Etu esi eji ọgwụ Vipidia 25? > Ọgwụgwọ na mgbochi

Dodị usoro iji wepụta Vipidia bụ mbadamba ihe eji etinye fim: biconvex, oval, 12.5 mg nke ọ bụla; odo, n'otu akụkụ nke ihe ndị e dere “ALG-12.5” na “TAK”, 25 mg nke ọ bụla - uhie uhie, na "ALG-25" na "TAK" na-ezi ozi na ink dee ya n'otu akụkụ (7 na blisters, 4 blisters na kaadiboodu).

Ngwakọta 1 mbadamba:

ihe na - arụ ọrụ: alogliptin - 12.5 ma ọ bụ 25 mg (alogliptin benzoate - 17 ma ọ bụ 34 mg),
ihe inyeaka (12.5 / 25 mg): mannitol - 96.7 / 79.7 mg, magnesium stearate - 1.8 / 1.8 mg, croscarmellose sodium - 7.5 / 7.5 mg, microcrystalline cellulose - 22 5 / 22.5 mg, hyprolose - 4.5 / 4.5 mg,
mkpuchi ihe nkiri: hypromellose 2910 - 5.34 mg, acha odo odo oxide - 0.06 mg, titanium dioxide - 0.6 mg, macrogol 8000 - na ọnụọgụ ọnya, isi awọ nke F1 (shellac - 26%, sọks iron oxide ojii - 10%, ethanol - 26%, butanol - 38%) - na ọnụọgụ ọnụọgụ.

Mlọ ọgwụ

Alogliptin bụ ihe na - egbochi oke nke DPP (dipeptidyl peptidase) -4. Nhọrọ ya maka DPP-4 dị ihe dịka 10,000 oge karịa mmetụta ya na enzyme ndị ọzọ metụtara, karịchaa DPP-8 na DPP-9. DPP-4 bụ enzyme bụ isi so na mbibi nke homonụ nke ezinụlọ nke dị na nso nso: glucose na-adabere inspeototic polypeptide (HIP) na peptide-1 (HIP-1). A na-emepụta homonụ nke ezinụlọ dị na eriri afọ, mmụba nke ọkwa ha na emetụta nri. HIP na GLP-1 na-eme ka insulin na-arụ ọrụ na imepụta ya site na mkpụrụ ndụ beta dị na pancreas. GLP-1 belata mmepụta glucagon ma gbochie njikọta glucose.

Maka nke a, alogliptin abụghị naanị na-eme ka ọdịnaya nke incretins dịkwuo elu, kamakwa ọ na - eme ka njikọ glucose na - ebute glucose na - egbochi ogo nke glucagon na ọkwa glucose dị elu. N'ime ndị ọrịa nwere ụdị ọrịa shuga nke 2 tinyere hyperglycemia, mgbanwe ndị a na njikọta glucagon na insulin na-eme ka mbelata mkpakọ ọbara glycated HbA.₁_c na mbelata nke ọkwa glucose na plasma ọbara mgbe ewere ya n’afọ na-enweghị isi, na ịta ọkwa glucose postprandial.

Mlọ ọgwụ

Ndị ọgwụ ọgwụ alogliptin bụ otu ndị ahụ siri ike na ndị ọrịa nwere ụdị ọrịa shuga mellitus 2. Nnukwu bioav adị nke ihe na-arụ ọrụ dị ihe dị ka 100%. Nlekọta nke alogliptin n’otu oge nwere nri nwere abụba na nnukwu oke anaghị emetụta mpaghara n’okpuru oge ịta ahụhụ (AUC), yabụ enwere ike iwere Vipidia n’oge ọ bụla, n’agbanyeghi nri nri.

Otu nchịkwa ọnụ nke alogliptin na dose nke ihe ruru 800 mg site na ndị nwere ahụ ike na-eduga n'ịhapụ ọgwụ ngwa ngwa, ebe a na-enweta ngụkọta oge kachasị mgbe awa 1-2 gachara site n'oge nchịkwa. Mgbe nchịkwa ugboro ugboro, achọpụtaghị nchịkọta alogliptin dị ukwuu na ndị ọrịa nwere ụdị ọrịa shuga nke 2 ma ọ bụ na ndị ọrụ afọ ofufo nwere ahụike.

AUC nke alogliptin gosipụtara ịdabere kpọmkwem na oke ọgwụ ahụ, na-abawanye na otu ọgwụ Vipidia na usoro ọgwụgwọ nke 6.25-100 mg. Ngwakọta dị iche iche nke ihe ngosi ọgwụ a nke dị n'etiti ndị ọrịa pere mpe ma nweekwa nha 17%.

Site na otu ọgwụ AUC (0-inf), alogliptin yiri AUC (0-24) mgbe ọ takingụsịrị otu ụdị otu oge kwa ụbọchị maka ụbọchị 6. Nke a na - egosi enweghị oge ị inụ ọgwụ na ọgwụ ọgwụ mgbe ọgwụ nlekọta ugboro ugboro.

Mgbe otu nchịkwa intravenous nke Vipidia na-arụ ọrụ n'ime ọgwụ nke 12.5 mg na ndị ọrụ afọ ofufo ahụike, olu nkesa n'ime ọnụ okwu bụ 417 l, nke na-egosi ezigbo nkesa nke alogliptin na anụ ahụ. Ogo nke jikọtara na protein plasma bụ ihe dịka 20-30%.

Alogliptin adịghị etinye aka na usoro nke metabolism kpụ ọkụ n'ọnụ, yabụ 60-70% nke ihe dị na ọgwụ a na -ewere emegharị dị na mmamịrị.

Site na ntinye nke 14 C nke akpọrọ alogliptin akara n'ime, emere ka ịdị adị nke metabolites abụọ bụ isi: N-demethylated alogliptin, M-I (ihe na-erughị 1% nke ihe amalite) na N-acetylated alogliptin, M-II (ihe na-erughị 6% nke ihe amalite). M-M bụ metabolite na-arụsi ọrụ ike nke na-egosipụta ihe nhọta a na-ahụkarị nke ọma megide DPP-4, nke yiri ya na arụmọrụ ozugbo na alogliptin. Maka M-II, ihe mgbochi a na-emegide DPP-4 ma ọ bụ enzymes DPP ndị ọzọ abụghị njirimara.

Nnyocha ọmụmụ vitro na-egosi na CYP3A4 na CYP2D6 na-etinye aka na metabolism nke amachi alogliptin. Nsonaazụ ha gosikwara na ihe Vipidia na-arụ ọrụ abụghị ihe na-eweta CYP2B6, CYP2C9, CYP1A2 na onye na-egbochi CYP3A4, CYP1A2, CYP2D6, CYP2B6, CYP2C19, CYP2C8 ma ọ bụ CYP2C9 kpebiri na ngụkọta ahụ na-akwadozi na 25 ahụ na-agbaso uru ahụ. N'okpuru ọnọdụ vitro, alogliptin nwere ike inwetara CYP3A4, mana n'okpuru ọnọdụ vivo, akụrụngwa ndị na-eweta ya adịghị apụta n'ihe gbasara isoenzyme a.

N'ime ahụ mmadụ, alogliptin abụghị ihe na - egbochi ndị na - ebugharị ebugharị ebugharị ebumpụta ụwa nke ụdị nke abụọ na ndị na - ebugharị ebugharị ebugharị ebumpụta ụwa nke ụdị nke mbụ na nke atọ.

Alogliptin dị n'ụdị a (R) -enantiomer (karịa 99%) na obere obere na vivo ma ọ bụ na-etinyeghị aka na usoro mgbanwe mgbanwe nke chiral n'ime (S) -enantiomer. A naghị ekpebi nke ikpeazụ mgbe ị na-ewere Vipidia na usoro ọgwụgwọ.

Site na nchịkwa ọnụ nke 14 C nke alogliptin akara, gosipụtara na 76% nke ọgwụ aepụrụ dị na mmamịrị, yana 13% nwere ọnya. Nkezi mkpochapu mkpo ihe ahụ bụ 170 ml / min ma karịa karịa nhicha nhicha nke glomerular dị ihe dị ka 120 l / min, nke na-enye ohere iwepu mpaghara alogliptin site na mpụta ezumike siri ike. Na nkezi, ọkara ndụ nke ihe ndị na-arụ ọrụ nke Vipidia bụ ihe dị ka awa iri abụọ na abụọ.

N'ime ndị ọrịa na-arịa oke akụrụ na-adịghị ala ala nke ịdị iche iche, emere ihe omumu banyere mmetụta nke alogliptin mgbe ewere ya kwa ụbọchị nke 50 mg. E kee ndị ọrịa esonye n'ọmụmụ ihe ahụ ụzọ anọ dịka usoro Cockcroft - Gault siri dị, dabere na nha nrụrụ akwara na mkpo QC (nkọwapụta nke creatinine), inweta nsonaazụ ndị a:

Otu I (ọdịda obere aha ịgbazi, CC 50-80 ml / min): AUC nke alogliptin mụbara site na 1.7 ugboro ma e jiri ya tụnyere ìgwè ndị na-achịkwa. Agbanyeghị, mmụba a na AUC nọgidere na-anabata ndị na-ahụ maka njikwa,
Otu II (nghapu akuko gbasara ezumike nká, CC 30-50 ml / min): a hụrụ ihe fọrọ nke nta ka ọ bụrụ okpukpu abụọ nke AUC nke alogliptin ma e jiri ya tụnyere ìgwè ndị na-achịkwa,
Otu III na IV (odida renal siri ike, CC erughi 30 ml / min, yana ogwugwu ogwugwu nke akwara itughari ma oburu na odi nkpa, usoro onodu agha): AUC gbagoro ihe ruru ugboro anọ ma e jiri ya na ndi na-ahụ maka ya. Ndị ọrịa nwere nsogbu gbasara akwara dị n'okirikiri sonyere na usoro ọgwụgwọ metụtara akwara ụkwụ ozugbo ha nwetasịrị Vipidia. N’oge ọmụmụ gbasara elekere atọ, a gụpụrụ ihe dị n’ime asaa nke ọgwụ alogliptin n’ahụ.

Maka nke a, na otu m, ọ dịghị mkpa maka ndozi dose. N'ime ndị ọrịa nwere nnukwu akụrụ gbasara akwara, iji mezuo ntinye uche nke ihe na-arụ ọrụ na plasma ọbara, na nso ndị ọrịa nwere ọrụ gbasara akụrụngwa nkịtị, achọrọ ịgbatị Vipidia. Alogaghị Alogliptin maka ọrịa ezughi oke gbasara akụrụ, yana maka ndị ọrịa nwere akwara gbasara njedebe, na-anabataghị usoro akwara.

N'ime ndị ọrịa nwere ọrịa imeju na-agafeghị oke, a na-ebelata AUC na mkpokọta kachasị nke alogliptin ihe dị ka 10% na 8%, n'otu aka ahụ, ma e jiri ya tụnyere ndị ọrịa nwere imeju na-arụkarị ọrụ, mana a dịghị ele ihe omume a anya dị ka ọgwụ. Yabụ, idozigharị ọgwụ maka Vipidia maka obere hepatic insufficiency (5-9 isi dika ọnụego nke Child-Pugh). Enweghị data nyocha na ojiji nke alogliptin na ndị ọrịa nwere oke ịba ọcha n'anya (karịa isi 9).

Ikpa ahu, oria (tinyere ihe di elu - 65–81), agbụrụ na udiri ndi oria enweghi mmetuta ogwu di iche banyere ogwu ogwu, ya dika odighi mkpa idozi uzo. A mụọghị ọgwụ ọgwụ nke alogliptin na ndị ọrịa na-erubeghị afọ 18.

Ihe ngbanwe

ụdị shuga 1
oke mmebi imeju (karịa isi iteghete n'ihe banyere nwatakịrị-Pugh, n'ihi ụkọ data nyocha na arụmọrụ / nchekwa nke iji),
ọrịa mamịrị ketoacidosis,
obi anaghị ala ala (FC NYHA klas III - IV),
nnukwu nsogbu gbasara akwara
afọ ruo afọ 18 (n'ihi ụkọ data gbasara arụmọrụ / nchekwa nke ọgwụ a na ndị ọrịa a),
ime na lactation (n'ihi ụkọ data gbasara arụmọrụ / nchekwa nke iji Vipidia n'ime ndị ọrịa a),
mmadu anabataghi ya na mmiri nke Vipidia, data na-emekwa ihe banyere ezigbo nsogbu hypersensitivity na ihe nnabata ọ bụla nke DPP-4, gụnyere mmeghachi omume anaphylactic, angioedema na ujo anacticlactic.

Ikwu (oria / onodu nke ekwesiri iji mbadamba nkume Vipidia)

Nnukwu akụkọ banyere ọrịa pancreatitis
agafeghị oke gbasara akụrụngwa,
Nchikota ternary na thiazolidinedione na metformin,
jikọtara ya na insulin ma ọ bụ usoro nke sulfonylurea.

Ntụziaka maka iji Vipidia: usoro na usoro onunu ogwu

A na-ewere mbadamba Vipidia n'ọnụ, n'agbanyeghị nri ahụ, loda ya kpamkpam, na-enweghị ịwingụ mmiri na ị drinkingụ mmiri.

Usoro a na-atụ aro kwa ụbọchị bụ 25 mg na 1 dose. A na-ewere ọgwụ ahụ naanị, yana ngwakọta na metformin, thiazolidinedione, ọgwụ sulfonylurea ma ọ bụ insulin, ma ọ bụ dịka ihe mejupụtara atọ na metformin, insulin ma ọ bụ thiazolidinedione.

Ọ bụrụ n’ịfughị ọgwụ ọfụma na mberede, ị ga-ewere ya ngwa ngwa o kwere omume. Were okpukpu abụọ n’otu ụbọchị agaghị ekwe omume.

Mgbe etinyere Vipidia, na mgbakwunye na thiazolidinedione ma ọ bụ metformin, usoro usoro onunu ogwu ha agbanweghi.

Iji belata ohere nke hypoglycemia mgbe ejikọtara ya na ọgwụ mgbakwunye sulfonylurea ma ọ bụ insulin, a na-atụ aro ka belata ọgwụ ha.

Nhọpụta nke ihe atọ mejupụtara na thiazolidinedione na metformin chọrọ ịkpachara anya (ejikọtara ya na ọrịa hypoglycemia, mmezi nke ọgwụ ndị a nwere ike ịchọ).

N'ihe banyere ọdịda akụrụ, a na-atụ aro ka ị tulee ọnọdụ akụrụ arụ arụ tupu a gwọọ ya, ma oge ụfọdụ n’oge ọgwụgwọ. Ọgwụ kwa ụbọchị na ndị ọrịa nwere obere akwara na-agabigaghị ókè (na mwepụ nke creatinine site na ≥ 30 ruo ≤ 50 ml / min) bụ 12.5 mg. Na ogo / oke ọkwa nke ọdịda akụrụngwa, edeghị Vipidia.

Nyocha na Vipidia

Ọtụtụ mgbe, enwere nyocha dị mma banyere Vipidia dị ka ọgwụ na-ebelata shuga ma mee ka ọnụ ọgụgụ ọbara a sie ike. Ndị ọrịa na-akọ na mmetụta nke ọgwụ ahụ na-adịgide maka otu ụbọchị, ebe ọ na-anaghị abawanye agụụ, yana dịka akụkụ nke usoro ọgwụgwọ hypoglycemic, ọ na-enyere aka belata ibu ma kpochapụ mgbu ụkwụ. Ọzọkwa, ndị ọrịa nwere mmasị na iji Vipidia: enwere ike iwe ya n'oge ọ bụla n'ụbọchị.

Agbanyeghị, enwerekwa nyocha na-adịghị mma gbasara arụmọrụ ọgwụ adịghị arụ yana enwere ike ịnabata onye ọ bụla.

Ndị ọkachamara na-adọ aka na ntị megide ojiji Vipidia na-ezighi ezi maka ịta oke.

Ozi izugbe

Ngwá ọrụ a na-ezo aka n'ihe ndị ọhụrụ gbasara ọrịa shuga. O kwesiri ndi mmadu nke nwere oria oria nke oria abuo. Enwere ike iji Vipidia mee ihe naanị ma ya na ọgwụ ndị ọzọ otu a.

Ikwesiri ịghọta na iji ọgwụ a na-achịkwaghị achịkwa nwere ike njọ ọnọdụ nke onye ọrịa, yabụ ị ga-agbaso ndụmọdụ dọkịta. Gaghị eji ọgwụ a na-edeghị akwụkwọ, ọkachasị mgbe ị na-a medicationsụ ọgwụ ndị ọzọ.

Aha ahia maka ogwu a bu Vipidia. Na ọkwa mba ụwa, a na-eji aha Alogliptin mee ihe, nke sitere na akụrụngwa nọ n'ọrụ n'ime ihe mejupụtara ya.

Mbadamba ngwaahịa ndị nwere ụdị oval a na-anọchi anya ya. Ha nwere ike ịdị odo ma ọ bụ acha uhie uhie (ọ dabere na usoro onunu ogwu). Ihe ngwugwu a gụnyere pcs iri abụọ na abụọ. - 2 blister maka mbadamba 14.

Omume ọgwụ

Ngwá ọrụ a sitere na Alogliptin. Nke a bụ otu n'ime ihe ọhụụ eji eme ihe iji chịkwaa ọkwa shuga. Ọ bụ nke ọnụọgụ hypoglycemic, nwere mmetụta siri ike.

Mgbe ị na-eji ya, enwere mmụba na nnabata insulin na-egbochi glucose ma na -ebelata mmepụta glucagon ma ọ bụrụ na-abawanye glucose ọbara.

Site n'ọrịa shuga ụdị 2, tinyere hyperglycemia, ihe ndị a nke Vipidia na-atụnye ụtụ na mgbanwe ndị dị mma dị ka:

mbelata na ego haemoglobin glycated (НbА1С),
belata ogo glucose.

Nke a na - eme ka ngwa ọrụ a dị irè n'ịgwọ ọrịa shuga.

Ihe ngosi na contraindications

Ọgwụ ndị e ji eme ihe siri ike chọrọ ịkpachara anya na-eji ya. Ntụziaka maka ha kwesịrị ịdị nke ọma, ma ọ bụghị n ’uru nke ahụ onye ọrịa ahụ ka ọ ga-emebi. Ya mere, ịnwere ike iji Vipidia naanị na nkwanye nke onye ọkachamara na idebe iwu ahụ.

A na-atụ aro ka eji rụọ ọrụ maka ụdị shuga 2. Ọ na-enye iwu nke usoro glucose na ọnọdụ mgbe anaghị eji usoro ọgwụgwọ nri yana adịghị mkpa mmega ahụ. Jiri ọgwụ ahụ eme ihe n'ụzọ ziri ezi maka monotherapy. A na-ahapụ ya ka ejiri ya na ọgwụ ndị ọzọ na - enyere aka belata ọkwa shuga.

Utionkpachara anya mgbe ị na-eji ọgwụ a na-arịa ọrịa shuga eme ihe site na ọnụnọ nke contraindications. Ọ bụrụ na elebaraghị ha anya, ọgwụgwọ agaghị adị irè ma ọ nwere ike ibute nsogbu.

Anaghị anabata Vipidia n'ọnọdụ ndị a:

onye inyocha ọgwụ ọ bụla,
ụdị shuga 1
oke obi ike
ọrịa imeju
oke mmebi akụrụ
ime na lactation,
mmepe nke ketoacidosis kpatara ọrịa shuga,
Afọ onye ọrịa dị afọ 18.

Ndị a emebi iwu bụ contraindications siri ike maka iji.

E nwekwara steeti ndị edepụtara nke ọma banyere ọgwụ a:

ọria aru
gbasara akụrụngwa nke ogo ogo.

Na mgbakwunye, a ga-elezi anya mgbe ị na-ede Vipidia yana ọgwụ ndị ọzọ iji hazie ọkwa glucose.

Nsonaazụ

Mgbe ị na-a drugụ ọgwụ a, mgbe ụfọdụ mgbaàmà ọjọọ metụtara nsonaazụ nke ọgwụ a:

isi ọwụwa
anụ ahụ na-efe efe na-eku ume
nasopharyngitis,
mgbu afọ
itching
akpụkpọ anụ ahụ,
nnukwu pancreatitis
urticaria
mmepe nke imeju imeju.

Ọ bụrụ na mmetụta ndị ọ na-adịghị na-apụta, kpọọ dọkịta. Ọ bụrụ na ọnụnọ ha adịghị eweta ihe egwu na ahụike onye ọrịa, na ike ha anaghị abawanye, enwere ike ịga n'ihu na ọgwụgwọ Vipidia. Ọnọdụ siri ike nke onye ọrịa chọrọ ịhapụ ọgwụ ozugbo.

Usoro onunu ogwu na nhazi

Emere ọgwụ a maka nchịkwa ọnụ. A na-agbakọ usoro onunu ogwu n'otu n'otu, dabere ogo ọrịa ahụ, afọ onye ọrịa, ọrịa na-agbanwe agbanwe na atụmatụ ndị ọzọ.

Na nkezi, ekwesịrị iwere otu mbadamba ihe nwere 25 mg nke ihe eji arụ ọrụ. Mgbe ị na-eji Vipidia na usoro nke 12.5 mg, ego a na-eme kwa ụbọchị bụ mbadamba 2.

A na-atụ aro ị takeụ ọgwụ ahụ otu ugboro n'ụbọchị. Should shouldụ ọgwụ kwesịrị ị drunkụbiga mmanya ókè n’enyeghị atụ. Ọ bụ ihe amamihe dị na ya ị withụ ha. A na-anabata nnabata ma tupu nri ma mgbe emesiri.

Ejila ogwu okpukpu abuo nke ogwu ma oburu na atufuru otu uzo - nke a nwere ike ibute oria. Ikwesiri ị theụ ọgwụ ọ bụla ị na-eme ya n'ọdịnihu dị nso.

Ntụziaka pụrụ iche na mmekọrịta dị n'etiti ọgwụ

N'iji ọgwụ a, a na-atụ aro ka iburu n'uche ụfọdụ atụmatụ iji zere mmetụta ọjọọ:

N'oge ịmụ nwa, Vipidia bụ contraindicated. Emego nyocha etu esi edozigharị nsogbu nwa a n’ebe nwa ebu n’afọ nọ. Mana ndị dọkịta chọrọ ka ha ghara iji ya mee ihe, ka ha wee kpasuo ime ọpụpụ ma ọ bụ mmepe nke omume nwatakịrị. Otu a na-enye ara.
Ejighị ọgwụ ahụ agwọ ọrịa ụmụaka, ebe ọ bụ na enweghị ezigbo data na nsonaazụ ọ nwere n'ahụ ụmụaka.
Agadi agadi nke ndị ọrịa abụghị ihe kpatara iwepu ọgwụ. Mana iwere Vipidia na nke a choro nlebara anya site n’aka ndi dibia. Ndị ọrịa karịrị afọ 65 nwere ohere dị ukwuu nke ibute ọrịa akụrụ, yabụ achọrọ ịkpachara anya mgbe ị na-ahọrọ ọgwụ.
Maka obere nsogbu gbasara akụrụ, a na-enye ndị ọrịa ọgwụ ọgwụ ruru 12.5 mg kwa ụbọchị.
N'ihi egwu nke ịmalite ọrịa pancreatitis mgbe ị na-eji ọgwụ a, ndị ọrịa kwesịrị ịma ihe ịrịba ama bụ isi nke ọrịa a. Mgbe ha gosipụtara, ọ dị mkpa ịkwụsị ọgwụgwọ na Vipidia.
Theakingụ ọgwụ ahụ adịghị emebi ikike itinye uche. Ya mere, mgbe ị na-eji ya, ịnwere ike ịnya ụgbọ ala ma na-eme ihe ndị chọrọ ntinye. Agbanyeghị, hypoglycemia nwere ike ibute ihe isi ike na mpaghara a, yabụ achọrọ ịkpachara anya.
Ọgwụ nwere ike imetụta ọrụ nke imeju. Yabụ, tupu oge eruo, achọrọ nyocha nke anụ ahụ a.
Ọ bụrụ na akwadoro Vipidia yana ọgwụ ndị ọzọ iji belata ọkwa glucose, a ga-agbanwe usoro ha si arụ ọrụ.
Ọmụmụ ihe banyere mmekọrịta nke ọgwụ na ọgwụ ndị ọzọ egosighi mgbanwe dị ịrịba ama.

Mgbe eburu n'uche atụmatụ ndị a, enwere ike ịme ọgwụgwọ ga-adịwanye mma ma dị mma.

Iji ọgwụ ọjọọ eme ihe

Alogliptin nwere nnabata nhọrọ mgbochi ihe ụfọdụ n'ime enzymes, gụnyere dipeptidyl peptidase-4. Nke a bụ enzyme bụ isi na-abanye na ya homonụ na-agbadata ngwa ngwa n'ụdị polypeptide insulinotropic nwere glucose. Ha nọ na eriri afọ ma n'oge nri na-akpali mmepụta nke insulin na pancreas.

Peptide yiri glucone, na-agbadata ọkwa glucagon ma gbochie imepụta glucose n'imeju. Site na mmụba dị ntakịrị ma ọ bụ dị njọ na ọgwụ ndị dị na ya, isi ihe dị na ọgwụ Vipidia 25, alogliptin na-amalite iwelie mmepụta insulin ma belata glucagon na ịba ụba nke glucose n'ọbara. Ihe ndị a niile na - eduga n'ịbelata oke mmiri haemoglobin n'ime ndị ọrịa na-arịa ụdị ọrịa shuga 2.

Anaghị anabata Vipidia 25 ma ọ bụ mbadamba 12.5 maka ọrịa shuga n'ụlọ ahịa ọgwụ naanị site na ndenye ọgwụ.

Ihe ngosi maka ojiji

E gosipụtara Vipidia 25 maka ọrịa mellitus na njikọ ọgwụ ndị ọzọ nwere insulin. Ọgwụ bụ hypoglycemic ogwu ogwu, egosipụtara maka ọgwụgwọ nke ụdị ọrịa shuga 2 nke ọrịa shuga iji chịkwaa ọkwa glucose na enweghị nri na mmega ahụ.

Mpempe usoro onunu ogwu

12.5 mg na mbadamba 25-fim na-ekpuchi

Otu mbadamba ihe

ihe na-arụ ọrụ: alogliptin benzoate 17 mg (ihe ruru 12.5 mg nke alogliptin) na 34 mg (nke ha na 25 mg nke alogliptin)

Isi: mannitol, microcrystalline cellulose, hydroxypropyl cellulose, ssumum croscarmellose, magnesium stearate

Ngwakọta nke akpụkpọ ahụ ihe nkiri: hypromellose 2910, titanium dioxide (E 171), iron oxide yellow (E 172), iron oxide red (E 172), polyethylene glycol 8000, isi awọ ink F1

Mbadamba ụrọ nke biconvex, nke nwere ihe mkpuchi edo edo, nke akpọrọ “TAK” na “ALG-12.5” n'otu akụkụ nke mbadamba (maka iji dozie 12.5 mg),

Mbadamba ụrọ biconvex, nke gbara agba nwere agba uhie, nke akpọrọ “TAK” na “ALG-25” n'otu akụkụ nke mbadamba (maka ị were 25 mg).

Ngwongwo ogwu

Achọpụtala ọgwụ ọgwụ nke alogliptin na ọmụmụ metụtara ndị ọrụ afọ ofufo nwere ahụike na ndị ọrịa nwere ụdị ọrịa shuga 2. N'ime ndị ọrụ afọ ofufo ahụike, mgbe otu onye na-achịkwa ihe ruru 800 mg nke alogliptin, a na-achọpụta nnabata ọgwụ ngwa ngwa site na itinye ọkwa plasma kachasị nke otu elekere abụọ site na oge nchịkwa (nkezi Tmax). Mgbe ị takingụchara ọgwụ ọgwụ kacha akwadoro (25 mg), ọkara ndụ ikpeazụ (T1 / 2) dịkarịa ala awa iri abụọ na abụọ.

Mgbe nchịkwa ugboro ugboro ruo ihe dịka 400 mg maka ụbọchị 14 n'ime ndị ọrịa nwere ọrịa shuga 2, a hụrụ ntakịrị mkpokọta alogliptin na mmụba na mpaghara ahụ n'okpuru usoro ọgwụ pharmacokinetic (AUC) na mkpokọta plasma kachasị (Cmax) site na 34% na 9%, n'otu n'otu. Site na otutu onlogliptin otu na otutu onyoliptin, AUC na Cmax na-abawanye na mmụba nke ịba ụba site na 25 mg ruo 400 mg. Ọnụọgụ nke mgbanwe nke AUC nke alogliptin dị n'etiti ndị ọrịa dị obere (17%).

Ezigbo bioavailability nke alogliptin bụ ihe dịka 100%. Ebe ọ bụ na mgbe ị na-ewere nri alogliptin na nri nwere nnukwu abụba, enweghị mmetụta ọ bụla na AUC na Cmax ahụ, enwere ike ị drugụ ọgwụ ahụ n'agbanyeghị nri ahụ.

Mgbe otu nchịkwa introvenous nke alogliptin na onwa nke 12.5 mg na ndị ọrụ afọ ofufo ahụike, olu nkesa n'ime usoro ọnụ bụ 417 L, nke na-egosi na alogliptin na-ekesa nke ọma na anụ ahụ.

Nkwukọrịta na protein protein bụ 20%.

Alogliptin agbasaghị metabolism dị ukwuu, n'ihi nke sitere na 60% ruo 71% nke nchịkwa a na-agbanwe agbanwe na mmamịrị ahụ. Mgbe nchịkwa ọnụ nke 14C nke akara alogliptin, akara metabolites abụọ dị obere: N-demethylated alogliptin M-I (˂ erughị 1% nke ihe mbido) na N-acetylated alogliptin M-II (˂ erughị 6% nke ihe amalite). M-I bụ metabolite na-arụsi ọrụ ike ma na-ahọpụta onye na-egbochi DPP-4, nke yiri ya na alogliptin, M-II anaghị egosi ọrụ inhibitory megide DPP-4 ma ọ bụ enzymes DPP ndị ọzọ. Nnyocha ọmụmụ in vitro kpughere na CYP2D6 na CYP3A4 na-atụnye ụtụ metabolism nke alogliptin. Alogliptin dị ọkachasị n'ụdị enantiomer (R) karịa (99%) ma na-enwetakwa mgbanwe nke chiral n'ime eneriomer (S) na obere obere na vivo. Achọpụtaghị (S) -enantiomer mgbe ị na-alogliptin na usoro ọgwụgwọ (25 mg).

Mgbe ị mechara 14C akara alogliptin, 76% nke ngụkọta redioaktivu bụ akụrụ na 13% n'ime eriri afọ, na-erute 89%

ọgwụ a na-ahụ maka redioaktivu. Mkpochapu nzipu nke alogliptin (9.6 L / h) na-egosi itinye ahihia nzuzo akwara. Nyefee usoro bụ 14.0 l / h.

Pharmacokinetics na otu ndị ọrịa ọrịa pụrụ iche: arụ ọrụ ezughi ezu

AUC nke alogliptin dị n'ime ndị ọrịa nwere ọrụ mgbazinye nsogbu nke ịdị nro (60 (creatinine nwechapụ (CrCl)

Nsonaazụ

Ebe ọ bụ na a na-eme ọnwụnwa ụlọ ọgwụ n'okpuru ọnọdụ dị iche iche, ọ gaghị ekwe omume ịtụle ugboro ole nke mmeghachi omume ọjọọ ndị a na-ahụ na ọnwụnwa ụlọ ọgwụ nke ọgwụ a na-ahụ na ugboro ole a na-ahụ na ọnwụnwa nke ọgwụ ndị ọzọ, na ụdị ugboro ole a nwere ike ọ bụghị mgbe niile na-egosipụta ọnọdụ nke iji ọgwụ ahụ eme ihe na omume.

Na nchịkọta nyocha nke ule 14 nke ụlọ ọgwụ na-achịkwa, ihe dị oke njọ na ihe ọjọọ bụ 73% na ndị ọrịa na-anata alogliptin 25 mg, 75% na placebo otu, na 70% n'ime otu ahụ na ọgwụ ọzọ atụnyere. Na mkpokọta, ọnụego nkwụghachi n'ihi mmeghachi omume ọjọọ bụ 6.8% na 25 mg alogliptin 25, 8.4% nọ na placebo otu, ma ọ bụ 6.2% n'ime otu ahụ nwere ụzọ ọzọ ha si eme ntụnyere.

Enweela akụkọ banyere mmeghachi omume ọjọọ karịa 4% na ndị ọrịa natara alogliptin: nasopharyngitis, isi ọwụwa, ọrịa akụkụ okuku ume na elu.

A kọwara mmeghachi omume ọjọọ ndị a na ngalaba Ntuziaka Pụrụ Iche:

- Mmetụta imeju

A kọwo na ọrịa hypoglycemia dabere na ụkpụrụ glucose ọbara na / ma ọ bụ akara akara na akara nke hypoglycemia. N'ime ọmụmụ monotherapy, a chọpụtara ihe kpatara hypoglycemia na 1.5% na 1.6% nke ndị ọrịa na alogliptin na otu placebo, otu isi. Ojiji nke alogliptin dị ka njikọ na ọgwụgwọ nke glyburide ma ọ bụ insulin adịghị eme ka enwewanye hypoglycemia ma e jiri ya tụnyere placebo. N'ime ọmụmụ monotherapy na-atụnyere alogliptin na sulfonylureas na ndị ọrịa meworo agadi, nnabata nke hypoglycemia bụ 5.4% na 26% na alogliptin na glipizide.

Achọpụtara mmeghachi omume ọjọọ ndị a n'oge ịre ahịa nke alogliptin - hypersensitivity (anaphylaxis, edere Quincke, ọnya ọnya, urticaria), mmeghachi omume anụ ahụ (gụnyere ọrịa Stevens-Johnson syndrome), enzymes imeju dị elu, imeju na-agwụ ike, na-agwụ ike ma na-eme ka ọrịa arthralgia na ọrịa n’akwara mgbu, afọ ọsịsa, afọ ntachi, ọgbụgbọ, na mgbochi afọ.

Ebe ọ bụ na a kọrọ mmeghachi omume ọjọọ ndị a na afọ ofufo na ọnụọgụ edoghị anya, ọ gaghị ekwe omume ịgụta ugboro ole a, yabụ na-agụpụta ugboro ole a ka amabeghị.

Mkparịta ụka ọgwụ ọjọọ

Vipidium bụ nke akụrụ ga-apụrịrị ma sistem enzyme cytochrome (CYP) P450 bụ obere metabolized. N'oge nyocha, mba

Mkparịta ụka dị mkpa yana ndị na-egbochi ma ọ bụ ndị na-egbochi cytochrome ma ọ bụ ọgwụ ndị ọzọ ewepụrụ site na akụrụ.

Na ntule mmekọrịta nyocha ọgwụ ọgwụ vitro

Nnyocha ọmụmụ in vitro na-atụ aro na alogliptin anaghị ebute CYP1A2, CYP2B6, CYP2C9, CYP2C19 na CYP3A4, anaghịkwa egbochi CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP3A6 na CGP dị mkpa.

Na ntule mmekọrịta mkparịta ụka nke vivo

Mmetụta nke alogliptin na ọgwụ ndị ọzọ

N'ime ule nke ụlọ ọgwụ, ekpughere nsonaazụ nke alogliptin na ọgwụ ọgwụ ọgwụ nke ọgwụ CenP isoenzymes ma ọ bụ na-agbanweghị agbanwe. Dabere na nsonaazụ nke ọmụmụ ọgwụ pharmacookinetic kọwara, ọ dịghị atụ aro ndozi nke Vipidia ™.

Mmetụta ọgwụ ndị ọzọ dị na pharmacokinetics nke alogliptin Enweghị mgbanwe pụtara ìhè na ụlọ ọgwụ ahụ mgbe a na-eji usoro alogliptin na metformin, cimetidine gemfibrozil (CYP2C8 / 9), pioglitazone (CYP2C8), fluconazole (CYP2C9PCCCPCCCCCCCCPCCPCCPCCCPCCCCCCCCCCPCCCPCCPCCCPCCCPCCCPPCCCPCCCPCCCCPCCCCPCCCCPCCCCPCCCPCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCC digoxin.

Dodoụbiga ya ókè

Ogwu kachasị nke alogliptin na ule nke ụlọ ọgwụ bụ 800 mg otu oge na ndị ọrụ afọ ofufo mara mma yana 400 mg otu ugboro kwa ụbọchị maka ndị ọrịa nwere ụdị ọrịa shuga 2, nke bụ 32 na 16 ugboro karịa ogo ọgwụgwọ a tụrụ aro 25 mg. Onweghi mmeghachi omume ojoo siri ike na usoro onyonyo ndị a.

N'ihe banyere oke Vipidia do, ọ ga-adị mma ka iwepu ihe a na-ejighị n'aka na eriri afọ ma nye nlekọta ahụike dị mkpa, yana usoro ọgwụgwọ Symptomatic. Mgbe awa 3 nke hemodialysis, ihe dịka 7% nke alogliptin nwere ike wepu ya. N'ihi ya, ọ ga-ekwe omume ịba ọcha n'anya ma ọ bụrụ na ị doụbiga ya ókè bụ eleghi anya. Onweghi data banyere mkpochapu nke alogliptin site na nyocha obitoneal.

Njirimara ngwa

A naghị eji Vipidia agwọ ọrịa shuga n'etiti ụmụaka na ndị na-eto eto. Ntuziaka maka iji ya enweghị ozi gbasara ịme ule ụlọ ọgwụ na ụdị ndị ọrịa. N'ọnọdụ ndị dị otú a, ndị dọkịta na-eji analogues.

Maka ọgwụgwọ nke ụdị ndị ọrịa agadi, ọgwụ ọgwụ ka edepụtara nke ọma. Maka ọgwụgwọ nke ndị agadi, a na-eji ngụkọta ụbọchị kwa ụbọchị, nke na-adịghị mkpa idozigharị. Ọ bụ ezie na ịchefula na alogliptin, nke abanyela n'ahụ ahụ, nwere ike imetụta arụmọrụ nke imeju na akụrụ.

Mmekọrịta na ọgwụ ndị ọzọ

Site na usoro ọgwụgwọ na Vipidia na ọgwụ mgbochi ọrịa shuga ndị ọzọ, ọ dị mkpa ịkọwa usoro ziri ezi ma dozie usoro iji gbochie mmalite nke hypoglycemia.

Mmụta emere egosighi mgbanwe ọ bụla na ngwakọta nke alogliptin na ọgwụ ndị ọzọ nke ọgwụ shuga.

Mmetụta siri ike nke ọgwụ na ahụ ya bụ ihe ama ama, nke gbochiri ị beụ ihe ọ alcoụ alcoụ na-aba n'anya. Amachibidoro iji ọgwụ eme ihe n'oge oge ịmị nwa na inye nwa ya nsonaazụ ọjọọ. Nnyocha e mere egosiwo na ọgwụ ahụ anaghị akpata ụra ma ọ bụ ndọpụ uche, enweghị ike ịmetụta ịmụrụ anya, ma akwadoro ka ndị ọkwọ ụgbọala jiri ya.

Anyị na-enye ndị na-agụ saịtị anyị ego nlele

Nkwadebe nke mmemme yiri ya

Ọ bụ ezie na enweghị ọgwụ ọ bụla nke nwere otu ihe mejupụtara na nsonaazụ ya. Ma enwere ọgwụ ogwu ndi yiri ya na ọnụahịa, mana esitere na ngwa ndị ọzọ na - arụ ọrụ nke nwere ike ịrụ ọrụ dị ka analogues nke Vipidia.

Ndị a gụnyere:

Januvia. A na-atụ aro ọgwụ a iji belata shuga ọbara. Ngwakọta dị n'ọrụ bụ sitagliptin. Edere ya na otu okwu ahụ dị ka Vipidia.
Galvus. Ọgwụ a sitere na Vildagliptin. Akụ a bụ analog nke Alogliptin ma nwee otu ihe.
Janumet. Nke a bụ usọbọ jikọtara ya na mmetụta hypoglycemic. Ihe ndị bụ isi bụ Metformin na Sitagliptin.

Ndị na-ahụ maka ọgwụ na-enwe ike ịnye ọgwụ ndị ọzọ iji dochie Vipidia. Ya mere, ọ dịghị mkpa zoo dọkịta site na mgbanwe ọjọọ na ahụ metụtara ya.

Ntụziaka pụrụ iche na mmekọrịta

Ọgwụ Vipidia anaghị emetụta ọrụ metụtara itinye uche uche na-abawanye, ebe ị na-anabata ụgbọ ala n'oge ọgwụgwọ. Iji ọgwụ ndị ọzọ hypoglycemic emee ihe Nke dibia bekee lebara anya, ebe ọ nwere ike ịdị mkpa ịgbanwe nhazi usoro ọgwụgwọ ma belata usoro onunu ogwu. Ejikọtara nke a na ihe nwere ike ibute ọrịa hypoglycemic.

Tupu i detuo ndị ọrịa nwere nnukwu nsogbu gbasara akụrụ, ha na-eme nnyocha ndị ọzọ iji chọpụta mmeghachi omume nke ahụ ọrịa nwere ị takingụ ọgwụ.

Ọ bụrụ na siri ike arụ ọrụ akụrụ a akagbuo ọgwụ, a na-enyekwa ọgwụ analogues iwu. Site na usoro oria di nwayọ, a na-agbadata usoro ịba ahụ ruo 12.5 mg. Ngwakọta bụ isi na - arụ ọrụ, alogliptin nwere ike ịkpasu nnukwu ọrịa ụjọ, nke a na-elebara anya na ọrịa nke eriri afọ.

Ihe nrịba ama ga - egosi n ’ọnya afọ nwere radieshọn n’azụ.

Site na mgbaàmà ndị yiri ya, a na-akagbu ọgwụ ahụ.Ogologo oge iji Vipidia gwọọ ọrịa nwere ike ibute arụ ọrụ akụrụ, mana idozigharị usoro onunuche ya na nzaghachi anụ ahụ nkịtị maka ọgwụgwọ.