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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]
Milnacipran (trade names Ixel, Savella, Dalcipran, Toledomin) is a serotonin–norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia. It is not approved for the clinical treatment of major depressive disorder in the US, but it is in other countries.
Levomilnacipran (brand name Fetzima) is an antidepressant which was approved in the United States in 2013 for the treatment of major depressive disorder (MDD) in adults. [5] It is the levorotatory enantiomer of milnacipran, and has similar effects and pharmacology, acting as a serotonin–norepinephrine reuptake inhibitor (SNRI). [8] [9]
The half-life of venlafaxine is about 5 hours, and with once-daily dosing, steady-state concentration is achieved after about 3 days, though its active metabolite desvenlafaxine lasts longer. [59] The half-life of desvenlafaxine is about 11 hours, and steady-state concentrations are achieved after 4 to 5 days. [58]
Acute use (1–3 days) yields a potency about 1.5× stronger than that of morphine and chronic use (7 days+) yields a potency about 2.5 to 5× that of morphine. Similarly, the effect of tramadol increases after consecutive dosing due to the accumulation of its active metabolite and an increase of the oral bioavailability in chronic use.
Although described as SNRIs, duloxetine (Cymbalta), venlafaxine (Effexor), and desvenlafaxine (Pristiq) are in fact relatively selective as serotonin reuptake inhibitors (SRIs). [201] They are about at least 10-fold selective for inhibition of serotonin reuptake over norepinephrine reuptake. [201]
They act by antagonizing the α 2-adrenergic receptor and certain serotonin receptors such as 5-HT 2A and 5-HT 2C, [1] but also 5-HT 3, [1] 5-HT 6, and/or 5-HT 7 in some cases. By blocking α 2 -adrenergic autoreceptors and heteroreceptors , NaSSAs enhance adrenergic and serotonergic neurotransmission in the brain involved in mood regulation ...
This is a complete list of clinically approved prescription antidepressants throughout the world, as well as clinically approved prescription drugs used to augment antidepressants or mood stabilizers, by pharmacological and/or structural classification.