Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Posterior pituitary lobe hormones (vasopressin and analogues) ATC code: H01B A04
Terlipressin (Triglycyl-Lysine-Vasopressin) is a synthetic analogue of the natural posterior pituitary hormone vasopressin.
Terlipressin is a pro-drug with partial, intrinsic activity by itself. Terlipressin is transformed into the fully active metabolite lysine-vasopressin (LVP) by enzymatic cleavage. LVP remains within the therapeutic concentration range over a period of 4-6 hours.
Doses of 1 and 2 mg terlipressin acetate effectively reduce the portal venous pressure and produce marked vasoconstriction. The lowering of portal pressure and azygos blood flow is dependent on dose. The effect of the low dose is reduced after 3 hours, while haemodynamic data show that 2 mg terlipressin acetate is more effective than 1 mg terlipressin acetate with a sustained effect throughout the treatment period (4 to 6 hours).

Pharmacokinetic Properties

5.2 Pharmacokinetic properties
Glypressin is administered by bolus IV injection. It shows a biphasic plasma level curve which indicates that a two-compartment model can be applied. The half life of Distribution (T ½ α) is about 8-10 minutes. The half-life of elimination (T ½ β) is about 50-70 minutes.
Lysine vasopressin reaches maximum plasma levels about 1-2 hours following i.v. administration and has a duration of activity of 4-6 hours.