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Zilola
Last reviewed: 03.07.2025
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Zilola is a systemic antihistamine drug, a derivative of piperazine.
Indications Zilola
It is indicated for the elimination of allergic forms of rhinitis (including year-round ones), and also the chronic form of idiopathic urticaria.
Release form
Available in tablets, 7 pieces in 1 blister. One pack contains 1 or 4 blister strips.
Pharmacodynamics
Levocetirizine is a stable active R-enantiomer of the substance cetirizine, and belongs to the category of selective competitive antagonists of receptors (H1) of histamine. At the same time, the affinity for these receptors of levocetirizine is twice as high as that of the substance cetirizine.
The drug affects the histamine-dependent stage of the allergic response, and at the same time reduces the movement of eosinophils, strengthens blood vessels and prevents the release of inflammatory conductors. In addition, it prevents the development and alleviates the course of allergic symptoms, has antiallergic, antiexudative and anti-inflammatory properties. At the same time, it has almost no antiserotonin and cholinolytic effect. At therapeutic doses, it has virtually no sedative effect.
ECG testing did not reveal any relevant effect of levocetirizine on the QT interval.
Pharmacokinetics
The pharmacokinetics of the active ingredient changes linearly. It depends on the dosage, has weak individual variability and is practically no different from the indicators of cetirizine.
Levocetirizine is absorbed fairly quickly when taken orally. Food intake does not affect the absorption rate, but it does slow it down. The peak of plasma levels is observed 0.9 hours after taking the drug in a medicinal dose and is 207 ng/ml (with a single dose) and 308 ng/ml (with repeated use of the drug in a dose of 5 mg). Equilibrium levels in serum are reached after 2 days.
There is no information on the distribution of the drug inside the tissues of the human body, and in addition to this, on the passage of the substance through the BBB. During animal testing, the highest indicator was observed inside the kidneys with the liver, and the lowest - inside the central nervous system. The distribution volume is 0.4 l / kg, and the synthesis with plasma protein reaches 90%.
About 14% of the active component is involved in the metabolism process inside the body. This includes oxidation, binding to taurine, and N- together with O-dealkylation. The latter processes are performed by the hemoprotein CYP ZA4, and several hemoprotein isoforms are involved in the oxidative processes. The active substance does not affect the activity of hemoprotein isoenzymes 1A2 and 2C9, and in addition 2C19 with 2D6 and 2E1 with ZA4 at their values, which exceed the peak level after taking an oral dose of 5 mg. Since the metabolism process is low, and the suppressive effect is not enhanced, the likelihood of interaction of the active component with other substances is extremely low.
Excretion of the drug is often carried out by actively occurring tubular secretion, as well as glomerular filtration. The half-life is 7.9+1.9 hours, and the total clearance rate is 0.63 ml/minute/kg. The substance does not accumulate, being completely excreted within 96 hours. Excretion of approximately 85.4% of the drug dosage is carried out with urine (unchanged form), and approximately 12.9% is excreted with feces.
In patients with renal impairment (with a CC value of <40 ml/min), the drug clearance rate decreases and the half-life increases (in patients receiving hemodialysis, the overall rate decreases by 80%), which is why they need to select an appropriate dosage regimen. During a standard hemodialysis procedure (4 hours), only a small part (less than 10%) of the active ingredient is removed.
Dosing and administration
The medicine can be taken by children over 6 years old and adults (the daily dosage is a single dose of 5 mg of the drug). The tablet can be taken either on an empty stomach or with food, washed down with water. It cannot be chewed.
For people suffering from chronic renal failure, the drug can be prescribed only after consultation with a doctor. The dosage should be calculated in accordance with the CC indicator:
- at a mild stage of the disorder (clearance is 50-79 ml/minute), tablets are taken in a standard dose - 5 mg once a day;
- moderate form of the disorder (clearance within 30-49 ml/minute) – 5 mg once a day; every 2 days;
- severe form of the disorder (clearance less than 30 ml/minute) – every 3 days, 5 mg once a day;
- For individuals with terminal stage pathology who are on hemodialysis (clearance less than 10 ml/minute), taking the drug is completely contraindicated.
The duration of the therapeutic course depends on the severity of the pathology, its type, and the strength of the manifestation of the signs of the disease (these parameters are determined by the attending physician). In case of short-term contact with an allergen (for example, with plant pollen), it is enough to use the medicine for 1 week. On average, the course lasts 3-6 weeks.
To eliminate chronic forms of allergic rhinitis or urticaria, the medicine must be taken for 1 year.
Use Zilola during pregnancy
Zilol should not be prescribed to pregnant women.
The active component can pass into breast milk, which is why if it is necessary to use the drug during the lactation period, breastfeeding should be stopped for a while.
Contraindications
Among the contraindications of the drug:
- intolerance to levocetirizine, as well as other derivatives of piperazine or any other elements of the drug;
- severe form of renal failure, in which CC is less than 10 ml/minute;
- hereditary form of galactose intolerance (severe), deficiency of the enzyme lactase (β-galactosidase) or problems with the body's absorption of galactose with glucose;
- children under 6 years of age.
Side effects Zilola
The use of the drug may cause the development of the following side effects:
- organs of the nervous system: the appearance of headaches, paresthesia, convulsions, dizziness, dysgeusia or tremor, as well as fainting, severe fatigue, a feeling of drowsiness and asthenia;
- visual organs: blurred vision or visual impairment;
- cardiovascular system organs: the appearance of tachycardia or changes in heart rhythm;
- respiratory organs: occurrence of dyspnea;
- gastrointestinal tract: vomiting, abdominal pain, constipation or diarrhea, and along with this nausea and dry mouth;
- digestive system organs: development of hepatitis;
- subcutaneous tissue with skin: drug rash (resistant type), Quincke's edema, urticaria, and in addition other rashes and itching;
- musculoskeletal system: development of muscle pain;
- organs of the immune system: manifestations of hypersensitivity, including anaphylaxis;
- urinary system organs and kidneys: urinary retention, development of dysuria;
- metabolic disorders: increased appetite;
- general disorders: the appearance of swelling;
- laboratory tests: changes in liver function tests, and in addition, weight gain.
The use of the drug must be discontinued if any of the above reactions develop, after which a doctor should be consulted.
Overdose
As a result of drug overdose, intoxication may manifest itself in the form of a feeling of drowsiness. And in children, it sometimes manifests itself in the form of restlessness and strong excitement, which then turn into drowsiness.
If the patient shows signs of overdose (especially in children), the drug should be discontinued. Then, a doctor should be called as soon as possible, the person's stomach should be washed out, and activated carbon should be given. Otherwise, treatment is symptomatic. There is no specific antidote, and hemodialysis will be ineffective.
Interactions with other drugs
When used in combination with cimetidine, azithromycin and pseudoephedrine, as well as with erythromycin, diazepam, ketoconazole and glipizide, no significant negative drug interactions occur.
In combination with theophylline (at a daily dose of 400 mg), the overall clearance rate of levocetirizine decreases (-16%), but the pharmacokinetic properties of theophylline remain unchanged.
Levocetirizine does not increase the effects of alcoholic beverages, but in people with high sensitivity, when combining the drug with alcohol or other drugs that depress the function of the central nervous system, such an effect may develop.
During the course of treatment with Zilola, it is necessary to stop using sedatives.
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Shelf life
Zilola can be used for 2 years from the date of release of the drug.
Attention!
To simplify the perception of information, this instruction for use of the drug "Zilola" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.