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Desvenlafaxine is a synthetic phenethylamine bicyclic derivative with antidepressant activity. Desvenlafaxine is a selective reuptake inhibitor of serotonin and norepinephrine due to its high binding affinities to the pre-synaptic serotonin and norepinephrine transporters. By blocking both transporters, this agent prolongs neurotransmitter activities of both serotonin and norepinephrine, thereby alleviating depressive state.
O-Desmethylvenlafaxine is a metabolite of Venlafaxine. Desvenlafaxine (brand name: Pristiq), also known as O-desmethyl venlafaxine, is an antidepressant of the serotonin-norepinephrine reuptake inhibitor 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 Effexor). It is being targeted as the first non-hormonal based treatment for menopause.
Mechanism of Action of Desvenlafaxine
Desvenlafaxine, the major active metabolite of venlafaxine, is a selective serotonin and norepinephrine reuptake inhibitor. The clinical effect of desvenlafaxine is thought to occur via potentiation of serotonin and norepinephrine in the central nervous system. Unlike venlafaxine, desvenlafaxine is thought to have a differential serotonergic and noradrenergic activity profile.
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The exact mechanism of antidepressant action of desvenlafaxine has not been fully elucidated but appears to be associated with the drug’s potentiation of serotonergic and noradrenergic activity in the CNS. Like venlafaxine and duloxetine, desvenlafaxine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake; however, inhibition of dopamine reuptake at concentrations that inhibit serotonin and norepinephrine reuptake appears unlikely in most patients. The drug does not inhibit monoamine oxidase (MAO) and has not demonstrated a significant affinity for muscarinic cholinergic, H1-histaminergic, alpha1-adrenergic, dopaminergic, gamma-aminobutyric acid (GABA), glutamate, and opiate receptors in vitro.
Indications of Desvenlafaxine
- Desvenlafaxine is indicated for the treatment of major depressive disorder in adults
- Major Depressive Disorder (MDD)
- Menopausal Hot Flushes
- Major Depressive Disorder
- ADHD
- Anxiety
- Bipolar Disorder
- Depression
- Fibromyalgia
- Hot Flashes
- Narcolepsy
- Neuralgia
- Obesity
- Panic Disorder
- Post Traumatic Stress Disorder
- Postmenopausal Symptoms
- Somatoform Pain Disorder
Therapeutic Uses of Desvenlafaxine
- Antidepressive Agents; Neurotransmitter Uptake Inhibitors
- Used to treat major depressive, generalized anxiety, social anxiety, and panic disorders /Desvenlafaxine succinate monohydrate/
- Like some other selective serotonin and norepinephrine reuptake inhibitors (SNRIs) and selective serotonin reuptake inhibitors (SSRIs), desvenlafaxine succinate has been studied for the management of vasomotor symptoms in postmenopausal women. /NOT included in US product labeling/
- Desvenlafaxine succinate is used in the treatment of major depressive disorder in adults. /Included in US product labeling/
- Recent reviews have questioned whether the serotonin-norepinephrine reuptake inhibitor (SNRI) desvenlafaxine succinate offers any practical clinical advantages over existing SNRIs. The following case is one instance where it appears that this SNRI offers unique safety and benefit.
- Presented is a case report of a patient with Gilbert’s syndrome, longstanding social phobia, and more recent depressive disorder not otherwise specified, who was found to have elevated liver transaminases when prescribed both duloxetine and venlafaxine. The patient subsequently responded to desvenlafaxine but without liver abnormalities.
- In this patient with Gilbert’s Syndrome, desvenlafaxine’s lack of metabolism through the cytochrome P450 (CYP) 2D6 pathway may explain the avoidance of these abnormalities and thus suggests a possible therapeutic role for this SNRI in similarly susceptible patients.
Contraindications of Desvenlafaxine
- Syndrome of Inappropriate Antidiuretic Hormone Secretion
- High cholesterol
- The high amount of triglyceride in the blood
- Low amount of sodium in the blood
- Increased risk of bleeding due to a clotting disorder
- Increased risk of bleeding
- Behaving with Excessive Cheerfulness and Activity
- Mild Degree of Mania
- Manic-Depression
- Having thoughts of suicide
- Neuroleptic Malignant Syndrome
- Serotonin syndrome – adverse drug interaction
- Closed-angle glaucoma
- High blood pressure
- Heart attack within the last 30 days
- Disorder of the Blood Vessels of the Brain
- Bleeding
- Liver problems
- Seizures
- Lung Tissue Problems
- Risk of angle-closure glaucoma due to narrow-angle of the anterior chamber of the eye
- Chronic kidney disease stage 3A (moderate)
- Chronic kidney disease stage 3B (moderate)
- Chronic kidney disease stage 4 (severe)
- Chronic kidney disease stage 5 (failure)
- Allergies to Venlafaxine Analogues
Dosage of Desvenlafaxine
Depression
- 50 mg orally once a day, with or without food
- Doses of 10 to 400 mg/day were studied in clinical trials.
- There is no evidence that doses greater than 50 mg per day provide additional benefit.
- Side effects and discontinuations were more common at higher doses.
- Efficacy in patients with the major depressive disorder was established in 4 short-term and 2 maintenance studies.
Side Effects of Desvenlafaxine
The most common
- Constipation
- abnormal dreams
- difficulty concentrating
- sexual problems (such as decreased sex drive, difficulty getting an erection, or difficulty having an orgasm)
- tingling, burning, or prickly sensations
- trembling or shaking
- decreased interest in sexual intercourse
- sleepiness or unusual drowsiness
- clumsiness or unsteadiness
- dizziness
- drowsiness
- dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
- a light-headed feeling, like you, might pass out;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- A headache.
- Skin rashes.
- Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Serious
- agitation
- anxiety
- behavioral changes, including aggressiveness, angry outbursts, bizarre behavior, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
- signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
- sleepwalking
Drug Interactions of Desvenlafaxine
Desvenlafaxine may interact with following drugs, supplements & may change the efficacy of drugs
- alcohol
- antipsychotics (e.g., haloperidol, quetiapine, olanzapine, risperidone)
- “azole” antifungal medications (e.g., fluconazole, ketoconazole, itraconazole)
- axitinib
- benzodiazepines (e.g., lorazepam, diazepam, clonazepam)
- bromocriptine
- cabergoline
- cyclobenzaprine
- desipramine
- dextromethorphan
- epinephrine
- linezolid
- lithium
- nefazodone
- norepinephrine
- MAO inhibitors (e.g., tranylcypromine, phenelzine, selegiline)
- midazolam
- NSAIDs (e.g., ibuprofen, indomethacin, naproxen)
- narcotic pain medications (e.g., codeine, morphine)
- phenobarbital
- pseudoephedrine
- saxagliptan
- sedating antihistamines (e.g., diphenhydramine, hydroxyzine)
- serotonin antagonists (e.g., granisetron, ondansetron)
- SSRIs (e.g., citalopram, paroxetine, escitalopram)
- St. John’s wort
- sibutramine
- simeprevir
- tramadol
- trazodone
- tricyclic antidepressants (e.g., amitriptyline, imipramine)
- triptan medications (e.g., naratriptan, rizatriptan, sumatriptan)
- tryptophan supplements
- venlafaxine
- warfarin
Pregnancy & Lactation
FDA Pregnancy Category – C
Pregnancy
Newborns whose mothers take medications such as desvenlafaxine during the third trimester of pregnancy may experience complications that require prolonged hospitalization. These complications normally resolve over time.
This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately. Do not stop taking this medication without talking to your doctor. If this medication is stopped, it should be stopped gradually as directed by your doctor.
Lactation
This medication passes into breast milk. If you breastfeeding and are taking desvenlafaxine, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. If your baby experiences breathing problems, feeding problems, seizures, tense or overly relaxed muscles, jitters, or constant crying, contact your doctor as soon as possible.
References
- https://www.drugs.com/mtm/desvenlafaxine.html
- https://chealth.canoe.com/drug/getdrug/pristiq
- https://www.drugs.com/cons/desvenlafaxine.html
- https://www.webmd.com/drugs/2/drug-163933/desvenlafaxine-oral/details/list-contraindications
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