AHFS/Drugs.com Monograph License data US FDA: Desvenlafaxine | MedlinePlus a608022 Routes of
administration Oral | |
 | ||
Trade names Pristiq, Desfax, Ellefore Pregnancy
category AU: B2
US: C (Risk not ruled out) | ||
Desvenlafaxine (brand name: Pristiq, Desfax, Ellefore), also known as O-desmethylvenlafaxine, is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) 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. It is an example of evergreening.
Contents
Medical uses
Desvenlafaxine's primary use in medicine is the treatment of major depressive disorder.
Adverse effects
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 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.
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:
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 the disorder in 50 mg and 100 mg 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).