Zodak express, 200 mg 7 pcs.

Zodak express is an anti-allergic.

Pharmacodynamics

Levocetirizine, the (R)-enantiomer of cetirizine, is an inhibitor of peripheral H1-histamine receptors with 2 times higher affinity than that of cetirizine. After a single dose of levocetirizine, there was 90% binding of H1-histamine receptors after 4 h and 57% binding after 24 h.

Levocetirizine has an effect on the histamine-dependent stage of allergic reactions, it reduces migration of eosinophils, decreases vascular permeability, limits release of inflammatory mediators, prevents development and facilitates allergic reactions, has antiexudative and antipruritic effects, practically has no anticholinergic and antiserotonic action, in therapeutic doses it practically has no sedative action.

The action of levocetirizine starts 12 minutes after a single dose in 50% of patients, after 1 hour – in 95% of patients and lasts for 24 hours. Administration of levocetirizine has no effect on the QT interval on ECG.

Pharmacokinetics

The pharmacokinetics of levocetirizine is linear, independent of dose and time and varies slightly in different patients.

Levocetirizine is quickly and completely absorbed from the gastrointestinal tract after oral administration.

Eating does not affect the completeness of absorption, although its rate is reduced.

The plasma Cmax is reached 0.9 h (54 min) after drug administration.

The Css is established after 2 days. Plasma Cmax after a single dose of 5 mg of levocetirizine is 270 ng/ml, and 308 ng/ml after repeated doses of 5 mg.

Levocetirizine is 90% bound to plasma proteins. Vd is 0.4 l/kg. There are no data on distribution of levocetirizine in tissues and its penetration through the BBB in humans.

Levocetirizine is metabolized in small amounts (<14%) in the body by N- and O-dealkylation (unlike other H1-histamine receptor antagonists, which are metabolized in the liver by the cytochrome system) to form a pharmacologically inactive metabolite.

Owing to limited metabolism and absence of metabolic inhibitory activity, interaction of levocetirizine on the metabolic level with other substances is unlikely. T1/2 in adults is 7.9±1.9 h; T1/2 in young children is shorter. The average observed total clearance is 0.63 ml/min/kg.

Levocetirizine is primarily excreted unchanged in the urine, on average, about 85.4% of the administered dose by glomerular filtration and active tubular secretion. Excretion through the intestine (in the feces) is only 12.9% of the taken dose.

Patients with renal insufficiency. Total clearance of levocetirizine depends on creatinine cl. Therefore, in patients with moderate and severe renal insufficiency it is recommended to increase the intervals between doses of the drug according to creatinine Cl. In patients with anuria and terminal renal failure, total clearance of levocetirizine is reduced by approximately 80% compared to healthy subjects. The amount of levocetirizine excreted by a standard 4-hour hemodialysis procedure is less than 10%.

Indications

Active ingredient

Composition

Active ingredient:

levocetirizine dihydrochloride 5 mg;

Excipients:

Lactose monohydrate, 67.5 mg;

MCC, 25 mg;

sodium carboxymethyl starch, 1 mg;

/p>

colloidal silicon dioxide – 0.5 mg;

magnesium stearate – 1 mg;

film film sheath:

Hypromellose 2910/5 – 3.3 mg;

macrogol 6000 – 0.35 mg;

talc – 0.85 mg;

titanium dioxide (E171) – 0.5 mg

How to take, the dosage

Overly, without chewing and with liquids, regardless of meals. It is recommended to take the daily dose in one dose.

Adults, adolescents and children over 6 years of age. The recommended daily dose is 5 mg (1 tablet).

Interaction

The study of interaction of levocetirizine with other medicinal products, including studies with inducers of CYP3A4 isoenzyme, has not been conducted.

In the study of drug interactions of cetirizine racemate with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam no clinically significant adverse interactions were found.

Concomitant administration with theophylline (400 mg/day) decreases total clearance of cetirizine by 16% (theophylline kinetics is not changed).

In a study with concomitant administration of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), cetirizine exposure was shown to increase by 40% and ritonavir exposure was not significantly altered (11%).

In sensitive patients, concomitant administration of levocetirizine and alcohol or other CNS-depressant substances may increase CNS effects, although cetirizine racemate has not been shown to increase the effects of alcohol.

Special Instructions

It is not recommended to take ethanol during treatment with the drug.

Impact on the ability to drive vehicles or engage in other potentially dangerous activities. Levocetirizine, when taken in recommended doses, does not adversely affect attention and speed of psychomotor reactions and the ability to drive vehicles. Nevertheless, during the period of taking the drug it is reasonable to refrain from potentially dangerous activities requiring high concentration and speed of psychomotor reactions.

Contraindications

Side effects

Immune system disorders: very rarely – hypersensitivity reactions, including anaphylactic reactions.

Nervous system disorders: often – headache; infrequent – somnolence; very rare – aggression, agitation, hallucinations, depression, seizures.

An organ of vision: very rarely – visual disorders.

Heart: very rare – feeling of palpitations, tachycardia.

Respiratory system, thoracic and mediastinal organs: very rarely – shortness of breath.

Gastrointestinal disorders: frequently – dry mouth; infrequently – abdominal pain; very rarely – nausea, diarrhea.

Liver and biliary tract: very rare – hepatitis.

Skin and subcutaneous tissue disorders: very rare – angioedema, pruritus, rash, including drug rash, urticaria.

Skeletal, muscular and connective tissue disorders: very rare – myalgia.

General disorders: frequently – fatigue; infrequently – asthenia.

Laboratory and instrumental data: very rarely – abnormal liver function tests, weight gain.

Overdose

Symptoms: drowsiness and agitation (in adults) and restlessness followed by sleepiness (in children) are possible.

Treatment: there are no specific antidotes for levocetirizine. In case of overdose symptomatic or supportive treatment is recommended. If a little time has passed after taking the drug, gastric lavage should be performed. Levocetirizine is practically not excreted by hemodialysis.

Pregnancy use

Pregnancy

The data on the use of levocetirizine in pregnancy are scarce or limited (less than 300 pregnancy outcomes). However, the use of cetirizine, the racemate of levocetirizine, in pregnancy (more than 1000 pregnancy outcomes) was not accompanied by malformations and intrauterine and neonatal toxic effects. In animal studies no direct or indirect adverse effects on pregnancy, fetal and foetal development, childbirth and postnatal development were found.
Caution should be exercised when prescribing levocetirizine to pregnant women.

Breastfeeding period

Cetirizine, the racemate of levocetirizine, is excreted with breast milk. Therefore, excretion of levocetirizine with breast milk is also likely. Breast-fed children may have adverse reactions to levocetirizine. Therefore, caution should be exercised when prescribing levocetirizine during breastfeeding.

Fertility
There are no clinical data on levocetirizine.

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