311C90: increasing the options for therapy with effective acute antimigraine 5HT1B/1D receptor agonists.
The novel antimigraine drug 311C90 (Zomig; zolmitriptan) has a high selectivity for serotonin (5HT)1 receptors, mainly 5HT1B and 5HT1D subtypes, and in preclinical studies it has been shown to act on four different sites within the trigemino-vascular system (blockade of neurogenic inflammation by inhibition of peptide release, vasoconstriction, inhibition of neuronal depolarization at peripheral sites, and effects at central sites). Oral 311C90 has a favorable pharmacokinetic profile. It is rapidly absorbed, with 75% of maximal plasma concentration (Cmax) attained within 1 hour and good absolute oral bioavailability (approximately 40%). Clinical studies have shown 311C90 to be rapidly and consistently effective in relieving migraine headache, with initial doses of between 2.5 and 5 mg providing an optimal balance between efficacy and safety considerations. Moreover, the good tolerability of 311C90 is supported by clinical data showing that doses up to 10-fold the therapeutic dose (2.5 mg) did not raise any serious safety concerns, highlighting the favorable safety profile of this drug.
Ferrari
M D
MD
Department of Neurology, Leiden University Hospital, Netherlands.
D006261:Headache / Q000188:drug therapy; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy*; D010080:Oxazoles / Q000009:adverse effects / Q000627:therapeutic use*; D023303:Oxazolidinones; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin / Q000502:physiology*; D017366:Serotonin Receptor Agonists / Q000009:adverse effects / Q000627:therapeutic use*; D014363:Tryptamines
C470302:HTR1B protein, human; D010080:Oxazoles; D023303:Oxazolidinones; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D014363:Tryptamines; C089750:zolmitriptan