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, incl. chronic idiopathic urticaria.
– Year-round and seasonal allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia).
– Hay fever (hay fever).
– Quincke’s edema.
– Allergic dermatoses, accompanied by itching and rashes.

Pharmacological effect

antiallergic agent – H1-histamine receptor blocker

ATX code: R06A E09

Pharmacological properties

Pharmacodynamics

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

Prevents the development and facilitates the course of allergic reactions, has an antiexudative and antipruritic effect; has virtually no anticholinergic and antiserotonergic effects. In therapeutic doses it has virtually no sedative effect.

Pharmacokinetics

Pharmacokinetics is linear.
Rapidly absorbed when taken orally; food intake does not affect the completeness of absorption, but reduces its speed.

Bioavailability – 100%. Time to reach maximum concentration (TCmax) is about 0.9 hours, maximum concentration (Cmax) is 207 ng/ml.

The volume of distribution is about 0.4 l/kg. Communication with plasma proteins – 90%. Less than 14% of the drug is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite.
The half-life (T1/2) is 7-10 hours. The total clearance is about 0.63 ml/min/kg. Completely excreted from the body within 96 hours. Excreted by the kidneys (approximately 85%). In case of renal failure (creatinine clearance less than 40 ml/min), clearance decreases (in patients on hemodialysis – by 80%), T1/2 – lengthens. Less than 10% is removed during hemodialysis.

Passes into breast milk.

Special instructions

During the treatment period, it is recommended to refrain from drinking ethanol.
Suprastinex® film-coated tablets contain lactose and should not be administered to patients with lactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, it is recommended to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Levocetirizine

Composition

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

Excipients:

silicon microcrystalline cellulose (microcrystalline cellulose, colloidal anhydrous silicon dioxide),

lactose monohydrate (37.9 mg),

low-substituted hyprolose (L-HPC11),

magnesium stearate.

Shell composition:

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

Pregnancy

Animal studies have shown no direct or indirect harmful effects on pregnancy, embryonic or fetal development, childbirth or postnatal development. There have been no controlled clinical studies on the safety of the drug in pregnant women, so the drug should not be prescribed during pregnancy.

Levocetirizine is excreted in breast milk, so if it is necessary to use it during lactation, breastfeeding should be discontinued while taking the drug.

Contraindications

Hypersensitivity to the active (including piperazine derivatives) or any auxiliary component of the drug; severe renal failure (creatinine clearance less than 10 ml/min); children under 6 years of age (for this dosage form); pregnancy and lactation; lactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome.

With caution

Chronic renal failure, old age (possibly decreased glomerular filtration).

Side Effects

The parameters used below for the frequency of side effects are defined as follows: very often – >1/10; often – 1/100; infrequently – 1/1000; rarely – 1/10000; very rare From the immune system:
very rarely – allergic reactions, including anaphylaxis.

Metabolism:
very rarely – weight gain.

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

From the respiratory system:
very rarely – dyspnea.

From the gastrointestinal tract:
often – dry mouth, infrequently – abdominal pain,
very rarely – nausea, dyspepsia.

From the side of subcutaneous fat:
very rarely – angioedema, itching, rash, urticaria.

From the laboratory parameters:
very rarely – changes in functional “liver” tests.

If any side effects occur, incl. not specified in the instructions, you must consult a doctor.

Interaction

Interaction studies of levocetirizine have shown no clinically significant interactions with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam. Combined use with macrolides or ketoconazole did not cause significant changes in the ECG.

Theophylline (400 mg/day) reduces the total clearance of levocetirizine by 16%. In this case, the pharmacokinetics of theophylline does not change.

Levocetirizine does not enhance the effects of ethanol, however, in sensitive patients, concomitant use of levocetirizine with ethanol or other CNS depressants may cause CNS effects.

Overdose

Symptoms of overdose in adults include drowsiness, in children – agitation, anxiety, which are replaced by drowsiness.

In case of overdose, you must rinse your stomach and consult a doctor. There is no specific antidote. Symptomatic and supportive therapy is recommended. Hemodialysis is not effective.

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

5 years

Manufacturer

EGIS, Hungary