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Psychotropic Use during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Trazodone is an antidepressant that is also given for its sedative activity. First-trimester exposure to trazodone in 100 infants was not associated with an increased frequency of congenital anomalies (Rosa, personal communication, cited in Briggs et al., 2021), although this study is not peer reviewed. In another investigation that was peer reviewed, 121 women took trazodone or nefazodone during the first trimester. The frequency of congenital anomalies was not increased above that expected in the general population (3.5 percent) (Einarson et al., 2003). Trazodone is a category C drug.
Psychopharmacological Interventions for Functional Bowel Disease
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
Psychoactive drugs have been utilized in a variety of pain syndromes, and often result in significant improvement in symptoms (60). Psychopharmacological approaches to pain in functional GI disorders may be indicated in a variety of situations (61). By extrapolation, for patients who have significant pain—a frequent concomitant of functional GI disorders—treatment for this component may be indicated. Most of the available literature on chronic pain includes reports of the effects of tricyclic antidepressants. These agents have known beneficial effects, but also have a significant side-effects burden, including significant anticholinergic effects. Trazodone, a second-generation antidepressant, has beneficial effects in pain syndromes and no significant anticholinergic effects. Newer agents that are selective and potent inhibitors of serotonin may also be beneficial in treatment of pain syndromes. One study (46) reported beneficial effects of fluoxetine in a patient with chronic abdominal pain. Agents that modify visceral afferent transmission include the tricyclic antidepressants (TCAs) (imipramine, amitriptyline, and others), selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine, sertraline, paroxetine, fluvoxamine, and clomipramine (the last is both a tricyclic and serotonin-selective). Nefazodone, an atypical antidepressant with serotonin and norepinephrine reuptake inhibition and post-synaptic serotonin receptor (type 2) blockade, also may have clinical utility in pain syndromes.
Treatment of Psychological Disorders
Published in Mohamed Ahmed Abd El-Hay, Understanding Psychology for Medicine and Nursing, 2019
Two 5-HT2 receptor antagonists, nefazodone and trazodone, are used to treat depression. Trazodone is a serotonin 5-HT2 antagonist and also has some serotonin reuptake inhibiting properties. It has a sedative effect and therefore may be a useful choice in patients with mixed depressive and anxiety symptoms or in those who suffer from insomnia. Conversely, unwanted effects may include over-sedation and dizziness.
Designing multi-target drugs for the treatment of major depressive disorder
Published in Expert Opinion on Drug Discovery, 2023
Amit Kumar Halder, Soumya Mitra, Maria Natalia D. S. Cordeiro
Nefazodone, which is a potent 5-HT2A ligand with moderate potency toward 5-HT1A, may be used for the treatment of patients who are less responsive to other antidepressant drugs [42,43]. Adatanserin and flibanserin, which demonstrate antidepressant activities in animal models, interact with both these receptors. Considering these, Wang et al. synthesized a series of benzoxazole/benzothiazole-2,3-dihydrobenzo[b] [1,4]-dioxine derivatives (C1-C2, cf. Figure S1, Supplemental file) as dual 5-HT1A/5-HT2A ligands. The design was based on the fact that structurally similar compounds (lead compounds) had previously been reported as dual 5-HT1A/serotonin transporter (SERT) ligands. The most potent derivative (1, Figure 1) obtained from such lead modification exhibited low nanomolar and sub-nanomolar affinities for 5-HT1A (Ki = 17 nM) and 5-HT2A (Ki = 0.71 nM), respectively. It is worth mentioning here that forced swim test (FST) and tail suspension test (TST) are the two most common in vivo analyses performed to determine antidepressant efficacy. Compound 1 reduced the immobility time and exhibited potent antidepressant-like effects in the FST in an mice model with ED50 value of 39 mg/kg. Similarly, TST also depicted considerable antidepressant activity of this compound [44].
The serotonin toxidrome: shortfalls of current diagnostic criteria for related syndromes
Published in Clinical Toxicology, 2022
Angela L. Chiew, Nicholas A. Buckley
The incidence of serotonin toxicity in those on therapeutic serotonergic agents appears to be very low. A retrospective cohort study of 15 million patients exposed to at least one serotonergic agent, the incidence for serotonin toxicity lay between 0.9 and 2.3/1000 individuals exposed [37]. While a retrospective review of 4538 hospital in patients on a serotonergic agent administered fentanyl found only 23 had documented symptoms consistent with serotonin toxicity and 4 met Hunter criteria [38]. What does it mean when a study reports the incidence of serotonin syndrome was estimated to be 0.5–0.9 cases per 1000 patient-months of nefazodone treatment [39]? Nefazodone inhibits reuptake of serotonin, but also blocks serotonin receptors. It is useful to do research on whether it causes serotonin toxicity. However, it is unclear if the “serotonin syndromes” just had three of the above adverse effects or something more serious. Labelling a few coincident minor adverse effects as serotonin syndrome or serotonin toxicity, a terminology also used for life-threatening adverse effects generates uncertainty.
Pharmacotherapeutic options for co-morbid depression and alcohol dependence
Published in Expert Opinion on Pharmacotherapy, 2019
Thomas Hillemacher, Helge Frieling
Nefazodone is a serotonin antagonist and reuptake inhibitor. An open-label pilot trial with 13 patients with DSM-IV criteria for alcohol dependence and major depressive episode indicated a significant decrease in depression (HRSD), alcohol craving, drinks/week, and days of alcohol use/week [79]. This was partly confirmed by a placebo-controlled study in 64 patients with comorbid major depressive disorder and AUD [80]. All subjects received weekly group therapy for AUD over 12 weeks of treatment. Nefazodone-treated subjects were more likely to complete treatment than placebo-treated patients (62 vs. 34%, respectively). At the end of the 12-week study, patients on nefazodone had lower depressive symptom scores and a better antidepressant response rate than those taking placebo (48 vs. 16%, respectively). There was no effect on nefazodone relative to placebo on the number of alcoholic drinks consumed per day [80].