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Fexofenadine

ALLEGRA®

(fexofenadine hydrochloride) Capsules and Tablets

Fexofenadine hydrochloride, the active ingredient of ALLEGRA, is a histamine H1 -receptor antagonist with the chemical name (±) , -dimethyl benzeneacetic acid hydrochloride. It has the following chemical structure The molecular weight is 538.13 and the empirical formula is C32H39NO4 Fexofenadine hydrochloride is a white to off-white crystalline powder. It is freely soluble in methanol and ethanol, slightly soluble in chloroform and water, and insoluble in hexane. Fexofenadine hydrochloride is a racemate and exists as a zwitterion in aqueous media at physiological pH. ALLEGRA is formulated as a capsule or tablet for oral administration. Each capsule contains 60 mg fexofenadine hydrochloride and the following excipients: croscarmellose sodium, gelatin, lactose, microcrystalline cellulose, and pregelatinized starch. The printed capsule shell is made from gelatin, iron oxide, silicon dioxide, sodium lauryl sulfate, titanium dioxide, and other ingredients. Each tablet contains 30, 60, or 180 mg fexofenadine hydrochloride (depending on the dosage strength) and the following excipients: croscarmellose sodium, magnesium stearate, microcrystalline cellulose, and pregelatinized starch. The aqueous tablet film coating is made from hydroxypropyl methylcellu-lose, iron oxide blends, polyethylene glycol, povidone, silicone dioxide, and titanium dioxide.

Seasonal Allergic Rhinitis

ALLEGRA is indicated for the relief of symptoms associated with seasonal allergic rhinitis in adults and children 6 years of age and older. Symptoms treated effectively were sneezing, rhinorrhea, itchy nose/palate/throat, itchy/watery/red eyes.

Chronic Idiopathic Urticaria

ALLEGRA is indicated for treatment of uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older. It significantly reduces pruritus and the number of wheals.

PRECAUTIONS
Carcinogenesis, Mutagenesis, Impairment of Fertility

The carcinogenic potential and reproductive toxicity of fexofenadine hydrochloride were assessed using terfenadine studies with adequate fexofenadine hydrochloride exposure (based on plasma area-under-the-concentration vs. time [AUC] values). No evidence of carcinogenicity was observed in an 18-month study in mice and in a 24-month study in rats at oral doses up to 150 mg/kg of terfen-adine (which led to fexofenadine exposures that were respectively approximately 3 and 5 times the exposure from the maximum recommended daily oral dose of fexofenadine hydrochloride in adults and children). In in vitro (Bacterial Reverse Mutation, CHO/HGPRT Forward Mutation, and Rat Lymphocyte Chromo-somal Aberration assays) and in vivo (Mouse Bone Marrow Micronucleus assay) tests, fexofenadine hydrochloride revealed no evidence of mutagenicity.

In rat fertility studies, dose-related reductions in implants and increases in postimplantation losses were observed at an oral dose of 150 mg/kg of terfenadine (which led to fexofenadine hydrochloride exposures that were approximately 3 times the exposure of the maximum recommended daily oral dose of fexofenadine hydrochloride in adults).

Pregnancy

Teratogenic Effects: Category C. There was no evidence of teratogenicity in rats or rabbits at oral doses of terfenadine up to 300 mg/kg (which led to fexofenadine exposures that were approximately 4 and 31 times, respectively, the exposure from the maximum recommended daily oral dose of fexofenadine in adults). There are no adequate and well controlled studies in pregnant women. Fexofenadine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nonteratogenic Effects. Dose-related decreases in pup weight gain and survival were observed in rats exposed to an oral dose of 150 mg/kg of terfenadine (approximately 3 times the maximum recommended daily oral dose of fexofenadine hydrochloride in adults based on comparison of fexofenadine hydrochloride AUCs).

Nursing Mothers

There are no adequate and well-controlled studies in women during lactation. Because many drugs are excreted in human milk, caution should be exercised when fexofenadine hydrochloride is administered to a nursing woman.

Pediatric Use

The recommended dose in patients 6 to 11 years of age is based on cross-study comparison of the pharmacokinetics of ALLEGRA in adults and pediatric patients and on the safety profile of fexofena-dine hydrochloride in both adult and pediatric patients at doses equal to or higher than the recommended doses. The safety of ALLEGRA tablets at a dose of 30 mg twice daily has been demonstrated in 438 pediatric patients 6 to 11 years of age in two placebo-controlled 2-week seasonal allergic rhinitis trials. The safety of ALLEGRA for the treatment of chronic idiopathic urticaria in patients 6 to 11 years of age is based on cross-study comparison of the pharmacokinetics of ALLEGRA in adult and pediatric patients and on the safety profile of fexofenadine in both adult and pediatric patients at doses equal to or higher than the recommended dose. The effectiveness of ALLEGRA for the treatment of seasonal allergic rhinitis in patients 6 to 11 years of age was demonstrated in one trial (n=411) in which ALLEGRA tablets 30 mg twice daily significantly reduced total symptom scores compared to placebo, along with extrapolation of demonstrated efficacy in patients ages 12 years and above, and the pharmacokinetic comparisons in adults and children. The effectiveness of ALLEGRA for the treatment of chronic idiopathic urticaria in patients 6 to 11 years of age is based on an extrapolation of the demonstrated efficacy of ALLEGRA in adults with this condition and the likelihood that the disease course, pathophysiology and the effect are substantially similar in children to that of adult patients. Three clinical safety studies comparing 15 mg BID (n=85) and 30 mg BID (n=330) of an experimental formulation of fexofenadine to placebo (n=430) have been conducted in pediatric patients aged 6 months to 5 years. In general, fexofenadine hydrochloride was well tolerated in these studies. No unexpected adverse events were seen given the known safety profile of fexofenadine and likely adverse reactions for this patient population. (See ADVERSE REACTIONS and CLINICAL PHARMACOLOGY.) The safety and effectiveness of fexofenadine hydrochloride in pediatric patients under 6 years of age have not been established.

Geriatric Use

Clinical studies of ALLEGRA tablets and capsules did not include sufficient numbers of subjects aged 65 years and over to determine whether this population responds differently from younger patients. Other reported clinical experience has not identified differences in responses between the geriatric and younger patients. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and may be useful to monitor renal function.

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