Suprastinex tab. p / o film. 5mg # 14

Release form, composition and packaging

Film-coated tablets of white or almost white color, round, biconvex

engraved with E" on one side and "281" on the other, with little or no odor.

1 tab.

levocetirizine dihydrochloride 5 mg,

- which corresponds to the content of levocetirizine 4.21 mg

silicon microcrystalline cellulose (ProsolvHD90) - 40.4 mg (microcrystalline cellulose (98%), colloidal anhydrous silicon dioxide (2%)), lactose monohydrate - 37.9 mg, low-substituted hyprolose (L-HPC11) - 10 mg, magnesium stearate - 1.7 mg.

Shell composition: opadry II 33G28523 white - 5 mg (hypromellose 2910 (40%), titanium dioxide (25%), lactose monohydrate (21%) - 1.05 mg, macrogol 3350 (8%), triacetin (6%)).

7 pcs.

- blisters (1) - cardboard packs.

7 pcs.

- blisters (2) - cardboard packs.

10 pieces.

- blisters (1) - cardboard packs.

10 pieces.

- blisters (2) - cardboard packs.

10 pieces.

- blisters (3) - cardboard packs.

pharmachologic effect

Levocetirizine - the R-enantiomer of cetirizine, which belongs to the group of competitive histamine antagonists, blocks histamine H1 receptors.

It has an effect on the histamine-dependent stage of allergic reactions, reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators.

It prevents the development and facilitates the course of allergic reactions, has an antiexudative, antipruritic effect.

Virtually no anticholinergic and antiserotonergic action.

In therapeutic doses, it practically does not have a sedative effect.

The action of the drug Suprastinex drops begins 12 minutes after taking a single dose in 50% of patients, after 1 hour - in 95% and lasts for 24 hours.

Pharmacokinetics

Suction

The pharmacokinetic parameters of levocetirizine vary linearly and practically do not differ from the pharmacokinetics of cytirizine.

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract.

Food intake does not affect the completeness of absorption, but reduces its rate.

In adults, after a single dose of the drug in a therapeutic dose (5 mg), Cmax in blood plasma is reached after 0.9 h and is 207 ng / ml (for tablets) and 270 ng / ml (for drops), after repeated administration at a dose of 5 mg - 308 ng / ml.

Bioavailability reaches 100%.

Distribution

Levocetirizine is 90% bound to blood plasma proteins.

Vd is 0.4 l / kg.

Css is reached after 2 days.

Metabolism

Less than 14% of the drug is metabolized in the liver by N- and O-dealkylation (in contrast to other antagonists of histamine H1-receptors, which are metabolized in the liver using the CYP system).

Due to the low metabolism and metabolic potential, the interaction of levocetirizine with other drugs seems unlikely.

Withdrawal

In adults, T1 / 2 is 7.9 hours +/- 1.9 hours (for drops), 7-10 hours (for tablets), the total clearance is 0.63 ml / min / kg.

About 85.4% of the taken dose of the drug is excreted by the kidneys unchanged by glomerular filtration and tubular secretion

about 12.9% - through the intestines.

Pharmacokinetics in special patient groups

In renal failure (CC less than 40 ml / min), clearance is reduced, and T1 / 2 is lengthened (for example, in patients on hemodialysis, total clearance is reduced by 80%), which requires a corresponding change in the dosage regimen.

Less than 10% of levocetirizine is removed during a standard 4-hour hemodialysis procedure.

In young children, T1 / 2 is shortened.

Indications for use

Symptomatic treatment:

- Year-round (persistent) and seasonal (intermittent) allergic rhinitis and conjunctivitis (itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia)

- hay fever (hay fever)

- urticaria, incl.

chronic idiopathic

Name ENG

SUPRASTINEX

Clinical and pharmacological group

Blocker of histamine H1 receptors.

Antiallergic drug

ATX code

Levocetirizine

Dosage

5mg

Structure

1 film-coated tablet contains: active ingredient: levocetirizine dihydrochloride 5 mg (equivalent to 4.21 mg levocetirizine), excipients: silicon microcrystalline cellulose Prosolv HD90 (MCC - 98%, anhydrous colloidal silicon dioxide - 2%) - 40, 4 mg

lactose monohydrate - 37.9 mg

low-substituted hyprolosis (L-HPC11) - 10 mg

magnesium stearate - 1.7 mg, shell: Opadry II 33G28523 white (hypromellose 2910 - 40%, titanium dioxide - 25%, lactose monohydrate - 21%, macrogol 3350 - 8%, triacetin - 6%) - 5 mg.

Indications

Indications

Symptomatic treatment:

- Year-round and seasonal allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia).

- Hay fever (hay fever).

- Hives, incl.

chronic idiopathic urticaria.

- Quincke's edema.

- Allergic dermatoses, accompanied by itching and rashes.

Contraindications

Severe renal failure (CC less than 10 ml / min).

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

- Pregnancy.

- Lactation period.

- Lactose intolerance, hereditary lactase deficiency lapp (lactase deficiency in some peoples of the North) or glucose-galactose malabsorption syndrome (due to the content of lactose in tablets).

- Hypersensitivity to the active (including piperazine derivatives) or any auxiliary component of the drug.

Care should be taken when:

- Chronic renal failure.

- Elderly patients (possibly decreased glomerular filtration).

Storage conditions and periods

At a temperature not higher than 30 degrees.

Expiration date: 5 years

INN / Active ingredient

Levocetirizine

Specifications

Category

Allergy

Scope of the drug

General

Release form

Tablet

Manufacturer country

Hungary

Package quantity, pcs

14

Minimum age from

2 years old

Way of introduction

Through the mouth

Vacation conditions

Without recipe

Shelf life after opening

Store an open bottle no more than 6 weeks.

Volume, ml.

20 ml

Brand name

Egis

The amount of the dosage form in the primary package

7 pcs.

Primary packaging type

Blister

Type of consumer packaging

Pack of cardboard

Anatomical and therapeutic characteristics

R06AE09 Levocetirizine

Dosage form

Film-coated tablets

The target audience

Children

Expiration date in days

1460

Package weight, g

twenty

Mode of application

:

The drug should be taken with food or on an empty stomach with a small amount of water, do not chew the tablets.

The daily dose is recommended to be taken in 1 dose.

Recommended dose for adults and children over 6 years old, elderly patients: (subject to normal renal function) - 5 mg (1 tablet) / day.

The duration of admission depends on the disease.

The course of treatment for hay fever is on average 1-6 weeks.

Pharmaco-therapeutic group

:

Antiallergic agent - H1-histamine receptor blocker

Dosage (volume) of the substance in the preparation

:

levocetirizine dihydrochloride 5 mg, which corresponds to the content of levocetirizine 4.21 mg

Information on technical characteristics, delivery set, country of manufacture "