Influence of itraconazole on the pharmacokinetics and electrocardiographic effects of astemizole

British Journal of Clinical Pharmacology

Volumn 43, Issue 3, 1997, Pages 319-322

  Lefebvre, Romain A ^a   Van Peer, Achiel ^b   Woestenborghs, Robert ^b  

^a GHENT UNIVERSITY   (Belgium)

^b JANSSEN RESEARCH FOUNDATION   (Belgium)

Author keywords

astemizole; drug interaction; itraconazole

Indexed keywords

ASTEMIZOLE; DRUG METABOLITE; ITRACONAZOLE; NORASTEMIZOLE; PLACEBO;

ADULT; AREA UNDER THE CURVE; ARTICLE; CARDIOVASCULAR EFFECT; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOUBLE BLIND PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; ELECTROCARDIOGRAM; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PHARMACOKINETICS; PRIORITY JOURNAL; RADIOIMMUNOASSAY; RANDOMIZED CONTROLLED TRIAL; REPOLARIZATION; VOLUNTEER;

EID: 0031055852     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.1997.00548.x     Document Type: Article

References (22)

1. Smith SJ. Cardiovascular toxicity of antihistamines. Otolaryngol Head Neck Surg 1994; 111: 348-354.
2. Jurima-Romet M, Crawford K, Cyr T, Inaba T. Terfenadine metabolism in human liver. In vitro inhibition by macrolide antibiotics and azole antifungals. Drug Metab Dispos 1994; 22: 849-857.
3. Honig PK, Wortham DC, Zamani K, Conner DP, Mullin JC, Cantilena LR. Terfenadine-ketoconazole interaction. Pharmacokinetic and electrocardiographic consequences. JAMA 1993; 269: 1513-1518.
4. Honig PK, Wortham DC, Hull R, Zamani K, Smith JE, Cantilena LR. Itraconazole affects single-dose terfenadine pharmacokinetics and cardiac repolarization pharmacodynamics. J Clin Pharmacol 1993; 33: 1201-1206.
5. Monahan BP, Ferguson CL, Killeavy ES, Lloyd BK, Troy J, Cantilena LR. Torsades de pointes occurring in association with terfenadine use. JAMA 1990; 264: 2788-2790.
6. Pohjola-Sintonen S, Viitasalo M, Toivonen L, Neuvonen P. Itraconazole prevents terfenadine metabolism and increases risk of torsades de pointes ventricular tachycardia. Eur J Clin Pharmacol 1993; 45: 191-193.
7. 1-antihistamines. Clin Pharmacokin 1995; 28: 419-432.
8. Adamantidis MM, Lacroix DL, Caron JF, Dupuis BA. Electrophysiological and arrhythmogenic effects of the histamine type 1-receptor antagonist astemizole on rabbit Purkinje fibers: clinical relevance. J Cardiovasc Pharmacol 1995; 26: 319-327.
9. Berul CI, Morad M. Regulation of potassium channels by nonsedating antihistammes. Circulation 1995; 91: 2220-2225.
10. Lavrijsen K, Van Houdt J, Meuldermans W, Janssens M, Heykants J. The interaction of ketoconazole, itraconazole and erythromycin with the in vitro metabolism of antihistamines in human liver microsomes. Allergy 1993; 48: (Supplement): 34.
11. Woestenborghs R, Geuens I, Michiels M, Hendriks R, Heykants J. Radioimmunoassay procedures for astemizole and metabolites in plasma. Drug Developm Res 1986; 8: 63-69.
12. Koch GG. The use of non-parametric methods in the statistical analysis of the two-period change over design. Biometr 1972; 28: 577-584.
13. Grant SM, Clissold SP. Itraconazole. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in superficial and systemic mycoses. Drugs 1989; 37: 310-344.
14. Dollery C. Therapeutic drugs, Supplement 1. Edinburgh: Churchill Livingstone, 1992: 14-17.
15. Van Peer A, Woestenborghs R, Heykants J, Gasparini R, Cauwenbergh G. The effect of food and dose on the oral systemic availability of itraconazole in healthy subjects. Eur J Clin Pharmacol 1989; 36: 423-426.
16. Hardin T, Graybill J, Fetchik R, Woestenborghs R, Rinaldi M, Kuhn J. Pharmacokinetics of itraconazole following oral administration to normal volunteers. Antimicrob Agents Chemother 1988; 32: 1310-1313.
17. Heykants J, Van Peer A, Woestenborghs R, Jageneau A, Vandenbussche G. Dose-proportionality, bioavailability, and steady-state kinetics of astemizole in man. Drug Developm Res 1986; 8: 71-78.
18. Honig PK, Woosley RL, Zamani K, Conner DP, Cantilena LR. Changes in the pharmacokinetics and electrocardiographic pharmacodynamics of terfenadine with concomitant administration of erythromycin. Clin Pharmacol Ther 1992; 52: 231-238.
19. Craft TM, Vandenbussche G, De Cree J, Griffiths JV. ECG studies with astemizole. Human Toxicol 1987; 6: 527-528.
20. Démolis P, Annane D, Duhazé P, Giudicelli JF. Systemic, regional and cerebral hemodynamic effects of a new angiotensin converting enzyme inhibitor, imidapril, in healthy volunteers. Fundam Clin Pharmacol 1994; 8: 80-89.
21. Tester-Dalderup CBM. Antifungal drugs. In Meyler's side effects of drugs, ed Dukes MNG, 12th ed. Amsterdam: Elsevier, 1992: 672-686.
22. Napolitano C, Priori SG, Schwartz PJ. Torsade de pointes. Mechanisms and management. Drugs 1994; 47: 51-65.