Composition, form of production and packaging
? The tablets covered with a film shell of white or almost white color, cylindrical, biconcave, on a break two layers are visible - a kernel of white or almost white color and a film shell.
1 tab.
desloratadine 5 mg
Excipients: lactose monohydrate 70 mg, microcrystalline cellulose 12.1 mg, povidone 3 mg, magnesium stearate 0.9 mg, croscarmellose sodium 4 mg.
Composition of the film shell: opadrai II 85F48105 White 3 mg (including polyvinyl alcohol 1.407 mg, macrogol 3350 0.708 mg, talc 0.522 mg, titanium dioxide 0.363 mg).
10 pieces. - Cellular outline packaging (aluminum / PVC) (1) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (2) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (3) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (4) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (5) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (6) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (8) - cardboard packs.
10 pieces. - Cellular outline packaging (aluminum / PVC) (10) - cardboard packs.
10 pieces. - polymer cans (1) - packs of cardboard.
20 pcs. - polymer cans (1) - packs of cardboard.
30 pcs. - polymer cans (1) - packs of cardboard.
40 pcs. - polymer cans (1) - packs of cardboard.
50 pcs. - polymer cans (1) - packs of cardboard.
100 pieces. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Blocker H 1 - histamine receptors (long-acting). It is the primary active metabolite of loratadine. Inhibits the cascade of allergic inflammation reactions, including the release of anti-inflammatory cytokines, including interleukins IL-4, IL-6, IL-8, IL-13, release of pro-inflammatory chemokines (RANTES), production of superoxide anions by activated polymorphonuclear neutrophils, adhesion and chemotaxis of eosinophils , isolation of adhesion molecules such as P-selectin, IgE-mediated release of histamine, prostaglandin D2 and leukotriene C4. Thus, it prevents development and facilitates the course of allergic reactions, has antipruritic and antiexcudative action, reduces permeability of capillaries, prevents the development of edema of tissues, spasm of smooth muscles.
The drug has no effect on the central nervous system, has almost no sedative effect (does not cause drowsiness) and does not affect the rate of psychomotor reactions. Does not cause an extension of the QT interval on the ECG. The action of the drug begins within 30 minutes after ingestion and lasts for 24 hours.
PHARMACOKINETICS
Suction
After taking the drug inside desloratadine is well absorbed from the gastrointestinal tract, while determined concentrations of desloratadine in the blood plasma are reached within 30 minutes, and the maximum concentration is approximately after 3 hours.
Distribution
The binding of desloratadine to plasma proteins is 83-87%. When used in adults and adolescents for 14 days at a dose of 5 mg to 20 mg 1 time / day clinically significant cumulation of desloratadine is not noted. Simultaneous food intake or simultaneous consumption of grapefruit juice does not affect the distribution of desloratadine (when taken at a dose of 7.5 mg 1 time / day). Does not penetrate the blood-brain barrier.
Metabolism
It is subjected to intensive metabolism in the liver by hydroxylation to form 3-OH-desloratadine, combined with glucuronide. It is not an inhibitor of CYP3A4 and CYP2D6 isoenzymes and is not a substrate or inhibitor of P-glycoprotein.
Excretion
Only a small part of the dose taken internally is excreted by the kidneys (<2%) and through the intestine (<7%). T 1/2 - 20-30 hours (on the average - 27 hours.
INDICATIONS
- allergic rhinitis (elimination or relief of sneezing, nasal congestion, discharge of mucus from the nose, itching of the nose, itching of the palate, itching and redness of the eyes, lachrymation);
- urticaria (reduction or elimination of itching, rash).
DOSING MODE
The tablet should be swallowed whole, not liquid, squeezed with a small amount of water. The drug should preferably be taken at the same time of the day, regardless of the time of ingestion.
Adults and adolescents aged 12 years - 1 tab. (5 mg) 1 time / day.
SIDE EFFECT
The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%.
From the immune system: very rarely - a rash, including hives, angioedema, urticaria, dyspnea, anaphylactic shock.
From the side of the central nervous system: infrequently - a headache, very rarely - dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions, hallucinations.
From the cardiovascular system: very rarely - tachycardia, a feeling of palpitations.
From the digestive tract: rarely - dry mouth; very rarely - nausea, vomiting, indigestion, diarrhea, abdominal pain, increased activity of liver enzymes, increased bilirubin concentration, hepatitis.
From the osteomuscular system and connective tissue: very rarely - myalgia.
Other: often - increased fatigue.
CONTRAINDICATIONS
- Hypersensitivity to any of the components that make up the drug;
- Pregnancy and lactation;
- age up to 12 years;
- lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
With caution: severe renal failure.
PREGNANCY AND LACTATION
The use of the drug in pregnancy is contraindicated due to the lack of clinical data on the safety of its use during pregnancy.
Desloratadine is excreted in breast milk, so the use of the drug during breastfeeding is contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should be used in severe kidney failure.
APPLICATION FOR CHILDREN
Contraindicated for children under 12 years.
SPECIAL INSTRUCTIONS
Influence on the ability to drive and drive machinery
In the recommended dose, the drug does not affect the ability to drive vehicles or control mechanisms.
OVERDOSE
Symptoms: taking a dose that exceeds the recommended dose 5 times did not lead to any symptoms. In clinical trials, the daily use of desloratadine in adults and adolescents at doses up to 20 mg for 14 days was not accompanied by statistically or clinically significant changes in the cardiovascular system. In the clinical pharmacological study of the use of desloratadine at a dose of 45 mg per day (9 times higher than recommended) for 10 days did not cause prolongation of the QT interval and was not accompanied by serious side effects.
Treatment: with the occasional ingestion of a large amount of the drug - gastric lavage, the reception of activated charcoal; if necessary, symptomatic therapy. Desloratadine is not excreted in hemodialysis, the effectiveness of peritoneal dialysis is not established.
DRUG INTERACTION
Interactions with other drugs have not been identified.
Eating does not affect the effectiveness of the drug.
Desloratadine does not enhance the effect of alcohol on the central nervous system.
TERMS OF RELEASE FROM PHARMACY
Without recipe.
TERMS AND CONDITIONS OF STORAGE
In the dark place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 3 years.
