Lordestin, 5 mg 10 pcs.

Lordestin is an anti-allergic.

Pharmacodynamics

H₁-histamine receptor blocker, is the primary active metabolite of loratadine. Suppresses the release of histamine and LT C4 from mast cells. Prevents the development and facilitates the course of allergic reactions. It has anti-allergic, antipruritic and antiexudative effects. Reduces capillary permeability, prevents the development of tissue edema. It has practically no sedative effect and when used in therapeutic doses it does not influence the speed of psychomotor reactions.

Pharmacokinetics

Intake

After oral administration desloratadine is well absorbed from the GI tract, with detectable plasma concentrations of desloratadine being reached within 30 minutes. After a single dose of 5 or 7.5 mg, C_max is reached after approximately 3 h (2-6 h). 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 that of 3-hydroxydesloratadine is 85-89%. When used in dose from 5 mg to 20 mg once a day for 14 days no signs of clinically significant cumulation of desloratadine were found. Concomitant intake of food or simultaneous consumption of grapefruit juice does not affect bioavailability and distribution of desloratadine (when administered at a dose of 7.5 mg once daily). It does not penetrate through the HEB.

Metabolism and excretion

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

Cronic renal failure (CKD). C_max and AUC of desloratadine increase from 1.2 to 1.7 times and from 1.9 to 2.5 times, respectively (compared with data of healthy volunteers). Concentration of 3-hydroxydesloratadine changes insignificantly. Binding of desloratadine and 3-hydroxydesloratadine to plasma proteins in CKD does not change. Desloratadine and 3-hydroxydesloratadine are poorly excreted by hemodialysis.

Hepatic failure. In patients with hepatic impairment AUC is increased by 2.4 times compared to data of healthy volunteers. Total clearance of desloratadine when administered orally in patients with mild, moderate and severe hepatic impairment is 37, 36 and 28% respectively (as compared to data of healthy volunteers). There is an increase in T_1/2 of desloratadine in patients with hepatic impairment. The C_max and AUC of 3-hydroxydesloratadine in patients with hepatic impairment are not different from those in healthy subjects with normal liver function.

Indications

Seasonal allergic rhinitis (to relieve the following symptoms – sneezing, rhinorrhea, itching, stuffy nose, itchy eyes, lacrimation, red eyes, itching palate, cough); chronic idiopathic urticaria (skin itching and rash).

Active ingredient

Composition

The active ingredient:

desloratadine hemisulfate 5.788 (equivalent to 5 mg of desloratadine);

Excipients:

MCC – 39 mg;

calcium hydrophosphate dihydrate – 46.712 mg;

Pregelatinized starch – 7 mg;

Colloidal silica (aerosil) – 0.5 mg;

Magnesium stearate – 1 mg;

Filmed wrapper:

Opadry AMV 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)

How to take, the dosage

In the mouth, swallowed whole, without chewing. It is recommended to take the drug at the same time of the day, regardless of meals, with a small amount of water.

Adults and adolescents 12 years of age and older: Take once daily in a dose of 5 mg (1 tablet).

In case of CPN and hepatic insufficiency – dosing adjustment is required – the initial dose of 5 mg is recommended every other day (according to pharmacokinetics data). There are no dosing recommendations in children with CKD and hepatic impairment (due to insufficient data).

Interaction

When co-administered with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine no clinically significant changes in plasma concentrations of desloratadine were found.

Lordestine does not increase the inhibitory effect of ethanol on psychomotor function.

Special Instructions

Impact on driving and operating machinery

Lordestine when used in recommended doses has not been observed to affect the ability to drive and operate machinery.

However, given that patients may experience somnolence, caution is advised in case of central nervous system side effects.

Contraindications

With caution: severe renal insufficiency.

Side effects

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

Side effects according to post-marketing studies.

CNS side: dizziness, hallucinations, psychomotor hyperreactivity, insomnia, somnolence.

Cardiovascular system disorders: tachycardia, palpitations.

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

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

Others: dysmenorrhea, increased fatigue, myalgia.

Overdose

Symptoms: drowsiness.

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

Pregnancy use

The drug is contraindicated during pregnancy.

Because desloratadine is excreted with breast milk, the use of the drug during lactation (breast-feeding) is contraindicated.

Similarities