The Pharmacokinetics and Safety of Single Escalating Oral Doses of Eletriptan

The pharmacokinetics, safety, and tolerability of the 5‐HT1B/1D agonist eletriptan were characterized in a randomized, double‐blind, placebo‐controlled, dose escalation study. Healthy males received single oral doses of 10 to 120 mg. Following screening and baseline measurements, plasma and saliva e...

Full description

Saved in:
Bibliographic Details
Published in:Journal of clinical pharmacology 2002-05, Vol.42 (5), p.520-527
Main Authors: Shah, Ajit K., Harris, Stephen C., Greenhalgh, Catherine, Morganroth, Joel
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Area Under Curve
Biological and medical sciences
Blood Pressure - drug effects
Dose-Response Relationship, Drug
Double-Blind Method
Half-Life
Humans
Indoles - administration & dosage
Indoles - adverse effects
Indoles - chemistry
Indoles - pharmacokinetics
Liver Function Tests
Male
Medical sciences
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Pyrrolidines - administration & dosage
Pyrrolidines - adverse effects
Pyrrolidines - chemistry
Pyrrolidines - pharmacokinetics
Saliva - chemistry
Serotonin Receptor Agonists - administration & dosage
Serotonin Receptor Agonists - adverse effects
Serotonin Receptor Agonists - chemistry
Serotonin Receptor Agonists - pharmacokinetics
Serotoninergic system
Tryptamines
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The pharmacokinetics, safety, and tolerability of the 5‐HT1B/1D agonist eletriptan were characterized in a randomized, double‐blind, placebo‐controlled, dose escalation study. Healthy males received single oral doses of 10 to 120 mg. Following screening and baseline measurements, plasma and saliva eletriptan concentrations were measured at intervals over 48 hours and 24 hours, respectively. Samples were analyzed using high‐performance liquid chromatography with ultraviolet detection. Both the maximum plasma concentration and the area under the plasma eletriptan concentrationtime curve showed an essentially linear relationship to the administered dose. Eletriptan exhibited a median time to maximum plasma concentration of 1 to 1.25 hours and a mean elimination half‐life of 3.6 to 7.0 hours. Mean salivary‐plasma ratios for pharmacokinetic parameters generally remained constant across the 30 to 90 mg dose range. Eletriptan was well tolerated, with mostly mild and transient adverse events. In conclusion, oral doses of eletriptan in the therapeutic range were rapidly absorbed and exhibited essentially linear plasma and saliva pharmacokinetics.
ISSN:0091-2700
1552-4604
DOI:10.1177/00912700222011571