Help Support

Allergies_and_Urticaria Allergies_and_Urticaria
Allergies_and_Urticaria Allergies_and_Urticaria

Fexofenadine, a selective H1-antagonist and second-generation antihistamine, is FDA-approved to treat symptomatic seasonal allergic rhinitis and chronic idiopathic urticaria.

See All


Fexofenadine, a selective H1-antagonist and second-generation antihistamine, is FDA-approved to treat symptomatic seasonal allergic rhinitis and chronic idiopathic urticaria. It has approval for use in both adults and children. It does not cross the blood-brain barrier and therefore does not elicit drowsiness when compared to H1 blockers. Furthermore, it has less affinity for alpha-adrenergic and cholinergic receptors and thus does not exhibit anticholinergic adverse effects in comparison with other antihistamine agents. [1] 


Pharmacological Class: Antihistamines [2]


Fexofenadine (second-generation H1 receptor blocker) is indicated for the treatment of:

  • Chronic idiopathic urticaria
  • Allergic rhinitis [3]

Pharmachologic action

For mediation of allergic and hypersensitivity reactions, the H1 histamine receptor is accountable. Exposure to an allergen triggers degranulation of basophils and mast cells. This results in liberation of histamine and other mediators of inflammation. Histamine binds to H1 receptors and results in its activation. This, in turn, liberates pro-inflammatory cytokines (like interleukins) from mast cells and basophils. These downstream impact of histamine binding are accountable for a vast range of symptoms of allergy, like watery eyes, rhinorrhea, and pruritus.

Fexofenadine is deemed as an “inverse agonist” of H1 receptor. It has a selective and potent affinity for H1 receptors. It binds to and stabilizes inactive form of receptor. This, in turn, prevents its activation and subsequent downstream impact. [4] Fexofenadine selectively antagonizes H1 receptors on surface of cells. It is non-sedating and affects the inflammatory mediators. It can also suppress other mechanisms like mast cell, basophilic histamine, and inflammatory cell release. [1]


(I) Adult Dosing

  • For chronic urticaria and seasonal allergic rhinitis, dosing is same: 60 mg PO BID or 180 mg PO daily.


(II) Pediatrics Dosing (differs based on age and indication)

  • Seasonal Allergic Rhinitis
  • Not approved for usage in children less than 2 years of age
  • Children 2-12 years old: 30 mg PO BID
  • Children older than twelve years old: 60 mg PO BID or 180 mg PO daily
  • Chronic Urticaria
  • Not approved for usage in infants less than 6 months old
  • Children six months to two years old: 15 mg PO BID
  • Children 2-12 years old: 30 mg PO BID
  • Children older than twelve years: 60 mg PO BID or 180 mg PO daily


(III) Special Population

  • Renal Impairment (creatinine clearance <80 ml/min)
  • Adults should take 60 mg PO daily


Dosing for pediatric patients with renal impairment varies by age as follows:

(a) Children older than twelve years: 60 mg PO daily

(b) Children two-twelve years old: 30 mg PO daily

(c) Children six months to two years old: 15 mg PO daily [1]



After the oral administration of fexofenadine, it is rapidly absorbed with a bioavailability of about 33%. Post-administration Tmax is about 1 to 3 hours. The steady-state area under curve [AUCss (0-12h)] and Cmax after receiving 60 mg dosing twice daily are 1367 ng/mL.h and 299 ng/mL.

The AUC of fexofenadine is lowered by >20% when concomitantly administered with fruit juices due to their suppression of OATP transporters. It is recommended to take fexofenadine with water only. Likewise, fexofenadine coadministration with high-fat food seems to lower the Cmax and  AUC by >20%.


Volume of distribution

Fexofenadine's  volume of distribution is around 5.4-5.8 L/kg


Protein binding

There is 60-70% binding of fexofenadine with plasma proteins, majorly with albumin and α1-acid glycoprotein. In people with hepatic and renal impairment, the degree of protein binding is decreased to 56-75% and 56-68%



Fexofenadine is slightly metabolized, with only 5% of consumed dosage undergoing liver metabolism. MDL 4829 and methyl ester of fexofenadine are the only identified metabolites


Route of elimination

Elimination of ingested dose is via faeces (80%), and 11% through urine. Renal and biliary are the major pathways for the elimination of fexofenadine



The terminal elimination half-life of fexofenadine is found to be about 11-15 hours



The renal clearance of fexofenadine is approximately 4.32 L/h and the oral clearance is around 50.6 L/h[4]


  • It is contraindicated in people with known hypersensitivity to fexofenadine [2]
  • It must be used cautiously in patients with renal disease [3]

Drug interaction

  • It is contraindicated in people with known hypersensitivity to fexofenadine [2]
  • It must be used cautiously in patients with renal disease [3]

Side effects

The most commonly reported adverse effects are:

  • Otitis media
  • Back pain
  • Upper respiratory tract infection
  • Dizziness
  • Cough
  • Stomach discomfort
  • Pain in extremity
  • Vomiting
  • Pyrexia
  • Diarrhea
  • Somnolence/fatigue
  • Rhinorrhea
  • Headache [3]


  • The use of fexofenadine must be avoided in individuals who are allergic to it
  • Fexofenadine should be cautiously utilized in breast-feeding, pregnant, and women planning to become pregnant [2]

Clinical evidence

(a) Allergic rhinitis

In a systematic review and meta-analysis carried out by Huang CZ et al., fexofenadine exhibited a positive antihistamine effect with a favorable safety profile. Overall, 51 trials and 14,551 participants were included to compare safety and antihistamine effects of fexofenadine with either placebo or other antihistamine agents for healthy subjects and people with allergies.[6]

According to a phase 3, randomized, double-blind trial conducted by Anne K. Ellis et al. in 251 people with seasonal allergic rhinitis, fexofenadine HCl (180 mg) was efficient in ameliorating pollen-induced, air pollution-exacerbated symptoms of allergic rhinitis. [7]

A review demonstrated that compared to placebo, fexofenadine can effectively relieve nasal congestion linked with allergic rhinitis. [8] A study by Okubo K et al. reported that administration of fexofenadine HCl (60 mg twice a day) can elicit significant improvement in overall quality of life and work productivity in people with seasonal allergic rhinitis. [9]


(b) Urticaria

A quasi-experimental study aimed to explore efficacy of fexofenadine in 100 patients (aged 18 years and above) with chronic idiopathic urticaria. Participants received 120 mg of fexofenadine twice daily for four weeks. Following 4 weeks of therapy, 42% reported complete disappearance of symptoms, 24% exhibited marked improvement, 26% had moderate improvement, and 8.0% illustrated slight improvement. Fexofenadine was highly efficient in alleviating chronic idiopathic urticaria.[10]

In a network meta-analysis, fexofenadine demonstrated superior therapeutic efficacy (in terms of total symptom score [TSS] changes from baseline) when compared to placebo for treatment of people diagnosed with chronic spontaneous urticaria. [11] A narrative review suggested that second-generation antihistamines like fexofenadine HCl can considerably reduce urticaria symptoms such as wheals and angioedema. [12] In a systematic literature review, high doses of fexofenadine were found to elicit a significant dose-dependent response and controlled urticaria in most of the patients. [13]


    1. Craun KL, Schury MP. Fexofenadine. [Updated 2021 Oct 31]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan. Bookshelf ID: NBK556104. PMID: 32310564 Available from:  https://www.ncbi.nlm.nih.gov/books/NBK556104/
    2. Fexofenadine. Available online from: https://medlineplus.gov/druginfo/meds/a697035.html [Last accessed on: 18 May 2022]
    3. Fexofenadine. FDA LABEL. Available online from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021963s007lbl.pdf [Last accessed on: 18 May 2022]
    4. Fexofenadine. Drug Bank. Accession Number DB00950. Available online from: https://go.drugbank.com/drugs/DB00950 [Last accessed on: 18 May 2022].
    5. Axelrod D, Bielory L. Fexofenadine hydrochloride in the treatment of allergic disease: a review. Journal of Asthma and Allergy. 2008;1:19.
    6. Huang CZ, Jiang ZH, Wang J, Luo Y, Peng H. Antihistamine effects and safety of fexofenadine: a systematic review and Meta-analysis of randomized controlled trials. BMC Pharmacology and Toxicology. 2019 Dec;20(1):1-8.
    7. Ellis AK, Murrieta-Aguttes M, Furey S, Picard P, Carlsten C. Effect of fexofenadine hydrochloride on allergic rhinitis aggravated by air pollutants. ERJ open research. 2021 Apr 1;7(2).
    8. Bachert C. A review of the efficacy of desloratadine, fexofenadine, and levocetirizine in the treatment of nasal congestion in patients with allergic rhinitis. Clinical therapeutics. 2009 May 1;31(5):921-44. 
    9. Okubo K, Gotoh M, Shimada K, Ritsu M, Okuda M, Crawford B. Fexofenadine improves the quality of life and work productivity in Japanese patients with seasonal allergic rhinitis during the peak cedar pollinosis season. Int Arch Allergy Immunol. 2005 Feb;136(2):148-54.
    10. Jahan H, Akhter F, Nandi AK. Efficacy of Fexofenadine in the Treatment of Chronic Idiopathic Urticaria. Mymensingh Medical Journal: MMJ. 2020 Apr 1;29(2):414-9.
    11. Phinyo P, Koompawichit P, Nochaiwong S, Tovanabutra N, Chiewchanvit S, Chuamanochan M. Comparative Efficacy and Acceptability of Licensed Dose Second-Generation Antihistamines in Chronic Spontaneous Urticaria: A Network Meta-Analysis. J Allergy Clin Immunol Pract. 2021 Feb;9(2):956-970.e57.
    12. Ansotegui IJ, Bernstein JA, Canonica GW, Gonzalez-Diaz SN, Martin BL, Morais-Almeida M et al. Insights into urticaria in pediatric and adult populations and its management with fexofenadine hydrochloride. Allergy, Asthma & Clinical Immunology. 2022 Dec;18(1):1-7.
    13. Sotes P, Armisén M, Usero-Bárcena T, Fernandez A, Rivas OM, Gonzalez MT et al. Efficacy and safety of up-dosing antihistamines in chronic spontaneous urticaria: A systematic review of the literature. JOURNAL OF INVESTIGATIONAL ALLERGOLOGY AND CLINICAL IMMUNOLOGY. 2021 Jan 1;31(4):282-91.

Comments (0)

You want to delete this comment? Please mention comment Invalid Text Content Text Content cannot me more than 1000 Something Went Wrong Cancel Confirm Confirm Delete Hide Replies View Replies View Replies en ru