DefinitionThis section has been translated automatically.
Descarboethoxy-Loratadine. Effective main metabolite of loratadine. Selective second-generation H1 antihistamine.
Half-lifeThis section has been translated automatically.
27 h
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Pharmacodynamics (Effect)This section has been translated automatically.
Desloratadine is a non-sedating, long-acting, competitive, selective H1-receptor antagonist. Due to its dissolving behaviour, Desloratadine, in contrast to the H1 antihistamines of the 1st generation, no longer reaches the central nervous system or only in extremely small quantities. As a result, Desloratadine has only a very low sedative effect. In vitro Desloratadine shows a much higher affinity to H1 receptors than Loratadine. As a consequence, besides histamine release, the release of proinflammatory cytokines such as interleukin-3, -4, -6, -8 and -13 as well as the expression of the adhesion molecule P-selectin from endothelial cells is inhibited. In clinical studies in patients with seasonal allergic rhinitis, desloratadine alleviated allergic symptoms such as sneezing, nasal secretion, itching, tear secretion and redness of the eyes and especially nasal obstruction, which is not achieved by other antihistamines. Desloratadine has the highest H1-antihistaminergic potency, high anti-allergic, anti-inflammatory and clinical efficacy and side effect rates at placebo level.
IndicationThis section has been translated automatically.
Symptoms in allergic rhinitis and chronic idiopathic urticaria.
Limited indicationThis section has been translated automatically.
- Severe renal failure. No proof of efficacy and tolerance in children under 2 years of age (syrup) and children under 12 years of age. (tablets).
- Syrup additionally causes fructose intolerance, glucose-galactose metabolic disorders or saccharase-isomaltase insufficiency.
Pregnancy/nursing periodThis section has been translated automatically.
Insufficient data on use during pregnancy and lactation. As desloratadine enters the breast milk, its use during breastfeeding is not recommended.
Dosage and method of useThis section has been translated automatically.
- Tablets: Adults and children/young people > 12 years: once/day 5 mg p.o.
- Syrup: children 2-5 years: once/day 2,5 ml p.o.; children 6-11 years: once/day 5 ml p.o.; adults and teenagers > 12 years: once/day 10 ml p.o.
Undesirable effectsThis section has been translated automatically.
Rarely fatigue, dry mouth, headaches, gastrointestinal problems.
InteractionsThis section has been translated automatically.
Clinically relevant interactions with other drugs have not yet been identified. The effect of alcohol is not enhanced.
ContraindicationThis section has been translated automatically.
Severe renal failure. Hypersensitivity to the active substance or other ingredients of the preparations.
PreparationsThis section has been translated automatically.
Aerius film tablets, Aerius syrup
Note(s)This section has been translated automatically.
Most effective in reducing the symptoms of allergic rhinitis compared to fexofenadine (180 mg) and loratadine (10 mg). In urticaria the dosage can be significantly increased; according to the current EACCI/GA2LEN/EDF guidelines up to four times the recommended dose (e.g. 2-0-2 Tbl./day).
LiteratureThis section has been translated automatically.
- Borchard U (2003) New H1 antihistamines in comparison. Allergology 1: 23-32
- Greiff L et al (2002) Desloratadine reduces allergen challenge-induced mucinous secretion and plasma exudation in allergic rhinitis. Ann Allergy Asthma Immunol 89: 413-418
- Horak F (2002) Impact and modulation of nasal obstruction. Allergy 57 (Suppl 75): 25-28
- Limon L (2003) Desloratadine: a nonsedating antihistamine. Ann Pharmacother. 37: 237-246
- Monroe E et al (2003) Efficacy and safety of desloratadine 5 mg once daily in the treatment of chronic idiopathic urticaria: a double-blind, randomized, placebo-controlled trial. J Am Acad Dermatol 48: 535-541
- Rose water LJ (2002) Treatment of allergic rhinitis. On J Med 16 (Suppl 9A): 17-24
- Simons FE et al (2003) Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. J Allergy Clin Immunol 111: 617-622
- Simons FE (2002) Comparative pharmacology of H1 antihistamines: clinical relevance. Am J Med 16 (Suppl 9A): 38-46
- Simons FE et al (2003) Clinical pharmacology of H1-antihistamines in the skin. J Allergy Clin Immunol 110: 777-783
- Tedeschi A et al (2003) Chronic urticaria: a role for newer immunomodulatory drugs? Am J Clin Dermatol 4: 297-305
Prof. Dr. med. Peter Altmeyer