Cetirizine-Teva, 10 mg 10 pcs

Pharmacotherapeutic group: anti-allergic agent H₁-histamine receptor blocker

The ATX code: R06AE07

Pharmacological properties

Pharmacodynamics

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

In addition to its antihistamine effect, cetirizine prevents and relieves allergic reactions: in a dose of 10 mg once or twice daily, it inhibits the late phase of eosinophil aggregation in the skin and conjunctiva of patients with allergic reactions.

Clinical efficacy and safety. Studies in healthy volunteers have shown that cetirizine at doses of 5 or 10 mg significantly inhibits rash and redness reactions to high concentrations of histamine injected into the skin, but no correlation with efficacy has been established.

In a 6-week placebo-controlled study involving 186 patients with allergic rhinitis and concomitant mild to moderate bronchial asthma, cetirizine once daily at a dose of 10 mg was shown to reduce rhinitis symptoms and not affect lung function.

The results of this study confirm the safety of cetirizine in patients with allergies and mild to moderate bronchial asthma.

The placebo-controlled study showed that administration of cetirizine at a dose of 60 mg daily for 7 days did not cause clinically significant prolongation of the QT interval.

The administration of cetirizine at the recommended dose was shown to improve quality of life in patients with year-round and seasonal allergic rhinitis.

Children. A 35-day study involving patients aged 5-12 years showed no evidence of insensitivity to the antihistamine effect of cetirizine. Normal skin response to histamine was restored within three days of drug withdrawal with repeated use.

Pharmacokinetics

The pharmacokinetic parameters of cetirizine change linearly when used in doses from 5 to 60 mg.

Extraction. Maximum plasma concentration is reached after 1±0.5 hours and is 300 ng/ml.

The various pharmacokinetic parameters such as maximum plasma concentration (C_max) and area under the concentration-time curve (AUC) are uniform.

Eating does not affect the completeness of cetirizine absorption, although its rate is reduced. The bioavailability of different dosage forms of cetirizine (solution, capsules, tablets) is comparable.

Distribution. Cetirizine is 93±0.3% bound to blood plasma proteins. The apparent volume of distribution (V_d) is 0.5 l/kg. Cetirizine has no effect on warfarin binding to proteins.

Metabolism. Cetirizine does not undergo extensive primary metabolism.

Elimation. The elimination half-life (T_1/2) is approximately 10 hours.

There was no cetirizine cumulation when the drug was taken in a daily dose of 10 mg for 10 days.

Approximately 2/3 of the dose taken is excreted unchanged in the urine.

Elderly patients. In 16 elderly persons, the T_1/2 was 50% higher and clearance was 40% lower at a single dose of 10 mg compared with non-elderly persons.

The decreased clearance of cetirizine in elderly patients is probably due to decreased renal function in this patient population.

Patients with renal impairment. In patients with mild renal impairment (creatinine clearance (CK) > 40 ml/min), pharmacokinetic parameters are similar to those in healthy volunteers with normal renal function.

In patients with moderate renal impairment and in patients on hemodialysis (CK < 7 ml/min), the T_1/2 prolongs by 3 times and total clearance decreases by 70% relative to healthy volunteers with normal renal function when taking the drug orally in 10 mg dose.

In patients with moderate to severe renal impairment, an appropriate change in dosing regimen is required. Cetirizine is practically not eliminated from the body by hemodialysis.

Patients with hepatic impairment. In patients with chronic liver disease (hepatocellular, cholestatic, and biliary cirrhosis), a single dose of 10 or 20 mg increases T_1/2 by approximately 50% and decreases clearance by 40% compared to healthy subjects. Dose adjustment is necessary only if the patient with hepatic impairment also has concomitant renal impairment.

Children. T_1/2 in children 6 to 12 years old is 6 hours, 2 to 6 years old is 5 hours, 6 months to 2 years old is reduced to 3.1 hours.

Indications

Allergies, Increased lacrimation, Pollinosis, Eczema, Allergic conjunctivitis, Skin itching, Runny nose (rhinitis), Urticaria, Quincke’s oedema, Allergic rhinitis, Sneezing

Cetirizine dihydrochloride is indicated for use in adults and children 6 years and older for relief:

• nasal and ocular symptoms of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis: Itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia;
• symptoms of chronic idiopathic urticaria.

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Active ingredient

Cetirizine

Composition

One tablet contains:
active ingredient cetirizine dihydrochloride 10.00 mg;
excipients: Microcrystalline cellulose (Avicel PH 102) 40.00 mg, lactose monohydrate 63.50 mg, colloidal silica (colloidal anhydrous silica) 0.50 mg, magnesium stearate 1.00 mg; Opadray OY-GM-28900 white coating: Hypromellose (E464) 0.94 mg, polydextrose 0.94 mg, titanium dioxide (E171) 0.94 mg, macrogol-4000 (polyethylene glycol-4000) 0.18 mg.

How to take, the dosage

Ingestion. Tablets are recommended with a glass of water, without chewing, preferably in the evening.

Adults.

10 mg (1 tablet) once daily.

Elderly patients

There is no need to reduce the dosage in elderly patients if renal function is not impaired.

Patients with renal impairment

Because cetirizine-Teva is mainly excreted by the kidneys (see subsection “Pharmacokinetics of cetirizine-Teva”). If no alternative treatment is available, in patients with renal impairment the dosing regimen of the drug should be adjusted according to renal function (creatinine clearance CK value).

The creatinine clearance (CK) for men can be calculated based on serum creatinine concentration using the following formula:

The IQ for women can be calculated by multiplying the value obtained by a factor of 0.85.

Dosing in adult patients with renal failure

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Patients with impaired liver function

In patients with only impaired liver function, no dosing adjustment is necessary.

In patients with impaired hepatic and renal function, dosing adjustments are recommended (see table above. Table above)

Children

Children 6 to 12 years of age

5 mg (1/2 tablet) twice daily

Children over 12 years

10 mg (1 tablet) once daily

Sometimes an initial dose of 5 mg (1/2 tablet) may be sufficient if satisfactory symptom control can be achieved.

In children with renal insufficiency the dose is adjusted for CK and body weight.

If after treatment, there is no improvement or if new symptoms appear, a doctor should be consulted.

Please only use the drug according to the route and dosage listed in the directions.

Interaction

Based on the analysis of pharmacodynamics, pharmacokinetics of cetirizine interactions with other medicinal products are unlikely.

No significant interactions with pseudoephedrine and theophylline (at a dose of 400 mg per day) have been noted in specific drug interaction studies.

The level of absorption of cetirizine is not decreased in connection with food intake, but the rate of absorption is reduced.

The concomitant use of cetirizine with alcohol and other CNS depressant drugs may further decrease concentration and responsiveness, although cetirizine does not enhance the effect of alcohol (at a blood concentration of 0.5 g/l).

If you are using the above or other medicinal products
(including over-the-counter medicines), consult your doctor before using Cetirizine-Teva.

Special Instructions

In patients with spinal cord injury, prostatic hyperplasia,
as well as in the presence of other predisposing factors to urinary retention, caution is required because cetirizine may increase the risk of urinary retention.

In patients with renal insufficiency, the dosing regimen of the drug should be adjusted (see section “Dosage and administration”).

Because of the possible reduction of renal function in elderly patients, the dosing regimen of the drug should be adjusted (see section “Dosage and administration”).

We recommend caution when using cetirizine concomitantly
with alcohol, because cetirizine may lead to increased somnolence.

Caution should be exercised in patients with epilepsy and increased seizure readiness.

A 3-day “washout” period is recommended before allergy testing because H₁-histamine receptor blockers inhibit the development of cutaneous allergic reactions.

Cetirizine film-coated tablets should not be used in patients with hereditary galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome.

After discontinuation of cetirizine use, itching and/or urticaria may occur, even if these symptoms were absent at the beginning of treatment. In some cases, the symptoms may be intense and require resumption of cetirizine. Symptoms disappear when cetirizine administration is resumed.

Children. Cetirizine film-coated tablets are contraindicated in children
under 6 years of age because this dosage form does not allow for a suitable dosage for this age group.

Influence on driving and operating ability

An objective assessment of driving and operating ability has not reliably revealed any adverse effects when taking the drug in the recommended dose. However, patients with symptoms of somnolence during the use of the drug should refrain from driving a vehicle, engaging in potentially dangerous activities or operating machinery requiring increased concentration and quick psychomotor reactions.

Synopsis

Biconvex oblong-shaped, film-coated tablets of white or almost white color. On one side there is an engraving “C10”, on the other side there is a separating risk. On the cross section the core is white or almost white. The tablets should be without cracks and chips.

Contraindications

• High sensitivity to cetirizine, hydroxyzine or piperazine derivatives as well as other drug components.
• Terminal stage of renal failure (creatinine clearance < 10 ml/min).
• Children under 6 years of age (for this dosage form).
• Pregnancy.
• Hereditary galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.

With caution

In patients:

• with chronic renal insufficiency (with creatinine clearance > 10 ml per min requires dosing regimen adjustment);
• elderly (with age-related decrease in glomerular filtration);
• with epilepsy and with increased seizure readiness;
• with predisposing factors to urinary retention (see section “Special Indications.
• when breastfeeding

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Side effects

Data from clinical trials

Review

Results of clinical studies have demonstrated that the use of cetirizine in recommended doses results in the development of minor adverse effects on the CNS, including drowsiness, fatigue, dizziness, and headache.
In some cases paradoxical CNS stimulation has been reported.

While cetirizine is a selective blocker of peripheral
H₁ receptors and has virtually no anticholinergic effects, there have been
reported isolated cases of difficulty urinating, impaired accommodation and dry mouth.

Liver dysfunction accompanied by increased liver enzymes and bilirubin has been reported. In most cases the adverse events resolved after discontinuation of cetirizine dihydrochloride.

List of adverse reactions

. There are data from double-blind controlled clinical trials comparing cetirizine and placebo or other antihistamines used in recommended doses (10 mg once daily for cetirizine) in more than 3,200 patients from which reliable safety data analysis can be performed.

According to the pooled analysis, the following adverse reactions with an incidence of 1.0% or higher were identified in placebo-controlled trials when cetirizine was used in a dose of 10 mg:

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Although the incidence of somnolence was higher in the cetirizine group than in the placebo group, in most cases this adverse event was mild to moderate in severity. Objective evaluations in other studies have confirmed that the use of cetirizine at the recommended daily dose in healthy young volunteers does not affect their daily activities.

Children

In placebo-controlled studies, the following adverse reactions were found in children aged 6 months to 12 years with an incidence of 1% or higher:

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Post-registration experience

In addition to the adverse events identified in the clinical studies described above, the following adverse reactions have been observed during post-registration use of the drug.

The adverse reactions are classified according to the classification of the World Health Organization (WHO): Very common (≥1/10); common (≥1/100, < 1/10); infrequent (≥1/1000, < 1/100); rare (≥1/10000, < 1/1000); very rare (< 1/10000); frequency unknown (cannot be determined from available data).

Blood and lymphatic system: very rare – thrombocytopenia.

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

Metabolic disorders and eating disorders: frequency unknown – increase in appetite.

Mental disorders: infrequent – agitation; rare – aggression, confusion, depression, hallucinations, sleep disturbance; very rare – tics; frequency unknown – suicidal ideation, sleep disturbance (including nightmares).

Nervous system disorders: infrequent – paresthesias; rare – seizures; very rare – perversion of taste, dyskinesia, dystonia, syncope, tremor; frequency unknown – memory disorders, including amnesia, deafness.

Visual side: very rarely – accommodation disorder, blurred vision, nystagmus; frequency unknown – vasculitis.

Hearing organs: frequency unknown – vertigo.

Cardiovascular system: rare – tachycardia.

Digestive system disorders: infrequent – diarrhea.

Hepatobiliary disorders: frequently – liver failure with changes in functional liver function tests (increased activity of transaminases, alkaline phosphatase, gamma-glutamyltransferase and bilirubin).

Skin: infrequent – rash, pruritus; rare – urticaria; very rare – angioedema, persistent erythema drug; frequency unknown – acute generalized exanthematous pustulosis.

Since the urinary system: very rare – dysuria, enuresis; frequency unknown – urinary retention.

General disorders: infrequent – asthenia, malaise; rarely – peripheral edema.

Studies: frequently – increase in body weight.

Description of individual adverse reactions. After discontinuation of cetirizine, cases of pruritus, (including intense pruritus) and/or urticaria have been reported.

Adverse Reaction Alerting

The system for reporting suspected adverse reactions after drug registration is important.

This allows for continuous monitoring of the benefit/risk ratio of the drug.

If any of the side effects listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.