CETIRINAKS

Active material: Cetirizine
When ATH: R06AE07
CCF: Gistaminovыh blocker H₁-receptors. Allergy medication
ICD-10 codes (testimony): H10.1, J30.1, J30.3, L20.8, L23, L24, L28.0, L29, L30.0, L50, T78.3
When CSF: 13.01.01.02
Manufacturer: Actavis hf. (Iceland)

Pharmaceutical form, composition and packaging

◊ Pills, coated white or nearly white, lenticular, ellipsoidal, scored on one side.

Excipients: microcrystalline cellulose, lactose monohydrate, krospovydon, colloidal silicon dioxide, magnesium stearate.

The composition of the shell: gipromelloza, macrogol stearate, microcrystalline cellulose, propylene glycol, Titanium dioxide (E171).

7 PC. – blisters (1) – packs cardboard.

Pharmacological action

Blocker peripheral histamine H₁-receptors. Competitive antagonist of histamine, metabolite gidroksizina. It prevents the development and facilitates the allergic reactions, It has antipruritic and antiexudative action. It affects the early stage of allergic reactions, limits the release of inflammatory mediators late phase allergic reactions, reduces the migration of eosinophils, basophils, neutrophils and.

Decreases capillary permeability, prevents the development of edema, relieves smooth muscle spasm. Eliminates skin reaction to the introduction of histamine, specific allergens, and cooling (when cold urticaria).

Virtually no anticholinergic action and antiserotoninovogo. At therapeutic doses do not cause sedation.

The onset of action after a single administration of the drug at a dose 10 mg observed after 20 m (in 5% patients), through 60 m (in 95% patients), the duration of action of the drug more 24 no. Against the background of a course of treatment tolerance does not develop.

After cessation of treatment effect persists until 3 d.

Pharmacokinetics

Absorption

Cetirizine is rapidly absorbed from the gastrointestinal tract.

C_max plasma levels achieved after 1 hours after ingestion. Simultaneous food intake does not affect the degree of absorption of the drug, but lengthens the time to reach C_max on 1 h and lowers C_max on 23%.

Distribution

Plasma protein binding is 93% and does not change when the concentration of cetirizine in the range 25-1000 ng / ml. The pharmacokinetic parameters of cetirizine vary linearly in appointing him a dose of 5 mg 60 mg.

Before the drug at a dose of 10 mg 1 times / day for 10 days C_ss in plasma observed after 0.5-1.5 h and is 310 ng / ml.

V_d is about 0.5 l / kg. Cetirizine passes into breast milk.

Metabolism

Cetirizine in small amounts in the liver is metabolized by O-dealkylation with a pharmacologically inactive metabolite (Unlike other histamine H₁-receptors, metabolized in the liver involving the cytochrome P₄₅₀).

The drug does not cumulate.

Deduction

2/3 the dose of cetirizine is excreted unchanged by the kidneys, and about 10% – with feces. Systemic clearance of cetirizine 53 ml / min. T_1/2 in adults is 7-10 no, in children 6-12 years - 6 no, aged 2-6 years - 5 no.

Pharmacokinetics in special clinical situations

Elderly patients T_1/2 increases by 50%, systemic clearance is reduced by 40% (because of declining renal function).

In renal insufficiency (CC less than 40 ml / min) systemic clearance of the drug decreases, T_1/2 lengthens (so patients, hemodialysis, systemic clearance is reduced by 70% and is 0.3 ml / min / kg, a T_1/2 lengthened in 3 times), that requires appropriate correction dosing regimen.

In chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis) marked elongation T_1/2 of cetirizine 50% and a reduction in the systemic clearance 40% (correction mode is only required with a corresponding decrease in glomerular filtration rate).

Cetirizine is practically not removed by hemodialysis.

Testimony

- Seasonal and perennial allergic rhinitis and conjunctivitis (itch, chikhaniye, rhinorrhea, lacrimation, conjunctival hyperemia);

- Urticaria (incl chronic idiopathic urticaria);

- Hay fever (hay fever);

- Angioedema;

- Itchy allergic dermatitis.

Dosage regimen

Adults and children over the age of 6 years appoint 10 mg (1 tab.) 1 time / day or 5 mg (1/2 tab.) 2 times / day.

Patients with impaired renal function (KK from 30 to 49 ml / min) appointed 5 mg / day, at chronic renal failure, severe (KK from 10 to 29 ml / min) 5 mg / day every other day.

The tablets are taken orally, with a little water.

Side effect

From the digestive system: dry mouth, discomfort in the abdomen.

CNS: headache, dizziness, migraine.

Allergic reactions: hives, angioedema, itching, skin rash.

Contraindications

- Lack of lactase;

- Galactosemia;

- Glucose galaktoznыy syndrome malyabsorbtsii;

- Children up to age 6 years;

- Pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to the drug.

FROM caution should be prescribed to elderly patients, patients with chronic renal failure.

Pregnancy and lactation

Tsetirinaks is contraindicated during pregnancy and lactation (breast-feeding).

Cautions

If you exceed the daily dose 10 mg marked decrease in the ability to fast reactions.

It should be taken into account, that the CRF moderate and severe requires correction mode.

At recommended doses, the drug does not increase the effect of ethanol (at a concentration of no more than 0.8 g / l). However, it is recommended to abstain from alcohol during treatment with the drug Tsetirinaks.

Effects on ability to drive vehicles and management mechanisms

During treatment Tsetirinaksom should refrain from activities potentially hazardous activities, require increased attention and psychomotor speed reactions.

Overdose

Symptoms: in single dose of the drug at a dose of 50 mg developing sleepiness, anxiety, irritability, urinary retention, dry mouth, constipation.

Treatment: gastric lavage, administration of activated charcoal; if necessary, symptomatic therapy. No specific antidote. Hemodialysis nyeeffyektivyen.

Drug Interactions

Pharmacokinetic interactions of cetirizine with pseudoephedrine, cimetidine, ketoconazole, Erythromycin, Azithromycin, diazepamom, glipizide not established.

When concomitant administration of cetirizine with theophylline (400 mg / day) reduced systemic clearance of cetirizine. When this does not change the pharmacokinetics of theophylline.

Conditions of supply of pharmacies

The drug is resolved to application as an agent Valium holidays.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 3 year.