Next generation antihistamines: therapeutic rationale, accomplishments and advances

Bibliography

• HANDLEY DA, MAGNETTI A, HIGGINS AJ: Therapeutic advantages of third generation antihistamines. Expert Opin. Investig. Drugs (1998) 7:1045–1054.
   PubMedGoogle Scholar
• SIMONS FER, SIMONS KJ: The pharmacology and use of Hl-receptor-antangonist drugs. N Engl. Med. (1994) 330:1663–1670.
   PubMed Web of Science ®Google Scholar
• ••A pertinent review of the pharmacology,pharmacokinetics, efficacy and safety of second generation antihistamines.
   Google Scholar
• SIMONS FER, FRASER TG, REGGIN JD, SIMONS KJ: Comparison of the central nervous system effects produced by six H1-receptor antagonists. Clin. Exp. Allergy (1996) 26:1092–1097.
   PubMed Web of Science ®Google Scholar
• SALMUN LM, GATES D, SCHARF M et al.: Loratadine versus cetirizine: assessment of somnolence and motivation during the workday. Clin. flier. (2000) 22:573–582.
   Google Scholar
• WILSON JD, HILLAS JL: Astemizole: a new long-acting antihistamine in the treatment of seasonal allergic rhinitis. Clin. Allergy (1983) 13:131–140.
   PubMedGoogle Scholar
• KRSTENANSKY PM, CLUXTON RJ, Jr.: Astemizole: a long-acting, nonsedating antihistamine. Drug Int& Clin. (1987) 21:947–953.
   Google Scholar
• KEMP JP: Special considerations in the treatment of seasonal allergic rhinitis in adolescents: the role of antihistamine therapy. Clin. Pediatr. (Phil& (1996) 35:383–389.
   PubMed Web of Science ®Google Scholar
• WIHL JA, PETERSEN BN, PETERSEN LN et al.: Effect of the nonsedative H1-receptor antagonist astemizole in perennial allergic and nonallergic rhinitis. I Allergy Clin. bronunol (1985) 75:720–727.
   PubMed Web of Science ®Google Scholar
• WOOSLEY RL: Cardiac actions of antihistamines. Ann. Rev Pliarinacol Toxicol (1996) 36:233–252.
   PubMed Web of Science ®Google Scholar
• ••A review of the cardiovascular effects ofsecond generation antihistamines.
   Google Scholar
• SALATAJJ, JURKIEWICZ NK, WALLACE AA et al.: Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine. Circ. Res. (1995) 76:110–119.
   PubMed Web of Science ®Google Scholar
• WOOSLEY RL, CHEN Y, FREIMAN JP, GILLIS RA: Mechanism of the cardiotoxic actions of terfenadine. JAMA (1993) 269:1532–1536.
   PubMed Web of Science ®Google Scholar
• ••Clinical data on the cardiovascular effects ofterfenadine and its metabolites.
   Google Scholar
• RAMPE D, WIBLE B, BROWN AM, DAGE RC: Effects of terfenadine and its metabolites on a delayed rectifier K+ channel cloned from human heart. Ma Pliarinacol (1993) 44:1240–1245.
   Google Scholar
• ROY M, DUMAINE R, BROWN AM: HERG, a primary human ventricular target of the nonsedating antihistamine terfenadine. Circulation (1996) 94:817–823.
   PubMed Web of Science ®Google Scholar
• ZHOU Z, VORPERIAN VR, GONG Q, ZHANG S, JANUARY CT: Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. Cardiovasc. Electrophysiol (1999) 10:836–843.
   PubMed Web of Science ®Google Scholar
• HEY JA, DEL PRADO M, CUSS FM et al: Antihistamine activity, central nervous system and cardiovascular profiles of histamine H1 antagonists: comparative studies with loratadine, terfenadine and sedating antihistamines in guinea-pigs. Clin. Exp. Allergy (1995) 25:974–984.
   PubMed Web of Science ®Google Scholar
• 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) 46:153–158.
   PubMed Web of Science ®Google Scholar
• MCCULLOUGH JR, JOLLY SR, FANGKO, WEISHAAR RE: The effects of astemizole and norastemizole on cardiovascular responses in conscious dogs. Ann. Allergy Asthma Immunol (1997) 78. Abstract P163.
   Google Scholar
• BENTON RE, HONIG PK, ZAMANI K, CANTILENA LR, WOOSLEY RL: Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. Clin. Pharmacol Ther. (1996) 59:383–388.
   PubMed Web of Science ®Google Scholar
• HANDLEY DA, HONG Y, BAKALE R, SENANAYAKE C: Norastemizole. Drugs Fut. (1998) 23:966–969.
   Google Scholar
• ••A review of the predinical and clinicalpharmacology of tecastemizole.
   Google Scholar
• FOOD AND DRUG ADMINISTRATION: 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.
   Google Scholar
• ••Documentation of the events leading up tothe withdrawal of terfenadine from the market.
   Google Scholar
• BRANNAN MD, REIDENBERG P, RADWANSKI E et al.: Loratadine administered concomitantly with erythromycin: pharmacokinetic and electrocardiographic evaluations. Clin. Pharmacol The]: (1995) 58:269–278.
   PubMed Web of Science ®Google Scholar
• SALE ME, BARBEY JT, WOOSLEY RL et al.: The electrocardiographic effects of cetirizine in normal subjects. Clin. Pharmacol The]: (1994) 56:295–301.
   PubMed Web of Science ®Google Scholar
• CRUMB WJ, Jr.: Loratadine blockade of K+ channels in human heart: comparison with terfenadine under physiological conditions. J. Pharmacol Exp. Ther. (2000) 292:261–264.
   PubMed Web of Science ®Google Scholar
• GARTEIZ DA, HOOK RH, WALKER BJ, OKERHOLM RA: Pharmacokinetics and biotransformation studies of terfenadine in man. Drug Res. (1982) 32:1185–1190.
   PubMed Web of Science ®Google Scholar
• SIMONS FER, SIMONS KJ: Clinical pharmacology of new histamine H1 receptor antagonists. Clin. Pharmacokinet. (1999) 36:329–352.
   PubMed Web of Science ®Google Scholar
• RUSSELL T, STOLTZ M, WEIR S: Pharmacokinetics, pharmacodynamics, and tolerance of single- and multiple-dose fexofenadine hydrochloride in healthy male volunteers. Clin. Pharmacol Ther. (1998) 64:612–621.
   PubMed Web of Science ®Google Scholar
• GUPTA S, BANFIELD C, KANTESARIA B et al.: Pharmacokinetic and safety profile of desloratadine and fexofenadine when coadministrated with azithromycin: a randomized, placebo-controlled, parallel-group study. Clin. Ther. (2001) 23:451–466.
   PubMed Web of Science ®Google Scholar
• HAMMAN MA, BRUCE MA, HAEHNER-DANIELS BD, HALL SD: The effect of rifampin administration on the disposition of fexofenadine. Clin. Pharmacol Ther. (2001) 69:114–121.
   PubMed Web of Science ®Google Scholar
• MILNE RW, LARSEN LA, JERGENSEN KL et al.: Hepatic disposition of fexofenadine: influence of the transport inhibitors erythromycin and dibromosulphothalein. Pharm. Res. (2000) 17:1511–1515.
   PubMed Web of Science ®Google Scholar
• RACHELEFSKY GS, SALMUN LM, BANFIELD C: Predictability of desloratadine: lack of clinical interaction with food and concomitant medications. Allergy Clin. Immunol (2001) 107. Abstract 534.
   Google Scholar
• STOLTZ M, ARUMUGHAM T, LIPPERT C et al.: Effect of food on the bioavailability of fexofenadine hydrochloride. Biopharm. Drug Dispos. (1996) 18:645–648.
   Web of Science ®Google Scholar
• BRONSKY EA, FALLIERS CJ, KAISER HB, AHLBRANDT R, MASON J: Effectiveness and safety of fexofenadine, a new nonsedating H1-receptor antagonist, in the treatment of fall allergies. Allergy Asthma Proc. (1998) 19:135–141.
   PubMed Web of Science ®Google Scholar
• BERNSTEIN DI, SCHOENWETTER WE NATHAN RA et al.: Efficacy and safety of fexofenadine hydrochloride for treatment of seasonal allergic rhinitis. Ann. Allergy Asthma Immunol (1997) 79:443–448.
   PubMed Web of Science ®Google Scholar
• ••One of the first studies demonstrating theefficacy and safety of fexofenadine for the treatment of allergy symptoms.
   Google Scholar
• CASALE TB, ANDRADE C, QU R: Safety and efficacy of once-daily fexofenadine HC1 in the treatment of autumn seasonal allergic rhinitis. Allergy Asthma Proc. (1999) 20:193–198.
   PubMed Web of Science ®Google Scholar
• MELTZER EO, CASALE TB, NATHAN RA, THOMPSON AK: Once-daily fexofenadine HC1 improves quality of life and reduces work and activity impairment in patients with seasonal allergic rhinitis. Ann. Allergy Asthma Immunol (1999) 83:311–317.
   PubMed Web of Science ®Google Scholar
• DAY JH, BRISCOE MP, WELSH A et al.: Onset of action, efficacy, and safety of a single dose of fexofenadine hydrochloride for ragweed allergy using an environmental exposure unit. Ann. Allergy Asthma Immunol (1997) 79:533–540.
   PubMed Web of Science ®Google Scholar
• GRANT JA, DANIELSON L, RIHOUX JP, DEVOS C: A double-blind, single-dose, crossover comparison of cetirizine, ebastine, epinastine, fexofenadine, terfenadine, and loratadine versus placebo: suppression of histamine-induced wheal and flare response for 24 h in healthy male subjects. Allergy (1999) 54:700–707.
   PubMed Web of Science ®Google Scholar
• SIMONS FER, SIMONS KJ: Peripheral H1-blockade effect of fexofenadine. Ann. Allergy Asthma Immunol (1997) 79:530–532.
   PubMed Web of Science ®Google Scholar
• BALLMER-WEBER BK, GAX-COLLET C, WOTHRICH B: Inhibition of histamine or allergen-induced wheals by a single dose of acrivastine, fexofenadine or cetirizine. Invest. Allergol Clin. Immunol (1999) 9:351–355.
   PubMed Web of Science ®Google Scholar
• PUROHIT A, DUVERNELLE C, MELAC M, PAULI G, FROSSARD N: Twenty-four hours of activity of cetirizine and fexofenadine in the skin. Ann. Allergy Asthma Immunol (2001) 86:387–392.
   PubMed Web of Science ®Google Scholar
• TERRIEN MH, RAHM F, FELLRATH JM, SPERTINI F: Comparison of the effects of terfenadine with fexofenadine on nasal provocation tests with allergen. J. Allergy Clin. Immunol (1999) 103:1025–1030.
   PubMed Web of Science ®Google Scholar
• ••Clinical evidence that fexofenadine relievesallergy symptoms better than or just as well as terfenadine.
   Google Scholar
• HOWARTH PH, STERN MA, ROI L, REYNOLDS R, BOUSQUET J: Double-blind, placebo-controlled study comparing the efficacy and safety of fexofenadine hydrochloride (120 and 180 mg once daily) and cetirizine in seasonal allergic rhinitis. Allergy Clin. Immunol (1999) 104:927–933.
   Google Scholar
• VAN CAUWENBERGE P, JUNIPER EF: Comparison of the efficacy, safety and quality of life provided by fexofenadine hydrochloride 120 mg, loratadine 10 mg and placebo administered once daily for the treatment of seasonal allergic rhinitis. Clin. Exp. Allergy (2000) 30:891–899.
   PubMed Web of Science ®Google Scholar
• SIMONS FER, JOHNSTON L, GU X, SIMONS KJ: Suppression of the early and late cutaneous allergic responses using fexofenadine and montelukast. Ann. Allergy Asthma Immunol (2001) 86:44–50.
   PubMed Web of Science ®Google Scholar
• SUSSMAN GL, MASON J, COMPTON D, STEWART J, RICARD N: The efficacy and safety of fexofenadine HC1 and pseudoephedrine, alone and in combination, in seasonal allergic rhinitis. Allergy Clin. Immunol (1999) 104:100–106.
   Google Scholar
• WILSON AM, ORR LC, SIMS EJ, LIPWORTH BJ: A comparison of once daily fexofenadine (FEM alone or the combination of montelukast plus loratidine (ML + LT) on symptoms and nasal peak flow in seasonal allergic rhinitis (SAM. I Allergy Clin. Immunol (2001) 107. Abstract 1022.
   Google Scholar
• NELSON HS, REYNOLDS R, MASON J: Fexofenadine HC1 is safe and effective for treatment of chronic idiopathic urticaria. Ann. Allergy Asthma Immunol (2000) 84:517–522.
   PubMed Web of Science ®Google Scholar
• ABDELAZIZ MM, DEVALIA JL, KHAIR OA et al.: Effect of fexofenadine on eosinophil-induced changes in epithelial permeability and cytokine release from nasal epithelial cells of patients with seasonal allergic rhinitis. I Allergy Gin. Immunol (1998) 101:410–420.
   PubMed Web of Science ®Google Scholar
• MEEVES S, JOETHEM A, GELFAND EW: Fexofenadine exhibits antiallergic activity in vitro and vivo. .1. Allergy Gin. Immunol (2001) 107. Abstract 599.
   Google Scholar
• AMON U, AMON S: Fexofenadine inhibits activation of basophils and eosinophils in ex vivo-in vitro experiments. I Allergy Clin. Immunol (2001) 107. Abstract 497.
   Google Scholar
• PAOLIERI F, BATTIFORA M, RICCIO AM et al.: Terfenadine and fexofenadine reduce M vitro ICAM-1 expression on human continuous cell lines. Ann. Allergy Asthma Immunol (1998) 81:601–607.
   PubMed Web of Science ®Google Scholar
• TRIGGIANI M, GENTILE M, SECONDO A et al: Histamine H1-receptor-mediated activation of human lung macrophages and antagonism and fexofenadine. Allergy Clin. Immunol (2001) 107. Abstract 155.
   Google Scholar
• HANDLEY D: The evolution of modern III generation antihistamines. Pharmaceutical News (2000) 7:21–24.
   Google Scholar
• PRATT CM, MASON J, RUSSELL T, REYNOLDS R, AHLBRANDT R: Cardiovascular safety of fexofenadine HC1. Am. J. Cardiol (1999) 83:1451–1454.
   PubMed Web of Science ®Google Scholar
• PRATT C, BROWN AM, RAMPE D et al: Cardiovascular safety of fexofenadine HC1. Clin. Exp. Allergy (1999) 29 (Suppl. 3):212–216.
   Google Scholar
• PINTO YM, VAN GELDER IC, HEERINGA M, CRIJNS HJ: QT lengthening and life-threatening arrhythmias associated with fexofenadine. Lancet (1999) 353:980.
   PubMed Web of Science ®Google Scholar
• GIRAUD T: QT lengthening and arrhythmias associated with fexofenadine. Lancet (1999) 353:2072–2073.
   PubMed Web of Science ®Google Scholar
• VERMEEREN A, O'HANLON JF: Fexofenadine's effects, alone and with alcohol, on actual driving and psychomotor performance. Allergy Clin. Immunol (1998) 101:306–311.
   Google Scholar
• HINDMARCH I, SHAMSI Z, STANLEY N, FAIRWEATHER DB: A double-blind, placebo controlled investigation of the effects of fexofenadine, loratadine and promethazine on cognitive and psychomotor function. Br. Pharmacol (1999) 48:200–206.
   Web of Science ®Google Scholar
• HINDMARCH I, SHAMSI Z: A double-blind, placebo controlled investigation of the effects of fexofenadine on objective assessment of cognitive abilities, psychomotor function and car driving skills. Allergy Clin. Immunol (2001) 107. Abstract 515.
   Google Scholar
• WEILER JM, BLOOMFIELD JR, WOODWORTH GG et al.: Effects of fexofenadine, diphenhydramine, and alcohol on driving performance. A randomized, placebo-controlled trial in the Iowa driving simulator. Ann. Intern. Med. (2000) 132:354–363.
   PubMed Web of Science ®Google Scholar
• ANTHES J, ECKEL S, RICHARD C et al:Characterization of [3h]desloratadine at the human H1 receptor. I Allergy Clin. Immunol (2001) 107. Abstract 526.
   Google Scholar
• 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. Abstract P164.
   Google Scholar
• ELLIS J, SEIDENBERG M: Desloratadine interacts with muscarinic acetylcholine receptors with high affinity and antagonizes the cyclic AMP response at the M2 subtype. Allergy Clin. Immunol (2001) 107:528.
   Google Scholar
• KREUTNER W, HEY JA, ANTHES Jet al.: Preclinical pharmacology of desloratadine, a selective and nonsedating histamine HI receptor antagonist. 1st communication: receptor selectivity, antihistaminic activity, and antiallergenic effects. Arzneimittelforschung (2000) 50:345-352. Key clinical data demonstrating the efficacy of desloratadine.
   Google Scholar
• HENZ BM: The pharmacologic profile of desloratadine: a review. Allergy (2001) 56\(Suppl. 65):7–13.
   Google Scholar
• GEHA RS, MELTZER EO: Desloratadine: anew, nonsedating, oral antihistamine. Allergy Clin. Immunol (2001) 107:751–762.
   Google Scholar
• HWANG K, CORRELL M, OFFORD SJ: Evaluation of desloratadine for absorption drug-drug interactions with ketoconazole. Allergy Clin. Immunol (2001) 107. Abstract 504.
   Google Scholar
• KOSOGLOU T, SALFI M, LIM JM et al.:Evaluation of the pharmacokinetics and electrocardiographic pharmacodynamics of loratadine with concomitant administration of ketoconazole or cimetidine. Br. Pharmacol (2000) 50:581–589.
   Web of Science ®Google Scholar
• BANFIELD C, GUPTA S, KANTESARIA B et al.: No drug interaction between fluoxetine and desloratadine, a new nonsedating once-daily antihistamine. Allergy Clin. Immunol (2001) 107. Abstract 529.
   Google Scholar
• KLEINE-TEBBE J, JOSTIES C, FRANK Get al.: Inhibition of IgE- and non-IgE-mediated histamine release from human basophil leukocytes in vitro by a histamine Hl-antagonist, desethoxycarbonyl-loratadine. I Allergy Clin. Immunol (1994) 93:494–500.
   Google Scholar
• BERTHON B, TAUDOU G, COMBETTES L et al.: In vitro inhibition, by loratadine and descarboxyethoxyloratadine, of histamine release from human basophils, and of histamine release and intracellular calcium fluxes in rat basophilic leukemia cells (RBL-2H3). Biochem. Pharmacol (1994) 47:789–794.
   PubMed Web of Science ®Google Scholar
• VIGNOLA AM, CRAMPETTE L, MONDAIN M et al: Inhibitory activity of loratadine and descarboethoxyloratadine on expression of ICAM- I and HLA-DR by nasal epithelial cells. Allergy (1995) 50:200–203.
   PubMed Web of Science ®Google Scholar
• LIPPERT U, KRUGER-KRASAGAKES S, MOLLER A, KIESSLING U, CZARNETZKI BM: Pharmacological modulation of IL-6 and IL-8 secretion by the antagonist decarboethoxy-loratadine and dexamethasone by human mast and basophilic cell lines. Exp. Dermatol (1995) 4:272–276.
   PubMedGoogle Scholar
• GENOVESE A, PATELLA V, DE CRESCENZO G et al.: Loratadine and desethoxylcarbonyl-loratadine inhibit the immunological release of mediators from human Fc epsilon RI+ cells. Clin. Exp. Allergy (1997) 27:559–567.
   Google Scholar
• LICHTENSTEIN LM, SCHROEDER JT, SCHLEIMER RP, KREUTNER W: Inhibition of cytokine generation and mediator release in human basophils by desloratadine. I Allergy Clin. Innnunol. (2001) 107: Abstract 532.
   Google Scholar
• MELTZER EO: Rapid onset of action of desloratadine in patients with seasonal allergic rhinitis. I Allergy Clin. Inanunol. (2001) 107: Abstract 527.
   Google Scholar
• ••Recently published abstract demonstratingthe clinical effects of desloratadine.
   Google Scholar
• DUBUSKE LM: Once-daily desloratadine reduces the symptoms of perennial allergic rhinitis for at least 4 weeks. Allergy Clin. Inanunol. (2001) 107. Abstract 525.
   Google Scholar
• BERGER WE: Desloratadine reduces seasonal allergic rhinitis symptoms in patients with seasonal allergic rhinitis and asthma. I Allergy Clin. Inanunol (2001) 107. Abstract 533.
   Google Scholar
• RATNER PH: Long-term benefit of desloratadine against seasonal allergic rhinitis symptoms in patients with asthma. I Allergy Clin. Innnunol. (2001) 107. Abstract 531.
   Google Scholar
• SHAPIRO GG: Decongestant effects of desloratadine in patients with seasonal allergic rhinitis and asthma. I Allergy Clin. Inanunol. (2001) 107. Abstract 530.
   Google Scholar
• BAENA-CAGNANI CE: Desloratadine activity in concurrent seasonal allergic rhinitis and asthma. Allergy (2001) 56:21–27.
   PubMed Web of Science ®Google Scholar
• CORREN J: Desloratadine reduces the use of inhaled beta2-agonists and improves asthma symptoms in patients with seasonal allergic rhinitis and asthma. I Allergy Clin. Inanunol. (2001) 107:Abstract 535.
   Google Scholar
• RING J, HEIN R, GAUGER A, BRONSKY E, MILLER B: Once-daily desloratadine improves the signs and symptoms of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study. Int. Dermatol (2001) 40:72–76.
   PubMed Web of Science ®Google Scholar
• KREUTNER W, HEY JA, CHIU P, BARNETT A: Preclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist. 2nd communication: lack of central nervous system and cardiovascular effects. Arznehnittelforschung. (2000) 50:441–448.
   Google Scholar
• ••Extensive safety data for desloratadine arereported here including the lack of effect on the QT interval.
   Google Scholar
• CARDELOS I, ANTON F, BELETA PALACIOS JM: Anticholinergic effects of desloratadine, the major metabolite of loratadine, in rabbit and guinea-pig iris smooth muscle. Eur: I Pharmacol (1999) 374:249–254.
   PubMed Web of Science ®Google Scholar
• WANG DY, HANOTTE F, DE VOS C, CLEMENT P: Effect of cetirizine, levocetirizine, and dextrocetirizine on histamine- induced nasal response in healthy adult volunteers. Allergy (2001) 56:339–343.
   PubMed Web of Science ®Google Scholar
• ••Some of the earliest clinical efficacy data oflevocetirizine.
   Google Scholar
• DEVALIA JL, DE VOS C, HANOTTE F, BALTES E: A randomized, double-blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteers. Allergy (2001) 56:50–57.
   PubMed Web of Science ®Google Scholar
• MCCULLOUGH JR, BUTLER HT, FANGKO, HANDLEY D: Receptor binding properties of astemizole and its metabolite norastemizole. Ann. Allergy Asthma Inanunol. (1997) 78:144. Abstract P167.
   Google Scholar
• RUBIN PD, DEGRAW SS, KRAUSE AC et al.: Pharmacokinetics and pharmacodynamics of norastemizole in normal volunteers. Ann. Allergy Asthma Inanunol (1997) 78:144. Abstract P165.
   Google Scholar
• HANDLEY D, MCCULLOUGH JR, FANG KO, WRIGHT SE, SMITH ER: Comparative antihistamine effects of astemizole and a metabolite, norastemizole. Ann. Allergy Asthma Innnunol. (1997) 78:144 Abstract P166. The antihistamine effect, including the onset of action, of tecastemizole is compared with that of its parent compound, astemizole.
   Google Scholar
• 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.
   Web of Science ®Google Scholar
• RUBIN P, DONOGHUE A, DEGRAW S, DOCKHORN R, REASNER D, ROLLINS T: Effects of varying doses of norastemizole on histamine induced wheal (W) and flare (F) responses and ECG. I Allergy Clin. Inanunol (1998) S248. Abstract 1028.
   Google Scholar
• ••Clinical efficacy and safety of tecastemizoleis reported in this study.
   Google Scholar
• CASALE TB, KESSLER RJ, CLANCY J et al.: Norastemizole does not affect ECG parameters. I Allergy Clin. Inanunel (1998) 101: S245. Abstract 1016.
   Google Scholar