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Zeolola
Zylol is an antihistamine drug of systemic action, is a piperazine derivative.
Pharmacodynamics
Levocetirizine is a stable active R-enantiomer of the cetirizine substance, and is included in the category of selective competitive antagonists of the histamine receptor (H1). The affinity for these receptors in levocetirizine is twice that of cetirizine.
The medicine acts on the stage of the allergic response, which depends on histamine, and at the same time reduces the movement of eosinophils, strengthens the vessels and prevents the release of inflammatory conductors. In addition, it prevents the development, as well as facilitates the course of allergic symptoms, has anti-allergic, anti-exudative and anti-inflammatory properties. In this case, almost no antiserotoninovogo and cholinolytic effect. At therapeutic dosages, it practically has no sedative effect.
The ECG tests did not reveal the corresponding action of levocetirizine relative to the QT interval.
Pharmacokinetics
The pharmacokinetics of the active ingredient changes linearly. It depends on the dosage, has a weak individual variability and is practically not different from the indices of cetirizine.
Levocetirizin is absorbed quickly enough by oral administration of drugs. On the degree of absorption, eating does not affect, but at the same time lowers its speed. Peak indices inside the plasma are observed 0.9 hours after drug use in the drug dosage and is 207 ng / ml (for a single dose) and 308 ng / ml (with repeated use of the drug in the amount of 5 mg). The equilibrium values within the serum reach 2 days later.
There is no information on the distribution of drugs inside the tissues of the human body, and beyond that on the passage of matter through the BBB. In the animal testing process, the highest index was observed inside the kidneys with the liver, and the lowest was inside the central nervous system. The distribution volume is 0.4 l / kg, and the synthesis with plasma protein reaches 90%.
In the process of metabolism, approximately 14% of the active component is involved in the body. Oxidation, binding with taurine, and N- together with O-dealkylation are carried out. The latter processes are performed with the help of hemoprotein CYP 3A4, and several hemoprotein isoforms participate in the oxidative processes. The active substance has no effect on the activity of hemoprotein isoenzymes 1A2 and 2C9, and in addition 2C19 with 2D6 and 2E1 with 3A4 at their rates, which exceed the peak level after oral dosage in the amount of 5 mg. Since the metabolic process has a low degree, and the suppressive effect does not increase, the probability of interaction of the active ingredient with other substances is extremely small.
Excretion of drugs is often carried out with the help of actively occurring tubular secretion, and in addition glomerular filtration. The half-life is 7.9 + 1.9 hours, and the total purification rate is 0.63 ml / minute / kg. The substance does not accumulate, completely excreted for 96 hours. Excretion of approximately 85.4% of the drug dosage is performed with urine (unchanged form), and approximately 12.9% is excreted with feces.
In persons with disorders of renal activity (with a KC value of <40 ml / minute), the purification rate of the drug decreases, and the half-life increases (in patients receiving hemodialysis, the overall score is reduced by 80%), so they need to select a suitable dosage regimen. During the standard procedure of hemodialysis (4 hours) only a small part (less than 10%) of the active component is excreted.
Contraindications
Among the contraindications of drugs:
- intolerance to levocetirizine, as well as other derivatives of piperazine or any other elements of the drug;
- severe form of kidney failure, in which there is a CC less than 10 ml / minute;
- hereditary form of galactose intolerance (severe), lack of lactase enzyme (β-galactosidase) or problems with digestion of galactose with glucose by the body;
- children under 6 years of age.
Side effects of the zeolola
Use of the medicine may cause the development of the following side effects:
- organs of the National Assembly: the appearance of headaches, paresthesias, seizures, dizziness, dysgeusia or tremor, and in addition fainting, severe fatigue, a feeling of drowsiness and asthenia;
- visual organs: blurred vision or visual impairment;
- CAS organs: the appearance of tachycardia or changes in heart rate;
- respiratory organs: the onset of dyspnea;
- organs of the digestive tract: vomiting, abdominal pain, constipation or diarrhea, and with it nausea and dryness of the oral mucosa;
- organs of the digestive system: the development of hepatitis;
- subcutaneous tissue with skin: drug-induced rash (stable type), Quincke edema, urticaria, and besides other rashes and itching;
- organs of the ODA: development of muscle pain;
- organs of the immune system: manifestations of hypersensitivity, among which also anaphylaxis;
- organs of the urinary system and kidneys: retention of urination, development of dysuria;
- metabolic disorders: increased appetite;
- general disorders: the appearance of edemas;
- laboratory tests: a change in the values of liver tests, and in addition weight gain.
The use of drugs should be canceled if any of the above reactions develop, and then consult a doctor.
Dosing and administration
The medicine can be taken by children over 6 years old and adults (dosage per day - a single dose of 5 mg LS). You can drink a pill either on an empty stomach or with a meal, washed down with water. You can not chew it.
For people with a chronic form of kidney failure, a drug can be prescribed only after consulting a doctor. Calculate the size of the dosage required in accordance with the KK index:
- at an easy 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 impairment (clearance less than 30 ml / minute) - every 3 days for 5 mg once a day;
- Persons with terminal stage of pathology who are on hemodialysis (clearance less than 10 ml / minute) are completely contraindicated.
The duration of the therapeutic course depends on the severity of the pathology, its type, as well as the strength of manifestation of the signs of the disease (these parameters are determined by the attending doctor). In case of short contact with the allergen (for example, with pollen of plants), the medication should be used for the first week. On average, the course lasts 3-6 weeks.
To eliminate chronic forms of an allergic rhinitis or urticaria, the medicine should be taken during the first year.
Overdose
As a result of drug overdose, intoxication can manifest as a feeling of drowsiness. And in children it is sometimes expressed in the form of restlessness and strong arousal, which then turn into drowsiness.
If the patient has signs of an overdose (especially children), you must cancel the use of the medicine. Then, as soon as possible, call a doctor, wash the person's stomach and give activated charcoal. In the rest, the treatment is symptomatic. There is no specific antidote, and the procedure of hemodialysis will be ineffective.
Interactions with other drugs
When combined with cimetidine, azithromycin and pseudoephedrine, and in addition to erythromycin, diazepam, ketoconazole and glypezide, there is no medically significant negative interaction.
In combination with theophylline (in a daily dose of 400 mg), levocetirizine lowers the overall clearance (-16%), while the pharmacokinetic properties of theophylline remain unchanged.
Levocetirizine does not increase the effect of alcoholic beverages, but in people with high sensitivity, when combined with alcohol or other drugs that suppress the function of the central nervous system, the development of such an effect is possible.
During the course of treatment with Zilola, you must stop using sedatives.
Attention!
To simplify the perception of information, this instruction for use of the drug "Zeolola" 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.