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Clomipramine

Serotonin Uptake Inhibitors
CATEGORIES

Serotonin Uptake Inhibitors, Antidepressive Agents, Tricyclic


ALIASES

Anafranil, Anafranil Retard, Anafranil®, Anafranil® Retard, Klomipramin Mylan


SUBSTANCES

clomipramine, clomipramine hydrochloride


ENVIRONMENTAL CONCERN: MODERATE
Clomipramine, the 3-chloro analog of imipramine, is a dibenzazepine-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, clomipramine does not affect mood or arousal, but may cause sedation. In depressed individuals, clomipramine exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as clomipramine, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline and desipramine. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Clomipramine may be used to treat obsessive-compulsive disorder and disorders with an obsessive-compulsive component (e.g. depression, schizophrenia, Tourette’s disorder). Unlabeled indications include panic disorder, chronic pain (e.g. central pain, idiopathic pain disorder, tension headache, diabetic peripheral neuropathy, neuropathic pain), cataplexy and associated narcolepsy, autistic disorder, trichotillomania, onchophagia, stuttering, premature ejaculation, and premenstrual syndrome. Clomipramine is rapidly absorbed from the gastrointestinal tract and demethylated in the liver to its primary active metabolite, desmethylclomipramine.

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IN SCOPE
MODERATE

REFERENCES

  1. Fass.se för vårdpersonal
  2. Goodpoint. Jämförande bedömning av miljörisk vid användning av citalopram, escitalopram, sertralin, fluoxetin, venlafaxin, paroxetin och klomipramin. Stockholm: Goodpoint; 2018.
  3. SLL. Sammanställning av läkemedelsprovtagningar - Bearbetning av regional försäljningsstatistik av läkemedel samt datamaterial från Stockholms läns landstings mätprogram för läkemedelssubstanser i vattenmiljö, 2012–2016.
  4. 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.

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.