title: Correlation between lipophilicity and triptan outcomes.
abstract: 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, recurrence, 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 (logD(pH)7.4 = -2.1 almotriptan < -1.5 sumatriptan < -1.0 zolmitriptan < -0.7 rizatriptan < -0.2 naratriptan < 0.5 eletriptan).
  
  
  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 (P = .09, r = 0.74) and, to a lesser degree, with a reduction in recurrence rate (r = -0.36). The r values for response and pain free with placebo correction ranged from 0.04 to 0.34, 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, possibly, lower recurrence rates.
authors.affiliation: University Hospital M de Valdecilla, 39008 Santander, Spain.
authors.forename: Julio
authors.initials: J
authors.lastname: Pascual
authors.forename: Pedro
authors.initials: P
authors.lastname: Muñoz
mesh_terms: D002493:Central Nervous System Diseases / Q000139:chemically induced; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006801:Humans; D007211:Indoles / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D008881:Migraine Disorders / Q000188:drug therapy*; D023303:Oxazolidinones / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D010880:Piperidines / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D017366:Serotonin Receptor Agonists / Q000009:adverse effects / Q000737:chemistry* / Q000627:therapeutic use*; D013223:Statistics as Topic; D018170:Sumatriptan / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D016896:Treatment Outcome; D014230:Triazoles / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use; D014363:Tryptamines
chemical_list: D007211:Indoles; D023303:Oxazolidinones; D010880:Piperidines; D017366:Serotonin Receptor Agonists; D014230:Triazoles; D014363:Tryptamines; C409045:almotriptan; C089750:zolmitriptan; C093622:rizatriptan; D018170:Sumatriptan; C106783:naratriptan