Vasopressin preparation

Christensen M, Johansen P, Hau C. Storage of polyvinylpyrrolidone (PVP) in tissues following long-term treatment with a PVP containing vasopressin preparation. Acta Med Scand 1978 204 295-298. 

On occasion, a patient may need to self-administer vasopressin by the parenteral route. If so, the nurse instructs the patient or a family member in the preparation and administration of the drug and measurement of the specific gravity of the urine. 

Ki of 6 nM against a guinea-pig uterine oxytocin preparation and at least 100-fold selectivity over rat vasopressin tissue preparations. These molecules show a pseudo-irreversible pharmacology, with an extended action against spontaneous contractibility of rat uterus 24 h post partum. 

A. General description Oxytocin is a nonapeptide (molecular weight 1.0 kDa) that differs by two amino acids from vasopressin it is stored and released from the posterior pituitary gland. Commercially available oxytocin is prepared synthetically. 

Preparations of angiotensin-converting enzyme inhibitors and angiotensin receptor antagonists are found in Chapter 11 Antihypertensive Agents preparations of vasopressin are found in Chapter 37 Hypothalamic Pituitary Hormones. 

Desmopressin acetate (arginine vasopressin) increases the factor VIII activity of patients with mild hemophilia A or von Willebrand disease. It can be used in preparation for minor surgery such as tooth extraction without any requirement for infusion of clotting factors if the patient has a documented adequate response. High-dose intranasal desmopressin (see Chapter 17 Vasoactive Peptides) is available and has been shown to be efficacious and well tolerated by patients. 

Synthetic aqueous vasopressin is a short-acting preparation for intramuscular, subcutaneous, or intravenous administration. The dose is 5-10 units subcutaneously or intramuscularly every 3-6 hours for transient diabetes insipidus and 0.1-0.5 units/min intravenously for gastrointestinal bleeding. 

Many biologically active secreted peptides are also amidated at their carboxyl terminal, and acetylated at their amino-terminal. The consequences of these modifications are (a) to reduce the susceptibility of these peptides to degradative actions of extracellular aminopeptidases and carboxypeptidases after their secretion and (b) to influence the biological activity of the peptides. Corticotropin-releasing factor, gastrin, cholecystokinin and vasopressin require the C-terminal amide for full activity [54—56]. Acetylation of the N-terminus of a-MSH is necessary for activity, whereas acetylation of /3-endorphin inhibits its opioid activity [57], The enzymes responsible for acetylation have been identified from bovine and rat intermediate lobes [57] and enzymes with a-amidation activity have been reported in preparations of pituitary secretory granules [54,55]. 

Phenolic esters are obtained similarly. The presence of a nitro group in the aromatic nucleus and the use of pyridine as solvent facilitates the reaction. This reaction is recommended for the characterization of phenols. 2,4,5-Trichlorophenyl-, pentachlorophenyl-, 4-nitrophenyl- and thiophenyl esters of N-acylamino acids are prepared in this manner. These aromatic esters are used in the stepwise lengthening of peptides, du Vigneaud and coworkers synthesized lysine vasopressin from a nonapeptide which they prepared stepwise using the nitrophenyl ester method. Room temperature esterification of dicarboxylic acids and diphenols are also carbodiimide mediated using the 1 1 complex derived from DMAP and p-toluenesulfonic acid as catalyst Methacrylic acid is also esterified with phenols using carbodiimides and DMPA to mediate the reaction. ... 

Rat liver is the most convenient source of tissue for the preparation of crude plasma membranes that contain the Vj subtype of vasopressin receptor. Methods for the... 

Meienhofer J, du Vigneaud V. Preparation of lysine-vasopressin 116. through a crystalline protected nonapeptide intermediate and purification of the hormone by chromatography. J. Am. Chem. 

Poly(amino acid)s (PAAs) have also been used in drug delivery PEO-(l-aspartic acid) block copolymer nano-associates , formed by dialysis from a dimethyl acetamide solution against water, could be loaded with vasopressin. PLA-(L-lysine) block copolymer microcapsules loaded with fluorescently labelled (FITC) dextran showed release profiles dependent on amino acid content. In a nice study, poly(glutamate(OMe)-sarcosine) block copolymer particles were surface-grafted with poly(A-isopropyl acrylamide) (PNIPAAm) to produce a thermally responsive delivery system FITC-dextran release was faster below the lower critical solution temperature (LCST) than above it. PAAs are prepared by ring-opening polymerisation of A-carboxyanhydride amino acid derivatives, as shown in Scheme 1. 

Water deprivation and exogenous ADH administration are two diagnostic tests that can be used to differentiate neurogenic from nephrogenic DI. The latter test is pursued only after there is a failure to produce concentrated urine in response to the water-deprivation test (Schott 1998). Until recently, the most commonly used form of exogenous ADH was a water-insoluble tannate of arginine vasopressin extracted from the posterior pituitary and suspended in peanut oil. This preparation is no longer available. Currently,... 

Vasopressin Injection, USP. Vasopressin injection (Pi-ircssin) is a sterile solution of the water-soluble pre.ssor principle of the posterior lobe of the pituitary of healthy, domestic animals u.sed for food by humans it also may be prepared by synthesis. Each milliliter possesses a pres.sor activity equal to 20 USP posterior pituitary units expiration date. 3 )cars. 

Feldene piroxicam. felodipine [ban, inn, usan] (Plendil etc.) is a dihydropyridine calcium-channel blocker with VASODILATOR properties, which can be used in ANTIHYPERTENSIVE therapy and antianginal prophylaxis, felypressin [ban, inn, usan] ([Phe Lys ]vasopressin phelypressin PLV2 Octapressin Octopressin ) is a synthetic analogue of vasopressin. It is a VASOCONSTRICTOR and is incorporated into LOCAL ANAESTHETIC preparations to prolong their duration of action. (It is a constituent with prilocaine of Citanest with Octapressin .)... 

One of the best-known examples of this class is interferon (a glycoprotein), which has shown much promise as an antiviral agent and in the treatment of cancer (71). Numerous polymers (mostly polyelectrolytes) are effective in inducing the production of interferon in animals (72). Other well-known bioactive polypeptides are insulin, adrenocorticotropic hormone (ACTH), human growth hormone (HGH), prolactin, follicle stimulating hormone (FSH), and luteinizing hormone most of these have been synthesized, and some derivatives have been prepared (73). Some small bioactive polypeptides are the nonapeptides bradykinin, vasopressin, and oxytocin bioactive derivatives have been made for many of these also (74). 

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