Cetrine, pills 10mg 30pcs

Composition

Each film-coated tablet contains:

Active ingredient:

cetirizine dihydrochloride 10 mg.

Auxiliary substances:

lactose,

corn starch,

povidone (K-30),

magnesium stearate;

film coating:

hypromellose,

macrogol 6000,

titanium dioxide,

talc,

sorbic acid,

polysorbate 80,

dimethicone.

Pharmacological action

Pharmacodynamics competitive histamine antagonist, a metabolite of hydroxyzine, blocks H1-histamine receptors. It prevents the development and eases the course of allergic reactions, has an antipruritic and anti-exudative effect. It affects the early stage of allergic reactions, limits the release of inflammatory mediators at the “late” stage of an allergic reaction, and reduces the migration of eosinophils, neutrophils, and basophils. Reduces capillary permeability, prevents the development of tissue edema, relieves smooth muscle spasm. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as to cooling (with cold urticaria). Reduces histamine-induced bronchoconstriction in mild bronchial asthma. Practically does not have anticholinergic and antiserotonin effects. In therapeutic doses, it practically does not cause sedation. The beginning of the effect after a single dose of 10 mg of cetirizine – 20 minutes, lasts more than 24 hours. During the course of treatment, tolerance to the antihistamine action of cetirizine does not develop. After discontinuation of treatment, the effect persists for up to 3 days. Pharmacokinetics Rapidly absorbed from the gastrointestinal tract, the time to reach the maximum concentration (TCmax) after oral use is about 1 h. Food does not affect the fullness of absorption (AUC), but it lengthens the TCmax by 1 h and reduces the maximum concentration (Cmax) by 23%. When taken at a dose of 10 mg once a day for 10 days, the steady-state concentration of the drug (Css) in plasma is 310 ng / ml and is noted 0.5-1.5 hours after use. The binding to plasma proteins is 93% and does not change at cetirizine concentrations in the range of 25-1000 ng / ml. The pharmacokinetic parameters of cetirizine vary linearly when administered at 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 H1-histamine receptor blockers that are metabolized in the liver with the participation of the cytochrome P450 system). Cetirizine does not accumulate. About 2/3 of the drug is excreted unchanged by the kidneys and about 10% – with feces. Systemic clearance – 53 ml/min. The half-life (T1 / 2) in adults is 10 hours, in children 6-12 years-6 hours,2-6 years-5 hours,0.5-2 years-3.1 hours. In elderly patients, T1 / 2 increases by 50%, systemic clearance decreases by 40% (decreased renal function). In patients with impaired renal function (creatinine clearance below 40 ml / min), the drug clearance decreases, and T1 / 2 is prolonged (for example, in patients on hemodialysis, the total clearance decreases by 70% and amounts to 0.3 ml / min / kg, and T1 / 2 is extended by 3 times), which requires a corresponding change in the dosage regimen. It is practically not removed during hemodialysis. In patients with chronic liver diseases (hepatocellular, cholestatic, or biliary cirrhosis), T1/2 is prolonged by 50% and total clearance is reduced by 40% (dosage adjustment is required only with a concomitant decrease in glomerular filtration rate). Penetrates into breast milk.

Indications

• Seasonal and year-round allergic rhinitis;
• allergic conjunctivitis;
• pollinosis (hay fever);
• urticaria, including chronic idiopathic urticaria;
• pruritic allergic dermatoses (atopic dermatitis, neurodermatitis);
• angioedema (angioedema).

Use during pregnancy and lactation

Pregnancyin the analysis of prospective data on pregnancy outcomes, there were no cases of malformations, embryonic and neonatal toxicity with a clear causal relationship. Animal studies have not revealed any direct or indirect adverse effects of cetirizine on the developing fetus( including in the postnatal period), the course of pregnancy and childbirth. There have been no controlled clinical studies on the safety of the drug during pregnancy, so cetirizine should not be used during pregnancy. Breast-feeding Cetirizine is excreted in breast milk at concentrations representing 25% to 90% of the drug’s plasma concentration, depending on the time of use. During breastfeeding, the drug is used after consulting a doctor, if the intended benefit to the mother exceeds the potential risk to the child. Fertility Available data on effects on human fertility are limited, but no negative effects on fertility have been identified.

Contraindications

• Hypersensitivity (including to hydroxyzine);
• pregnancy, breast-feeding;
• children under 6 years of age (for this dosage form).

With caution: Chronic renal failure (moderate and severe severity – dosage adjustment is required), elderly age (glomerular filtration rate may decrease).

Side effects

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

No pharmacokinetic interactions were observed with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, and glipizide. Co-use with theophylline (400 mg / day) resulted in a 16% decrease in the total clearance of cetirizine (theophylline kinetics did not change).

How to take, course of use and dosage

Inside, regardless of food intake, without chewing, tablets are washed down with 200 ml of water. Adults – 10 mg (1 tab. ) 1 time a day or 5 mg (1/2 tab. ) 2 times a day. Children older than 6 years – 5 mg (1/2 tab. ) 2 times a day or 10 mg (1 tab. ) 1 time a day. In patients with reduced renal function (creatinine clearance 30-49 ml/min),5 mg/day (1/2 tab. ) is prescribed, in patients with severe chronic renal failure (creatinine clearance 10-30 ml / min) – 5 mg/day (1/2 tab. ) every other day.

Overdose

Symptoms:

drowsiness; with a significant overdose of the drug (exceeding the therapeutic dose by 30-40 times in adults and children) – drowsiness, restlessness, itching, rash, urinary retention, fatigue, tremor, tachycardia.

In all cases, complete normalization of the condition was observed.

Treatment:

gastric lavage; if necessary, symptomatic therapy. There is no specific antidote.

Hemodialysis is ineffective.

Description

Round biconvex tablets, film-coated in white or almost white color, with a risk on one side. On a cross-section, the core is white to almost white in color.

Special instructions

If the dose is exceeded 10 mg/day, the ability to react quickly may worsen.

In the recommended doses, it does not enhance the effect of ethanol (at its concentration of no more than 0.8 g/l),

however, it is recommended to refrain from using it during treatment.

For children (from 2 years old) Cetrine® is used in syrup form.

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

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children!

Shelf life

2 years

Active ingredient

Cetirizine

Dosage form

Tablets

Description

Children over 6 years old, For adults

Indications

Hay Fever, Neurodermatitis, Allergies, Allergic Rhinitis, Allergic Conjunctivitis, Dermatosis, Urticaria