Tricyclic antidepressant - Wikipedia, the free encyclopedia - The Diigo Meta page

• 05 Mar 13
  

  jonnycmw
  • rimarily as serotonin-norepinephrine reuptake inhibitors (SNRIs) by blocking the serotonin transporter (SERT) and the norepinephrine transporter (NET)
• 14 Jan 13
  

  Hannah Miller
  • Tricyclic antidepressants (TCAs) are heterocyclic chemical compounds
  • first discovered in the early 1950s and were subsequently introduced later in the decade; ^[1] they are named after their chemical structure, which contains three rings of atoms. The tetracyclic antidepressants (TeCAs), which contain four rings of atoms, are a closely related group of antidepressant compounds.
  • TCAs have been largely replaced in clinical use in most parts of the world by newer antidepressants such as the selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs), which typically have more favorable side-effects profiles, though they are still sometimes prescribed for certain indications.

  • The TCAs include the following agents which are predominantly serotonin and/or norepinephrine reuptake inhibitors:

     
     
     
    • Amitriptyline (Tryptomer, Elavil)
     
    • Amitriptylinoxide (Amioxid, Ambivalon, Equilibrin)
     
    • Butriptyline (Evadyne)
     
    • Clomipramine (Anafranil)
     
    • Demexiptiline (Deparon, Tinoran)
     
    • Desipramine (Norpramin, Pertofrane)
     
    • Dibenzepin (Noveril, Victoril)
     
    • Dimetacrine (Istonil, Istonyl, Miroistonil)
     
    • Dosulepin/Dothiepin (Prothiaden)
     
    • Doxepin (Adapin, Sinequan)
     
    • Imipramine (Tofranil, Janimine, Praminil)
  • • Imipraminoxide (Imiprex, Elepsin)
     
    • Lofepramine (Lomont, Gamanil)
     
    • Melitracen (Deanxit, Dixeran, Melixeran, Trausabun)
     
    • Metapramine (Timaxel)
     
    • Nitroxazepine (Sintamil)
     
    • Nortriptyline (Pamelor, Aventyl, Norpress)
     
    • Noxiptiline (Agedal, Elronon, Nogedal)
     
    • Pipofezine (Azafen/Azaphen)
     
    • Propizepine (Depressin, Vagran)
     
    • Protriptyline (Vivactil)
     
    • Quinupramine (Kevopril, Kinupril, Adeprim, Quinuprine)

  • and

     
     
    • Amineptine (Survector, Maneon, Directim) - Norepinephrine-dopamine reuptake inhibitor
     
    • Iprindole (Prondol, Galatur, Tetran) - 5-HT₂ receptor antagonist
     
    • Opipramol (Insidon, Pramolan, Ensidon, Oprimol) - σ receptor agonist
     
    • Tianeptine (Stablon, Coaxil, Tatinol) - Selective serotonin reuptake enhancer
     
    • Trimipramine (Surmontil) - 5-HT₂ receptor antagonist

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• 11 Mar 12
  

  agent808

  Medical

• 16 Nov 11
  

  hyoomen
  • Notably, the TCAs have negligible affinity for the dopamine transporter (DAT), and therefore have no efficacy as dopamine reuptake inhibitors (DRIs).^[15] Both serotonin and norepinephrine have been highly implicated in depression and anxiety, and it has been shown that facilitation of their activity has beneficial effects on these mental disorders.
  • As a result, they also act as potent antihistamines and anticholinergics. These properties are generally undesirable in antidepressants, however, and likely contribute to their large side effect profiles.^[25]
  • Such side effects are relatively common and may include dry mouth, dry nose, blurry vision, lowered gastrointestinal motility or constipation, urinary retention, cognitive and/or memory impairment, and increased body temperature.
  • drowsiness, anxiety, emotional blunting (apathy/anhedonia), confusion, restlessness, dizziness, akathisia, hypersensitivity, changes in appetite and weight, sweating, sexual dysfunction, muscle twitches, weakness, nausea and vomiting, hypotension, tachycardia, and rarely, irregular heart rhythms.
  • In tricyclics, discontinuation syndrome symptoms include anxiety, insomnia, headache, nausea, malaise, or motor disturbance. ^[37]
  • The TCAs are highly metabolised by the cytochrome P450 hepatic enzymes. Drugs that inhibit cytochrome P450 (for example cimetidine, methylphenidate, fluoxetine, antipsychotics, and calcium channel blockers) may produce decreases in the TCAs' metabolism, leading to increases in their blood concentrations and accompanying toxicity.
  • Treatment depends on severity of symptoms. If there is a metabolic acidosis, infusion of Sodium Bicarbonate is recommended by Toxbase (UK poisons advice website). Two mechanisms are postulated for its therapeutic effect. Tricyclics are protein bound and become less bound in more acidic conditions.

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