Desvenlafaxine
Medication used to treat major depressive disorder
From Wikipedia, the free encyclopedia
Desvenlafaxine, sold under the brand name Pristiq among others, is a medication used to treat depression.[4] It is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class and is taken by mouth.[4] It is recommended that the need for further treatment be occasionally reassessed.[4] Studies have shown similar effectiveness compared to its parent compound venlafaxine.[5][6]
des-ven-lə-FAK-seen
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| Pronunciation | /dɛsˌvɛnləˈfæksiːn/ des-ven-lə-FAK-seen |
| Trade names | Pristiq, Desfax, Ellefore, others |
| Other names | O-desmethylvenlafaxine, WY-45233 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a608022 |
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| Routes of administration | By mouth |
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| Bioavailability | 80% |
| Protein binding | Low (30%) |
| Metabolism | CYP2C19,[3] CYP3A4, (CYP2D6 is not involved) |
| Elimination half-life | 11 h |
| Excretion | 45% excreted unchanged in urine |
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| ECHA InfoCard | 100.149.615 |
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| Formula | C16H25NO2 |
| Molar mass | 263.381 g·mol−1 |
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Common side effects include dizziness, trouble sleeping, increased sweating, constipation, sleepiness, anxiety, and sexual problems.[4] Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and high blood pressure.[4] There is a high risk of withdrawal syndrome which may occur if the dose is decreased or the medication is completely stopped.[4][7] It is unclear if use during pregnancy or breastfeeding is safe.[8]
Desvenlafaxine was approved for medical use in the United States in 2008.[4] In Europe its application for use was denied in 2009, although has since been approved for Spain and Germany.[9] In 2023, it was the 189th most commonly prescribed medication in the United States, with more than 2 million prescriptions.[10][11]
Medical uses
Desvenlafaxine is primarily used as a treatment for major depressive disorder.[12] Use has only been studied up to 8 weeks.[4] Multiple studies have shown comparable effectiveness to venlafaxine as well as a lower rate of nausea.[5][6] Other studies have shown it to be either less effective[9] or more effective[13] than venlafaxine.
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.[14]
Desvenlafaxine improves the HAM-D17 score[15] and measures of well-being such as the Sheehan Disability Scale (SDS) and 5-item World Health Organization Well-Being Index (WHO-5).[16]
Desvenlafaxine may also be prescribed off label for the treatment of hot flashes.[17] A review of studies in 2014 found a 55% - 69% reduction in number of hot flashes.[18]
Adverse effects
Frequency of adverse effects:[12][19][20]
Very common adverse effects include:
- Nausea
- Headache
- Dizziness
- Dry mouth
- Hyperhidrosis
- Diarrhea
- Insomnia
- Constipation
- Fatigue
Common adverse effects include:
- Tremor
- Blurred vision
- Mydriasis
- Decreased appetite
- Sexual dysfunction
- Insomnia
- Anxiety
- Elevated cholesterol and triglycerides
- Proteinuria
- Vertigo
- Feeling jittery
- Asthenia
- Nervousness
- Hot flush
- Irritability
- Abnormal dreams
- Urinary hesitation
- Yawning
- Rash
Uncommon adverse effects include:
- Hypersensitivity
- Syncope
- Depersonalization
- Hypomania
- Withdrawal syndrome
- Urinary retention
- Epistaxis (nose bleed)
- Alopecia (hair loss)
- Orthostatic hypotension
- Peripheral coldness
Rare adverse effects include:
- Hyponatraemia (low blood sodium)
- Seizures
- Extrapyramidal side effects
- Hallucinations
- Angioedema
- Photosensitivity reaction
- Stevens–Johnson syndrome
Common adverse effects whose intensity is unknown include:
- Abnormal bleeding (gastrointestinal bleeds)
- Narrow-angle glaucoma
- Mania
- Interstitial lung disease
- Eosinophilic pneumonia
- Hypertension
- Suicidal behavior and thoughts
- Serotonin syndrome
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.[21] 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.[22]
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.[24]
The FDA approved the drug for antidepressant use in February 2008, and was to be available in US pharmacies in May 2008.[25]
In March 2017, the generic form of the drug was made available in the US.[citation needed]
Canada
On February 4, 2009, Health Canada approved use of desvenlafaxine for treatment of depression.[26][27]
European Union
In 2009, an application to market desvenlafaxine for major depressive disorder in the European Union was declined.[9] In 2012, Pfizer received authorization in Spain to market desvenlafaxine for the disorder.[28][29] In August 2022, following a 14-year approval process, desvenlafaxine was brought to the market for the disorder in Germany.[30] Desvenlaflaxine has been available in Italy since 2022.
Australia
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.[31]
