Cetirizine-Vertex, 10 mg 20 pcs

Name: Cetirizine-Vertex, 10 mg 20 pcs
SKU: 235421
Availability: InStock

€3.17

EAN: 4607003244705 SKU: 235421 Categories: Allergies, Medicine

Description

Pharmacotherapeutic group

Anti-allergic agent – H₁-histamine receptor blocker.

AtCode

R06AE07

Pharmacological properties

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Pharmacodynamic properties

Mechanism of action

Cetirizine, the active ingredient of the drug, is a metabolite of hydroxyzine and has an antihistamine effect with anti-allergic action. Cetirizine belongs to the group of competitive histamine antagonists and blocks H₁-histamine receptors with little effect on other receptors and has almost no anticholinergic and antiserotonin action.

Cetirizine affects the histamine-dependent stage of immediate allergic reactions and also reduces the migration of eosinophils and limits the release of mediators in delayed-type allergic reactions. It practically does not pass through the blood-brain barrier and therefore is almost incapable of reaching central H₁ receptors.

Pharmacodynamics

In studies of the effects of histamine on the skin, the effects of cetirizine at a dose of 10 mg began after 1 hour, peaked from the 2nd to 12th hour, and were still observed at statistically significant levels after 24 hours. In addition to its antihistamine effect, cetirizine also has an anti-inflammatory effect and thus has an effect on the late phase of the allergic reaction:

– At a dose of 10 mg once or twice daily, it inhibits the late phase of eosinophil aggregation in the skin;

– At a dose of 30 mg daily, it inhibits the release of eosinophils into the bronchial alveolar fluid after allergen-induced bronchial constriction;

-inhibits the kallikrein-induced late inflammatory response;

-inhibits the expression of inflammatory markers such as ICAM-1 or VCAM-1;

inhibits the action of histaminoliberators such as PAF or Substance P.

Pharmacokinetics:

Intake

After oral administration, the drug is rapidly absorbed from the gastrointestinal tract. The pharmacokinetic parameters of cetirizine change linearly when administered in doses from 5 to 60 mg. The equilibrium concentration is reached after 3 days.

The pharmacokinetic profile of cetirizine is similar in adults and children. In children after taking cetirizine in a dose of 5 mg, the concentration of the active substance in the body is the same as in adults after taking 10 mg. In adults after the use of cetirizine in dose of 10 mg the maximum concentration (C_max) in blood plasma is reached after 1-2 hours and is 350 ng/ml. In children after cetirizine administration in a dose of 5 mg, the maximum concentration (C_max) in plasma is reached after 1 hour and is 275 ng/ml.

When cetirizine is taken in the form of drops, maximum plasma concentrations are reached at a higher rate.

Distribution

Distribution after 10 mg administration is 35 liters in adults, and plasma protein binding is 93%. In children, the volume of distribution after administration of 5 mg is approximately 17 liters.

A small amount of cetirizine is excreted into breast milk.

Metabolism

In adults, 60% of the dose is excreted unchanged by the kidneys.

Elimation

After 10 mg administration in adults, total clearance of cetirizine is 0.60 ml/min/kg; the half-life (T_½) is approximately 10 hours. Multiple doses do not alter pharmacokinetic parameters. No cetirizine cumulation was observed when cetirizine was administered in a daily dose of 10 mg for 10 days.

After the end of treatment, plasma levels of cetirizine rapidly fall below detectable limits. Repeated allergy tests can be resumed after 3 days.

Separate patient groups

Elderly patients:

In 16 elderly individuals, the T_½ was 50% higher and the excretion rate was 40% lower in a single 10-mg dose of cetirizine compared with a control group. The decreased clearance of cetirizine in elderly patients is probably due to decreased renal function in this category of patients.

Children:

In children aged 6 to 12 years, 70% of the dose is excreted unchanged by the kidneys. After administration of 5 mg in children, the total clearance of cetirizine is 0.93 ml/min/kg.

The T_½ in children 6 to 12 years old is 6 hours, 2 to 6 years old is 5 hours.

Patients with renal impairment:

In patients with mild renal impairment (creatinine clearance (CK) > 50 ml/min), pharmacokinetic parameters are similar to those of healthy volunteers with normal renal function.

In patients with moderate renal impairment (CK 30-49 mL/min), T_½ is prolonged 3-fold and total clearance is reduced by 70% relative to healthy volunteers with normal renal function.

In patients on hemodialysis (CK < 7 ml/min), oral cetirizine doses of 10 mg decrease total clearance by approximately 70% relative to healthy volunteers with normal renal function, and T_½ is prolonged by a factor of 3.

Less than 10% of cetirizine is removed by standard hemodialysis procedures.

Patients with hepatic impairment:

In patients with chronic liver disease (hepatocellular, cholestatic, and biliary cirrhosis), a single dose of 10 or 20 mg of cetirizine increases T_½ by approximately 50% and decreases clearance by 40% compared with healthy subjects.

Dose adjustment is necessary only if the patient with hepatic impairment also has concomitant renal impairment.

Indications
Indications

Active ingredient
Active ingredient

Composition
Composition
One tablet contains:
Active substance:
Cetirizine dihydrochloride – 10.0 mg;
Auxiliary substances:
Lactose monohydrate, 70.0 mg;
Microcrystalline cellulose, 34.0 mg;
Crospovidone, 3.6 mg;
Magnesium stearate – 1.2 mg;
Colloidal silicon dioxide – 1.2 mg;
Film sheath:
[hypromellose – 2.40 mg, talc – 0.80 mg, titanium dioxide – 0.44 mg, macrogol 4000 (polyethylene glycol 4000) – 0.36 mg] or [dry film coating mixture containing hypromellose (60%), talc (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] – 4.0 mg.

How to take, the dosage
How to take, the dosage

Interaction
Interaction
Simultaneous use with azithromycin, cimetidine, erythromycin, ketoconazole or pseudoephedrine does not affect the pharmacokinetic parameters of cetirizine. No pharmacokinetic interactions were observed. According to in vitro tests, cetirizine does not affect the protein binding effect of warfarin.
Concomitant administration of azithromycin, erythromycin, ketoconazole, theophylline or pseudoephedrine showed no significant changes in clinical laboratory parameters, vital functions and ECG.
In a study with concomitant administration of theophylline (400 mg daily) and cetirizine (20 mg daily), there was a small but statistically significant increase in 24-hour AUC (area under the curve) of 19% for cetirizine and 11% for theophylline. In addition, maximum plasma levels increased to 7.7% and 6.4% for cetirizine and theophylline, respectively. Simultaneously, cetirizine clearance decreased by -16% and by -10% for theophylline when cetirizine was taken by patients who had previously been treated with theophylline. However, pretreatment with cetirizine had no significant effect on the pharmacokinetic parameters of theophylline.
The effect of alcohol (0.8 â°) was not significantly increased after a single 10-mg dose of cetirizine; a statistically significant interaction with 5 mg diazepam was proven in one of 16 psychometric tests.
Concomitant administration of 10 mg of cetirizine daily with glipizide resulted in a slight decrease in glucose values. This effect has no clinical significance. Nevertheless, separate administration – glipizide in the morning and cetirizine in the evening – is recommended.
The degree of absorption of cetirizine is not reduced by simultaneous food intake, although absorption is delayed by 1 hour.
In a study with multiple administration of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), cetirizine exposure was increased by approximately 40%, while ritonavir exposure was slightly different (-11%) due to concomitant administration of cetirizine.
If you are using the above or other medications (including over-the-counter medications), please consult your physician before using this medication.

Special Instructions
Special Instructions
In patients with spinal cord injury, prostatic hyperplasia, and 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 impairment, 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”).
Cautious use of cetirizine with alcohol is recommended, because cetirizine may lead to increased somnolence.
Caution should be exercised in patients with epilepsy and increased seizure activity.
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 lactose 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 resuming cetirizine administration.
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. It is recommended to use the pediatric dosage form (oral drops).
Please read the instructions carefully before using this medicine. Keep the instructions; you may need them again. Ask your doctor if you have any questions. The medicine you are taking is meant for you, and you should not give it to others, because it might cause them harm, even if you have the same symptoms as you do.
Influence on ability to drive, machinery
Cetirizine may cause increased somnolence, therefore the drug may affect your ability to drive, machinery.

Synopsis
Synopsis
Circular biconvex film-coated tablets, white or almost white.
On the cross section the core is white or almost white.

Contraindications
Contraindications

Side effects
Side effects
The drug is usually well tolerated. Side effects are rare and transient.
Digestive system disorders: dry mouth dyspepsia.
Nervous system disorders: dizziness headache drowsiness fatigue agitation migraine.
Allergic reactions: angioedema skin rash itching urticaria.

Overdose
Overdose
Symptoms
The symptoms observed after an apparent overdose of cetirizine affected the central nervous system or were associated with possible anticholinergic effects.
The symptoms observed 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 administration of activated charcoal may be effective if the overdose is recent. Cetirizine is partially excreted by dialysis.

Pregnancy use
Pregnancy use
Pregnancy
The data on the use of cetirizine during pregnancy are limited (300 – 1000 pregnancy outcomes). However, no cases of malformations, fetal or neonatal toxicity with a clear causal relationship have been identified.
The 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 labor.
In pregnancy, cetirizine may be administered after consultation with a physician if the anticipated benefit to the mother exceeds the potential risk to the fetus.
Breastfeeding period
Cetirizine should not be used during breastfeeding because cetirizine is excreted with breast milk in an amount from 25% to 90% of the plasma concentration, depending on the time of sampling after taking the drug. Adverse reactions associated with cetirizine may be observed in infants.
In the period of breastfeeding, use after consultation with a physician if the anticipated benefit to the mother exceeds the potential risk to the baby.
Fertility
The available data on effects on human fertility are limited, but no negative effects on fertility have been identified in animal studies.
Consult your doctor before using the drug if you are pregnant, or if you think you might be pregnant, or are planning a pregnancy.

Similarities
Similarities

Additional information
Weight 0.010 kg
Shelf life
3 years. Do not use after the expiration date.
Conditions of storage
Store in a light-protected place at a temperature not exceeding 25 ºC. Store out of the reach of children.
Manufacturer
Vertex, Russia
Medication form
pills
Brand
Vertex