Qee zaum cov khoom noj tshwj xeeb thiab kev tawm dag zog tsis tuaj yeem muab cov ntshav qab zib ib txwm nyob hauv cov ntshav qab zib uas muaj 2 daim ntawv ntawm tus kabmob.

Ib qho yeeb tshuaj nrog INN Repaglinide, qhov kev qhia ntawm uas txuas rau txhua pob ntawm cov tshuaj uas muaj nws, nws muaj qhov tsis zoo thaum tsis tuaj yeem tswj tau qhov kev ua kom muaj suab thaj hauv cov ntshav. Kab lus no yuav hais txog nqe lus nug ntawm kev siv tshuaj nrog repaglinide kom raug thiab qhov twg siv tsis tau.

Pharmacological cov yam ntxwv ntawm cov tshuaj

Cov khoom xyaw nquag, Repaglinide, muaj nyob hauv daim ntawv dawb hmoov rau kev siv sab hauv. Tus txheej txheem ntawm kev ua ntawm qhov kev sib xyaw yog qhov tso tawm ntawm cov kua dej (ib yam qab zib-txo cov tshuaj hormones) los ntawm beta hlwb nyob hauv cov txiav

Siv cov tshuaj repaglinide ntawm cov txais tshwj xeeb, ATP-nyob rau hauv qhov chaw nyob hauv cov qog ua ke ntawm cov beta hlwb. Cov txheej txheem no provokes depolarization ntawm cov hlwb thiab qhib ntawm calcium calcium. Raws li qhov tshwm sim, kev tsim cov tshuaj insulin yog nce ntxiv los ntawm kev nce tus kab mob calcium.

Tom qab tus neeg mob noj tshuaj kom zoo dua ntawm Repaglinide, cov tshuaj yog nqus rau hauv cov hnyuv. Nyob rau tib lub sijhawm, tom qab 1 teev tom qab noj mov, nws yog feem ntau ua haujlwm nyob rau hauv cov ntshav ntshav, tom qab ntawd tom qab 4 teev nws tus nqi nce sai dua thiab ua qis heev. Cov kev tshawb fawb ntawm cov tshuaj tau pom tias tsis muaj qhov sib txawv hauv pharmacokinetic qhov tseem ceeb thaum siv cov tshuaj Repaglinide ua ntej lossis thaum noj mov tau pom.

Cov tshuaj khi rau cov ntshav protein ntau dua 90%. Ntxiv mus, qhov tseeb txog kev nyab xeeb tsis pub dhau mus txog 63%, thiab nws qhov kev faib tawm yog 30 litres. Nws yog nyob rau hauv lub siab hais tias biotransformation ntawm Repaglinide tshwm sim, vim qhov kev ua haujlwm tsis muaj zog hauv cov metabolites. Yeej, lawv tau tawm nrog cov kua tsib, nrog rau cov zis (8%) thiab cov quav (1%).

30 feeb tom qab noj cov tshuaj Repaglinide, cov tshuaj hormones tso rau lub sijhawm pib. Vim li ntawd, cov ntsiab lus ntawm cov piam thaj hauv cov ntshav tau sai heev. Nruab nrab ntawm cov pluas noj, tsis muaj kev nce insulin ntau ntau.

Hauv cov neeg mob uas tsis mob ntshav qab zib cov kab mob insulin uas noj li 0.5 mus rau 4 g ntawm Repaglinide, qhov tshuaj tiv thaiv tsis muaj qab zib nyob rau hauv lub cev.

Cov lus qhia rau kev siv tshuaj

Repaglinide yog cov khoom tseem ceeb ntawm NovoNorm, uas yog tsim hauv Denmark. Pharmacological tuam txhab Novo Nordisk A / C tsim tawm tshuaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj nrog ntau qhov sib txawv - 0.5, 1 thiab 2 mg. Ib qho hlwv muaj 15 ntsiav tshuaj, hauv ib pob ob peb lub hlwv kuj yuav muaj.

Hauv txhua pob ntawm cov tshuaj nrog cov tshuaj tiv thaiv repaglinide, cov lus qhia rau kev siv yog qhov yuav tsum tau ua. Cov koob tshuaj yog xaiv los ntawm tus kheej ib tus kws kho mob tshwj xeeb uas ntsuas qhov tsis zoo ntawm cov piam thaj thiab cov kab mob sib cuam tshuam ntawm tus neeg mob. Ua ntej siv cov tshuaj, tus neeg mob yuav tsum ua tib zoo nyeem cov lus qhia uas txuas nrog.

Qhov koob tshuaj thawj zaug yog 0.5 mg, nws tuaj yeem nce ntxiv tsuas yog tom qab ib lossis ob lub lis piam, dhau kev kuaj sim rau qib qab zib. Qhov noj tshuaj ntau tshaj plaws yog 4 mg, thiab koob tshuaj txhua hnub yog 16 mg. Thaum lub sijhawm hloov los ntawm lwm qhov txo cov tshuaj yaj yeeb tshuaj Repaglinide noj 1 mg. Nws raug nquahu kom siv cov tshuaj 15-30 feeb ua ntej noj mov loj.

NovoNorm cov tshuaj yuav tsum muab tso kom deb ntawm cov menyuam yaus ntawm qhov kub ntawm 15-25C hauv qhov chaw tiv thaiv los ntawm ya raws.

Lub txee lub neej ntawm cov tshuaj yog txog li 5 xyoos, tom qab lub sijhawm no nws tsis tuaj yeem siv nws hauv qee kis.

Cov txheej txheem sib tsoo thiab cov phom sij uas yuav muaj

Hmoov tsis zoo, tsis yog txhua tus neeg tuaj yeem lees txais NovoNorm. Zoo li lwm yam tshuaj, nws muaj contraindications.

Cov tshuaj repaglinide tsis tuaj yeem nqa nrog:

hom mob ntshav qab zib insulin
ketoacidosis uas mob ntshav qab zib, nrog rau tsis nco qab,
mob rau lub siab thiab / lossis lub raum tsis ua hauj lwm zoo,
siv ntxiv ntawm cov tshuaj uas ntxias lossis inhibit CYP3A4,
lactose intolerance, lactase deficiency thiab glucose-galactose malabsorption,
ua kom raug rau cov khoom tivthaiv,
tsis tau muaj 18 xyoo
npaj los yog cev xeeb tub,
pub niam mis.

Cov ntawv soj ntsuam tau ua haujlwm ntawm cov nas ua pov thawj tias kev siv cov tshuaj repaglinide thaum lub sijhawm ua rau menyuam muaj qhov tsis zoo cuam tshuam rau lub cev hauv plab. Raws li kev haus dej, kev txhim kho ntawm qhov nruab nrab sab sauv thiab qis dua ntawm tus me nyuam hauv lub cev tsis tuaj yeem hloov kho. Tsis tas li, kev siv tshuaj yeeb dej caw yog txwv thaum lub sijhawm lactation, vim nws kis nrog niam cov kua mis rau menyuam.

Qee zaum nrog kev siv tshuaj tsis raug cai lossis kev haus ib qho dhau hwv lawm, qhov tshwm sim ntawm qhov tshwm sim tsis zoo xws li:

ntshav qog ntshav (tawm hws, tshee tshee, pw tsis tsaug zog, tachycardia, ntxhov siab),
kev tsis zoo ntawm cov cuab yeej siv qhov muag pom (thaum xub thawj, noj tshuaj, tom qab ntawd dhau),
mob plab zom mov (mob plab, xeev siab thiab ntuav, cem quav lossis zawv plab, nce kev ua haujlwm ntawm cov enzymes hauv daim siab),
kev ua xua (liab ntawm daim tawv nqaij - erythema, tawm pob, khaus).

Kev siv cov tshuaj loj dua li kws kho mob tau qhia yuav luag ib txwm ua rau lub qog ntshav qab zib. Yog tias cov ntshav qab zib xav tias ntau tshaj cov tsos mob me me thiab paub meej, nws yuav tsum noj khoom noj uas muaj cov khoom noj uas yog carbohydrate thiab sab laj nrog kws kho mob txog kev kho qhov ntau npaum li cas.

Hauv cov ntshav qog ntshav hnyav, thaum tus neeg mob tsis nco qab lossis tsis nco qab lawm, nws tau txhaj nrog 50% kua nplaum nyob hauv qab daim tawv nqaij nrog ntxiv kev tso ntshav ntawm 10% kev daws teeb meem kom muaj suab thaj tsawg kawg yog 5.5 mmol / L.

Kev sib cuam tshuam ntawm Repaglinide nrog Lwm Yam Tshuaj

Kev siv cov tshuaj concomitant feem ntau cuam tshuam rau cov hauj lwm zoo ntawm repaglinide ntawm cov piam thaj.

Nws cov nyhuv hypoglycemic yog kho kom zoo dua thaum tus neeg mob siv MAO thiab ACE inhibitors, tsis xaiv tshuaj beta-blockers, tsis-tshuaj steroidal anti-inflammatory tshuaj, salicylates, anabolic steroids, okreotide, tshuaj uas muaj ethanol.

Cov tshuaj hauv qab no cuam tshuam tsis zoo rau lub peev xwm ntawm cov tshuaj kom txo cov piam thaj:

thiazide diuretics,
tshuaj tiv thaiv siv rau qhov ncauj,
danazol
glucocorticoids,
cov thyroid hormones
sympathomimetics.

Tsis tas li, tus neeg mob yuav tsum coj mus rau hauv tus account uas repaglinide cuam tshuam nrog cov tshuaj uas tso tawm hauv cov kua tsib. CYP3A4 inhibitors xws li intraconazole, ketoconazole, fluconazole thiab qee yam tuaj yeem ntxiv nws cov ntshav. Kev siv CYP3A4 inducers, tshwj xeeb yog phomampicicin thiab phenytoin, txo qis qib ntawm ib yam khoom hauv ntshav. Muab qhov tseeb tias qib ntawm induction tsis tau txiav txim siab, kev siv cov tshuaj Repaglinide nrog cov tshuaj no yog txwv tsis pub.

Cov Duab Tsim Tshuaj Liab

Cov Duab Tsim Tshuaj Liab


Tshuaj lom neeg cov khoom sib txuas
IUPAC	(Qha) - (+) - 2-ethoxy-4-2- (3-methyl-1-2- (piperidin-1-yl) phenylbutylamino) -2-oxoethylbenzoic acid
Cov piav suav	C₂₇H₃₆N₂O₄
Molar loj	452,586 g / mol
Cas	135062-02-1
PubChem	65981
Tshuajqauj Tshuaj	DB00912
Kev faib tawm
ATX	A10BX02
Cov Tshuaj Pharmacokinetics
Bioav Tseem Muaj	56% (ntawm qhov ncauj)
Ntshav Protein losis tswvyim dabtsi	>98%
Kev zom zaub mov	Hepatic oxidation thiab glucuronidation (CYP3A4-mediated)
Ib nrab-lub neej.	1 teev
Kev cais tawm	Fecal (90%) thiab lub raum (8%)
Tus thawj coj kev tswj hwm
Qhov ncauj
Cov Ntaub Ntawv Hauv Xov Xwm Wikimedia

Cov Duab Tsim Tshuaj Liab - tshuaj tiv thaiv kab mob, tau tsim xyoo 1983. Repaglinide yog ib qho tshuaj noj hauv qhov ncauj siv ntxiv rau kev noj haus thiab kev tawm dag zog kom tswj ntshav qab zib hauv ntshav qab zib hom 2. Cov txheej txheem ntawm kev txiav txim ntawm Repaglinide qhia kev nce ntawm kev tso tawm ntawm insulin los ntawm β-islet hlwb ntawm lub txiav, zoo li nrog lwm cov tshuaj tiv thaiv kab mob, cov tshuaj tiv thaiv lub ntsiab yog hypoglycemia. Cov tshuaj yuav muag los ntawm Novo Nordisk hauv qab lub npe Qhuas nyob meskas Glucoorm hauv Canada Xab hauv Nyij Pooj Cov Duab Tsim Tshuaj Liab rau tim lyiv teb chaws los ntawm Ifi, thiab NovoNorm nyob rau lwm qhov chaw. Hauv Nyij Pooj, nws tsim tawm los ntawm Dainippon Sumitomo Pharma.

Cov cuab yeej fwm

Repaglinide yog ib qho tshuaj noj hauv qhov ncauj siv ntxiv rau kev noj haus thiab kev tawm dag zog kom tswj ntshav qab zib hauv ntshav qab zib hom 2.

Cov Yuav Tsum Muaj

Repaglinide yog cov neeg hauv nrog:

Ntshav qab zib ketoacidosis
Yam 1 ntshav qab zib
Concomitant siv nrog gemfibrozil
Hypersensitivity rau cov tshuaj los yog cov khoom xyaw tsis zoo

Sab sij huam

Cov kev mob tshwm sim muaj xws li:

Cov mob voos ua pa sab sauv (16%)
Kev mob ntsws (6%)
Rhinitis (3%)

Cov kev mob tshwm sim hnyav heev suav nrog:

Myocardial ischemia (2%)
Angina pectoris (1.8%)
Tuag vim yog mob plawv (0.5%)

Rau cov neeg tshwj xeeb

Cev xeeb tub qeb C: Kev nyab xeeb rau cov poj niam cev xeeb tub tsis tau tsim. Cov ntaub ntawv muaj tsawg, thiab muaj tsuas yog ib kis, daim ntawv ceeb toom sau tseg tias tsis muaj kev cuam tshuam nrog kev siv cov tshuaj repaglinide thaum cev xeeb tub.

Kev ceev faj yuav tsum tau siv nrog cov neeg muaj kab mob siab thiab lub raum tsis ua haujlwm thaum siv cov tshuaj no.

Yeeb tshuaj sib cuam tshuam

Repaglinide yog qhov tseem ceeb ntawm cov tshuaj SUR3A4 thiab yuav tsum tsis txhob siv ib txhij nrog gemfibrozil, clarithromycin, lossis azole antifungal tshuaj xws li Itraconazole thiab Ketoconazole. Kev noj tshuaj repaglinide ua ke nrog ib lossis ntau dua ntawm cov tshuaj no ua rau muaj ntau ntxiv ntawm plasma repaglinide ntau ntau thiab tuaj yeem ua rau lub qog ntshav qab zib. Kev tswj hwm ntawm clopidogrel thiab repaglinide (thiab cyp2c8 inhibitor) tuaj yeem ua rau txo qis cov ntshav qabzib ntau vim kev sib txuam tshuaj. qhov tseeb, kev siv cov tshuaj no ua ke rau tsawg kawg ib hnub tuaj yeem ua rau mob ntshav qab zib tsawg kawg. Repaglinide yuav tsum tsis txhob coj los ua ke nrog sulfonylurea, vim tias lawv muaj tib lub tshuab ntawm kev ua.

Mechanism ntawm kev ua

Repaglinide txo qis ntshav qabzib los ntawm kev ua kom tso cov kua dej tawm los ntawm cov roj ntsha ntawm tes ntawm pancreatic islet. Qhov no yog ua tiav los ntawm kev kaw ATP-cov neeg tso cia cov potassium nyob rau hauv daim nyias nyias ntawm cov beta hlwb. Qhov no depolarizes cov beta hlwb, qhib lub cell calcium calcium raws, thiab vim li ntawd, qhov kev nkag ntawm calcium ua rau cov kua dej tsis zais.

Cov Tshuaj Pharmacokinetics

Kev Zam Txim Cia: Repaglinide muaj 56% bioavailability thaum nqus tau ntawm txoj hnyuv plab. Bioavailability yog txo qis thaum noj nrog zaub mov, qhov siab tshaj plaws tau txo yog 20%.

Kev faib khoom faib: cov protein khi ntawm repalglinide rau albumin yog ntau dua li 98%.

Kev zom zaub mov: Repaglinide metabolized feem ntau hauv lub siab, tshwj xeeb hauv CYP450 2C8 thiab 3A4 thiab rau qee qhov tsawg dua los ntawm glucuronidation. Repaglinide metabolites nyob hauv lub zog thiab tsis ua kom pom cov piam thaj txo qis.

Kev Tawm Tseg: Repaglinide yog 90% nyob hauv cov quav thiab 8% zis. 0.1% tshem tawm nrog cov zis tsis hloov pauv. Tsawg dua 2% tsis hloov pauv hauv cov quav.

Zaj dab neeg

Repaglinide precursors tau tsim tawm thaum xyoo 1983 hauv Bieberrach ntawm Rice nyob rau yav qab teb lub teb chaws Yelemees.

Cov cuab yeej fwm

Hauv Tebchaws Meskas, muaj kev tiv thaiv Patent, kev sau npe yog tsim nyob rau lub Peb Hlis 1990, thaum kawg los ua Tebchaws Asmeskas patent 5,216,167 (Lub Rau Hli 1993), 5,312,924 (Tsib Hlis 1994) thiab 6,143,769 (Kaum Ib Hlis 2000). Tom qab

Kev pom zoo rau kev siv

Hauv qee qhov xwm txheej, cov neeg mob yuav tsum siv cov tshuaj nrog kev ceev faj heev los ntawm kev saib xyuas ntawm tus kws kho mob uas tau sau ntawv yuav noj tsawg kawg. Cov neeg mob no suav nrog cov neeg mob uas raug mob los ntawm kab mob siab thiab / lossis ob lub raum, uas tau muaj kev phais mob ntau ntxiv, uas nyuam qhuav muaj kab mob khaub thuas lossis kis tus kab mob, cov neeg laus (los ntawm 60 xyoo) uas ua raws li cov zaub mov tsis zoo.

Yog hais tias tus neeg mob tau mob hypoglycemic lub xeev nyob rau hauv me me los yog mob me, nws tuaj yeem raug tshem tawm ntawm nws tus kheej. Txhawm rau ua qhov no, koj yuav tsum tau noj cov zaub mov uas muaj cov zom zom tau yooj yim - ib qho qab zib, qab zib, kua txiv qab zib lossis txiv hmab txiv ntoo. Nyob rau hauv daim ntawv loj heev nrog qhov tsis nco qab, raws li twb tau hais los, cov kua nplaum ntawm cov tshuaj yog muab tshuaj rau hauv lub cev.

Nws yuav tsum raug sau tseg tias cov beta-blockers muaj peev xwm los npog qhov tshwm sim ntawm hypoglycemia. Cov kws kho mob nquahu kom tsis txhob haus cawv ntau ntxiv thaum ethanol txhim kho ntxiv thiab txuas ntxiv cov nyhuv hypoglycemic ntawm Repaglinide.

Tsis tas li, cov tshuaj txo qis ntawm kev saib xyuas.

Yog li, cov tsav tsheb tiv thaiv keeb kwm ntawm kev siv repaglinide, nws yog ib qho tsim nyog yuav tsum tsis txhob tsav tsheb lossis ua lwm yam kev ua haujlwm txaus ntshai thaum kev kho mob.

Nqi, tshuaj xyuas thiab analogues

Repaglinide yog cov tshuaj tseem ceeb tau siv nyob rau hauv cov tshuaj NovoNorm.

Koj mus yuav tau tom lub khw muag tshuaj lossis xaj online ntawm tus muag lub vev xaib. Txawm li cas los xij, kev yuav cov tshuaj yog ua tau tsuas yog thaum tso tawm tshuaj ntawm cov tshuaj.

Tus nqi ntawm cov tshuaj nws txawv:

1 mg ntsiav tshuaj (30 daim ib pob) - los ntawm 148 txog 167 rubles Lavxias,
2 mg ntsiav tshuaj (30 daim ib pob) - los ntawm 184 txog 254 rubles Lavxias.

Raws li koj tuaj yeem pom, tus nqi yog heev loyal rau cov neeg uas tau nyiaj tsawg. Nyeem cov kev ntsuam xyuas ntawm ntau tus neeg mob ntshav qab zib, nws tuaj yeem sau tseg tias pheej yig ntawm tshuaj yog ib qho loj ntxiv, muab nws cov hauj lwm zoo. Ib qho ntxiv, cov txiaj ntsig ntawm NovoNorm yog:

yooj yim ntawm kev siv cov ntsiav tshuaj piv rau kev txhaj tshuaj,
qhov ceev ntawm cov tshuaj, nyob rau hauv tsuas yog 1 teev,
sijhawm ntev noj cov tshuaj.

Qhov kawg txhais tau tias feem ntau cov neeg mob uas kuaj ntshav tsis muaj qhov mob ntshav qab zib-insulin tau noj NovoNorm li 5 xyoos lossis ntau dua. Lawv nco ntsoov tias nws tes haujlwm tseem nyob li qub thiab tsis vav. Txawm li cas los xij, kev tiv thaiv hypoglycemic ntawm cov tshuaj txo rau xoom yog tias TSIS:

ua raws li kev noj zaub mov kom zoo (tsis suav nrog cov khoom noj zom tau yooj yim carbohydrates thiab cov rog),
soj ntsuam kev ua lub neej nquag (mus taug kev tsawg kawg 30 feeb, kev tawm dag zog lub cev, thiab lwm yam),
pheej saib xyuas theem ntawm cov piam thaj (tsawg kawg peb zaug hauv ib hnub).

Feem ntau, cov neeg mob thiab kws kho mob suav tias NovoNorm yog tshuaj tua kabmob zoo. Tab sis qee zaum kev siv cov ntsiav tshuaj txwv tsis pub, vim tias lawv coj mus rau qhov tsis zoo tsim nyog. Hauv cov xwm txheej zoo li no, tus kws kho mob txiav txim siab hloov cov tshuaj ntawm cov tshuaj lossis mus yuav tshuaj kom yuav cov tshuaj sib txawv.

Cov lus txhais muaj tib cov tshuaj nquag thiab sib txawv hauv cov tshuaj ntxiv. NovoNorm ntsiav tshuaj tsuas muaj ib qho txhais - Diagniniside (qhov nruab nrab ntawm 278 rubles).

Zoo xws li cov tshuaj NovoNorm, uas txawv hauv lawv cov khoom sib txuam, tab sis muaj cov txiaj ntsig zoo ib yam, yog:

Jardins (tus nqi nruab nrab - 930 rubles),
Victoza (tus nqi nruab nrab - 930 rubles),
Saksenda (tus nqi nruab nrab - 930 rubles),
Forsyga (nruab nrab tus nqi - 2600 rubles),
Invokana (tus nqi nruab nrab - 1630 rubles).

Nws tuaj yeem xaus lus tias cov tshuaj NovoNorm, uas muaj cov tshuaj nquag rov ua kom zoo, zoo rau hauv kev kho mob ntshav qab zib hom 2. Nws sai sai ua kom cov suab thaj mus txog qib ib txwm. Yog tias koj ua raws li kev noj zaub mov zoo, kev tawm dag zog thiab nrog kev soj ntsuam cov piam thaj tsis tu ncua, koj tuaj yeem tshem tawm qhov tsis muaj ntshav qab zib thiab mob ntshav qab zib ntau. Daim vis dis aus hauv tsab xov xwm no yuav qhia koj kom paub kho ntshav qab zib li cas.