Abstract |
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.
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Authors | M D Ferrari |
Journal | Neurology
(Neurology)
Vol. 48
Issue 3 Suppl 3
Pg. S21-4
(Mar 1997)
ISSN: 0028-3878 [Print] United States |
PMID | 9071266
(Publication Type: Comparative Study, Journal Article, Review)
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Chemical References |
- HTR1B protein, human
- Oxazoles
- Oxazolidinones
- Receptor, Serotonin, 5-HT1B
- Receptor, Serotonin, 5-HT1D
- Receptors, Serotonin
- Serotonin Receptor Agonists
- Tryptamines
- zolmitriptan
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Topics |
- Headache
(drug therapy)
- Humans
- Migraine Disorders
(drug therapy)
- Oxazoles
(adverse effects, therapeutic use)
- Oxazolidinones
- Receptor, Serotonin, 5-HT1B
- Receptor, Serotonin, 5-HT1D
- Receptors, Serotonin
(physiology)
- Serotonin Receptor Agonists
(adverse effects, therapeutic use)
- Tryptamines
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