Pharmacokinetics, pharmacodynamics, and safety of the 5-HT(1B/1D) agonist eletriptan following intravenous and oral administration
by
Milton KA, Scott NR, Allen MJ, Abel S,
Jenkins VC, James GC, Rance DJ, Eve MD.
Clinical Sciences,
Pfizer Global Research and Development,
Sandwich, Kent, United Kingdom.
J Clin Pharmacol 2002 May;42(5):528-39


ABSTRACT

Four separate studies were conducted to examine the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of eletriptan, a 5-HT(1B/1D) receptor agonist being developed for the treatment of migraines, after oral and intravenous administration. Fifty-five males received oral (1.5-30 mg or 30-120 mg) or intravenous (1.67-50 microg/kg or 50-102 microg/kg) eletriptan in four double- and single-blind, placebo-controlled, ascending-dose crossover studies. The maximum plasma concentration (Cmax) and area under the concentration curve (AUC) appeared linear over all dose ranges, with an apparent terminal half-life of 4 to 5 hours. Clearance and volume of distribution remained constant with dose. The time to first occurrence of Cmax (tmax) for oral eletriptan was approximately 1 hour and was unaffected by dose. Comparison of AUC values suggested an absolute bioavailability of approximately 50%. A linear PK/PD model, fitted to the data, predicted small, transient elevations in diastolic blood pressure following eletriptan doses > or = 60 mg. These effects were considered unlikely to be clinically significant. Eletriptan was well tolerated, and treatment-related adverse events were mild to moderate and transient. These PK properties should result in eletriptan having a rapid onset and sustained duration of action in terms of migraine efficacy.
5-HT1b
Triptans
Migraine
Sumatriptan
Zolmitriptan
Moclobemide
Beta-blockers
Antidepressants
Eleptriptan (Relpax)
Migraine prophylaxis
Venlafaxine/headaches
Eleptriptan (Relpax): review
Sumatriptan (Imitrex, Imigran)
Triptans, migraine and depression
Eleptriptan (Relpax) v sumatriptan


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