Composition, form of production and packaging
? The tablets covered with a film shell of white color, oblong, with biconcave surfaces, with one-sided risk and engraving "Y" on both sides of the risks.
1 tab.
cetirizine dihydrochloride 10 mg
Excipients: microcrystalline cellulose, lactose monohydrate, silicon dioxide colloid, magnesium stearate; OpadraiВ® Y-1-7000 (hypromellose (E464), titanium dioxide (E171), macrogol 400).
7 pcs. - blisters (1) - packs of cardboard.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
? Drops for oral administration are colorless, transparent, with the smell of acetic acid.
1 ml
cetirizine dihydrochloride 10 mg
Excipients: glycerol, propylene glycol, sodium saccharinate, methylparabenzene, propyl parabenzene, sodium acetate, glacial acetic acid, purified water.
10 ml - a bottle of a dropper of dark glass (1) - packs cardboard.
20 ml - a bottle of a dropper of dark glass (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2012.
PHARMACHOLOGIC EFFECT
Anti-allergic drug. The blocker of histamine H 1 -receptors, a competitive histamine antagonist, a metabolite of hydroxyzine. Prevents development and facilitates the course of allergic reactions, has antipruritic and antiexudative action.
Affects the early histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators in the late stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils, stabilizes the membranes of mast cells. Reduces the permeability of capillaries, prevents the development of edema of tissues, relieves spasm of smooth muscles. Eliminates the skin reaction to the administration of histamine, specific allergens, and also to cooling (with "cold" urticaria). Reduces histamine-induced bronchoconstriction in bronchial asthma of mild course.
Virtually no anticholinergic and antiserotonin action. In therapeutic doses, it practically does not have a sedative effect.
After a single dose of cetirizine at a dose of 10 mg, the onset of the effect is observed after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients), the effect lasts more than 24 hours. Against the background of course treatment, tolerance to antihistamine effect of cetirizine does not develop. After the cessation of treatment, the effect lasts up to 3 days.
PHARMACOKINETICS
The pharmacokinetic parameters of cetirizine vary linearly.
Suction
After ingestion, the drug is quickly and completely absorbed from the digestive tract. In adults, after a single dose of the drug at a therapeutic dose, C max in plasma is achieved after 1 В± 0.5 h and is 300 ng / ml. The intake of the drug with food does not affect the amount of absorption.
Distribution
Cetirizine binds to plasma proteins by 93 В± 0.3%. V d - 0.5 l / kg.
When taking the drug at a dose of 10 mg for 10 days cumulation of cetirizine is not observed.
Metabolism
In small amounts, it is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other histamine H 1 -receptor blockers metabolized in the liver with the participation of cytochrome P450 isoenzymes).
Excretion
T 1/2 in adults is approximately 10 hours. About 2/3 of the dose is excreted by the kidneys unchanged.
Pharmacokinetics in special clinical cases
T 1/2 in children aged 6-12 years - 6 hours; in children 2-6 years - 5 hours; in children aged 6 months to 2 years - 3.1 hours.
In elderly patients and patients with chronic liver diseases, a single dose of 10 mg of T1 is increased by approximately 50%, and systemic clearance is reduced by 40%.
In patients with mild renal insufficiency (KK> 40 ml / min), pharmacokinetic parameters are similar to those in patients with normal renal function.
In patients with moderate renal insufficiency and in patients on hemodialysis (CC <7 ml / min), when taking the drug inside at a dose of 10 mg, T 1/2 increases by 3 times, and the overall clearance is reduced by 70% relative to patients with normal renal function, which requires a corresponding change in the dosing regimen.
Cetirizine is practically not removed from the body during hemodialysis.
INDICATIONS
- treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis such as itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia;
- hay fever (hay fever);
- urticaria (including chronic idiopathic urticaria);
- Quincke's edema;
- Other allergic dermatoses (including atopic dermatitis), accompanied by itching and rashes.
DOSING MODE
The drug is prescribed inside.
Adults and children over 6 years of age are prescribed in a dose of 10 mg (1 table or 20 drops) / day. Adults-10 mg once a day; children - 5 mg 2 times / day or 10 mg 1 time / day. Sometimes an initial dose of 5 mg may be sufficient to achieve a therapeutic effect.
Children aged 2 to 6 years are prescribed 2.5 mg (5 drops) 2 times / day or 5 mg (10 drops) 1 time / day.
Children aged 1 to 2 years are prescribed 2.5 mg (5 drops) up to 2 times / day.
Children aged 6 months to 12 months are prescribed 2.5 mg (5 drops) 1 time / day.
With renal failure and in elderly patients, the dose of the drug should be adjusted depending on the magnitude of the CC.
QA can be calculated from the serum creatinine concentration using the following formula:
For men: CK (ml / min) = [140 - age (years)] x body weight (kg) / 72 x serum creatinine (mg / dL);
KK for women can be calculated by multiplying the obtained value by a factor of 0.85.
Adults with renal and hepatic impairment dose set according to the following table.
Renal insufficiency KK (ml / min) Dosing regimen
Norm? 80 10 mg / day
Light 50-79 10 mg / day
Average 30-49 5 mg / day
Severe <30 5 mg every other day
Terminal stage - patients on dialysis <10 The drug is contraindicated
Patients with a violation of only liver function correction of the dosing regimen is not required.
SIDE EFFECT
From the hemopoietic system: thrombocytopenia.
From the nervous system: drowsiness, dizziness, headache, aggression, agitation, confusion, depression, hallucinations, insomnia, tick, seizures, dyskinesia, dystonia, paresthesia, syncope, tremor.
From the side of the organ of vision: a violation of accommodation, fuzzy vision, nystagmus.
From the cardiovascular system: tachycardia.
On the part of the respiratory system: rhinitis, pharyngitis.
On the part of the digestive system: dry mouth, nausea, abdominal pain, diarrhea, impaired liver function (increased levels of transaminases, alkaline phosphatase, GGT, bilirubin).
From the urinary system: urination disorder, enuresis.
Allergic reactions: itching, rashes, hives, angioedema, hypersensitivity, up to the development of anaphylactic shock.
From the side of metabolism: increase in body weight.
Other: fatigue, asthenia, malaise, swelling.
Side effects develop in very rare cases.
CONTRAINDICATIONS
- terminal stage of renal failure (CC <10 ml / min);
- Pregnancy;
- the period of lactation (breastfeeding);
- hereditary intolerance to galactose, a lack of lactase or a syndrome of glucose-galactose malabsorption;
- Children's age to 6 years (for tablets);
- Children's age to 6 months (for drops);
- hypersensitivity to the components of the drug;
- Hypersensitivity to hydroxyzine.
With caution should prescribe the drug for chronic kidney failure (requires a correction of the dosing regimen), with chronic liver disease, elderly patients (in connection with the possible reduction of glomerular filtration).
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug for chronic renal failure (moderate or severe severity), as well as patients of advanced age (in connection with the possible reduction of glomerular filtration).
With renal failure, the dose decreases depending on the CK.
Contraindicated in the terminal stage of renal failure (CC <10 ml / min).
APPLICATION FOR CHILDREN
Contraindicated in children under 6 years (for tablets), in children up to 6 months (for drops).
APPLICATION IN ELDERLY PATIENTS
With caution should prescribe the drug to elderly patients (in connection with the possible reduction of glomerular filtration).
SPECIAL INSTRUCTIONS
For children from 6 months to 6 years of age, Zirtek В® is prescribed in the form of a drop for ingestion of 10 mg / ml.
Impact on the ability to drive vehicles and manage mechanisms
With an objective assessment of the ability to drive vehicles and manage mechanisms, there were no undesirable reactions detected when taking the drug at the recommended dose. But, nevertheless, during the period of taking the drug, 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: when taking the drug once in a dose of more than 50 mg confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, itching, weakness, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention are possible.
Treatment: immediately after taking the drug, you should wash the stomach or artificially 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
When studying the drug interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically significant undesirable interaction was detected.
With a simultaneous appointment with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16% (theophylline kinetics does not change).
With simultaneous administration with macrolides and ketoconazole, there were no changes on the ECG.
When using the drug in therapeutic doses of data on the interaction with alcohol (at a blood alcohol concentration of 0.5 g / l) is not obtained. Nevertheless, the patient should refrain from drinking alcohol during therapy with the drug in order to avoid oppression of the CNS.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
Tablets should be stored in their original packaging at a temperature not exceeding 30 В° C. Drops for oral administration should be stored at a temperature of no higher than 25 В° C. Shelf life of the drug is 5 years.
The drug should be stored out of the reach of children.
