Universal reference book for medicines
Product name: CESERA (CESERA)

Active substance: levocetirizine

Type: The blocker of histamine H 1 -receptors.
Anti-allergic drug
Manufacturer: KRKA (Slovenia)
Composition, form of production and packaging
Tablets, film-coated
1 tab.

levocetirizine dihydrochloride 5 mg

10 pieces.
- packings of cellular contour (1) - packs cardboard.
10 pieces.
- packings cellular planimetric (3) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

Levocetirizine, cetirizine enantiomer is a selective histamine antagonist, blocks peripheral histamine H 1 receptors.
The affinity of levocetirizine (Ki = 3.2 nmol / l) is high for these receptors and 2 times higher than for cetirizine (Ki = 6.3 nmol / l). Levocetirizine influences the histamine-dependent stage of allergic reactions, reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators. Prevents development and facilitates the course of allergic reactions, has antiexudative, antipruritic effect, practically does not have anticholinergic and antiserotonergic action. In therapeutic doses, it practically does not have a sedative effect.
PHARMACOKINETICS

Pharmacokinetics is linear in nature, depends on dose and time, with a low degree of individual fluctuations.

Suction

Levocetirizine is quickly and well absorbed after ingestion.
The time to reach C max in blood plasma is achieved through 0.9 h after ingestion. Equilibrium concentrations are achieved after 2 days. C max is 270 ng / ml and 308 ng / ml after a single and repeated administration of 5 mg 1 time / day, respectively. The degree of absorption depends on the dose and does not change with the intake of the food, but C max is lower and is reached later.
Distribution

Binding to proteins - 90%.
The distribution is limited, and V d is 0.4 l / kg.
Metabolism

Less than 14% of the administered dose is metabolized in the liver by oxidation, N- and O-dealkylation and conjugation with taurine.
Levocetirizine does not influence the activity of cytochrome isoenzymes CYP 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 in concentrations much higher than the peak concentrations with oral administration of 5 mg.
Due to the insignificant metabolism and the absence of metabolic inhibition, the interaction of levocetirizine with other substances is unlikely.

Excretion

T 1/2 is 7.9 ± 1.9 h. The average overall clearance is 0.63 ml / min / kg.
Levocetirizine and its metabolite are excreted mainly by the kidneys (85.4% of the dose taken), by glomerular filtration and active tubular secretion. Excretion through the intestine is 12.9%. Penetrates into breast milk.
Pharmacokinetics in special clinical cases

The total clearance of levocetirizine correlates with creatinine clearance (CC).
Therefore, patients with renal insufficiency are recommended to reduce the dose of the drug depending on the QC. With anuria the clearance of the drug is reduced by approximately 80%. Less than <10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.
INDICATIONS

- symptomatic treatment of allergic rhinitis (including all-the-year-round allergic rhinitis);

- chronic idiopathic urticaria.

DOSING MODE

Inside, regardless of food intake, squeezed a small amount of liquid and nedozhevyvaya.

Adults and children older than 6 years: the recommended daily dose is 5 mg (1 tab.).

Elderly patients: under the condition of normal renal function, a decrease in the daily dose of levocetirizine is not required.

Patients with renal dysfunction: Individual selection of the interval between doses of the drug is recommended in accordance with the level of QC.
With QC from 30 to 49 ml / min - 1 tab. in one day; with KK from 10 to 29 ml / min - 1 tab. every 3 days; with CC <10 ml / min and patients on dialysis, levocetirizine is contraindicated. The level of QC can be calculated by the formula:
CK = [140 - age (s)] x body weight (kg) / 72 x serum creatinine (mg / dl) (x 0.85 for women)

In patients with an isolated dysfunction of the liver, dose adjustment is not required.

SIDE EFFECT

From the side of the central nervous system: often - headache, drowsiness, weakness, asthenia;
rarely - dizziness;
From the digestive system: often - dry mouth;
infrequently - abdominal pain; rarely - nausea, dyspepsia, hepatitis.
From the cardiovascular system: rarely - palpitation.

From the senses: rarely - visual impairment.

From the respiratory system: rarely - shortness of breath.

Allergic reactions: rarely - angioedema, skin itching, rash, urticaria.

Laboratory indicators: rarely - a short-term increase in the activity of liver enzymes.

Other: rarely - weight gain.

CONTRAINDICATIONS

- severe renal failure (creatinine clearance (CK) <10 ml / min) and patients on dialysis;

- galactosemia, lactase deficiency, glucose-galactose malabsorption syndrome;

- Children under 6 years of age (for this dosage form and dose);

- Pregnancy;

- lactation period (due to lack of data on the efficacy and safety of the drug);

- hypersensitivity to levocetirizine (including other derivatives of piperazine) or auxiliary components of the drug;

With caution, renal failure of moderate severity (QC less than 60 ml / min), advanced age (possibly reducing glomerular filtration).

PREGNANCY AND LACTATION

Contraindicated in pregnancy.

Levocetirizine is excreted in breast milk, therefore, if it is necessary to use it during the lactation period, breastfeeding while taking Ceser's drug should be discontinued.

APPLICATION FOR FUNCTIONS OF THE LIVER

With CC <10 ml / min and patients on dialysis, levocetirizine is contraindicated.

Patients with renal dysfunction: Individual selection of the interval between doses of the drug is recommended in accordance with the level of QC.
With QC from 30 to 49 ml / min - 1 tab. in one day; with KK from 10 to 29 ml / min - 1 tab. every 3 days.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with an isolated dysfunction of the liver, dose adjustment is not required.

APPLICATION FOR CHILDREN

Contraindicated in children under 6 years.

Children older than 6 years: the recommended daily dose is 5 mg (1 tab.).

APPLICATION IN ELDERLY PATIENTS

With caution: the elderly (possibly reducing glomerular filtration).
Under the condition of normal renal function, a decrease in the daily dose of levocetirizine is not required.
SPECIAL INSTRUCTIONS

It is necessary to use alcohol with caution during treatment with Ceser.

The preparation of Cesar contains lactose, therefore it is impossible to accept patients with galactosemia, lactase deficiency or glucose-galactose malabsorption syndrome.

Impact on the ability to drive vehicles and manage mechanisms

Care must be taken when driving vehicles and working with technical devices that require a high concentration of attention and speed of psychomotor reactions.

OVERDOSE

Symptoms: in adults - drowsiness, in children - excitement, irritability and anxiety, followed by drowsiness.

Treatment: symptomatic and supportive therapy;
gastric lavage. The specific antidote is not known. Hemodialysis is not effective.
DRUG INTERACTION

There are no clinically significant adverse interactions with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, and diazepam.

A decrease in the total clearance of racemic cetirizine (16%) was observed with multiple theophylline injections (400 mg 1 time / day);
while the pharmacokinetics of theophylline with simultaneous application with levocetirizine did not change.
Food does not reduce the absorption of levocetirizine, although the rate of absorption decreases.

In susceptible patients, simultaneous use of cetirizine / levocetirizine and alcohol or other CNS depressants may have an effect on the CNS.
At the same time, racemic cetirizine does not enhance the effect of alcohol.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The preparation should be stored at a temperature not exceeding 30 ° C.
Keep out of the reach of children. Shelf life - 3 years.
Do not use the drug after the expiration date.

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