Elcet pills 5mg, 7pcs

Composition

1 tablet contains:

Active ingredient-

levocetirizine dihydrochloride-5 mg;

Excipients

microcrystalline cellulose,

lactose monohydrate,

calcium hydrophosphate dihydrate,

sodium carboxymethyl starch (sodium starch glycolate),

povidone,

magnesium stearate;

Excipients for the shell

hypromellose (hydroxypropylmethylcellulose), macrogol 6000 (polyethylene glycol 6000), titanium dioxide.

Pharmacological action

Pharmacotherapy group

H1-histamine receptor blocker (anti-allergic agent).

ATX Code: R06AE09

Pharmacological properties

Pharmacodynamics

Levocetirizine-the Active ingredient of Elcet-is the R-enantiomer of cetirizine, a powerful and selective histamine antagonist that blocks H] – histamine receptors.

Levocetirizine has an effect on the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, and restricts the release of inflammatory mediators.

Levocetirizine prevents the development and eases the course of allergic reactions, has an anti-exudative, antipruritic effect, practically does not have an anticholinergic and antiserotonin effect. In therapeutic doses, it has practically no sedative effect.

Pharmacokinetics

The pharmacokinetic parameters of levocetirizine vary linearly.

Suction.

After oral use, the drug is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although it reduces its rate. The maximum concentration (Ctax) in blood plasma is reached after 0.9 hours and is 270 ng / ml, the equilibrium concentration is reached after 2 days.

Distribution

Levocetirizine is 90% bound to plasma proteins. The volume of distribution (Vd) is 0.4 l/kg. Bioavailability reaches 100%.

Metabolism

In small quantities ( Due to the low metabolism and lack of metabolic potential, the interaction of levocetirizine with drugs seems unlikely.

Deduction

The elimination half-life in adults is 7.9 ± 1.9 hours. In young children, the elimination half-life is shorter. In adults, the total clearance is 0.63 ml/min/kg. About 85.4% of the drug dose is excreted unchanged by the kidneys through glomerular filtration and tubular secretion; about 12.9% – through the intestines. Individual patient groups

Patients with renal insufficiency

In patients with renal insufficiency with creatinine clearance less than 40 ml / min, the drug clearance decreases. In patients undergoing hemodialysis, total clearance is reduced by 80%. Less than 10% of the drug is removed during a standard 4-hour hemodialysis procedure.

Children

Data from a study of the pharmacokinetics of the drug in 14 children aged 6 to 11 years with a body weight of 20 to 40 kg with a single oral dose of 5 mg of levocetirizine showed that the Ctax and area under the curve (AUC) values are approximately twice as high as those in healthy adults with cross-control.

The average Ctax value was 450 ng / ml, the maximum concentration was reached on average after 1.2 hours, the total clearance taking into account body weight was 30% higher, and the 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 from 1.25 mg to 30 mg. The data obtained during the analysis showed that taking the drug at a dose of 1.25 mg in children aged 6 months to 5 years leads to a plasma concentration corresponding to that in adults when taking the drug once a day.

Elderly patients

Data on pharmacokinetics in elderly patients are limited. When repeated use of 30 mg of levocetirizine once a day for 6 days in 9 elderly patients (aged 65 to 74 years), the total clearance was approximately 33% lower than that in younger adults. It has been shown that the distribution of cetirizine racemate depends more on kidney function than on age. This statement may also apply to levocetirizine, since both levocetirizine and cetirizine are primarily excreted in the urine. Therefore, in elderly patients, the dose of levocetirizine should be adjusted depending on renal function.

Indications

Symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis, pollinosis, urticaria, and other allergic dermatoses accompanied by itching and rashes.

Contraindications

Hypersensitivity to the Active ingredient, cetirizine, hydroxyzine, any piperazine derivative or to any other excipient of the drug. Lactase deficiency, lactose intolerance, glucose-galactose malabsorption. End-stage renal failure (creatinine clearance Children under 6 years of age (due to limited safety and efficacy data).

With caution

In case of chronic renal failure (correction of the dosage regimen is necessary).

In elderly patients (with an age-related decrease in glomerular filtration).

In patients with spinal cord injury, prostatic hyperplasia, or other predisposing factors to urinary retention, levocetirizine may increase the risk of urinary retention.

When used concomitantly with alcohol (see Interaction with other medications).

When prescribed to pregnant women and during breastfeeding.

Side effects

The drug Elcet is usually well tolerated by patients, in some cases patients have experienced the development of such side effects:

From the gastrointestinal tract and liver: dryness of the oral mucosa, nausea, vomiting, epigastric pain, hepatitis. It is also possible to change the indicators of liver tests.

From the central and peripheral nervous system: headache, dizziness, sleep and wake disorders, increased fatigue, weakness.

Allergic reactions: skin rash, pruritus, urticaria, anaphylactic shock, angioedema.

Others: palpitations, decreased visual acuity, shortness of breath, weight gain, muscle pain.

If side effects develop, you should stop taking the drug and consult your doctor.

Interaction

With the combined use of Elcet with theophylline, an increase in the half-life of levocetirizine is noted. The drug when used simultaneously with ketoconazole and antimicrobial agents of the macrolide group does not lead to ECG changes.

With the combined use of levocetirizine with drugs that depress the central nervous system, and ethanol, drowsiness may develop.

How to take, course of use and dosage

Inside, while eating or on an empty stomach, without chewing, with a small amount of water. The recommended daily dose for adults and children over 6 years of age is 5 mg (1 tablet) once a day.

Overdose

When using excessive doses of Elcet, patients develop nausea, vomiting, dryness of the oral mucosa, gastralgia, headache and drowsiness.

There is no specific antidote. In case of overdose, gastric lavage, use of enterosorbents and symptomatic therapy are indicated. Hemodialysis in patients with levocetirizine overdose is ineffective.

Form of production

Film-coated tablets.

Active ingredient

Levocetirizine

Dosage form

Tablets

Description

Children over 6 years old, For adults

Indications

Pollinosis, Dermatosis, Urticaria, Neurodermatitis, Allergy, Allergic Conjunctivitis, Allergic Rhinitis, Diathesis