Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy.
Chronic idiopathic urticaria (CIU) is a disabling affliction that considerably limits patients' daily activities and interferes with sleep. Clinical studies have shown that histamine H1-receptor antagonists (antihistamines) are highly effective for inhibiting the hives/wheals and pruritus associated with CIU, as well as improving patients' quality of life. Desloratadine is a rapid-acting, once-daily, nonsedating selective H1-receptor antagonist/inverse receptor agonist with proven clinical efficacy in patients with CIU. It has 10-20 times the in vivo H1 receptor-binding affinity of loratadine, its parent compound, and 52-194 times the H1 receptor-binding affinity of cetirizine, ebastine, loratadine, and fexofenadine. Desloratadine displays linear pharmacokinetics after oral administration. Age and sex have no apparent effect on the drug's metabolism and elimination, and food does not affect its bioavailability or absorption. Desloratadine also exerts anti-inflammatory effects via mechanisms that are independent of H1-receptor antagonism. Results from randomized, double-blind, placebo-controlled studies of 6 weeks' duration in adults and adolescents with moderate-to-severe CIU indicate that desloratadine significantly minimizes the severity of pruritus, reduces the number and size of hives, and improves disease-impaired sleep and daily activities. Improvements were noted after a single dose of desloratadine and were maintained over 6 weeks of treatment. Desloratadine was safe and well tolerated in clinical trials of patients with CIU. The adverse effect profile of desloratadine in adults, as well as in children aged from 6 months to 11 years, is comparable to that of placebo. Evaluations of cognitive and psychomotor performance in adults indicate no impairment of function with dosages of desloratadine 5 mg/day. In conclusion, desloratadine is an important therapeutic option for prompt and enduring symptom relief in patients with moderate-to-severe CIU. In addition to efficacy and safety, desloratadine affords a convenient administration regimen, rapid onset of action, and an absence of drug-drug or drug-food interactions. Other important prescribing considerations are that, unlike all first-generation and some second-generation antihistamines, desloratadine is nonsedating at its clinically approved dosage and does not impair psychomotor function.
DuBuske
Lawrence
L
Immunology Research Institute of New England, Gardner, Massachusetts 01440, USA. research@irine.org
D000085:Acetates / Q000627:therapeutic use; D000293:Adolescent; D000328:Adult; D002648:Child; D002908:Chronic Disease; D003521:Cyclopropanes; D004359:Drug Therapy, Combination; D039563:Histamine H1 Antagonists, Non-Sedating / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007223:Infant; D020024:Leukotriene Antagonists / Q000627:therapeutic use; D017336:Loratadine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D011788:Quality of Life; D011804:Quinolines / Q000627:therapeutic use; D013440:Sulfides; D014581:Urticaria / Q000145:classification / Q000188:drug therapy*
D000085:Acetates; D003521:Cyclopropanes; D039563:Histamine H1 Antagonists, Non-Sedating; D020024:Leukotriene Antagonists; D011804:Quinolines; D013440:Sulfides; D017336:Loratadine; C121345:desloratadine; C093875:montelukast