Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1 Pharmacodynamic properties
Pharmacotherapeutic group: Prostaglandins, ATC code: C01EA01

Prostaglandins are potent vasoactive derivatives of arachidonic acid that exert vasomotor, metabolic and cellular effects on the pulmonary and coronary circulation. The E series of prostaglandins produces vasodilation of the systemic and coronary circulation in most species: these prostaglandins have been used for maintaining the patency of the ductus arteriosus in children.

Pharmacokinetic Properties

5.2 Pharmacokinetic properties

Distribution
Based on studies in several animal species, intravenous or arterially administered prostaglandin E1 is very rapidly distributed throughout the entire body, with the exception of the central nervous system, where distribution, though detectable, is markedly reduced.

Biotransformation
Prostaglandin E1 is very rapidly metabolised. The primary organs for metabolism and inactivation of prostaglandin E1 are probably the lung, liver and kidney which remove and metabolise 40-95% of the prostaglandin E1 in a single pass through the organ. A number of other tissues possess lesser, but significant, capacity to metabolise prostaglandin E1. The predominant metabolites found in plasma, 15-oxo-prostaglandin E1 and 13,14-dihydro-15 oxo-prostaglandin E1 are extensively metabolised by β and ω- oxidation prior to excretion, primarily by the kidney. Few urinary metabolites of prostaglandin E1 have been characterised, but are widely believed to be analogous to those reported in detail for prostaglandin E2 and prostaglandin F2.

Elimination
Excretion is essentially complete within 24 hours after dosing, with no intact prostaglandin E1 being found in urine and no evidence of tissue retention of prostaglandin E1 or metabolites. In three species (rat, rabbit and lamb), the prostaglandin metabolising activity of lung from near-term fetal animals has been shown to be at least as effective as that of adults.

Pfleet 2021-0069764                   Page 6 of 8
Prostin VR LPD CC 040821