Jardins - nom * cov lus qhia rau siv

LUS QHIA
ntawm kev siv cov tshuaj
LOOJ CEEB

Daim ntawv tso tawm
zaj duab xis-ntsiav tshuaj ntsiav tshuaj

Muaj pes tsawg leeg
1 ntsiav tshuaj muaj:
cov tshuaj nquag: empagliflozin 10 thiab 25 mg
kev zam: lactose monohydrate, microcrystalline cellulose, hyprolose (hydroxypropyl cellulose), croscarmellose sodium, colloidal silicon dioxide, magnesium stearate.
zaj duab xis muaj pes tsawg leeg: opadry daj (02B38190) (hypromellose 2910, titanium dioxide (E171), talc, macrogol 400, daj hlau oxide zas (E172)).

Ntim
10 thiab 30 ntsiav tshuaj.

Pharmacological kev txiav txim
Jardins - Hom 2 Sodium Hlej Cov Hnav Cov Pauv Khoom Hloov Chaw

Jardins, kev qhia rau siv
Yam 2 Ntshav Qab Zib Hom:
raws li kev kho mob monotherapy hauv cov neeg mob uas tsis txaus glycemic tswj tsuas yog tiv thaiv tom qab ntawm kev noj haus thiab kev tawm dag zog, kev teem sijhawm tshuaj metformin uas pom tau tias tsis tsim nyog vim kev tsis txaus ntseeg,
raws li kev sib txuam nrog kev kho mob nrog lwm tus kab mob hypoglycemic, suav nrog cov tshuaj insulin, thaum kev siv tshuaj kho mob ua ke nrog kev noj haus thiab kev tawm dag zog tsis muab kev tswj hwm glycemic tsim nyog.

Cov Yuav Tsum Muaj
ua kom lub cev tsis haum rau ib qho tshuaj tiv thaiv,
ntshav qab zib hom 1
mob ketoacidosis,
muaj cov kab mob tsis muaj keeb txaus (lactase deficiency, lactose intolerance, glucose-galactose malabsorption),
lub raum tsis ua haujlwm nrog GFR ×

Daim ntawv noj tshuaj:

Kev piav qhia
10 mg ntsiav tshuaj
Muab cov ua ke ua ke nrog cov kab thawb npoo, npog nrog zaj duab xis ntawm lub teeb xim daj nrog lub ntsej muag sau ua lub tuam txhab cim ntawm ib sab ntawm lub ntsiav tshuaj thiab "S10" nyob rau sab nraud.
25 mg ntsiav tshuaj
Oval biconvex ntsiav tshuaj nrog cov ntug beveled, coated nrog zaj duab xis daim duab ntawm lub teeb xim daj, sau nrog lub tuam txhab cov cim ntawm ib sab ntawm lub ntsiav tshuaj thiab "S25" nyob rau sab nraud.

Cov chaw muag tshuaj

Cov Tshuaj Pharmacokinetics
Cov pharmacokinetics ntawm empagliflozin tau nkag siab ntau yam hauv cov neeg tuaj yeem noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2.
Xuas
Tom qab lub qhov ncauj tswj hwm, empagliflozin tau nrawm nrawm, qhov siab tshaj plaws ntawm empagliflozin hauv cov ntshav ntshav (Cmax) tau mus txog tom qab 1.5 teev. Tom qab ntawv, kev saib xyuas ntawm empagliflozin hauv ntshav txo qis hauv ob theem.
Tom qab tau txais empagliflozin, thaj tsam thaj tsam nruab nrab hauv qhov chaw siab-lub sijhawm nkhaus (AUC) thaum lub sijhawm khov kho hauv lub xeev ntshav yog 4740 nmol x h / l, thiab Cmax - 687 nmol / l.
Cov tshuaj pharmacokinetics ntawm empagliflozin hauv cov neeg tuaj yeem noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2 feem ntau zoo sib xws.
Noj mov tsis muaj kev cuam tshuam loj hauv tsev kho mob ntawm pharmacokinetics ntawm empagliflozin.
Kev xa Khoom
Qhov ntim ntawm kev faib tawm thaum lub sijhawm khov kho hauv lub xeev ntshav muaj li ntawm 73.8 litres. Tom qab qhov ncauj tswj hwm los ntawm kev noj qab haus huv tuaj pab dawb ntawm daim ntawv lo empagliflozin 14 C, ntshav protein ntshav khi yog 86%.
Kev zom zaub mov
Txoj hauv kev tseem ceeb ntawm empagliflozin metabolism hauv tib neeg yog glucuronidation nrog kev koom tes ntawm uridine-5'-diphospho-glucuronosyltransferases UGT2B7, UGT1A3, UGT1A8 thiab UGT1A9. Kev kuaj pom muaj ntau tshaj ntawm cov tshuaj empagliflozin yog peb glucuronic conjugates (2-0, 3-0 thiab 6-0 glucuronides). Cov haujlwm ua haujlwm ntawm txhua lub cev ntawm cov metabolite yog me me (tsawg dua 10% ntawm tag nrho cov nyhuv ntawm empagliflozin).
Chaw Sau Ntawv
Qhov kev tshem tawm ib nrab-lub neej yog kwv yees li 12.4 teev. Kev siv empagliflozin ib zaug ib hnub, ib qho ntshav plasma concentration tau mus txog tom qab koob thib tsib. Tom qab qhov ncauj tswj hwm ntawm daim ntawv lo empagliflozin 14 C hauv cov neeg ua haujlwm pab dawb noj qab haus huv, kwv yees li 96% ntawm cov koob tshuaj tau tawm (los ntawm txoj hnyuv 41% thiab lub raum 54%). Los ntawm txoj hnyuv, feem ntau ntawm cov ntawv lo ntawm cov tshuaj tsis txawv txav. Tsuas yog ib nrab ntawm cov tshuaj cim uas tau tso nrog tsis hloov pauv ntawm lub raum.
Pharmacokinetics hauv cov neeg mob tshwj xeeb
Lub raum khiav tsis zoo
Hauv cov neeg mob uas mob mentsis, nruab nrab, thiab mob raum tsis zoo (30 2) thiab hauv cov neeg mob uas mob raum tsis ua haujlwm, AUC ntawm empagliflozin tau nce, feem ntau, kwv yees li 18%, 20%, 66%, thiab 48% piv nrog cov neeg mob uas ib txwm muaj raum muaj nuj nqi. Hauv cov neeg mob uas muaj mob raum tsawg thiab cov neeg mob uas mob raum lub raum tsis ua haujlwm, qhov ntau tshaj plaws ntawm lub ntsej muag ntshav ntawm empagliflozin zoo ib yam li cov nuj nqis sib luag hauv cov neeg mob uas lub raum muaj nuj nqi. Hauv cov neeg mob uas mob raum me thiab mob raum tsis ua haujlwm, qhov siab tshaj plaws ntshav ntshav ntawm empagliflozin yog kwv yees li 20% ntau dua ntawm cov neeg mob uas lub raum tsis ua haujlwm. Cov pejxeem pharmacokinetic tsom xam cov ntaub ntawv qhia tias tag nrho kev ua kom tsis txhob muaj cov tshuaj empagliflozin nrog GFR txo qis, uas ua rau muaj qhov nce ntxiv ntawm cov nyhuv ntawm cov tshuaj.
Lub siab ua haujlwm tsis zoo
Hauv cov neeg mob uas muaj lub siab ua haujlwm tsis txaus siab ntawm qhov mob me, nruab nrab thiab mob hnyav (raws li cov menyuam-Pugh kev faib tawm), AUC qhov tseem ceeb ntawm empagliflozin nce, ntsig txog, kwv yees li 23%, 47% thiab 75%, thiab Stax cov nuj nqis, feem ntau, los ntawm kwv yees li 4%, 23 % thiab 48% (piv nrog rau cov neeg mob lub siab ua haujlwm).
Lub cev nyhav taw qhia, poj niam txiv neej, haiv neeg thiab hnub nyoog tsis muaj kev cuam tshuam loj hauv kev kho mob rau lub chaw muag tshuaj ntawm cov tshuaj empagliflozin.
Cov menyuam
Kev tshawb fawb ntawm cov tshuaj pharmacokinetics ntawm empagliflozin hauv cov menyuam yaus tsis tau ua.

Cov Yuav Tsum Muaj

• Hypersensitivity rau ib feem twg ntawm cov tshuaj,
• Yam 1 ntshav qab zib
• Ntshav qab zib ketoacidosis
• Tsis tshua muaj cov kab mob muaj keeb (cov lactase deficiency, lactose intolerance, glucose-galactose malabsorption),
• Cov hlaws tsis ua hauj lwm hauv GFR 2 (vim tsis muaj txiaj ntsig),
• Cev xeeb tub thiab lactation,
• Muaj hnub nyoog tshaj 85 xyoo
• Kev siv nyob rau hauv kev sib xyaw nrog cov khoom sib piv ntawm glucagon-zoo li peptide 1 (vim tias tsis muaj cov ntaub ntawv ntawm kev ua tau zoo thiab kev nyab xeeb),
• Cov me nyuam qis dua 18 xyoo (vim tsis muaj ntaub ntawv hais txog kev ua tau zoo thiab kev nyab xeeb).

Sab sij huam
Tag nrho qhov tshwm sim ntawm qhov tshwm sim tsis zoo hauv cov neeg mob uas tau txais empagliflozin lossis cov placebo hauv kev sim kho mob tau zoo ib yam. Feem ntau cov kev phiv tshuaj yog hypoglycemia, uas tau pom nrog kev siv cov tshuaj empagliflozin sib xyaw nrog sulfonylurea lossis insulin derivatives (saib cov lus piav qhia ntawm tus neeg muaj kev tsis zoo).
Cov kev tsis zoo tshwm sim hauv cov neeg mob tau txais empagliflozin nyob rau hauv cov kev soj ntsuam cov tshuaj placebo tau nthuav tawm hauv cov lus hauv qab no (cov kev phiv tshuaj tau muab cais raws li cov plab hnyuv siab raum thiab cov tshuab thiab raws li cov lus uas nyiam los ntawm MedDRA) nrog qhov qhia txog ntawm lawv cov zaus. Cov qeb uas nquag tau txhais raws li hauv qab no: nquag heev (> 1/10), nquag (ntawm>, 1/100 txog> 1/1000 txog> 1/10000 Kev piav qhia ntawm cov neeg muaj kev phiv tshuaj
Kev ntshav siab
Qhov tshwm sim ntawm kev mob ntshav qab zib yog nce mus rau kev kho tus mob ntshav qab zib tsawg dua.
Cov ntshav qog ntshav qab zib me me (ntshav qabzib 3.0 - 3.8 mmol / L (54-70 mg / dl)) Qhov tshwm sim ntawm cov ntshav qog ntshav me ntsis tau zoo ib yam li cov neeg mob noj empagliflozin lossis placebo li monotherapy, zoo ib yam li ntxiv empagliflozin rau metformin thiab Xws li kev ntxiv ntawm empagliflozin rau pioglitazone (± metformin). Thaum empagliflozin tau muab nrog kev sib xyaw nrog metformin thiab sulfonylurea derivatives, qhov tshwm sim ntawm cov ntshav qog ntshav siab dua (10 mg: 10.3%, 25 mg: 7.4%) dua li nrog cov tshuaj placebo hauv qhov sib xyaw ua ke (5.3%).
Mob ntshav qab zib heev (ntshav qab zib hauv qab 3 mmol / L (54 mg / dL))
Qhov xwm txheej ntawm cov ntshav qog ntshav ntshav yog qhov zoo sib xws hauv cov neeg mob noj empagliflozin thiab cov placebo raws li kev kho mob monotherapy. Thaum empagliflozin tau muab nrog kev sib xyaw nrog metformin thiab sulfonylurea derivatives, qhov tshwm sim ntawm cov ntshav qog ntshav siab dua (10 mg: 5.8%, 25 mg: 4.1%) dua li nrog cov placebo hauv kev sib xyaw ua ke (3.1%).
Kev ceev ceev tso zis
Qhov nquag ntawm kev tso zis (cov tsos mob xws li pollakiuria, polyuria, nocturia tau ntsuas) yog ntau dua nrog empagliflozin (ntawm koob tshuaj 10 mg: 3.4%, ntawm koob tshuaj 25 mg: 3.2%) dua li nrog placebo (1 %). Qhov tshwm sim ntawm nocturia yog piv rau hauv pab pawg ntawm cov neeg mob noj empagliflozin thiab hauv pawg ntawm cov neeg mob noj cov placebo (tsawg dua 1%). Cov kev siv ntawm cov kev mob tshwm sim no yog mob sib khuav los yog mob pesnrab.
Mob txeeb zig
Qhov tshwm sim ntawm cov mob txeeb zig yog qhov zoo sib xws nrog empagliflozin 25 mg thiab placebo (7.6%), tab sis ntau dua nrog empagliflozin 10 mg (9.3%). Ib yam li cov placebo, cov mob txeeb zig muaj nrog empagliflozin muaj ntau dua rau cov neeg mob uas muaj keeb kwm ua mob mus ntev thiab rov ua mob txeeb zig. Qhov tshwm sim ntawm cov mob txeeb zig yog qhov zoo sib xws hauv cov neeg mob noj empagliflozin thiab cov placebo. Mob txeeb zig muaj ntau tus poj niam.
Chaw mos kis tau tus mob
Kev tshwm sim ntawm qhov tshwm sim tsis zoo xws li mob txeeb tau ntawm qhov chaw mos, mob vulvovaginitis, balanitis thiab lwm yam mob ntawm qhov chaw mos tau siab dua nrog empagliflozin (ntawm koob tshuaj 10 mg: 4.1%, ntawm koob tshuaj 25 mg: 3.7%) dua li nrog placebo (0 , 9%). Chaw mos muaj tshwm sim rau cov poj niam. Cov kev siv ntawm kev kis mob ntawm qhov chaw mos yog mob sib khuav lossis ntsis.
Kev Hypovolemia
Qhov tshwm sim ntawm hypovolemia (uas tau tshwm sim los ntawm kev txo ntshav siab, orthostatic arterial hypotension, lub cev qhuav dej, tsaus muag) yog qhov zoo sib xws ntawm empagliflozin (ntawm koob tshuaj 10 mg: 0.5%. Hauv koob ntawm 25 mg: 0.3%) thiab cov placebo (0, 3%). Hauv cov neeg mob uas laus dua 75 xyoo, qhov kev tshwm sim ntawm hypovolemia piv rau cov neeg mob noj empagliflozin ntawm koob tshuaj 10 mg (2.3%) thiab cov placebo (2.1%), tab sis ntau dua rau cov neeg mob noj empagliflozin ntawm koob tshuaj 25 mg (4.4%) )

Noj ntau dhau

Kev cuam tshuam nrog lwm yam tshuaj
Hauv tshuaj ntsuam xyuas tshuaj vitro
Empagliflozin tsis inhibit, inactivate, lossis ntxias CYP450 isoenzymes. Txoj hauv kev tseem ceeb ntawm tib neeg cov khoom noj khoom haus metabolism yog glucuronidation nrog kev koom tes ntawm uridine-5'-diphospho-glucuronosyltransferases UGT2B7, UGT1A3, UGT1A8 thiab UGT1A9. Empagliflozin tsis inhibit UGT1A1. Kev sib cuam tshuam yeeb tshuaj ntawm cov tshuaj empagliflozin thiab cov tshuaj uas yog cov me me ntawm CYP450 thiab UGT1A1 isoenzymes yog suav tias yog qhov tsis zoo.
Empagliflozin yog ib qho tshuaj tiv thaiv kab mob glycoprotein P (P-gp) thiab cov qog mis tiv thaiv mob cancer mis (BCRP). tab sis hauv kev kho mob tsis haum cov protein. Raws li cov ntaub ntawv los ntawm kev tshawb fawb hauv vitro, nws ntseeg tau tias kev muaj peev xwm ntawm empagliflozin cuam tshuam nrog cov tshuaj uas yog cov kab mob rau me me glycoprotein P (P-gp) tsis zoo li. Empagliflozin yog cov txheej txheem rau cov organic anionic nqa khoom: OATZ, OATP1B1 thiab OATP1VZ, tab sis tsis muaj txheej txheem rau cov organic anionic nqa khoom 1 (OAT1) thiab organic cationic carriers 2 (OST2). Txawm li cas los xij, kev sib cuam tshuam txog yeeb tshuaj ntawm empagliflozin nrog cov tshuaj uas yog cov substrates rau cov cab kuj muaj cov roj ntsha tau piav qhia saum toj yog suav tias tsis zoo li.
Hauv vivo tshuaj ntsuam kev sib cuam tshuam
Cov chaw muag tshuaj ntawm empagliflozin tsis hloov pauv rau cov neeg tuaj yeem noj qab haus huv thaum siv ua ke nrog metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, torasemide thiab hydrochlorothiazide. Kev sib xyaw ntawm kev siv empagliflozin nrog gemfibrozil, rifampicin thiab probenecid pom tias muaj kev nce ntxiv ntawm AUC ntawm empagliflozin los ntawm 59%, 35% thiab 53%, feem ntau, tab sis cov kev hloov no tsis tau pom tias yog kev kho mob tseem ceeb.
Empagliflozin tsis muaj kev cuam tshuam los ntawm kev mob loj rau lub pharmacokinetics ntawm metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin. digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide thiab qhov ncauj tshuaj tiv thaiv.
Kev tshuaj ntsuab
Empagliflozin tuaj yeem txhim kho lub diuretic nyhuv ntawm thiazide thiab "voj" diuretics, uas nyob rau hauv lem yuav ua rau muaj kev pheej hmoo ntawm lub cev qhuav dej thiab cov hlab ntsha hypotension.
Cov tshuaj insulin thiab tshuaj uas txhim kho nws qhov kev zais cia
Cov tshuaj Insulin thiab cov tshuaj uas pab txhawb nws txoj kev zais, xws li sulfonylureas, tuaj yeem ua rau muaj kev pheej hmoo ntawm hypoglycemia. Yog li no, nrog rau kev siv empagliflozin sib xyaw nrog insulin thiab tshuaj uas txhim kho nws qhov kev tso cia, nws yuav tsim nyog txo lawv cov koob tshuaj, txhawm rau kom tsis txhob muaj kev pheej hmoo ntawm hypoglycemia.

Cov lus qhia tshwj xeeb

Muaj feem xyuam rau kev muaj peev xwm tsav tsheb thiab cov txheej txheem
Cov kev tshawb fawb soj ntsuam ntawm cov txiaj ntsig ntawm empagliflozin ntawm kev muaj peev xwm tsav tsheb thiab lub tswv yim tsis tau ua. Cov neeg mob yuav tsum tau ceev faj thaum tsav tsheb thiab cov txheej txheem, txij li thaum siv tshuaj JARDINS (tshwj xeeb tshaj yog ua ke nrog sulfonylurea derivatives thiab / lossis insulin), hypoglycemia tuaj yeem tsim kho.

Chaw tsim tshuaj paus

Lub npe thiab chaw nyob ntawm qhov chaw tsim khoom ntawm cov khoom lag luam tshuaj
Beringer Ingelheim Pharma GmbH & Co.KG
Binger Strasse 173, 55216 Ingelheim am Rhein, Lub Tebchaws Yelemees

Koj tuaj yeem tau txais cov ntaub ntawv ntxiv ntsig txog cov tshuaj, nrog rau xa koj cov kev tsis txaus siab thiab cov ntaub ntawv ntsig txog cov xwm txheej tsis zoo mus rau qhov chaw nyob hauv Russia hauv qab no
LLC Beringer Ingelheim
125171. Moscow, Leningradskoye Shosse, 16A p. 3

Jardins tshuaj ntsuab

Cov no yog cov ua yeeb yaj kiab-coated ntsiav tshuaj. Tsos: lub teeb daj, oval lossis puag ncig (nyob ntawm seb ntau npaum li cas), tsim qauv - biconvex ntsiav tshuaj nrog beveled sawv thiab engraved cov cim ntawm cov khw ntawm ib sab. Ib cov tshuaj tsim hauv lub tebchaws Ntsaws Mes Kas los txo cov ntshav ntshav hauv ntshav qab zib hom 2.

Qhov ncauj tshuaj hypoglycemic, nrog rau cov tshuaj nquag - empagliflozin. Cov ncauj lus kom ntxaws thiab ntau npaum li cas muaj nyob hauv cov lus:

Koob tshuaj 1 ntsiav tshuaj (mg)

opadray daj (hypromellose, titanium dioxide, talc, macrogol, hlau zas hlau oxide daj)

Pharmacological kev txiav txim

Empagliflozin yog qhov thim rov qab, ua haujlwm nquag, xaiv cov tshuaj tiv thaiv ntawm hom 2 sodium-dependent glucose transporter. Nws tau dhau los ntawm kev tshawb fawb tau hais tias empagliflozin tau xaiv siab heev rau lwm tus neeg coj ua lub luag haujlwm rau kua nplaum homeostasis hauv cov nqaij hauv lub cev. Cov tshuaj muaj cov txiaj ntsig glycemic hauv cov neeg mob uas muaj ntshav qab zib hom 2 los ntawm kev txo qhov nqus ntawm cov piam thaj hauv ob lub raum. Qhov ntau npaum li cas ntawm cov piam thaj tso tawm los ntawm qhov tshuab no ncaj qha nyob ntawm tus nqi ntawm kev ua haujlwm ntawm cov glomeruli ntawm ob lub raum.

Cov kev tshawb fawb pom tau tias hauv cov neeg mob uas muaj ntshav qab zib hom 2, cov ntshav qabzib ntau ntxiv tom qab thawj zaug noj thawj zaug thiab cov nyhuv ntev li ib hnub. Cov ntsuas no tseem tshuav thaum noj 25 mg ntawm empagliflozin rau ib hlis. Kev nce ntxiv ntawm cov ntshav qab zib los ntawm ob lub raum ua rau nws qhov kev txo qis hauv nws cov ntshav hauv tus neeg mob. Cov tshuaj txo cov concentration ntawm cov piam thaj hauv cov ntshav, tsis hais txog ntawm cov zaub mov noj.

Ib qho tshuaj insulin-ywj pheej txo qhov kev pheej hmoo ntawm kev mob ntshav qab zib.Lub tshuab ntawm kev ua ntawm cov tshuaj nquag tsis yog nyob ntawm kev ua haujlwm ntawm cov islets ntawm Langerhans thiab insulin metabolism. Cov kws tshawb fawb hais txog qhov zoo ntawm empagliflozin rau surrogate peptides ntawm kev ua haujlwm ntawm cov hlwb no. Kev nce ntxiv ntawm cov piam thaj ua rau cov calories poob, uas ua rau lub cev hnyav dua. Thaum lub sij hawm siv ntawm empagliflozin, glucosuria yog pom.

Kev ntsuas rau siv

Nws yog qhia rau cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus ntawm kev noj zaub mov nruj thiab ua kis las, uas nws tsis tuaj yeem tswj tau cov cim glycemic. Nrog Metformin intolerance, monotherapy nrog Jardins yog ua tau. Yog tias kev kho kom tsis muaj cov txiaj ntsig tsim nyog, ua ke siv nrog lwm cov tshuaj hypoglycemic, suav nrog insulin, ua tau.

Cov Lus Qhia Jardins

Cov ntsiav tshuaj tau noj ntawm qhov ncauj, tsis hais lub sijhawm nruab hnub lossis kev noj haus. Nws raug nquahu kom pib noj nrog 10 mg rau ib hnub, yog tias cov txiaj ntsig kom raug tsis tshwm sim, ces nce ntxiv rau 25 mg. Yog tias vim qee qhov laj thawj lawv tsis tau siv tshuaj, koj yuav tsum haus nws tam sim ntawd, raws li lawv nco qab. Muab ob npaug rau nyiaj tsis tuaj yeem noj. Yog tias lub plab tsis ua haujlwm, tsis kho, thiab cov neeg mob raum tsis tso cai.

Thaum cev xeeb tub

Kev siv cov ntsiav tshuaj thaum cev xeeb tub yog contraindicated vim tsis muaj cov ntaub ntawv los ntawm kev kawm txog kev ua tau zoo thiab kev nyab xeeb. Cov kev tshawb fawb tsiaj ua ntej pom tau hais tias muaj peev xwm ua kom muaj kev zais ntshis ntawm cov leeg ntshav hauv plab. Txoj kev pheej hmoo ntawm kis tau tus me nyuam hauv plab thiab cov menyuam yug tshiab tsis suav nrog. Yog tias tsim nyog, koj yuav tsum tsis txhob noj cov tshuaj thaum cev xeeb tub.

Hauv thaum yau

Kev kho nrog cov tshuaj hauv cov menyuam yaus thiab cov tub ntxhais hluas hnub nyoog qis dua 18 xyoo yog txwv tsis pub muaj. Sib txuam nrog cov ntaub ntawv tshawb fawb tsis txaus. Qhov ua tau zoo thiab kev nyab xeeb ntawm cov tshuaj ua kom yuag empagliflozin rau cov menyuam yaus tsis tau raug pov thawj. Txhawm rau tshem tawm cov kev pheej hmoo ntawm kev ua mob rau menyuam txoj kev noj qab haus huv, Jardins yog txwv tsis pub. Zoo dua los xaiv lwm cov tshuaj muaj ntawv pov thawj.

3D duab

Kev piav qhia ntawm daim ntawv tshuaj

10 mg ntsiav tshuaj: puag ncig biconvex nrog beveled sawv, them nrog zaj duab xis daim duab ntawm lub teeb daj xim, nrog lub lag luam ntawm lub tuam txhab cim ntawm ib sab thiab "S10" nyob rau sab nraud.

25 mg ntsiav tshuaj: oval biconvex nrog beveled npoo, them nrog zaj duab xis ntawm lub teeb xim daj, sau nrog lub tuam txhab cov cim ntawm ib sab thiab "S25" nyob rau sab nraud.

Cov Tshuaj Hauv Tshuaj

Empagliflozin yog qhov thim rov qab nquag xaiv tau thiab muaj kev sib tw inhibitor ntawm hom 2 sodium-dependant glucose transporter nrog qhov xav tau yuav tsum tau inhibit 50% ntawm qhov kev ua enzyme (IC₅₀), sib npaug rau 1.3 nmol. Qhov xaiv kom tau ntawm empagliflozin yog 5,000 npaug ntau dua qhov xaiv ntawm hom 1 sodium-dependant transporter, uas yog lub luag haujlwm rau kev nqus ntawm cov piam thaj hauv txoj hnyuv. Tsis tas li ntawd, nws tau pom tias empagliflozin muaj qhov siab xaiv rau lwm cov neeg thauj khoom qabzib lub luag haujlwm rau cov piam thaj homeostasis hauv cov nqaij ntau yam.

Sodium-dependent glucose transporter type 2 yog qhov tseem ceeb tshaj tawm cov protein vim lub luag hauj lwm rau reabsorption ntawm qabzib los ntawm lub raum glomeruli rov qab rau hauv cov ntshav. Empagliflozin txhim kho glycemic tswj nyob rau hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus (T2DM) los ntawm kev txo cov ntshav qabzib reabsorption. Tus nqi ntawm cov piam thaj zais tawm los ntawm ob lub raum siv lub tshuab no nyob ntawm kev saib xyuas cov piam thaj hauv cov ntshav thiab GFR. Kev txwv tsis pub cov tshuaj sodium sodium dependant transporter type 2 hauv cov neeg mob uas muaj ntshav qab zib hom 2 thiab hyperglycemia ua rau kev tshem tawm cov piam thaj ntau dhau los ntawm lub raum.

Hauv kev tshawb nrhiav 4 lub lim tiam, nws tau pom tias hauv cov neeg mob uas muaj ntshav qab zib hom 2, raum qabzib cov zis tau nce ntxiv tom qab siv thawj zaug ntawm empagliflozin tau siv, cov nyhuv no txuas ntxiv mus 24 teev. ib koob tshuaj 25 mg 1 zaug hauv ib hnub, qhov nruab nrab kwv yees li 78 g / hnub. Hauv cov neeg mob uas muaj ntshav qab zib hom 2, ib qho kev nce ntxiv ntawm cov kua nplaum los ntawm ob lub raum ua rau muaj kev cuam tshuam sai li sai tau ntawm cov ntshav qabzib hauv cov ntshav ntshav.

Empagliflozin (ntawm ib koob ntawm 10 thiab 25 mg) txo cov concentration ntawm cov piam thaj hauv ntshav ntshav ob leeg ntawm kev yoo mov thiab tom qab noj mov.

Lub tshuab ntawm kev ua ntawm empagliflozin tsis yog nyob ntawm lub xeev kev ua haujlwm ntawm pancreatic beta hlwb thiab cov tshuaj insulin metabolism, uas ua rau muaj kev pheej hmoo tsawg ntawm kev txhim kho hypoglycemia. Cov txiaj ntsig zoo ntawm empagliflozin rau kev ntsuas mob siab ntawm beta cell muaj nuj nqi, suav nrog HOMA-β index (qauv rau kev ntsuam xyuas homeostasis-B) thiab piv ntawm proinsulin rau insulin, tau sau tseg. Tsis tas li ntawd, ntxiv kev tshem tawm cov piam thaj los ntawm ob lub raum ua rau poob phaus, uas yog nrog cov suab nrov me me hauv lub cev txo thiab qhov hnyav hauv lub cev.

Glucosuria tau pom thaum siv empagliflozin yog nrog los ntawm diuresis me ntsis, uas tuaj yeem ua rau txo qis hauv cov ntshav siab.

Hauv cov kev tshawb fawb soj ntsuam qhov twg empagliflozin tau siv nyob rau hauv kev kho mob monotherapy, kev sib txuas ua ke nrog metformin, kev sib txuas ua ke nrog metformin hauv cov neeg mob uas nyuam qhuav muaj ntshav qab zib tshiab 2, kev sib txuas nrog kev kho mob nrog metformin thiab sulfonylurea derivatives, kev sib txuas nrog kev kho nrog pioglitazone +/− metformin, kev sib txuas nrog kev kho nrog linagliptin hauv cov neeg mob uas nyuam qhuav soj ntsuam mob ntshav qab zib mellitus 2, kev sib xyaw ua ke nrog linagliptin, ntxiv rau metformin kev kho mob, kev sib txuas ua ke nrog linagliptin hauv kev sib piv nrog paracet o nyob rau hauv cov neeg mob uas tsis muaj kev tswj glycemic thaum noj cov tshuaj linagliptin thiab metformin, kev sib xyaw ua ke nrog metformin tiv thaiv glimepiride (cov ntaub ntawv los ntawm kev tshawb fawb 2-xyoo), kev sib xyaw nrog kev kho mob nrog insulin (ntau txoj kev txhaj tshuaj insulin) +/− metformin, kev sib txuas ua ke nrog kev siv tshuaj insulin basal , kev sib txuas ua ke nrog DPP-4 inhibitor, metformin +/ − lwm qhov kev tiv thaiv qhov ncauj qhov ntswg ntshav, qhov kev txo qis hauv HbA1 tau pom tseeb_c, qhov txo qis hauv kev yoo plasma ntshav qab zib ntau ntau, nrog rau kev txo ntshav siab thiab lub cev qhov hnyav.

Kev soj ntsuam tshawb xyuas qhov tshwm sim ntawm cov tshuaj Jardins ® rau ntawm lub sijhawm ntawm kev mob plawv hauv cov neeg mob ntshav qab zib hom 2 thiab mob ntshav siab (txhais tau tias muaj tsawg kawg ib ntawm cov kab mob hauv qab no thiab / lossis cov mob: mob rau cov hlab ntsha hlab ntsha (keeb kwm myocardial infarction, mob ntshav hlab plawv los ntawm kev sib tsoo)) , IHD nrog kev puas tsuaj rau ib lub hlab ntshav, IHD nrog kev puas tsuaj rau ntau txoj hlab ntsha), keeb kwm ntawm ischemic lossis hemorrhagic mob stroke, mob hlab ntsha hlwb nrog lossis tsis muaj tsos mob) tau txais tus qauv hydrochloric txoj kev kho, uas muaj hypoglycemic neeg thiab cov neeg ua hauj rau cov kev kho mob ntawm cov hlab plawv tus kab mob. Cov mob ntawm cov hlab plawv tuag, tsis mob nqaij ntshav ntshav myocardial infarction thiab mob ntshav tsis tuag yog raug ntsuas raws li thawj qhov kawg. Kev tuag plawv, kev tuag rau neeg tuag, kev txhim kho ntawm nephropathy lossis kev txhawj xeeb zuj zus ntxiv ntawm nephropathy, thiab pw hauv tsev kho mob rau lub plawv tsis ua haujlwm tau raug xaiv raws li kev xav ua ntej ntxiv.

Empagliflozin tau txhim kho kev muaj sia nyob tag nrho los ntawm kev txo cov neeg mob plawv. Empagliflozin txo qis kev pheej hmoo mus pw hauv tsev kho mob rau lub plawv tsis ua haujlwm. Tsis tas li ntawd, hauv kev tshawb nrhiav, nws tau pom tias cov tshuaj Jardins ® txo qis kev pheej hmoo ntawm nephropathy lossis nce zuj zus ntawm kev mob qog nqaij hlav nephropathy.

Hauv cov neeg mob uas pib mob macroalbuminuria, nws tau pom tias Jardins ® cov tshuaj ntau dua piv rau cov placebo uas ua rau muaj kev tiv thaiv kev nyab xeeb - lossis microalbuminuria (qhov pheej hmoo sib piv 1.82, 95% CI: 1.4-2.37).

Cov Tshuaj Pharmacokinetics

Cov pharmacokinetics ntawm empagliflozin tau nkag siab ntau ntxiv hauv cov neeg tuaj yeem noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2.

Xuas. Empagliflozin tom qab kev tswj hwm qhov ncauj tau nrawm nrawm, C_max empagliflozin nyob rau hauv cov ntshav tau mus txog tom qab 1.5 teev. Tom qab ntawd, cov ntsiab lus ntawm empagliflozin hauv ntshav txo qis hauv ob theem. Tom qab noj cov tshuaj empagliflozin ntawm koob tshuaj 25 mg ib hnub ib zaug, qhov nruab nrab AUC hauv lub sijhawm C_ss hauv plasma yog 4740 nmol · h / l, thiab tus nqi ntawm C_max - 687 nmol / L.

Cov pharmacokinetics ntawm empagliflozin hauv cov neeg tuaj yeem noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2 feem ntau zoo sib xws.

Noj mov tsis muaj kev cuam tshuam loj hauv tsev kho mob ntawm pharmacokinetics ntawm empagliflozin.

Kev xa Khoom. V_d thaum lub sijhawm ntshav C_ss yog kwv yees li 73,8 litres. Tom qab lub qhov ncauj tswj hwm los ntawm kev noj qab haus huv tuaj pab dawb ntawm daim ntawv lo empagliflozin 14 C, ntshav protein ntshav khi yog 86.2%.

Kev zom zaub mov. Txoj hauv kev tseem ceeb ntawm empagliflozin metabolism hauv tib neeg yog glucuronidation nrog kev koom tes ntawm UDP-GT (UGT2B7, UGT1A3, UGT1A8 thiab UGT1A9). Kev tshuaj xyuas feem ntau ntawm cov tshuaj metabolite ntawm empagliflozin yog 3 glucuronic conjugates (2-O, 3-O thiab 6-O glucuronide). Cov haujlwm ua haujlwm ntawm txhua lub cev ntawm cov metabolite yog me me (tsawg dua 10% ntawm tag nrho cov nyhuv ntawm empagliflozin).

Chaw Sau Ntawv. T_1/2 tau kwv yees li 12.4 teev. Nyob rau hauv rooj plaub ntawm kev siv empagliflozin 1 zaug hauv ib hnub C_ss nyob rau hauv ntshav tau tiav tom qab koob thib tsib. Tom qab qhov ncauj tswj hwm ntawm daim ntawv lo empagliflozin 14 C hauv cov neeg ua haujlwm pab dawb noj qab haus huv, kwv yees li 96% ntawm cov koob tshuaj tau tawm (los ntawm txoj hnyuv 41% thiab lub raum 54%).

Los ntawm txoj hnyuv, feem ntau ntawm cov ntawv lo ntawm cov tshuaj tsis txawv txav. Tsuas yog ib nrab ntawm cov tshuaj cim uas tau tso nrog tsis hloov pauv ntawm lub raum.

Pharmacokinetics hauv cov neeg mob tshwj xeeb

Lub raum khiav tsis zoo. Hauv cov neeg mob uas mob mentsis (60 2), mob hnyav (30 2), mob hnyav (GFR 2) lub raum tsis ua haujlwm, thiab cov neeg mob raum tsis ua haujlwm, cov AUC ntawm empagliflozin tau nce ntxiv kwv yees li 18, 20, 66, thiab 48%, piv, piv nrog cov neeg mob nrog coj raum zoo li cas. Hauv cov neeg mob uas mob raum tsis ua haujlwm thiab cov neeg mob raum lub raum tsis ua haujlwm C_max empagliflozin nyob rau hauv ntshav muaj qhov zoo sib xws rau yam tseem ceeb hauv cov neeg mob uas lub raum muaj nuj nqi. Hauv cov neeg mob uas mob mentsis mus rau lub raum tsis ua haujlwm lawm_max empagliflozin nyob rau hauv cov ntshav ntshav yog kwv yees li 20% siab dua ntawm cov neeg mob uas lub raum tsis ua haujlwm. Cov pejxeem pharmacokinetic tsom xam cov ntaub ntawv qhia tias tag nrho kev ua kom tsis txhob muaj cov tshuaj empagliflozin nrog GFR txo qis, uas ua rau muaj qhov nce ntxiv ntawm cov nyhuv ntawm cov tshuaj.

Lub siab ua haujlwm tsis zoo. Hauv cov neeg mob uas muaj lub siab tsis ua haujlwm ntawm lub cev me me, nruab nrab thiab hnyav (raws li kev faib tawm Tus Menyuam-Pugh), AUC qhov tseem ceeb ntawm empagliflozin nce ntxiv kwv yees li 23, 47 thiab 75%, thiab_max los ntawm kwv yees li 4, 23 thiab 48%, feem (piv nrog rau cov neeg mob uas lub siab ua haujlwm).

BMI, poj niam txiv neej, haiv neeg, thiab lub hnub nyoog tsis muaj kev cuam tshuam loj hauv lub chaw muag tshuaj ntawm empagliflozin.

Cov menyuam. Kev tshawb fawb ntawm cov tshuaj pharmacokinetics ntawm empagliflozin hauv cov menyuam yaus tsis tau ua.

Kev taw qhia ntawm cov tshuaj Jardins ®

Yam 2 Ntshav Qab Zib Hom:

- raws li kev kho mob monotherapy hauv cov neeg mob uas tsis txaus glycemic tswj tsuas yog tiv thaiv tom qab ntawm kev noj haus thiab kev tawm dag zog, kev teem sijhawm tshuaj metformin uas tsis yooj yim sua vim tsis nco qab,

- raws li kev sib txuam nrog kev kho mob nrog lwm tus kab mob hypoglycemic, suav nrog cov tshuaj insulin, thaum cov tshuaj thov siv ua ke nrog kev noj haus thiab kev tawm dag zog tsis muab cov kev tswj glycemic tsim nyog.

Nws yog qhia rau cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus thiab kev muaj kab mob plawv ntau dua * ua ke nrog cov qauv kev kho mob rau cov mob plawv txhawm rau txo:

- tag nrho cov kev ploj tuag los ntawm kev txo cov kab mob plawv,

- kev mob plawv tuag lossis tsev kho mob rau lub plawv tsis ua haujlwm.

* Kev mob ntshav siab yog txhais tias muaj tsawg kawg ib ntawm cov kab mob hauv qab no thiab / lossis cov mob: mob plawv rau lub plawv (keeb kwm ntawm myocardial infarction, mob hlab ntsha o hla kev phais, mob hlab ntsha nrog rau kev puas tsuaj rau ib lub hlab ntshav hlab ntshav, cov hlab ntsha hlab ntsha nrog rau kev puas tsuaj rau ntau txoj hlab ntshav hlab ntsha) keeb kwm ntawm kab mob txha caj qaum (nrog lossis tsis muaj tsos mob).

Cev xeeb tub thiab lactation

Kev siv cov tshuaj empagliflozin thaum cev xeeb tub yog contraindicated vim cov ntaub ntawv tsis txaus ntawm kev ua tau zoo thiab kev nyab xeeb.

Cov ntaub ntawv tau hauv cov kev tshawb fawb hauv preclinical hauv cov tsiaj qhia txog kev nkag mus ntawm empagliflozin rau hauv cov kua mis. Txoj kev pheej hmoo ntawm kis tau tus me nyuam tshiab thiab menyuam thaum lub sijhawm pub niam mis tsis suav nrog. Kev siv cov tshuaj empagliflozin thaum lub sijhawm pub mis niam yog contraindicated. Yog tias tsim nyog, yuav tsum tsis txhob siv cov tshuaj empagliflozin thaum pub niam mis rau menyuam noj.

Sab sij huam

Tag nrho qhov tshwm sim ntawm qhov tshwm sim tsis zoo hauv cov neeg mob uas tau txais empagliflozin lossis cov placebo hauv kev sim kho mob tau zoo ib yam. Feem ntau cov kev phiv tshuaj yog hypoglycemia, pom nrog kev siv cov tshuaj empagliflozin txuam nrog sulfonylurea derivatives los yog insulin (saib Kev piav qhia ntawm kev xaiv phiv tshuaj).

Cov kev phiv tshuaj pom nyob rau hauv cov neeg mob uas tau txais empagliflozin hauv cov kev tshawb fawb tshuaj placebo yog qhia hauv qab no hauv (cov kev tsis haum tau raug cais raws li cov plab hnyuv siab raum thiab cov tshuab thiab raws li nyiam MedDRA cov lus uas) taw qhia lawv qhov ntau zaus. Ntau pawg tau txhais raws li hauv qab no: feem ntau (/1 / 10), feem ntau (los ntawm ≥1 / 100 rau ntshav siab, orthostatic arterial hypotension, lub cev qhuav dej, tsaus muag) yog qhov zoo sib xws ntawm empagliflozin (ntawm koob tshuaj 10 mg - 0.6%, ntawm ib koob ntawm 25 mg - 0.4%) thiab cov placebo (0.3%). Hauv cov neeg mob uas laus dua 75 xyoo, qhov kev tshwm sim ntawm hypovolemia piv rau cov neeg mob noj empagliflozin ntawm koob tshuaj 10 mg (2.3%) thiab cov placebo (2.1%), tab sis ntau dua rau cov neeg mob noj empagliflozin ntawm koob tshuaj 25 mg (4.3%) )

Kev sib txuam

Kev tshuaj ntsuab. Empagliflozin tuaj yeem txhim kho lub diuretic nyhuv ntawm thiazide thiab lub voj diuretics, uas, nyeg, yuav ua rau muaj kev pheej hmoo ntawm lub cev qhuav dej thiab cov hlab ntsha hypotension.

Cov tshuaj insulin thiab tshuaj uas txhim kho nws qhov kev zais cia. Cov tshuaj Insulin thiab cov tshuaj uas pab txhawb nws txoj kev zais, xws li sulfonylureas, tuaj yeem ua rau muaj kev pheej hmoo ntawm hypoglycemia. Yog li no, nrog rau kev siv empagliflozin sib xyaw nrog insulin thiab tshuaj uas txhim kho nws qhov kev tso cia, nws yuav tsim nyog txo lawv cov koob tshuaj, txhawm rau kom tsis txhob muaj kev pheej hmoo ntawm hypoglycemia.

Kev ntsuas cov tshuaj sib txuam hauv vitro. Empagliflozin tsis inhibit, inactivate, lossis ntxias CYP450 isoenzymes. Txoj hauv kev tseem ceeb ntawm tib neeg cov khoom noj khoom haus metabolism yog glucuronidation nrog kev koom tes ntawm UDP-GT (UGT2B7, UGT1A3, UGT1A8 thiab UGT1A9). Empagliflozin tsis inhibit UGT1A1, UGT1A3, UGT1A8, UGT1A9 lossis UGT2B7. Kev sib cuam tshuam yeeb tshuaj ntawm cov tshuaj empagliflozin thiab cov tshuaj uas yog cov me me ntawm CYP450 thiab UGT isoenzymes yog suav tias yog qhov tsis zoo. Empagliflozin yog lub cev rau P-gp thiab cov protein uas txiav txim siab BCRP, tab sis hauv kev siv tshuaj tsis thaiv cov protein. Raws li cov ntaub ntawv los ntawm kev tshawb fawb hauv vitro , nws tau ntseeg tias muaj peev xwm ntawm empagliflozin sib cuam tshuam nrog kev siv yeeb tshuaj uas tau hloov chaw rau P-gpyog tsis zoo li. Empagliflozin yog cov txheej txheem rau cov organic anionic nqa khoom: OAT3, OATP1B1 thiab OATP1B3, tab sis tsis yog lub cev rau cov organic anionic nqa khoom 1 (OAT1) thiab organic cationic carriers 2 (OCT2). Txawm li cas los xij, kev sib cuam tshuam txog yeeb tshuaj ntawm empagliflozin nrog cov tshuaj uas yog cov substrates rau cov cab kuj muaj cov roj ntsha tau piav qhia saum toj yog suav tias tsis zoo li.

Kev ntsuas cov tshuaj sib txuam hauv vivo. Nrog rau kev siv empagliflozin nrog rau lwm cov tshuaj uas feem ntau siv, qhov sib cuam tshuam ntawm kev sib raug zoo pharmacokinetic tsis tau pom. Cov txiaj ntsig ntawm kev tshawb fawb pharmacokinetic qhia tau hais tias tsis tas yuav hloov pauv qhov koob tshuaj ntawm Jardins ® thaum nws siv nrog cov tshuaj siv feem ntau.

Cov chaw muag tshuaj ntawm empagliflozin tsis hloov pauv rau cov neeg tuaj yeem noj qab haus huv thaum siv ua ke nrog metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, thiab hauv cov neeg mob uas muaj ntshav qab zib hom 2 yog siv ua ke nrog torasemoridide thiab hydrochloride.

Nrog rau kev siv empagliflozin nrog gemfibrozil, rifampicin thiab probenecid, kev nce ntxiv ntawm AUC ntawm empagliflozin tau pom los ntawm 59, 35 thiab 53%, xwm yeem, txawm li cas los xij, cov kev hloov no tsis tau pom tias tseem ceeb hauv kev kho mob.

Cov tshuaj Empagliflozin tsis muaj kev cuam tshuam loj hauv lub chaw muag tshuaj ntawm metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide thiab tshuaj tiv thaiv hauv qhov ncauj hauv cov neeg tuaj noj qab haus huv.

Yeeb tshuaj sib cuam tshuam

Nws txhim kho lub diuretic nyhuv ntawm ntau cov tshuaj diuretics, uas ua rau muaj kev pheej hmoo ntawm lub cev qhuav dej thiab cov hlab ntsha hypotension. Cov tshuaj insulin thiab sulfonylurea qee zaum yuav ua rau lub qog ntshav qab zib. Nrog rau kev siv tshuaj ua ke nrog cov tshuaj insulin, kev txo tshuaj ntau ntau yog tsim nyog kom tsis txhob muaj lub ntsej muag ntshav qab zib.Qhov kev siv tshuaj ntawm empagliflozin thiab tshuaj uas yog cov roj ntsha ntawm isoenzymes yog suav tias yog kev nyab xeeb.

Empagliflozin - cov tshuaj ua mob hauv cov ntsiav tshuaj, tsis muaj kev cuam tshuam cov khoom lag luam pharmacological ntawm cov tshuaj hauv qab no: Metformin, Glimepiride, Pioglitazone, Warfarin, Digoxin, Ramipril, Simvastatin, Hydrochlorothiazide, Torasemide thiab tshuaj tiv thaiv qhov ncauj. Nrog rau kev siv thooj txhij nrog cov tshuaj no feem ntau, tsis tas yuav hloov cov koob tshuaj.

Jardins Analogs

Ntawm kev lag luam tshuaj ntawm Lavxias teb sab, muaj tsuas yog ib cov tshuaj tsim nyob rau hauv lub hauv paus ntawm ib yam khoom - empagliflovin. Jardins tsis muaj daim ntawv pov thawj zoo. Lwm cov ntsiav tshuaj hypoglycemic muaj lwm yam tshuaj nyob rau hauv muaj pes tsawg leeg thiab coj txawv ntawm tib neeg lub cev. Cov no suav nrog:

Jardins - cov lus qhia rau kev siv, nqi, xyuas thiab analogues

Ntshav qab zib mellitus raug suav hais tias yog ib qho ntawm cov kev sib txawv ntawm cov ntiaj teb. Hauv Lavxias Lavxias, muaj txog 10 lab pej xeem raug mob los ntawm tus kabmob no. Ntau ntawm lawv nyiam siv tshuaj Jardins vim tias nws cov hauj lwm zoo.

Lub npe Latin yog Jardiance. Tshuaj hauv INN: Empagliflozin (Empagliflozin).

Jardins muaj cov nyhuv tshuaj tiv thaiv kab mob.

Cov kev faib tawm ATX: A10BK03.

Cov tshuaj muaj nyob rau hauv daim ntawv ntawm cov tshuaj soluble-coated. 1 ntsiav tshuaj muaj 25 lossis 10 mg ntawm empagliflozin (cov tshuaj ua kom nquag plias). Lwm yam khoom:

• talcum hmoov
• titanium dioxide
• oxide daj hlau (zas xim),
• lactose monohydrate,
• Kev Hyprolose
• cellulose microcrystals.

Cov tshuaj muaj nyob rau hauv daim ntawv ntawm cov tshuaj soluble-coated.

Cov ntsiav tshuaj tau ntim rau hauv cov hlwv ntawm 10 pcs. 1 lub thawv muaj 1 lossis 3 lub hlwv.

Nrog saib xyuas

Cov tshuaj tau sau tseg kom zoo thaum:

• tsawg zais cia kev ua ub ua no ntawm cov hlwb nyob rau hauv kev txiav,
• ua ke nrog sulfonylurea thiab insulin derivatives,
• lub plab zom mov cov kab mob uas cuam tshuam nrog cov kua dej ua kom poob,
• laus lawm.

Tsuas tshuaj thiab tswj hwm

Ntsiav tshuaj yog noj ntawm qhov ncauj. Qhov tshuaj thawj zaug yog 10 mg 1 zaug nyob rau ib hnub. Yog tias cov tshuaj no tsis muaj peev xwm muab cov tshuaj glycemic tswj, tom qab ntawd cov koob tshuaj nce mus rau 25 mg. Qhov ntau kawg noj yog 25 mg / hnub.

Ntsiav tshuaj yog noj ntawm qhov ncauj.

Kev siv cov ntsiav tshuaj tsis khi rau lub sijhawm ntawm hnub lossis txoj kev noj mov. Nws yog qhov tsis tsim nyog rau 1 hnub los thov ob koob.

Kho Ntshav Qab Zib los ntawm Jardins

Cov chaw soj ntsuam tau ua pov thawj tias cov tshuaj hauv nqe lus nug tsuas yog siv tshuaj rau kev kho mob ntshav qab zib mellitus (hom II), uas cov kev pheej hmoo ntawm kev tshwm sim ntawm CVD cov kab mob thiab kev tuag los ntawm cov kev kho tshiab yog txo. Nws raug txwv tsis pub siv cov tshuaj rau cov neeg mob ntshav qab zib hom 1.

Kev sim ua pov thawj ntawm cov kws kho mob thiab cov neeg mob txog Jardins

Galina Aleksanina (tus kws kho mob), hnub nyoog 45 xyoos, St. Petersburg.

Cov tshuaj zoo uas tsis ua rau muaj kev phiv (hauv kuv xyaum). Tus nqi siab yog tag nrho los ntawm tag nrho cov pharmacological kev ua si ntawm cov tshuaj. Cov placebo nyhuv yog kiag li txiav txim siab. Tsis tas li ntawd, nws tsis muaj analogues nyob hauv Russia, thiab cov tshuaj zoo sib xws nyias coj txawv nyias.

Anton Kalinkin, 43 xyoo, Voronezh.

Cov cuab yeej siv tau zoo. Kuv, uas yog tus mob ntshav qab zib nrog kev paub, kuv txaus siab kiag li nrog nws qhov kev txiav txim. Qhov tseem ceeb tshaj plaws yog ua tib zoo kawm cov lus qhia rau kev siv. Tsuas yog hauv qhov no yuav muaj kev phiv tuaj yeem zam, uas yog tus kheej tau txheeb xyuas qhov tseeb. Ntawm qhov tsis txaus, ib tus muaj peev xwm paub qhov txawv tsuas yog tus nqi siab thiab qhov tseeb tias cov tshuaj tsis raug muag hauv txhua lub tsev muag tshuaj.

Jardins: cov lus qhia rau kev siv

Cov Tshuaj Hauv Tshuaj

Empagliflozin yog qhov thim rov qab, nquag, xaiv thiab sib tw inhibitor ntawm hom 2 sodium-dependent glucose transporter nrog qhov xav tau yuav tsum tau inhibit 50% ntawm qhov kev ua enzyme (IC50) ntawm 1.3 nmol.

Qhov xaiv ntawm empagliflozin yog 5,000 npaug ntau dua qhov xaiv ntawm hom 1 sodium-dependent glucose transporter lub luag haujlwm rau kev nqus ntawm cov piam thaj hauv txoj hnyuv. Tsis tas li ntawd, nws tau pom tias empagliflozin muaj qhov siab xaiv rau lwm cov neeg thauj khoom qabzib lub luag haujlwm rau cov piam thaj homeostasis hauv cov nqaij ntau yam.

Cov sodium-depend type 2 glucose transporter yog lub ntsiab thauj cov protein rau lub luag haujlwm kom rov muaj cov piam thaj ntawm ntshav qabzib rov qab los rau hauv cov ntshav. Empagliflozin txhim kho glycemic tswj nyob rau hauv cov neeg mob uas muaj hom 2 mob ntshav qab zib mellitus (T2DM) los ntawm kev txo cov ntshav qabzib reabsorption.

Tus nqi ntawm cov piam thaj zais tawm los ntawm ob lub raum siv cov txheej txheem no nyob ntawm kev saib xyuas cov piam thaj hauv ntshav thiab glomerular filtration rate (GFR). Kev txwv tsis pub los ntawm sodium-muaj neeg nqa khoom ntawm hom 2 piam thaj hauv cov neeg mob uas muaj ntshav qab zib hom 2 thiab hyperglycemia ua rau kev tshem tawm cov piam thaj ntau dhau los ntawm ob lub raum.

Hauv kev tshawb nrhiav, nws tau pom tias nyob rau hauv cov neeg mob uas muaj ntshav qab zib hom 2, qhov tsis pom qabzib los ntawm lub raum nce ntxiv tom qab siv thawj zaug ntawm empagliflozin, cov nyhuv no txuas ntxiv mus 24 teev.

Kev nce ntxiv ntawm cov kua nplaum tawm ntawm lub raum txuas ntxiv mus kom txog rau thaum lub sijhawm 4-lub lim tiam kho mob, nrog empagliflozin ntawm ib koob ntawm 25 mg ib hnub ib zaug, qhov nruab nrab, kwv yees li 78 g / hnub. Hauv cov neeg mob uas muaj ntshav qab zib hom 2, ib qho kev nce ntxiv ntawm cov kua nplaum los ntawm ob lub raum ua rau muaj kev cuam tshuam sai li sai tau ntawm cov ntshav qabzib hauv cov ntshav ntshav.

Empagliflozin txo cov ntsiab lus ntawm cov piam thaj hauv ntshav ntshav ob leeg ntawm kev yoo mov thiab tom qab noj mov. Lub non-insulin-ua rau lub tswv yim ntawm kev txiav txim ntawm empagliflozin ua rau muaj kev pheej hmoo tsawg ntawm qhov kev txhim kho uas muaj peev xwm ntawm hypoglycemia. Cov nyhuv ntawm empagliflozin tsis yog nyob ntawm lub xeev kev ua haujlwm ntawm pancreatic beta hlwb thiab cov tshuaj insulin metabolism.

Cov txiaj ntsig zoo ntawm empagliflozin rau surrogate cim ntawm beta cell ua haujlwm, suav nrog HOMA-? Index, tau sau tseg (qauv rau kev ntsuam xyuas homeostasis-B) thiab kev faib ua feem ntawm proinsulin rau insulin. Tsis tas li ntawd, ntxiv kev tshem tawm cov piam thaj los ntawm ob lub raum ua rau poob phaus, uas yog nrog cov suab nrov me me hauv lub cev txo thiab qhov hnyav hauv lub cev. Glucosuria tau pom thaum siv empagliflozin yog nrog los ntawm diuresis me ntsis, uas tuaj yeem ua rau txo qis hauv cov ntshav siab.

Hauv kev sim tshuaj saib qhov twg empagliflozin raug siv los kho monotherapy, kev sib txuas ua ke nrog metformin, kev sib txuas ua ke nrog metformin thiab sulfonylurea derivatives, kev sib txuas nrog kev kho mob nrog metformin piv rau glimepiride, kev sib xyaw nrog kev kho mob nrog pioglitazone +/- metformin, ua kev kho mob sib xyaw nrog dipeptidyl peptide inhibitor 4 (DPP-4), metformin +/- lwm qhov tshuaj hypoglycemic hauv qhov ncauj, nyob rau hauv kev sib xyaw ua ke nrog kev kho mob nrog insulin, nws muaj cov lus tseem ceeb. kuv qhov txo qis hauv glycosylated HbAlc hemoglobin thiab txo qis hauv kev yoo plasma ntshav qab zib.

Cov pharmacokinetics ntawm empagliflozin tau nkag siab ntau yam hauv cov neeg tuaj yeem noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2.

Tom qab lub qhov ncauj tswj hwm, empagliflozin tau nrawm nrawm, qhov siab tshaj plaws ntawm empagliflozin hauv cov ntshav ntshav (Cmax) tau mus txog tom qab 1.5 teev. Tom qab ntawv, kev saib xyuas ntawm empagliflozin hauv ntshav txo qis hauv ob theem.

Tom qab noj cov tshuaj empagliflozin, thaj tsam nruab nrab hauv qab qhov nruab nrab-lub sijhawm nkhaus (AUC) thaum lub sijhawm khov kho hauv lub xeev ntshav yog 4740 nmol x teev / L, thiab tus nqi Cmax yog 687 nmol / L. Cov tshuaj pharmacokinetics ntawm empagliflozin hauv cov neeg tuaj yeem noj qab haus huv thiab cov neeg mob ntshav qab zib hom 2 feem ntau zoo sib xws.

Noj mov tsis muaj kev cuam tshuam loj hauv tsev kho mob ntawm pharmacokinetics ntawm empagliflozin.

Qhov ntim ntawm kev faib tawm thaum lub sijhawm khov kho hauv lub xeev ntshav muaj li ntawm 73.8 litres. Tom qab lub qhov ncauj tswj hwm los ntawm noj qab haus huv tuaj pab dawb ntawm daim ntawv lo empagliflozin 14C, ntshav protein ntshav khi yog 86%.

Txoj hauv kev tseem ceeb ntawm empagliflozin metabolism hauv tib neeg yog glucuronidation nrog kev koom tes ntawm uridine-5'-diphospho-glucuronosyltransferases UGT2B7, UGT1A3, UGT1A8 thiab UGT1A9. Kev kuaj pom muaj ntau tshaj ntawm cov tshuaj empagliflozin yog peb glucuronic conjugates (2-0, 3-0 thiab 6-0 glucuronides). Cov haujlwm ua haujlwm ntawm txhua lub cev ntawm cov metabolite yog me me (tsawg dua 10% ntawm tag nrho cov nyhuv ntawm empagliflozin).

Qhov kev tshem tawm ib nrab-lub neej yog kwv yees li 12.4 teev. Kev siv empagliflozin ib zaug ib hnub, ib qho ntshav plasma concentration tau mus txog tom qab koob thib tsib.

Tom qab qhov ncauj tswj hwm ntawm daim ntawv lo empagliflozin 14C hauv kev tuaj yeem pab dawb noj qab haus huv, kwv yees li 96% ntawm cov koob tshuaj tau tawm (los ntawm txoj hnyuv 41% thiab lub raum 54%). Los ntawm txoj hnyuv, feem ntau ntawm cov ntawv lo ntawm cov tshuaj tsis txawv txav.

Tsuas yog ib nrab ntawm cov tshuaj cim uas tau tso nrog tsis hloov pauv ntawm lub raum. Pharmacokinetics hauv cov neeg mob tshwj xeeb

Lub raum khiav tsis zoo

Hauv cov neeg mob uas mob me, qis thiab mob raum tsis ua haujlwm (30 https: //apteka.103.xn--p1ai/jardins-13921690-instruktsiya/

Jardins ™ ntsiav tshuaj 10 mg 30 pcs

Jardins® tsis pom zoo rau cov neeg mob uas muaj ntshav qab zib hom 1 thiab rau kev kho mob ntshav qab zib ketoacidosis.

Nrog rau kev siv hom 2 piam thaj transporter inhibitors, suav nrog empagliflozin, muaj tsawg tus neeg mob ntshav qab zib ketoacidosis tau tshaj tawm. Hauv qee qhov xwm txheej no, cov kev pom tshwm sim yog atypical thiab qhia tias qhov nce ntawm cov ntshav qabzib hauv siab (tsis ntau tshaj 14 mmol / L (250 mg / dl)).

Txoj kev pheej hmoo ntawm kev muaj mob ntshav qab zib ketoacidosis yuav tsum tau txiav txim siab yog tias tsis muaj qhov tsos mob zoo xws li xeev siab, ntuav, tsis qab los noj mov, mob plab, nqhis dej heev, ua tsis taus pa, tsis meej pem, nkees nkees lossis qaug zog tshwm sim. Yog tias cov tsos mob tshwm sim, cov neeg mob yuav tsum tau soj ntsuam ketoacidosis tam sim ntawd, tsis hais seb cov ntshav qabzib ntau npaum li cas. Kev siv cov tshuaj Jardins® yuav tsum tau tsum txuas mus ntxiv lossis ncua kom txog thaum kuaj tau tsim.

Txoj kev pheej hmoo siab dua ntawm kev mob ntshav qab zib ketoacidosis muaj peev xwm ua tau rau cov neeg mob noj cov zaub mov uas muaj cov carbohydrate tsawg, cov neeg mob lub cev qhuav dej tsis txaus, cov neeg mob uas muaj keeb kwm ketoacidosis, lossis cov neeg mob uas tsis muaj cov kev ua haujlwm ntawm pancreatic β-hlwb. Hauv cov neeg mob no, Jardins® yuav tsum siv nrog ceev faj. Ceev faj yog xav tau thaum txo qhov koob tshuaj insulin.

Qhov kev npaj Jardins® hauv ib lub ntsiav tshuaj 10 mg muaj 162,5 mg ntawm lactose, nrog qhov ntau npaum li 25 mg muaj 113 mg ntawm lactose, yog li, cov tshuaj yuav tsum tsis txhob siv rau hauv cov neeg mob uas muaj mob tsis tshua muaj mob xws li lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Cov kev tshawb fawb soj ntsuam tau pom tias kev kho mob nrog empagliflozin tsis muaj kev pheej hmoo mob plawv. Kev siv cov tshuaj empagliflozin ntawm ib koob ntawm 25 mg tsis ua rau lub sijhawm ntev ntawm QT luv.

Nrog rau kev siv tshuaj ua ke Jardins® nrog sulfonylurea derivatives los yog nrog insulin, yuav tsum tau txo koob tshuaj sulfonylurea / insulin derivatives vim tias qhov kev pheej hmoo ntawm hypoglycemia.

Empagliflozin tsis tau kawm txog kev sib xyaw nrog glucagon zoo li peptide-1 analogues (GLP-1).

Kev ua haujlwm ntawm cov tshuaj Jardins® nyob ntawm kev ua haujlwm ntawm lub raum, yog li nws raug nquahu kom kuaj xyuas lub raum ua haujlwm ua ntej nws teem sijhawm thiab tsis tseg thaum kho (tsawg kawg 1 zaug hauv ib xyoos), nrog rau ua ntej kev teem sijhawm kho tus mob, uas tuaj yeem cuam tshuam rau lub raum kev ua haujlwm. Kev siv cov tshuaj rau hauv cov neeg mob uas lub raum tsis ua haujlwm (GFR tsis pom zoo