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

Excipients: lactose monohydrate - 59.80 mg, microcrystalline cellulose - 49.02 mg, kopividone - 5.20 mg, crospovidone - 3.90 mg, magnesium stearate - 1.56 mg, silicon dioxide colloid - 0.52 mg.

Film Sheath: talc - 2,15 mg, hypromellose - 1,94 mg, titanium dioxide - 0,53 mg, macrogol 6000 - 0,38 mg.

Description:Round biconvex tablets covered with a film coat, white, with a slight roughness, with a risk on one side.

Pharmacotherapeutic group:antiallergic agent-H1 histamine receptor blocker.

ATX: & nbsp

E.06.A.E.07 Cetirizine

Pharmacodynamics:Cetirizine belongs to the group of competitive histamine antagonists, blocks H1-histamine receptors, has almost no anticholinergic and antiserotonin 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 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 After the drug is withdrawn, the effect lasts up to 3 days.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 preparation is quickly and well absorbed from the gastrointestinal tract. The maximum level of concentration is determined after about 30-60 minutes.

The intake of food does not have a significant effect on the amount of absorption, but lengthens the time to reach the maximum concentration (Tcax) by 1 hour and reduces the maximum concentration (Cmah) by 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 quantities metabolized by O-dealkylation to form an inactive metabolite. With a 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 amount of 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 in patients on hemodialysis (creatinine clearance less than 7 ml / min) period value the elimination half-life increases 3-fold, 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).

- Hives, including chronic idiopathic urticaria, angioedema.

- 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 <10 ml / min).

Lactose intolerance, lactase deficiency or glucose-galactase malabsorption (the preparation contains lactose).

Pregnancy, lactation.

Children under 6 years (for this dosage form).

Carefully:

Chronic renal failure (correction of the dosing regimen is required).

Chronic liver diseases.

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 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 * CC 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
Norm	>80	10 mg / day
Lightweight	50-79	10 mg / day
Average	30-49	5 mg / day
Heavy	<30	5 mg every other day
Terminal stage - patients on dialysis	<10	contraindicated

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

Children with renal insufficiency the recommended dose should be halved. Patients with a violation of liver function only correction of the dosing regimen is not required.

Side effects:

Possible side effects on the body systems and frequency of occurrence: often (> 1%, <10%), infrequently (> 0.1%, <1%), rarely (> 0.01%, <0.1%), very rarely (<0.01%).

- From the nervous system: infrequently - headache, fatigue, dizziness, drowsiness; rarely - asthenia, paresthesia, agitation; very rarely - aggression, confusion, hallucinations, depression, convulsions, sleep disturbance; single cases - perversion of taste, dyskinesia, dystonia, fainting, tremor, tick,

amnesia, memory impairment.

- On the part of the organs of vision: single cases - violation of accommodation, lack of clarity

sight, nystagmus.

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

- Co cardiovascular system: very rarely, tachycardia.

- From the respiratory system: infrequently - rhinitis, pharyngitis.

- From the side of metabolism: very rarely - weight gain.

- From the urinary system: single cases - upset urination, enuresis.

- From the laboratory indicators: very rarely - a change in functional liver samples (increased levels of transaminases, alkaline phosphatase, gamma-glutamate transferase, bilirubin); single cases - thrombocytopenia.

- Allergic Reagents: rarely - a rash, itching; very rarely - hives, hypersensitivity reactions; single cases - angioedema, anaphylactic shock, persistent erythema.

- Other: rarely - malaise; very rarely - 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 the appointment of activated charcoal, the conduct of 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.

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

With simultaneous administration with macrolides and ketoconazole, there is no change in the electrocardiogram.

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.

Special instructions: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, film-coated, 10 mg.

Packaging:For 10 tablets, film-coated, in a contour mesh package. 2 contour squares with instructions for use in a pack of cardboard.

Storage conditions:In a dry, protected from light 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:LS-001670

Date of registration:14.10.2011

The owner of the registration certificate:REPLEK FARM Skopje, OOOREPLEK FARM Skopje, OOO Macedonia

Manufacturer: & nbsp

REPLEK PHARM, Ltd. Macedonia

Representation: & nbspREPLECK FARM LTD SCOPJEREPLECK FARM LTD SCOPJERussia

Information update date: & nbsp11.10.2015

Illustrated instructions

Instructions

Cetirizine (Cetirizine)