Description
Latin name
Zodac
Release form
Drops for oral administration.
Packaging
Bottle 20 ml.
Pharmacological action of
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 facilitates the course of allergic reactions: at a dose of 10 mg 1 or 2 times a day inhibits the late phase of aggregation of eosinophils in the skin and conjunctiva of patients prone to atopy. After oral administration, the antiallergic effect of cetirizine lasts 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 reaction in the form of a rash and redness to the introduction of high concentration of histamine into the skin, but there is no correlation with effectiveness.
In a 6-week placebo-controlled study involving 186 patients with allergic rhinitis and concomitant mild to moderate bronchial asthma, it was shown that the use of cetirizine in 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 cetirizine in patients with mild to moderate allergies and bronchial asthma.
A placebo-controlled study showed that the use of cetirizine at a dose of 60 mg per day for 7 days did not cause a clinically significant extension of the QT interval. The use of cetirizine in 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 in patients aged 5-12 years, no signs of immunity to the antihistamine effect of cetirizine were detected. The normal skin reaction to histamine was restored within three days after discontinuation of the drug with its repeated use.
In a 7-day, placebo-controlled study of cetirizine in a syrup dosage form, involving 42 patients aged 6 to 11 months, the safety of its use was demonstrated. Cetirizine was prescribed at a dose of 0.25 mg / kg 2 times a day, which approximately corresponded to 4.5 mg per day (dose range ranged from 3.4 to 6.2 mg per day).
Use in children from 6 to 12 months is possible only as directed by a doctor and under strict medical supervision.
Pharmacokinetics
The pharmacokinetic parameters of cetirizine when applied in doses of 5 to 60 mg vary linearly.
Absorption
The maximum concentration (Cmax) in plasma is reached after 1 ± 0.5 hours and is 300 ng / ml.
Various pharmacokinetic parameters, such as the maximum concentration in blood plasma and the area under the curve “concentration-time” are homogeneous. Eating does not affect the completeness of absorption of cetirizine, although its speed decreases. The bioavailability of various dosage forms of cetirizine (solution, capsules, tablets) is comparable.
Distribution of
Cetirizine 93 ± 0.3% binds to 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.
Excretion
The elimination half-life (T1 / 2) is approximately 10 hours.
When using the drug in a daily dose of 10 mg for 10 days, cumulation 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, T1 / 2 was 50% higher and clearance was 40% lower than in non-elderly patients.
Decreased cetirizine clearance in elderly patients is likely associated with decreased renal function in this category of patients.
Patients with renal failure
In patients with mild renal insufficiency (creatinia clearance (CC)> 40 ml / min), pharmacokinetic parameters are similar to those in healthy volunteers with normal renal function.
In patients with moderate renal failure and in patients undergoing hemodialysis (CC <7 ml / min), when the drug is administered orally at a dose of 10 mg, T1 / 2 is 3 times longer. and overall clearance is reduced by 70% relative to healthy volunteers with normal renal function. For patients with moderate or severe renal insufficiency, a corresponding change in dosage regimen is required. Cetirizine is poorly excreted by hemodialysis. Patients with liver failure In patients with chronic liver diseases (hepatocellular, cholestatic and biliary cirrhosis), with a single dose of 10 or 20 mg T1 / 2 increases by about 50%, and clearance decreases by 40% compared with healthy subjects . Dose adjustment is necessary only if the patient with liver failure also has concomitant renal failure. Children T1 / 2 in children from 6 to 12 years is 6 hours, from 2 to 6 years – 5 hours, from 6 months to 2 years reduced to 3.1 hours. Indications Indicated in adults and children 6 months and older to relieve: nasal and ocular symptoms of perennial (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis: itching, sneezing, nasal congestion, rhinorrhea, symptoms of chronic idiopathic urticaria. Contraindications Hypersensitivity to cetirizine, hydroxyzine or piperazine derivatives, as well as other components of , end-stage renal failure (CC <10 ml / min) children under 6 months of age (due to limited data on efficacy and safety) . Caution Chronic renal failure (KK> 10 ml / min, dosage adjustment required)
elderly patients (with an age-related decrease in glomerular filtration rate)
epilepsy and patients with increased convulsive readiness
patients with predisposing factors for mild delay spinal cord, prostate hyperplasia)
period of breastfeeding.
Special instructions
Due to the potential depressing effect on the central nervous system, caution should be exercised when prescribing Zodak ® to children under the age of 1 year in the presence of the following risk factors for sudden childhood death syndrome, such as (but not limited to this list):
apnea syndrome in a dream or sudden infant death syndrome in infants of a
brother or sister mother abuse drug or smoking during pregnancy
mother’s young age (19 years or younger)
abused of smoking babysitter caring for a child (one pack of cigarettes a day or more)
children who regularly fall asleep face down and who do not put
on their back prematurely (gestational age less than 37 weeks) or born with insufficient body weight (below the 10th percentile of gestational age)
children with co-administration of drugs that have a depressing effect on the central nervous system. The composition of the drug includes excipients methyl parabenzene and propyl parabenzene, which can cause allergic reactions, including delayed type.
Caution is required in patients with spinal cord injury, prostatic hyperplasia, and other predisposing factors for urinary retention, since cetirizine may increase the risk of urinary retention. Caution is advised when using cetirizine concomitantly with alcohol, although there are no clinically significant interactions with alcohol in therapeutic doses (at a blood alcohol concentration of 0.5 g / l).
Caution should be observed in patients with epilepsy and increased convulsive readiness.
A three-day ² Ñwash-out ² Ñ period is recommended before allergy tests, because H1-histamine receptor blockers inhibit the development of skin allergic reactions.
Influence on the ability to drive vehicles and work with mechanisms
An objective assessment of the ability to drive vehicles and work with mechanisms did not reliably reveal any adverse effects when using the Zodak ® preparation in recommended doses. However, it is advisable for patients with manifestations of drowsiness while taking the drug during the treatment period to refrain from driving, engaging in potentially dangerous activities or controlling mechanisms that require an increased concentration of attention and speed of psychomotor reactions.
Composition
1 ml contains:
Active ingredient:
Naphazoline nitrate 0.5 mg
Excipients:
Boric acid
Ethylenediamine
Methyl parahydroxybenzo
rplrd 37pkrdlpprdprrdprrdpfrd 1 mg prdrodprrdprdprrd46prdprrd excipients:
Methyl parahydroxybenzoate, propyl parahydroxybenzoate, glycerol, propylene glycol, sodium saccharinate dihydrate, sodium acetate trihydrate, glacial acetic acid, purified water.
Dosage and administration
Inside, drip into a spoon or dissolve in water.
The amount of water to dissolve the drug should correspond to the amount of fluid that the patient (especially the child) is able to swallow.
The solution should be taken immediately after preparation.
Adults
10 mg (20 drops) 1 time per day.
Elderly patients
There is no need to reduce dosage in elderly patients if renal function is not impaired.
Patients with renal failure
Since Zodak ® is excreted mainly by the kidneys (see the Pharmacokinetics subsection), if alternative treatment is not possible for patients with renal insufficiency, the dosage regimen should be adjusted depending on renal function (creatinine clearance, QC).
KK for men can be calculated based on the concentration of serum creatinine, according to the following formula:
Dosing in adult patients with renal failure
Renal failure KK (ml / min) Dosing regimen
Normal? 80 10 mg 1 time per day
Mild 50-79 10 mg 1 time per day
Average 30-49 5 mg 1 time per day
Severe 10-29 5 mg every other day
Terminal stage (patients on dialysis) <10 taking the drug is contraindicated Patients with impaired liver function In patients with impaired hepatic function, dosage adjustment is not required. In patients with impaired liver and kidney function, dosage adjustment is recommended (see table above). Children Use in children from 6 to 12 months is possible only as directed by a doctor and under strict medical supervision. Children 6 to 12 months of age 2.5 mg (5 drops) 1 time per day. Children 1 to 6 years of age 2.5 mg (5 drops) 2 times a day. Children 6 to 12 years old 5 mg (10 drops) 2 times a day. Children over 12 years of age 10 mg (20 drops) 1 time per day. Sometimes an initial dose of 5 mg (10 drops) may be enough if satisfactory control of symptoms can be achieved. In children with renal failure, the dose is adjusted taking into account QC and body weight. Side effects From the digestive system: dry mouth, dyspepsia. From the side of the central nervous system: headache, drowsiness, fatigue, dizziness, agitation, migraine. Allergic reactions: skin rash, angioedema, urticaria, pruritus. Zodak is usually well tolerated. Side effects occur rarely and are transient in nature. Drug Interactions No drug interactions of cetirizine with other drugs have been observed. Based on the results of studies of the drug interaction of cetirizine, in particular, studies of interaction with pseudoephedrine or theophylline at a dose of 400 mg per day, no clinically significant interactions were found. The simultaneous use of cetirizine with alcohol and other drugs that depress the central nervous system, may contribute to a further decrease in the concentration of attention and speed of reactions, although cetirizine does not enhance the effect of alcohol (when its concentration in the blood is 0.5 g / l). Overdose The clinical picture observed with an overdose of cetirizine was due to its effect on the CNS. Symptoms: following a single 50 mg dose of cetirizine, the following clinical picture was observed: confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, skin itching, anxiety, sedation, drowsiness, stupor, tachycardia urine. Treatment: Immediately after the administration of the drug, it is necessary to wash the stomach or stimulate vomiting. The use of activated charcoal, symptomatic and supportive therapy is recommended. There is no specific antidote. Hemodialysis is ineffective. Storage conditions Store in a dry, dark place at a temperature not exceeding 20 ° C. Shelf life 3 years. Deystvuyushtee substance Cetirizine Terms and conditions without prescription Prescription Prescription Prescription Prescription s18lrdf4068 prescription srdlfp p68 d68 For adults, Children over 6 months of age A. Nattermann and Sie GmbH, Czech Republic
