Trazodone antidepressant

Antidepressants Trazodone, mirtazapine, paroxetine, other selective serotonin reuptake inhibitors venlafaxine... 

Due to the important pharmacological applications of this system, in particular the antidepressant trazodone, numerous articles deal with either its synthesis, or its incorporation into more complex substances, as a pharmacophore (see Section 11.13.12). Synthetic methods have been reviewed <1996CHEC-II(8)367>, and most of them are still in use or have been modified. Recent literature essentially focuses on the formation of the triazole ring. 

Antidepressants. In the early 1980s, the recognition that depression is a frequent comorbid feature of BN coupled with the observation that appetite changes are a common feature of depression led researchers to evaluate antidepressant treatment for BN. Since that time, a series of controlled studies have demonstrated efficacy for a wide assortment of antidepressants including the TCAs imipramine (Tofranil) and desipramine (Norpramin), the MAOl phenelzine (Nardil), the SSRl fluoxetine (Prozac), and the atypical antidepressants trazodone (Desyrel) and bupropion (Wellbutrin). Overall, approximately two-thirds of antidepressant-treated patients with bulimia experience symptomatic improvement while nearly one-third achieves complete remission of binging and purging. In addition, the improvement in the symptoms of BN is not dependent on the presence of comorbid depression. 

The antidepressant trazodone (Desyrel) is commonly used in low doses to treat agitation or insomnia in dementia patients. However, older patients often do not tolerate the higher doses of trazodone needed to treat depression. 

When we talk about serotonin-blocking medications, a point of clarification must be made. In most cases, medications do not block overall serotonin activity but instead block the activity at one of the many serotonin receptor types. For example, the antidepressants trazodone, nefazodone, and mirtazapine increase total serotonin activity yet they block certain of the serotonin receptors. Mirtazapine increases both serotonin and norepinephrine activity by interfering with the alpha-2 receptor. By also blocking the serotonin-2 and serotonin-3 receptors, mirtazapine avoids the sexual dysfunction and GI side effects commonly experienced with other serotoninboosting medications. We cannot truly call these serotonin-blocking medications, because they are serotonin-boosting medications that selectively block certain serotonin receptors. 

Trazodone is an older antidepressant that is associated with significant sedation. Currently, trazodone is not recommended as a first-line antidepressant because of an increased risk of orthostatic hypotension, arrhythmias, and priapism. Also, compared with other available antidepressants, trazodone does not offer an advantage in terms of therapeutic efficacy. However, trazodone may be useful in patients with insomnia. It is currently common practice to use low doses of trazodone (e.g., 50-100 mg) to assist with initial insomnia while starting treatment with one of the newer antidepressants to address the underlying depression. If this strategy is used, we recommend tapering the trazodone dose and discontinuing treatment with trazodone after 4—6 weeks. 

Tranks see Benzodiazepine Tranxene see Benzodiazepine Tranylcypromine see Antidepressants Trazodone see Antidepressants Treat see Heroin Triamterene see Diuretics Triazolam see Benzodiazepine Trichlormethiazide see Diuretics Trifluoperazine see Tranquilizers Trifluoromethylphenylpiperazine see Benzylpiperazine/ Trifluoromethylphenylpiperazine Trifuluopromazine see Tranquilizers Trilafon see Tranquilizers Trimipramine see Antidepressants Tripper see LSD (lysergic acid diethylamide)... 

Kalgutkar, A.S. et al., Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4, Chem. Biol. Interact., 155(1-2), 10, 2005. 

The l,2,4-triazolo[4,3-fl]pyridine nuclens can be accessed by cyclocondensation of 2-hydrazino-pyridines the synthesis of the antidepressant trazodone, shown below, is an example. Condensation of 2-hydrazinopyridines with carboxylic acids, promoted by polymer-supported triphenylphosphine with tri-chloroacetonitiile and heated with microwave irradiation, is also efficient. °... 

Trimipramine is contraindicated in patients with known hypersensitivity to tricyclic antidepressants, trazodone, and related compounds in the acute recovery phase of myocardial infarction (MI), because the drug depresses cardiac function and causes dysrhythmia in patients in coma or severe respiratory depression (additive CNS and respiratory depression) and during or within 14 days of therapy with monoamine oxidase inhibitors. 

Fluoxetine at a dose of 20-60 mg/day, may cause a 2-4-fold increase in plasma concentration of tricyclic antidepressants (TCAs), possibly associated with signs of toxicity, including decreased energy, psychomotor retardation, sedation, dry mouth, and memory loss. The mechanism of this interaction may be attributed to the potent inhibitory effect of fluoxetine and norfluoxetine on the CYP2D6-mediated hydroxylation of TCAs. When given in combination with the heterocyclic antidepressant trazodone, fluoxetine was found to produce a significant elevation in plasma levels of both trazodone and its metabolite m-cbloropbenylpiperazine (mCPP)... 

Anxiolytic antidepressants (trazodone, venlafaxine), clonazepam (or other benzodiazepines note that, generally, benzodiazepines are not recommended for long-term use in SAD), gabapentin,... 

In 10 of 109 patients receiving methadone maintenance treatment in whom the QTc interval was prolonged (>400 ms), the susceptibility factors were older age, higher methadone dose, and the use of antidepressants (trazodone and mirtazapine) [88 ]. 

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