Супрастинекс drops

General characteristics. Structure:

Drops for intake 1 фл.
active agent:  levotsetirizina dihydrochloride of 0,1 g
(1 ml of solution contains 5 mg of a levotsetirizin of dihydrochloride)  
excipients: глицерол (85%) — 5 g; propylene glycol — 7 g; sodium saccharinate — 0,2 g; acetate sodium trihydrate — 0,12 g; methylparahydroxybenzoate — 0,027 g; пропилпарагидроксибензоат — 0,003 g; acetic acid ice — 0,01 g; the water purified — to 20 ml
Description of a dosage form
Drops for intake: colourless or almost colourless liquid without deposit, with a slight smell of acetic acid.

Pharmacological properties:

Pharmacodynamics. Antiallergic means. 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 in
current of 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%. Time of achievement of the maximum concentration (TCmax) - 0.9 h, the maximum concentration (Cmax) - 207 ng/ml. Distribution volume - 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. An elimination half-life (T1/2) - 7-10 h. The general clearance - 0.63 ml/min. It is completely brought out of an organism during 96 h. It is removed by kidneys (85,4%). At a renal failure (clearance of creatinine 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 year-round (persistent) and seasonal allergic rhinitis and conjunctivitis (itch, sneezing, rhinorrhea, dacryagogue, conjunctiva gipermiya); hay fever (pollinosis); small tortoiseshells, including chronic idiopathic small tortoiseshell; Quincke's edema; allergic der -
the matoz which are 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 (including to piperazin derivatives) or to any auxiliary component of drug; heavy renal failure (clearance of creatinine less than 10 ml/min.); children's age up to 2 years (due to the lack of clinical data); pregnancy and period of a lactation.

WITH CARE.
Chronic renal failure, advanced age (decrease in glomerular filtering is possible).
USE AT PREGNANCY AND IN THE PERIOD OF THE LACTATION.
Use of drug at pregnancy is contraindicated as controlled clinical trials on safety of use of drug for pregnant women were not conducted. In need of use of drug at a lactation it is recommended to stop breastfeeding.

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:

Drops for intake, 5 mg/ml. 20 ml in a bottle of brown glass with PE the dropper and a polypropylene cover with internal PE a layer supplied with special protection against opening by children and control of the first opening. 1 фл. it is packed into a cardboard pack.