Gistafen

General characteristics. Structure:

Active agent: сехифенадин (in the form of a hydrochloride) 50 mg.

Excipients: lactoses monohydrate - 302 mg, cellulose microcrystallic - 20 mg, starch corn - 20 mg, silicon dioxide - 2 mg, calcium stearate - 6 mg.

Pharmacological properties:

Blocker histamine H1 receptors with antiserotoninovy activity. Moderately blocks serotoninovy 5HT1-receptors, weakening action of mediators of an allergy of a histamine and serotonin. The histamine causes clinical manifestations of an allergic inflammation: hypostasis (permeability of capillaries increases), a dermahemia (vasodilatation), a skin itch and pain.
Feature of a sekhifenadin is that it has antihistaminic effect not only blocking histamine H1 receptors, but also reducing the maintenance of a histamine in fabrics by acceleration of its destruction by diaminoxidase.
At allergic diseases serotonin level in blood also increases. Serotonin raises the ABP, causes a bronchospasm, increases permeability of capillaries, strengthens action of mediators of an inflammation - a histamine, bradikinin, prostaglandins. Sekhifenadin prevents or weakens spazmogenny influence of a histamine and serotonin on smooth muscles of bronchial tubes, intestines, vessels; disturbance of permeability of capillaries and development of hypostases.
Sekhifenadin has the expressed antipruritic and anti-exudative effect of long character.
Influences an immune responsiveness of an organism, reducing quantity of B-lymphocytes in a spleen, marrow, lymph nodes, and also reduces the increased concentration of immunoglobulins of classes A and G.
Slightly gets through GEB, than lack of the expressed oppressing influence on TsNS speaks, however in some cases at individual hypersensitivity easy sedation is observed.
At reception of a sekhifenadin do not observe change of biochemical indicators of blood and urine, drug does not influence the ABP, ECG indicators, content of glucose and cholesterol in blood, does not influence EEG indicators.

Pharmacokinetics.
Absorption. Sekhifenadin is quickly soaked up from a GIT. Cmax in a blood plasma is reached in 1-2 h.

Distribution. Collects preferential in lungs, a liver; the lowest concentration - in a brain.

Metabolism. It is metabolized by oxidation, forming pharmacological inactive metabolite.

Removal. After reception in a single dose of 50 mg of T1/2 makes 12 h. After repeated doses of T1/2 it is shortened to 5-8 h, i.e. drug does not kumulirut in an organism.
Through intestines 50% of a dose, by kidneys - 20% are brought out of an organism. About 30% are removed in not changed look, 40-50% - in the form of metabolites.

Indications to use:

— allergic rhinitis;
— allergic conjunctivitis;
— pollinosis;
— small tortoiseshell;
— Quincke's edema;
— allergic pruritic dermatosis (including atopic dermatitis);
— prevention of diseases of allergic character till the period of their seasonal aggravation and a maintenance therapy.

Route of administration and doses:

Drug should be accepted inside after food, washing down with water.
The adult at acute and chronic allergic diseases appoint 50-100 mg 2-3 Usually therapeutic effect occur in 3 days after an initiation of treatment. Duration of a course of treatment makes 5-15 days.
For the purpose of prevention of diseases of allergic character till the period of their seasonal aggravation and for a maintenance therapy appoint 50 mg 2 Administration of drug is recommended to be begun in 2 weeks prior to the expected influence of seasonal allergen.

Features of use:

There are no clinical trials about use of drug for children and patients senile (more than 70 years) age.
Tablets of a sekhifenadin can be combined with drugs for topical administration (ointment, eye drops, drops for a nose).
In most cases drowsiness decreases or disappears in 2-5 days from an initiation of treatment.

Influence on ability to driving of motor transport and to control of mechanisms
Patients whose work demands bystry psychomotor reactions (including drivers of transport) during treatment need to refrain from driving of transport and occupations potentially dangerous types of activity.

Side effects:

- From the alimentary system: dryness in a mouth, pain in epigastriums, dyspepsia, appetite strengthening.
- From TsNS: headache, drowsiness; at use in high doses excitement, sleeplessness are possible.
- Other: seldom - a leukopenia, disturbances of a menstrual cycle, increase of an urination.

Interaction with other medicines:

Sekhifenadin does not strengthen the oppressing action of hypnagogues and alcohol on TsNS, however during treatment it is necessary to refrain from alcohol intake.

Contraindications:

— bronchial asthma;
— pregnancy;
— period of a lactation (breastfeeding);
— children's and teenage age up to 18 years;
— simultaneous use of MAO inhibitors;
— hypersensitivity to drug components;
— lactose therefore drug should not be used at deficit of lactase, a rare hereditary lactose intolerance or glyukozo-galaktozny malabsorption is a part of a tablet.

With care it is necessary to use drug at renal failures, a serious illness of cardiovascular system, a GIT, liver.

Use of the drug GISTAFEN® at pregnancy and feeding by a breast
Use of drug at pregnancy and in the period of a lactation (breastfeeding) is contraindicated.

Use at abnormal liver functions
With care it is necessary to use drug at abnormal liver functions (treatment begin with the minimum dose).

Use at renal failures
With care it is necessary to use drug at renal failures (treatment begin with the minimum dose).

Overdose:

Symptoms: dryness of mucous membranes, headache, vomiting, abdominal pain.
Treatment: symptomatic therapy. The antidote is unknown.

Storage conditions:

Drug should be stored in the unavailable to children, protected from light place at a temperature not above 25 °C. A period of validity - 4 years.

Issue conditions:

According to the recipe

Packaging:

Tablets of white or almost white color, round, ploskotsilindrichesky, with a facet and risky.
10 - blisters (1) - packs cardboard.
10 - blisters (2) - packs cardboard.
10 - blisters (3) - packs cardboard.
10 - blisters (4) - packs cardboard.
10 - blisters (5) - packs cardboard.