Tigofast-120

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT TIGOFAST-120 TIGOFAST-180 (TIGOFAST-120 TIGOFAST-180)

Composition:

Active substance: fexofenadine hydrochloride;

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

Excipients:

Tablets of 120 mg: microcrystalline cellulose, maize starch, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, film coating Insta Coat White (ethylcellulose, hydroxypropylmethylcellulose, titanium dioxide (E 171)), talc;

Tablets of 180 mg: microcrystalline cellulose, maize starch, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, film coating Insta Coat Sunset Yellow (ethylcellulose, hydroxypropylmethylcellulose, Sunset Yellow FCF (E 110)), talc.

Pharmaceutical form. Film-coated tablets.

Main physicochemical properties:

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

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

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06AX26.

Pharmacological properties.

Pharmacodynamics.

Fexofenadine hydrochloride is a nonsedating antihistamine belonging to the group of specific H1-receptor antagonists. Fexofenadine is the pharmacologically active metabolite of terfenadine. It stabilizes the membranes of mast cells and prevents the release of histamine. It relieves allergy symptoms such as sneezing, rhinorrhea, itching, eye redness, and tearing. It does not produce sedative effects.

The antihistaminic effect of fexofenadine hydrochloride, administered once or twice daily, begins within 1 hour, reaches maximum at 6 hours, and lasts for 24 hours. There were no signs of tolerance development even after 28 days of treatment. Clinical effect was observed after single oral doses ranging from 10 to 130 mg. A dose of 120 mg is sufficient to ensure 24-hour efficacy.

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

Fexofenadine hydrochloride (5–10 mg/kg orally) prevents antigen-induced bronchospasm in sensitized animals and, at concentrations above therapeutic levels (10–100 micromolar), induces histamine release from peritoneal mast cells.

Pharmacokinetics.

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

60–70% of fexofenadine is protein-bound in plasma. The active substance does not cross the blood-brain barrier.

Fexofenadine undergoes almost no metabolism (either hepatic or extrahepatic): only unchanged fexofenadine is found in significant amounts in human and animal urine and feces.

Elimination of fexofenadine from plasma occurs in a biexponential manner, with a terminal half-life ranging from 11 to 15 hours after repeated dosing. The kinetics of single and multiple doses are linear at oral doses up to 120 mg twice daily. At saturation doses up to 240 mg twice daily, a slightly more than proportional increase in AUC was observed (8.8%). This indicates that the pharmacokinetics of fexofenadine are nearly linear within the daily dose range of 40–240 mg.

The majority of the dose is excreted via bile; up to 10% is excreted unchanged in urine.

Mutagenic and carcinogenic properties.

Various in vitro and in vivo mutagenicity tests revealed no mutagenic properties of fexofenadine hydrochloride.

In carcinogenicity studies, fexofenadine exposure was determined (based on plasma AUC) following administration of terfenadine during secondary pharmacokinetic studies. No evidence of carcinogenicity was observed when terfenadine was administered to rats and mice at doses up to 150 mg/kg body weight per day.

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 active substance or any of the excipients, age under 12 years.

Interaction with other medicinal products and other forms of interaction.

Tigofast is not metabolized in the liver and therefore does not interact with other drugs that are 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 P-gp inhibitors or inducers may affect fexofenadine exposure. When Tigofast is coadministered with P-gp inhibitors such as erythromycin or ketoconazole, plasma concentrations of Tigofast increase by 2–3 times. These changes are not associated with alterations in the QT interval and do not lead to an increased incidence of adverse reactions compared to the incidence observed when each of these drugs is administered separately.

A clinical drug interaction study demonstrated that concomitant administration 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 has been observed. When antacids containing aluminum or magnesium are taken 15 minutes prior to Tigofast, its bioavailability is reduced due to binding in the gastrointestinal tract. It is recommended to maintain a 2-hour interval between the administration of Tigofast and antacids containing aluminum or magnesium hydroxide.

Special precautions for use

Caution should be exercised when administering TigoFast to elderly patients and patients with impaired hepatic or renal function due to insufficient data.

Patients with a history of, or currently suffering from, cardiovascular diseases should be aware that antihistamine agents may contribute to the occurrence of adverse effects such as tachycardia and increased heart rate (see section "Adverse reactions").

Use during pregnancy or breastfeeding

Pregnancy. Data on the use of this medication in pregnant women are inadequate. Limited animal studies do not indicate any direct or indirect harmful effects on pregnancy, embryonic/fetal development, parturition, or postnatal development. However, hydrochloride of fexofenadine should not be used during pregnancy except in cases of clear medical need, when the expected benefit to the mother outweighs the potential risk to the fetus.

Breastfeeding. Since fexofenadine is excreted in breast milk, the drug should not be used during breastfeeding.

Ability to influence reaction speed when driving vehicles or operating machinery.

Based on the pharmacodynamic profile and known adverse effects, it can be concluded that TigoFast does not affect the ability to drive vehicles or perform tasks requiring concentration. Objective studies have shown that TigoFast does not exert a significant effect on central nervous system (CNS) functions. Nevertheless, it is recommended to assess individual response to the medicinal product before driving vehicles or performing tasks requiring mental concentration.

Method of administration and dosage.

For adults and children aged 12 years and older:
Tigofast should be administered for seasonal allergic rhinitis at a dose of 120 mg once daily, and for chronic idiopathic urticaria at a dose of 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 on 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 involving patients from certain risk groups (elderly patients, patients with impaired renal or hepatic function), dose adjustment is not required for these patients.

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

Children

The drug in this dosage strength should not be used in children under 12 years of age.

Overdose.

Most reports of fexofenadine hydrochloride overdose are insufficiently informative. The most commonly reported symptoms include dizziness, drowsiness, and dry mouth.

In case of overdose, standard measures to remove unabsorbed active substances should be applied. Symptomatic and supportive therapy is recommended. Hemodialysis is ineffective for removing fexofenadine hydrochloride from the blood.

Adverse reactions.

From the nervous system: headache, drowsiness, dizziness.

From the eye: blurred vision.

From the gastrointestinal tract: nausea, diarrhea, epigastric spasms.

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

From the immune system: hypersensitivity reactions, including Quincke's edema, chest tightness, dyspnea, facial flushing, systemic anaphylactic reactions, dyspnea, hot flushes.

From the psyche: insomnia, increased irritability, and sleep disturbances or unusual dreams (paroniria).

From the heart: tachycardia, palpitations.

From the skin and subcutaneous tissue: rash, exanthema, urticaria, pruritus.

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

Shelf life. 2 years.

Do not use the medicinal product after the expiry date.

Storage conditions.

Keep out of reach of children. Store in the original packaging at a temperature not exceeding 25 °C.

Packaging. 10 tablets per blister, 1 or 3 blisters per carton.

Supply category. Over-the-counter.

Manufacturer.

Arthura Pharmaceuticals Pvt. Ltd.

Manufacturer's address and location of business operations.

1505 Portia Road, Sri City SEZ, Sityavedu Mandal, Chittoor District – 517 588, Andhra Pradesh State, India.

Marketing Authorization Holder.

Ananta Medikare Ltd.

Address of the Marketing Authorization Holder.

Suite 1, 2 Station Court, Imperial Wharf, Townmead Road, Fulham, London, United Kingdom.

Instructions

for medical use of the medicinal product

TIGOFAST-120

TIGOFAST-180

(TIGOFAST-120

TIGOFAST-180)

Composition:

Active substance: fexofenadine hydrochloride;

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

Excipients:

Tablets of 120 mg: microcrystalline cellulose, maize starch, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, film coating Insta Coat White (ethylcellulose, hydroxypropylmethylcellulose, titanium dioxide (E 171)), talc;

Tablets of 180 mg: microcrystalline cellulose, maize starch, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, film coating Insta Coat Sunset Yellow (ethylcellulose, hydroxypropylmethylcellulose, Sunset Yellow FCF (E 110)), talc.

Pharmaceutical form. Film-coated tablets.

Main physicochemical properties:

Tablets of 120 mg: film-coated, round, biconvex tablets, white or almost white;

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

Pharmacotherapeutic group. Antihistamines for systemic use.

ATC code R06A X26.

Pharmacological properties.

Pharmacodynamics.

Fexofenadine hydrochloride is a nonsedating antihistamine belonging to the group of specific H1-receptor antagonists. Fexofenadine is the pharmacologically active metabolite of terfenadine. It stabilizes the membranes of mast cells and prevents the release of histamine. It relieves allergy symptoms such as sneezing, rhinorrhea, itching, eye redness, and lacrimation. It does not produce sedative effects.

The antihistaminic effect of fexofenadine hydrochloride, administered once or twice daily, begins within 1 hour, reaches its maximum at 6 hours, and lasts for 24 hours. There were no signs of tolerance development even after 28 days of treatment. Clinical effects were observed after single oral doses ranging from 10 to 130 mg. A dose of 120 mg is sufficient to ensure 24-hour efficacy.

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

Fexofenadine hydrochloride (5–10 mg/kg orally) inhibits antigen-induced bronchospasm in sensitized animals and, at concentrations above therapeutic levels (10–100 micromoles), causes histamine release from peritoneal mast cells.

Pharmacokinetics.

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

60–70% of fexofenadine is bound to plasma proteins. The active substance does not cross the blood-brain barrier.

Fexofenadine undergoes almost no metabolism (either hepatic or extrahepatic): only unchanged fexofenadine is found in significant amounts in human and animal urine and feces.

Elimination of fexofenadine from plasma occurs in a biexponential manner, with a terminal half-life ranging from 11 to 15 hours after repeated dosing. The kinetics of single and multiple doses are linear at oral doses up to 120 mg twice daily. At saturation levels, doses up to 240 mg twice daily resulted in an increase in AUC slightly greater than proportional (8.8%). This indicates that the pharmacokinetics of fexofenadine are nearly linear within the daily dose range of 40–240 mg.

The majority of the dose is excreted via bile; up to 10% is excreted unchanged in urine.

Mutagenic and carcinogenic properties.

Various in vitro and in vivo mutagenicity tests showed no evidence of mutagenic properties of fexofenadine hydrochloride.

In carcinogenicity studies, exposure to fexofenadine was determined (based on plasma AUC) following administration of terfenadine in secondary pharmacokinetic studies. No evidence of carcinogenicity was observed when terfenadine was administered to rats and mice at doses up to 150 mg/kg body weight per day.

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 metabolized 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 administration of fexofenadine with P-gp inhibitors or inducers may affect fexofenadine exposure. When Tigofast is co-administered with P-gp inhibitors such as erythromycin or ketoconazole, plasma concentrations of Tigofast increase 2–3 fold. These changes are not associated with alterations in the QT interval and do not lead to an increased incidence of adverse reactions compared to the incidence of adverse reactions when each of these drugs is administered separately.

A clinical drug interaction study demonstrated that concomitant administration 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 has been observed. When antacids containing aluminium or magnesium are taken 15 minutes prior to Tigofast, its bioavailability is reduced due to binding in the gastrointestinal tract. It is recommended to maintain a 2-hour interval between administration of Tigofast and antacids containing aluminium or magnesium hydroxide.

Special precautions for use

Caution should be exercised when administering TigoFast to elderly patients and to patients with impaired hepatic or renal function due to insufficient data.

Patients with a history of, or current, cardiovascular disorders should be aware that antihistamine-class drugs may contribute to the occurrence of adverse effects such as tachycardia and increased heart rate (see section "Adverse reactions").

Use during pregnancy or breastfeeding

Pregnancy. Data on use in pregnant women are insufficient. Limited animal studies do not indicate any direct or indirect adverse effects on pregnancy, embryonal/fetal development, parturition, or postnatal development. Hydrochloride of fexofenadine should not be used during pregnancy except in cases of urgent medical need, when the expected benefit to the mother outweighs the potential risk to the fetus.

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

Ability to influence reaction rate while driving or operating machinery

Based on the pharmacodynamic profile and known adverse effects, it can be concluded that TigoFast does not impair the ability to drive vehicles or perform tasks requiring mental alertness. Objective studies have shown that TigoFast has no significant effect on central nervous system (CNS) function. Nevertheless, it is recommended to assess individual response to the medication before driving or performing tasks that require concentration.

Method of Administration and Dosage

For adults and children aged 12 years and older:
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 on the efficacy and tolerability of the drug TigoFast-120 or TigoFast-180 in children under 12 years of age.

Special populations

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

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

Children
The drug in this dosage strength should not be used in children under 12 years of age.

Overdose

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

In case of overdose, standard measures for removing unabsorbed active substances should be applied. Symptomatic and supportive therapy is recommended. Hemodialysis is ineffective for removing fexofenadine hydrochloride from the blood.

Adverse Reactions.

Central nervous system disorders: headache, drowsiness, dizziness.

Eye disorders: blurred vision.

Gastrointestinal disorders: nausea, diarrhea, epigastric cramps.

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

Immune system disorders: hypersensitivity reactions including angioedema, chest tightness, dyspnea, facial flushing, systemic anaphylactic reactions, dyspnea, hot flushes.

Psychiatric disorders: insomnia, increased irritability, 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 "Yellow Sunset FCF" (E 110), which may cause allergic reactions.

Shelf life. 2 years.

Do not use the medicinal product after the expiry date.

Storage conditions.

Keep out of reach of children. Store in the original packaging at a temperature not exceeding 25 ºC.

Packaging. 10 tablets in a blister, 1 or 3 blisters per carton.

Supply category. Over-the-counter.

Manufacturer.

Flamingo Pharmaceuticals Ltd.

Manufacturer's address and place of business.

E-28, Opp. Fire Brigade, M.I.D.C., Talegaon, Raigad District, Maharashtra, IN– 410208, India.

Marketing Authorization Holder.

Ananta Medicare Ltd.

Address of Marketing Authorization Holder.

Suite 1, 2 Station Court, Imperial Wharf, Townmead Road, Fulham, London, United Kingdom.