Composition, form of production and packaging
Tablets covered with a film coat of white or almost white color, oval; with the stamped "Y" marking on one side.
1 tab.
levocetirizine dihydrochloride 5 mg
Excipients: lactose monohydrate, microcrystalline cellulose, silicon dioxide colloid, magnesium stearate.
Sheath composition: opadrai Y-1-7000 (hypromellose, titanium dioxide (E171), macrogol 400).
7 pcs. - blisters (1) - packs of cardboard.
7 pcs. - blisters (2) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
Drops for oral administration in the form of an almost colorless, slightly opalescent solution.
1 ml
levocetirizine dihydrochloride 5 mg
Excipients: sodium acetate, acetic acid, propylene glycol, glycerol 85%, methyl parahydroxybenzoate, propyl parahydroxybenzoate, sodium saccharinate, purified water.
10 ml - bottles of dark glass with a dropper (1) - packs of cardboard.
20 ml - bottles of dark glass with a dropper (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2012.
PHARMACHOLOGIC EFFECT
The histamine H 1 -receptor blocker, the cetirizine enantiomer, belongs to the group of competitive histamine antagonists. The affinity for histamine H 1 -receptors in levocetirizine is 2 times higher than that of cetirizine.
Levocetirizine influences the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators. Prevents development and facilitates the course of allergic reactions, has antiexudative, antipruritic effect, practically does not have anticholinergic and antiserotonin action. In therapeutic doses, it practically does not have a sedative effect.
PHARMACOKINETICS
Suction
Pharmacokinetic parameters of levocetirizine vary linearly and practically do not differ from the pharmacokinetics of cetirizine. After ingestion, levocetirzine is rapidly absorbed from the digestive tract. The intake of food does not affect the degree of absorption, although its rate decreases. After a single oral intake in a therapeutic dose, Cmax in blood plasma in adults is achieved after 0.9 hours and is 207 ng / ml, after repeated administration at a dose of 5 mg / day - 308 ng / ml.Bioavailability is 100%.
Distribution
C ss is reached after 2 days. The binding of levocetirizine to plasma proteins is 90%.
V d is 0.4 l / kg.
Metabolism
Less than 14% is metabolized in the liver by N- and O-dealkylation (unlike other histamine H 1 -receptor blockers that are metabolized in the liver with the participation of cytochrome P450 isoenzymes) to form a pharmacologically inactive metabolite. Because of the low level of metabolism and the lack of a metabolic potential, the interaction of levocetirizine with other drugs is unlikely.
Excretion
In adults it is 7.9 В± 1.9 h, the total clearance is 0.63 ml / min / kg. About 85.4% of the dose is excreted by the kidneys unchanged by glomerular filtration and tubular secretion; about 12.9% is excreted through the intestine.
Pharmacokinetics in special clinical cases
In patients with renal insufficiency (CC less than 40 ml / min), the clearance of levocetirizine decreases, and T 1/2 increases (in patients on hemodialysis, the total clearance is reduced by 80%), which requires a corresponding change in the dosage regimen. Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.
In young children, T 1/2 is shortened.
INDICATIONS
Symptomatic therapy of allergic diseases and conditions:
- All-the-year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, congestion hyperemia, nasal congestion);
- Pollinosis (hay fever);
- urticaria (including chronic idiopathic urticaria);
- Quincke's edema;
- other allergic dermatoses, accompanied by itching and rashes.
DOSING MODE
The drug is administered orally during meals or on an empty stomach.
Tablets are taken with a small amount of water, without chewing.
Drops for ingestion are taken with a teaspoon. If necessary, the dose of the drug can be diluted in a small amount of water immediately before use.
Adults and children over 6 years of age : daily dose of 5 mg (1 table or 20 drops).
Children aged 2 to 6 years: 1.25 mg (5 drops) 2 times / day; daily dose of 2.5 mg (10 drops).
Since levocetirizine is excreted by the kidneys, when the drug is prescribed for elderly patients and patients with renal insufficiency, the dose should be adjusted depending on the magnitude of the CC.
QA can be calculated from the serum creatinine concentration, according to the following formula.
For men:
KK (ml / min) = [140-years (years)]? body weight (kg) / 72? serum creatinine (mg / dL)
For women: the value obtained? 0.85
Renal insufficiency KK (ml / min) Dose and frequency of admission
Norm> 80 5 mg / day
Light degree 50-79 5 mg / day
Average degree 30-49 5 mg / day 1 time in 2 days
Severe degree <30 5 mg / day 1 every 3 days
Terminal stage (patients on hemodialysis) <10 The drug is contraindicated
For patients with renal and hepatic insufficiency, dosing is carried out according to the table given above.
Patients with violations of only liver function correction dosage regimen is not required.
The duration of use depends on the readings. The course of treatment of pollinosis is on average 1-6 weeks. In chronic diseases (year-round rhinitis, atopic dermatitis), the duration of treatment can be increased to 18 months.
SIDE EFFECT
Possible side effects are given below for body systems and frequency of occurrence: often (? 1/10); infrequently (from? 1/100 to <1/10); rarely (from? 1/1000 to <1/100); very rarely (from? 1/10 000 to <1/1000).
From the side of the central nervous system: infrequently - headache, fatigue, drowsiness; rarely - asthenia; very rarely - aggression, agitation, convulsions, hallucinations, depression, impaired vision.
From the cardiovascular system: very rarely - tachycardia.
From the respiratory system: very rarely - dyspnoea.
From the side of the digestive system: infrequently - dry mouth; rarely - abdominal pain; very rarely - nausea, diarrhea, hepatitis, changes in functional liver tests.
From the musculoskeletal system: very rarely - myalgia.
From the side of metabolism: very rarely - an increase in body weight.
Allergic reactions: very rarely - itching, rashes, hives, angioedema, anaphylaxis.
CONTRAINDICATIONS
- terminal stage of renal failure (CC less than 10 ml / min);
- Children's age to 6 years (for tablets);
- Children under 2 years of age (for drops for oral administration);
- Pregnancy;
- Hypersensitivity to the components of the drug, especially in patients with galactosemia or severe intolerance to lactose (for tablets);
- hypersensitivity to levocetirizine or piperazine derivatives.
With caution should be used in chronic renal failure (correction of the dosing regimen is required), in elderly patients (with an age-related decrease in glomerular filtration).
PREGNANCY AND LACTATION
Adequate and strictly controlled clinical studies on the safety of the drug in pregnant women have not been carried out, therefore Xisal В® should not be administered during pregnancy.
Levocetirizine is excreted in breast milk, so if you need to use the drug during lactation, breastfeeding should be discontinued at the time of admission.
In experimental animal studies, there were no direct or indirect adverse effects of levocetirizine on the developing fetus (including in the postnatal period), the course of pregnancy and childbirth also did not change.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in the terminal stage of renal failure (CC less than 10 ml / min).
Patients with chronic kidney failure with CC 49-30 ml / min dose reduced by 2 times (1 tab every other day), with QA 29-10 ml / min dose is reduced by 3 times (1 tablet every 3 days ).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Patients with hepatic insufficiency do not need dose adjustment.
APPLICATION FOR CHILDREN
Contraindicated in children under 6 years (for tablets); in children under 2 years (for drops for oral administration).
Children older than 6 years : daily dose of 5 mg (1 tab. Or 20 drops).
Children aged 2 to 6 years: 1.25 mg (5 drops) 2 times / day; daily dose of 2.5 mg (10 drops).
APPLICATION IN ELDERLY PATIENTS
Since levocetirizine is excreted by the kidneys, when the drug is prescribed for elderly patients, the dose should be adjusted depending on the magnitude of the CC.
SPECIAL INSTRUCTIONS
The patient should be careful when taking the drug and drinking alcohol at the same time.
Impact on the ability to drive vehicles and manage mechanisms
At an objective estimation of ability to driving of motor transport and work with mechanisms it is authentic not revealed any undesirable phenomena at purpose or appointment of a preparation in the recommended dose. Nevertheless, during the treatment period, it is advisable to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: drowsiness (in adults), agitation and anxiety, followed by drowsiness (in children).
Treatment: Immediately after taking the drug, wash the stomach or induce vomiting. It is recommended the appointment of activated charcoal, the conduct of symptomatic and maintenance therapy. There is no specific antidote. Hemodialysis is ineffective.
DRUG INTERACTION
The interaction of levocetirizine with other drugs has not been studied.
When studying the drug interaction of the racemate cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically significant undesirable interaction was detected.
With simultaneous application with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16%, the pharmacokinetic parameters of theophylline do not change.
In a number of cases, with the simultaneous use of levocetirizine with ethanol or drugs that have an inhibitory effect on the central nervous system, it is possible to increase their effect on the central nervous system, although it has been shown that the racemate of cetirizine potentiates the effect of alcohol.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
Tablets should be stored out of the reach of children, dry place at a temperature of no higher than 25 В° C. Shelf life - 4 years.
Drops for ingestion should be stored out of the reach of children, protected from light at a temperature of no higher than 30 В° C. Shelf life - 3 years. After opening the bottle, the expiration date is 3 months.
