Desvenlafaxine, a serotonin and norepinephrine reuptake inhibitor (SNRI), is indicated for the treatment of major depressive disorder (MDD). The efficacy of Desvenlafaxine has been established in four short-term (8-week, placebo-controlled studies) and two maintenance studies in adult outpatients who met DSM-IV criteria for major depressive disorder.
Serotonin-norepinephrine reuptake inhibitor (SNRI)
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 protein 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.
The exact mechanism of the antidepressive action of Desvenlafaxine is unknown, but is thought to be related to the potentiation of Serotonin and Norepinephrine in the central nervous system, through inhibition of their reuptake. Non-clinical studies have shown that Desvenlafaxine is a potent Serotonin and Norepinephrine Reuptake Inhibitor (SNRI).
The recommended dose for Desvenlafaxine is 50 mg once daily, with or without food. The 50 mg dose is both a starting dose and the therapeutic dose. Desvenlafaxine should be taken at approximately the same time each day. Tablets must be swallowed whole with fluid and not divided, crushed, chewed, or dissolved. In clinical studies, doses of 10 mg to 400 mg per day were studied. In clinical studies, doses of 50 mg to 400 mg per day were shown to be effective, although no additional benefit was demonstrated at doses greater than 50 mg per day and adverse reactions and discontinuations were more frequent at higher doses. The 25 mg per day dose is intended for a gradual reduction in dose when discontinuing treatment. When discontinuing therapy, gradual dose reduction is recommended whenever possible to minimize discontinuation symptoms.
Clinical studies have shown that Desvenlafaxine does not have a clinically relevant effect on CYP2D6 (e.g., Desipramine, Atomoxetine, Dextromethorphan, Metoprolol, Nebivolol, Perphenazine, Tolterodine) metabolism at the dose of 100 mg daily. Reduce the dose of these substrates by one-half if co-administered with 400 mg of Desvenlafaxine. Avoid use of Desvenlafaxine with other Desvenlafaxine-containing products or Venlafaxine products. The concomitant use of Desvenlafaxine with other Desvenlafaxine-containing products or Venlafaxine will increase Desvenlafaxine blood levels and increase dose-related adverse reactions. Like CNS acting drugs, patients should be advised to avoid alcohol consumption while taking Desvenlafaxine.
Concurrent use or within 14 days of discontinuing MAOIs (e.g. linezolid, IV methylene blue). Initiation of MAOI at least 7 days after discontinuing desvenlafaxine. Concurrent use or within 14 days of discontinuing MAOIs (e.g. linezolid, IV methylene blue). Initiation of MAOI at least 7 days after discontinuing desvenlafaxine.
Suicidal thinking/ behaviour, HTN, mydriasis, seizure, hyponatraemia, interstitial lung disease and eosinophilic pneumonia; nausea, dizziness, insomnia, hyperhidrosis, constipation, somnolence, decreased appetite, anxiety, sexual function disorders in males (e.g. anorgasmia, decreased libido, abnormal orgasm, delayed ejaculation, erectile dysfunction, ejaculation disorder, ejaculation failure, sexual dysfunction).
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
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