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Desmethylcitalopram
Desmethylcitalopram is an active metabolite of the antidepressant drugs citalopram ( racemic) and escitalopram (the ''S''-enantiomer, which would be called desmethylescitalopram). Like citalopram and escitalopram, desmethylcitalopram functions as a selective serotonin reuptake inhibitor (SSRI), and is responsible for some of its parents' therapeutic benefits. See also * Desmethylsertraline * Desmethylvenlafaxine * Didesmethylcitalopram * Norfluoxetine Seproxetine, also known as (''S'')-norfluoxetine, is a selective serotonin reuptake inhibitor (SSRI). It is the ''S'' enantiomer of norfluoxetine, the main active metabolite of the widely used antidepressant fluoxetine; but little is known abo ... References Isobenzofurans Fluoroarenes Nitriles Human drug metabolites Selective serotonin reuptake inhibitors {{nervous-system-drug-stub ...
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Desmethylsertraline
Desmethylsertraline (DMS), also known as norsertraline, is an active metabolite of the antidepressant drug sertraline. Like sertraline, desmethylsertraline acts as a monoamine reuptake inhibitor, and may be responsible for some of its parent's therapeutic benefits; however, the effects of DMS's main activity of increasing serotonin levels via binding to the serotonin transporter appears to be negligible as in vivo testing showed no measurable change in brain activity despite a nearly 20-fold increase in DMS blood levels compared to the EC50 (i.e. the amount required to achieve the desired effect in 50% of the population) of its parent drug sertraline. DMS is significantly less potent relative to sertraline as a serotonin reuptake inhibitor (''K''i = 76 nM vs. 3 nM, respectively), but conversely, is more balanced as a monoamine reuptake inhibitor (5-HT (''K''i) = 76 nM; NE (''K''i) = 420 nM; DA (''K''i) = 440 nM), which has the effective result of DMS co ...
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Citalopram
Citalopram, sold under the brand name Celexa among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and social phobia. The antidepressant effects may take one to four weeks to occur. It is taken by mouth. Common side effects include nausea, trouble sleeping, sexual problems, shakiness, feeling tired, and sweating. Serious side effects include an increased risk of suicide in those under the age of 25, serotonin syndrome, glaucoma, and QT prolongation. It should not be used in persons who take or have recently taken a MAO inhibitor. Antidepressant discontinuation syndrome may occur when stopped. There are concerns that use during pregnancy may harm the fetus. Citalopram was approved for medical use in the United States in 1998. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication. In ...
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Didesmethylcitalopram
Didesmethylcitalopram is an active metabolite of the antidepressant drug citalopram ( racemic). Didesmethyl''es''citalopram is an active metabolite of the antidepressant escitalopram, the ''S''-enantiomer of citalopram. Like citalopram and escitalopram, didesmethyl(es)citalopram functions as a selective serotonin reuptake inhibitor (SSRI), and is responsible for some of its parents' therapeutic benefits. See also * Desmethylcitalopram * Desmethylsertraline * Desmethylvenlafaxine * Norfluoxetine Seproxetine, also known as (''S'')-norfluoxetine, is a selective serotonin reuptake inhibitor (SSRI). It is the ''S'' enantiomer of norfluoxetine, the main active metabolite of the widely used antidepressant fluoxetine; but little is known abo ... References Isobenzofurans Nitriles Fluoroarenes Human drug metabolites {{nervous-system-drug-stub ...
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Active Metabolite
An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide). Certain drugs such as codeine and tramadol have metabolites (morphine and ''O''-desmethyltramadol respectively) that are stronger than the parent drug and in these cases the metabolite may be responsible for much of the therapeutic action of the parent drug. Sometimes, however, metabolites may produce toxic effects and patients must be monitored carefully to ensure they do not build up in the body. This is an issue with some well-known drugs, such as pethidine (meperidine) and dextropropoxyphene. Prodrugs Sometimes drugs are formulated in an inactive form that is de ...
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Nitriles
In organic chemistry, a nitrile is any organic compound that has a functional group. The prefix '' cyano-'' is used interchangeably with the term ''nitrile'' in industrial literature. Nitriles are found in many useful compounds, including methyl cyanoacrylate, used in super glue, and nitrile rubber, a nitrile-containing polymer used in latex-free laboratory and medical gloves. Nitrile rubber is also widely used as automotive and other seals since it is resistant to fuels and oils. Organic compounds containing multiple nitrile groups are known as cyanocarbons. Inorganic compounds containing the group are not called nitriles, but cyanides instead. Though both nitriles and cyanides can be derived from cyanide salts, most nitriles are not nearly as toxic. Structure and basic properties The N−C−C geometry is linear in nitriles, reflecting the sp hybridization of the triply bonded carbon. The C−N distance is short at 1.16  Å, consistent with a triple bond. Nitr ...
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Norfluoxetine
Seproxetine, also known as (''S'')-norfluoxetine, is a selective serotonin reuptake inhibitor (SSRI). It is the ''S'' enantiomer of norfluoxetine, the main active metabolite of the widely used antidepressant fluoxetine; but little is known about its pharmacological actions. Seproxetine was being investigated by Eli Lilly and Company Eli Lilly and Company is an American pharmaceutical company headquartered in Indianapolis, Indiana, with offices in 18 countries. Its products are sold in approximately 125 countries. The company was founded in 1876 by, and named after, Colon ... as an antidepressant; however, cardiac side effects were discovered and development was discontinued. References Eli Lilly and Company brands Human drug metabolites Trifluoromethyl compounds Phenol ethers Selective serotonin reuptake inhibitors {{nervous-system-drug-stub ...
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Desmethylvenlafaxine
Desvenlafaxine, sold under the brand name Pristiq among others, is a medication used to treat depression. It is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class and is taken by mouth. It is recommended that the need for further treatment be occasionally reassessed. It may be less effective than its parent compound venlafaxine, although some studies have found comparable efficacy. Common side effects include dizziness, trouble sleeping, increased sweating, constipation, sleepiness, anxiety, and sexual problems. Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and high blood pressure. A withdrawal syndrome may occur if the dose is decreased or the medication completely stopped. It is unclear if use during pregnancy or breastfeeding is safe. Desvenlafaxine was approved for medical use in the United States in 2008. In Europe its application for use was denied in 2009. But it is available ...
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Therapeutic Benefit
Therapeutic effect refers to the response(s) after a treatment of any kind, the results of which are judged to be useful or favorable. This is true whether the result was expected, unexpected, or even an unintended consequence. An adverse effect (including nocebo) is the converse and refers to harmful or undesired response(s). What constitutes a therapeutic effect versus a side effect is a matter of both the nature of the situation and the goals of treatment. No inherent difference separates therapeutic and undesired side effects; both responses are behavioral/physiologic changes that occur as a response to the treatment strategy or agent. Treatment scope To maximize therapeutic effects (desired) and minimize side effects (undesired) requires recognition and quantification of the treatment in multiple dimensions. In the specific case of targeted pharmaceutical interventions, a combination of therapies is often needed to achieve the desired results. Pharmacology examples *A 201 ...
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Antidepressant
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of ...
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Selective Serotonin Reuptake Inhibitor
Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions. SSRIs increase the extracellular level of the neurotransmitter serotonin by Reuptake inhibitor, limiting its reuptake, reabsorption (reuptake) into the presynaptic cell. They have varying degrees of selectivity for the other monoamine transporters, with pure SSRIs having strong affinity for the serotonin transporter and only weak affinity for the norepinephrine transporter, norepinephrine and dopamine transporters. SSRIs are the most widely prescribed antidepressants in many countries. The efficacy of SSRIs in mild or moderate cases of depression has been disputed and may or may not be outweighed by side effects, especially in adolescent populations. Medical uses The main indication for SSRIs is major depressive disorder; however, they are frequently prescribed for a ...
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