Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: Aspire Pharma Limited, Unit 4 Rotherbrook Court, Bedford Road, Petersfield, Hampshire, GU32 3QG, United Kingdom
Pharmacotherapeutic group: Posterior pituitary lobe hormones, Vasopressin and analogues.
ATC code: H01BA02
Desmopressin is a synthetic analogue of the natural human neurohypophyseal hormone L-arginine vasopressin from which it differs chemically in that the amino group of the cysteine in position 1 is removed and L-arginine has been substituted by the stereoisomeric D-arginine. As a consequence of these changes, the vasopressor action of the molecule is largely lost, whereas the antidiuretic action is enhanced and prolonged many times.
In the distal renal tubules and collecting ducts of the kidneys, desmopressin increases the permeability for water and thus water reabsorption from the primary urine.
After intranasal administration of desmopressin, the maximum plasma concentration is attained after about 50 minutes.
The plasma half-life is 2-3 hours. Desmopressin is excreted via the kidneys.
After intranasal administration, the systemic bioavailability of desmopressin is approximately 10% of the dose administered.
The antidiuretic effect already begins after 15 minutes. Depending on the dose, it is sustained for 6-24 hours.
The apparent distribution volume of desmopressin is relatively small: about 0,2 l/kg bodyweight, which suggests that the peptide is not distributed in the intracellular compartment. It has been shown that desmopressin does not pass the blood-brain-barrier.
Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, genotoxicity and toxicity to reproduction.
Impairment of renal function, with a rise in serum creatinine as well as hyaline degeneration of tubule epithelia, has been demonstrated in rats at a daily dose of 47.4 micrograms/kg body weight, i.e. at exposures considered sufficiently in excess of the maximum human exposure. The alterations were reversible after termination of desmopressin treatment.
Investigations on the carcinogenic properties are not available.
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