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Allegra

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Parent: Sanofi Hop 4
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Allegra
IUPAC name(±)-4-(1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl)-α,α-dimethylbenzeneacetic acid
TradenameAllegra, Telfast, others
Drugs.commonograph, fexofenadine
MedlinePlusa697035
Licence USAllegra
Pregnancy AUB1
Routes of administrationBy mouth
ATC prefixR06
ATC suffixAX26
CAS number83799-24-0
PubChem3348
DrugBankDB00950
ChemSpiderID3231
UNIIE6582LOH6V
KEGGD07927
ChEBI5001
ChEMBL975
SynonymsFexofenadine hydrochloride
Molecular weight538.13 g/mol (hydrochloride)

Allegra is a widely recognized brand name for the antihistamine drug fexofenadine, a second-generation H1 receptor antagonist primarily used to treat symptoms of allergic rhinitis and chronic idiopathic urticaria. Developed as the active carboxylic acid metabolite of terfenadine, it was designed to provide effective relief from allergic conditions without the cardiotoxic risks associated with its parent compound. Marketed globally by Sanofi, it is available in various formulations, including tablets, orally disintegrating tablets, and oral suspension, and is approved for use in many countries, including the United States, the United Kingdom, and Australia.

Medical uses

Allegra is indicated for the relief of symptoms associated with seasonal allergic rhinitis, such as sneezing, rhinorrhea, itchy eyes, and itchy palate, in adults and children. It is also approved for the treatment of chronic idiopathic urticaria, reducing pruritus and the number of hives. Clinical studies, including those reviewed by the Food and Drug Administration, have demonstrated its efficacy in improving quality-of-life scores for patients with these conditions. Dosage varies by age and formulation, with common regimens involving once- or twice-daily administration as directed by a healthcare professional.

Pharmacology

Fexofenadine functions as a selective peripheral H1 receptor inverse agonist, competitively inhibiting histamine binding at these receptors. This action blocks the downstream effects of histamine, such as vasodilation and increased vascular permeability, which are responsible for classic allergy symptoms. Unlike first-generation antihistamines like diphenhydramine, it exhibits minimal penetration of the blood-brain barrier, resulting in a low incidence of sedation. Its pharmacokinetics show rapid absorption after oral administration, with peak plasma concentrations reached within 1-3 hours, and it is predominantly excreted unchanged in feces and urine, with a terminal elimination half-life of approximately 14 hours.

Adverse effects

Allegra is generally well-tolerated, with a side effect profile considered favorable compared to older antihistamines. The most commonly reported adverse reactions in clinical trials include headache, drowsiness, nausea, and dyspepsia. Serious adverse effects are rare but can include hypersensitivity reactions such as rash, urticaria, and angioedema. Importantly, at therapeutic doses, it does not prolong the QT interval on an electrocardiogram, a significant safety advantage over its predecessor, terfenadine, which was withdrawn from the U.S. market due to risks of torsades de pointes.

History

The development of fexofenadine originated from research at Sepracor aimed at creating a safer metabolite of the antihistamine terfenadine, which was marketed by Marion Merrell Dow under the brand name Seldane. Following reports of fatal cardiac arrhythmias linked to terfenadine, the FDA mandated new warnings, prompting the search for a non-cardiotoxic alternative. Hoechst AG (later part of Sanofi) licensed and developed the active metabolite, filing a New Drug Application which received approval from the FDA in 1996. The successful launch of Allegra marked a significant advancement in allergy medication, leading to the eventual discontinuation of terfenadine in many markets.

Society and culture

Allegra has become a prominent brand in the over-the-counter allergy medication market following its transition from prescription-only status in the United States in 2011. It has been widely advertised in direct-to-consumer campaigns, competing with other second-generation antihistamines like cetirizine (marketed as Zyrtec) and loratadine (Claritin). The drug is on the World Health Organization's List of Essential Medicines, underscoring its public health importance. Patent expirations have led to the availability of numerous generic fexofenadine products, increasing patient access, though the Allegra brand remains strongly associated with effective non-sedating allergy relief in popular culture.

Category:Antihistamines Category:Sanofi brands Category:Drugs developed in the United States