Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.4.21.1 (chymotrypsin)
 10,938 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The new long-acting somatostatin analogue octreotide (SMS 201-995) was investigated for its influence on secretagogue-stimulated human exocrine pancreatic secretion. Eighteen healthy volunteers participated in the study. During duodenal intubation with a background stimulation of either secretin 1 U.kg/h or secretin 1 U.kg/h + ceruletide, 120 ng.kg/h, octreotide was infused at doses of 5, 20 and 80 micrograms/h in a placebo-controlled randomized double-blind crossover trial. Duodenal juice samples were collected in 10-min intervals, and amylase, trypsin, chymotrypsin, and bicarbonate were measured in the individual fractions. During secretin stimulation, amylase was inhibited between 41 and 59%, trypsin between 28 and 72%, chymotrypsin between 55 and 70%, and bicarbonate between 0 and 31% with 5, 20 and 80 micrograms/h octreotide. During secretin and ceruletide stimulation, amylase was significantly inhibited by 84%, 78%, 81%, trypsin by 76%, 55%, 52%, chymotrypsin by 77%, 55%, 60%, and bicarbonate by 25%, 11%, 19% with 5, 20, and 80 micrograms/h octreotide, respectively (all decreases P less than 0.05). The long-acting somatostatin analogue octreotide was confirmed to be a potent inhibitor of stimulated human exocrine pancreatic secretion. The near maximal inhibitory potency of octreotide was achieved at a dose of only 5 micrograms/h. This finding may be of value in the planning of therapeutic studies with octreotide.
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PMID:Inhibition of human exocrine pancreatic secretion by the long-acting somatostatin analogue octreotide (SMS 201-995). 137 38

The somatostatin analogue octreotide (SMS 201-995) is a potent inhibitor of human exocrine pancreatic secretion. In the present study we analyzed the effect of octreotide (3 x 100 micrograms, daily) given over a time period of 7 days on hormone-stimulated exocrine pancreatic secretion in 6 healthy volunteers using a secretin-ceruletide test. The secretin-ceruletide test was carried out before, following the first injection of octreotide (day 1) and after a 7-day treatment with 3 x 100 micrograms octreotide daily. Duodenal fluid was collected over 30 min without stimulation, over 60 min following a bolus injection of 1 U/kg body weight secretin, and over 60 min during a continuous infusion of secretin and ceruletide. Following the first injection of octreotide and following 7 days of octreotide treatment secretin/ceruletide-stimulated amylase secretion was significantly reduced. Trypsin and chymotrypsin secretion was significantly reduced after the first injection of octreotide when pancreatic secretion was stimulated by secretin and ceruletide simultaneously. However, secretin and ceruletide-induced trypsin and chymotrypsin secretion was not inhibited after 7 days of octreotide treatment. Baseline, secretin and secretin/ceruletide-stimulated bicarbonate output were not influenced by octreotide either following the first injection of octreotide or the 7 days' treatment. Octreotide is a potent inhibitor of secretin/ceruletide-stimulated pancreatic amylase, trypsin and chymotrypsin secretion. However, following a 7-day treatment with octreotide this inhibition is only persistent for pancreatic amylase secretion.
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PMID:Inhibition of pancreatic secretion under long-term octreotide treatment in humans. 813 33

The aim of the present study was to determine the effects of a therapeutical dose of the long-acting cyclic somatostatin analogue octreotide (SMS 201-995) on cyclical interdigestive small intestinal motor function and exocrine pancreatic secretion in humans. Five fasting healthy subjects swallowed a gastroduodenal multi-lumen tube assembly and received continuous infusions of saline and octreotide (720 ng/kg/hr) for at least one interdigestive motor cycle or two hours. Upper gastrointestinal motility was recorded continuously by standard manometry. Duodenal chymotrypsin outputs were measured at 15 minutes intervals using polyethylene glycol as a dilution marker. Octreotide significantly decreased the length of the interdigestive motor cycle to one third of the control period (p < 0.01). Phase II proportion was reduced to less than 5% of the cycle length (controls: 66%; p < 0.01). The propagation velocity of octreotide-induced motor activity fronts was significantly slower compared with migrating motor complexes during the control period (controls: 6.8 +/- 0.4 cm/min, octreotide: 2.3 +/- 0.4 cm/min; p < 0.05). Overall duodenal chymotrypsin output was markedly inhibited by octreotide (5% of controls; p < 0.01). Moreover, during octreotide administration coupling between interdigestive motor activity and pancreatic exocrine enzyme secretion was disrupted. In conclusion short administration of a therapeutical dose of octreotide exerts similar effects on upper intestinal interdigestive human motor secretory parameters as naturally occurring molecular forms of somatostatin at pharmacological doses.
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PMID:[The synthetic somatostatin analog octreotide: effect on interdigestive pancreas secretion and gastrointestinal motility in man]. 846 93