Suprastinex, 5 mg 14 pcs

Suprastinex has antihistamine, anti-allergic action.

Pharmacodynamics

The 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 the migration of eosinophils, reduces 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 minutes 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. It is quickly absorbed when administered orally; eating has no effect on completeness of absorption, but reduces its speed. Bioavailability is 100%. Time to maximum concentration (TC_max) – 0.9 hours, maximum concentration (Stah) – 207 ng/ml. Volume of distribution – 0.4 l/kg. Binding to plasma proteins -90%. Less than 14% of the drug is metabolized in the liver through O-dealkylation to form pharmacologically inactive metabolite.

Half-life (T1/2) is 7-10 hours. Total clearance is 0.63 ml/min/kg. It is completely eliminated from the body within 96 hours. Excreted by the kidneys (85.4%). In renal insufficiency (creatinine clearance less than 40 ml/min) clearance is decreased (in patients undergoing hemodialysis – by 80%), T1/2 is prolonged. Less than 10% is removed during hemodialysis. It penetrates into breast milk.

Indications

Symptomatic treatment of the following conditions:

Active ingredient

Composition

1 film-coated tablet contains:

the active ingredient:

levocetirizine dihydrochloride 5 mg (equivalent to 4.21 mg of levocetirizine),

auxiliary substances:

Persolv HD90 silicon microcrystalline cellulose (MCC – 98%, colloidal silicon dioxide anhydrous – 2%) – 40.4 mg;

Lactose monohydrate – 37.9 mg;

Low substituted hyprolose (L-HPC11) – 10 mg;

Magnesium stearate – 1.7 mg,

coating:

Opadry II 33G28523 white (hypromellose 2910 – 40%, titanium dioxide – 25%, lactose monohydrate – 21%, macrogol 3350 – 8%, triacetin – 6%) – 5 mg

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 that the daily dose be taken in 1 sitting.

The recommended dose for adults and children over 6 years of age, elderly patients: (assuming normal renal function) 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

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

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

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

Special Instructions

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

Impact on the ability to drive a car or perform work requiring increased speed of physical and mental reactions.

During treatment, it is recommended to refrain from engaging in potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

With caution: chronic renal failure, advanced age (decreased glomerular filtration is possible).

Side effects

The following side effect frequency parameters are defined as follows: very frequently – >1/10; frequently – >1/100 and <1/10; infrequently – >1/1000 and <1/100; rarely – >1/10000 and <1/1000; very rarely – <1/10000.

Immune system disorders: very rare – allergic reactions, including anaphylaxis.

Metabolic system disorders: very rarely – weight gain.

The central and peripheral nervous system: often – somnolence, headache, fatigue; infrequent – asthenia; rarely – migraine, dizziness.

Respiratory system: very rarely – dyspnea.

Gastrointestinal disorders: frequent – dry mouth; infrequent – abdominal pain; very rare – nausea, dyspepsia.

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

Laboratory findings: very rarely – changes in liver function tests.

In case of any side effects, including those not mentioned in the instructions, consult a physician.

Overdose

Symptoms: in adults it is manifested by drowsiness, in children – excitement, restlessness, which is replaced by sleepiness.

Treatment: it is necessary to flush the stomach and see a doctor. There is no specific antidote. Symptomatic and supportive therapy is recommended. Hemodialysis is ineffective.

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 take the drug during lactation, breastfeeding should be stopped.

Similarities