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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Ketotifen is a cycloheptathiophene derivative that selectively blocks histamine H1 receptors and prevents the typical symptoms caused by histamine release. This agent also interferes with the release of inflammatory mediators from mast cells involved in hypersensitivity reactions, thereby decreasing chemotaxis and activation of eosinophils. Ketotifen is indicated as an add-on or prophylactic oral medication in the chronic treatment of mild atopic asthma in children. It is also used in eye drops for the temporary relief of itching of the eye due to allergic conjunctivitis (ketotifen ophthalmic) (1). It has also proven useful in urticaria (4). In pharmaceutical products, ketotifen is employed as ketotifen fumarate (CAS number 34580-14-8, EC number 252-100-0, molecular formula C23H23NO5S) (1).
Urticaria and Angioedema
Published in Pudupakkam K Vedanthan, Harold S Nelson, Shripad N Agashe, PA Mahesh, Rohit Katial, Textbook of Allergy for the Clinician, 2021
Jenny M Stitt, Stephen C Dreskin
Acute urticaria is typically self-limited and responds well to antihistamines. First generation antihistamines such as diphenhydramine and hydroxyzine cause sedation in many patients. Second generation antihistamines such as fexofenadine, cetirizine and loratadine are recommended as first line therapy as they cause minimal or no sedation due to less mobility across the blood-brain barrier. Third generation antihistamines can also be used, including desloratadine and levocetirizine. Superior results are achieved when these medications are taken on a scheduled basis and can block binding of histamine to the histamine receptor, rather than when they are taken to treat already existing hives. In some patients, it is useful to add a first generation antihistamine at night for breakthrough symptoms (Dreskin 2012, Hiragun et al. 2013). Ketotifen is an antihistamine-mast cell stabilizer and can also be used as an alternative agent (Egan and Rallis 1997). NSAIDs and opioids should be discontinued, at least temporarily, in all patients with urticaria if medically tolerable.
Infantile Atopic Dermatitis
Published in Donald Rudikoff, Steven R. Cohen, Noah Scheinfeld, Atopic Dermatitis and Eczematous Disorders, 2014
Sadaf H. Hussain, James R. Treat, Albert C. Yan
Interestingly, in one study of 121 children with atopic dermatitis aged between 1 and 36 months the group receiving ketotifen for 1 year had fewer patients with high IgE compared with those who received placebo (Iikura et al. 1992). In another study of 100 children aged up to 24 months, the group receiving ketotifen had a 25% lower rate of asthma than the control group (Bustos et al. 1995). Finally, in a study of 817 young children aged between 1 and 2 years who received high-dose cetirizine, statistically significant differences in the rates of dust mite-induced asthma (51.5% with cetirizine vs 28.6% with placebo) and grass-associated asthma (58.8% with cetirizine vs 27.8% with placebo) were observed (Diepgen 2002). Although these data are provocative, further studies into the role of antihistamines in the atopic march are needed to validate these initial observations.
Biologics for dengue prevention: up-to-date
Published in Expert Opinion on Biological Therapy, 2023
Adam T Waickman, Krista Newell, Timothy P Endy, Stephen J Thomas
Ketotifen fumarate is a histamine antagonist and mast cell stabilizer and inhibits the release of mediators associated with hypersensitivity reactions. It is currently licensed as an ophthalmic solution for allergic conjunctivitis and as an oral pill to minimize the frequency and severity of asthma attacks [119]. Studies using ketotifen fumarate in DENV infection of cells in vitro demonstrated that ketotifen fumarate reduced the expression of β-hexosamidase, a marker for granule exocytosis during mast cell activation [120]. In a mouse model of DENV infection, ketotifen was demonstrated to reduce the metabolic dysregulation and inflammation associated with infection as compared to control mice [121]. Ketotifen is currently in clinical trials in Singapore as a treatment for vascular leakage associated with severe DENV infection, ClinicalTrials.gov Identifier: NCT02673840.
Mast cell stabilizer modulates Sirt1/Nrf2/TNF pathway and inhibits oxidative stress, inflammation, and apoptosis in rat model of cyclophosphamide hepatotoxicity
Published in Immunopharmacology and Immunotoxicology, 2020
Walaa Yehia Abdelzaher, Abdel Hamid Sayed AboBakr Ali, Nashwa Fathy Gamal El-Tahawy
In this study, CYC significantly increased the level of IL-1 β which was confirmed by immuno-expression of TNF which markedly observed in the liver sections of the CYC group. In the same line studies of Jnaneshwari and his coworkers [38] established the increase in oxidation and inflammation in CYC hepatotoxicity. MC are presented perivascularly producing inflammatory mediators and proinflammatory cytokines [39]. IL-1 activates MC to release inflammatory chemical mediators [40]. The ability of ketotifen as a MCS is preventing the release of allergic mediators from it and antagonizing H1 receptors [14]. Ketotifen also, reduced neurofibroma growth which exaggerated by MC [41] Nrf2 has a negative effect on TNF expression, which suggests that upregulation of Nrf2 by ketotifen may target inactivation of CYC-induced inflammatory signaling pathways [28,42]. The previous studies of Anoush and Khani [43], Refaie and her coworkers [18], and Huang et al. [17] who reported that ketotifen is able to decrease proinflammatory mediators support our results. Rats treated with ketotifen and CYC improved the inflammatory condition by decreasing IL-1 β and confirmed by the decreased number and intensity of TNF immuno-expression in liver tissues of this group. Our results supported faint immuno-expression of TNF.
Thai pediatricians' current practice toward childhood asthma
Published in Journal of Asthma, 2018
Harutai Kamalaporn, Pongpan Chawalitdamrong, Aroonwan Preutthipan
Ketotifen and theophylline are no longer popular. In contrast, a study in 2001 demonstrated that ketotifen was the most popular controller medication, with 90%, while ICS were preferred by only 10% [3]. A 2010 study in Thailand demonstrated that ketotifen and inhaled budesonide were comparable in reducing emergency visits of children with asthma [28]. Ketotifen could be used as an alternative drug for children with a low socio-economic status, but the side effects need to be monitored. The considerations in using these drugs a decade ago had to do with the prices of (relatively) novel ICS that were beyond the reach for most of the population in Thailand rather than lack of recognition of superiority of ICS. This study demonstrated the change in controller patterns in Thailand through different eras.