Fexofenadine Hydrochloride Tablets

Pharmacological action: Fexofenadine hydrochloride is an antihistamine with selective peripheral H1 receptor antagonism. Fexofenadine hydrochloride inhibits the release of histamine from peritoneal mast cells in rats. In experimental animals, no anticholinergic, α1-adrenergic or β-adrenergic receptor blocking effects were observed, nor were sedation or other central nervous system effects observed. This product cannot pass the blood-brain barrier. Toxicological study on QTc effect: Dogs were given fexofenadine hydrochloride orally twice a day at a dose of 30 mg/kg (the original drug concentration in plasma was equivalent to 9 times the maximum recommended adult oral dose), and rabbits were given 10 mg/kg intravenously (the original drug concentration in plasma was equivalent to 20 times the maximum recommended adult oral dose). No significant effect was observed on calcium channel current, delayed potassium channel current, guinea pig muscle cell action potential period, newborn rat muscle cell sodium channel current, and multiple delayed rectifier potassium channels cloned from human heart (the concentration of fexofenadine hydrochloride reached 1×10°M). Genotoxicity: The results of the in vitro bacterial reverse mutation test, CHO/HGPRT forward mutation test, and rat lymphocyte chromosome aberration test of fexofenadine hydrochloride were all negative. The results of the in vivo micronucleus test in mice were negative. Reproductive toxicity: When rats were given fexofenadine hydrochloride at an oral dose of 150 mg/kg (equivalent to 3 times the exposure at the recommended clinical maximum oral dose), a dose-dependent decrease in the number of embryo implantations and an increase in post-implantation loss were observed, and the weight growth and survival rate of the pups decreased in a dose-related manner. No teratogenic effects were observed when rats or rabbits were given fexofenadine hydrochloride at an oral dose of 300 mg/kg (equivalent to 4 times or 31 times the exposure at the recommended clinical maximum oral dose). Carcinogenicity: In studies of mice for 18 months or rats for 24 months, the oral dose of fexofenadine hydrochloride was 150 mg/kg (3 times or 5 times the exposure at the recommended maximum oral dose for adults and children, respectively), and no carcinogenicity was observed.

Fexofenadine hydrochloride. Chemical name: (±)-4[1-hydroxy-4-[4-(hydroxybenzhydryl)-1-piperidinyl]butyl]-α,α-dimethylphenylacetic acid hydrochloride Molecular weight: C32H39NO4?HCl

This product is a film-coated tablet, which appears white or off-white after removing the coating.

No data yet

1. For seasonal allergic rhinitis in adults and children aged 12 years and over, the recommended dose of fexofenadine hydrochloride is 60 mg twice a day, or 180 mg once a day. The recommended starting dose for patients with renal insufficiency is 60 mg once a day. For children aged 6 to 11 years, the recommended dose of fexofenadine hydrochloride is 30 mg twice a day, and the recommended starting dose for children with renal insufficiency is 30 mg once a day. 2. For chronic idiopathic urticaria in adults and children aged 12 years and over, the recommended dose of fexofenadine hydrochloride is 60 mg twice a day. The recommended starting dose for patients with renal insufficiency is 60 mg once a day. For children aged 6 to 11 years, the recommended dose of fexofenadine hydrochloride is 30 mg twice a day. For children with renal insufficiency

1. Seasonal allergic rhinitis In a placebo-controlled clinical trial of seasonal allergic rhinitis, 2461 patients aged 12 years and over were treated with 20 mg to 240 mg of fexofenadine hydrochloride twice a day, and the adverse reactions of fexofenadine hydrochloride were similar to those of placebo. In a placebo-controlled clinical trial of seasonal allergic rhinitis, 570 patients aged 12 years and over were treated with 120 mg or 180 mg of fexofenadine hydrochloride once a day, and the adverse reactions of fexofenadine hydrochloride were similar to those of placebo. The above studies show that the incidence of adverse reactions, including drowsiness, is not dose-related and is similar among various age, gender, and racial groups. Fexofenadine hydrochloride 60 mg, twice daily oral Adverse Reactions with an incidence greater than 1% and greater than placebo Adverse Reactions Fexofenadine hydrochloride 60 mg, placebo, twice daily, twice daily (n=679) (n=671) Viral infections (cold, flu) 2.5% 1.5% Nausea 1.6% 1.5% Dysmenorrhea 1.5% 0.3% Somnolence 1.3% 0.9% Dyspepsia 1.3% 0.6% Fatigue 1.3% 0.9% Once daily Fexofenadine hydrochloride 180 mg oral Adverse Reactions with an incidence greater than 2% Adverse Reactions Fexofenadine hydrochloride 60 mg, placebo, once daily, once daily (n=283) (n=293) Headache 10.6% 7.5% Upper respiratory tract infection 3.2% 3.1% Back pain 2.8% 1.4% The frequency and number of laboratory abnormalities were similar in the fexofenadine hydrochloride and placebo treatment groups. In the placebo-controlled trials of seasonal allergic rhinitis conducted in the United States and Canada, the following adverse reactions occurred in children aged 6 to 11 years: Adverse Reactions Fexofenadine 30 mg Placebo twice daily (n=209) (n=229) Headache 7.2% 6.6% Accidental injury 2.9% 1.3% Cough 3.8% 1.3% Fever 2.4% 0.9% Pain 2.4% 0.4% Otitis media 2.4% 0.0% Upper respiratory tract infection 4.3% 1.7% 2. Chronic idiopathic urticaria Patients aged 12 years and older The incidence of adverse reactions reported in placebo-controlled studies of chronic idiopathic urticaria was similar to that reported in studies of seasonal allergic rhinitis. The placebo-controlled clinical validation of chronic idiopathic urticaria included 726 patients aged 12 years and older who were treated with fexofenadine hydrochloride at doses ranging from 20 mg to 240 mg twice daily. The side effects of fexofenadine hydrochloride were similar to those of placebo. The following table lists the adverse reactions of fexofenadine hydrochloride 60 mg twice daily compared with placebo in the United States and Canada. The adverse reactions that are clinically verified to be generally higher than placebo and with an incidence rate greater than 2% are as follows: Adverse Reactions Fexofenadine hydrochloride 60 mg Placebo twice daily (n=186) (n=178) Back pain 2.2% 1.1% Sinusitis 2.2% 1.1% Dizziness 2.2% 0.6% Somnolence 2.2% 0.0%

It is contraindicated for those who are allergic to the ingredients of this product.

Precautions for children: The safety and efficacy of fexofenadine hydrochloride for children under 6 years of age have not been established. Precautions for pregnancy and lactation: This product does not show obvious teratogenic effects on animals. When rats were given oral doses 3 times the maximum human dose, a dose-related decrease in weight gain and survival rate of pups was observed. However, since there have been no adequate, well-controlled studies on pregnant women, fexofenadine can only be used during pregnancy when the potential benefits far outweigh the risk to the fetus. There have been no adequate, well-controlled studies on lactating women. Because many drugs can be secreted through breast milk, fexofenadine hydrochloride should be used with caution in lactating women. Precautions for the elderly: It is not yet certain whether the response of elderly patients is different from that of young patients. However, since the drug is fully excreted by the kidneys, the risk of drug toxicity in patients with renal impairment may increase. Elderly patients are likely to have decreased renal function, so the dose should be selected with caution and renal function monitoring should be performed if necessary.

1. Drug interactions with erythromycin and ketoconazole Although fexofenadine hydrochloride shows a small liver metabolism rate (5%), it will lead to an increase in the blood concentration of fexofenadine hydrochloride when it interacts with erythromycin and ketoconazole. Fexofenadine hydrochloride has no effect on the pharmacokinetics of erythromycin and ketoconazole. In trials that studied the effects of fexofenadine hydrochloride with erythromycin or ketoconazole, healthy volunteers (n=24 in each study experiment) took fexofenadine hydrochloride 120 mg twice a day (twice the recommended dose twice a day) with erythromycin 500 mg every 8 hours or ketoconazole 400 mg once a day. The results showed that there was no difference in side effects or QTc intervals between patients taking fexofenadine hydrochloride alone or with erythromycin or ketoconazole. The results of these studies

seal.

60mg

24 months

Beijing Foyou Pharma Co., Ltd.

• Founded in:

  1999-02-03

• Address:

  No. 8 Guangyuan East Street, Tongzhou Industrial Development Zone, Tongzhou District, Beijing

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  91110112700216160K

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