The pharmacologic profile of desloratadine: a review

doi:10.1034/j.1398-9995.2001.00101.x

Paper

The pharmacologic profile of desloratadine: a review

Published Mar 1, 2001 · B. Henz

Allergy

Q1 SJR score

96

Citations

4

Influential Citations

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Abstract

Desloratadine is a new agent for the treatment of diseases such as seasonal allergic rhinitis and chronic urticaria. The pharmacologic profile of desloratadine offers particular benefits in terms of histamine H1‐receptor binding potency and H1 selectivity. Desloratadine has a half‐life of 21–24 h, permitting once‐daily dosing. No specific cautions are required with respect to administration in renal or hepatic failure, and food or grapefruit juice have no effect on the pharmacologic parameters. No clinically relevant racial or sex variations in the disposition of desloratadine have been noted. In combination with the cytochrome P450 inhibitors, ketoconazole and erythromycin, the AUC and Cmax of desloratadine were increased to a small extent, but no clinically relevant drug accumulation occurred. With high‐dose treatment (45 mg/day for 10 days), no significant adverse events were observed, despite the sustained elevation of plasma desloratadine levels. Specifically, desloratadine had no effects on the corrected QT interval (QTc) when administered alone, at high dose, or in combination with ketoconazole or erythromycin. Preclinical studies also show that desloratadine does not interfere with HERG channels or cardiac conduction parameters even at high dose. Desloratadine is nonsedating and free of antimuscarinic/anticholinergic effects in preclinical and clinical studies. Novel antiallergic and anti‐inflammatory effects have also been noted with desloratadine, a fact which may be relevant to its clinical efficacy.

Literature Review

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Study Snapshot

Desloratadine is a promising new treatment for seasonal allergic rhinitis and chronic urticaria, offering potent H1-receptor binding and no significant adverse events at high doses.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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The pharmacologic profile of desloratadine: a review

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References

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Mast cells play a crucial role in initiation and maintenance of innate and acquired immune reactions, contributing to host defense and immune response.

Preclinical Pharmacology of Desloratadine, a Selective and Nonsedating Histamine H1 Receptor Antagonist2nd Communication: Lack of central nervous system and cardiovascular effects

Desloratadine is a safe and nonsedating histamine H1 receptor antagonist with no central nervous system or cardiovascular effects in preclinical studies.

Preclinical Pharmacology of Desloratadine, a Selective and Nonsedating Histamine H1 Receptor Antagonist

Desloratadine is a more potent antihistaminic agent than loratadine and shows potential antiallergic effects.

Inhibition of cytokine secretion from human leukemic mast cells and basophils by H1‐ and H2‐receptor antagonists

Different antihistamines exhibit distinct inhibitory patterns in cytokine production from human mast cells and basophils, potentially contributing to their anti-inflammatory effects in allergic diseases.

Chemokines and allergic disease.

Chemokines play a crucial role in allergic inflammation, and understanding their genetic variations could improve understanding and treatment of allergic diseases.

Citations

Efficacy and safety of combinations of H1 antihistamines in the treatment of urticaria: A scoping review.

Combining H1 antihistamines leads to enhanced efficacy and reduced safety risks compared to monotherapy in treating urticaria.

The Efficacy and Safety of High Dose (10 mg) of Desloratadine (Dazit® 10) in the Treatment of Chronic Spontaneous Urticaria in India: A Phase III, Multicentric, Open-Label, Single-Arm Study

A twofold dose of desloratadine (Dazit® 10) is effective and safe for improving disease severity and quality of life in nonresponsive moderate to severe chronic spontaneous urticaria patients.

Antimicrobial and antibiofilm activities of desloratadine against multidrug-resistant Acinetobacter baumannii.

Desloratadine, when combined with meropenem, shows potential as a safe and low-cost alternative for treating multidrug-resistant Acinetobacter baumannii infections.

Current status of antihistamine drugs repurposing for infectious diseases

Antihistamines show potential as anti-infective agents, but high doses and lack of systematic preclinical trials hinder their advancement for off-label evaluation.

Current status of antihistamines repurposing for infectious diseases (preprint)

Antihistamines show potential as anti-infective agents, but a lack of systematic preclinical trials hinders their advancement for off-label evaluation.

Assessing the effect of prolonged use of desloratadine on adipose Brillouin shift and composition in rats

Prolonged use of desloratadine increases Brillouin shift in both white and brown adipose tissue types, with a location-dependent effect on protein-to-lipid ratio in brown adipose tissue.

Statistical assessment of in vitro drug release kinetics and quality evaluation of desloratadine orally disintegrating generic tablets available in Bangladesh

Most desloratadine orally disintegrating tablets in Bangladesh do not meet compendial requirements in dissolution behavior, but all products comply with official specifications.

The effect of desloratadine on ischemia reperfusion induced oxidative and inflammatory renal injury in rats

Desloratadine may be useful in treating renal ischemia-reperfusion injury in rats, reducing oxidative stress and inflammation.