Clinical data | |
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Trade names | Pristiq, Desfax, Ellefore, others |
Other names | O-desmethylvenlafaxine, WY-45233 |
AHFS/Drugs.com | Monograph |
MedlinePlus | a608022 |
License data | |
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, [4] CYP3A4, (CYP2D6 is not involved) |
Elimination half-life | 11 h |
Excretion | 45% excreted unchanged in urine |
Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
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. [5] It is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class and is taken by mouth. [5] It is recommended that the need for further treatment be occasionally reassessed. [5] It may be less effective than its parent compound venlafaxine, [6] although some studies have found comparable efficacy. [7]
Common side effects include dizziness, trouble sleeping, increased sweating, constipation, sleepiness, anxiety, and sexual problems. [5] Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and high blood pressure. [5] A withdrawal syndrome may occur if the dose is decreased or the medication is completely stopped. [5] It is unclear if use during pregnancy or breastfeeding is safe. [8]
Desvenlafaxine was approved for medical use in the United States in 2008. [5] In Europe its application for use was denied in 2009, [6] but it is available in Spain and Germany.[ citation needed ] In 2021, it was the 178th most commonly prescribed medication in the United States, with more than 2 million prescriptions. [9] [10]
Desvenlafaxine is primarily used as a treatment for major depressive disorder. [11] Use has only been studied up to 8 weeks. [5] It may be less effective than venlafaxine, [6] although some studies have found comparable efficacy with a lower rate of nausea. [7]
Doses of 50 to 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. [12]
Desvenlafaxine improves the HAM-D17 score [13] and measures of well-being such as the Sheehan Disability Scale (SDS) and 5-item World Health Organization Well-Being Index (WHO-5). [14]
Frequency of adverse effects: [11] [15] [16]
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. [17] 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. [18]
Transporter | Ki[nM] [18] [19] | IC50 [nM] [18] |
---|---|---|
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. [21]
In March 2017, the generic form of the drug was made available in the US.[ citation needed ]
On February 4, 2009, Health Canada approved use of desvenlafaxine for treatment of depression. [22] [23]
In 2009, an application to market desvenlafaxine for major depressive disorder in the European Union was declined. [6] In 2012, Pfizer received authorization in Spain to market desvenlafaxine for the disorder. [24] [25] In August 2022, following a 14-year approval process, desvenlafaxine was brought to the market for the disorder in Germany. [26]
Desvenlafaxine is classified as a schedule 4 (prescription only) drug in Australia. It was listed on the Pharmaceutical Benefits Scheme (PBS) in 2008 for the treatment of major depressive disorders. [27]
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