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Venlafaxine, sold under the brand name Effexor among others, is an antidepressant medication of the serotonin–norepinephrine reuptake inhibitor (SNRI) class. [ 6 ] [ 9 ] It is used to treat major depressive disorder , generalized anxiety disorder , panic disorder , and social anxiety disorder . [ 9 ]
The half-life of desvenlafaxine is about 11 hours, and steady-state concentrations are achieved after 4 to 5 days. [58] The half-life of duloxetine is about 12 hours (range: 8–17 hours), and steady-state is achieved after about 3 days. [11] Milnacipran has a half-life of about 6 to 8 hours, and steady-state levels are reached within 36 to 48 ...
[12] [13] A 2012 meta-analysis of fluoxetine and venlafaxine concluded that statistically and clinically significant treatment effects were observed for each drug relative to placebo irrespective of baseline depression severity; some of the authors however disclosed substantial relationships with pharmaceutical industries.
[40] [41] Venlafaxine (Effexor) is sometimes referred to as an SNDRI, but is extremely imbalanced with k i values of 82 nM for SERT, 2480 nM for NET, and 7647 nM for DAT, with a ratio of 1:30:93. [42] It may weakly inhibit the reuptake of dopamine at high doses. [43]
Desvenlafaxine is a synthetic form of the isolated major active metabolite of venlafaxine, 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. [18]
Absorption half-life 1 h, elimination half-life 12 h. Biological half-life (elimination half-life, pharmacological half-life) is the time taken for concentration of a biological substance (such as a medication) to decrease from its maximum concentration (C max) to half of C max in the blood plasma.
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Fluoxetine also has a long half-life which can reduce withdrawal symptoms which are characteristic for some SSRIs after abrupt discontinuation, but it also means that it takes a long time to clear the drug and its active metabolite after discontinuing fluoxetine treatment. [18] Figure 5 Chemical structure of (–)-(3S,4R)-paroxetine
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