- 1. Name of the medicinal product
- 2. Qualitative and quantitative composition
- 3. Pharmaceutical form
- 4. Clinical particulars
- 4.1 Therapeutic indications
- 4.2 Posology and method of administration
- 4.3 Contraindications
- 4.4 Special warnings and precautions for use
- 4.5 Interaction with other medicinal products and other forms of interaction
- 4.6 Fertility pregnancy and lactation
- 4.7 Effects on ability to drive and use machines
- 4.8 Undesirable effects
- 4.9 Overdose
- 5. Pharmacological properties
- 5.1 Pharmacodynamic properties
- 5.2 Pharmacokinetic properties
- 5.3 Preclinical safety data
- 6. Pharmaceutical particulars
- 6.1 List of excipients
- 6.2 Incompatibilities
- 6.3 Shelf life
- 6.4 Special precautions for storage
- 6.5 Nature and contents of container
- 6.6 Special precautions for disposal and other handling
- 7. Marketing authorisation holder
- 8. Marketing authorisation number(s)
- 9. Date of first authorisation/renewal of the authorisation
- 10. Date of revision of the text
- Legal classification
AdultsThe recommended dose of fexofenadine hydrochloride for adults is 120 mg once daily taken before a meal.Fexofenadine is a pharmacologically active metabolite of terfenadine.Paediatric population• Children aged 12 years and overThe recommended dose of fexofenadine hydrochloride for children aged 12 years and over is 120 mg one daily taken before a meal.• Children under 12 years of ageThe efficacy and safety of fexofenadine hydrochloride 120 mg has not been studied in children under 12.In children from 6 to 11 years of age: fexofenadine hydrochloride 30 mg tablet is the appropriate formulation for administration and dosing in this population.
Special populationsStudies in special risk groups (elderly, renally or hepatically impaired patients) indicate that it is not necessary to adjust the dose of fexofenadine hydrochloride in these patients.
PregnancyThere are no adequate data from the use of fexofenadine hydrochloride in pregnant women. Limited animal studies do not indicate direct or indirect harmful effects with respect to effects on pregnancy, embryonal/foetal development, parturition or postnatal development (see section 5.3). Fexofenadine hydrochloride should not be used during pregnancy unless clearly necessary.
Breast-feedingThere are no data on the content of human milk after administering fexofenadine hydrochloride. However, when terfenadine was administered to nursing mothers fexofenadine was found to cross into human breast milk. Therefore fexofenadine hydrochloride is not recommended for mothers breast-feeding their babies.
FertilityNo human data on the effect of fexofenadine hydrochloride on fertility are available. In mice, there was no effect on fertility with fexofenadine hydrochloride treatment (see section 5.3).
Nervous system disordersCommon: headache, drowsiness, dizziness
Gastrointestinal disordersCommon: nausea
General disorders and administration site conditionsUncommon: fatigueIn adults, the following undesirable effects have been reported in post-marketing surveillance. The frequency with which they occur is not known (can not be estimated from available data):
Immune system disordershypersensitivity reactions with manifestations such as angioedema, chest tightness, dyspnoea, flushing and systemic anaphylaxis
Psychiatric disordersinsomnia, nervousness, sleep disorders or nightmares/excessive dreaming (paroniria)
Cardiac disorderstachycardia, palpitations
Skin and subcutaneous tissue disordersrash, urticaria, pruritus
Reporting of suspected adverse reactionsReporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard
Mechanism of actionFexofenadine hydrochloride is a non-sedating H1 antihistamine. Fexofenadine is a pharmacologically active metabolite of terfenadine.
Clinical efficacy and safetyHuman histamine wheal and flare studies following single and twice daily doses of fexofenadine hydrochloride demonstrate that the medicinal product exhibits an antihistaminic effect beginning within one hour, achieving maximum at 6 hours and lasting 24 hours. There was no evidence of tolerance to these effects after 28 days of dosing. A positive dose-response relationship between doses of 10 mg to 130 mg taken orally was found to exist. In this model of antihistaminic activity, it was found that doses of at least 130 mg were required to achieve a consistent effect that was maintained over a 24 hour period. Maximum inhibition in skin wheal and flare areas were greater than 80%. Clinical studies conducted in seasonal allergic rhinitis have shown that a dose of 120 mg is sufficient for 24 hour efficacy.No significant differences in QTc intervals were observed in seasonal allergic rhinitis patients given fexofenadine hydrochloride up to 240 mg twice daily for 2 weeks when compared to placebo. Also, no significant change in QTc intervals was observed in healthy subjects given fexofenadine hydrochloride up to 60 mg twice daily for 6 months, 400 mg twice daily for 6.5 days and 240 mg once daily for 1 year, when compared to placebo. Fexofenadine at concentrations 32 times greater than the therapeutic concentration in man had no effect on the delayed rectifier K+ channel cloned from human heart.Fexofenadine hydrochloride (5-10 mg/kg po) inhibited antigen induced bronchospasm in sensitised guinea pigs and inhibited histamine release at supratherapeutic concentrations (10-100 μM) from peritoneal mast cells.
AbsorptionFexofenadine hydrochloride is rapidly absorbed into the body following oral administration, with Tmax occurring at approximately 1-3 hours post dose. The mean Cmax value was approximately 427 ng/ml following the administration of a 120 mg dose once daily.
DistributionFexofenadine is 60-70% plasma protein bound.
Biotransformation and eliminationFexofenadine undergoes negligible metabolism (hepatic or non-hepatic), as it was the only major compound identified in urine and faeces of animals and man. The plasma concentration profiles of fexofenadine follow a bi-exponential decline with a terminal elimination half-life ranging from 11 to 15 hours after multiple dosing. The single and multiple dose pharmacokinetics of fexofenadine are linear for oral doses up to 120 mg BID. A dose of 240 mg BID produced slightly greater than proportional increase (8.8%) in steady state area under the curve, indicating that fexofenadine pharmacokinetics are practically linear at these doses between 40 mg and 240 mg taken daily. The major route of elimination is believed to be via biliary excretion while up to 10% of ingested dose is excreted unchanged through the urine.
Tablet core:Microcrystalline CellulosePregelatinised Maize StarchCroscarmellose SodiumMagnesium Stearate
Film coat:HypromellosePovidone K30Titanium Dioxide (E171)Colloidal Anhydrous SilicaMacrogol 400Red Iron oxide (E172)Yellow Iron oxide (E172)
Or trading asSanofi-aventis or SanofiOne Onslow StreetGuildfordSurreyGU1 4YSUnited Kingdom
1 Onslow Street, Guildford, Surrey, GU1 4YS, UK
+44 (0)1483 535 432
+44 (0)1483 505 515
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