Allergy - instructions for use, dose, side effects, contraindications

Oval, biconcave tablets covered with a film shell of white or almost white color, on one side smooth, on the other side of the engraving "R 5 ".The cross-section of the nucleus is from white to almost white.

Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.E. Piperazine derivatives

E.06.A.E.09 Levocetirizine

Pharmacodynamics:

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

Levocetirizine has a pronounced antihistaminic and anti-allergic effect. It affects the histamine-dependent phase of the allergic reaction, reduces the migration of eosinophils, reduces the permeability of the vascular wall, and limits the release of inflammatory mediators.

Levocetirizine prevents development and facilitates the course of allergic reactions, has antipruritic and antiexclusive action. Virtually does not affect the cholinergic and serotonin receptors, in therapeutic doses does not have a sedative effect.

Pharmacokinetics:

The pharmacokinetics of levocetirizine changes linearly.

Suction

After ingestion, the drug is rapidly and completely adsorbed from the gastrointestinal tract. The intake of food does not affect the completeness of absorption, although its rate decreases. In adults, after a single dose at a therapeutic dose (5 mg), the maximum concentration (C_mOh) in the blood plasma is 270 ng / ml and is achieved after 0.9 hours, after repeated intake in a dose of 5 mg - 308 ng / ml. Equilibrium plasma concentration (C_ss) is achieved after 2 days.

Distribution

Levocetirizine binds to blood plasma proteins by 90%. The volume of distribution (V_d) 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 (as opposed to other antagonists of H₁-gistaminovyh receptors, which are metabolized in the liver with the help of a system of cytochromes) to form a pharmacologically inactive metabolite. Due to limited metabolism and the absence of metabolic inhibitory activity, the interaction of levocetirizine at the metabolic level with other substances is unlikely.

Excretion

In adults, the half-life (T_1/2) is 7.9 ± 1.9 hours, the total clearance is 0.63 ml / min / kg.

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

Peculiarities of pharmacokinetics the individual patients

Patients with impaired renal function

Have patients with renal insufficiency (creatinine clearance (CK) <40 ml / min) clearance of the drug decreases, and T_1/2lengthens. In patients on hemodialysis, the total clearance is reduced by 80%, which requires a change in the dosage regimen. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

Indications:

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

- treatment of allergic rhinitis symptoms, including year-round (persistent) and seasonal (intermittent) allergic rhinitis, and allergic conjunctivitis such as pruritus, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia;

- Pollinosis (hay fever);

- urticaria;

- other allergic dermatoses, accompanied by itching and rashes.

Contraindications:

Hypersensitivity to the active ingredient, cetirizine, hydroxyzine, any piperazine derivative or to any auxiliary substance of the preparation.

Deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Terminal stage of renal failure (CC <10 ml / min).

Children under 6 years of age (due to limited safety and efficacy data).

Carefully:

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

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

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

When used concomitantly with alcohol {cm. section "Interaction with other medicinal products").

When appointing pregnant women and during breastfeeding.

Pregnancy and lactation:

Pregnancy

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

Care should be taken when prescribing levocetirizine to pregnant women.

Breastfeeding period

Cetirizine, the racemate of levocetirizine, is excreted in breast milk. Therefore, it is also likely the isolation of levocetirizine with breast milk. Infants who are breast-fed may experience adverse reactions to levocetirizine. Therefore, care should be taken when prescribing levocetirizine during breastfeeding.

Fertility

Clinical data on levocetirizine are absent.

Dosing and Administration:

The tablet should be taken orally, without liquid and squeezed liquid, regardless of food intake.

Adults and children over 6 years of age

The daily dose is 5 mg (1 tablet) once.

Duration of the drug

In the treatment of seasonal (intermittent) rhinitis (the presence of 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 symptomatology; Treatment can be stopped if symptoms disappear and are resumed when symptoms appear.

In the treatment of year-round (persistent) allergic rhinitis (the presence of symptoms more than 4 days a week and their total duration of more than 4 weeks) treatment can continue throughout the exposure period of allergens.

The course of treatment is determined by a doctor.

There is a clinical experience of the continuous use of levocetirizine in adult patients lasting up to 6 months.

If you miss a dose, do not take a double dose, take the next dose at the usual time.

Special patient groups

Patients with impaired renal function

Because the levocetirizine is excreted from the body by the kidneys, when the drug is administered, the dose should be adjusted depending on the degree of renal failure.

At the value of KK 50-79 ml / min dose adjustment is not required, with a QC of 30 to 49 ml / min, the recommended dose of 5 mg (1 tablet) every other day (1 every 2 days), in patients with severe renal failure 30 ml / min) the recommended dose of 5 mg (1 tablet) 1 every 3 days.

Patients with terminal renal insufficiency (CC less than 10 ml / min) receive the drug contraindicated.

Patients with renal and hepatic insufficiency

Dosage is carried out according to the above scheme.

Patients with impaired hepatic function

With an isolated violation of liver function, dose adjustment is not required.

Elderly patients without impaired renal function

Correction of the dose is not required.

Side effects:

Clinical researches

During clinical trials in men and women 12-71 years with a frequency of 1% or more (often ≥ 1/100, <1/10), the following side effects occurred: headache, drowsiness, dry mouth, fatigue, infrequent (≥ 1/1000, <1/100) asthenia and abdominal pain.

During clinical trials in children aged 6 to 12 years with a frequency of 1% or more (often ≥ 1/100, <1/10) there was a headache and drowsiness.

Post-marketing research

The frequency of side effects is not known (can not be estimated from available data).

Immune system disorders

Hypersensitivity reactions, including anaphylaxis.

Metabolic and nutritional disorders

Increased appetite.

Disorders from the psyche

Anxiety, aggression, agitation, depression, hallucinations, insomnia, suicidal thoughts.

Disturbances from the nervous system

Convulsions, thrombosis sinuses of the dura mater, paresthesia, dizziness, syncope, tremor, dysgeusia.

Hearing disorders and labyrinthine disorders

Vertigo

Disturbances on the part of the organ of sight

Visual impairment, blurred vision, inflammatory manifestations.

Disorders from the cardiovascular system

Angina pectoris, tachycardia, palpitation, thrombosis of the jugular vein.

Disturbances from the respiratory system

Shortness of breath, increased symptoms of rhinitis.

Disorders from the gastrointestinal tract

Nausea, vomiting, diarrhea.

Disturbances from the liver and bile ducts

Hepatitis, changes in functional liver samples.

Disorders from the kidneys and urinary system

Dysuria, urine retention.

Disturbances from the skin and subcutaneous tissues

Angioedema, drug resistant erythema, rash, pruritus, urticaria, hypotrichosis, cracks, photosensitivity.

Disturbances from musculoskeletal and connective tissue

Pain in the muscles, arthralgia.

Common violations

Peripheral edema, weight gain.

Other

Cross reactivity.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

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

Treatment: wash your stomach or take Activated carbon, if after the drug has passed a little time. Symptomatic and maintenance therapy is recommended. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

The interaction of levocetirizine with other drugs has not been studied.

In the study of the drug interaction of the racemate cetirizine with antipyrine, azithromycin, cimetidine, diazepam, erythromycin, glipizide, ketoconazole, pseudoephedrine and phenazone, no clinically relevant undesirable interactions have been identified.

With simultaneous appointment with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16% (theophylline kinetics does not change).

In a study with simultaneous administration of ritanovir (600 mg twice daily) and cetirizine (10 mg per day), it was shown that the exposure of cetirizine increased by 40%, and exposure to ritonavir slightly changed (-11%).

In a number of cases, with the simultaneous use of levocetirizine with alcohol or drugs that have an inhibitory effect on the central nervous system (CNS), it can cause inhibition and impairment of performance.

Special instructions:

Intervals between doses should be selected individually depending on the renal function.

It is advisable to use caution when using alcohol together.

If patients have predisposing factors to urinary retention (for example, spinal cord injury, prostatic hyperplasia), care should be taken since levocetirizine may increase the risk of urinary retention.

Effect on the ability to drive transp. cf. and fur:

Levocetirizine can lead to increased drowsiness, therefore, the drug may affect the ability to drive or work with machinery.During the treatment period it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 5 mg.

Packaging:

For 7 or 10 tablets in a blister of (PA / AL / PVC) foil / aluminum foil.

For 1, 2 or 3 blisters with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004008

Date of registration:07.12.2016

Expiration Date:07.12.2021

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDr. Reddy`c Laboratoris Ltd.Dr. Reddy`c Laboratoris Ltd.

Information update date: & nbsp08.07.2017

Illustrated instructions

Instructions

Allervay (Allervey)