Zodak, drops 10 mg/ml 20 ml

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

In addition to its antihistamine effect, cetirizine prevents the development and facilitates the course of allergic reactions: in a dose of 10 mg once or twice daily, it inhibits the late phase of eosinophil aggregation in the skin and conjunctiva of atopic patients. After oral administration, the antiallergic effect of cetirizine lasts for 24 hours.

Clinical efficacy and safety:

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

In a 6-week placebo-controlled study involving 186 patients with allergic rhinitis and concomitant mild to moderate bronchial asthma, cetirizine in a dose of 10 mg once daily was shown to reduce rhinitis symptoms and not affect lung function.

The results of this study confirm the safety of the use of cetirizine in patients with allergies and mild to moderate bronchial asthma.

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

Children

A 35-day study involving patients aged 5-12 years showed no evidence of insensitivity to the antihistamine effect of cetirizine. Normal skin response to histamine was restored within three days of drug withdrawal with repeated use.

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

The use in children from 6 to 12 months of age is only possible by prescription and under strict medical supervision.

Pharmacokinetics

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

Intake

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

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

Distribution

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

Metabolism

Cetirizine does not undergo extensive primary metabolism.

Elimation

The elimination half-life (T1/2) is approximately 10 hours.
No cetirizine cumulation was observed when using the drug in a daily dose of 10 mg for 10 days.
Approximately 2/3 of the dose taken is excreted unchanged in the urine.

Elderly patients

The T1/2 was 50% higher and clearance was 40% lower in 16 elderly patients at a single dose of 10 mg compared to non-elderly patients.

The decreased clearance of cetirizine in elderly patients is probably due to decreased renal function in this patient population.

Patients with renal impairment

In patients with mild renal impairment (creatinia clearance (CK) > 40 ml/min) pharmacokinetic parameters are similar to those in healthy volunteers with normal renal function.

In patients with moderate renal insufficiency and in patients on hemodialysis (CK < 7 ml/min), when using the drug orally at a dose of 10 mg, T1/2 is prolonged by 3 times and total clearance is reduced by 70% relative to healthy volunteers with normal renal function.

In patients with moderate to severe renal impairment, an appropriate change in dosing regimen is required.

Cetirizine is poorly excreted by hemodialysis.

Patients with hepatic impairment
Patients with chronic liver disease (hepatocellular, cholestatic and biliary cirrhosis) have a T1/2 increased by approximately 50% and clearance decreased by 40% in a single dose of 10 or 20 mg compared to healthy subjects. Dose adjustment is necessary only if the patient with hepatic impairment also has concomitant renal impairment.

Children

The T1/2 in children 6 to 12 years old is 6 hours, 2 to 6 years old is 5 hours, and 6 months to 2 years old is reduced to 3.1 hours.

Indications

Active ingredient

Composition

1 ml contains:

the active ingredient:

cetirizine dihydrochloride 10 mg

excipients:

Methylparahydroxybenzoate,

propylparahydroxybenzoate,

How to take, the dosage

Ingestion, drop into a spoon or dissolve in water.

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

The solution should be taken immediately after preparation.

Adults
10 mg (20 drops) once daily.

Patients in the elderly
There is no need to reduce the dosage in elderly patients if renal function is not impaired.

Patients with renal impairment
Since Zodac® is mainly excreted by the kidneys (see subsection “Pharmacokinetics”), if no alternative treatment is available for patients with renal impairment the drug dosing regimen should be adjusted according to renal function (creatinine CK clearance values).

The CK for men can be calculated based on serum creatinine concentration using the following formula:

Dosing in adult patients with renal impairment

Patients with impaired liver function
In patients with only impaired liver function, dosing adjustments are not required.
In patients with impaired hepatic and renal function, dosing adjustments are recommended (see table above).

Children
Use in children from 6 to 12 months is only possible by prescription and under strict medical supervision.

Children 6 to 12 months
2.5 mg (5 drops) once daily.

Children 1 to 6 years
2.5 mg (5 drops) 2 times daily.

Children 6 to 12 years
5 mg (10 drops) 2 times daily.

Children over 12 years
10 mg (20 drops) once daily.

Sometimes an initial dose of 5 mg (10 drops) may be sufficient if satisfactory symptom control can be achieved.

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

Interaction

On the basis of the results of conducted studies of drug interactions of cetirizine, in particular, studies of interaction with pseudoephedrine or theophylline in the dose of 400 mg per day, no clinically significant interactions have been found.

The concomitant use of cetirizine with alcohol and other CNS depressant drugs may further decrease concentration and reaction time, although cetirizine does not increase the effect of alcohol (at a blood concentration of 0.5 g/l).

Special Instructions

Because of the potential CNS depressant effects, caution should be exercised when prescribing Zodac® in children less than 1 year of age if the following risk factors for sudden infant death syndrome are present, such as (but not limited to)

Contraindications

Side effects

Digestive system disorders: dry mouth, dyspepsia.

CNS disorders: headache, drowsiness, fatigue, dizziness, agitation, migraine.

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

Overdose

The clinical picture observed in cetirizine overdose was due to its effect on the CNS.

Symptoms: after a single dose of 50 mg of cetirizine the following clinical presentation was observed: confusion, diarrhea, dizziness, increased fatigue, headache, malaise, mydriasis, skin itching, anxiety, sedation, somnolence, stupor, tachycardia, tremor, urinary retention.

Treatment: gastric lavage or induce vomiting should be performed immediately after taking the drug. Administration of activated charcoal, symptomatic and supportive therapy are recommended. There is no specific antidote. Hemodialysis is ineffective.

Pregnancy use

Pregnancy
An analysis of prospective data from more than 700 cases of pregnancy outcomes showed no cases of malformations, fetal or neonatal toxicity with a clear cause-effect relationship.

The experimental studies on animals did not reveal any direct or indirect adverse effects of cetirizine on the developing fetus (including in the postnatal period), the course of pregnancy and postnatal development.

There have been no adequate and strictly controlled clinical trials on safety of the drug administration during pregnancy, therefore the drug Zodac® should not be used during pregnancy.

Breast-feeding
Cetirizine is excreted with breast milk at concentrations from 25% to 90% of the drug concentration in blood plasma, depending on the time after administration. During breastfeeding, use after consultation with a physician if the estimated benefit to the mother exceeds the potential risk to the baby.

Fertility
The available data on effects on human fertility are limited, but no adverse effects on fertility have been identified.

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