H1-histamine receptor blocker (anti-allergic agent).
The ATX code: R06AE09
Levocetirizine, the active ingredient of Elcet, is the R-enantiomer of cetirizine, a potent and selective histamine antagonist that blocks H]-histamine receptors.
Levocetirizine influences the histamine-dependent stage of allergic reactions and also reduces migration of eosinophils, decreases vascular permeability and limits the release of inflammatory mediators.
Levocetirizine prevents the development and facilitates allergic reactions, has antiexudative and antipruritic effects, it has practically no anticholinergic and antiserotonin action. In therapeutic doses it has practically no sedative effect.
The pharmacokinetic parameters of levocetirizine change linearly.
The drug is quickly and completely absorbed from the gastrointestinal tract after oral administration. Food intake does not affect the completeness of absorption, although it reduces its rate. The maximum concentration (Stah) in blood plasma is reached after 0.9 hour and is 270 ng/ml, the equilibrium concentration is reached after 2 days.
Levocetirizine is 90% bound to plasma proteins. The volume of distribution (Vd) is 0.4 l/kg. Bioavailability reaches 100%.
In small amounts (< 14%) it is metabolized in the body by N- and O-dealkylation (unlike other H|-histamine receptor antagonists, which are metabolized in the liver by the cytochrome system) to form a pharmacologically inactive metabolite. Due to insignificant metabolism and lack of metabolic potential, interaction of levocetirizine with drugs seems unlikely.
The elimination half-life (Tx) in adults is 7.9 ± 1.9 hours. In young children the half-life is shorter. In adults, the total clearance is 0.63 ml/min/kg. About 85.4% of the drug dose taken is excreted unchanged by kidneys via glomerular filtration and tubular secretion; about 12.9% – via intestine. Certain groups of patients
Patients with renal failure
In patients with renal failure with creatinine clearance less than 40 ml/min, the drug clearance is decreased. In patients on hemodialysis total clearance is reduced by 80%. Less than 10% of the drug is removed during a standard 4-hour hemodialysis procedure.
The data from a study of the pharmacokinetics of the drug in 14 children aged 6 to 11 years with a body weight between 20 and 40 kg when 5 mg of levocetirizine was taken orally once showed that the Stache and area under the curve (AUC) were about twice that of healthy adults in a cross-match control.
The mean Stache was 450 ng/mL, the maximum concentration was reached after an average of 1.2 hours, total clearance with body weight was 30% higher, and the elimination half-life was 24% shorter in children than in adults.
A retrospective pharmacokinetic analysis was performed in 324 patients (181 children aged 1 to 5 years, 18 children aged 6 to 11 years, and 124 adults aged 18 to 55 years) who received one or more doses of levocetirizine between 1.25 mg and 30 mg. The data obtained in the analysis showed that administration of the drug in a dose of 1.25 mg in children aged 6 months to 5 years resulted in plasma concentrations corresponding to those in adults when the drug was taken once daily.
There are limited data on pharmacokinetics in elderly patients. When 30 mg of levocetirizine was repeatedly administered once daily for 6 days in 9 elderly patients (age 65 to 74 years), total clearance was approximately 33% lower than that of younger adults.
The distribution of cetirizine racemate has been shown to be more dependent on renal function than on age. This statement may also be applicable to levocetirizine, since both levocetirizine and cetirizine are primarily excreted with the urine. Therefore, in elderly patients, the dose of levocetirizine should be adjusted depending on renal function.
Neurodermitis, Dermatosis, Diathesis, Skin itching, Allergy, Runny nose (rhinitis), Pollinosis, Increased tear production, Allergic rhinitis, Allergic conjunctivitis, Sneezing, UrticariaSymptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis, pollinosis, urticaria, other allergic dermatosis, accompanied by itching and rashes.
1 tablet contains:
The active ingredient-
Levocetirizine dihydrochloride – 5 mg;
calcium hydrophosphate dihydrate,
sodium carboxymethyl starch (sodium starch glycolate),
Magnesium stearate.Excipients for the shell
Hypromellose (hydroxypropyl methylcell lulose), macrogol 6000 (polyethylene glycol 6000), titanium dioxide.
How to take, the dosage
Orally, with meals or on an empty stomach, without chewing, with a small amount of water. Recommended daily dose for adults and children over 6 years of age is 5 mg (1 tablet) once a day.
In concomitant use of Elcet with theophylline an increase in the elimination half-life of levocetirizine is observed.
Simultaneous use of the drug with ketoconazole and antimicrobial agents of macrolide group does not lead to ECG changes.
In concomitant use of levocetirizine with central nervous system depressant drugs and ethanol drowsiness may occur.
Hypersensitivity to the active substance, cetirizine, hydroxyzine, any piperazine derivative or any other excipient of the drug. Lactase deficiency, lactose intolerance, glucose-galactose malabsorption. End-stage renal failure (creatinine clearance < 10 ml/min). Children under 6 years of age (due to limited data on safety and efficacy).
In chronic renal failure (dosing regimen must be adjusted).
In elderly patients (with age-related decrease in glomerular filtration).
In patients with spinal cord injury, prostatic hyperplasia, and other predisposing factors to urinary retention, because levocetirizine may increase the risk of urinary retention.
In concomitant use with alcohol (see Interaction with other medicinal products).
When administered to pregnant women and during breastfeeding.
The drug Elcet is usually well tolerated by patients, in some cases, patients have noted the development of such side effects:
Gastrointestinal and liver side effects: dry mouth, nausea, vomiting, epigastric pain, hepatitis. There may also be changes in liver function tests.
Central and peripheral nervous system disorders: headache, dizziness, sleep and wakefulness disorders, increased fatigue, weakness.
Allergic reactions: skin rash, itching, urticaria, anaphylactic shock, Quincke’s edema.
Others: palpitations, decreased visual acuity, shortness of breath, weight gain, muscle pain.
If side effects develop, stop taking the drug and see your doctor.
When using excessive doses of Elcet, patients have reported nausea, vomiting, dry mouth, gastralgia, headache and drowsiness.
There is no specific antidote. In case of overdose gastric lavage, enterosorbents and symptomatic therapy are indicated. Hemodialysis in case of overdose of levocetirizine is ineffective.
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