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Green Chemistry and Green Catalysts
Published in Ahindra Nag, Greener Synthesis of Organic Compounds, Drugs and Natural Products, 2022
Ahindra Nag, Himadri Sekhar Maity
(-) Paroxetine hydrochloride is a selective serotonin (5-HT) reuptake inhibitor used as an antidepressant. (-) Paroxetine alcohol intermediate can also be prepared by the enzymatic hydrolysis of the corresponding ester derivative or the enzymatic acylation of the primary alcohol in the reaction by Candida antarctica lipases CAL-A and CAL-B by Fernandez et al.48 Both enzymes gave very good results in terms of yield and enatioselectivities. In the reaction process, the two Candida antarctica lipases showed opposite stereochemical preference. CAL-A catalyzes the acylation of the (3S, 4R) alcohol, whereas CAL-B prefers the (3R, 4S) enantiomer. In the last case, the remaining alcohol posses the correct absolute correct for the synthesis of (-) Paroxetine (Figure 1.18).
High Information Content Physiological Biosensors
Published in George K. Knopf, Amarjeet S. Bassi, Smart Biosensor Technology, 2018
Guenter W. Gross, Joseph J. Pancrazio, Kamakshi Gopal
The NNBS was used for a survey of serotonergic and noradrenergic effects in an attempt to quantify responses and compare them to clinical results. As a first step, fluoxetine (Prozac) was selected because of common usage and reports of deaths (Spier and Frontera, 1991; Goeringer et al., 2000; Sallee et al., 2000; Chopra et al., 2004), and because acute effects had not been quantified. Decreased serotonergic neurotransmission is thought to play an important role in depression, and fluoxetine is a selective serotonin reuptake inhibitor that is widely used clinically in the treatment of depression. The primary action of fluoxetine is to selectively inhibit serotonin reuptake into the presynaptic cell by blocking the 5-HT transporters, thus increasing the level of serotonin in the synaptic cleft for binding to the postsynaptic receptor. The optimal clinical dose range recommended is 20–40 mg/day, which translates to a plasma concentration of approximately 1 μM (Altamura et al., 1994). As fluoxetine is lipid soluble with a high brain-to-blood ratio, the brain concentration is close to 20 μM (Karson et al., 1993; Tsuneizumi et al., 1992).
Pulmonary hypertension induced by drugs and toxins
Published in Philippe Camus, Edward C Rosenow, Drug-induced and Iatrogenic Respiratory Disease, 2010
Kim Bouillon, Yola Moride, Lucien Abenhaim, Marc Humbert
Fluoxetine is a selective serotonin reuptake inhibitor (SSRI), as are aminorex and fenfluramines (see Fig. 29.2). However, we are not aware of any report of a relationship between the chronic intake of SSRI antidepressants and PAH in adults. It is estimated that 2–3 per cent of pregnant women receive anti-depressive medication of which the SSRI class of drugs is the most commonly utilized.114 In 1996, Chambers et al. observed in a prospective small cohort an increased risk for perinatal complications among women who took fluoxetine in the third trimester.115 They suggested a possible association between maternal use of fluoxetine late in the third trimester of pregnancy and the risk of PPHN in the infant. Recent data from a retrospective case–control study conducted between 1998 and 2003 by Chambers et al. support the association between the maternal use of SSRIs after the completion of the 20th week of gestation and PPHN in the offspring: 14 infants with PPHN had been exposed to an SSRI compared with 6 in a control group (adjusted odds ratio of 6.1; 95% CI: 2.2–16.8).116 Another cohort study based on the Swedish Medical Birth Register was in favour for this association.117
Eco-friendly based stability-indicating RP-HPLC technique for the determination of escitalopram and etizolam by employing QbD approach
Published in Green Chemistry Letters and Reviews, 2022
Durga Devi Perumal, Manikandan Krishnan, K.S. Lakshmi
Escitalopram + etizolam (ESC) (ETZ) is a blend of two medications, ESC and ETZ, which have anti-anxiety and anti-depressant properties. C20H21FN2O is the chemical formula for ESC. It has the chemistry (1S)−1-[3-(dimethylamino) propyl]−1-(4-fluorophenyl)−1, 3-dihydro-2-benzofuran-5-carbonitrile. C17H15ClN4S is the chemical formula of ETZ. It has the chemistry 4-(2-chlorophenyl)−2-ethyl-9-methyl-6H-thieno[3,2-f] [1,2,4] triazolo [4,3 – a][1,4] diazepine. The ESC and ETZ structures are shown in Figure 1 (11). ESC is a medicine known as a selective serotonin reuptake inhibitor. It works by increasing serotonin levels in the brain. Serotonin is a chemical substance in the brain that aids in the relief of depressive symptoms, including mood and physical symptoms. It also helps with anxiety, panic attacks, and symptoms of obsessive – compulsive disorder. ETZ is a benzodiazepine that induces sleep by boosting GABA activity (a chemical messenger in the brain that serves as a natural nerve-calming agent). Consequently, ESC + ETZ helps relax muscles, reduce anxiety, and fall asleep. This combination has also been approved by the US Food and Drug Administration for use in African – American patients (12). In IP'10, ESC is official, whereas in JP XV, ETI is official (13, 14).
Novel evidence on the effect of tramadol on self-paced high-intensity cycling
Published in Journal of Sports Sciences, 2021
Thomas Zandonai, Darías Holgado, Luis F. Ciria, Mikel Zabala, James Hopker, Tristán Bekinschtein, Daniel Sanabria
Tramadol did, however, exert an effect on physiological responses recorded during exercise. Similar to Bejder et al.’s study (Bejder et al., 2019) (4 bpm in the TT), tramadol induced higher HR than both placebo and paracetamol during the 40 min at 60% of VO2max and the 20-min TT. A reliable difference between tramadol and placebo was also found in Holgado et al.’s (Holgado, Zandonai et al., 2018) Experiment 1 (4 bpm). This outcome could be accounted for by tramadol’s action as both a serotonin and norepinephrine reuptake inhibitor, which can lead to cardiac effects (Behzadi et al., 2018; Chen & Ashburn, 2015). However, the 8 bpm difference reported in the present study could be negligible in practical terms, as it was not followed by changes in performance. In addition, the lack of a reliable difference in Holgado et al.’s (Holgado, Zandonai et al., 2018) Experiment 2 hinders any explanation of the tramadol effect on HR.
Emergency drug usage during flight and airline safety management for passengers
Published in Journal of Toxicology and Environmental Health, Part A, 2021
In this study, a questionnaire was developed in consideration of the emergency drugs and job characteristics of flight attendants in the aircraft (see Supplementary Table S1; Appendix A). The questionnaire items were revised and subsequently adjusted to suit the aviation industry. Further, with the help of flight attendants currently on duty, the list of in-flight emergency medicines onboard domestic airlines was obtained. In the factual survey, the following information: 1) storage location and storage method of in-flight medical supplies, 2) the expiration dates of medical supplies, 3) whether the instruction labels were stored, and 4) whether the pharmaceutical products contained phenylpropanolamine (PPA, a nonselective adrenergic receptor agonist, and norepinephrine reuptake inhibitor used as a decongestant and an appetite suppressant) was obtained. Out of the 120 questionnaires distributed from January 1 to 15, 2020, 115 were collected. Finally, 112 were used for the analysis, excluding three questionnaires containing poor responses. The frequency analysis was performed on the in-flight emergency drugs and demographic characteristics of the respondents, using SPSS 22.0.