Zyrtec drops for oral use 10mg/ml, 20ml

Composition

Active ingredient:

cetirizine hydrochloride 10 mg;

Auxiliary substances:

glycerol-250 mg;

propylene glycol-350 mg;

sodium saccharinate-10 mg;

methylparabenzene-1.35 mg;

propylparabenzene-0.15 mg;

sodium acetate-10 mg;

glacial acetic acid-0.53 mg;

purified water-up to 1 ml

Pharmacological action

of Zyrtek-antihistamine, antiallergic.

Pharmacodynamics

Cetirizine-the Active ingredient of Zyrtek® – is a metabolite of hydroxyzine, belongs to the group of competitive histamine antagonists and blocks H1-histamine receptors.

Cetirizine prevents the development and eases the course of allergic reactions, has antipruritic and anti-exudative effects. Cetirizine affects the early histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators in the late stage of an 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 smooth muscle spasm. Eliminates skin reactions to the introduction of histamine, specific allergens, as well as cooling (with cold urticaria). Reduces histamine-induced bronchoconstriction in mild bronchial asthma.

Cetirizine does not have anticholinergic and antiserotonin effects. In therapeutic doses, the drug practically does not cause sedation. After taking cetirizine in a single dose of 10 mg, its effect develops in 20 minutes( in 50% of patients), in 60 minutes (in 95% of patients) and lasts more than 24 hours. Against the background of course treatment, tolerance to the antihistamine effect of cetirizine does not develop. After discontinuation of therapy, the effect persists for up to 3 days.

Pharmacokinetics

The pharmacokinetic parameters of cetirizine vary linearly.

Suction. After oral use, the drug is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although its rate decreases. In adults, after a single dose of the drug in a therapeutic dose, Cmax in blood plasma is 300 ng / ml and is reached in (1±0.5) hours.

Distribution. Cetirizine binds to plasma proteins by 93±0.3%. Vd is 0.5 l/kg. When taking the drug at a dose of 10 mg for 10 days, accumulation of cetirizine is not observed.

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

Output. 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 of the drug is excreted unchanged by the kidneys.

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

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

In patients with moderate renal insufficiency and in patients on hemodialysis (creatinine clearance 1/2 is extended by 3 times, and total clearance decreases by 70% relative to these indicators in patients with normal renal function, which requires an appropriate change in the dosage regimen.

Cetirizine is practically not removed from the body during hemodialysis.

Indications

• treatment of symptoms of year-round and seasonal allergic rhinitis and allergic conjunctivitis (such as itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia);
• hay fever (pollinosis);
• urticaria;
• allergic dermatoses, including atopic dermatitis, accompanied by itching and rashes.

Contraindications

• hypersensitivity to cetirizine, hydroxyzine or piperazine derivatives, as well as other components of the drug;
• end-stage renal failure (Cl creatinine
• ); breast-feeding period;
• children under 6 months of age (due to limited data on the effectiveness and safety of drugs).

With caution:  children under 1 year of age.

Side effects

From the immune system:  rarely-hypersensitivity reactions; very rarely-anaphylactic shock.

Nervous system disorders:  often-headache, fatigue, dizziness, drowsiness; infrequently-paresthesia; rarely-convulsions; very rarely-taste distortion, dyskinesia, dystonia, fainting, tremor, tic; frequency unknown-memory impairment, including amnesia.

Psychiatric disorders:  infrequently-agitation; rarely-aggression, confusion, depression, hallucinations, sleep disorders; frequency unknown-suicidal ideation.

From the side of the visual organ:  very rarely-accommodation disorders, blurred vision, nystagmus.

From the side of the hearing organ:  frequency unknown-vertigo.

From the digestive system:  often — dry mouth, nausea; infrequently-diarrhea, abdominal pain.

From the CCC side:  rarely-tachycardia.

Respiratory system disorders:  often — rhinitis, pharyngitis.

From the side of metabolism:  rarely-increased body weight.

From the urinary system:  very rarely — dysuria, enuresis; frequency unknown-urinary retention.

From the side of laboratory parameters:  rarely-changes in liver function tests (increased activity of hepatic transaminases, alkaline phosphatase, GGT, and bilirubin concentration); very rarely — thrombocytopenia.

From the side of the skin:  infrequently-rash, pruritus; rarely-urticaria; very rarely-angioedema, persistent erythema.

Common disorders:  infrequently-asthenia, malaise; rarely-peripheral edema; frequency unknown-increased appetite.

Interaction

When studying the drug interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide and antipyrine, clinically significant undesirable interactions were not detected.

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

When co-administered with ritonavir, the AUC of cetirizine increased by 40%, while the same indicator of ritonavir slightly changed (-11%).

No ECG changes were observed when concomitantly administered with macrolides (azithromycin, erythromycin) and ketoconazole.

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

A three-day “wash-off” period is recommended before the appointment of allergological tests, since H1-histamine receptor blockers inhibit the development of allergic skin reactions.

How to take, course of use and dosage

Inside.

Children over 6 years of age and adults:  the initial dose is 5 mg (1/2 tablet or 10 drops) 1 time a day, if necessary, you can increase to 10 mg (1 tablet or 20 drops) 1 time a day. Sometimes an initial dose of 5 mg (1/2 tablet or 10 drops) may be sufficient to achieve a therapeutic effect. The daily dose is 10 mg (1 tablet or 20 drops).

Children from 6 to 12 months: 2.5 mg (5 drops) 1 time a 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.

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

Overdose

Symptoms (when taking the drug once at a dose of 50 mg): confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, itching, weakness, anxiety, 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 charcoal, conduct symptomatic and maintenance therapy. There is no specific antidote. Hemodialysis is ineffective.

Special instructions

Caution should be exercised in patients with spinal cord injury, prostatic hyperplasia, or other predisposing factors to urinary retention, as cetirizine may increase the risk of urinary retention.

It is recommended to refrain from drinking alcohol (see “Interaction”).

Influence on the ability to drive vehicles and work with mechanisms. Objective assessment of the ability to drive vehicles and manage mechanisms 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 dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Due to the potential depressing effects on the central nervous system, caution should be exercised when prescribing Zyrtek® to children under the age of 1 year in the presence of the following risk factors for sudden children death syndrome, such as for example (but not limited to this list):

• the syndrome of sleep apnea or sudden children death syndrome children have a brother or sister;
• the mother’s drug abuse or Smoking during pregnancy;
• young maternal age (19 years and younger);
• the abuse of Smoking nurses who care for a child (one pack of cigarettes per day or more);
• children, regularly falling asleep face down and where not laid on the back;
• prematurity (gestational age less than 37 weeks) or born with insufficient body weight (below 10th percentile of gestational age) children;
• when co-administered drugs, providing a depressing effect on the Central nervous system.

The drug contains excipients methylparabenzene and propylparabenzene, which can cause allergic reactions, including delayed type.

Storage conditions

At a temperature not exceeding 30 °C.

Shelf life

5 years

Active ingredient

Cetirizine

Dosage form

oral drops