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Clinical Pharmacokinetics

, Volume 41, Supplement 1, pp 13–19 | Cite as

A Pharmacokinetic Profile of Desloratadine in Healthy Adults, Including Elderly

  • Melton Affrime
  • Samir Gupta
  • Christopher Banfield
  • Albert Cohen
Original Research Article

Abstract

Objective: To characterise the pharmacokinetic profile of desloratadine and its main metabolite, 3-hydroxy (3-OH) desloratadine, in a patient population representative of the population studied in the desloratadine clinical efficacy and safety studies, including the elderly.

Design: A multicentre, multidose, open-label pharmacokinetic trial.

Participants: 113 healthy adult volunteers (57 men, 56 women; 95 White, 18 Black) were enrolled, and 112 completed the study.

Interventions: A 5mg oral dose of desloratadine once daily for 10 days.

Main outcome measures: Cmax, tmax, t1/2 and AUC24h.

Results: Steady-state plasma concentrations were attained by day 7. Peak plasma concentrations (Cmax) of desloratadine (mean 3.98 μg/L) and 3-OH desloratadine (mean 1.99 μg/L) were reached at a mean of 3.17 and 4.76 hours (tmax), respectively, after administration. The area under the plasma concentration-time curve from 0 to 24 hours (AUC24h) was 56.9 μg/L · h for desloratadine and 32.3 μg/L · h for 3-OH desloratadine. The mean half-lives (t1/2) of desloratadine and 3-OH desloratadine were 26.8 and 36 hours, respectively. There were no clinically relevant differences in the calculated pharmacokinetic parameters of desloratadine when participants were stratified into 3 age groups (19 to 45, 46 to 64 and 65 to 70 years). Treatment-emergent adverse events occurred in 31 of the 113 participants (3 of the 17 aged ≥65 years reported adverse events). All adverse events were mild to moderate in severity, and none resulted in discontinuation of treatment. There were no consistent clinically relevant changes in blood pressure, pulse, oral body temperature or electrocardiogram evaluations and no reports of syncope or sedation.

Conclusion: Daily administration of desloratadine 5mg is well tolerated. The 27-hour half-life of desloratadine permits once daily administration. No dosage adjustment of desloratadine is required in the elderly.

Keywords

Pharmacokinetic Parameter Allergic Rhinitis Terfenadine Loratadine Astemizole 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Notes

Acknowledgements

Supported by a research grant from Schering-Plough Research Institute, Kenilworth, New Jersey.

References

  1. 1.
    Dykewicz MS, Fineman S, Skoner DP, et al. Diagnosis and management of rhinitis: complete guidelines of the Joint Task Force on Practice Parameters in Allergy, Asthma and Immunology. Ann Allergy Asthma Immunol 1998; 81: 478–518PubMedCrossRefGoogle Scholar
  2. 2.
    Barbey JT, Anderson M, Ciprandi G, et al. Cardiovascular safety of second-generation antihistamines. Am J Rhinol 1999; 13: 235–43PubMedCrossRefGoogle Scholar
  3. 3.
    Ramaekers JG, Uiterwijk MM, O’Hanlon JF. Effects of loratadine and cetirizine on actual driving and psychometric test performance, and EEG during driving. Eur J Clin Pharmacol 1992; 42: 363–9PubMedGoogle Scholar
  4. 4.
    Mann RD, Pearce GL, Dunn N, et al. Sedation with ‘non-sedating’ antihistamines: four prescription-event monitoring studies in general practice. BMJ 2000; 320: 1184–6PubMedCrossRefGoogle Scholar
  5. 5.
    Meltzer EO, Premier BM, Nayak A. Efficacy and tolerability of once-daily 5mg desloratadine, an H1-receptor antagonist, in patients with seasonal allergic rhinitis. Assessment during the spring and fall allergy seasons. Clin Drug Invest 2001; 21(1): 25–32CrossRefGoogle Scholar
  6. 6.
    Gibaldi M, Perrier D. Pharmacokinetics. 2nd ed. New York: Marcel Dekker, 1982Google Scholar
  7. 7.
    Marino M, Glue P, Herron JM, et al. Lack of electrocardiographic effects of multiple high doses of desloratadine. Allergy 2000; 55 Suppl. 63: 279Google Scholar
  8. 8.
    Affrime M, Banfield C, Gupta S, et al. Effect of race and sex on single and multiple dose pharmacokinetics of desloratadine. Clin Pharmacokinet 2002; 41 Suppl. 1: 21–8PubMedCrossRefGoogle Scholar
  9. 9.
    Banfield C, Herron J, Keung A, et al. Desloratadine has no clinically relevant electrocardiographic or pharmacodynamic interactions with ketoconazole. Clin Pharmacokinet 2002; 41 Suppl. 1: 37–44PubMedCrossRefGoogle Scholar
  10. 10.
    Banfield C, Hunt T, Reyderman L, et al. Lack of clinically relevant interaction between desloratadine and erythromycin. Clin Pharmacokinet 2002; 41 Suppl. 1: 29–35PubMedCrossRefGoogle Scholar

Copyright information

© Adis International Limited 2002

Authors and Affiliations

  • Melton Affrime
    • 1
  • Samir Gupta
    • 1
  • Christopher Banfield
    • 1
  • Albert Cohen
    • 2
  1. 1.Department of Clinical PharmacologySchering-Plough Research InstituteKenilworthUSA
  2. 2.Peninsular Testing CorporationMiamiUSA

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