Desvenlafaxine Pharmacology

Desvenlafaxine

About Desvenlafaxine
Desvenlafaxine (O-desmethylvenlafaxine) is the major acgive metabolite of the
antidepressant venlafaxine.it is a serotonin-norepinephrine reuptake inhibitor.

Mechanism of Action of Desvenlafaxine
Desvenlafaxine is a synthetic form of the isolated major active metabolite of venlafaxine, and is categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI). It works by blocking the transporter "reuptake" proteins 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. It does not have monoamine oxidase (MAO) inhibitory activity; and has not shown significant affinity for muscarinic cholinergic, H1-histaminergic, ?-adrenergic, dopaminergic, ?-aminobutyric acid (GABA), glutamate, and opiate receptors in vitro.
Pharmacokinets of Desvenlafaxine
1.Absorption: Absolute oral bioavailability: About 80%. Mean Tmax: About 7.5 hr.
2.Distribution: Plasma protein binding: About 30%; independent of drug concentration
3.Metabolism: Hepatic via conjugation, lesser extent by oxidation via CYP3A4 isozyme.
4.Excretion: Excreted in urine
Onset of Action for Desvenlafaxine
N/A
Duration of Action for Desvenlafaxine
N/A
Half Life of Desvenlafaxine
About 11 hr, prolonged in renal failure
Side Effects of Desvenlafaxine
1.Dizziness
2.Nausea and vomiting
3.Dry mouth
4.Headache
5.Tinnitus
6.Insomnia
7.Abnormal dreams
8.Fatigue
9.Constipation
10.Diarrhea
11.Somnolence
12Decreased appetite
13.Irritability
14.Anxiety
15.Tremor
16.Paresthesia
17.Male sexual function disorders (e.g. Decreased libido, delayed ejaculation, erectile dysfunction)
18.Urinary hesitancy
19.Hyperhidrosis
20.Blurred vision
21.Mydriasis
22.Palpitations
23.Hypertension
24.Orthostatic hypotension
25.Dyslipidemia
26.Proteinuria
27.Abnormal liver function test.
28.Potentially Fatal: Serotonin syndrome or neuroleptic malignant syndrome-like reactions.

Contra-indications of Desvenlafaxine
1.Hypersensitivity to Desvenlafaxine, venlafaxine or any component of the formulation.
2.Concomitant/recent (within preceeding 14 days) use of MAOI.
3.Do not initiate MAOI at least 7 days after discontinuing Desvenlafaxine.
Special Precautions while taking Desvenlafaxine
1.May be associated with increased risk of suicidal thinking and behaviour in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
2.Serotonin syndrome or neuroleptic malignant syndrome (NMS) have occurred.
3.Gradually taper dose if discontinuing to reduce risk of withdrawal symptoms.
4.Caution in patients with pre-existing glaucoma, hypertension, cardiovascular, cerebrovascular, or lipid metabolism and seizure disorders.
5.May increase risk of bleeding.
6.May be associated with development of syndrome of inappropriate antidiuretic hormone (SIADH) and Hyponatraemia, elderly and patients who are taking diuretics or with volume depletion may be at greater risk
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Not recommended
Children Related Information
Safety and efficacy have not been established.
Indications for Desvenlafaxine
1.Depression.
2.Depression with associated symptoms of anxiety.
3.Generalized anxiety disorder, and social anxiety disorder.
4.Treatment of adults with panic disorder.
Interactions for Desvenlafaxine
1.Desvenlafaxine may diminish the therapeutic effect of Iobenguane I-123.
2.May enhance adverse effects of other CNS depressants.
3.Concomitant use with alpha-/beta-agonists may enhance tachycardic and vasopressor effect.
4.Desvenlafaxine may increase concentration of CYP2D6 substrates (e.g. desipramine); decrease exposure of CYP3A4 substrates (e.g. midazolam).
5.CYP3A4 inhibitors (e.g. ketoconazole) may increase concentration of desvenlafaxine.
6.May enhance the antiplatelet effect of nonselective NSAIDs, aspirin; and anticoagulant effect of warfarin.
7.Potentially Fatal: Concurrent use with MAOIs may lead to fatal serotonin syndrome or NMS-like reactions. Do not use within at least 14 days of discontinuing MAOI treatment and start MAOI at least 7 days after stopping desvenlafaxine.
8.Increased risk of serotonin syndrome with sibutramine.
Typical Dosage for Desvenlafaxine
Adult: 50 mg once daily. With or without food
Schedule of Desvenlafaxine
N/A
Storage Requirements for Desvenlafaxine
Store in a dry place at 20-25?C
Effects of Missed Dosage of Desvenlafaxine
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
Effects of Overdose of Desvenlafaxine
Symptoms may include: Headache, agitation, dizziness, nausea, vomiting, constipation, diarrhoea, dry mouth, paresthesia, and tachycardia (reported within 5 days of an overdose >600 mg).

Management: Treatment is supportive and symptomatic. Activated charcoal may be administered. Induction of emesis is not recommended. Forced diuresis, dialysis

Home Delivery for Desvenlafaxine in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including desvenlafaxine.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for desvenlafaxine and other medicines and health products. Home delivery services for desvenlafaxine may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take desvenlafaxine only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for desvenlafaxine before they complete the sale. You can get this information while placing the order for desvenlafaxine with the pharmacy.

Desvenlafaxine is a generic medicine name and there are several brands available for it. Some of the brands for desvenlafaxine might be better known than desvenlafaxine itself. If the pharmacy that's willing to deliver medicines to your home doesn't have desvenlafaxine in stock, you can ask for one of the branded alternatives for desvenlafaxine.