Mechanism of Action of Venlafaxine
Abstract: PubMed
Uses / Indications of Venlafaxine
- For the management of major depressive disorder (MDD), generalized anxiety disorder (GAD), social anxiety disorder (social phobia), panic disorder with or without agoraphobia, vasomotor symptoms in women with breast cancer and in postmenopausal women, and neuropathic pain.
- Treatment of major depressive episodes. For prevention of recurrence of major depressive episodes
- Treatment of major depressive episodes, social and generalized anxiety disorder, panic disorder, agoraphobia. For prevention of recurrence of major depressive episodes
- Generalized Anxiety Disorder (GAD)
- Major Depressive Disorder
- Pain, Neuropathic
- Panic Disorders
- Social Anxiety Disorder
- Vasomotor Symptoms
- Anxiety and Stress
- Autism
- Depression
- Bipolar Disorder
- Bulimia
- Dissociative Identity Disorder
- Fibromyalgia
- Generalized Anxiety Disorder
- Irritable Bowel Syndrome
- Migraine
- Obsessive Compulsive Disorder
- Post Traumatic Stress Disorder
- Postpartum Depression
- Premenstrual Dysphoric Disorder
- Social Anxiety Disorder
- Somatoform Pain Disorder
- Vulvodynia
Therapeutic Uses of Venlafaxine
- Antidepressive Agents, Second-Generation; Serotonin Uptake Inhibitors
National Library of Medicine’s Medical Subject Headings online file (MeSH, 2011)
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Venlafaxine hydrochloride is used in the treatment of a major depressive disorder.
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Venlafaxine hydrochloride is used in the treatment of generalized anxiety disorder.
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Venlafaxine hydrochloride is used in the treatment of social phobia (social anxiety disorder).
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Venlafaxine has been used for the management of vasomotor symptoms in women with breast cancer and in postmenopausal women.
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Venlafaxine hydrochloride is used in the treatment of panic disorder with or without agoraphobia.
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A number of studies have indicated that selective serotonin reuptake inhibitors (SSRIs) are effective in reducing the symptomatology accompanying borderline personality disorder (BPD). The SSRIs have proven efficacious in reducing self-injury, suicidality, affective instability, rage, impulsivity, psychosis, and obsessionality.
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Fluoxetine and sertraline have been shown to be effective in clinical trials, although no single SSRI has emerged as the treatment of choice. Individuals failing one SSRI often respond to another.
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The data presented in this article indicate that venlafaxine is effective in treating borderline personality disorder (BPD) as an initial intervention and may benefit many individuals for whom fluoxetine or sertraline treatment has failed.
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Stimulant medications are the most widely accepted treatment of attention deficit hyperactivity disorder (ADHD) in spite of controversy over their use. Stimulants have consistently been shown to potentiate noradrenergic brain transmission, a property also characteristic of the recently marketed antidepressant venlafaxine. Eighteen adults who met the Utah Criteria for ADHD in adults were enrolled in an open trial of venlafaxine.
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To evaluate the efficacy and safety of venlafaxine, a new-generation antidepressant that selectively inhibits serotonin and norepinephrine reuptake, in the treatment of the premenstrual dysphoric disorder (PMDD). We conducted a randomized, double-blind, placebo-controlled, parallel-group, flexible-dose trial.
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After three screening cycles, including a single-blind placebo cycle, 164 women were randomly assigned to double-blind treatment with venlafaxine (50-200 mg/day) or placebo for four menstrual cycles.
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Primary outcome measures were the total premenstrual symptom scores as assessed by a daily symptom report (DSR) and the Hamilton Rating Scale for Depression. Venlafaxine was significantly more effective than placebo in reducing PMDD symptoms as assessed by DSR scores (P <.001 for last observation carried forward and observed analyses).
Contra-Indications of Venlafaxine
- Syndrome of Inappropriate Antidiuretic Hormone Secretion
- high cholesterol
- 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
- having thoughts of suicide
- serotonin syndrome – adverse drug interaction
- closed angle glaucoma
- Severe Uncontrolled High Blood Pressure
- heart attack within the last 30 days
- Hardening of the Liver
- liver problems
- Mild to Moderate Kidney Impairment
- seizures
- weight loss
- moderate to severe kidney impairment
- risk of angle-closure glaucoma due to narrow-angle of the anterior chamber of the eye
- Allergies to Venlafaxine Analogues
Dosage of Venlafaxine
- Strengths: 25 mg; 50 mg; 75 mg; 100 mg; 37.5 mg; 150 mg; 225 mg
Depression
Immediate release
- Initial dose: 37.5 mg orally twice a day or 25 mg orally 3 times a day
- Maintenance dose: May increase in daily increments of up to 75 mg orally at intervals of no less than 4 days
- Maximum dose: (moderately depressed outpatients): 225 mg orally per day
- Maximum dose (severely depressed inpatients): 375 mg orally per day
Extended-release
- Initial dose: 75 mg orally once a day
- Maintenance dose: May increase in daily increments of up to 75 mg orally at intervals of no less than 4 days
- Maximum dose (moderately depressed outpatients): 225 mg orally per day
- Maximum dose (severely depressed inpatients): 375 mg orally per day
Anxiety
Extended-release
- Initial dose: 75 mg orally once a day
- Maintenance dose: May increase in daily increments of 75 mg orally at intervals of no less than 4 days
- Maximum dose: 225 mg orally per day
Panic Disorder
Extended-release
- Initial dose: 37.5 mg orally once a day
- Maintenance dose: May increase dose in daily increments of 75 mg orally at intervals of no less than 7 days
- Maximum dose: 225 mg orally per day
Side Effects of Venlafaxine
The most common
- Constipation
- 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 Venlafaxine
Venlafaxine may interact with following drugs, supplements & may change the efficacy of drugs
- general anesthetics
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- aripiprazole
- baclofen
- barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- bupropion
- celecoxib
- cilostazol
- clopidogrel
- cyclosporine
- diabetes medications (e.g., chlorpropamide, metformin, nateglinide, rosiglitazone)
- diltiazem
- estrogens (e.g., conjugated estrogen, )
- glucosamine
- heparin
- low molecular weight heparins
- mirtazapine
- monoamine oxidase inhibitors (MAOIs; e.g. rasagiline, selegiline, )
- multivitamins
- muscle relaxants
- nifedipine
- non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, naproxen)
- omega-3 fatty acids
- pentoxifylline
- propranolol
- quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
- rasagiline
- seizure medications ( phenobarbital, phenytoin, valproic acid, )
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
- tapentadol
- theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
- thiazide diuretics (water pills; e.g., hydrochlorothiazide, )
- thyroid replacements (e.g., desiccated thyroid, levothyroxine)
- tizanidine
- tramadol
- sibutramine
- St. John’s wort
- tramadol
- tricyclic antidepressants(e.g., amitriptyline, desipramine, imipramine)
- triptans (e.g., sumatriptan, rizatriptan)
This medication may interfere with certain medical/laboratory tests (including a brain scan for Parkinson’s disease), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
Pregnancy & Lactation of Venlafaxine
FDA Pregnancy Category – C
Pregnancy
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.
Lactation
This medication passes into breast milk. If you are a breastfeeding mother and are taking venlafaxine, it may affect your baby. Talk to your doctor about whether you should breastfeeding-feeding. The safety and effectiveness of this medication have not been established for children under 18 years of age. There have been reports that using this and similar medications in children below the age of 18 may cause behavioral and emotional changes, such as suicidal thoughts and behavior.
References
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