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Saturday, March 7, 2015

Desvenlafaxine (brand name: Pristiq), also known as O-desmethylvenlafaxine, is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class developed and marketed by Wyeth (now part of Pfizer). Desvenlafaxine is a synthetic form of the major active metabolite of venlafaxine (sold under the brand names Effexor and Efexor). It is being targeted as the first non-hormonal based treatment for menopause.

§Medical uses


Desvenlafaxine

Desvenlafaxine's primary use in medicine is in the treatment of major depressive disorder.

§Adverse effects


Desvenlafaxine

Adverse effect incidence

Very common (>10% incidence) adverse effects include:

Common (1-10% incidence) adverse effects include:

Uncommon (0.1-1% incidence) adverse effects include:

Rare (<0.1% incidence) adverse effects include:

Unknown frequency adverse effects include:

§Pharmacology


Desvenlafaxine

Desvenlafaxine is a synthetic form of the isolated major active metabolite of venlafaxine, and is categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI). When most normal metabolizers take venlafaxine, approximately 70% of the dose is metabolized into desvenlafaxine, so the effects of the two drugs are expected to be very similar. It works by blocking the "reuptake" transporters for key neurotransmitters affecting mood, thereby leaving more active neurotransmitters in the synapse. The neurotransmitters affected are serotonin (5-hydroxytryptamine) and norepinephrine (noradrenaline). It is approximately 10 times more potent at inhibiting serotonin uptake than norepinephrine uptake.

The molecule resembles hordenine with additions.

§Approval status



§United States

Wyeth announced on 23 January 2007 that it received an "approvable" letter from the Food and Drug Administration for desvenlafaxine. Final approval to sell the drug was contingent on a number of things, including:

  • a satisfactory FDA inspection of Wyeth's Guayama, Puerto Rico facility, where the drug is to be manufactured;
  • several postmarketing surveillance commitments, and follow-up studies on low-dose use, relapse, and use in children;
  • clarity by Wyeth around the company's product education plan for physicians and patients;
  • approval of desvenlafaxine's proprietary name, Pristiq.

The FDA approved the drug for antidepressant use in February 2008, and was to be available in US pharmacies in May 2008.

§Canada

On February 4, 2009, Health Canada approved use of desvenlafaxine for treatment of depression in Canada. Pristiq is now available in Canadian pharmacies.

§European Union

In 2008, Wyeth withdrew its application for Ellefore, the product under review for treatment of major depressive disorder in the European Union. In 2012, Pfizer received authorization in Spain to market Pristiq for such disorder under 50mg and 100mg tablets.

§Clinical efficacy



In clinical trials, desvenlafaxine demonstrated a significant superiority to placebo both in changes from baseline in the HAM-D17 score and in measures of well being such as the Sheehan Disability Scale (SDS) and 5-item World Health Organization Well-Being Index (WHO-5).

§References



§External links



  • Pfizer's Pristiq site for U.S. residents


 
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