Suprastinex, 5 mg 7 pcs

anti-allergic agent – H1-histamine receptor blocker

ATC code: R06A E09

Pharmacological properties

Pharmacodynamics

Anti-allergic agent. Enantiomer of cetirizine; competitive histamine antagonist; blocks H1-histamine receptors, affinity for which is 2 times higher than for cetirizine. It influences the histamine-dependent stage of allergic reactions; it reduces migration of eosinophils, decreases vascular permeability and limits the release of inflammatory mediators.

It prevents and facilitates the development of allergic reactions, has antiexudative, antipruritic effects; it has practically no anticholinergic and antiserotoninergic action. In therapeutic doses has practically no sedative effect.

Pharmacokinetics

Pharmacokinetics is linear.
It is rapidly absorbed when taken orally; eating has no effect on the completeness of absorption, but reduces its rate.

The bioavailability is 100%. Time of reaching maximum concentration (TCmax) – about 0.9 h, maximum concentration (Cmax) – 207 ng/ml.

The volume of distribution is about 0.4 l/kg. Binding to plasma proteins is 90%. Less than 14% of the drug is metabolized in the liver through O-dealkylation to form pharmacologically inactive metabolite.
Half-life period (T1/2) – 7-10 hours. Total clearance is about 0.63 ml/min/kg. It is completely eliminated from the body within 96 hours. Excreted by the kidneys (about 85%). In renal insufficiency (creatinine clearance less than 40 ml/min), clearance is decreased (in patients on hemodialysis – by 80%), T1/2 is prolonged. Less than 10% is removed during hemodialysis.

It penetrates into breast milk.

Indications

Symptomatic treatment:
– Urticaria, including chronic idiopathic urticaria.

Active ingredient

Composition

1 film-coated tablet contains: levocetirizine dihydrochloride 5 mg, which corresponds to the content of levocetirizine 4.21 mg.

Auxiliary substances:

Microcrystalline cellulose (microcrystalline cellulose, colloidal anhydrous silica),

Lactose monohydrate (37.9 mg),

Hyprolose low substituted (L-HPC11),

Magnesium stearate.

Shell contents:

Opadray II 33G28523 white (hypromellose 2910, titanium dioxide, lactose monohydrate (1.05 mg), macrogol 3350, triacetin)

How to take, the dosage

The drug should be taken with a meal or on an empty stomach with a small amount of water, do not chew the tablets. It is recommended to take the daily dose in 1 dose.

The recommended dose for adults and children over 6 years old, elderly patients: (if kidney function is normal) 5 mg (1 tablet)/day.

The duration of treatment depends on the disease. The course of treatment of pollinosis is on average 1-6 weeks.

Interaction

Interaction studies of levocetirizine showed no clinically significant interaction with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam. Co-administration with macrolides or ketoconazole did not cause significant ECG changes.

Theophylline (400 mg/) decreases total clearance of levocetirizine by 16%. The pharmacokinetics of theophylline is not altered.

Levocetirizine does not potentiate the effects of ethanol; however, in sensitive patients, concomitant administration of levocetirizine with ethanol or other CNS depressants may affect the CNS.

Special Instructions

The drug Suprastinex® coated tablets contain lactose, therefore it should not be administered to patients with lactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome.

Impact on driving and operating machinery

At the time of treatment, it is recommended to refrain from performing potentially hazardous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

With caution

Chronic renal insufficiency, advanced age (decreased glomerular filtration is possible).

Side effects

Metabolic disorders:
very rarely – weight gain.

As to the central and peripheral nervous system:
often – drowsiness, headache, increased fatigue;
infrequently – asthenia;
rarely – migraine, dizziness.

Respiratory system disorders:
very rarely – dyspnea.

Gastrointestinal tract:
often – dry mouth, infrequent – abdominal pain,
very rare – nausea, dyspepsia.

In the subcutaneous fatty tissue:
very rarely – angioedema, skin itching, rash, urticaria.

Laboratory findings:
very rarely – changes of functional “liver” tests.

In case of any side effects, including those not specified in the instructions, it is necessary to consult a physician.

Overdose

The symptoms of overdose in adults are manifested by drowsiness, in children – excitement, anxiety, which is replaced by drowsiness.

In case of overdose it is necessary to flush the stomach and seek medical attention. There is no specific antidote. Symptomatic and supportive therapy is recommended. Hemodialysis is not effective.

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Pregnancy use

Animal studies have shown no direct or indirect harmful effects on pregnancy, embryonic or fetal development, labor or postnatal development. Controlled clinical studies on the safety of the drug in pregnant women have not been conducted; therefore, the drug should not be prescribed in pregnancy.

Levocetirizine is excreted with breast milk, therefore if it is necessary to use the drug during lactation, breastfeeding should be stopped.

Similarities