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Paroxetine

Serotonin Uptake Inhibitors
CATEGORIES

Serotonin Uptake Inhibitors, Antidepressive Agents


ALIASES

Arketis, Euplix, Paroxetin 2care4, Paroxetin Actavis, Paroxetin Alpharma, Paroxetin Amneal, Paroxetin Aurobindo, Paroxetin EQL Pharma, Paroxetin Ebb, Paroxetin HEXAL, Paroxetin Hexal, Paroxetin Mylan, Paroxetin Orifarm, Paroxetin Orion, Paroxetin Sandoz, Paroxetin Teva, Paroxetin ratiopharm, Paroxiflex, Seroxat, Seroxat®


SUBSTANCES

paroxetine, paroxetine hydrochloride, paroxetine hydrochloride hemihydrate, paroxetine mesylate


ENVIRONMENTAL CONCERN: HIGH
Paroxetine hydrochloride and paroxetine mesylate belong to a class of antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs). Despite distinct structural differences between compounds in this class, SSRIs possess similar pharmacological activity. As with other antidepressant agents, several weeks of therapy may be required before a clinical effect is seen. SSRIs are potent inhibitors of neuronal serotonin reuptake. They have little to no effect on norepinephrine or dopamine reuptake and do not antagonize α- or β-adrenergic, dopamine D2 or histamine H1 receptors. During acute use, SSRIs block serotonin reuptake and increase serotonin stimulation of somatodendritic 5-HT1A and terminal autoreceptors. Chronic use leads to desensitization of somatodendritic 5-HT1A and terminal autoreceptors. The overall clinical effect of increased mood and decreased anxiety is thought to be due to adaptive changes in neuronal function that leads to enhanced serotonergic neurotransmission. Side effects include dry mouth, nausea, dizziness, drowsiness, sexual dysfunction and headache (see Toxicity section below for a complete listing of side effects). Side effects generally occur during the first two weeks of therapy and are usually less severe and frequent than those observed with tricyclic antidepressants. Paroxetine hydrochloride and mesylate are considered therapeutic alternatives rather than generic equivalents by the US Food and Drug Administration (FDA); both agents contain the same active moiety (i.e. paroxetine), but are formulated as different salt forms. Clinical studies establishing the efficacy of paroxetine in various conditions were performed using paroxetine hydrochloride. Since both agents contain the same active moiety, the clinical efficacy of both agents is thought to be similar. Paroxetine may be used to treat major depressive disorder (MDD), panic disorder with or without agoraphobia, obsessive-compulsive disorder (OCD), social anxiety disorder (social phobia), generalized anxiety disorder (GAD), post-traumatic stress disorder (PTSD) and premenstrual dysphoric disorder (PMDD). Paroxetine has the most evidence supporting its use for anxiety-related disorders of the SSRIs. It has the greatest anticholinergic activity of the agents in this class and compared to other SSRIs, paroxetine may cause greater weight gain, sexual dysfunction, sedation and constipation.

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IN SCOPE
HIGH

REFERENCES

  1. Fass.se för vårdpersonal
  2. Stockholm Vatten. Läkemedelsrester i Stockholms vattenmiljö. 2010. ISBN 978-91-633-6642-0.
  3. IVL Swedish Environmental Research Institute Ltd. Fick J, Lindberg RH, Kaj L, Brorström-Lundén E. Results from the Swedish National Screening Programme 2010. Subreport 3, B 2014 Pharmaceuticals.
  4. IVL Swedish Environmental Research Institute Ltd Fick J, Lindberg RH, Fång J, Magnér J, Kaj L, Brorström-Lundén E. Screening 2014. Analysis of pharmaceuticals and hormones in samples from WWTPs and receiving waters. Rapport C 135.
  5. Goodpoint. Jämförande bedömning av miljörisk vid användning av citalopram, escitalopram, sertralin, fluoxetin, venlafaxin, paroxetin och klomipramin. Stockholm: Goodpoint; 2018.

SOURCES

  1. Drugbank, The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug data with comprehensive drug target information.
  2. PubChem, PubChem is the world's largest collection of freely accessible chemical information. Search chemicals by name, molecular formula, structure, and other identifiers
  3. ECHA, The European Chemicals Agency (ECHA) is the driving force among regulatory authorities in implementing the EU's groundbreaking chemicals legislation for the benefit of human health and the environment as well as for innovation and competitiveness.
  4. EMA, The mission of the European Medicines Agency (EMA) is to foster scientific excellence in the evaluation and supervision of medicines, for the benefit of public and animal health in the European Union (EU).
  5. EU watch-list, Commission Implementing Decision (EU) 2018/840 of 5 June 2018 establishing a watch list of substances for Union-wide monitoring in the field of water policy pursuant to Directive 2008/105/EC of the European Parliament.
  6. Umweltbundesamt, Since its founding in 1974, the German Environment Agency (Umweltbundesamt – UBA) has been Germany’s main environmental protection agency.
  7. Naturvårdsverket, A public agency in Sweden that is responsible for environmental issues. The Agency carries out assignments on behalf of the Swedish Government relating to the environment in Sweden, the EU and internationally
  8. Läkemedelsverket, The Swedish Medical Products Agency (MPA) is the Swedish national authority responsible for regulation and surveillance of the development, manufacturing and marketing of drugs and other medicinal products.
  9. FASS, The Swedish environmental classification of pharmaceuticals at www.fass.se has now been running since October 2005. Since then a large amount of environmental information of pharmaceuticals has been published.
  10. Janusinfo, Janusinfo is providing drug information to support healthcare professionals in their everyday work. The website is the electronic means of communication of the Drug Therapeutic Committee and the Health and Medical Care Administration of the Stockholm County Council, Sweden.