Suprastinex, drops 5 mg/ml 20 ml

anti-allergic agent H1-histamine receptor blocker

ATX code: R06AE09

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 almost no sedative effect.

The action begins 12 hours after a single dose in 50% of patients, after 1 hour in 95% of patients and lasts for 24 hours.

Pharmacokinetics

The pharmacokinetics is linear. Absorption is fast when administered orally; eating has no effect on completeness of absorption, but reduces its speed. Bioavailability is 100%. Time to reach maximum concentration (TCmax) – 0.9 h, maximum concentration (Cmax) – 207 ng/ml. Volume of distribution is 0.4 l/kg.

The binding to plasma proteins is 90%. Less than 14% of the drug is metabolized in the liver by O-dealkylation to form pharmacologically inactive metabolite. Half-life (T1/2) is 7-10 hours. Total clearance is 0.63 ml/min/kg. Completely eliminated from the body within 96 hours. Excreted by the kidneys (85.4%). In renal failure (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

Active ingredient

Composition

How to take, the dosage

The drug should be taken with meals or on an empty stomach.

The required number of drops should be measured with a dropper into a tablespoon or glass of water. The drops should be taken orally immediately after dilution. The daily dose is recommended to be taken in one sitting.

The recommended dose for adults and children over 6 years of age, elderly patients (subject to normal renal function) is 5 mg (1 ml drops or 20 drops from a dropper) per day.
The maximum daily dose should not exceed 5 mg.

In children aged 2 to 6 years, the daily recommended dose is 2.5 mg in two doses in equal doses of 1.25 mg (2 times 0.25 ml = 2×5 drops from a dropper).
The maximum daily dose should not exceed 2.5 mg.

Patients with impaired renal function
Frequency of administration should be determined individually according to renal function. In patients with chronic renal insufficiency in creatinine clearance (CK) from 30 to 49 ml/min, the dose should be reduced twice (by 5 mg (1 ml drops or 20 drops from the dropper) every 3 days); in CKD from 10 to 29 ml/min the dose should be reduced by 3 times (by 5 mg (1 ml drops or 20 drops from the dropper) every 3 days). In severe renal failure (CKR less than 10 ml/min) the drug is contraindicated.

Patients with hepatic impairment
When prescribing the drug in patients with isolated hepatic impairment no dose changes are required. In patients with concomitant hepatic and renal impairment a dose adjustment is recommended (see section “Patients with renal impairment” above).

The duration of the drug
The duration of administration depends on the disease.

When treating persistent allergic rhinitis (symptoms When treating seasonal allergic rhinitis (symptoms > 4 days/1 week or lasting more than 4 weeks), treatment continues for the duration of allergen exposure.

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

In chronic diseases (year-round rhinitis, chronic idiopathic urticaria) the course of treatment may be longer in agreement with the doctor.

There is clinical experience of using the drug for up to 6 months.

Interaction

Levocetirizine interaction studies have shown no clinically significant interactions with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam.

The co-administration with macrolides or ketoconazole did not cause significant ECG changes.

Theophylline (400 mg/day) decreases total clearance of levocetirizine by 16%, and the kinetics of theophylline are not changed.

In sensitive patients, concomitant administration of levocetirizine with alcohol or other CNS depressants may affect the central nervous system.

Special Instructions

Suprastinex® Drops is not recommended for use in children under 2 years of age due to insufficient data on the administration of the drug.

It is recommended to refrain from the use of ethanol during treatment.
Suprastinex® Drops may cause allergic reactions (sometimes late) because they contain methyl parahydroxybenzoate and propyl parahydroxybenzoate.

Impact on driving and operating machinery

At the time of treatment, it is recommended to refrain from engaging in potentially dangerous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Hypersensitivity to the active (including piperazine derivatives) or any excipient of the drug; severe renal insufficiency (creatinine clearance less than 10 ml/min); children under 2 years of age (due to lack of clinical data); pregnancy and lactation.

With caution

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

Side effects

The side effect frequency parameters used below are defined as follows: Very frequent: >1/10; frequent: 1/100; infrequent: 1/1000; rare: 1/10000; very rare: Immune system disorders:
very rare – allergic reactions, including anaphylaxis.

Metabolic side:
very rare – increase in body weight.

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.

Subcutaneous fatty tissue:
very rarely – angioedema, skin itching, rash, urticaria.

As for laboratory examination data:
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

Pregnancy use

Similarities