ime izdelka:Vapreotid,oktastatin,Vapreotid
Zaporedje: D-Phe-[Cys-Tyr-D-Trp-Lys-Val-Cys]-Trp-NH2
vzdevek:Sanvar,RC-160;VAPREOTID;D-PHE-CYS-TYR-D-TRP-LYS-VAL-CYS-TRP-NH2; oktastatin;
FCYWKVCW-NH2;D-Phe-L-Cys(1)-L-Tyr-D-Trp-L-Lys-L-Val-L-Cys(1)-L-Trp-NH2;
Cas Št.: 103222-11-3
Molekularna formula: C57H70N12O9S2
Molekularna teža: 1131.40
Čistost (HPLC): 98.0%
Videz: Bel prah
Ena nečistoča(HPLC): 1.0%
Aminokislinska sestava: 10% teoretičnega
Vsebnost peptidov(N%): 80%(avtor %N)
Vsebnost vode(Karl Fischer): 6.0%
Vsebnost acetata(HPIC): 15.0%
Masno ravnotežje: 95.0~105,0 %
Ocena : Farmacevtski razred
Shranjevanje: Zaprto, spodaj 2 ~ 8℃ ohranjanje
Uporaba : Zdravilo se lahko uporablja za zdravljenje zgodnje akutne krvavitve iz krčnih žil požiralnika (EVB) in endoskopsko intervencijsko terapijo pred hemostazo, lahko pride tudi do notranje krvavitve 5 d leča za zdravljenje in preprečevanje ponovitve po endoskopiji. Vapreotid acetat bo edino odobreno zdravilo za krvavitev iz krčnih žil požiralnika v Združenih državah.
Variceal bleeding is a life-threatening complication of portal hypertension. The recommended treatment includes the early administration of a vasoactive drug. Vapreotide is a somatostatin analogue with a different receptor affinity to octreotide. It decreases portal pressure and blood flow of collateral circulation in rats with cirrhosis. The pivotal study of early administration of vapreotide in patients with cirrhosis and variceal bleeding has shown a significant improvement in bleeding control and, in the subset of patients with significant bleeding, a significant reduction in mortality. In addition, a meta-analysis of four randomized studies has shown a significant improvement in bleeding control. Vapreotide administrated via the intravenous route is simple to use, with practically no contraindications and few, usually minor, side effects.
The immediate release formulation of Sanvar, a somatostatin analogue, is used in the treatment of acute esophageal variceal bleeding (EVB).Sanvar is used prior to endoscopic intervention to control haemorrhage and prevent re-bleeding during the critical five days following the onset of bleeding. EVB is a life threatening condition and the mortality rate is high (about 15% do 25%) in the first six weeks following the haemorrhage. EVB is the cause of about 70% of gastro-intestinal bleeding in patients suffering from liver cirrhosis.