Symptoms (when taking the drug once at a dose of 50 mg): confusion, diarrhea, dizziness, increased fatigue, headache, malaise, medriasis, itching, weakness, anxiety, sedative effect, drowsiness, stupor, tachycardia, tremor, urine delay.
Treatment: immediately after taking the drug - gastric lavage or vomiting induction. The appointment of activated carbon, symptomatic and supportive therapy are recommended. There is no specific antidote. Hemodialysis is ineffective.
Symptoms (when taking the drug in a dose of more than 5 tablets.): signs of intoxication in the form of drowsiness; in children - anxiety, increased irritability, the appearance of signs of anticholinergic action in the form of a delay in urine, dry mouth, constipation.
Treatment: taking the drug should be stopped, peeled, take activated carbon, immediately consult a doctor.
Increased sensitivity to cetyrizin, hydroxysine or any derivative of piperazine; terminal stage of renal failure (Cl creatinine <10 ml / min); age up to 6 months (for the medicinal form of the drop, due to limited data on the effectiveness and safety of the use of cetyrinine); age up to 6 years (for the drug form of the tablet); pregnancy.
When studying the drug interaction of cetyrizin with pseudoephedrine, cimetidine, ketokonazole, redytromycin, azithromycin, diazepam, glypidine and antipyrin, clinically significant unwanted interactions were not detected.
With simultaneous use with theophylline (400 mg / day), the total clearance of cetyrizin is reduced by 16% (theophylline kinetics does not change).
With simultaneous use with AUC ritonavir, cetyrizin increased by 40%, while the same indicator of the ritonavir slightly changed (−11%).
With simultaneous use with macrolides (azitromycin, red bloodmicin) and ketoconazole, changes to the ECG were not noted.
When using the drug in therapeutic doses, data on the interaction with alcohol were not obtained (at a blood alcohol concentration of 0.5 g / l). Nevertheless, one should refrain from drinking alcohol during therapy with a drug in order to avoid oppression of the central nervous system.
A three-day “laundering” period is recommended before the appointment of allergological samples due to the fact that H1-histamines blockers inhibit the development of skin allergic reactions.
It is not recommended to combine taking the drug Zinzet with other drugs without a doctor’s consultation. At the same time, taking with broncholithic drugs containing the theophylline as the active substance, an increase in the frequency of side effects of the drug Zincet. Data on the interaction of cetyricine with alcohol has not yet been received. Despite this, the use of alcoholic beverages in the treatment of Zincet is not recommended.
Data obtained in clinical trials
Clinical research has shown that the use of cetyrizin in recommended doses leads to the development of minor undesirable effects on the central nervous system, including drowsiness, fatigue, dizziness and headache. In some cases, paradoxical stimulation of the central tax system was recorded.
Although cetirisin is a selective blocker of peripheral H1receptors and practically do not have an anti-cholinergic effect, isolated cases of urination difficulties, impaired accomodation and dry mouth were reported.
Liver function disorders were reported, accompanied by an increase in the level of liver enzymes and bilirubin. In most cases, undesirable phenomena were resolved after the cessation of cetyrizin.
List of unwanted side reactions. There is evidence obtained from double blind controlled clinical trials aimed at comparing cetyrin and placebo or other antihistamines used in recommended doses (10 mg 1 time per day for cetyrizin) in more than 3200 patients, on the basis of which a reliable analysis of data can be carried out safety.
According to the results of the combined analysis, the following unwanted reactions with a frequency of 1% or higher were detected in placebo-controlled studies when using cetyrizin at a dose of 10 mg (n = 3260) and placebo (n = 3061).
General violations and violations at the place of introduction : fatigue - 1.63 and 0.95%.
From the side of the nervous system : dizziness - 1.1 and 0.98%; headache - 7.42 and 8%.
From the side of the LCD : abdominal pain - 0.98 and 1.08%; dry mouth - 2.09 and 0.82%; nausea - 1.07 and 1.14%.
From the psyche : drowsiness - 9.63 and 5%.
From the respiratory system, chest organs and mediastinum : pharyngitis - 1.29 and 1.34%.
Although the incidence of drowsiness in the cetrizin group was higher than that in the placebo group, in most cases this undesirable phenomenon was mild or moderate. An objective assessment conducted in other studies confirmed that the use of cetyrizin in the recommended daily dose in healthy young volunteers does not affect their daily activity.
Children. In placebo-controlled studies in children aged 6 months to 12 years, the following undesirable reactions were revealed with a frequency of 1% and higher in groups that took cetirisin (n = 1656) and placebo (n = 1294).
From the side of the LCD : diarrhea - 1 and 0.6%.
From the psyche : drowsiness - 1.8 and 1.4%.
From the respiratory system, chest organs and mediastinum : rhinitis - 1.4 and 1.1%.
General violations and violations at the place of introduction : fatigue - 1 and 0.3%.
Experience in post-striding use
In addition to the undesirable phenomena identified during the clinical trials and described above, the following unwanted reactions were observed as part of the post-restrictive use of cetyrin.
Unwanted phenomena are presented below in the classes of the organ system MedDRA and frequency of development, based on data on the post-restrictive use of cetyrizin.
The frequency of development of undesirable phenomena was determined as follows: very often (≥1/10); often (≥1/100, <1/10); infrequently (≥1/1000, <1/100); rarely (≥1/10000, <1/1000); very rarely (<1/1000); frequency.
From the blood and lymphatic system : very rarely - thrombocytopenia.
From the side of the immune system : rarely - hypersensitivity reactions; very rarely - anaphylactic shock.
Metabolic and nutritional disorders : frequency unknown - increase in appetite.
From the psyche : infrequently - excitement; rarely - aggression, confusion, depression, hallucinations, sleep disturbance; very rarely - tick; frequency unknown - suicidal ideas.
From the side of the nervous system : infrequently - pastezia; rarely - cramps; very rarely - perversion of taste, dyskinesia, dystonia, fainting, tremor; frequency unknown - memory impairment, including.h. amnesia.
From the side of the body of view : very rarely - impaired accomodality, blurred vision, nystagmus.
From the side of the hearing organs : frequency unknown - vertigo.
From the side of the MSS : rarely - tachycardia.
From the digestive system : infrequently - diarrhea.
Hepatobiliary disorders : rarely - a change in functional liver samples (increased activity of transaminases, alkaline phosphatase, gamma-glutamyltransferase and bilirubin level).
From the side of the skin : infrequently - rash, itching; rarely - urticaria; very rarely - angioneurotic swelling, persistent medicinal erythema.
From the urinary system : very rarely - dysuria, enuresis; frequency unknown - urine delay.
General disorders : infrequently - asthenia, malaise; rarely - peripheral edema.
Research: rarely - increasing body weight.
treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis (such as itching, sneezing, nose congestion, rhinorea, lacrimation, conjunctiva hypermia);
hay fever (flaymaking) ;
urticaria;
allergic dermatoses, including.h. atopic dermatitis, accompanied by itching and rashes.
Symptomatic treatment of allergic rhinitis and conjunctivitis (including year-round and seasonal), hay fever (pollinosis), idiopathic urticaria and other allergic dermatoses, accompanied by itching and rashes.
Cetrine is an active substance of Cetrine® - is a metabolite of hydroxysine, belongs to the group of competitive antagonists of histamine and blocks H1histamine receptors.
Cetirisin warns development and facilitates the course of allergic reactions, and has antitudent and anti-exudative effect. Cetirisin affects the early histone-dependent stage of allergic reactions, limits the release of inflammation mediators at a late stage of an allergic reaction, and also reduces the migration of eosinophiles, neutrophils and basophiles, stabilizes the membranes of fat cells. Reduces the permeability of capillaries, prevents the development of tissue edema, relieves the spasm of smooth muscles. Eliminates the skin reaction to the introduction of histamine, specific allergens, as well as cooling (with cold urticaria). Reduces histin-induced bronchocongricia with bronchial asthma of the light current.
Cetirisin does not have an anti-cholinergic and anti-serotonin effect. In therapeutic doses, the drug has virtually no sedative effect. After taking cetyrizin in a single dose of 10 mg, its action develops after 20 minutes (in 50% of patients), after 60 minutes (in 95% of patients) and lasts more than 24 hours. Against the background of course treatment, tolerance for the antihistamine action of cetyrizin does not develop. After the cancellation of therapy, the effect persists up to 3 days.
The pharmaceutical parameters of cetyrizin change linearly.
Suction. After taking it inside, the drug is quickly and completely absorbed from the LCD. Eating does not affect the completeness of absorption, although its speed decreases. In adults, after a single medication in therapeutic dose Cmax in blood plasma is 300 ng / ml and is achieved through (1 ± 0.5) h.
Distribution. Cetirisin on (93 ± 0.3)% binds to blood plasma proteins. Vd is 0.5 l / kg. When taking the drug at a dose of 10 mg for 10 days, cetyrizin cumulation is not observed.
Metabolism. In small quantities, it is metabolized in the body by O-dealkylation (unlike other antagonists H1-histamines that are metabolized in the liver using a cytochrome system) with the formation of pharmacologically inactive metabolite.
The conclusion. In adults T1/2 is approximately 10 hours; in children from 6 to 12 years old - 6 hours, from 2 to 6 years old - 5 hours, from 6 months to 2 years old - 3.1 hours. Approximately 2/3 of the accepted dose of the drug is withdrawn by the kidneys unchanged.
In elderly patients and patients with chronic liver diseases with a single medication at a dose of 10 mg T1/2 increases by about 50%, and system clearance is reduced by 40%.
In patients with renal failure of mild severity (Cl creatinine> 40 ml / min), pharmacokinetic parameters are similar to those in patients with normal kidney function.
In patients with moderate renal failure and in patients undergoing hemodialysis (Cl creatinine <7 ml / min), when taking the drug inward at a dose of 10 mg T1/2 lengthens 3 times, and the total clearance is reduced by 70% relative to these indicators in patients with normal kidney function, which requires a corresponding change in the dosing mode.
Cetirisin is practically not removed from the body during hemodialysis.
When analyzing prospective data, more than 700 cases of pregnancy outcomes did not reveal cases of formation of malformations, embryonic and neonatal toxicity with a clear causal relationship with the use of cetyrizin.
Experimental studies on animals did not reveal any direct or indirect adverse effects of cetrizin on a developing fetus, pregnancy and postnatal development.
Adequate and strictly controlled clinical studies on the safety of the use of cetyrizin during pregnancy have not been conducted, so it should not be used during pregnancy.
FDA fruit action category - B .
Cetirisin stands out with breast milk - from 25 to 90% of its concentration in blood plasma, depending on the time after appointment. During breastfeeding, they are used after consultation with the doctor if the intended benefit for the mother exceeds the potential risk for the child.
Fertility. Available data on the effect on human fertility are limited, but no negative impact on fertility has been identified.
Inside.
Children over 6 years old and adults : initial dose - 5 mg (1/2 table. or 10 drops) once a day, if necessary, can be increased to 10 mg (1 table. or 20 drops) 1 time a day. Sometimes the initial dose is 5 mg (1/2 tab. or 10 drops) may be sufficient to achieve a therapeutic effect. Daily dose - 10 mg (1 table. or 20 drops).
Children from 6 to 12 months : 2.5 mg (5 drops) 1 time per day.
Children from 1 year to 2 years : 2.5 mg (5 drops) up to 2 times a day.
Children from 2 to 6 years old : 2.5 mg (5 drops) 2 times a day or 5 mg (10 drops) 1 time a day.
Sick with renal failure, the dose decreases depending on the creatinine clearance: with Cl creatinine 30–49 ml / min - 5 mg 1 time per day, at 10–29 ml / min - 5 mg per day.
Because Cetrine® excreted by kidneys, when prescribing the drug, patients with renal failure and elderly patients should be adjusted to the extent of creatinine clearance. Creatinin clearance for men can be calculated based on the concentration of serum creatinine, according to the following formula:
Cl creatinine, ml / min
Creatinine clearance for women can be calculated by multiplying the value obtained by a coefficient of 0.85.
| Renal failure | Cl creatinine, ml / min | Dosing mode |
| Missing (norm) | ≥80 | 10 mg / day |
| Easy | 50–79 | 10 mg / day |
| Medium | 30–49 | 5 mg / day |
| Heavy | 10–29 | 5 mg per day |
| The terminal stage is patients on hemodialysis | <10 | taking the drug is contraindicated |
For adult patients with renal and liver failure, dosing is carried out according to the table above.
Children with renal failure are adjusted for creatinine clearance and body weight.
Patients with impaired liver function only do not need to correct the dosing mode.
Inside, swallowing in its entirety, drinking with a small amount of water, regardless of the time of eating.
Zinzet is used as prescribed by a doctor (to avoid complications).
Children from 2 to 6 years old: 2.5 mg each (1/2 h.syrup spoons) 2 times a day or 5 mg (1 h.spoon) 1 time per day; from 6 to 12 years: 10 mg each (1 table. or 2 hours. syrup spoons) 1 time per day or 5 mg (1/2 table. or 1 h.spoon syrup) 2 times a day, morning and evening; adults and children over 12 years old: 10 mg each (1 table. or 2 hours. spoons of syrup) 1 time per day.
For elderly people or patients with severe impaired liver and / or kidney function, the drug is prescribed individually by a doctor, in a reduced dose.
If the time of taking the drug is accidentally missed, the next dose should be taken as soon as possible. In the event that the time for the next drug is approaching, the next dose should be taken on schedule, without increasing the total dose.
