Супрастинекс

General characteristics. Structure:

Tablets, film coated 1 table.

Active agent: levotsetirizina dihydrochloride of 5 mg
(4,21 mg of a levotsetirizin are equivalent)  
excipients: cellulose silicon microcrystallic Prosolv® HD90 (MKTs — 98%, silicon dioxide colloid anhydrous — 2%) — 40,4 mg; lactoses monohydrate — 37,9 mg; a hypro rod low-replaced (L-HPC11) — 10 mg; magnesium stearate — 1,7 mg  
cover: Opadry II 33G28523 white (a gipromelloza of 2910 — 40%, titanium dioxide — 25%, lactoses monohydrate — 21%, a macrogoal of 3350 — 8%, triacetin — 6%) — 5 mg
Description of a dosage form

Tablets, film coated: white or almost white round biconvex, film coated, without or almost inodorous, with the engraving "Е" — on one party and "281" — on another.

Pharmacological properties:

Pharmacological action - antihistaminic, antiallergic.
Pharmacodynamics. Enantiomer of a tsetirizin; competitive antagonist of a histamine; blocks H1-histamine receptors to which affinity is twice higher, than at a tsetirizin. Exerts impact on a gistaminozavisimy stage of allergic reactions; reduces migration of eosinophils, reduces vascular permeability, limits release of mediators of an inflammation. Prevents development and facilitates the course of allergic reactions, has anti-exudative, antipruritic effect; practically has no anticholinergic and antiserotoninergichesky effect. In therapeutic doses has practically no sedative effect.

Action begins in 12 min. after reception of a single dose at 50% of patients, through 1 h — at 95% and continues during 24 h.

Pharmacokinetics. The pharmacokinetics has linear character. It is quickly soaked up at intake; meal does not exert impact on completeness of absorption, but reduces its speed. Bioavailability — 100%. Tmax is about 0,9 h; Cmax — 207 ng/ml. Vd — about 0,4 l/kg. Communication with proteins of plasma — 90%.

Less than 14% of drug are metabolized in a liver by O-dealkylation with formation pharmacological of an inactive metabolite.

T1/2 is 7–10 h. The general Cl — about 0,63 ml/min. It is completely brought out of an organism during 96 h. It is removed by kidneys (about 85%). At a renal failure (creatinine Cl less than 40 ml/min.) the clearance decreases (at the patients who are on a hemodialysis — by 80%), T1/2 — is extended. Less than 10% leave during a hemodialysis. Gets into breast milk.

Indications to use:

Symptomatic treatment of the following states:

year-round (persistent) and seasonal allergic rhinitis and conjunctivitis (itch, sneezing, rhinorrhea, dacryagogue, conjunctiva hyperemia);

hay fever (pollinosis);

small tortoiseshell, including chronic idiopathic small tortoiseshell;

Quincke's edema;

the allergic dermatosis which is followed by an itch and rashes.

Route of administration and doses:

For intake. Drug needs to be accepted during food or on an empty stomach, washing down with a small amount of water, not chewing. The daily dose is recommended to be accepted at one time. The recommended dose to adults and children is more senior than 6 years, to elderly patients (on condition of normal function of kidneys) - 5 mg (1 tablet) a day. The maximum daily dose should not pre-vyshat 5 mg. Patients with a renal failure. Frequency of reception is established by the doctor individually according to a renal failure. At patients with a chronic renal failure at the clearance of creatinine (CC) from 30 to 49 ml/min. it is necessary to lower a dose twice (on 5 mg (1 tablet) every other day); at KK from 10 to 29 ml/min. it is necessary to lower a dose by 3 times (on 5 mg (1 tablet) each 3 days). At a heavy renal failure (KK less than 10 ml/min.) administration of drug is contraindicated. Patients with an abnormal liver function. At purpose of drug the patient with the isolated abnormal liver function, any changes of a dose are not required. And kidneys dose adjustment is recommended to patients with the combined abnormal liver function. Duration of administration of drug. Duration of reception depends on a disease. At treatment of persistent allergic rhinitis (symptoms <4 days / 1 weeks or lasting less than 4 weeks) treatment is continued before disappearance of symptoms; at emergence of symptoms treatment can be resumed. At treatment of seasonal allergic rhinitis (symptoms> of 4 days / 1 weeks or lasting more than 4 weeks) treatment continue the entire period of influence of allergens.
The course of treatment of a pollinosis is established by the doctor; it averages 1-6 weeks. At chronic diseases (including a chronic idiopathic small tortoiseshell) the course of treatment can be longer in coordination with the doctor. There is a clinical experience of use of drug lasting up to 6 months.

Features of use:

During treatment it is recommended to abstain from the ethanol use. The tablet drug Suprastineks®, coated, contains lactose therefore patients should not appoint it with a lactose intolerance, hereditary deficit of lactase or a sprue of glucose -
galactoses.
INFLUENCE ON SPOSOBNOS TO DRIVING OF MOTOR TRANSPORT AND CONTROL OF MECHANISMS.
During treatment it is recommended to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

The used lower than the parameters of frequency of side effects are determined as follows: very often —> 1/10; often —> 1/100 and <1/10; infrequently —> 1/1000 and <1/100; seldom —> 1/10000 and <1/1000; very seldom — <1/10000.

From immune system: very seldom — allergic reactions, including an anaphylaxis.

From a metabolism: very seldom — increase in body weight.

From the central and peripheral nervous system: often — drowsiness, a headache, increased fatigue; infrequently — an adynamy; seldom — migraine, dizziness.

From a respiratory organs: very seldom — диспноэ.

From a GIT: often — dryness in a mouth; infrequently — an abdominal pain; very seldom — nausea, dyspepsia.

From a hypodermic fatty tissue: very seldom — a Quincke's disease, a skin itch, rash, a small tortoiseshell.

From laboratory indicators: very seldom — change of functional hepatic trials.

At emergence of any side effects, including not specified in the instruction it is necessary to see a doctor.

Interaction with other medicines:

Researches of interactions of a levotsetirizin showed lack of clinically significant interactions with pseudoephedrine, Cimetidinum, ketokonazoly, erythromycin, azithromycin, glipizidy and diazepam.
Combined use with macroleads or ketokonazoly did not cause reliable changes on an ECG. Theophylline (400 mg/days) reduces the general clearance of a levotsetirizin by 16%, at the same time the kinetics of theophylline does not change. Levotsetirizin does not strengthen effects of alcohol, however sensitive patients have a concomitant use of a levotsetirizin with alcohol or other means, the oppressing TsNS, can make impact on TsNS.

Contraindications:

hypersensitivity to active agent (including to piperazin derivatives) or to any auxiliary component of drug;

heavy renal failure (creatinine Cl less than 10 ml/min.);

children's age up to 6 years (for tablets, film coated) and up to 2 years (for drops for intake) — due to the lack of clinical data;

pregnancy and the period of a lactation (see. "Use at pregnancy and feeding by a breast");

lactose intolerance, hereditary deficit of lactase or sprue of glucose galactose — for tablets, film coated (see. "Special instructions").

With care: a chronic renal failure, advanced age (decrease in glomerular filtering is possible).

Use at pregnancy and feeding by a breast

The researches conducted on animals did not reveal the direct or mediated harmful effect on pregnancy, development of an embryo or fruit, childbirth or post-natal development. Controlled clinical trials on safety of use of drug for pregnant women were not conducted therefore it is not necessary to appoint drug at pregnancy.

Levotsetirizin is allocated with breast milk therefore in need of its inclusion in the lactation period breastfeeding for the period of administration of drug should be stopped.

Overdose:

Overdose symptoms at adults are shown by drowsiness, at children — excitement, concern which are replaced by drowsiness. In case of overdose it is necessary to wash out also a stomach and to see a doctor. There is no specific antidote. The symptomatic and maintenance therapy is recommended. The hemodialysis is inefficient.

Storage conditions:

Period of validity 4 years. Not to use after the expiry date specified on packaging. To store in the place, unavailable to children, at a temperature not higher than 30 ˚C.

Issue conditions:

Without recipe

Packaging:

Tablets film coated 5 mg: on 7 or 10 tablets in the blister from polyamide / an aluminum foil / PVC//aluminum foil. 1 or 2 blisters (on 7 tablets) or 1, 2 or 3 blisters (on 10 tablets) are packed together with the application instruction into a cardboard pack.