Instructions for medical use of the drug "Lordestin"

Directions for use and doses

Inside.
For adults and adolescents aged 12 years and older, the drug is prescribed once a day at a dose of 5 mg (1 tablet). It is recommended to take the drug at the same time of day, regardless of meals, with a small amount of water. The tablet should be swallowed whole without chewing.

For chronic renal failure and liver failure, adjustment of the dosage regimen is required: an initial dose of 5 mg is recommended to be taken every other day (according to pharmacokinetics data). Recommendations for dosing in children with chronic renal failure and liver failure are not available due to insufficient data.

Lordestin, 30 pcs., 5 mg, film-coated tablets

Suction

After taking the drug orally, desloratadine is well absorbed from the gastrointestinal tract, and detectable concentrations of desloratadine in the blood plasma are achieved within 30 minutes. After a single dose of 5 or 7.5 mg, Cmax is achieved in approximately 3 hours (2–6 hours). The bioavailability of desloratadine is dose proportional (dose range 5–20 mg).

Distribution

Plasma protein binding of desloratadine is 83–87%, and 3-hydroxydesloratadine is 85–89%. When used in a dose of 5 mg to 20 mg 1 time per day for 14 days, no signs of clinically significant accumulation of desloratadine were detected. Concomitant 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 1 time per day). Does not penetrate the BBB.

Metabolism and excretion

It is extensively metabolized in the liver to 3-hydroxydesloratodine, which is then glucuronidized. The main route of metabolism of desloratadine 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 from the body in the form of a glucuronide compound and in small amounts unchanged (by the kidneys - less than 2% and through the intestines - less than 7%). T1/2 for both desloratadine and 3-hydroxydesloratadine is 20–30 hours (average 27 hours).

Chronic renal failure (CRF).

Cmax and AUC of desloratadine increase from 1.2 to 1.7 times and from 1.9 to 2.5 times, respectively (compared to data from healthy volunteers). The concentration of 3-hydroxydesloratadine changes slightly. The binding of desloratadine and 3-hydroxydesloratadine to plasma proteins does not change in chronic renal failure. Desloratadine and 3-hydroxydesloratadine are poorly excreted by hemodialysis.

Liver failure.

In patients with liver failure, AUC increases 2.4 times compared to healthy volunteers. The overall oral clearance of desloratadine in patients with mild, moderate and severe hepatic impairment is 37, 36 and 28%, respectively (compared with data in healthy volunteers). There is an increase in T1/2 of desloratadine in patients with liver failure. The Cmax and AUC of 3-hydroxydesloratadine in patients with hepatic impairment do not differ from those in healthy subjects with normal liver function.

Side effect

The most common side effects: 1.2% - fatigue, 8% - dry mouth, 0.6% - headache.
Side effects according to post-marketing studies: dizziness, tachycardia, palpitations, abdominal pain, dyspepsia (including nausea, vomiting, diarrhea), hyperbilirubinemia, increased activity of liver enzymes, hepatitis, allergic reactions (skin rash, itching, urticaria, angioedema, anaphylactic shock), dysmenorrhea, fatigue, myalgia, hallucinations, psychomotor hyperreactivity, insomnia, drowsiness.

Lordestin

Manufacturer: GEDEON RICHTER-RUS CJSC (Russia)

◊ tab., cover. film-coated, 5 mg: 10 or 30 pcs. Reg. No.: LSR-006570/10

Clinical and pharmacological group:

Histamine H1 receptor blocker. Antiallergic drug

Release form, composition and packaging

◊ Film-coated tablets

yellow, round, biconvex; at the break - white or almost white.

Excipients:

microcrystalline cellulose, calcium hydrogen phosphate dihydrate, pregelatinized starch, colloidal silicon dioxide (Aerosil), magnesium stearate, 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).

10 pieces. — cellular contour packages (1) — cardboard packs. 10 pieces. — cellular contour packages (3) — cardboard packs.

Description of the active components of the drug "Lordestin"

pharmachologic 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 antiallergic, antipruritic and antiexudative effects. Reduces capillary permeability, prevents the development of tissue edema. It has virtually no sedative effect and, when taken in therapeutic doses, does not affect the speed of psychomotor reactions.

Indications

- seasonal allergic rhinitis (to relieve the following symptoms: sneezing, rhinorrhea, itching, nasal congestion; itching in the eyes, lacrimation, redness of the eyes; itching in the palate, cough);

- chronic idiopathic urticaria (skin itching and rash).

Dosage regimen

Inside. Adults and teenagers aged 12 years and older

the drug is prescribed in a dose of 5 mg (1 tablet) 1 time/day.

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

For chronic renal and liver failure

correction of the dosage regimen is required: the initial dose of 5 mg is recommended to be taken every other day (according to pharmacokinetics data).

Dosing recommendations for children with chronic renal and liver failure

missing due to insufficient data.

Side effect

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

Side effects based on post-marketing studies

.

From the side of 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, itching, urticaria, angioedema, anaphylactic shock.

Other:

dysmenorrhea, increased fatigue, myalgia.

Contraindications

- pregnancy;

- lactation period;

- children under 12 years of age;

- hypersensitivity to the components of the drug.

Carefully _

the drug should be prescribed for severe renal failure.

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.

Use for liver dysfunction

For chronic liver failure

correction of the dosage regimen is required: the initial dose of 5 mg is recommended to be taken every other day (according to pharmacokinetics data).

Use for renal impairment

For chronic renal failure

correction of the dosage regimen is required: the initial dose of 5 mg is recommended to be taken every other day (according to pharmacokinetics data).

special instructions

Impact on the ability to drive vehicles and operate machinery

There was no observed effect of Lordestin when used in recommended doses on the ability to drive vehicles and operate machinery. However, given that patients may experience drowsiness, caution is recommended if central nervous system side effects occur.

Overdose

In case of overdose, drowsiness is observed.

Treatment:

gastric lavage, activated carbon, symptomatic therapy. The drug is not eliminated by hemodialysis. The effectiveness of peritoneal dialysis has not been established.

Drug interactions

When used together with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine, no clinically significant changes in plasma concentrations of desloratadine were detected.

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

Conditions for dispensing from pharmacies

The drug is approved for use as a means of OTC.

Storage conditions and periods

The drug should be stored out of the reach of children at a temperature not exceeding 25°C. Shelf life: 4 years. Do not use after the expiration date.

Drug interactions

When used together with ketoconazole, erythromycin, azithromycin, fluoxetine and cimetidine, no clinically significant changes in plasma concentrations of desloratadine were detected.

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

Lordestin®

In children aged 6 to 23 months, the following side effects were observed, the frequency of which was slightly higher than when using placebo (“dummies”): diarrhea (in 3.7% of cases), increased body temperature (2.3%), insomnia (2.3%).

In children aged 2 to 11 years, the incidence of side effects when using desloratadine syrup was the same as when using placebo.

According to the results of clinical studies in children aged 6 to 11 years, no side effects were identified when taking desloratadine syrup in recommended doses (2.5 mg/day).

In children aged 12-17 years, according to the results of clinical studies, the most common side effect was headache (5.9%), the frequency of which was no higher than when taking placebo (6.9%).

In adults and adolescents (12 years of age and older), according to the results of clinical studies, side effects were recorded in 3% of patients compared to the placebo group, the most common of which were: increased fatigue (1.2%), dry mouth (0). .8%), headache (0.6%).

Information on side effects is presented based on the results of clinical studies and observations of the post-registration period.

According to the World Health Organization (WHO), side effects are classified according to their frequency as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to <1/100), rare (from ≥ 1/10000 to <1/1000), very rare (<1/10000); frequency unknown - based on available data, it was not possible to determine the frequency of occurrence.

From the mental side

: very rarely - hallucinations; frequency unknown - abnormal behavior, aggression.

From the nervous system

: often - headache; often (in children under 2 years of age) - insomnia; very rarely - dizziness, drowsiness, insomnia, psychomotor hyperactivity, convulsions.

From the liver and biliary tract:

very rarely - increased activity of liver enzymes, increased bilirubin concentration, hepatitis; frequency unknown - jaundice.

From the digestive system:

often - dry mouth, often (in children under 2 years of age) - diarrhea; very rarely - abdominal pain, nausea, vomiting, dyspepsia, diarrhea.

From the cardiovascular system:

very rarely - tachycardia, palpitations; frequency unknown - prolongation of the QT interval.

From the musculoskeletal system:

very rarely - myalgia.

For the skin and subcutaneous tissues:

frequency unknown - photosensitivity.

Common disorders:

often - increased fatigue, often (in children under 2 years of age) - fever; very rarely - anaphylaxis, angioedema, shortness of breath, itching, rash, including urticaria; frequency unknown - asthenia.

Post-registration period

Children

: frequency unknown - QT prolongation, arrhythmia, bradycardia, abnormal behavior, aggression.

If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.

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 antiallergic, antipruritic and antiexudative effects. Reduces capillary permeability, prevents the development of tissue edema. It has virtually no sedative effect and, when taken in therapeutic doses, does not affect the speed of psychomotor reactions.