INSTRUCTIONS

for medical use of the medicinal product

TIGOFAST-120

TIGOFAST-180

 

 

 

Composition:

active substance: fexofenadine hydrochloride;

1 film-coated tablet contains fexofenadine hydrochloride 120 mg or 180 mg;

excipients:

120 mg tablets: microcrystalline cellulose, corn starch, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, film coating Insta Coat White (ethylcellulose, hydroxypropyl methylcellulose, titanium dioxide (E 171)), talc;

180 mg tablets: microcrystalline cellulose, corn starch, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, film coating Insta Coat Sunset Yellow (ethylcellulose, hydroxypropyl methylcellulose, Sunset Yellow FCF (E 110)), talc.

 

Pharmaceutical form. Film-coated tablets.

Basic physicochemical properties:

120 mg tablets: film-coated tablets, round, biconvex, white or almost white in colour;

180 mg tablets: film-coated tablets, round, biconvex, orange in colour.

 

Pharmacotherapeutic group. Antihistamines for systemic use. ATC code R06AX26.

 

Pharmacological properties.

Pharmacodynamics.

Fexofenadine hydrochloride is a non-sedating antihistamine belonging to the group of specific H₁ receptor antagonists. Fexofenadine is the pharmacologically active metabolite of terfenadine. It stabilizes mast cell membranes, preventing histamine release. It eliminates allergy symptoms: sneezing, rhinorrhea, itching, redness of eyes, and lacrimation. It does not have a sedative effect.

The antihistamine effect of fexofenadine hydrochloride, administered once or twice daily, manifested within 1 hour, reached maximum after 6 hours, and lasted for 24 hours. No signs of tolerance development were detected even after 28 days of administration. Clinical effect was observed after single oral doses from 10 to 130 mg. A dose of 120 mg is sufficient to ensure 24-hour effectiveness.

Even at plasma concentrations 32 times higher than therapeutic concentrations, fexofenadine showed no effect on slow potassium channels of the human heart.

Fexofenadine hydrochloride (5-10 mg/kg orally) relieves bronchospasm of antigenic origin in sensitized animals and at concentrations above therapeutic (10-100 micromol) causes histamine release from peritoneal mast cells.

Pharmacokinetics.

Fexofenadine hydrochloride is rapidly absorbed after oral administration. Maximum concentration is reached approximately after 1-3 hours. At a daily dose of 120 mg, the mean maximum concentration is ≈ 427 ng/ml. At a daily dose of 180 mg, the mean maximum concentration is ≈ 494 ng/ml.

60-70% of fexofenadine binds to plasma proteins. The active substance does not penetrate the blood-brain barrier.

Fexofenadine is almost not metabolized (either in the liver or extrahepatically): only fexofenadine was detected in significant quantities in the urine and feces of humans and animals.

Elimination of fexofenadine from plasma occurs with biexponential decline and a terminal half-life of 11 to 15 hours after repeated administration. The kinetics of single and multiple doses is linear at oral doses up to 120 mg twice daily. At saturation stage, doses up to 240 mg twice daily caused an increase in AUC that was somewhat more than proportional (8.8%). This indicates that at daily doses of 40-240 mg, the pharmacokinetics of fexofenadine is almost linear.

Most of the dose is excreted in bile; up to 10% is excreted unchanged in urine.

Mutagenic and carcinogenic properties.

Various mutagenicity tests in vitro and in vivo did not reveal mutagenic properties of fexofenadine hydrochloride.

In a carcinogenicity study, fexofenadine exposure was determined (by plasma AUC indices) after terfenadine administration in secondary pharmacokinetic studies. When terfenadine was administered to rats and mice (up to 150 mg/kg body weight per day), no signs of carcinogenicity were detected.

 

Clinical characteristics.

Indications.

Tigofast-120: symptomatic treatment of seasonal allergic rhinitis in adults and children aged 12 years and older.

Tigofast-180: symptomatic treatment of chronic idiopathic urticaria in adults and children aged 12 years and older.

 

Contraindications.

Hypersensitivity to the components of the medicinal product, age under 12 years.

 

Interaction with other medicinal products and other types of interactions.

Tigofast is not biotransformed in the liver and therefore does not interact with other drugs metabolized by hepatic microsomal enzymes.

Fexofenadine is a substrate of P-glycoprotein (P-gp) and organic anion transporting polypeptide (OATP). Concomitant use of fexofenadine with inhibitors or inducers of P-gp may affect fexofenadine exposure. With simultaneous administration of Tigofast with P-gp inhibitors erythromycin or ketoconazole, the plasma concentration of Tigofast increases by 2-3 times. These changes are not accompanied by changes in the QT interval and do not cause an increase in the frequency of adverse reactions compared to the frequency of adverse reactions when each of these drugs is prescribed separately.

A clinical drug interaction study showed that concomitant use of apalutamide (a weak P-gp inducer) and a single oral dose of 30 mg fexofenadine resulted in a 30% reduction in fexofenadine AUC.

No interaction between Tigofast and omeprazole was observed. When taking antacids containing aluminum or magnesium 15 minutes before taking Tigofast, its bioavailability decreases due to binding in the digestive tract. It is recommended to make an interval of 2 hours between taking Tigofast and antacids containing aluminum or magnesium hydroxide.

 

Precautions for use.

Caution should be exercised when using Tigofast in elderly patients and patients with impaired hepatic or renal function due to insufficient data.

Patients who have had in the past or currently have cardiovascular diseases should be aware that antihistamine class drugs may contribute to the occurrence of such adverse effects as tachycardia and palpitations (see section "Adverse reactions").

 

Pregnancy or lactation.

Pregnancy. Data on use in pregnant women are insufficient. Limited animal studies do not indicate the presence of direct or indirect effects on pregnancy, embryonic/foetal development, childbirth, or postnatal development. Fexofenadine hydrochloride should not be used during pregnancy, except in cases of urgent need, when the expected benefit to the mother outweighs the possible risk to the foetus.

Breastfeeding. Since fexofenadine passes into breast milk, the drug should not be used during breastfeeding.

 

Effects on ability to drive and use machines.

Based on the pharmacodynamic profile and known adverse effects, it can be concluded that taking Tigofast does not affect the ability to drive vehicles and perform work requiring concentration of attention. Objective studies have shown that Tigofast does not have a significant effect on central nervous system (CNS) functions. However, it is recommended to assess the individual response to the medicinal product before starting to drive vehicles or perform work requiring concentration of attention.

 

Method of administration and dosage.

Adults and children over 12 years of age should be prescribed Tigofast for seasonal allergic rhinitis – 120 mg once daily, for chronic idiopathic urticaria – 180 mg once daily. Take orally before meals, with water. The duration of treatment should be determined individually, depending on the severity of the disease.

Children under 12 years of age

No studies have been conducted to study the efficacy and tolerability of Tigofast-120 or Tigofast-180 in children under 12 years of age.

Special populations

According to the results of studies with patients from certain risk groups (elderly patients, patients with impaired renal or hepatic function), dose adjustment for such patients is not required.

The duration of treatment depends on the course of the disease and is determined by the physician individually.

 

Children.

In this dosage, the drug should not be used in children under 12 years of age.

 

Overdose.

Most reports of fexofenadine hydrochloride overdose are insufficiently informative. Thus, dizziness, drowsiness, and dry mouth have been reported.

In case of overdose, standard measures should be taken to remove unabsorbed active substances. Symptomatic and supportive therapy is recommended. Removal of fexofenadine hydrochloride from the blood by haemodialysis is ineffective.

 

Adverse reactions.

Nervous system disorders: headache, drowsiness, dizziness.

Eye disorders: blurred vision.

Gastrointestinal disorders: nausea, diarrhea, epigastric spasms.

General disorders and administration site conditions: feeling of increased fatigue.

Immune system disorders: hypersensitivity reactions, including angioedema, feeling of chest tightness, dyspnoea, facial flushing, and systemic anaphylactic reactions, dyspnoea, flushing.

Psychiatric disorders: insomnia, increased irritability and sleep disturbances or unusual dreams (paroniria).

Cardiac disorders: tachycardia, palpitations.

Skin and subcutaneous tissue disorders: rash, exanthema, urticaria, pruritus.

The medicinal product contains the dye "Sunset Yellow FCF" (E 110), which may cause allergic reactions.

 

Shelf life. 2 years.

Do not use the product after the expiry date.

 

Storage conditions.

Keep out of reach of children.

Store in the original package at a temperature not exceeding 25 °C.

 

Packaging.

10 tablets in a blister, 1 or 3 blisters in a box.

 

Terms of dispensing. On prescription.

 

Date of last update.

15.07.2026