| Clinical data | |
|---|---|
| Trade names | Pristiq, Desfax, Ellefore, others |
| Other names | O-desmethylvenlafaxine, WY-45233 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a608022 |
| License data |
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| Pregnancy category |
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| Routes of administration | By mouth |
| ATC code | |
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| Pharmacokinetic data | |
| Bioavailability | 80% |
| Protein binding | Low (30%) |
| Metabolism | CYP2C19,[1] CYP3A4, (CYP2D6 is not involved) |
| Elimination half-life | 11 h |
| Excretion | 45% excreted unchanged in urine |
| Identifiers | |
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| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.149.615 |
| Chemical and physical data | |
| Formula | C16H25NO2 |
| Molar mass | 263.381 g·mol−1 |
| 3D model (JSmol) | |
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Desvenlafaxine, sold under the brand name Pristiq among others, is a medication used to treat depression.[2] It is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class and is taken by mouth.[2] It is recommended that the need for further treatment be occasionally reassessed.[2] It may be less effective than its parent compound venlafaxine,[3] although some studies have found comparable efficacy.[4]
Common side effects include dizziness, trouble sleeping, increased sweating, constipation, sleepiness, anxiety, and sexual problems.[2] Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and high blood pressure.[2] A withdrawal syndrome may occur if the dose is decreased or the medication completely stopped.[2] It is unclear if use during pregnancy or breastfeeding is safe.[5]
Desvenlafaxine was approved for medical use in the United States in 2008.[2] In Europe its application for use was denied in 2009.[3] But it is available in Spain and Germany. In 2020, it was the 176th most commonly prescribed medication in the United States, with more than 3 million prescriptions.[6][7]
Desvenlafaxine is primarily used as a treatment for major depressive disorder.[8] Use has only been studied up to 8 weeks.[2] It may be less effective than venlafaxine,[3] although some studies have found comparable efficacy with a lower rate of nausea.[4]
Doses of 50–400 mg/day appear effective for major depressive disorder, although no additional benefit was demonstrated at doses greater than 50 mg/day, and adverse events and discontinuations were more frequent at higher doses.[9]
Desvenlafaxine improves the HAM-D17 score[10] and measures of well-being such as the Sheehan Disability Scale (SDS) and 5-item World Health Organization Well-Being Index (WHO-5).[11]
Frequency of adverse effects:[8][12][13]
Very common adverse effects include:
Common adverse effects include:
Uncommon adverse effects include:
Rare adverse effects include:
Common adverse effects whose intensity is unknown include:
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.[14] 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.[15]
| Transporter | Ki[nM][15][16] | IC50 [nM][15] |
|---|---|---|
| SERT | 40.2 | 47.3 |
| NET | 558.4 | 531.3 |
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.[18]
In March 2017, the generic form of the drug was made available in the US.
On February 4, 2009, Health Canada approved use of desvenlafaxine for treatment of depression.[19][20]
In 2009, an application to market desvenlafaxine for major depressive disorder in the European Union was declined.[3] In 2012, Pfizer received authorization in Spain to market desvenlafaxine for the disorder.[21][22] In August 2022, following a 14-year approval process, desvenlafaxine was brought to the market for the disorder in Germany.[23]
Desvenlafaxine is classified as a schedule 4 (prescription only) drug in Australia. It was listed on the PBS (Pharmaceutical Benefits Scheme) in 2008 for the treatment of major depressive disorders.
