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Fexofenadine

Fexofenadine
Skeletal formula of fexofenadine
Ball-and-stick model of fexofenadine
Clinical data
Trade names originally Allegra, otherse
AHFS/Drugs.com Monograph
MedlinePlus a697035
License data
Pregnancy
category
  • AU: B2
  • US: C (Risk not ruled out)
Routes of
administration
by mouth
ATC code
Legal status
Legal status
  • AU: Unscheduled
  • CA: OTC
  • UK: POM (Prescription only)
  • US: OTC
Pharmacokinetic data
Bioavailability 30-41%
Protein binding 60-70%
Metabolism Hepatic (≤5% of dose)
Biological half-life 14.4 hours
Excretion Feces (~80%) and urine (~10%) as unchanged drug
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.228.648
Chemical and physical data
Formula C32H39NO4
Molar mass 501.68 g/mol
3D model (Jmol)
Chirality Racemic mixture
 NYesY (what is this?)  

Fexofenadine, sold under the trade name Allegra among others is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever, nasal congestion, and urticaria. Therapeutically, fexofenadine is a selective peripheral H1-blocker.

Fexofenadine is classified as a second-generation antihistamine because it is less able to pass the blood-brain barrier and cause sedation, compared to first-generation antihistamines. It has also been called a third-generation antihistamine, although there is some controversy associated with the use of the term.

Fexofenadine has been manufactured in generic form since 2011.

Fexofenadine is used for relief from physical symptoms associated with seasonal allergic rhinitis and for treatment of chronic urticaria. It does not cure but rather prevents the aggravation of allergic rhinitis and chronic idiopathic urticaria and reduces the severity of the symptoms associated with those conditions, providing relief from repeated sneezing, runny nose, itchy eyes or skin, and general body fatigue.

Fexofenadine has been demonstrated to be safe and effective for children ages 2–5 years old and 6–11 years old in treatment of seasonal allergic rhinitis. Recommended doses of fexofenadine in UK labeling referenced below are: For adults with seasonal allergic rhinitis (hay fever): 60 mg twice daily or 120 mg taken once a day. For children aged 6–12 years with seasonal allergic rhinitis (hay fever): 30 mg taken twice a day, in the morning and evening. For adults with chronic urticaria: 180 mg taken once a day. For adults with chronic nasal congestion.

The most common side effect demonstrated in adults was headache, but some also experienced back and muscle pain, miosis or pinpoint pupils, nausea, drowsiness, and menstrual cramps. There have also been rare reports of anxiety and insomnia. The most common side effects demonstrated during clinical trials were cough, upper respiratory tract infection, fever, and otitis media for children ages 6 to 11 and fatigue for children ages 6 months to 5 years.


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