Prowse C V, Douglas J G, Forrest J A, Forsling M L
Eur J Clin Invest. 1980 Feb;10(1):49-54. doi: 10.1111/j.1365-2362.1980.tb00009.x.
Eight patients with cirrhosis were infused with lysine vasopressin (10 microgram LVP) and triglyclylysine vasopressin (750 microgram and 2000 microgram Glypressin, GVP) on separate occasions. LVP infusion resulted in an increase in factor VIII, factor VIII-related antigen and plasminogen activator (PA). The factor VIII antigen: activity ratio decreased following infusion, but factor VIII electrophoretic mobility and in vitro decay rate were unchanged. GVP infusion produced no change in factor VIII or PA. Assay of vasopressin-like antigen and antidiuretic activity showed that GVP is cleaved to LVP in vivo. The low levels of LVP formed by this reaction might explain the prolonged vasometer effects of GVP, as well as its inability to cause release of factor VIII or PA. Compared to LVP, GVP has a longer pressor effect in vivo, has no effect on fibronolysis and exhibits no cardiotoxic effects and may therefore be the treatment of choice in bleeding oesophageal varices.
八名肝硬化患者分别接受了赖氨酸加压素(10微克LVP)和三甘氨酰赖氨酸加压素(750微克和2000微克甘氨加压素,GVP)的输注。输注LVP导致因子VIII、因子VIII相关抗原和纤溶酶原激活物(PA)增加。输注后因子VIII抗原:活性比值降低,但因子VIII电泳迁移率和体外衰变率未改变。输注GVP后因子VIII或PA无变化。对加压素样抗原和抗利尿活性的测定表明,GVP在体内被裂解为LVP。该反应形成的低水平LVP可能解释了GVP的血管收缩作用持续时间延长,以及其无法引起因子VIII或PA释放的原因。与LVP相比,GVP在体内具有更长的升压作用,对纤维蛋白溶解无影响,且无心脏毒性作用,因此可能是治疗食管静脉曲张出血的首选药物。