Metabolism and pharmacokinetics of prostaglandin E1 administered by intravenous infusion in human subjects

  title={Metabolism and pharmacokinetics of prostaglandin E1 administered by intravenous infusion in human subjects},
  author={Willi Cawello and Horst Schweer and Robert M{\"u}ller and Rainer Bonn and Hannsj{\"o}rg W. Seyberth},
  journal={European Journal of Clinical Pharmacology},
In a single-blind, randomized, two-way crossover study with 12 healthy male volunteers, 60 μg of prostaglandin E1 (PGE1) or placebo was administered by intravenous infusion during a 120-min period. PGE1, 13,14-dihydro-PGE1 (PGE0) and 15-keto-PGE0 plasma concentrations were measured by a highly specific and sensitive GC-MS/MS method.Endogenous PGE1 plasma concentrations ranged between 1.2 and 1.8 pg·ml−1. Endogenous PGE0 and 15-keto-PGE0 plasma concentrations varied from 0.8 to 1.3 pg·ml−1 and… 
Progress in the prostaglandin E1-therapy of the intermittent claudication by means of bolus injections of LIPO-prostaglandin E1 (LIPO-PGE1)
Compared to conventional PGE1-cyclodextrin infusions given over 2 h, a clearly prolonged increase in perfusion of the affected limb after LIPO-PGE1 was demonstrated and no serious adverse effects were observed.
Systemic levels following PGE1 inhalation in neonatal hypoxemic respiratory failure
Although a reversible increase in PGE1 levels was detected following a dose of 50 ng/kg/min (p <0.05), there was no association between PGE 1 levels and IPGE1 duration, Pa O2, temperature, heart rate, and blood pressure.
An approach to predict the ductus-arteriosus dilating effect induced by lipo-prostaglandin E1 in newborn rats lacking plasma concentration-time data by the pharmacological response kinetic model.
Findings indicate that PRK modeling based on the intensities of the observed pharmacological response-time data is a meaningful tool in some targeting-type drugs, for which pharmacokinetic analysis itself is meaningless or acquisition of pharmacokinetics data is technically impossible, in predicting the time courses of the drug's pharmacologicalresponse in different dosage regimens.
Local sustained release of prostaglandin E1 induces neovascularization in murine hindlimb ischemia.
Local administration of a single dose of sustained-release PGE(1) enhances neovascularization in mice hindlimb ischemia more efficiently than daily systemic administration.
In vivo Endocrine Secretion of Prostacyclin Following Expression of a Cyclooxygenase-1/Prostacyclin Fusion Protein in the Salivary Glands of Rats Via Nonviral Gene Therapy.
The feasibility of gene therapy to drive endogenous biosynthesis of PGI2 as a therapeutic strategy for the treatment of PAH is suggested.
The two-step model of prostaglandin signal termination: in vitro reconstitution with the prostaglandin transporter and prostaglandin 15 dehydrogenase.
The data represent reconstitution of the longstanding model of PG metabolism consisting of sequential carrier-mediated PG uptake, cytoplasmic oxidation, and diffusional efflux of the PG metabolite.
Effect of Prostanoids on Human Platelet Function: An Overview
Prostanoids are bioactive lipid mediators and take part in many physiological and pathophysiological processes in practically every organ, tissue and cell, including the vascular, renal,
Pharmacologic platelet anesthesia by glycoprotein IIb/IIIa complex antagonist and argatroban during in vitro extracorporeal circulation.
Intravenous infusion of prostaglandin E1 therapy in extremity ischemia
The review of literature and the use of PGE1 in CLI is presented here along with the experience in NIMS, where the agent was the agent used since 1973 for cardiovascular diseases.
Prostacyclin as an Anticoagulant for Continuous Renal Replacement Therapy in Children
Prostacyclin is a platelet inhibitor that can be safely used as an efficient anticoagulant in CRRT in children requiring CRRT and induces a heparin-sparing effect, which can reduce the dosage and side effects ofHeparin.


On the metabolism of prostaglandin E1 administered intravenously to human volunteers.
It was found that levels of 15-keto-13, 14-dihydro-PGE1, but not those of PGE1 itself, increased in a dose-dependent manner, and increased formation of 13,14-dismemberment-of-prostaglandin (PG) E1 with increasing doses of P GE1 can be expected to occur.
Metabolic disposition of prostaglandin E1 in man.
A radioimmunoassay for the unstable pulmonary metabolites of prostaglandin E1 and E2: an indirect index of their in vivo disposition and pharmacokinetics.
A radioimmunoassay with a sensitivity of 12-pg was developed for this analytically suitable bicyclic derivative of prostaglandin E2 and the accuracy, precision and sensitivity of the method permitted its application to certain intractable problems.
Formation of biologically active 13,14-dihydro-prostaglandin E1 during intravenous infusion of prostaglandin E1 in newborns with ductus arteriosus-dependent congenital heart disease.
Plasma concentrations of prostaglandin (PG) E1 and 13,14-dihydro-PGE1 were measured by gas chromatography-mass spectrometry in eight newborns with ductus arteriosus-dependent congenital heart disease during continuous intravenous infusion of PGE1.
Determination of prostaglandin E1 and its main plasma metabolites 15-keto-prostaglandin E0 and prostaglandin E0 by gas chromatography/negative ion chemical ionization triple-stage quadrupole mass spectrometry.
Prostaglandin E1 (PGE1), 15-keto-PGE0 and PGE0 in plasma were determined in an isotope dilution assay by gas chromatography/triple-stage quadrupole mass spectrometry. After addition of deuterated
On the Metabolism of Prostaglandins E1 and E2 in Man
Prostaglandin E1 and arterial occlusive disease: pharmacological considerations
A large number of uncontrolled and small number of controlled clinical studies has been published claiming significant beneficial effects of PGEI therapy in patients with arterial occlusive disease, although some studies have suggested strong placebo effects.
Compartmental Model Analysis in Pharmacokinetics
Compartmental model analysis appears to be a tool that is still used and remains useful in the fields of pharmacokinetics and clinical pharmacology, and the applications of compartmental models inclinical pharmacology are discussed.
Effect of iron deficiency anaemia and its treatment on sulphadimidine absorption
Sulphadimidine absorption by the anaemic patients was significantly greater than in normals, and it was not significantly different before and after iron therapy or correction of anaemia.