Universal reference book for medicines
Product name: CETRIN ® (CETRINE)

Active substance: cetirizine

Type: The blocker of histamine H 1 -receptors.
Anti-allergic drug
Manufacturer: DR.
REDDY`S LABORATORIES (India)
Composition, form of production and packaging

?
The tablets covered with a film cover of white or almost white color, round, biconcave, with risk on one side.
1 tab.

cetirizine dihydrochloride 10 mg

Excipients: lactose - 106.5 mg, corn starch - 65 mg, povidone K30 - 2 mg, magnesium stearate - 1.5 mg.

Composition of the film coat: hypromellose - 3.3 mg, macrogol 6000 - 0.661 mg, titanium dioxide - 0.706 mg, talc - 1.183 mg, sorbic acid - 0.05 mg, polysorbate 80 - 0.05 mg, dimethicone - 0.05 mg.

10 pieces.
- blisters (2) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
?
Drops for oral administration in the form of a transparent, colorless liquid, free from visible particles.
1 ml

cetirizine dihydrochloride 10 mg

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

10 ml - bottles of dark glass with a dropper-dispenser (1) - packs of cardboard.

20 ml - bottles of dark glass with a dropper-dispenser (1) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

The blocker of histamine H 1 -receptors.
Cetirizine is a metabolite of hydroxyzine, a competitive histamine antagonist. Prevents development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action.
Affects the early histamine-dependent stage of allergic reactions, limits the release of inflammatory mediators in 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 drops in a single dose of 10 mg develops in 20 minutes in 50% of patients and after 60 minutes in 95% of patients, lasts more than 24 hours. After taking the pill, the effect comes in 20 minutes.
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 with the administration of the drug at a dose of 5-60 mg.

Suction

After ingestion, cetirizine is rapidly and completely absorbed from the digestive tract.
Eating does not affect the fullness of the intake, although the rate of absorption decreases and the C max decreases by 23%. In adults, after a single dose at a therapeutic dose of C max in blood plasma is achieved after 1 ± 0.5 h and is 300 ng / ml.
Distribution

Binding to blood plasma proteins composes 93 ± 0.3% and does not change with a concentration of cetirizine in the range of 25-1000 ng / ml.
V d is 0.5 l / kg. When taking the drug at a dose of 10 mg for 10 days cumulation of cetirizine is not observed. Cetirizine excreted in breast milk.
Metabolism

In small amounts, it is metabolized in the body by O-dealkylation (in contrast to other antagonists of histamine H 1 -receptors, which are metabolized in the liver with the participation of the cytochrome P450 system), with the formation of a pharmacologically inactive metabolite.

Excretion

In adults, T 1/2 is approximately 10 hours. About 2/3 of the dose of the drug is excreted unchanged in urine, 10% with feces.
Systemic clearance - 53 ml / min.
Pharmacokinetics in specific patient groups

In elderly patients and patients with chronic liver disease, a single dose of 10 mg of T 1/2 is increased approximately 50%, and systemic clearance is reduced by 40%.

T 1/2 in children aged 6 to 12 years is 6 hours, at the age of 2 to 6 years - 5 hours, at the age from 6 months to 2 years - 3.1 hours.

In patients with mild renal insufficiency (KK> 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 is 3 times longer, and the total clearance is reduced by 70% (is 0.3 ml / min / kg), 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.
In patients with chronic liver disease (hepatocellular, cholestatic or biliary cirrhosis), T 1/2 elongation by 50% and a 40% overall clearance decrease (correction of the dosing regimen is required only with the concomitant decrease in GFR).

INDICATIONS

- seasonal and year-round allergic rhinitis;

- allergic conjunctivitis;

- Pollinosis (hay fever);

- urticaria (including chronic idiopathic);

- Other allergic dermatoses (including atopic dermatitis and neurodermatitis), accompanied by itching and rashes;

- angioedema (edema Quincke).

DOSING MODE

The drug is taken orally.

Tablets should be taken regardless of food intake, without chewing and washing down with 200 ml of water.

Adults and children over 6 years of age the drug is prescribed in the form of tablets 10 mg (1 tab.) 1 time / day or 5 mg (1/2 tab.) 2 times / day, or in the form of drops - the initial dose is 5 mg 1 once / day (10 drops), if necessary, the dose can be increased to 10 mg (20 drops) 1 time / day.
Sometimes an initial dose of 5 mg (10 drops) may be sufficient to achieve a therapeutic effect.
Children aged 6 months to 12 months are prescribed 2.5 mg (5 drops) 1 time / day;
children aged 1 to 2 years - 2.5 mg (5 drops) up to 2 times / day; children aged 2 to 6 years - 2.5 mg (5 drops) 2 times / day or 5 mg (10 drops) 1 time / day.
Because
cetirizine is excreted mainly by the kidneys, when the drug is prescribed for patients with renal insufficiency and elderly patients, the dose should be adjusted depending on the magnitude of the CC.
With CC> 80 ml / min (normal) or 50-79 ml / min (mild renal failure), the drug is prescribed in the usual dosing regimen - 10 mg (1 tab or 20 drops) / day.
WithSC from 30 to 49 ml / min (average degree of renal failure), the drug is prescribed 5 mg (1/2 table or 10 drops) of the drug 1 time / day. With SC from 10 to 29 ml / min (severe stage of kidney failure) of 5 mg (1/2 tablets or 10 drops) every other day. With CC less than 10 ml / min (terminal stage of renal failure), the use of the drug is contraindicated.
CK for men can be calculated based on the serum creatinine concentration, according to the following formula:

KK (ml / min) = [140 - age (years)]?
body weight (kg) / 72? CK serum (mg / dl).
KK for women can be calculated by multiplying the obtained value by a factor of 0.85.

When combined renal and hepatic insufficiency, the drug is also prescribed in the above mode.

Patients with a dysfunction of the liver with normal kidney function correction dosage is not required.

Older patients with normal renal function are not required to adjust the dose.

SIDE EFFECT

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).
On the part of the digestive system: often - dry mouth, nausea;
infrequently - diarrhea, abdominal pain.
From the immune system: rarely - hypersensitivity reactions;
very rarely - anaphylactic shock.
From the nervous system: often - headache, fatigue, dizziness, drowsiness;
infrequently - paresthesia (impaired sensation); rarely convulsions; very rarely - dysgeusia, dyskinesia, dystonia, fainting, tremor, tick; unknown - memory impairment, incl. amnesia.
Mental disturbances: infrequent excitation;
rarely - aggression, confusion, depression, hallucinations, sleep disturbances; unknown - suicidal ideation.
From the side of the organ of vision: very rarely - disorders of accommodation, blurred vision, nystagmus.

From the side of the hearing organ and labyrinthine disturbances: the frequency is unknown - vertigo.

From the cardiovascular system: rarely - tachycardia.

From the respiratory system: often - rhinitis, pharyngitis.

From the skin and subcutaneous tissues: infrequently - rash, itching;
rarely - hives; very rarely - angioedema, persistent erythema.
From the urinary system: very rarely - dysuria, enuresis;
unknown - urinary retention.
Other: infrequently - asthenia, malaise;
rarely - peripheral edema, weight gain; unknown - increased appetite.
Laboratory and instrumental data: rarely - increased activity of hepatic transaminases, alkaline phosphatase, GGT, and bilirubin concentrations;
very rarely - thrombocytopenia.
If any of the side effects indicated in the manual are aggravated or any other side effects not indicated in the instructions are noted, the patient should inform the physician about it.

CONTRAINDICATIONS

- Children under 6 months (for drops), due to the limited data on the effectiveness and safety of the drug;

- Children's age to 6 years (for tablets);

- Pregnancy;

- lactation period;

- terminal stage of renal failure (CC less than 10 ml / min);

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

With caution should prescribe the drug for chronic kidney failure (with KK> 10 ml / min requires a correction of the dosing regimen);
patients with predisposing factors to urinary retention; with epilepsy and patients with increased convulsive readiness; patients of advanced age (with age-related decline in glomerular filtration);in childhood to 1 year (for drops).
PREGNANCY AND LACTATION

Experimental studies in 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 childbirth also did not change.
Adequate and strictly controlled clinical studies on the safety of the drug during pregnancy have not been conducted, so cetirizine should not be used during pregnancy.
Cetirizine excreted in breast milk, so it is necessary to resolve the issue of stopping breastfeeding for the period of application of the drug.

APPLICATION FOR FUNCTIONS OF THE LIVER

Because
cetirizine are excreted mainly by the kidneys, when the drug is prescribed for patients with renal insufficiency, the dose should be adjusted depending on the magnitude of the CC.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Patients with a dysfunction of the liver with normal kidney function correction dosage is not required.

APPLICATION FOR CHILDREN

Contraindicated use of the drug in the form of drops in children up to 6 months, due to limited data on the effectiveness and safety of the drug;
in the form of tablets - in children under 6 years.
Caution should be given to the drug in the form of drops to children under the age of 1 year.

APPLICATION IN ELDERLY PATIENTS

With caution should prescribe the drug to elderly patients (with an age-related decrease in glomerular filtration).

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 sinceCetirizine may increase the risk of urinary retention.

Methyl parahydroxybenzoate and propyl parahydroxybenzoate, which are part of the drug in the form of drops, can cause allergic reactions, including.
delayed type.
Drops do not contain sugar, as a sweetener, sucralose is used that does not affect the glucose level in the blood serum, so Cetrin ® in drops can be prescribed to patients with diabetes mellitus.

Prior to the appointment of allergological samples, a three-day "wash-out" period is recommended because inhibitors of histamine H 1 -receptors (including cetirizine) inhibit the development of skin allergic reactions.

When the dose is exceeded 10 mg / day, the speed of psychomotor reactions can be slowed down.

Use in Pediatrics

In view of the potential depressing effect on the central nervous system, caution should be exercised in prescribing cetirizine in drops to children under the age of 1 year if there are 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 tobacco during pregnancy;

- young mother's age (19 years and younger);

- Abuse of tobacco by a nanny caring for a child (1 pack of cigarettes a day or more);

- Children who regularly fall asleep face down, which do not fit on their backs;

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

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

Impact on the ability to drive vehicles and manage mechanisms

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 .

OVERDOSE

Symptoms: a single dose of cetirizine at a dose of 50 mg showed confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, itching, anxiety, weakness, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention.

Treatment: immediately after taking the drug - gastric lavage or stimulation of vomiting.
It is recommended to take activated charcoal, conduct symptomatic and maintenance therapy. There is no specific antidote. Hemodialysis is ineffective.
DRUG INTERACTION

When studying the pharmacokinetic interaction of cetirizine with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, diazepam and antipyrin, no clinically significant undesirable interaction was detected.

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

With concomitant use with ritonavir, AUC of cetirizine increased by 40%, while that of ritonavir slightly changed (-11%).

The simultaneous use with the antibiotics of macrolides (azithromycin, erythromycin) and ketoconazole does not lead to changes in the ECG of patients.

In therapeutic doses, cetirizine did not demonstrate a clinically significant interaction with ethanol (at an ethanol concentration of 0.5 g / l in the blood).
Nevertheless, one should refrain from drinking alcohol.
Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

TERMS OF RELEASE FROM PHARMACY

The drug is dispensed without a prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 25 ° C.
Shelf life of the tablets is 2 years, drops are 3 years.
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