Desmopressin (DDAVP) is a synthetic analogue of the endogenous hormone vasopressin (antidiuretic hormone, ADH). Deamination of the first amino acid and substitution of L-arginine with D-arginine give it selective activity at the V2 receptor with strongly reduced pressor (V1) activity. It has been approved for decades for indications including central diabetes insipidus, primary nocturnal enuresis, and bleeding tendency in von Willebrand disease type 1 and mild haemophilia A. The principal safety concern is hyponatremia or water intoxication.
Desmopressin is a structurally modified analogue of the nine-residue peptide hormone vasopressin. Deamination at the N-terminus (1-deamino) and replacement of L-arginine by D-arginine at position 8 prolong the duration of action and render the compound largely selective for the vasopressin V2 receptor, while the V1-mediated vasoconstrictive effect is strongly reduced. Acting on V2 receptors in the renal collecting ducts, it promotes insertion of aquaporin-2 water channels into the apical membrane, increasing water reabsorption and reducing urine volume (antidiuretic effect). In addition, via V2 receptors on the vascular endothelium, desmopressin stimulates the release of von Willebrand factor and factor VIII from endothelial stores (Weibel-Palade bodies), improving primary haemostasis.
Теоретическая кривая концентрации при периоде полувыведения 3 h. Чисто фармакокинетическая модель — не рекомендация по дозировке.
Open in PK tool →Desmopressin can lead to water retention and consequent hyponatremia; careful restriction of fluid intake and monitoring of serum sodium are emphasised in the labeling.
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