1. Nzira Yekuita
Glucagon-like peptide-1 (GLP-1)iri anincretin hormoneyakavanzwa ne intestinal L-masero mukupindura kudya kwekudya. GLP-1 receptor agonists (GLP-1 RAs) inotevedzera iyi hormone physiological mhedzisiro kuburikidza akati wandei metabolic nzira:
-
Kudzvinyirirwa Kwekudya uye Kunonoka Kubvisa Gastric
-
Ita pane hypothalamic satiety centers (kunyanya POMC / CART neurons), kuderedza nzara.
-
Kuslow gastric emptying, kuwedzera kunzwa kwekuzara.
-
-
Yakawedzera Insulin Secretion uye Yakaderedzwa Glucagon Kuburitswa
-
Kurudzira pancreatic β-masero kuti abudise insulin nenzira inoenderana neglucose.
-
Dzvinyirira glucagon secretion, uchivandudza kutsanya uye postprandial glucose mazinga.
-
-
Kuvandudzwa Kwesimba Metabolism
-
Wedzera insulin senitivity uye kukurudzira mafuta oxidation.
-
Deredza hepatic mafuta synthesis uye kuvandudza lipid metabolism.
-
2. Key GLP-1-Yakavakirwa Weight Loss Agents
| Zvinodhaka | Main Chiratidzo | Administration | Avhareji Yehuremu |
|---|---|---|---|
| Liraglutide | Type 2 chirwere cheshuga, kufutisa | Zuva nezuva jekiseni | 5–8% |
| Semaglutide | Type 2 chirwere cheshuga, kufutisa | Weekly jekiseni / nemuromo | 10–15% |
| Tirzepatide | Type 2 chirwere cheshuga, kufutisa | Majekiseni evhiki nevhiki | 15–22% |
| Retatrutide (mumiyedzo) | Kufutisa (kwete-diabetic) | Majekiseni evhiki nevhiki | Kusvika ku24% |
Trend:Kushanduka kwezvinodhaka kuri kufambira mberi kubva kune imwechete GLP-1 receptor agonists → mbiri GIP/GLP-1 agonists → katatu agonists (GIP/GLP-1/GCGR).
3. Makiriniki Makuru Miedzo uye Migumisiro
Semaglutide - STEP Miedzo
-
STEP 1 (NEJM, 2021)
-
Vatori vechikamu: Vakuru vane kufutisa, vasina chirwere cheshuga
-
Dose: 2.4 mg vhiki nevhiki (subcutaneous)
-
Results: Kureruka kwehuremu hwemuviri we14.9%pamavhiki e68 vs. 2.4% ne placebo
-
~ 33% yevatori vechikamu vakawana ≥20% kurasikirwa.
-
-
STEP 5 (2022)
-
Yakaratidza kurasika kwakaramba kurema pamusoro pemakore maviri uye kuvandudzwa mune cardiometabolic njodzi zvinhu.
-
Tirzepatide - SURMOUNT & SURPASS Zvirongwa
-
SURMOUNT-1 (NEJM, 2022)
-
Vatori vechikamu: Vakuru vane kufutisa, vasina chirwere cheshuga
-
Dose: 5 mg, 10 mg, 15 mg vhiki nevhiki
-
Results: Kurevesa uremu hwe15–21%mushure memavhiki makumi manomwe nemaviri (zvinoenderana nedose)
-
Vanoda kusvika 40% vakawana ≥25% kuderedza uremu.
-
-
SURPASS Miedzo (Chirwere cheshuga)
-
HbA1c kuderedza: kusvika2.2%
-
Concurrent average weight loss of10–15%.
-
4. Hutano Hwekuwedzera uye Metabolic Benefits
-
Kuderedzwa mukatiBP, LDL-cholesterol,uyetriglycerides
-
Yakaderedzwavisceraluyehepatic mafuta(kuvandudzwa muNAFLD)
-
Ngozi yakaderera yezviitiko zvemoyo(semuenzaniso, MI, sitiroko)
-
Kunonoka kufambira mberi kubva kuprediabetes kuenda kune Type 2 chirwere cheshuga
5. Kuchengetedza Profile uye Kufunga
Zvinowanzoitika (kazhinji zvinyoro kusvika pakati nepakati):
-
Nausea, kurutsa, bloating, constipation
-
Havi yekudya
-
Kusagadzikana kwegastrointestinal kwenguva pfupi
Yambiro / contraindications:
-
Nhoroondo yepancreatitis kana medullary thyroid carcinoma
-
Kubata pamuviri nekuyamwisa
-
Zvishoma nezvishoma dose titration inokurudzirwa kuvandudza tolerability
6. Remangwana Rekutsvaga Mazano
-
Next-chizvarwa akawanda-agonists:
-
Triple agonist yakananga GIP/GLP-1/GCGR (semuenzaniso,Retatrutide)
-
-
Oral GLP-1 magadzirirwo:
-
High-dose oral semaglutide (kusvika ku50 mg) pasi pekuongororwa
-
-
Combination therapies:
-
GLP-1 + insulin kana SGLT2 inhibitors
-
-
Yakawedzera metabolic zviratidzo:
-
Isiri-doro fatty chiropa chirwere (NAFLD), polycystic ovary syndrome (PCOS), kufema kwehope, kudzivirira kwemwoyo.
-
7. Mhedziso
GLP-1-yakavakirwa mishonga inomiririra shanduko kubva pakudzora chirwere cheshuga kuenda kune yakazara metabolic uye huremu manejimendi.
Nevamiririri vakaitaSemaglutideuyeTirzepatide, kwete-kuvhiya uremu huremu hunodarika 20% hwave huchikwanisika.
Remangwana akawanda-receptor agonist anotarisirwa kuwedzera kusimudzira kushanda, kusimba, uye cardiometabolic mabhenefiti.
Nguva yekutumira: Oct-11-2025