Desvenlafaxine
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Desvenlafaxine, sold under the brand name Pristiq among others, is a medication used to treat depression. It is an
antidepressant Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...
of the serotonin-norepinephrine reuptake inhibitor (SNRI) class and is taken by mouth. It is recommended that the need for further treatment be occasionally reassessed. It may be less effective than its parent compound
venlafaxine Venlafaxine, sold under the brand name Effexor among others, is an antidepressant medication of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. It is used to treat major depressive disorder, generalized anxiety disorder, panic di ...
, although some studies have found comparable efficacy. Common side effects include dizziness,
trouble sleeping Insomnia, also known as sleeplessness, is a sleep disorder in which people have trouble sleeping. They may have difficulty falling asleep, or staying asleep as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, ...
, increased sweating, constipation, sleepiness,
anxiety Anxiety is an emotion which is characterized by an unpleasant state of inner turmoil and includes feelings of dread over anticipated events. Anxiety is different than fear in that the former is defined as the anticipation of a future threat wh ...
, and sexual problems. Serious side effects may include
suicide Suicide is the act of intentionally causing one's own death. Mental disorders (including depression, bipolar disorder, schizophrenia, personality disorders, anxiety disorders), physical disorders (such as chronic fatigue syndrome), and s ...
in those under the age of 25,
serotonin syndrome Serotonin syndrome (SS) is a group of symptoms that may occur with the use of certain serotonergic medications or drugs. The degree of symptoms can range from mild to severe, including a potentiality of death. Symptoms in mild cases include high ...
, bleeding,
mania Mania, also known as manic syndrome, is a mental and behavioral disorder defined as a state of abnormally elevated arousal, affect, and energy level, or "a state of heightened overall activation with enhanced affective expression together wit ...
, and
high blood pressure Hypertension (HTN or HT), also known as high blood pressure (HBP), is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. High blood pressure usually does not cause symptoms. Long-term high bl ...
. A
withdrawal syndrome Drug withdrawal, drug withdrawal syndrome, or substance withdrawal syndrome, is the group of symptoms that occur upon the abrupt discontinuation or decrease in the intake of pharmaceutical or recreational drugs. In order for the symptoms of wit ...
may occur if the dose is decreased or the medication completely stopped. It is unclear if use during
pregnancy Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ca ...
or
breastfeeding Breastfeeding, or nursing, is the process by which human breast milk is fed to a child. Breast milk may be from the breast, or may be expressed by hand or pumped and fed to the infant. The World Health Organization (WHO) recommends that br ...
is safe. Desvenlafaxine was approved for medical use in the United States in 2008. In Europe its application for use was denied in 2009. 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 3million prescriptions.


Medical uses

Desvenlafaxine is primarily used as a treatment for
major depressive disorder Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities. Introdu ...
. Use has only been studied up to 8 weeks. It may be less effective than
venlafaxine Venlafaxine, sold under the brand name Effexor among others, is an antidepressant medication of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. It is used to treat major depressive disorder, generalized anxiety disorder, panic di ...
, although some studies have found comparable efficacy with a lower rate of nausea. 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. Desvenlafaxine improves the HAM-D17 score and measures of well-being such as the Sheehan Disability Scale (SDS) and 5-item World Health Organization Well-Being Index (WHO-5).


Adverse effects

Frequency of adverse effects: Very common adverse effects include: *Nausea *Headache *Dizziness *Dry mouth *
Hyperhidrosis Hyperhidrosis is a condition characterized by abnormally increased sweating, in excess of that required for regulation of body temperature. Although primarily a benign physical burden, hyperhidrosis can deteriorate quality of life from a psychologi ...
*Diarrhea *Insomnia *Constipation *Fatigue Common adverse effects include: *Tremor *Blurred vision *
Mydriasis Mydriasis is the dilation of the pupil, usually having a non-physiological cause, or sometimes a physiological pupillary response. Non-physiological causes of mydriasis include disease, trauma, or the use of certain types of drugs. Normally, as ...
*Decreased appetite *Sexual dysfunction *Insomnia *Anxiety *Elevated cholesterol and triglycerides *
Proteinuria Proteinuria is the presence of excess proteins in the urine. In healthy persons, urine contains very little protein; an excess is suggestive of illness. Excess protein in the urine often causes the urine to become foamy (although this symptom ma ...
*Vertigo *Feeling jittery *
Asthenia Weakness is a symptom of a number of different conditions. The causes are many and can be divided into conditions that have true or perceived muscle weakness. True muscle weakness is a primary symptom of a variety of skeletal muscle diseases, i ...
*Nervousness *Hot flush *Irritability *Abnormal dreams *Urinary hesitation *Yawning *Rash Uncommon adverse effects include: *Hypersensitivity * Syncope *Depersonalization *
Hypomania Hypomania (literally "under mania" or "less than mania") is a mental and behavioural disorder, characterised essentially by an apparently non-contextual elevation of mood (euphoria) that contributes to persistently disinhibited behaviour. The ...
*Withdrawal syndrome *
Urinary retention Urinary retention is an inability to completely empty the bladder. Onset can be sudden or gradual. When of sudden onset, symptoms include an inability to urinate and lower abdominal pain. When of gradual onset, symptoms may include loss of bladd ...
*Epistaxis (nose bleed) *Alopecia (hair loss) *
Orthostatic hypotension Orthostatic hypotension, also known as postural hypotension, is a medical condition wherein a person's blood pressure drops when standing up or sitting down. Primary orthostatic hypertension is also often referred to as neurogenic orthostatic hyp ...
*Peripheral coldness Rare adverse effects include: * Hyponatraemia (low blood sodium) *Seizures * Extrapyramidal side effects *Hallucinations *
Angioedema Angioedema is an area of swelling ( edema) of the lower layer of skin and tissue just under the skin or mucous membranes. The swelling may occur in the face, tongue, larynx, abdomen, or arms and legs. Often it is associated with hives, which ...
*Photosensitivity reaction *
Stevens–Johnson syndrome Stevens–Johnson syndrome (SJS) is a type of severe skin reaction. Together with toxic epidermal necrolysis (TEN) and Stevens–Johnson/toxic epidermal necrolysis (SJS/TEN), it forms a spectrum of disease, with SJS being less severe. Erythema ...
Common adverse effects whose intensity is unknown include: *Abnormal bleeding (gastrointestinal bleeds) *Narrow-angle
glaucoma Glaucoma is a group of eye diseases that result in damage to the optic nerve (or retina) and cause vision loss. The most common type is open-angle (wide angle, chronic simple) glaucoma, in which the drainage angle for fluid within the eye rem ...
*
Mania Mania, also known as manic syndrome, is a mental and behavioral disorder defined as a state of abnormally elevated arousal, affect, and energy level, or "a state of heightened overall activation with enhanced affective expression together wit ...
*
Interstitial lung disease Interstitial lung disease (ILD), or diffuse parenchymal lung disease (DPLD), is a group of respiratory diseases affecting the interstitium (the tissue and space around the alveoli (air sacs)) of the lungs. It concerns alveolar epithelium, pulmo ...
*
Eosinophilic pneumonia Eosinophilic pneumonia is a disease in which an eosinophil, a type of white blood cell, accumulates in the lungs. These cells cause disruption of the normal air spaces (alveoli) where oxygen is extracted from the atmosphere. Several different kind ...
*
Hypertension Hypertension (HTN or HT), also known as high blood pressure (HBP), is a long-term medical condition in which the blood pressure in the arteries is persistently elevated. High blood pressure usually does not cause symptoms. Long-term high bl ...
*Suicidal behavior and thoughts *
Serotonin syndrome Serotonin syndrome (SS) is a group of symptoms that may occur with the use of certain serotonergic medications or drugs. The degree of symptoms can range from mild to severe, including a potentiality of death. Symptoms in mild cases include high ...


Pharmacology

Desvenlafaxine is a synthetic form of the isolated major active metabolite of
venlafaxine Venlafaxine, sold under the brand name Effexor among others, is an antidepressant medication of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. It is used to treat major depressive disorder, generalized anxiety disorder, panic di ...
, 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
neurotransmitter A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell. Neuro ...
s affecting mood, thereby leaving more active neurotransmitters in the
synapse In the nervous system, a synapse is a structure that permits a neuron (or nerve cell) to pass an electrical or chemical signal to another neuron or to the target effector cell. Synapses are essential to the transmission of nervous impulses from ...
. The neurotransmitters affected are
serotonin Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...
(5-hydroxytryptamine) and
norepinephrine Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad'', ...
(noradrenaline). It is approximately 10 times more potent at inhibiting
serotonin Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...
uptake than
norepinephrine Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad'', ...
uptake.


Approval status


United States

Wyeth announced on 23 January 2007 that it received an
approvable letter Approvable letters, and the related non-approvable letters (alternately not-approvable letters), were notifications sent out by the Food and Drug Administration (FDA) to drug manufacturers alerting them to the approval prospects of their drugs unde ...
from the
Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...
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 Guayama (, ), officially the Autonomous Municipality of Guayama ( es, Municipio Autónomo de Guayama) is a city and municipality on the Caribbean coast of Puerto Rico. As of the 2020 U.S. Census, the city had a population of 36,614. It is the ce ...
facility, where the drug is to be manufactured; *Several
postmarketing surveillance Postmarketing surveillance (PMS), also known as post market surveillance, is the practice of monitoring the safety of a pharmaceutical drug or medical device after it has been released on the market and is an important part of the science of pharmac ...
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. In March 2017, the generic form of the drug was made available in the US.


Canada

On February 4, 2009,
Health Canada Health Canada (HC; french: Santé Canada, SC)Health Canada is the applied title under the Federal Identity Program; the legal title is Department of Health (). is the Structure of the Canadian federal government#Departments, with subsidiary unit ...
approved use of desvenlafaxine for treatment of depression.


European Union

In 2009, an application to market desvenlafaxine for
major depressive disorder Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities. Introdu ...
in the European Union was declined. In 2012, Pfizer received authorization in Spain to market desvenlafaxine for the disorder. In August 2022, following a 14-year approval process, desvenlafaxine was brought to the market for the disorder in Germany.


Australia

Desvenlafaxine is classified as a schedule 4 (prescription only) drug in Australia. It was listed on th
PBS
(Pharmaceutical Benefits Scheme) in 2008 for the treatment of major depressive disorders.


See also

* Ansofaxine


References


External links

* {{Portal bar , Medicine Serotonin–norepinephrine–dopamine reuptake inhibitors Cyclohexanols Dimethylamino compounds Phenethylamines Phenols Wyeth brands Pfizer brands Tertiary alcohols Human drug metabolites Wikipedia medicine articles ready to translate Antidepressants