Onglisa: nyocha banyere iji ogwu a, ntuziaka

Onglisa bu ogwu maka ndi oria mamiri, ihe ndi n’eji eme ihe bu saxagliptin. Saxagliptin bụ ọgwụ edepụtara maka ịgwọ ụdị ọrịa shuga 2.

N'ime awa 24 mgbe nchịkwa gasịrị, ọ na-egbochi ọrụ nke enzyme DPP-4. Mgbochi nke enzyme mgbe ị na-emekọrịta glucose na-abawanye site na okpukpu abụọ karịa ọkwa glucagon-peptide-1 (nke dị n'okpuru nke a GLP-1) na glucose na-adabere insulinotropic polypeptide (HIP), na-ebelata mkpokọta glucagon ma na-akpali nzaghachi nke sel beta.

N'ihi ya, ihe insulin na C-peptide dị n’ahụ na-abawanye. Mgbe ewepụtara insulin site na mkpụrụ ndụ beta nke pancreas na glucagon site na mkpụrụ ndụ alfa, glycemia na-ebu ọnụ na postprandial glycemia na-ebelata nke ukwuu.

Ejila nlezianya nyocha ojiji iji saxagliptin na usoro onunu ogwu dị iche iche n'ọmụmụ ihe abụọ nwere nchịkwa mmadụ abụọ, nke gụnyere ndị ọrịa 4148 chọpụtara ụdị ọrịa shuga mellitus 2.

N'oge ọmụmụ ihe ahụ, ọganihu dị ukwuu na gemoclobin glycated, glucose plasma glucose na glucose postprandial kwuru. Ọrịa ndị ọgwụ adaagliptin butereghị nsonaazụ a tụrụ anya ka ejiri ọgwụ ndị ọzọ dịka ọgwụ metformin, glibenclamide na thiazolidinediones.

Ihe akaebe sitere n’aka ndị ọrịa na ndị dọkịta: izu 4 ka mmalite nke ọgwụgwọ gasịrị, ọ bụ naanị saxagliptin, ọkwa nke gemoclobin glycated belatara, ọkwa glucose plasma na-ebu ọnụ ka izu abụọ gachara.

Edeputara otu ihe ngosi a na otu ndi oria ndi edeputara ọgwụgwọ ogwu na mgbakwunye nke metformin, glibenclamide na thiazolidinedion; analogues na aru oru ha.

N'okwu niile, achọpụtaghị mmụba dị arọ nke ndị ọrịa.

Mgbe itinye ongliza

Edere ọgwụ ahụ ka ndị ọrịa nwere ọrịa shuga nke ụdị shuga 2 n'ụdị ndị a:

• Na monotherapy yana ọgwụ a na mmega ahụ na usoro ọgwụgwọ nri,
• Na nkwanye ọgwụ na agwakọta na metformin
• Na enweghị ọgwụgwọ nke monotherapy na metformin, ihe ndị na-eme ka sulfonylurea, thiazolidinediones dị ka ọgwụ ọzọ.

N'agbanyeghi eziokwu na onglise ọgwụ abanyela n'ọtụtụ ọmụmụ na ule, nyocha banyere ya kachasị mma, ọgwụgwọ nwere ike ịmalite naanị n'okpuru nlekọta dọkịta.

Ihe mgbochi iji nke onglise

Ebe ọgwụ ahụ na-emetụta ọrụ beta na mkpụrụ ndụ alfa, na-akpali ọrụ ha nke ukwuu, a gaghị eji ya mgbe niile. A na-egbochi ọgwụ ahụ:

1. N’ime afọ ime, ịmụ nwa na n’ara ara.
2. Ndị na-eto eto na-erubeghị afọ 18.
3. Ndị ọrịa nwere ụdị ọrịa shuga mellitus nke 1 (nke a na-amụghị).
4. Na insulin ọgwụ.
5. Na ketoacidosis na-arịa ọrịa mamịrị.
6. Ndị ọrịa nwere afọ ndụ galactose anabataghị ya.
7. N'uche uche onye ọbụla n’ime ihe ọgwụ a.

N'ọnọdụ ọ bụla ekwesighi ileghara ntuziaka maka ọgwụ a anya. Ọ bụrụ na enwere obi abụọ banyere nchekwa nke iji ya, aga-ahọpụta ndị na - egbochi analog ma ọ bụ usoro ọgwụgwọ ọzọ.

Usoro Ọgwụ na Nchịkwa

A na-eji ọnụ na-ahụ Onglisa, na-enweghị ihe gbasara nri. Ihe dị ka ọgwụ a tụrụ aro ya kwa ụbọchị bụ 5 mg.

Ọ bụrụ na a na-eme ọgwụgwọ ngwakọta, ị ,ụ ọgwụ kwa ụbọchị nke saxagliptin na-agbanwe agbanwe, a na-ekpebi usoro ọgwụgwọ nke metformin na sulfonylurea iche.

Na mbido nchikota ọgwụ na iji ọgwụ metformin, usoro ogwu a ga - adị ka ndị a:

• Onglisa - 5 mg kwa ụbọchị,
• Metformin - 500 mg kwa ụbọchị.

Ọ bụrụ na ekwetaghị mmeghachi omume na-ezighi ezi, usoro ọgwụgwọ nke metformin kwesịrị idozi, ọ na-abawanye.

Ọ bụrụ na, maka ihe ọ bụla, oge ị theụ ọgwụ ahụ na-efu, onye ọrịa ahụ kwesịrị ị shouldụ ọgwụ ahụ ozugbo enwere ike. Ọ baghị uru ịgbanye okpukpo abụọ kwa ụbọchị.

Maka ndị ọrịa nwere ọrịa azụ na-adịghị ala ala dị ka ọrịa nwere njikọ, ọ dịghị mkpa ịgbanwe usoro onglise. Ysji arụ ọrụ ezighi ezi nke onglis kwesịrị iwere obere elekere - 2.5 mg otu ugboro n'ụbọchị.

Ọ bụrụ na a na-eme nyocha ahụ, a na - ewere onglisa mgbe emechara ahụ. Achọpụtabeghị nsonaazụ saxagliptin na ndị ọrịa na-ele anya mgbaze. Ya mere, tupu ịmalite iji ọgwụ a, nyocha zuru oke nke ọrụ akụrụ kwesịrị ịrụ.

Site na imeju imeju, enwere ike ịkọ ọnụọgụ onglise n'enweghị nsogbu na usoro ọgwụgwọ egosipụtara - 5 mg kwa ụbọchị. Maka ọgwụgwọ nke ndị ọrịa meworo agadi, a na-eji onglise eme ihe n'otu usoro onunu ogwu. Mana ekwesiri icheta na ihe ọghọm nke ịmalite ịrịa akụrụ na ụdị ndị ọrịa shuga dị elu.

Enweghị nyocha ma ọ bụ ọmụmụ nyocha nke mmetụta ọgwụ a nwere n'ahụ ndị ọrịa na-erubeghị afọ 18. Ya mere, maka ndị nọ n'afọ iri na ụma nwere ụdị ọrịa shuga 2, a na-ahọrọ analogues nwere akụkụ ọzọ na-arụ ọrụ.

Achọrọ ị theụ ọgwụ onglise ma ọ bụrụ na etinyere ọgwụ ọgwụ n'otu oge yana ndị na - egbochi ya. Nke a bụ:

1. ketoconazole,
2. critithromycin,
3. atazanavir
4. indinavir
5. igraconazole
6. nelfinavir
7. ritonavir
8. saquinavir na telithromycin.

Ya mere, usoro ọgwụgwọ kachasị elu kwa ụbọchị bụ 2.5 mg.

Njirimara nke ọgwụgwọ nke ụmụ nwanyị dị ime na nsonaazụ

Achọpụtabeghị etu ọgwụ a si emetụta afọ ime, ma ọ nwere ike ịbanye na mmiri ara ara, yabụ, edeghị ọgwụ ahụ n’oge ị na-azụ nwa. A na-atụ aro ka iji ọgwụ analogues ndị ọzọ ma ọ bụ kwụsị inye ara.

Ọtụtụ mgbe, na-agbaso usoro onunu ogwu na usoro nke ọgwụgwọ ngwakọta, a na-anabata ọgwụ ahụ nke ọma, n'ọnọdụ ụfọdụ, dịka nyocha na-egosi, enwere ike ịhụ ihe ndị a:

• Vomiting
• Ọrịa mamịrị,
• Isi ọwụwa
• Guzobe ọrịa nke elu akụkụ okuku ume na,
• Ọrịa na-efe efe nke usoro mkpụrụ ndụ.

Ọ bụrụ na enwere otu ọrịa ma ọ bụ karịa, ikwesiri ikwusi ọgwụ ahụ ma ọ bụ dozie usoro ahụ.

Dika nyocha, oburu na ejiri onglise mee ihe ogologo oge onunu ogwu akari ugboro iri itolu a tụrụ aro ya, ekwughi ihe mgbaàmà nke nsị. Iji wepu ọgwụ ahụ n'ahụ ahụ enwere ike ịxụbiga mmanya ókè, a na-eji usoro geomdialysis eme ihe.

Ihe ozo mara

Edebere Onglis na insulin ma obu ogwu nke okpukpu ato na metformin na thiazolididones, ebe obu na emebeghi ihe omumu banyere nmekorita ha. Ọ bụrụ na onye ọrịa na-ata ahụhụ na oke akụrụ gbasara akwara oke, e kwesịrị ibelata usoro ubochi ọ bụla. Ndị ọrịa mamịrị nwere ọrịa akụrụ dị nwayọ na-achọ nyocha oge niile maka ọnọdụ akụrụ n'oge ọgwụgwọ.

E guzobere ya na usoro sulfanilurea nwere ike ịkpalite hypoglycemia. Iji gbochie ihe ize ndụ nke hypoglycemia, usoro ọgwụgwọ nke sulfanilurea yana ọgwụgwọ onglise kwesịrị idozi. Nke ahụ bụ, belata.

Ọ bụrụ na onye ọrịa nwere akụkọ banyere mmụọ na-egbochi ọgwụ ndị ọzọ na - egbochi DPP-4 inhibitors, edeghị saxagliptin. Banyere nchekwa na ịdị irè nke ọgwụgwọ nke ndị ọrịa agadi (karịa afọ 6) na ọgwụ a, enweghị ịdọ aka ná ntị na nke a. A na-anabata Onglisa ma na-eme otu ihe ahụ dịka ọ dị na ndị ọrịa na-eto eto.

Ebe ngwaahịa a nwere lactose, o kwesịghị maka ndị nwere nsogbu ịmụpụta ihe a, ụkọ lactose, glucose-galactose malabsorption.

Emebeghị nyocha nke ọgwụ a nwere ike ịkwọ ụgbọala na akụrụngwa ndị ọzọ chọrọ nnukwu nlebara anya.

Enweghị contraindications kpọmkwem na-anya ụgbọ ala, mana ekwesịrị icheta na n'etiti mmetụta mmetụta akpịrị na isi ọwụwa kwuru.

Mmekọrịta na ọgwụ ndị ọzọ

Dika ihe omumu banyere ogwu, ihe omuma nke imekorita onglises na ogwu ndi ozo, ma oburu n’otu oge, pere mpe.

Ndị sayensị amabeghị etu ị smokingụ sịga, ị alcoholụ mmanya na-aba n'anya, iji ọgwụ homeopathic, ma ọ bụ nri nri na-emetụta mmetụta nke ọgwụ ahụ, n'ihi enweghị nyocha na mpaghara a.

Mwepụta wepụtara ya na ihe mejupụtara

Thedị usoro iji wepụta Onglis bụ mbadamba ihe nkiri: agba, biconvex, a na-etinyere ihe odide na-acha anụnụ anụnụ, 2.5 mg nke ọ bụla - site na ọkụ gaa na odo na-acha odo odo, ihe e dere “2.5” n'otu akụkụ, yana “ 4214 ", 5 mg nke ọ bụla - pink, n'otu akụkụ ihe odide" 5 ", na nke ọzọ -" 4215 "(pcs 10. Na blisters, na kaadiboodu igbe 3 blisters).

Ngwakọta 1 mbadamba:

• ihe na-arụ ọrụ: saxagliptin (n'ụdị saxagliptin hydrochloride) - 2,5 ma ọ bụ 5 mg,
• ihe inyeaka: lactose monohydrate - 99 mg, microcrystalline cellulose - 90 mg, shịm croscarmellose - 10 mg, magnesium stearate - 1 mg, 1M ngwọta nke hydrochloric acid - na ọnụ ọgụgụ zuru ezu,
• shei: Opadry II ọcha (mmanya polyvinyl - 40%, titanium dioxide - 25%, macrogol - 20.2%, talc - 14.8%) - 26 mg, Opadry II odo (maka mbadamba 2.5 mg) mmanya polyvinyl - 40%, titanium dioxide - 24.25%, macrogol - 20,2%, talc - 14.8%, ọla edo na-acha ọcha edo edo (E172) - 0.75% - 7 mg, Opadry II pink (maka mbadamba 5 mg) Polyvinyl mmanya - 40%, titanium dioxide - 24.25%, macrogol - 20,2%, talc - 14.8%, ihe eji esiji akwa oxide uhie (E172) - 0.75% - 7 mg,
• ink: Opacode acha anụnụ anụnụ - (45% shellac na ethyl mmanya - 55.4%, FD&C Blue # 2 / indigo carmine aluminom pigmenti - 16%, n-butyl mmanya - 15%, propylene glycol - 10.5%, isopropyl mmanya - 3% , 28% ammonium hydroxide - 0.1%) - na ọnụ ọgụgụ zuru ezu.

Mlọ ọgwụ

Saxagliptin nwere ike ịhọrọ nke ga - agbanwegharị dipeptidyl peptidase-4 (DPP-4) inhibitor. Na ụdị ọrịa shuga abụọ nke ọrịa mellitus, nchịkwa ya na-eduga na ịkwụsịlata ọrụ nke enzyme DPP-4 ruo awa 24. Mgbe abatamara glucose, inhibido nke DPP-4 na-eduga na mmụba okpukpu abụọ nke polypeptide glucose-glucose (HIP) na gluptagon-dị ka peptide-1 (GLP-1), mmụba nke mkpụrụ ndụ beta glucose na mbelata nke ịta glucagon, nke na-akpata mmụba nke ịta ahụhụ. C-peptide na insulin.

Mbelata ntọhapụ nke glucagon site na mkpụrụ ndụ alịcreatic na mwepụta nke insulin site na mkpụrụ ndụ beta nke pancreatic na-eduga na mbelata mgbatị postprandial glycemia na glycemia.

N'ihi ọmụmụ ihe ndị na-achịkwa ịwa ahụ, a chọpụtara na iwere Onglisa wee nwee ọganihu dị ukwuu na glucose plasma na-ebu ọnụ (HbA)._1c) na plasma glucose postprandial (BCP) ma e jiri ya tụnyere njikwa.

Ndị ọrịa na-enwebeghị ike imezu ọkwa glycemic lekwasịrị anya mgbe ị na-ewere saxagliptin dị ka monotherapy ka agbakwunyere metformin, thiazolidinediones ma ọ bụ glibenclamide. Mgbe ị na-ewere 5 mg nke saxagliptin, mbelata na HbA_1c kwuru ka izu anọ gachara, GPN - ka izu abụọ gachara. N'ime ndị ọrịa natara saxagliptin yana metformin, thiazolidinediones ma ọ bụ glibenclamide, a hụrụ mbelata yiri ya.

Na nloghachi iwere Onglisa, ahuteghugoro ibu ahu. Mmetụta saxagliptin na profaịlụ nke egbugbere ọnụ yiri nke placebo.

Mlọ ọgwụ

N'ime ndị ọrụ afọ ofufo ahụike na ndị ọrịa nwere ụdị shuga 2, a na-ahụ ọgwụ ọgwụ nke saxagliptin na metabolite ya bụ isi.

A na-etinye obi gị dum n’ihe gbasara nchịkwa ọnụ n’obere afọ. Mmuzu C_max (ịba uru nke ihe) nke saxagliptin na isi metabolite na plasma pụtara ihe karịrị awa 2 na awa anọ. Site na mmụba nke ọnụọgụ, mmụba nke C_max na AUC (mpaghara dị n'okpuru usoro ịta ahụhụ) nke ihe ahụ na metabolite ya. Mgbe otu pacenti 5 nke ziriagliptin nke ndị ọrụ afọ ofufo siri ike, nkezi nke C_max saxagliptin na isi metabolite ya na plasma bụ 24 ng / ml na 47 ng / ml, ụkpụrụ AUC bụ 78 ng × h / ml na 214 ng × h / ml, n'otu n'otu.

Na oge nkezi nke T ikpeazụ_1/2 (ọkara ndụ) nke saxagliptin na isi metabolite ya bụ elekere 2.5 na awa 3.1, otu ọ dị, uru ọkara nke ihe mgbochi T_1/2 Plasma DPP-4 - awa 26,9 9. Mkpuchi Plasma DPP-4 ọrụ opekata mpe awa iri abụọ ka ewerechara saxagliptin na njikọta ya dị elu maka DPP-4 na ogologo oge na ya. Achọpụtara cumulation nke ihe ya na metabolite ya n'oge ogologo oge na njikwa oge nke 1 oge kwa ụbọchị anaghị ahụ. Achọpụtaghị ịdabere na mwepụ nke saxagliptin na metabolite bụ isi ya na ọgwụ kwa ụbọchị na oge ọgwụgwọ mgbe ị theụ ọgwụ 1 otu ụbọchị kwa ụbọchị na ọnụọgụ abụọ nke 2.5-400 mg maka ụbọchị 14.

Mgbe nchịkwa ọnụ gasịrị, ọ bụghị ihe na-erughị 75% nke ọgwụ a na-etinye. Iri nri na pharmacokinetics nke saxagliptin emetụtaghi nke oma. Nri oriri riri oke na-emetụta C_max enweghi oke, mana ụkpụrụ nke AUC ma e jiri ya tụnyere ibu ọnụ na-abawanye na 27%. Mgbe ị na-a theụ ọgwụ ahụ na nri, ma e jiri ya tụnyere ibu ọnụ, oge ị ga-eru C na-abawanye ihe dị ka nkeji iri atọ_max. Mgbanwe ndị a enweghị ihe ọria.

Saxagliptin na metabolite ya bụ isi na-ejikọ protein protein n'ime ntakịrị. N'akụkụ a, enwere ike iche na ngbanwe mgbanwe nke protein protein nke ọbara ọbara nke a hụrụ na akụrụ ma ọ bụ ọrịa ịba ọcha n'anya, nkesa saxagliptin agaghị enwe mgbanwe ndị dị mkpa.

A na-agwakọta ihe a ka ukwuu na ntinye cytochrome P450 3A4 / 5 isoenzymes (CYP 3A4 / 5). N'okwu a, etolite metabolite bụ isi na-arụ ọrụ, mmetụta mgbochi nke megide DPP-4 bụ ugboro abụọ adịghị ike karịa nke saxagliptin.

Saxagliptin nwere bile na mmamịrị na-apụ apụ. Ibelata mkpochapu ihe gbasara ihe ruru ihe dị ka 230 ml / min, nkezi mkpochasị ngwongwo dị ihe dị ka 120 ml / min. Mkpochapu ntaramahụhụ maka ihe na-akpata metabolite ka ya na nkezi nke mkpokọta ụwa.

Uru nke AUC nke saxagliptin na metabolite isi ya na ọdịda akwara dị nrịrị bụ 1.2 na 1.7 karịa, karịa, na ndị ọrịa nwere ezigbo ọrụ mkpo ya. Mmụba a na ụkpụrụ AUC adịghị mkpa ọgwụgwọ, yana ekwesighi ịme mgbazi ọgwụ.

Na ọdịda akụrụngwa / oke akwara, yana ndị ọrịa nwere ọrịa metụtara ọrịa, ụkpụrụ AUC nke ihe ahụ na metabolite ya kacha elu bụ 2.1 na oge 4.5 karịa. N'akụkụ a, kwa ụbọchị maka otu a nke ndị ọrịa ekwesịghị gafere 2.5 mg na 1 dose. N'ihe banyere ọrụ ịba ọcha n'anya, a chọpụtapụtaghị mgbanwe mgbanwe dị ukwuu na ọgwụ ọgwụ nke saxagliptin na, n'ihi ya, idozi dose adịghị mkpa.

Amabeghị ọdịiche dị na ọgwụ na ọgwụ pharmacokinetics nke saxagliptin n'ime ndị ọrịa afọ 65 ruo 80 ma e jiri ya mata ndị ọrịa dị obere. N'agbanyeghi eziokwu na achoghi imeghari onodu a maka ndi otu a, odi nkpa iburu ibu di elu na oru mbelata.

Ihe ngosi maka ojiji

Edere Onglisa maka ịgwọ ụdị ọrịa shuga mellitus nke 2 dị ka ụzọ ọzọ mmega ahụ na nri iji meziwanye njikwa glycemic.

Enwere ike ịkọ ọgwụ a dị ka ndị a:

• monotherapy
• na-amalite usoro ọgwụgwọ na metformin,
• mgbakwunye na monotherapy nwere thiazolidinediones, metformin, ọgwụ nke sulfonylurea na enweghị nchịkwa glycemic zuru oke n'oge ọgwụgwọ dị otú ahụ.

Ntuziaka maka iji Onglises: usoro na usoro onunu ogwu

Onglisa were ọnụ were ọnụ n'agbanyeghị nri a na-eri.

Usoro a tụrụ aro bụ 5 mg na 1 dose.

Mgbe ị na-eme ọgwụgwọ ngwakọta, a na-eji Onglisa mee ihe na metformin, sulfonylureas ma ọ bụ thiazolidinediones.

Mgbe ịmalite usoro ọgwụgwọ na metformin, ọgwụ mbụ ya kwa ụbọchị bụ 500 mg. N'ihe banyere nzaghachi ezughị ezu, enwere ike ịba ụba.

Y’oburu na iwee otutu Onglisa, aghaghi iburu ya ozugbo enwere osiso, ekwesighi iri okpukpu abuo n’ime awa iri abuo n’abuo.

Ọgwụ kwa ụbọchị maka ndị ọrịa nwere obere akwara na-ada ada (na mkpochapụ in 50 ml / min), yana ndị ọrịa na hemodialysis, bụ 2.5 mg na 1 dose. Ekwesịrị iwere Ongliz mgbe njedebe nke usoro hemodialysis gasịrị. Edebeghi iji ogwu a na ndi oria onitalial dialita anya. Tupu ịmalite / n'oge ọgwụgwọ, a na-atụ aro ka ị nyochaa ọrụ akụrụ.

Thebọchị a tụrụ aro maka Onglisa mgbe ejikọtara ya na indinavir, nefazodone, ketoconazole, atazanavir, ritonavir, clarithromycin, itraconazole, nelfinavir, saquinavir, telithromycin na ndị ọzọ siri ike CYP 3A4 / 5 inhibitors bụ 2.5 mg.