Expiration date: 05/2025
Dosage Form: tablet, film-coated
Composition
1 tablet coated with a film cover, comprising:
surfactant: 5.000 mg of desloratadine,
Other ingredients: microcrystalline cellulose 65,800 mg, 2,250 mg of magnesium oxide, starch pregelatinized 4,750 mg, 4,500 mg of lactose, Valium, 4 thousand 1,700 mg, 1,000 mg of zinc stearate,.
film coating: Opadry Blue 03V90819 2,975 mg (Valium 60.00%, 27.21% titanium dioxide, macrogol 400 8.00% indigo carmine (E132 aluminum nail) 4,79%).
Description
Round biconvex tablets, film-coated cyan, engraved "D" on one side and smooth on the other side.
Pharmacotherapeutic group: anti-allergic agent - H1-histamine receptor blocker
ATC code: R06AX27
Pharmacodynamics
Antihistamines long-acting peripheral histamine H1-receptor blocker. Desloratadine is the primary active metabolite of loratadine. It inhibits the cascade of allergic inflammation, including release of inflammatory cytokines including the interleukins IL-4, IL-6, IL-8, IL-13, the release of proinflammatory chemokines, production of superoxide anion by activated polymorphonuclear neutrophils adhesion and chemotaxis of eosinophils, allocation of adhesion molecules such as P-selectin, IgE - mediated release of histamine, prostaglandin D2 and leukotriene C4. Thus, it prevents the development and facilitates the allergic reactions, has antipruritic and antiexudativ effect, reduces the permeability of capillaries, prevents the development of edema, smooth muscle spasm.
The drug has no effect on the central nervous system (CNS), virtually no sedative effect (does not cause drowsiness) and does not affect the speed of psychomotor reactions does not cause QT interval elongation in the electrocardiogram (ECG).
Action desloratadine starts within 30 minutes after ingestion and lasts for 24 hours.
Pharmacokinetics
Suction.
After oral administration desloratadine well absorbed from the gastrointestinal tract (GIT), the defined desloratadine plasma concentrations are reached within 30 minutes, and the maximum plasma concentration (Cmax) -. Approximately 3 h food or alcohol reception practically changes the pharmacological properties of the drug.
Distribution.
desloratadine Plasma protein binding is 83-87%. When applied in a dose of 5 mg to 20 mg 1 time per day for 14 days, signs of clinically significant accumulation of desloratadine is not revealed. Simultaneous eating or drinking grapefruit juice at the same time does not affect the distribution of desloratadine (when receiving a dose of 7.5 mg 1 time per day). It does not cross the blood-brain barrier (BBB).
Metabolism.
Subjected to intensive metabolism by hydroxylation with the formation of 3-OH-desloratadine connected to the glucuronide. Not an inhibitor of CYP3A4 and CYP2D6 isozyme and is not a substrate or inhibitor of P-glycoprotein.
Withdrawal. Report from the body in the form of glucuronide compounds and a small amount in an unmodified form, a small portion excreted by the kidneys (2%) and feces (7%). The half-life (T1 / 2) averages 27 h (20-30 h).
Testimony
Seasonal (hay fever) and perennial allergic rhinitis (elimination or relief of sneezing, nasal congestion, discharge of mucus from the nose, itchy nose, itching palate, itching and redness of eyes, watery eyes).
Chronic idiopathic urticaria (reduction or elimination of itching, rash).
Contraindications
Hypersensitivity to desloratadine, and the other components of the drug, pregnancy, lactation, age 12 years, lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Carefully
Severe renal insufficiency.
Application of pregnancy and during breastfeeding
Use of the drug-Desloratadine Teva is contraindicated during pregnancy and lactation (insufficient efficacy and safety data).
Dosing and Administration
Inside, regardless of meals at the same time. Tablets should be swallowed whole without chewing, with a small amount of water.
Adults and children over 12 years: 5 mg 1 time per day.
Side effect
The incidence of adverse events classified according to the recommendations of the World Health Organization: very often - at least 10%, often - at least 1% but less than 10%, infrequently - at least 0.1% but less than 1%, rare - at least 0 , 01%, but less than 0.1%, very rare - less than 0.01%.
Immune system: very rarely - rash including urticaria, angioedema, dyspnoea, anaphylactic shock.
CNS: rarely - headache, very rarely - dizziness, somnolence, insomnia, psychomotor hyperactivity, seizures, hallucinations.
Since the cardiovascular system: very rarely - tachycardia, palpitations.
From the gastrointestinal tract: rarely - dry mouth, rarely - nausea, vomiting, dyspepsia, diarrhea, abdominal pain, increased activity of "liver transaminases", increasing the concentration of bilirubin, hepatitis.
On the part of the musculoskeletal system and connective tissue disorders: very rarely - myalgia.
Other: often - fatigue.
Overdose
Symptoms: receiving doses higher than the recommended 5 times, does not cause any symptoms.
In clinical trials, daily use in adults and adolescents desloratadine dose of 20 mg for 14 days was not associated with statistically or clinically significant changes of the cardiovascular system.
The clinical and pharmacological study of the use of desloratadine in a dose of 45 mg per day (9 times the recommended) for 10 days did not cause QT prolongation and is not accompanied by the appearance of serious side effects.
Treatment: gastric lavage, activated charcoal, if necessary - symptomatic therapy. Desloratadine does not appear in hemodialysis, peritoneal dialysis efficacy has not been established.
Interaction with other drugs
Clinically significant interactions with other drugs have been identified.
Desloratadine does not increase ethanol effects on the central nervous system.
Food intake does not affect the efficacy of the drug.
special instructions
In order to protect the tablets from light blisters should be stored in a carton box.
Effects on ability to transport management and work with equipment
With the development of adverse reactions from the central nervous system, such as drowsiness, dizziness, hallucinations, is not recommended to perform actions that require high concentration and speed of psychomotor reactions.
release Form
Tablets, film-coated, 5 mg.
At 7 or 10 tablets in a blister made of PVC / PCTFE / aluminum foil.
At 1, 2 or 3 blisters with instruction for use in a cardboard box.
Storage conditions
The temperature is not above 25 ° C.
Keep out of the reach of children.
Shelf life
3 years.
Do not use beyond the expiration date printed on the package.
