Cetirizine dihydrochloride 10 mg Auxiliary substances: microcrystalline cellulose, lactose monohydrate, crospovidone, magnesium stearate, colloidal silicon dioxide. Shell composition: [hypromellose, talc, titanium dioxide, macrogol 4000] or [dry white film coating containing hypromellose, talc, titanium dioxide, macrogol 4000].
A competitive histamine antagonist, a hydroxyzine metabolite, blocks histamine H1 receptors. Prevents the development and facilitates the course of allergic reactions, has antipruritic and anti-exudative action. It affects the early stage of allergic reactions, limits the release of inflammatory mediators at the late stage of an allergic reaction, reduces the migration of eosinophils, neutrophils and basophils. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as cooling (with cold urticaria). Practically no anticholinergic and antiserotonin action. In therapeutic doses, practically does not cause a sedative effect. Onset of action after a single dose of 10 mg cetirizine - after 20 min (in 50% of patients) and after 60 min (in 95% of patients) lasts more than 24 hours. Against the background of a course treatment, tolerance to the antihistamine effect of cetirizine does not develop. After cessation of treatment, the effect lasts up to 3 days.
It is rapidly absorbed from the gastrointestinal tract, the time to reach Cmax after ingestion is 1 hour. Food does not affect the completeness of absorption (AUC), but it lengthens the time to reach Cmax by 1 h and reduces the value of Cmax by 23%. When taken in a dose of 10 mg 1 time / day for 10 days, the equilibrium concentration in plasma is 310 ng / ml and is noted 0.5–1.5 h after administration. Communication with plasma proteins - 93% and does not change when the concentration of cetirizine in the range of 25-1000 ng / ml. The pharmacokinetic parameters of cetirizine change linearly with its appointment in a dose of 5-60 mg. Vd - 0.5 l / kg. In small quantities, it is metabolized in the liver by O-dealkylation with the formation of a pharmacologically inactive metabolite (unlike other H1-histamine receptor blockers metabolized in the liver using the cytochrome P450 system). Does not accumulate. 2/3 of the drug is excreted unchanged by the kidneys and about 10% through the intestines. Systemic clearance - 53 ml / min.T1 / 2 in adults - 7-10 hours, in children 6-12 years old - 6 hours, in children 2-6 years old - 5 hours, in children from 6 months to 2 years old - 3 hours. In elderly patients, T1 / 2 increases by 50%, systemic clearance is reduced by 40% (reduced kidney function). In patients with impaired renal function (creatinine clearance below 40 ml / min), the clearance of the drug decreases and T1 / 2 lengthens (for example, in patients on hemodialysis, the total clearance decreases by 70% and is 0.3 ml / min / kg, and T1 / 2 is extended by 3 times), which requires a corresponding change in the dosage regimen. In patients with chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), T1 / 2 lengthened by 50% and the total clearance decreased by 40% (correction of the dosing regimen is required only with a concomitant decrease in glomerular filtration rate). Penetrates into breast milk.
- seasonal and perennial allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, tearing, conjunctival hyperemia); - urticaria (including chronic idiopathic urticaria); - hay fever (pollinosis); - itching; - angioedema (angioedema); - pruritic allergic dermatosis.
- reduced kidney function (creatinine clearance 30-49 ml / min); - chronic renal failure; - children's age up to 6 years; - pregnancy; - lactation period; - hypersensitivity to cetirizine, other components of the drug, hydroxyzine. With care: advanced age (reduction of glomerular filtration is possible).
Use during pregnancy and lactation
The use of the drug during pregnancy is not recommended. Since Cetirizine passes into breast milk, it is not prescribed during lactation.
Dosage and administration
Inside, regardless of the meal, not chewing and drinking plenty of fluids, preferably in the evening. Adults and children over the age of 6 years (with a body weight of more than 30 kg) - 1 tab. 1 time / day
The drug is usually well tolerated. Side effects are rare and have a transient nature. On the part of the digestive system: dry mouth, dyspepsia. Nervous system disorders: dizziness, headache, drowsiness, fatigue, agitation, migraine. Allergic reactions: angioedema, skin rashes, itching, urticaria.
Symptoms (when taking a single dose of 50 mg): dry mouth, drowsiness, urinary retention, constipation, anxiety, irritability. Treatment: gastric lavage, symptomatic therapy. The specific antidote is not revealed. Hemodialysis is ineffective.
Interaction with other drugs
Combined use with theophylline (400 mg / day) leads to a decrease in the total clearance of cetirizine (the kinetics of theophylline does not change). Myelotoxic drugs increase the hematoxicity of the drug. No clinically significant interactions with other drugs (pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide) were detected.
Not recommended simultaneous use with alcohol and drugs that depress the central nervous system. Impact on the ability to drive motor vehicles and control mechanisms: During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration of attention and quickness of psychomotor reactions. If you exceed the dose of 10 mg / day, the ability for rapid reactions may deteriorate.