Desmopressin (dDAVP), a artificial analogue of eight-arginine vasopressin (ADH), is an antidiuretic peptide drug modified by way of deamination of one-cysteine and substitution of eight-L-arginine with the aid of eight-D-arginine. ADH is an endogenous pituitary hormone that has a important position within the control of the water content material within the body. Upon release from the stimulation of increased plasma osmolarity or reduced circulating blood volume, ADH specifically acts on the cells of the distal part of the nephron and the collecting tubules in the kidney [T28]. The hormone interacts with V1, V2 or V3 receptors with differing sign cascade systems. Desmopressin shows more suitable antidiuretic efficiency, fewer pressor consequences because of V2-selective movements, and a prolonged half-life and length of motion as compared to endogenous ADH [A31661]. it has been employed clinically on the grounds that 1972 and is to be had in diverse formulations consisting of intranasal answer, intravenous answer, oral pill and oral lyophilisate [A31662]. Desmopressin is indicated for the remedy of polyuric conditions which include primary nocturnal enuresis, nocturia, and diabetes insipidus. It was also newly approved for the treatment of mild classical hemophilia and von Willebrand's sickness for minor surgeries. The lively aspect in maximum formulations is desmopressin acetate. Nocdurna, or desmopressin acetate, became permitted by the FDA on June 21st, 2018 for the remedy of nocturia because of nocturnal polyuria in adults. it's miles to be had as a sublingual tablet.
By mimicking the actions of endogenous ADH, desmopressin acts as a selective agonist of V2 receptors expressed in the renal collecting duct (CD) to increase water re-absorption and reduce urine production. Desmopressin has been shown to be more potent than ADH in increasing plasma levels of factor VIII activity in patients with hemophilia and von Willebrand's disease Type I [L1183]. Desmopressin demonstrates markedly diminished pressor activity. Desmopressin administered intranasally has an antidiuretic effect about one-tenth that of an equivalent dose administered by injection [L1182].
- Indicated for the treatment of nocturia due to nocturnal polyuria in adults who awaken at least 2 times per night to void (intranasal). - Indicated as antidiuretic replacement therapy in the management of central cranial diabetes insipidus and for management of the temporary polyuria and polydipsia following head trauma or surgery in the pituitary region (intranasal/parenteral). - Indicated for patients with hemophilia A with factor VIII coagulant activity levels greater than 5% or mild to moderate classic von Willebrand's Disease (Type I) with factor VIII levels greater than 5% during surgical procedures and postoperatively to maintain hemostasis (parenteral).
Upon binding of desmopressin to V2 receptors in the basolateral membrane of the cells of the distal tubule and collecting ducts of the nephron, adenylyl cyclase is stimulated. The resulting intracellular cascades in the collecting duct lead to increased rate of insertion of water channels, called aquaporins, into the lumenal membrane and enhanced the permeability of the membrane to water [T28].