Telfast 120mg 10 pcs film-coated tablets

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Fexofenadine is an antihistamine with selective activity towards H1 receptors and does not have anticholinergic or α1-adrenergic blocking effects. Also, fexofenadine does not demonstrate sedation or other effects on nervous activity.

The antihistamine effect is detected within 60 minutes, reaches its greatest strength after 6 hours and lasts for 1 day after administration. Tolerance to the drug does not develop. The effect of fexofenadine when taken orally is dose-dependent.

Pharmacokinetics

When taken orally, it is rapidly absorbed, the maximum content is reached in approximately 2–3 hours. Reacts 65–70% with plasma proteins.

Poorly metabolized in the liver and some other tissues. The half-life is 12–14 hours. Pharmacokinetics is linear.

According to currently available data, most of the drug is excreted unchanged in the bile and approximately 10% in the urine.

Telfast 180 mg tablet p/o No. 10

Dosage

180 mg

Active substance

Fexofenadine

Manufacturer

Sanofi-Aventis USA LLC (USA)

Shelf life

3 years

Storage conditions

At a temperature not exceeding 25 °C

Registration certificate number

P N016292/01 dated 11/29/2013

Compound

Characteristic

Description of the dosage form

120 mg tablets:

oblong, biconvex tablets, light pink film-coated, engraved “012” on one side and a stylized “e” on the other.

180 mg tablets:

oblong, biconvex tablets, light pink film-coated, engraved “018” on one side and a stylized “e” on the other.

Pharmacokinetics

When taken orally, it is rapidly absorbed, Tmax is approximately 1-3 hours. The average Cmax value when taking 120 mg/day is approximately 289 ng/ml, and when taking 180 mg/day is approximately 494 ng/ml.

Fexofenadine is 60–70% bound to plasma proteins.

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

With a course of taking the drug, the elimination curve of fexofenadine from plasma decreases biexponentially, and the final T1/2 is 11–15 hours.

Pharmacokinetics with single and course administration of fexofenadine (up to 120 mg twice a day orally) is linear. A dose of 240 mg twice daily produced a slightly greater than proportional (8.8%) increase in AUC, indicating that the pharmacokinetics of fexofenadine are essentially linear over the dose range from 40 to 240 mg/day.

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

Pharmacodynamics

Fexofenadine (a pharmacologically active metabolite of terfenadine) is an antihistamine with selective H1 receptor antagonistic activity without anticholinergic and α1-adrenergic receptor blocking effects. In addition, fexofenadine does not have sedative effects or other central nervous system effects.

In human studies assessing histamine-induced wheals and flushing, the antihistamine effect of fexofenadine taken orally once or twice daily appears within 1 hour, peaks at 6 hours, and continues for 24 hours after dosing. Even after 28 days of taking fexofenadine, no development of tolerance to the drug was detected. With a single oral dose of fexofenadine, a dose-dependent increase in the antihistamine effect is observed when the dose is increased from 10 to 130 mg. Using the same model of antihistamine action, it was found that a dose of at least 130 mg was required for continuous action over 24 hours. The maximum suppression of blistering and skin hyperemia is more than 80%.

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

There were also no changes in the QTc interval when healthy volunteers took fexofenadine 60 mg 2 times a day for 6 months, 400 mg 2 times a day for 6.5 days and 240 mg/day for 1 year compared with the interval QTc when taking placebo.

Even at plasma concentrations 32 times higher than therapeutic concentrations in humans, fexofenadine had no effect on delayed rectifier potassium channels in the human heart.

Contraindications

hypersensitivity to any of the components of the drug;

pregnancy;

breastfeeding period;

children's age up to 12 years.

Carefully:

chronic renal and liver failure, as well as elderly patients (lack of clinical experience in this category of patients); cardiovascular diseases, incl. and history (antihistamines can cause palpitations and tachycardia, see “Side effects”).

Use during pregnancy and breastfeeding

There is insufficient data on the use of fexofenadine in pregnant women. Limited studies in animals have shown no evidence of adverse effects on pregnancy, fetal development, childbirth or postnatal development. Fexofenadine should not be used during pregnancy.

There are no data on the content of fexofenadine in breast milk when taken by breastfeeding women. However, when taking terfenadine, it was observed to penetrate into the breast milk of lactating women. Therefore, the use of fexofenadine during breastfeeding is not recommended.

Directions for use and doses

Inside,

before eating.

Seasonal allergic rhinitis:

The recommended dose for adults and children 12 years of age and older is 120 mg once a day.

Chronic idiopathic urticaria:

The recommended dose for adults and children 12 years of age and older is 180 mg once a day.

Patients at risk.

Studies in special risk groups (elderly patients, with renal and hepatic insufficiency) have shown that for patients in these categories no dosage adjustment is required.

Side effects

In placebo-controlled clinical trials, the most commonly (≥1 to <10%) observed adverse effects were headache (7.3%), somnolence (2.3%), dizziness (1.5%), and nausea (1.5%). %). The incidence of the above adverse effects with fexofenadine was similar to that with placebo.

In placebo-controlled studies with a frequency of less than 1% (the same when taking fexofenadine and placebo) and during post-marketing use of the drug, weakness, insomnia, and nervousness were noted; sleep disturbances or unusual dreams (paronyria), such as nightmares; tachycardia, palpitations; diarrhea.

In rare cases (≥0.01 - <0.1%), exanthema, urticaria, itching and other hypersensitivity reactions, such as Quincke's edema, difficulty breathing, shortness of breath, skin hyperemia, systemic anaphylactic reactions, were observed.

Interaction

When fexofenadine is co-administered with erythromycin or ketoconazole, the plasma concentration of fexofenadine increases 2-3 times, but this is not associated with a significant prolongation of the QTc interval. There were no significant differences in the incidence of adverse effects when using these drugs in monotherapy and in combination. Animal studies have shown that the above-mentioned increase in plasma concentrations of fexofenadine is likely due to improved absorption of fexofenadine and a decrease in its biliary excretion or secretion into the GI lumen.

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, apparently, of binding in the gastrointestinal tract.

Overdose

Symptoms:

dizziness, drowsiness, dry mouth. Healthy volunteers took single doses of up to 800 mg and course doses of up to 690 mg twice daily for 1 month or 240 mg twice daily for 1 year without any significant adverse effects compared to placebo. The maximum tolerated dose for fexofenadine has not been established.

Treatment:

gastric lavage, administration of activated carbon, and, if necessary, symptomatic and supportive therapy. Hemodialysis is ineffective.

special instructions

It is recommended that a minimum of 2 hours be allowed between taking fexofenadine and antacids containing aluminum or magnesium hydroxide.

Effect on the ability to drive a car and perform work requiring concentration.

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 a non-standard reaction). It is therefore recommended to check your individual response to fexofenadine before engaging in such activities.

Conditions for dispensing from pharmacies

Over the counter.

Pharmgroups

Antiallergic agent - H1-histamine receptor blocker (H1-antihistamines)

Pharmaceutical actions

antihistamine

Side effects

The most common symptoms are: drowsiness , headache , insomnia , palpitations, dizziness, nausea, weakness, nervousness , tachycardia , unusual dreams, diarrhea .

In rare cases urticaria , difficulty breathing, exanthema , itching, Quincke's edema , shortness of breath, skin flushing, anaphylactic reactions .

Telfast tablets, instructions for use (Method and dosage)

The tablets are taken orally, before meals.

Instructions for use Telfast 120

When treating allergic seasonal rhinitis , persons 12 years of age and older are prescribed to take 120 mg of medication once a day.

Instructions for use Telfast 180

In the treatment of idiopathic chronic urticaria , persons 12 years of age and older are prescribed to take 1 tablet of the drug Telfast 180 1 time per day.

In elderly patients, as well as those suffering from kidney or liver failure, dosage adjustment of the drug is not required.

Special instructions for the use of the drug Telfast

There is no data on the safety of fexofenadine hydrochloride during pregnancy, so it should be prescribed only when the expected therapeutic effect for the expectant mother outweighs the potential risk to the fetus. If it is necessary to use Telfast during breastfeeding, the issue of stopping breastfeeding should be decided, since fexofenadine hydrochloride passes into breast milk. Based on the pharmacodynamic profile and known side effects, it can be assumed that the effect of taking fexofenadine hydrochloride on the ability to drive vehicles and perform tasks requiring concentration is unlikely. When conducting objective tests, it was revealed that Telfast does not have a significant effect on the functions of the central nervous system. However, it is recommended to evaluate your individual response to the drug before driving or performing other demanding activities.

Analogues of Telfast

Level 4 ATC code matches: Dezal
Gistafen

Clarisens

Erius

Claridol

Claritin

Loratadine

Fexofast

Peritol

Desloratadine

LauraHEXAL

Clarotadine

Rupafin

Ciel

Dramamine

Lordestin

Lomilan

Fenkarol

Kestin

Loratek

The most accessible analogues of Telfast are listed below: Allerfex, Fexo, Allegra, Beksist-sanovel, Fexadin, Dinox, Gifast, Rapido, Telfadin, Fexofast.