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Pronunciation
(feks oh FEN a deen)
Generic Available (U.S.)
Yes: Excludes orally disintegrating tablet and suspension
Index Terms
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Relief of symptoms associated with seasonal allergic rhinitis; treatment of chronic idiopathic urticaria
OTC labeling: Relief of symptoms associated with allergic rhinitis
Pregnancy Risk Factor
C
Pregnancy Considerations
Decreased fetal weight gain and survival were observed in animal studies; teratogenic effects were not observed.
Lactation
Excretion in breast milk unknown/use caution (AAP rates “compatible”; AAP 2001 update pending)
Contraindications
Hypersensitivity to fexofenadine or any component of the formulation
Warnings/Precautions
Disease-related concerns:
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children <6 months of age; orally disintegrating tablet not recommended for use in children <6 years of age.
Dosage form specific issues:
• Orally disintegrating tablet: Contains phenylalanine.
Adverse Reactions
>10%:
Central nervous system: Headache (5% to 11%)
Gastrointestinal: Vomiting (children 6 months to 5 years: 4% to 12%)
1% to 10%:
Central nervous system: Fatigue (1% to 3%), somnolence (1% to 3%), dizziness (2%), fever (2%), pain (2%), drowsiness (1%)
Endocrine & metabolic: Dysmenorrhea (2%)
Gastrointestinal: Diarrhea (3% to 4%), nausea (2%), dyspepsia (1% to 2%)
Neuromuscular & skeletal: Myalgia (3%), back pain (2% to 3%), pain in extremities (2%)
Otic: Otitis media (2% to 4%)
Respiratory: Upper respiratory tract infection (3% to 4%), cough (2% to 4%), rhinorrhea (1% to 2%)
Miscellaneous: Viral infection (3%)
<1%, postmarketing, and/or case reports: Hypersensitivity reactions (anaphylaxis, angioedema, chest tightness, dyspnea, flushing, pruritus, rash, urticaria); insomnia, nervousness, paroniria, sleep disorders
Metabolism/Transport Effects
Substrate of CYP3A4 (minor), P-glycoprotein, SLCO1B1; Inhibits CYP2D6 (weak)
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Antacids: May decrease the serum concentration of Fexofenadine. Management: No specific recommendations concerning the time required between their administration are provided. Separate administration of each agent by as much time as possible to decrease the risk of an interaction. Exceptions: Calcium Carbonate; Magaldrate; Sodium Bicarbonate. Risk D: Consider therapy modification
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Management: Upon completion/discontinuation of conivaptan, allow at least 7 days before initiating therapy with drugs that are CYP3A4 substrates. Risk D: Consider therapy modification
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
Eltrombopag: May increase the serum concentration of OATP1B1/SLCO1B1 Substrates. Management: According to eltrombopag prescribing information, consideration of a preventative dose reduction may be warranted. Risk D: Consider therapy modification
Erythromycin: May increase the serum concentration of Fexofenadine. Risk C: Monitor therapy
Erythromycin (Systemic): May increase the serum concentration of Fexofenadine. Risk C: Monitor therapy
Grapefruit Juice: May decrease the serum concentration of Fexofenadine. Risk C: Monitor therapy
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Itraconazole: May increase the serum concentration of Fexofenadine. Risk C: Monitor therapy
Ketoconazole: May increase the serum concentration of Fexofenadine. Risk C: Monitor therapy
Ketoconazole (Systemic): May increase the serum concentration of Fexofenadine. Risk C: Monitor therapy
P-Glycoprotein Inducers: May decrease the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-Glycoprotein Inhibitors: May increase the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Rifampin: May decrease the serum concentration of Fexofenadine. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Verapamil: May increase the bioavailability of Fexofenadine. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Food: Fruit juice (apple, grapefruit, orange) may decrease bioavailability of fexofenadine by ~36%.
Herb/Nutraceutical: St John's wort may decrease fexofenadine levels.
Storage
Store at controlled room temperature of 20°C to 25°C (68°F to 77°F). Protect from excessive moisture.
Mechanism of Action
Fexofenadine is an active metabolite of terfenadine and like terfenadine it competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels and respiratory tract; it appears that fexofenadine does not cross the blood brain barrier to any appreciable degree, resulting in a reduced potential for sedation
Pharmacodynamics/Kinetics
Onset of action: 60 minutes
Duration: Antihistaminic effect: ≥12 hours
Protein binding: 60% to 70%, primarily albumin and alpha1-acid glycoprotein
Metabolism: Minimal (~5%)
Half-life elimination: 14.4 hours (31% to 72% longer in renal impairment)
Time to peak, serum: ODT: 2 hours (4 hours with high-fat meal); Tablet: ~2.6 hours; Suspension: ~1 hour
Excretion: Feces (~80%) and urine (~11%) as unchanged drug
Dosage
Oral:
Chronic idiopathic urticaria: Children 6 months to <2 years: 15 mg twice daily
Chronic idiopathic urticaria, seasonal allergic rhinitis:
Children 2-11 years: 30 mg twice daily
Children ≥12 years and Adults: 60 mg twice daily or 180 mg once daily
Elderly: Starting dose: Use caution; adjust dose for renal impairment
Allergic rhinitis (OTC labeling):
Children 2-11 years: 30 mg twice daily
Children ≥12 years and Adults: 60 mg twice daily or 180 mg once daily
Dosing adjustment in renal impairment: Clcr <80 mL/minute:
Children 6 months to <2 years: Initial: 15 mg once daily
Children 2-11 years: Initial: 30 mg once daily
Children ≥12 years and Adults: Initial: 60 mg once daily
Hemodialysis: Not effectively removed by hemodialysis
Administration: Oral
Suspension, tablet: Administer with water only; do not administer with fruit juices. Shake suspension well before use.
Orally disintegrating tablet: Take on an empty stomach. Do not remove from blister pack until administered. Using dry hands, place immediately on tongue. Tablet will dissolve within seconds, and may be swallowed with or without liquid (do not administer with fruit juices). Do not split or chew.
Monitoring Parameters
Relief of symptoms
Dietary Considerations
Some products may contain phenylalanine and/or sodium. Take suspension and tablets with water only; do not administer with fruit juices.
Patient Education
Avoid use of alcohol. You may experience mild drowsiness, dizziness, or nausea. Report persistent sedation or drowsiness, lack of improvement, or worsening of condition.
Geriatric Considerations
Plasma levels in the elderly are generally higher than those observed in other age groups. Once daily dosing is recommended when starting therapy in elderly patients or patients with decreased renal function.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause drowsiness or dizziness
Mental Health: Effects on Psychiatric Treatment
None reported
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Suspension, oral, as hydrochloride:
Allegra®: 6 mg/mL (300 mL) [contains propylene glycol; raspberry cream flavor]
Allegra® Children's Allergy: 6 mg/mL (120 mL) [contains propylene glycol, sodium 18 mg/5 mL; berry flavor]
Tablet, oral, as hydrochloride: 30 mg, 60 mg, 180 mg
Allegra®: 60 mg [DSC], 180 mg [DSC]
Allegra® Allergy 12 Hour: 60 mg
Allegra® Allergy 24 Hour: 180 mg
Allegra® Children's Allergy: 30 mg
Tablet, orally disintegrating, oral, as hydrochloride:
Allegra® Children's Allergy ODT: 30 mg [contains phenylalanine 5.3 mg/tablet, sodium 5 mg/tablet; orange cream flavor]
Allegra® ODT: 30 mg [DSC] [contains phenylalanine 5.3 mg/tablet; orange cream flavor]
Pricing: U.S. (www.drugstore.com)
Suspension (Allegra)
30 mg/5 mL (300): $69.99
Tablet, orally-disintegrating (Allegra ODT)
30 mg (60): $126.00
Tablets (Allegra)
60 mg (60): $98.99
180 mg (30): $79.98
References
American Academy of Pediatrics Committee on Drugs, "Transfer of Drugs and Other Chemicals Into Human Milk," Pediatrics, 2001, 108(3):776-89.
Day JH, Briscoe M, Welsh A, et al, “Onset of Action, Efficacy and Safety of a Single Dose of 60 mg and 120 mg Fexofenadine HCl for Ragweed Allergy Using Controlled Antigen Exposure in an Environmental Exposure Unit (EEU),” J Allergy Clin Immunol, 1996, 97(1 Pt 3):434.
“Fexofenadine,” Med Lett Drugs Ther, 1996, 38(986):95-6.
Simons FE, Bergman JN, Watson WT, et al, “The Clinical Pharmacology of Fexofenadine in Children,” J Allergy Clin Immunol, 1996, 98(6 Pt 1):1062-4.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
Content last modified May 2011
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