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The non-tricyclic SNRIs have several important differences that are based on pharmacokinetics, metabolism to active metabolites, inhibition of CYP isoforms, effect of drug-drug interactions, and the half-life of the nontricyclic SNRIs. [28] [35]
These drugs inhibit the uptake of the neurotransmitter 5-HT by blocking the SERT, thus increasing its synaptic concentration, and have shown to be efficacious in the treatment of depression, however sexual dysfunction and weight gain are two very common side-effects that result in discontinuation of treatment.
Metabolism Active metabolites [27] Excretion Fluoxetine: 6–8 [28] 60–80 [28] 20–45 [28] 94.5 [28] Acute administration, 1–3 days. Chronic administration, 4–6 days. Norfluoxetine, acute and chronic administration, 4–16 days [28] [29] Extensive first-pass hepatic mainly by CYP2D6 by desmethylation. Non-linear pharmacokinetic profile ...
Duloxetine is one of the most commonly used prescription medications in the U.S. Patients with depression are usually prescribed 40 to 60 milligrams per day, with a potential increase of up to 120 ...
The pharmacology of antidepressants is not entirely clear.. The earliest and probably most widely accepted scientific theory of antidepressant action is the monoamine hypothesis (which can be traced back to the 1950s), which states that depression is due to an imbalance (most often a deficiency) of the monoamine neurotransmitters (namely serotonin, norepinephrine and dopamine). [1]
Metabolism of amitriptyline to major active metabolites. Nortriptyline, the main active metabolite of amitriptyline, is an antidepressant on its own right. Nortriptyline reaches 10% higher level in the blood plasma than the parent drug amitriptyline and 40% greater area under the curve, and its action is an important part of the overall action ...
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