CONCLUSION
Les études pharmacodynamiques sont une aide pour comprendre
l’effet clinique des médicaments antihistaminiques. Elles défi-
nissent le délai d’apparition de l’activité anti-H1 après la prise du
médicament. Elles évaluent la durée de cette activité, donnée par-
ticulièrement importante pour établir la posologie et le nombre de
prises quotidiennes. Elles mesurent la puissance de l’activité anti-
histaminique au niveau cutané, en utilisant différentes doses d’his-
tamine à un moment donné ou sur une période de 24 heures. Ces
études précliniques permettent de comparer ces données pour dif-
férents antihistaminiques et de prédire l’activité d’un antihistami-
nique en pratique clinique (délai, puissance et durée d’action). Ces
études pharmacodynamiques cutanées ne pourront évidemment
jamais remplacer les essais cliniques, mais elles constituent une
aide indiscutable pour établir les stratégies d’administration des
médicaments en se fondant sur l’étude d’un nombre limité de
sujets volontaires.
■
RÉFÉRENCES BIBLIOGRAPHIQUES
1.Barnes PJ. Histamine and serotonin. Pulm Pharmacol Ther 2001;14(5):
329-39.
2. Pauli G, Frossard N. Étude des antihistaminiques par la technique du “wheal
and flare” : quelle signification faut-il lui accorder ? Rev Fr Allergol 2004;
44:194-8.
3.Simons FER, Mc Millan JLM, Simons KJ. A double-blind, single-dose, cross-
over comparison of cetirizine, terfenadine, loratadine, astemizole, and chlorphe-
niramine versus placebo: suppressive effects on histamine-induced wheals and
flares during 24 hours in normal subjects. J Allergy Clin Immunol 1990;86:540-7.
4. Frossard N, Mélac M, Benabdesselam O, Pauli G. Consistency of the efficacy
of cetirizine and ebastine on skin reactivity. Ann Allergy Asthma Immunol 1998;
80:61-5.
5.Grant JA, Danielson L, Rihoux JP, De Vos C. A double-blind, single dose,
crossover comparison of cetirizine, ebastine, epinastine, fexofenadine, terfena-
dine, and loratadine versus placebo: suppression of histamine-induced wheal
and flare response for 24 h in healthy male subjects. Allergy 1999;54:700-7.
6. Devalia JL, De Vos C, Hanotte F, Baltes E. A randomized, double-blind, cross-
over comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-
induced cutaneous responses in healthy adult volunteers. Allergy 2001;56:50-7.
7.Purohit A, Duvernelle C, Mélac M, Pauli G, Frossard N. Twenty-four hours
activity of cetirizine and fexofenadine in the skin. Ann Allergy Asthma Immunol
2001;86:387-92.
8.Simons FER, Simons KJ. The pharmacology and use of H1-receptor antago-
nist drugs. N Engl J Med 1994;330:1663-70.
9. Simons FER, Murray HE, Simons KJ. Quantitation of H1-receptor antagonists
in skin and serum. J Allergy Clin Immunol 1995;95:759-64.
10. Simons FER. H1-receptor antagonists: safety issues. Ann Allergy Clin
Immunol 1999;83:481-8.
11. Purohit A, Duvernelle C, Mélac M, Benabdesselam O, Pauli G, Fros-
sard N. Consistency and efficacy of cetirizine (10 mg) versus ebastine (20 mg)
at 4 h on skin reactivity. Eur J Clin Pharmacol 1999;55:589-92.
12. Simons FER, Norman AS, Xiaochen G, Simons KJ. Clinical pharmacology
of H1-antihistamines in the skin. J Allergy Clin Immunol 2002;110:777-83.
13. Demoly P, Bousquet J, Manderscheid JC et al. Precision of skin prick and
puncture tests with nine methods. J Allergy Clin Immunol 1991;88:758-62.
14. Frossard N, Walsh GM. Comparing the H1 profile of second generation
antihistamines. Allergy 2000;55:40-5.
15. Frossard N. Pharmacodynamics of H1-antihistamines: from concept to
reality. Clin Exp Allergy Rev 2003;3:87-9.
16. Walsh GM, Annunziato L, Frossard N et al. New insights into the second
generation antihistamines. Drugs 2001;61:207-36.
17. Grant JA, Riethuisen JM, Moulaert B, De Vos C. A double-blind, rando-
mized, single dose, crossover comparison of levocetirizine with ebastine,
fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-
induced wheal-and-flare response during 24 hours in healthy male subjects.
Ann Allergy Asthma Immunol 2002;88:190-7.
18. Purohit A, Mélac M, Pauli G, Frossard N. Twenty-four hours activity and
consistency of activity of levocetirizine and desloratadine in the skin. Br J Clin
Pharmacol 2003;56:388-94.
19. Purohit A, Mélac M, Pauli G, Frossard N. Comparative activity of cetiri-
zine and desloratadine on histamine-induced wheal and flare responses over
24 hours. Ann Allergy Asthma Immunol 2004;92:635-40.
20. Purohit A, Mélac M, Pauli G, Frossard N. Comparative activity of cetiri-
zine and mizolastine on histamine-induced skin wheal and flare responses at
24 h. Br J Clin Pharmacol 2002;53:250-4.
21. Wood-Baker R, Holgate ST. The comparative actions and adverse effect
profile of single doses of H1-receptor antihistamines in the airways and skin of
subjects with asthma. J Allergy Clin Immunol 1993;91:1005-14.
22. Frossard N, Benabdesselam O, Purohit A, Mounedji N, Pauli G. Activity
of ebastine 10 and 20 mg and cetirizine at 24 hours of a steady state treatment
in the skin of healthy volunteers. Fund Clin Pharmacol 2000;14:409-13.
23. Esau S, del Carpio J, Martin JG. A comparison of the effects of ketotifen
and clemastine on cutaneous and airway reactivity to histamine and allergen
in atopic asthmatic subjects. J Allergy Clin Immunol 1984;74:270-4.
24. Frossard N, Vital-Durand D, Mounedji N, Valleteau A. Duration of the
antihistaminic effect following discontinuation of ebastine. Allergy 2001;56:
553-7.
25. Day JH, Briscoe M, Rafeiro E, Chapman P, Kramer B. Comparative
onset of action and symptom relief with cetirizine, loratadine or placebo in an
environmental exposure unit in subjects with seasonal allergic rhinitis: confir-
mation of a test system. Ann Allergy Clin Immunol 2001;87:474-81.
26. Horak F, Stubner P, Zieglmayer R et al. Controlled comparison of the
efficacy and safety of cetirizine 10 mg o.d. and fexofenadine 120 mg o.d. in
reducing symptoms of seasonal allergic rhinitis. Int Arch Allergy Immunol
2001;125:73-9.
27. Van Cauwenberge, Juniper EF, and the STAR study investigating group.
Comparison of the efficacy, safety, and quality of life of fexofenadine hydro-
chloride 120 mg, loratadine 10 mg and placebo, once a day in the treatment of
seasonal allergic rhinitis. Clin Exp Allergy 2000;30:891-9.
28. Persi L, Demoly P, Harris AG, Tisserand B, Michel FB, Bousquet J. Compa-
rison between nasal provocation tests and skin tests in patients treated with lora-
tadine and cetirizine. J Allergy Clin Immunol 1999;103:591-4.
29. Simons FER, Norman AS, Xiaochen G, Simons KJ. Skin concentrations of
H1-receptor antagonists. J Allergy Clin Immunol 2001;107:526-30.
30. Bousquet J, Godard P, Michel FB. Antihistamines in the treatment of
asthma. Eur Respir J 1992;5:1137-42.
31. Kopferschmitt-Kubler MC, Couchot A, Pauli G. Evaluation of the effect of
oral cetirizine on antigen-induced immediate asthmatic response. Ann Allergy
1990;65:501-3.
32. Rédier H, Chanez P, De Vos C et al. Inhibitory effect of cetirizine on the
bronchial eosinophil recruitment induced by allergen inhalation challenge in
allergic patients with asthma. J Allergy Clin Immunol 1992;90:215-24.
33. Ciprandi G, Bouscaglia S, Pesce G et al. Cetirizine reduces inflammatory
cell recruitment and ICAM-1 (OR CD54) expression on conjunctival epithelium
in both early- and late-phase reations after allergen-specific challenge. J Allergy
Clin Immunol 1995;95:612-21.
34. Campbell A, Chanal I, Carlewski W, Michel FB, Bousquet J. Reduction of
soluble ICAM-1 levels in nasal secretion by H1-blockers in seasonal allergic
rhinitis. Allergy 1997;52:1022-5.
35. Ciprandi G, Catrullo A, Cerquiti P, Tosca M, Fiorino N, Canonica GW.
Loratadine reduces the expression of ICAM-1. Allergy 1998;53:545-6.
MISE AU POINT
184
La Lettre du Pneumologue - Volume VIII - no5 - septembre-octobre 2005