Cetirizine - instructions for use, dose, side effects, contraindications

Excipients (core): cellulose microcrystalline - 119.0 mg, lactose - 60.0 mg, croscarmellose sodium - 7.0 mg, magnesium stearate - 3.0 mg, silicon dioxide colloid - 1.0 mg.

Auxiliary substances (shell): Opapray II 85F48105 White - 6.0 mg, polyvinyl alcohol - 2.814 mg, macrogol 3350 - 1.416 mg, talc - 1.044 mg, titanium dioxide - 0.726 mg.

Description:

Round tablets of biconvex form with a risk on one side, covered with a film shell of white or almost white color, on the fracture are visible two layers - a core of white or almost white color and a film membrane.

Pharmacotherapeutic group:Anti-allergic agent-H1 histamine receptor blocker.

ATX: & nbsp

E.06.A.E.07 Cetirizine

Pharmacodynamics:Cetirizine belongs to the group of competitive antagonists of histamine, blocks H1-histamine receptors, has almost no anticholinergic and antiseritonin action. Has a pronounced anti-allergic effect, prevents development and facilitates the course of allergic reactions. Has antipruritic and anti-exsudative effect. Affects the "early" stage of allergic reactions, and also reduces the migration of inflammatory cells; oppresses the selection of mediators involved in the "late" stage of an allergic reaction. Reduces the permeability of capillaries, prevents the development of edema of tissues, relieves spasm of smooth muscles. Eliminates the skin reaction to the administration of histamine, specific allergens, and also to cooling (with cold urticaria).

In therapeutic doses, it practically does not have a sedative effect. Against the background of the course, tolerance does not develop.

The effect of the drug after taking cetirizine in a single dose of 10 mg begins in 20 minutes (in 50% of patients), after 1 hour (in 95% of patients), and persists for 24 hours. After the drug is withdrawn, the effect lasts up to 3 days.

Pharmacokinetics:

Suction: after ingestion the drug is quickly and well absorbed from the gastrointestinal tract. The maximum concentration (Cmah) cetirizine is determined after about 30 to 90 minutes.

Eating does not have a significant effect on the amount of absorption, but lengthens the time to reach the maximum concentration (TCmax) for 1 hour and reduces the value of Cmah on 23%.

Distribution: cetirizine binds to blood plasma proteins by about 93%.

The volume of the distribution (Vd) low (0.5 l / kg).

Metabolism: cetirizine in small amounts is metabolized by O-dealkylation to form an inactive metabolite. At 10-day application in a dose of 10 mg accumulation of the drug is not observed.

Excretion: approximately 70% of the kidneys are mostly unchanged. In addition to the kidneys is excreted through the intestine. The system clearance is about 54 ml / min.

The half-life is about 10 hours. In children aged 6 to 12 years, the half-life is reduced to 6 hours. In case of impaired renal function (creatinine clearance below 11-31 ml / min) and hemodialysis patients (creatinine clearance less than 7 ml / min), the half-life period increases by 3 times, the total clearance decreases by 70%.On the background of chronic liver diseases and elderly patients taking the drug at a dose of 10 mg marked increase in half-life values of 50% and a decrease in systemic clearance of 40%.

Indications:

- Treatment of the 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;

- Other allergic dermatoses, including atopic dermatitis, accompanied by itching and rashes.

Contraindications:

- Hypersensitivity to cetirizine, hydroxyzine or piperazine derivative, as well as other components of the drug;

- Terminal stage of renal failure (creatinine clearance less than 10 ml / min);

- Lactose intolerance, lactase deficiency or glucose-galactase malabsorption;

- Pregnancy, lactation;

- Children under 6 years.

Carefully:

- Chronic renal failure (creatinine clearance more than 10 ml / min) - correction of the dosing regimen is required;

- Chronic liver disease;

- Epilepsy, patients with increased convulsive readiness;

- Patients with predisposing factors to urinary retention;

- Elderly age (glomerular filtration may be reduced).

Pregnancy and lactation:The use of the drug during pregnancy is contraindicated. If you need to use the drug during lactation, you should decide whether to stop breastfeeding.

Dosing and Administration:

Inside, washing down a glass of liquid.

Adults and children over 6 years of age - the daily dose is 10 mg (1 tablet). Sometimes achieving therapeutic effect is possible with prescribing the drug at an initial dose of 5 mg (1/2 tablet).

Patients with creatinine clearance less than 10 ml / min and those on dialysis are contraindicated.

Patients with renal insufficiency and elderly patients The dose should be adjusted depending on the amount of creatinine clearance (CC). The creatinine clearance for men can be calculated based on the serum creatinine concentration, according to the following formula:

[140 - age (years)] * body weight (kg)

KK (ml / min) = ------------------------------------------- ------------- 72 * KK serum (mg / dL)

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

Renal insufficiency	CK (ml / min)	Dosing regimen
Normal liver function	>80	10 mg / day
Lightweight	50-79	10 mg / day
Average	30-49	5 mg / day
Heavy	10-30	5 mg every other day

Adult patients with renal and hepatic impairment dosing is carried out according to the table above.

Children with renal insufficiency dose adjusted for QA and body weight.

Patients with a violation of liver function only correction of the dosing regimen is not required.

Side effects:

- From the blood and lymphatic system: thrombocytopenia.

- From the central and peripheral nervous system: drowsiness, dizziness, headache, aggression, agitation, confusion, depression, hallucinations, insomnia, teak, seizures, dyskinesia, dystonia, paresthesia, syncope, tremor, memory impairment, confusion, suicidal ideation, vertigo.

- On the part of the organs of vision: violation of accommodation, fuzzy vision, nystagmus.

- From the cardiovascular system: tachycardia.

- From the respiratory system: rhinitis, pharyngitis.

- On the part of the organs of the gastrointestinal tract: dry mouth, perversion of taste, nausea, abdominal pain, diarrhea, increased appetite.

- From the hepatobiliary system: violation of liver function (increased activity of transaminases, alkaline phosphatase, gamma-glutamate transferase, bilirubin concentration).

· From the urinary system: upset urination, enuresis, urinary retention.

- From the skin and subcutaneous tissue: itching, rash, hives, persistent erythema, angioedema.

- From the immune system: hypersensitivity, up to the development of anaphylactic shock.

- From the side of metabolism: increase in body weight.

- Other: fatigue, asthenia, malaise, peripheral edema.

Overdose:

With a single admission of the drug at a dose of 50 mg, the following can be observed symptoms: 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 artificial challenge of vomiting. It is recommended to take activated charcoal, conduct symptomatic and maintenance therapy. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

When studying the drug interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, and glipizide, no clinically relevant interactions were detected.

Joint application with theophylline (400 mg / day) leads to a decrease in the total clearance of cetirizine by 16% (theophylline kinetics does not change).

With simultaneous application with macrolides and ketoconazole, there are no changes on the electrocardiogram.

Cetirizine, when used simultaneously with the HIV-1 protease inhibitor ritonavir, did not alter the pharmacokinetics of ritonavir.

When using the drug in therapeutic doses, data on the interaction with alcohol is not obtained (at a blood alcohol concentration of 0.5 g / l). However, one should refrain from drinking alcohol during therapy with the drug in order to avoid the depression of the central nervous system.

Before the allergological tests, a three-day "wash-out" period is recommended because the H1-histamine receptors blockers inhibit the development of skin allergic reactions.

Special instructions:

In patients with spinal cord injury, prostate hyperplasia,and in the presence of other predisposing factors to urinary retention, caution is required, since cetirizine may increase the risk of urinary retention.

At an objective estimation of ability to driving of motor transport and management of mechanisms it is authentic not revealed any undesirable phenomena at reception of a preparation in a researched dose. But, nevertheless, during the period of using the drug, it is advisable to refrain from engaging in potentially dangerous activities that require an increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets coated with a film coat of 10 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 10, 20, 30, 40, 50 or 100 tablets per can of polymer for medicines.

One jar or 1, 2, 3, 4, 5 or 10 contour mesh packages together with the instruction for use are placed in a cardboard package (bundle).

Storage conditions:Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-002087

Date of registration:03.06.2013

Date of cancellation:2018-06-06

The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp11.10.2015

Illustrated instructions

Instructions

Cetirizine (Cetirizine)