Chemistry:Ditan

From HandWiki
Short description: Drug class
Ditan
Drug class
Lasmiditan skeletal.svg
Lasmiditan
Class identifiers
UseMigraine
Biological target5-HT1F receptor

Ditans are a class of abortive medication for the treatment of migraines.[1] The first ditan, Eli Lilly's lasmiditan, was approved by the FDA in 2019.

Ditans selectively bind to the 5-HT1F receptor subtype. A number of triptans have been shown to act on this subtype as well, but only after their affinity for 5-HT1B and 5-HT1D has been made responsible for their anti-migraine activity. The lack of affinity for these receptors might result in fewer side effects related to vasoconstriction compared to triptans in susceptible patients, such as those with ischemic heart disease, Raynaud's phenomenon or after a myocardial infarction.[2] A 1998 review has found such side effects to rarely occur in most patients taking triptans.[3][4]

One clinical trial showed that 200 mg lasmiditan provided pain freedom by 2 hours in 32% of individuals with migraine attacks of moderate or severe intensity, and 100 mg lasmiditan did so in 28%, compared with 15% after a placebo.[5] Subsequently, these results were confirmed in another trial.[6]

References

  1. "Migraine Pathophysiology.". Headache 107: 1–6. 2020. doi:10.1016/j.pediatrneurol.2019.12.014. PMID 32192818. 
  2. "Molecule of the Month July 2010: Lasmiditan hydrochloride". Prous Science. http://www.prous.com/molecules/default.asp?ID=198. Retrieved 2011-08-03. 
  3. Dahlöf, CG; Mathew, N (1998). "Cardiovascular safety of 5HT1B/1D agonists--is there a cause for concern?". Cephalalgia: An International Journal of Headache 18 (8): 539–45. doi:10.1046/j.1468-2982.1998.1808539.x. PMID 9827245. 
  4. Mutschler, Ernst; Geisslinger, Gerd; Kroemer, Heyo K.; Schäfer-Korting, Monika. Arzneimittelwirkungen. Wissenschaftliche Verlagsgesellschaft. 
  5. Kuca, B; Silberstein, SD; Wietecha, L; Berg, PH (December 11, 2018). "Lasmiditan is an effective acute treatment for migraine: a phase 3 randomised stuty.". Neurology 91 (24): e2222–e2232. doi:10.1212/WNL.0000000000006641. PMID 30446595. 
  6. Goadsby, PJ; Wietecha, LA; Dennehy, EB; Kuca, B; Case, MG; Aurora, SK; Gaul, C (Jul 1, 2019). "Phase 3 randomized, placebo-controlled, double-blind study of lasmiditan for acute treatment of migraine.". Brain 142 (7): 1894–1904. doi:10.1093/brain/awz134. PMID 31132795.