Jardins - ntuziaka maka ọrụ *

INWETA
n'iji ọgwụ eme ihe
JARDINS

Mpempe mwepụta
mbadamba ihe mkpuchi

Ngwakọta
Mbadamba otu 1 nwere:
ihe na-arụ ọrụ: empagliflozin 10 na 25 mg
ndị na-ahụkarị: lactose monohydrate, celclose microcrystalline, hyprolose (hydroxypropyl cellulose), sodium croscarmellose, silloon silicon dioxide, magnesium stearate.
Nchikota ihe nkiri: odo odo (02B38190) (hypromellose 2910, titanium dioxide (E171), talc, macrogol 400, odo iron oxide odo (E172).

Mbukota
10 na 30 mbadamba.

Omume ọgwụ
Jardins - hibdị Inhibitor Type 3 Sodium glucose Transporter Inhibitor

Jardins, ihe ngosi maka ojiji
2dị ọrịa shuga abụọ:
dị ka monotherapy na ndị ọrịa na-ezughị ezu nchịkwa glycemic naanị megide ndabere nke nri na mmega ahụ, nhọpụta nke metformin nke a na-ahụta adịghị mma n'ihi ntachi obi,
dị ka usoro njikọta na ndị ọrịa hypoglycemic ndị ọzọ, gụnyere insulin, mgbe ọgwụgwọ etinyere na njikọta na nri na mmega ahụ anaghị enye njikwa glycemic dị mkpa.

Ihe ngbanwe
hypersensitivity na akụkụ ọ bụla nke ọgwụ,
ụdị shuga 1
ọrịa mamịrị ketoacidosis,
Ọrịa ndị a na - adịghị ahụkebe (ụkọ lactase, ekweghị anabata lactose, glucose-galactose malabsorption),
ọdịda gbasara mkpịsị aka ya na GFR ×

Usoro onunu ogwu:

Nkọwa
10 mg mbadamba
Mpempe akwụkwọ okirikiri biconvex gbara ya gburugburu, kpuchie ya na fim nwere agba odo na-acha odo odo na ihe osise ụlọ ọrụ dị n'otu akụkụ nke mbadamba ya na “S10” n'akụkụ nke ọzọ.
Mbadamba 25 mg
Mbadamba ụrọ nke biconvex nke nwere agba gbara agba, kpuchie ya na mpempe ihe nkiri nke agba odo na-acha odo odo, nke e sere na akara ụlọ ọrụ dị n'otu akụkụ nke mbadamba ya na “S25” n'akụkụ nke ọzọ.

Ngwongwo ogwu

Mlọ ọgwụ
A mụọla ọgwụ ọgwụ nke empagliflozin nke ọma na ndị ọrụ afọ ofufo ahụike na ndị ọrịa nwere ụdị shuga 2.
Egwu
Mgbe nchịkwa ọnụ gachara, etinyere empagliflozin ngwa ngwa, ọnụnọ kachasị nke empagliflozin na plasma ọbara (Cmax) ruru 1.5 awa. Mgbe ahụ, itinye uche nke empagliflozin na plasma belatara n'ụzọ abụọ.
Ke ama ọkọbọ empagliflozin, nkezi ebe n'okpuru usoro nlebara anya oge (AUC) n'oge ọkwa plasma kwụ ọtọ bụ 4740 nmol x h / l, yana Cmax - 687 nmol / l.
Ndị ọgwụ ọgwụ empagliflozin na ndị ọrụ afọ ofufo nwere ahụike na ndị ọrịa nwere ụdị shuga 2 bụkarị otu.
Iri nri adighi enwe ogwu di egwu banyere ogwu ogwu nke empagliflozin.
Nkesa
Olu nke nkesa Plasma steetị dị ka 73.8 lita. Mgbe nchịkwa ọnụ gasịrị site n'aka ndị ọrụ afọ ofufo nwere ahụike nke akpọrọ empagliflozin 14 C, ọgwụ mgbochi plasma bụ 86%.
Metabolism
Mainzọ kachasị nke metabolagliflozin metabolism n’ime mmadụ bụ glucuronidation na ntinye nke uridine-5'-diphospho-glucuronosyltransferases UGT2B7, UGT1A3, UGT1A8 na UGT1A9. Ihe ndị na-achọpụtakarị metabolites nke empagliflozin bụ glucuron conjugates atọ (2-0, 3-0 na 6-0). Mmetụta sistemụ nke metabolite ọ bụla dị ntakịrị (ihe na-erughị 10% nke ngụkọta nke empagliflozin).
Ojiji
Iwepu ọkara ndụ bụ ihe dịka awa 6.4. N'ihe banyere iji empagliflozin otu ugboro kwa ụbọchị, a na-enweta mkpo plasma kwụsịrị mgbe ọgwụ nke ise gasịrị. Mgbe nchịkwa ọnụ nke akara ejiri akara 14 C mara na ndị ọrụ afọ ofufo ahụike, ihe dị ka 96% nke ọgwụ ahụ ka ewepụrụ (site na eriri afọ 41% na akụrụ 54%). Site na eriri afọ, ọtụtụ n'ime ọgwụ akpọrọ agbanweela agbanweghị. Ọ bụ nanị ọkara nke ọgwụ akpọrọ ahaghị ya na akụrụ na-agbanweghị.
Pharmacokinetics na ndị ọrịa ọrịa pụrụ iche
Renrụ ọrụ na-arụ ọrụ na ụlọ
N'ime ndị ọrịa nwere ajọ akụrụngwa dị nro, na-akwụkarị ọtọ (30 2) yana ndị ọrịa nwere ọdịda akụrụngwa njedebe, AUC nke empagliflozin mụbara, n'otu n'otu, ihe dịka 18%, 20%, 66%, na 48% ma e jiri ya tụnyere ndị ọrịa nwere ọrịa nkịtị. ọrụ akụrụ. N'ime ndị ọrịa nwere nnukwu akwara ezughị oke na ndị ọrịa nwere njedebe akụrụngwa njedebe, oke plasma ịta nke empagliflozin yiri ụkpụrụ kwekọrọ na ndị ọrịa nwere ọrụ gbasara ọrụ nkịtị. N'ime ndị ọrịa nwere nsogbu gbasara akụrụ dị obere ma dị njọ, ihe kachasị plasma nke empagliflozin dị ihe dị ka 20% karịa ndị ọrịa nwere ọrụ mkpo nkịtị. Nchịkọta nyocha nke ndị na-ahụ maka ọgwụ na onu ogugu na-egosi na mkpochapụ nke empagliflozin belatara na ibelata GFR, nke butere mmụba na ọgwụ ahụ.
Ọrụ imeju na-arụ ọrụ
N'ime ndị ọrịa nwere ọrụ imeju na-arụ ọrụ nke obere, agafeghị oke na nnukwu nha (dịka ọkwa ụmụaka-Pugh si kọọ), ụkpụrụ AUC nke empagliflozin mụbara, n'otu n'otu, ihe dịka 23%, 47% na 75%, na ụkpụrụ Stax, otu n'otu, ihe dịka 4%, 23 % na 48% (ma e jiri ya tụnyere ndị ọrịa nwere ọrụ imeju nkịtị).
Isi uka, aru nwoke, agbụrụ na afọ enweghị mmetụta ọmarịcha ụlọ ọgwụ na ọgwụ ọgwụ nke ọgwụ emagliflozin.
Childrenmụaka
Emebeghị nnyocha banyere ọgwụ ọgwụ nke empagliflozin n'ime ụmụaka.

Ihe ngbanwe

• Hypersensitivity n'akụkụ ọ bụla nke ọgwụ ahụ,
• Ọrịa shuga 1dị 1
• Ọrịa mamịrị ketoacidosis
• Ọrịa ọgbụgba sitere oke oke (ụkọ lactase, ekweghị anabata lactose, glucose-galactose malabsorption),
• Mkpesa ikpere na GFR 2 (n'ihi enweghị ike),
• Ime na inye ara,
• Ihe karịrị afọ 85
• Ojikọtara ya na analogues nke glucagon dị ka peptide 1 (n'ihi ụkọ data na arụmọrụ yana nchekwa),
• Undermụaka na-erubeghị afọ 18 (n'ihi ezughi oke data na arụmọrụ yana nchekwa).

Mmetụta akụkụ
Ọnọdụ dị oke njọ nke ihe ọjọọ na ndị ọrịa na-anata empagliflozin ma ọ bụ placebo na ule ụlọ ọgwụ yiri nke ahụ. Mmeghachi omume kachasị emetụta bụ hypoglycemia, nke a hụrụ site na iji nke empagliflozin yana mgbakwunye na sulfonylurea ma ọ bụ ọgwụ insulin (lee nkọwa nke mmeghachi omume ọjọọ nke mmadụ).
Mmeghachi omume ọjọọ a chọpụtara na ndị ọrịa na-anata empagliflozin n'ọmụmụ ihe nchịkwa placebo ka etinyere na Tebụlụ n'okpuru (a na-ahọta mmeghachi omume dịka akụkụ na sistemụ si dị na usoro nke MedDRA họọrọ) na ngosipụta nke oge ha zuru oke. A kọwapụtara otu ugboro ugboro dị ka ndị a: ugboro ugboro (> 1/10), ugboro ugboro (si>, 1/100 ruo> 1/1000 ruo> 1/10000 na Nkọwa nke mmeghachi omume ọjọọ nke onwe onye
Hypoglycemia
Ihe kpatara hypoglycemia dabere na hypoglycemic hypoglycemic ọgwụgwọ ejiri.
Ọrịa hypoglycemia obere (glucose ọbara 3.0 - 3.8 mmol / L (54-70 mg / dl)) Ọnọdụ nke hypoglycemia dị nro yiri nke ndị ọrịa na-ewere empagliflozin ma ọ bụ placebo dị ka monotherapy, yana mgbe agbakwunye empagliflozin na metformin na n'ihe banyere mgbakwunye nke empagliflozin na pioglitazone (± metformin). Mgbe enyere empagliflozin yana ngwakọta na usoro metformin na sulfonylurea, onodu hypoglycemia dị elu (10 mg: 10.3%, 25 mg: 7.4%) karịa na placebo na otu agwakọta (5.3%).
Nnukwu hypoglycemia (glucose ọbara dị n'okpuru 3 mmol / L (54 mg / dL))
Ọrịa hypoglycemia yiri nke ndị ọrịa na-ewere empagliflozin na placebo dị ka monotherapy. Mgbe enyere empagliflozin yana ngwakọta na ntinye metformin na sulfonylurea, nnabata hypoglycemia dị elu (10 mg: 5.8%, 25 mg: 4.1%) karịa na placebo na otu agwakọta (3.1%).
Urinjọ ngwa ngwa
Ugboro ugboro nke urination na-abawanye (akara dị ka pollakiuria, polyuria, nocturia bụ nke a na-enyocha) dị elu na empagliflozin (na 10 mg: 3.4%, na dose nke 25 mg: 3.2%) karịa na placebo (1 %). Ọnọdụ nke nocturia bụ ihe yiri otu n'ime ndị ọrịa na - ewere empagliflozin yana n'ìgwè ndị ọrịa na - ewere placebo (ihe na - erughị 1%). Ike nke mmetụta ndị a dị nfe ma ọ bụ agafeghị oke.
Ọrịa ọnya na-efe efe
Ọnọdụ nke ọrịa urinary na-efe efe yiri nke ahụ na empagliflozin 25 mg na placebo (7.6%), mana nke kachasị elu na empagliflozin 10 mg (9.3%). Dị ka ọ dị placebo, ọrịa urinary na-enwekarị na empagliflozin bụ ndị a na-ahụkarị ebe ndị ọrịa nwere ọrịa ọnya na-efe efe na nke na-eme ugboro ugboro. Ọnọdụ nke ọrịa urinary na-efe efe yiri nke ahụ na ndị ọrịa na-ewere empagliflozin na placebo. Ọrịa kansa na-efekarị ụmụ nwanyị.
Ọrịa afọ
Ọnọdụ nke ihe ọjọọ dị ka candidiasis, vulvovaginitis, balanitis, na ọrịa ndị ọzọ na-ebute ọnụọgụ ọrịa kachasị elu na empagliflozin (na 10 mg: 4.1%, na dose nke 25 mg: 3.7%) karịa na placebo (0 , 9%). Ọrịa ndị a na-ebutekarị bụ ndị inyom. Ike nke ọrịa ọnya nwoke bụ nke nwayọ ma ọ bụ agafeghị oke.
Hypovolemia
Ọnọdụ nke hypovolemia (nke gosipụtara site na mbelata ọbara mgbali, orthostatic artpot hypotension, akpịrị ịkpọ nkụ, nkụda mmụọ) yiri nke ahụ mgbe empagliflozin (na dose nke 10 mg: 0,5%. Na dose nke 25 mg: 0.3%) na placebo (0, 3%). N’ime ndị ọrịa toro afọ 75, ọnọdụ nke hypovolemia bụ ihe a pụrụ iche n’ebe ndị ọrịa na-ewere empagliflozin na dose nke 10 mg (2.3%) na placebo (2.1%), mana dị elu na ndị ọrịa na-ewere empagliflozin na dose 25 mg (4.4%) )

Dodoụbiga ya ókè

Mmekọrịta na ọgwụ ndị ọzọ
Na ntule mmekọrịta nyocha ọgwụ ọgwụ vitro
Empagliflozin anaghị egbochi, inactivate, ma ọ bụ kpalite CYP450 isoenzymes. Routezọ nke metabolism nke empagliflozin mmadụ bụ glucuronidation yana ntinye nke uridine-5'-diphospho-glucuronosyltransferases UGT2B7, UGT1A3, UGT1A8 na UGT1A9. Empagliflozin anaghị egbochi UGT1A1. Mkparịta ụka ọgwụ ọjọọ nke empagliflozin na ọgwụ ndị na-anọchi anya CYP450 na UGT1A1 isoenzymes bụ ihe a na-agaghị ele anya.
Empagliflozin bụ mkpụrụ maka glycoprotein P (P-gp) na protein cancer ara ure (BCRP). mana na ọgwụgwọ ogwu anaghị egbochi protein ndị a. Dabere na data sitere na ọmụmụ banyere vitro, ekwenyere na ike nke empagliflozin soro ndị ọgwụ na-eji glycoprotein P (P-gp) meekọrịta mmekọrịta. Empagliflozin bụ mkpụrụ maka ndị na - eburu ikuku anionic: OATZ, OATP1B1 na OATP1VZ, mana ọ bụghị ntụgharị maka ndị na - ebu ikuku anionic 1 (OAT1) na ndị na - ebu cationic 2 (OST2). Agbanyeghị, mmekọrịta mmadụ na ọgwụ nke empagliflozin ya na ọgwụ ndị na-edochi protein na ebu dị ka akọwara n’elu anaghị ele anya na-agaghị enwe isi.
Na ntule mmekọrịta mkparịta ụka nke vivo
Aclọ ọgwụ ọgwụ nke empagliflozin anaghị agbanwe agbanwe na ndị ọrụ afọ ofufo mara mma mgbe ejiri ya na metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, torasemide na hydrochlorothiazide. Combinedjikọtara ojiji nke empagliflozin na gemfibrozil, rifampicin na probenecid gosipụtara mmụba na AUC nke empagliflozin site na 59%, 35% na 53%, n'otu n'otu, mana echeghị mgbanwe ndị a dị ka ọgwụ.
Empagliflozin enweghị mmetụta dị egwu na ụlọ ọgwụ na ọgwụ ọgwụ nke metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin. digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide na mgbochi igbo.
Diuretics
Empagliflozin nwere ike ịkwalite mmetụta diuretic nke thiazide na "loop", nke n'aka nke ya nwere ike ịbawanye n'ihe ize ndụ nke akpịrị ịkpọ nkụ na hypotension.
Insulin na ọgwụ nke na - eme ka ihe nzuzo ya dịkwuo elu
Insulin na ọgwụ na-eme ka ihe nzuzo ya dịkwuo elu, dị ka sulfonylureas, nwere ike ịbawanye ohere nke hypoglycemia. Ya mere, n'iji insagliflozin na-ejikọ ya na insulin na ọgwụ na-eme ka nzuzo ya dịkwuo elu, ọ nwere ike ịdị mkpa iji belata ọgwụ ha, iji zere ihe ize ndụ nke hypoglycemia.

Ntụziaka pụrụ iche

Mmetụta ikike ịkwọ ụgbọala na usoro
Emebeghị nnyocha omumu ihe banyere nsogbu nke emagharilozin n’ikike igbapu ugbo ala na ihe ndi ozo. Ndị ọrịa kwesịrị ịkpachara anya mgbe ha na-anya ụgbọ ala na usoro, ebe ọ bụ na mgbe ị na-eji ọgwụ JARDINS (karịsịa yana njikọta na usoro sulfonylurea na / ma ọ bụ insulin), hypoglycemia nwere ike ịmalite.

Emeputa

Aha na adres ebe a na-emepụta ọgwụ
Beringer Ingelheim Pharma GmbH & Co.KG
Binger Strasse 173, 55216 Ingelheim am Rhein, Germany

Nwere ike nweta ozi ndị ọzọ gbasara ọgwụ ahụ, zigakwa mkpesa na ozi gbasara ajọ ihe na adres ndị a na Russia
LLC Beringer Ingelheim
125171. Moscow, Leningradskoye Shosse, 16A p. 3

Jardins ọgwụ

Ndị a bụ mbadamba ihe mkpuchi. Ọdịdị: edo edo edo, okpu ma ọ bụ okirikiri (dabere na usoro onunu ogwu), imewe - mbadamba biconvex nke nwere mpekere na akara akara ụlọ ọrụ nke onye na-emepụta ya n'otu akụkụ. Emepụtara otu ọgwụ na Germany iji belata glucose ọbara n'ọrịa shuga nke 2.

Ọgwụ hypoglycemic ọgwụ, ya na ihe na - arụ ọrụ - empagliflozin. Egosiputara ihe ichoro na uzo onodu ya si di na tebul:

Usoro onunu ogwu 1 mbadamba (mg)

odo odo opadray (hypromellose, titanium dioxide, talc, macrogol, iron dye oxide odo)

Omume ọgwụ

Empagliflozin bụ onye atụgharịgharịgharị, na-arụ ọrụ nke ukwuu, na-ahọta onye na-ebuga ụdị glucose dị afọ 2 sodium. Ekwenyesiri ya na sayensị na empagliflozin na-ahọrọ oke maka ndị ọzọ na-eduzi glucose homeostasis na anụ ahụ. Nri ahụ nwere mmetụta glycemic na ndị ọrịa nwere ọrịa shuga nke 2 site na ibelata nnabata shuga na akụrụ. Ole glucose wepụtara site na usoro a dabere na ọnụego nzacha nke glomeruli nke akụrụ.

Nnyocha e mere egosiwo na ndị ọrịa nwere ọrịa shuga nke 2, ọ̀tụ̀tụ̀ glucose dị elu mụbara mgbe ọgwụ ọgwụ mbụ e butere na mmetụta ahụ rutere otu ụbọchị. Ihe ngosi ndị a dịgidere mgbe ha na-ewere 25 mg nke empagliflozin maka otu ọnwa. Mmụba nwere ume nke akụrụ sitere na akụrụ mere ka mbelata n'ọbara ya na ọbara onye ọrịa. Ọgwụ na -ebelata mkpụkọ glucose dị n'ọbara, n'agbanyeghị nri nri.

Akụkụ insulin na-eme ka ọ ghara ịdị obere ọrịa hypoglycemia.Usoro nke ihe eji arụ ọrụ arụ ọrụ anaghị adabere na ọrụ nke agwaetiti Langerhans na metabolulin metabolism. Ndị ọkà mmụta sayensị chọpụtara mmetụta dị mma nke empagliflozin na peptides peptides nke ọrụ mkpụrụ ndụ ndị a. Mmụba glucose na-aba ụba na-eduga na calorie, nke na-ebelata oke ahụ. N'oge a na-eji empagliflozin, a na-ahụ glucoseuria.

Ihe ngosi maka ojiji

Ekwuputara ya maka ndị ọrịa nwere ụdị ọrịa shuga 2 na nri siri ike ma na-egwu egwuregwu, nke na-agaghị ekwe omume ịchịkwa ndị na-egosipụta glycemic n'ụzọ kwesịrị ekwesị. Site na ntachi obi Metformin, monotherapy na Jardins kwere omume. Ọ bụrụ na ọgwụgwọ enweghị mmetụta kwesịrị ekwesị, ijikọ ya na ọgwụ hypoglycemic ndị ọzọ, gụnyere insulin, ga-ekwe omume.

Jardins

A na-ewere mbadamba okwu ọnụ, n'agbanyeghị oge ụbọchị ma ọ bụ nri. A na-atụ aro ịmalite ịmalite na 10 mg kwa ụbọchị, ọ bụrụ na mmetụta dị mma anaghị eme, wee mụbaa ruo 25 mg. Ọ bụrụ na n'ihi ihe ụfọdụ ha ewereghị ọgwụ ahụ, mgbe ahụ ị ga-a itụ ya ozugbo, dịka ha chetara. Enweghi ike iwesa okpukpu abụọ. N'ọnọdụ arụ ọrụ na-emebi emebi, a chọghị mgbazi, anaghị anabata ndị ọrịa nwere ọrịa akụrụ.

N’oge ime ime

Ihe mbadamba ụrọ n'oge ime dị contraindicated n'ihi ụkọ data sitere na ọmụmụ nke ịdịmma na nchekwa. Ihe omumu omumu nke umu anumanu gosiputala na ohere nke enwere ike inwe nsogbu nokwa na obara uteroplacental. E wepu ihe ize ndụ nke itinye nwa ebu n’afọ na nwa amụrụ ọhụrụ. Ọ bụrụ na ọ dị mkpa, ịkwesịrị ịkwụsị ị theụ ọgwụ n’oge ịtụrụ ime.

Na nwata

Treatmentgwọ ọgwụ ya na ụmụaka yana ụmụaka nọ n’agbata afọ iri na asatọ ka machibidoro ya iwu. Ejikọtara ya na data nyocha ezughi oke. Egosiputaghi nzizi na nchekwa nke ihe eji eme ihe achoglolozin maka umu aka. Iji wepu ihe egwu nke nsogbu ahụike ụmụaka, a machibidoro Jardins. Ọ ka mma ịhọrọ ọgwụ ọzọ a gbaara ezi àmà.

Ihe onyonyo 3D

Nkọwa nke ụdị usoro onunu ogwu

10 mg mbadamba: gburugburu biconvex nwere beveled n'ọnụ, kpuchie ya na fim nke agba odo na-acha odo odo, ya na ihe osise nke ụlọ ọrụ akara n'otu akụkụ na "S10" n'akụkụ nke ọzọ.

Mbadamba 25 mg: oval biconvex nwere beveled n'ọnụ, kpuchie ya na fim nke agba odo na-acha odo odo, kanyere akara ụlọ ọrụ dị n'otu akụkụ na "S25" n'akụkụ nke ọzọ.

Mlọ ọgwụ

Empagliflozin bụ onye na - atụgharị uche dị ukwuu ma na - esokwa onye na - egbochi ụdị ụgbọ mmiri sodium abụọ na - akpata glucose na ntinye uche chọrọ igbochi 50% nke ọrụ enzyme (IC)₅₀), hà nmol 1.3. Nhọrọ nke empagliflozin ji okpukpu 5,000 dị elu karịa n ’ụdị onye na-ebugharị gluu na-akpata glucose dị n’ime 1, bụ́ nke na-ahụ maka ịnakwere glucose na eriri afọ. Na mgbakwunye, achọpụtara na empagliflozin nwere oke nhọrọ maka ndị na-ebuga glucose ndị ọzọ na-ahụ maka glucose homeostasis n'ụdị anụ ahụ dị iche iche.

2dị sodium na-adabere n'ụgbọ ibu gwọọ 2 bụ protein na-ebu ebu ibu nke na-ahụ maka ịmaliteghachi glucose site na renal glomeruli ma banye n'ọbara. Empagliflozin na-emezi nchịkwa glycemic na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa mellitus (T2DM) site na ibelata realsorption kelion. Ọbara glucose na-eto site na akụrụ jiri usoro a dabere na ntinye glucose dị n'ọbara na GFR. Mmachi nke ndị na-ebugharị glucose n'ụdị 2 nke ndị ọrịa nwere ụdị ọrịa shuga 2 na hyperglycemia na-eduga na mkpochapụ glucose oke site na akụrụ.

N’ime ọmụmụ izu ụka anọ, a chọpụtara na n’ime ndị ọrịa nwere ọria mamịrị nke 2, a na-eme ka nri glucose gbagowe ozugbo ejiri ọgwụ emagliflozin nke mbụ rụọ ọrụ a, wee gaa n’ihu awa 24. Mmụba nke mgbatị ahụ akụrụ gara n’ihu ruo mgbe ngwụcha ọgwụgwọ, na-aka ogwu nke 25 mg 1 oge kwa ubochi, na onwa dika 78 g / ubochi. N'ime ndị ọrịa nwere ụdị shuga nke 2, akụrụba mụbara site na akụrụ mere ka mbelata glucose plasma ozugbo.

Empagliflozin (na dose nke 10 na 25 mg) na -ebelata mkpụkọ glucose na plasma ọbara ma n'ihe gbasara ibu ọnụ na mgbe ha risịrị nri.

Usoro ihe omume nke empagliflozin na-adabere na ọnọdụ arụ ọrụ nke mkpụrụ ndụ beta nke pancreatic na metabolism metabolism, nke na-enye aka na ihe egwu dị ala nke mmepe hypoglycemia. Achọpụtala mmetụta dị mma nke empagliflozin na akara ndị nọchiri anya arụmọrụ beta, gụnyere ntanye HOMA-β (ihe atụ maka ịlele homeostasis-B) na oke nke proinsulin na insulin. Na mgbakwunye, iwepụ glucose ọzọ site na akụrụ na-eme ka a ghara inwe calorie, nke na-esobelata olu nke anụ ahụ adipose na mbelata nke ahụ.

A na-ahụkarị Glucosuria n'oge eji empagliflozin yana ntakịrị mmụba na diuresis, nke nwere ike itinye aka na mbelata ọbara mgbali elu.

Na omumu ihe omumu ebe eji eji monaghelolodi mee ihe dika monotherapy, ogwu ngwakọta ya na metformin, ogwu ihe mejuputara ya na metformin n’ime ndi oria nwere oria ohuru a gbara aru, ihe jikoro ya na metformin na uzo ogwu, ngwusi ogwu ya na pioglitazone +/− metformin, nmekorita ogwu ya na linagliptin na ndị ọrịa nwere ọrịa mellitus nke abụọ chọpụtara ọrịa ọhụụ, njikọta ọgwụgwọ na linagliptin, agbakwunyere ọgwụgwọ metformin, ọgwụgwọ njikọta na linagliptin na ntụnyere paracet o n'ime ndị ọrịa na-enweghị nchịkwa glycemic zuru oke mgbe ha na-ewere linagliptin na metformin, ọgwụgwọ njikọta na metformin vesos glimepiride (data sitere n'ọmụmụ afọ 2), njikọta ọgwụ na insulin (otutu insulin injection regimen) +/− metformin, njikọta ọgwụ na basal insulin. , ngwakọta ọgwụgwọ na Dhib-4 inhibitor, metformin +/− ọgwụ ọgwụ hypoglycemic ọzọ, ọnụọgụ dị ịrịba ama na HbA1 gosipụtara_c, mbelata nke ịba uru glucose plasma na-ebu ọnụ, yana mbelata ọbara mgbali elu na oke ahụ.

Otu omumu ihe omumu nyochara uto nke ogwu Jardins ® na ugboro ugboro ihe omume obi na ndi oria nwere oria 2 na oke oria obi (nke akowara dika ọnụnọ nke otu ọrịa na / ma ọ bụ ọnọdụ: akwara ọnya akwara (ọrịa akụkọ akwara nke ọrịa myocardial infarction, coronary artery bypass grafting)) , IHD nwere mmebi nke otu arịa ọbara, IHD nwere mmebi ọtụtụ arịa arịa), akụkọ ihe mere eme nke ischemic ma ọ bụ hemorrhagic strok, ọrịa akwara akụkụ na ma ọ bụ na-enweghị mgbaàmà) na-enweta ọkọlọtọ hydrochloric ọgwụ, nke gụnyere hypoglycemic elekọta mmadụ na mmadụ maka ọgwụgwọ nke ọrịa obi. A na-enyocha ikpe nke ọnwụ obi, adịghị ike myocardial infarction na ọrịa strok na-enweghị egbu dịka isi ihe mmechi. Ọrịa obi, ọnwụ nke izugbe, mmepe nke nephropathy ma ọ bụ ọganiihu nke nephropathy, yana ụlọ ọgwụ maka ọrịa obi na-ahọpụtara ihe ndị ọzọ ebu ụzọ kwuo.

Empagliflozin emeela ka ndụ ka mma site n’ibelata okwu gbasara ọrịa obi. Empagliflozin belatara ihe ize ndụ nke ụlọ ọgwụ maka nkụchi obi. Ọzọkwa, n'ọmụmụ ihe ọmụmụ, e gosipụtara na ọgwụ Jardins ® belatara ihe ize ndụ nke nephropathy ma ọ bụ ọganiihu nke nephropathy.

N'ime ndị ọrịa nwere macroalbuminuria mbụ, achọpụtara na ọgwụ Jardins significantly dịkarịrị elu karịa na-etinye ya na placebo dugara na Normo- ma ọ bụ microalbuminuria kwụ ọtọ (oke ihe egwu 1.82, 95% CI: 1.4-2.37).

Mlọ ọgwụ

A mụọla ọgwụ ọgwụ nke empagliflozin nke ọma na ndị ọrụ afọ ofufo nwere ahụike na ndị ọrịa nwere ụdị shuga 2.

Egwu. Empagliflozin mgbe enwetara nchịkwa ọnụ, C_max E meturu empagliflozin na plasma mgbe awa 1.5 gachara, mmachi nke empagliflozin na plasma belatara n'ụzọ abụọ. Mgbe iwere empagliflozin na dose 25 mg otu ugboro kwa ụbọchị, nkezi AUC na oge C_ss na plasma dị 4740 nmol · h / l, na ọnụ ahịa nke C_max - 687 nmol / L.

Ndị ọgwụ ọgwụ empagliflozin na ndị ọrụ afọ ofufo nwere ahụike na ndị ọrịa nwere ụdị shuga 2 bụkarị otu.

Iri nri adighi enwe ogwu di egwu banyere ogwu ogwu nke empagliflozin.

Nkesa. Ise_d n'oge plasma C_ss dị ihe dị ka lita 73.8. Mgbe nchịkwa ọnụ gasịrị site n'aka ndị ọrụ afọ ofufo nwere ahụike nke akpọrọ empagliflozin 14 C, ọgwụ mgbochi plasma bụ 86,2%.

Metabolism. Mainzọ nke usoro metabolagliflozin metabolism n’ime mmadụ bụ glucuronidation site na ntinye UDP-GT (UGT2B7, UGT1A3, UGT1A8 na UGT1A9). Metabolites ndị a na-ahụkarị nke empagliflozin bụ glucuronide 3 glucuronic (2-O, 3-O na 6-O). Mmetụta sistemụ nke metabolite ọ bụla dị ntakịrị (ihe na-erughị 10% nke ngụkọta nke empagliflozin).

Ojiji. Ndi_1/2 bụ ihe dịka awa 12.4. N'ihe banyere iji empagliflozin 1 oge kwa ụbọchị C_ss enwetara na plasma mgbe emume nke ise gasịrị. Mgbe nchịkwa ọnụ nke akara ejiri akara 14 C mara na ndị ọrụ afọ ofufo ahụike, ihe dị ka 96% nke ọgwụ ahụ ka ewepụrụ (site na eriri afọ 41% na akụrụ 54%).

Site na eriri afọ, ọtụtụ n'ime ọgwụ akpọrọ agbanweela agbanweghị. Ọ bụ nanị ọkara nke ọgwụ akpọrọ ahaghị ya na akụrụ na-agbanweghị.

Pharmacokinetics na ndị ọrịa ọrịa pụrụ iche

Renrụ ọrụ na-arụ ọrụ na ụlọ. N'ime ndị ọrịa nwere obere (60 2), agafeghị oke (30 2), nnukwu (GFR 2) ọdịda ọdịda, yana ndị ọrịa nwere ọdịda ezughị ezu, AUC nke empagliflozin mụbara site na ihe dịka 18, 20, 66, na 48%, n'otu aka ahụ, ma e jiri ya tụnyere ndị ọrịa nwere arụ ọrụ akụrụ. N'ime ndị ọrịa nwere ezughị oke gbasara akụrụngwa yana ndị ọrịa nwere njedebe ọdịda ezumike nka C_max empagliflozin na plasma yiri ụkpụrụ kwekọrọ na ndị ọrịa nwere ọrụ gbasara ụlọ ọrụ. N'ime ndị ọrịa nwere nnukwu akụrụ siri ike_max empagliflozin na plasma dị ihe dị ka 20% karịa ndị ọrịa nwere ọrụ mkpo nkịtị. Nchịkọta nyocha nke ndị na-ahụ maka ọgwụ na onu ogugu na-egosi na mkpochapụ nke empagliflozin belatara na ibelata GFR, nke butere mmụba na ọgwụ ahụ.

Ọrụ imeju na-arụ ọrụ. N'ime ndị ọrịa nwere ọrụ imeju na-arụ ọrụ nke ogo dị nwayọọ, na-agafe agafe na nke siri ike (dị ka nhazi nke ụmụaka-Pugh), ụkpụrụ AUC nke empagliflozin mụbara ihe dịka 23, 47 na 75%, n'otu n'otu, na C_max odika 4, 23 na 48%, otu (ma e jiri ya tụnyere ndị ọrịa nwere ọrụ imeju nkịtị).

BMI, okike, agbụrụ, na afọ enwebeghị mmetụta dị mkpa na ụlọ ọgwụ na ọgwụ ọgwụ nke empagliflozin.

Childrenmụaka. Emebeghị nnyocha banyere ọgwụ ọgwụ nke empagliflozin n'ime ụmụaka.

Ihe ngosiputa nke ogwu Jardins ®

2dị ọrịa shuga abụọ:

- dị ka monotherapy na ndị ọrịa na-ezughị ezu nchịkwa glycemic naanị megide ndabere nke nri na mmega ahụ, nhọpụta nke metformin nke na-agaghị ekwe omume n'ihi ntachi obi,

- dịka ọgwụ nkwonkwo ya na ndị ọrụ hypoglycemic ndị ọzọ, gụnyere insulin, mgbe ọgwụgwọ etinyere ya na nri na mmega ahụ anaghị enye njikwa glycemic dị mkpa.

E gosipụtara ya maka ndị ọrịa nwere ọrịa shuga nke abụọ ọrịa obi na oke egwu obi * yana yana usoro ọgwụgwọ maka ọrịa obi iji belata:

- ngụkọta ọnwụ site na mbenata ọnwụ nke ọbara.

- onwu obi ma obu ulo ogwu maka obi adighi nma.

A na-akọwapụta ihe dị oke egwu ọrịa obi dị ka ọnụnọ ọ dịkarịa ala otu ọrịa na / ma ọ bụ ọnọdụ: ọrịa obi obi (akụkọ ihe mere eme nke akwara obi, ọrịa akwara na-emebi otu arịa, akwara obi na mbibi nke ọtụtụ akwara ọbara), ọrịa akpịrị ọbara ma ọ bụ ọbara ọgbụgba. akụkọ banyere ọrịa akwara na-arịa ya (ma ọ bụ na-enweghị mgbaàmà).

Ime na lactation

A na-egbochi ojiji nke empagliflozin n'oge afọ ime n'ihi data ezughi oke na arụmọrụ yana nchekwa.

Ihe omuma enwetara na omumu omumu banyere umu anumanu na egosi ezi nnabata nke empagliflozin n’ime mmiri ara. E wezuga ohere ịmụrụ nwa amụrụ ọhụrụ na ụmụaka n’oge a na-enye nwa ara. A na - egbochi contraagliflozin maka inye ara ara. Ọ bụrụ na ọ dị mkpa, a ga-akwụsị ịhapụ ịagụ empagliflozin mgbe a na-enye nwa ara.

Nsonaazụ

Ọnọdụ dị oke njọ nke ihe ọjọọ na ndị ọrịa na-anata empagliflozin ma ọ bụ placebo na ule ụlọ ọgwụ yiri nke ahụ. Mmeghachi omume kachasị emetụta bụ hypoglycemia, nke a hụrụ site na iji nke empagliflozin yana mgbakwunye na ọgwụ ma ọ bụ insulin (lee. Nkọwa nke mmeghachi omume oghom).

Mmeghachi omume ọjọọ ndị a hụrụ na ndị ọrịa na-anata empagliflozin n'ọmụmụ ihe nchịkwa placebo bụ ndị a ka e gosipụtara n'okpuru ebe a MedDRA usoro) na-egosi oge ha zuru oke. A kọwapụtara otu ugboro ugboro dị ka ndị a: oge ​​mgbe (≥1 / 10), ọtụtụ mgbe (site na ≥1 / 100 ruo n'ọbara ọbara, orthostatic artpot hypotension, akpịrị ịkpọ nkụ, nkụda mmụọ) bụ otu ihe ahụ n'ihe banyere empagliflozin (na ọnụọgụ 10 mg - 0.6%, na onodu ogwu nke 25 mg - 0.4%) na placebo (0.3%). N’ime ndị ọrịa toro afọ 75, ọnọdụ nke hypovolemia bụ ihe a pụrụ ịbara na ndị ọrịa na-ewere empagliflozin na dose nke 10 mg (2.3%) na placebo (2.1%), mana dị elu na ndị ọrịa na-ewere empagliflozin na dose 25 mg (4.3%) )

Mmekorita

Diuretics. Empagliflozin nwere ike ịkwalite nsonaazụ nke thiazide na akwara loop, nke, n'aka nke ya, nwere ike ịbawanye ihe ize ndụ nke akpịrị mmiri na hypotension akwara.

Insulin na ọgwụ nke na - eme ka ihe nzuzo ya dịkwuo elu. Insulin na ọgwụ na-eme ka ihe nzuzo ya dịkwuo elu, dị ka sulfonylureas, nwere ike ịbawanye ohere nke hypoglycemia. Ya mere, n'iji insagliflozin na-ejikọ ya na insulin na ọgwụ na-eme ka nzuzo ya dịkwuo elu, ọ nwere ike ịdị mkpa iji belata ọgwụ ha, iji zere ihe ize ndụ nke hypoglycemia.

Ntụle nke mmekọrịta mmekọrịta ọgwụ na vitro. Empagliflozin anaghị egbochi, inactivate, ma ọ bụ kpalite CYP450 isoenzymes. Routezọ nke metabolism nke empagliflozin mmadụ bụ glucuronidation site na ntinye UDP-GT (UGT2B7, UGT1A3, UGT1A8 na UGT1A9). Empagliflozin anaghị egbochi UGT1A1, UGT1A3, UGT1A8, UGT1A9 ma ọ bụ UGT2B7. Mkparịta ụka ọgwụ ọjọọ nke empagliflozin na ọgwụ ndị na-anọchi anya CYP450 na UGT isoenzymes bụ ndị a na-eleghi anya. Empagliflozin bụ mkpụrụ maka P-gp na protein na-ekpebi BCRP, mana na usoro ọgwụgwọ anaghị egbochi protein ndị a. Dabere na data sitere na ọmụmụ in vitro , ekwenyere na ikike nke empagliflozin soro ndị ọgwụ na-emekọrịta ihe P-gpbụ eleghi anya. Empagliflozin bụ mkpụrụ maka ndị na - eburu ikuku anionic: OAT3, OATP1B1 na OATP1B3, mana abụghị ihe ndabere maka ndị na - eburu ikuku anionic 1 (OAT1) na ndị na - ebu cationic 2 (OCT2). Agbanyeghị, mmekọrịta mmadụ na ọgwụ nke empagliflozin ya na ọgwụ ndị na-edochi protein na ebu dị ka akọwara n’elu anaghị ele anya na-agaghị enwe isi.

Ntụle mmekọrịta mmekọrịta ọgwụ na vivo. Site na ijiri empagliflozin na ọgwụ ndị ọzọ a na-ejikarị, enwebeghị mmekọrịta dị n'etiti ọgwụ na ụlọ ọgwụ. Nsonaazụ nke ọmụmụ pharmacokinetic na-egosi na ọ dịghị mkpa ịgbanwe mkpụrụ ọgwụ ọgwụ Jardins while ka a na-eji ọgwụ ndị a na-ejikarị eme ya.

The pharmacokinetics nke empagliflozin anaghị agbanwe na ndị ọrụ afọ ofufo mara mma mgbe ejiri ya na metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, verapamil, ramipril, simvastatin, na ndị ọrịa nwere ụdị shuga 2 ma ọ bụrụ na ejiri ya na torasemoridide na hydrochloride hydrochlor.

Site na iji empagliflozin jikọtara ya na gemfibrozil, rifampicin na probenecid, mmụba na AUC nke empagliflozin site na 59, 35 na 53%, n'otu n'otu, agbanyeghị, atụghị mgbanwe ndị a echiche dị ka ọgwụgwọ.

Empagliflozin enweghị mmetụta dị egwu na ọgwụ na ọgwụ ọgwụ nke metformin, glimepiride, pioglitazone, sitagliptin, linagliptin, warfarin, digoxin, ramipril, simvastatin, hydrochlorothiazide, torasemide na ọgwụ mgbochi na mma na ndị ọrụ afọ ofufo.

Mkparịta ụka ọgwụ ọjọọ

Ọ na - eme ka mkpụrụ ndụ diuretic dị iche iche na –eme ka mmetụta diuretic na hypotension ike. Ngwakọta insulin na sulfonylurea nwere ike ibute hypoglycemia. Site na ojiji ọgwụ a jikọtara ya na insulin, mbelata usoro ọgwụgwọ dị mkpa iji zere ọnọdụ hypoglycemic .. Mmekọrịta ọgwụ nke empagliflozin na ọgwụ ndị mejupụtara nke isoenzymes adịghị mma.

Empagliflozin - ihe na-arụ ọrụ na mbadamba nkume, anaghị emetụta ọgwụ ọgwụ ndị ọgwụ ndị a: Metformin, Glimepiride, Pioglitazone, Warfarin, Digoxin, Ramipril, Simvastatin, Hydrochlorothiazide, Torasemide na mgbochi mgbochi. Iji otu oge a na ọgwụ ndị a na-ejikarị, mgbanwe ọgwụ adịghị achọrọ.

Jardins Analogs

Na ahịa ọgwụ nke Russian Federation, enwere naanị otu ọgwụ mepụtara na ndabere nke ihe - empagliflovin. Jardins enweghị asambodo enyere aka. Mbadamba ụrọ hypoglycemic ndị ọzọ nwere ihe ọzọ na-arụ ọrụ n'ime ihe mejupụtara ma na-eme ihe dị iche na ahụ mmadụ. Ndị a gụnyere:

Jardins - ntuziaka maka ojiji, ọnụahịa, nyocha na analogues

A na-ewere ọrịa shuga mellitus dị ka otu n'ime ọrịa a na-ahụkarị na mbara ala. N’obodo Russia, ihe dị ka nde ụmụ amaala iri na-arịa ọrịa a. Ọtụtụ n'ime ha na-ahọrọ iji ọgwụ Jardins n'ihi ịdị irè ya.

Aha Latin bụ Jardiance. Ọgwụ INN: Empagliflozin (Empagliflozin).

Jardins nwere mmetụta antidiabetic.

Nhazi ATX: A10BK03.

Ogwu a di n ’udiri ogwu eji eme ihe. Otu mbadamba 1 nwere 25 ma ọ bụ 10 mg nke empagliflozin (ihe na-arụ ọrụ). Ihe ndi ozo:

• ntụ ntụ talcum
• titanium dioxide
• iron oxide na agba odo
• lactose monohydrate,
• Hyprolose
• cellulose microcrystals.

Ogwu a di n ’udiri ogwu eji eme ihe.

Mbadamba ụrọ dị n’ime blisters nke PC 10. Igbe dị 1 ma ọ bụ 3 na-eme ya.

Jiri nlezianya

Edere ọgwụ a nke ọma mgbe:

• ọrụ dị ala nke sel ndị dị na pancreas,
• Nchikota na mmanu ndi mmadu na insulin.
• ọrịa eriri afọ na-emetụta oke nsị mmiri,
• nká.

Usoro onunu ogwu na nhazi

A na-ewere ọgwụ ọnụ. Usoro ọgwụgwọ oge mbụ bụ 10 mg 1 oge kwa ụbọchị. Ọ bụrụ na ọgwụ a enweghị ike inye nchịkwa glycemic, mgbe ahụ, ọgwụ ahụ na-ebili na 25 mg. Usoro kachasị elu bụ 25 mg / ụbọchị.

A na-ewere ọgwụ ọnụ.

Ejikọghị iji mbadamba nkume n'oge ụbọchị ma ọ bụ ibubata nri. Ọ bụ ihe na-achọghị ka ụbọchị 1 tinye okpukpu abụọ.

Ọgwụ shuga site n'aka Jardins

Nnwale ndị ọrịa gosipụtara na ọgwụ a na-a isụ a theụ bụ naanị ọgwụ maka ọgwụgwọ maka ọrịa shuga mellitus (ụdị nke II), ebe enwere ike belata ihe egwu nke ọrịa CVD na ọnụ ọgụgụ ndị na-anwụ na ọrịa ahụ. Amachibidoro iji ọgwụ maka ndị ọrịa nwere ọrịa shuga 1.

Ihe akaebe nke ndi dibia na ndi oria banyere Jardins

Galina Aleksanina (onye na-achọ ọgwụgwọ), gbara afọ 45, St. Petersburg.

Ngwọta dị mma nke anaghị ebute nsonaazụ (na omume m). Ekwesiri ịkwụ ụgwọ dị elu maka ọrụ ọgwụ nke ọgwụ. A machibidoro mmetụta ị na-ahụ anya kpamkpam. Na mgbakwunye, ọ nweghị ọgwụ analogues na Russia, ọgwụ ndị yiri ya na-eme ihe dị iche.

Anton Kalink, dị afọ 43, Voronezh.

Ngwá ọrụ dị mma. M, dị ka onye ọrịa mamịrị nwere ahụmịhe, enwere m afọ ojuju kpamkpam n'ihe ọ na-eme. Ihe kachasị mkpa bụ iji nlezianya mụọ ntuziaka maka ojiji. Naanị na nke a ka enwere ike ịhapụ irighiri nsonaazụ, bụ nke emere n'onwe ya na omume. N'ime adịghị ike, mmadụ nwere ike ịmata ọdịiche dị naanị ụgwọ dị elu yana eziokwu ahụ bụ na ereghị ọgwụ ahụ n'ụlọ ahịa ọgwụ niile.

Jardins: Ntụziaka maka ojiji

Mlọ ọgwụ

Empagliflozin bụ onye agbanweegharị, na-agbasi mbọ ike, na-ahọrọ ma na-asọ mpi nke onye na-ebuga ụdị glucose abụọ sodium na ntinye uche chọrọ igbochi 50% nke ọrụ enzyme (IC50) nke 1.3 nmol.

Nhọrọ nke empagliflozin ji okpukpu puku ise dị elu karịa n ’ụdị onye na-ebuga glucose n'ụdị 1 sodium na-ahụ maka nnabata nke glucose na eriri afọ. Na mgbakwunye, achọpụtara na empagliflozin nwere oke nhọrọ maka ndị na-ebuga glucose ndị ọzọ na-ahụ maka glucose homeostasis n'ụdị anụ ahụ dị iche iche.

Transportdị onye na-ebubata mmiri sodium nke abụọ bụ protein na-ebu ebu ibu nke na-ahụ maka ịmaliteghachi glucose site na renal glomeruli azụ banye n'ọbara. Empagliflozin na-emezi nchịkwa glycemic na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa mellitus (T2DM) site na ibelata realsorption kelion.

Ọbara glucose na-eto site na akụrụ jiri usoro a dabere na ntinye glucose na ọbara yana ọnụego mkpokọta ụwa (GFR). Mmachi nke ndị na-ebu sodium na-ebute ụdị glucose ụdị 2 n'ime ndị ọrịa nwere ụdị shuga 2 na hyperglycemia na-eduga na mkpocha glucose oke site na akụrụ.

N'ime ọmụmụ ụlọ ọgwụ, achọpụtara na na ndị ọrịa nwere ọrịa shuga 2, akụrụ na-enwewanye glucose ngwa ngwa mgbe ejiri ọgwụ mbụ nke empagliflozin, mmetụta a gara n'ihu ruo awa 24.

Mmụba nke mwepụta glucose site na akụrụ ya dịgidere ruo ngwụsị nke oge izu anọ, na-enwe empagliflozin na dose nke 25 mg otu ugboro kwa ụbọchị, na nkezi, ihe dịka 78 g / ụbọchị. N'ime ndị ọrịa nwere ụdị shuga nke 2, akụrụba mụbara site na akụrụ mere ka mbelata glucose plasma ozugbo.

Empagliflozin na -ebelata mkpokọ glucose na plasma ọbara ma n'okwu ọnụ na mgbe e risịrị nri. Uzo a na - abu ndi na - adighi adi n’ime insulin, nke na - eme ka enwee nsogbu di na ogwugwu. Mmetụta nke empagliflozin adịghị adabere na ọnọdụ arụ ọrụ nke mkpụrụ ndụ beta nke pancreatic na metabolism metabolism.

E gosipụtara mmetụta dị mma nke empagliflozin na ihe nrịbama nke ọrụ sel beta, gụnyere HOMA-? Index. (ihe atụ maka ịlele homeostasis-B) yana ogo proinsulin na insulin. Na mgbakwunye, iwepụ glucose ọzọ site na akụrụ na-eme ka a ghara inwe calorie, nke na-esobelata olu nke anụ ahụ adipose na mbelata nke ahụ. A na-ahụkarị Glucosuria n'oge eji empagliflozin yana ntakịrị mmụba na diuresis, nke nwere ike itinye aka na mbelata ọbara mgbali elu.

N'ime ule nke ụlọ ọgwụ ebe ejiri mee ihe empagliflozin dị ka monotherapy, ọgwụgwọ ngwakọta na metformin, ọgwụgwọ ngwakọta na metformin na usoro sulfonylurea, ọgwụgwọ njikọta na metformin ma e jiri ya tụnyere glimepiride, ọgwụgwọ njikọta na pioglitazone +/- metformin, dịka ọgwụgwọ nkwonkwo ya na dipeptidyl peptide inhibitor 4 (DPP-4), metformin +/- ọgwụ ọgwụ hypoglycemic ọzọ, n'ụdị njikọta ọgwụ na insulin, ọ bụ ihe ndekọ ọnụ ọgụgụ buru ibu mbelata m nke ịba ọcha n'anya HbAlc na mbelata glucose plasma na-ebu ọnụ.

A mụọla ọgwụ ọgwụ nke empagliflozin nke ọma na ndị ọrụ afọ ofufo ahụike na ndị ọrịa nwere ụdị shuga 2.

Mgbe nchịkwa ọnụ gachara, etinyere empagliflozin ngwa ngwa, ọnụnọ kachasị nke empagliflozin na plasma ọbara (Cmax) ruru 1.5 awa. Mgbe ahụ, itinye uche nke empagliflozin na plasma belatara n'ụzọ abụọ.

Mgbe iwere empagliflozin, mpaghara ọkara n'okpuru usoro ịta ahụhụ (AUC) n'oge ọkwa plasma kwụ ọtọ bụ 4740 nmol x hour / L, ọnụ ahịa Cmax bụ 687 nmol / L. Ndị ọgwụ ọgwụ empagliflozin na ndị ọrụ afọ ofufo nwere ahụike na ndị ọrịa nwere ụdị shuga 2 bụkarị otu.

Iri nri adighi enwe ogwu di egwu banyere ogwu ogwu nke empagliflozin.

Olu nke nkesa Plasma steetị dị ka 73.8 lita. Mgbe nchịkwa ọnụ gachara site n'aka ndị ọrụ afọ ofufo nwere ahụike nke akpọrọ empagliflozin 14C, ọgwụ mgbochi plasma bụ 86%.

Mainzọ kachasị nke metabolagliflozin metabolism n’ime mmadụ bụ glucuronidation na ntinye nke uridine-5'-diphospho-glucuronosyltransferases UGT2B7, UGT1A3, UGT1A8 na UGT1A9. Ihe ndị na-achọpụtakarị metabolites nke empagliflozin bụ glucuron conjugates atọ (2-0, 3-0 na 6-0). Mmetụta sistemụ nke metabolite ọ bụla dị ntakịrị (ihe na-erughị 10% nke ngụkọta nke empagliflozin).

Iwepu ọkara ndụ bụ ihe dịka awa 6.4. N'ihe banyere iji empagliflozin otu ugboro kwa ụbọchị, a na-enweta mkpo plasma kwụsịrị mgbe ọgwụ nke ise gasịrị.

Mgbe nchịkwa ọnụ kwupụtara empagliflozin 14C na ndị ọrụ afọ ofufo ahụike, ihe dị ka 96% nke ọgwụ ahụ ka ewepụrụ (site na eriri afọ 41% na akụrụ 54%). Site na eriri afọ, ọtụtụ n'ime ọgwụ akpọrọ agbanweela agbanweghị.

Ọ bụ nanị ọkara nke ọgwụ akpọrọ ahaghị ya na akụrụ na-agbanweghị. Pharmacokinetics na ndị ọrịa ọrịa pụrụ iche

Renrụ ọrụ na-arụ ọrụ na ụlọ

N'ime ndị ọrịa nwere nnukwu nsogbu gbasara akụrụngwa (30 https: //apteka.103.xn--p1ai/jardins-13921690-instruktsiya/

Jardins ™ mbadamba 10 mg 30 pcs

A naghị akwado Jardins® maka ndị ọrịa nwere ọrịa shuga 1 na maka ọgwụgwọ ketoacidosis nke ọrịa mamịrị.

Site na iji ụdị mgbochi 2 na-ebu glucose, gụnyere empagliflozin, a kọwo akụkọ banyere ọrịa ketoacidosis nke ọrịa mamịrị. N'ụfọdụ n'ime okwu ndị a, ngosipụta ndị ahụ jọgburu onwe ha ma gosipụta ya dị ka mmụba dị elu n'ọbara glucose ọbara (ọ bụghị ihe karịrị 14 mmol / L (250 mg / dl).

Ihe ize ndụ nke ịmalite ọrịa ketoacidosis nke ọrịa mamịrị kwesịrị ịtụle ma ọ bụrụ na enweghị mgbaàmà ndị dị ka ọgbụgbọ, ọgbụgbọ, enweghị agụụ, afọ mgbu, akpịrị ịkpọ nkụ, mkpụmkpụ ume, enweghị nchekasị, ike ọgwụgwụ na-enweghị isi ma ọ bụ ụra. Ọ bụrụ na ọrịa ndị dị otú a bidoro, a ga-enyocha ndị ọrịa ozugbo maka ketoacidosis, agbanyeghị nbara ọkwa glucose ọbara. Ekwesịrị ịkwụsị ma ọ bụ kwụsịlata iji ọgwụ Jardins® mee ihe ruo mgbe achọpụtala nchọpụta ahụ.

Egwu dị elu nke ịmalite ọrịa ketoacidosis nke ọrịa mamịrị ga-ekwe omume na ndị ọrịa nwere nri carbohydrate dị ala, ndị ọrịa nwere nnukwu mmiri mmiri, ndị ọrịa nwere akụkọ ketoacidosis, ma ọ bụ ndị nwere obere ọrụ nzuzo nke mkpụrụ ndụ reat-pancreatic. N'ime ndị ọrịa dị otú ahụ, ekwesịrị iji akọ mee Jardins®. Ọ dị mkpa ịkpachara anya mgbe ị na -ebelata ogo insulin.

Nkwadebe nke Jardins in na mbadamba 10 mg nwere 162.5 mg nke lactose, na usoro onunu ogwu nke 25 mg nwere 113 mg nke lactose, ya mere, ekwesighi iji ogwu mee ihe na ndi ọrịa nwere nsogbu hereditary dị ka ụkọ lactase, nnagide lactose, glucose-galactose malabsorption.

Ọmụmụ ihe omimi egosila na ịgwọ ya na nsogbu nke ọgwụ na ọgaghị ebute mmụba n'ihe gbasara obi. Ojiji nke empagliflozin na dose nke 25 mg adịghị eduga n'ịgbatịkwu oge etiti QT.

Site na iji ọgwụ Jardins® jikọtara ya na ihe ndị na-enye sulfonylurea ma ọ bụ ya na insulin, enwere ike ịbelata mbelata nke sulfonylurea / insulin n'ihi ohere nke hypoglycemia.

A mụbeghị Empagliflozin na njikọ glucagon-like peptide-1 analogues (GLP-1).

Ofdị irè nke ọgwụ Jardins® na-adabere na ọrụ akụrụ, ya mere, a na-atụ aro ka ọ nyochaa ọrụ akụrụ tupu oge a kara aka ya na oge site n'oge ọgwụgwọ (ọ dịkarịa ala 1 oge kwa afọ), yana tupu oge ịhọpụta ọgwụgwọ concoitant, nke nwere ike imetụta ọrụ akụrụ. Iji ọgwụ a eme ihe na ndị ọrịa nwere akụrụ akwara (a naghị akwado GFR)