Premium
N α ‐Methylhistamine Safety and Efficacy in Migraine Prophylaxis: Phase I and Phase II Studies
Author(s) -
MillánGuerrero Rebeca O.,
PinedaLucatero Alicia G.,
HernándezBenjamín Trujillo,
Tene Carlos E.,
Pacheco Mauro F.
Publication year - 2003
Publication title -
headache: the journal of head and face pain
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.14
H-Index - 119
eISSN - 1526-4610
pISSN - 0017-8748
DOI - 10.1046/j.1526-4610.2003.03074.x
Subject(s) - histaminergic , migraine , medicine , agonist , pharmacology , placebo , anesthesia , histamine , receptor , alternative medicine , pathology
Objective.—To study the therapeutic potential of the subcutaneous administration of N α ‐methylhistamine in migraine prophylaxis. Background.—The histamine catabolite, N α ‐methylhistamine, possesses a selective affinity for H 3 receptors. We consequently considered it viable to conduct a clinical pharmacological study to evaluate the safety and efficacy of this histaminergic H 3 agonist in migraine prophylactic treatment, which specifically may inhibit the neurogenic edema response involved in migraine pathophysiology. Methods.— Phase I. —In a clinical trial of 30 healthy volunteers, the effects of the subcutaneous administration of N α ‐methylhistamine and placebo were studied to assess undesirable symptomatic effects. Phase II .—In a clinical open study, we evaluated the efficacy of N α ‐methylhistamine in reducing headache intensity, frequency, and duration; and in decreasing analgesic intake in 18 patients with migraine. Results.— Phase I. —None of the variables studied showed significant differences ( P >.05), and no secondary effects were observed at doses below 10 ng. Phase II. —N α ‐methylhistamine, at doses of 1 to 3 ng, significantly reduced ( P <.0001) the frequency, intensity, and duration of migraine attacks, as well as the need for rescue analgesics. However, at doses greater than 3 ng, patients experienced intense headache. Conclusions.—The present study provides evidence of the safety and efficacy of N α ‐methylhistamine applied subcutaneously at doses of 1 to 3 ng twice a week.