Telfast OD/Telfast HD

Telfast OD/Telfast HD

fexofenadine

Manufacturer:

PT. Aventis Pharma
Full Prescribing Info
Contents
Fexofenadine HCl.
Description
Each Telfast OD and Telfast HD tablet contains fexofenadine 112 and 168 mg equivalent to fexofenadine HCl 120 and 180 mg, respectively.
Excipients/Inactive Ingredients: Microcrystalline cellulose, pregelatinised maize starch, croscarmellose sodium, magnesium stearate, hypromellose, povidone, titanium dioxide (E171), colloidal anhydrous silica, macrogol 400 and iron oxide (E172).
Action
Pharmacology: Fexofenadine HCl is a 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 HCl demonstrate that the drug exhibits an antihistaminic effect beginning within 1 hr, achieving maximum at 6 hrs and lasting 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 of skin wheal and flare areas were >80%.
Clinical studies conducted in allergic rhinitis have shown that a dose of 120 mg is sufficient for 24 hrs efficacy.
No significant differences in QTc intervals were observed in seasonal allergic rhinitis patients given fexofenadine HCl 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 HCl 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 HCl (5-10 mg/kg orally) inhibited antigen-induced bronchospasm in sensitised guinea pigs and inhibited histamine release at supratherapeutic concentrations (10-100 micromoles) from peritoneal mast cells.
Pharmacokinetics: Fexofenadine HCl is rapidly absorbed into the body following oral administration, with Tmax occurring at approximately 1-3 hrs post-dose. The mean Cmax value was approximately 427 and 494 ng/mL following the administration of a 120-mg (Telfast OD) and 180-mg (Telfast HD) dose once daily, respectively.
Fexofenadine is 60-70% plasma protein-bound. Fexofenadine 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 11-15 hrs after multiple-dosing. The single- and multiple-dose pharmacokinetics of fexofenadine are linear for oral doses 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 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: Dogs tolerated 450 mg/kg administered twice daily for 6 months and showed no toxicity other than occasional emesis. Also, in single-dose dog and rodent studies, no treatment-related gross findings were observed following necropsy.
Radiolabelled fexofenadine HCl in tissue-distribution studies of the rat indicated that fexofenadine did not cross the blood-brain barrier.
Fexofenadine HCl was found to be non-mutagenic in various in vitro and in vivo mutagenicity tests.
The carcinogenic potential of fexofenadine HCl was assessed using terfenadine studies with supporting pharmacokinetic studies showing fexofenadine HCl exposure (via plasma AUC values). No evidence of carcinogenicity was observed in rats and mice given terfenadine (up to 150 mg/kg/day).
Indications/Uses
Telfast OD: Relief of symptoms associated with allergic rhinitis in adults and children ≥12 years.
Telfast HD: Relief of symptoms associated with chronic idiopathic urticaria in adults and children ≥12 years.
Dosage/Direction for Use
Adults and Children ≥12 years: Recommended Dose: 1 tab once daily.
Children <12 years: The efficacy and safety of fexofenadine HCl has not been studied in children <12 years.
Special Risk Groups: Studies in special risk groups (elderly, renally or hepatically impaired patients) indicate that it is not necessary to adjust the dose of fexofenadine HCl in these patients.
Overdosage
There has been no reported case of an acute overdose of fexofenadine HCl. Standard measures should be considered to remove any unabsorbed drug. Haemodialysis does not effectively remove fexofenadine HCl from blood.
Contraindications
Patients with known hypersensitivity to any ingredient of Telfast OD/HD.
Special Precautions
As with most new drugs, there is only limited data in the elderly and renally or hepatically impaired patients. Fexofenadine HCl should be administered with care in these special groups.
Effects on the Ability to Drive or Operate Machinery: On the basis of the pharmacodynamic profile and reported adverse events, it is unlikely that fexofenadine HCl tablets will produce an effect on the ability to drive or use machines. In objective tests, Telfast OD/HD has been shown to have no significant effects on the 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 an 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 HCl. 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 HCl in pregnant women. As with other medications, fexofenadine HCl 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 HCl. However, when terfenadine was administered to nursing mothers, fexofenadine was found to cross into human breast milk. Therefore, fexofenadine HCl is not recommended for mothers breastfeeding their babies.
Use in Children: Safety and effectiveness of Telfast OD/HD in pediatric patients <12 years have not been established.
Telfast BD: Across well-controlled clinical trials in patients with allergic rhinitis, a total of 205 patients between 12-16 years, received doses ranging from 20-240 mg twice daily for up to 2 weeks. Adverse events were similar in this group compared to patients >16 years.
Use in Elderly: In placebo-controlled trials, 42 patients, 60-68 years, received doses of 20-240 mg of fexofenadine twice daily for up to 2 weeks. Adverse events were similar in this group to patients <60 years.
Use In Pregnancy & Lactation
No animal reproduction studies have been performed with fexofenadine HCl. 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 HCl in pregnant women. As with other medications, fexofenadine HCl 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 HCl. However, when terfenadine was administered to nursing mothers, fexofenadine was found to cross into human breast milk. Therefore, fexofenadine HCl is not recommended for mothers 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.
Drug Interactions
Fexofenadine does not undergo hepatic biotransformation and therefore will not interact with other drugs through hepatic mechanisms. Co-administration of fexofenadine HCl 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 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.
No interaction between fexofenadine and omeprazole was observed. However, the administration of an antacid containing aluminium and magnesium hydroxide gels 15 min prior to fexofenadine HCl 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 HCl and aluminium- and magnesium hydroxide-containing antacids.
Storage
Store at temperature below 30°C.
ATC Classification
R06AX26 - fexofenadine ; Belongs to the class of other antihistamines for systemic use.
Presentation/Packing
Telfast OD: Film-coated tab 120 mg x 10 x 10's.
Telfast HD: Film-coated tab 180 mg x 10's.
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