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

Excipients: Glycerol 250 mg, propylene glycol 350 mg, sucralose 7 mg, methyl parahydroxybenzoate 1.62 mg; propyl parahydroxybenzoate 0.18 mg; sodium hydrogen phosphate 28.4 mg, citric acid monohydrate to pH 6.0, water purified to 1 ml.

Description:

A colorless, clear liquid free from visible particles.

Pharmacotherapeutic group:antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

E.06.A.E.07 Cetirizine

Pharmacodynamics:

The active substance of the preparation Cetrin®- cetirizine - a metabolite of hydroxyzine, a competitive histamine antagonist, blocks H₁-gistaminovye receptors. Prevents development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action. Affects the "early" histamine-dependent stage of allergic reactions, restricts the release of inflammatory mediators at the "late" stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils, stabilizes the membranes of mast cells. 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). Reduces histamine-induced bronchoconstriction with bronchial asthma of the lung course. Cetirizine does not have anticholinergic and antiserotonin action. In therapeutic doses, it does not have a sedative effect.

The effect after taking cetirizine in a single dose of 10 mg develops in 20 minutes in 50% of patients and after 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 the cessation of treatment, the effect lasts up to 3 days.

Pharmacokinetics:

The pharmacokinetic parameters of cetirizine vary linearly.

Suction. After ingestion, the drug is quickly and completely absorbed from the gastrointestinal tract. Eating does not affect the completeness of absorption, although the rate of absorption decreases. In adults, after a single dose at the therapeutic dose, the maximum concentration (C_max) in the blood plasma is achieved after 1 ± 0.5 hours and is 300 ng / ml.

Distribution. Cetirizine at 93.0 ± 0.3% binds to blood plasma proteins. Volume of distribution (Vd) is 0.5 l / kg. When taking the drug at a dose of 10 mg for 10 days cumulation of cetirizine is not observed.

Metabolism. In small amounts, it is metabolized in the body by O-dealkylation (unlike other antagonists H₁-gistaminovyh receptors, which are metabolized in the liver using isoenzymes of the cytochrome system), with the formation of a pharmacologically inactive metabolite.

Excretion. In adults, the half-life (T_1/2) is approximately 10 hours, for children from 6 to 12 years - 6 hours, from 2 to 6 years - 5 hours, from 6 months to 2 years - 3.1 hours. About 2/3 of the dose of the drug is excreted by the kidneys unchanged.

In elderly patients and patients with chronic liver disease with a single dose of the drug at a dose of 10 mg T_1/2increases by about 50%, and systemic clearance is reduced by 40%.

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

In patients with moderate renal insufficiency and in patients on hemodialysis (CC <7 ml / min), when taking the drug inside at a dose of 10 mg T_1/2 lengthened 3 times, and the total clearance is reduced by 70%, relative to patients with normal renal function, which requires a corresponding change in the dosing regimen.

Cetirizine is practically not removed from the body during hemodialysis.

Indications:

Treatment of symptoms of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis: itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia; Pollinosis (hay fever); hives; 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);

- children's age up to 6 months (due to limited data on the effectiveness and safety of the drug);

- pregnancy, lactation.

Carefully:

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

- patients of advanced age (with an age-related decrease in glomerular filtration);

- epilepsy and patients with increased convulsive readiness;

- patients with predisposing factors to urinary retention (see section "Special instructions");

- children under 1 year.

Pregnancy and lactation:

Experimental studies in animals did not reveal any direct or indirect adverse effects of cetirizine on the developing fetus (including the postnatal period), the course of pregnancy and childbirth also did not change.

Adequate and strictly controlled clinical trials on the safety of the drug during pregnancy have not been conducted, therefore cetirizine should not be used during pregnancy.

Cetirizine excreted in breast milk, so the treating doctor should decide on the termination of feeding for the period of use of the drug.

Dosing and Administration:

Inside.

Children from 6 months to 12 months:

2,5 mg (5 drops) once 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) once a day.

Children over 6 years and adults:

the initial dose of 5 mg once a day (10 drops), if necessary, can be increased to 10 mg (20 drops) once a day. Sometimes an initial dose of 5 mg (10 drops) may be sufficient to achieve a therapeutic effect.

Daily dose of cetirizine - 10 mg (20 drops or 1 ml).

Special patient groups

As cetirizine are excreted mainly by the kidneys, when the drug is administered patients with renal insufficiency and patients of advanced age The dose should be adjusted depending on the amount of creatinine clearance (CC).

KK> 80 ml / min (normal) or 50-79 ml / mi (mild renal failure) - the usual dosing regimen is 10 mg (20 drops) of the drug orally per day.

KK from 30 to 49 ml / min (average degree of renal failure) - the dosage regimen of the drug - 5 mg (10 drops) of the drug 1 time inday.

KK from 10 to 29 ml / min (severe stage of kidney failure) - 5 mg (10 drops) every other day.

KK less than 10 ml / min (terminal stage of renal failure) - the drug is contraindicated.

Creatinine clearance for men can be calculated from the concentration serum creatinine, according to the following formula:

CK (ml / min) = [140 - age (years)] х body weight (kg) / 72 x KCyros (mg / dL)

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

When combination of renal and hepatic insufficiency the drug is also prescribed in the above mode.

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

Patients old age with normal renal function no dose adjustment is required.

Side effects:

Possible side effects are given below for body systems and frequency of occurrence: very often (> 1/10); often (1/10 - 1/100); infrequently (1/100 - 1/1000); rarely (1/1000 - 1/10 000); very rarely (<1/10 000), is unknown (it is impossible to estimate, based on available data).

Disorders from the gastrointestinal tract

Often: dry mouth, nausea; infrequently: diarrhea, abdominal pain.

Immune system disorders

Rarely: hypersensitivity reactions; very rarely: anaphylactic shock.

Disturbances from the nervous system

Often: headache, fatigue, dizziness, drowsiness; infrequently: paresthesia (impaired sensation); rarely: convulsions; very rarely: dysgeusia (perversion of taste), dyskinesia, dystonia, fainting, tremor, tick; unknown: memory impairment, including amnesia.

Disorders of the psyche

Infrequently: arousal; rarely: aggression, confusion, depression, hallucinations, sleep disorders; unknown: suicidal ideation.

Disturbances on the part of the organ of sight

Very rarely: disruption of accommodation, blurred vision, movement of the eyeball (nystagmus).

Disorders from the metabolism and nutrition

Rarely: weight gain.

Hearing disorders and labyrinthine disorders

The frequency is unknown: vertigo (the illusion of the movement of your body or objects around).

Heart Disease

Rarely: tachycardia.

Disturbances from the respiratory system

Often: rhinitis, pharyngitis.

Disturbances from the skin and subcutaneous tissues

Infrequent: rash, itching: rarely: urticaria; very rarely: angioedema, persistent erythema.

Disorders from the kidneys and urinary tract

Very rarely: dysuria, enuresis; unknown: retention of urine.

General disorders

Infrequently: asthenia, malaise; rarely: peripheral edema; unknown: increased appetite.

Laboratory and instrumental data

Rarely: increased activity of "hepatic transaminases", alkaline phosphatase, gamma-glutamine transferase and bilirubin concentration); very rarely: thrombocytopenia.

If any of the side effects indicated in the manual are aggravated or you notice any other side effects not listed in the instructions, inform your doctor.

Overdose:

Symptoms

With a single admission of 50 mg of cetirizine, confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis (dilated pupil), itching, restlessness, weakness, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention are noted.

Treatment

Immediately after taking the drug - gastric lavage or stimulation of vomiting. It is recommended to take activated charcoal, symptomatic and supportive therapy. There is no specific antidote. Hemodialysis is ineffective.

Interaction:

When studying the drug interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, diazepam and antipyrine, no clinically relevant undesirable interactions have been identified.

With simultaneous appointment with theophylline (400 mg / day), the total clearance of cetirizine is reduced by 16% (theophylline kinetics does not change).

When used simultaneously with ritonavir, the area under the pharmacokinetic curve "concentration-time" (AUC) cetirizine increased by 40%, while the similar index of ritonavir slightly changed (-11%).

Simultaneous appointment with macrolides (azithromycin, erythromycin) and ketoconazole does not lead to changes in the electrocardiogram of patients.

In therapeutic doses cetirizine did not demonstrate clinically significant interactions with alcohol (at a blood alcohol level of 0.5 g / l). Nevertheless, one should refrain from drinking alcohol.

Special instructions:

Due to the potential oppressive effect on the central nervous system, caution should be exercised in prescribing cetirizine in drops to children under 1 year of age, with the following risk factors for the occurrence of sudden infant death syndrome (but not limited to this list):

- sleep apnea syndrome or sudden infant death syndrome in infants from a brother or sister;

- abuse of the mother of drugs or smoking during pregnancy;

- young age of mother (19 years and younger);

- the abuse of smoking by a nanny caring for a child (one pack of cigarettes a day or more);

- children who fall asleep face down on a regular basis and who are not laid on their backs;

- premature (less than 37 weeks of gestation) or those born with insufficient body weight (below the 10th percentile of gestational age);

- with the joint intake of drugs that have a depressing effect on the central nervous system.

Methyl parahydroxybenzoate and propyl parahydroxybenzoate can cause allergic reactions, including delayed type.

Drops do not contain sugar, as a sweetener used sucralose, which does not affect the level of glucose in the blood serum, so Cetrin® in drops can be prescribed to patients with diabetes mellitus.

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

Impact on laboratory tests

Prior to the appointment of allergological samples, a three-day "washout" period is recommended because inhibitors H₁-gistaminovyh receptors (including cetirizine) inhibit the development of skin allergic reactions.

Effect on the ability to drive transp. cf. and fur:

With an objective assessment of the ability to drive vehicles and manage mechanisms, there were no significant adverse events when taking the drug at the recommended dose, but during treatment it is advisable to refrain from driving vehicles and other potentially dangerous activities that require increased concentration and speed of psychomotor reactions .

Form release / dosage:Drops for oral administration, 10 mg / ml.

Packaging:

For 10 ml or 20 ml in a bottle of dark with a screw neck, equipped with a dropper dispenser made of low-density polyethylene and a screw cap made of white plastic with a first-opening control system and child safety locks.

Each bottle, along with instructions for use, is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003473

Date of registration:26.02.2016

Expiration Date:26.02.2021

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDr. Reddy`c Laboratoris Ltd.Dr. Reddy`c Laboratoris Ltd.

Information update date: & nbsp29.07.2016

Illustrated instructions

Instructions

Cetrin® (Cetrine®)