Zodak Express - instructions for use, doses, side effects, contraindications

Excipients: core: lactose monohydrate - 67.50 mg, microcrystalline cellulose - 25.00 mg, sodium carboxymethyl starch - 1.00 mg, silicon colloidal dioxide - 0.50 mg, magnesium stearate - 1.00 mg; film sheath: hypromellose 2910/5 - 3,30 mg, macrogol-6000 - 0,35 mg, talc - 0,85 mg, titanium dioxide E171-0.50 mg.

Description:Oblong biconvex tablets covered with a film shell, white or almost white, engraved "e" on one side.

Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.E. Piperazine derivatives

E.06.A.E.09 Levocetirizine

Pharmacodynamics:

Levocetirizine, (R) -enantiomer cetirizine, is an inhibitor of peripheral H₁-gistaminovyh receptors, the affinity of which is 2 times higher than that of cetirizine. After a single administration of levocetirizine, binding was observed H₁-gistaminovyh receptors by 90% after 4 hours and na 57% after 24 hours. Levocetirizine affects the histamine-dependent stage allergic reactions, reduces the migration of eosinophils, reduces vascular permeability, limits the release mediators of inflammation, prevents the development and facilitates the course of allergic reactions, has an antiexudative, antipruritic effect, practically has no anticholinergic and antiserotonin action, in therapeutic doses practically does not have a sedative effect.The effect of levocetirizine begins 12 minutes after a single dose in 50% of patients, after 1 hour in 95% of patients and lasts for 24 hours. The intake of levocetirizine does not affect the RT interval on the ECG.

Pharmacokinetics:

The pharmacokinetics of levocetirizine is linear, independent of dose and time, and varies only slightly in different patients.

After oral administration levocetirizine quickly and completely absorbed from the gastrointestinal tract. The intake of food does not affect the completeness of absorption, although its rate decreases.

The maximum plasma concentration is achieved after 0.9 hours (54 minutes) after taking the drug. Equilibrium concentration is established after 2 days. Maximum the plasma concentration after single administration of 5 mg of levocetirizine is 270 ng / ml, and after repeated administration at a dose of 5 mg -308 ng / ml. Levocetirizine 90% bound to proteins plasma. The volume of distribution is 0.4 l / kg. Data on the distribution of levocetirizine in tissues and its penetration through the blood-brain barrier in humans are absent.

Levocetirizine is metabolized in small amounts (<14%) in the body by N- and O-dealkylation (unlike other antagonists H₁-gistaminovyh receptors that are metabolized in the liver by the cytochrome system) to form a pharmacologically inactive metabolite.

Due to limited metabolism and the absence of metabolic inhibitory activity, the interaction of levocetirizine at the metabolic level with other substances is unlikely.

Half-life (T_1/2) in adults is 7.9 ± 1.9 hours; in young children T_1/2 is shortened. The average observed total clearance is 0.63 ml / min / kg. Levocetirizine mainly excreted unchanged in the urine, on average, about 85.4% of the dose taken by glomerular filtration and active tubular secretion. Excretion through the intestine (with feces) is only 12.9% of the dose.

Patients from renal insufficiency

The total clearance of levocetirizine depends on the creatinine clearance (CK). Therefore, patients with moderate and severe renal insufficiency are encouraged to increase the intervals between doses of the drug in accordance with QC. In patients with anuria and terminal stage of renal failure, the total clearance of levocetirizine is reduced by approximately 80% compared to healthy people. amount Levocetirizine, output with a standard 4-hour procedure of hemodialysis is less than 10%.

Indications:

- Treatment of symptoms of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis such as itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia.

- Pollinosis (hay fever).

- Hives, including chronic idiopathic urticaria.

- Edema Quincke (as an auxiliary therapy).

- Other allergic dermatoses, accompanied by itching and rashes.

Contraindications:

- Hypersensitivity to levocetirizine and other piperazine derivatives or to any of the auxiliary components of the drug.

- Terminal renal failure with QC less than 10 ml / min.

- Pregnancy.

- Children under 6 years (for this dosage form).

- Congenital intolerance of galactose, deficiency of lactase or malabsorption of glucose-galactose (due to the content of lactose in the preparation).

Carefully:

- Take care when taking alcohol at the same time (see section "Interaction with other medicines").

- Chronic renal failure with QC more than 10 ml / min, but less than 50 ml / min (dosage adjustment is required).

- Elderly age (glomerular filtration may be reduced).

Pregnancy and lactation:

The use of the drug during pregnancy is contraindicated.

Levocetirizine is excreted in breast milk, so if it is necessary to use the drug in lactation it is recommended to stop breastfeeding.

Dosing and Administration:

The tablet should be taken orally, without chewing and washing with liquid, regardless of food intake. It is recommended to take a daily dose at one time.

Adults, teenagers and children over 6 years of age

The recommended daily dose is 5 mg (1 tablet).

Elderly patients

In elderly patients with moderate and severe renal failure, dose adjustment is recommended (see "Patients with impaired renal function" below).

Patients with impaired renal function

The interval between doses of the drug is determined individually, taking into account the function of the kidneys. Information on dose adjustment is given in the table below. For its use, the creatinine clearance (CK) in a patient in ml / min should be calculated based on serum creatinine concentration (mg / dl) using the following formula:

CK =[140 - increases)] x weight (kg) / 72 x serum creatinine (mg / dl) x 0.85 for women

Correction of dose in patients with impaired renal function:

Group	Creatinine clearance (ml / min)	Dose and multiplicity of admission
Normal function	>80	5 mg once daily
Easy CRF	50-79	5 mg once daily
Moderate CRF	30-49	5 mg once every 2 days
Severe CRF	<30	5 mg once every 3 days
Terminal CRF - patients on dialysis	<10	Contraindicated

In children with impaired renal function the dose is adjusted individually taking into account the clearance of creatinine and body weight. There are no separate data on the use in children with impaired renal function.

Patients with impaired hepatic function

With an isolated violation of liver function, dose adjustment is not required. In patients with hepatic renal failure, dose adjustment is recommended (see "Patients with impaired renal function" above).

Duration of treatment

Treatment of allergic rhinitis is carried out in accordance with the course of the disease; The drug can be stopped if symptoms disappear and resume when relapsed. In the case of chronic allergic rhinitis, prolonged treatment during the period of action of allergens can be prescribed.Currently, clinical experience with the use of levocetirizine in the form of tablets coated with a film membrane, 5 mg is limited to 6 months.

Side effects:

The side effects of levocetirizine are divided according to the system-organ classes according to the classification of the Medical Dictionary on Regulatory Activities (MedDRA) with the frequency of their occurrence: often (≥ 1/100 and 1/10); infrequently (≥ 1/1000 and <1/100); very rarely (<1/10000).

Immune system disorders:

Very rarely: hypersensitivity reactions, including anaphylactic reactions.

Impaired nervous system:

Often: headache. Infrequently: drowsiness

Very rarely: aggression, agitation, hallucinations, depression, convulsions.

Disorders from the side of the organ of vision:

Very rarely: visual disorders.

Heart Disease:

Very rarely: palpitations, tachycardia.

Disturbances from the respiratory system, chest and mediastinal organs:

Very rarely: dyspnea.

Disorders from the gastrointestinal tract:

Often: dryness of the oral mucosa.

Infrequent: pain in the abdomen.

Very rarely: nausea, diarrhea.

Disorders from the liver and bile ducts:

Very rarely: hepatitis.

Disturbances from the skin and subcutaneous tissues:

Very rarely: angioedema, itching, rash, including a rash, hives.

Disturbances from the musculoskeletal and connective tissue:

Very rarely: myalgia.

Common violations:

Often: fatigue.

Infrequently: asthenia

Violations from laboratory and instrumental data:

Very rarely: a violation of liver function indicators, weight gain.

Overdose:Symptoms

Symptoms of overdose may include drowsiness in adults and agitation, and anxiety, followed by drowsiness, in children.

Treatment

There are no specific antidotes of levocetirizine.

In case of an overdose, symptomatic or supportive treatment is recommended. If you take a little time after taking the medication, you should wash the stomach. Levocetirizine practically not excreted by hemodialysis.

Interaction:

Study of the interaction of levocetirizine with other drug preparations, including studies with inducers of the isoenzyme CYP3A4, have not been performed.

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

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

In a study with simultaneous administration of ritanovir (600 mg twice daily) and cetirizine (10 mg per day), it was shown that the exposure of cetirizine increased by 40%, and the exposure of ritanovir slightly changed (-11%).

In sensitive patients, simultaneous the intake of levocetirizine and alcohol or other substances depressing the central nervous system (CNS) may increase the effect on the central nervous system, although it has been shown that the racemate of cetirizine does not enhance the effect of alcohol.

Special instructions:During treatment with the drug is not recommended to take ethanol.

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

Levocetirizine, when administered at recommended doses, does not adversely affect the attention and speed of psychomotor reactions and the ability to drive vehicles. However, during the period of taking the drug, it is advisable to refrain from engaging in potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets, 5 mg.

Packaging:For 7 or 10 tablets in PVC / Aclar / PVC / Al or A1 / A1 blister. 1 or 4 blisters with 7 tablets; 2 blisters for 10 tablets together with instructions for use are placed in a cardboard box.

Storage conditions:Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

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

Terms of leave from pharmacies:Without recipe

Registration number:LP-002216

Date of registration:03.09.2013 / 17.04.2014

Expiration Date:03.09.2018

The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic

Manufacturer: & nbsp

ZENTIVA, k.s. Czech Republic

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp15.10.2017

Illustrated instructions

Instructions

Zodak® Express (Zodac® Express)