Allergic Rhinitis
John C Watkinson, Raymond W Clarke, Louise Jayne Clark, Adam J Donne, R James A England, Hisham M Mehanna, Gerald William McGarry, Sean Carrie in Basic Sciences Endocrine Surgery Rhinology, 2018
Cysteinyl leukotrienes are a family of eicosanoid inflammatory mediators (LTC4, LTD4 and LTE4) produced in leukocytes, mast cells, eosinophils, basophils and macrophages by the oxidation of arachidonic acid by the enzyme arachidonate 5–lipoxygenase. Their effects are to cause bronchoconstriction, increase vascular permeability and attract inflammatory cells and as such are involved in the processes underlying asthma and allergic rhinitis.63 In the UK montelukast (a leukotriene receptor antagonist) is licensed for the treatment of allergic rhinitis associated with asthma. In studies it was found to be as effective as loratadine in reducing nasal symptoms but less effective than a topical nasal steroid.64 Combined use of cetirizine and montelukast was shown not to improve symptom control above each drug individually in one study65 but to be more effective when combined in another.66 There is a significant variation in responsiveness to LTRAs and a closely monitored trial of treatment may be useful in some patients. It now has a place in the updated ARIA treatment guidelines (Figure 91.3).
Information on level of drugs into breastmilk
Wendy Jones in 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
Wendy Jones in Breastfeeding and Medication, 2013
Loratadine is a long-acting, non-sedating anti-histamine and is used to 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 g per litre, 2 hours after the mother took 40 mg and a total excretion of 11.7 g of loratadine and its metabolite desloratadine via breastmilk. In the normal UK dose of 10 mg daily this would represent approximately 3 g passing to the baby. Relative infant dose quoted as 0.3% (Hale 2012 online access). It is licensed for use in children over 2 years at a dose of 5 mg daily. The BNF states that significant amounts of some antihistamines are present in breastmilk – although not known to be harmful, manufacturers advise avoiding use in mothers who are breastfeeding. Compatible with breastfeeding. Preferred antihistamine for regular use during breastfeeding.
Association of H1-antihistamines with torsade de pointes: a pharmacovigilance study of the food and drug administration adverse event reporting system
Published in Expert Opinion on Drug Safety, 2021
Zahid Ali, Mohammad Ismail, Fahadullah Khan, Hira Sajid
There also exist mixed reports in the literature regarding the association of loratadine with QTIP and TdP, one study reported the possibility that loratadine when dosed higher than the therapeutic one can cause 40% blockade of potassium channel thus causing QTIP and subsequent TdP [31]. One study reported the association of loratadine with TdP mainly due to drug-interactions (especially with amiodarone) and enzyme inhibitors [29]. In our study loratadine was associated with the highest number of QTIP cases, cardiac reactions, electrolyte abnormalities, drug–drug interactions, and overdose cases among new signals (Table 5). Literature also supports the association of chlorpheniramine with QTIP and TdP [32]. Chlorpheniramine can increase the duration of action potential and induce QT prolongation by blocking the hERG channel as evident from studies [33,34]. One study concluded that chlorpheniramine can induce cardiac toxicity when used in higher doses [10].
Second-generation antihistamines: a study of poisoning in children
Published in Clinical Toxicology, 2020
Eva Verdu, Ingrid Blanc-Brisset, Géraldine Meyer, Gaël Le Roux, Chloé Bruneau, Marie Deguigne
In this study, the primary symptoms observed in overdoses were drowsiness and anticholinergic symptoms. These effects, largely described with first-generation antihistamines at therapeutic doses, were observed here, but to a lesser degree and in cases of overdose. In the literature, some rare and isolated cases of overdoses have been described. In an infant of 18 months, 180 mg of cetirizine or 13.8 mg/kg, led to agitation, irritability and then drowsiness [20]. Another infant of 18 months also ingested 180 mg of cetirizine and presented with signs of agitation for 12 h. The child’s ECG was normal in the 15th hour [21]. A child of four years old ingested 60 mg of cetirizine or 3.17 mg/kg and showed signs of drowsiness for six hours. The child’s ECG remained normal [22]. An overdose of 300 mg of loratadine for a child of six years old caused tachycardia of 150/min. No lengthening of the QT interval was observed [23]. No case of overdose in children was described for the other substances.
Evaluation about wettability, water absorption or swelling of excipients through various methods and the correlation between these parameters and tablet disintegration
Published in Drug Development and Industrial Pharmacy, 2018
Baixue Yang, Chen Wei, Yang Yang, Qifang Wang, Sanming Li
In this work, these parameters were systematically measured by WCR, SDT and modified WAS test. MCC, a purified and partially depolymerized cellulose, is always considered as filler or binder [24] with direct compression method. When the above methods were employed, MCC with the high interparticle porosity was chosen as the reference substrate owing to its good capillary action [25]. Loratadine is an antihistaminic drug and belongs to the Class II of the Biopharmaceutics Classification System (BCS) on account of its low solubility and high permeability [26]. When the oral tablets were taken by patients, this drug in salt form existed in acid medium, which increased its solubility in the stomach [27]. In the present work, it was selected as the model drug. In the end, the disintegration of tablets with or without loratadine was carried out in water, which would contribute to verify the correlation between these parameters and tablet disintegration.
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