How Do Alpha-2 Antagonist Antidepressants Work?

Reviewed on 9/22/2021

How do alpha-2 antagonist antidepressants work?

Alpha-2 antagonist antidepressants are medications prescribed to treat depression. Alpha-2 agonist antidepressants work on the central nervous system to increase the levels and modulate the activity of norepinephrine and serotonin, chemical messengers (neurotransmitters) released by nerve cells (neurons).

Mood regulation is one of the many functions of norepinephrine and serotonin and increased levels and modulation of their activity improves mood. It is not clear how exactly alpha-2 antagonist antidepressants are effective for depression, but studies suggest they may work in the following ways to reduce depression:

  • Block alpha-2 receptors, protein molecules on the membranes of neurons that play an inhibitory role, enhancing the availability and activity of norepinephrine and serotonin. Norepinephrine stimulates the sympathetic nervous system, which results in an increase in metabolism and activity.
  • Block serotonin receptors 5HT2 and 5HT3 which increase anxiety when stimulated by serotonin. The increased level of serotonin stimulates 5HT1, which improves mood.
  • Block H1 histamine receptors which produce a calming and sedating effect.

How are alpha-2 antagonist antidepressants used?

Alpha-2 antagonist antidepressants are oral tablets approved by the FDA for the treatment of major depressive disorder in adults. In addition, alpha-2 antagonist antidepressants are used off-label in the treatment of the following conditions:

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What are side effects of alpha-2 antagonist antidepressants?

Side effects of alpha-2 antagonist antidepressants may include the following:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What are names of some alpha-2 antagonist antidepressant drugs?

Generic and brand names of alpha-2 antagonist antidepressant drugs include:

References
https://reference.medscape.com/drugs/antidepressants-alpha-2-antagonists

https://www.ncbi.nlm.nih.gov/books/NBK519059/

https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020415s023s024.pdf

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