Tigofast

Tigofast is an antihistamine drug that is systemically used for allergy therapy.

Its active element is the substance fexofenadine (the main metabolic component of the element terfenadine). It is an antihistamine element that acts on the body in the form of a selective peripheral antagonist of the H-1 endings. [1]

The drug demonstrates significant antihistamine activity, helping to quickly prevent the occurrence of certain allergic reactions. [2]

Indications Tigofast

It is used in the treatment of diseases of an allergic nature. Its therapeutic activity is determined by the size of the dosage of drugs: tablets with a volume of 0.12 g are used to eliminate signs of an allergic rhinitis , and tablets with a volume of 0.18 g are used to treat symptoms of idiopathic urticaria (in the chronic stage).

Release form

The release of the medication is made in tablets - 10 pieces inside a blister pack; inside the box - 1 or 3 such packs.

Pharmacodynamics

Fexofenadine hydrochloride is an antihistamine non-sedating substance from the subgroup of antagonists of specific H1 endings; this component acts as a metabolic element of terfenadine and has medicinal activity. It stabilizes the mast cell walls and prevents the secretion of histamine. In addition, it removes the signs of allergies: rhinorrhea, lacrimation, itching with sneezing and redness of the eyes. Has no sedative effect.

The antihistamine effect of fexofenadine hydrochloride, applied 1-2 times a day, develops over a period of 1 hour, reaching a maximum level after 6 hours. Its effect lasts for a period of 24 hours. [3]

Manifestations of intolerance were not observed after 28 days of drug use. The therapeutic effect developed with a 1-time serving of a portion in the range of 0.01-0.13 g. A dosage of 0.12 g is sufficient to obtain a 24-hour effect.

Even in the case of obtaining plasma values 32 times higher than the therapeutic indicators, fexofenadine did not affect the relatively slow cardiac tubules of potassium.

Fexofenadine hydrochloride, after oral administration of a portion of 5-10 mg / kg, relieves bronchial spasm, which is of an antigenic nature, in sensitized animals, and also, at values exceeding therapeutic (10-100 μmol), leads to the release of histamine from peritoneal mast cells.

Pharmacokinetics

Fexofenadine hydrochloride is absorbed at high speed after oral administration. It reaches the Cmax level after 1-3 hours. In the case of using a daily dosage of 0.12 g, the average Cmax is ≈ 427 ng / ml; with a daily portion of 0.1 g is ≈ 494 ng / ml.

Protein synthesis of fexofenadine is 60-70%. The active element does not overcome the BBB.

Fexofenadine practically does not participate in metabolic processes (inside and outside the liver): only fexofenadine is noted in large volumes inside the feces and urine of humans and animals.

Plasma excretion of fexofenadine is realized with a biexponential decrease and a terminal half-life within 11-15 hours with repeated use.

Pharmacokinetic parameters with 1-fold and repeated administration are linear (in the case of oral administration of 0.12 g portions 2 times a day).

During the saturation stage, drug dosages up to 0.24 g twice a day led to an increase in the AUC level, which was slightly more than the proportional indicator (8.8%). From this it can be concluded that at daily dosages of 0.04-0.24 g, the pharmacokinetic properties of fexofenadine are practically linear.

Basically, the drug is excreted in the bile; in an unchanged state, no more than 10% is excreted in the urine.

Dosing and administration

The medication should be prescribed by the attending doctor. In case of elimination of the signs of urticaria, which has a chronic form, it is necessary to use 0.18 g of medication 1 time per day. In the treatment of manifestations of a seasonal rhinitis of an allergic nature, 0.12 g of the drug is used 1 time per day.

It is recommended to take the medicine at the same time of the day.

The duration of the treatment cycle is selected taking into account the nature and severity of the pathology, as well as the body's response to treatment.

• Application for children

You can not prescribe medication in pediatrics (persons under 12 years of age).

Use Tigofast during pregnancy

Tigofast cannot be used during pregnancy, since tests that can confirm its safety in this group of patients have not been performed.

If you need to take drugs during hepatitis B, you need to stop breastfeeding for the period of therapy.

Contraindications

It is contraindicated to use in situations where a person has a strong intolerance to the main substance or additional elements.

Side effects Tigofast

The main side symptoms:

• manifestations affecting the work of the NA: drowsiness, headaches and dizziness;
• disorders of the gastrointestinal tract: diarrhea, nausea and epigastric spasms;
• systemic disorders: a feeling of increased fatigue;
• problems with immune function: signs of intolerance, including compression in the sternum, hot flashes, Quincke's edema, dyspnea, facial flushing and general anaphylactic manifestations;
• mental disorders: increased irritability, insomnia and sleep disorders or strange dreams;
• disorders of the heart: increased heart rate and tachycardia;
• lesions of the subcutaneous layer and epidermis: rash, itching and urticaria.

Overdose

Poisoning with medicine is noted only occasionally. In acute intoxication or accidental overdose, fatigue, drowsiness, xerostomia and dizziness may occur.

In such situations, symptomatic and supportive actions are required - gastric lavage and the use of enterosorbents.

Interactions with other drugs

In the case of the combined administration of the drug with ketoconazole or erythromycin, the plasma level of Tigofast doubles / triples. This is due to increased absorption within the gastrointestinal tract and a decrease in biliary elimination. The described changes do not change the QT-interval and do not lead to an increase in the number of negative signs (in comparison with the number of side effects when using each of the medicines separately).

When using antacids containing the element Mg or Al, 15 minutes before using the drug, the indicator of its bioavailability decreases (due to synthesis processes inside the gastrointestinal tract). It is required to observe a 2-hour interval between the introduction of these medications.

Storage conditions

Tigofast must be kept in a place closed from small children; temperature indicators - no more than 25oС.

Shelf life

Tigofast can be applied within a 24-month term from the date of manufacture of the medicinal product.

Analogs

Analogues of drugs are the substances Claritin, Agistam, Ketotifen and Allergo with Ds-lor, and in addition, Fexofast, Allergostop, Loridin and Astemizole with Eweik. In addition, the list also includes Lorano, Desorus, Semprex, Aeol and Flondian.