Fexofenadine Subject

Grant JA, Riethuisen JM, Moulaert B, DeVos C A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo sup- 59 pression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects. 

In 42 healthy naval aviation personnel in a double-blind, randomized, placebo-controlled, crossover study, subjective drowsiness, cognitive performance, and vigilance were measured after three treatments fexofenadine 180 mg, diphenhydramine 50 mg as a positive control, or placebo. Diphenhydramine significantly impaired... 

Wilson AM, Haggart K, Sims EJ, Lipworth BJ. Effects of fexofenadine and desloratadine on subjective and objective measures of nasal congestion in seasonal allergic rhinitis. Clin Exp Allergy 2002 32(10) 1504-9. 

Special population pharmacokinetics (for geriatric subjects, renal, and hepatic impairment), obtained after a single dose of 80 mg fexofenadine hydrochloride, were compared to those for normal subjects from a separate study of similar design. While subject weights were relatively uniform between studies, these adult special population patients were substantially older than the healthy, young volunteers. Thus, an age effect may be confounding the pharmacokinetic differences observed in some of the special populations. 

In older subjects (= 65 years old), peak plasma levels of fexofenadine were much greater than those observed in normal volunteers (<65 years old). Mean elimination half-lives were similar to those observed in normal younger volunteers. 

Cross-study comparisons indicated that fexofenadine hydrochloride distribution in the body of 7-12-year-old pediatric allergic rhinitis patients following oral administration of a 60 mg dose was 56% greater compared to healthy adult subjects given the same dose. Plasma concentrations in pediatric patients given a dose that is one-half of what an adult would receive (30 mg fexofenadine hydrochloride in child versus 60 mg for adult) is comparable to adults. 

Shon J, Chun H, Kim K, Kim E, Yoon Y, et al. 2002. The PK and PD of fexofenadine in relation to MDR1 genetic polymorphism in Korean healthy subjects. Clin. Pharmacol. Ther. 71 P71(Abstr.)... 

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. 

A study in healthy subjects indicated that the pharmacokinetics of pioglitazone 4S mg daily are not significantly affected by fexofenadine 60 mg twice daily, and that pioglitazone does not affect the pharmacokinetics of fexofenadine. ... 

In a single dose study, administration of itraconazole 200 mg one hour prior to fexofenadine 180 mg increased the AUC of fexofenadine 2.3-fold, and 3-fold in two groups of subjects of different genotypes for the gene encoding P-glycoprotein. Itraconazole pretreatment increased the effect of fexofenadine on histamine-induced wheal and flare reaction. ... 

Fexofenadine 120 mg twice daily Ketoconazole 400 mg daily 7 24 healthy subjects 135% 164% No change 7... 

I. 2 L. A subsequent study found that a single 300 mL dose of normal strength grapefruit juice reduced the AUC of a single 120-mg dose of fexofenadine by 42% when they were given simultaneously. An effect was apparent for 300 mL of grapefruit juice given up to 10 hours prior to fexofenadine 120 mg in at least some of 12 subjects involved in this study. ... 

Cimetidine 400 mg twice daily for 6 days did not cause any changes in the plasma pharmacokinetics of a single 120-mg dose of fexofenadine in 12 healthy subjects. However, the renal clearance of fexofenadine was decreased by 39%. ... 

Fexofenadine 60 mg twice daily Azithromycin 500 mg, then 250 mg daily 5 18 healthy subjects 69% 67% No change 4... 

A single 60-mg dose of fexofenadine was given to 24 healthy subjects 2 days before and on the last day of a 6-day course of rifampicin 600 mg daily. The oral clearance of fexofenadine was increased 1.3- to 5.3-fold, with no effect on renal clearance or half-life. This was thought to be due to the effect of rifampicin on P-glycoprotein, which is involved in the up-... 

A group of healthy subjects were given a single 120-mg dose of terfenadine on day 8 of a 10-day course of atorvastatin 80 mg daily. It was found that the atorvastatin caused some small to moderate changes in the pharmacokinetics of the terfenadine and its metabolite fexofenadine (AUC increased by 35% and decreased by 2% respectively, maximum serum levels decreased by 8% and decreased by 16% respectively), none of which reached statistical significance. More importantly there were no changes in the QTc interval, which indicates that atorvastatin does not increase the cardiotoxicity of the terfenadine. There would therefore appear to be no reason for avoiding concurrent use. 

Robertson, S.M., R.T. Davey, J. VoeU, et al. 2008. Effect of Ginkgo biloba extract on lopinavir, midazolam and fexofenadine pharmacokinetics in healthy subjects. Curr. Med. Res. Opin. 24(2) 591-599. 

Table 10.2 Pharmacokinetic parameters of fexofenadine enantiomers (in human subjects, p.o.)...

---