Zyrtec 10 mg/ml drops for oral administration, 20 ml dropper bottle

Composition and release form

in a blister 7 or 10 pcs.; in a cardboard pack there are 1 (7 or 10 tablets) or 2 (10 tablets) blisters.

in dark glass dropper bottles of 10 or 20 ml (1 ml = 20 drops); 1 bottle in a cardboard pack.

Pharmacodynamics

Cetirizine, the active substance of Zyrtec®, is a metabolite of hydroxyzine, belongs to the group of competitive histamine antagonists and blocks H1 histamine receptors. Cetirizine prevents the development and alleviates the course of allergic reactions, has antipruritic and antiexudative effects. Cetirizine affects the early histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators at the late stage of the allergic reaction, and also reduces the migration of eosinophils, neutrophils and basophils, and stabilizes mast cell membranes. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as to cooling (with cold urticaria). Reduces histamine-induced bronchoconstriction in mild bronchial asthma. Cetirizine has virtually no anticholinergic and antiserotonin effects. In therapeutic doses, the drug has virtually no sedative effect. The effect after taking cetirizine in a single dose of 10 mg develops after 20 minutes (in 50% of patients), after 60 minutes (in 95% of patients) and lasts more than 24 hours. During a course of treatment, tolerance to the antihistamine effect of cetirizine does not develop. After discontinuation of therapy, the effect lasts up to 3 days.

Zyrtec 10 mg/ml drops for oral administration, 20 ml dropper bottle

Registration Certificate Holder

UCB FARCHIM (Switzerland)

Dosage form

Medicine - Zyrtec®

Description

Drops for oral administration

colorless, transparent, with the smell of acetic acid.

1 ml

Cetirizine dihydrochloride 10 mg

Excipients

: glycerol, propylene glycol, sodium saccharinate, methylparabenzene, propylparabenzene, sodium acetate, glacial acetic acid, purified water.

10 ml - dark glass dropper bottle (1) - cardboard packs. 20 ml - dark glass dropper bottle (1) - cardboard packs.

Indications

• treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis, such as itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia;
• hay fever (hay fever);
• urticaria (including chronic idiopathic urticaria);
• Quincke's edema;
• other allergic dermatoses (including atopic dermatitis), accompanied by itching and rashes.

Contraindications for use

• end-stage renal failure (CC < 10 ml/min);
• pregnancy;
• lactation period (breastfeeding);
• hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;
• children under 6 years of age (for tablets);
• children up to 6 months (for drops);
• hypersensitivity to the components of the drug;
• hypersensitivity to hydroxyzine.

Carefully

The drug should be prescribed for chronic renal failure (correction of the dosage regimen is required), for chronic liver diseases, and for elderly patients (due to a possible decrease in glomerular filtration).

pharmachologic effect

Antiallergic drug. Histamine H1 receptor blocker, competitive histamine antagonist, hydroxyzine metabolite. Prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects.

Affects the early histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators at the late stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils, stabilizes mast cell membranes. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as to cooling (with “cold” urticaria). Reduces histamine-induced bronchoconstriction in mild bronchial asthma.

It has virtually no anticholinergic and antiserotonin effects. In therapeutic doses it has virtually no sedative effect.

After a single dose of cetirizine at a dose of 10 mg, the onset of effect is observed after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients), the effect lasts more than 24 hours. During a course of treatment, tolerance to the antihistamine effect of cetirizine does not develop. After stopping treatment, the effect lasts up to 3 days.

Drug interactions

When studying the drug interactions of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically significant adverse interactions were identified.

When administered simultaneously with theophylline (400 mg/day), the total clearance of cetirizine is reduced by 16% (the kinetics of theophylline does not change).

When administered simultaneously with macrolides and ketoconazole, no changes were noted on the ECG.

When using the drug in therapeutic doses, no data on interaction with alcohol (at a blood alcohol concentration of 0.5 g/l) were obtained. However, the patient should refrain from drinking alcohol during drug therapy to avoid depression of the central nervous system.

Dosage regimen

The drug is prescribed orally.

Adults and children over 6 years old

prescribed at a dose of 10 mg (1 tablet or 20 drops)/day. Adults - 10 mg 1 time/day; children - 5 mg 2 times / day or 10 mg 1 time / day. Sometimes an initial dose of 5 mg may be sufficient to achieve a therapeutic effect.

Children aged 2 to 6 years

prescribed 2.5 mg (5 drops) 2 times/day or 5 mg (10 drops) 1 time/day.

Children aged 1 to 2 years

Prescribe 2.5 mg (5 drops) up to 2 times a day.

Children aged 6 months to 12 months

prescribed 2.5 mg (5 drops) 1 time/day.

For renal failure

and in elderly patients, the dose of the drug should be adjusted depending on the value of CC.

CC can be calculated based on serum creatinine concentration using the following formula:

For men: CC (ml/min) = [140 - age (years)] x body weight (kg)/72 x serum creatinine (mg/dl);

CC for women can be calculated by multiplying the resulting value by a coefficient of 0.85.

Adult patients with renal and hepatic insufficiency

The dose is set according to the following table.
Renal failure KK (ml/min) Dosage regimen
Norm≥8010 mg/day Mild50-7910 mg/dayModerate30-495 mg/daySevere<305 mg every other dayTerminal stage - patients on dialysis<10 The drug is contraindicated

Patients with impaired liver function only

no dosage adjustment is required.

Overdose

Symptoms:

When taking the drug once in a dose of more than 50 mg, confusion, diarrhea, dizziness, increased fatigue, headache, malaise, mydriasis, itching, weakness, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention are possible.

Treatment:

Immediately after taking the drug, you should perform gastric lavage or artificially induce vomiting. It is recommended to prescribe activated carbon and carry out symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective.

Side effect

From the hematopoietic system:

thrombocytopenia.

From the nervous system:

drowsiness, dizziness, headache, aggression, agitation, confusion, depression, hallucinations, insomnia, tic, convulsions, dyskinesia, dystonia, paresthesia, fainting, tremor.

From the side of the organ of vision:

disturbance of accommodation, blurred vision, nystagmus.

From the cardiovascular system:

tachycardia.

From the respiratory system:

rhinitis, pharyngitis.

From the digestive system:

dry mouth, nausea, abdominal pain, diarrhea, liver dysfunction (increased levels of transaminases, alkaline phosphatase, GGT, bilirubin).

From the urinary system:

urination disorder, enuresis.

Allergic reactions:

itching, rash, urticaria, angioedema, increased sensitivity, up to the development of anaphylactic shock.

From the side of metabolism:

increase in body weight.
Other:
fatigue, asthenia, malaise, swelling.

Side effects occur in very rare cases.

special instructions

Children aged 6 months to 6 years

Zyrtec® is prescribed in the dosage form of drops for oral administration at 10 mg/ml.
Effect on the ability to drive vehicles and operate machinery.
An objective assessment of the ability to drive vehicles and operate machinery did not reliably reveal any adverse reactions when taking the drug at the recommended dose. But, nevertheless, during the period of taking the drug, it is advisable to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Storage conditions

Tablets should be stored in their original packaging at a temperature not exceeding 30°C. Drops for oral administration should be stored at a temperature not exceeding 25°C.

Best before date

The shelf life of the drug is 5 years.

The drug should be stored out of the reach of children.

Use during pregnancy and breastfeeding

Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Use for renal impairment

Restrictions for impaired renal function - With caution.

Carefully _

the drug should be prescribed for chronic renal failure (moderate or severe), as well as for elderly patients (due to a possible decrease in glomerular filtration).

In case of renal failure, the dose is reduced depending on the QC.

Contraindicated in end-stage renal failure (CC < 10 ml/min).

Use in elderly patients

Restrictions for elderly patients - Use with caution.

Carefully _

the drug should be prescribed to elderly patients (due to a possible decrease in glomerular filtration).

Use in children

Restrictions for children - Contraindicated. Contraindicated in children under 6 years of age (for tablets), in children under 6 months of age (for drops).

Terms of sale

The drug is approved for use as a means of OTC.

Contacts for inquiries

YUSB PHARMA S.A. (Belgium)

YUSB Pharma LLC

105082 Moscow, Perevedenovsky per. 13, p. 21 Tel.; Fax

Pharmacokinetics

The pharmacokinetic parameters of cetirizine change linearly.

Suction.

After oral administration, the drug is quickly and completely absorbed from the gastrointestinal tract. Eating does not affect the completeness of absorption, although its speed decreases. In adults, after a single dose of the drug in a therapeutic dose, Cmax in blood plasma is 300 ng/ml and is achieved after (1±0.5) hours.

Distribution.

Cetirizine is (93±0.3)% bound to blood plasma proteins. Vd is 0.5 l/kg. When taking the drug at a dose of 10 mg for 10 days, no accumulation of cetirizine is observed.

Metabolism.

In small quantities, it is metabolized in the body by O-dealkylation (unlike other H1-histamine receptor antagonists, which are metabolized in the liver using the cytochrome system) to form a pharmacologically inactive metabolite.

Excretion.

In adults, T1/2 is approximately 10 hours; in children from 6 to 12 years - 6 hours, from 2 to 6 years - 5 hours, from 6 months to 2 years - 3.1 hours. Approximately 2/3 of the dose taken is excreted unchanged by the kidneys.

In elderly patients and patients with chronic liver diseases, with a single dose of 10 mg, T1/2 increases by approximately 50%, and systemic clearance decreases by 40%.

In patients with mild renal failure (Cl creatinine >40 ml/min), pharmacokinetic parameters are similar to those in patients with normal renal function.

In patients with moderate renal failure and in patients on hemodialysis (Cl creatinine <7 ml/min), when taking the drug orally at a dose of 10 mg, T1/2 is extended by 3 times, and the total clearance is reduced by 70% relative to patients with normal renal function, which requires appropriate changes in the dosage regimen. Cetirizine is practically not removed from the body during hemodialysis.

Contraindications

Common to all dosage forms

hypersensitivity to cetirizine, hydroxyzine or piperazine derivatives, as well as to any of the components of the drug;

end-stage renal failure (creatinine clearance <10 ml/min)

pregnancy;

breastfeeding period.

Carefully:

chronic renal failure (moderate to severe, dosage adjustment required); old age (possibly decreased glomerular filtration rate).

For film-coated tablets, additionally:

hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;

children under 6 years of age.

Carefully:

chronic liver diseases.

For drops additionally:

children under 6 months of age (due to limited data on the effectiveness and safety of drugs).

Carefully:

epilepsy and patients with increased convulsive readiness; children's age up to 1 year.

Use during pregnancy and breastfeeding

Experimental studies on animals did not reveal any direct or indirect adverse effects of cetirizine on the developing fetus (including in the postnatal period), the course of pregnancy and childbirth also did not change.

Adequate and strictly controlled clinical studies on the safety of the drug have not been conducted, therefore Zirtec® should not be prescribed during pregnancy.

Cetirizine is excreted in breast milk, so the attending physician should decide whether to stop breastfeeding while using the drug.

Can I take Zyrtec during pregnancy?

Medical research on the effect of the drug on the body during pregnancy was carried out exclusively on animals. Their results deny the possibility of a negative impact on the developing fetus and the condition of the expectant mother. Due to the lack of necessary data, the medication can be used only after examination by a doctor.

The active ingredient may pass into breast milk. Therefore, if there is a need to take the drug, you should temporarily switch to artificial feeding.

Side effects

Common to all dosage forms

Possible side effects are listed below by body system and frequency of occurrence: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥ 1/10000, <1/1000), very rare (<1/10000), frequency unknown (due to insufficient data).

From the nervous system:

often - headache, increased fatigue, dizziness, drowsiness; infrequently - asthenia, paresthesia, agitation; rarely - aggression, confusion, hallucinations, depression, convulsions, sleep disturbance; very rarely - taste perversion, dyskinesia, dystonia, fainting, tremor, tic; frequency unknown - memory impairment, including amnesia.

From the side of the organ of vision:

very rarely - disturbance of accommodation, blurred vision, nystagmus.

From the digestive system:

often - dry mouth, nausea; infrequently - diarrhea, abdominal pain.

From the SSS side:

rarely - tachycardia.

From the respiratory system:

often - rhinitis, pharyngitis.

From the side of metabolism:

rarely - weight gain.

From the urinary system:

very rarely - dysuria, enuresis.

From the laboratory parameters:

rarely - changes in liver function tests (increased activity of transaminases, alkaline phosphatase, GGT and bilirubin); very rarely - thrombocytopenia.

Allergic reactions:

uncommon - rash, itching; rarely - urticaria, hypersensitivity reactions; very rarely - angioedema, anaphylactic shock, persistent erythema.

Common disorders:

infrequently - malaise; rarely - peripheral edema.

Adverse reactions and overdose

Common negative side effects from taking the drug include:

• headache;
• lethargy;
• dizziness;
• excessive fatigue;
• vomiting, nausea;
• feeling of dryness in the mouth.

Slightly less common:

• stomach upset;
• nervous state;
• allergic skin reaction.

• peripheral edema;
• hives;
• abnormal heart rhythm;
• weight gain;
• aggressive or depressive state;
• disturbed sleep;
• convulsions.

It is extremely rare:

• taste disturbance;
• tremor;
• fainting;
• blurred vision.

There may be cases of overdose, manifested by the adverse reactions described above. In this condition, you need to induce vomiting or rinse the stomach. You can also start symptomatic therapy.

Interaction

No pharmacokinetic interaction or clinical effect was observed when co-administered with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide. When co-administered with theophylline at a dose of 400 mg 1 time per day, a decrease in creatinine Cl by 16% was noted. When co-administered with macrolides and ketoconazole, no changes were noted on the ECG.

When used in therapeutic doses, no data on interaction with alcohol have been obtained (at a blood alcohol concentration of 0.5 g/l). However, it is best to avoid drinking alcohol during treatment with cetirizine to avoid CNS depression.

Before prescribing allergy tests, a three-day “washing out” period is recommended due to the fact that H1-histamine receptor blockers inhibit the development of skin allergic reactions.

Zyrtec 10 mg 30 pcs. film-coated tablets

pharmachologic effect

Antiallergic H1-histamine receptor blocker.

Composition and release form Zirtec 10 mg 30 pcs. film-coated tablets

Film-coated tablets - 1 tablet:

• cetirizine dihydrochloride - 10 mg;
• excipients: MCC; lactose; colloidal silicon dioxide; magnesium stearate; hypromellose; titanium dioxide; Macrogol 400 (polyethylene glycol)

There are 7 or 10 pcs in a blister; 1 blister in a cardboard pack.

Description of the dosage form

Tablets: white oblong, film-coated, scored and marked on one side Y/Y.

Directions for use and doses

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: 2.5 mg (5 drops) 2 times a day or 5 mg (10 drops) 1 time a day.

Adults and children over 6 years of age: daily dose - 10 mg (1 tablet or 20 drops).

Adults - 10 mg once a day, children - 5 mg 2 times a day or 10 mg once. Sometimes an initial dose of 5 mg may be sufficient to achieve a therapeutic effect.

For patients with renal failure, the dose is reduced depending on creatinine clearance: with creatinine clearance of 30–49 ml/min - 5 mg once a day, with 10–29 ml/min - 5 mg every other day.

Pharmacodynamics

A competitive histamine antagonist, a metabolite of hydroxyzine, blocks H1 histamine receptors. Prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects. Affects the “early” histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators at the “late” stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils, stabilizes mast cell membranes. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as to cooling (with cold urticaria). Reduces histamine-induced bronchoconstriction in mild bronchial asthma. It has virtually no anticholinergic and antiserotonin effects.

In therapeutic doses it has virtually no sedative effect. The onset of effect after a single dose of 10 mg of cetirizine is after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients), the effect lasts more than 24 hours. During a course of treatment, tolerance to the antihistamine effect of cetirizine does not develop.

After stopping treatment, the effect lasts up to 3 days.

Pharmacokinetics

Rapidly absorbed when taken orally. Cmax in serum is achieved 1 hour after oral administration. Food does not affect the completeness of absorption, but prolongs the absorption process by 1 hour. 93% of cetirizine is protein bound.

The pharmacokinetic parameters of cetirizine have a linear dependence on the dose.

Volume of distribution - 0.5 l/kg. In small quantities, it is metabolized in the liver by O-desalcation to form a pharmacologically inactive metabolite (unlike other H1-histamine receptor blockers, which are metabolized in the liver with the participation of the cytochrome P450 system). Does not accumulate. 2/3 of the drug is excreted unchanged by the kidneys and about 10% in the feces. Systemic Cl - 53 ml/min. T1/2 is 7-10 hours (in children 6-12 years old - 6 hours, 2-6 years old - 5 hours, from 6 months to 2 years - 3.1 hours). In elderly patients, T1/2 increases by 50%, systemic Cl - by 40%.

Practically not removed by hemodialysis.

Passes into breast milk.

Indications for use: Zyrtec 10 mg 30 pcs. film-coated tablets

For adults and children from 6 months. and older: treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis, such as itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia, hay fever (hay fever); urticaria, including chronic idiopathic urticaria, Quincke's edema; other allergic dermatoses (including atopic dermatitis), accompanied by itching and rashes.

Contraindications

Hypersensitivity to any of the components of the drug or to hydroxyzine.

The drug is not intended for children under 6 months.

Application of Zyrtec 10 mg 30 pcs. film-coated tablets during pregnancy and breastfeeding

Not used during pregnancy and lactation.

Overdose

Symptoms (when taking the drug once in a dose of over 50 mg): drowsiness, anxiety, increased irritability, urinary retention, dry mouth, constipation, mydriasis, tachycardia. Treatment: stop taking the drug, empty your stomach, take activated charcoal, consult a doctor immediately.

Side effects of Zyrtec 10 mg 30 pcs. film-coated tablets

Drowsiness, headache, dry mouth, rarely - headache, dizziness, migraine, diarrhea, allergic reactions: angioedema, itching, rash, urticaria.

Drug interactions

No pharmacokinetic interaction or clinical effect was observed when co-administered with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide. When co-administered with theophylline at a dose of 400 mg 1 time per day, a decrease in creatinine Cl by 16% was noted.

When co-administered with macrolides and ketoconazole, no changes were noted on the ECG. When used in therapeutic doses, no data on interaction with alcohol have been obtained (at a blood alcohol concentration of 0.5 g/l). However, it is best to avoid drinking alcohol during treatment with cetirizine.

Directions for use and doses

Inside.

The tablets should be taken with a glass of liquid

Adults and children over 6 years of age: daily dose - 10 mg (1 tablet or 20 drops), sometimes an initial dose of 5 mg (1/2 tablet) may be sufficient to achieve a therapeutic effect.

Children from 6 to 12 months - 2.5 mg (5 drops) 1 time per day.

Children aged 1 to 2 years - 2.5 mg (5 drops) 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.

For patients with renal failure, the dose is reduced depending on creatinine clearance: with creatinine Cl 30-49 ml/min - 5 mg once a day, with 10-29 ml/min - 5 mg every other day.

Since Zirtec® is excreted from the body by the kidneys, when prescribing the drug to patients with renal failure and elderly patients, the dose should be adjusted depending on the creatinine clearance. Creatinine clearance for men can be calculated from serum creatinine concentration using the following formula:

Creatinine Cl, ml/min

Creatinine clearance for women can be calculated by multiplying the resulting value by a factor of 0.85.

Elderly patients with normal renal function do not require dose reduction; in patients with chronic renal failure, dose calculation should be carried out taking into account creatinine clearance according to the table below.

For adult patients with renal and hepatic insufficiency, dosing is carried out according to the table above.

For children with renal failure, adjustments are made based on creatinine clearance and body weight.

In patients with impaired liver function only, dosage regimen adjustment is not required.

Overdose

Symptoms

(when taking the drug once in a dose of 50 mg): confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, itching, weakness, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention.

Treatment:

immediately after taking the drug - gastric lavage or induction of vomiting. It is recommended to prescribe activated carbon and carry out symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective.

Negative manifestations and overdose

The most common adverse reactions are:

• headache;
• fatigue;
• dizziness;
• fast fatiguability;
• gagging;
• feeling of dry mouth.

No less common adverse reactions include:

• stomach upset;
• excited state;
• allergies in the form of skin rash;

• abnormal heartbeat;
• weight gain;
• aggressive or depressive behavior;
• disturbed sleep.

The following reactions occur much less frequently:

• taste disturbance;
• tremor;
• fainting;
• deterioration of visual acuity.

An overdose may occur, which is characterized by the above negative reactions in a more pronounced form. With such signs, it is necessary to induce vomiting or rinse the stomach. It is also worth starting treatment based on symptoms

special instructions

For children from 6 months to 6 years of age, Zyrtec® is prescribed in the dosage form of drops for oral administration at a dose of 10 mg/ml.

For drops:

Due to the potential for CNS depressant effects, caution should be exercised when prescribing Zyrtec® to children under 1 year of age who have the following risk factors for sudden infant death syndrome, such as (but not limited to):

- sleep apnea syndrome or sudden infant death syndrome in a brother or sister;

- maternal drug abuse or smoking during pregnancy;

- young age of mother (19 years and younger);

- smoking abuse by a nanny caring for a child (one pack of cigarettes a day or more);

- children who regularly fall asleep face down and are not placed on their back;

- premature (gestational age less than 37 weeks) or low birth weight (below the 10th percentile of gestational age) children;

- when taking drugs together that have a depressing effect on the central nervous system.

Caution is required when used concomitantly with alcohol (see Interactions section).

For all dosage forms

Influence on the ability to drive vehicles and operate machinery.

An objective assessment of the ability to drive vehicles and operate machinery did not reliably reveal any adverse events when taking the drug at the recommended dose. But nevertheless, during the period of taking the drug, it is advisable to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.