Antidiuretic activity of terlipressin (triglycyl-lysine vasopressin)--role of pressure natriuresis.
Terlipressin (triglycyl-lysine vasopressin TP), a "hormonogen" analogue, was introduced in gastroenterology for its low and protracted vasopressor action, reducing bleeding from gastrointestinal tract. Its antidiuretic activity, estimated originally in ethanol-anaesthetized rats (Sawyer's method) was claimed to be equally low and protracted. We performed several series of antidiuretic tests on conscious rats (Burn's method) with the following results. TP in low doses of 0.05-1.0 micrograms/kg exhibited typical dose-dependent antidiuretic effect. In the dose of 0.2 micrograms/kg, the dynamics of urine and sodium excretion did not differ from that after equivalent dose of lysine vasopressin and equipotent dose of DDAVP. The antidiuretic potency of TP (estimated by parallel line assay) was 175.0 U/mg. TP in doses of 5.0 and 20.0 micrograms/kg exhibited limited diuresis and marked natriuresis. High osmolality and sodium content were present in all portions of excreted urine. The discrepancy between previous and our results concerning antidiuretic activity of TP and the role of pressure natriuresis for overall renal action of TP are discussed.
Machová
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Research Institute for Pharmacy and Biochemistry, Prague.
D000818:Animals; D003894:Deamino Arginine Vasopressin / Q000494:pharmacology; D004232:Diuretics / Q000037:antagonists & inhibitors*; D004305:Dose-Response Relationship, Drug; D007668:Kidney / Q000502:physiology; D008236:Lypressin / Q000031:analogs & derivatives* / Q000494:pharmacology; D008297:Male; D009318:Natriuresis / Q000187:drug effects / Q000502:physiology*; D051381:Rats; D017208:Rats, Wistar; D012964:Sodium / Q000652:urine; D000077585:Terlipressin
D004232:Diuretics; D008236:Lypressin; D000077585:Terlipressin; D012964:Sodium; D003894:Deamino Arginine Vasopressin