Cov Tshuaj Dianormet: cov lus qhia rau kev siv
Cov Tshuaj Pharmacokinetics Dianormet (nquag muaj cov tshuaj metformin -1.1 - dimethylbiguanide hydrochloride) yog tus neeg sawv cev hypoglycemic rau kev tswj hwm qhov ncauj ntawm cov pab pawg biguanide. Txo cov ntshav qabzib ntau hauv cov neeg mob ntshav qab zib. Cov tshuaj siv tawm ntawm nws cov nyhuv tsis hais txog qhov secretory kev ua haujlwm ntawm tus txiav. Lub tshuab kev ua ntawm Dianormet yog vim muaj kev txwv tsis pub thauj khoom ntawm cov khoom siv hluav taws xob ntawm cov pa ntawm txoj hlab ua pa mitochondrial, uas ua rau kev poob qis hauv kev ua haujlwm ntawm intracellular ATP thiab kev ua haujlwm ntawm anaerobic glycolysis, vim li ntawd cov kua nplaum nkag mus rau hauv lub hlwb los ntawm qhov chaw tso tawm, glycogen depot hauv cov qog ua kom tsawg, thiab kev tsim tawm ntawm pyruvate. zoo nkaus li cov hnyuv, siab, thiab tseem nyob rau hauv cov leeg nqaij thiab adipose.
Qhov kev txiav txim ntawm Dianormet txuas ntxiv mus rau:
- Kev kho mob txoj hnyuv - inhibits qhov nqus ntawm cov piam thaj hauv cov hnyuv, txo lub cev kom sai ntawm lub plab thiab cov hnyuv,
- mob siab - inhibits gluconeogenesis thiab ntws ntawm cov piam thaj rau hauv cov ntshav, txhim kho glycerlysis anaerobic,
- peripheral cov ntaub so ntswg - nce cov ntaub so ntswg kev nqus ntawm cov ntshav qabzib, uas yog vim muaj qhov ua haujlwm ntau ntxiv ntawm cov tshuaj insulin endogenous (qhov kev txiav txim ntawm qib ntawm insulin receptor - qhov nce ntawm cov naj npawb thiab kev sib txuam ntawm cov txais, nrog rau cov kev sib txuam - kev ua haujlwm ntawm cov tshuab uas thauj cov kua nplaum rau cov hlwb). Raws li qhov tshwm sim, Dianormet tsis txhawb qhov kev tso tawm ntawm cov kua dej los ntawm lub hlwb ntawm cov islet apparatus ntawm lub txiav, nws pab tshem tawm hyperinsulinemia, uas yog ib qho tseem ceeb ua rau muaj kev vam meej ntawm vascular teeb meem thiab qhov hnyav nce hauv cov ntshav qab zib hom II.
Ntxiv rau, Dianormet muaj cov txiaj ntsig zoo metabolic rau:
- ntshav lipids - txo cov theem ntawm cov roj (cholesterol) tag nrho los ntawm 10 its20% thiab nws cov feem ua haujlwm: LDL thiab VLDL, uas cuam tshuam nrog kev cuam tshuam ntawm lawv cov biosynthesis hauv lub plab hnyuv phab ntsa thiab nce ntxiv los ntawm cov hnyuv plab. Nws nce HDL los ntawm 10–20% thiab txo TG los ntawm 10 %20% (txawm tias lawv qib nce los ntawm 50%) los ntawm inhibiting qhov oxidation ntawm fatty acids, qis insulin concentration, thiab inhibiting qhov nqus ntawm cov piam thaj hauv plab hnyuv,
- coagulation thiab fibrinolysis system - txo qhov kev nkag siab ntawm cov platelets rau cov kev sib xyaw ua ke, txhawb kev ua kom cov leeg fibrinolysis los ntawm kev ua haujlwm ntau ntawm t-PA (cov nqaij mos plasminogen activator), txo qis qib PAI-1 (nqaij plasminogen activator inhibitor) thiab txo qib fibrinogen,
- txog hlab ntsha phab ntsa - inhibits qhov loj hlob ntawm vascular du leeg cov leeg.
Cov nyhuv hauv lub cev hauv lub cev ntxiv txiav txim rau nws cov txiaj ntsig zoo ntawm cov kab mob hauv lub plawv, inhibition ntawm kev txhim kho mob ntshav qab zib angiopathy thiab kev tiv thaiv ntawm cov teeb meem xws li mob ntshav siab (arterial hypertension) thiab mob plawv. Hauv cov neeg mob rog, nws tuaj yeem txo lub cev qhov hnyav, tshwj xeeb tshaj yog thaum pib kho.
Cov Tshuaj Pharmacokinetics Nws yog nqus hauv duodenum thiab hnyuv me. Bioavailability yog 50-60%. Cov tshuaj tsis khi rau cov ntshav protein, yog faib tawm sai heev hauv ntau cov ntaub so ntswg, accumulates tsuas yog nyob hauv txoj hnyuv phab ntsa (plab, duodenum thiab plab hnyuv me), mob siab, leeg, raum, salivary qog. Qhov siab tshaj plaws hauv kev ntsuas ntshav yog ua tiav 2 teev tom qab kev tswj hwm. Ib nrab-lub neej yog 1.5-6 teev. Tsis zoo li phenformin, Dianormet tsis muaj cev nqaij daim tawv hauv lub cev. Cov tshuaj tawm tom qab tsis hloov pauv ntawm cov zis (li 90% hauv 12 teev). Hauv cov neeg mob laus thiab cov uas tsis zoo lub raum lub ntsej muag, cov chaw muag tshuaj ntawm metformin hloov pauv ntau. Tag nrho thiab cov mob raum ntxuav hauv cov neeg mob laus yog txo los ntawm 35-40%, hauv cov neeg mob uas muaj mob me thiab mob raum tsis ua haujlwm - los ntawm 74-78%. Thaum lub plab tsis zoo ua haujlwm, lub zog ntawm cov tshuaj yog ua tau.
Kev Siv Tshuaj Dianormet
Sab hauv lub sijhawm lossis tom qab noj mov tas.
Dianormet 500: thawj koob tshuaj 500 mg rau ib hnub. Cov koob tshuaj yuav tsum tau nce siab ntxiv kom tau txais cov txiaj ntsig zoo. Feem ntau noj 500 mg (1 ntsiav tshuaj) 2-3 zaug ib hnub. Qhov siab tshuaj ntau tshaj txhua hnub yog 2500 mg.
Dianormet 850: thawj koob tshuaj 850 mg / hnub. Cov koob tshuaj yuav tsum tau nce siab ntxiv kom tau txais cov txiaj ntsig zoo. Feem ntau noj 1 lub tshuaj 2-3 zaug ib hnub. Qhov siab tshaj plaws yog 2500 mg / hnub.
Qhov siab tshaj plaws kho tau zoo yuav pib tom qab 10-14 hnub ntawm kev kho mob, thiab yog li ntawd cov koob tshuaj yuav tsum tsis txhob nce nrawm dua.
Thaum siv Dianormet ib txhij nrog cov tshuaj insulin hauv thawj 4-6 hnub, koob tshuaj insulin tsis hloov pauv, yav tom ntej, cov koob tshuaj insulin yog maj mam txo (los ntawm 4-8 IU rau ob peb hnub).
Cov Cim Txheeb Rau Siv Tshuaj Dianormet
Cov tshuaj tiv thaiv tsis haum rau cov tshuaj, mob ntshav qab zib tsis nco qab, metabolic acidosis, kab mob lactic acidosis, lub xeev ntawm hypoxia (vim yog hypoxemia, poob siab, thiab lwm yam), lub raum, daim siab tsis ua haujlwm, lub plawv tsis ua haujlwm nrog cov nqaij hypoxia, myocardial infarction, ua tsis taus pa, mob hnyav, ua haujlwm, kis mob , kev siv ntawm iodine-muaj cov tshuaj tiv thaiv kev cuam tshuam, kev quav dej caw, lub sijhawm ntawm cev xeeb tub thiab lactation.
Kev phiv tshuaj ntawm Dianormet
Tsis tshua muaj qab los noj mov, yog xim nqaij hauv lub qhov ncauj, xeev siab, ntuav, mob plab, raws plab. Kev txo qis ntawm qhov mob hnyav ntawm cov tshwm sim tau ua tiav los ntawm kev siv cov tshuaj nrog zaub mov lossis pib kho nrog kev noj tshuaj tsawg txhua hnub. Yog hais tias dyspeptic tshwm sim tsis dhau lawv tus kheej rau lub sij hawm ntev, cov tshuaj yuav tsum tau tsum tsis ua ntxiv.
Tsis tshua muaj, mob taub hau thiab kiv taub hau, qaug zog, ua xua ntawm daim tawv nqaij qhia.
Nrog kev kho mob ntev hauv qee yam mob, megaloblastic anemia yuav tshwm sim vim malabsorption ntawm cov vitamin B12 thiab folic acid. Thaum siv cov tshuaj, nws muaj peev xwm tsim tau cov kab mob lactic acidosis, qhov tshwm sim uas raug txhawb los ntawm cov nqaij mos hypoxia, lub raum, lub siab lossis lub ntsws ua tsis taus pa, mob ntshav tsis ua haujlwm, nqaij hypoxia, kis mob thiab oncological, hypovitaminosis, haus cawv, tshuaj loog, laus hnub nyoog. Hauv cov xwm txheej zoo li no, hemodialysis yog qhia. Thaum kho nrog Dianormet ua ke nrog sulfonylurea derivatives thiab / los yog insulin hypoglycemia tuaj yeem tsim kho, nyob rau hauv cov xwm txheej zoo li no, kev kho tshuaj ntawm cov tshuaj uas siv yog tsim nyog.
Cov lus qhia tshwj xeeb rau kev siv tshuaj Dianormet
Thaum kho nrog Dianormet, cov piam thaj hauv ntshav thiab zis yuav tsum tau saib xyuas tsis tseg. Yog tias tsim nyog, kev phais mob, kev qhia txog kev kuaj mob sib txawv Dianormet rau lub sijhawm luv luv. Kev haus dej cawv ua kom muaj kev phom sij ntau ntawm cov kab mob lactic acidosis hauv kev kho mob ntawm Dianormet. Nrog rau kev siv ua ke ntawm Dianormet nrog sulfonylurea derivatives thiab insulin, nrog cov khoom noj tsis txaus, tom qab kev tawm dag zog lub cev lossis thaum muaj dej cawv ua rau qaug cawv, lub xeev hypoglycemic tuaj yeem tsim kho, uas yuav tsum tau suav nrog thaum tsav tsheb thiab ua haujlwm nrog cov phom sij txaus ntshai.
Ua ntej thiab thaum kho nrog Dianormet, nws yog ib qho tsim nyog yuav tsum tau soj ntsuam daim siab thiab raum ua haujlwm tsis tu ncua. Nrog rau kev siv sijhawm ntev ntawm cov tshuaj, kuaj ntshav morphological yuav tsum tau nqa ib xyoos ib zaug, txij li metformin tuaj yeem muab tso rau hauv cov ntshav liab.
Tshuaj sib cuam tshuam tshuaj Dianormet
Dianormet ua synergistically nrog sulfonylurea derivatives (glibenclamide, glipizide), insulin thiab acarbose. Amiloride, digoxin, quinidine, morphine, procainamide, triamteren, trimethoprim, cimetidine, ranitidine, famotidine, calcium channel blockers (tshwj xeeb tshaj yog nifedipine) inhibit tubular ua rau hauv lub raum thiab tuaj yeem nce qhov concentration ntawm Dianormet hauv cov ntshav. Furosemide tsub kom lub siab ntawm Dianormet hauv cov ntshav cov ntshav, thiab Dianormet txo qhov kev xav thiab ib nrab ntawm lub neej ntawm furosemide.
Thaum siv nrog cov tshuaj uas tuaj yeem ua rau mob ntshav qab zib (clofibrate, probenecid, propranalol, rifampicin, sulfonamides, salicylates), qhov koob tshuaj Dianormet txo.
Cov tshuaj uas tuaj yeem ua rau hyperglycemia (qhov ncauj tiv thaiv estrogen-muaj cov tshuaj, corticosteroids, diuretics, isoniazid, nicotinic acid, phenytoin, chlorpromazine, thyroid hormones, sympathomimetics) tuaj yeem txo qhov kev ua haujlwm ntawm Dianormet. Nyob rau hauv cov ntaub ntawv ntawm nws ua ke siv nrog cov tshuaj no, cov ntshav qab zib cov ntsiab lus yuav tsum tau saib xyuas thiab, yog tias tsim nyog, ib qho kev sib txuam ntawm cov koob tshuaj Dianormet. Kev haus dej cawv kom tsis txhob muaj feem ua rau cov kab mob lactic acidosis. Colestyramine thiab guar qeeb qeeb nqus ntawm Dianormet, txo nws cov nyhuv. Cov nyiaj no yuav tsum tau siv ob peb teev tom qab siv Dianormet. Cov tshuaj txhim kho cov nyhuv ntawm qhov ncauj anticoagulants ntawm pab pawg coumarin.
Ntau tshaj ntawm cov tshuaj Dianormet, cov tsos mob thiab kev kho mob
Txawm tias ib qho kev noj qab haus huv tseem ceeb tshaj plaws feem ntau tsis ua rau kev txhim kho hypoglycemia, tab sis muaj kev hem thawj ntawm cov kab mob lactic acid: ua kom muaj kev noj qab haus huv, tsis muaj zog, mob leeg, xeev siab, ntuav, raws plab, mob plab, ua tsis taus pa. Kev kho mob ntawm cov kab mob lactic acidosis - hemodialysis.
Cov tsos mob mob me dhau: ua kom tsaug zog, plooj tsis pom kev, qhov hnoos qeev qhuav ntawm qhov ncauj qhov ncauj. Thaum cov tsos mob no tshwm sim, tus neeg mob yuav tsum nyob hauv kev saib xyuas ntawm tus kws kho mob. Kev Kho Mob khuv xim.
Hauv kev siv tshuaj ntau dhau, txo qis lossis nce ntshav siab, ceev cov tub ntxhais kawm, tachy lossis bradycardia, ischuria (vim yog atony ntawm lub zais zis), mob plab hnyuv hypokinesia, hypo- lossis hyperthermia, nce ntxiv ntawm leeg lub cev, ua tsis taus pa, ua tsis taus pa, coma tau. Kev Kho Mob - kev tshem tawm yeeb tshuaj, mob plab zom mov, hemodialysis, rov qab kho cov ntshav pH, tshem tawm hypoxia, kho cov tshuaj tiv thaiv kab mob siab, ua kom lub luag haujlwm ntawm lub plawv thiab lub ntsws ua pa.
Cov lus qhia rau siv Dianormet
Metformin 500 mg, 850 mg lossis 100 mg.
Lwm cov khoom xyaw: povidone, talc, magnesium stearate.
hom 2 mob ntshav qab zib mellitus (non-insulin-dependant) nrog qhov tsis muaj txiaj ntsig ntawm kev kho kev noj zaub mov, tshwj xeeb tshaj yog nyob rau cov neeg mob rog dhau: kev kho mob monotherapy lossis kev sib xyaw ua ke nrog kev sib xyaw nrog lwm tus neeg lub qhov ncauj hypoglycemic lossis sib xyaw nrog insulin rau kev kho mob ntawm cov neeg laus, xws li monotherapy lossis kev sib txuas nrog kev kho mob nrog insulin. rau kev kho mob menyuam yaus los ntawm 10 xyoo.
Txo txo cov mob ntshav qab zib muaj teeb meem ntau rau cov neeg laus neeg mob ntshav qab zib hom 2 thiab cov rog nyhav uas tau siv cov tshuaj metformin ua thawj cov tshuaj nrog rau kev kho cov zaub mov tsis muaj txiaj ntsig.
Yuav siv li cas: noj ntau thiab hom tshuaj kho
Sab hauv, lub sijhawm lossis tom qab noj mov tag, rau cov neeg mob tsis tau txais insulin, 1 g (2 ntsiav tshuaj) 2 zaug hauv ib hnub rau thawj 3 hnub lossis 500 mg 3 zaug hauv ib hnub, tom qab ntawd txij li 4 rau 14 hnub - 1 g 3 zaug hauv ib hnub, tom qab 15 hnub kev noj tshuaj tuaj yeem txo qis rau hauv tus account cov ntsiab lus ntawm cov piam thaj hauv cov ntshav thiab zis. Kev tu cov koob tshuaj txhua hnub - 1-2 g.
Cov ntsiav tshuaj rov qab (850 mg) tau noj 1 thaum sawv ntxov thiab yav tsaus ntuj. Qhov siab tshaj plaws niaj hnub noj yog 3 g.
Nrog rau kev siv tshuaj insulin ib txhij ntawm ib koob tsawg dua 40 units / hnub, kev noj tshuaj ntawm cov tshuaj metformin yog qhov qub, thaum lub koob tshuaj insulin tuaj yeem maj mam txo qis (los ntawm 4-8 units / hnub txhua lwm hnub). Thaum lub koob tshuaj insulin ntau dua 40 units / hnub, kev siv tshuaj metformin thiab txo qis ntawm cov tshuaj insulin yuav tsum muaj kev saib xyuas zoo thiab nqa tawm hauv tsev kho mob.
Pharmacological kev txiav txim
Biguanide, tus neeg sawv cev hypoglycemic rau kev tswj hwm ntawm qhov ncauj. Hauv cov neeg mob ntshav qab zib, nws txo cov ntsiab lus ntawm cov piam thaj hauv cov ntshav los ntawm inhibiting gluconeogenesis nyob rau hauv daim siab, txo qis kev nqus ntawm cov piam thaj los ntawm kev mob plab thiab nce nws siv nyob rau hauv cov ntaub so ntswg, Nws txo cov concentration ntawm TG, cov roj cholesterol thiab LDL (txiav txim siab ntawm lub plab tsis muaj dab tsi) hauv cov ntshav thiab tsis hloov lub siab ntawm lwm qhov lipoproteins ceev. Stabilizes lossis txo qhov hnyav lub cev.
Thaum tsis muaj cov tshuaj insulin nyob rau hauv cov ntshav, kev kho mob tsis pom tseeb. Kev ua kom lub cev ntshav qis tsis tuaj yeem ua. Txhim kho cov khoom fibrinolytic ntawm cov ntshav vim yog kev tsuj ntawm ib qho inhibitor ntawm tus activator profibrinolysin (plasminogen) cov ntaub so ntswg hom.
Sab sij huam
Los ntawm lub plab zom mov: xeev siab, ntuav, "nws yog xim hlau" saj hauv lub qhov ncauj, tsis qab los, ua tsis taus pa, tsis meej pem, mob plab.
Los ntawm ib sab ntawm cov metabolism: hauv qee kis - lactic acidosis (tsis muaj zog, myalgia, ua pa tsis meej, qaug zog, mob plab, hypothermia, txo cov ntshav siab, reflex bradyarrhythmia), nrog kev kho mob mus ntev - hypovitaminosis B12 (malabsorption).
Los ntawm cov kabmob hemopoietic: qee kis - megaloblastic anemia.
Kev ua xua rau: xoo pob khaus.
Yog tias muaj kev phiv, qhov tshuaj yuav tsum tau txo lossis txiav tawm ib ntus. Cov tsos mob: lactic acidosis.
Kev sib txuam
Txo Cmax thiab T1 / 2 ntawm furosemide los ntawm 31 thiab 42.3%, feem.
Tsis sib haum nrog ethanol (lactic acidosis).
Siv nrog ceev faj nyob rau hauv ua ke nrog indirect anticoagulants thiab cimetidine.
Cov khoom siv ntawm sulfonylureas, insulin, acarbose, MAO inhibitors, oxytetracycline, ACE inhibitors, clofibrate, cyclophosphamide thiab salicylates txhim kho cov nyhuv.
Nrog rau kev siv ua ke nrog GCS, tshuaj tiv thaiv kev tiv thaiv qog rau kev tswj hwm qhov ncauj, epinephrine, glucagon, cov thyroid hormones, phenothiazine derivatives, thiazide diuretics, nicotinic acid derivatives, txo qis hauv cov nyhuv hypoglycemic ntawm metformin yog ua tau.
Furosemide nce Cmax los ntawm 22%.
Nifedipine nce ntxiv kev nqus, Cmax, maj mam txo qis kev nthuav tawm.
Cov tshuaj Cationic (amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamteren thiab vancomycin) zais cia rau hauv cov tubules sib tw rau cov tshuab thauj tubular thiab tuaj yeem nce Cmax los ntawm 60% nrog kev kho mob ntev.