Selective serotonin reuptake inhibitor (SSRI)

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Contents

Mechanism of Action

Selective Serotonin Reuptake Inhibitors (SSRIs) exert their actions by inhibiting the CNS presynaptic neuronal reuptake of serotonin. This increases the concentration of serotonin in the synaptic cleft and the potential of serotonergic binding at postsynaptic receptors. While SSRIs have been shown to weakly inhibit the reuptake of norepinephrine and dopamine, these effects are often considered clinically insignificant. Long term SSRI use has been associated with down regulation of norepinephrine receptors in the brain. SSRIs have side effect profiles that are generally considered favorable compared to other classes due to their lack of anticholinergic activity and their lack of monoamine oxidase inhibition[1].

Serotonin Syndrome

Serotonin Syndrome is one of the possible adverse effects of SSRIs. Due to the reduced reuptake of serotonin in CNS, the concentration of serotonin increases.The higher serotonin level causes "Serotonin Syndrome". The symptoms may include confusion, seizures, restless, dyskinesia and severe hypertension as well as less severe symptoms. The risk of this uncommon adverse effect can be augmented by concomitant use of other medications which potentiate serotonin activity or decrease the metabolism of serotonin ie. monoamine oxidase inhibitors(MAOIs).[1][2]

Medical Uses

FDA Approved Indications:

Non FDA Approved Indications[9]:

FDA Black Box Warning

On October 15, 2004 the FDA mandated the inclusion of a black box warning in the package inserts of all antidepressants outlining the potential for increased suicidal ideations and behavior in children and adolescents who use these medications.A Patient Medication Guide(MedGuide)concerning this risk is also required to be dispensed with each filling of an antidepressant medication. The regulations have been created due to recent findings in the literature. [10]

Available Medications in this Class

Complete Medication Classification List

References

  1. ↑ 1.0 1.1 Dipiro JT, Talbert RL, Yee GC, Matzke GR, Wells BG, Posey LM. Pharmacotherapy: A Pathophysiologic Approach. 5th Edition ed. New York, NY: The McGraw-Hill Companies, Inc 2002.
  2. ↑ Lane R and Baldwin D. Selective serotonin reuptake inhibitor-induced serotonin syndrome:review.J Clin Psychopharmacol 17(3):208-221(1997).
  3. ↑ 3.0 3.1 Forest Pharmaceutials. Lexapro® (escitalopram oxalate) Package Insert. St. Louis, MO September 2006.
  4. ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 GlaxoSmithKline. Paxil® (paroxetine hydrochloride) Package Insert. Research Triangle Park, NC July 2006.
  5. ↑ 5.0 5.1 5.2 5.3 5.4 Eli Lilly. Prozac® (fluoxetine) Package Insert. Indianapolis, IN December 4, 2006.
  6. ↑ Forest Pharmaceuticals. Celexa® (citalopram hydrobromide) Package Insert. St Louis, MO September 2006.
  7. ↑ 7.0 7.1 7.2 7.3 7.4 Pfizer. Zoloft® (sertraline hydrochloride) Package Insert. New York, NY October 2002.
  8. ↑ PurePac Pharmaceutical Co. Fluvoxamine Maleate Package Insert. Elizabeth, NJ October 2000.
  9. ↑ Lacy C, Armstrong L, Goldman M, Lance L. Drug Information Handbook 11th edition: APhA 2003.
  10. ↑ Tiihonen J, Lonnqvist J, Wahlbeck K, Klaukka T, Tanskanen A, Haukka J. Antidepressants and the risk of suicide, attempted suicide, and overall mortality in a nationwide cohort. Archives of general psychiatry. 2006 Dec;63(12):1358-67.

External Links

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