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Psychiatric disorders
Published in Anne Lee, Sally Inch, David Finnigan, Therapeutics in Pregnancy and Lactation, 2019
There are few published data on the outcome of pregnancies exposed to paroxetine, sertraline, citalopram, fluvoxamine, venlafaxine, nefazadone, mirtazepine and reboxetine so their use in pregnancy cannot be supported.
Substrates of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Fluvoxamine, one of the first SSRIs developed, is used in the treatment of major depression and anxiety disorders (Figgitt and McClellan 2000; Wilde et al. 1993). It is mainly metabolized by CYP2D6 and, to a less extent, by 1A2 (Spigset et al. 2001). Fluvoxamine is extensively metabolized in human liver via oxidative demethylation and oxidative deamination and N-acetylation, and <4% is excreted as unchanged form (Spigset et al. 1998). Approximately 30%–60% of the metabolites appear to be produced by oxidative demethylation of the methoxy group, whereas 20%–40% seem to be produced by oxidative deamination to fluvoxethanol or by removal of the entire ethanolamino group (Perucca et al. 1994). Fluvoxamine is converted to its major urinary metabolite, the 5-demethox-ylated carboxylic acid metabolite, which is pharmacologically inactive, mainly by CYP2D6 and, to a less extent, by 1A2 (Figure 3.12) (Spigset et al. 2001). No other active metabolites are formed from fluvoxamine (DeVane and Gill 1997). Relative to other SSRIs, fluvoxamine is a potent inhibitor of CYP1A2, a moderate inhibitor of CYP2C19 and 3A4 and a weak inhibitor of CYP2D6 (van Harten 1995), and a number of drug interactions with fluvoxamine have been documented (Spina et al. 2008; Wagner and Vause 1995).
Treatment of bulimia nervosa
Published in Stephen Wonderlich, James E Mitchell, Martina de Zwaan, Howard Steiger, Annual Review of Eating Disorders Part 2 – 2006, 2018
The findings from a large RCT involving the antidepressant drug fluvoxamine have long been awaited. Schmidt and colleagues (2004) are to be congratulated on obtaining the data and presenting the findings, albeit in outline. The study had a complex design in which 267 patients were randomized to fluvoxamine or placebo, or fluvoxamine then placebo, combined with three different intensities of psychological support, all provided over one year. Somewhat surprisingly, fluvoxamine proved to be no more effective than placebo in both the short and long term and, disturbingly, its use was associated with a high rate of adverse effects, some of which were serious (grand mal seizures). The reason why fluvoxamine was ineffective is not clear, given that most antidepressant drugs seem to have an ‘antibulimic’ effect, but one possibility is that the dose was too low (range 50 mg to 300 mg; no further details given), although a higher dose might have been associated with even more adverse effects.
Drugs that offer the potential to reduce hospitalization and mortality from SARS-CoV-2 infection: The possible role of the sigma-1 receptor and autophagy
Published in Expert Opinion on Therapeutic Targets, 2021
James Michael Brimson, Mani Iyer Prasanth, Dicson Sheeja Malar, Sirikalaya Brimson, Premrutai Thitilertdecha, Tewin Tencomnao
Despite the roll out of safe and effective vaccines, there has been suspicion and unwillingness by certain sections of the population to take the vaccine. Furthermore, some nations have found difficulty securing a supply of vaccines, while doses in developed nations go to waste due to lack of demand. Without a comprehensive and cooperative worldwide effort to vaccinate enough of the population such that herd immunity takes effect, SARS-CoV-2 will continue to spread, and we will continue to see mutant strains, such as the alpha (B.1.1.7), beta (B.1.351), delta (B.1617.2), and gamma (P.1) variants, which in a worst-case scenario may evade vaccination or prove even more virulent and deadly. For this reason, drugs that lessen the severity of the infection and keep patients out of the ITU will take the strain from healthcare systems worldwide and save thousands of lives. Drugs like fluvoxamine have been identified as drugs that may prevent the worst symptoms of SARS-CoV-2 infection, and small clinical studies have backed this up (Table 1). We wait for more extensive ongoing clinical study results before we can say for sure whether fluvoxamine is indeed as effective as the initial study has indicated.
Depression during pregnancy amidst COVID-19
Published in Hospital Practice, 2021
Balaji Subramanian Srinivasa Sekaran, Steven Lippmann
The most commonly recommended SSRI medications during pregnancy are sertraline, citalopram, fluvoxamine, paroxetine, escitalopram, and fluoxetine; less data is documented for others in this class [7]. Concerns about the cardiac development-safety of prescribing paroxetine are not fully understood, but it is sometimes considered as a possible pharmacotherapeutic option [7]. Prescribing duloxetine and venlafaxine NSRIs is reported to be safe [8]. Yet, there remain issues, changes in indications or efficacy, safety ratings, and restrictions involving SSRI and NSRI prescribing; drugs within each class have different actions. QT prolongation remains a concern with citalopram and escitalopram, questions about the effectiveness of duloxetine, and there are numerous reviews about these medicines [7,9–11]; these have sometimes resulted in changing patterns of prescribing, for example, with more reliance on sertraline and venlafaxine and less for paroxetine. Tricyclic antidepressant medicines have a long-known efficacy. Monotherapy with any of these agents is preferred. Higher dosages are sometimes needed later in pregnancy. Sustained, consistent management and follow-up is important throughout.
Pathophysiology, diagnosis, and pharmacological treatment of prurigo nodularis
Published in Expert Review of Clinical Pharmacology, 2021
Kyle A. Williams, Youkyung S. Roh, Isabelle Brown, Nishadh Sutaria, Pegah Bakhshi, Justin Choi, Sylvie Gabriel, Rajeev Chavda, Shawn G. Kwatra
Finally, antidepressants have been suggested in literature to be an adjunctive therapy that can improve pruritus and aid in healing of scratch lesions in recalcitrant PN, although they often have only modest antipruritic benefits in real-world clinical settings. Antidepressants may be particularly helpful for patients with PN who have a concomitant mental health condition, or patients with stinging or burning sensations at the lesions. The most commonly used antidepressant drugs for PN include paroxetine, fluvoxamine, duloxetine, and amitriptyline [89–92]. Paroxetine is administered at a dose of 10 mg daily for three days followed by a maintenance dose of 20–60 mg daily. Fluvoxamine is administered at a dose of 25 mg daily for three days followed by a maintenance dose of 50–150 mg daily. Duloxetine is administered at a dose of 20–60 mg daily [90]. Amitriptyline is administered at an initial dose of 60 mg for 3 weeks, then dose of 30 mg daily for two weeks and a dose of 10 mg daily for one week [93].