Lordestin 5mg Coated Tablet N30
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Active ingredients
Desloratadine
Release form
Pills
Composition
Desloratadine hemisulphate 5.788 mg,; which corresponds to the content of desloratadine 5 mg; Refs: apt: microcrystalline cellulose, calcium hydrophosphate dihydrate, pregelatinized starch, colloidal silicon dioxide (Aerosil), magnesium stearate, amB yellow 80W22099, (17 oz) tere (2242099 opt) nitre (Zerf res); , lecithin, aluminum lacquer based on quinoline yellow dye, xanthan gum, iron yellow oxide, aluminum lacquer based on indigo carmine dye).
Pharmacological effect
Histamine H1 receptor blocker. It is the primary active metabolite of loratadine. Suppresses the release of histamine and leukotriene C4 from mast cells. Prevents the development and facilitates the course of allergic reactions. It has anti-allergic, antipruritic and anti-exudative action. Reduces capillary permeability, prevents the development of tissue edema. Practically does not have a sedative effect and when taken in therapeutic doses does not affect the speed of psychomotor reactions.
Pharmacokinetics
Absorption; After taking the drug inside, desloratadine is well absorbed from the gastrointestinal tract, with detectable plasma concentrations of desloratadine within 30 minutes. After a single dose in a dose of 5 mg or 7.5 mg Cmax is reached in approximately 3 hours (2-6 hours). The bioavailability of desloratadine is proportional to the dose (in the dose range of 5-20 mg); Distribution; The binding of desloratadine to plasma proteins is 83-87%, and 3-hydroxydeslolododine - 85-89%. When used in a dose of 5 mg to 20 mg 1 time / day for 14 days, there was no evidence of clinically significant cumulation of desloratadine. Simultaneous ingestion of food or simultaneous consumption of grapefruit juice does not affect the bioavailability and distribution of desloratadine (when taken in a dose of 7.5 mg 1 time per day). Does not penetrate through the BBB.; Metabolism and excretion; It is extensively metabolized in the liver to 3-hydroxydlozloratodin, which is then glucuronic. The main metabolic pathway of desloratadine is hydroxylation. It is not an inhibitor of isoenzymes CYP3A4 and CYP2D6 and is not a substrate or inhibitor of P-glycoprotein.Desloratadine is eliminated from the body as a glucuronide compound and in a small amount in an unchanged form (by the kidneys - less than 2% and through the intestine - less than 7%). T1 / 2 for both desloratadine and 3-hydroxydloxodine ratine is 20-30 hours (average 27 hours); Pharmacokinetics in special clinical cases; In chronic renal failure, Cmax and AUC desloratadine increase from 1.2 to 1.7 times and from 1.9 to 2.5 times, respectively (compared with data from healthy volunteers). The concentration of 3-hydroxydloxidine varies slightly. The binding of desloratadine and 3-hydroxydlozloratodina with plasma proteins in chronic renal failure does not change. Desloratadine and 3-hydroxydeloratodin are poorly excreted by hemodialysis. In patients with hepatic insufficiency, the AUC increases by 2.4 times compared with those in healthy volunteers. The total clearance of desloratadine in oral administration in patients with mild, moderate, and severe liver failure is 37%, 36%, and 28%, respectively (compared with data from healthy volunteers). There is an increase in T1 / 2 desloratadine in patients with hepatic insufficiency.; Cmax and AUC of 3-hydroxydeloxloratodine in patients with hepatic insufficiency do not differ from those in healthy people with normal liver function.
Indications
- seasonal allergic rhinitis (to relieve the following symptoms: sneezing, rhinorrhea, itching, nasal congestion; itching in the eyes, tearing, redness of the eyes; itching in the palate, cough); - Chronic idiopathic urticaria (pruritus and rash).
Contraindications
- pregnancy; - lactation period; - children's age up to 12 years; - Hypersensitivity to the components of the drug. With caution should be prescribed the drug in severe renal failure.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy. Since desloratadine is excreted in breast milk, the use of the drug during lactation (breastfeeding) is contraindicated.
Dosage and administration
Inside Adults and adolescents aged 12 years and older, the drug is prescribed in a dose of 5 mg (1 tab.) 1 time / day. The drug is recommended to take at the same time of day, regardless of the meal, drinking a small amount of water.The tablet should be swallowed whole without chewing.; In chronic renal and hepatic insufficiency, a dosage regimen is required: the initial dose of 5 mg is recommended every other day (according to pharmacokinetics) .; Dosing recommendations in children with chronic renal and hepatic insufficiency are absent due to lack of data.
Side effects
The most frequent side effects: fatigue (1.2%), dry mouth (8%), headache (0.6%); Side effects according to post-marketing research.; CNS: dizziness.; Cardiovascular: tachycardia ; heartbeat.; From the alimentary system: abdominal pain, dyspepsia (including nausea, vomiting, diarrhea), hyperbilirubinemia, increased liver enzymes, hepatitis.; Allergic reactions: skin rash, itching, urticaria, angioedema, anaphylactic shock.; Other: dysmenorrhea, increased fatigue incapability, myalgia.
Overdose
In case of overdose, drowsiness is observed.; Treatment: gastric lavage, activated carbon, symptomatic therapy. The drug is not excreted by hemodialysis. The effectiveness of peritoneal dialysis has not been established.
Interaction with other drugs
When combined with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine, there are no clinically significant changes in the concentration of desloratadine in the plasma. Lordestin does not increase the inhibitory effect of ethanol on the psychomotor function.
special instructions
Influence on ability to drive motor vehicles and control mechanisms; No influence of Lordestin, when used in recommended doses, on ability to drive motor vehicles and control mechanisms. However, given that patients may experience drowsiness, caution is advised when side effects appear on the CNS side.