Fexadine, 180 mg 10 pcs

Pharmacodynamics.

Fexophenadine hydrochloride is a blocker of H1-histamine receptors with practically no sedative action. Fexophenadine is the pharmacologically active metabolite of terfenadine.

The antihistamine effect of the drug appears 1 hour after ingestion, reaches its maximum after 6 hours and lasts for 24 hours. After 28 days of use there is no development of tolerance. There is a linear dose-response relationship when oral doses of 10 mg to 130 mg are administered. A dose of 120 mg is sufficient for 24-hour effectiveness of the drug (for allergic rhinitis). In the dose up to 240 mg the drug does not cause changes in the QT interval.

Pharmacokinetics

Fexofenadine hydrochloride is rapidly absorbed from the gastrointestinal tract after oral administration, time to reach maximum concentration (TSmax) is 1-3 hours. The average value of maximum concentration (Cmax) after a dose of 120 mg is 289 ng/ml, and after a dose of 180 mg – about 494 ng/ml. Plasma protein binding is 60-70% (predominantly with albumin and alpha1-glycoprotein). Does not penetrate the blood-brain barrier. Fexofenadine undergoes partial (5% of the dose) metabolism.

The excretion is biphasic. The elimination half-life (T1/2) after repeated administration is 11 to 15 hours. In patients with moderate (creatinine clearance 41-80 ml/min) and severe (11-40 ml/min) renal insufficiency T1/2 is increased by 59 and 72 % accordingly; in patients on hemodialysis T1/2 is increased by 31 %. Pharmacokinetics with single and repeated administration of fexofenadine (up to 120 mg twice a day) is linear.

It is eliminated mainly (80%) in bile, up to 10% of the taken dose is excreted unchanged in the urine.

Indications

Seasonal allergic rhinitis: Sneezing, itching, rhinitis, eye mucosal redness and other symptoms of hay fever – tablets, 120 mg;

Chronic idiopathic urticaria: redness, skin itching and other symptoms of urticaria – tablets, 180 mg.

Active ingredient

Composition

Each film-coated tablet contains:

The active ingredient:

Fexophenadine hydrochloride 120 mg or 180 mg

For 180 mg tablets

Auxiliary ingredients:

Sodium croscarmellose 30.00 mg, microcrystalline cellulose 266.13 mg, gelatinized starch 87.00 mg, colloidal silicon dioxide 21.00 mg, povidone 9.0 mg, magnesium stearate 6.00 mg, purified water* up to 600.00 mg.
Film coating:

Pink opadray pink (OY-54957) – 23.40 mg (hypromellose, titanium dioxide, macrogoal-400, iron oxide red dye (CI №77491), purified water*.
Printing Ink:

Opacode S-1-17823 black – q.s.:
glazed shellac-45% (20% etherified) in ethanol, iron oxide black dye, N-butyl alcohol, propylene glycol, isopropanol, ammonium hydroxide 28%.
(*-evaporated during production).

How to take, the dosage

The tablets are intended for oral administration.

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

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

Interaction

When co-administered with erythromycin or ketoconazole, the plasma concentration of fexofenadine is increased by 2-3 times.

There is no significant effect on QT interval prolongation.

Entake of aluminum- or magnesium-containing antacids 15 min before taking fexofenadine decreases bioavailability of the latter (the time interval between their intake should be at least 2 hours).

It does not interact with omeprazole.

Special Instructions

In elderly patients or patients with hepatic impairment, fexofenadine should be used with caution due to lack of data. It is recommended that the time interval between taking fexofenadine hydrochloride and antacids containing aluminum or magnesium hydroxide should be 2 hours.

Impact on ability to drive and perform work requiring concentration

When taking Fexadine it is possible to perform work requiring high concentration and quick psychomotor reactions (except for people who have unusual reactions to medicines). Thus, before starting to perform these works (driving, operating machinery) it is necessary to check the individual reaction to the drug first.

Contraindications

Hypersensitivity to any of the ingredients of the drug, pregnancy, lactation, children (under 12 years), chronic renal failure.

Side effects

Headache, drowsiness, nausea, dyspepsia, dizziness.

Rarely (less than 1 case per 1000 prescriptions): feeling of fatigue, insomnia, nervousness, sleep disturbance.

In isolated cases: skin rash, urticaria, skin itching, other hypersensitivity reactions: angioedema, shortness of breath.

Overdose

Symptoms: dizziness, drowsiness and dry mouth.

In case of overdose, standard measures to remove the unabsorbed drug from the gastrointestinal tract are recommended.

Symptomatic and supportive therapy is recommended.

Hemodialysis is ineffective.

Pregnancy use

Possible if the expected effect of therapy exceeds the potential risk to the fetus.

Breastfeeding should be stopped during treatment.

Similarities