Figure 1. Chemical structure of lysipressin
Lysipressin ([Lys8]-vasopressin) has been identified in the North America opossum (Didelphis virginiana) by amino acid composition and high pressure liquid chromatography. It is a lysine vasopressin that maintains body water and contracts blood vessels for the treatment of bleeding esophageal varices. As a pressurized peptide, Lysipressin is similar to human vasopressin receptor, which is isolated from marsupials and pigs that binds to the receptors. Lysipressin produces smooth muscle contraction and strengthens gastric damage in animal models.
As an endogenous vasopressin in mammals, lysipressin is used to regulate blood pressure. It is released into the blood from the nerve endings in the posterior and median bulges of the pituitary gland. It is a neurotransmitter of the central nervous system and also involves various physiological processes, such as regulating water balance through antidiuretic effects. Lysipressin is one of the active peptides containing nine amino acid residues. It also belongs to the category of octapeptide because two cysteines are linked by a disulfide bond. In addition to the extraction from the posterior lobe of the pituitary gland, it can also be synthesized artificially.
The physiological function of lysipressin is mainly to promote the reabsorption of water by the renal tubules. Lysipressin can also induce the contraction of systemic arterioles including coronary and pulmonary arteries, thereby raising blood pressure. In view of the adverse effect of elevated blood pressure on cardiac activity, lysipressin is mainly used for the treatment of diabetes insipidus caused by the lack of vasopressin in clinical practice, but it is noneffective for renal polyuria. The administration can be carried out by subcutaneous or intramuscular injection, and it can also be made into nasal spray powder.
Pharmacokinetics and metabolism
The activity of lysipressin is 50 post-pituitary (pressurized) units per ml. Lysipressin can be rapidly absorbed by the nasal mucosa, therefore, if administered frequently, it can be used alone to treat mild to moderate central diabetes insipidus. For severe cases, due to its short duration of action, severe sudden polyuria may occur during the treatment, so the effect of treatment with desmopressin or tannate vasopressin is more satisfactory. Lysipressin has no effect on nephrogenic diabetes insipidus.
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