Jardins - malangizo * ogwiritsidwa ntchito

MALANGIZO
pa kugwiritsa ntchito mankhwalawa
JARDINS

Kutulutsa Fomu
mapiritsi okhala ndi filimu

Kupanga
Piritsi limodzi lili:
yogwira mankhwala: empagliflozin 10 ndi 25 mg
zotuluka: lactose monohydrate, microcrystalline cellulose, hyprolose (hydroxypropyl cellulose), croscarmellose sodium, colloidal silicon dioxide, magnesium stearate.
kapangidwe ka kanema: opadry chikasu (02B38190) (hypromellose 2910, titanium dioxide (E171), talc, macrogol 400, utoto wachikasu wachitsulo (E172).

Kulongedza
10 ndi 30 mapiritsi.

Zotsatira za pharmacological
Jardins - Type 2 Sodium Glucose Transporter Inhibitor

Jardins, zikuwonetsa kuti mugwiritse ntchito
Type 2 matenda a shuga:
monga monotherapy odwala omwe ali ndi vuto lokwanira la glycemic kokha motsutsana ndi maziko azakudya ndi masewera olimbitsa thupi, kusankha metformin yomwe imawonedwa ngati yosayenera chifukwa cha tsankho,
monga kuphatikiza mankhwala ndi ena othandizira a hypoglycemic, kuphatikiza insulin, pamene mankhwalawa amagwiritsidwa ntchito molumikizana ndi zakudya komanso kuchita masewera olimbitsa thupi samapereka kuyenera kwa glycemic.

Contraindication
Hypersensitivity ku gawo lililonse la mankhwala,
mtundu 1 shuga
matenda ashuga ketoacidosis,
zovuta za cholowa (kuperewera kwa lactase, tsankho lactose, shuga wa galactose malabsorption),
kulephera kwaimpso ndi GFR ×

Fomu ya Mlingo:

Kufotokozera
Mapiritsi 10 mg
Mapiritsi ozungulira a biconvex okhala ndi mbali zometedwa, atakutidwa ndi utoto wowoneka bwino wachikasu wokhala ndi chithunzi cha kampani mbali ina ya piritsi ndi "S10" mbali inayo.
25 mg mapiritsi
Mapiritsi a ovic biconvex okhala ndi mbali zopindika, zokutira ndi utoto wamafuta owala achikasu, wolemba dzina la kampani mbali ina ya piritsi ndi "S25" mbali inayo.

Mankhwala

Pharmacokinetics
Ma pharmacokinetics a empagliflozin adaphunziridwa kwathunthu mu odzipereka athanzi komanso odwala omwe ali ndi matenda a shuga a mtundu wachiwiri.
Zogulitsa
Pambuyo pakukonzekera pakamwa, empagliflozin idayamba kugwira ntchito mwachangu, kuchuluka kwakukulu kwa empagliflozin m'madzi a m'magazi (Cmax) kunafika pambuyo pa maola 1.5. Kenako, kuchuluka kwa empagliflozin mu plasma kunachepa m'magawo awiri.
Atalandira empagliflozin, dera wamba pansi pa ndende ya nthawi-yocheperako (AUC) yolumikizidwa nthawi yayitali inali 4740 nmol x h / l, ndi Cmax - 687 nmol / l.
Ma pharmacokinetics a empagliflozin mwa odzipereka athanzi komanso odwala omwe ali ndi matenda a shuga a 2 anali ofanana.
Kudya sikukhala ndi vuto lililonse pama pharmacokinetics a empagliflozin.
Kugawa
Kuchuluka kwa magawidwe panthawi ya plasma yosasunthika kunali pafupifupi malita 73.8. Pambuyo pakulankhula pakamwa ndi odzipereka athanzi olembedwa enagliflozin 14 C, mapuloteni am'magazi a plasma anali 86%.
Kupenda
Njira yayikulu yogwiritsira ntchito mphamvu ya metabolaguriflozin mwa anthu ndi glucuronidation ndikuchita nawo uridine-5'-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9. Ma metabolites omwe amadziwika kwambiri a empagliflozin ndi ma glucuronic conjugates atatu (2-0, 3-0 ndi 6-0 glucuronides). Mphamvu ya metabolite iliyonse imakhala yochepa (zosakwana 10% ya mphamvu yonse ya empagliflozin).
Kuswana
Kuchotsa theka-moyo anali pafupifupi maola 12.4. Pankhani yogwiritsa ntchito empagliflozin kamodzi patsiku, ndende ya plasma yokhazikika idakwaniritsidwa pambuyo pa mlingo wachisanu. Pambuyo m`kamwa makonzedwe olembedwa enagliflozin 14 C odzipereka athanzi, pafupifupi 96% ya mlingo anachotsedwa (m'matumbo 41% ndi impso 54%). Kudzera m'matumbo, mankhwala ambiri omwe adalembedwa kuti anali osasinthika sanasinthidwe. Hafu imodzi yokha yolembedwa yomwe idatulutsidwa ndi impso ndi yosasinthika.
Pharmacokinetics mwapadera odwala odwala
Matenda aimpso
Odwala omwe ali ndi vuto lochepa, ochepa komanso owonjezera aimpso (30 2) komanso odwala omwe amalephera kusintha kwa impso, AUC ya empagliflozin inakula, motero, pafupifupi 18%, 20%, 66%, ndi 48% poyerekeza ndi odwala omwe ali ndi vuto labwinobwino ntchito impso. Odwala omwe amalephera kupweteka aimpso komanso odwala omwe amalephera kusintha kwa impso, kuchuluka kwa plasma ndende ya empagliflozin kunali kofanana ndi mfundo zomwe zimagwirizana ndi odwala omwe ali ndi vuto laimpso. Odwala omwe ali ndi vuto lochepa kwambiri komanso aimpso, pazipita plasma ndende ya empagliflozin anali pafupifupi 20% kuposa omwe ali ndi vuto laimpso. Zotsatira za kusanthula kwa anthu a zakumwa zamtundu wa anthu zidawonetsa kuti chiwonetsero chonse cha empagliflozin chatsika ndikuchepa kwa GFR, zomwe zidapangitsa kuti chiwopsezo cha mankhwalawo chikwanire.
Kuwonongeka kwa chiwindi
Odwala omwe ali ndi vuto la chiwindi chofatsa, modekha komanso mwamphamvu kwambiri (malinga ndi gulu la ana-Pugh), mfundo za AUC za empagliflozin zimakula, motero, pafupifupi 23%, 47% ndi 75%, ndi mfundo za Stax, motsatana, pafupifupi 4%, 23 % ndi 48% (poyerekeza ndi odwala omwe ali ndi chiwindi chokwanira).
Mndandanda wamasamba ambiri, jenda, mtundu ndi zaka sanakhale ndi chiwonetsero chamatenda kwambiri pa pharmacokinetics of empagliflozin.
Ana
Maphunziro a pharmacokinetics a empagliflozin mwa ana sanachitike.

Contraindication

• Hypersensitivity ku gawo lililonse la mankhwala,
• Mtundu woyamba wa shuga
• Matenda a shuga ketoacidosis
• Mavuto obadwa nawo obwera chifukwa cha kuchepa kwa thupi (lactase kuchepa, tsankho lactose, glucose-galactose malabsorption),
• Kulephera kwina ku GFR 2 (chifukwa cha kusakwanira),
• Mimba komanso kuyamwa,
• Zoposa zaka 85
• Kugwiritsa ntchito kuphatikiza kwa glucagon-peptide 1 (chifukwa cha kusowa kwa chidziwitso pakuchita bwino ndi chitetezo),
• Ana ochepera zaka 18 (chifukwa chosakwanira ndi chidziwitso chokwanira ndi chitetezo).

Zotsatira zoyipa
Zomwe zimachitika nthawi zambiri zovuta kwa odwala omwe amalandila empagliflozin kapena placebo pamavuto azachipatala zinali zofanana. Chotsatira chovuta kwambiri chinali hypoglycemia, chomwe chimagwiritsidwa ntchito ndi empagliflozin kuphatikiza ndi sulfonylurea kapena zotumphukira za insulin (onani kufotokozera kwa zovuta zina).
Zotsatira zoyipa zomwe zimawoneka mwa odwala omwe amalandila empagliflozin m'maphunziro oyendetsedwa ndi placebo amaperekedwa mu Gome ili m'munsiyi (zoyipa zomwe zimachitika zimayikidwa malinga ndi ziwalo ndi machitidwe komanso molingana ndi mawu omwe amasankhidwa ndi MedDRA) ndi chisonyezo cha kupendekera kwawo kwathunthu. Magawo a pafupipafupi amatanthauziridwa motere: pafupipafupi (> 1/10), pafupipafupi (kuchokera>, 1/100 mpaka> 1/1000 mpaka> 1/10000 Kufotokozera zamomwe zimachitikira motsutsana
Hypoglycemia
Zotsatira za hypoglycemia zimadalira chithandizo chogwirizana cha hypoglycemic chomwe chimagwiritsidwa ntchito.
Hypoflycemia wofatsa (glucose 3.0 - 3.8 mmol / L (54-70 mg / dl)) Zotsatira za hypoglycemia wofatsa zinali zofanana kwa odwala omwe amatenga mphamvu ya empagliflozin kapena placebo monga monotherapy, komanso nthawi ya empagliflozin atawonjezeredwa ndi metformin ndi pankhani ya kuwonjezera pa empagliflozin kuti pioglitazone (± metformin). Pamene empagliflozin idaperekedwa limodzi ndi metformin ndi zotumphukira zochokera ku sulfonylurea, chiwopsezo cha hypoglycemia chinali chachikulu (10 mg: 10,3%, 25 mg: 7.4%) kuposa ndi placebo palimodzi (5.3%).
Sekulu hypoglycemia (shuga m'magazi ochepera 3 mmol / L (54 mg / dL))
Zomwe zimachitika kwambiri hypoglycemia zinali zofanananso ndi odwala omwe amatenga mphamvu ya empagliflozin ndi placebo ngati monotherapy. Pamene empagliflozin idaperekedwa limodzi ndi metformin ndi zotumphukira zochokera ku sulfonylurea, chiwopsezo cha hypoglycemia chinali chachikulu (10 mg: 5.8%, 25 mg: 4.1%) kuposa ndi placebo palimodzi (3,1%).
Kuyamwa mwachangu
Pafupipafupi kuchuluka kukodza (Zizindikiro monga polakiuria, polyuria, nocturia adayesedwa) anali okwera ndi empagliflozin (pa 10 mg: 3.4%, pa mlingo wa 25 mg: 3.2%) kuposa ndi placebo (1) %). Kuchuluka kwa nocturia kunali kofanana ndi gulu la odwala omwe amatenga empagliflozin komanso pagulu la odwala omwe akutenga placebo (osakwana 1%). Kukula kwa zotsatirapo zake kunali kofatsa kapena kwapakati.
Matenda amitsempha
Zomwe zimayambitsa matenda a kwamikodzo matendawa zinali zofanana ndi empagliflozin 25 mg ndi placebo (7.6%), koma zokwera ndi empagliflozin 10 mg (9.3%). Monga placebo, matenda amkodzo thirakiti wokhala ndi mphamvu ya impagliflozin anali ochulukirachulukira kwa odwala omwe ali ndi mbiri yodwala matenda obwera chifukwa cha mkodzo. Matenda a kwamikodzo thirakiti anali ofanana ndi odwala omwe amatenga mphamvu ya empagliflozin ndi placebo. Matenda amitsempha yam'mimba anali ofala kwambiri mwa akazi.
Matenda amtunduwu
Zomwe zimachitika pazochitika monga vaginal candidiasis, vulvovaginitis, balanitis, ndi matenda ena amiseche zinali zokulirapo ndi empagliflozin (pa 10 mg: 4.1%, pa mlingo wa 25 mg: 3.7%) kuposa ndi placebo (0 , 9%). Matenda amtunduwu anali ofala kwambiri mwa akazi. Kukula kwa matenda amtundu anali ofatsa kapena odziletsa.
Hypovolemia
Zomwe zimachitika mu hypovolemia (zomwe zimawonetsedwa ndi kuchepa kwa kuthamanga kwa magazi, orthostatic arterial hypotension, kuchepa madzi m'thupi, kukomoka) zinali zofanananso ndi mankhwala a empagliflozin (pa 10 mg: 0,5%) pa mlingo wa 25 mg: 0.3%) ndi placebo (0, 3%). Mwa odwala omwe ali ndi zaka zopitilira 75, kuchuluka kwa hypovolemia kuyerekezera kwa odwala omwe amatenga mphamvu ya empagliflozin pa 10 mg (2.3%) ndi placebo (2.1%), koma apamwamba mwa odwala omwe amamwa mankhwala a empagliflozin pa 25 mg (4,4%) )

Bongo

Kuchita ndi mankhwala ena
Mu vitro kugwiritsa ntchito mankhwala
Empagliflozin sikuletsa, kutsatsa, kapena kuyambitsa CYP450 isoenzymes. Njira yayikulu yogwiritsira ntchito kagayidwe ka mankhwala kaumunthu ndi glucuronidation ndi kutenga uridine-5'-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9. Empagliflozin sikuletsa UGT1A1. Kugwiritsa ntchito mankhwala osokoneza bongo a empagliflozin ndi mankhwala omwe ali gawo lapansi la CYP450 ndi UGT1A1 isoenzymes amawonedwa ngati osatheka.
Empagliflozin ndi gawo lapansi la glycoprotein P (P-gp) ndi mapuloteni odana ndi khansa ya m'mawere (BCRP). koma mu zochizira Mlingo sichiletsa mapuloteni awa. Kutengera ndi kafukufuku wochokera mu maphunziro a in vitro, akukhulupirira kuti kuthekera kwa empagliflozin kulumikizana ndi mankhwala omwe ali gawo lapansi la glycoprotein P (P-gp) ndizokayikitsa. Empagliflozin ndi gawo lapansi lonyamula ma organic anionic: OATZ, OATP1B1 ndi OATP1VZ, koma si gawo limodzi la organic anionic onyamula 1 (OAT1) ndi organic cationic onyamula 2 (OST2). Komabe, kulumikizana kwa mankhwala a empagliflozin ndi mankhwala omwe ali ophatikizana ndi mapuloteni onyamula omwe afotokozedwa pamwambapa ndiwowona kuti sangayike.
Mu vivo kuyanjana kwa mankhwala osokoneza bongo
Ma pharmacokinetics a empagliflozin sasintha mwa odzipereka athanzi akagwiritsidwa ntchito limodzi ndi metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, torasemide ndi hydrochlorothiazide. Kugwiritsa ntchito kwa empagliflozin ndi gemfibrozil, rifampicin ndi probenecid kuwonetsa kuwonjezeka kwa AUC ya empagliflozin ndi 59%, 35% ndi 53%, motsatana, koma kusintha kumeneku sikunawonedwe kukhala kofunika kwambiri.
Empagliflozin ilibe gawo lililonse pama pharmacokinetics a metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin. digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide ndi kulera kwamlomo.
Zodzikongoletsera
Empagliflozin imatha kukongoletsa kukodzetsa kwa thiazide ndi "loop" diuretics, yomwe imatha kukulitsa vuto lakusowa kwamadzi ndi magazi ochepa.
Insulin ndi mankhwala omwe amathandizira kubisalira kwake
Insulin ndi mankhwala omwe amathandizira kubisika kwake, monga sulfonylureas, amatha kukulitsa chiopsezo cha hypoglycemia. Chifukwa chake, ndi munthawi yomweyo kugwiritsa ntchito mphamvu ya empagliflozin ndi insulin ndi mankhwala omwe amathandizira kutulutsa kwake, kungakhale kofunikira kuti muchepetse mlingo wawo, kuti mupewe chiopsezo cha hypoglycemia.

Malangizo apadera

Zokhudza mphamvu pakutha kuyendetsa magalimoto ndi zida
Kafukufuku wamankhwala wokhudzana ndi mphamvu ya empagliflozin pa kuyendetsa magalimoto ndi machitidwe sanachitike. Odwala ayenera kusamala poyendetsa magalimoto ndi maginito, popeza mukamagwiritsa ntchito mankhwala JARDINS (makamaka kuphatikiza ndi zotumphukira za sulfonylurea ndi / kapena insulin), hypoglycemia imayamba.

Wopanga

Tchulani adilesi ndi malo omwe amapangira mankhwala
Beringer Ingelheim Pharma GmbH & Co.KG
Binger Strasse 173, 55216 Ingelheim am Rhein, Germany

Mutha kupeza zowonjezera zokhudzana ndi mankhwalawa, komanso kutumiza madandaulo anu ndi zambiri zokhudzana ndi zochitika zotsutsana ndi adilesi yotsatira ku Russia
LLC Beringer Ingelheim
125171. Moscow, Leningradskoye Shosse, 16A p. 3

Mapiritsi a Jardins

Awa ndi mapiritsi okhala ndi filimu. Mawonekedwe: chikasu chopepuka, chowongoka kapena chozungulira (kutengera mtundu), kapangidwe - mapiritsi a biconvex okhala ndi mbali zometedwa ndi zikwangwani zolembedwa za wopanga mbali imodzi. Mankhwala amapangidwa ku Germany kuti achepetse shuga m'magazi a 2 shuga.

Oral hypoglycemic mankhwala, yogwira mankhwala - empagliflozin. The mwatsatanetsatane kapangidwe ndi Mlingo zikuwonetsedwa patebulo:

Mlingo 1 piritsi (mg)

chikasu cha opadray (Hypromellose, titanium dioxide, talc, macrogol, utoto wa okusayidi wachikasu)

Zotsatira za pharmacological

Empagliflozin ndiwosinthika, wogwira ntchito kwambiri, wosankha inhibitor wa mtundu 2 wodalira shuga. Zatsimikizika mwasayansi kuti empagliflozin imasankha kwambiri operekera ena omwe ali ndi glucose homeostasis mu thupi. Thupi limakhala ndi vuto la glycemic kwa odwala omwe ali ndi matenda amtundu wa 2 pochepetsa kuyamwa kwa impso. Kuchuluka kwa glucose komwe kumatulutsidwa ndi njirayi kumatengera mwachangu kuchuluka kwa impso.

Kafukufuku akuwonetsa kuti mwa odwala omwe ali ndi matenda a shuga a 2, kuchuluka kwa shuga kumawonjezeka pambuyo piritsi loyamba kumwa ndipo zotsatirapo zake zidakhala tsiku limodzi. Zizindikirozi zidatsalira pomatenga 25 mg ya empagliflozin kwa mwezi umodzi. Kuchuluka kwa shuga kwa impso kunapangitsa kuchepa kwake m'magazi a wodwalayo. Mankhwala amachepetsa kuchuluka kwa shuga m'magazi, mosasamala kanthu za kudya.

Gululi lodziyimira payekha limachepetsa chiopsezo cha hypoglycemia.Mphamvu ya zochita za yogwira ntchito sizitengera ntchito ya magawo a Langerhans ndi insulin metabolism. Asayansi amawona zabwino za empagliflozin pa ma peptides okhathamira a magwiridwe antchito a maselo amenewa. Kuchuluka kwa shuga m'thupi kumabweretsa kuchepa kwa zopatsa mphamvu, zomwe zimachepetsa thupi. Pogwiritsa ntchito empagliflozin, glucosuria imawonedwa.

Zizindikiro zogwiritsidwa ntchito

Amawonetsedwa kwa odwala omwe ali ndi mtundu wa 2 shuga mellitus pachakudya chokhazikika ndikusewera masewera, momwe sizingatheke kuwongolera bwino zizindikiro za glycemic. Ndi Metformin tsankho, monotherapy ndi Jardins ndikotheka. Ngati mankhwala alibe zoyenera, kugwiritsa ntchito mankhwala ena a hypoglycemic, kuphatikizapo insulin, ndikotheka.

Mayendedwe Jardins

Mapiritsi amatengedwa pakamwa, mosasamala nthawi yatsiku kapena zakudya. Ndikulimbikitsidwa kuti muthe kutenga ndi 10 mg patsiku, ngati zotsatira zoyenera sizikuchitika, onjezerani ku 25 mg. Ngati pazifukwa zina sanamwe mankhwalawo, ndiye kuti muyenera kumwa nthawi yomweyo, monga momwe amakumbukirira. Kuchuluka kawiri sikungathe kuwononga. Pankhani ya chiwindi chodwala, kuwongolera sikofunikira, ndipo odwala omwe ali ndi matenda a impso saloledwa.

Pa nthawi yoyembekezera

Kugwiritsa ntchito mapiritsi pa nthawi ya pakati kumapangidwa chifukwa cha kusowa kwa chidziwitso kuchokera ku kafukufuku wothandiza komanso chitetezo. Kafukufuku wazinyama adawonetsa mwayi wokhudzana ndi kubisala kwa impagliflozin m'magazi a uteroplacental. Kuopsa kukhudzana ndi mwana wosabadwa komanso wakhanda sikusiyidwa. Ngati ndi kotheka, muyenera kusiya kumwa mankhwalawa panthawi yapakati.

Muubwana

Kuchiza ndi mankhwalawa kwa ana ndi achinyamata ochepera zaka 18 kumakhala kotsutsana. Zophatikizidwa ndi kafukufuku wosakwanira. Kuchita bwino ndi chitetezo cha yogwira mankhwala enagliflozin kwa ana sichinatsimikizidwe. Kuti athetse zoopsa zowononga thanzi la ana, Jardins ndi oletsedwa. Bwino kusankha mtundu wina wovomerezeka.

Zithunzi za 3D

Kufotokozera za mtundu wa kipimo

Mapiritsi 10 mg: mozungulira biconvex wokhala ndi mbali zokutidwa, yokutidwa ndi chithunzi cha utoto wowala wachikaso, ndikulemba chizindikiro cha kampani mbali inayo ndi "S10" mbali inayo.

25 mg mapiritsi: biconvex chowulungika cham'mphepete mwa beve, wokutidwa ndi kanema wopota wa utoto wachikasu, wokhala ndi chithunzi cha kampani mbali inayo ndi "S25" mbali inayo.

Mankhwala

Empagliflozin ndi chosinthika mwanjira yosankha komanso yampikisano yoyendetsa mtundu 2 wa glucose wopatsirana ndi ndende yomwe ikufunika poletsa 50% ya ntchito ya enzyme (IC₅₀), lofanana ndi 1.3 nmol. Kusankha kwa empagliflozin ndi kokwera 5,000 kuchulukirapo kuposa mtundu wa transporter wa glucose wa mtundu 1, womwe umayendetsa shuga m'matumbo. Kuphatikiza apo, zidapezeka kuti empagliflozin imasankha kwambiri anthu ena okhathamira omwe amayendetsa glucose homeostasis m'malo osiyanasiyana.

Mtundu wachiwiri wa glucose wotengera glucose ndiye njira yayikulu yonyamula glucose kuchokera ku renal glomeruli kubwerera m'magazi. Empagliflozin imathandizira kuwongolera kwa glycemic mwa odwala omwe ali ndi mtundu wa 2 shuga mellitus (T2DM) pochepetsa reghorpose glucose. Kuchuluka kwa shuga komwe impso zimagwiritsidwa ntchito m'njira imeneyi zimadalira kuchuluka kwa shuga m'magazi ndi GFR. Kuletsa shuga wodalira glucose transporter mtundu 2 mwa odwala matenda ashuga 2 ndi hyperglycemia kumabweretsa kuchotsedwa kwa shuga ndi impso.

Pakufufuza kwamankhwala kwa milungu inayi, zidapezeka kuti odwala omwe ali ndi matenda a shuga a 2, kuchuluka kwa shuga wa impso kumawonjezeka nthawi yoyamba ya mankhwala a empagliflozin atagwiritsidwa ntchito, izi zimachitika kwa maola 24. Kuchulukana kwa shuga kwa impso kunapitilira mpaka kumapeto kwa chithandizo, mpaka Mlingo wa 25 mg 1 nthawi patsiku, pafupifupi 78 g / tsiku. Odwala omwe ali ndi matenda a shuga a mtundu wachiwiri, kuchuluka kwa shuga kwa impso kunayambitsa kutsika kwamphamvu kwa glucose m'madzi a m'magazi.

Empagliflozin (pa mlingo wa 10 ndi 25 mg) amachepetsa kuchuluka kwa shuga m'magazi am'magazi onse posala kudya komanso mukatha kudya.

Mphamvu ya zochita za empagliflozin sikudalira magwiridwe antchito a ma cell a pancreatic beta ndi insulin metabolism, yomwe imapangitsa chiopsezo chochepa cha kukula kwa hypoglycemia. Zotsatira zabwino za empagliflozin pazizindikiro za ma cell a beta, kuphatikiza cholembera cha HOMA-β (mtundu wa kuwunika kwa homeostasis-B) ndi kuchuluka kwa proinsulin kuti apange insulin, zalembedwa. Kuphatikiza apo, kuchotsa kwa shuga ndi impso kumayambitsa kuchepa kwa zopatsa mphamvu, komwe kumayendetsedwa ndi kuchepa kwa kuchuluka kwa minofu ya adipose komanso kuchepa kwa thupi.

Glucosuria yomwe imagwiritsidwa ntchito pa empagliflozin imayendera limodzi ndi kuwonjezeka pang'ono kwa diuresis, zomwe zimapangitsa kuchepa kwambiri kwa magazi.

M'maphunziro azachipatala komwe empagliflozin adagwiritsidwa ntchito ngati mankhwala a monotherapy, kuphatikiza mankhwala ophatikizika ndi metformin, kuphatikiza mankhwala ophatikizidwa ndi metformin mwa odwala omwe ali ndi matenda 2 a shuga, kuphatikiza mankhwala ophatikizika ndi metformin ndi sulfonylurea, kuphatikiza mankhwala ndi pioglitazone +/− metformin, kuphatikiza mankhwala ndi linagliptin mu odwala omwe adapezeka ndi matenda a shuga 2, kuphatikiza mankhwala omwe ali ndi linagliptin, omwe amawonjezera mankhwala a metformin, kuphatikiza mankhwala ndi linagliptin poyerekeza ndi paracet o odwala omwe ali ndi vuto losakwanira la glycemic pomwe akutenga linagliptin ndi metformin, kuphatikiza mankhwala ophatikizidwa ndi metformin motsutsana ndi glimepiride (kafukufuku wazaka 2), kuphatikiza mankhwala othandizira insulin (ma insulin angapo a insulin) +/− metformin, kuphatikiza mankhwalawa ndi insulin insulin , mankhwala ophatikiza ndi DPP-4 inhibitor, metformin +/− mankhwala ena apakamwa a hypoglycemic, kuchepa kwakukulu kwa HbA1 kwatsimikiziridwa_c, kuchepa kwa kusala kwa glucose, komanso kuchepa kwa kuthamanga kwa magazi ndi kunenepa kwambiri kwa thupi.

Kafukufuku wachipatala adawunika momwe mankhwala a Jardins ® amafotokozera pafupipafupi zochitika za mtima ndi odwala omwe ali ndi vuto la matenda a shuga a 2 komanso omwe ali ndi chiwopsezo cha mtima (chofotokozedwa ngati kukhalapo kwa chimodzi mwa matenda ndi / kapena mikhalidwe: matenda amitsempha ya m'mitsempha yam'mimba). , IHD yowonongeka ndi chotengera chimodzi cha coronary, IHD yowonongeka m'matumbo angapo a coronary), mbiri ya ischemic kapena hemorrhagic stroke, matenda a m'mitsempha ya m'mitsempha okhala ndi zizindikiro kapena zopanda zizindikiro) kulandira muyezo mankhwala hydrochloric, zimene zinaphatikizapo wothandizila hypoglycemic ndi wothandizila zochizira matenda a mtima. Milandu yokhudzana ndi kufa kwa mtima, kupweteka kwamkati popanda kuphwanya magazi ndi kuwonongeka koopsa kunayesedwa ngati njira yoyamba. Kufa kwa mtima, kufa kwa anthu ambiri, kukulitsa kwa nephropathy, komanso kuthandizira kuchipatala chifukwa cha kulephera kwa mtima kunasankhidwa kukhala njira zowonjezerapo kale.

Empagliflozin yasintha kupulumuka kwathunthu pochepetsa imfa ya mtima. Empagliflozin adachepetsa chiopsezo chakuchipatala chifukwa cholephera mtima. Komanso, mu kafukufuku wazachipatala, adawonetsedwa kuti mankhwalawa Jardins ® adachepetsa chiopsezo cha nephropathy kapena kufalikira kwapang'onopang'ono kwa nephropathy.

Odwala omwe ali ndi macroalbuminuria oyamba, adapezeka kuti mankhwala a Jardins ® kwambiri nthawi zambiri kuyerekeza ndi placebo adayambitsa kukhazikika kwa Normo- kapena microalbuminuria (chiopsezo 1.82, 95% CI: 1.4-2.37).

Pharmacokinetics

The pharmacokinetics of empagliflozin adawerengera mozama mu odzipereka athanzi komanso odwala omwe ali ndi matenda amtundu wa 2.

Zogulitsa. Empagliflozin pambuyo pakamwa makonzedwe ake anali otengeka mwachangu, C_max empagliflozin mu plasma idafikira pambuyo maola 1.5. Kenako, kuchuluka kwa empagliflozin mu plasma kunachepa m'magawo awiri. Mutatha kumwa empagliflozin pa 25 mg kamodzi patsiku, AUC wamba nthawi C_ss mu plasma anali 4740 nmol · h / l, ndipo mtengo wa C_max - 687 nmol / L.

Ma pharmacokinetics a empagliflozin mwa odzipereka athanzi komanso odwala matenda a shuga a 2 anali ofanana.

Kudya sikukhala ndi vuto lililonse pama pharmacokinetics a empagliflozin.

Kugawa. V_d nthawi ya plasma C_ss chinali pafupifupi malita 73.8. Pambuyo pakulankhula pakamwa ndi odzipereka othandiza olembedwa enagliflozin 14 C, mapuloteni a plasma omwe anali 85,2%.

Kupenda. Njira yayikulu ya mphamvu ya metabolism ya empagliflozin mwa anthu ndi glucuronidation ndi gawo la UDP-GT (UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9). Ma metabolites omwe amadziwika kwambiri a empagliflozin ndi ma glucuronic conjugates (2-O, 3-O ndi 6-O glucuronide). Mphamvu ya metabolite iliyonse imakhala yochepa (zosakwana 10% ya mphamvu yonse ya empagliflozin).

Kuswana. T_1/2 anali pafupifupi maola 12.4 Panthawi ya kugwiritsa ntchito empagliflozin 1 nthawi patsiku C_ss mu plasma zimatheka pambuyo lachisanu. Pambuyo m`kamwa makonzedwe olembedwa enagliflozin 14 C odzipereka athanzi, pafupifupi 96% ya mlingo anachotsedwa (kudzera m'matumbo 41% ndi impso 54%).

Kudzera m'matumbo, mankhwala ambiri omwe adalembedwa kuti anali osasinthika sanasinthidwe. Hafu imodzi yokha yolembedwa yomwe idatulutsidwa ndi impso ndi yosasinthika.

Pharmacokinetics mwapadera odwala odwala

Matenda aimpso. Odwala omwe ali ndi zofatsa (60 2), zolimbitsa thupi (30 2), zovuta (GFR 2), kulephera kwa impso, komanso odwala omwe amalephera kusintha kwa impso, AUC ya empagliflozin inakulirakulira pafupifupi 18, 20, 66, ndi 48%, motsatana, poyerekeza ndi odwala omwe ali ndi ntchito yachilendo ya impso. Odwala ndi zolimbitsa aimpso kulephera ndi odwala end-siteji aimpso kulephera C_max empagliflozin mu plasma inali yofanana ndi mfundo zofanana mwa odwala omwe ali ndi vuto laimpso. Odwala wofatsa kwambiri aimpso kulephera_max empagliflozin mu plasma anali pafupifupi 20% kuposa kuposa odwala wamba yachilendo ntchito. Zotsatira za kusanthula kwa anthu a zakumwa zamtundu wa anthu zidawonetsa kuti chiwonetsero chonse cha empagliflozin chatsika ndikuchepa kwa GFR, zomwe zidapangitsa kuti chiwopsezo cha mankhwalawo chikwanire.

Kuwonongeka kwa chiwindi. Odwala omwe ali ndi vuto la chiwindi chodwala, wofatsa komanso wowonda kwambiri (malinga ndi gulu la ana-Pugh), mfundo za AUC za empagliflozin zimakula pafupifupi 23, 47 ndi 75%, motero, ndi C._max pafupifupi 4, 23 ndi 48%, motero (poyerekeza ndi odwala omwe ali ndi chiwindi chambiri).

BMI, jenda, mtundu, komanso zaka sizinakhale ndi vuto lililonse pakamerokamziki.

Ana. Maphunziro a pharmacokinetics a empagliflozin mwa ana sanachitike.

Zisonyezero za mankhwala Jardins ®

Type 2 matenda a shuga:

- monga monotherapy odwala omwe ali ndi vuto lokwanira la glycemic pokhapokha poyambira kudya ndi masewera olimbitsa thupi, kusankha metformin komwe sikutheka chifukwa cha tsankho,

- monga kuphatikiza mankhwala ndi othandizira ena a hypoglycemic, kuphatikiza insulin, pamene mankhwalawa amagwiritsidwa ntchito limodzi ndi zakudya komanso kuchita masewera olimbitsa thupi samapereka kuyenera kwa glycemic.

Amawonetsa kwa odwala omwe ali ndi vuto la matenda a shuga a 2 komanso chiwopsezo chachikulu cha mtima * limodzi ndi zochizira zamatenda amtima kuti achepetse:

- kufa kwathunthu pochepetsa kuchepa kwa mtima,

- Kufa kwamtima kapena kuchipatala chifukwa cha kulephera kwa mtima.

* Kuopsa kwa mtima wam'mimba kumatanthauza kukhalapo kwa chimodzi mwazina za matenda ndi / kapena mikhalidwe: mtima wamatumbo (mbiri ya kulowetsedwa kwa myocardial, opaleshoni yam'mitsempha yotupa, matenda amitsempha yamagazi ndi kuwonongeka kwa chotengera chimodzi cha coronary, matenda amitsempha yamagazi ndi kuwonongeka kwa ziwiya zingapo za coronary), ischemic kapena hemorrhagic stroke mbiri yodwala matenda oopsa (okhala ndi kapena opanda zizindikiro).

Mimba komanso kuyamwa

Kugwiritsa ntchito kwa empagliflozin pa nthawi ya pakati kumapangidwa chifukwa cha kusakwanira kwa chidziwitso chokwanira ndi chitetezo.

Zambiri zomwe zimapezeka mu preclinical maphunziro mu zinyama zimasonyezera kulowa kwa empagliflozin mkaka wa m'mawere. Ngozi yokhala ndi ana akhanda ndi ana pa nthawi yoyamwitsa sichimakhudzidwa. Kugwiritsa ntchito empagliflozin nthawi yoyamwitsa kumatsutsana. Ngati ndi kotheka, kugwiritsa ntchito mankhwala a empagliflozin pa nthawi yoyamwitsa kuyenera kutha.

Zotsatira zoyipa

Zomwe zimachitika nthawi zambiri zovuta kwa odwala omwe amalandila empagliflozin kapena placebo pamavuto azachipatala zinali zofanana. Chotsatira chovuta kwambiri chinali hypoglycemia, chomwe chimagwiritsidwa ntchito ndi empagliflozin kuphatikiza ndi zotumphukira za sulfonylurea kapena insulin (onani. Kufotokozera kwa zoyipa zomwe zasankhidwa).

Zotsatira zoyipa zomwe zimawoneka mwa odwala omwe amalandila empagliflozin m'maphunziro oyendetsedwa ndi placebo amaperekedwa pansipa (zoyipa zimasankhidwa malinga ndi ziwalo ndi machitidwe komanso malinga ndi zomwe amakonda MedDRA mawu) kuwonetsa kutsata kwawo kwathunthu. Magawo a pafupipafupi amafotokozedwa motere: pafupipafupi (≥1 / 10), nthawi zambiri (kuchokera ku ≥1 / 100 mpaka kuthamanga kwa magazi, orthostatic arterial hypotension, kuchepa kwa madzi, kukomoka) zinali zofanana pankhani ya empagliflozin (pa 10 mg - 0,6%, pa mlingo wa 25 mg - 0,4%) ndi placebo (0.3%). Mwa odwala omwe ali ndi zaka zopitilira 75, kuchuluka kwa hypovolemia kuyerekezera kwa odwala omwe amatenga empagliflozin pa 10 mg (2.3%) ndi placebo (2.1%), koma apamwamba mwa odwala omwe amamwa mankhwala a empagliflozin pa 25 mg (4,3%) )

Kuchita

Zodzikongoletsera. Empagliflozin imatha kupititsa patsogolo okodzetsa a thiazide ndi malupu okodzetsa, omwe, amawonjezeranso chiopsezo cha kuchepa madzi m'thupi komanso kuwonongeka kwa ubongo.

Insulin ndi mankhwala omwe amathandizira kubisalira kwake. Insulin ndi mankhwala omwe amathandizira kubisika kwake, monga sulfonylureas, amatha kukulitsa chiopsezo cha hypoglycemia. Chifukwa chake, ndi munthawi yomweyo kugwiritsa ntchito mphamvu ya empagliflozin ndi insulin ndi mankhwala omwe amathandizira kutulutsa kwake, kungakhale kofunikira kuti muchepetse mlingo wawo, kuti mupewe chiopsezo cha hypoglycemia.

Kuunika kwa kuyanjana kwa mankhwala mu vitro. Empagliflozin sikuletsa, kutsatsa, kapena kuyambitsa CYP450 isoenzymes. Njira yayikulu yogwiritsira ntchito kagayidwe kaumunthu ndi kuphatikizika kwa gluPuronidation ndi kutenga nawo gawo kwa UDP-GT (UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9). Empagliflozin sikuletsa UGT1A1, UGT1A3, UGT1A8, UGT1A9 kapena UGT2B7. Kugwiritsa ntchito mankhwala osokoneza bongo a empagliflozin ndi mankhwala omwe ali gawo lapansi la CYP450 ndi UGenz isoenzymes amawonedwa ngati osatheka. Empagliflozin ndi gawo laling'ono la P-gp ndi mapuloteni omwe amasankha BCRP, koma mu mankhwala othandizira saletsa mapuloteni awa. Kutengera ndi kafukufuku kuchokera ku maphunziro mu vitro , akukhulupirira kuti kuthekera kwa empagliflozin kulumikizana ndi mankhwala omwe ali gawo lapansi P-gpsizingatheke. Empagliflozin ndi gawo lapansi lonyamula ma organic anionic: OAT3, OATP1B1 ndi OATP1B3, koma si gawo laling'ono lonyamula anionic 1 (OAT1) ndi organic cationic onyamula 2 (OCT2). Komabe, kulumikizana kwa mankhwala a empagliflozin ndi mankhwala omwe ali ophatikizana ndi mapuloteni onyamula omwe afotokozedwa pamwambapa ndiwowona kuti sangayike.

Kuwunika kwa zochitika zamankhwala mu vivo. Pogwiritsa ntchito mankhwala opagliflozin ophatikizidwa pamodzi ndi mankhwala ena omwe amagwiritsidwa ntchito, makondedwe ofunikira a pharmacokinetic sanawonedwe. Zotsatira za kafukufuku wa pharmacokinetic zikuwonetsa kuti palibe chifukwa chosintha mlingo wa mankhwala a Jardins ® pomwe amagwiritsidwa ntchito ndi mankhwala omwe amagwiritsidwa ntchito masiku onse.

Ma pharmacokinetics a empagliflozin sasintha odzipereka athanzi akagwiritsidwa ntchito limodzi ndi metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, komanso kwa odwala omwe ali ndi matenda a mtundu wa 2 ngati agwiritsidwa ntchito limodzi ndi torasemoridide ndi hydrochloride hydrochloride.

Ndi kuphatikiza kwa ntchito kwa empagliflozin ndi gemfibrozil, rifampicin ndi probenecid, kuchuluka kwa AUC kwa empagliflozin ndi 59, 35 ndi 53%, motsatana, kunadziwika, komabe, kusintha kumeneku sikunawonedwe kukhala kofunika kwambiri pakuchipatala.

Empagliflozin ilibe gawo lalikulu pakumera kwa pharmacokinetics ya metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide ndi njira yolerera pakamwa mwa odzipereka athanzi.

Kuyanjana kwa mankhwala osokoneza bongo

Imawonjezera mphamvu ya okodzetsa osiyanasiyana okakamiza angapo, zomwe zimawonjezera chiopsezo cha kuchepa madzi m'thupi komanso owopsa. Zotsatira za insulin ndi sulfonylurea zimatha kuyambitsa hypoglycemia. Pogwiritsa ntchito mankhwalawa limodzi ndi insulin, kuchepetsedwa kwa mankhwalawa ndikofunikira kuti muchepetse vuto la hypoglycemic .Magwiridwe antchito a empagliflozin ndi mankhwala omwe ali magawo a isoenzymes amawoneka kuti ndi otetezeka.

Empagliflozin - chophatikiza chomwe chimagwiritsidwa ntchito pamapiritsi, sichikuwakhudza mankhwalawa: - Metformin, Glimepiride, Pioglitazone, Warfarin, Digoxin, Ramipril, Simvastatin, Hydrochlorothiazide, Torasemide ndi njira yolerera pakamwa. Pogwiritsa ntchito pamodzi ndi mankhwala omwe amagwiritsidwa ntchito masiku ano, kusintha kwa mlingo sikufunika.

Jardins Analogs

Pamsika wa mankhwala ku Russian Federation, pali mankhwala amodzi okha omwe amapangidwa pamaziko a chinthu - empagliflovin. Jardins alibe chitsimikizo chotsimikizika. Mapiritsi ena a hypoglycemic ali ndi chinthu china chomwe chimagwira pakapangidwe ndipo amachita mosiyanasiyana pa thupi la munthu. Izi zikuphatikiza:

Jardins - malangizo, gwiritsani ntchito, mtengo, ndemanga

Matenda a shuga ndi omwe amadziwika kuti ndi amodzi mwa matenda padziko lapansi. Mu Russian Federation, nzika pafupifupi 10 miliyoni zimadwala nthendayi. Ambiri aiwo amakonda kugwiritsa ntchito mankhwala Jardins chifukwa chogwira ntchito.

Dzinalo Lachilatini ndi Jardiance. Mankhwala a INN: Empagliflozin (Empagliflozin).

Jardins ali ndi vuto la antiidiabetes.

Gulu la ATX: A10BK03.

Mankhwalawa amapezeka mu mapiritsi osungunuka. Piritsi limodzi lili ndi 25 kapena 10 mg ya empagliflozin (chophatikizira). Zinthu zina:

• talcum ufa
• titanium dioxide
• utoto wachikasu wachitsulo (utoto),
• lactose monohydrate,
• Hyprolose
• ma cellcrystals a cellulose.

Mankhwalawa amapezeka mu mapiritsi osungunuka.

Mapiritsi ali ndi matuza a ma PC 10. Bokosi 1 lili ndi matuza 1 kapena 3.

Ndi chisamaliro

Mankhwalawa amatchulidwa mosamala ngati:

• ntchito zazinsinsi zama cell zomwe zimapezeka mu kapamba,
• kuphatikiza ndi sulfonylurea ndi zotumphukira za insulin,
• matenda am'mimba ophatikizira kuchepa kwamadzi,
• ukalamba.

Mlingo ndi makonzedwe

Mapiritsi amatengedwa pakamwa. Mlingo woyambirira ndi 10 mg 1 nthawi patsiku. Ngati kuchuluka kwa mankhwalawa sikungapereke chiwongolero cha glycemic, ndiye kuti mlingo umakwera mpaka 25 mg. Mlingo wapamwamba ndi 25 mg / tsiku.

Mapiritsi amatengedwa pakamwa.

Kugwiritsa ntchito mapiritsi sikugwirizana ndi nthawi ya tsiku kapena kuyamwa kwa chakudya. Ndiosafunika kuti tsiku 1 mugwiritse ntchito kawiri mlingo.

Chithandizo cha Matenda a shuga ndi Jardins

Mayeso azachipatala atsimikizira kuti mankhwalawo omwe amafunsidwa ndi okhawo omwe amathandizira odwala matenda a shuga mellitus (mtundu II), momwe ngozi za kupezeka kwa matenda a CVD ndi ziwopsezo zakufa kuchokera ku ma pathologies amenewa zimachepetsedwa. Sizoletsedwa kugwiritsa ntchito mankhwalawa kwa odwala omwe ali ndi matenda a shuga 1.

Umboni wa madotolo ndi odwala za Jardins

Galina Aleksanina (wochiritsa), wazaka 45, St. Petersburg.

Mankhwala otetezeka omwe samayambitsa mavuto (machitidwe anga). Mtengo wokwera umavomerezeka mokwanira ndi zochitika zamankhwala. Zotsatira za placebo zimatsimikiziratu. Kuphatikiza apo, alibe ma fanizo ku Russia, ndipo mankhwalawa amafanana mosiyanasiyana.

Anton Kalinkin, wazaka 43, Voronezh.

Chida chake ndi chabwino. Ine, monga munthu wodwala matenda ashuga, ndimakhutira ndi zomwe akuchita. Chofunika kwambiri ndikuphunzira mosamala malangizo ogwiritsa ntchito. Pokhapokha ngati izi zitha kupewedwa, zomwe zimatsimikiziridwa pakokha. Mwa zoperewera, munthu amatha kusiyanitsa mtengo wokhawo komanso kuti mankhwalawo sagulitsidwa m'mafakitala onse.

Jardins: malangizo ogwiritsira ntchito

Mankhwala

Empagliflozin ndiwosinthika, wogwira ntchito kwambiri, wosankha komanso wampikisano wa mtundu 2 wowonjezera shuga. Ndi ndende yoyenera kuletsa 50% ya ntchito ya enzyme (IC50) ya 1.3 nmol.

Kusankha kwa empagliflozin ndi okwera 5,000 kuchulukirapo kuposa mtundu wa glucose wopatsirana ndi sodium yemwe amachititsa kuti shuga ayambe kuyamwa. Kuphatikiza apo, zidapezeka kuti empagliflozin imasankha kwambiri anthu ena okhathamira omwe amayendetsa glucose homeostasis m'malo osiyanasiyana.

Mtundu 2 wa glucose wopatsirana ndi sodium ndiye puloteni yonyamula kwambiri yomwe imapangitsa kuti shuga ayambidwenso kuchokera ku chimpso chamadzimadzi kulowa m'magazi. Empagliflozin imathandizira kuwongolera kwa glycemic mwa odwala omwe ali ndi mtundu wa 2 shuga mellitus (T2DM) pochepetsa reghorpose glucose.

Kuchuluka kwa shuga komwe impso zimagwiritsidwa ntchito pamakina amenewa kumadalira kuchuluka kwa shuga m'magazi komanso kuchuluka kwa kusefedwa kwa glomerular (GFR). Kuletsa kwa sodium wodalira wa mtundu 2 shuga mwa odwala matenda ashuga a 2 ndi hyperglycemia kumabweretsa kuchotsedwa kwa shuga ndi impso.

M'maphunziro azachipatala, zidapezeka kuti odwala omwe ali ndi matenda amtundu wa 2, kuchuluka kwa shuga mwa impso kumawonjezeka atangolowa muyezo woyamba wa empagliflozin, izi zimachitika kwa maola 24.

Kuwonjezeka kwa shuga kwa impso kumapitirirabe mpaka kumapeto kwa sabata la 4, atagwiritsa ntchito mphamvu ya 25 mg kamodzi patsiku, pafupifupi pafupifupi 78 g / tsiku. Odwala omwe ali ndi matenda a shuga a mtundu wachiwiri, kuchuluka kwa shuga kwa impso kunayambitsa kutsika kwamphamvu kwa glucose m'madzi a m'magazi.

Empagliflozin amachepetsa kuchuluka kwa shuga m'magazi am'magazi posala kudya komanso mukatha kudya. Makina osagwiritsa ntchito insulin omwe amadalira zochita za empagliflozin amathandizira kukhala pachiwopsezo chochepa cha kukula kwa hypoglycemia. Zotsatira za empagliflozin sizitengera magwiridwe antchito a maselo a pancreatic beta ndi insulin metabolism.

Zotsatira zabwino za empagliflozin pazotsimikizira ma cell a beta cell, kuphatikiza HOMA-? Index, zidadziwika. (chitsanzo pakuwunika homeostasis-B) komanso kuchuluka kwa proinsulin kuti apange insulin. Kuphatikiza apo, kuchotsa kwa shuga ndi impso kumayambitsa kuchepa kwa zopatsa mphamvu, komwe kumayendetsedwa ndi kuchepa kwa kuchuluka kwa minofu ya adipose komanso kuchepa kwa thupi. Glucosuria yomwe imagwiritsidwa ntchito pa empagliflozin imayendera limodzi ndi kuwonjezeka pang'ono kwa diuresis, zomwe zimapangitsa kuchepa kwambiri kwa magazi.

M'mayesero azachipatala omwe empagliflozin adagwiritsidwa ntchito ngati monotherapy, kuphatikiza mankhwala ndi metformin, kuphatikiza mankhwala ophatikizika ndi metformin ndi sulfonylurea, kuphatikiza mankhwala ophatikizika ndi metformin poyerekeza ndi glimepiride, kuphatikiza mankhwala ndi pioglitazone +/- metformin, ngati mankhwala ophatikizika ndi dipeptidyl peptide inhibitor 4 (DPP-4), metformin +/- mankhwala ena apakamwa a hypoglycemic, m'njira yophatikiza mankhwalawa ndi insulin, inali yofunikira mokomera kutsika kwanga kwa glycosylated HbAlc hemoglobin ndikuchepetsa kusala kwa plasma glucose.

Ma pharmacokinetics a empagliflozin adaphunziridwa kwathunthu mu odzipereka athanzi komanso odwala omwe ali ndi matenda a shuga a mtundu wachiwiri.

Pambuyo pakukonzekera pakamwa, empagliflozin idayamba kugwira ntchito mwachangu, kuchuluka kwakukulu kwa empagliflozin m'madzi a m'magazi (Cmax) kunafika pambuyo pa maola 1.5. Kenako, kuchuluka kwa empagliflozin mu plasma kunachepa m'magawo awiri.

Atalandira empagliflozin, dera wamba pansi pa ndende ya nthawi-yocheperako (AUC) yolumikizidwa nthawi yayitali inali 4740 nmol x h / l, ndi Cmax - 687 nmol / l. Ma pharmacokinetics a empagliflozin mwa odzipereka athanzi komanso odwala omwe ali ndi matenda a shuga a 2 anali ofanana.

Kudya sikukhala ndi vuto lililonse pama pharmacokinetics a empagliflozin.

Kuchuluka kwa magawidwe panthawi ya plasma yosasunthika kunali pafupifupi malita 73.8. Pambuyo pakukonzekera pakamwa ndi odzipereka athanzi odziwika kuti ndi enagliflozin 14C, mapuloteni a plasma omwe anali 85% anali.

Njira yayikulu yogwiritsira ntchito mphamvu ya metabolaguriflozin mwa anthu ndi glucuronidation ndikuchita nawo uridine-5'-diphospho-glucuronosyltransferase UGT2B7, UGT1A3, UGT1A8 ndi UGT1A9. Ma metabolites omwe amadziwika kwambiri a empagliflozin ndi ma glucuronic conjugates atatu (2-0, 3-0 ndi 6-0 glucuronides). Mphamvu ya metabolite iliyonse imakhala yochepa (zosakwana 10% ya mphamvu yonse ya empagliflozin).

Kuchotsa theka-moyo anali pafupifupi maola 12.4. Pankhani yogwiritsa ntchito empagliflozin kamodzi patsiku, ndende ya plasma yokhazikika idakwaniritsidwa pambuyo pa mlingo wachisanu.

Pambuyo m`kamwa makonzedwe olembedwa enagliflozin 14C odzipereka athanzi, pafupifupi 96% ya mlingo anachotsedwa (kudzera m'matumbo 41% ndi impso 54%). Kudzera m'matumbo, mankhwala ambiri omwe adalembedwa kuti anali osasinthika sanasinthidwe.

Hafu imodzi yokha yolembedwa yomwe idatulutsidwa ndi impso ndi yosasinthika. Pharmacokinetics mwapadera odwala odwala

Matenda aimpso

Odwala omwe ali ndi vuto lochepa kwambiri, modekha, komanso mwamphamvu kwambiri (30 https: //apteka.103.xn--p1ai/jardins-13921690-instruktsiya/

Mapiritsi a Jardins ™ 10 mg 30 ma PC

Jardins ® siivomerezeka kwa odwala omwe ali ndi matenda a mtundu woyamba 1 komanso amathandizira odwala matenda ashuga a ketoacidosis.

Pogwiritsa ntchito mitundu 2 ya glucose transporter inhibitors, kuphatikizapo empagliflozin, milandu yovuta ya matenda a shuga a ketoacidosis akuti. Mwa zina mwazomwezi, mawonetseredwe anali atypical ndikuwonetsedwa monga kuwonjezeka kwapang'onopang'ono kwa ndende yamagazi (osapitirira 14 mmol / L (250 mg / dl)).

Chiwopsezo cha kukhala ndi matenda a shuga a ketoacidosis ayenera kuganiziridwanso ngati zizindikiro zosakhazikika monga mseru, kusanza, kusowa kudya, kupweteka kwam'mimba, ludzu lalikulu, kupuma movutikira, kusokonezeka, kutopa kosagwedezeka kapena kugona. Ngati zizindikiro zotere zilipo, odwala amayenera kuwunika nthawi yomweyo ketoacidosis, mosasamala kanthu za kuchuluka kwa shuga m'magazi. Kugwiritsa ntchito mankhwalawa Jardins® kuyenera kusiyidwa kapena kuyimitsidwa mpaka chizindikiritsocho chikhazikike.

Chiwopsezo chachikulu chokhala ndi matenda a diabetesic ketoacidosis ndi chotheka mwa odwala omwe ali ndi chakudya chochepa kwambiri chamafuta, odwala omwe ali ndi vuto lotha kuchepa thupi, odwala omwe ali ndi mbiri ya ketoacidosis, kapena odwala omwe ali ndi chinsinsi chochepa kwambiri cha maselo a pancreatic β-cell. Odwala otere, Jardins® iyenera kugwiritsidwa ntchito mosamala. Kusamala kumafunikira pakuchepetsa mlingo wa insulin.

Jardins in piritsi la 10 mg lili ndi 162,5 mg wa lactose, mulingo wa 25 mg uli ndi 113 mg wa lactose, chifukwa chake, mankhwalawa sayenera kugwiritsidwa ntchito mwa odwala omwe ali ndi zovuta monga cholowa cha lactase, tsankho la lactose, glucose-galactose malabsorption.

Kafukufuku wachipatala awonetsa kuti chithandizo ndi empagliflozin sichimabweretsa chiwopsezo cha mtima. Kugwiritsa ntchito mphamvu ya empagliflozin pa 25 mg sikupangitsa kuti pakhale nthawi yayitali ya QT.

Ndi kuphatikiza kwa mankhwala Jardins® omwe ali ndi zotumphukira za sulfonylurea kapena insulin, kuchepetsedwa kwa mankhwala a sulfonylurea / insulin kungafunike chifukwa cha chiopsezo cha hypoglycemia.

Empagliflozin sanaphunziridwe limodzi ndi glucagon-monga peptide-1 analogues (GLP-1).

Kugwiritsa ntchito kwa mankhwala a Jardins® kumadalira ntchito ya impso, chifukwa chake amalimbikitsidwa kuwunikira ntchito ya impso isanakhazikitsidwe komanso nthawi ya mankhwala (osachepera 1 pachaka), komanso asanaikidwe pochita chithandizo chamankhwala, chomwe chitha kuwononga ntchito ya impso. Kugwiritsa ntchito mankhwalawa odwala omwe ali ndi vuto la impso (GFR) osavomerezeka