Acts at the GPCR Vasopressin receptors
V1 on vascular smooth muscle – vasoconstrictive – markedly less than ADH (1500x less than ADH)
V1 on platelets - increase platelet aggregation – more potent than ADH
V2 on the nephron - expressed in the renal collecting duct (CD) - antidiuretic actions (10x ADH)

Acts at the GPCR Vasopressin receptors
V1 on vascular smooth muscle - vasoconstrictive
V1 on platelets - increase platelet aggregation
V2 on the nephron - antidiuretic actions

Vasoconstriction (less)
Increased platelet aggregation
Antidiuretic (more)

Vasoconstriction
Increased platelet aggregation
Antidiuretic

BA
SL: 0.25%
PO: 0.08-0.16%
Intranasal: 10%

IV only

20%

30%

0.2-0.32 L/kg

0.5 L/kg
Biphasic plasma curve

Minimal hepatic metabolism

minimal

65% unchanged in urine

urine

2-3hrs

50-70min

OD – Hyponatremia (Seizure, altered mental state, arrythmias, edema)

Hyponatraemia with H2O retention
May cause severe vasoconstriction -CVC only
Arrhythmias at higher doses
GIT smooth muscle constriction
cramping, nausea, diarrhoea

Deamino Arginine Vasopressin

Prodrug of lysine Vasopressin

Vasopressin Analogue

Vasopressin Analogue

Central DI – ADH replacement (Intranasal/parenteral)
Nocturnal polyuria (intranasal).
Haemostasis in Haemophilia with fVIII def or Type 1 Von Willebrand disease during surgical procedures and postoperatively to maintain hemostasis (parenteral).

Commonly used to stop bleeding of varices in the food pipe (oesophagus).

Hepatorenal syndrome

Synthetic analogue of 8-arginine vasopressin (ADH)

Antidiuretic peptide drug

displays enhanced antidiuretic potency, fewer pressor effects due to V2-selective actions, and a prolonged half-life and duration of action compared to endogenous ADH

analogue of vasopressin – Prodrug
Peiptidases  Lysine vasopressin

used as a vasoactive drug in the management of hypotension. It has been found to be effective when norepinephrine does not help

Longer duration of action than Vasopressin

Level 2

Level 2

Acts at the GPCR Vasopressin receptors

Acts at the GPCR Vasopressin receptors

sublingual tablet, intra nasal spray, IV/IM

IV

sublingual tablet, intra nasal spray, IV/IM
0.1 to 1.2 mg divided into 2 or 3 doses

IV
1-2mg terlipressin acetate (0.85-1.7mg Terlipressin) Q6 hourly