Cov tshuaj yog muaj nyob hauv cov qauv tshuaj. Cov ntsiav tshuaj kuj yuav muaj xim txawv. Nws nyob ntawm qhov kev kub siab ntawm cov nquag ua ke thiab cov tshuaj pleev xim hauv lawv. Lawv tau them nrog lub plhaub tshwj xeeb.

1 ntsiav tshuaj muaj 2.5 mg ntawm saxagliptin thiab 500 lossis 1000 mg ntawm metformin hydrochloride. Cov ntsiav tshuaj muaj lub convex oblong puab. Ua raws li cov concentration ntawm metformin, lawv tuaj yeem muaj xim av, xim paj yeeb lossis xim daj. Ntawm ob sab muaj cov ntsuas qhia tau ua nrog xiav number case. Cov khoom siv pabcuam yog: carmellose sodium, magnesium stearate thiab cellulose.

Cov tshuaj yog muaj nyob hauv cov qauv tshuaj.

Cov ntsiav tshuaj muaj nyob rau hauv cov hlwv tshwj xeeb ntawm 7 pcs. nyob hauv txhua. Ib pob ntawv cardboard khaws 4 lub hlwv thiab tag nrho cov lus qhia rau siv.

Pharmacological kev txiav txim

Cov tshuaj ua ke ntawm nws cov muaj pes tsawg leeg 2 kev sib txuas. Qhov no ua rau nws yog cov khoom siv rau hauv kev kho mob ntshav qab zib hom 2. Saxagliptin ua yeeb yam xws li tshuaj tiv thaiv, koom tes nrog kev tsim cov peptide, thiab Metformin belongs rau cov pab pawg ntawm biguanides. Lub cev ua kom nquag plias raug tso tawm ntau yam hloov kho.

Metformin muaj peev xwm txo qis gluconeogenesis. Cov roj oxidation nres, thiab cov tshuaj insulin ua rau muaj ntau ntxiv. Kev siv cov kua nplaum nyob rau hauv lub hlwb sai dua. Raws li kev cuam tshuam ntawm Metformin, glycogen synthesis yog txhim kho. Cov piam thaj pib ua kom yuag qeeb dua hauv cov plab hnyuv plab hnyuv, ua rau lub cev yuag sai.

Saxagliptin txhawb nqa txoj kev tso tawm sai sai ntawm cov insulin los ntawm pancreatic beta hlwb. Tus txheej txheem no nyob ntawm cov piam thaj hauv cov ntshav ntshav. Glucagon secretion txo qis, uas txwv tsis pub muaj cov piam thaj ntau ntxiv hauv qee cov txheej txheem ntawm nplooj siab. Saxagliptin pab txo qis qhov tsis ua dab tsi ntawm cov tshuaj hormones tshwj xeeb, nce ntxiv. Nyob rau tib lub sijhawm, lawv qib hauv cov ntshav nce siab, thiab cov piam thaj ntawm lub plab yuav poob qis tom qab noj mov tseem ceeb.

Cov Tshuaj Pharmacokinetics

Saxagliptin ib txwm yauv hloov pauv mus rau qhov chaw tshiab. Metformin, txawm hais tias tom qab tau lim dej zoo hauv lub raum hlaus, raug tawm hauv lub cev ua ib daim ntawv tsis txawv txav. Qhov siab tshaj plaws ntawm cov tshuaj yeeb dej caw yog pom txog 6 teev tom qab noj tshuaj ntsiav.

Metformin, txawm hais tias tom qab tau lim dej zoo hauv lub raum hlaus, raug tawm hauv lub cev ua ib daim ntawv tsis txawv txav.

Cov Yuav Tsum Muaj

Nws tsis yog siv rau hauv kev kho mob ntshav qab zib hom 1, nrog rau qhov muaj kev txhim kho mob ntshav qab zib ketoacidosis, txij li nyob rau hauv cov xwm txheej zoo li no cov tshuaj yuav tsis muaj qhov xav tau kho kom zoo.

Tsis tas li ntawd, muaj ntau txoj kev nruj me ntsis rau kev noj tshuaj:

lub raum tsis ua hauj lwm zoo,
lactic acidosis,
lactose tsis kam lees thiab siv rau kev kho mob ntau kawg ntawm insulin,
kev mob plawv
hlab plawv poob siab, septicemia,
mob myocardial infarction,
hypersensitivity rau lub active Cheebtsam ntawm cov tshuaj,
mob hnyav thiab mob ntev metabolic acidosis,
hnub nyoog txog 18 xyoo
cov khoom noj tsis muaj calorie tsawg
cev xeeb tub thiab lub sijhawm lactation,
siv rau kev kho mob ntawm iodine-muaj cov tshuaj tiv thaiv kev cuam tshuam, uas tuaj yeem ua rau txoj kev txhim kho ntawm lub raum tsis ua haujlwm.

Comboglyz yog contraindicated nyob rau hauv kev ua txhaum ntawm ib txwm lub raum muaj nuj nqi.
Comboglis yog contraindicated nyob rau hauv kev mob plawv mob plawv.
Comboglyz yog contraindicated nyob rau hauv mob myocardial infarction.
Comboglyz yog sib xyaw rau hauv cov zaub mov uas tsis muaj calorie ntau.

Tag nrho cov contraindications yog tsis. Feem ntau cov feem ntau, nrog cov pathologies li no, cov tshuaj insulin yog siv los kho ntshav qab zib.

Yuav ua li cas noj combogliz?

Kev siv tshuaj kho mob antiglycemic, qhov koob tshuaj Combogliz yuav tsum yog kws kho mob ib leeg rau ib tus neeg mob, nyob ntawm lub xeev kev noj qab haus huv. Cov tshuaj yog pom zoo kom noj rau thaum yav tsaus ntuj, zoo dua nrog zaub mov. Qhov loj npaum li cas ntawm ib qho hnoos tshuaj Saxagliptin yuav tsum tsis pub tshaj 2.5 mg lossis hauv cov muaj mob hnyav 5 mg ib hnub.

Nws yog qhov pom zoo kom nqos cov ntsiav tshuaj tag nrho yam tsis muaj ntxo. Nws yuav tsum tau ntxuav nrog ntau cov dej rhaub.

Thaum muab sib xyaw nrog kev siv rov qab siv nrog cytochrome isoenzymes, cov koob tshuaj pom zoo yog 1 ntsiav tshuaj ntawm 2.5 mg rau ib hnub.

Nws yog qhov pom zoo kom nqos cov ntsiav tshuaj tag nrho yam tsis muaj ntxo.

Kev phiv los ntawm Comboglize

Cov neeg mob feem ntau nco txog kev txhim kho uas tsis xav pom qhov tsis zoo:

mob taub hau, nce mus rau hauv cov tsos tshwm sim ntawm migraines,
cov tsos mob ntawm intoxication, manifested los ntawm xeev ntuav, ntuav thiab raws plab heev,
rub teeb meem mob hauv plab
cov kab mob sib kis ntawm cov kab mob tso zis,
o ntawm lub ntsej muag thiab nqua,
pob txha tsis zoo nce ntxiv, feem, qhov no kuj nce qhov kev pheej hmoo ntawm pob txha lov thaum noj Saksagliptin (pawg tshuaj ntsuam ntawm cov tshuaj ntau npaum li cas los ntawm 2.5 txog 10 mg) thiab cov placebo,
ntshav qab zib,
ua xua tshwm sim nyob rau hauv daim ntawv ntawm daim tawv nqaij ua pob thiab urticaria,
flatulence
ua txhaum ntawm kev saj ntawm qee yam khoom yog ua tau.

Cov neeg mob feem ntau nco ntsoov txoj kev txhim kho tsis xav txog cov teeb meem nyob rau hauv daim ntawv ntawm mob taub hau.
Cov neeg mob feem ntau nco txog kev txhim kho qhov tsis xav hnov tus mob nyob rau hauv daim ntawv ntawm flatulence.
Cov neeg mob feem ntau nco ntsoov txoj kev txhim kho tsis xav pom cov nyom nyob hauv daim ntawv ntawm xeev siab.

Cov tsos mob zoo li no yuav tsum ploj mus tom qab kev hloov kho ntau dua lossis kev tshem tawm tag nrho ntawm cov tshuaj. Yog tias cov tsos mob ntawm intoxication nyob twj ywm, yuav tsum muaj kev tshem tawm cov tsos mob ua kom tshem tawm.

Cov lus qhia tshwj xeeb

Thaum noj tshuaj, nws yog qhov yuav tsum tau ua kev soj ntsuam los saib xyuas qhov hloov ntawm lub raum. Nws muaj qhov pheej hmoo siab ntawm lactic acidosis. Qhov no muaj tseeb tshwj xeeb ntawm cov neeg laus.

Thaum siv Saksagliptin, ib qho koob tshuaj nce qis hauv qhov nruab nrab ntawm lymphocytes yuav tshwm sim. Cov nyhuv no raug pom thaum noj ib koob tshuaj 5 mg hauv kev pib nrog Metformin piv nrog kev kho mob monotherapy nrog Metformin ib leeg.

Siv thaum cev xeeb tub thiab lactation

Nws tsis pom zoo kom noj thaum lub sijhawm menyuam. Niaj hnub no, muaj kev tshawb nrhiav tsis txaus ntawm seb cov ntsiav tshuaj puas muaj cov teratogenic lossis embryogenic cov teebmeem ntawm tus menyuam hauv plab. Cov tshuaj tuaj yeem pab ua kom pom qhov txawv txav ntawm lub plab thiab kev huam tuaj ntawm plab. Yog tias tsim nyog, txhua tus poj niam cev xeeb tub raug pauv mus rau kev kho mob Insulin ntawm kev siv tshuaj me me.

Nws tsis pom zoo kom noj cov tshuaj thaum lub sijhawm xeeb tub.

Tsis muaj ib qho ntaub ntawv txaus ntseeg ntawm seb cov tshuaj puas tuaj yeem xa mus rau niam mis. Yog li no, cov kws tshaj lij qhia kom tsis txhob lactation.

Siv rau lub sijhawm qub

Nrog rau kev saib xyuas tshwj xeeb, cov tshuaj raug muab rau cov neeg laus. Lawv muaj kev pheej hmoo siab los ntawm kev txhim kho ntau yam teeb meem, yog li ntawd, kev saib xyuas tas li ntawm lub xeev kev noj qab haus huv los ntawm tus kws kho mob thiab tus mob endocrinologist yuav tsum. Yog tias muaj qhov xav tau ntawd, tom qab ntawd cov koob tshuaj tau raug txo kom qis qis, thaum yam xav tau kho tau tseem ua tiav. Txhawm rau tsim cov placebo kev txiav txim siab, kev tsim cov vitamin ntxiv kom raug rau qee tus neeg laus, tshwj xeeb tshaj yog cov neeg muaj kev puas siab ntsws.

Daim ntawv thov rau lub raum khiav tsis zoo

Nws muaj kev pheej hmoo siab ntxiv ntawm kev mob metabolic acidosis nrog kev siv ntev. Nws yog qhov zoo dua rau cov neeg mob uas mob raum tsis txaus los txo cov koob tshuaj kom tsawg kawg lossis tsis kam lees noj.

Nws yog nruj me ntsis txwv tsis pub coj cov neeg mob siab concomitant siab pathologies.

Noj tshuaj ntau dhau ntawm Comboglize

Cov tshuaj no zoo rau cov neeg mob pom zoo. Muaj qee zaum ntawm overdose. Tsuas yog nrog kev tswj hwm qhov kev huam yuaj ntawm koob tshuaj loj tuaj yeem pom cov tsos mob qee zaum qhia txog kev txhim kho ntawm cov kab mob lactic acidosis. Cov feem ntau cov ntawm lawv:

teeb meem nrog cov txheej txheem ua pa
qaug zog thiab mob siab sai,
mob leeg
mob plab heev
cov tsos ntawm tsis hnov tsw ntawm acetone los ntawm lub qhov ncauj.

Hauv qhov xwm txheej no, pais plab lav los yog hemodialysis tuaj yeem pab. Nrog cov mob ntshav qab zib me ntsis, nws pom zoo kom noj qab zib lossis haus dej qab zib.

Kev cuam tshuam nrog lwm yam tshuaj

Kev siv Tshuaj Comboglize nrog lwm cov tshuaj tuaj yeem pab ua kom plasma ntau dua ntawm lactate. Cov tshuaj no suav nrog:

magnesium npaj
Nicotinic acid
Rifampicin,
tshuaj kho mob
Isoniazid,
cov thyroid hormones,
calcium tubule blockers,
estrogens.

Kev siv ua ke nrog Comboglize nrog Nicotinic acid tuaj yeem pab txhawb kev nce ntshav ntxiv ntawm lactate.
Cov tshuaj sib xyaw ua ke nrog Combogliz nrog Rifampicin tuaj yeem nce ntshav plasma concentration ntawm lactate.
Cov tshuaj sib xyaw nrog Comboglize nrog cov diuretics tuaj yeem ua rau kom ntshav plasma concentration ntawm lactate.

Kev sib xyaw nrog Pioglitazone tsis cuam tshuam rau pharmacokinetics ntawm Saxagliptin. Tsis tas li ntawd, kev sib xyaw ua ke yog ib qho siv Saksagliptin, tom qab ntawd tom qab 3 teev 40 mg ntawm Famotidine, cov yam ntxwv ntawm tshuaj kuj tsis hloov.

Thaum noj cov tshuaj Combogliz, cov hauj lwm zoo ntawm cov nyiaj yuav txo qis:

Fluconazole
Erythromycin,
Ketoconazole,
Furosemide
Verapamil
ethanol.

Yog tias tus neeg mob noj ib qho ntawm cov tshuaj uas teev tseg, koj yuav tsum qhia koj tus kws kho mob.

Cawv tau zoo

Cawv yog txwv rau cov neeg mob ntshav qab zib mellitus. Nws tuaj yeem cuam tshuam cov nyhuv ntawm cov tshuaj noj.

Txhais tau tias muaj qhov sib txawv hauv kev muaj pes tsawg leeg, tab sis muaj qhov sib txawv hauv kev siv tshuaj:

Combogliz Prolong,
Bagomet,
Janumet
Galvus Met,
Glibomet.

Cov tsiaj txhu ntawm Combogliz yog Bagomet.
Cov analogue ntawm Comboglize yog Glybomet.
Cov analogue ntawm Comboglize yog Yanumet.

Ua ntej pib hloov kho, koj yuav tsum ua tib zoo nyeem cov lus qhia rau txoj kev kho mob uas tau xaiv, vim lawv txhua tus muaj kev cuam tshuam loj heev thiab muaj kev phiv tshuaj. Txuas ntxiv, qhov ntau npaum ntawm cov tshuaj yog txawv.

Cia rau cov mob rau cov tshuaj

Khw rau hauv ib qho chaw uas qhov ncaj qha tshav ntuj tsis poob. Cia kub - chav. Cov tshuaj yuav tsum nyob hauv qhov chaw qhuav thiab tiv thaiv los ntawm menyuam yaus me kom ntau li ntau tau.

Cov tshuaj tuaj yeem raug yuav ntawm lub tsev muag tshuaj nrog cov tshuaj noj.

Kev txheeb xyuas txog Comboglize

Stanislav, hnub nyoog 44 xyoo, kws kho mob ntshav qab zib, St. Petersburg: "Kuv tau siv cov tshuaj ntev los kho kuv cov kev coj ua tau zoo. Cov ntshav qab zib hauv cov neeg mob hom mob ntshav qab zib mellitus tsawg zuj zus lawm tom qab kev kho mob. Nws tseem nyob rau theem ib txwm siv tau ntev, uas ua rau cov tshuaj muaj ntshav. "Nws raug nqi tsawg dua li kev ua kom ntev, tab sis lawv cov txiaj ntsig zoo ib yam. Txawm tias qhov muaj pes tsawg leeg zoo li qub. Qee tus neeg mob ua xua nyob rau hauv kev ua urticaria. Tab sis txhua yam ploj mus sai.

Varvara, 46 xyoo, endocrinologist, Penza: "Kuv tau siv tshuaj los kho kuv cov ntshav qab zib kom zoo li qub. Tab sis muaj kev soj ntsuam ntau yam tsis zoo los ntawm cov neeg mob. Qhov no yog vim muaj qhov tshwm sim tsis zoo ntau zaus. Thaum zoo li no, koj yuav tsum tshem tawm txoj kev kho mob thiab xav txog qhov hloov pauv. Yog li, kuv xav kom cov neeg mob pib qis qis tshaj plaws los saib cov tshuaj tiv thaiv ntawm lub cev. Yog tias txhua yam muaj peev xwm, cov txheej txheem kho tuaj yeem txuas ntxiv thiab cov koob tshuaj tau nce ntxiv.

Valery, 38 xyoo, Lub nroog Moscow: "Nws tau sau tshuaj kho mob los ntawm endocrinologist. Kuv raug mob ntshav qab zib hom yam thib ob. Cov ntshav qab zib rov qab zoo li qub. txhua yam ploj mus, cov nyhuv ntawm cov tshuaj tau pib nce ntxiv xwb. Cov tshuaj yog me ntsis kim. "

Andrei, hnub nyoog 47 xyoo, Rostov-on-Don: "Cov tshuaj tsis haum. Tom qab cov ntsiav tshuaj thawj zaug kuv hnov tsis zoo. Kuv pib ntuav, mob taub hau tsis tsum ntev heev. Kuv yuav tsum tau mus ntsib kws kho mob. Tom qab txhua yam rov qab zoo li qub, ib qho tshuaj sib piv ntawm cov tshuaj no tau raug sau tseg, tab sis kuj tom qab nws muaj kev phiv tshuaj ua rau mob hnyav. Tsis tas li ntawd, kev tawm tsam ua xua tshwm sim ntawm daim tawv nqaij. Yog li ntawd, Insulin tau sau tseg. "

Julia, 43 xyoo, Saratov: "Kuv txaus siab rau qhov kev ua ntawm cov tshuaj. Cov piam thaj sai sai rov qab zoo li qub. Kuv poob phaus tsis noj zaub mov. Kuv lub plawv nres mob. Kuv lub cev noj qab haus huv zoo dua. Thawj hnub kuv lub taub hau mob me ntsis, tab sis tom qab ntawd txhua yam nyob ruaj khov. Kuv pom zoo kom txhua tus neeg."

Pharmacological pawg

Qhov ncauj tshuaj hypoglycemic. Dipeptidyl peptidase inhibitor (DPP-4 inhibitor). PBX code A10B N.

Raws li kev ntxiv rau kev noj haus thiab kev tawm dag zog txhawm rau txhim kho glycemic tswj hauv cov neeg mob cov neeg mob ntshav qab zib hom II, yog tias kho nrog saxagliptin thiab metformin yog qhov tsim nyog.

Tsuas tshuaj thiab tswj hwm

Nrog rau kev kho mob antihyperglycemic, qhov koob tshuaj ntawm Comboglyz XR yuav tsum tau kho raws tus kheej, nyob ntawm tus neeg mob txoj kev kho tam sim no, qhov ua tau zoo thiab kam rau ua, thiab yuav tsum tsis txhob ntau tshaj qhov kev pom zoo tshaj plaws ntawm 5 mg metformin txhawb kev tso tawm 2000 mg. Raws li txoj cai, Kev Siv Tshuaj Combogliz XR yuav tsum siv ib hnub ib zaug, thaum yav tsaus ntuj, thaum noj mov, maj mam nce cov koob tshuaj kom txo cov kev phiv los ntawm txoj hnyuv txuas cuam tshuam nrog kev siv cov metformin.

Yog tias kev kho mob nrog cov tshuaj sib xyaw uas muaj saxagliptin thiab metformin pom tau tias tsim nyog, qhov koob tshuaj saxagliptin yog 2.5 mg lossis 5 mg ib hnub ib zaug.

Qhov pom zoo kom pib koob ntawm kev tso tawm ntev ntxiv metformin hydrochloride yog 500 mg ib hnub ib zaug, uas tuaj yeem yog titrated rau koob tshuaj 2000 mg ib hnub ib zaug. Qhov siab tshaj plaws ntawm Comboglyz XR - Saxagliptin 5 mg / Metformin Txhawb Kev Tso Cai 2000 mg siv tau li ob ntsiav tshuaj ntawm 2.5 mg / 1000 mg ib hnub ib zaug.

Tsis muaj cov kev tshawb fawb tshwj xeeb los tshawb txog kev nyab xeeb thiab kev ua tau zoo ntawm Combogliz XR hauv cov neeg mob yav tas los kho nrog lwm tus neeg tuaj yeem tiv thaiv kabmob, thiab tom qab ntawd pauv mus rau Combogliz XR. Ib qho pauv hloov ntawm kev kho mob ntshav qab zib hom II yuav tsum tau ua tib zoo ua thiab tswj hwm tas mus li, vim tias yuav muaj kev hloov pauv hauv glycemic tswj.

XR Combogliz ntsiav tshuaj yuav tsum tau nqos tag nrho tab sis tsis tawg, tsoo lossis zom. Qee zaum cov khoom siv tsis haum ntawm Combogliz XR hauv cov quav yuav zoo li mos, noo noo uas zoo ib yam li cov ntsiav tshuaj qub.

Lub cev muaj zog CYP3A4 / 5 inhibitors.

Thaum siv nrog lub zog cytochrome P450 3A4 / 5 inhibitors (CYP3A4 / 5) (e. Ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, tlithromicin, tlithromicin, tlithromicin, tlithromicin, tlithromicin, tlithromicin, tlithromicin Cov.

Kev phiv tshuaj

Kho mob thiab kho kom zoo ua ke

Cov kev mob tshwm sim feem ntau (kev txhim kho uas tau tshaj tawm nyob rau hauv tsawg kawg 2 cov neeg mob tau txais saxagliptin ntawm koob tshuaj 2.5 mg, lossis tsawg kawg 2 cov neeg mob tau txais saxagliptin ntawm koob tshuaj 5 mg) cuam tshuam nrog kev tawm ntxov ntawm kev kho yog lymphopenia (0.1% thiab 0.5% tiv thaiv 0%, feem)) ua pob xoo (0.2% thiab 0.3% tiv thaiv 0.3%), ua kom cov ntshav creatinine nce (0.3% thiab 0) % piv rau 0%) thiab nce qib ntawm CPK hauv cov ntshav (0.1% thiab 0.2% tiv thaiv 0%).

Hauv cov neeg mob tau txais saxagliptin ntawm koob tshuaj 2.5 mg, mob taub hau (6.5%) tsuas yog muaj kev phiv tshuaj uas tau tshaj tawm nrog lub zaus ³5% thiab ntau zaus ntau dua li ntawm cov neeg mob tau txais cov placebo.

Cov kev mob tshwm sim hauv ³2% ntawm cov neeg mob tau txais saxagliptin ntawm koob tshuaj 2.5 mg saxagliptin ntawm koob tshuaj 5 mg, thiab ³1% ntau zaus dua cov placebo, suav nrog cov leeg mob (2.9% thiab 2.6% tiv tiag 1 , 6%, feem)) mob plab (2.4% thiab 1.7% tawm tsam 0.5%), mob ncauj plab (1.9% thiab 2.3% tiv thaiv 0.9%) thiab ntuav (2.2 % thiab 2.3% tiv thaiv 1.3%).

Qhov ntau zaus ntawm cov pob txha lov yog 1 thiab 0.6 rau 100 tus neeg mob-xyoo, ntsig txog, rau saxagliptin (kev sib xyaw ua ke ntawm kev ntsuam xyuas ntawm 2.5 mg, 5 mg thiab 10 mg) thiab placebo. Qhov ntau ntawm cov pob txha lov nyob rau hauv cov neeg mob kho nrog saxagliptin tsis tau nce ntxiv thaum lub sijhawm. Ib qho laj thawj kev sib raug zoo tsis tau tsim, thiab kev tshawb nrhiav ua ntej tsis tau pom qhov tsis zoo ntawm saxagliptin rau cov pob txha.

Ib qho kev tshwm sim xws li thrombocytopenia, uas yog ua tau zoo ib yam nrog kev kuaj mob ntawm idiopathic thrombocytopenic purpura, tau pom thaum lub sijhawm tshawb fawb soj ntsuam.

Cov kev phiv tsis haum nrog saxagliptin siv nrog metformin hauv cov neeg mob ntshav qab zib hom II uas tsis tau txais kev kho mob

Hauv cov neeg mob uas tau txais kev kho mob sib xyaw nrog saxagliptin thiab metformin, ua ib qho txuas lossis ua kev kho mob thaum pib, kev noj zaub mov plab yog qhov tshwm sim mob plab nkaus xwb uas tau tshwm sim hauv ≥5% ntawm cov neeg mob hauv txhua pawg kho mob. Qhov tshwm sim ntawm kev mob plab zom mov yog 9.9%, 5.8%, thiab 11.2% hauv cov pab pawg tau txais saxagliptin ntawm koob tshuaj 2.5 mg, 5 mg thiab cov placebo pawg, feem, thaum kawm nrog ntxiv ntawm saxagliptin rau metformin. Qhov ntau zaus yog 6.9% thiab 7.3% hauv cov pab pawg uas tau txais 5 mg saxagliptin ntxiv rau metformin thiab metformin monotherapy hauv kev kawm txog kev kho mob ua ke nrog kev siv tshuaj metformin.

Cov ntaub ntawv hais txog kev phiv tshuaj "hypoglycemia" yog raws li txhua daim ntawv tshaj tawm ntawm hypoglycemia. Kev sim tib lub sij hawm ntsuas cov piam thaj tsis tsim nyog. Qhov tshwm sim ntawm kev mob ntshav qab zib yog 3.4% hauv cov neeg mob uas tsis muaj kev paub txog kev kho mob uas tau sau tseg saxagliptin ntawm koob tshuaj 5 mg ntxiv rau metformin, thiab 4.0% hauv cov neeg mob tau txais tshuaj metformin monotherapy.

Kev ua haujlwm tsis haum siab

Xws li qhov tshwm sim tsis zoo ntawm kev tso tawm ntawm urticaria thiab tshuaj tiv thaiv ntsej muag tau tshaj tawm hauv 1.5%, 1.5% thiab 0.4% ntawm cov neeg mob tau txais saxagliptin ntawm koob tshuaj 2.5 mg, saxagliptin ntawm koob tshuaj 5 mg thiab placebo, feem. Tsis muaj leej twg ntawm cov neeg mob no yuav tsum tau mus pw hauv tsev kho mob, thiab tsis muaj leej twg qhia tias muaj mob txaus ntshai tau tuag.

Cov cim tseem ceeb ntawm lub xeev ntawm lub cev

Hauv cov neeg mob uas tau txais kev kho mob monotherapy nrog saxagliptin lossis kev sib txuas ua ke nrog metformin, qhov chaw kho mob tau hloov pauv tseem ceeb hauv cov ntsuas ntawm lub xeev ntawm lub cev tsis tau pom.

Cov kev mob tshwm sim ntau tshaj plaws hauv cov kev tshawb fawb qhia txog kev tsim kho> 5% ntawm cov neeg mob tau txais tshuaj metformin txhawb kev kho hydrochloride, thiab ntau zaus dua li cov neeg siv cov placebo, yog zawv plab thiab xeev siab / ntuav.

Tus naj npawb tsis muaj ntawm lymphocytes

Hauv kev tshawb fawb hauv chav kho mob, qhov tshwm sim ntawm kev kuaj pom qhov txawv ntawm qhov tsis zoo yog qhov zoo sib xws hauv cov neeg mob noj saxagliptin ntawm koob tshuaj 5 mg thiab cov uas noj tshuaj.

Saxagliptin tsis tau ua rau pom txoj kev muaj mob lossis tseem ceeb rau lub platelet suav.

Kev Txo Txoj Kev Theem Vitamin Ntau Ntau ₁₂ hauv kev ntsuas ntshav, yam tsis muaj kev tshawb nrhiav, tau pom nyob hauv kwv yees li ntawm 7% ntawm cov neeg mob.

Siv thaum cev xeeb tub lossis lactation

Tsis muaj ntaub ntawv txaus rau kev siv cov tshuaj los ntawm cov poj niam cev xeeb tub.

Cov tshuaj yuav tsum tsis txhob siv thaum cev xeeb tub.

Yog tias tsim nyog, kev kho mob yuav tsum tso tseg tsis pub niam mis.

Kev nyab xeeb thiab ua tau zoo ntawm Combogliz XR hauv kev kho cov menyuam yaus tsis tau tsim.

Daim ntawv thov nta

Cov kab mob lactic acidosis yog ib qho mob uas tsis tshua pom tab sis ua mob hnyav uas tuaj yeem tsim tau los ntawm kev sib txuam nrog cov tshuaj metformin thaum kho nrog Comboglyz XR; kev tuag ntawm cov kab mob lactic acidosis yog 50%. Lactic acidosis tuaj yeem tsim txuas nrog qee yam kev mob pathophysiological, suav nrog mob ntshav qab zib mellitus, thiab tawm tsam keeb kwm ntawm cov nqaij mob hnyav hypoperfusion thiab hypoxemia. Lactic acidosis yog tus cwj pwm los ntawm kev nce hauv cov ntshav lactate ntau ntau (> 5 mmol / L), txo pH, qhov kev ua txhaum ntawm cov roj ntsha sib xyaw nrog rau kev nce ntawm lub anion interval thiab nce ntxiv ntawm qhov feem ntawm lactate / pyruvate. Yog tias metformin yog qhov ua rau cov kab mob lactic acidosis, ntshav plasma metformin feem ntau yog li 5 μg / ml. Kev tshaj tawm tias lactic acidosis hauv cov neeg mob uas tau txais cov tshuaj metformin hydrochloride muaj tsawg heev. Hauv cov ntawv tshaj tawm, lactic acidosis feem ntau tshwm sim hauv cov neeg mob ntshav qab zib thiab mob raum tsis zoo, suav nrog kev mob raum thiab lub raum hypoperfusion, feem ntau ntawm ntau cov teeb meem kev kho mob / phais mob thiab ntau cov tshuaj ntxiv. Txoj kev pheej hmoo ntawm kev tsim mob lactic acidosis tau nce ntxiv hauv cov neeg mob uas muaj lub plawv tsis ua haujlwm txaus uas yuav tsum tau muaj kev kho mob, tshwj xeeb hauv cov neeg mob uas tsis khov kho lossis mob hnyav tsis ua haujlwm nrog lub siab ntawm hypoperfusion thiab hypoxemia.

Feem ntau, qhov pib ntawm lactic acidosis yog qhov tsis meej thiab muaj nrog cov kev mob tshwj xeeb nkaus xwb xws li malaise, myalgia, ua pa nyuaj, nce siab tsaug zog, thiab tsis hnov mob tsis meej. Nrog ntau cov lus tawm acidosis, mob hypothermia, mob ntshav qab zib hypotension, thiab bradyarrhythmia tuaj yeem tshwm sim. Tus neeg mob thiab nws tus kws kho mob yuav tsum nco ntsoov qhov tseem ceeb ntawm cov tsos mob zoo li no, thiab tus neeg mob yuav tsum raug ceeb toom txog qhov yuav tsum tau ceeb toom rau kws kho mob yog tias lawv txhim kho. Metformin yuav tsum tsis ua mus ntxiv kom txog thaum qhov xwm txheej meej meej. Txhawm rau ua qhov no, koj tuaj yeem txiav txim siab txog qib electrolytes hauv ntshav dej, qib ketones, ntshav qabzib hauv cov ntshav thiab, yog tias qhia, pH ntawm cov ntshav, qib lactate thiab txawm tias qib metformin hauv ntshav.

Kev yoo plasma ntshav lactate nyob rau hauv cov ntshav, saum toj siab ntau dua, tab sis tsawg dua 5 mmol / L hauv cov neeg mob noj metformin, tsis tas yuav qhia tias muaj kev hem thawj ntawm cov kab mob lactic acidosis thiab yuav piav qhia los ntawm lwm cov txheej txheem, xws li tswj ntshav qab zib tsis zoo lossis rog rog, ua si lub cev ntau dhau lossis kev teeb meem hauv kev kuaj cov qauv.

Lactacidosis yuav tsum muaj kev ntseeg nyob hauv txhua tus neeg mob ntshav qab zib uas mob metabolic acidosis yam tsis muaj ketoacidosis (ketonuria thiab ketonemia).

Lactic acidosis yog ib qho xwm txheej ceev uas kev kho mob nqa tawm hauv tsev kho mob. Rau cov neeg mob uas muaj cov kab mob lactic acidosis uas tau siv tshuaj metformin, cov tshuaj tam sim ntawd raug muab tso tseg thiab kev txhawb nqa dav dav yog cov kws kho mob. Metformin hydrochloride yauv raug lim ntshav (nrog rau kev tshem tawm ntawm 170 ml / min. Nrog rau qhov ntsuas ntshav zoo), yog li ntawd, tam sim ntawv hemodialysis raug pom zoo rau kev kho mob acidosis thiab tshem tawm ntawm cov tshuaj metformin. Cov kev ntsuas zoo li no feem ntau ua rau muaj kev rov ua kom sai ntawm cov tsos mob thiab rov qab los.

Lub siab ua haujlwm tsis zoo

Txij li thaum lub siab ua haujlwm tsis zoo tau cuam tshuam nrog ntau kis mob lactic acidosis, kev tswj hwm ntawm Combogliz XR yuav tsum zam rau cov neeg mob kuaj mob lossis kuaj pom tias muaj kab mob siab.

Kev ntsuam xyuas lub raum kev ua haujlwm

Cov neeg mob uas muaj cov ntshav creatinine qib siab uas tsis pub tshaj qhov xwm txheej ib txwm rau lawv lub hnub nyoog yuav tsum tsis txhob txais Combogliz XR. Hauv cov neeg mob laus, Kev Siv Tshuaj Comboglize XR yuav tsum tau ua kom zoo zoo kom txog rau thaum qhov kev txhaj tshuaj tsawg kawg tau tsim los rau cov txiaj ntsig glycemic txaus, txij li lub raum ua haujlwm zuj zus nrog lub hnub nyoog. Hauv cov neeg mob laus, tshwj xeeb hauv cov neeg mob tshaj 80 xyoo, lub raum kev ua haujlwm yuav tsum tau soj ntsuam tas li, thiab, feem ntau, Comboglize XR yuav tsum tau suav rau qhov siab tshaj plaws metformin uas yog ib feem ntawm cov tshuaj.

Ua ntej pib txoj kev kho nrog Combogliz XR, thiab tom qab ntawd tsawg kawg 1 zaug hauv ib xyoos, nws yog qhov yuav tsum tau soj ntsuam lub raum thiab ua haujlwm raws li niaj zaus.

Kwv yees li 7% ntawm cov neeg mob tau txo qis vitamin B ₁₂ rau cov theem ntawm cov ntshav hauv cov ntshav uas yav dhau los sib piv rau cov qauv, tsis muaj kev kuaj mob hauv lub cev. Ib qho kev txo qis zoo sib xws, muaj vim muaj cov txiaj ntsig ntawm qhov nqus ntawm vitamin B ₁₂ nrog intrinsic factor-B complex ₁₂ yog qhov tsis tshua muaj feem cuam tshuam nrog kev mob ntshav tsis txaus thiab sai sai tom qab kev ncua metformin lossis tso tshuaj ntxiv muaj cov vitamin B ₁₂ Cov. Cov neeg mob uas siv Combogliz XR raug nquahu kom kuaj ntshav txhua xyoo, thiab txhua yam kev hloov pauv yuav tsum raug txheeb xyuas thiab kho.

Qee tus neeg (nrog kev siv tsis txaus lossis nqus cov vitamin B ₁₂ los yog calcium) yog cov yuav ua rau qis dua cov vitamin B ₁₂ hauv qab ib txwm muaj. Cov neeg mob no yuav tsum tau ua kev soj ntsuam cov qib vitamin B qib siab. ₁₂ nyob rau hauv cov ntshav ntshav nrog ncua sij hawm 2-3 xyoos.

Cawv ua kom cov nyhuv ntawm metformin rau cov lactate metabolism. Cov neeg mob yuav tsum tau ceeb toom txog kev phom sij ntawm kev haus cawv ntau dhau, ob qho tib si ntawm qee zaum thiab tsis tu ncua, thaum siv cov tshuaj Combogliz XR.

Kev siv Combogliz XR yuav tsum tsis ua rau lub sijhawm txiav tawm ib ntus (tshwj tsis yog kev cuam tshuam me uas tsis cuam tshuam txog kev txwv zaub mov lossis haus dej) thiab yuav tsum tsis siv kom txog thaum tus neeg mob tuaj yeem noj zaub mov noj thiab lub raum tsis ua haujlwm.

Hloov pauv chaw tshuaj ntawm cov neeg mob uas tiv thaiv hom mob ntshav qab zib hom II

Tus neeg mob uas mob ntshav qab zib hom II, yav dhau los tswj tau zoo nrog kev siv Combogliz XR, uas muaj qhov txawv txav ntawm kev kuaj ntshav lossis kuaj mob (tshwj xeeb tshaj yog vague lossis cov kab mob tsis zoo), yuav tsum tau ntsuas sai rau qhov muaj ketoacidosis lossis lactic acidosis.

Siv nrog cov tshuaj uas ua rau cov ntshav qab zib

Kev siv tshuaj tua kab mob insulin secretion xws li sulfonylurea ua rau cov ntshav qog ntshav qab zib. Yog li no, thaum siv ua ke nrog saxagliptin, qhov kev txo qhov koob tshuaj ntawm lub zog ntawm lub cev insulin muaj peev xwm ua kom txo qis kev pheej hmoo ntawm hypoglycemia.

Kev mob ntshav qab zib tsis tsim nyob rau hauv cov neeg mob uas tau txais cov tshuaj metformin monotherapy nyob rau hauv ib txwm mob ntawm kev siv, tab sis tej zaum yuav tshwm sim thaum noj cov zaub mov tsis muaj zaub mov ntau, thaum lub cev ua si tsis yog pab txhawb los ntawm cov tshuaj muaj kuab, lossis tiv thaiv keeb kwm ntawm kev siv txuas ntxiv ntawm lwm yam tshuaj uas txo cov piam thaj (xws li sulfonylurea thiab insulin) los yog ethyl haus cawv. Tshwj xeeb tshaj yog rhiab rau hypoglycemic kev ua yog lub caij ntuj sov thiab cov neeg mob uas tsis muaj zog, cov neeg uas noj tsis zoo, nrog adrenal tsis txaus lossis qog pituitary, nrog cawv intoxication. Hauv cov neeg mob laus thiab cov neeg mob noj beta adrenergic receptors, mob ntshav qab zib tsis tuaj yeem paub nyuaj.

Cov tshuaj tsis haum xeeb uas cuam tshuam rau lub raum kev ua haujlwm lossis metformin pharmacokinetics

Cov tshuaj tsis haum xeeb uas tuaj yeem cuam tshuam rau lub raum kev ua haujlwm lossis ua rau muaj kev hloov pauv ntshav ntau dua, lossis cuam tshuam cov pharmacokinetics ntawm metformin, xws li cov tshuaj cationic uas raug tso tawm los ntawm lub raum plab zais zis, yuav tsum siv nrog ceev faj.

Cov kev ntsuas mob radiological uas koom nrog kev tswj hwm hauv lub cev ntawm iodinated cov neeg sawv cev sib piv

Cov kev tshawb fawb nrog kev saib xyuas intravascular ntawm cov tshuaj tiv thaiv iodinated ua rau cov neeg tuaj yeem ua rau lub raum tsis ua haujlwm ntawm lub raum thiab tau cuam tshuam nrog cov kab mob lactic acidosis hauv cov neeg mob uas tau txais tshuaj metformin.

Nrog cov kab mob lactic acid cuam tshuam txog kev mob plawv rau lub plawv poob qis (poob siab) rau ib qho laj thawj, mob tsis txaus ntseeg lub plawv tsis ua haujlwm, mob myocardial infarction thiab lwm yam kab mob tshwm sim los ntawm kev loj hlob ntawm hypoxemia thiab tseem tuaj yeem ua rau prerenal azotemia. Thaum cov kab mob no tshwm sim hauv cov neeg mob uas tau txais Combogliz XR, cov tshuaj yuav tsum tau muab ncua sai.

Poob ntawm cov ntshav qabzib tswj

Yog tias ib tug neeg mob uas nws tus mob tau hloov kho nyob rau hauv ib qho kev mob ntshav qab zib muaj qhov mob xws li kub ib ce, mob, mob kis, lossis phais, ib ntus ntawm glycemic tswj yuav tshwm sim. Thaum zoo li no, nws yuav tsim nyog yuav tsum txiav tawm Combogliz XR thiab muab tshuaj insulin ib ntus. Noj Combogliz XR yuav rov pib dua los sab laj tswv yim tawm tsam tsis zoo.

Vascular cov teebmeem

Cov kev tshawb fawb soj ntsuam uas tau muab cov pov thawj ua tiav ntawm kev txo qis kev pheej hmoo ntawm kev pheej hmoo ntawm kev muaj mob macrovascular nrog kev siv Combogliz XR lossis lwm yam tshuaj tiv thaiv kab mob tsis tau ua.

Siv rau cov neeg mob laus

Txij li thaum saxagliptin thiab metformin raug qee tawm los ntawm lub raum thiab feem ntau lub raum ua haujlwm raug txo qis hauv cov neeg mob laus, Comboglize XR yuav tsum siv nrog ceev faj hauv cov neeg laus.

Saxagliptin. Tsis muaj qhov sib txawv hauv cov tshuaj tiv thaiv thaum lub caij ntuj sov thiab cov neeg hluas, tab sis qhov kev rhiab ntawm qee tus neeg laus dua tsis tuaj yeem txiav txim tau.

Metformin hydrochloride. XR comboglyz tsuas yog siv rau hauv cov neeg mob uas lub raum tsis ua haujlwm. Qhov pib thiab saib xyuas cov koob tshuaj metformin yuav tsum nyob ruaj khov rau cov neeg laus vim tias qhov ua kom lub raum tsis ua haujlwm nyob hauv pawg neeg mob no. Kev hloov koob tshuaj yuav tsum tau ua tom qab kev ntsuas kom paub meej ntawm lub raum ua haujlwm.

Tsis muaj cov kev tshawb fawb tshwj xeeb tau ua los kawm txog kev nyab xeeb thiab ua tau zoo ntawm Combogliz XR hauv cov neeg mob yav tas los kho nrog lwm tus neeg tuaj yeem tiv thaiv kab mob thiab tom qab ntawd pauv mus rau Combogliz XR.

Ib qho pauv hloov ntawm kev kho mob ntshav qab zib hom II yuav tsum tau ua tib zoo ua thiab tswj hwm tas mus li, vim tias yuav muaj kev hloov pauv hauv glycemic tswj.

Cov neeg mob nrog pancreatitis. Thaum lub sijhawm kev tshawb fawb txog kev tshaj tawm tom qab muag, cov lus ceeb toom ntawm kab mob pancreatitis tau txais. Cov neeg mob yuav tsum tau qhia paub txog cov yam ntxwv ntawm tus yam ntxwv mob sai sai: mob plab tas mus li. Yog pom tias muaj tus mob pancreatitis, XR Kev Ntaus Tus Cuam Tshuam yuav tsum tsis ua mus ntxiv.

Lub plawv tsis ua hauj lwm. Hauv txoj kev tshawb nrhiav SAVOR, qhov tshwm sim ntawm tsev kho mob vim lub plawv tsis ua haujlwm hauv cov neeg mob uas tau txais saxagliptin tau ntau dua li cov uas tau txais cov placebo, txawm hais tias kev sib raug zoo hauv tsev tsis tau tsim. Ceev faj yog qhia kom siv Comboglize XR rau cov neeg mob uas paub txog kev pheej hmoo txaus rau kev mus pw hauv tsev kho mob vim lub plawv tsis ua haujlwm, xws li keeb kwm ntawm lub plawv tsis ua haujlwm lossis mob hnyav los sis mob raum. Cov neeg mob yuav tsum paub txog cov xeeb ceem ntawm lub plawv tsis ua hauj lwm thiab qhia kom ceeb toom tam sim qhov tshwm sim ntawm cov tsos mob no.

Mob hnyav thiab muaj peev xwm tiv thaiv mob pob txha. Hauv lub sijhawm sau npe tom qab, cov mob ntawm kev mob hnyav thiab xiam oob qhab tau kaw nrog kev siv DPP-4 inhibitors. Lub sijhawm pib ntawm cov tsos mob muaj nyob rau ib hnub txog ntau xyoo tom qab pib kev kho mob. Qhov tsis txaus ntseeg ntawm cov tsos mob txo qis tom qab tsis cuam tshuam nrog cov tshuaj. Qee tus neeg mob tau rov tshwm sim dua cov tsos mob tom qab rov pib kho txoj kev kho mob nrog tib cov tshuaj los yog sau ntawv rau lwm tus DPP-4 inhibitor.

Lub peev xwm los cuam tshuam cov tshuaj tiv thaiv tus nqi thaum tsav tsheb lossis ua haujlwm nrog lwm cov txheej txheem.

Qhov kev tshawb nrhiav ntawm qhov ntxim rau ntawm kev muaj peev xwm tsav tsheb thiab kev ua haujlwm nrog cov txheej txheem tsis tau ua. Muab rau pom tias kiv taub hau yog qhov tshwm sim tsis zoo, lub sijhawm kho yuav tsum tsis txhob tsav tsheb lossis ua haujlwm nrog cov txheej txheem.

Kev sib cuam tshuam nrog lwm yam tshuaj thiab lwm yam kev sib cuam tshuam

Enzyme Inducers CYP3A4 / 5

Saxagliptin. Rifampicin tseem ceeb attenuated raug rau saxagliptin, tsis yog nrog los ntawm kev hloov hauv thaj chaw hauv qab qhov nkhaus-sijhawm nkhaus (AUC) ntawm nws cov metabolite, 5-hydroxyaxaxagliptin. Rifampicin tsis cuam tshuam qhov inhibition ntawm ntshav ntshav dipeptidyl peptidase-4 (PPP-4) kev ua haujlwm dhau 24 teev. Yog li, kev kho qhov koob tshuaj saxagliptin tsis pom zoo.

CYP3A4 / 5 Cov Khoom Siv Enzyme

Ntsig CYP3A4 / 5 Tus Inhibitionitors

Saxagliptin. Diltiazem qhov ua kom zoo rau saxagliptin. Zoo sib xws hauv plasma concentration ntawm saxagliptin yog xav tias muaj lwm cov kev txwv tsis pub muaj cytochrome P450 3A4 / 5 (CYP3A4 / 5) (e.g., amprenavir, aprepitant, erythromycin, fluconazole, fosamprenavir, txiv kab ntxwv qaub kua txiv thiab verapamil). Txawm li cas los xij, kev kho qhov koob tshuaj saxagliptin tsis pom zoo.

Lub Cev Muaj Zog CYP3A4 / 5 Kev Tso Tseg

Ketoconazole tau nce ntau ntxiv rau kev cuam tshuam rau saxagliptin. Qhov zoo sib xws nce ntxiv hauv plasma cov ntsiab lus ntawm saxagliptin yog xav tias muaj lwm qhov muaj zog CYP3A4 / 5 inhibitors (e.g., atazanavir, clarithromycin indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir thiab telithromycin).

Raws li kev xav, tshuaj cationic (piv txwv li, amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamteren, trimethoprim lossis vancomycin), uas yog tawm los ntawm cov hlab ntsws ua kom tiav, tuaj yeem sib cuam tshuam nrog metformin, sib tw rau kev sib koom ua ke tubular thauj. Cov kev sib thooj zoo sib xws ntawm metformin thiab cimetidine rau kev tswj hwm qhov ncauj tau pom nyob rau hauv cov neeg tuaj yeem noj qab haus huv hauv kev tshawb fawb txog kev sib cuam tshuam ntawm metformin thiab cimetidine ob qho tib si nrog ib koob thiab nrog ntau koob, thiab ib qho kev nce siab tshaj plaws tau pom (C _max ) metformin hauv plasma thiab tag nrho cov ntshav tau 60% thiab nce AUC ntawm metformin ntawm 40% hauv plasma thiab tag nrho cov ntshav tau 40%. Hauv kev tshawb fawb ib zaug xwb, ib nrab-lub neej tsis tau pauv. Metformin tsis cuam tshuam dabtsi rau pharmacokinetics ntawm cimetidine. Txawm hais tias kev sib cuam tshuam zoo li no yog theoretical (tshwj tsis yog kev sib txuam nrog cimetidine), nws raug nquahu kom kuaj xyuas feem ntau ntawm cov neeg mob thiab kho cov koob tshuaj ntawm Comboglyz XR thiab / lossis cuam tshuam cov tshuaj yog tias cov neeg mob no siv tshuaj cationic uas raug tso tawm los ntawm qhov ze ntawm lub raum tubular excretory system.

Hauv tib qho kev kawm cuam tshuam rau cov neeg mob uas muaj ntshav qab zib hom II, kev tswj hwm ntawm metformin thiab glibenclamide tsis hloov pauv tsis tau rau hauv cov chaw muag tshuaj los yog cov chaw muag tshuaj ntawm metformin. AUC thiab C poob qis _max glibenclamide, tab sis cov xwm txheej no tsis txawv txav heev. Txij li thaum qhov kev tshawb fawb no tau siv ib zaug, thiab tsis muaj kev sib txheeb ntawm cov qib ntawm glibenclamide hauv cov ntshav thiab cov nyhuv ntawm pharmacodynamics, qhov tseem ceeb hauv kev kho mob ntawm kev sib cuam tshuam no tseem tsis tau paub meej.

Kev kawm txog kev cuam tshuam ntawm kev sib xyaw ntawm metformin thiab furosemide siv ib koob tshuaj nrog kev koom tes ntawm cov neeg tuaj yeem noj qab haus huv tau qhia txog cov txiaj ntsig ntawm kev sib koom tes ntawm pharmacokinetic cov tshuaj ntawm ob qho tshuaj.

Kev kawm txog kev cuam tshuam ntawm metformin thiab nifedipine nrog tib koob hauv cov neeg tuaj yeem noj qab haus huv pom tau tias kev sib koom tes nrog nifedipine nce tus nqi ntawm C _max thiab AUC ntawm metformin hauv plasma los ntawm 20% thiab 9%, ntsig txog, thiab nce cov tshuaj uas tso rau hauv cov zis. Tus nqi T _max thiab ib nrab-lub neej tsis tau pauv. Nifedipine txhim kho kev nqus ntawm metformin. Cov nyhuv ntawm metformin ntawm nifedipine yog qhov tsawg heev.

Siv nrog lwm cov tshuaj

Qee cov tshuaj tuaj yeem ua rau hyperglycemia thiab tuaj yeem ua rau poob ntawm kev tswj cov ntshav hauv lub cev. Cov tshuaj no suav nrog thiazides thiab lwm cov tshuaj diuretics, corticosteroids, phenothiazides, cov thyroid hormones npaj, estrogens, qhov ncauj tawm tsam, phenytoin, nicotinic acid, sympathomimetics, calcium channel blockers thiab isoniazid. Thaum muab cov nyiaj tawm mus rau tus neeg mob tau txais Combogliz XR, nws yog ib qho tsim nyog yuav tau soj ntsuam xyuas cov cim kom tsis txhob muaj kev tswj hwm ntawm cov ntshav qabzib nyob hauv tus neeg mob. Thaum cov tshuaj no raug muab tso tseg hauv tus neeg mob uas tau txais Combogliz XR, nws yuav tsum tau saib xyuas tus neeg mob kom zoo tsis txhob mob hypoglycemia

Hauv cov neeg tuaj yeem noj qab haus huv, thaum sib koom tes ua ib feem ntawm kev tshawb fawb txog kev sib txuam nrog ib koob tshuaj, cov kws kho mob ntawm metformin thiab propanolol, nrog rau metformin thiab ibuprofen, tsis hloov.

Metformin tsis cuam tshuam tseem ceeb rau cov ntshav plasma protein; yog li ntawd, nws cov kev cuam tshuam nrog cov tshuaj uas khi rau cov protein kom ntau (xws li salicylates, sulfonamides, chloramphenicol thiab probenecid) tsis zoo li piv rau sulfonylureas, uas ntau txuas rau cov ntshav plasma protein.

Kev sib cuam tshuam txog yeeb tshuaj

Saxagliptin thiab Metformin Hydrochloride

Kev siv ntau yam tshuaj ib zaug ntawm saxagliptin (100 mg) thiab metformin (1000 mg) tsis hloov pauv pharmacokinetics ntawm saxagliptin lossis metformin hauv cov neeg ua haujlwm noj qab haus huv.

Cov kev tshawb fawb tshwj xeeb ntawm kev sib txuam pharmacokinetic ntawm cov tshuaj nrog kev siv Combogliz XR tseem tsis tau ua, txawm hais tias kev tshawb fawb zoo sib xws tau coj los siv sib txawv saxagliptin thiab cais metformin.

Hauv tshuaj lom tshuaj vitro tsom xam

Saxagliptin metabolism feem ntau yog kho los ntawm CYP3A4 / 5.

Hauv hauv vitro Hauv kev tshawb fawb, saxagliptin thiab nws cov tshuaj tiv thaiv metabolite tshem tawm CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 lossis 3A4 tab sis tsis tau txhawb CYP1A2, 2B6, 2C9 lossis 3A4.

Qhov khi ntawm saxagliptin thiab nws cov metabolite rau cov protein hauv vitro nyob rau hauv tib neeg cov ntshav yog negligible. Yog li, kev khi cov protein yuav tsis muaj kev cuam tshuam tseem ceeb ntawm pharmacokinetics ntawm saxagliptin lossis lwm yam tshuaj.

Hauv vivo tshuaj sib cuam tshuam tshuaj ntsuam

Cov nyhuv ntawm saxagliptin rau lwm yam tshuaj

Hauv kev tshawb fawb, saxagliptin tsis hloov pauv ntau yam ntawm cov khw muag tshuaj ntawm metformin, glibenclamide, pioglitazone, digoxin, simvastatin, diltiazem, thiab ketoconazole.

Metformin. Kev siv tib lub sij hawm ntawm saxagliptin (100 mg) thiab metformin (1000 mg), cov hauv qab hOCT-1 thiab hOCT-2, tsis hloov pauv pharmacokinetics ntawm metformin hauv cov neeg muaj kev noj qab haus huv. Yog li, saxagliptin tsis yog qhov khoo hOCT-1 thiab hOCT-2-mediated thauj.

Gliburide. Raws li kev txiav txim siab ntawm kev tswj hwm ib zaug ntawm saxagliptin (10 mg) thiab glibenclamide (5 mg), ib qho keeb ntawm CYP2C9, Cmax tus nqi ntawm glibenclamide hauv ntshav plasma nce 16%. Txawm li cas los xij, AUC tus nqi ntawm glibenclamide tsis hloov pauv. Yog li, saxagliptin yuav luag tsis thaiv cov metabolism hauv kev sib kho los ntawm CYP2C9.

Pioglitazone. Raws li qhov tshwm sim ntawm kev siv cov tshuaj concomitant (ib zaug ib hnub) ntawm ntau yam tshuaj saxagliptin (10 mg) thiab pioglitazone (45 mg), cov CYP2C8, cov Cmax tus nqi ntawm pioglitazone hauv cov ntshav ntshav tau nce 14%. Txawm li cas los xij, AUC tus nqi ntawm pioglitazone tsis hloov pauv. Yog li, saxagliptin tseem ceeb tsis txo qis lossis txhim kho cov metabolism hauv CYP2C8.

Digoxin. Hauv raws li qhov tshwm sim ntawm kev siv concomitant (ib zaug ib hnub) ntawm ntau yam tshuaj saxagliptin (10 mg) thiab digoxin (0.25 mg), cov P-gp, cov tshuaj pharmacokinetics ntawm digoxin tsis hloov. Yog li, saxagliptin tsis yog ib qho inhibitor tsis yog qhov inducer ntawm P-gp kho kom haum xeeb hloov.

Simvastatin. Raws li qhov txiaj ntsig ntawm kev siv concomitant (ib zaug ib hnub) ntawm ntau yam tshuaj saxagliptin (10 mg) thiab simvastatin (40 mg), cov kab mob CYP3A4 / 5, lub pharmacokinetics ntawm simvastatin tsis hloov pauv. Yog li, saxagliptin tsis yog ib qho tsis haum thiab tsis muaj qhov cuam tshuam ntawm cov metabolism hauv nruab nrab los ntawm CYP3A4 / 5.

Diltiazem. Raws li kev siv cov tshuaj concomitant (ib zaug ib hnub) ntawm ntau yam tshuaj saxagliptin (10 mg) thiab diltiazem (360 mg, ntev ntev ntawm daim ntawv noj tshuaj ntawm qhov sib npaug), qhov ntsuas tsis txaus ntawm CYP3A4 / 5, tus nqi ntawm Cmax ntawm diltiazem hauv ntshav ntshav nce ntxiv 16%. Txawm li cas los xij, AUC tus nqi ntawm diltiazem tsis tau hloov pauv.

Ketoconazole Raws li ib qho txiaj ntsig ntawm concomitant siv ib koob tshuaj saxagliptin (100 mg) thiab

Tso tawm daim ntawv, muaj pes tsawg leeg thiab ntim khoom

Zaj Duab Xis Tso Daim Qauv Duab Tsoo Tso Tawm. Ib ntsiav tshuaj muaj: Cov tshuaj nquag: metformin - 1000 mg, saxagliptin - 2.5 mg. 7 Pcs - hlwv (4) - pob khoom los ntawm cardboard.
7 Pcs - hlwv (8) - pob khoom los ntawm cardboard.

Zaj Duab Xis Tso Daim Qauv Duab Tsoo Tso Tawm. Ib ntsiav tshuaj muaj: Cov tshuaj nquag: metformin - 1000 mg, saxagliptin - 5 mg. 7 Pcs - hlwv (4) - pob khoom los ntawm cardboard.

Zaj Duab Xis Tso Daim Qauv Duab Tsoo Tso Tawm. Ib ntsiav tshuaj muaj: Cov tshuaj nquag: metformin - 500 mg, saxagliptin - 5 mg. 7 Pcs - hlwv (4) - pob khoom los ntawm cardboard.

Yeeb tshuaj sib cuam tshuam

Qee cov tshuaj nce hyperglycemia (thiazide thiab lwm yam diuretics, glucocorticosteroids, phenothiazines, kev npaj ntawm iodine-muaj cov thyroid hormones, estrogens, qhov ncauj tawm tsam, phenytoin, nicotinic acid, sympathomimetics, qeeb calcium channel blockers thiab isoniazid). Thaum sau ntawv lossis tso tseg cov tshuaj no rau hauv tus neeg mob noj Combogliz, kev saib xyuas cov piam thaj hauv cov ntshav yuav tsum tau ua tib zoo saib. Qhov sib khi ntawm metformin rau cov ntshav plasma proteins muaj tsawg, yog li nws tsis pom zoo tias nws yuav cuam tshuam nrog cov tshuaj uas cuam tshuam rau cov ntshav plasma protein ntau, xws li salicylates, sulfonamides, chloramphenicol thiab probenecid (hauv kev sib piv ntawm sulfonylurea derivatives, uas muaj ntau yam tseem ceeb) nrog cov ntshiab protein).

Qhov ntsuas ntawm isoenzymes CYP3A4 / 5

Rifampicin cuam tshuam txo qis kev cuam tshuam ntawm saxagliptin yam tsis hloov AUC ntawm nws cov nquag metabolite, 5-hydroxy-saxagliptin. Rifampicin tsis cuam tshuam rau qhov kev txwv tsis pub DPP-4 nyob rau hauv cov ntshav ntshav thaum lub sijhawm 24-teev kev kho mob.

CYP3A4 / 5 Isoenzyme Tus Neeg Txom Nyem

Diltiazem txhim kho kev muaj txiaj ntsig ntawm saxagliptin thaum siv ua ke. Kev nce siab ntawm saxagliptin nyob rau hauv cov ntshav ntshav yog yuav tsum siv amprenavir, aprepitant, erythromycin, fluconazole, fosamprenavir, kua txiv kab ntxwv qaub thiab verapamil, txawm li cas los xij, koob tshuaj saxagliptin tsis pom zoo. Ketoconazole ua rau ntau cov kev xav ntawm saxagliptin hauv ntshav. Ib qho zoo sib xws tseem ceeb ntxiv rau qhov kev txiav txim ntawm saxagliptin hauv cov ntshav ntshav yog xav tau thaum lwm qhov muaj zog inhibitors ntawm nzoenzymes CYP3A4 / 5 tau siv (piv txwv, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir). Thaum muab sib xyaw nrog ib qho muaj zog inhibitor ntawm CYP3A4 / 5 isoenzymes, qhov koob tshuaj saxagliptin yuav tsum txo kom tsawg li 2.5 mg.

Cov tshuaj Cationic (e.g., amiloride, digoxin, morphine, procainamide, quinidine, quinine, ranitidine, triamterone, trimethoprim lossis vancomycin), uas yog tawm los ntawm lub raum los ntawm kev lim ntshav, txhawm rau qhov kev sib txuas lus nrog metformin, kev sib tw rau cov kev thauj mus los ntawm cov leeg. Hauv kev tshawb fawb txog kev sib cuam tshuam yeeb tshuaj ntawm metformin thiab cimetidine nrog ib zaug thiab rov ua dua ntawm cov tshuaj, kev sib cuam tshuam ntawm metformin thiab cimetidine rau kev tswj hwm qhov ncauj hauv kev noj qab haus huv tau pom, nrog 60% nce ntxiv ntawm qhov siab tshaj plaws ntawm metformin hauv plasma thiab tag nrho cov ntshav thiab nce 40% hauv AUC ntawm metformin hauv plasma thiab tag nrho ntshav. Metformin tsis cuam tshuam rau pharmacokinetics ntawm cimetidine. Nws raug nquahu kom ua tib zoo saib xyuas cov neeg mob thiab, yog tias tsim nyog, kho cov koob tshuaj rau cov neeg mob noj tshuaj cationic uas raug tso tawm los ntawm qhov siab nyob ze lub plab hlaub.

Hauv kev kawm txog kev sib cuam tshuam yeeb tshuaj ntawm metformin thiab furosemide nrog ib zaug ntawm cov tshuaj, ua rau cov neeg ua haujlwm noj qab haus huv, lawv cov kev sib raug zoo pharmacokinetic tau qhia. Furosemide nce Cmax ntawm metformin hauv plasma thiab ntshav los ntawm 22% thiab AUC hauv ntshav li 15% yam tsis muaj kev hloov pauv tseem ceeb hauv kev ua haujlwm ntawm lub raum tshem tawm ntawm metformin. Thaum ua ke nrog metformin, Cmax thiab AUC, furosemide tsawg dua 31% thiab 12%, feem, thiab ib nrab lub neej txo qis los ntawm 32% yam tsis muaj qhov pom tseeb ntawm kev hloov ua kom zoo ntawm furosemide. Tsis muaj cov ntaub ntawv hais txog kev cuam tshuam ntawm metformin thiab furosemide nrog ua ke siv ntev.

Hauv kev kawm txog kev sib txuas yeeb tshuaj-tshuaj ntawm metformin thiab nifedipine nrog ib koob tshuaj, ua rau cov neeg tuaj yeem noj qab haus huv, nifedipine nce Cmax ntawm plasma metformin los ntawm 20% thiab AUC los ntawm 9%, thiab nce raum ntxiv rau lub raum. Tmax thiab T1 / 2 tsis hloov. Nifedipine tsub kom ntau ntxiv kev nqus ntawm metformin. Metformin tsis muaj kev cuam tshuam zoo li ntawm cov tshuaj pharmacokinetics ntawm nifedipine.

Saxagliptin thiab Metformin

Kev sib xyaw ntawm kev siv ib zaug ntawm saxagliptin (100 mg) thiab metformin (1000 mg) tsis muaj kev cuam tshuam ntau yam ntawm cov tshuaj pharmacokinetics ntawm saxagliptin lossis metformin hauv cov neeg ua haujlwm noj qab haus huv. Tsis muaj kev kawm tshwj xeeb pharmacokinetic txog kev sib txuam nrog tshuaj nrog kev siv ntawm Combogliz tau ua, txawm hais tias cov kev tshawb fawb no tau ua nrog nws cov khoom siv: saxagliptin thiab metformin.

Cov nyhuv ntawm lwm cov tshuaj ntawm saxagliptin

Glibenclamide: Kev siv tib lub saxagliptin (10 mg) thiab glibenclamide (5 mg), ib qho pauv ntawm isoenzyme CYP2C9, nce Cmax ntawm saxagliptin los ntawm 8%, txawm li cas los xij, saxagliptin AUC tsis hloov pauv.

Pioglitazone: Cov kev sib xyaw ua ke siv dua ntawm saxagliptin ib zaug ib hnub (10 mg) thiab pioglitazone (45 mg), cov kab mob hauv isoenzyme CYP2C8 (muaj zog) thiab CYP3A4 (tsis muaj zog), tsis cuam tshuam rau pharmacokinetics ntawm saxagliptin.

Digoxin: Cov tshuaj sib xyaw ua ke siv saxagliptin ib zaug ib hnub (10 mg) thiab digoxin (0.25 mg), ib qho tshuaj P-glycoprotein, tsis cuam tshuam rau lub pharmacokinetics ntawm saxagliptin.

Simvastatin: Kev sib xyaw ua ke rov qab siv saxagliptin ib zaug ib hnub (10 mg) thiab simvastatin (40 mg), ib qho pauv ntawm CYP3A4 / 5 isoenzymes, nce Cmax ntawm saxagliptin los ntawm 21%, txawm li cas los xij, saxagliptin AUC tsis hloov pauv.

Diltiazem: Kev siv tib yam ntawm saxagliptin (10 mg) thiab diltiazem (360 mg ntev npaum li cas hauv tshuaj sib npaug), qhov ntsuas mob tsis txaus ntawm isoenzymes CYP3A4 / 5, nce Cmax ntawm saxagliptin los ntawm 63%, thiab AUC - los ntawm 2.1 zaug. Qhov no yog nrog los ntawm qhov txo qis hauv Cmax thiab AUC ntawm cov metabolite nquag los ntawm 44% thiab 36%, feem.

Ketoconazole: Kev sib xyaw ua ke ntawm kev siv ib koob tshuaj saxagliptin (100 mg) thiab ketoconazole (200 mg txhua 12 teev hauv kev sib npaug) nce Cmax thiab AUC ntawm saxagliptin 2.4 thiab 3.7 npaug, ntsig txog. Qhov no yog nrog los ntawm qhov txo qis hauv Cmax thiab AUC ntawm cov metabolite nquag los ntawm 96% thiab 90%, feem.

Rifampicin: Kev sib xyaw ua ke ntawm kev siv ib koob tshuaj saxagliptin (5 mg) thiab rifampicin (600 mg ib hnub ib zaug hauv qhov sib luag) txo qis Cmax thiab AUC ntawm saxagliptin los ntawm 53% thiab 76%, feem ntau, nrog sib luag hauv Cmax (39%), tab sis tsis muaj qhov tseem ceeb AUC hloov pauv hauv cov nquag metabolite.

Omeprazole: Kev sib xyaw ua ke siv ntau yam saxagliptin ntawm koob tshuaj 10 mg ib hnub ib zaug thiab omeprazole ntawm koob tshuaj 40 mg, ib qho tshuaj tiv thaiv isoenzyme CYP2C19 (muaj zog) thiab isoenzyme CYP3A4 (qaug zog), ib qho inhibitor ntawm isoenzyme CYP2C19 thiab tus tshuaj tsis cuam tshuam.

Aluminium hydroxide + magnesium hydroxide + simethicone: Kev sib xyaw ua ke ntawm kev siv ib zaug ntawm saxagliptin (10 mg) thiab kev ncua uas muaj txhuas hydroxide (2400 mg), magnesium hydroxide (2400 mg) thiab simethicone (240 mg), txo Cmax ntawm saxagliptin los ntawm 26%, txawm li cas los AUC saxagliptin tsis hloov.

Famotidine: Noj ib koob tshuaj saxagliptin (10 mg) 3 teev tom qab txhaj koob tshuaj famotidine (40 mg), ib qho inhibitor ntawm hOCT-1, hOCT-2, thiab hOCT-3, nce Cmax ntawm saxagliptin los ntawm 14%, tab sis AUC ntawm saxagliptin tsis hloov.

Cev xeeb tub thiab lactation

Vim tias qhov tseeb hais tias kev siv tshuaj yeeb tshuaj Comboglis thaum cev xeeb tub tsis tau kawm, cov tshuaj yuav tsum tsis txhob siv tshuaj thaum cev xeeb tub.

Kuj tsis paub meej tias saxagliptin lossis metformin kis mus rau leej niam cov kua mis tau li cas. Txij li thaum ua tau ntawm kev nkag mus ntawm cov tshuaj Combogliz rau hauv niam cov kua mis tsis raug cais tawm, kev siv cov tshuaj thaum lub sijhawm lactation yog contraindicated.

Yuav siv li cas rau cov tshuaj Comboglize?

Comboglize yog ib qho tshuaj zoo siv nyob rau hauv txoj kev kho mob ntawm cov ntshav qab zib hom 2. Pab ua kom cov ntshav qab zib ib txwm. Cov muaj pes tsawg leeg suav nrog 2 kev ua ub ua no, uas tuaj yeem tso cai rau koj siv ntau yam twj.