Lordestin pills 5mg, 10pcs

Composition

Active ingredient:

desloratadine hemisulfate 5,788 (equivalent to 5 mg of desloratadine);

Auxiliary substances:

MCC-39 mg;

calcium hydrophosphate dihydrate-46.712 mg;

pregelatinized starch-7 mg;

colloidal silicon dioxide (aerosil) – 0.5 mg;

magnesium stearate-1 mg;

Film shell:  

Opadry AMB yellow 80W22099 (partially hydrolyzed polyvinyl alcohol, titanium dioxide, talc, lecithin, aluminum varnish based on quinoline yellow dye, xanthan gum, iron oxide yellow, aluminum varnish based on indigo carmine dye)

Pharmacological action

Lordestin is an anti-allergic drug.

Pharmacodynamics

_H1-histamine receptor blocker, is the primary active metabolite of loratadine. Inhibits the release of histamine and LT C4 from mast cells. Prevents the development and eases the course of allergic reactions. It has anti-allergic, antipruritic and anti-exudative effects. Reduces capillary permeability, prevents the development of tissue edema. It has practically no sedative effect and when taken in therapeutic doses does not affect the speed of psychomotor reactions.

Pharmacokinetics

Suction

After oral use, desloratadine is well absorbed from the gastrointestinal tract, and detectable plasma concentrations of desloratadine are reached within 30 minutes. After a single dose of 5 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-hydroxydesloratadine is 85-89%. When used at a dose of 5 mg to 20 mg once a day for 14 days, there were no signs of clinically significant accumulation of desloratadine. Simultaneous food intake or simultaneous consumption of grapefruit juice does not affect the bioavailability and distribution of desloratadine (when taken at a dose of 7.5 mg once a day). It does not penetrate the BBB.

Metabolism and elimination

It undergoes intensive metabolism in the liver to 3-hydroxydesloratodine, which is then glucuronized. The main route of metabolism of desloratadine is hydroxylation. It is not an inhibitor of the CYP3A4 and CYP2D6 isoenzymes and is not a substrate or inhibitor of P-glycoprotein. Desloratadine is excreted from the body as a glucuronide compound and in small amounts unchanged (by the kidneys-less than 2% and through the intestines-less than 7%). T_1/2 for both desloratadine and 3-hydroxydesloratadine is 20-30 hours (on average-27 hours).

Chronic renal failure (CRF). The_cmax and AUC of desloratadine increase from 1.2 to 1.7 times and from 1.9 to 2.5 times, respectively (compared with the data of healthy volunteers). The concentration of 3-hydroxydesloratadine varies slightly. The binding of desloratadine and 3-hydroxydesloratadine to plasma proteins does not change in CRF. Desloratadine and 3-hydroxydesloratadine are poorly excreted during hemodialysis.

Liver failure. In patients with hepatic insufficiency, AUC increases by 2.4 times compared to the data of healthy volunteers. The total clearance of desloratadine when taken orally in patients with mild, moderate and severe hepatic insufficiency is 37,36 and 28%, respectively (compared with data in healthy volunteers). There is an increase in T_1/2 of desloratadine in patients with hepatic insufficiency. Cmax and AUC of 3-hydroxydesloratadine in patients with hepatic insufficiency do not differ from those in healthy people with normal liver function.

Indications

Seasonal allergic rhinitis (for relief of the following symptoms: sneezing, rhinorrhea, itching, nasal congestion, itchy eyes, watery eyes, redness of the eyes, itchy palate, cough); chronic idiopathic urticaria (skin itching and rash).

Use during pregnancy and lactation

The drug is contraindicated during pregnancy.

Since desloratadine is excreted in breast milk, the use of the drug during lactation (breastfeeding) is contraindicated.

Contraindications

• hypersensitivity to the components of the drug;
• pregnancy;
• lactation;
• children under 12 years of age.

With caution:  severe renal failure.

Side effects

The most common side effects were fatigue (1.2%), dry mouth (8%), and headache (0.6%).

Side effects according to post-marketing studies.

From the central nervous system: dizziness, hallucinations, psychomotor hyperreactivity, insomnia, drowsiness.

From the cardiovascular system: tachycardia, palpitations.

From the digestive system: abdominal pain, dyspepsia (including nausea, vomiting, diarrhea), hyperbilirubinemia, increased activity of liver enzymes, hepatitis.

Allergic reactions: skin rash, pruritus, urticaria, angioedema, anaphylactic shock.

Others: dysmenorrhea, fatigue, myalgia.

Interaction

When co-administered with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine, clinically significant changes in the concentration of desloratadine in plasma were not detected.

Lordestin does not enhance the inhibitory effect of ethanol on psychomotor function.

How to take, course of use and dosage

Inside, swallowing whole, without chewing. The drug is recommended to be taken at the same time of day, regardless of food intake, with a small amount of water.

Adults and adolescents aged 12 years and older-the drug is prescribed once a day at a dose of 5 mg (1 tablet).

In case of CRF and hepatic insufficiency-correction of the dosage regimen is required — the initial dose of 5 mg is recommended to be taken every other day (according to pharmacokinetic data). Dosage recommendations for children with CRF and hepatic insufficiency are not available (due to insufficient data).

Overdose

Symptoms:  drowsiness.

Treatment:  appointment of gastric lavage, activated charcoal, symptomatic therapy. The drug is not excreted by hemodialysis. The effectiveness of peritoneal dialysis has not been established.

Special instructions

Influence on the ability to drive motor vehicles and manage mechanisms

There was no effect of Lordestin when used in the recommended doses on the ability to drive vehicles and manage mechanisms.

However, given that patients may experience drowsiness, it is recommended to exercise caution if side effects from the central nervous system occur.

Form of production

Lordestin pills.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

4 years

Active ingredient

Desloratadine

Dosage form

Tablets

Description

For adults, Children over 12 years of age

Indications

Diathesis, Urticaria, Conjunctivitis, Dermatosis, Pollinosis, Allergic Rhinitis, Allergic Conjunctivitis, Runny Nose, Dermatitis, Allergy