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Fexofenadine Hydrochloride Capsules

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Indications: 1. Seasonal allergic rhinitis is suitable for alleviating the symptoms associated with seasonal allergic rhinitis in adults and children 6 years and older. Such as sneezing, runny nose, itchy nose, epicondylitis, throat, itchy, wet, reddened eyes. 2. Chronic idiopathic urticaria is suitable for treating skin symptoms of chronic idiopathic urticaria in adults and children aged 6 years and over, and can reduce the number of itching and wind masses.

Approval date: June 05, 2006

Please read the instructions carefully and use under the guidance of a physician

【Drug Name】

Common name: Fexofenadine Hydrochloride Capsules

English name: Fexofenadine Hydrochloride Capsules

Phonetic script: Hansuan Feisuofeinading Jiaonang

[Ingredients]

The main ingredient of this product is fexofenadine hydrochloride.
Chemical name: a, a-dimethyl-4- [1-hydroxy-4- [4- (hydroxydiphenylmethyl) -1-piperidinyl] butyl] -phenylacetic acid hydrochloride.
Molecular formula: C 32 H 39 NO 4 · HCl
Molecular weight: 538.13

[Properties] This product is a capsule, the contents are white or off-white particles and powder.

[Specifications] 60mg

【Dosage】

Seasonal allergic rhinitis

The recommended dose of fexofenadine hydrochloride for adults, children 12 years of age and older is 60 mg (1 capsule) twice daily, or 180 mg (3 capsules) once daily. The recommended starting dose for patients with renal insufficiency is 60 mg (1 capsule) once a day.

For children 6 to 11 years old, the recommended dose of fexofenadine hydrochloride is 30 mg (half capsule) twice a day. The recommended starting dose for children with renal insufficiency is 30 mg (half capsule) once a day.

2. Chronic idiopathic urticaria

The recommended dose of fexofenadine hydrochloride for adults, children 12 years of age and older is 60 mg (1 capsule) twice daily. The recommended starting dose for patients with renal insufficiency is 60 mg once daily.

For children 6 to 11 years old, the recommended dose of fexofenadine hydrochloride is 30 mg (half capsule) once a day, twice a day. The recommended starting dose for children with renal insufficiency is 30 mg (half-grain) once a day.

【Adverse reactions】

1.Seasonal allergic rhinitis

In a placebo-controlled seasonal allergic rhinitis clinical trial, 2,461 patients aged 12 years and older received fexofenadine hydrochloride 20 mg to 240 mg twice daily, and fexofenadine hydrochloride was poorly treated with placebo. The response is similar.

In a placebo-controlled seasonal allergic rhinitis clinical trial, 570 patients aged 12 years and older received fexofenadine hydrochloride 120 mg or 180 mg once a day. Fexofenadine hydrochloride had similar adverse effects to placebo .

The above studies show that the incidence of adverse reactions, including sleepiness, is not dose-related and is similar across age, gender, and ethnic groups.

The frequency and number of laboratory abnormalities were similar in the fexofenadine hydrochloride and placebo-treated groups.

In the placebo-controlled trials of seasonal allergic rhinitis in the United States and Canada, adverse reactions in children aged 6 to 11 years were as follows:

Chronic idiopathic urticaria
The incidence of side effects reported by patients with 12 years of age and older in the placebo-controlled chronic idiopathic urticaria study was similar to that reported by the seasonal allergic rhinitis study.

Clinical validation of placebo-controlled chronic idiopathic urticaria, including 726 patients aged 12 years and older receiving fexofenadine hydrochloride at a dose of 20 mg to 240 mg twice daily. Side effects of fexofenadine hydrochloride and The placebo is similar. The following table lists the side effects of fexofenadine hydrochloride 60 mg twice daily in the United States and Canada compared with placebo.

[Taboo]

Those who are allergic to the ingredients of this product are prohibited.

【Precautions】

    still uncertain.

[Medication for pregnant and lactating women]

This product does not show obvious teratogenic effects in animals. A dose-related decrease in weight gain and survival in pups was observed when rats were administered orally to humans at 3 times the maximum dose.

Because adequate, well-controlled studies have not been conducted on pregnant women, fexofenadine should be used during pregnancy only if the potential benefits far outweigh the harm to the fetus.

There are no adequate, well-controlled studies of lactating women. Because many drugs can be secreted through breast milk, lactating women should be used with caution with fexofenadine hydrochloride.

[Child medication]

The safety and efficacy of fexofenadine hydrochloride in children under 6 years of age have not been established.

[Medicine for the elderly]

It has not been determined whether there is a difference in the response between elderly patients and young patients. However, because the drug is fully excreted by the kidney, the risk of drug toxicity in patients with renal impairment may increase. Elderly patients are likely to have a decline in renal function, so the choice of dosage must be careful, and renal function monitoring needs to be performed if necessary.

【medicine interactions】

1. Drug interactions with erythromycin and ketoconazole Although fexofenadine hydrochloride shows a small liver metabolic rate (about 5%), it can cause Increased plasma concentration of fexofenadine hydrochloride. Fexofenadine hydrochloride has no effect on the pharmacokinetics of erythromycin and ketoconazole.

In trials to study the compatibility of fexofenadine hydrochloride with erythromycin or ketoconazole, healthy volunteers (n = 24 in each research experiment) took fexofenadine hydrochloride 120 mg twice a day (yes Twice the recommended dose twice a day) with erythromycin 500mg every 8 hours or ketoconazole 400mg once daily, the results show that patients take fexofenadine hydrochloride alone or with erythromycin and ketoconazole There were no differences in side effects or QTc intervals. The results of these studies are summarized in the following table:

Effect of 120 mg of fexofenadine hydrochloride every 12 hours (twice the recommended daily dose) and the following drugs on the pharmacokinetics of stable fexofenadine hydrochloride after simultaneous administration for 7 days (n = 24)

Changes in plasma concentration levels are within a sufficient and well-controlled range of clinically validated plasma concentrations.

The mechanisms of these interactions have been validated by adequate in situ and in vivo and in vitro animal models. Studies show that co-administration of ketoconazole or erythromycin with fexofenadine hydrochloride can promote gastrointestinal absorption of fexonadine hydrochloride. In vivo animal studies have also shown that not only can it promote absorption, ketoconazole can also reduce the gastrointestinal secretion of fexofenadine hydrochloride, and erythromycin may also reduce its biliary secretion.

2. Drug interactions with antacids. Taking 120 mg fexofenadine hydrochloride (2 × 60 mg) with aluminum and magnesium antacids within 15 minutes will reduce the AUC and Cmax of fexofenadine hydrochloride by 41% 43%. Therefore, fexofenadine hydrochloride and aluminum and magnesium antacids should not be taken at the same time.

[Drug overdose]

Reports of overdose of fexofenadine hydrochloride are rare and little information is available. However, dizziness, lethargy and dry mouth have been reported. Single dose of fexofenadine hydrochloride 800 mg (six healthy volunteers at this dose level), 690 mg twice daily for one month (three healthy volunteers at this dose level) or 240 mg once daily One year (234 healthy volunteers at this dose level) had no clinically significant adverse events compared to placebo.

In the case of overdose, standard measures should be considered to remove unabsorbed drugs. Symptomatic treatment and supportive treatments are recommended.

The data show that after taking terfenadine, hemodialysis therapy cannot effectively remove fexofenadine hydrochloride from the blood (only 1.7% was removed).

[Pharmacology and Toxicology]

Pharmacological effects: Fexofenadine hydrochloride is an antihistamine drug with selective peripheral H1 receptor antagonism. Fexofenadine inhibits histamine release from peritoneal mast cells in rats. In experimental animals, no anticholinergic, α1-adrenergic or β-adrenergic receptor blocking effects were observed, and no sedation or other central nervous system effects were observed. This product cannot cross the blood-brain barrier.

Toxicology study: Effect on QTc: dogs take fexofenadine hydrochloride twice a day at a dose of 30㎎ / ㎏ (the plasma drug concentration is equivalent to 9 times the recommended maximum oral dose for adults), and rabbits are injected intravenously with 10mg / kg (concentration in plasma equivalent to 20 times the recommended maximum oral dose for adults), no increase in QTc occurred for 1 hour after administration. For calcium channel flow, delayed potassium channel flow, guinea pig muscle cell action potential cycle, newborn rat muscle cell sodium channel flow, multiple delayed rectifying potassium channels of human heart clones (fexofenadine hydrochloride concentration reaches 1 × 10 5 M).

Genotoxicity: Fexofenadine hydrochloride in vitro bacterial reverse mutation test, CHO / HGPRT forward mutation test, rat lymphocyte chromosome aberration test results were negative. Micronucleus test results in mice were negative.

Reproductive toxicity: 150 mg / kg of fexofenadine hydrochloride taken orally in rats (equivalent to 3 times the maximum clinical exposure at the recommended clinical oral dose). A dose-dependent decrease in the number of embryo implantations and an increase in post-implantation loss were observed. The increase in litter weight and survival decreased in a dose-related manner. No teratogenic effect was observed in rats or rabbits given fexofenadine hydrochloride by oral administration of 300 mg / kg (equivalent to 4 or 31 times the recommended maximum clinical exposure).

Carcinogenicity: In studies of 18 months in mice and 24 months in rats, the dose of oral fexofenadine hydrochloride was 150 mg / kg (three or five times the recommended maximum oral dose for adults and children, respectively). ), No carcinogenicity was observed.

【Pharmacokinetics】

Studies abroad have shown:

Absorption: Fexofenadine hydrochloride is rapidly absorbed. Healthy male volunteers take 120 mg of fexofenadine hydrochloride in a single dose, and the average peak blood concentration time is 2.6 hours. The maximum plasma concentration of fexofenadine hydrochloride was 131ng / ml when healthy volunteers took a single dose of 60mg. Results from other similar studies were similar. Healthy adult male volunteers took a single oral 60 or 180 mg tablet with average maximum plasma concentrations of 142 and 494 ng / ml, respectively. Fexofenadine hydrochloride has a linear pharmacokinetics when the daily oral dose is within 240 mg (120 mg, twice a day).

Distribution: The binding rate of fexofenadine hydrochloride to plasma proteins is 60% to 70%. The main plasma binding proteins are albumin and α1-acid glycoprotein.

Elimination: After taking healthy volunteers 60mg twice a day, the elimination half-life of fexofenadine is 14.4 hours. Human mass balance studies have shown that approximately 80% and 11% of [14C] -fexofenadine hydrochloride are recovered in feces and urine, respectively. Since the absolute bioavailability of fexofenadine hydrochloride has not been established, it is currently unknown whether the fexofenadine hydrochloride component in feces is an unabsorbed drug or is derived from bile duct excretion.

Metabolism: About 5% of the total dose is metabolized.

Special population:

Geriatric subjects Among elderly subjects (≥ 65 years of age), the highest plasma levels of fexofenadine were 99% higher than normal subjects (<65 years of age). The mean elimination half-life was similar to healthy subjects.

Pediatric Patients In a study of allergic rhinitis patients and healthy adult subjects aged 7 to 12 years, 60 mg of this product was taken orally. The area under the curve (AUC) of the child subjects was lower than that of healthy adult subjects who received the same dose. 56% bigger. In contrast, plasma concentrations of 30 mg of fexofenadine hydrochloride in children were similar to those of 60 mg of adults.

Renal injury. The highest plasma levels of fexofenadine in patients with mild to moderate (creatinine clearance 41 to 80 ml / min) and severe (creatinine clearance 11 to 40 ml / min). Increased by 87% and 111%, respectively, and the average elimination half-life extended by 59% and 72%, respectively. In dialysis patients (creatinine clearance ≤10ml / min), the highest plasma level increased by 82%, and the half-life increased by 31%. Based on the increase in bioavailability and half-life, a daily dose of 60 mg is recommended as the starting dose for patients with reduced renal function. (See Dosage and Administration)

Pharmacokinetics of liver injury fexofenadine in patients with liver disease is similar to healthy subjects.

[Storage] Sealed and stored in a dry place at room temperature (10 ~ 30 ℃).

[Packaging] Aluminum plastic packaging, 10 tablets / board, 1 board / box.

[Validity] Tentatively 24 months

[Executive Standard] YBH13632006

[Approval number] National Medicine Standard H20060995

【manufacturer】