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Nutritional and Dietary Supplementation during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Phenothiazines are used for several medical indications (nausea, vomiting, psychotic disorders, mild pain). This drug class is also effective as an antidyskinetic and a mild sedative. Prochlorperazine, chlorpromazine, and promethazine are the most commonly used phenothiazine derivatives used to treat nausea and vomiting during pregnancy. Phenothiazine use during pregnancy may be associated with extrapyramidal symptoms in the mother as well as the fetus, but these adverse effects are uncommon. The phenothiazine class does not seem to be associated with an increased frequency of congenital anomalies when used during gestation. The frequency of birth defects was not increased among infants of 315 exposed to phenothiazines during the first trimester (Rumeau-Rouquette et al., 1977).
Nausea/Vomiting of Pregnancy and Hyperemesis Gravidarum
Published in Vincenzo Berghella, Maternal-Fetal Evidence Based Guidelines, 2022
Phenothiazines (prochlorperazine [Compazine], promethazine [Phenergan]) appear to be safe in pregnancy. A case-control study of promethazine showed no evidence of increase risk/rate of congenital anomalies in humans [95, 101]. Phenothiazines are often used in addition to or instead of antihistamines. The level 1 evidence for effectiveness is limited. As stated earlier, metoclopramide (with one IM shot of 50 mg of pyridoxine) is superior in decreasing vomiting and subjective improvement compared to monotherapy with either prochlorperazine or promethazine in NVP [86], it had similar efficacy with reduced side effects in HG [90]. Compared to ondansetron, there was no difference in severity of nausea in the setting of HG [100]. Two studies compared promethazine and corticosteroids in patients with HG. One study [102] found a decreased rate of hospital readmission with corticosteroids, the other study [103] found an increase in n/v at 48 hours but not after 17 days with prednisolone [2].
Antipsychotics: pharmacology
Published in Kathy J Aitchison, Karena Meehan, Robin M Murray, First Episode Psychosis, 2021
Kathy J Aitchison, Karena Meehan, Robin M Murray
Chronic dosage leads to a fourth phase in drug clearance known as deep compartment washout. Urinary metabolites may be detected up to 3 months after the discontinuation of chronically dosed phenothiazines;160 this deep compartment effect is likely to be even greater for depot preparations and may contribute to the delay in relapse seen on cessation of a depot preparation as compared to cessation of an equivalent dose of oral antipsychotic.
Antihistamines, phenothiazine-based antipsychotics, and tricyclic antidepressants potently activate pharmacologically relevant human carbonic anhydrase isoforms II and VII
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Francesco Fiorentino, Alessio Nocentini, Dante Rotili, Claudiu T. Supuran, Antonello Mai
Furthermore, the evidence collected through this study offers additional insights into the pharmacological profile and therapeutic effects of clinically employed drugs such as antihistamines, phenothiazine-based antipsychotics, and TCAs. Indeed, both their therapeutic activity and adverse effects are connected to polypharmacology-based mechanisms, and the enhancement of hCA activity should now be considered. Ultimately, the present research may provide novel perspectives into the complex network linking hCA function and CNS homeostasis. Indeed, while CAAs have only recently been considered for their pharmacological applications in memory and cognition therapy,43,45,47,48 their potential is undeniable, and research aimed at investigating hCA activation at central level is critical for the development of new drugs with possible applications in neurodegeneration.
Current understanding of the etiology of cyclic vomiting syndrome and therapeutic strategies in its management
Published in Expert Review of Clinical Pharmacology, 2022
Rosita Frazier, Thangam Venkatesan
5HT3 antagonists are highly effective in treating acute, delayed, and anticipatory chemotherapy-induced nausea and vomiting [84]. However, there are no clinical trials in CVS, although they are frequently used in these patients. It would likely not be logistically feasible to conduct such studies in CVS given its proven efficacy as an anti-emetic and its widespread use. The 2019 guideline on the management of CVS in adults recommends ondansetron as a first-line agent in aborting an episode of CVS. The recommended dose of ondansetron is 8 mg every 8 hours either as a sublingual tablet or intravenously. Adding a benzodiazepine and/or a phenothiazine for sedation is also recommended [56]. Ondansetron is well tolerated, and side effects include headache, dizziness, drowsiness, diarrhea, or constipation [85].
Phenylalanine 4-monooxygenase: the “sulfoxidation polymorphism”
Published in Xenobiotica, 2020
Stephen C. Mitchell, Glyn B. Steventon
Methylene blue was the first xenobiotic cited in the literature as undergoing oxygenation at the sulfur moiety (Underhill & Closson, 1905). The metabolite referred to as methylene azure was presumed to be the sulfone derivative (Williams, 1959), but now the several methylene azures (and thionine) are recognised as a series of sequential N-demethylated products (Disanto & Wagner, 1972). Likewise, the sulfone of mustard gas, presumably formed via the sulfoxide, was postulated in a 1921 publication but was not experimentally confirmed at that time (Flury & Wieland, 1921). However, later work has shown the existence of both these sulfoxide and sulfone metabolites (Davison et al., 1961; Somani & Babu, 1989). The first demonstration of the in vivo formation of a xenobiotic sulfoxide metabolite was that of the anthelmintic, phenothiazine, reported in 1947 (Clare, 1947). This compound itself enjoyed a period of widespread fame as an effective vermifuge but is now known mainly as the parent molecule of a host of clinically useful phenothiazine drugs.