Cetirinax - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 39.26 mg, lactose monohydrate 117.0 mg, crospovidone 1.70 mg, silicon dioxide colloid 0.34 mg, magnesium stearate 1.70 mg.

Shell: hypromellose 1.08-2.17 mg, macrogol stearate (Polyoxyl-8-stearate) 0.20-0.41 mg, microcrystalline cellulose 0.82-1.63 mg, propylene glycol 0.69-1.38 mg, titanium dioxide (E 171) 0.60-1.21 mg.

Description:

For tablets produced by JSC "Actavis", Iceland: biconcave, ellipsoidal tablets, covered with a film shell of white or almost white color, with a risk on one side.

For tablets produced by "Aktavis UKLimidid", Great Britain: biconcave, ellipsoidal tablets, covered with a film shell of white or almost white color. With the "C" marking on one side of the tablet. On the other side of the tablet there is a risk, on one side of which there is a marking "J", and on the other side marking "E".

The markings "C", "J"and" E "are applied to the tablets by embossing.

Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

E.06.A.E.07 Cetirizine

Pharmacodynamics:

A competitive histamine antagonist, a hydroxyzine metabolite, blocks H₁-gistaminovye receptors. Prevents development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action. Affects the early stage of allergic reactions, restricts the release of inflammatory mediators at the "late" stage of the 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 for 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 cetirizine - after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients), the duration of action is more than 24 hours.

Against the background of course treatment tolerance to the antihistamine effect of cetirizine does not develop. After the cessation of treatment, the effect is preserved up to 3 days.

Pharmacokinetics:

Quickly absorbed from the gastrointestinal tract (GIT). Achieves maximum concentration 1 hour after ingestion. Food does not affect the full suction, but extends to 1 h time to reach the maximum concentration in the blood plasma and reduces the maximum concentration by 23%. When taken at a dose of 10 mg 1 time per day for 10 day, the equilibrium plasma concentration is 310 ng / ml and is noted 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 mg to 60 mg. The volume of distribution is 0.5 l / kg.

In small quantities cetirizine metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other blockers H₁-gistaminovyh receptors, metabolized in the liver with the participation of the cytochrome P system₄₅₀). The drug does not cumulate. 2/3 of the drug is excreted unchanged by the kidneys and about 10% - through the intestine.

Systemic clearance of cetirizine is 53 ml / min. The half-life (T_1/2) in adults is 7-10 hours, in children 6-12 years - 6 hours.

In elderly patients, T_1/2 increases by 50%, systemic clearance is reduced by 40% (decreased kidney function), Cetirizine penetrates into breast milk.

Renal insufficiency. In patients with impaired renal function (creatinine clearance (CK) below 40 ml / min), the clearance of the drug decreases, and T_1/2 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 lengthened 3-fold), which requires a corresponding change in the dosage regimen.

Cetirizine is practically not removed during hemodialysis.

Liver failure. In patients with chronic liver disease (hepatocellular, cholestatic or biliary cirrhosis), an increase in T_1/2 cetirizine by 50% and a reduction in its total clearance by 40% (correction of the dosing regimen is required only with the concomitant decrease in glomerular filtration rate).

With normal kidney and liver function, dose adjustment in elderly patients is not required.

Indications:

Seasonal and all-the-year-round allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia), urticaria (including chronic idiopathic urticaria), pollinosis (hay fever); other allergic dermatoses, including atopic dermatitis, accompanied by itching and rashes; angioedema.

Contraindications:

Hypersensitivity to the drug component (including derivatives of piperazine such as hydroxyzine), lack lactase, galactosemia, glucose-galactose malabsorption syndrome, lactation, infancy (up to 6 years), severe renal impairment (creatinine clearance less than 10 mL / min) .

Carefully:XRandom renal failure (CRF) with CC 10-79 ml / min, chronic liver disease, pregnancy.

Pregnancy and lactation:

During pregnancy, the drug should be used only if the expected benefit to the mother exceeds the potential risk to the fetus.

Because the cetirizine is excreted in breast milk, for the time of taking the drug Cetirinax should be abandoned breastfeeding.

Dosing and Administration:

Inside, the tablets are washed down with a small amount of water.

Adults and children over 6 years of age prescribe 10 mg (1 tablet) 1 time per day or 5 mg (1/2 tablet) 2 times a day.

In patients with decreased renal function (KK - 30-49 ml / min) is prescribed 5 mg / day, with severe CRF (KK - 10-30 ml / min) - 5 mg / day every other day.

Side effects:

Clinical studies have shown that cetirizine in recommended doses minimally affects the central nervous system (CNS). As a rule, it does not affect the daily activity of patients, but some people may experience such symptoms as drowsiness, fatigue, dizziness, headache and paradoxical stimulation of the CNS.

Incidence of adverse reactions: sometimes (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000).

From the hematopoiesis side: very rarely - thrombocytopenia.

From the immune system: rarely - allergic reactions (angioedema, skin rash, hives, itching).

From the side of the central nervous system: sometimes - agitation; rarely convulsions; very rarely - syncope.

Visual disorders: very rarely - oculogic crisis.

From the side of the cardiovascular system: rarely - tachycardia.

From the digestive tract: sometimes - complaints of discomfort and GI disorders.

On the part of the liver: rarely - changes in laboratory parameters of liver function; very rarely - hepatitis.

Other: sometimes - dry mouth; rarely - weight gain.

Overdose:

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

Treatment: Vomiting, rinsing the stomach, prescribing symptomatic medicines. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

The pharmacokinetic interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, and glipizide was not detected.

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

It is recommended that the drug be used with caution together with alcohol, since cetirizine can potentiate its action (see section "Special instructions").

Special instructions:

If the dose exceeds 10 mg / day, the reaction rate may deteriorate.

In recommended doses, the drug does not enhance the effect of ethanol (at a concentration of no more than 0.5 g / l), nevertheless it is recommended to refrain from its use during treatment, as well as from joint intake of drugs depressing the central nervous system.

Patients with CRF of moderate to severe severity require correction of the dosing regimen.

Particular attention should be given to patients with epilepsy and patients who are predisposed to developing convulsive seizures.

Effect on the ability to drive transp. cf. and fur:

When taken in the recommended doses (10 mg per day) does not affect the ability to drive and work with mechanisms. Patients in the period of treatment with Cetirinax should strictly follow the recommended dose of the drug and monitor the possible occurrence of symptoms of drowsiness.

Patients who report symptoms of drowsiness, it is recommended to refrain from driving the car and working with mechanisms.

Form release / dosage:

Tablets, film-coated, 10 mg.

Packaging:

For tablets produced by JSC "Aktovye", Iceland:

7 or 10 tablets in a blister of PVC film and aluminum foil; 1 bliser in a cardboard box with instructions for use.

For tablets produced by "Aktavis UKLimidid", Great Britain:

7 or 10 tablets in a blister aluminum foil / aluminum foil; 1 blister in a cardboard box with instructions for use.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LS-000215

Date of registration:01.03.2010 / 18.05.2012

Expiration Date:Unlimited

The owner of the registration certificate:Actavis PTS ehf GroupActavis PTS ehf Group Iceland

Manufacturer: & nbsp

ACTAVIS hf. Iceland

ACTAVIS UK, Ltd. United Kingdom

Representation: & nbspAktavis, Open Company Aktavis, Open Company

Information update date: & nbsp10.01.2017

Illustrated instructions

Instructions

Cetiriax (Cetirinax)