Amertil

General characteristics. Structure:

Active agent: the amertila contains 10 mg of a tsetirizin of dihydrochloride;

Other components: lactoses monohydrate, cellulose microcrystallic, the starch modified magnesium stearate, titanium dioxide, a gidroksipropilmetiltsellyuloz, propylene glycol.

Pharmacological properties:

Pharmacodynamics. Tsetirizin belongs to group of antihistaminic drugs of the second generation who is the selection antagonists of peripheral H1 - histamine receptors. On chemical structure is to the carboxylated derivatives of Hydroxyzinum which is its main metabolite. The molecule of a tsetirizin, unlike Hydroxyzinum, has big polarity and stronger contacts proteins of a blood plasma. Thanks to it drug almost does not get through a blood-brain barrier, and it in turn explains almost total absence of the suppressing influence on the central nervous system in comparison with antihistaminic drugs of the first generation. Thanks to such selectivity does not block cholinergic and serotonergic 5HT2, dopaminergic D2, adrenergic a1 and muskarinovy receptors.
Influence of a tsetirizin results dvukhfazno. At an initial stage of allergic reaction drug reduces quantity endo-and an exogenous histamine in close proximity to peripheral H1 - histamine receptors, thus suppressing development of an erythema. In the following phase – slows down migration of eosinophilic granulocytes to the center of an inflammation and reduces release of mediators of an inflammation from mast cells. Tsetirizin, reducing a nadreaktivnost of bronchial tubes, interferes with their spazmirovaniye, caused by a histamine. Considerably reduces permeability of vessels of mucous membranes, including a mucous membrane of a nose. Suppresses development of the skin allergic reactions caused by antigens of herbs, a factor 48/80, and also action of neuropeptids like VIP and substances P. At persons with атопиею suppresses formations of D2 prostaglandin which is responsible for formations of the allergic inflammatory centers.

Pharmacokinetics. Absorption. At oral administration цетиризин it is quickly and completely soaked up. The maximum concentration of drug in plasma is reached approximately in 60 min. after introduction and almost 24th hour remains. Use of drug during the period or right after food can slow down several the speed of absorption of active ingredient, but it does not influence an absorption povnota.

Distribution. Absorption and distribution of a tsetirizin is slowed down at administration of drug for the night that causes lengthenings of time of its action. Extent of linkng with proteins of plasma makes nearly 93%. Distribution volume in equilibrium state at a single dose in a dose of 10 mg of a tsetirizin makes 0, 56-0, 8 l/kg. Considering on considerably difficulty penetration of a tsetirizin into cerebrospinal fluid, its concentration in TsNS fabrics much more lower, than at blood.

Metabolism. Tsetirizin is partially metabolized in an organism. One from the revealed metabolites is its dealkirovany derivative.

Elimination (removal). The renal clearance of a tsetirizin at adults at normal function of kidneys makes 7ml/minutes, and at children slightly higher and reaches value 0, 06 - 0, 07 of l/hour / 1 body weight kg. The elimination half-life at adults makes about 8 hours, at children – almost 7th hour.
At elderly people the elimination half-life of drug can last even for 50%, and at patients with a renal failure even more that is connected with decrease in clearance of creatinine and increase in time of achievement of the maximum concentration of drug in plasma. So, at moderately expressed renal failure the renal clearance of drug makes 1,5 ml/min. The hepatic unsufficiency an insignificant measure prolongs a drug elimination half-life. The hemodialysis is not an effective method of elimination of a tsetirizin.
At systematic use of a tsetirizin equilibrium state is reached in 3 days, at the same time value of clearance of drug does not change. Long reception of a tsetirizin does not influence a way and speed removal of other drugs. Theophylline can reduce an insignificant measure clearance of a tsetirizin.
On average 60% of once accepted dose of 10 mg of drug are removed in an invariable view with urine during the first days, another 10% - during the next 4 days. Only 10% are removed with bile within 5 days.

Indications to use:

For a symptomatic treatment of allergic diseases:
- chronic (tsilorichesky) allergic rhinitis;
- seasonal allergic rhinitis;
- allergic conjunctivitis;
- chronic idiopathic small tortoiseshell;
- allergic dermatitis.

Route of administration and doses:

To adults and children 12 years are more senior it is recommended to accept 10 mg (1 tablet, coated) in days, it is the best of all in the evening. To children by age from 6 to 12 years the dose of drug is established depending on body weight: if the body weight of the child makes more than 30 kg, then drug appoint in a dose 10 mg (1 tablet, coated) once a day, it is the best of all in the evening. In case the body weight of the child makes less than 30 kg, drug is used in a dose 5 mg (1/2 tablets, coated) once a day, it is the best of all in the evening. To the persons especially sensitive to effect of drug, and also children, the recommended dose it is possible to distribute on two receptions every the 12th hour.

Duration of treatment depends by nature, durations and loudspeakers of symptomatology and is defined by the doctor individually for each patient.

Features of use:

In usage time of Amertil it is not necessary to take alcohol. Elderly people have a drug removal which is slowed down therefore the interval between receptions of separate doses should be increased. The drug dose for patients with a renal failure has to be lowered twice.
Administration of drug it is necessary to stop some days before planned carrying out skin allergic tests. Tsetirizin does not influence results of other clinical tests and laboratory indicators.

Influence on ability to manage vehicles and moving mechanisms which need big attention of concentration.
Considering a possibility of emergence of side effects (drowsiness) that makes decrease in psychomotor activity, at Amertil's use it is necessary to refrain from control of vehicles and not to work with potentially unsafe mechanisms.

Side effects:

In isolated cases tranzitorny side effects, including a headache, dizziness, excitement, weakness, a xerostomia, manifestations of skin allergic reactions, increased fatigue, laryngitis, an abdominal pain, cough, diarrhea, nasal bleeding, a bronchospasm, nausea, vomiting, a Quincke's disease are possible.

At certain patients hypersensitivity reactions and displays of hepatic dysfunction (hepatitis, increase in activity of transaminases) were observed. These phenomena disappear after drug withdrawal.

Interaction with other medicines:

It is unknown about clinically significant interaction of a tsetirizin with erythromycin, azithromycin, ketokonazoly, pseudoephedrine, phenazine. Theophylline in a dose of 400 mg/days can cause insignificant delay of clearance of a tsetirizin. Interaction with other medicines meanwhile is unknown. However it is necessary to adhere to special care at simultaneous use together with hypnotic drugs and sedatives, and also alcohol. Use of a tsetirizin along with medicines which have ototoksichesky action, for example, gentamycin can mask such symptoms of ototoxicity as a sonitus, dizziness.

Contraindications:

Amertil it is not necessary to apply at patients with hypersensitivity to a tsetirizin or other components of drug; at severe forms of a nephropathy; during pregnancy and a lactation; to children age up to 6 years.

Overdose:

Exceeding of the recommended doses several times does not cause emergence of specific symptoms of toxic action (researches on animals with a pharmacokinetic profile, to human showed similar that LD50 dose, at least by 500 times exceeds the recommended therapeutic dose). A symptom adults can have an overdose drowsiness. The overdose at children can be shown by excitement. Has no specific antidote. Treatment – symptomatic. In a case suspicion of poisonings tsetiriziny it is necessary to cause as soon as possible vomiting and to carry out a gastric lavage.

Storage conditions:

To store in the unavailable to children, protected from light, dry place, at a temperature not of the highest for 25 °C.

Issue conditions:

According to the recipe

Packaging:

Drug is packed on 7 tablets in the blister in a cardboard box; on 10 tablets in the blister on 2 or 3 blisters in a cardboard box.