Disease relevance of gabexate

• Sixteen patients in the placebo group and five in the gabexate group had acute pancreatitis (8 percent vs. 2 percent, P=0.03) [1].
• Twelve patients in the gabexate group and 29 in the placebo group had abdominal pain (6 percent vs. 14 percent, P=0.009) [1].
• One patient in the gabexate group died, from a myocardial infarction [1].
• Increases in amylase and activated trypsin in ascites were markedly reduced by lavage and even more so by lavage with addition of gabexate [2].
• Gabexate as a therapy for disseminated intravascular coagulation [3].

High impact information on gabexate

• METHODS: We conducted a multicenter, double-blind comparison of gabexate (1 g given by intravenous infusion starting 30 to 90 minutes before endoscopy and continuing for 12 hours afterward) with placebo (mannitol and sodium chloride, administered in the same fashion) [1].
• Injection of nontoxic doses of CCK-8 before proglumide or gabexate injections completely abolished all beneficial effects and also increased the severity of pancreatitis due to CDE diet alone [4].
• Lavage without gabexate had a greater effect on survival, serum amylase, and histology [2].
• In clinical trials, both gabexate and somatostatin appear equally effective in reducing the incidence of pancreatitis by two-thirds compared with controls [5].
• Each drug tested was administered i.a. Graded doses of gabexate (1-10 mg) elicited dose-dependent biphasic responses for the secretory rates, bicarbonate concentrations and outputs of pancreatic juice, with maximum effects at approximately 5 mg, but had little effect on the protein concentrations [6].

Chemical compound and disease context of gabexate

• Injections of gabexate and proglumide from initiation of CDE diet (before induction of pancreatitis) increased survival from 37% (diet alone) to 85 and 75%, respectively, and also ameliorated histological alterations and increases in serum amylase concentration and pancreatic activated trypsin [4].
• CR 1409, a glutaramic acid derivative with competitive cholecystokinin-antagonistic activity, was administered IP and evaluated in comparison with proglumide (the model CCK-receptor antagonist), gabexate (protease inhibitor) and PGE2 (cytoprotective) on two different models of experimental pancreatitis [7].
• CONCLUSION: The administration of low- and high-dose ulinastatin has similar effects to high-dose gabexate in the prevention of post-ERCP pancreatitis [8].
• While octreotide was confirmed to be ineffective, somatostatin and gabexate seem to be the best for the prevention of post-ERCP pancreatitis, but both can present some limits such as unreported sample size calculation in the statistical analysis for somatostatin studies and lack of widespread commercial availability for gabexate [9].

Biological context of gabexate

• Nafamostat was more efficient than gabexate or gelatin on wound healing [10].
• CONCLUSIONS: In patients of severe acute pancreatitis with organ dysfunction and receiving gabexate treatment, neutrophil apoptosis is associated with the severity of organ dysfunction [11].

Anatomical context of gabexate

• In dogs gabexate inhibits sphincter of Oddi motility but no data are available in humans [12].
• Effects of gabexate, a protease inhibitor, on smooth muscle of guinea-pig stomach fundus [13].

Associations of gabexate with other chemical compounds

• Several drugs are discussed in this review, but only somatostatin and gabexate (gabexate mesilate) have consistently shown a moderate beneficial effect [5].

Gene context of gabexate

• Improvement in wound healing by epidermal growth factor (EGF) ointment. I. Effect of nafamostat, gabexate, or gelatin on stabilization and efficacy of EGF [10].

Analytical, diagnostic and therapeutic context of gabexate

• Gabexate, a protease inhibitor, has been used to prevent pancreatic damage related to ERCP [1].
• Peritoneal lavage with gabexate showed the greatest benefit of the various regimens for acute severe pancreatitis and is worthy of clinical trials [2].
• To the UTI group, 10,000 units/kg of UTI was administrated during reperfusion, and to the GM group, 20 mg/kg of gabexate mecilate was administrated similarly [14].
• All subjects enrolled were first treated with a 500-mg continuous intravenous infusion of gabexate, starting 30 min before the endoscopic maneuvers and continuing up to 6.5 h after it [15].
• The meta-analysis of trials of short-term infusion of gabexate or somatostatin did not show efficacy for either drug [16].

References