Cetirizine drops for oral administration 10 mg/ml 20 ml No. 1

Composition and release form

The drug is available in the form of tablets and drops for oral administration.

The tablets have a special soluble coating. Packaged in paper packaging with attached instructions for use.

The drops are a light liquid. Sold in bottles of 10 or 20 ml.

The active ingredient is cetirizine dihydrochloride. Its content in tablets and drops is 10 mg.

Excipients: magnesium stearate, silicon dioxide, lactose in tablets. Also benzoic acid, glycerol, sodium acetate, propylene glycol and pure water in the form of drops.

pharmachologic effect

The medicine belongs to the pharmacological group of antiallergic drugs. The active components of the drug block H1 type histamine receptors, providing a pronounced antiexudative, antipruritic and decongestant effect.

There is a decrease in the permeability of the walls of blood vessels and capillaries, muscle spasms and skin reactions are stopped.

The drug does not exhibit sedative properties and almost does not cause anticholinergic effects.

The therapeutic effect is observed quickly, within an hour after application. Maximum after 4 hours and lasts throughout the day. After discontinuation of the drug, pharmacological activity is recorded for another 3 days. Addiction to Cetirizine does not develop.

Cetirizine FT

Pharmacodynamics Cetirizine is a piperazine derivative and is a carboxylated metabolite of hydroxyzine. Cetirizine has selective antagonism of peripheral H1 receptors and has a pronounced antiallergic effect. Has antipruritic and antiexudative effect. It has almost no effect on other types of receptors, does not have anticholinergic and antiserotonergic effects. Cetirizine affects the “early” histamine-dependent stage of the allergic reaction, and also limits the release of inflammatory mediators at the “late” stage of the allergic reaction, and has an anti-inflammatory effect. It reduces the migration of eosinoyls, neutrophils and basophils, stabilizes the membranes of mast cells. Reduces capillary permeability, prevents the development of tissue edema, and eliminates spasm of smooth muscles. Eliminates skin reaction to the introduction of histamine, specific allergens, cooling, reduces histamine-induced bronchial obstruction in mild bronchial asthma. Cetirizine is less lipophilic compared to hydroxyzine, practically does not penetrate the blood-brain barrier and does not act on H1 receptors in the central nervous system. In therapeutic doses it does not have a sedative effect. After taking 10 mg of cetirizine, the effect develops within 20 minutes in 50% of patients, after 60 minutes in 95% of patients and lasts more than 24 hours. With repeated doses, addiction to the drug does not develop. After discontinuation of treatment, the effect persists for three days.

Pharmacokinetics Absorption: After oral administration, cetirizine is rapidly and completely absorbed from the gastrointestinal tract. Cmax in blood plasma is reached within 1.0±0.5 hours and is approximately 300 ng/ml. When taken simultaneously with food, the completeness of absorption does not change, but its rate decreases. The equilibrium state is achieved on the third day. In volunteers, pharmacokinetic parameters such as Cmax and AUC are unimodal. The degree of bioavailability is similar when cetirizine is used in the form of a solution, tablets or capsules. In the dose range from 5 to 60 mg, the pharmacokinetics are linear.

Distribution: In adults, after taking 10 mg of the drug orally and in children after taking 5 mg of the drug, the volume of distribution is approximately 35 l (0.5 l/kg) and 17 l, respectively. The binding of cetirizine to plasma proteins is 93±0.3%. Cetirizine does not alter the binding of warfarin to blood proteins. When taking 10 mg/day for 10 days, no accumulation of the drug was observed.

Metabolism: Cetirizine does not undergo first-pass metabolism. In small quantities, it is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other H1-histamine receptor blockers, which metabolize with the participation of the cytochrome P 450 system).

Excretion: About 2/3 of the administered dose of cetirizine is excreted unchanged from the body in the urine. The half-life in adults is about 10 hours, in children 6-12 years old - about 6 hours, in children aged 2-6 years - 5 hours, from 6 months to 2 years - 3.1 hours. After taking 10 mg of the drug in adults, total clearance increases to 0.6 ml/min/kg. in children after taking 5 mg - up to 0.93 ml/min/kg. After discontinuation of cetirizine, its blood level quickly decreases to undetectable low values.

In elderly patients and patients with chronic liver dysfunction, after a single dose of cetirizine at a dose of 10 mg, T1/2 increases by approximately 50%, and clearance decreases by 40% compared to middle-aged patients. In patients with mild renal impairment (creatinine clearance > 40 ml/min), the pharmacokinetic parameters of cetirizine are similar to those in healthy volunteers. In patients with moderate renal failure and in patients. patients on hemodialysis (creatinine clearance < 7 ml/min), a single dose of 10 mg of the drug led to a threefold prolongation of T1/2 and a decrease in clearance by 70%, which requires dose adjustment. Cetirizine is not removed from the body by hemodialysis.

Contraindications

Do not use an antihistamine in the following cases:

1. The period of bearing a child.
2. Breast-feeding.
3. Children's age up to 6 years.
4. Lactose intolerance and poor absorption.
5. Kidney failure.
6. Individual intolerance to drugs.
7. Malalabsorption of glucose and galactose.

Cetirizine should be prescribed with caution to elderly people and those with serious kidney disease. Also for patients undergoing treatment with barbiturates, narcotic analgesics, and benzodiazepines.

Cetirizine

Description of selected adverse reactions:

Cases of pruritus, including intense itching and/or urticaria, have been reported following discontinuation of cetirizine.

If you experience the side effects listed in the instructions, or they get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms observed after apparent drug overdose have affected the central nervous system or have been associated with a possible anticholinergic effect. Symptoms that occurred after taking at least five times the recommended daily dose included the following: confusion, diarrhea, fatigue, headache, malaise, mydriasis, itching, restlessness, sedation, somnolence, stupor, tachycardia, tremor, urinary retention.

Treatment:

There is no specific antidote.

In case of overdose, symptomatic or supportive treatment is recommended. Gastric lavage and/or activated charcoal may be effective if the overdose has occurred recently. Cetirizine is partially eliminated by dialysis.

Interaction with other drugs

Concomitant use with azithromycin, cimetidine, erythromycin, ketaconazole or pseudoephedrine does not affect the pharmacokinetic parameters of cetirizine.

No pharmacokinetic interactions were observed. in vitro test

, cetirizine does not affect the protein binding effect of warfarin. Concomitant use of azithromycin, erythromycin, ketoconazole, theophylline and pseudoephedrine did not reveal significant changes in clinical laboratory parameters, vital signs and ECG.

In a study of co-administration of theophylline (400 mg per day) and cetirizine (20 mg per day), a small but statistically significant increase in 24-hour AUC (area under the curve) was found by 19% for cetirizine and 11% for theophylline. In addition, maximum plasma levels increased to 7.7% and

6.4%, respectively, for cetirizine and theophylline. At the same time, the clearance of cetirizine decreased by -16%, and also by -10% in the case of theophylline, when cetirizine was taken by patients who had previously received treatment with theophylline. However, pretreatment with cetirizine did not significantly affect the pharmacokinetic parameters of theophylline.

Side effects

Taking an antihistamine may be accompanied by side effects. More common:

1. Stool disorder.
2. Excitement, nervousness.
3. Asthenia.
4. Skin rashes, itching, swelling.
5. Parasthesia.
6. The following side effects occur less frequently:
7. Quincke's edema, urticaria.
8. Urinary dysfunction.
9. Increased body weight.
10. Movement disorders.
11. Drowsiness or insomnia.
12. Loss of consciousness.
13. Depression, aggression.
14. Increased heart rate.
15. Signs of hepatitis.

Instructions for use

The dosage and duration of the course of Cetirizine depends on the age of the patient, diagnosis and dosage form of the drug.

The product in the form of drops is used according to the following scheme:

• Children 1-2 years old - 5 drops 2 times a day.
• Children 3-6 years old - 10 drops before bedtime.
• Patients 6-12 years old - no more than 20 drops in the evening.
• Children over 12 years of age and adults - 20 drops once.

For elderly people, the dosage is not changed. In case of kidney disease, dosage adjustment is important. For long-term allergic reactions, the course is 3-6 weeks. In case of short-term effects of allergens on the body, the medicine is used for no more than a week.

Cetirizine tablets are taken orally and should not be chewed. It is recommended to drink before bedtime. Children from 6 to 12 years old are prescribed 10 mg once a day if their weight is more than 30 kg and 5 mg per day if their body weight is up to 30 kg. For patients over 12 years of age, 10 mg per day is indicated.

Cetirizine, drops

Dosage regimen

Adults and children over 12 years old

The recommended dose is 10 mg (24 drops) once daily.

Children 6-12 years old

The recommended dose is 5 mg (12 drops) twice daily.

Children 2-5 years old

The recommended dose is 2.5 mg (6 drops) twice daily.

Children from 1 year to 2 years

The recommended dose is 2.5 mg (6 drops) once or twice daily.

Children from 6 months to 1 year

The recommended dose is 2.5 mg (6 drops) once daily.

The maximum duration of treatment in children with seasonal rhinitis should not exceed 4 weeks.

Special patient groups

Elderly

According to available data, with normal renal function, age is not a reason to reduce the dose.

Patients with impaired renal function

There is no data confirming the effectiveness/safety of the drug in patients with impaired renal function. Since cetirizine is mainly excreted through the kidneys (see section “Pharmacokinetic properties”), if it is impossible to use alternative treatment, the dose of the drug should be selected individually, taking into account renal function. The table below helps you choose the right dose. To use this table, it is necessary to determine creatinine clearance (CC) in ml/min. To do this, it is necessary to determine the serum creatinine level and calculate CC using the following formula:

CC = [140 - age (in years)] x weight (kg) (x 0.85 for women)

72 x serum creatinine (mg/dL)

Dose adjustment in patients with impaired renal function:

For children with impaired renal function, the dose should be selected individually, taking into account renal clearance, as well as the age and body weight of the patient.

Patients with impaired liver function

In patients with only liver dysfunction, there is no need for dose adjustment.

Patients with impaired liver and kidney function

Dose adjustment is recommended (see section “Patients with impaired renal function” above).

Mode of application

Drops for oral administration.

The use of the drug does not depend on food intake (see section “Pharmacokinetic properties”).

The solution should either be dripped into a spoon or diluted with water and taken orally. If the solution is diluted with water, then it should be taken into account that the volume of liquid used to dissolve the drug corresponds to the amount of liquid that the patient is able to drink. This is especially important when dosing the drug to children.

How many days should you take Cetirizine?

The duration of antihistamine therapy directly depends on the diagnosis. On average, the medicine is prescribed for 1 week. The maximum duration is a month.

According to external factors and the patient’s well-being, course correction is possible.

Can I take it during pregnancy?

There have been no clinical trials on the use of the drug during pregnancy. Therefore, bearing a child is an absolute contraindication to the use of the drug.