Zyrtec 10 mg, 30 film-coated tablets

Contraindications

You should stop taking the drug in the following cases:

• increased susceptibility to any component of the drug;
• kidney disease;
• period of bearing a child;
• lactation period;
• children under 6 months.

Can be used with caution when:

• epilepsy;
• elderly people;
• chronic renal failure;
• tendency to urinary retention.

The medicine in tablet form is also contraindicated in case of galactose allergy and in children under 6 years of age.

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.

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.

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.

How to take Zyrtec

Drops

The dose is determined depending on the age category of the patient:

• a child over 6 years old and an adult can be given 10 drops (if necessary, you can gradually increase to 20 drops);
• children aged 2-6 years are given 5 drops 2 times a day or 10 drops per 1 dose;
• a child from 1 to 2 years old can be given 5 drops up to 2 times a day;
• from 6 months to a year, 5 drops are prescribed once a day.

Pills

An adult patient and a child over 6 years old can be given ½ tablet per day (depending on the condition, a whole tablet may be prescribed).

Up to 6 years of age, the drug in tablet form is contraindicated.

Zyrtec 10 mg, 30 film-coated tablets

Registration Certificate Holder

UCB FARCHIM (Switzerland)

Dosage form

Medicine - Zyrtec®

Description

Film-coated tablets

white, oblong, with biconvex surfaces, with one-sided score and “Y” engraving on both sides of the score.

1 tab.

Cetirizine dihydrochloride 10 mg

Excipients

: microcrystalline cellulose, lactose monohydrate, colloidal silicon dioxide, magnesium stearate; Opadry® Y-1-7000 (hypromellose (E464), titanium dioxide (E171), macrogol 400).

7 pcs. - blisters (1) - cardboard packs. 10 pieces. - blisters (1) - cardboard packs. 10 pieces. - blisters (2) - 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

special instructions

Shelf life is 5 years from the date of production of the drug. Can be purchased at any pharmacy without a doctor's prescription. It should be kept in a cool place, out of reach of children.

The drug should not be taken together with alcohol, since alcohol increases the likelihood of negative effects on the central nervous system.

The drug should be taken with extreme caution in conditions such as spinal cord injuries, prostatic hyperplasia, which can lead to urinary retention. The medicine may cause the condition to worsen.

After taking the medication, it is better to refrain for some time from driving a vehicle or other mechanisms that require increased concentration.

Under no circumstances should the drug be given to children under 1 year of age who are at risk of sudden death syndrome.

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.

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.

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.

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.

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.