INSTRUCTION

for medical use of the preparation

TIGOFAST- 120

TIGOFAST-180

Composition of the medicinal preparation.

Active substance: Fexofenadin hydrochloride; 1 tablet contains Fexofenadin hydrochloride 120 mg or 180 mg;

Auxiliary substances:

tablets 120 mg: microcrystalline cellulose, corn starch, sodium starch glycolate (type A), titanium dioxide colloidal anhydrous, colour coating Insta Coat White (ethylcellulose, hydroxypropylmethylcellulose, titanium dioxide(Е 171)), talcum;

tablets 180 mg: microcrystalline cellulose, corn starch, sodium starch glycolate (type A), titanium dioxide colloidal anhydrous, colour coating Insta Coat Sunset Yellow (ethylcellulose, hydroxypropylmethylcellulose, colorant Sunset Yellow FCF (Е 110)), talcum.

Medicinal form. Film-coated tablets.

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

Tablets 180 mg: orange or almost white round biconvex film-coated tablets.

Name and Address of the Manufacturer. Ananta Medicare Ltd.

Suite 1, 2 Station Court, Imperial Wharf, Townmead Road, Fulham, London, Great Britain.

Pharmacotherapeutical group. Antihistamine preparations for systemic use. АТС code R06A X26.

Fexofenadin hydrochloride is a non-sedating, antihistamine preparation of histamine H₁-receptor antagonist group. Fexofenadin is a pharmacologically active metabolite of terfenadine. It stabilizes mast cell membranes, inhibits histamine release. It eliminates allergy symptoms: sneezing, rhinorrhea, itching, eye reddening and lacrimation. It has no sedative action.

Antihistamine effect of Fexofenadin hydrochloride, indicated once and twice a day, exhibited within 1 h, reaching its maximum in 6 h and lasted for 24 h. There was no evidence of tolerance even after 28 days of dosing. Clinical effect was observed after single oral doses of 10 – 130 mg. The dose of 120 mg is sufficient to provide 24-h effect.

Even at plasma concentrations 32-fold exceeding therapeutic concentrations, Fexofenadin exhibited no action on slow potassium channels of human heart.

Fexofenadin hydrochloride (5-10 mg/kg orally) arrests bronchospasm of antigen origin in sensibilized guinea pigs and at concentration that is higher than a therapeutic one (10-100 micromole) causes histamine release from peritoneal mast cells. 

Fexofenadin hydrochloride absorbs readily after the intake. Maximal concentration is achieved in about 1-3 h. At daily dose of 120 mg the average value of maximal concentration is ≈ 427 ng/ml.

Fexofenadin is 60-70% bound to plasma proteins. The active substance does not cross blood-brain barrier.

Fexofenadin nearly does not metabolize (neither in the liver, nor outside it): in human and animal urine and faces only Fexofenadin was detected in significant amounts.

Excretion of Fexofenadin from plasma took place with biexpotential decrease and terminal period of half-life from 11 to 15 h after multiple intake. The kinetics of single and multiple doses is linear at oral doses up to 120 mg twice a day. In the stage of saturation doses up to 240 mg 2 twice a day caused increased АUС, which somewhat exceeded the proportional one (8,8 %). It indicates that at daily doses of 40-240 mg pharmacokinetics of Fexofenadin is nearly linear.

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

Mutagenic and cancerogenic properties.

Various mutagenic tests in vitro and in vivo did not reveal mutagenic properties in Fexofenadin hydrochloride.

Cancerogenity study of Fexofenadin hydrochloride were conducted on the basis of studies where Fexofenadin exposure was determined (with plasma АUС values) after indication of terfenadine during secondary pharmacokinetic studies. At the use of terfenadine in rats and mice (up to 150 mg/kg of body weight a day) no cancerogenity signs were revealed.

Indications.

Tigofast-120: symptomatic treatment of seasonal allergic rhinitis.

Tigofast-180: symptomatic treatment of seasonal allergic rhinitis, chronic urticaria.

Contraindications.

Hypersensitivity to the components of the preparation; children under 12 years old.

Proper security measures at use.

There is no need to adjust the dose for patients with impaired renal or hepatic function.

For elderly patients’ treatment the dose of the preparation should be selected with due caution and monitor, if necessary, renal function.

There are no special recommendations as for treatment individuals with impaired cardiovascular and/or respiratory system.

Special precautions.

Use during pregnancy and lactation.

There is no data as for safety use of Tigofast during pregnancy, therefore it should be indicated when the expected therapeutic effect for the mother overcomes the potential risk for the fetus. In case of need to use Tigofast during lactation discontinuation of breast-feeding should be considered as Tigofast excretes into breast milk.

Capacity to influence reaction rate at driving or operating other mechanisms.

On the basis of pharmacodynamic profile and known side effects it can be concluded that Tigofast intake does not influence the capacity to drive or carry out other activities which require attention focusing. In objective studies it was revealed that Tigofast has no significant influence CNS functions. However, it is recommended to estimate individual reaction to the preparation before driving or carrying out other activities which require attention focusing.

Children.

The preparation in this dosage is not used in children under 12 years old.

Way of introduction and doses.

Adults and children over 12 years old Tigofast is indicated for seasonal allergic rhinitis – 120 mg or 180 mg once a day, for chronic idiopathic urticaria – 180 mg once a day. Take with water before meals. The course of treatment is established individually due to the severity of the disease

Overdose.

Most reports on Fexofenadin hydrochloride overdose are not enough informative. So, there was registered dizziness, sleepiness and dry mouth.

In case of overdose it is necessary to use usual measures for removal of unabsorbed active substances. Symptomatic and supportive therapies are recommended. Removal of Fexofenadin hydrochloride from blood with hemodialysis is ineffective .

Side effects.

Sometimes there can be observed headache, sleepiness, giddiness, nausea, in single cases – feeling of increased fatigability.

Insomnia, increased irritability and sleep disturbances or strange dreams (paroniria), tachycardia, palpitation, diarrhea with frequency < 1% are also possible.

In single cases: exanthema, urticaria, itching and other hypersensitivity reactions: Quincke's edema, pressing feeling in the chest, short breath, face reddening and systemic anaphylactic reactions, dyspnoea, hot flushes.

In comparison with placebo, single doses up to 800 mg and doses up to 690 mg twice a day for one month, as well as 240 mg once a day for one year were taken by healthy volunteers took without any significant, from clinical point of view, side effects.

Interaction with other medicinal preparations and other forms of interaction.

Tigofast does not undergo biotransformation in the liver and thus does not interact with other preparations that are metabolized by microsomal enzymes of the liver. At single intake of Tigofast with erythromycin or ketoconazole, the concentration of Tigofast in plasma increases by 2 – 3 times, which is conditioned by increased absorption in digestive tract and decreased elimination with bile. Indicated changes are not accompanied with the change of QT interval and do not result in increased frequency of side effects in comparison with frequency of side effects at indication of these preparations. Interactions of Tigofast and Omeprazole were not observed. At the intake of antacids containing aluminium or magnesium 15 minutes before Tigofast intake, its bioavailability decreases due to binding in the digestive tract. It is recommended to make 2-hour interval between the intake of Tigofast and antacids containing aluminium or magnesium hydroxide.

Shelf life. 2 years. Do not use the preparation after its expiry date.

Storage conditions. Store in dry place at temperature not exceeding 25ºC. Keep out of the reach of children.

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

Terms of dispensing. Without prescription.

Date of the last review.