Alersat-L - instructions for use, dose, side effects, contraindications

composition of the shell: instacoate (IC-S-344) 1 mg [hypromellose 48%, diethyl phthalate 12%, ethyl cellulose 40%], hypromellose-E15 3.11 mg, titanium dioxide (E171) 0.8 mg, macrogol-400 0.64 mg, iron dye red oxide (E172) 0.1 mg. talc 0.8 mg.

Description:Tablets of oblong form, covered with a film shell of light pink color, with a risk on one side. Type of tablet on a cross-section: the shell - light pink color, a kernel - white color.

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-enantiomerc of cetirizine; a competitive histamine antagonist; blocks H₁-gistaminovye receptors, affinity for which is 2 times higher than that of cetirizine. Levocetirizine affects the histamine-dependent stage of allergic reactions; reduces the migration of eosinophils, reduces vascular permeability, limits the release of inflammatory mediators and cytokines (VCAM-1 and others).

Levocetirizine prevents development and facilitates the course of allergic reactions, has an antiexudative, antipruritic effect; practically does not have anticholinergic and antiserotonin action. In therapeutic doses, it practically does not have a sedative effect.

The action begins 12 minutes after taking a single dose in 50% of patients, after 1 hour - in 95% and lasts for 24 hours.

Pharmacokinetics:

Pharmacokinetics is linear.Levocetirizip is rapidly and completely absorbed from the gastrointestinal tract when administered orally; food intake does not affect the fullness of absorption, but reduces its speed. Bioavailability reaches 100%. Time to reach the maximum concentration in the blood plasma (TCmax) - 0.9 hours, the maximum concentration in the blood plasma (Cmax) - 270 mg / ml, the equilibrium concentration is achieved after 2 days.

The volume of distribution is 0.4 l / kg. Binding to blood plasma proteins - 90%. Less than 14% of the drug is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite. The half-life (T1 / 2) in adults is -7.9 ± 1.9 hours. In adults, the total clearance is 0.63 ml / min / kg. Completely eliminated from the body for 95 hours. About 85,4% of the accepted dose of the drug is excreted by the kidneys, about 12,9% - through the intestine. With renal insufficiency (creatinine clearance less than 40 ml / min), the clearance decreases (in patients on hemodialysis - by 80%, which requires a change in the appropriate dosing regimen), the half-life (T1 / 2) - is prolonged. Less than 10% is removed during a standard 4-hour hemodialysis procedure.

Indications:

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

Pollinosis (hay fever);

Hives, including chronic idiopathic urticaria. Other allergic dermatoses, accompanied by itching and rashes.

Contraindications:

Hypersensitivity to levocetirizine (including piperazine derivatives), as well as to other components of the drug;

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

Terminal stage of renal failure (creatinine clearance (CC) below 10 ml / min);

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

Pregnancy and the period of breastfeeding.

Carefully:Chronic renal failure (correction of the dosing regimen is required); elderly age (glomerular filtration may be decreased); patients with spinal cord injury, prostatic hyperplasia, and other predisposing factors to urinary retention,since levocetirizip may increase the risk of urinary retention; when used concomitantly with alcohol (see Interaction with other medicines).

Pregnancy and lactation:

The use of the drug during pregnancy is contraindicated.

Levocetirizine is excreted in breast milk, so if it is necessary to use the drug in lactation it is recommended to stop breastfeeding.

Dosing and Administration:

Film coated tablets are taken orally, swallowing whole, with food or on an empty stomach, with a small amount of water.

Adults and children over 6 years of age: The daily dose is 5 mg (1 tablet) once. Since levocetirizip is excreted from the body by the kidneys, when the drug is used in patients with renal insufficiency and elderly patients The dose should be adjusted depending on the degree of renal failure. Patients with mild renal impairment (creatinine clearance 50-79 ml / min) dose adjustment is not required.

Patients with moderate renal insufficiency (clearance of creatinine from 30 to 49 ml / min) the recommended dose of 5 mg every other day.

Patients with severe renal insufficiency (creatinine clearance less than 30 ml / min) the recommended dose of 5 mg once every 3 days.

Patients with renal and hepatic impairment dosing is carried out according to the above scheme.

Patients with a violation of only liver function correction of the dosing regimen is not required.

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. If you are taking (or have recently taken) other medications, including over-the-counter drugs, tell your doctor about it.

If you forget to take the drug, do not take a double dose to compensate for the missed, take the next dose at the usual time.

Side effects:

Depending on the frequency of occurrence, the following groups of side effects are distinguished: very often (≥1/10), often (from ≥1 / 100 to <1/10), infrequently (from ≥1 / 1000 to <1/100), rarely (from ≥ 1/10000 to <1/1000), very rarely (<1/10000, including individual messages), the frequency is unknown (the frequency can not be determined from the available data).

Immune system disorders: frequency unknown - hypersensitivity reactions, including anaphylactic reactions;

Disorders from the metabolism and nutrition: frequency unknown - increased appetite, weight gain;

Disorders of the psyche: often - headache, drowsiness, fatigue; infrequently - asthenia; frequency unknown - anxiety, aggression, agitation, insomnia, hallucinations, depression, suicidal thoughts.

Impaired nervous system: the frequency is unknown - convulsions, thrombosis of the dura mater, paresthesia, dizziness, fainting, tremor, dysgeusia (impaired taste).

Disorders from the side of the organ of vision: frequency unknown - impaired vision, diplopia, inflammation.

Hearing disorders and labyrinthine disturbances: frequency unknown - vertigo.

Heart Disease: often that is unknown - a tachycardia, a stenocardia, sensation of palpitation.

Vascular disorders: frequency unknown - thrombosis of the jugular vein. Disturbances from the respiratory system, chest and mediastinal organs: frequency is unknown - dyspnea, increased symptoms of rhinitis.

Disorders from the gastrointestinal tract: often - dry mouth; infrequently - abdominal pain; frequency unknown-nausea, diarrhea, vomiting.

Disorders from the liver and bile ducts: frequency is unknown - hepatitis. Disturbances from the skin and subcutaneous tissues: frequency unknown - angioedema, persistent drug erythema, rash, itching, urticaria, hypotrichosis, cracks, photosensitivity.

Disturbances from the musculoskeletal and connective tissue: frequency unknown - pain in the muscles.

Disorders from the kidneys and urinary tract: the frequency is unknown - dysuria, urinary retention, urge to urinate.

Laboratory and instrumental data: frequency unknown - change in functional liver samples.

Other: frequency unknown - cross-reactivity, peripheral edema.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, inform the doctor about it.

Overdose:

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

Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy. There is no specific antidote. Hemodialysis is not effective.

Interaction:

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

Theophylline (400 mg / day) reduces the total clearance of levocetirizine by 16%, while the kinetics of theophylline does not change.

In the study, while taking ritonavir (600 mg twice daily) and cetirizine (10 mg per day), it was shown that the exposure of cetirizine increased by 40%, and the exposure of ritonavir slightly changed (-11%).

Joint use with macrolides or ketoconazole did not cause significant changes in the ECG.

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 is possible to increase their effect on the central nervous system, although it has not been proven that the racemate of cetirizine potentiates the effect of alcohol.

Special instructions:During treatment with the drug is not recommended to take ethanol.

Effect on the ability to drive transp. cf. and fur:Levocetirizine may lead to increased drowsiness, therefore, the drug may affect the ability to drive vehicles, mechanisms. 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:

Film coated tablets 5 mg.

Packaging:

10 tablets per blister, made of PVC film and aluminum foil.

According to 1. 2, 10 blisters together with the instruction for use will be prevented in a cardboard box.

Storage conditions:In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002900

Date of registration:06.03.2015

Expiration Date:06.03.2020

Date of cancellation:2020-03-06

The owner of the registration certificate:Micro Labs LimitedMicro Labs Limited India

Manufacturer: & nbsp

MICRO LABS, Limited India

Representation: & nbspMICRO LABS LIMITED MICRO LABS LIMITED India

Information update date: & nbsp06.07.2017

Illustrated instructions

Instructions

Alersat-L (Alercet-L)