Zodac oral drops 10mg/ml, 20ml

Composition

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1 ml contains:

Active ingredient:

cetirizine dihydrochloride 10 mg

excipients:  

Methyl parahydroxybenzoate,

propyl parahydroxybenzoate,

glycerol,

propylene glycol,

sodium saccharinate dihydrate,

sodium acetate trihydrate,

ice-cold acetic acid,

purified water.

Pharmacological action

Cetirizine is a metabolite of hydroxyzine, belongs to the group of competitive histamine antagonists and blocks H1-histamine receptors.

In addition to the antihistamine effect, cetirizine prevents the development and eases the course of allergic reactions: at a dose of 10 mg 1 or 2 times a day, it inhibits the late phase of eosinophil aggregation in the skin and conjunctiva of patients subject to atopy. After oral use, the anti-allergic effect of cetirizine continues for 24 hours.

Clinical efficacy and safety:

Studies in healthy volunteers have shown that cetirizine in doses of 5 or 10 mg significantly inhibits the rash and redness response to the introduction of histamine into the skin in high concentrations, but no correlation with effectiveness has been established.

In a 6-week placebo-controlled study involving 186 patients with allergic rhinitis and concomitant mild and moderate bronchial asthma, it was shown that the use of cetirizine at a dose of 10 mg once a day reduces the symptoms of rhinitis and does not affect lung function.

The results of this study confirm the safety of using cetirizine in patients suffering from allergies and mild to moderate bronchial asthma.

A placebo-controlled study showed that cetirizine 60 mg daily for 7 days did not cause clinically significant prolongation of the QT interval. The use of cetirizine at the recommended dose showed an improvement in the quality of life of patients with year-round and seasonal allergic rhinitis.

Children

In a 35-day study involving patients aged 5-12 years, there were no signs of immunity to the antihistamine effect of cetirizine. Normal skin response to histamine was restored within three days after discontinuation of the drug with repeated use.

In a 7-day placebo-controlled trial of cetirizine in the dosage form syrup involving 42 patients aged 6 to 11 months, the safety of its use was demonstrated. Cetirizine was administered at a dose of 0.25 mg / kg twice daily, which approximately corresponded to 4.5 mg per day (the dose range was from 3.4 to 6.2 mg per day).

Use in children from 6 to 12 months is possible only as prescribed by a doctor and under strict medical supervision.

Pharmacokinetics

The pharmacokinetic parameters of cetirizine when used in doses from 5 to 60 mg vary linearly.

Suction

The maximum concentration (Cmax) in blood plasma is reached after 1 ±0.5 hours and is 300 ng / ml.

Different pharmacokinetic parameters, such as the maximum concentration in blood plasma and the area under the concentration-time curve, are homogeneous. Food intake does not affect the completeness of cetirizine absorption, although its rate decreases. The bioavailability of various dosage forms of cetirizine (solution, capsules, tablets) is comparable.

Distribution

Cetirizine binds to plasma proteins by 93 ± 0.3%. The volume of distribution (Vd) is 0.5 l/kg. Cetirizine does not affect the binding of warfarin to proteins.

Cetirizine does not undergo extensive primary metabolism.

Deduction

The elimination half-life (T 1/2) is approximately 10 hours. When using the drug in a daily dose of 10 mg for 10 days, accumulation of cetirizine was not observed. Approximately 2/3 of the dose taken is excreted unchanged in the urine.

Elderly patients

In 16 elderly patients with a single dose of 10 mg, T 1/2 was 50% higher and clearance was 40% lower compared to non-elderly patients.

A decrease in cetirizine clearance in elderly patients is probably associated with a decrease in renal function in this category of patients.

Patients with renal insufficiency

In patients with mild renal insufficiency (creatinine clearance > 40 ml / min), the pharmacokinetic parameters are similar to those in healthy volunteers with normal renal function.

In patients with moderate renal insufficiency and in patients undergoing hemodialysis (CC

For patients with moderate or severe renal insufficiency, an appropriate change in the dosage regimen is required.

Cetirizine is poorly excreted during hemodialysis.

Patients with hepatic insufficiency In patients with chronic liver diseases (hepatocellular, cholestatic, and biliary cirrhosis), with a single dose of 10 or 20 mg of the drug, T 1/2 increases by approximately 50% and clearance decreases by 40% compared to healthy subjects. Dose adjustment is necessary only if the patient with hepatic insufficiency also has concomitant renal insufficiency.

Children

T 1/2 in children from 6 to 12 years is 6 hours, from 2 to 6 years-5 hours, from 6 months to 2 years is reduced to 3.1 hours.

Indications

Indicated in adults and children 6 months and older for relief:

• nasal and ocular symptoms of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis: itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia;
• symptoms of chronic idiopathic urticaria.

Contraindications

• Hypersensitivity to cetirizine, hydroxyzine or piperazine derivatives, as well as other components of the drug;
• end-stage renal failure (creatinine clearance < 10 ml / min);
• children under 6 months of age (due to limited data on efficacy and safety);
• pregnancy.

With caution in

• Chronic renal insufficiency (CC > 10 ml/min, requires correction dosing regimen);
• patients of advanced age (age-related decline in glomerular filtration rate);
• epilepsy and patients with increased convulsive readiness;
• patients with predisposing factors for urinary retention (lesions of the spinal cord, prostatic hyperplasia);
• the period of breastfeeding.

Side effects

From the digestive system:  dry mouth, dyspepsia.

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

Allergic reactions:  skin rash, angioedema, urticaria, pruritus.

Interaction

No drug interactions of cetirizine with other drugs were observed.

Based on the results of the conducted drug interaction studies of cetirizine, in particular, interaction studies with pseudoephedrine or theophylline at a dose of 400 mg per day, no clinically significant interactions were established.

Concomitant use of cetirizine with alcohol and other drugs that depress the central nervous system may further reduce the concentration of attention and speed of reactions, although cetirizine does not enhance the effect of alcohol (at a blood concentration of 0.5 g / l).

How to take, course of use and dosage

Inside, drop in a spoon or dissolve in water.

The amount of water to dissolve the drug should correspond to the amount of liquid that the patient (especially a child) is able to swallow.

The solution should be taken immediately after preparation.

Adults 10 mg (20 drops) 1 time a day.

Elderly patients There will be an increased need to reduce the dosage in elderly patients if renal function is not impaired.

Patients with renal insufficiency Since Zodac® is mainly excreted from the body by the kidneys (see section “Pharmacokinetics”), if alternative treatment is not possible for patients with renal insufficiency, the dosage regimen of the drug should be adjusted depending on renal function (creatinine clearance).

CC for men can be calculated based on the concentration of serum creatinine, using the following formula: :

Dosage in adult patients with renal insufficiency

Patients with impaired hepatic functionin patients with impaired liver function alone, no dosage adjustment is required.In patients with impaired hepatic and renal function, dosage adjustment is recommended (see table above).

DetyPrimenenie in children from 6 to 12 months can only be prescribed by a doctor and under strict medical supervision.

Children from 6 to 12 months 2.5 mg (5 drops) 1 time a day.

Children from 1 year to 6 years 2.5 mg (5 drops) 2 times a day.

Children from 6 to 12 years of age 5 mg (10 drops) 2 times a day.

Children over 12 years of age 10 mg (20 drops) 1 time a day.

Sometimes an initial dose of 5 mg (10 drops) may be sufficient if it allows for satisfactory control of symptoms.

In children with renal insufficiency, the dose is adjusted for creatinine clearance and body weight.

Overdose

The clinical picture observed with an overdose of cetirizine was due to its effect on the central nervous system.

Symptoms: after a single dose of cetirizine 50 mg, the following clinical picture was observed: confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, anxiety, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention.

Treatment: immediately after taking the drug, it is necessary to perform gastric lavage or stimulate vomiting. It is recommended to take activated charcoal, conduct symptomatic and maintenance therapy. There is no specific antidote. Hemodialysis is ineffective.

Special instructions

Due to the potential depressing effects on the central nervous system, caution should be exercised when prescribing Zodak® to children under 1 year of age who have the following risk factors for sudden children death syndrome, such as (but not limited to):

• the syndrome of sleep apnea or sudden children death syndrome children have a brother or sister;
• the mother’s drug abuse or Smoking during pregnancy;
• young maternal age (19 years and younger);
• the abuse of Smoking nurses who care for a child (one pack of cigarettes per day or more);
• children, regularly falling asleep face down and where not laid on the back;
• prematurity (gestational age less than 37 weeks) or born with insufficient body weight (below the 10th percentile from gestational age) children;
• when co-administered drugs, providing a depressing effect on the Central nervous system. The drug contains excipients methylparabenzene and propylparabenzene, which can cause allergic reactions, including delayed type.

Caution should be exercised in patients with spinal cord injury, prostatic hyperplasia, or other predisposing factors to urinary retention, as cetirizine may increase the risk of urinary retention. Caution is recommended when using cetirizine concomitantly with alcohol, although no clinically significant interaction with alcohol was observed at therapeutic doses (at a blood alcohol concentration of 0.5 g / l).

Caution should be exercised in patients with epilepsy and increased convulsive readiness.

A three-day “wash-off” period is recommended before the appointment of allergological tests, since H1-histamine receptor blockers inhibit the development of allergic skin reactions.

Influence on the ability to drive vehicles and work with mechanisms

Objective assessment of the ability to drive vehicles and work with mechanisms did not reliably reveal any adverse events when using Zodak® in the recommended doses. However, patients with signs of drowsiness while taking the drug during treatment should refrain from driving, engaging in potentially dangerous activities or operating mechanisms that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Drops for oral use

Storage conditions

No special storage conditions are required

Shelf life

3 years

Active ingredient

Cetirizine

Dosage form

oral drops