Eltset

General characteristics. Structure:

Active ingredient: 5 mg of a levotsetirizin of dihydrochloride in 1 tablet.

Excipients: cellulose microcrystallic, lactoses monohydrate, hydrophosphate calcium dihydrate, sodium carboxymethylstarch, povidone, magnesium stearate; cover: gipromelloza, macrogoal 6000 (polyethyleneglycol 6000), titanium dioxide.

Pharmacological properties:

Pharmacodynamics. Levotsetirizin — active agent of drug of Eltset is R-enantiomer of a tsetirizin which concerns to group of competitive antagonists of a histamine and blocks H1 - histamine receptors. Affinity to H1 - histamine receptors at a levotsetirizin is twice higher, than at a tsetirizin.

Levotsetirizin exerts impact on a gistaminozavisimy stage of allergic reactions, and also reduces migration of eosinophils, reduces permeability of vessels, limits release of mediators of an inflammation and cytokines (VCAM-1, etc.).

Levotsetirizin prevents development and facilitates the course of allergic reactions, possesses antiexudative, antipruritic action, has practically no anticholinergic and antiserotoninovy effect. In therapeutic doses practically does not render sedation.

Pharmacokinetics. Pharmacokinetic parameters of a levotsetirizin change linearly and practically do not differ from pharmacokinetics of a tsetirizin.

After intake drug is quickly and completely absorbed from a GIT. Meal does not influence completeness of absorption though its speed decreases. At adults after a single dose of drug in a therapeutic dose (5 mg) Cmax in a blood plasma makes 270 ng/ml and is reached in 0,9 h, after repeated reception in a dose of 5 mg — 308 ng/ml. Css is reached in 2 days Levotsetirizin for 90% contacts proteins of a blood plasma. Vd makes 0,4 l/kg. Bioavailability reaches 100%.

In small amounts (<14%) it is metabolized in an organism by N-and O-dealkylation (unlike other antagonists of H1-histamine receptors which are metabolized in a liver by means of system of tsitokhrom) with formation pharmacological of an inactive metabolite. Because of a low metabolic rate and lack of metabolic potential interaction of a levotsetirizin with other medicines is represented improbable.

At adult T1/2 makes (7,9±1,9) h; at small children of T1/2 it is shortened. At adults the general clearance makes 0,63 ml/min. About 85,4% of the accepted dose of drug are removed by kidneys in not changed look by glomerular filtering and canalicular secretion; about 12,9% — through intestines. At patients with a renal failure (creatinine Cl <40 ml/min.) clearance of drug decreases, and T1/2 is extended (so, at the patients who are on a hemodialysis, the general clearance decreases by 80%) that demands corresponding change of the mode of dosing. Less than 10% of a levotsetirizin are removed during the standard 4-hour procedure of a hemodialysis.

Indications to use:

Treatment of such symptoms year-round (persistent) and seasonal (intermittent) allergic rhinitises and allergic conjunctivitis, as itch, sneezing, nose congestion, rhinorrhea, dacryagogue, conjunctiva hyperemia; pollinosis (hay fever); small tortoiseshell, including chronic idiopathic small tortoiseshell, Quincke's edema; other allergic dermatosis which is followed by an itch and rashes.

Route of administration and doses:

Inside, without chewing, with food or on an empty stomach, washing down with a small amount of water. To adults and children 6 years — in a daily dose of 5 mg (1 tab.) are more senior.

As левоцетиризин it is brought out of an organism by kidneys, at purpose of drug patients with a renal failure and to patients of advanced age should adjust a dose depending on the size of clearance of creatinine.

The clearance of creatinine for men can be calculated, proceeding from concentration of serumal creatinine, on the following formula:

KK (мл.мин) = (140 – age (years)) * the body weight (kg) / 72 * KK (сыворот) (mg/dl)

The clearance of creatinine for women can be calculated, having increased the received value by coefficient 0,85.

At normal function of kidneys of a dose decline it is not required to elderly patients; at patients with a chronic renal failure calculation of a dose needs to be carried out taking into account clearance of creatinine according to information below:

- norm (clearance of creatinine of ≥80 ml/min.) - a dosage: 5 mg once a day;

- easy degree of a renal failure (clearance of creatinine of 50-79 ml/min.) - a dosage: 5 mg once a day;

- average degree of a renal failure (clearance of creatinine of 30-49 ml/min.) - a dosage: 5 mg of 1 times in 2 days;

- heavy degree of a renal failure (clearance of creatinine <30) - a dosage: 5 mg of 1 times in 3 days;

- an end-stage, a hemodialysis (clearance of creatinine <10) - administration of drug is contraindicated.

To patients with a renal and liver failure dosing is carried out according to information which is stated above.

Only with a liver failure of correction of the mode of dosing it is not required to patients.

Duration of treatment depends on a disease: at a pollinosis appoint on average during 1–6 weeks; at chronic diseases (year-round allergic rhinitis, atopic dermatitis) duration of treatment can increase (at use of drug in the form of drops — up to 18 months). There is a clinical experience of continuous use of Eltset  of tablets lasting up to 6 months.

Features of use:

It is required to be careful at simultaneous use with the ethanol or medicines oppressing the central nervous system.

Influence on ability to manage vehicles and mechanisms. During administration of drug it is reasonable to abstain from control of vehicles and from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Pregnancy and lactation. Use of drug during pregnancy is contraindicated. In need of use of drug during breastfeeding, feeding by a breast should be stopped.

Side effects:

From TsNS: often - a headache, drowsiness, increased fatigue; infrequently - an adynamy.

From the alimentary system: often - dryness in a mouth; infrequently - an abdominal pain; very seldom - nausea, disturbance of functional hepatic trials.

Allergic reactions: very seldom - a Quincke's disease, an itch, skin rash, a small tortoiseshell, an anaphylaxis.

Others: very seldom - increase in body weight, диспноэ.

Interaction with other medicines:

At simultaneous use with theophylline (400 mg/days) the general clearance of a racemic tsetirizin decreases by 16%, at the same time the kinetics of theophylline does not change.

In some cases at simultaneous use of a levotsetirizin with the ethanol or medicines oppressing the central nervous system strengthening of their influence on the central nervous system is possible.

Contraindications:

Classification of frequency of development of undesirable reactions (WHO): very often (> 1/10 cases), it is frequent (> 1/100 and <1/10 cases), infrequently (> 1/1000 and <1/100), is rare (> 1/10000 and <1/1000 cases) and is very rare (<1/10000 cases). The undesirable reactions registered in the post-marketing period of use of a levotsetirizin which frequency of development cannot be counted according to available data have the designation "frequency is unknown".

Allergic reactions: very seldom - an itch, rash, urticaria, a Quincke's disease, an anaphylaxis; frequency is unknown - hypersensitivity reactions, a resistant medicinal erythema.

From a nervous system: infrequently - a headache, fatigue, drowsiness; seldom - an adynamy; very seldom - aggression, excitement, hallucinations, a depression, spasms; frequency is unknown - sleeplessness, a sleep disorder, paresthesias, dizziness, a faint, a tremor, taste disturbance, suicide thoughts.

From an organ of sight: very seldom - a vision disorder; frequency is unknown - a diplopia.

From an acoustic organ and labyrinth disturbances: frequency is unknown - вертиго.

From cardiovascular system: very seldom - tachycardia; frequency is unknown - a heart consciousness.

From respiratory system: very seldom - диспноэ.

From the alimentary system: infrequently - dryness in a mouth; seldom - an abdominal pain; very seldom - nausea, diarrhea, hepatitis; frequency is unknown - vomiting, a lock, increase in appetite.

From kidneys and urinary tract: frequency is unknown - an ischuria, a dysuria.

From a musculoskeletal system: very seldom - a mialgiya.

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

Laboratory indicators: very seldom - change of functional trials of a liver.

Other: frequency is unknown - peripheral hypostases.

If any of the undesirable reactions specified in the instruction are aggravated, or you noticed other undesirable reactions which are not specified in the instruction, report about it to the doctor.

Overdose:

Symptoms: drowsiness (adults), excitement and concern which are replaced by drowsiness (children).

Treatment: gastric lavage, reception of absorbent carbon, carrying out a symptomatic and maintenance therapy. There is no specific antidote. The hemodialysis is not effective.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 7, 10, 14, 28, 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3 blister strip packagings together with the application instruction place in a pack from a cardboard.