1. Usoro nke Action
Glucagon-dị ka peptide-1 (GLP-1)bụ iheincretin hormonezoro ezo site na eriri afọ L-cell na nzaghachi nri oriri. Ndị na-anabata GLP-1 (GLP-1 RAs) na-eṅomi mmetụta physiological nke hormone a site na ọtụtụ ụzọ metabolic:
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Mgbochi agụụ na igbu oge igbu oge
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Mee ihe na ụlọ ọrụ satiety hypothalamic (karịsịa POMC/CART neurons), na-ebelata agụụ.
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Ngwa ngwa imeju afọ, na-agbatị mmetụta nke afọ ojuju.
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Mwepụta insulin na-abawanye na mwepu Glucagon belatara
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Na-akpali sel β-pancreatic iji mepụta insulin n'ụzọ dabere na glucose.
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Na-ebelata ihe nzuzo nke glucagon, na-emeziwanye ọkwa glucose n'ebu ọnụ na postprandial.
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Metabolism ike emelitere
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Mee ka mmetụta insulin dịkwuo elu ma kwalite oxidation abụba.
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Belata njikọ abụba imeju ma melite metabolism lipid.
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2. Igodo GLP-1–Ndị na-ahụ maka mbelata ibu dabere
| Ọgwụ ọjọọ | Isi Ngosipụta | nchịkwa | Nkezi Mbelata ịdị arọ |
|---|---|---|---|
| Liraglutide | Ụdị ọrịa shuga 2, oke ibu | Ịgba ọgwụ kwa ụbọchị | 5-8% |
| Semaglutide | Ụdị ọrịa shuga 2, oke ibu | Ịgba ọgwụ kwa izu / ọnụ | 10-15% |
| Tirzepatide | Ụdị ọrịa shuga 2, oke ibu | Ịgba ọgwụ kwa izu | 15-22% |
| Retatrutide (n'ọnwụnwa) | Oke ibu (anaghị arịa ọrịa shuga) | Ịgba ọgwụ kwa izu | Ruo 24% |
Usoro:Evolushọn ọgwụ na-aga n'ihu site na otu GLP-1 agonists nnabata → abụọ GIP/GLP-1 agonists → atọ agonists (GIP/GLP-1/GCGR).
3. Nnukwu ọnwụnwa na nsonaazụ ụlọ ọgwụ
Semaglutide – Nnwale nzọụkwụ
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Nzọụkwụ 1 (NEJM, 2021)
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Ndị sonyere: Ndị okenye nwere oke ibu, enweghị ọrịa shuga
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Usoro onunu ogwu: 2.4 mg kwa izu (subcutaneous)
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Nsonaazụ: Mbelata arọ ahụ pụtara14.9%na izu 68 vs. 2.4% nwere placebo
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~ 33% nke ndị sonyere nwetara ≥20% ọnwụ ọnwụ.
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Nzọụkwụ 5 (2022)
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Egosipụtara mbelata ịdị arọ na-adịgide karịa afọ 2 yana nkwalite n'ihe egwu cardiometabolic.
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Tirzepatide – Mmemme SURMOUNT & SURPASS
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SURMOUNT-1 (NEJM, 2022)
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Ndị sonyere: Ndị okenye nwere oke ibu, enweghị ọrịa shuga
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Usoro: 5 mg, 10 mg, 15 mg kwa izu
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Nsonaazụ: pụtara ọnwụ ọnwụ nke15-21%mgbe izu 72 gachara (dose-dabere)
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Ihe fọrọ nke nta ka ọ bụrụ 40% nwetara ≥25% mbelata ịdị arọ.
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Ọnwụnwa SURPASS (ọnụọgụ ndị ọrịa shuga)
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Mbelata HbA1c: ruo2.2%
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Nkezi arọ ọnwụ nke10-15%.
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4. Ahụike agbakwunyere na uru metabolic
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Mbelata naọbara mgbali elu, LDL-cholesterol, natriglycerides
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Mbelatavisceralnaabụba imeju(mmelite na NAFLD)
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Obere ihe ize ndụ nkeihe omume obi(dịka ọmụmaatụ, MI, ọrịa strok)
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Ọganihu na-egbu oge site na prediabetes gaa na ụdị ọrịa shuga 2
5. Profaịlụ nchekwa na echiche
Mmetụta ndị a na-ahụkarị (na-adịkarị nwayọọ ma na-agafeghị oke):
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Ọgbụgbọ, vomiting, afọ ntachi, afọ ntachi
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Enweghị agụụ
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Ahụhụ eriri afọ na-agafe agafe
Ịdọ aka ná ntị / contraindications:
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Akụkọ banyere ọrịa pancreatitis ma ọ bụ medullary thyroid carcinoma
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Ime na inye nwa ara
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Titration nke nwayo nke nta nke nta ka akwadoro iji kwalite nnabata
6. Ntuziaka nyocha n'ọdịnihu
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Ọtụtụ agonists nke ọgbọ na-abịa:
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Ndị agonists atọ na-elekwasị anya GIP/GLP-1/GCGR (dịka ọmụmaatụ,Retatrutide)
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Usoro GLP-1 nke ọnụ:
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Semaglutide ọnụ nwere oke dose (ihe ruru 50 mg) n'okpuru nyocha
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Usoro ọgwụgwọ ngwakọta:
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GLP-1 + insulin ma ọ bụ SGLT2 inhibitors
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Ihe ngosi metabolic sara mbara:
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Ọrịa imeju abụba na-adịghị egbu egbu (NAFLD), polycystic ovary syndrome (PCOS), apnea ụra, mgbochi obi.
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7. Nkwubi okwu
Ọgwụ dabere na GLP-1 na-anọchite anya mgbanwe mgbanwe site na njikwa ọrịa shuga gaa na njikwa metabolic na oke ibu.
Na ndị nnọchi anya dị kaSemaglutidenaTirzepatide, Mbelata arọ na-abụghị nke ịwa ahụ karịrị 20% aghọwo ihe a pụrụ imezu.
A na-atụ anya na ndị agonists ọtụtụ ndị na-anabata ihe n'ọdịnihu ga-emekwuwanye arụmọrụ, ịdịte aka na uru cardiometabolic.
Oge nzipu: Ọktoba 11-2025