Vasopressin PHARMACOLOGY

Desmopressin
Lypressin
Terlipressin
Felypressin
Argipressin
ornipressin
Desmopressin: It is a selective V2-receptor agonist and is more potent than vasopressin as an antidiuretic. It has negligible vasoconstrictor action. It is administered by oral, nasal and parenteral routes. Lypressin: It acts on both V1- and V2-receptors. It is less potent but longer acting than vasopressin. It is administered parenterally. Terlipressin: It is a prodrug of vasopressin with selective V1 action. It is administered intravenously. Felypressin: It is a synthetic analogue of vasopressin. It is mainly used for its vasoconstrictor (V1 ) action along with local anaesthetics to prolong the duration of action. Felypressin should be avoided in pregnancy because of its oxytocic (uterine stimulant) activity.

1. Vasopressin D r . S P Srinivas Nayak , PharmD , RPh , (M S c), (PGDND) ( P h D) Assistant Professor, Dept. of Pharmacy Practice, PU.

2. Vasopressin an arginine vasopressin ( AVP) Also called as antidiuretic hormone ( ADH) It is a peptide hormone synthesized in the supraoptic and paraventricular nuclei of the hypothalamus and stored in posterior pituitary Vasopressin

3. Sunday, October 31, 2021 PIPR, PARUL UNIVERSITY

4. Vasopressin receptors RECEPTOR V1 V2 V3 LOCATION of Vasopressin Receptors and ACTIONS of Vasopressin upon receptor activation Blood vessels: Vasoconstriction GIT: Increases peristalsis Liver: Glycogenolysis Platelets: Aggregation CNS: Release of ACTH from anterior pituitary Renal tubules: Increases water reabsorption, hence reduces urinary output Vascular endothelium: Release of clotting factor VIII and von Willebrand’s factor from vascular endothelium Anterior pituitary : Releases ACTH, prolactin, endorphins Uterus: Contraction of the smooth muscle by vasopressin is mediated through oxytocin receptors.

5. Vasopressin Analogues Desmopressin Lypressin Terlipressin Felypressin Argipressin ornipressin Sunday, October 31, 2021 PIPR, PARUL UNIVERSITY

6. Vasopressin Analogues Desmopressin : It is a selective V2-receptor agonist and is more potent than vasopressin as an antidiuretic. It has negligible vasoconstrictor action. It is administered by oral, nasal and parenteral routes .

7. USES OF DESMOPRESSIN USED IN Haemophilia and von Willebrand’s disease : Desmopressin , administered intravenously, controls bleeding by increasing factor VIII and von Willebrand’s factor . Primary nocturnal enuresis : Administration of desmopressin at bedtime reduces nocturnal urine volume.

8. Neurogenic diabetes insipidus (DI) : Desmopressin is the drug of choice. DI is a condition characterized by excretion of large volume of urine either due to N eurogenic DI: D ecreased secretion of ADH from the neurohypophysis or due to Nephrogenic DI: inadequate renal tubular response to ADH. OTHER DRUGS TO REMEMBER: Thiazides are useful for both central and nephrogenic DI . Amiloride is used for the treatment of lithium-induced nephrogenic DI . Indomethacin reduces urine volume in nephrogenic DI by inhibiting renal prostaglandin synthesis .

9. Lypressin : It acts on both V1 and V2 receptors . It is less potent but longer acting than vasopressin. It is administered parenterally .

10. Terlipressin : It is a prodrug of vasopressin with selective V1 action. It is administered intravenously . USAGE: For emergency control of bleeding oesophageal varices : ADH controls bleeding by constricting mesenteric blood vessels .

11. Felypressin : It is a synthetic analogue of vasopressin. It is mainly used for its vasoconstrictor ( V1) action along with local anaesthetics to prolong the duration of action. Felypressin should be avoided in pregnancy because of its oxytocic (uterine stimulant) activity.

12. Adverse effects Nausea , vomiting, diarrhoea , belching and abdominal cramps . Backache is due to uterine contraction . Intranasal administration may cause local irritation and ulceration . Fluid retention and hyponatraemia can occur.

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