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Immunologically mediated skin disorders
Published in Ronald Marks, Richard Motley, Common Skin Diseases, 2019
Drug treatment with antihistamines of the H1 receptor blocker type is most effective at relieving symptoms in this disorder. It is better to become familiar with just a few of these than to try to memorize the whole range available. The ‘older’ antihistamines such as promethazine and diphenhydramine are quite effective, but have a hypnotic effect precluding driving or using machinery. Newer antihistamines such as fexofenadine, cetirizine, levocetirizine, loratadine, and desloratadine are very effective, with little or no hypnotic effect. A few patients obtain increased benefit by adding an H2 antagonist such as cimetidine to the H1 antagonist already being administered. In some cases it may be necessary to give higher than the normal recommended doses of the antihistamine, but this should only be considered when a conventional dose has failed and with full knowledge of possible side effects and drug interactions. The normal daily dose of desloratadine is 5 mg but this may be increased to 20 mg if necessary.
Information on level of drugs into breastmilk
Published in Wendy Jones, Breastfeeding and Medication, 2018
Loratadine is a long-acting, non-sedating anti-histamine and is used to treat children from age 2 years. No adverse effects have been seen in breastfeeding infants whose mothers were receiving loratadine. After a single oral dose of loratadine, Hilbert et al. (1988) measured a maximum dose in the breastmilk of six mothers of 29.2 µg per litre, two hours after the mother took 40 mg and a total excretion of 11.7 µg of loratadine and its metabolite desloratadine via breastmilk. In the normal UK dose of 10 mg daily this would represent approximately 3 µg passing to the baby. Relative infant dose quoted as 0.3% (Hale 2017 online access). It is licenced for use in children over 2 years at a dose of 5 mg daily. The BNF states that significant amounts of some anti-histamines are present in breastmilk – although not known to be harmful, manufacturers advise avoiding use in mothers who are breastfeeding.
Information on level of drugs into breastmilk
Published in Wendy Jones, Breastfeeding and Medication, 2013
Desloratadine is the active metabolite of loratadine. There is no data on the transfer into breastmilk. The prodrug loratadine is generally well tolerated and is a better choice in breastfeeding mothers at this time, although data from the Hilbert et al. (1988) study may be extrapolated. It is licensed for use in children over 1 year at a dose of 1.25 mg daily. The BNF states that significant amounts of some anti-histamines are present in breastmilk. Although not known to be harmful, manufacturers advise avoiding use in mothers who are breastfeeding. Probably compatible with breastfeeding as it is the active metabolite of loratadine but no data on levels transferred are available. Use loratadine unless choice is essential.
Desloratadine and loratadine stand out among common H1-antihistamines for association with improved breast cancer survival
Published in Acta Oncologica, 2020
Ildikó Fritz, Philippe Wagner, Per Broberg, Rickard Einefors, Håkan Olsson
Desloratadine in particular stands out as a candidate for cancer therapy based on our findings, and its known properties: it has the highest H1-receptor affinity among these antihistamines, outperforming fexofenadine and other compounds in pharmacokinetic studies [21]. Worth noting is that our findings are based on the use of antihistamines to treat allergies, and it remains to be seen what a therapeutic dose of desloratadine as a drug for the treatment of breast cancer may be, though we suspect that it could be higher, as risk appears to decrease with an increasing cumulative dose. Despite the low dosage and the suspected dilution by prescription-free loratadine use, the possible effects of desloratadine and loratadine that we report here are already comparable to those of chemotherapeutic and endocrine agents currently used in breast cancer therapy [6,8].
Metabolism of desloratadine by chimeric TK-NOG mice transplanted with human hepatocytes
Published in Xenobiotica, 2020
Shotaro Uehara, Nao Yoneda, Yuichiro Higuchi, Hiroshi Yamazaki, Hiroshi Suemizu
Desloratadine, a long-acting tricyclic antihistamine with selective peripheral histamine H1-receptor antagonistic activity, has been widely used to treat seasonal allergic rhinitis and chronic idiopathic urticaria (Morgan et al., 2005). In humans, the major in vivo metabolite of desloratadine is 3-hydroxydesloratadine, which is subsequently converted to 3-hydroxydesloratadine O-glucuronide (Ramanathan et al., 2007). 3-Hydroxydesloratadine and its glucuronide are excreted in roughly equal amounts in human urine and feces, respectively (Ramanathan et al., 2007), while 5- and 6-hydroxydesloratadine are minor metabolites in the urine and feces (Ramanathan et al., 2007). Notably, the formation of 3-hydroxydesloratadine and its glucuronide are reportedly detectable at only trace levels in nonclinical species such as mice, rats and monkeys (Kazmi et al., 2015a; Ramanathan et al., 2005).
The effect of desloratadine on ischemia reperfusion induced oxidative and inflammatory renal injury in rats
Published in Renal Failure, 2020
Huseyin Kocaturk, Fevzi Bedir, Mehmet Sefa Altay, Ebubekir Bakan, Bahadir Suleyman, Gulce Naz Yazici, Mukadder Sunar, Zeynep Suleyman, Halis Suleyman
Desloratadine to be examined in this study for its protective effect against kidney I/R injury, is a potent and non-sedative H1 histamine receptor antagonist used in the symptomatic treatment of urticaria and allergic rhinitis [7]. Desloratadine has been reported to antagonize the increase of MDA, the final product of lipid peroxidation, and to reduce endogenous antioxidant glutathione (GSH) in the allergy model [8]. Roumestan et al. showed that there was a desloratadine inhibited NF-κB production whereas [9] Wu et al. argued that desloratadine inhibited both basal and histamine-induced NF-κB [10]. This data suggested that desloratadine can protect kidney tissue from I/R damage. There is no study in the literature examining the protective effect of desloratadine against renal I/R injury. Therefore, the aim of this study was to examine the effect of desloratadine on kidney I/R injury in albino Wistar male rats using biochemical and histopathological methods.