Suprastinex, pills 5mg 14pcs

Composition

1 film-coated tablet contains:

Active ingredient:

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

excipients:

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

lactose monohydrate-37.9 mg;

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

magnesium stearate-1.7 mg,

shell:

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

Pharmacological action

Suprastinex has an antihistamine, anti-allergic effect.

Pharmacodynamics

Cetirizine enantiomer; competitive histamine antagonist; blocks H1-histamine receptors, the 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, reduces vascular permeability, and limits the release of inflammatory mediators. Prevents the development and eases the course of allergic reactions, has an antiexudative, antipruritic effect; practically does not have anticholinergic and antiserotonergic effects. In therapeutic doses, it has practically no sedative effect.

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

Pharmacokinetics

The pharmacokinetics are linear. It is rapidly absorbed when taken orally; food intake does not affect the completeness of absorption, but reduces its rate. Bioavailability – 100%. The time to reach the maximum concentration (TC_max) is 0.9 hours, the maximum concentration (Ctax) is 207 ng/ml. The volume of distribution is 0.4 l / kg. Binding to plasma proteins -90%. Less than 14% of the drug is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite.

The elimination half-life (T 1/2) is 7-10 hours. The total clearance is 0.63 ml / min / kg. Completely eliminated from the body within 96 hours. It is excreted by the kidneys (85.4%). With renal insufficiency (creatinine clearance less than 40 ml / min), clearance decreases (in patients on hemodialysis – by 80%), T 1/2-lengthens. Less than 10% is removed during hemodialysis. Penetrates into breast milk.

Indications

Symptomatic treatment of the following conditions:

• year-round (persistent) and seasonal allergic rhinitis and conjunctivitis (pruritus, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia);
• hay fever (pollinosis);
• urticaria, including chronic idiopathic urticaria;
• angioedema;
• allergic dermatoses accompanied by itching and rashes.

Use during pregnancy and lactation

Animal studies have shown no direct or indirect adverse effects on pregnancy, embryo or fetal development, delivery, or postnatal development. No controlled clinical studies have been conducted 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 take it during lactation, breastfeeding should be discontinued while taking the drug.

Contraindications

• hypersensitivity to the Active ingredient (including piperazine derivatives) or any auxiliary component of the drug;
• severe renal insufficiency (creatinine clearance less than 10 ml / min);
• children under 6 years of age (for film-coated tablets) and up to 2 years (for oral drops) – due to lack of clinical data;
• pregnancy and lactation;
• lactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome – for film-coated tablets.

With caution: chronic renal failure, advanced age (glomerular filtration rate may decrease).

Side effects

The side effect frequency parameters used below are defined as follows: very common – >1/10; common – > > 1/100 and >><1/10; uncommon – >1/1000 and <1/10; uncommon – ><1/100; rare – >1/10000 and <1/100; rare – ><1/1000; very rare —

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

From the side of 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 — dyspnoea.

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

Subcutaneous fat disorders: very rare — angioedema, pruritus, rash, urticaria.

From the side of laboratory parameters: very rarely — changes in functional liver tests.

If you experience any side effects, including those not specified in the instructions, you should consult a doctor.

Interaction

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

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

Levocetirizine does not enhance the effects of alcohol, but in sensitive patients, concomitant use of levocetirizine with alcohol or other CNS depressants may have an effect on the central nervous system.

How to take, course of use and dosage

The drug should be taken with a meal or on an empty stomach, washed down with a small amount of water, tablets should not be chewed. The daily dose is recommended to be taken in 1 dose.

The recommended dose for adults and children over 6 years of age, elderly patients: (subject to normal renal function) – 5 mg (1 tablet)/day.

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

Overdose

Symptoms: adults show drowsiness, children-agitation, anxiety, which are replaced by drowsiness.

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

Special instructions

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

Influence on the ability to drive a car or perform work that requires an increased rate of physical and mental reactions.

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

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

5 years

Active ingredient

Levocetirizine

Dosage form

Tablets

Description

Children over 6 years old, For adults

Indications

Urticaria, Dermatosis, Allergy, Neurodermatitis, Allergic Conjunctivitis, Allergic Rhinitis, Pollinosis