Universal reference book for medicines
Name of the preparation: CETIRIZINE (CETIRIZINE)

Active substance: cetirizine

Type: The blocker of histamine H 1 -receptors.
Anti-allergic drug
Manufacturer: ВЕРТЕКС (Russia)
Composition, form of production and packaging
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The tablets covered with a film membrane of white or almost white color, round, biconcave; on the cross section - the core is white or almost white.
1 tab.

cetirizine dihydrochloride 10 mg

Excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, magnesium stearate, silicon dioxide colloid.

Sheath composition: [hypromellose, talc, titanium dioxide, macrogol 4000] or [dry film membrane dry, containing hypromellose, talc, titanium dioxide, macrogol 4000].

10 pieces.
- packings of cellular contour (1) - packs cardboard.
10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (3) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2011.

PHARMACHOLOGIC EFFECT

A competitive histamine antagonist, a hydroxyzine metabolite, blocks H 1 -gistamine receptors.
Prevents development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action. Affects the early stage of allergic reactions, limits the release of inflammatory mediators in the late stage of an allergic reaction, reduces the migration of eosinophils, neutrophils and basophils. 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).

Virtually no anticholinergic and antiserotonin action.
In therapeutic doses, it practically does not cause sedation. The onset of action after a single dose of 10 mg of cetirizine - after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients) continues for more than 24 hours. Against the background of course treatment, tolerance to antihistaminic effects of cetirizine does not develop. After the cessation of treatment, the effect lasts up to 3 days.
PHARMACOKINETICS

Quickly absorbed from the gastrointestinal tract, time to reach C max after ingestion - 1 hour. Food does not affect the completeness of absorption (AUC), but lengthens for 1 hour the time to reach C max and reduces the C max by 23%.
When administered at a dose of 10 mg 1 time / day for 10 days the equilibrium concentration in the plasma is 310 ng / ml and is noted after 0.5-1.5 h after administration. The connection with plasma proteins is 93% and does not change with the concentration of cetirizine in the range of 25-1000 ng / ml. The pharmacokinetic parameters of cetirizine change linearly when administered in a dose of 5-60 mg. V d - 0.5 l / kg. In small amounts, it is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other H 1 -gistaminic receptor blockers metabolized in the liver involving the cytochrome P450 system). Do not cumulate. 2/3 of the drug is excreted unchanged by the kidneys and about 10% - through the intestine.
Systemic clearance - 53 ml / min.
T 1/2 in adults - 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, T 1 / 2 increases by 50%, systemic clearance is reduced by 40% (decreased kidney function).
In patients with impaired renal function (clearance of creatinine below 40 ml / min), the clearance of the drug decreases, and T 1/2 is lengthened (for example, in patients on hemodialysis, the total clearance is reduced by 70% and is 0.3 ml / min / kg, and T 1/2 is extended 3 times), which requires a corresponding change in the dosage regimen.

In patients with chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), the elongation of T 1/2 is 50% and the overall clearance is reduced by 40% (correction of the dosing regimen is required only with the concomitant decrease in the glomerular filtration rate).
Penetrates into breast milk.
INDICATIONS

- seasonal and year-round allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, congestion hyperemia);

- urticaria (including chronic idiopathic urticaria);

- hay fever (hay fever);

- itching;

- angioedema (edema of Quincke);

itching allergic dermatosis.

DOSING MODE

Inside, regardless of food intake, without chewing and drinking with a sufficient amount of liquid, 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.
SIDE EFFECT

The drug is usually well tolerated.
Adverse events occur rarely and have a transient nature.
On the part of the digestive system: dry mouth, indigestion.

From the nervous system: dizziness, headache, drowsiness, fatigue, agitation, migraine.

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

CONTRAINDICATIONS

- decreased renal function (creatinine clearance 30-49 ml / min);

- chronic renal failure;

- children's age till 6 years;

- Pregnancy;

- lactation period;

- Hypersensitivity to cetirizine, other components of the drug, hydroxyzine.

With caution: the elderly (possibly reducing glomerular filtration).

PREGNANCY AND LACTATION

It is not recommended to use the drug during pregnancy.
Because Cetirizine penetrates into breast milk, it is not prescribed during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindicated:

- decreased renal function (creatinine clearance 30-49 ml / min);

chronic renal failure.

APPLICATION FOR CHILDREN

Children over the age of 6 years (with a body weight of more than 30 kg) - 1 tab.
1 time / day.
Contraindicated in children under 6 years.

APPLICATION IN ELDERLY PATIENTS

With caution: the elderly (possibly reducing glomerular filtration).

SPECIAL INSTRUCTIONS

It is not recommended simultaneous use with alcohol and drugs that depress the central nervous system.

Influence on the ability to drive vehicles and control mechanisms:

During the treatment period it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
When the dose is exceeded 10 mg / day, the ability for rapid reactions may worsen.
OVERDOSE

Symptoms (when taking a single dose of 50 mg): dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability.

Treatment: gastric lavage, symptomatic therapy.
A specific antidote has not been identified. Hemodialysis is ineffective.
DRUG INTERACTION

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

Myelotoxic drugs increase manifestations of hematoxicity of the drug.

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

TERMS OF RELEASE FROM PHARMACY

The drug is approved for use as a means of OTC.

TERMS AND CONDITIONS OF STORAGE

Keep the drug in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life - 2 years.

Do not use after expiry date.

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