Na pathogenesis nke ụdị shuga 2, usoro atọ bụ ọdịiche:
- Nri insulin na-eguzogide;
- Ọdachi na mmepụta insulin nke endogenous;
- Nnukwu mkpụkọ glucose site na umeji.
Ibu ọrụ maka mmepe ụdị ọrịa a siri ike dabere na mkpụrụ ndụ b na c nke pancreas. Nke ikpeazụ a na - emepụtakwa homonụ nke na - akpali ntụgharị nke glucose na ume maka akwara na ụbụrụ. Ọ bụrụ na ọnụego nrụpụta ya na-adalata, nke a na-akpalite hyperglycemia.
Mkpụrụ ndụ B-dịịrị maka ịmịpụta glucagon, ngafe ya na - emepụta ihe achọrọ maka oke oke glucose site na imeju. Glucagon ngafe na enweghị insulin na-enye ọnọdụ maka ịba uru glucose na-enweghị ike n'ọbara.
Njikwa dị mma nke ụdị ọrịa shuga 2 agaghị ekwe omume na-enweghị nkwụsi ike na ogologo oge (maka oge ọrịa niile) na-achịkwa metabolism nke carbohydrate. Ọtụtụ ule mba dị iche iche na-akwado na naanị ụgwọ shuga na-enye ọnọdụ maka igbochi nsogbu ma mee ka ndụ onye ọrịa mamịrị na-atụ anya ndụ.
N'agbanyeghị ụdị ọgwụ dịgasị iche iche nke antidiabetic, ọ bụghị ndị ọrịa niile na-ejikwa ike ha. Dabere na nchọpụta UKPDS nwere ikike, 45% nke ndị ọrịa mamịrị natara nkwụghachi 100% maka mgbochi microangiopathy mgbe afọ 3 gasịrị, naanị 30% mgbe afọ 6 gasịrị.
Ihe isi ike ndị a na-ekwupụta mkpa ọ dị ịmalite usoro ọgwụ ọhụụ na - eme ọhụụ nke na - agaghị enyere aka iwepụ nsogbu metabolic, kama ọ na - enwekwa ọria, na - akpali usoro ahụ iji mezie insulin na glycemia.
Medicationsdị ọgwụ dị n'ụdị nke nwere ike ịchịkwa ụdị ọrịa shuga 2 na-enweghị mkpali nke pancreas, mgbanwe mberede na glycemia, ihe ize ndụ nke hypoglycemia bụ ihe ọhụrụ kachasị ọhụrụ site n'aka ndị ahịa ọgwụ.
GLP-4 enzyme inhibitor Sitagliptin na-enyere onye na-arịa ọrịa shuga aka ịchịkwa agụụ na ibu nke anụ ahụ, na-enye anụ ahụ ikike iji aka ya merie nsogbu nke glucose na-egbu egbu.
Mwepụta wepụtara ya na ihe mejupụtara
A na-emepụta ọgwụ ahụ na sitagliptin na aha ahịa Janavia n'ụdị mbadamba okirikiri nwere pink ma ọ bụ beige akara ma akara “227” kwa 100 mg, “112” kwa 50 mg, “221” kwa 25 mg. Mbadamba mbadamba ihe ahụ na igbe plastik ma ọ bụ pensụl. Enwere ike inwe ọtụtụ efere n’ime igbe.
A na - agbakwụnye ihe ndị dị mkpa sitagliptin phosphate hydrate site na sodium croscarmellose, magnesium sterate, cellulose, sodium stearyl fumarate, hydrogen phosphate a na-akọwaghị.
Maka sildagliptin, ọnụahịa ahụ na-adabere na nkwakọ ngwaahịa, ọkachasị maka mbadamba 28 ịchọrọ ịkwụ 1,596-1724 rubles. A na-enye ọgwụ ọgwụ, ndụ nchekwa ahụ bụ 1 afọ. Ogwu a choghi onodu puru iche maka ichekwa ya. A na-echekwa nkwakọ ngwaahịa emepe n'ọnụ ụzọ friji maka otu ọnwa.
Ngwọta Sitagliptinum ọgwụ
A na-emepụta homonụ ndị a site na mucosa eriri afọ, imepụta ihe dị na ya na-abawanye site na iri nri. Ọ bụrụ na ọkwa glucose dị mma ma dị elu, homonụ na-abawanye ruo 80% nke mmepụta insulin na nzuzo ya site na mkpụrụ ndụ β-mkpụrụ ndụ n’ihi usoro ihe mgbaàmà na mkpụrụ ndụ. GLP-1 na - egbochi mkpụrụ ndụ glucagon hormone nke ukwuu site na mkpụrụ ndụ b.
Mbelata mgbanye glucagon megide mmalite nke mmụba nke insulin ana achi achi belata mmịkọ glucose na umeji. Usoro ndị a ma hụ na nhazi nke glycemia. Egosiputara ihe ụfọdụ n’ọkpụkpụ ọrụ, ọkachasị ya na hypoglycemia, ha anaghị emetụta njikọ nke glucagon na insulin.
N'iji DPP-4, a na-ejikọ mmiri ọgwụ ndị ahụ dị na ya iji mepụta metabolites metabolites. Na-egbochi ọrụ nke enzyme a, sitagliptin na-abawanye ọdịnaya nke incretins na insulin, na-ebelata mmepụta glucagon.
Site na hyperglycemia, otu n'ime ihe ịrịba ama nke ụdị ọrịa shuga 2, usoro a na-enyere aka belata Hemoglobin glycated, shuga agụụ na glucose mgbe eburu oke ibu. Otu ọgwụ sitagliptin na-enwe ike igbochi arụmọrụ nke DPP-4 maka otu ụbọchị, na-abawanye mgbasa nke ọgwụ ndị nwere ọbara n'ọbara ugboro abụọ.
Pharmacokinetics nke sitagliptin
Ntinye ọgwụ a na - eme ngwa ngwa, ebe enwere bioav adị 87%. Ọnụ a na-enweta maka nri anaghị adabere n'oge nri na nhazi nke nri, ọkachasị, nri ndị nwere abụba anaghị agbanwe ọgwụ ọgwụ nke ọgwụ incretin mimetic.
Na mmezu, ojiji ọzọ nke mbadamba 100 mg na-abawanye mpaghara n'okpuru usoro ntụpọ nke AUC, nke na-akọwapụta ịdabere na oke nkesa n'oge, site na 14%. Otu ngaji mbadamba 100 mg na-emesi oke ike nke 198 l.
A na-ahụzi akụkụ nke obere ihe dị na mbụ. Achọpụtara 6 metabolites na enweghi ike inhibido DPP-4. Mkpochapu ntaramahụhụ (QC) - 350 ml / min. Akụkụ akụrụngwa ọgwụ ahụ na-ewepụ akụrụ (79% n'ụdị na-agbanweghi na 13% n'ụdị metabolites), eriri afọ na-ewepụ ihe ndị ọzọ.
N'iburu ibu dị arọ akụrụ na ndị ọrịa mamịrị nwere ọrịa na-adịghị ala ala (CC - 50-80 ml / min.), Ihe ndị na-egosi ya yikwara, ya na CC 30-50 ml / min. ọnụnọ AUC na-agbagha ugboro abụọ, yana CC n'okpuru 30 ml / min. - ugboro anọ. Ọnọdụ ndị dị otú a na-atụ aro iri titration.
Site na ọrịa ịba ọcha n'anya nke ịdaba oke, Cmax na AUC mụbara site na 13% na 21%. N’ụdị siri ike, ọgwụ ọgwụ sitagliptin anaghị agbanwe agbanwe nke ukwuu, ebe ọ bụ n’eriri akụrụ ọgwụ n’uche.
Onye gosiputara incretinomimetic
Edere ọgwụ a maka ọrịa shuga 2dị nke Abụọ na mgbakwunye na nri nri nwere obere carb yana ọrụ ahụ ike zuru oke.
A na-eji ya dị ka otu ọgwụ na ọgwụ agwakọta na metformin, nkwadebe sulfonylurea ma ọ bụ thiazolidinediones. Ọ ga - ekwe omume iji usoro ntụtụ insulin ma ọ bụrụ na nhọrọ a na - enyere aka idozi nsogbu nke nguzogide insulin.
Contraindications maka sitagliptin
Edekwala ọgwụ:
N’ime oke uche nke mmadụ;- Ndị ọrịa mamịrị nwere oria 1;
- Ime na inye nwa ara;
- Na ọnọdụ ketoacidosis nke ọrịa mamịrị;
- Maka ụmụaka.
N’ime oke uche nke mmadụ;Ndị ọrịa mamịrị nwere ụdị ọrịa akwara gbasara akwara chọrọ nlebara anya pụrụ iche.
Etu ị ga-esi
Maka sitagliptin, ntuziaka maka iji ya akwado ị drinkingụ ọgwụ tupu nri. Standardtọ usoro ọgwụgwọ bụ otu maka usoro ọgwụgwọ ọ bụla - 100 mg / ụbọchị. Ọ bụrụ na usoro ịgba akwụkwọ agbajiri agbaji, pill a ga-a beụ mmanya n'oge ọ bụla, ịnakwere ịnwe okpukpu abụọ ahụ anabataghị.
Ihe Omume Ọjọọ
Na-ekpe ikpe site na nyocha, ọtụtụ ndị ọrịa mamịrị na-enwe nchegbu banyere dyspepsia, stool iwe. N'ime nyocha ụlọ nyocha, hyperuricemia, mbelata arụmọrụ nke gland thyroid, na leukocytosis.
N'ime mmetụta ndị ọzọ a na-atụghị anya ya (njikọta na incretin mimetic ka egosighi) - ọrịa na-efe efe, arthralgia, migraine, nasopharyngitis). Ọnọdụ nke hypoglycemia yiri nke a rụpụtara na ìgwè nchịkwa placebo.
Nyere aka ịdoụbiga mmanya ókè
N'ihe banyere ịdoụbiga ihe ókè, a na-ewepụ oke ọgwụ a na-akabeghị aka na eriri afọ, a na-enyocha usoro niile dị mkpa (gụnyere ECG). E gosipụtara usoro Symptomatic na nkwado, gụnyere hemodialysis na ike ogologo oge (a na-ewepụ ihe 13.5 nke ọgwụ ahụ na awa 3-4).
Nsonaazụ Njikọ Ọgwụ
Site na iji sitagliptin na-eme n'otu oge na metformin, rosiglitazone, ọgwụ mgbochi, glibenclamide, warfarin, simvastatin, ọgwụ ọgwụ nke otu ọgwụ a anaghị agbanwe agbanwe.
Nlekọta oge nke sitagliptin nwere digoxin anaghị egosuta mgbanwe n’usoro ogwu. A na-enye ndụmọdụ ndị yiri ya site na ntụziaka na na mmekọrịta nke sitagliptin na cyclosporin, ketoconazole.
Sildagliptin - analogues
Sitagliptin bu aha obodo ahu ogwu ahu; aha ahia ya bu Januvius. Enwere ike ịtụle analoget ọgwụ jikọtara ọnụ, nke gụnyere sitagliptin na metformin. Galvus bụ otu nke DPP-4 inhibitors (Novartis Pharma AG, Switzerland) yana akụkụ vildagliptin nọ n'ọrụ, ọnụahịa 800 rubles.
Ọgwụ hypoglycemic dịkwa mma maka koodu ATX nke ọkwa 4:
- Nesina (Takeda Pharmaceuticals, USA, sitere na alogliptin);
- Onglisa (ristlọ ọrụ Bristol-Myers Squibb, dabere na saxagliptin, ọnụahịa - 1800 rubles);
- Trazhenta (ristlọ ọrụ Bristol-Myers Squibb, Italy, Britain, nwere ihe dị na linagliptin na-arụ ọrụ), ọnụahịa - 1700 rubles.
Agaghị etinye ọgwụ ndị a dị egwu na listi ọgwụ a na-ahọrọ; ọ bara uru ịnwale onwe gị n'ihe ize ndụ ma tinye ego gị na ahụike gị n'ihe egwu gị?
Sitagliptin - nyocha
Na-ekpe ikpe site na akụkọ banyere nzukọ mkparịta ụka, Januvius na-edenyekarị ndị ọrịa mamịrị n'isi mmalite nke ọrịa ahụ. Banyere sitagliptin, nyocha nke ndị dọkịta na ndị ọrịa na-egosi na ojiji nke incretinomimetic nwere ọtụtụ nuances.
Januvia bu ogwu ohuru ohuru ma obughi ndi dibia nile ahu enwetarala ahuko nke oma site na iji ya. Ruo n'oge na-adịbeghị anya, metformin bụ ọgwụ mbụ; ugbu a, a na-ahọkwa Januvia ka monotherapy. Ọ bụrụ na ike ya ezuola, ịgbakwunye ya na metformin na ọgwụ ndị ọzọ agaghị abụ ihe amamihe dị na ya.
Ndị ọrịa mamịrị na-eme mkpesa na ọgwụ anaghị egboro ihe ndị akọwapụtara mgbe niile, ka oge na-aga ịdị irè ya na-ebelata. Nsogbu dị ebe a abụghị iji ọgwụ eme ihe, kama na njirimara nke ọrịa ahụ: ụdị shuga 2 bụ ọrịa na-adịghị ala ala, na-aga n'ihu.
Nkwupụta niile na-eduga ná nkwubi okwu na iwebata usoro nke sitagliptin, nke bụ klas nke ọgwụ ọhụrụ, na-enye ohere zuru oke maka njikwa ụdị ọrịa shuga 2 na ọkwa ọ bụla, site na ọrịa shuga na usoro ọgwụgwọ ọzọ, yana nsonaazụ na-enweghị afọ ojuju site na itinye usoro atụmatụ ụgwọ glycemic ọdịnala.
Nkwupụta sitere n’aka Prọfesọ A.S. Ametov, endocrinologist-diabetologist banyere edemede na omume nke sitagliptin - na vidiyo.
