Drug: Allegra-D 24 Hour

ALLEGRA-D® 24 HOUR (fexofenadine hydrochloride and pseudoephedrine hydrochloride) Extended-Release Tablets for oral administration contain 180 mg fexofenadine hydrochloride for immediate release and 240 mg pseudoephedrine hydrochloride for extended release. Tablets also contain as excipients: microcrystalline cellulose, sodium chloride, cellulose acetate, polyethylene glycol, opadry white, povidone, talc, hypromellose, croscarmellose sodium, copovidone, titanium dioxide, magnesium stearate, colloidal silicon dioxide, brilliant blue aluminum lake, acetone, isopropyl alcohol, methyl alcohol, methylene chloride, water, and black ink. Fexofenadine hydrochloride, one of the active ingredients of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) , is a histamine H1-receptor antagonist with the chemical name (±)-4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-butyl]-α, α-dimethyl benzeneacetic acid hydrochloride and the following chemical structure: The molecular weight is 538.13 and the empirical formula is C32H39NO4•HCl. 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. Pseudoephedrine hydrochloride, the other active ingredient of ALLEGRA-D 24 HOUR, is an adrenergic (vasoconstrictor) agent with the chemical name [S-(R*,R*)]-α-[1-(methylamino)ethyl]-benzenemethanol hydrochloride and the following chemical structure: The molecular weight is 201.70 and the molecular formula is C10H15NO•HCl. Pseudoephedrine hydrochloride occurs as fine, white to off-white crystals or powder, having a faint characteristic odor. It is very soluble in water, freely soluble in alcohol, and sparingly soluble in chloroform.

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Fexofenadine Hydrochloride In a placebo-controlled clinical study in the United States, which included 570 subjects with seasonal allergic rhinitis aged 12 years and older receiving fexofenadine hydrochloride tablets at doses of 120 or 180 mg once daily, adverse events were similar in fexofenadine hydrochloride and placebo-treated subjects. The following table lists adverse experiences that were reported by greater than 2% of subjects treated with fexofenadine hydrochloride tablets at doses of 180 mg once daily and that were more common with fexofenadine hydrochloride than placebo. Once daily dosing with fexofenadine hydrochloride tablets at rates of greater than 2%
Adverse experience Fexofenadine 180 mg once daily
(n=283) Placebo
(n=293) Headache 10.6% 7.5% Upper Respiratory Tract Infection 3.2% 3.1% Back Pain 2.8% 1.4% Events that have been reported during controlled clinical trials involving subjects with seasonal allergic rhinitis at incidences less than 1% and similar to placebo and have been rarely reported during postmarketing surveillance include: insomnia, nervousness, and sleep disorders or paroniria. In rare cases, rash, urticaria, pruritus and hypersensitivity reactions with manifestations such as angioedema, chest tightness, dyspnea, flushing and systemic anaphylaxis have been reported. Pseudoephedrine Hydrochloride Pseudoephedrine hydrochloride may cause mild CNS stimulation in hypersensitive patients. Nervousness, excitability, restlessness, dizziness, weakness, or insomnia may occur. Headache, drowsiness, tachycardia, palpitation, pressor activity, cardiac arrhythmias and ischemic colitis have been reported. Sympathomimetic drugs have also been associated with other untoward effects such as fear, anxiety, tenseness, tremor, hallucinations, seizures, pallor, respiratory difficulty, dysuria, and cardiovascular collapse. Read the Allegra-D 24 Hour (fexofenadine hcl 180 and pseudoephendrine hcl 240) Side Effects Center for a complete guide to possible side effectsLearn More »

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The recommended dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) Extended-Release Tablets is one tablet once daily administered on an empty stomach with water for adults and children 12 years of age and older. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) tablets should generally be avoided in patients with renal insufficiency. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) must be swallowed whole and never crushed or chewed.

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Fexofenadine hydrochloride and pseudoephedrine hydrochloride do not influence the pharmacokinetics of each other when administered concomitantly. Fexofenadine has been shown to exhibit minimal (ca. 5%) metabolism. However, co-administration of fexofenadine hydrochloride with either ketoconazole or erythromycin led to increased plasma concentrations of fexofenadine. Fexofenadine had no effect on the pharmacokinetics of either erythromycin or ketoconazole. In 2 separate studies, fexofenadine hydrochloride 120 mg twice daily was co-administered with either erythromycin 500 mg every 8 hours or ketoconazole 400 mg once daily under steady-state conditions to healthy volunteers (n=24, each study). No differences in adverse events or QTc interval were observed when subjects were administered fexofenadine hydrochloride alone or in combination with either erythromycin or ketoconazole. The findings of these studies are summarized in the following table: Effects on steady-state fexofenadine pharmacokinetics after 7 days of co-administration with fexofenadine hydrochloride 120 mg every 12 hours (two times the recommended twice daily dose) in healthy volunteers (n=24)
Concomitant Drug CmaxSS
(Peak plasma concentration) AUCss(0-12h)
(Extent of systemic exposure) Erythromycin (500 mg every 8 hrs) +82% +109% Ketoconazole (400 mg once daily) +135% +164% The changes in plasma levels were within the range of plasma levels achieved in adequate and well-controlled clinical trials. The mechanism of these interactions has been evaluated in in vitro, in situ, and in vivo animal models. These studies indicate that ketoconazole or erythromycin co-administration enhances fexofenadine gastrointestinal absorption. This observed increase in the bioavailability of fexofenadine may be due to transport-related effects, such as p-glycoprotein. In vivo animal studies also suggest that in addition to enhancing absorption, ketoconazole decreases fexofenadine gastrointestinal secretion, while erythromycin may also decrease biliary excretion. Due to the pseudoephedrine component, ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) is contraindicated in patients taking monoamine oxidase inhibitors and for 14 days after stopping use of an MAO inhibitor. Concomitant use with antihypertensive drugs which interfere with sympathetic activity (e.g., methyldopa, mecamylamine, and reserpine) may reduce their antihypertensive effects. Increased ectopic pacemaker activity can occur when pseudoephedrine is used concomitantly with digitalis. Care should be taken in the administration of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) concomitantly with other sympathomimetic amines because combined effects on the cardiovascular system may be harmful to the patient (see WARNINGS). Drug Interactions with Antacids Administration of 120 mg of fexofenadine hydrochloride (2 x 60 mg capsule) within 15 minutes of an aluminum and magnesium containing antacid (Maalox®) decreased fexofenadine AUC by 41% and Cmax by 43%. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) should not be taken closely in time with aluminum and magnesium containing antacids. Interactions with Fruit Juices Fruit juices such as grapefruit, orange and apple may reduce the bioavailability and exposure of fexofenadine. This is based on the results from 3 clinical studies using histamine induced skin wheals and flares coupled with population pharmacokinetic analysis. The size of wheal and flare were significantly larger when fexofenadine hydrochloride was administered with either grapefruit or orange juices compared to water. Based on the literature reports, the same effects may be extrapolated to other fruit juices such as apple juice. The clinical significance of these observations is unknown. In addition, based on the population pharmacokinetics analysis of the combined data from grapefruit and orange juices studies with the bioequivalence study data, the bioavailability of fexofenadine was reduced by 36%. Therefore, to maximize the effects of fexofenadine, it is recommended that ALLEGRA-D 24 HOUR should be taken with water (see DOSAGE AND ADMINISTRATION). Read the Allegra-D 24 Hour Drug Interactions Center for a complete guide to possible interactions Learn More »

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ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) Extended-Release Tablets are indicated for the relief of symptoms associated with seasonal allergic rhinitis in adults and children 12 years of age and older. Symptoms treated effectively include sneezing, rhinorrhea, itchy nose/palate/ and/or throat, itchy/watery/red eyes, and nasal congestion. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) should be administered when both the antihistaminic properties of fexofenadine hydrochloride and the nasal decongestant properties of pseudoephedrine hydrochloride are desired (see CLINICAL PHARMACOLOGY).

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ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) is contraindicated in patients with known hypersensitivity to any of its ingredients. Due to its pseudoephedrine component, ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) is contraindicated in patients with narrow-angle glaucoma or urinary retention, and in patients receiving monoamine oxidase (MAO) inhibitor therapy or within fourteen (14) days of stopping such treatment (see DRUG INTERACTIONS section). It is also contraindicated in patients with severe hypertension, or severe coronary artery disease, and in those who have shown idiosyncrasy to its components, to adrenergic agents, or to other drugs of similar chemical structures. Manifestations of patient idiosyncrasy to adrenergic agents include: insomnia, dizziness, weakness, tremor, or arrhythmias. Last reviewed on RxList: 5/10/2010
This monograph has been modified to include the generic and brand name in many instances.

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Most reports of fexofenadine hydrochloride overdose contain limited information. However, dizziness, drowsiness, and dry mouth have been reported. For the pseudoephedrine hydrochloride component of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) , information on acute overdose is limited to the marketing history of pseudoephedrine hydrochloride. Single doses of fexofenadine hydrochloride up to 800 mg (6 healthy volunteers at this dose level), and doses up to 690 mg twice daily for one month (3 healthy volunteers at this dose level), were administered without the development of clinically significant adverse events. In large doses, sympathomimetics may give rise to giddiness, headache, nausea, vomiting, sweating, thirst, tachycardia, precordial pain, palpitations, difficulty in micturition, muscular weakness and tenseness, anxiety, restlessness, and insomnia. Many patients can present a toxic psychosis with delusions and hallucinations. Some may develop cardiac arrhythmias, circulatory collapse, convulsions, coma, and respiratory failure. In the event of overdose, consider standard measures to remove any unabsorbed drug. Symptomatic and supportive treatment is recommended. Following administration of terfenadine, hemodialysis did not effectively remove fexofenadine, the major active metabolite of terfenadine, from blood (up to 1.7% removed). The effect of hemodialysis on the removal of pseudoephedrine is unknown. No deaths occurred in mature mice and rats at oral doses of fexofenadine hydrochloride up to 5000 mg/kg (approximately 110 and 230 times, respectively, the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) on a mg/m2 basis.) The median oral lethal dose in newborn rats was 438 mg/kg (approximately 20 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) on a mg/m2 basis). In dogs, no evidence of toxicity was observed at oral doses up to 2000 mg/kg (approximately 300 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) on a mg/m2 basis). The oral median lethal dose of pseudoephedrine hydrochloride in rats was 1674 mg/kg (approximately 55 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR on a mg/m2 basis).

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ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) Extended-Release Tablets contain 180 mg fexofenadine hydrochloride for immediate release and 240 mg pseudoephedrine hydrochloride for extended release. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) Extended-Release Tablets are available in high-density polyethylene (HDPE) bottles of 100 (NDC 0088-1095-47), with an activated charcoal pouch. All bottles have a polypropylene screw cap containing a pulp/wax liner with heat-sealed foil inner seal. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) Extended-Release Tablet is a white, round, film coated tablet. The tablet has 308AV printed on one side in black ink. Store ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) Extended-Release Tablets at 20-25°C (68-77°F). (See USP Controlled Room Temperature.) Rev. December 2009. sanofi-aventis U.S. LLC Bridgewater, NJ 08807. Last reviewed on RxList: 5/10/2010
This monograph has been modified to include the generic and brand name in many instances.

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General Because ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) is a once-daily, fixed-dose combination that cannot be titrated and renal insufficiency increases the bioavailability and prolongs the half-life of fexofenadine hydrochloride and pseudoephedrine hydrochloride, ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) tablets should generally be avoided in patients with renal insufficiency (see CLINICAL PHARMACOLOGY, and DOSAGE AND ADMINISTRATION). Carcinogenesis, Mutagenesis, Impairment of Fertility There are no animal or in vitro studies on the combination product fexofenadine hydrochloride and pseudoephedrine hydrochloride to evaluate carcinogenesis, mutagenesis, or impairment of fertility. The carcinogenic potential and reproductive toxicity of fexofenadine hydrochloride were assessed using terfenadine studies with adequate fexofenadine exposure (area-under-the plasma concentration versus time curve [AUC]). No evidence of carcinogenicity was observed when mice and rats were given daily oral doses up to 150 mg/kg of terfenadine for 18 and 24 months, respectively. In both species, 150 mg/kg of terfenadine produced AUC values of fexofenadine that were approximately 2 and 3 times, respectively, the exposure from the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) . Two-year feeding studies in rats and mice conducted under the auspices of the National Toxicology Program (NTP) demonstrated no evidence of carcinogenic potential with ephedrine sulfate, a structurally related drug with pharmacological properties similar to pseudoephedrine, at doses up to 10 and 27 mg/kg, respectively (less than the maximum recommended human daily oral dose of pseudoephedrine hydrochloride on a mg/m2 basis). In in vitro (Bacterial Reverse Mutation, CHO/HGPRT Forward Mutation, and Rat Lymphocyte Chromosomal Aberration assays) and in vivo (Mouse Bone Marrow Micronucleus assay) tests, fexofenadine hydrochloride revealed no evidence of mutagenicity. Reproduction and fertility studies with terfenadine in rats produced no effect on male or female fertility at oral doses up to 300 mg/kg/day (approximately 3 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) based on comparison of the AUCs of fexofenadine). However, reduced implants and post-implantation losses were reported at 300 mg/kg. A reduction in implants was also observed at an oral dose of 150 mg/kg/day (approximately 3 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) based on comparison of the AUCs). In mice, fexofenadine produced no effect on male or female fertility at average dietary doses up to 4438 mg/kg (approximately 10 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) based on comparison of the AUCs). Pregnancy Teratogenic Effects: Category C. Terfenadine alone was not teratogenic in rats at oral doses up to 300 mg/kg (approximately 3 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) based on comparison of the AUCs of fexofenadine) and in rabbits at oral doses up to 300 mg/kg (approximately 25 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) based on comparison of the AUCs of fexofenadine). In mice, no adverse effects and no teratogenic effects during gestation were observed with fexofenadine at dietary doses up to 3730 mg/kg (approximately 10 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) based on comparison of the AUCs). The combination of terfenadine and pseudoephedrine hydrochloride in a ratio of 1:2 by weight was studied in rats and rabbits. In rats, an oral combination dose of 150/300 mg/kg produced reduced fetal weight and delayed ossification with a finding of wavy ribs. The dose of 150 mg/kg of terfenadine in rats produced an AUC value of fexofenadine that was approximately 3 times the AUC of the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) . The dose of 300 mg/kg of pseudoephedrine hydrochloride in rats was approximately 10 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) on a mg/m2 basis. In rabbits, an oral combination dose of 100/200 mg/kg produced decreased fetal weight. By extrapolation, the AUC of fexofenadine for 100 mg/kg orally of terfenadine was approximately 8 times the human AUC of the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) . The dose of 200 mg/kg of pseudoephedrine hydrochloride was approximately 15 times the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) on a mg/m2 basis. There are no adequate and well-controlled studies in pregnant women. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) 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; this dose produced an AUC of fexofenadine that was approximately 3 times the human AUC of the maximum recommended human daily oral dose of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) . Nursing Mothers It is not known if fexofenadine is excreted in human milk. Because many drugs are excreted in human milk, caution should be used when fexofenadine hydrochloride is administered to a nursing woman. Pseudoephedrine hydrochloride administered alone distributes into breast milk of lactating human females. Pseudoephedrine concentrations in milk are consistently higher than those in plasma. The total amount of drug in milk as judged by AUC is 2 to 3 times greater than the plasma AUC. The fraction of a pseudoephedrine dose excreted in milk is estimated to be 0.4% to 0.7%. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Caution should be exercised when ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) is administered to nursing women. Pediatric Use Safety and effectiveness of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) in children below the age of 12 years have not been established. In addition, the doses of the individual components in ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) exceed the recommended individual doses for pediatric patients under 12 years of age. ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) is not recommended for pediatric patients under 12 years of age. Geriatric Use Clinical studies of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) did not include sufficient numbers of subjects aged 65 and older to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients, although the elderly are more likely to have adverse reactions to sympathomimetic amines. The pseudoephedrine component of ALLEGRA-D 24 HOUR (fexofenadine hcl 180 and pseudoephendrine hcl 240) 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, it may be useful to monitor renal function. Last reviewed on RxList: 5/10/2010
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

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