Levotsetirizin - Teva

General characteristics. Structure:

Active agent: levotsetirizina dihydrochloride of 5,00 mg;
excipients: cellulose of microcrystallic 30,00 mg, lactoses monohydrate of 63,50 mg, silicon dioxide of colloid 0,50 mg, magnesium stearate of 1,00 mg;
cover of Opadray of Y1-7000H white: macrogoal-400 of 0,1875 mg, titanium dioxide (E171) of 0,9375 mg, gipromelloza-2910 (E464) of 1,875 mg.

Description
Oval tablets, film coated white or almost white color. On one party - an engraving of "LC5". On cross section a kernel of white or almost white color.

Pharmacological properties:

Pharmacodynamics. Levotsetirizin is an enantiomer of a tsetirizin, treats group of competitive antagonists of a histamine, blocks H1-histamine receptors (N1-GR), has the high level of selectivity to N1-GR. Levotsetirizin exerts impact on a gistaminozavisimy stage of allergic reactions, inhibiting the eotaksina promoting transendothelial migration of eosinophils, blocking an expression of a vascular molecule of cellular adhesion 1, reduces migration of eosinophils, reduces vascular permeability, limits release of mediators of an inflammation. Prevents development and facilitates the course of allergic reaction, possesses anti-exudative, antipruritic action, has practically no anticholinergic and antiserotoninovy effect. In therapeutic doses has practically no sedative effect, does not change indicators of the electrocardiogram (ECG), in particular a QT interval.

Pharmacokinetics. Pharmacokinetic parameters of a levotsetirizin change linearly and practically do not differ from pharmacokinetics of a tsetirizin.
Absorption. After intake левоцетиризин it is quickly soaked up in digestive tract. Meal does not influence extent of absorption though its speed decreases. After a single dose inside in a therapeutic dose the maximum concentration (Cmax) in a blood plasma at adults is reached in 0,9 h and makes 207 ng/ml, after repeated reception in a dose of 5 mg/days - 308 ng/ml. Bioavailability makes 100%.
Distribution. Equilibrium concentration is reached in 2 days. Linkng of a levotsetirizin with proteins of plasma makes 90%. The volume of distribution of drug makes 0,4 l/kg.
Metabolism. Less than 14% are metabolized in a liver by inclusion of processes of oxidation of aromatic connections, N-and O-dealkylation and conjugation of taurine. Dealkylation happens in the presence of CYP3A4 isoenzyme, and the numerous and/or not identified P450 isoenzymes participate in oxidation of aromatic connections. Levotsetirizin does not exert impact on activity of isoenzymes of CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 in concentration much to the exceeding Cmax after intake of a dose of 5 mg. Because of a low metabolic rate and lack of metabolic potential interaction of a levotsetirizin with other medicines is represented improbable.
Removal. Adults have an elimination half-life (T1/2)) makes 7,9±1,9 h, the general clearance - 0,63 ml/min. It is completely brought out of an organism during 96 h. About 85,4% of a dose are removed by kidneys in not changed look by glomerular filtering and canalicular secretion; about 12,9% are removed with a stake.
Pharmacokinetics in special clinical cases. At patients with a renal failure (the clearance of creatinine (CC) less than 40 ml/min.) the clearance of a levotsetirizin decreases, and T1/2 increases (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. At children of a younger age group of T1/2 decreases.

Indications to use:

Symptomatic treatment:
- year-round allergic rhinitis;
- seasonal allergic rhinitis;
- chronic idiopathic small tortoiseshell.

Route of administration and doses:

Inside, irrespective of meal. Tablets are chewed and washed down with water.
Adults and children are more senior than 6 years: on 5 mg once a day daily.
Duration of use depends on duration of manifestation of symptomatology of a disease. On average apply 3-6 weeks, in case of the short-term period of influence of allergen there can be enough use within 1 week. At the long chronic course of a disease treatment can continue up to 6 months.
Elderly patients: there is no need to adjust a dose.
Patients with renal failures: the dose should be adjusted depending on KK (see the table).

Renal failure                       of KK (ml/min.)                  Dose and frequency rate of reception
Norm                                                           of more than 80                          5 mg/days
Easy degree                                              of 50-79                              5 mg/days
Average degree                                            of 30-49                             5 mg/days of 1 times in 2 days
Heavy degree                                         less than 30                           5 mg/days of 1 times in 3 days
End-stage (patients,
being on a hemodialysis)                     less than 10                         Reception are contraindicated

KK calculate on formulas:
for men: the body weight (kg) x (140 age (full years)) / 72 x concentration of creatinine in a blood plasma (mg/dl);
for women: 0,85 x KK men.
Patients with abnormal liver functions: correction of the mode of dosing is not required.

Features of use:

It is impossible to exceed the recommended daily dose.
The patient needs to be warned that alcohol intake during treatment levotsetiriziny is not recommended.

Influence on ability to driving of motor transport and to control of mechanisms
Ability to driving of motor transport and work with mechanisms at use of a levotsetirizin in the recommended dose does not change. Nevertheless, considering that during treatment side reactions can develop (drowsiness, dizziness) it is necessary to be careful during the occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of development of side effects is classified according to recommendations of the World organization of health care: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; seldom - not less than 0,01%, but less than 0,1%; very seldom - less than 0,01%, including isolated cases.
From a nervous system: often - a headache, drowsiness, aggression, excitement, spasms; seldom - migraine, dizziness.
From an organ of sight: often - vision disorders.
From cardiovascular system: very seldom - tachycardia.
From respiratory system: very seldom - диспноэ.
From the alimentary system: often - dryness of a mucous membrane of an oral cavity; infrequently - an abdominal pain; very seldom - nausea, dyspepsia, diarrhea, change of functional trials of a liver, hepatitis.
From a musculoskeletal system: seldom - a mialgiya.
From a metabolism: seldom - increase in body weight.
Allergic reactions: very seldom - a skin itch, skin rash, a small tortoiseshell, a Quincke's disease, an anaphylaxis.
Others: often - bystry fatigue, feeling of fatigue; infrequently - an adynamy.

Interaction with other medicines:

When studying medicinal interaction of a levotsetirizin with pseudoephedrine, Cimetidinum, ketokonazoly, erythromycin, azithromycin, glipizidy and diazepam of clinically significant undesirable interaction it is not revealed. Simultaneous use with macroleads or ketokonazoly did not cause reliable changes on an ECG.
At simultaneous use with theophylline (400 mg/days) the general clearance of a tsetirizin decreases by 16%, pharmacokinetic parameters of theophylline do not change.
In some cases at simultaneous use of a levotsetirizin with the ethanol or medicines having the oppressing effect on the central nervous system (CNS) strengthening of their influence on TsNS is possible though it is proved that левоцетиризин does not strengthen effect of ethanol.

Contraindications:

Hypersensitivity to a levotsetirizin and other components of drug; hypersensitivity to piperazin derivatives; end-stage of a renal failure (KK less than 10 ml/min.); lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption; children's age up to 6 years; pregnancy; breastfeeding period.

With care
Average and heavy degree of a renal failure (KK more than 10 ml/min., but less than 50 ml/min.); advanced age (decrease in glomerular filtering is possible).

Use at pregnancy and during breastfeeding
Not enough clinical data on use of a levotsetirizin for pregnant women therefore it is not necessary to use drug Levotsetirizin - Teva at pregnancy.
Levotsetirizin is allocated with breast milk. In need of drug use Levotsetirizin - Teva it is necessary to stop breastfeeding.

Overdose:

Symptoms: drowsiness (at adults), the excitement and concern which are replaced by drowsiness (at children).
Symptomatic treatment: right after administration of drug to carry out a gastric lavage or to cause artificial vomiting. Use of absorbent carbon, carrying out a symptomatic and maintenance therapy is recommended. There is no specific antidote. The hemodialysis is inefficient.

Storage conditions:

To store at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 5 mg.
On 7 tablets in the blister from the aluminum laminated foil. 1 or 2 blisters with the application instruction in a pack cardboard.
On 10 tablets in the blister from the aluminum laminated foil. 1 blister with the application instruction in a pack cardboard.