Telfast

Telfast

fexofenadine

Manufacturer:

sanofi-aventis

Distributor:

DKSH
Full Prescribing Info
Contents
Fexofenadine HCl.
Description
Each film-coated tablet contains fexofenadine hydrochloride 180 mg.
It also contains microcrystalline cellulose, pre-gelatinized maize starch, croscarmellose sodium, magnesium stearate, hydroxypropyl methylcellulose (E-15), hydroxypropyl methylcellulose (E-5), povidone, titanium dioxide (E171), colloidal anhydrous silica, macrogol 400 and pink iron oxide blend and yellow iron oxide blend as excipients.
Action
Pharmacology: Fexofenadine hydrochloride is a 3rd generation nonsedating H1-antihistamine. Fexofenadine is a pharmacologically active metabolite of terfenadine.
Human histamine wheal and flare studies following single- and twice-daily doses of fexofenadine hydrochloride demonstrate that the drug exhibits an antihistaminic effect beginning within 1 hr, achieving maximum at 6 hrs and lasting up to 24 hrs. There was no evidence of tolerance to these effects after 28 days of dosing.
A positive dose-response relationship between doses of 10-130 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-hr period.
Maximum inhibition in skin wheal and flare areas were >80%.
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 orally) inhibited antigen-induced bronchospasm in sensitized guinea pigs and inhibited histamine release at supratherapeutic concentrations (10-100 mcm) from peritoneal mast cells.
Pharmacokinetics: Fexofenadine hydrochloride is rapidly absorbed into the body following oral administration, with Tmax occurring at approximately 1-3 hrs post-dose, 180 mg dose once daily.
Fexofenadine is 60-70% plasma protein bound. It undergoes negligible metabolism (hepatic or nonhepatic), as it was the only major compound identified in the urine and faeces of man and animals. The plasma concentration profiles of fexofenadine follow a biexponential decline with a terminal elimination half-life ranging from 11-15 hrs after multiple dosing. The single- and multiple-dose pharmacokinetics of fexofenadine are linear for oral doses of up to 120 mg twice daily. A dose of 240 mg twice daily produced slightly greater than proportional increase (8.8%) in steady-state area under the curve, indicating that the fexofenadine pharmacokinetics are practically linear at these doses.
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.
Toxicology: Preclinical Safety Data: The carcinogenic potential of fexofenadine hydrochloride was assessed through studies with terfenadine and supporting pharmacokinetic studies which demonstrated the proper exposure to fexofenadine hydrochloride through the area under the curve (AUC) concentration-plasma values. No evidence of carcinogenicity was observed in rats and mice with terfenadine (up to 150 mg/kg/day), resulting in a plasma exposure to fexofenadine of up to 4 times the therapeutic value in humans (based on fexofenadine hydrochloride 60 mg twice daily). Several in vitro and in vivo studies conducted with fexofenadine hydrochloride did not demonstrate mutagenicity. When fexofenadine hydrochloride was administered as 2000 mg/kg oral doses in acute toxicity studies conducted with several animal species, no clinical signs of toxicity and no effect on bodyweight or food intake were observed. No relevant treatment-related effects were observed in rodents after necropsy. Dogs tolerated 450 mg/kg, administered twice daily, for 6 months and did not exhibit any toxicity other than occasional vomit.
Indications/Uses
For the relief of symptoms associated with chronic idiopathic urticaria and allergic rhinitis in adults and children ≥12 years. Symptoms treated effectively include: Sneezing; rhinorrhea; itchy nose/palate/throat; itchy/watery red eyes.
Dosage/Direction for Use
Adults and Children ≥12 years: 1 tab once daily.
Children ≤12 years: The efficacy and safety of tablet fexofenadine hydrochloride has not been studied.
Special Risk Groups: Elderly, renally or hepatically impaired patients, indicate that it is not necessary to adjust the dose.
Overdosage
Symptoms: Dizziness, drowsiness and dry mouth have been reported with fexofenadine hydrochloride overdosage. Single doses of fexofenadine hydrochloride up to 800 mg (6 healthy subjects at this dose level) and doses up to 690 mg twice daily for 1 month (3 healthy subjects at this dose level) or 240 mg once daily for 1 year (234 healthy subjects at this dose level) were administered without the development of clinically significant adverse events as compared to placebo. No deaths occurred at oral doses of fexofenadine hydrochloride up to 5000 mg/kg in mice (110 times the maximum recommended daily oral dose in adults and children based on mg/m2) and up to 5000 mg/kg in rats (230 times the maximum recommended daily oral dose in adults and 210 times the maximum recommended daily oral dose in children based on mg/m2). Additionally, no clinical signs of toxicity or gross pathological findings were observed. In dogs, no evidence of toxicity was observed at oral doses up to 2000 mg/kg (300 times the maximum recommended daily oral dose in adults and 280 times the maximum recommended daily oral dose in children based on mg/m2).
Treatment: In the event of overdose, consider standard measures to remove any unabsorbed drug. Symptomatic and supportive treatment is recommended. Following administration of terfenadine, hemodialysis did not effectively remove fexofenadine, the major active metabolite of terfenadine, from blood (up to 1.7% removed).
Contraindications
Known hypersensitivity to any of the ingredients of Telfast.
Special Precautions
As with most new drug, there is only limited data in the elderly and renally or hepatically impaired patients. Fexofenadine hydrochloride should be administered with care in these special groups.
Effects on the Ability to Drive or Operate Machinery: On the basis of pharmacodynamic profile and reported adverse events, it is unlikely that fexofenadine hydrochloride will produce an effect on the ability to drive or use machines. In objective tests, Telfast has been shown to have no significant effects on central nervous system function. This means that patients may drive or perform tasks that require concentration. However, in order to identify sensitive people who have unusual reaction to drugs, it is advisable to check the individual response before driving or performing complicated tasks.
Use in pregnancy & lactation: No animal reproduction studies have been performed with fexofenadine hydrochloride. Supportive pharmacokinetic studies with terfenadine have been performed and show exposure to fexofenadine at the high dose level in animal reproduction studies performed with terfenadine to be higher than is achieved at the recommended clinical fexofenadine dose. In these studies, no evidence of teratogenicity or effects on male fertility were observed. Effects on female fertility and on peri- and postnatal development were seen only at maternally toxic doses.
There is no experience with fexofenadine hydrochloride in pregnant women. As with other medications, fexofenadine hydrochloride should not be used during pregnancy unless the expected benefit to the patient outweighs any possible risk to the foetus.
There 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 who are breastfeeding their babies.
Use in children: The efficacy and safety of fexofenadine hydrochloride have not been established in children <2 years for seasonal allergic rhinitis and in children <6 months of age for chronic idiopathic urticaria.
Use In Pregnancy & Lactation
No animal reproduction studies have been performed with fexofenadine hydrochloride. Supportive pharmacokinetic studies with terfenadine have been performed and show exposure to fexofenadine at the high dose level in animal reproduction studies performed with terfenadine to be higher than is achieved at the recommended clinical fexofenadine dose. In these studies, no evidence of teratogenicity or effects on male fertility were observed. Effects on female fertility and on peri- and postnatal development were seen only at maternally toxic doses.
There is no experience with fexofenadine hydrochloride in pregnant women. As with other medications, fexofenadine hydrochloride should not be used during pregnancy unless the expected benefit to the patient outweighs any possible risk to the foetus.
There 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 who are breastfeeding their babies.
Adverse Reactions
In controlled clinical trials, the most commonly reported adverse events were headache, drowsiness, nausea, dizziness and fatigue. The incidence of these events observed with fexofenadine was similar to that observed with placebo.
Dysmenorrhea, back pain, stomach discomfort, diarrhea, rhinorrhea, cough, upper respiratory tract infection, pyrexia and otitis media may also occur.
Drug Interactions
Fexofenadine does not undergo hepatic biotransformation and therefore will not interact with other drugs through hepatic mechanisms. Co-administration of fexofenadine hydrochloride with erythromycin or ketoconazole has been found to result in a 2-3 times increase in the level of fexofenadine in plasma. The changes were not accompanied by any effects on the QT interval and were not associated with any increase in adverse events compared to the drugs given singly.
Animal studies have shown that the increase in plasma levels of fexofenadine observed after co-administration of erythromycin or ketoconazole, appears to be due to an increase in gastrointestinal absorption and either a decrease in biliary excretion or gastrointestinal secretion, respectively.
Administration of an antacid containing aluminium and magnesium hydroxide gels 15 min prior to fexofenadine hydrochloride, caused a reduction in bioavailability most likely due to binding in the gastrointestinal tract. It is advisable to leave 2 hrs between administration of fexofenadine hydrochloride and aluminium- and magnesium hydroxide-containing antacids. Fruit juices eg, grapefruit, orange and apple may redure the bioavailability and exposure of fexofenadine.
Storage
Store below 30°C.
ATC Classification
R06AX26 - fexofenadine ; Belongs to the class of other antihistamines for systemic use.
Presentation/Packing
FC tab 180 mg x 50's.
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