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

Excipients: lactose monohydrate (Tabletose 100), microcrystalline cellulose (Avicel PH 112), silicon dioxide colloid (Aerosil 200), magnesium stearate.

Shell:

Ramp-white (Opadrai White) Y-1-7000) [hypromellose-5cP, titanium dioxide, macrogol-400 (polyethylene oxide-400)].

Description:

White, biconvex tablets of oval form, covered with a film membrane, on one side of the tablet there is a fault line with an engraving "G"on either side of it, the other side of the tablet is smooth.

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) -the enantiomer of cetirizine, a competitive histamine antagonist, blocks H₁-gistaminovye receptors, affinity for which is 2 times higher than that of cetirizine. It affects the histamine-dependent stage of allergic reactions, reduces the migration of eosinophils, 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, has almost no anticholinergic and antiserotonin action. In therapeutic doses, sedation is very poorly expressed. The action begins 12 minutes after receiving a single dose in 50% of patients, after 1 hour - in 95% and lasts for 24 hours. Does not affect the interval QT on the ECG.

Pharmacokinetics:

Pharmacokinetics is linear in nature, independent of dose and time, and varies insignificantly among different people.

Absorption

Quickly absorbed when taken orally; food intake does not affect the fullness of absorption, but reduces its speed. Bioavailability is 100%. Time to reach the maximum concentration in the blood (TC_mOh) - 0,9 h, the maximum concentration in the blood (C_mOh) - 207 ng / ml. The volume of distribution is 0.4 l / kg. The degree of absorption depends on the dose and is not disturbed by eating, but when eating, the maximum concentration decreases, and its achievement slows down.

Distribution

Levocetirizine binds to plasma proteins by 90%. Data on the distribution of levocetirizine in tissues and its penetration through the blood-brain barrier in humans are absent. Levocetirizine penetrates into breast milk.

Metabolism

In humans, less than 14% of the dose of levocetirizine is metabolized, since the expected differences in the pharmacokinetic profile of levocetirizine due to genetic polymorphism or the simultaneous administration of enzyme inhibitors are negligible. Metabolic transformations consist in oxidation of an aromatic ring, N- and O-dealkylation and conjugation with taurine.The dealkylation process is mainly carried out by means of an isoenzyme CYP3A4, while the oxidation of the aromatic ring occurs by means of many and / or unidentified CYP-isoform. Levocetirizine when administered orally at a dose of 5 mg and / or when exceeding the maximum concentrations in the blood plasma, does not affect the activity CYP-isoenzymes 1A2, 2C9, 2C19, 2B6, 2E1, 3A4.

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

Excretion

The half-life (T_1/2) - 7-10 hours Total ground clearance - 0.63 ml / min / kg. It is completely eliminated from the body within 96 hours. It is excreted mainly with urine (85.4%) from the accepted dose.

Patients with renal insufficiency

The total clearance of levocetirizine depends on the creatinine clearance (CC), so 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.The amount of levocetirizine withdrawn with a standard 4-hour hemodialysis procedure is less than 10%.

Indications:

Symptomatic treatment of year-round and seasonal allergic rhinitis and allergic conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, congestion hyperemia); hay fever (hay fever).

Symptomatic treatment of urticaria, incl. chronic idiopathic urticaria; edema of Quincke; other allergic dermatoses, accompanied by itching and rashes.

Contraindications:

Hypersensitivity to levocetirizine, drug components, piperazine derivatives, severe chronic renal failure (CRF, CC less than 10 ml / min), pregnancy, lactation, children under 6 years.

Intolerance to galactose, deficiency of lactase and glucose-galactose malabsorption.

Carefully:

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

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).

When used concomitantly with alcohol (see Interaction with other medicinal products).

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 liquid and squeezed 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 - age (years)] 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

There is a clinical experience of the continuous use of levocetirizine in adult patients lasting up to 6 months.

In the treatment of seasonal (intermittent) allergic rhinitis (the presence of symptoms less than 4 days a week or their total duration is less than 4 weeks), the duration of treatmentdepends on the duration of the symptomatology; Treatment can be stopped if symptoms disappear and are resumed when symptoms appear.

In the treatment of year-round (persistent) allergic rhinitis (the presence of symptoms more than 4 days a week and their total duration of more than 4 weeks) treatment can continue throughout the exposure period of allergens.

The course of treatment is determined by a doctor; on average, it is 1-6 weeks.

In chronic diseases (including chronic idiopathic urticaria), the course of treatment can be longer in agreement with the doctor.

Side effects:

Side effects of levocetirizine are divided according to the system-organ classes in accordance with the classification of the Medical Dictionary on regulatory legal activity (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.

Metabolic and nutritional disorders:

Frequency unknown: increased appetite.

Disturbances from the nervous system:

Often: headache.

Infrequently: drowsiness.

Rarely: dizziness.

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

The frequency is unknown: insomnia, thrombosis of the sinuses of the dura mater, paresthesia, fainting, anxiety, tremor, dysgeusia, suicidal thoughts.

Hearing impairments:

Frequency unknown: vertigo.

Vision disorders:

The frequency is unknown: blurred vision, inflammatory manifestations.

Disorders from the cardiovascular system:

Very rarely: palpitations, tachycardia.

The frequency is unknown: thrombosis of the jugular vein, stenocardia.

Disturbances from the respiratory system, chest and mediastinal organs:

Very rarely: dyspnea.

Frequency unknown: increased symptoms of rhinitis.

Disorders from the gastrointestinal tract:

Often: dryness of the oral mucosa.

Infrequent: pain in the abdomen.

Very rarely: nausea, diarrhea.

Frequency unknown: vomiting.

Disorders from the kidneys and urinary system:

The frequency is unknown: dysuria, urinary retention.

Disturbances 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.

The frequency is unknown: hypotrichosis, cracks, photosensitivity.

Disturbances from musculoskeletal and connective tissue:

Very rarely: myalgia Common violations:

Often: fatigue.

Infrequently: asthenia.

Frequency unknown: peripheral edema.

Violations from laboratory and instrumental data:

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

Other:

Frequency unknown: cross reactivity.

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

Overdose:

Symptoms

Symptoms of overdose may include drowsiness in adults and agitation, as well as restlessness, 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:

The interaction of levocetirizine with other drugs has not been studied.

Investigations of the interactions of the racemate of cetirizine showed no clinically significant interactions with pseudoeprin, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, and diazepam.

Theophylline (400 mg / day) reduces the total clearance of cetirizine by 16%, while the kinetics of theophylline does not change.

With the simultaneous administration of ritanovir (600 mg twice daily) and cetirizine (10 mg per day), cetirizine exposure is increased (40%), and exposure to ritanovir varies insignificantly.

The degree of absorption of cetirizine did not decrease, under the influence of food, although the rate of absorption decreased.

In some cases, with simultaneous application of levocetirizine with ethanol or drugs that have an inhibitory effect on the central nervous system, it is possible to intensify this action.

Special instructions:

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

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

It is necessary to refrain from driving and other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 5 mg.

Packaging:

At 7, 10 or 14 tablets in a strip of aluminum foil or 7, 10 and 14 tablets in a blister made of white opaque film of PVC / PVDC - aluminum foil.

For 1, 2 or 5 strips and for 1,2 or 5 blisters together with instructions for use in a cardboard bundle.

Storage conditions:

In dry, dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-007273/10

Date of registration:28.07.2010 / 11.11.2015

Expiration Date:Unlimited

The owner of the registration certificate:Glenmark Pharmaceuticals Co., Ltd.Glenmark Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

GLENMARK PHARMACEUTICALS, Ltd. India

Representation: & nbspGLENMARK IMPEX LLCGLENMARK IMPEX LLCRussia

Information update date: & nbsp26.04.2017

Illustrated instructions

Instructions

Glenceth (Glencet)