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Psychotropic Drugs
Published in Diana Riley, Perinatal Mental Health, 2018
Information on viloxazine (Vivalan) is limited to a single study of one patient who took 300 mg daily for two days (JR Holmes, 1977, internal publication, Fairmile journal). The concentration in breast milk was 10-20% of that in maternal serum. This drug, which is chemically distinct from the tri- and tetracyclics, is probably unsuitable for nursing mothers.
Psychiatric Emergencies Associated with Drug Overdose
Published in R. Thara, Lakshmi Vijayakumar, Emergencies in Psychiatry in Low- and Middle-Income Countries, 2017
S. Haque Nizamie, Sai Krishna Tikka, Nishant Goyal
Apart from anabolic steroids, an overdose of steroids used in clinical medical settings is also known to cause psychiatric manifestations. The reported incidence of steroid psychosis is 3%–57% (Ling, Perry and Tsuang 1981; Lewis and Smith 1983). The risk factors for steroid psychosis are female sex, doses of above 40 mg/day in the case of prednisolone, and long-term administration (Ling, Perry and Tsuang 1981; Hall et al. 1979). Steroid psychosis occurs within the first two weeks of corticosteroid therapy and is dose-related (Brown, Khan and Nejtek 1999). The psychiatric manifestations are often both affective, in the form of over-talkativeness, distractibility, or low mood, and non-affective, in the form of hallucinations or core delusions. It is, however, depression that is the most prevalent among these patients, its incidence being as high as about 40% (Ling, Perry and Tsuang 1981; Hall et al. 1979). The treatment involves a reduction in the dose or discontinuation of steroids. The use of psychotropic agents becomes essential in such a setting because a reduction in the dose or discontinuation of the steroid results in worsening of the underlying disease requiring steroid therapy. Antipsychotics are the mainstay of treatment, while lithium has been used to treat mood symptoms, both manic as well as depressive (Siegal 1978). Tricyclic and tetracyclic antidepressants should be used cautiously as they have been reported to induce the exacerbation of agitation (Hall, Popkin and Kirkpatrick 1978).
A patent review of BRD4 inhibitors (2013-2019)
Published in Expert Opinion on Therapeutic Patents, 2020
Tian Lu, Wenchao Lu, Cheng Luo
The Abbvie patents mainly describe azepine compounds as BRD4 inhibitors (Figure 5). Among them, compound 31 showed a significant inhibitory effect on BRD4 BD1/BD2 in vitro, with KI value of 0.6 and 2.5 nM. In the OPM-2 human multiple myeloma xenograft model, the treatment with compound 32 had a TGI of 81% at a dose of 5 mg/kg. While in the same model, tetracyclic Compound 33 showed a TGI of 79% at a dose of 2.5 mg/kg [62]. Other tetracyclic compounds from Abbvie Inc. have also shown greater BRD4 inhibition and inhibitory activity against the proliferation of MX-1 breast cancer cells. Compounds 34–36 are reported to have significant anti-tumor activity in OPM-2 human multiple myeloma xenograft models [63]. Patent WO2016157221A1 describes compounds containing oxepane and azepine scaffolds as potent BRD4 inhibitors (Figure 5). These analogs show significant anti-proliferative activity against MV4-11 leukemia cells and can effectively inhibit the expression of c-Myc [64].
Optimization of mirtazapine loaded into mesoporous silica nanostructures via Box-Behnken design: in-vitro characterization and in-vivo assessment
Published in Drug Delivery, 2022
Abeer A. Musallam, M. A. Mahdy, Hanan M. Elnahas, Reem A. Aldeeb
Depression is a prevalent and dangerous health condition that interrupts an individual's ability to feel, think and behave normally. People suffering from depression seem to have a lousy mindset with a deep feeling of melancholy, anxiety, suicidal tendencies, interrupted sleep, and perhaps a diminished interest in formerly pleasurable activities for most of the day. It can also result in a vast number of mental and physical issues, as well as an impaired performance at work and home (Ph.D. Nemeroff et al., 2022). Regrettably, nearly 280 million individuals suffer from depression on a global scale. Depression, at its worst, can result in suicide. Regarding the degree and sequence of depressive episodes in a time, medical care providers may recommend psychotherapy in addition to various drugs, such as selective serotonin reuptake inhibitors (SSRIs), tricyclic antidepressants (TCAs), and tetracyclic antidepressants (Rouini et al., 2014; WHO, 2021). Mirtazapine (MRT) is an unconventional antidepressant authorized to treat moderate to severe depression patients, usually accompanied by anxiety disorders. It is a tetracyclic antidepressant that works on noradrenergic and specific serotonergic receptors (NaSSA). It is the only tetracyclic antidepressant licensed for the treatment of depression by the food and drug administration (FDA) (Rouini et al., 2014). Mirtazapine shows poor water solubility, with a partition coefficient of 2.9 (K. M. Ezealisiji et al., 2017). Additionally, it has a low bioavailability of about 50%. It was estimated that increasing its water solubility might result in increased bioavailability and reduce the dose required to achieve the desired therapeutic effect (K. E. Ezealisiji et al., 2015).
Evaluating the efficacy and safety of antidepressants in patients with bipolar disorder
Published in Expert Opinion on Drug Safety, 2019
Elie Cheniaux, Antonio E. Nardi
Pacchiarotti et al. [129] published in 2013 recommendations on the use of antidepressants in BD. According to the authors, in the acute treatment of a depressive episode, adjunctive antidepressants may be used when there is a history of positive response to these substances, but should be avoided if there are concomitant manic symptoms, psychomotor agitation, rapid cycling or a history of treatment-emergent mania. Antidepressant monotherapy is contraindicated, especially in BD type I. In addition, among antidepressants, norepinephrine-serotonin reuptake inhibitors, and tri- and tetracyclics should not be the first option.