Fexofenadine
Sanofi-aventis
1595 Items
2019-09-19
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Clinical Pharmacology
Fexofenadine (a pharmacologically active metabolite of terfenadine) is an antihistamine agent with selective antagonistic activity to H1 receptors without anticholinergic and alpha-adrenergic blocking action receptors. In addition, fexofenadine does not show a sedative effect and other effects from the central nervous system.
In human studies on the assessment of histamine-induced wheals and hyperemia, the antihistamine effect of fexofenadine, taken orally once or twice a day, appears after 1 hour, reaches a maximum after 6 hours, and lasts for 24 hours after taking it. Even after 28 days of taking fexofenadine, no tolerance to the drug was detected. With a single dose of fexofenadine, a dose-dependent increase in the antihistamine effect is observed with an increase in the dose from 10 mg to 130 mg. When using the same model of antihistamine action, it was found that a dose of at least 130 mg was necessary for a constant action over 24 hours. The maximum suppression of blistering and hyperemia of the skin is more than 80%.
In patients with seasonal allergic rhinitis who received up to 240 mg of fexofenadine 2 times a day for 2 weeks, the duration of the QTc interval (corrected QT) did not differ from that taken with placebo.
Also, no QTc changes were observed when taking fexofenadine by healthy volunteers 60 mg 2 times a day for 6 months, 400 mg 2 times a day for 6.5 days and 240 mg a day for 1 year compared with the duration of QTc when taking placebo .
Even with a plasma concentration 32 times the therapeutic concentration in humans, fexofenadine did not affect the potassium channels of the delayed straightening in the human heart.
Indications
- seasonal allergic rhinitis (to reduce symptoms) - pills, 120 mg;
- Chronic idiopathic urticaria (to reduce symptoms) - pills, 180 mg.
Composition
Excipients: croscarmellose sodium - 24 mg, pregelatinized starch - 120 mg, microcrystalline cellulose - 133 mg, magnesium stearate - 3 mg.
Shell composition: Hypromellose E-15 - 2.84 mg, Hypromellose E-5 - 1.89 mg, Povidone - 510 mcg, titanium dioxide (E171) - 2.025 mg, Colloidal silicon dioxide - 730 mcg, Macrogol 400 - 3.94 mg, Pink mixture of iron dye oxide (iron oxide red (E172), titanium dioxide (E171)) - 250 μg, yellow mixture of iron dye (iron oxide yellow (E172), titanium dioxide (E171)) - 40 μg.
Fexofenadine is marketed under different brands and generic names, and comes in different dosage forms:
| Brand name | Manufacturer | Country | Dosage form |
|---|---|---|---|
| Allegra | Sanofi-aventis | France | pills |
| Fexofast | Micro Labs Ltd | India | pills |
| Fexadine | Ranbaxy Laboratories Ltd | India | pills |
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Dosage and Administration
pills are intended for ingestion.
The recommended dose of fexofenadine for seasonal allergic rhinitis for adults and children 12 years and older is 120 mg 1 time per day before meals.
The recommended dose of fexofenadine for chronic urticaria for adults and children 12 years and older is 180 mg once a day before meals.
Patients at risk
Studies in special risk groups (elderly patients, patients with renal and hepatic insufficiency) showed that they do not require correction of the dosage regimen.
Adverse reactions
In placebo-controlled clinical trials, the most frequent (≥1% headache (7.3%), drowsiness (2.3%), dizziness (1.5%) and nausea 1.5%. When taking fexofenadine, the incidence of the above adverse effects was similar to that taken with placebo.
In placebo-controlled studies with a frequency of less than 1% (equally when taking fexofenadine and placebo) and with post-marketing use of the drug were weakness, insomnia, nervousness and sleep disorders or unusual dreams (paroniria), such as nightmares; tachycardia, palpitations; diarrhea.
Contraindications
- hypersensitivity to any of the components of the drug;
- pregnancy;
- lactation period;
- children's age (up to 12 years).
Carefully:
- in patients with chronic renal and hepatic insufficiency, as well as in elderly patients (lack of clinical experience in this category of patients);
- in patients with cardiovascular diseases, including in the anamnesis (antihistamines can cause heartbeat and tachycardia).
In violation of renal function.
Use with caution in chronic renal failure. Correction of the dosing regimen is not required.
In violation of the liver.
Use with caution in chronic liver failure. Correction of the dosing regimen is not required.
Drug interactions
When combined with fexofenadine with erythromycin or ketoconazole, the concentration of fexofenadine in plasma increases by a factor of 2-3, but this is not associated with a significant lengthening of the QTc interval. There were no significant differences in the incidence of adverse effects when using these drugs in monotherapy and in combination. Animal studies have shown that the aforementioned increase in plasma concentrations of fexofenadine is probably associated with improved absorption of fexofenadine and a decrease in its biliary excretion or secretion into the lumen of the gastrointestinal tract.
The interaction between fexofenadine and omeprazole is not observed.
Does not interact with drugs that metabolize in the liver.
Acceptance of aluminum or magnesium containing antacids 15 minutes before taking fexofenadine results in a decrease in bioavailability of the latter as a result of apparently binding in the gastrointestinal tract.
Pregnancy and Lactation
Pregnancy
There is not enough data on the use of fexofenadine in pregnant women. Limited animal studies have shown no signs of adverse effects on pregnancy, fetal development, childbirth, and postnatal development. Fexofenadine should not be used during pregnancy.
Lactation
Data on the content of fexofenadine in breast milk when it is taken by nursing women is not available. However, when taking terfenadine, its penetration into breast milk of lactating women was observed. Therefore, the use of fexofenadine during the lactation period is not recommended.
Special instructions
It is recommended that the time interval between taking fexofenadine and antacids containing aluminum or magnesium hydroxide is at least 2 hours.
For use in children from 6 to 11 years old pills are available 30 mg.
Influence on ability to drive motor transport and control mechanisms
When taking the drug, it is possible to perform work that requires a high concentration of attention and speed of psychomotor reactions (with the exception of patients with non-standard reaction). Therefore, it is recommended to check individual response to fexofenadine prior to engaging in such activities.
Overdosage
Symptoms: dizziness, drowsiness and dry mouth. Healthy volunteers took single doses up to 800 mg, and course doses up to 690 mg 2 times a day for 1 month or 240 mg 2 times a day for 1 year without any significant adverse effects compared to placebo. The maximum tolerated dose for fexofenadine has not been established.
Treatment: in the case of overdose, it is recommended to carry out gastric lavage, taking activated charcoal, if necessary, symptomatic and supportive therapy. Hemodialysis is ineffective.
- Brand name: Allegra
- Active ingredient: Fexofenadine
- Dosage form: pills, film coated light pink, oblong, biconvex, engraved with "012" on one side and stylized "e" - on the other.
- Manufacturer: Sanofi-aventis
- Country of Origin: France
Studies and clinical trials of Fexofenadine (Click to expand)
- Effect of food on the bioavailability of fexofenadine hydrochloride (MDL 16 455A)
- The utility of mixed-effects covariate analysis in rapid selection of doses in pediatric subjects: A case study with fexofenadine hydrochloride
- Analysis of fexofenadine in pharmaceutical formulations using tris(1,10-phenanthroline)–ruthenium(II) peroxydisulphate chemiluminescence system in a multichip device
- Measurement of fexofenadine concentration in micro-sample human plasma by a rapid and sensitive LC-MS/MS employing protein precipitation: application to a clinical pharmacokinetic study
- Quantification of fexofenadine in human plasma by liquid chromatography coupled to electrospray tandem mass spectrometry using mosapride as internal standard
- ChemInform Abstract: An Efficient and Facile Synthesis of Racemic and Optically Active Fexofenadine.
- ChemInform Abstract: A New Synthesis of Carboxyterfenadine (Fexofenadine) and Its Bioisosteric Tetrazole Analogues.
- ChemInform Abstract: Novel and Efficient Method for the Synthesis of Racemic Fexofenadine.
- Pharmacokinetics of fexofenadine enantiomers in healthy subjects
- Comparative study of acute effects of single doses of fexofenadine, olopatadine, d-chlorpheniramine and placebo on psychomotor function in healthy volunteers
- Effects of fexofenadine and hydroxyzine on brake reaction time during car-driving with cellular phone use
- Effect of fruit juices on the oral bioavailability of fexofenadine in rats
- Poloxamer/cyclodextrin/chitosan-based thermoreversible gel for intranasal delivery of fexofenadine hydrochloride
- Enhancing effect of surfactants on fexofenadine·HCl transport across the human nasal epithelial cell monolayer
- Relative contribution of absorptive and secretory transporters to the intestinal absorption of fexofenadine in rats
- Preparation and evaluation of fexofenadine microemulsions for intranasal delivery
- Spectrofluorimetric determination of fexofenadine hydrochloride in pharmaceutical preparation using silver nanoparticles
- Effect of the sex-related MDR1 gene polymorphisms on fexofenadine disposition
- A variant 2677A allele of the gene affects fexofenadine disposition
- Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics
- Effect of Grapefruit Juice Volume on the Reduction of Fexofenadine Bioavailability: Possible Role of Organic Anion Transporting Polypeptides*
- A pilot study to assess simultaneous administration of oral midazolam (MDZ) and fexofenadine (FEX) for the evaluation of cytochrome (CYP) 3A4 and P-glycoprotein (P-GP) activities
- Pharmacokinetics (PK) of multiple oral doses of desloratadine (DCL) and fexofenadine (FEX) in a population of healthy adults identified phenotypically as desloratadine slow metabolizers (DSMS)
- Effect of itraconazole on the pharmacokinetics and pharmacodynamics of fexofenadine in relation to the genetic polymorphism
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