwm, yog li ntawd, kev kho tshuaj tsis tas yuav tsum tau. Txawm li cas los xij, hauv cov neeg mob uas mob raum ua rau lub raum tsis ua haujlwm, kev txiav txim siab nruab nrab yog txo mus rau 0.9 l / h (piv rau 9.1 l / teev hauv cov ntsiab lus noj qab haus huv).

Cov neeg mob uas muaj lub siab ua haujlwm tsis zoo

Txij li thaum exenatide tsuas yog ua tawm los ntawm lub raum, nws ntseeg tau tias qhov ua tsis tau haujlwm hepatic tsis hloov qhov concentration ntawm exenatide hauv cov ntshav. Cov neeg laus Lub hnub nyoog tsis cuam tshuam rau pharmacokinetic cov yam ntxwv ntawm exenatide. Yog li, cov neeg laus laus tsis tas yuav tsum ua qhov hloov kho koob tshuaj.

Cov menyuam Cov pharmacokinetics ntawm exenatide hauv cov menyuam yaus tsis tau kawm.

Cov Hluas (12 txog 16 xyoo)

Hauv kev muab tshuaj pharmacokinetic ua nrog cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus hauv pawg hnub nyoog ntawm 12 txog 16 xyoo, kev tswj hwm ntawm exenatide ntawm koob tshuaj 5 μg tau nrog pharmacokinetic tsis zoo ib yam li cov uas tau pom nyob hauv cov neeg laus.

Tsis muaj qhov sib txawv ntau qhov sib txawv ntawm tus txiv neej thiab poj niam hauv pharmacokinetics ntawm exenatide. Kwv Txhiaj Cov haiv neeg tsis muaj qhov cuam tshuam tseem ceeb ntawm pharmacokinetics ntawm exenatide. Tsis tas yuav muab hloov kho los ntawm haiv neeg keeb kwm.

Rog cov neeg mob

Tsis muaj qhov tshwm sim pom tseeb ntawm kev ntsuas lub cev (BMI) thiab exenatide pharmacokinetics. Koob tshuaj hloov kho raws li BMI yog tsis xav tau.

Kev ntsuas rau siv

Hom 2 mob ntshav qab zib mellitus raws li kev kho mob monotherapy ntxiv rau kev noj haus thiab kev tawm dag zog kom ua tiav kev tswj glycemic.

Kev sib txuas ua ke
Hom 2 mob ntshav qab zib mellitus ua kev kho mob ntxiv rau metformin, sulfonylurea derivative, thiazolidinedione, kev sib xyaw ntawm metformin thiab sulfonylurea derivative lossis metformin thiab thiazolidinedione thaum tsis muaj glycemic txaus. Hom 2 mob ntshav qab zib mellitus raws li kev kho mob ntxiv rau kev sib xyaw ntawm basal insulin thiab metformin kev npaj los txhim kho glycemic tswj.

Cov Yuav Tsum Tau Ua

Hypersensitivity rau exenatide lossis excipients uas ua cov tshuaj
Hom 1 mob ntshav qab zib mellitus lossis qhov muaj ntshav qab zib ketoacidosis
Mob raum tsis ua haujlwm (creatinine tshem tawm Kev Kho Mob Los Ntawm Kev Kho Mob)

Cov kev tsis haum siab uas tau tshwm sim ntau dua li ntawm qhov raug rho tawm raug teev tseg raws li cov kev paub hauv qab no: feem ntau (≥10%), feem ntau (≥1%, 0.1%, 0.01%, kev sib xyaw ua ke

Cov kev tshwm sim tsis zoo uas tshwm sim ntau dua hauv ib rooj plaub yog teev raws li cov ntawv sau hauv qab no: feem ntau (≥10%), feem ntau (≥1%, 0.1%, 0.01%, NPE THIAB TXHEEJ TXHEEM NYOB RAU HAUV HOLDER (TUS TSWV) NTAWV SIB THAM

AstraZeneca UK Limited, UK 2 Kingdom Street, London W2 6BD, UK AstraZeneca UK Limited, United Kingdom 2 Kingdom Street, London W2 6BD, Tebchaws Askiv

Chaw tsim tshuaj paus

Baxter Pharmaceutical Solutions ELC, Tebchaws Asmeskas
927 South Curry Pike, Bloomington, Indiana, 47403, Tebchaws Asmeskas
Baxter Tshuaj Kho Mob LLC, USA
927 South Curry Pike, Bloomington, Indiana 47403, Asmeskas

TUS MIV TAWB (THAWJ COV PHOOJ YWG)

1. Baxter Pharmaceutical Solutions ELC, Tebchaws Asmeskas 927 South Curry Pike, Bloomington, Indiana, 47403, Tebchaws Asmeskas Baxter Cov Tshuaj Kho Mob LLC, Tebchaws Asmeskas 927 South Curry Pike, Bloomington, Indiana 47403, Tebchaws Asmeskas (cartridge filling)

2. Sharp Corporation, USA 7451 Keebler Txoj Kev, Allentown, PA, 18106, USA Sharp Corporation, Tebchaws Asmeskas 7451 Keebler Txoj Kev, Allentown, Pennsylvania, 18106, Tebchaws USA (cartridge sib dhos hauv rab koob xaum xim)

QHOV ROOJ (OB TXHAIS LUS) (NTIM) NTIM)

Enestia Belgium NV, Belgium
Kloknerstraat 1, Hamont-Ahel, B-3930,
Belgium Enestia Belgium NV, Belgium
Klocknerstraat 1, Hamont-Achel, B-3930, Belgium

TSWJ ZOO LICAS

AstraZeneca UK Luag, UK
Silk Road Business Park, Mcclesfield, Cheshire, SK10 2NA, UK
AstraZeneca UK Limited, United Kingdom brSilk Txoj Kev Lag Luam Chaw Ua Si, Macclesfield, Cheshire, SK10 2NA, United Kingdom

Lub npe, chaw nyob ntawm lub koom haum tso cai los ntawm tus tuav lossis tus tswv ntawm daim ntawv sau npe ntawm cov khoom lag luam rau kev kho mob kom lees txais kev thov los ntawm cov neeg siv khoom:

Sawv cev ntawm AstraZeneca UK Limited, United Kingdom,
hauv Moscow thiab AstraZeneca Cov Tshuaj LLC
125284 Moscow, st. Khiav, 3, p. 1

Baeta lossis Victoza: uas yog qhov zoo dua?

Ob qhov tshuaj suav nrog tib pab pawg - cov khoom hluavtaws sib xyaw ntawm incretin, muaj kev kho mob zoo sib xws.

Tab sis Victoza muaj cov txiaj ntsig zoo dua ntxiv uas pab txo qhov hnyav ntawm cov neeg rog rog uas muaj ntshav qab zib hom II.

Victoza muaj cov nyhuv ntev dua, thiab nws raug pom zoo tias subcutaneous txhaj tshuaj ntawm cov tshuaj tau muab ib hnub ib zaug thiab tsis hais txog kev noj zaub mov, thaum Bayetu yuav tsum tau noj ob zaug ib hnub ib teev ua ntej noj mov.

Tus nqi muag ntawm Viktoza hauv cov khw muag tshuaj yog qhov siab dua.

Tus kws kho mob uas tuaj koom ua tus txiav txim siab txog kev xaiv tshuaj, suav txog tus yam ntxwv ntawm tus neeg mob, qhov tsis zoo ntawm kev mob tshwm sim thiab kev ntsuas qhov tsis ua kom raug tus kabmob.