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Combined reuptake inhibitors and receptor blockers

Dual-action antidepressants — classed as combined reuptake inhibitors and receptor blockers — relieve depression symptoms and boost your mood. Discover how they work and what side effects they may cause.

By Mayo Clinic staff

Certain brain chemicals called neurotransmitters are associated with depression, including the neurotransmitters serotonin (ser-oh-TOE-nin) and norepinephrine (nor-ep-ih-NEF-rin). Research suggests that abnormalities in neurotransmitter activity can affect mood and behavior.

How combined reuptake inhibitors and receptor blockers work

Combined reuptake inhibitors and receptor blockers are dual-action antidepressants. That is, they act on brain cells in two ways — both by inhibiting the reabsorption (reuptake) of neurotransmitters into nerve cells and by blocking nerve cell receptors. This leaves more of these neurotransmitters available in the brain, which boosts mood.

Antidepressants, in general, may also work by playing a neuroprotective role in how they relieve anxiety and depression. It's thought that antidepressants may increase the effects of brain receptors that help nerve cells keep sensitivity to glutamate — an organic compound of a nonessential amino acid — in check. This increased support of nerve cells lowers glutamate sensitivity, providing protection against the glutamate overwhelming and exciting key brain areas related to anxiety and depression.

Therapeutic effects of antidepressants may vary in people, due in part to each person's genetic makeup. It's thought that people's sensitivity to antidepressant effects, especially selective serotonin reuptake inhibitor effects, can vary depending on:

  • How each person's serotonin reuptake receptor function works
  • His or her alleles — the parts of chromosomes that determine inherited characteristics, such as height and hair color, which combine to make each person unique

Antidepressant medications are often the first treatment choice for adults with moderate or severe depression, sometimes along with psychotherapy. Although antidepressants may not cure depression, they can help you achieve remission — the disappearance or nearly complete reduction of depression symptoms.

Combined reuptake inhibitors and receptor blockers approved to treat depression

Here are the combined inhibitors and blockers approved by the Food and Drug Administration specifically to treat depression:

  • Trazodone
  • Nefazodone
  • Maprotiline

These antidepressants are available only in generic form. The brand-name versions are no longer manufactured for various reasons.

Although trazodone's mechanism of action leads to its classification as a combined reuptake inhibitor and receptor blocker, it is a triazolopyridine antidepressant. Trazodone often is prescribed along with other antidepressants because of its sleep-inducing effect. The chemical structure of triazolopyridines is unrelated to that of other antidepressant types.

Some of these medications may also be used to treat conditions other than depression.

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References
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  2. Questions and answers on antidepressant use in children, adolescents, and adults. U.S. Food and Drug Administration. http://www.fda.gov/cder/drug/antidepressants/QA20070502.htm. Accessed Sept. 29, 2008.
  3. Hall-Flavin DK (expert opinion). Mayo Clinic, Rochester, Minn. Oct. 1, 2008.
  4. Orap (prescribing information). Sellersville, Pa.: Gate Pharmaceuticals; 2005. http://www.gatepharma.com/ORAP/orapscriptinfo.pdf. Accessed Oct. 15, 2008.
  5. Carbatrol (prescribing information). Wayne, Pa.: Shire US; 2007. http://www.carbatrol.com/Assets/PI.pdf. Accessed Oct. 10, 2008.
  6. Tegretol (prescribing information). East Hanover, N.J.: Novartis Pharmaceuticals; 2008. http://www.pharma.us.novartis.com/product/pi/pdf/tegretol.pdf. Accessed Oct. 3, 2008.
  7. Halcion (prescribing information). New York, N.Y.: Pharmacia and Upjohn Co.; 2008. http://www.fda.gov/cder/foi/label/2008/017892s038lbl.pdf. Accessed Oct. 3, 2008.
  8. Single interactions table. Micromedex Healthcare Series. http:www.micromedex.com. Accessed Oct. 14, 2008.
  9. Antidepressants: Selecting one that's right for you. MayoClinic.com. http://www.mayoclinic.com/health/antidepressants/HQ01069. Accessed Oct. 16, 2008.
  10. Trazodone hydrochloride (prescribing information). Pomona, N.Y.: Barr Laboratories; 2008. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=7039. Accessed Nov. 9, 2008.
  11. Single interactions table. Micromedex Healthcare Series. http:www.micromedex.com. Accessed Nov. 9, 2008.

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Dec. 10, 2008

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