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

Excipients: glycerol 100.00 mg, sucrose 450.00, benzoic acid 1.50 mg, disodium edetate 1.00 mg, sorbitol 200.00 mg, sodium citrate 1.00 mg, fruit flavoring 2.07 mg, water purified to 1 ml.

Description:

Colorless to go colorless with a slightly yellowish hue, a clear liquid with a pleasant fruity odor, free of visible particles. Insignificant opalescence is allowed.

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 to cooling (with cold urticaria). Reduces histamine-induced bronchoconstriction with bronchial asthma of the lung course.

Virtually no anticholinergic and antiserotonin action.

In therapeutic doses, it practically does not cause sedation. The onset of the effect after a single dose of 10 mg cetirizine - 20 minutes, lasts more than 24 hours. Against the background of course treatment, tolerance to antihistamine effect, 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 the maximum concentration (TFROM_m_Oh) after oral administration - about 1 hour.The food does not affect the fullness of the intake (AUC), but lengthens the TC for 1 h_m_Oh and reduces the maximum concentration (C_m_Oh) by 23%. When taken at a dose of 10 mg once a day for 10 days, the equilibrium concentration of the drug (Css) in plasma 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 5-60 mg. The volume of distribution is 0.5 l / kg.

In small amounts, it is 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). Citirizine is not cumulated. About 2/3 of the drug is excreted unchanged by the kidneys and about 10% - with caloric masses.

Systemic clearance - 53 ml / min. The half-life (T_1/2) in adults - 10 hours, in children 6-12 years - 6 h, 2-6 years - 5 hours, 0.5-2 years - 3.1 hours. In elderly patients T_1/2increases by 50%, systemic clearance is reduced by 40% (decreased kidney function).

In patients with impaired renal function (creatinine clearance below 40 ml / min), the clearance of the drug decreases, and T_1/2lengthened (for example, in patients on hemodialysis, the total clearance is reduced by 70% and is 0.3 ml / min / kg, and T_1/2lengthened 3-fold), which requires a corresponding change in the dosage regimen.

Virtually not removed during hemodialysis.

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

Indications:

- Seasonal and all-the-year-round allergic rhinitis;

- allergic conjunctivitis;

- Pollinosis (hay fever);

- urticaria, including chronic idiopathic urticaria;

- itching allergic dermatoses (atopic dermatitis, neurodermatitis);

- angioedema (angioedema) (angioedema).

Contraindications:

- Hypersensitivity (including hydroxyzine);

- pregnancy, lactation;

- children's age until 2-years old.

Carefully:

Chronic renal failure (with moderate to severe severity, correction of the dosing regimen is required), elderly age (glomerular filtration may be reduced).

Dosing and Administration:

Inside, regardless of food intake, washed down with a small amount of water, preferably in the evening.

Adults and children over 6 years of age - 10 mg (10 ml of syrup) once a day or 5 mg (5 ml of syrup) 2 times a day.

Children 2-6 years old - 5 mg (5 ml syrup) once a day or 2.5 mg (2.5 ml syrup) 2 times a day, depending on the severity of the b-response state.

In patients with decreased renal function (creatinine clearance 30-49 ml / min) is prescribed 5 mg / day (5 ml syrup), with severe chronic renal failure (creatinine clearance 10-30 ml / min) - 5 mg / day (5 ml syrup) every other day.

Elderly patients with normal renal function, no dose adjustment is required.

Side effects:

In some cases, possible: drowsiness, dry mouth; rarely - headache, dizziness, migraine, discomfort in the gastrointestinal tract (dyspepsia, abdominal pain, flatulence), allergic reactions (angioedema, rash, hives, itching).

Overdose:

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

Treatment: gastric lavage, prescription of symptomatic medicines. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

Pharmacokinetic interaction with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam and glipizide was not detected.

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

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

Special instructions:

When the dose is exceeded 10 mg / day, the ability for rapid reactions may worsen.

In recommended doses does not enhance the effect of ethanol (at a concentration of no more than 0,8 g / l), nevertheless it is recommended to abstain fromt its use during treatment.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Syrup, 1 mg / ml.

Packaging:

For 30 or 60 ml of the drug in dark glass bottles with a screw mouth, sealed with screw caps of polypropylene white with a gasket,with the control of the first autopsy and the child safety fuse, complete with a measuring spoon.

Each bottle, along with instructions for use, is placed in a cardboard box.

Storage conditions:

In a dry place, at a temperature of no higher than 25 ° C.

Shelf life:

2 of the year.

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

Terms of leave from pharmacies:Without recipe

Registration number:LSR-010597/08

Date of registration:25.12.2008

Expiration Date:Unlimited

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDr. Reddy`c Laboratoris Ltd.Dr. Reddy`c Laboratoris Ltd.

Information update date: & nbsp10.01.2017

Illustrated instructions

Instructions

Cetrin® (Cetrine)