Topic summary
Methysergide
Methysergide, sold under the brand names Deseril and Sansert, is a monoaminergicmedication which is used in the prevention and treatment of migraine and cluster headaches. It has been withdrawn from the market in the United States and Canada due to safety concerns. The drug has also been found to produce psychedelic effects at high doses. It is taken orally.
The drug is a prodrug of methylergometrine (methylergonovine), which circulates at levels about 10times higher than those of methysergide. Whereas methysergide is a mixed agonist of some serotonin receptors (e.g., the serotonin5-HT1 receptors) and antagonist of other serotonin receptors (e.g., the serotonin 5-HT2 receptors), methylergonovine is a non-selectiveagonist of most of the serotonin receptors, including of both the serotonin 5-HT1 and 5-HT2 receptor subgroups. Methysergide and methylergometrine are ergolines and lysergamides and are related to the ergot alkaloids.
Methysergide was first described in the literature by 1958. It is no longer recommended as a first-line therapy for migraines or cluster headaches. This is due to toxicity, such as cardiac valvulopathy, which was first reported with long-term use in the late 1960s. Ergot-based medications like methysergide fell out of favor for treatment of migraine with the introduction of the triptans in the 1980s.