Cetrin

Cetrin is a systemic antihistamine that is a derivative of the piperazine component.

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Indications Cetrina

It is used to treat nasal manifestations of chronic or seasonal allergic rhinitis (such as sneezing, nasal itching and rhinorrhea) and nasal symptoms that develop due to conjunctivitis. In addition, it helps in the treatment of any type of urticaria (including idiopathic) and itching.

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Release form

Released in the form of syrup in glass bottles with a capacity of 30 or 60 ml. Inside the pack there is 1 bottle with syrup.

Pharmacodynamics

Cetirizine is a competitive histamine antagonist, a breakdown product of hydroxyzine, and a blocker of H1 histamine endings.

It has anti-allergenic, as well as anti-exudative and antipruritic properties, prevents the release of inflammatory conductors at a late stage of an allergic response, and at the same time limits the movement of neutrophils with eosinophils and basophils, and prevents the development of edema in tissues.

The drug eliminates the skin reaction to the introduction of certain specific allergens and histamine, and also reduces histamine-induced bronchoconstriction during moderate or mild bronchial asthma. It also has weak antiserotonin and anticholinergic properties.

Pharmacokinetics

The development of the effect when taking 10 mg of the drug begins after 20 minutes (in 5% of people) or after 1 hour (in 95% of people), and the total duration is 24+ hours. During the course of therapy, patients do not develop tolerance to the antihistamine effect. After the course is completed, the effect of the drug lasts for about 3 more days.

The drug is rapidly absorbed from the gastrointestinal tract, with peak levels occurring after approximately 1 hour. Food does not affect the degree of absorption, but increases the time it takes to reach peak levels.

The synthesis of the component with plasma protein is 93%.

It is poorly metabolized by the liver – it undergoes the process of O-dealkylation, during which medicinally inactive decay products are formed (unlike other H1-ending blockers, which are metabolized in the liver using the P450 hemoprotein system).

Two-thirds of the drug is excreted unchanged via the kidneys, and approximately 10% of the substance is excreted in the feces. The systemic clearance rate is 53 ml/minute.

Half-life is within 7-10 hours (adults). In children 2-6 years old – 5 hours, 6-12 years old – 6 hours.

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Dosing and administration

The syrup is taken orally, regardless of food intake.

Dose size for ages 2-6 years: single daily use of 2.5 mg (or 2.5 ml) of the drug. It is allowed to increase the daily dose to 5 mg: take 2.5 mg (or 2.5 ml) every 12 hours, taking into account the effectiveness of the therapy, the severity of the disease and the patient's weight.

For children aged 6 years and over, as well as adults, the dose is a single dose of 10 mg (or 10 ml) of syrup per day. Taking into account the severity of symptoms and the effectiveness of therapy, the initial dosage can be reduced to 5 mg (or 5 ml). No more than 20 mg of the drug is allowed per day (for adults).

People who have kidney problems (severe or moderate) require individual determination of the dose size:

• normal renal function (creatinine clearance is ≥80 ml/minute) – 10 mg taken once a day;
• mild form of the disorder (CC level: 50-79 ml/minute) – take 10 mg once a day;
• moderate form of the disorder (CC values within 30-49 ml/minute) – take 5 mg once a day;
• severe form of pathology (CC level <30 ml/minute) – take 5 mg of the drug once every other day;
• at the terminal stage of the disease; during dialysis procedures (the level of CC is <10 ml/minute), taking the syrup is prohibited.

For children with kidney problems, dosages are adjusted separately, taking into account the CC indicators, and along with this, the patient's weight.

The duration of the course is prescribed by the doctor, taking into account the effectiveness of the treatment.

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Use Cetrina during pregnancy

Cetrin is not used during pregnancy or lactation.

Contraindications

Main contraindications:

• history of hypersensitivity to the drug components, hydroxyzine, and any piperazine derivatives;
• severe renal dysfunction (creatinine clearance less than 10 ml/minute);
• intolerance to sucrose-isomaltose with fructose, as well as glucose-galactose malabsorption or calcium deficiency.

It is prohibited to prescribe to children under 2 years of age, because there is no information on the use of the drug in this age group of patients.

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Side effects Cetrina

Taking the syrup may cause the following side effects:

• systemic disorders: the appearance of edema, the development of asthenia, fatigue and malaise;
• reactions of the nervous system: development of tremor, dyskinesia, dysgeusia, and dystonia, the appearance of headaches, convulsions, dizziness and paresthesia, as well as fainting;
• gastrointestinal disorders: diarrhea, nausea, dry mouth and abdominal pain;
• mental disorders: feelings of aggression, drowsiness, confusion or anxiety, as well as the development of tics, depression, insomnia and the appearance of hallucinations;
• manifestations from the respiratory system: runny nose or pharyngitis;
• test results and analyses: weight gain;
• disorders in the functioning of the heart: the appearance of tachycardia;
• lymph and organs of the hematopoietic system: development of thrombocytopenia;
• problems with the visual organs: blurred vision, accommodation disorder and nystagmus;
• urinary system and kidneys: development of enuresis or dysuria;
• reactions of the subcutaneous layers and skin: development of urticaria, Quincke's edema, local drug rashes, and itching;
• immune reactions: hypersensitivity and development of anaphylaxis;
• hepatobiliary system: liver function disorders (increased levels of alkaline phosphatase, transaminases, bilirubin, and GGT).

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Overdose

Overdose of cetirizine usually manifests itself through effects on the central nervous system or reactions that may develop due to the anticholinergic properties. Disturbances that have occurred as a result of taking a dosage at least five times the standard daily dose include: dizziness, diarrhea, itching, malaise and headaches, as well as feelings of anxiety, confusion, fatigue and drowsiness. Urinary retention, tachycardia and mydriasis may also develop.

The drug has no specific antidote. Overdose care should be aimed at eliminating disorders and maintaining the victim's condition. At the initial stage of overdose development, vomiting should be induced, as well as gastric lavage. In addition, laxatives and activated carbon are prescribed. The dialysis procedure will be ineffective. If severe intoxication is observed, professional medical supervision of the cardiovascular system and respiratory organs is required.

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Interactions with other drugs

Studies have been performed to examine the drug's interaction with antipyrine and erythromycin, as well as with the substances ketoconazole, pseudoephedrine, and azithromycin. These tests have not revealed any pharmacokinetic interactions between the above drugs and cetirizine.

Combination with theophylline reduces the level of cetirizine clearance coefficient, as a result of which the substance can accumulate in the body. As a result, an overdose can occur.

Alcohol or CNS depressants in combination with cetirizine may further impair alertness and concentration.

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Storage conditions

Cetrin should be kept in a place protected from sunlight and inaccessible to children. Temperature values are maximum 25°C.

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Shelf life

Cetrin is permitted to be used within 2 years from the date of syrup production.

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