Cetirizine DC,10 mg 10 pcs

Cetirizine is a competitive histamine antagonist, a metabolite of hydroxyzine, blocks H1-histamine receptors. It prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects. It affects the early stage of allergic reactions, limits the release of inflammatory mediators at the later stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils. It reduces capillary permeability, prevents the development of tissue edema, relieves smooth muscle spasm.

It eliminates the skin reaction to the introduction of histamine, specific allergens and also to cooling (with cold urticaria). It has practically no anticholinergic and antiserotonin action. In therapeutic doses there is practically no sedative effect. Onset of action after a single dose of 10 mg of cetirizine is within 20 minutes (in 50% of patients) and 60 minutes (in 95% of patients), and lasts more than 24 hours. During a course of treatment, tolerance to the antihistamine action of cetirizine does not develop. After discontinuation of treatment the action lasts up to 3 days.

Pharmacokinetics

It is quickly absorbed from the gastrointestinal tract, time to reach Cmax after oral administration – 1 hour. Food does not affect the completeness of absorption (AUC), but prolongs by 1 hour the time to reach Cmax and reduces the Cmax value by 23%. When administered at a dose of 10 mg once daily for 10 days, the equilibrium plasma concentration is 310 ng/ml and is noted 0.5-1.5 hours after administration. The binding to plasma proteins is 93% and does not change at cetirizine concentrations in the range of 25-1000 ng/ml.

The pharmacokinetic parameters of cetirizine change linearly when administered at a dose of 5-60 mg. Vd is 0.5 l/kg. In small amounts it is metabolized in the liver by O-dealkylation to form pharmacologically inactive metabolite (unlike other H1-histamine receptor blockers, which are metabolized in the liver involving the cytochrome P450 system). It does not cumulate. 2/3 of the drug is excreted unchanged by the kidneys and about 10% – through the intestine.

Systemic clearance is 53 ml/minute. T1/2 in adults is 7-10 hours, in children 6-12 years – 6 hours, in children 2-6 years – 5 hours, in children from 6 months to 2 years – 3 hours. In elderly patients T1/2 is increased by 50%, systemic clearance is decreased by 40% (decreased renal function).

In patients with impaired renal function (creatinine clearance below 40 ml/min) the drug clearance decreases and T1/2 is prolonged (so, in patients on hemodialysis total clearance decreases by 70% and is 0.3 ml/min/kg, and T1/2 is prolonged by 3 times), which requires appropriate changes in dosing regimen.

In patients with chronic liver disease (hepatocellular, cholestatic or biliary cirrhosis) a prolongation of T1/2 by 50% and reduction of total clearance by 40% are observed (dosage regimen adjustment is required only in concomitant decrease of glomerular filtration rate). It penetrates into the breast milk.

Indications

Active ingredient

Composition

1 film-coated tablet contains:

Active substance:

Cetirizine dihydrochloride 10 mg.

How to take, the dosage

Cetirizine is taken orally. Adults and children over 6 years of age (with body weight over 30 kg) – 1 tablet once a day.

Interaction

Co-administration with theophylline (400 mg/day) decreases total clearance of cetirizine (the kinetics of theophylline is not changed).

Myelotoxic drugs increase manifestations of hematoxicity of the drug.

No clinically significant interactions with other drugs (pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide) were found.

Special Instructions

The simultaneous use of alcohol and CNS depressant drugs is not recommended.

Impact on the ability to drive and operate machinery:

During treatment, it is necessary to refrain from engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

The ability to react quickly may worsen if the dose of 10 mg/day is exceeded.

Contraindications

With caution: Elderly people (decreased glomerular filtration is possible).

Side effects

The drug Cetirizine is usually well tolerated. Side effects are rare and transient.

Digestive system disorders: dry mouth, dyspepsia.

Nervous system disorders:dizziness, headache, drowsiness, fatigue, agitation, migraine.

Allergic reactions: angioedema, skin rashes, itching, urticaria.

Overdose

Symptoms: A single dose of the drug over 50 mg may be accompanied by signs of intoxication in the form of drowsiness, restlessness and increased irritability; there may be signs of anticholinergic action in the form of urinary retention, dry mouth, constipation.

Treatment:induce vomiting, flush the stomach, take activated charcoal, see a doctor immediately.

There is no specific antidote.

Hemodialysis is ineffective.

Similarities