Ọgwụ Xelevia: ntuziaka maka ojiji > Ọgwụgwọ na mgbochi

Odikwa na mbadamba ihe mkpuchi. Mpempe akwụkwọ na-acha ude, n'elu akpụkpọ ahụ ihe nkiri n'otu akụkụ, a kanyere akara "277", n'akụkụ nke ọzọ ha na-agbanwe kpamkpam.

Isi ihe na - arụ ọrụ bụ sitagliptin phosphate monohydrate na usoro nke 128.5 mg. Ihe ndi ozo: microcrystalline cellulose, calcium hydrogen phosphate, croscarmellose sodium, magnesium stearate, magnesium stearyl fumarate. Ihe mkpuchi ihe nkiri a mejupụtara polyvinyl mmanya, titanium dioxide, polyethylene glycol, talc, odo na odo iron.

Ọgwụ dị na blisters maka mbadamba 14. N'ime ngwugwu kaadiboodu enwere blisters abụọ na ntuziaka maka ojiji.

Ebe na otu esi abanye insulin na ọrịa shuga mellitus - gụọ akụkọ a.

Omume ọgwụ

Ebumnuche maka ọgwụgwọ nke ọrịa shuga n'ụdị nke abụọ. Usoro nke ihe a dabere na mgbochi nke enzyme DPP-4. Ihe nọ n'ọrụ dị iche na ihe insulin na ndị ọzọ na - egbochi antiglycemic. Ta ụbara nke glucose na-egbochi insulinotropic homonụ.

Enwere mwepu nzuzo nke glucagon site n’akwara mkpụrụ ndụ. Nke a na - enyere aka belata njikọ glucose na umeji, n'ihi nke a na - ebelata ihe mgbaàmà hypoglycemia. Ezubere nke sitagliptin bụ igbochi hydrolysis nke enzymes pancreatic. Glucagon zoro ezo belata, si otú ahụ na-akpali ntọhapụ nke insulin. N'okwu a, nchịkọta glycosylated insulin index na itinye uche nke glucose na ọbara.

Xelevia bu n’obi ịgwọ ụdị ọrịa shuga 2.

Mlọ ọgwụ

Mgbe oburu iburu ogwu ahu n’ime, a na - enweta ihe di n’ime ya n’ime ngwa ngwa diges. Nri na-emetụta nnabata. Ọ bụ n’oche ka elebara anya n’ime ọbara ka a na-ekpebi. Bioavailability dị elu, mana ike ijikọ ihe owuwu protein dị ala. Metabolism pụtara na imeju. A na-ewepụ ọgwụ ahụ site na ahụ yana mmamịrị site na mkpochasi akụrụ ma agbanweghi ya na n'ụdị metabolites dị mkpa.

Ihe ngosi maka ojiji

Onwere otutu uzo gosiputara iji ogwu a:

monotherapy iji melite glycemic metabolism na ndị ọrịa nwere ụdị shuga 2,
amalite usoro ọgwụgwọ siri ike na ụdị metformin ụdị ọrịa shuga 2,
Usoro ọgwụgwọ shuga nke 2, mgbe nri na mmega ahụ anaghị arụ ọrụ.
mgbakwunye insulin
iji meziwanye njikwa glycemic yana njikọta sulfonylurea,
ngwakọta ọgwụgwọ nke ọrịa shuga nke ụdị nke abụọ na thiazolidinediones.

Ihe ngbanwe

Ntuziaka a na -ezozi iji ọgwụ ahụ, nke egosiri na ntuziaka maka ojiji a bụ:

hypersensitivity nke mmiri ọgwụ,
ime na lactation
afọ ruo afọ 18
ọrịa mamịrị ketoacidosis,
ụdị shuga 1
arụ ọrụ akụrụ.

A na-eji Xelevia na ọgwụgwọ nke ọrịa shuga 2, mgbe nri na mmega ahụ anaghị arụ ọrụ.

N'inwe nlekọta dị ukwuu, Edere Xelevia ka ndị mmadụ nwere ajọ akụrụngwa akwara na-adalata adalata, na-arịa ndị nwere ọrịa ọria.

Etu esi ewere Xelevia?

Usoro onunu ogwu ya na oge ogwu ya dabere na ogo onodu a.

Mgbe ị na-eduzi monotherapy, a na-ewere ọgwụ ahụ na ọgwụ mbụ kwa ụbọchị nke 100 mg kwa ụbọchị. A na-ahụ otu usoro onunu ogwu ahụ mgbe iji ọgwụ ahụ yana metformin, insulin na sulfonylureas. Mgbe ị na-eme ọgwụgwọ mgbagwoju anya, ọ bụ ihe amamihe dị na ya belata insulin nke a na-ewe iji zere mmepe nke hypoglycemia.

Ejila okpukpu abụọ nke ọgwụ otu ụbọchị. Site na mgbanwe dị omimi na ahụike niile, enwere ike ịchọ ndozi dose. N'ọnọdụ ụfọdụ, etinyere ọkara mbadamba ma ọ bụ nkeji iri na ise, nke na-enwe naanị mmetụta nsị. Dosebọchị kwa ụbọchị nwere ike ịdị iche na-eburu n'uche ngosipụta nke nsogbu nke ọrịa a na arụmọrụ ojiji nke ọgwụ a.

Nsonaazụ Xelevia

Mgbe ị na-ewere Xelevia, mmetụta ndị na-esote ya nwere ike ime:

mmeghachi omume nfụkasị ahụ
agụụ
afọ ntachi
ogwe
tachycardia
ehighi ura
paresthesia
obi erughi ala.

N'ọnọdụ ndị a na-adịghị ahụkebe, oke iwe nke hemorrhoid ga-ekwe omume. Ọgwụgwọ bụ Symptomatic. N'ọnọdụ dị egwu, yana nkwonkwo ụkwụ, a na-eme hemodialysis.

Jiri na agadi

N'ụzọ bụ isi, ndị ọrịa mere agadi anaghị achọ ọgwụgwọ mmezi. Ma ọ bụrụ na ọnọdụ ahụ na-akawanye njọ ma ọ bụ ọgwụgwọ adịghị enye nsonaazụ ndị ị tụrụ anya ya, mgbe ahụ, ọ ka mma ịkwụsị ị theụ ọgwụ ma ọ bụ dozie usoro iji belata.

Ndị ọrịa agadi anaghị achọ mmezi usoro ọgwụgwọ nke Xelevia.

Jiri n'oge ime na lactation

Enweghị data ziri ezi na nsonaazụ nke ihe nọ n'ọrụ nwa ebu n'afọ. Ya mere, amachibido ị ofụ ọgwụ a n'oge mmebi.

Ebe ọ bụ na enweghi data a pụrụ ịdabere na ya na ọgwụ ahụ na-abanye na mmiri ara, ọ ka mma ịhapụ inye ara ma ọ bụrụ na ọgwụgwọ dị mkpa.

Ngwa maka ọrụ ezughi oke ọrụ

Ihe ndenye ọgwụ ahụ ga-adabere na nhazi nke creatinine. Ka ọ dị elu, belata obere ọgwụ etinyere ya. N'ọnọdụ arụmọrụ ezumike ezughi oke, enwere ike idozi dose mbụ na 50 mg kwa ụbọchị. Ọ bụrụ na ọgwụgwọ adịghị enye ọgwụgwọ ọgwụgwọ achọrọ, ịkwesịrị ịkagbu ọgwụ ahụ.

Ngwa maka ọrụ imeju na-arụ ọrụ

Site na ogo dị nwayọ gbasara akụrụ, a chọghị ndozi usoro onunu ogwu. Dosebọchị kwa ụbọchị na nke a kwesịrị ịbụ 100 mg. Naanị na oke ogo imeju, anaghị agwọ ya ọgwụ a.

Site na oke ọrịa imeju, Xelevia edeghị ọgwụ.

Do Overụbiga ihe ókè nke Xelevia

Odi ihe ikpe adighi eme. Ọnọdụ nke ịingụ ọgwụ ọjọọ nwere ike ime naanị mgbe ị na-a aụ otu ọgwụ were karịa 800 mg. N'okwu a, mgbaàmà nke mmetụta ndị ọzọ na-aka njọ.

Ọgwụgwọ na-agụnye lavage gastric, ịpụpụ ọzọ na ọgwụgwọ mmezi. Ọ ga - ekwe omume iwepụ nsí na ahụ site na iji usoro ọgwụgwọ ogologo oge, n'ihi ọkọlọtọ ịba ọcha n'anya dị irè naanị n'ọnọdụ dị nro nke ịdoụbiga mmanya ókè.

Mmekọrịta na ọgwụ ndị ọzọ

Enwere ike ijikọ ọgwụ a na metformin, warfarin, ụfọdụ mgbochi ọgwụ. Aclọ ọgwụ ọgwụ nke ihe na-arụ ọrụ adịghị agbanwe agbanwe yana ọgwụ ejikọtara ya na ndị na - egbochi ACE, ndị na - egbochi antiplatelet, ọgwụ ndị na - egbu mmụọ, ndị na - egbochi beta na ndị na - egbochi calcium.

Nke a gụnyere ọgwụ ndị na - abụghị steroidal anti-inflammatory ọgwụ, antidepressants, antihistamines, proton pump inhibitors na ụfọdụ ọgwụ iji wepụ dysfunction erectile.

Mgbe ejikọtara ya na Digoxin na Cyclosporine, a na-achọpụta ntakịrị ntakịrị na itinye uche nke ihe na-arụ ọrụ n'ime plasma ọbara.

Mmanya ndakọrịta

Nweghị ike ị takeụ ọgwụ a. Mmetụta ọgwụ ahụ na-ebelata, ihe mgbaàmà dyspeptik ga-abawanye.

Ogwu a nwere otutu analogues nke yiri ya n’ihe banyere ihe ike na aru oru ya. Kacha nkịtị n’ime ha bụ:

Sitagliptin,
Sitagliptin phosphate monohydrate,
Januvius
Yasitara.

Emeputa

Companylọ ọrụ na-emepụta ihe: Berlin-Chemie, Germany.

Zere Xelevia n'ebe umuaka no.

Mikhail, 42 afọ, Bryansk

Dọkịta dụrụ ị were Xelevia ka ọ bụrụ ọgwụgwọ bụ isi. Mgbe ọnwa nke iji, shuga na-ebu ọnụ, mụbara ntakịrị, tupu ọ dị n’agbata ise, ugbu a ọ ruru 6-6.5. Mmeghachi omume nke anụ ahụ na mmega ahụ agbanwewokwa. Tupu mgbe ahụ, mgbe ọ gbasịrị ma ọ bụ egwuregwu, shuga dara nke ukwuu, ma na-egbusi ike, onye na-egosi ihe dịka 3. Mgbe ị na-ewere Xelevia, shuga mgbe mmega ahụ jiri nwayọ daa, nwayọ, wee laghachi na nkịtị. Obi malitere ịdị ya mma. Ya mere ana m akwado ọgwụ ahụ.

Alina, 38 afọ, Smolensk

Ana m anabata Xelevia dị ka mgbakwunye insulin. Anọ m ọrịa shuga kemgbe ọtụtụ afọ ma nwalee ọtụtụ ọgwụ na njikọ. Ọ na-amasị m nke a karịa. Ọgwụ na-aza naanị shuga dị elu. Ọ bụrụ na wedata ya ugbu a, ọgwụ ahụ agaghị emetụ ya ma bulie ya elu. Ọrụ nwayọ. Ọ nweghị spikes na shuga n'ụbọchị. Enwere isi okwu ọzọ dị mma, nke a na-akọwaghị na ntuziaka maka ojiji: nri na-agbanwe agbanwe. Agụụ na-ebelata ọkara. Nke a dị mma.

Mark, 54 afọ, Irkutsk

Ọgwụ bịara ozugbo. Mbemiso ini oro, enye ama emen Januvia. Mgbe ọ nwụsịrị, ọ dịghị mma. Mgbe ọnwa ole na ole nke iwere Xelevia, ọ bụghị naanị ọkwa shuga laghachiri na nkịtị, kamakwa ahụike niile. Ahụ dị m ike karịa, enweghị m mkpa ịdị na-eri nri mgbe niile. Ọ fọrọ nke nta ka m chefuo ihe hypoglycemia bụ. Sugar adịghị ama elu, ọ na-amị ala ma na-ada nwayọ nwayọ nwayọ, nke ahụ ya na-eme nke ọma.

Mwepụta wepụtara ya na ihe mejupụtara

Mpempe usoro nke Xelevia bụ mbadamba ihe nkiri: agba aja aja, biconvex, gburugburu, dị larịị n'otu akụkụ, na-akanye "277" (na igbe kaadi 2 blisters nwere mbadamba 14 ọ bụla) na ntuziaka maka ojiji Xelevia.

Ngwakọta 1 mbadamba:

ihe na-arụ ọrụ: sitagliptin phosphate monohydrate - 128.5 mg (kwekọrọ na ọdịnaya nke sitagliptin - 100 mg),
ihe inyeaka: sodium stearyl fumarate - 12 mg, magnesium stearate - 4 mg, croscarmellose sodium - 8 mg, mkpụrụ ndụ hydrogen phosphate na - akọwaghị - 123.8 mg, microcrystalline cellulose - 123.8 mg,
mkpuchi ihe nkiri: Opadry II beige 85F17438 iron oxide red (E 172) - 0.37%, iron oxide yellow (E 172) - 3.07%, talc - 14.8%, polyethylene glycol (macrogol 3350) - 20.2% titanium dioxide (E 171) - 21.56%, polyvinyl mmanya - 40% - 16 mg.

Mlọ ọgwụ

Xelevia bụ onye na - egbochi oke enzyme DPP-4, nke na - arụ ọrụ mgbe a na -eme ya n'ọnụ ma bu n'obi maka ọgwụgwọ ụdị shuga mellitus nke 2.

Ihe na - arụ ọrụ nke Xelevia (sitagliptin) sitere na analogues nke glucagon-dị ka peptide-1 (GLP-1) na amylin, α-glucosidase inhibitors, γ-receptor agonists nke na - arụ ọrụ nke onye na - eme mkpọ peroxisome (PPAR-γ), insulin, sistemu kemịkalị dị iche iche na ọgwụ ọgwụ. Site na igbochi DPP-4, sitagliptin na-eme ka ịbawanye ụba nke homonụ abụọ nke ezinụlọ incretin - GLP-1 na glucose-polyulinptide insulinotropic (HIP).

Hormones nke ezinụlọ a na-ezo n'ime eriri afọ ruo awa iri abụọ na anọ, na nzaghachi nri nri, itinye uche ha na-abawanye. Mgbakwụnye ahụ bụ akụkụ nke sistem nke anụ ahụ maka idozi glucose homeostasis. Na-emegide usoro glucose ọbara dị elu ma ọ bụ dị elu, homonụ nke ezinụlọ dị n'ihu na-enye aka na insulin njikọ na ihe nzuzo ya site na mkpụrụ ndụ reat-pancreatic through site na ị na-egosi usoro intracellular nke metụtara cyclic adenosine monophosphate (AMP).

Ọzọkwa, GLP-1 na-egbochi sel na-egbochi glucagon site na mkpụrụ ndụ reat-pancreatic. Mbelata ịbawanye glucagon na mmụba nke insulin na-eduga n'ịbelata mmepụta glucose site na imeju, nke na-emesị mee ka mbelata glycemia. Ofzọ a na-arụ ọrụ dị iche na nke dị iche iche sitere na usoro sulfonylurea, nke ọbụna nwere obere glucose ọbara nwere ume na-akpali ntọhapụ nke insulin. Nke a na - eme ka ọdịdị nke hypoglycemia nke sulfone akpata, ọ bụghị naanị na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa mellitus, kamakwa ndị mmadụ nwere ahụ ike.

N'itinye ala glucose dị ala n'ọbara, ahụghị ihe edepụtara edepụtara nke mbelata ịbelata glucagon na mwepụta insulin. HIP na GLP-1 anaghị emetụta ntọhapụ glucagon na nzaghachi hypoglycemia. Enzyme DPP-4 na-egbochi ọrụ nke incretins n'okpuru ọnọdụ physiological, nke na-eme ka ha dị ike ngwa ngwa na ịmalite nke ngwaahịa adịghị arụ ọrụ. Sitagliptin gbochiri usoro a, n'ihi nke plasma na-etinye uche n'ụdị ọrụ HIP na GLP-1 na-abawanye.

Site na ịba ụba ọdịnaya, Xelevia na-abawanye ntọhapụ glucose na insulin ma na-enyere aka belata nzuzo nke glucagon. N'ime ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa hyperglycemia, mgbanwe ndị dị otú a na nzuzo nke glucagon na insulin na-arụ ọrụ iji belata mkpokọta nke hemoglobin HbA nke glycated. _1C na mbelata nke glucose na plasma ọbara, kpebisiri ike n’afọ na-adịghị n’ime ya na mgbe nnwale gasịrị.

Anara otu Xelevia n'ime ụdị shuga mellitus nke 2 na-eduga n'ịrụ ọrụ nke enzyme DPP-4 maka awa 24, nke na-arụ ọrụ iji belata glucose na-ebu ọnụ, yana mgbe glucose ma ọ bụ itinye nri, belata mkpokọta glucagon na plasma ọbara, mụbaa ịba uru nke insulin na C. peptide, na-abawanye ịta ahụhụ nke ikesa incretins GLP-1 na ISU na 2 ma ọ bụ ugboro atọ.

Odida ntaramahụhụ

Emere nnyocha mepere emepe nke sitagliptin kwa ụbọchị nke 50 mg iji mụọ ọgwụ ọgwụ maka ogo dị iche iche nke ọdịda akwara afọ n’ala. Ekesinyere ndị ọrụ afọ ofufo a gụnyere n'ọmụmụ ihe ahụ:

ndị ọrịa nwere nsogbu gbasara akụrụ dị nro: mwepu creatinine (CC) 50-80 ml n'ime 1 min,
ndị ọrịa nwere nnukwu nsogbu gbasara akụrụngwa: CC 30-50 ml kwa 1 min,
ndị ọrịa nwere nnukwu nsogbu gbasara akụrụngwa: isi CC 9) anaghị anọ. Agbanyeghị, enyere na akụrụ ya bụ nke akụrụ ga - apụta, mmadụ ekwesịghị ịtụ anya mgbanwe dị ukwuu na ọgwụ ọgwụ ya n'ọnọdụ ndị a.

Agadi

Afọ ndụ ndị ọrịa enweghị mmetụta dị ukwuu n'ụlọ ọgwụ na usoro ọgwụ ọgwụ ọgwụ. E jiri ya tụnyere ndị ọrịa na-eto eto, ntinye nke sitagliptin n'ime ndị agadi (afọ 65 ruo 80) dị elu site na ihe dịka 19%. Dabere na afọ, a naghị eme mgbanwe usoro ọgwụgwọ nke Xelevia.

Xelevia, ntuziaka maka ojiji: usoro na usoro onunu ogwu

Mbadamba ụrọ na-ewere ọnụ, n'agbanyeghị nri. Usoro ọgwụ a tụrụ aro ya bụ 1 mbadamba (100 mg) otu ugboro n'ụbọchị. A na-eji Xelevia mee ihe na monotherapy, ma ọ bụ n'otu oge na usoro metformin / sulfonylurea / PPAR-agonists, ma ọ bụ na metformin na sulfonylureaeri / metformin na PPAR-γ agonists / insulin (na-enweghị ma ọ bụ ya na metformin).

Usoro ogwu nke ogwu eji eme ihe na oge Xelevia bu ndi ahutara n’uche udiri ogwu ndia.

N ’usoro gbasara ọgwụgwọ ejikọtara ya na Xelevia nwere insulin ma ọ bụ sọlfọlilurea, ọ ga-adị mma ka ịbelata usoro ọgwụgwọ insulin na-enyekarị site na iji mee ka ọ belata ma ọ bụ hypoglycemia.

Mgbe ịwụsị ọgwụ, a na-atụ aro ka ọ themụọ ha ngwa ngwa o kwere mee mgbe onye ọrịa chetara usoro ahụ echefuru. Okwesiri iburu n’uche na iji okpukpu abuo nke ogwu n’otu ubochi ekwenyeghi.

Ndozigharị usoro dosing maka ọdịda obere akwara (CC ≥ 50 ml kwa 1 min, ihe kwekọrọ na ndọtị creatinine ≤ 1.5 mg kwa 1 dL n'ime ụmụ nwanyị na ≤ 1.7 mg kwa 1 dL n'ime ụmụ nwoke).

N'ime ndị ọrịa nwere nnukwu akụrụ oke, oke sitagliptin chọrọ ka a gbanwee ya.Ebe ọ bụ na enweghị nsogbu nkewa na mbadamba ụrọ nke Xelevia na ewepụtaghị ha na usoro nke 25 ma ọ bụ 50 mg (mana naanị na usoro nke 100 mg), ọ gaghị ekwe omume ịchọpụta usoro ọgwụgwọ dị mkpa ndị ọrịa dị. N'akụkụ a, ọgwụ a na ụdị ndị ọrịa edeghị ọgwụ.

Ojiji nke sitagliptin megide ndabere nke ọdịda akụrụngwa chọrọ nyocha gbasara ọrụ gbasara akụrụ tupu ịmalite ọgwụgwọ na oge ụfọdụ n'oge eji ya.

Na ogo dị nwayọ ruo na ogo nke ọrịa imeju, yana na ndị ọrịa katarala ahụ, a naghị edozi usoro ọgwụ ahụ. Emebeghị nchọpụta maka ojiji nke Xelevia megide ọrịa nke ọrịa imeju dị njọ.

Usoro ọgwụgwọ mbu na metformin

Emere ihe omumu ihe omumu nke izu iri-abuo nke 24 nke sitagliptin na nha nke kwa ubochi 100 mg na metformin kwa ubochi nke 1000 ma obu 2000 mg (50 mg sitagliptin + 500 ma obu 1000 mg nke metformin ugboro abuo na ubochi). Dika data enwetara, a hụrụ ihe ojoo na ị withụ ọgwụ ahụ ọtụtụ oge (yana otutu with 1%) n'ime otu na-anata sitagliptin + metformin karịa na metformin monotherapy. Ọrịa nke sitagliptin + metformin na metformin na monotherapy bụ (n'otu n'otu):

afọ ọsịsa - 3.5 na 3.3%,
vomiting - 1.1 na 0.3%,
isi ọwụwa - 1.3 na 1.1%,
dyspepsia - 1.3 na 1.1%,
hypoglycemia - 1.1 na 0,5%,
flatulence - 1.3 na 0,5%.

Ojiri nkpokorita nke sulfonylurea ma obu ihe ndi sulfonylurea na metformin

N'ime izu iri abụọ na anọ, a na-ahụta ịmụgharị ihe na-achịkwa ojiji nke nchịkọta 100 mg sitagliptin kwa ụbọchị na glimepiride ma ọ bụ glimepiride na metformin, a hụrụ ugboro ugboro (yana with 1%) mmepe nke hypoglycemia ma e jiri ya tụnyere otu na-enweta placebo na glimepiride ma ọ bụ glimepiride na metformin. Oge nke mmepe ya bụ 9.5 / 0.9%, n'otu n'otu.

Nchikota nkwuputa izizi ya na ndi agonists PPAR-γ

Mgbe ị na-eme ọmụmụ ihe izu iri abụọ na anọ nke usoro ọgwụgwọ izizi na sitagliptin na ọgwụ kwa ụbọchị nke 100 mg na pioglitazone na ọgwụ kwa ụbọchị nke 30 mg na otu na-anata sitagliptin na njikọta, a hụrụ nsonaazụ ugboro ugboro (yana ọtụtụ ≥ 1%) karịa na otu na-anata pioglitazone na monotherapy . Ihe kpatara ihe ojoo na otu sitagliptin + pioglitazone na pioglitazone na monotherapy (n'otu n'otu):

hypoglycemia Symptomatic: 0.4 na 0.8%,
mbelata asymptomatic n'ọbara glucose ọbara: 1.1 na 0%.

Ngwakọta ọgwụ na metformin na PPAR-y agonists

A na-eme ọmụmụ ihe na-achịkwa placebo site na iji 100 mg nke sitagliptin kwa ụbọchị n'otu oge na rosiglitazone na metformin na ntinye nke ìgwè abụọ - ndị ọrịa na-anata nchikota na ọgwụ ọmụmụ, na ndị mmadụ na-enweta nchikota na placebo. Dika data enwetara, a na-ahụta mmeghachi omume ọjọọ oge karịa (yana ugboro ole ≥ 1%) n'ime otu na-anata sitagliptin karịa na otu na-anata placebo.

N'izu nke iri na asatọ nke otu ndị a, a chọpụtara ugboro ole a na-esote ya:

vomiting - 1.2 na 0%,
isi ọwụwa - 2.4 na 0%,
hypoglycemia - 1.2 na 0%,
ọgbụgbọ - 1.2 na 1.1%,
afọ ọsịsa - 1.8 na 1.1%.

N’izu nke iri-ise-ise nke nlebara anya n’ime ndị a, a chọpụtara ọtụtụ ihe mmetụta dị iche iche n’otu ugboro a:

mpaghara ọgụ - 1.2 na 0%,
isi ọwụwa - 2.4 na 0%,
ọgbụgbọ - 1.2 na 1.1%,
fungal ọrịa nke anụahụ - 1.2 na 0%,
ụkwara - 1.2 na 0%,
hypoglycemia - 2.4 na 0%,
ọrịa akụkụ akụkụ okuku ume na elu - 1.8 na 0%,
vomiting - 1.2 na 0%.

Ngwakọta ọgwụ na insulin

N'ime ọmụmụ 24 na-achịkwa placebo na - achịkwa ojiji nke 100 mg nke sitagliptin kwa ụbọchị na ọgwụ insulin (na-enweghị ma ọ bụ na metformin), a na-ahụkarị mmetụta ndị ọzọ ugboro ugboro (yana ọtụtụ ≥ 1%) na otu na-anata sitagliptin na njikọ insulin (na-enweghị ma ọ bụ na metformin) ) karịa insịnụ nọ n'ime insulin (na-enweghị ma ọ bụ ya na metformin). Ihe nke ihe ojoo (dika nlebara anya):

isi ọwụwa - 1.2 / 0%,
flu - 1.2 / 0.3%,
hypoglycemia - 9.6 / 5.3%.

Ọmụmụ ihe iri abụọ na anọ ọzọ, nke eji sitagliptin rụọ ọrụ ka ọ bụrụ ngwa mgbakwunye insulin na-agwọ ọrịa (na-enweghị ma ọ bụ na metformin), ekpughere mmeghachi omume ọ bụla metụtara ị theụ ọgwụ ahụ.

Ọrịa mgbu

Nnyocha zuru oke nke nyocha mmadụ abụọ kpuru ìsì, nyochara ule nyocha nke sitagliptin na mkpụrụ ọgwụ kwa ụbọchị nke 100 mg ma ọ bụ ọgwụ njikwa ya (arụ ọrụ ma ọ bụ placebo) gosipụtara na ọrịa pancreatitis na-enwetaghị nkwarụ bụ 0.1 ikpe na 100 ọrịa afọ ọ bụla.

Edebeghị ihe nrịba ama nke ọgwụ na akara ama dị mkpa ma ọ bụ elektrik, gụnyere oge nke oge QTc na sitagliptin.

Ọmụmụ nyocha Sitụliptin Sitena Nchekwa Ahụhụ (TECOS)

TECOS gụnyere ndị ọrịa 7332 natara 100 mg nke sitagliptin kwa ụbọchị (ma ọ bụ 50 mg kwa ụbọchị ma ọ bụrụ na ihe ndabere ahụ na-ekwu na ọnụego nhicha nke glomerular bụ ≥ 30 na 2), na ndị ọrịa 7339 na-anata placebo na ọnụ ọgụgụ ndị ọrịa niile edepụtara. ọgwụ

A gbakwunyekwara ọgwụ ahụ ma ọ bụ placebo na usoro ọgwụgwọ dabere na ụkpụrụ mba dị adị maka ịhọrọ ọkwa nke HbA_1C na ịchịkwa ihe ndị dị ize ndụ obi. Ngụkọta nke ndị ọrịa afọ 2004 site na afọ 75 ka etinyere na nlere ahụ, nke 970 natara sitagliptin, na 1034 natara placebo. Ọnọdụ ndị dị oke egwu na otu abụọ ahụ bụ otu. Ntụle nke nsogbu ndị metụtara ọrịa shuga mellitus, nke egosiri na mbụ maka nleba anya, kpughere ọnọdụ nke mmetụta ọjọọ n'etiti otu dị iche iche mgbe ị na-ewere sitagliptin / placebo, gụnyere ọrụ ezumike arụ ọrụ (1.4 / 1.5%) na ọrịa (18, 18) 4 / 17,7%). Nsonaazụ mmetụta dị n'akụkụ ndị ọrịa afọ 75 gbagoro bụ otu ndị ahụ n'ozuzu ha.

Ọnụ ọgụgụ nke ọrịa hypoglycemia siri ike na ọnụọgụ ndị ọrịa nke enyere ọgwụ “atụmatụ-ịgwọ” ma nwetakwa ọgwụ sulfonylurea na / ma ọ bụ ọgwụ insulin mgbe ị na-anọdụ sitagliptin / placebo bụ 2.7 / 2.5%, n'otu n'otu. Ọzọkwa, n'ime ndị ọrịa na-ewereghị ọgwụ sulfonylurea na / ma ọ bụ ọgwụ insulin, ugboro ole a bụ 1 / 0.7%, n'otu n'otu. N'oge nyocha ahụ, nnabata nke ọrịa pancreatitis ekwenyela mgbe ị na-a theụ ọgwụ / placebo bụ 0.3 / 0.2%, yana neoplasms ọjọọ - 3.7 / 4%, n'otu n'otu.

Ndenye aha na ndebanye aha

Nyochaa debanye aha na ojiji nke sitagliptin na monotherapy yana / ma ọ bụ yana yana ọgwụ hypoglycemic ndị ọzọ kpughere nsonaazụ ndị ọzọ. Ebe ọ bụ na enwetara data ndị a afọ ofufo site na ọnụọgụgụ akatabeghị, ọnụọgụ oge na mmekọrịta na -elekọta ọgwụgwọ ndị a enweghị ike.

Ndị a gụnyere:

angioedema,
mmeghachi omume hypersensitivity, gụnyere anaphylaxis,
pruritus / ihe ọkụ ọkụ, urticaria, pemphigoid, vasculitis anụ ahụ, ọrịa anụ ahụ exfoliative, gụnyere ọrịa Stevens-Johnson,
nnukwu pancreatitis, tinyere oria ọbara na ọdịdị necrotic na / enweghị nsonaazụ na-egbu egbu,
ọrụ akụrụngwa ezughi ezu, tinyere nnukwu akwara gbasara akwara (n'ọnọdụ ụfọdụ, achọrọ usoro oku),
ọrịa akụkụ akụkụ okuku ume na nke elu
nasopharyngitis,
ọgbụgbọ, afọ ntachi,
isi ọwụwa
arthralgia, myalgia,
mgbu na aka, azụ.

Mgbanwe ụlọ nyocha

N'ọtụtụ ọmụmụ ụlọ ọgwụ, enwere ntakịrị mmụba na ọnụ ọgụgụ leukocyte na ndị ọrịa na-anata sitagliptin (100 mg kwa ụbọchị) ma e jiri ya tụnyere ndị otu placebo (200 μl na nkezi, ihe ngosi ahụ bụ 6600 μl na mmalite ọgwụgwọ), nke a bụ n'ihi mmụba na ọnụ ọgụgụ nke neutrophils.

Achọpụtara ntakịrị mmụba na uric acid (site 0.2 mg kwa 1 dl) na 100 na 200 mg nke sitagliptin kwa ụbọchị ma e jiri ya tụnyere placebo. Tupu mmalite ọgwụgwọ, nkezi nkezi bụ 5-5.5 mg kwa 1 dL. Enweghị ikpe nke gout ka akọwara.

Enwekwara ntakịrị mbelata na alkaline phosphatase na otu ahụ na-anata ọgwụ, ma e jiri ya tụnyere ndị otu placebo (ihe fọrọ nke nta ka ọ bụrụ 5 IU kwa 1 lita, na nkezi, tupu mmalite ọgwụgwọ, ịta ahụ dị site na 56 ruo 62 IU kwa 1 liter), nke jikọtara ya na obere obere. ọrụ mgbada nke enzyme.

A na-atụle mgbanwe maka plọg nke ụlọ nyocha anaghị enwe ọgwụgwọ.

Hypoglycemia

Dika ihe nlere banyere ulo ogwu si kwuo, onodu a nke hypoglycemia n'oge monotherapy nwere sitagliptin ma obu otu oge ya na ogwu adighi eme ka onodu ojoo a (pioglitazone, metformin) yiri nke ahu na otu placebo. Dị ka ọ dị na ọgwụ hypoglycemic ndị ọzọ, hypoglycemia mere n'oge nchịkwa nke Xelevia na njikọta ma ọ bụ insulin insulin. Iji belata ohere a nwere ike ị nweta hypoglycemia nke sulfon, a na-ebelata usoro nke usoro sulfonylurea.

Usoro ọgwụgwọ n’ebe ndị ọrịa agadi nọ

Nchebe na arụmọrụ nke Xelevia na nnwale ụlọ ọgwụ na ndị ọrịa agadi (ndị ọrịa 409) karịa afọ 65 ka ndị ahụ nọ n'otu ndị ọrụ afọ ofufo na-erubeghị afọ 65. N'akụkụ a, ịgbanwe usoro usoro usoro ọgwụgwọ dabere na afọ onye ọrịa adịghị achọrọ. Ekwesịrị iburu n'uche na ndị ọrịa mere agadi nwere ike ịkarị ahụike gbasara akụrụ nke akwara. Yabụ, na ọnụnọ nke nnukwu akụrụngwa nke afọ a, dị ka ọ bụla ọzọ, usoro ọgwụ sitagliptin na-ahazi.

N'ime ọmụmụ TECOS, ndị ọrụ afọ ofufo natara sitagliptin na ọgwụ kwa ụbọchị nke 100 mg (ma ọ bụ 50 mg kwa ụbọchị na ọnụahịa mbụ nke ọnụego mgbaze ụwa ≥ 30 na 2) ma ọ bụ placebo. Agụnyere ha na usoro ọgwụgwọ dabere na ụkpụrụ mba dị adị maka ikpebi ọkwa HbA ezubere iche._1C na ịchịkwa ihe ndị dị ize ndụ obi. Na ngwụsị oge ọmụmụ ihe (afọ 3), n'ime ndị ọrịa nwere ụdị ọrịa shuga mellitus nke 2, ị takingụ ọgwụ na mgbakwunye usoro ọgwụgwọ emeghị ka ọ gaa ụlọ ọgwụ n'ihi ọrịa obi (oke ihe ize ndụ - 1, 95% ntụkwasị obi oge - site na 0.83 ruo 1.2, p = 0.98 maka ọdịiche na ugboro ole nke ihe ọghọm) ma ọ bụ ihe egwu dị oke nsonaazụ site na sistemụ akụrụngwa (oke ihe egwu - 0.98, 95% etiti ntụkwasị obi - site na 0.89 ruo 1.08, p CYP 2C8, CYP 2C9 na CYP 3 A 4. Dabere na data vitro , ọ naghị egbochi CYP 1A2, CYP 2B6, CYP 2C19 na CYP 2 D 6 isoenzymes ma ghara itinye CYP 3 A 4 isoenzyme.

Site na iji metformin na sitagliptin jikọtara ọnụ, enwebeghị mgbanwe dị ukwuu na ọgwụ ọgwụ nke nke abụọ na ndị ọrịa nwere ụdị ọrịa mellitus 2 dị.

Ihe omuma nke enwetara site na nyocha nke onu ogugu nke ndi oria nwere oria nke abuo gosiputara na ọgwụgwọ ajuju adighi enwe ezi ogwu na ogwu nke ogwu. Ihe omumu a nyochara ogwu a na-edekarị maka ọrịa shuga 2, gụnyere ndị a:

Ndị na-egbochi ya
ọgwụ egbugbere ọnụ (dịka ezetimibe, fibrates, statins),
antidepressants (dika sertraline, fluoxetine, bupropion),
ndị na - egbochi antiplatelet (dịka ọmụmaatụ clopidogrel),
antihistamines (dịka ọmụmaatụ cetirizine),
ọgwụ maka ọgwụgwọ dysfunction erectile (dịka ọmụmaatụ sildenafil),
ọgwụ mgbochi-anaghị egbochi steroidal (dịka celecoxib, diclofenac, naproxen),
ndị na-egbochi proton mgbapụta (dịka lansoprazole, omeprazole),
ọgwụ antihypertensive (dịka hydrochlorothiazide, ndị na-egbochi calcium ọsụsọ, angiotensin II receagonor antagonists, angiotensin na-agbanwe enzyme inhibitors).

Obere mmụba na AUC na C _m_ah A kọwara digoxin (site na 11 na 18%, n'otu n'otu) yana ojiji ya na sitagliptin. A naghị atụle mmụba a dị ka ọgwụ. Site na ọgwụgwọ nkwonkwo, a naghị atụ aro mgbanwe mgbanwe dose.

Ubara na AUC na C _m_ah Sitagliptin (29 na 68%, nke abụọ) ka a hụrụ mgbe ejiri ya na 100 mg na mgbakwunye otu cyclosporine (ike inhibitor nke P-glycoprotein) maka nchịkwa ọnụ na dose nke 600 mg. Mgbanwe ndị a chọpụtara na njirimara ọgwụ nke ọgwụ anaghị atụle ọgwụ dị mkpa. Mgbe ị na-ejikọ ya na cyclosporine ma ọ bụ onye ọzọ na P-glycoprotein inhibitor (dịka ọmụmaatụ, ketoconazole), a gaghị atụ aro ka ịgbanwere Xelevia.

Dika onu ogugu ogwu nke onu ogugu nke ndi oria na ndi n’enye onwe ha nke oma (N = 858) maka otutu ogwu (N = 83, ihe dika okara nke putara site na akiri), ihe ndia enweghi otutu ogwu putara ihe banyere pharmacokinetics nke sitagliptin.

Analogs nke Xelevia bụ Yasitara, Sitagliptin phosphate monohydrate, Januvia.

Ihe ngosi na contraindications

Ihe ngosi maka iji "Xelevia" bu:

ịdị omimi nke ọrịa mamịrị na hypoglycemia n'okpuru nduzi nke neuropathy ma ọ bụ nsogbu ahụike ndị ọzọ,
ihe ga-eme ka obi ịrịa ọrịa hypoglycemia n'abalị,
nká
mkpa ịbawanye itinye uche n'ihe mgbe ị na-anya ụgbọ ma ọ bụ na-arụ ọrụ site na usoro eji arụ ọrụ;
ọgụ ugboro ugboro nke hypoglycemia mgbe ị na-ewere sulfonylurea.

Tupu iwere ya, ọ dị ezigbo mkpa ịmata onwe gị na contraindications. Ndị a gụnyere:

na-amụ nwa, na-enye ya ara,
ụdị shuga 1
ọrịa mamịrị ketoacidosis, onye na-erubeghị afọ 18,
gbasara akụrụngwa nke ọdịdị adịghị ala ma ọ bụ nke dị oke njọ.

N'ihi enweghị ọmụmụ na-achịkwa banyere ịdị irè na nchekwa nke ọgwụ maka ụmụ nwanyị dị ime, a naghị akwado Xelevia maka ojiji n'oge ime. Ọzọkwa, enwere ike ịmụ ya na mmiri ara ehi amabeghị, yabụ, a na-enye nwa ara, ọ bụ contraindicated.

Usoro onunu ogwu na ịdoụbiga mmanya ókè

Usoro ọgwụ a tụrụ aro ya bụ 100 mg 1 oge kwa ụbọchị. A na-ewere ya ọnụ dị ka ọgwụ bụ isi ma ọ bụ jiri mgbakwunye na metformin ma ọ bụ ọgwụ nwere ihe ndị ọzọ na-arụ ọrụ. Theakingụ ọgwụ ahụ enweghị nri. Usoro onunu ogwu nke "Xelevia" na ogwu ndi ozo, a na-ehiwe ike ha site na dibia bekee na –echebara ntuziaka nke ntuziaka aka.

Ọ bụrụ n ’ọgwụ na-atụfu gị, a na-atụ aro ka ị were ya ngwa ngwa o kwere mee mgbe onye ahụ mechara nke a. N’otu ụbọchị, amachibidoro ị doubleụ ọgwụ abụọ.

N'ime ule nke ụlọ ọgwụ na ndị ọrụ afọ ofufo nwere ahụ ike, ọgwụ were ogologo ọgwụ 800 nke ndị ọrịa shuga nabatara nke ọma. Obere mgbanwe na ngosipụta abụghị ihe dị mkpa. Achọghị usoro ọgwụgwọ dị elu karịa 800 mg. Achọpụtaghị mmeghachi omume na-adịghị mma mgbe ị na-ewere 400 mg nke "Xelevia" maka izu 4.

Mana, ọ bụrụ na inyefere oke maka ihe ọ bụla mere, onye ọrịa ahụ nwere ahụike, yabụ nzukọ chọrọ ihe omume ndị a:

wepụ ọgwụ na - anaghị egbochi ya na eriri afọ,
nlekota nke ihe ngosi, tinyere nlebara anya nke obi site na ECG,
na-eme ọgwụgwọ mmezi.

Sitagliptin nọ n'ọrụ na-arụ ọrụ nke ọma. Naanị 13.5% ka ewepụrụ maka oge anọ nke usoro ahụ. A na-ahọpụta ya naanị ka ọ bụrụ ebe ikpeazụ.

Mainzọ kachasị mma iji nwude ọgwụ ọgwụ site n'ahụ ahụ bụ site na mkpụrụ ume. Maka ndị ọrịa nwere ọrịa a akụrụ, akwara a na-anwale onwonye ha, mana n'ihe banyere akara nke nsogbu akụrụ, ọ na-ebelata:

agafeghị oke ma ọ bụ nnukwu ọdịda
ọnụ nke ọdụdụ na-adịghị ala ala.

Mmechi

Dabere na nkọwa ọgwụ a na nyocha banyere ya, anyị nwere ike ikwubi na ọ dị mma ma nwee mmetụta dị mma n'ọdịmma ndị ọrịa. Otu uru a na-apụghị ịgbagha agbagha bụ ihe fọrọ nke nta ka ọ bụrụ na enweghị mmetụta ọ bụla na-emetụta akụkụ ahụ. Dị ka o kwesịrị ịdị, mmadụ agaghị enwe ike ịhọrọ ọgwụ ahụ, yana nchikota ọgwụ ziri ezi na ọgwụ ọzọ, na-enweghị mmerụ ahụ ike ya. Iji mee nke a, ịkwesịrị ịkpọtụrụ endocrinologist, ma ghara iduzi ọgwụ gbasara onwe gị.

Ngwakọta na ụdị ntọhapụ

Mbadamba ụrọ - 1 mbadamba:

Ihe na-arụ ọrụ: sitagliptin phosphate monohydrate - 128.5 mg, nke kwekọrọ na ọdịnaya nke sitagliptin - 100 mg,
Ndị na-ahụ maka ihe: microcrystalline cellulose - 123.8 mg, hydrogen phosphate calrusili na - - 123,8 mg, croscarmellose sodium - 8 mg, magnesium stearate - 4 mg, sodium stearyl fumarate - 12 mg,
mejupụtara sheath: opadry II beige, 85F17438 - 16 mg (polyvinyl mmanya - 40%, titanium dioxide (E171) - 21.56%, macrogol 3350 (polyethylene glycol)) - 20.2%, talc - 14.8%, iron oxide (E172) - 3.07% , iron oxide red (E172) - 0.37%).

14 pi. - blisters (2) - ngwugwu nke kaadiboodu.

Mbadamba nkume ndị ahụ, nke a na-eji ihe mkpuchi beige gbara gburugburu, dị okirikiri, biconvex, na-etinye ihe osise "277" n'otu akụkụ ma dị mma n'akụkụ nke ọzọ.

Ọgwụ Xelevia (sitagliptin) bụ ọgwụ ọnụ na-arụ ọrụ, ihe na - egbochi oke nke enzyme dipeptidyl peptidase-4 (DPP-4), ezubere maka ịgwọ ụdị ọrịa shuga mellitus nke 2. Sitagliptin dị iche n'ụdị kemịkalụ na ọgwụ ọgwụ site na analogues nke glucagon-peptide-1 (GLP-1), insulin, sulfonylureaeri, biguanides, gamon receptor agonists nke peroxisome proliferator (PPAR-γ), alpha-glucosidase inhibitors, amylin ana. Site na igbochi DPP-4, sitagliptin na-eme ka ịbawanye ụba nke homonụ abụọ nke ezinụlọ incretin: GLP-1 na glucose-polyulinptide insulinotropic (HIP). Hormones nke ezinụlọ dị na nzuzo na-abanye na eriri afọ n'oge ụbọchị, itinye uche ha na-abawanye na nzaghachi maka nri oriri. Mgbakwụnye ahụ bụ akụkụ nke sistem nke anụ ahụ maka idozi glucose homeostasis. Na nkwekọrịta glucose ọbara dị elu ma ọ bụ dị elu, homonụ nke ezinụlọ dị na mbụ na-enye aka na mmụba nke insulin njikọ, yana ihe nzuzo ya site na mkpụrụ ndụ beta nke pancreatic n'ihi akara nke usoro intracellular metụtara cyclic adenosine monophosphate (AMP).

GLP-1 na - enye aka belata mmụkọ nke glucagon site na mkpụrụ ndụ alịpịrị. Mbelata ịbawanye glucagon megide mmalite nke mmụba nke insulin na-enyere aka belata imepụta glucose site na imeju, nke na-eduga ná mbelata nke glycemia. Usoro a dị iche na usoro nke usoro sulfonylurea, nke na-akpali ntọhapụ nke insulin ọbụlagodi na nchịkọta glucose dị n'ọbara, nke e mepụtara na mmepe nke hypoglycemia hypoglycemia ọ bụghị naanị na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa mellitus, kamakwa ndị mmadụ nwere ahụ ike.

N'itinye ala glucose dị ala n'ọbara, ahọpụtaghị nsonaazụ nke ọgwụ ndị a na-enwe na mwepụta insulin na mbelata ihe nzuzo glucagon. GLP-1 na HIP anaghị emetụta ntọhapụ glucagon na nzaghachi hypoglycemia. N'okpuru ọnọdụ physiological, ọrụ nke incretins nwere oke site na enzyme DPP-4, nke na-eme ngwa ngwa hydrolyze ibu na ngwaahịa nke anaghị arụ ọrụ.

Sitagliptin na-egbochi hydrolysis nke incretins site na enzyme DPP-4, si otú a na-abawanye ụba plasma nke ụdị arụ ọrụ GLP-1 na HIP. Site na ịba ụba nke incretins, sitagliptin na-abawanye ntọhapụ glucose na insulin ma na - enyere aka belata glucagon. N'ime ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa hyperglycemia, mgbanwe ndị a na nzuzo nke insulin na glucagon na-eduga n'ịbelata mkpokọta gemocosylated heblolobin HbA1C na mbelata n'ọbara plasma nke glucose, kpebisiri ike na afọ efu na mgbe ule nnwale.

N'ime ndị ọrịa nwere ụdị ọrịa shuga 2 nke mellitus, ị oneụ otu Xelevia na-eduga na mgbochi nke ọrụ enzyme DPP-4 maka awa 24, nke na-eduga n'ịba ụba na mkpokọta nke na-ekesa incretins GLP-1 na HIP site na ihe dị ka 2-3, mmụba na mkpokọta plasma nke insulin na C- peptide, mbelata nke mkpokọta glucagon n’ime plasma ọbara, mbelata glucose na-ebu ọnụ, yana mbelata nke glycemia mgbe ịbubatịrị glucose ma ọ bụ itinye nri.

A kọwaala ọgwụ ọgwụ sitagliptin n'ime ndị ahụike yana ndị ọrịa nwere ụdị shuga 2. N'ime ndị mmadụ nwere ahụike, mgbe nchịkwa ọnụ nke 100 mg nke sitagliptin, a na-ahụ ntinye ọgwụ ngwa ngwa site na itinye uche kachasị (Cmax) na oke site na 1 ruo 4 awa site na nchịkwa. Mpaghara dị n'okpuru usoro nlebara anya oge oge (AUC) na-abawanye na nha ka ọkpụrụkpụ ahụ yana n’ihe ọmụmụ ahụike bụ elekere 8.52 μmol / L * mgbe ewere ọgwụ mgwo 100 mg, Cmax bụ 950 nmol / L. AUC plasma nke sitagliptin mụbara site na ihe dịka 14% mgbe ọgwụ nke ọgwụ ọgwụ ga-esote 100 mg iji mezuo ọnọdụ ịha nhata mgbe ị takingụchara ọgwụ nke mbụ. Ngwakọta nzuzo na ntanetị iche nke sitagliptin AUC enweghị nlele.

Ezigbo bioavailability nke sitagliptin dị ihe dị ka 87%. Ebe ọ bụ na nri sitagliptin na nri ndị nwere abụba enweghị mmetụta na pharmacokinetics, enwere ike ịkọ ọgwụ Xelevia n'agbanyeghị n'agbanyeghị nri.

Ogologo nha nke nkesa n’usoro izizi ihe n’otu mgbe 100 mg sitagliptin n’ime ndị ọrụ afọ ofufo ahụike dị ihe dịka 198 l. Ngwurugwu sitagliptin na-ejikọ na protein plasma dị obere na 38%.

Ihe dị ka 79% nke sitagliptin bụ akụrụ na-agbanweghi. Naanị ọgwụ pere mpe n received ọgwụ a nabatara n ’anụ ahụ na - metabolized.

Mgbe nchịkwa sitagliptin 14C nke 14C kpọrọ aha n'ime, ihe dịka 16% nke sitagliptin redio na-egosipụta dị ka metabolites ya. Achọpụtara ọnụọgụ nke metabolites 6 nke sitagliptin, ikekwe enweghị ọrụ inhibitory DPP-4. Nnyocha ọmụmụ in vitro kpughere na ihe isoenzymes bụ isi so na metabolism nke sitagliptin nwere bụ CYP3A4 na CYP2C8.

Mgbe nchịkwa sitagliptin 14C pụtara 14 n'ime ndị ọrụ afọ ofufo nwere ahụike, ihe dị ka 100% sitagliptin na-achịkwa ka ewepụtara: 13% site na eriri afọ, 87% site na akụrụ n'ime otu izu mgbe ị theụsịrị ọgwụ. Ogologo ngwụcha ọkara ndụ sitagliptin site na nchịkwa ọnụ nke 100 mg dị ihe dị ka awa 12.4; mkpochapu ezigara dị ihe dị ka 330 ml / min.

A na - emegharị sitagliptin na mbụ site na excretion site na akụrụ site na usoro ịgbari tubular na-arụ ọrụ. Sitagliptin bụ mkpụrụ maka onye na - ebugharị ebumnuche mmadụ na - ebugharị ụdị nke atọ (hOAT-3), nke nwere ike itinye aka na mpụta sitagliptin site na akụrụ. Dika ogwu, iminye ihe banyere hOAT-3 na mbufe sitagliptin. Sitagliptin bụkwa mkpụrụ nke p-glycoprotein, nke nwekwara ike itinye aka na mpụta nke sitagliptin site na akụrụ. Agbanyeghị, cyclosporin, onye na-egbochi p-glycoprotein, bebeghi nhicha nke sitagliptin.

Pharmacokinetics na otu ndị ọrịa n'otu n'otu:

Ọrịa nwere ọdịda gbasara akụrụngwa:

Emere nnyocha na-emeghe emeghe nke sitagliptin na dose nke 50 mg kwa ụbọchị iji mụọ ọgwụ ọgwụ ya n'ime ndị ọrịa nwere ogo ogo ogo adịghị ike gbasara akụrụ. A na-ekewa ndị ọrịa gụnyere n'ọmụmụ ihe dị iche iche nke ndị ọrịa nwere nsogbu akwara dị nro (mwepụ nke mkpụrụ osisi sitere na 50 ruo 80 ml / min), na-agbatịzi (njikwa nke creatinine site na 30 ruo 50 ml / min) na ọdịda akwara siri ike (mwepụ nke ihe na-erughị 30 ml / min) , yana yana ọnụ ala ọgbụgba na-adịghị ala ala nke na-achọ ịba ahụ.

N'ime ndị ọrịa nwere ajọ akụrụngwa obere ọrịa, enweghị mgbanwe dị ukwuu n'ụlọ ọgwụ na nsonaazụ plasma nke sitagliptin ma e jiri ya tụnyere ìgwè ndị ọrụ afọ ofufo na-achịkwa ahụ ike.

A hụrụ mmụba okpukpu abụọ na sitagliptin AUC ma e jiri ya tụnyere ndị na-ahụ maka njikwa ka a hụrụ na ndị ọrịa nwere obere gbasara akwara na-ada ada, ihe dị ka okpukpu anọ na AUC ka a hụrụ na ndị ọrịa nwere nnukwu akwara na-ada ada, yana ndị ọrịa nwere njedebe akwara na-adịghị ala ala ma e jiri ya tụnyere otu njikwa ahụ. Sitagliptin jiri obere hemodial wepụrụ Sitagliptin: naanị 13.5% nke ọgwụ ahụ ka e wepụrụ n'ahụ ya n'oge nnọkọ nyocha nke awa 3-4.

Ya mere, iji nweta ọgwụgwọ ịgwọ ọrịa nke sitagliptin na plasma ọbara (dị ka nke a na ndị ọrịa nwere ọrụ gbasara akwara dị ogologo) na ndị ọrịa nwere obere akwara siri ike, a chọrọ idozi dose.

Ọrịa ọrịa imeju mebiri:

N'ime ndị ọrịa nwere oke ịba ọcha n'anya (isi ihe 7-9 maka -mụaka-Pugh), nkezi AUC na Cmax nke sitagliptin nwere otu ọgwụ nke 100 mg na-abawanye site na ihe dịka 21% na 13%. Yabụ, achọrọ nhazigharị maka ọrịa imeju dị nwayọ na nke ekwesighi.

Enweghị data nyocha ọ bụla banyere ojiji nke sitagliptin na ndị ọrịa nwere oke ịba ọcha n'anya (ihe karịrị isi 9 na ọnụ ọgụgụ nke Child-Pugh). Agbanyeghị, n'ihi eziokwu ahụ bụ sitagliptin na-akachasị akụrụ, mmadụ ekwesịghị ịtụ anya mgbanwe dị ukwuu na ọgwụ ọgwụ nke sitagliptin na ndị ọrịa nwere nkwarụ hepatic siri ike.

Afọ ndụ nke ndị ọrịa enweghị mmetụta dị ukwuu na-adakarị na ọgwụ ọgwụ nke sitagliptin. E jiri ya tụnyere ndị ọrịa na-eto eto, ndị ọrịa agadi (65-80 afọ) nwere ọnọdụ sitagliptin dị ihe dịka 19% dị elu. Ọ nweghị mgbanwe ọ bụla dabere na afọ ole achọrọ.

Ogwu hypoglycemic ọgwụ.

Mmetụta Xelevia

Sitagliptin na-anabata nke ọma ma na monotherapy yana yana ọgwụ hypoglycemic ndị ọzọ. N'ime ule a na-adakarị, ọnọdụ nke ihe ọghọm, yana ugboro ole ọgwụ iwepụrụ n'ihi ajọ ihe, yụrụ ndị nke nwere placebo.

Dabere na ọmụmụ 4 na-achịkwa placebo (izu 18-18) nke sitagliptin na mkpụrụ ọgwụ kwa ụbọchị nke 100-200 mg dị ka ọgwụgwọ mono- ma ọ bụ ọgwụ ngwakọta na metformin ma ọ bụ pioglitazone, ọ nweghị mmeghachi omume ọjọọ metụtara ọgwụ ọmụmụ, a hụrụ ugboro ole nke gafere 1% na ndị ọrịa ahụ. na-ewere sitagliptin. Ihe nchekwa nchekwa kwa ụbọchị nke 200 mg dị ka profaịlụ nchekwa nke ọgwụ kwa ụbọchị nke 100 mg.

Nyochaa data enwetara n’oge ule dị n’elu ahụ gosipụtara n’ogologo hypoglycemia n’ime ndị ọrịa na-ewere sitagliptin yiri nke ahụ na placebo (sitagliptin 100 mg-1.2%, sitagliptin 200 mg-0.9%, placebo - 0.9%). Ugboro ugboro nke na-enyocha ihe ọgbụgba na -eme onwe ya mgbe ị na-ewere sitagliptin na ọgwụ abụọ a yiri nke ahụ mgbe ị na-ewere placebo (ma e wezụga oge karịa ọgbụgba mgbe ị na-ewere sitagliptin na ọnụọgụ 200 mg kwa ụbọchị): mgbu afọ (na-egbu sitagliptin 100 mg - 2) , 3%, sitagliptin 200 mg - 1.3%, placebo - 2.1%), ọgbụgbọ (1.4%, 2.9%, 0.6%), vomiting (0.8%, 0.7% , 0.9%), afọ ọsịsa (3.0%, 2.6%, 2.3%).

N ’ọmụmụ niile, a na-edekọ mmeghachi omume dị n’ ụdị hypoglycemia n’edere akụkọ niile nke akara ngosipụta akparamagwa nke hypoglycemia, atụghị nnochiba anya glucose ọbara.

Na-amalite usoro ọgwụgwọ na metformin:

N’ime izu iri abụọ na anọ, ọmụmụ ihe na - achịkwa ọgwụ ịba uru nke ịmalite ọgwụgwọ na sitagliptin na mkpụrụ ọgwụ kwa ụbọchị nke 100 mg na metformin kwa ụbọchị nke 1000 mg ma ọ bụ 2000 mg (sitagliptin 50 mg + metformin 500 mg ma ọ bụ 1000 mg x 2 ugboro kwa ụbọchị) na ìgwè ọgwụgwọ mmakọ. Tụnyere ndị metformin monotherapy, a hụrụ ihe ojoo ndị a:

A hụrụ mmeghachi omume ọjọọ na ị theụ ọgwụ ahụ na ọtụtụ & & gt1% na usoro ọgwụgwọ sitagliptin na ọtụtụ oge karịa na usoro ọgwụgwọ metformin na monotherapy: afọ ọsịsa (sitagliptin + metformin - 3,5%, metformin - 3.3%), dyspepsia (1, 3%, 1.1%), isi ọwụwa (1.3%, 1.1%), flatulence (1.3%, 0,5%), hypoglycemia (1.1%, 0,5%), vomiting (1.1%, 0.3%).

Njikọ ya na ihe njikọ sulfonylurea ma ọ bụ usoro sulfonylurea na metformin:

N'ime ọmụmụ 24-placebo na-achịkwa usoro ọgwụgwọ njikọta na sitagliptin (ọgwụ kwa ụbọchị nke 100 mg) na glimepiride ma ọ bụ glimepiride na metformin, a hụrụ ihe omume ndị na-esote na otu nke ọgwụ ọmụmụ ahụ tụnyere ìgwè ndị ọrịa na-ewere placebo na glimepiride ma ọ bụ glimepiride na metformin:

A hụrụ mmeghachi omume ọjọọ na ị theụ ọgwụ ahụ na ọtụtụ & & gt1% na usoro ọgwụgwọ na sitagliptin na ọtụtụ oge karịa na njikọta na placebo: hypoglycemia (sitagliptin - 9.5%, placebo - 0.9%).

Nchikota nkwuputa izizi ya na ndi agonists PPAR-::

N'ime ọmụmụ izu iri abụọ na anọ nke ịmalite ọgwụ ịgwọ ọrịa na sitagliptin na ọgwụ kwa ụbọchị nke 100 mg na pioglitazone kwa ụbọchị nke 30 mg, a hụrụ ihe ndị na-esote ihe omume ndị a na-ejikọta ya na usoro ọgwụgwọ pioglitazone monotherapy:

A hụrụ mmeghachi omume ọjọọ na ị theụ ọgwụ ahụ na ọtụtụ & & gt1% na usoro ọgwụgwọ nke sitagliptin na ọtụtụ mgbe karịa na ọgwụgwọ pioglitazone na monotherapy: mbelata asymptomatic na ịta ọbara glucose (sitagliptin + pioglitazone - 1.1%, pioglitazone - 0.0%) hypoglycemia Symptomatic (0.4%, 0.8%).

Njikọ ya na ndị agonists PPAR-y na metformin:

Dika omumu ihe omumu putara n’ime ogwu sitagliptin (onwa kwa ubochi nke onwa) na rosiglitazone na metformin n’ime ndi n’ulo ogwu a, a huru ihe ojoo ndi a na atụnyere ndi otu ndi oria na-achu aria srosiglitazone na metformin:

N ’izu nke iri na asatọ:

A hụrụ mmeghachi omume ọjọọ na ị theụ ọgwụ ahụ na ọtụtụ & & gt1% na usoro ọgwụgwọ na sitagliptin na ọtụtụ oge karịa na njikọta na placebo: isi ọwụwa (sitagliptin - 2.4%, placebo - 0.0%), afọ ọsịsa (1.8 %, 1.1%), ọgbụgbọ (1.2%, 1.1%), hypoglycemia (1.2%, 0.0%), vomiting (1.2%, 0.0%).

N'afọ iri ise na ise nke nleba anya:

A hụrụ mmeghachi omume ọjọọ na ị theụ ọgwụ ahụ na ọtụtụ & & gt1% na usoro ọgwụgwọ na sitagliptin na ọtụtụ oge karịa na njikọta na placebo: isi ọwụwa (sitagliptin - 2.4%, placebo - 0.0%), hypoglycemia (2.4 %, 0.0%), ọrịa elu akụkụ okuku ume (1.8%, 0.0%), ọgbụgbọ (1.2%, 1.1%), ụkwara (1.2%, 0.0%), ọrịa fungal nke anụ ahụ (1.2%, 0.0%), akụkụ ụbụrụ (1.2%, 0.0%), vomiting (1.2%, 0.0%).

Njikọ ya na insulin:

N'ime izu iri abụọ na anọ, ọmụmụ ihe na - achịkwa ọgwụ mmịnye ọgwụ na sitagliptin (na mkpụrụ ọgwụ kwa ụbọchị 100) yana insulin kwa ụbọchị (yana ma ọ bụ na - enweghị metformin) n'ime ìgwè ndị na - amụ ọgwụ ma e jiri ya tụnyere ìgwè ndị ọrịa na - a placeụ ọgwụ na insulin (ya na ma ọ bụ na - enweghị metformin), ihe ndia:

A hụrụ mmeghachi omume ọjọọ na ị theụ ọgwụ ahụ na ọtụtụ & & gt1% na usoro ọgwụgwọ sitagliptin na ọtụtụ oge karịa na usoro ọgwụgwọ insulin (na ma ọ bụ na-enweghị metformin): hypoglycemia (sitagliptin + insulin (yana ma ọ bụ na-enweghị metformin)) - 9.6%, placebo + insulin (ya na ma obu n’enweghi metformin) - 5.3%), flu (1.2%, 0.3%), isi ọwụwa (1.2%, 0.0%).

N'ime ọmụmụ ihe izu 24 ọzọ, nke ndị ọrịa natara sitagliptin dị ka usoro ọgwụgwọ ọzọ maka ọgwụgwọ insulin (na ma ọ bụ na-enweghị metformin), enweghị mmeghachi omume ọjọọ metụtara ị takingụ ọgwụ ahụ na ọtụtụ ugboro & gt1% na ìgwè ọgwụgwọ sitagliptin (na dose nke 100 mg ), na ọtụtụ mgbe karịa na placebo otu.

Na nyocha juputara na nyocha nke nnwale afọ abụọ nke ojiji nke sitagliptin na ọgwụ kwa ụbọchị nke 100 mg ma ọ bụ ọgwụ nchịkwa kwekọrọ (arụ ọrụ ma ọ bụ placebo), ihe kpatara ọrịa pancreatitis na-enwetaghị nkwarụ bụ 0.1 maka otu ọrịa 100 afọ nke ọgwụgwọ na otu ọ bụla.

Onweghi ihe ndaghari di omimi banyere ogwu di nkpa ma obu ECG (tinyere oge nke QTc oge) ahuru na anagide sitagliptin.

Ọmụmụ Sitagliptin Sitena Ntụle Nchekwa Ahụhụ (TECOS):

Ọmụmụ ihe banyere nchekwa obi yana sitagliptin (TECOS) gụnyere ndị ọrịa 7332 na-ewere sitagliptin 100 mg kwa ụbọchị (ma ọ bụ 50 mg kwa ụbọchị ma ọ bụrụ na ntụpọ ahụ na-ekwu na ọnụego nzacha ọnụ ọnụ (eGFR)) bụ & gt30 na & lt50 ml / min / 1, 73 m), yana ndị ọrịa 7339 na-ewere placebo na ọnụ ọgụgụ ndị ọrịa niile enyere iwu ka a gwọọ ha. A tinyekwara ihe ọmụmụ a (sitagliptin ma ọ bụ placebo) na usoro ọgwụgwọ dabere na ụkpụrụ mba dị adị maka ịhọrọ ọkwa lekwasịrị anya nke HbA1C yana nchịkwa nke ihe ndị nwere ike ibute ọrịa obi. Ọmụmụ ihe a gụnyere ngụkọta nke ndị ọrịa 2004 dị afọ 75 na karịa (970 were sitagliptin na 1034 wee placebo). Ọnọdụ dị oke njọ nke ihe ọjọọ dị na ndị ọrịa na-ewere sitagliptin bụ otu ihe ahụ na ndị ọrịa na-ewere placebo. Nyochaa nsogbu ndị a chọpụtara na mbụ na-arịa ọrịa shuga kpughere ọnọdụ yiri nke ajọ ihe n'etiti otu dị iche iche, gụnyere oria (18.4% na ndị ọrịa na-ewere sitagliptin na 17.7% na ndị ọrịa na-a placeụ ọgwụ) yana arụ ọrụ ezumike arụ ọrụ ( 1.4% na ndị ọrịa na-ewere sitagliptin na 1.5% na ndị ọrịa na-ewere placebo). Ihe omuma nke ihe ojoo na ndi oria noo n’agbata afọ iri asaa na asaa gbagowekwara nke ahụ maka ndị nkịtị.

N'ime ọnụ ọgụgụ ndị ọrịa nyere ọgwụ (“ebumnuche ịgwọ ya)”, n'etiti ndị natara ọgwụ insulin na / ma ọ bụ sulfonylureas na mbụ, oke nke hypoglycemia dị 2.7% n'ime ndị ọrịa na-ewere sitagliptin, na 2, 5% na ndị ọrịa na-ewere placebo. N'ime ndị ọrịa na-anatabeghị insulin na / ma ọ bụ sulfonylurea, ọnọdụ nke nnukwu hypoglycemia bụ 1.0% na ndị ọrịa na-ewere sitagliptin na 0.7% na ndị ọrịa na-ewere placebo. Ọnọdụ nke ọrịa pancreatitis kwenyesiri ike bụ 0.3% na ndị ọrịa na-ewere sitagliptin na 0.2% na ndị ọrịa na-ewere placebo. Ọnọdụ nke ọrịa cancer egosipụtara na neoplasms ọjọọ bụ 3.7% na ndị ọrịa na-ewere sitagliptin na 4.0% na ndị ọrịa na-ewere placebo.

N'oge nlele ntinye aha na ojiji nke sitagliptin na monotherapy na / ma ọ bụ na njikọta ọgwụ na ndị nnọchianya hypoglycemic ndị ọzọ, a chọpụtara ihe omume ndị ọzọ na-adịghị mma. Ebe ọ bụ na enwetara data ndị a afọ ofufo site na ọnụ ọgụgụ ebighi-ebi, a gaghị ekpebi ugboro ole na mmekọrịta dị n'etiti ọgwụgwọ nke ihe ọjọọ ndị a. Ndị a gụnyere:

Ihe mmeghachi omume hypersensitivity, gụnyere anaphylaxis, angioedema, ihe ọkụ ọkụ, urticaria, akpụkpọ vasculitis, ọrịa anụ ahụ na-efe efe, gụnyere ọrịa Stevens-Johnson syndrome, nnukwu ọrịa akwara, gụnyere ọbara ọgbụgba na necrotic n'ụdị na-akpata ọnwụ na-adịghị egbu egbu, ọrụ na-arụ ọrụ na-arụ ọrụ na-arụ ọrụ, gụnyere akwara akwara. ezughi oke (mgbe ụfọdụ a na-achọ ya), ọrịa na-efe efe nke elu akụkụ, nasopharyngitis, afọ ntachi, ọgbụgbọ, isi ọwụwa, arthralgia, myalgia, mgbu aka, azụ mgbu, itching, pemphigoid.

Mgbanwe na egosi ulo laabu:

Ugboro ugboro ihe nlere nlere n'ụlọ ime ụlọ na usoro ọgwụgwọ sitagliptin (na ọgwụ kwa ụbọchị nke 100 mg) bụ nke a pụrụ iji tụnyere ugboro ole a na-etinye na placebo. N'ọtụtụ, mana ọ bụghị ule niile nke ụlọ ọgwụ, enwere ntakịrị mmụba na ọnụ ọgụgụ leukocyte (ihe dị ka 200 / comparedl ma e jiri ya tụnyere placebo, nkezi ọdịnaya na mmalite ọgwụgwọ bụ 6600 / )l), n'ihi mmụba na ọnụ ọgụgụ nke ndị na - enwe nsogbu.

Nyocha nyocha nke nyocha ụlọ ọgwụ nke ọgwụ gosipụtara ntakịrị mmụba na mkpo uric acid (ihe dịka 0.2 mg / dl ma e jiri ya tụnyere placebo, ngụkọta oge tupu ọgwụgwọ bụ 5-5.5 mg / dl) na ndị ọrịa na-anata sitagliptin na dose nke 100 na 200 mg ụbọchị. Enweghị ikpe ọ bụla nke mmepe gout. Enwere ntakịrị mbelata na mkpokọta alkaline phosphatase (ihe dị ka 5 IU / L ma e jiri ya tụnyere placebo, ngụkọta oge tupu ọgwụgwọ bụ 56-62 IU / L), na-esonye na ntakịrị mbelata na mgbakasị ọkpụkpụ nke alkaline phosphatase.

Achọpụtaghị mgbanwe ndị edepụtara na plọg nke ụlọ nyocha anaghị achọpụta ọgwụgwọ dị mkpa.

N'ime omumu banyere nmekorita ya na ogwu ndi ozo, sitagliptin enwebeghi nsogbu ogwu di na ogwu nke ogwu ndia: metformin, rosiglitazone, glibenclamide, simvastatin, warfarin, mgbochi ogwu. Dabere na data ndị a, sitagliptin anaghị egbochi CYP3A4, 2C8, ma ọ bụ 2C9 isoenzymes. Dabere na data vitro, sitagliptin adịghị egbochi CYP2D6, 1A2, 2C19 na 2B6 icheenzyme ma ghara ibulite CYP3A4 isoenzyme. Nchịkwa ugboro ugboro nke metformin yana ijikọ sitagliptin emetụtaghị ọgwụ pokpat nke sitagliptin na ndị ọrịa nwere ụdị ọrịa shuga 2 nke ọrịa mellitus.

Dika onu ogugu ogwu nke onu ogugu nke ndi oria nwere oria nke abuo n’ariri oria abuo, ihe ogugu adabeghị nsogbu ogwu na sitagliptin. Ọmụmụ ahụ nyochara ọtụtụ ọgwụ ndị ọrịa na-ejikarị ụdị ọrịa shuga mellitus 2, gụnyere: ọgwụ ndị na-egbu ume (statins, fibrates, ezetimibe), ndị nnọchi antiplatelet (clopidogrel), ọgwụ antihypertensive (AC inhibitors, angiotensin II rece antor antagonists, beta-blockers, blockers Ọgwụ calcium “dị nwayọ”, hydrochlorothiazide), ọgwụ mgbochi na-abụghị steroidal (naproxen, diclofenac, celecoxib), antidepressants (bupropion, fluoxetine, sertraline), antihistamines (cetiri) zine), proton pump inhibitors (omeprazole, lansoprazole) na ọgwụ iji gwọọ dysfunction erectile (sildenafil).

Enwere ntakịrị mmụba na AUC (11%), yana nkezi Cmax (18%) nke digoxin mgbe ejikọtara ya na sitagliptin. A naghị atụle mmụba a dị ka ọgwụ. A naghị atụ aro ịgbanwe ọgwụ nke digoxin ma ọ bụ sitagliptin mgbe ejikọtara ọnụ.

Mmụba na AUC na Cmax nke sitagliptin bụ 29% na 68%, n'otu aka ahụ, n'ime ndị ọrịa nwere ojiji otu ọgwụ ọnụ na 100 mg nke sitagliptin na otu ọgwụ ọnụ nke 600 mg nke cyclosporin, onye na-egbochi p-glycoprotein. Mgbanwe ndị a hụrụ na njikwa ọgwụ nke sitagliptin adịghị atụle ụlọ ọgwụ dị mkpa. Agaghị atụ aro ịgbanwe ọgwụ Xelevia mgbe ejikọtara ya na cyclosporine na ndị ọzọ na-egbochi p-glycoprotein (dịka ọmụmaatụ ketoconazole).

Nyocha ndị ọgwụ na-eme ka ndị ọrịa na ndị ọrụ afọ ofufo dị mma (N = 858) wee nwee ọtụtụ ọgwụ ọgwụ (N = 83, ihe dị ka ọkara nke akụrụ wepụta) ekpughere mmetụta ọfụma dị ukwuu nke ihe ndị a na pharmacokinetics nke sitagliptin.

Usoro ọgwụgwọ Xelevia

Nlekọta akwadoro nke Xelevia bụ 100 mg otu ugboro kwa ụbọchị dị ka ọgwụ monotherapy, ma ọ bụ yana metformin, ma ọ bụ ihe ndị na-eme ka sulfonylurea, ma ọ bụ PPAR-γ agonists (thiazolidinediones), ma ọ bụ insulin (yana ma ọ bụ na-enweghị metformin), ma ọ bụ na metformin na usoro sitere na sulfonylurea, ma ọ bụ metformin na PPAR-γ agonists.

Enwere ike iwere Xelevia na-eri nri. A ga-ahọpụta usoro usoro usoro ọgwụgwọ metformin, ọgwụ sulfonylurea na ndị na-ahụ maka PPAR-based dabere na usoro usoro ọgwụ ndị a tụrụ aro ya.

Mgbe ị na-ejikọ ndị Xelevia na ọgwụ sulfonylurea ma ọ bụ insulin, ọ ga-adị mma ka ị belata usoro ọdịnala na-atụ aro sulfonylurea ma ọ bụ ọgwụ insulin iji belata ohere ị nwere ịmalite hypoglycemia na-akpata.

Ọ bụrụ na onye ọrịa ahụfuru ị Xụ ọgwụ Xelevia, a ga-a takenụ ọgwụ ngwa ngwa o kwere mee mgbe onye ọrịa chetara ọgwụ ahụ furu efu.

Ọ bụ ihe anabataghị iji were okpukpu abụọ nke Xelevia n'otu ụbọchị.

Ọrịa nwere ọdịda gbasara akụrụngwa:

Ndị ọrịa nwere ezughi oke gbasara akụrụngwa (mkpụsị creatinine (CC) & gt50 ml / min, ihe dika ngbanwe a serin creatinine of & lt1.7 mg / dl na ụmụ nwoke na & lt1.5 mg / dl na ụmụ nwanyị) anaghị achọ mmezi dose nke Xelevia.

N'ihi mkpa ịhazigharị ọgwụ sitagliptin na ndị ọrịa nwere obere akwara ezughi oke, enweghị Xelevia adịghị egosi na ụdị ndị ọrịa a (enweghị ihe ize ndụ dị na mbadamba 100 mg na enweghị 25 mg na 50 mg onunu ogwu anaghị enye ohere maka usoro ọgwụgwọ ya na ndị ọrịa nwere akụrụ. ezughi oke nke ogo na oke aka).

N'ihi mkpa ịhazigharị dose, a na-atụ aro ka ndị ọrịa nwere nsogbu gbasara akwara na-enyocha ọrụ gbasara aha tupu ịmalite ọgwụgwọ na sitagliptin na oge site n'oge ọgwụgwọ.

Ọrịa ọrịa imeju mebiri:

Enweghị mgbanwe mmegharị nke Xelevia chọrọ na ndị ọrịa nwere nkwarụ hepatic dị nfe na obere. Agụghị ọgwụ a n’ime ndị ọrịa nwere nnukwu ọrịa imeju.

Onweghi mmezi ogwu nke Xelevia choro n’ebe ndi agadi no.

N'oge ọnwụnwa nke ụlọ ọgwụ na ndị ọrụ afọ ofufo nwere ahụ ike, a na-anabata otu ọgwụ 800 sitagliptin nke ọma. A hụrụ ntakịrị mgbanwe na oge QTc, na-atụleghị ọgwụ dị ka ụlọ ọgwụ, na otu n'ime ọmụmụ sitagliptin n'ọtụtụ 800 mg kwa ụbọchị. Agụghị ọgwụ karịrị 800 mg kwa ụbọchị n’ime ụmụ mmadụ.

N'ime usoro izizi nke ụlọ ọgwụ, ọtụtụ usoro ọgwụgwọ ọ bụla na-esochi mmeghachi omume metụtara ọgwụgwọ na sitagliptin mgbe ị na-a theụ ọgwụ ahụ kwa ụbọchị ruo 400 mg maka ụbọchị 28.

N'ihe banyere oke ịdoụbiga mmanya ókè, ọ dị mkpa ịmalite usoro nkwado ọkọlọtọ: iwepu ọgwụ a na-ejighị n'aka na eriri afọ, nyochaa akara ndị dị mkpa, gụnyere ECG, yana ntinye ọgwụgwọ mmezi, ma ọ bụrụ na ọ dị mkpa.

Sitagliptin nwere nkụda mmụọ. N'ime ọmụmụ ụlọ ọgwụ, naanị 13.5% nke ọgwụ ahụ ka ewepụrụ n'ahụ ya n'oge nnọkọ nyocha nke awa 3-4. Enwere ike ịkọ ọgwụ ogologo oge ọ bụrụ na ọ dị mkpa. Enweghi ihe akaebe banyere ịdị irè nke mgbapụta peritoneal maka sitagliptin.

Routezọ kachasị ewepụta sitagliptin site n’anụ ahụ bụ excretion gbasara akwara. Iji mezuo otu plasma ahụ dịka ndị ọrịa nwere akụrụngwa akachaghị nke akụrụ, ndị ọrịa nwere obere akwara siri ike, yana ndị ọrịa nwere ngwụcha akwara na-adịghị ala ala nke chọrọ akwara hemodialysis ma ọ bụ mgbawa ọnọdụ, chọrọ mgbanwe nke dose nke Xelevia. .

Enweela akụkọ banyere mmepe nke ọrịa pancreatitis, gụnyere ọbara ọgbụgba ma ọ bụ necrotic na nsonaazụ na-egbu egbu na adịghị egbu egbu, na ndị ọrịa na-ewere sitagliptin. Ekwesịrị ịgwa ndị ọrịa banyere njirimara njirimara nke nnukwu pancreatitis: na-adịgide, mgbu na-egbu mgbu. Ngosiputa nke ogwu nke pancreatitis wepu aka mgbe akwusiri sitagliptin. N'ihe banyere ntụrụaka a na-enyo enyo, ọ dị mkpa ịkwụsị ị Xụ Xelevia na ọgwụ ndị ọzọ dị ize ndụ.

Dabere na nnwale nke ụlọ ọgwụ sitagliptin, nnabata nke hypoglycemia n'oge monotherapy ma ọ bụ ọgwụgwọ njikọta na ọgwụ na-adịghị akpata hypoglycemia (metformin, pioglitazone) yiri nke ahụike hypoglycemia na placebo otu. Dị ka ọ dị na ọgwụ hypoglycemic ndị ọzọ, a hụrụ hypoglycemia na sitagliptin yana njikọ insulin ma ọ bụ ọgwụ sulfonylurea. Iji belata ihe ize ndụ nke ịmalite hypoglycemia nke sulfone, a ga-ebelata dose nke usoro sulfonylurea.

Jiri ndị agadi:

N'ime omumu ihe omumu, ihe oma na nchekwa nke sitagliptin n’ile ndi oria agadi (? 65 noo, ndi oria 409) dika ndi nke ndi oria n’erughi 65. Ndozigharị Doro dị afọ ole achọrọ. Okenye ndị okenye nwere ike ịzụlite gbasara akụrụngwa. Dika odi, dika ndi n’agba ndi ozo, odika idozi odi nkpa n’ebe ndi obia juputara na ezughi oke.

Ọmụmụ Sitagliptin Sitena Ntụle Nchekwa Ahụhụ (TECOS):

Leasedị ntọhapụ, ihe mejupụtara na nkwakọ

A na-emepụta ya n'ụdị beige, mbadamba biconvex n'ime mkpuchi fim. Ngwakọta:

sitagliptin phosphate monohydrate (100 mg sitagliptin),
calcium hydrogen phosphate emechighi,
microcrystalline cellulose,
sodium stearyl fumarate
sodium croscarmellose
stereta magnesium.

A na-etinye mbadamba nkume iri na anọ na bliri (2 n'ime katọn).

Mkparịta ụka ọgwụ ọjọọ

Enweghi mmetụta pụtara ìhè dị n'etiti ndị ọrụ ndị ọzọ na arụmọrụ Xelevia. Ya mere, onodu a anaghi acho igbanwe uzo ha si eme ya. Ihe ndi ozo bu sulfonylurea na insulin.

Sitagliptin anaghị emetụta ịdị irè nke ọgwụ ndị ọzọ. Enweghị mmekọrịta dị egwu na usoro ijikọ ọgwụgwọ na ndị ọrụ ndị ọzọ.

Agbanyeghị, iji zere nsogbu ahụike, mgbe ị na-edepụta ọgwụgwọ, ekwesịrị ịgwa onye ọkachamara banyere eziokwu nke ị otherụ ọgwụ ndị ọzọ.

Ntụziaka pụrụ iche

Iji zere hypoglycemia, a na-atụ aro ka ọ belata ọgwụ nke hypoglycemic ọgwụ ọzọ na usoro nkwonkwo.

Ọ dị mkpa ka ndị okenye karịa afọ 65 nyochaa ọnọdụ nke akụrụ, ebe ọ bụ na akụkụ ahụ a na-emetụtakarị nsogbu. Ndị ọrịa dị otú a yikarịrị ka ha ga-enwe hypoglycemia n'oge usoro ọgwụgwọ ọzọ na ọgwụ ndị ọzọ yiri ya.

Enweghi mmetụta ọ bụla na sistem.

Akụrụngwa nọ n'ọrụ n'onwe ya anaghị emetụta ikike iji igwe ma ọ bụ rụọ ọrụ. Agbanyeghị, na njikọta ọgwụgwọ, mmetụta nke akụkụ a yikarịrị. Ya mere, na nke a, ọ ka mma ịhapụ ịnya ụgbọ ala.

A na-ewepụta ya naanị na ndenye ọgwụ!

Tụnyere ihe analogues

Januvius. Ọgwụ na-adabere na sitagliptin. Na-emepụta ụlọ ọrụ "Merck Sharp", Netherlands. Ọnụahịa maka ịkwakọ ngwaahịa ga-abụ 1600 rubles na elu. Ihe akụrụngwa enyere dị ka Xelevia. Ọ bụ ihe dị n'ụdị dị omimi, na-emetụta shuga ọbara ma na-ebelata agụụ nke ndị ọrịa mamịrị. Ya mere, a na-edenyekarị ya ndị nwere oke ibu dịka ọrịa n'akụkụ. Nke minuses - ọnụ ahịa. Nke a bụ analogue zuru oke.

Yasitara. Mbadamba ndị nwere sitagliptin na ihe mejupụtara. Onye rụpụtara ya bụ Pharmasintez, Russia. Analogue nke ọgwụ ahụ, nke nwere mmetụta yiri ya na sete contraindications.Costkwụ ụgwọ maka ụdị a. Ọ ka adaba adaba maka ịdepụta ọgwụgwọ, ebe o nwere usoro atọ nke akụrụngwa nọ n'ọrụ - 25, 50 na 100 mg nke sitagliptin. Amachibidoro ndị inyom dị ime na ụmụaka. N'ime ụmụ obere minines - ọ na-akpatakarị hypoglycemia.

Vipidia. Ọ bụkwa ihe dị n'ụdị nkọ ahụ, ma enwere apogliptin. Odikwa n'ụdị mbadamba 12.5 na 25 mg. Ọnụahịa - site na 800 ruo 1150 rubles, dabere na usoro onunu ogwu. Takeda GmbH, Japan rụpụtara. Ihe o mere yiri nke a, mana ọ na-arụ ọrụ karịa. Edobela umuaka na ndi di ime n’ihi enweghi data nyocha. Nkọwa nke contraindications na ndepụta nke nsonaazụ ndị ọzọ.

Invokana. Mbadamba ndị dabeere na Canagliflozin. Na-emepụta ụlọ ọrụ Jantali Janssen-Silag. Ọnụ ego dị elu: site na 2600 rubles kwa 100 iberibe. A na-eji ya na ọgwụgwọ nke ọrịa shuga na enweghi ike nke metformin na nri. Agbanyeghị, a ga-ejikọrị ọgwụgwọ na nri ndị dọkịta họpụtara. Contraindications bụ ọkọlọtọ.

Galvus Met. Nke a bụ ọgwụgwọ ngwakọta maka ọrịa shuga, mgbe nsonaazụ nke otu ihe ezughi oke. Ihe mejuputara metformin na vildagliptin. Mbadamba bụ nke ụlọ ọrụ Switzerland bụ Novartis mepụtara. Ọnụahịa - site na 1500 rubles na n'elu. Nsonaazụ ahụ dị ogologo, ihe dịka awa 24. Enweghi ike iji ya na ọgwụgwọ umuaka, ndi di ime na ndi na-ete nwa. N'ime ndị agadi, a na-eji nlezianya mee ihe. Adabaraghị dị ka onye nnọchi insulin.

Trazenta. Ọgwụ a nwere linagliptin, nke bụkwa ihe na-egbochi DPP-4. Ya mere, mmemme ya na nke Xelevia. Ọ bụ ọkacha mma na e wepụrụ ya site na eriri afọ, ya bụ, nrụgide dị ntakịrị na-aputa akụrụ. Enwere ike iji ya na ọgwụ ndị ọzọ. Amachibidoro maka mbanye. Enwerekwa ọtụtụ mmetụta ndị ọzọ. Efu - site na 1500 rubles. A na - emepụta ụlọ ọrụ "Beringer Ingelheim Pharma" na Germany na USA.

Chingbughari na ogwu ozo bu nke dọkịta gha eme. Onweghi anakwere ọgwụ banyere onwe gị!

Na mkpokọta, ndị mmadụ na-arịa ọrịa shuga na-ekwu okwu ọma banyere ọgwụ a. A chọpụtara na arụmọrụ ya dị elu na ịdị mfe nke nnabata. Maka ụfọdụ, usọbọ a adabaghị.

Valery: “M na - akpọ Galvus, ahụrụ m ya n'anya. Mana mgbe ahụ ha kwụsịrị inye ya uru n'ụlọ ọgwụ m, dọkịta ahụ dụrụ m ọdụ ka m gaa Xelevia. Ahụghị m ọdịiche ahụ. Ha na-arụ ọrụ n'ụzọ yiri nke ahụ, dị ka dọkịta ahụ kọwara. Sugar dị nkịtị, anaghị m elele mmali. N'oge usoro ọgwụgwọ ahụ, “mmetụta ọjọọ” emeghị. Enwere m obi ụtọ na ọgwụ a. ”

Alla: “Dọkịta ahụ gbakwunyekwara Xelevia na insulin, ebe ọ bụ na onye nke mbụ anaghị anagide njigide shuga n'ụzọ nkịtị. Mgbe otu ụzọ nkeji anọ belatara usoro ọgwụgwọ ya, amalitere m inwe mmetụta nke ọma ruo na oke. Ihe ndị na-egosi na-amapụ, nnwale ahụ dị mma, yana ọnọdụ ahụike niile. Achọpụtara m na m chọrọ iri nri dị ala. Dọkịta ahụ kọwara na ọgwụ niile dị n'ụdị a na-eme otu a. Ọ dị mma, nke ahụ bụ mgbakwunye. ”