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Telfast

Fexofenadine HCI

 

Composition

Each tablet TELFAST 180 mg contains 168 mg of the active ingredient fexofenadine (as 180 mg of fexofenadine
hydrochloride).

Excipients: Mycrocrystalline cellulose, pregelatinised maize starch, croscarmellose sodium, magnesium stearate. hydroxypropyl methylcellulose (E-15), hydroxypropyl methylcellulose (E-5), povidone, titanium dioxide (E 171), colloidal anhydrous silica, macrogol 400 and pink iron oxide, yellow iron oxide blend.

Clinical Pharmacology
Pharmacodynamics


Wheal and Flare: Human histamine skin wheal and flare studies in adults following single and twice daily doses of 20 and 40 mg fexofenadine hydrochloride demonstrated that the drug exhibits an antihistamine effect by I hour, achieves maximum effect at 2 to 3 hours, and an effect is still seen at 12 hours. There was no evidence of tolerance to these effects after 28 days of dosing. The clinical significance of these observations is unknown.

Histamine skin wheal and flare studies in 7 to 12 year old subjects showed that following a single dose of 30 or 60 mg, antihistamine effect was observed at 1 hour and reached a maximum by 3 hours. Greater than 49% inhibition of wheal area, and 74% inhibition of flare area were maintained for 8 hours following the 30 and 60 mg dose.

No statistically significant increase in mean QTc interval compared to placebo was observed in 714 adult subjects with seasonal allergic rhinitis given fexofenadine hydrochloride capsules in doses of 60 to 240 mg twice daily for 2 weeks. Pediatric subjects from 2 placebo-controlled trials (n=855) treated with up to 60 mg fexofenadine hydrochloride twice daily demonstrated no significant treatment- or dose-related increases in QTc. In addition, no statistically significant increase in mean QTc interval compared to placebo was observed in 40 healthy adult subjects given fexofenadine hydrochloride as an oral solution at doses up to 400 mg twice daily for 6 days, or in 230 healthy adult subjects given fexofenadine hydrochloride 240 mg once daily for 1 year. In subjects with chronic idiopathic urticaria, there were no clinically relevant differences for any ECG intervals, including QTc, between those treated with fexofenadine hydrochloride 180 mg once daily (n=163) and those treated with placebo (n=91) for 4 weeks.

Pharmacokinetics

The pharmacokinetics of fexofenadine hydrochloride in subjects with seasonal allergic rhinitis and subjects with chronic urticaria were similar to those in healthy subjects.

Absorption:
TELFAST tablets: Fexofenadine hydrochloride was absorbed following oral administration of a single dose of two 60 mg capsules to healthy male subjects with a mean time to maximum plasma concentration occurring at 2.6 hours post-dose. After administration of a single 60 mg capsule to healthy adult subjects, the mean maximum plasma concentration (Cmax) was 131 ng/mL. Following single dose oral administrations of either the 60 and 180 mg tablet to healthy adult male subjects, mean Cmax were 142 and 494 ng/mL, respectively. The tablet formulations are bioequivalent to the capsule when administered at equal doses.


Fexofenadine hydrochloride pharmacokinetics are linear for oral doses up to a total daily dose of 240 mg (120 mg twice daily). The administration of the 60 mg capsule contents mixed with applesauce did not have a significant effect on the pharmacokinetics of fexofenadine in adults. Co-administration of 180 mg fexofenadine hydrochloride tablet with a high fat meal decreased the mean area under the curve (AUC) and (Cmax) of fexofenadine by 21 and 20% respectively.

Distribution:
Fexofenadine hydrochloride is 60% to 70% bound to plasma-proteins, primarily albumin and α1-acid glycoprotein.

Metabolism:
Approximately 5% of the total dose of fexofenadine hydrochloride was eliminated by hepatic metabolism.

Elimination:
The mean elimination half-life of fexofenadine was 14.4 hours following administration of 60 mg twice daily in healthy adult subjects.


Human mass balance studies documented a recovery of approximately 80% and 11% of the [14C] fexofenadine hydrochloride dose in the feces and urine, respectively. Because the absolute bioavailability of fexofenadine hydrochloride has not been established, it is unknown if the fecal component represents primarily unabsorbed drug or is the result of biliary excretion.

Special Populations:
Pharmacokinetics in renally and hepatically impaired subjects and geriatric subjects, obtained after a single dose of 80 mg fexofenadine hydrochloride, were compared to those from healthy subjects in a separate study of similar design.

Renally Impaired:
In subjects with mild to moderate (creatinine clearance 41-80 mL/min) and severe (creatinine clearance 11-40 mL/min) renal impairment, peak plasma concentrations of fexofenadine were 87% and 111% greater, respectively, and mean elimination half-lives were 59% and 72% longer, respectively, than observed in healthy subjects. Peak plasma concentrations in subjects on dialysis (creatinine clearance ≤10 mL/min) were 82% greater and half-life was 31% longer than observed in healthy subjects. Based on increases in bioavailability and half-life, a dose of 60 mg once daily is recommended as the starting dose in adult patients with decreased renal function. For pediatric patients with decreased renal function, the recommended starting dose of fexofenadine is 30 mg once daily for patients 2 to 11 years of age and 15 mg once daily for patients 6 months to less than 2 years of age [see Dosage and Administration].

Hepatically Impaired:
The pharmacokinetics of fexofenadine hydrochloride in subjects with hepatic impairment did not differ substantially from that observed in healthy subjects.

Geriatric Subjects:
In older subjects (≥65 years old), peak plasma levels of fexofenadine were 99% greater than those observed in younger subjects (<65 years old). Mean fexofenadine elimination halflives were similar to those observed in younger subjects.

Effect of Gender:
Across several trials, no clinically significant gender-related differences were observed in the pharmacokinetics of fexofenadine hydrochloride.

INDICATION
TELFAST 180mg is indicated for the relief of symptoms associated with chronic idiopathic urticaria and allergic rhinitis in adults and children 12 years of age and older. Symptoms treated effectively include sneezing, rhinorrhea, itchy nose/ palate/ throat, itchy/ watery red eyes.

DOSAGE AND ADMINISTRATION
TELFAST tablets
Seasonal Allergic Rhinitis and Chronic Idiopathic Urticaria
Adults and Children 12 Years and Older:
The recommended dose of TELFAST tablets is 180 mg once daily with water. A dose of 60 mg once daily is recommended as the starting dose in patients with decreased renal function [see Clinical Pharmacology].

CONTRAINDICATIONS
TELFAST tablets are contraindicated in patients with known hypersensitivity to fexofenadine and any of the ingredients of TELFAST. Rare cases of hypersensitivity reactions with manifestations such as angioedema, chest tightness, dyspnea flushing and systemic anaphylaxis have been reported.

WARNINGS AND 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.

USE IN SPECIFIC POPULATIONS
Pregnancy

Teratogenic Effects: Pregnancy Category C. There was no evidence of teratogenicity in rats or rabbits at oral doses of terfenadine up to 300 mg/kg (which led to fexofenadine exposures that were approximately 4 and 30 times, respectively, the exposure at the maximum recommended human daily oral dose of 180 mg of fexofenadine hydrochloride based on comparison of AUCs).

In mice, no adverse effects and no teratogenic effects during gestation were observed with fexofenadine hydrochloride at oral doses up to 3730 mg/kg (which led to fexofenadine exposures that were approximately 15 times the exposure at the maximum recommended human daily oral dose of 180 mg of fexofenadine hydrochloride based on comparison of AUCs).

There are no adequate and well controlled studies in pregnant women. Fexofenadine hydrochloride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nonteratogenic Effects: Dose-related decreases in pup weight gain and survival were observed in rats exposed to an oral dose of 150 mg/kg of terfenadine (which led to fexofenadine exposures that were approximately 3 times the exposure at the maximum recommended human daily oral dose of 180 mg of fexofenadine hydrochloride based on comparison of AUCs).

Nursing Mothers
It is not known if fexofenadine is excreted in human milk. There are no adequate and well-controlled studies in women during lactation. Because many drugs are excreted in human milk, caution should be exercised when fexofenadine hydrochloride is administered to a nursing woman.

Geriatric Use
Clinical studies of TELFAST tablets and capsules did not include sufficient numbers of subjects aged 65 years and over to determine whether this population responds differently from younger subjects. Other reported clinical experience has not identified differences in responses between the geriatric and younger subjects. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function (see Clinical Pharmacology.)
 

Renal Impairment
Based on increases in bioavailability and half-life a dose of 60 mg once as the starting dose in adult patients with decreased renal function (mild, moderate or severe renal impairment). For pediatric patients with decreased renal function (mild, moderate or severe renal impairment). For pediatric patients with decreased renal function (mild, moderate or severe renal impairment), the recommended starting dose of fexofenadine is 30 mg once daily for patients 2 to 11 years of age and 15 mg once daily for patients 6 months to less than 2 years of age [See Dosage and Administration and Clinical Pharmacology].

Hepatic Impairment
The pharmacokinetics of fexofenadine hydrochloride in subjects with hepatic impairment did not differ substantially from that observed in healthy subjects.

Effects on ability to drive and use machines
On the basis of the pharmacodynamic profile and reported adverse events it is unlikely that fexofenadine hydrochloride tablets will produce an effect on the ability to drive or use machines. In objective tests. TELFAST 180 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 an unusual reaction to drugs, it is advisable to check the individual response before driving or performing complicated tasks.

ADVERSE REACTIONS
Clinical Studies Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The safety data described below reflect exposure to fexofenadine hydrochloride in 5083 patients in trials for allergic rhinitis and chronic idiopathic urticaria.

 

In these trials, 3010 patients 12 years of age and older with seasonal allergic rhinitis were exposed to fexofenadine hydrochloride at doses of 20 to 240 mg twice daily or 120 to 180 mg once daily.

 

A total of 646 patients 6 to 11 years of age with seasonal allergic rhinitis were exposed to fexofenadine hydrochloride at doses of 15 to 60 mg twice daily. The duration of treatment in these trials was 2 weeks. A total of 534 patients 6 months to 5 years of age with allergic rhinitis were exposed to fexofenadine hydrochloride at doses of 15 to 30 mg twice daily. The duration of treatment in these trials ranged from 1 day to 2 weeks. There were 893 patients 12 years of age and older with chronic idiopathic urticaria exposed to fexofenadine hydrochloride at doses of 20 to 240 mg twice daily or 180 mg once daily. The duration of treatment in these trials was 4 weeks.

Seasonal Allergic Rhinitis
Adults and Adolescents: In placebo-controlled seasonal allergic rhinitis clinical trials in subjects 12 years of age and older, 2439 subjects received fexofenadine hydrochloride capsules at doses of 20 mg to 240 mg twice daily. All adverse reactions that were reported by greater than 1% of subjects who received the recommended daily dose of fexofenadine hydrochloride (60 mg capsules twice daily) are listed in Table 1.

In another placebo-controlled clinical study in the United States, 571 subjects aged 12 years and older received fexofenadine hydrochloride tablets at doses of 120 or 180 mg once daily. Table 1 also lists adverse reactions that were reported by greater than 2% of subjects treated with fexofenadine hydrochloride tablets at doses of 180 mg once daily.

The incidence of adverse reactions, including somnolence/fatigue, was not dose-related and was similar across subgroups defined by age, gender, and race.

 

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