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Lypressin, in the form Post Date: Sun, 12 Oct 2008 22:03:21 +0000
An inefficient but convenient and inexpensive means of administration has been to apply rather large amounts of the hormone, in the form of posterior pituitary powder, to the nasal mucous membranes. The amounts of ADH absorbed are sufficientfor the control of diabetes insipidus for a period of 6 to 12 hours. Lypressin, in the form of a nasal spray, is administered for this purpose.
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ADH is removed from plasma Post Date: Sun, 12 Oct 2008 21:52:06 +0000
Upon reaching the circulation, endogenous or injected ADH is rapidly removed. Its half-life in plasma, in concentrations within the physiological range, is approximately 15 minutes in man. ADH is removed from plasma and inactivated largely during passage through the liver and kidneys.
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The urinary clearance of endogenous Post Date: Sun, 12 Oct 2008 21:40:55 +0000
A portion of the hormone removed from the plasma by the kidney is enzymatically inactivated. The remainder appears in the urine bound to unidentified large molecules. The urinary clearance of endogenous or exogenous ADH is 5 to 10% of the glomerular filtration rate.
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During pregnancy a peptidase appears Post Date: Sun, 12 Oct 2008 21:23:43 +0000
Most investigators have found that circulating ADH is largely unbound and is confined to extracellular fluid. The fate of lypressin is similar to that of ADH.During pregnancy a peptidase appears in plasma that is capable of inactivating a portion of ADH as well as oxytocin (see Chapter 42) by cleavage of the 1-cysteine to 2-tyrosine bond of the ring.
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ADH isavailable Post Date: Sun, 12 Oct 2008 21:08:09 +0000
For details of the biological fate of ADH, see Sawyer (1961) and Lauson (1967, 1970).Preparations, Bioassay, and Unitage. ADH isavailable in two types of preparations.
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Activity is compared Post Date: Sun, 12 Oct 2008 20:55:38 +0000
One is an extract in which no separation of the antidiuretic and oxytocic principles has been made. It is assayed for its oxytocic activity, which parallels antidiuretic ac-tivity. Activity is compared to that of a USP bovine pituitary standard and is expressed in terms of USP posterior pituitary units.
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Pos-terior pituitary injection (5) (PITUITRIN-S) Post Date: Sun, 12 Oct 2008 20:36:44 +0000
Posterior pituitary consists of desiccated posterior pituitary powder that contains the equivalent of 1 USP posterior pituitary unit in each milligram; it is marketed as capsules containing approximately 45 mg, and as an inhalator. Posterior pituitary injection (PITUITRIN) is a sterile aqueous extract of the gland that contains the equivalent of 10 USP posterior pituitary units per milliliter. Pos-terior pituitary injection (5) (PITUITRIN-S), for use as a local hemostatic agent in surgery, contains 20 USP units per milliliter.
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The test method Post Date: Sun, 12 Oct 2008 20:22:31 +0000
Vasopressin Injection, USP (PITRESSIN), is pre-pared from the posterior pituitary glands of domestic animals by separation of ADH from the oxytocic hormone, or by synthesis. It is assayed for pressor activity rather than antidiuretic activity, but these are identical, unit for unit. The test method is the blood pressure of the rat.
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Vaso-pressin injection contains 20 pressor Post Date: Sun, 12 Oct 2008 20:03:27 +0000
Activity is designated as pressor units and is determined by comparison with a USP standard. Theoretically, there should be no differ-ence in antidiuretic activity between a USP poste-rior pituitary unit and a USP pressor unit. Vaso-pressin injection contains 20 pressor units and not more than 1 oxytocic unit per milliliter.
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However, for reasons of chemical Post Date: Sun, 12 Oct 2008 19:50:40 +0000
The pure synthetic hormones, when subjected to bioassay, show an activity of approximately 370 USP pressor units per milligram of arginine vaso-pressin, and about two thirds of this activity for lysine vasopressin (lypressin). Their ratio of anti-diuretic activity is similar. However, for reasons of chemical stability, lysine vasopressin is the more acceptable of the two synthetic hormones for thera-peutic use.
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