Which antidepressants with 5-HT1 receptor agonist activity are available for the treatment of fibromyalgia?

Updated: Apr 23, 2020
  • Author: Chad S Boomershine, MD, PhD, CPI, CPT; Chief Editor: Herbert S Diamond, MD  more...
  • Print

Currently available drugs with 5-HT1a receptor agonist activity include buspirone (Buspar), vilazodone (Viibryd), and vortioxetine (Brintellix). Buspirone is indicated as an anti-anxiety agent and is also used off-label to augment antidepressant activity, while vilazodone and vortioxetine are both indicated only for the treatment of depression. The most common side effect of both vilazodone and vortioxetine is nausea, so both should be taken with food. All three medications should be started in the morning, since they can cause activation.

Bupropion is structurally different from other antidepressants and its ability to reduce pain is due to its inhibition of the neuronal reuptake of norepinephrine and dopamine. [143, 144] While bupropion is available in an extended release (ER) preparation that allows for once daily dosing, it is activating and can cause or worsen insomnia, so patients should start with immediate-release tablets in the morning with gradual up-titration, or switch to the ER preparation as tolerated. The activating aspect of bupropion can be particularly helpful for fatigue, which is common in fibromyalgia.

Did this answer your question?
Additional feedback? (Optional)
Thank you for your feedback!