Cetirizine DS - instructions for use, dose, side effects, contraindications

Excipients: pregelatinized starch, lactose monohydrate, starch, povidone (K30), sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate.

Sheath: hypromellose, macrogol 6000, titanium dioxide, talc, lacquer aluminum based on the dye of the crimson (Ponso 4R).

Description:Oblong tablets covered with a film coating of red color, with a risk on one side. On the fracture, the core of the tablet is white or almost white in color.

Pharmacotherapeutic group:Anti-allergic agent-H1 histamine receptor blocker.

ATX: & nbsp

E.06.A.E.07 Cetirizine

Pharmacodynamics:

Cetirizine belongs to the group of competitive histamine antagonists, blocks Hi-histamine receptors, has almost no anticholinergic and antiserotonin action. Has a pronounced anti-allergic effect, prevents development and facilitates the course of allergic reactions. Has antipruritic and anti-exsudative effect. Affects the early stage of allergic reactions, and also reduces the migration of inflammatory cells; inhibits the release of mediators involved in the late stage of an allergic reaction. 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). In therapeutic doses, it practically does not have a sedative effect. Against the background of the course, tolerance does not develop.

The effect of the drug begins in 20 minutes (in 50% of patients), after 1 hour (in 95% of patients), and persists for 24 hours.

Pharmacokinetics:

Suction: after ingestion cetirizine quickly and well absorbed from the gastrointestinal tract.The maximum concentration is determined after about 30-60 minutes.

The intake of food does not have a significant effect on the amount of absorption, However, in this case, the rate of absorption is slightly reduced.

Distribution: cetirizine binds to blood plasma proteins by about 93%. The volume of the distribution (V_d) low (0.5 l / kg), the drug inside the cell does not penetrate.

The drug does not penetrate the blood-brain barrier.

Metabolism: cetirizine is poorly metabolized in the liver by O-dealkylation with the formation of an inactive metabolite.

At 10-day application in a dose of 10 mg accumulation of the drug is not observed. Excretion: when the drug is used at a dose of 10 mg, about 60% of cetirizine is excreted unchanged for 24 hours, 10% is excreted in the next 4 days; 10% - is excreted with feces for 5 days. Inactive metabolite is excreted with feces, it is also supposed to excrete with bile. The system clearance is about 54 ml / min.

After a single dose of a single dose, the half-life is about 7-10 hours. In children aged 6 to 12 years, the half-life is reduced to 6 hours, in children from 2 to 6 years, the half-life is about 5 hours, in children from 6 months to 2 years - 3.1 hours.

If the kidney function is impaired (creatinine clearance is below 11-31 ml / min) and in patients, (creatinine clearance less than 7 ml / min), the half-life of the hemoglobin increases by a factor of 3, the clearance decreases by 70%. Against the backdrop of chronic diseases and in elderly patients there is an increase in the half-life of 50% and a decrease in clearance by 40%. In patients with chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), the half-life is prolonged by 50% and the clearance is reduced by 40% (correction of the dosing regimen is required only with the concomitant decrease in the glomerular filtration rate). The drug is practically not removed during hemodialysis. Penetrates into breast milk.

Indications:

- seasonal and year-round allergic rhinitis; allergic conjunctivitis;

- Pollinosis (hay fever);

- urticaria, incl. chronic idiopathic;

- itching allergic dermatoses (including atopic dermatitis, neurodermatitis);

- angioedema.

Contraindications:Increased individual sensitivity to the components of the drug (including hydroxyzine), lactose intolerance, lactase deficiency, glucose-galactose malabsorption. Children under 6 years. Pregnancy, lactation.

Carefully:In chronic renal failure of moderate to severe severity (correction of the dosing regimen is required), as well as in elderly patients (glomerular filtration may be reduced).

Dosing and Administration:

Inside, regardless of food intake, without chewing and washing down with a small amount of water, preferably in the evening.

Adults and children over 12 years of age - 1 tablet (10 mg) once a day.

Children from 6 to 12 years old - 1 tablet (10 mg) - 1 time per day or 1/2 tablet (5 mg) 2 times a day.

With renal insufficiency should reduce the recommended dose in 2 times.

When a violation of liver function it is necessary to select a dose individually, especially with simultaneous renal failure.

Elderly patients with normal renal function, dose adjustment is not required.

Side effects:

Usually cetirizine is transferred well.

In some cases, weakness, headache, dizziness, drowsiness, fatigue, anxiety, increased motor activity, migraine, dry mouth, disorders of the gastrointestinal tract in the form of dyspepsia, abdominal pain, flatulence.

The intensity of the aforementioned side effects can be reduced by dividing the daily dose into 2 doses.

Hypersensitivity reactions (skin rash, Quincke's edema) are extremely rare (< 2%).

Overdose:

Symptoms: taking the drug once in a dose of more than 50 mg can be accompanied by signs of intoxication in the form of drowsiness, anxiety and increased irritability, possibly the appearance of signs of anticholinergic action in the form of urine retention, dry mouth, constipation.

Treatment: cause vomiting, rinse the stomach, take Activated carbon, immediately consult a doctor.

There is no specific antidote. Hemodialysis is ineffective.

Interaction:

Clinically significant interactions of cetirizine with other drugs have not been established.

Joint application with theophylline (400 mg / day) leads to a decrease in the total clearance of cetirizine (theophylline kinetics does not change).

Special instructions:

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

It is not recommended simultaneous use of drugs that depress the central nervous system.

Data on the interaction of cetirizine with alcohol have not been obtained to date, despite this, the use of alcoholic beverages during treatment with cetirizine is not recommended.

Form release / dosage:

Film-coated tablets, 10 mg.

Packaging:For 10 tablets per blister AL / PVC, 1 blister together with instructions for medical use in a cardboard box.

Storage conditions:In dry, dark place at a temperature of 15 to 25 ° C Keep out of reach of children!

Shelf life:

3 years. Do not use after the expiration date stated on the package

Terms of leave from pharmacies:Without recipe

Registration number:LSR-000833/10

Date of registration:09.02.2010

The owner of the registration certificate:Danafa Pharmaceutical Joint Stock Company Danafa Pharmaceutical Joint Stock Company Vietnam

Manufacturer: & nbsp

DANAPHA PHARMACEUTICAL, Joint Stock Company Vietnam

Representation: & nbspDominanta-Service CJSCDominanta-Service CJSC

Information update date: & nbsp12.10.2015

Illustrated instructions

Instructions

Cetirizine DS (Cetirizine DS)