Allegra - instructions for use, dose, side effects, contraindications

composition of the shell: E-15 2.84 mg, hypromellose E-5 1.89 mg, povidone 0.51 mg, titanium dioxide (E 171) 2,025 mg, silicon dioxide colloid 0.73 mg, macrogol-400 3.94 mg, dye iron oxide (pink mixture *) 0.025 mg, iron oxide dye (yellow mixture **) 0.040 mg.

For dosage 180 mg:

active substance: fexofenadine hydrochloride 180.0 mg;

Excipients: croscarmellose sodium 36.0 mg, pregelatinized starch 180.0 mg, microcrystalline cellulose 199.5 mg, magnesium stearate 4.5 mg;

composition of the shell: E-15 4.26 mg, hypromellose E-5 2.835 mg, povidone 0.765 mg, titanium dioxide (E 171) 3,038 mg, silicon dioxide colloid 1,095 mg, macrogol 400 5.91 mg, iron oxide dye (pink mixture *) 0.038 mg, iron oxide dye (yellow mixture **) 0.060 mg.

* - pink mixture of iron oxide dye is a mixture of iron red oxide (E 172) and titanium dioxide (E 171).

** - yellow mixture of iron oxide dye is a mixture of iron oxide of yellow (E 172) and titanium dioxide (E 171).

Description:

For the dosage of 120 mg: oblong, biconvex tablets, covered with a film coating of light pink color, on one side engraving "012", on the other - a stylized" e ".

For a dosage of 180 mg: oblong, biconvex tablets, covered with a film coating of light pink color, on one side engraving "018", on the other - a stylized" e ".

Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.X.26 Fexofenadine

Pharmacodynamics:

Fexofenadine (a pharmacologically active metabolite of terfenadine) is an antihistamine with selective antagonistic activity to H₁-receptors without anticholinergic and blocking alpha 1-adrenergic action receptors. In addition, fexofenadine is not observed sedation and other effects from the central nervous system.

In human studies, the antihistamine effect of fexofenadine ingested once or twice a day in human studies on the assessment of histamine-induced blisters and hyperemia manifests itself after 1 hour, reaches a maximum after 6 hours, and lasts for 24 hours after its administration. Even after 28 days of fexofenadine, there was no development of tolerance to the drug. With a single dose of fexofenadine inside, a dose-related increase in antihistamine effect is observed with an increase in the dose from 10 mg to 130 mg. When using the same model of antihistamine action, it was found that a dose of at least 130 mg was necessary for a constant action for 24 hours. Maximum suppression of blistering and hyperemia of the skin is more than 80%.

In patients with seasonal allergic rhinitis who received up to 240 mg of fexofenadine twice a day for 2 weeks, the duration of the interval QTc (QT corrected) did not differ from that when taking placebo.

Also there were no changes QTc when fexofenadine is taken by healthy volunteers at 60 mg twice a day for 6 months, 400 mg twice a day for 6.5 days and 240 mg per day for 1 year compared to the duration QTc when taking placebo.

Even with plasma concentrations 32 times higher than therapeutic concentrations in humans fexofenadine It had no effect on the potassium channels of delayed rectification in the human heart.

Pharmacokinetics:

Fexofenadine after intake is rapidly absorbed, the time to reach the maximum concentration (T_mOh) is about 1-3 hours. The average value of the maximum concentration (C_mOh) with the intake of 120 mg per day is approximately 289 ng / ml, and with the intake of 180 mg per day - approximately 494 ng / ml.

Fexofenadine binds to plasma proteins by 60-70%.

Fexofenadine is slightly metabolized in the liver and outside it, which is confirmed by the fact that it is the only substance detected in significant quantities in urine and feces of humans and animals.

With the course of taking the drug, the curve of excretion of fexofenadine from plasma decreases bi-expentially, and the final half-life is 11-15 hours.

Pharmacokinetics with a single and course of fexofenadine (up to 120 mg twice a day inwards) is linear. The dose of 240 mg twice daily gives slightly more than the proportional (by 8.8%) increase in the area under the "concentration time" curve, which indicates that the pharmacokinetics of fexofenadine is practically linear in the dosage range of 40 to 240 mg per day .

According to the data available to date, most of the dose taken in unchanged form is excreted with bile, and up to 10% of the drug - with urine.

Indications:

Seasonal allergic rhinitis (to reduce symptoms) - tablets, 120 mg.

Chronic idiopathic urticaria (to reduce symptoms) - tablets, 180 mg.

Contraindications:

- Hypersensitivity to any of the components of the drug;

- Pregnancy;

- lactation period;

- Children's age (up to 12 years).

Carefully:

- In patients with chronic renal and hepatic insufficiency, as well as in elderly patients (lack of clinical experience in this category of patients);

- in patients with cardiovascular diseases, including in the anamnesis (antihistamines can cause palpitations and tachycardia, see the "Side effect" section).

Pregnancy and lactation:

Pregnancy

There is insufficient data on the use of fexofenadine in pregnant women. Limited animal studies showed no evidence of adverse effects on pregnancy, intrauterine development, childbirth and postnatal development.

Fexofenadine should not be used during pregnancy.

Lactation

Data on the content of fexofenadine in breast milk when it is taken by breast-feeding women are not available. However, when taking terfenadine, its penetration into breast milk of lactating women was observed. Therefore, the use of fexofenadine during the period of breastfeeding is not recommended.

Dosing and Administration:

Tablets are intended for oral administration.

The recommended dose of fexofenadine for seasonal allergic rhinitis for adults and children 12 years and older is 120 mg once a day before meals.

The recommended dose of fexofenadine for chronic urticaria for adults and children 12 years and older is 180 mg once a day before meals.

Patients at risk

Studies in special risk groups (elderly patients, patients with renal and hepatic insufficiency) showed that they do not require correction of the dosing regimen.

Side effects:

In placebo-controlled clinical trials, the most frequently (≥1% - ≤10%) the observed undesirable effects were headache (7,3%), drowsiness (2.3%), dizziness (1.5%) and nausea 1.5%. When receiving the above-mentioned fexofenadine frequency of adverse effects was similar to that of placebo.

In a placebo-controlled studies, with a frequency of less than 1% (when receiving equally fexofenadine and placebo) and post-marketing drug application were fatigue, insomnia, anxiety and sleep disorders or abnormal dreams (paroniriya) such as nightmares; tachycardia, palpitations; diarrhea.

In rare cases (≥0,01% - ≤0,1%) observed exanthema, urticaria, pruritus and other hypersensitivity reactions such as angioedema, difficulty breathing, dyspnea, flushing of the skin, systemic anaphylactic reaction.

Overdose:

Symptoms

In case of an overdose, dizziness, drowsiness and dry mouth were observed.Healthy volunteers were given single doses up to 800 mg and exchange doses up to 690 mg twice a day for 1 month or 240 mg twice a day for 1 year without any significant undesirable effects compared with placebo. The maximum tolerated dose for fexofenadine is not established.

Treatment

In case of an overdose, it is recommended to perform gastric lavage, taking activated charcoal, symptomatic and supportive therapy if necessary. Hemodialysis is ineffective.

Interaction:

With the combined use of fexofenadine with erythromycin or ketoconazole, the concentration of fexofenadine in plasma increases by 2-3 times, but this is not associated with a significant lengthening of the interval QTc. There were no significant differences in the incidence of adverse effects in the use of these drugs in monotherapy and in combination. Animal studies have shown that the above increase in plasma concentrations of fexofenadine is probably associated with an improvement in fexofenadine absorption and a decrease in its biliary excretion or secretion into the lumen of the gastrointestinal tract.

There is no interaction between fexofenadine and omeprazole.

Does not interact with drugs metabolized in the liver.

Taking antacids containing aluminum or magnesium 15 minutes before taking fexofenadine leads to a decrease in the bioavailability of the latter as a result of, apparently, binding in the gastrointestinal tract.

Special instructions:

It is recommended that the time interval between taking fexofenadine and antacids containing aluminum or magnesium hydroxide is at least 2 hours.

For use in children from 6 to 11 years, 30 mg tablets are produced.

Effect on the ability to drive transp. cf. and fur:

When taking the drug, it is possible to perform work that requires a high concentration of attention and speed of psychomotor reactions (with the exception of patients who have an unconventional reaction). Therefore, it is recommended to check the individual response to fexofenadine before taking these activities.

Form release / dosage:

Tablets, film-coated, 120 mg and 180 mg.

Packaging:

For 10 tablets in a blister of PVC / aluminum foil.

One blister along with the instructions for use are placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

After the expiration date, the drug can not be used.

Terms of leave from pharmacies:Without recipe

Registration number:П N016292 / 01

Date of registration:13.04.2010 / 28.03.2017

Expiration Date:Unlimited

The owner of the registration certificate:Sanofi-Aventis Deutschland GmbHSanofi-Aventis Deutschland GmbH Germany

Manufacturer: & nbsp

SANOFI WINTHROP INDUSTRIE France

Representation: & nbspSanofi Aventis GroupSanofi Aventis Group

Information update date: & nbsp08.07.2017

Illustrated instructions

Instructions

Allegra (Allegra)