Levocabastine Ketoconazole

When single doses of erjdhromycin (333 mg) or ketoconazole (200 mg) were given to healthy men who used levocabastine, two sprays per nostril (0.05 mg/spray) bd for 6 days, there were no changes in the pharmacokinetics of levocabastine or in the QTc interval (30). 

Pesco-Koplowitz L, Hassell A, Lee P, Zhou H, HaU N, Wiesinger B, Mechlinski W, Grover M, Hunt T, Smith R, Travers S. Lack of effect of erythromycin and ketoconazole on the pharmacokinetics and pharmacodynamics of steady-state intranasal levocabastine. J Qin Pharmacol 1999 39(l) 76-85. 

Many Hj antihistamines are metabolized by CYPs. Thus, inhibitors of CYP activity such as macrolide antibiotics (e.g., erythromycin) or imidazole antifungals (e.g.,ketoconazole) can increase Hj antihistamine levels, leading to toxicity. Some newer antihistamines, such as cetirizine, fexofenadine, levocabastine, and acrivastine, are not subject to these drug interactions. 

Ketoconazole raises the levels of desloratadine, emedastine, fexofenadine but as no adverse cardiac effects were seen these combinations are considered safe. No interaction occurs between ketoconazole and azelastine, cetirizine, intranasal levocabastine, and none is expected with levocetirizine. 

Levocabastine 200 micrograms twice daily intranasal Ketoconazole 200 mg single dose Single dose 37 subjects No change No change No change 8... 

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See also in sourсe #XX -- [ ]

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