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Correlation Between Lipophilicity and Triptan Outcomes
Julio Pascual, MD; Pedro Munoz MD
Posted: February 2005  
Headache 2005;45:3-6

Background:   It has been suggested that triptans achieving higher central nervous system (CNS) levels should have an advantage in efficacy, if central actions are important.

Objective:   Our aim was to correlate the efficacy and tolerability results of triptans with their lipophilicity.

Methods:   Data for response and pain free at 2 hours, recurrent, adverse events (AE), CNS AE, and chest symptoms taken from Ferrari et al’s meta-analysis publications for the recommended doses of oral triptans were correlated with their lipophilicity coefficients.

Results:   We found no significant correlation between lipophilicity coefficients and any of the analyzed parameters. There was, however, some correlation between lipophilicity and CNS AE and, to a lesser degree, with a reduction in recurrence rate, suggesting almost no correlation between lipophilicity and efficacy variables.

Conclusions:   According to this analysis, a higher lipophilicity does not seem crucial to improve triptan efficacy. This physico-chemical property, however, correlates with higher CNS AE and, possible, lower recurrence rates.