Vasopressins analogues

Ungell AL, Andreasson A, Lundin K, Utter L (1992) Effects of enzymatic inhibition and increased paracellular shunting on transport of vasopressin analogues in the rat. J Pharm Sci 81 640-645. 

Active bleeding. Acutely bleeding varices can be treated by injection sclerotherapy, by tamponade and by infusion systemically of vasopressin analogues or octreotide (which reduce variceal pressure). Results of controlled trials generally reflect efficacy in oesophageal rather than gastric variceal disease, which form a minority of cases, and can be more difficult to manage. 

Scheme 3 Synthesis of a Monocarba-vasopressin Analogue by the Solid-Phase Cyclization Method116 ...

Terlipressin, a long-acting vasopressin analogue, is metabolized to the active drug lysine vasopressin. The use of terlipressin to treat acute variceal bleeding has been reviewed (2,3). 

Von Willebrand factor plays a key role in thrombogenesis. Lack of this factor is the cause of thrombasthenia, the inability to staunch bleeding by platelet aggregation. A relative deficiency of von Willebrand factor can be transiently relieved by injection of the vasopressin analogue desmopressin because this substance makes factor available from stored supplies. 

Ornipressin is a vasopressin analogue that primarily leads to vasoconstriction of the splanchnic vasculature. The first report outlining its use was compiled in 1985 by K. Lenz et al. (36) Dosage was 25 IU/12 hr or 6 IU/4 hr. The outcome was a fall in renal vascular resistance and an improvement in the glomerular filtration rate. (23 quot. 6, 10, 12, 43) The combined administration of ornipressin (2-6 lU/hr) and albumin (20-60 g/day) for a period of 2 weeks (with intensive care monitoring ) has led to remarkable therapeutic success. (24)... 

Svedman, P. Lundin, S. Svedman, C. Administration of antidiuretic peptide (DDAVP) by way of suction de-epithelialised skin. Lancet 1991, 337, 1506-1509. Lundin, S. Svedman, P. Hoglund, P. Jonsson, K. Breeders, A. Melin, P. Absorption of an oxytocin antagonist (antocin) and a vasopressin analogue (dDAVP) through a standardized skin erosion in volunteers. Pharm. Res. 1995,12, 2024-2029. 

Treatment of HRS is best accomplished by either increasing systemic vascular resistance, as with the vasopressin analogue terlipressin, or reducing portal venous pressure, most commonly accomplished with TIPS. Both have shown promise in improving renal function in... 

Howl, J., Prochazka, Z., Wheatley, M., and Slaninova, J. (1999) Novel strategies for the design of receptor-selective vasopressin analogues Aib-substitution and retro-inverso transformation. Br. J. Pharmacol. 128,647-652. 

Jard, S Lombard, C., Seyer, R., Aumelas, A., Manning, M. and Sawyer, W.H. (1987) lodination of vasopressin analogues with agonistic and antagonistic properties effects on biological properties and affinity for vascular and renal vasopressin receptors. Mol. Pharmacol. 32 369-375. 

Lundin S, Pierzynovski S G, Westrom B R, et al. (1991). Biliary excretion of the vasopressin analogue DDAVP after intraduodenal, intrajugular and intraportal administration in the conscious pig. Pharmacol. Toxicol. 68 177-180. 

DDAVP (l-desamino-8-d-arginine vasopressin), a synthetic vasopressin analogue, was found effective and superior to antidiuretic drugs in maintaining normal diuresis in 6 patients with diabetes insipidus centralis (42C). 

Kauli, R. and Larox, Z. (1974) A vasopressin analogue in treatment of diabetes insipidus. Arch. Dis. Childh., 49,482. 

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