Elset tablets 5mg, No. 7

Symptomatic therapy of allergic diseases and conditions:

• perennial (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia, nasal congestion);

• hay fever (hay fever);

• urticaria (including chronic idiopathic urticaria);

• Quincke's edema;

• other allergic dermatoses, accompanied by itching and rashes.

The drug is administered orally during meals or on an empty stomach.

The tablets are taken with a little water without chewing.

Adults and children over 6 years old : daily dose of 5 mg (1 tab)

Film-coated tablets

levocetirizine dihydrochloride

...

• end-stage renal failure (CC less than 10 ml / min);

• children under 6 years of age (for tablets);

• pregnancy;

• hypersensitivity to the components of the drug, especially in patients with galactosemia or severe lactose intolerance (for tablets);

• hypersensitivity to levocetirizine or piperazine derivatives.

The drug should be used with caution in chronic renal failure (correction of the dosage regimen is required), in elderly patients (with age-related decrease in glomerular filtration).

pharmachologic effect

The histamine H1 receptor blocker, the enantiomer of cetirizine, belongs to the group of competitive histamine antagonists. The affinity for histamine H1 receptors in levocetirizine is 2 times higher than that of cetirizine.

Levocetirizine affects the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators. It prevents the development and facilitates the course of allergic reactions, has an antiexudative, antipruritic effect, practically does not have an anticholinergic and antiserotonin effect. In therapeutic doses, it has practically no sedative effect.

Pharmacokinetics

Suction

The pharmacokinetic parameters of levocetirizine vary linearly and practically do not differ from the pharmacokinetics of cetirizine. After oral administration, levocetirzine is rapidly absorbed from the gastrointestinal tract. Food intake does not affect the rate of absorption, although the rate of absorption decreases. After a single oral administration in a therapeutic dose, Cmax in blood plasma in adults is reached after 0.9 h and is 207 ng / ml, after repeated administration at a dose of 5 mg / day - 308 ng / ml. Bioavailability is 100%.

Distribution

Css is reached after 2 days. Plasma protein binding of levocetirizine is 90%.
Vd is 0.4 l / kg.

Metabolism

Less than 14% is metabolized in the liver by N- and O-dealkylation (unlike other blockers of histamine H1 receptors, which are metabolized in the liver with the participation of isoenzymes of the cytochrome P450 system) with the formation of a pharmacologically inactive metabolite. Due to the low metabolic rate and the lack of metabolic potential, the interaction of levocetirizine with other drugs seems unlikely.

Withdrawal

In adults, it is 7.9 ± 1.9 h, the total clearance is 0.63 ml / min / kg. About 85.4% of the dose is excreted by the kidneys unchanged by glomerular filtration and tubular secretion; about 12.9% is excreted through the intestines.

Pharmacokinetics in special clinical cases

In patients with renal insufficiency (CC less than 40 ml / min), the clearance of levocetirizine decreases, and T1 / 2 increases (in patients on hemodialysis, the total clearance decreases by 80%), which requires a corresponding change in the dosage regimen. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

In young children, T1 / 2 is shortened.

Indications of the drug

Symptomatic therapy of allergic diseases and conditions:

• perennial (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia, nasal congestion);

• hay fever (hay fever);

• urticaria (including chronic idiopathic urticaria);

• Quincke's edema;

• other allergic dermatoses, accompanied by itching and rashes.

  Side effect

  Possible side effects are listed below by body systems and frequency of occurrence: often (? 1/10); infrequently (from? 1/100 to <1/10); rarely (from? 1/1000 to <1/100); very rare (from? 1/10 000 to <1/1000).

  From the side of the central nervous system: infrequently - headache, fatigue, drowsiness; rarely - asthenia; very rarely - aggression, agitation, convulsions, hallucinations, depression, visual impairment.

  From the side of the cardiovascular system: very rarely - tachycardia.

  From the respiratory system: very rarely - dyspnea.

  From the digestive system: infrequently - dry mouth; rarely - abdominal pain; very rarely - nausea, diarrhea, hepatitis, changes in liver function tests.

  From the musculoskeletal system: very rarely - myalgia.

  From the side of metabolism: very rarely - an increase in body weight.

  Allergic reactions: very rarely - itching, rash, urticaria, angioedema, anaphylaxis.

  Contraindications for use

  • end-stage renal failure (CC less than 10 ml / min);

  • children under 6 years of age (for tablets);

  • children under 2 years of age (for oral drops);

  • pregnancy;

  • hypersensitivity to the components of the drug, especially in patients with galactosemia or severe lactose intolerance (for tablets);

  • hypersensitivity to levocetirizine or piperazine derivatives.

  The drug should be used with caution in chronic renal failure (correction of the dosage regimen is required), in elderly patients (with age-related decrease in glomerular filtration).

  Application during pregnancy and lactation

  Adequate and strictly controlled clinical studies on the safety of using the drug in pregnant women have not been conducted, so it should not be prescribed during pregnancy.

  Levocetirizine is excreted in breast milk, therefore, if it is necessary to use the drug during lactation, breastfeeding should be discontinued at the time of admission.

  In experimental studies in animals have not revealed any direct or indirect adverse effects on the developing fetus levocetirizine (including in the postnatal period), during pregnancy and childbirth are not changed.

  Application for violations of liver function

  No dose adjustment is required in patients with hepatic impairment.

  Application for impaired renal function

  Contraindicated in end-stage renal failure (CC less than 10 ml / min).

  Application in children

  Contraindicated in children under 6 years of age (for tablets); in children under 2 years of age (for oral drops).

  Children over 6 years old : daily dose of 5 mg (1 tab. Or 20 drops).

  Children aged 2 to 6 years: 1.25 mg (5 drops) 2 times / day; daily dose - 2.5 mg (10 drops).

  Use in elderly patients

  Since levocetirizine is excreted by the kidneys, when prescribing the drug to elderly patients, the dose should be adjusted depending on the CC value.

  special instructions

  The patient should be careful when taking the drug and drinking alcohol at the same time.

  Influence on the ability to drive vehicles and use mechanisms

  An objective assessment of the ability to drive vehicles and work with mechanisms did not reliably reveal any undesirable effects when prescribing the drug at the recommended dose. Nevertheless, during the period of treatment, it is advisable to refrain from engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

  Overdose

  Symptoms: drowsiness (in adults), agitation and anxiety, followed by drowsiness (in children).

  Treatment: immediately after taking the drug, rinse the stomach or induce artificial vomiting. The appointment of activated carbon, symptomatic and supportive therapy is recommended. There is no specific antidote. Hemodialysis is ineffective.

  Drug interactions

  The study of the interaction of levocetirizine with other drugs has not been conducted.

  When studying the drug interaction of cetirizine racemate with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically significant undesirable interaction was revealed.

  With simultaneous use with theophylline (400 mg / day), the total clearance of cetirizine decreases by 16%, the pharmacokinetic parameters of theophylline do not change.

  In some cases, with the simultaneous use of levocetirizine with ethanol or drugs that have a depressing effect on the central nervous system, their effect on the central nervous system may be enhanced, although it has been proven that the racemate of cetirizine potentiates the effect of alcohol.