Levocetirizine

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Available since: 2019-09-19

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Clinical Pharmacology

Pharmacotherapeutic group: antiallergic agent - H1-histamine receptor blocker.

ATC code: R06AE09

Pharmacological properties

Pharmacodynamics

Levocetirizine (R), an enantiomer of cetirizine, is an inhibitor of peripheral H1-histamine receptors.

Levocetirizine has a pronounced antihistamine and antiallergic effect. It has an effect on the histamine-dependent phase of an allergic reaction, reduces the migration of eosinophils, reduces the permeability of the vascular wall and limits the release of inflammatory mediators.

Levocetirizine prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative action. Virtually no effect on cholinergic and serotonin receptors, in therapeutic doses does not have a sedative effect.

Pharmacokinetics

The pharmacokinetics of levocetirizine varies linearly.

Suction

After ingestion, the drug is quickly and completely adsorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although its rate decreases. In adults, after a single dose of the drug in a therapeutic dose (5 mg), the maximum concentration (Cmax) in the blood plasma is 270 ng / ml and is reached after 0.9 hours, after repeated administration at a dose of 5 mg - 308 ng / ml. Equilibrium plasma concentration (Css) 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

Less than 14% of the drug is metabolized in the body by N- and O-dealkylation (unlike other histamine H1 receptor antagonists, which are metabolized in the liver using a cytochrome system) to form a pharmacologically inactive metabolite. Due to limited metabolism and lack of metabolic inhibitory activity, the interaction of levocetirizine at the metabolic level with other substances is unlikely.

Removal

In adults, the half-life (T1 / 2) is 7.9 ± 1.9 hours, the total clearance of 0.63 ml / min / kg.

About 85.4% of the accepted dose of the drug is excreted by the kidneys unchanged by glomerular filtration and tubular secretion; about 12.9% through the intestines.

Peculiarities of pharmacokinetics in individual patients

Patients with impaired renal function

In patients with renal insufficiency (creatinine clearance (CC) <40 ml="" min="" the="" clearance="" of="" drug="" decreases="" and="" t1="" 2="" is="" lengthened="" in="" patients="" on="" hemodialysis="" total="" reduced="" by="" 80="" which="" requires="" a="" change="" dosage="" regimen="" less="" than="" 10="" levocetirizine="" removed="" during="" standard="" 4-hour="" p="">

Indications

Allerway, film-coated pills, 5 mg is indicated in adults and children 6 years and older with:

treatment of symptoms of allergic rhinitis, including year-round (persistent) and seasonal (intermittent) allergic rhinitis, and allergic conjunctivitis, such as itching, sneezing, nasal congestion, rhinorrhea, tearing, conjunctival hyperemia;
pollinosis (hay fever);
hives;
other allergic dermatosis, accompanied by itching and rash.

Composition

Each film-coated tablet contains:
active ingredient: levocetirizine dihydrochloride 5.00 mg;
excipients: lactose monohydrate 88.00 mg; microcrystalline cellulose 34.10 mg; colloidal silicon dioxide 1.60 mg; magnesium stearate 1.30 mg; film shell: White opadry OY 58900 (hypromellose (5 cP) 62.5%, titanium dioxide (E171) 31.25%, macrogol-400 6.25%) 3.25 mg.

Levocetirizine is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
			pills
Elcet®	Obolensky OP	Russia	pills
Levocetirizin-Teva	Teva	Israel	pills
Zodac Express	Zentiva KS	Czech	pills
Zodac pills	Zentiva KS	Czech	pills
Glencet®	Glenmark	India	pills
Suprastinex	Egis	Hungary	drops
Suprastinex	Egis	Hungary	pills
Xyzal	UCB Pharma	Belgium	drops
Xyzal	UCB Pharma	Belgium	pills

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Dosage and Administration

The pill should be taken orally, without chewing and squeezed with a liquid, regardless of the meal.
Adults and children over 6 years old
The daily dose is 5 mg (1 tablet) once.
The duration of the drug
When treating seasonal (intermittent) rhinitis (symptoms less than 4 days a week or their total duration is less than 4 weeks), the duration of treatment depends on the duration of the symptoms; treatment may be discontinued when the symptoms disappear and resumed when symptoms appear.
In the treatment of year-round (persistent) allergic rhinitis (symptoms more than 4 days a week and their total duration is more than 4 weeks), treatment may continue throughout the entire period of exposure to allergens.
The course of treatment of pollinosis sets a doctor.
There is clinical experience of continuous use of levocetirizine in adult patients with a duration of up to 6 months. If you skip taking, do not take a double dose, take the next dose at the usual time.
Special patient groups
Patients with impaired renal function
Since levocetirizine is excreted by the kidneys, when using the drug, the dose should be adjusted depending on the degree of renal failure.
With a QA value of 50-79 ml / min, dose adjustment is not required, with QC from 30 to 49 ml / min the recommended dose is 5 mg (1 tablet) every other day (1 time in 2 days), in patients with severe renal failure (QC less 30 ml / min) the recommended dose of 5 mg (1 tablet) 1 time in 3 days.
Patients with end-stage renal insufficiency (CC less than 10 ml / min) are contraindicated.
Patients with renal and hepatic impairment
Dosing is carried out according to the above scheme.
Patients with impaired liver function
With an isolated violation of liver function dose adjustment is not required.
Elderly patients without kidney dysfunction
Dose adjustment is not required.

Adverse reactions

Clinical researches
During clinical trials in men and women 12–71 years old with a frequency of 1% or more (often ≥ 1/100, <1/10), the following side effects occurred: headache, drowsiness, dry mouth, fatigue, infrequently (≥ 1/1000, <1/100) met asthenia and abdominal pain.
During clinical studies in children aged 6 to 12 years with a frequency of 1% or more (often ≥ 1/100, <1/10), headache and drowsiness occurred.
Post-registration studies
The frequency of side effects is not known (cannot be estimated from the available data).
Immune system disorders
Hypersensitivity reactions, including anaphylaxis.
Metabolic disorders and eating disorders
Increased appetite.
Mental Disorders
Anxiety, aggression, agitation, depression, hallucinations, insomnia, suicidal thoughts.
Nervous system disorders
Convulsions, thrombosis of the dura mater sinuses, paresthesia, dizziness, fainting, tremor, dysgeusia.
Disturbances from an organ of hearing and labyrinth disturbances
Vertigo
Violations by the organ of vision
Visual impairment, blurred vision, inflammatory manifestations.
Violations of the cardiovascular system
Angina pectoris, tachycardia, palpitations, jugular vein thrombosis.
Respiratory disorders
Shortness of breath, aggravation of rhinitis symptoms.
Disorders of the gastrointestinal tract
Nausea, vomiting, diarrhea.
Disorders of the liver and biliary tract
Hepatitis, changes in liver function tests.
Kidney and urinary system disorders
Dysuria, urinary retention.
Violations of the skin and subcutaneous tissue
Angioedema, persistent drug erythema, rash, pruritus, urticaria, hypotrichosis, fissures, photosensitization.
Disorders of the musculoskeletal and connective tissue
Muscle pain, arthralgia.
General violations
Peripheral edema, weight gain.
Other
Cross reactivity.
If any of the side effects indicated in the instruction are aggravated, or you have noticed any other side effects that are not indicated in the instruction, inform your doctor.

Contraindications

Hypersensitivity to the active substance, cetirizine, hydroxyzine, any piperazine derivative or to any excipient of the drug.
Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.
End-stage renal disease (CC <10 ml="" min="" li="">
Children under 6 years old (due to limited safety and efficacy data).

Carefully

In chronic renal failure (correction of the dosage regimen is necessary).
In elderly patients (with age-related reduction of glomerular filtration).
In patients with spinal cord injury, prostatic hyperplasia, and in the presence of other predisposing factors for urinary retention, since levocetirizine may increase the risk of urinary retention.
With simultaneous use of alcohol (see the section "Interaction with other drugs").
When prescribed to pregnant women and during breastfeeding.

Drug interactions

The study of the interaction of levocetirizine with other drugs was not conducted. When studying the drug interaction of the racemate cetirizine with antipyrine, azithromycin, cimetidine, diazepam, erythromycin, glipizide, ketoconazole, pseudoephedrine and phenazone, there were no clinically significant undesirable interactions.
With simultaneous appointment with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16% (the kinetics of theophylline does not change).
The study, while taking ritanovir (600 mg 2 times a day) and cetirizine (10 mg per day), showed that the exposure to cetirizine increased by 40%, and the exposure to ritonavir changed slightly (-11%).
In some cases, the simultaneous use of levocetirizine with alcohol or drugs that have an overwhelming effect on the central nervous system (CNS), can cause inhibition and deterioration of efficiency.

Pregnancy and Lactation

Pregnancy

Data on the use of levocetirizine during pregnancy are practically absent or limited (less than 300 outcomes of pregnancies). However, the use of cetirizine, a racemate of levocetirizine, during pregnancy (more than 1000 outcomes of pregnancies) was not accompanied by developmental defects and fetal and neonatal toxic effects. In animal studies, no direct or indirect adverse effects on pregnancy, fetal and fetal development, childbirth and postnatal development were identified.

Caution should be exercised when prescribing levocetirizine in pregnant women.

Breastfeeding period

Cetirizine, a racemate of levocetirizine, is excreted in breast milk. Therefore, the release of levocetirizine with breast milk is also likely. Breastfed babies may have adverse reactions to levocetirizine. Therefore, care must be taken when prescribing levocetirizine during breastfeeding.

Fertility

Clinical data on levocetirizine are not available.

Special instructions

The intervals between doses should be chosen individually depending on the renal function.
It is recommended to be careful at simultaneous use with alcohol.
If patients have predisposing factors for urinary retention (eg, spinal cord injury, prostatic hyperplasia), caution should be exercised, since levocetirizine may increase the risk of urinary retention.
Influence on ability to drive vehicles and mechanisms
Levocetirizine may lead to increased drowsiness, therefore, the drug may affect the ability to drive a car or work with equipment. During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and psychomotor speed.

Overdosage

Symptoms: drowsiness (in adults), agitation and anxiety, alternating with sleepiness (in children).

Treatment: it is necessary to flush the stomach or take activated carbon, if not enough time has passed after taking the drug. Symptomatic and maintenance therapy is recommended. There is no specific antidote. Hemodialysis is not effective.