Shaanxi BLOOM Tech Co., Ltd. yog ib tug ntawm cov uas paub txog manufacturers thiab lwm tus neeg ntawm terlipressin acetate txhaj nyob rau hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo terlipressin acetate txhaj rau muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Terlipressin acetate txhaj tshuajyog ib qho hluavtaws lysine vasopressin analogue thiab ntev - ua haujlwm xaiv vasopressin V1 receptor agonist. Nws kuj tseem ua haujlwm tseem ceeb hauv chaw kho mob vasoconstrictive polypeptide ua haujlwm ntawm cov hlab ntsha splanchnic. Piv nrog cov neeg vasopressin, nws cov qauv molecular tau ua kom zoo dua los ntawm kev sib ntxiv ntawm triglycine sab saw ntawm cysteine residue ntawm peptide qaum. Qhov kev hloov kho no ua rau txhim kho metabolic stability thiab receptor selectivity, ua rau lub sijhawm ntev ntawm kev ua, thiab txo qis qhov tshwm sim ntawm qhov tsis zoo tshwm sim.
Tom qab nkag mus rau tib neeg lub cev, terlipressin acetate maj mam cleaved los ntawm endogenous esterases mus txuas ntxiv tso tawm nquag lysine vasopressin. Nws yog lub hom phiaj ntawm V1a receptors ntawm vascular du nqaij ntawm splanchnic thiab portal venous systems thiab exerts potent thiab sustained vasoconstriction. Nws ua rau muaj kev sib raug zoo tsawg heev rau lub raum V2 receptors, yog li ua kom tsis txhob muaj cov tshuaj tiv thaiv diuretic - cuam tshuam txog kev phiv.
Peb cov khoom tsim
Terlipressin / Terlipressin Acetate COA
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| Certificate of Analysis | ||
| Compound npe | Terlipressin / Terlipressin Acetate hmoov | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 14636-12-5 | |
| Ntau | 80g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202601090056 | |
| MFG | Peb 9, 2026 | |
| EXP | Peb 8, 2029 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.54% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.42% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.98% |
| Ib qho impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 95 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500ppm ua |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree | |
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| Tshuaj Formula: | C52H74N16O15S2 |
| Exact Mass: | 1226 |
| Molecular Luj: | 1227 |
| m/z: | 1226 (100.0%), 1227 (56.2%), 1229 (15.5%), 1228 (9.0%), 1227 (5.9%), 1229 (5.1%), 1228 (3.3%), 1229 (3.1%), 1230 (2.8%), 1230 (1.7%), 1227 (1.6%), 1230 (1.4%) |
| Elemental Analysis: | C, 50.89; H, 6.08; N, 18.26; O, 19.55; S, 5.22 |
Clinical indications
Daim ntawv thov ntawm terlipressin hauv kev txhim kho lub plawv ua haujlwm yog qhov dav thiab ua haujlwm.Terlipressin acetate txhaj tshuajTxoj kev kho mob tsis yog tsuas yog nthuav tawm cov kev hloov pauv hloov pauv ntawm cov kab mob plawv thiab mob ntev, tab sis tseem cuam tshuam nrog cov txheej txheem pathological ntawm cov kab mob organic thiab kev ua haujlwm tsis zoo. Los ntawm ntau- phiaj xwm kev cuam tshuam, tag nrho lub voj voog thiab ntau- theem kev kho mob suav nrog kev tiv thaiv, kho, thiab kho kom rov zoo.
1. Muaj kev cuam tshuam rau lub plawv tsis ua hauj lwm
(1) Kev kho mob sai ntawm mob plawv tsis ua hauj lwm (ADHF)
Hauv kev tswj hwm thaum muaj xwm txheej ceev ntawm ADHF, nws yog cov tshuaj vasoactive tiam tshiab, xaiv cov kab mob visceral vascular txaj (xws li tus po, ob lub raum, thiab cov hlab ntsha hauv plab) kom rov faib cov ntshav mus rau cov hauv nruab nrog cev. Nws lub sijhawm pib tsuas yog 5-10 feeb, nrawm dua li cov tshuaj diuretics (furosemide siv sijhawm 30-60 feeb), tshwj xeeb tshaj yog rau cov neeg mob ADHF uas muaj kev sib txuam nrog hypotension (systolic ntshav siab.<90mmHg).
Ib qho kev sim ntau qhov kev sib tw nrog 200 tus neeg mob tau pom tias pab pawg kho mob nrog terlipressin (0.5-1.0 μ g / min txuas ntxiv cov tshuaj intravenous infusion) ua ke nrog cov tshuaj dopamine qis (3-5 μ g / kg / min) muaj 40% luv dua lub sij hawm txhim kho hauv kev ua pa nyuaj (piv txwv li kev kho mob ib leeg) (B. lub sij hawm 2.1 teev vs 3.5 teev), thiab txo 35% hauv 72 teev nyeem ntawv tus nqi (12% vs 18.5%). Mechanistically, los ntawm kev nce peripheral vascular resistance (SVR), lub plawv tom qab tau nce, thaum venous constriction txhim kho cov ntshav rov qab los, ua rau "siab ntim" dual tswj cov nyhuv, sai sai tshem tawm pulmonary congestion (PCWP txo ntawm 25% -30%) thiab cov ntaub so ntswg hypoperfusion ( zis ntim nce 40.5%) -
(2) Hemodynamic reconstruction ntawm cardiogenic poob siab
Rau cov neeg mob nrog cardiogenic poob siab (CS), ruaj khov hemodynamic kev txhawb nqa tuaj yeem ua tiav los ntawm kev ncua ntev ntawm vasoconstriction (ib nrab-lub neej 6-8 teev, tsis tu ncua ntau dua norepinephrine 2-4 teev). Nws mechanism ntawm kev txiav txim muaj xws li:
Kev tswj xyuas qhov tseeb ntawm qhov siab ntawm lub siab (MAP): Hauv kev kho mob septic shock ua ke nrog lub plawv tsis ua haujlwm, MAP tuaj yeem khaws cia nyob rau hauv qhov zoo tshaj plaws ntawm 65-75mm Hg, thaum tsis txhob cuam tshuam tachycardia tshwm sim los ntawm norepinephrine (lub plawv dhia nce.<10 beats/minute).
Cardiac function optimization: By maintaining coronary artery perfusion pressure (CPP>60mmHg), qhov kev pheej hmoo ntawm myocardial ischemia yog txo, thiab lub plawv Performance index (CI) yog khaws cia ntawm 2.5-3.0L / (min · m ²), thaum lub oxygen xa index (DO ₂ I) yog nce 20% -25% (los ntawm 550mL / (min · m²) / 8 · 8 (m²) min.
Kev tiv thaiv microcirculation: Tsiaj thwm sim tau pom tias nws tuaj yeem ua rau cov hnyuv mucosal cov ntshav ntws los ntawm 25% -30%, txo cov qib lactate (los ntawm 4.2mmol / L txog 2.8mmol / L), thiab txhim kho cov nqaij mos oxygenation.
2. Kev kho mob hloov kho rau lub plawv tsis ua hauj lwm
(1) Lub sij hawm ntev tswj lub plawv tsis ua hauj lwm nrog txo ejection feem (HFrEF)
Hauv chav kawm ntev ntawm HFrEF, qhov thim rov qab ntawm ventricular remodeling yog ua tiav los ntawm inhibiting neuroendocrine overactivation (xws li txo cov ntshav plasma angiotensin II los ntawm 30% -40%) thiab ncaj qha los tiv thaiv fibrotic teebmeem:
Kev txhim kho tus qauv: Txo qis ventricular mass index (LVMI) los ntawm 0.5-1.0g / m ² ib xyoos twg thiab txo qis ventricular end diastolic txoj kab uas hla (LVEDD) los ntawm 3% -5%.
Kev txhim kho kev ua haujlwm: Ib 12-hloov kev tshawb nrhiav pom tau tias hauv pab pawg tau txaisKev txhaj tshuaj terlipressin acetate(0.5mg subcutaneous txhaj, 3 zaug ib lub lim tiam) ua ke nrog cov qauv kev kho mob (ACEI / ARB + beta blocker + aldosterone antagonist), LVEF nce 5% -7% (los ntawm 32% mus rau 38%) piv rau cov hauv paus, thiab N-terminal B-type natriuretic peptide 4% (NT - NT - 4% NP) 2500pg / mL txog 1500pg / mL).
Prognostic optimization: Tag nrho - ua rau cov neeg tuag tau txo qis 18% (HR=0.82, 95% CI 0.71-0.95), thiab qhov kev nyeem ntawv tau txo qis los ntawm 22% (RR=0.78, 95% CI 0.69-0.89).
(2) Kev tswj ntawm diastolic muaj nuj nqi hauv plawv tsis ua hauj lwm nrog khaws cia ejection feem (HFpEF)
Txhawm rau hais txog qhov tseem ceeb ntawm diastolic tsis ua haujlwm hauv cov neeg mob HFpEF, cov txheej txheem hauv qab no tau siv los txhim kho ventricular ua raws:
Kev ua kom zoo siab gradient: txo qis sab laug ventricular kawg diastolic siab (LVEDP) los ntawm 15% -20% (los ntawm 22mmHg mus rau 18mmHg), thiab txo qis kev ua pa nyuaj los ntawm kev siab ntsws ntsws.
Kev txhim kho hauv kev ua haujlwm siab: Ua kom lub diastolic tshaj tawm (e ') ntawm mitral annulus los ntawm 10% -15% (ntawm 7cm / s txog 8cm / s), txo qhov E / e piv los ntawm 20% -25% (ntawm 15 txog 11), qhia txog kev txhim kho ntawm sab laug ventricular filling siab.
Kev tswj hwm kev sib koom tes ntawm comorbidities: Hauv cov neeg mob HFpEF nrog kev kub siab sib xyaw, kev sib xyaw ua ke ntawm calcium channel blockers (xws li amlodipine) tuaj yeem nce 6-feeb taug kev deb ntawm 50 meters (los ntawm 320m mus rau 370m) thiab txhim kho cov qhab nia ntawm lub neej zoo (MLHFQ) los ntawm 20%.
3. Perioperative cardiac function tiv thaiv thaum phais plawv
(1) Kev Tiv Thaiv Mob Ntshav Qab Zib Tsawg (POCS) tom qab Extracorporeal Circulation
Tom qab kev phais mob plawv xws li coronary artery bypass grafting (CABG), qhov kev pheej hmoo ntawm POCS tuaj yeem raug txo los ntawm cov hauv qab no:
Coronary artery perfusion maintenance: Ensure CPP>60mmHg kom txo tau cov xwm txheej myocardial ischemic (txo qhov tshwm sim ntawm ST ntu nce ntawm electrocardiogram ntawm 12% mus rau 4%).
Kev txo cov tshuaj vasoactive: Txo cov tshuaj norepinephrine los ntawm 40% -50% (los ntawm 0.2 μ g / kg / min mus rau 0.1 μ g / kg / min) kom tsis txhob muaj lub raum hypoperfusion los ntawm vasoconstriction ntau dhau.
Kev txhim kho cov txiaj ntsig kev kho mob: Kev tshawb fawb txog 150 CABG cov neeg mob tau pom tias qhov tshwm sim ntawm POCS hauv pab pawg siv tshuaj tiv thaiv tau txo qis los ntawm 40% (8% vs 13%) piv rau pawg tswj hwm, thiab lub sijhawm pw hauv tsev kho mob tau luv los ntawm 2-3 hnub (nruab nrab 7 hnub vs 10 hnub).
(2) Kev tswj kev ua haujlwm ntawm lub plawv rov qab thiab tsis lees txais tom qab hloov lub plawv
Tom qab hloov lub plawv, txhawb lub plawv ua haujlwm rov qab los ntawm ob lub tshuab:
Kev tiv thaiv lub plawv pub dawb: txo cov mob khaub thuas ischemia-kev raug mob rov ua dua, nce LVEF los ntawm 10% -15% (los ntawm 45% mus rau 55%) hauv lub sijhawm ua haujlwm thaum ntxov, thiab txo cov troponin I (cTnI) tso tawm los ntawm 50% -60% (ntawm 5.2ng / mL txog 2.1ng / m).
Kev tiv thaiv kab mob sib koom ua ke: Hauv kev tsis lees paub kev kho mob, kev sib xyaw ntawm cov tshuaj tiv thaiv kab mob (xws li tacrolimus + mycophenolate mofetil) tuaj yeem txo qhov kev pheej hmoo ntawm lub plawv ua haujlwm tsis zoo los ntawm 30% -40% (ua tiav los ntawm kev txo qis TNF - thiab IL-6 qib), yam tsis muaj qhov tshwm sim ntawm kev kis kab mob.
Indirect Potential Anti-Inflammatory Mechanisms
Cov tshuaj tiv thaiv -inflammatory nyhuv ntawmKev txhaj tshuaj terlipressin acetatetsis ua tiav los ntawm kev ncaj ncees lub hom phiaj ntawm inflammatory yam. Hloov chaw, nws thaiv qhov kev nthuav dav ntawm cov kab mob inflammatory thiab suppresses hauv zos thiab cov kab mob inflammatory raug mob los ntawm ntau txoj hauv kev tsis ncaj ncees, suav nrog kev hloov pauv ntawm hemodynamic homeostasis, lub cev tiv thaiv kab mob polarization, kev saib xyuas lub plab zom mov tsis zoo, thiab kev tswj hwm ntawm cov teeb meem tseem ceeb. Qhov no tau dhau los ua ib qho ntawm kev txiav- ntug kev tshawb fawb pem hauv ntej ntawm cov tshuaj pharmacology nyob rau hauv xyoo tas los no, thiab nws cov txheej txheem tau raug lees paub nyob rau hauv ntau yam kev raug mob hauv nruab nrog cev qauv. Ua ntej, cov tshuaj indirectly alleviates ischemic inflammatory raug mob nyob rau hauv cov ntaub so ntswg los ntawm regulating splanchnic hemodynamic homeostasis.
Nyob rau hauv cov kab mob pathological xws li mob siab cirrhosis, mesenteric ischemia thiab sepsis, splanchnic vasodilation tseem ceeb tshwm sim thiab tsis muaj txiaj ntsig zoo ntawm cov ntim ntim, ua rau cov ntaub so ntswg tsis txaus, ischemia thiab hypoxia.
Cov kev hloov no txuas ntxiv ua rau oxidative kev nyuaj siab thiab inflammatory kab mob thiab ua rau loj tso tawm ntawm pro-inflammatory yam xws li qog necrosis factor- (TNF- ), interleukin-1 (IL-1) thiab interleukin-6 (IL-6), tsim ib lub voj voog vicious ntawm ischemia thiab inflammatory puas.By selectively activately receptors. constricts dilated mesenteric thiab portal hlab ntsha, kho splanchnic hyperdynamic ncig, restores lub cev perfusion siab thiab ameliorates cov ntaub so ntswg ischemia thiab hypoxia.
Nws txo cov ischemia- pib inflammatory signaling ntawm qhov chaw, indirects inhibits qhov pib ua rau inflammatory teb thiab txo cov basal cov ntaub so ntswg o. Ntau qhov kev sim tsiaj tau lees paub tias cov tshuaj tuaj yeem ua rau nce siab hauv cov hlab ntsha hauv cov nas qauv ntawm mesenteric ischemia, txhim kho txoj hnyuv thiab lub raum perfusion, txo cov ischemia-induced inflammatory infiltration, thiab txo cov kab mob hauv nruab nrog cev.
Thib ob, kev hloov pauv ntawm macrophage polarization los tiv thaiv pro- cov lus teb tiv thaiv kab mob ua rau nws cov ntsiab lus tsis ncaj qha los tiv thaiv - inflammatory mechanism.
Qhov tsis txaus ntseeg M1/M2 macrophage polarization yog ib qho tseem ceeb ntawm kev mob tsis tu ncua.Classically activated M1 macrophages dominate pro-inflammatory reactions thiab secrete abundant pro-inflammatory mediators to aggravate tissue damage, whereas the other activated M2 macrophages exert anti-cov ntaub so ntswg thiab cov ntaub so ntswg functions.Txiav-ntev hauv vitro cellular kev soj ntsuam thiab hauv vivo tsiaj kev tshawb fawb pom tau tias terlipressin acetate ua rau PI3K/Akt signaling txoj hauv kev rau tshwj xeeb inhibit lipopolysaccharide-induced M1 macrophage polarization.
Nws txo qis kev tswj hwm mRNA thiab cov protein qhia ntawm M1 cov cim suav nrog iNOS thiab IL-1 thiab txo qis kev tso tawm ntawm TNF-, IL-6 thiab lwm yam pro-inflammatory cytokines, tsis cuam tshuam nrog basal M2 polarization.
Yog li ntawd, nws muaj txiaj ntsig zoo rov ua kom lub cev tsis muaj zog polarization.Piv nrog cov pa vasopressor norepinephrine, terlipressin acetate nthuav tawm cov txiaj ntsig zoo hauv immunomodulation.
Thaum txhawb nqa hemodynamic stability, nws tshwj xeeb thaiv kev tiv thaiv kab mob -kev kho mob inflammatory amplification thiab mitigates systemic inflammatory teb syndrome. Cov txheej txheem no muab cov pov thawj tshiab rau kev kho mob ntxiv ntawm sepsis thiab ischemia- raug mob reperfusion.
Tsis tas li ntawd, nws kho cov kab mob hauv plab hnyuv thiab inhibits cov kab mob translocation rau indirect tiv thaiv inflammatory activation nyob rau hauv lub distal kab mob.Kev cuam tshuam ntawm plab hnyuv barrier thiab dysbiosis-induced translocation ntawm cov kab mob thiab endotoxins yog ib qho tseem ceeb ua rau lub cev o thiab ntau yam kab mob.
Cov kev tshawb fawb tshaj tawm tshiab tshaj tawm qhia tias terlipressin acetate upregulates kev qhia ntawm VE-cadherin thiab PV-1 nyob rau hauv plab hnyuv vascular endothelial hlwb, restores plab hnyuv endothelial integrity, txo txoj hnyuv permeability, thiab txwv translocation ntawm plab hnyuv kab mob thiab endotoxins. Yog li ntawd, nws cuam tshuam endotoxin- ua rau muaj kev ua haujlwm ntawm TLR4/NF-κB inflammatory pathway thiab tiv thaiv kev puas tsuaj rau cov kab mob hauv nruab nrab xws li daim siab, ob lub raum thiab lub ntsws.Qhov kev tsis ncaj ncees no qhia meej txog cov khoom nruab nrog - tiv thaiv cov nyhuv ntawm cov tshuaj uas ua rau cov kab mob loj heev nkag mus rau hauv lub cev. system, thiab zoo heev nthuav cov kev tshawb fawb ntawm nws cov kev siv tshuaj tiv thaiv.
Terlipressin acetate yog qhov ntev - ua yeeb yam polypeptide tsim los kov yeej cov kev txwv kev kho mob ntawm cov neeg vasopressin.
Nyob rau xyoo 1950, ib txwm muaj vasopressin twb tau siv rau kev kho mob hemostasis thiab ntshav siab. Txawm li cas los xij, nws luv luv ib nrab- lub neej, tsis zoo receptor selectivity, nquag phiv thiab tsis ruaj khov ua tau zoo heev txwv kev siv tshuaj kho mob.
Tawm tsam keeb kwm yav dhau los no, pab pawg tshawb fawb European tau ua qhov kev hloov pauv ntawm vasopressin molecular qauv hauv xyoo 1970s. Kev taw qhia ntawm glycine side chains optimized peptide sequence, zoo heev txhim kho V1 receptor selectivity thiab txo qis kev cuam tshuam rau V2 receptors. Cov tshuaj antidiuretic tsis zoo cuam tshuam nrog cov neeg ua haujlwm ib txwm raug zam kom zoo, thiab cov tshuaj terlipressin tau tsim.
Nyob rau hauv 1980, formulation optimization ntawmKev txhaj tshuaj terlipressin acetateua tiav. Nws nyob rau hauv -vivo sustained- tso tawm profile enabled ntev - cov tshuaj pharmacological kav ntev, thiab cov khoom tau txais kev pom zoo kev lag luam hauv Tebchaws Europe nyob rau nruab nrab -1980s raws li kev kho thawj kab rau variceal los ntshav ntawm txoj hlab pas thiab plab hnyuv.
Tom qab xyoo 2000, nws cov nqi kho mob hauv hepatorenal syndrome tau txheeb xyuas, thiab cov lus qhia cuam tshuam tau pom zoo.
Xyoo 2022, US FDA tau pom zoo terlipressin acetate rau mob raum raug mob txuam nrog hepatorenal syndrome, ua rau nws yog thawj hom tshuaj rau qhov kev qhia no. Nyob rau hauv xyoo tas los no, cov kev tshawb fawb pib tshiab tau nthuav tawm nws cov peev xwm tiv thaiv - mob thiab tiv thaiv -fibrotic cov dej num, muab kev txhawb nqa tseem ceeb rau kev tshawb nrhiav cov lus qhia tshiab thiab kev siv tshuaj kho mob ntawm tus neeg sawv cev.
FAQ
Terlipressin acetate siv rau dab tsi?
Kev piav qhia. Kev txhaj tshuaj Terlipressin yog sivtxhawm rau txhim kho lub raum ua haujlwm hauv cov neeg mob hepatorenal syndrome (qhov teeb meem rau lub raum uas tshwm sim hauv cov neeg mob uas muaj kab mob siab heev) nrog rau kev hloov pauv sai ntawm lub raum.. Cov tshuaj no tsuas yog muab los ntawm lossis nyob rau hauv kev saib xyuas tam sim ntawm koj tus kws kho mob.
Thaum twg tsis muab terlipressin?
Terlipressin yuav tsum tau zamnyob rau hauv cov neeg mob uas muaj kab mob siab heev txhais tau tias mob siab - ntawm- Chronic Liver Failure (ACLF) qib 3 thiab/los yog Tus Qauv rau Kev Xaus - Kab Mob Siab (MELD) tau qhab nia Ntau dua lossis sib npaug rau 39, thaum kho nrog terlipressin rau hom 1 hepatorenal syndrome, tshwj tsis yog tias cov txiaj ntsig raug txiav txim siab tshaj qhov txaus ntshai.
Dab tsi yog qhov txaus ntshai ntawm terlipressin?
Terlipressin tuaj yeem ua rau mob ua pa tsis ua haujlwm loj lossis tuag taus rau cov neeg mob uas muaj hom 1 hepatorenal syndrome (hom 1 HRS) ntawm qhov zaus siab dua li yav dhau los paub. TerlipressinTej zaum yuav ua rau muaj kev pheej hmoo ntawm sepsis / septic shock rau cov neeg mob hom 1 HRS.
Cim npe nrov: terlipressin acetate txhaj, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom