Desmopressin

• CAS Number: 16679-58-6

Desmopressin is a synthetic protein substance (protein) and structurally related to the endogenous peptide hormone vasopressin ( antidiuretic hormone also, ADH, called ). Desmopressin inhibits the excretion of water and is used as a drug.

Structure

The primary structure of desmopressin (1- desamino -8 -D -arginine vasopressin, DDAVP ) is derived from the natural vasopressin. The modified peptide consisting of 9 amino acids with a N-terminal cysteine ​​deaminated and a D -arginine instead of L - arginine at position 8 (see chirality (chemistry) ).

Mechanism of Action

Desmopressin is a synthetic analogue of the endogenous arginine vasopressin (ADH = antidiuretic hormone) and an agonist at the AVP receptors. It differs from this physiological hormone from the pituitary gland but in the receptor affinity: During AVP with similar affinity to the V1, which is mainly responsible for vasoconstriction, such binds to the V2 receptor, desmopressin is not equal affinity to the V2 receptor and negligible the V1. The AVP receptor 2 is in turn mainly responsible for water retention in the collecting ducts of the kidney. When it is activated, it causes the installation of water channels ( aquaporins ) in cell membranes, which allow water molecules to pass. Thus the urine is drained / thickened and retain more water in the body. There are also other effects of V2: It triggers the release of von Willebrand factor and the expression of P -selectin during exocytosis of Weibel- Palade bodies of endothelial cells.

Desmopressin is an anti- diuretic. It inhibits occurring in a central diabetes insipidus typically massive water excretion. Characterized the quality of life of affected patients is significantly improved. Also for the treatment of polyuria and polydipsia traumatic it has been approved, as well as in other diseases associated with ADH deficiency, or the like after surgery in Hypophysenbereich craniocerebral trauma. And as a diagnostic tool for the differential diagnosis of diabetes insipidus. Another field of application is the treatment of nighttime bedwetting ( nocturnal enuresis ).

Desmopressin can be given as Antihämorrhagikum eg hemophilia, uremic Thombozytopathie or von Willebrand's syndrome.

Side effects

The more common side effects generally depend on the pharmacodynamics together. Especially with increased fluid intake is leading to increased water retention ( Desmopressin is a highly potent anti- diuretic), thereby increasing volume with relative electrolyte deficiency. Warning signs of this are headache, nausea / vomiting and weight gain. In rare severe cases it can lead to cerebral edema, leading partly associated with seizures or consciousness restrictions. Furthermore, there are often side effects such as allergies and Herzkreislaufprobeme (e.g., angina pectoris ), which are associated with the increase in blood pressure.

Dosage forms

Desmopressin is one of the few medicinal products for which a nasal spray is offered in addition to the tablets and orodispersible tablet. Due to the low molecular weight of the hormone occurs well enough through the nasal mucosa into the bloodstream. However, the indication for nocturnal enuresis is retracted to the nasal spray, as the tablet form has been found to be safer to use. The orodispersible tablet, which is now approved in Germany since 1 June 2011 and is already longer sold in other countries, is to ensure a safer absorption and effect. The improved bioavailability of a lower drug load is possible with the same effect. Minirin is furthermore available as an infusion solution for intravenous and subcutaneous administration.

Trade names

Adin (A), Desmogalen (D), Desmospray (D), Desmotabs (D), Minirin (D, A, CH), Nocutil (D, A, CH), Novidin (A), Octostim (D, A, CH ), various generics (D, A).