Peringatan Keamanan

No deaths were observed following the oral administration of up to 5000 mg/kg in both mice and rats (equivalent to approximately 100-200x the recommended human dose). Single doses of up to 800 mg and chronic exposure of up to 690 mg twice daily for 1 month in humans did not result in clinically significant adverse events. Symptoms of overdosage are consistent with fexofenadine's adverse effect profile and are likely to include dizziness, drowsiness, and dry mouth.L4269

If overdosage occurs, employ symptomatic and supportive treatment. Hemodialysis does not effectively remove fexofenadine from the blood and is therefore of no benefit.L4269

Fexofenadine

DB00950

small molecule approved investigational

Deskripsi

Fexofenadine is an over-the-counter second-generation antihistamine used in the treatment of various allergic symptoms.L4269 It is selective for the H1 receptor, carries little-to-no activity at off-targets, and does not cross the blood-brain barrierL10779 - this is in contrast to previous first-generation antihistamines, such as diphenhydramine, which readily bind to off-targets that contribute to side effects such as sedation.A1452 Fexofenadine is the major active metabolite of terfenadineA1495 and is administered as a racemic mixture in which both enantiomers display approximately equivalent antihistamine activity.L10779

Struktur Molekul 2D

Berat 501.6564
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life is approximately 11-15 hours.[L10779,A1495]
Volume Distribusi The volume of distribution is approximately 5.4-5.8 L/kg.[A1495]
Klirens (Clearance) The oral clearance of fexofenadine is approximately 50.6 L/h and the renal clearance is approximately 4.32 L/h.[L10779]

Absorpsi

Fexofenadine is rapidly absorbed following oral administration and its absolute bioavailability is approximately 33%.L10779 The Tmax following oral administration is approximately 1-3 hours.L10779,A1495 The steady-state AUCss(0-12h) and Cmax following twice daily dosing of 60mg are 1367 ng/mL.h and 299 ng/mL, respectively.L10779 Fexofenadine AUC is decreased by >20% when coadministered with fruit juices (e.g. apple, orange, grapefruit) due to their inhibition of OATP transporters - for this reason, prescribing information recommends administering fexofenadine only with water.A188754 Similarly, coadministration of fexofenadine with a high-fat meal appears to decrease AUC and Cmax by >20%.L4269

Metabolisme

Fexofenadine is very minimally metabolized, with only 5% of an ingested dose undergoing hepatic metabolism.L4269,A1495 The only identified metabolites are a methyl ester of fexofenadine (3.6% of the total dose) and MDL 4829 (1.5% of the total dose).L10779 The enzymes responsible for this metabolism have not been elucidated.

Rute Eliminasi

Approximately 80% of an ingested dose is eliminated in the feces, likely largely unchanged due to fexofenadine's limited metabolism, and 11% is eliminated in the urine.A1495 The principal pathways of fexofenadine elimination are biliary and renal.L10779

Interaksi Makanan

2 Data
  • 1. Avoid fruit juice. Fruit juices like grapefruit, orange, and apple may reduce bioavailability and overall exposure to the medication.
  • 2. Take with or without food. Co-administration with food does not significantly affect absorption.

Interaksi Obat

427 Data
Ranolazine The serum concentration of Fexofenadine can be increased when it is combined with Ranolazine.
Erythromycin Erythromycin can cause an increase in the absorption of Fexofenadine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Benzylpenicilloyl polylysine Fexofenadine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Fexofenadine.
Minocycline The excretion of Fexofenadine can be decreased when combined with Minocycline.
Aspartame The excretion of Fexofenadine can be decreased when combined with Aspartame.
Cefotiam The excretion of Fexofenadine can be decreased when combined with Cefotiam.
Liothyronine The excretion of Fexofenadine can be decreased when combined with Liothyronine.
Aminohippuric acid The excretion of Fexofenadine can be decreased when combined with Aminohippuric acid.
Cefalotin The excretion of Fexofenadine can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Fexofenadine can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Fexofenadine can be decreased when combined with Cefotaxime.
Guanidine The excretion of Fexofenadine can be decreased when combined with Guanidine.
Piroxicam The excretion of Fexofenadine can be decreased when combined with Piroxicam.
Cephalexin The excretion of Fexofenadine can be decreased when combined with Cephalexin.
Oxytetracycline The excretion of Fexofenadine can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Fexofenadine can be decreased when combined with Leucovorin.
Furosemide The excretion of Fexofenadine can be decreased when combined with Furosemide.
Acyclovir The excretion of Fexofenadine can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Fexofenadine can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Fexofenadine can be decreased when combined with Cefaclor.
Bumetanide The excretion of Fexofenadine can be decreased when combined with Bumetanide.
Dinoprostone The excretion of Fexofenadine can be decreased when combined with Dinoprostone.
Salicylic acid The excretion of Fexofenadine can be decreased when combined with Salicylic acid.
Ganciclovir The excretion of Fexofenadine can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Fexofenadine can be decreased when combined with Ketoprofen.
Probenecid The excretion of Fexofenadine can be decreased when combined with Probenecid.
Mercaptopurine The excretion of Fexofenadine can be decreased when combined with Mercaptopurine.
Novobiocin The excretion of Fexofenadine can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Fexofenadine can be decreased when combined with Benzylpenicillin.
Ouabain The excretion of Fexofenadine can be decreased when combined with Ouabain.
Rosuvastatin The excretion of Fexofenadine can be decreased when combined with Rosuvastatin.
Cefadroxil The excretion of Fexofenadine can be decreased when combined with Cefadroxil.
Cefamandole The excretion of Fexofenadine can be decreased when combined with Cefamandole.
Cefazolin The excretion of Fexofenadine can be decreased when combined with Cefazolin.
Ceftizoxime The excretion of Fexofenadine can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Fexofenadine can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Fexofenadine can be decreased when combined with Ceftibuten.
Liotrix The excretion of Fexofenadine can be decreased when combined with Liotrix.
Cilastatin The excretion of Fexofenadine can be decreased when combined with Cilastatin.
Tazobactam The excretion of Fexofenadine can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Fexofenadine can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Fexofenadine can be decreased when combined with Topiroxostat.
Cholic Acid The excretion of Fexofenadine can be decreased when combined with Cholic Acid.
Glutaric Acid The excretion of Fexofenadine can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Fexofenadine can be decreased when combined with Benzoic acid.
Caprylic acid The excretion of Fexofenadine can be decreased when combined with Caprylic acid.
Ataluren The excretion of Fexofenadine can be decreased when combined with Ataluren.
Teriflunomide The excretion of Fexofenadine can be decreased when combined with Teriflunomide.
Cefaloridine The excretion of Fexofenadine can be decreased when combined with Cefaloridine.
Cabotegravir The excretion of Fexofenadine can be decreased when combined with Cabotegravir.
Pradigastat The excretion of Fexofenadine can be decreased when combined with Pradigastat.
Valproic acid The excretion of Fexofenadine can be decreased when combined with Valproic acid.
Famotidine The excretion of Fexofenadine can be decreased when combined with Famotidine.
Melatonin The excretion of Fexofenadine can be decreased when combined with Melatonin.
Gemfibrozil The excretion of Fexofenadine can be decreased when combined with Gemfibrozil.
Pantoprazole The excretion of Fexofenadine can be decreased when combined with Pantoprazole.
Indomethacin The excretion of Fexofenadine can be decreased when combined with Indomethacin.
Diclofenac The excretion of Fexofenadine can be decreased when combined with Diclofenac.
Conjugated estrogens The excretion of Fexofenadine can be decreased when combined with Conjugated estrogens.
Lansoprazole The excretion of Fexofenadine can be decreased when combined with Lansoprazole.
Zidovudine The excretion of Fexofenadine can be decreased when combined with Zidovudine.
Cimetidine The excretion of Fexofenadine can be decreased when combined with Cimetidine.
Methotrexate The excretion of Fexofenadine can be decreased when combined with Methotrexate.
Enalapril The excretion of Fexofenadine can be decreased when combined with Enalapril.
Tetracycline The excretion of Fexofenadine can be decreased when combined with Tetracycline.
Acetylsalicylic acid The excretion of Fexofenadine can be decreased when combined with Acetylsalicylic acid.
Ibuprofen The excretion of Fexofenadine can be decreased when combined with Ibuprofen.
Letermovir The excretion of Fexofenadine can be decreased when combined with Letermovir.
Esomeprazole The excretion of Fexofenadine can be decreased when combined with Esomeprazole.
Ceftriaxone The excretion of Fexofenadine can be decreased when combined with Ceftriaxone.
Cefoperazone The excretion of Fexofenadine can be decreased when combined with Cefoperazone.
Taurocholic acid The excretion of Fexofenadine can be decreased when combined with Taurocholic acid.
Favipiravir The excretion of Fexofenadine can be decreased when combined with Favipiravir.
Tafamidis The excretion of Fexofenadine can be decreased when combined with Tafamidis.
Linezolid The excretion of Fexofenadine can be decreased when combined with Linezolid.
Ketoconazole The serum concentration of Fexofenadine can be increased when it is combined with Ketoconazole.
Rifampin The serum concentration of Fexofenadine can be increased when it is combined with Rifampicin.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Fexofenadine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Amphetamine Amphetamine may decrease the sedative activities of Fexofenadine.
Phentermine Phentermine may decrease the sedative activities of Fexofenadine.
Benzphetamine Benzphetamine may decrease the sedative activities of Fexofenadine.
Diethylpropion Diethylpropion may decrease the sedative activities of Fexofenadine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Fexofenadine.
Mephentermine Mephentermine may decrease the sedative activities of Fexofenadine.
MMDA MMDA may decrease the sedative activities of Fexofenadine.
Midomafetamine Midomafetamine may decrease the sedative activities of Fexofenadine.

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

Synthesis reference: Federico Milla, "Processes for the production of fexofenadine." U.S. Patent US20030166682, issued September 04, 2003.
Artikel (PubMed)
  • PMID: 19545214
    Smith SM, Gums JG: Fexofenadine: biochemical, pharmacokinetic and pharmacodynamic properties and its unique role in allergic disorders. Expert Opin Drug Metab Toxicol. 2009 Jul;5(7):813-22. doi: 10.1517/17425250903044967.
  • PMID: 19539095
    Bachert C: A review of the efficacy of desloratadine, fexofenadine, and levocetirizine in the treatment of nasal congestion in patients with allergic rhinitis. Clin Ther. 2009 May;31(5):921-44. doi: 10.1016/j.clinthera.2009.05.017.
  • PMID: 9506246
    Markham A, Wagstaff AJ: Fexofenadine. Drugs. 1998 Feb;55(2):269-74; discussion 275-6.
  • PMID: 15669879
    Golightly LK, Greos LS: Second-generation antihistamines: actions and efficacy in the management of allergic disorders. Drugs. 2005;65(3):341-84.
  • PMID: 15312146
    Molimard M, Diquet B, Benedetti MS: Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans. Fundam Clin Pharmacol. 2004 Aug;18(4):399-411.
  • PMID: 29635947
    Akamine Y, Miura M: An update on the clinical pharmacokinetics of fexofenadine enantiomers. Expert Opin Drug Metab Toxicol. 2018 Apr;14(4):429-434. doi: 10.1080/17425255.2018.1459565. Epub 2018 Apr 11.
  • PMID: 18336052
    Devillier P, Roche N, Faisy C: Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30.
  • PMID: 28414144
    Yu J, Zhou Z, Tay-Sontheimer J, Levy RH, Ragueneau-Majlessi I: Intestinal Drug Interactions Mediated by OATPs: A Systematic Review of Preclinical and Clinical Findings. J Pharm Sci. 2017 Sep;106(9):2312-2325. doi: 10.1016/j.xphs.2017.04.004. Epub 2017 Apr 13.

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