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Review

Therapeutic advantages of third generation antihistamines

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Pages 1045-1054 | Published online: 23 Feb 2005

Bibliography

  • BLACK JW, DUNCAN WA, DURANT CJ, GANELLIN CR, PARSONS EM: Definition and antagonism of histamine 112 receptors. Nature (1972) 236:385–390.
  • HOECHST MARION ROUSSEL, INC. AND BAKER NORTON PHARMACEUTICALS, INC.: Terfenadine; proposal to withdraw approval of two new drug applications and one abbreviated new drug application; opportunity for a hearing. Federal Register (1997) 62:1889–1892.
  • ••Documents the history of second generation antihistaminesand explains FDA policy on arrhythmia liabilities. Also makes it clear why fexofenadine was fast-tracked, and how it changed the FDA stance on terfenadine.
  • SIMONS FER, SIMONS KJ: The pharmacology and use of Hi-receptor-antagonist drugs. New Engl. J. Med. (1994) 330:1663–1670.
  • ••Good review covering pharmacology, clinical efficacy,ADME and side-effects of first and second generation agents.
  • TIMMERMAN H: Factors involved in the central nervous system effects of Hi-blockers. In: Therapeutic Index of Antihistamines. Church MK, Rihoux J-P (Eds.), Hogrefe and Huber, Lewiston, NY, USA (1992):19–31.
  • HOLGATE ST: Antihistamines in the treatment of asthma. Clin. Rev. Allergy (1994) 12:65–78.
  • •Comprehensive review of mechanisms and clinical efficacy.
  • EKSTROM T, OSTERMAN K, ZETTERSTROM 0: Lack of ef-fect of loratadine on moderate to severe asthma. Ann. Allergy Asthma Immunol (1995) 75:287–289.
  • WOOD-BAKER R, SMITH R, HOLGATE ST: A double-blind, placebo-controlled study of the effect of the spe-cific histamine Hi-receptor antagonist, terfenadine, in chronic severe asthma. Br. J. Clin. Pharmacol. (1995) 39:671–675.
  • GARTEIZ DA, HOCH RH, OKERHOLM RA: Pharmacoki-netic and biotransformational studies of terfenadine in man. Drug Res. (1982) 32:1185–1190.
  • WOOSLEY RL: Cardiac actions of antihistamines. Ann. Rev. Pharmacol. Toxicol (1996) 36:233–252.
  • ••Comprehensive review by an FDA advisor. Details historyand mechanisms of cardiac toxicity with both first and sec-ond generation antihistamines.
  • JANSSENS MM-L: Astemizole: a non-sedating antihista-mine with fast and sustained activity. Clin. Rev. Allergy (1993) 11:35–63.
  • KALINER MA: Nonsedating antihistamines: pharmacol-ogy, clinical efficacy and adverse effects. Am. Fam. Phy-sician (1992) 45:1337–1342.
  • ANDRI L, SENNA GE, BETTELI C et al. A comparison of the efficacy of cetirizine and terfenadine. A double- blind, controlled study of chronic idiopathic urticaria. Allergy (1993) 48:358–365.
  • TABORDA-BARATA L, JACOBSON M, WALKER S et al.: Ef-fect of cetirizine and prednisolone on cellular infiltra-tion and cytokine mRNA expression during allergen-induced late cutaneous responses. Clin. Exp. Allergy (1996) 26:68–78.
  • OKADA C, EDA R, MIYAGAWA H et al.: Effect of cetirizine on human eosinophil superoxide generation, eosino-phil chemotaxis and eosinophil peroxidase in vitro. Int. Arch. Allergy Immunol. (1994) 103:384–390.
  • MICHEL L, DEVOS C, RIHOUX JP et al.: Inhibitory effect of oral cetirizine on in vivo antigen-induced histamine and PAF-acether release and eosinophil recruitment in human skin. J. Allergy Clin. Immunol (1988) 82:101–109.
  • ADELSBERG BR: Sedation and performance issues in the treatment of allergic conditions. Arch. Intern. Med. (1997) 157:494–500.
  • WOOSLEY RL, CHEN Y, FREIMAN JP, GILLIS RA: Mecha-nism of the cardiotoxic actions of terfenadine. JAMA (1993) 269:1532–1536.
  • RAMPED, WIBLE B, BROWN AM, DAGE RC: Effects of ter-fenadine and its metabolites on a delayed rectifier It channel cloned from human heart. Mol. Pharmacol. (1993) 44:1240–1245.
  • ROY M-L, DUMAINE R, BROWN AM: HERG, a primary human ventricular target of the nonsedating antihista-mine terfenadine. Circulation (1996) 94:817–823.
  • VORPERIAN VR, ZHOU Z, MOHAMMAD S: Torsades de pointes with an antihistamine metabolite: potassium channel blockade with dimethylastemizole. J. Am. Coll. Cardiol (1996) 28:1556–61.
  • SALATA JJ, JURKIEWICZ NK, WALLACE AA: Cardiac elec-trophysiological actions of the histamine Hi-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ. Res. (1995) 76:110–119.
  • LACERDA AE, ROY M-L, LEWIS EW, RAMPE D: Interac-tions of the nonsedating antihistamine loratadine with a Kv1.5-type potassium channel cloned from hu-man heart. Mol Pharmacol (1997) 52:314–322.
  • DELPON E, VALENZUELA C, GAY P: Block of human car-diac Kv1.5 channels by loratadine: voltage-, time- and use-dependent block at concentrations above thera-peutic levels. Cardiovasc. Res. (1997) 35:341–350.
  • CABALLERO R, DELPON E, VALENZUELA C et al: Effect of descarboethoxyloratadine, the major metabolite of lo-ratadine on the human cardiac potassium channel Kv1.5. Br. J. Pharmacol (1997) 122:796–798.
  • HEY JA, DEL PRADO M, SHERWOOD J, KREUTNER W, EGAN RW Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects. Drug Res. (1996) 46 (0:153-158. Comparative dose-response data for various antihistamines against histamine challenges and ECG changes in guinea-pigs.
  • MCCULLOUGH JR, JOLLY SR, FANG KQ, WEISHAAR RE: The effects of astemizole and norastemizole on cardio-vascular responses in conscious dogs. Ann. Allergy Asthma Immunol (1997) 78:143.
  • •Abstract demonstrating superiority of norastemizole over astemizole in terms of ECG changes.
  • YUN CH, OBERHOLM RA, GUENGERICH FP: Oxidation of the antihistamine drug terfenadine in human liver mi-crosomes: role of cytochrome P-450 3A(4) in N-dealkylation and C-hydroxylation. Drug Metab. Dispos. (1993) 21:403–409.
  • LINDQUIST M, EDWARDS IR: Risks of nonsedating anti-histamines. Lancet (1997) 349:1322.
  • ••Letter summarising data from the WHOADR database.Clearly shows high incidence of cardiac rate and rhythm dis-turbances with terfenadine, but also reveals a significant number of reports on both astemizole and loratadine.
  • HEY JA, DEL PRADO M, CUSS FM eta].: Antihistamine ac-tivity, central nervous system and cardiovascular pro-files of histamine Hi antagonists: comparative studies with loratadine, terfenadine and sedating antihista-mines in guinea-pigs. Clin. Exp. Allergy (1995) 25:974–984.
  • BRANNAN MD, REIDENBERG P, RADWANASKI E: Lo-ratadine administered concomitantly with erythro-mycin: Pharmacokinetic and electrocardiographic evaluations. Clin. Pharmacol. Ther. (1995) 58:269–278.
  • BERSTEIN DI, SCHOENWETTER WF, NATHAN RA etal.: Ef-ficacy and safety of fexofenadine hydrochloride for treatment of seasonal allergic rhinitis. Ann. Allergy Asthma Immunol (1997) 79:443–448.
  • Allegra. In: Physicians Desk Reference. Montvale, NJ, USA (1997) :1189–1190.
  • •One of the few comprehensive summaries of fexofenadine available at present.
  • RAO N, WEILERT DR, GRACE MGA, ELLER MG, WEIR SJ:Pharmacokinetics of terfenadine-acid-metabolite, MDL 16,455, in healthy geriatric subjects. Pharmacol Res. (1995) 12:S386.
  • RUSSELL T, ELLER M, HUTCHESON S, OKERHOLM R, MCNUTT B: Effect of renal disease on terfenadine me-tabolite pharmacokinetics. Clin. Pharmacol Ther. (1993) 56:162.
  • MCCULLOUGH JR, BUTLER HT, FANG KQ, HANDLEY DA:Receptor binding properties of astemizole and its me-tabolite norastemizole. Ann. Allergy Asthma Immunol (1997) 78:144.
  • HANDLEY DA, MCCULLOUGH JR, FANG KQ, WRIGHT SE,SMITH ER: Comparative antihistamine effects of astemizole and a metabolite, norastemizole. Ann. Al-lergy Asthma Immunol (1997) 78:144.
  • •Abstract showing that norastemizole is 20- to 40-times more potent than astemizole and has a more rapid onset of action.
  • KAMEI C, MIO M, IZUSHI K et al.: Antiallergic effects of major metabolites of astemizole in rats and guinea pigs. Drug Res. (1991) 41:932–936.
  • RUBIN PD, DEGRAW SS, KRAUSE AC et al.: Pharmacoki-netics and pharmacodynamics of norastemizole in normal volunteers. Ann. Allergy Asthma Immunol. (1997) 78:144.
  • RUBIN P, DONOGHUE A, DEGRAW S et al.: Effects of varying doses of norastemizole on histamine induced wheal (W) and flare (F) responses and ECG. J. Allergy Immunol. (1998) 101:S248.
  • CASALE T, CLANCY J, DOCKHORN RJ et al.: Norastemi-zole does not affect ECG parameters. J. Allergy Clin. Im-munol (1998) 101:S245.
  • HANDLEY DA, MCCULLOUGH JR, FANG Y, WRIGHT SE,SMITH ER: Descarboethoxyloratadine, a metabolite of loratadine, is a superior antihistamine. Ann. Allergy Asthma Immunol. (1997) 78:143. Abstract showing that DCL has a superior in vitro profile to loratadine in terms of H1 and muscarinic receptor blockade, and lack of effect on cardiac potassium channels.
  • Loratadine - a new antihistamine. The Medical Letter (1993) 35:71–72.
  • Safety of antihistamines reviewed after report. Reuters (1 May 1997).
  • The assessment of the potential for QT interval prolon-gation by non-cardiovascular medicinal products. European Medicines Evaluation Agency (1997).
  • HARIA M, FITTON A, PETERS DH: Loratadine: a reap-praisal of its pharmacological properties and thera-peutic use in allergic disorders. Drugs (1994) 48:617–637.
  • •Review of loratadine's clinical and preclinical activities.
  • LUCK J, EVRARD H: Atrial fibrillation associated with lo- ratadine use. J. Allergy Clin. Immunol. (1995) 95:282.

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