Loratavel, tablets 10 mg 10 pcs

Pharmacotherapeutic group: anti-allergic agent – H₁-histamine receptor blocker.

The ATX code: [R06AX13]

Pharmacological properties

Loratadine is a tricyclic compound with pronounced antihistamine action and is a selective blocker of peripheral H₁-histamine receptors. It has a rapid and prolonged antiallergic effect. The onset of action is within 30 minutes after oral administration of loratadine. Antihistamine effect reaches its maximum after 8-12 hours from the beginning of action and lasts for more than 24 hours.

Loratadine does not penetrate through the blood-brain barrier and has no effect on the central nervous system. It has no clinically significant anticholinergic or sedative effect, i.e. it does not cause drowsiness and does not affect the speed of psychomotor reactions when used in the recommended doses. Administration of loratadine does not lead to prolongation of the QT interval on electrocardiogram (ECG). During long-term treatment, no clinically significant changes of vital signs, physical examination data, results of laboratory tests or electrocardiography have been observed. It does not inhibit norepinephrine reuptake and has virtually no effect on cardiovascular system or rhythm driver function.

Pharmacokinetics

Loratadine is rapidly and well absorbed in the gastrointestinal tract. Time to reach maximum concentration (Tmax) of loratadine in blood plasma is 1-1.5 hours, and its active metabolite desloratadine – 1.5-3.7 hours. Food intake increases the time to reach maximum concentration (Tmax) of loratadine and desloratadine by 1 hour, but has no effect on the effectiveness of the drug. Maximum concentration (Cmax) of loratadine and desloratadine is independent of food intake. Maximum concentration (Cmax) and area under the curve “concentration – time” (AUC) of loratadine and its active metabolite are increased in patients with chronic kidney disease compared to patients with normal renal function. Half-lives of loratadine and its active metabolite do not differ from those of healthy patients. In patients with alcoholic liver damage Cmax and AUC of loratadine and its active metabolite are increased twice as much compared to these indices in patients with normal liver function.

Loratadine has a high degree (97-99%) and its active metabolite a moderate degree (73-76%) of binding to plasma proteins.

Loratadine is metabolized to desloratadine via the cytochrome P450 3A4 system and, to a lesser extent, the cytochrome P450 2D6 system. It is excreted via the kidneys (approximately 40% of the oral dose) and the intestine (approximately 42% of the oral dose) for more than 10 days, mainly as conjugated metabolites. Approximately 27% of the oral dose is excreted through the kidneys within 24 hours after drug administration. Less than 1% of the active substance is excreted unchanged through the kidneys within 24 hours after taking loratadine. Bioavailability of loratadine and its active metabolite is dose-dependent.

The pharmacokinetic profiles of loratadine and its active metabolite in adult and elderly healthy volunteers were comparable.

The elimination half-life of loratadine ranged from 3 to 20 hours (mean 8.4 hours) and that of desloratadine from 8.8 to 92 hours (mean 28 hours); in older patients, from 6.7 to 37 hours (mean 18.2 hours) and 11 to 39 hours (mean 17.5 hours), respectively. The half-life increases with alcoholic liver damage (depending on the severity of the disease) and does not change in the presence of chronic renal failure.

Hemodialysis in patients with chronic renal failure has no effect on the pharmacokinetics of loratadine and its active metabolite.

Indications

Seasonal (hay fever) and year-round allergic rhinitis and allergic conjunctivitis – elimination of symptoms associated with these diseases – sneezing, itching of the nasal mucosa, rhinorrhea, burning and itching in the eyes, lacrimation.

Chronic idiopathic urticaria.

Pharmacological effect

Pharmacotherapeutic group: antiallergic agent – ​​H₁-histamine receptor blocker.

ATX code: [R06AX13]

Pharmacological properties

Pharmacodynamics

Loratadine is a tricyclic compound with a pronounced antihistamine effect and is a selective blocker of peripheral H₁-histamine receptors. Has a quick and long-lasting antiallergic effect. The onset of action is within 30 minutes after taking loratadine orally. The antihistamine effect reaches its maximum after 8-12 hours from the onset of action and lasts more than 24 hours.

Loratadine does not penetrate the blood-brain barrier and has no effect on the central nervous system. It does not have a clinically significant anticholinergic or sedative effect, that is, it does not cause drowsiness and does not affect the speed of psychomotor reactions when used in recommended doses. Taking loratadine does not prolong the QT interval on the electrocardiogram (ECG). With long-term treatment, no clinically significant changes in vital signs, physical examination data, laboratory tests or electrocardiography were observed. Loratadine does not have significant selectivity for histamine H2 receptors. Does not inhibit norepinephrine reuptake and has virtually no effect on the cardiovascular system or pacemaker function.

Pharmacokinetics

Loratadine is quickly and well absorbed from the gastrointestinal tract. The time to reach the maximum concentration (Tmax) of loratadine in the blood plasma is 1-1.5 hours, and its active metabolite desloratadine is 1.5-3.7 hours. Eating increases the time to reach maximum concentration (Tmax) of loratadine and desloratadine by 1 hour, but does not affect the effectiveness of the drug. The maximum concentration (Cmax) of loratadine and desloratadine does not depend on food intake. In patients with chronic kidney disease, the maximum concentration (Cmax) and area under the concentration-time curve (AUC) of loratadine and its active metabolite are increased compared to patients with normal renal function. The half-lives of loratadine and its active metabolite do not differ from those in healthy patients. In patients with alcoholic liver damage, the Cmax and AUC of loratadine and its active metabolite are doubled compared to these values ​​in patients with normal liver function.

Loratadine has a high degree (97-99%), and its active metabolite has a moderate degree (73-76%) of binding to plasma proteins.

Loratadine is metabolized to desloratadine via the cytochrome P450 3A4 system and, to a lesser extent, the cytochrome P450 2D6 system. Excreted through the kidneys (approximately 40% of the oral dose) and intestines (approximately 42% of the oral dose) for more than 10 days, mainly in the form of conjugated metabolites. Approximately 27% of an oral dose is excreted through the kidneys within 24 hours of taking the drug. Less than 1% of the active substance is excreted unchanged through the kidneys within 24 hours after taking loratadine. The bioavailability of loratadine and its active metabolite is dose-dependent.

The pharmacokinetic profiles of loratadine and its active metabolite were comparable in adults and elderly healthy volunteers.

The half-life of loratadine ranges from 3 to 20 hours (average 8.4 hours), and that of desloratadine ranges from 8.8 to 92 hours (average 28 hours); in elderly patients, respectively, from 6.7 to 37 hours (average 18.2 hours) and from 11 to 39 hours (average 17.5 hours). The half-life increases with alcoholic liver damage (depending on the severity of the disease) and does not change in the presence of chronic renal failure.

Hemodialysis in patients with chronic renal failure does not affect the pharmacokinetics of loratadine and its active metabolite.

Special instructions

The drug should be stopped at least two days before skin allergy tests, since loratadine may affect their results. Impact on the ability to drive vehicles and machinery

There was no negative effect of loratadine on the ability to drive a car or perform other activities requiring increased concentration.

However, in very rare cases, some patients experience drowsiness while taking loratadine, which may affect their ability to drive or operate machines.

Active ingredient

Loratadine

Composition

For one tablet:

Active ingredient: loratadine – 10.0 mg.

Pregnancy

The safety of loratadine during pregnancy has not been established. The use of the drug during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

Loratadine and its active metabolite are excreted into breast milk, therefore, when prescribing the drug during breastfeeding, the issue of stopping breastfeeding should be considered.

Contraindications

– hypersensitivity to loratadine or any other component of the drug;

– lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

– period of breastfeeding;

– children under 3 years of age and body weight less than 30 kg.

With caution

– severe liver dysfunction;

– pregnancy.

Side Effects

In clinical studies involving children aged 2 to 12 years, headache (2.7%), nervousness (2.3%), and fatigue (1%) were observed more often than in the placebo group (“dummy”).

In clinical studies in adults, adverse events observed more frequently than with placebo occurred in 2% of patients taking the drug. In adults, when using the drug more often than in the placebo group, headache (0.6%) and drowsiness (1.2%) were observed.

%), increased appetite (0.5%) and insomnia (0.1%). In addition, there have been very rare post-marketing reports (<1/10,000) of dizziness, fatigue, dry mouth, gastrointestinal disorders (nausea, gastritis), allergic reactions such as rash, anaphylaxis including angioedema, alopecia, liver dysfunction, palpitations, tachycardia and convulsions.

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.

Interaction

Eating does not affect the effectiveness of loratadine.

Loratadine does not enhance the effects of alcohol on the central nervous system.

When loratadine is taken together with ketoconazole, erythromycin or cimetidine, an increase in the concentration of loratadine and its metabolite in plasma is observed, but this increase is not clinically significant, including according to electrocardiography.

Overdose

Symptoms: drowsiness, tachycardia, headache. In case of overdose, consult a doctor immediately.

Treatment: symptomatic and supportive therapy. It is possible to lavage the stomach, take adsorbents (crushed activated carbon with water). Loratadine is not excreted during hemodialysis. After emergency care is provided, it is necessary to continue monitoring the patient’s condition.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life

3 years.

Do not use after expiration date.

Manufacturer

Velfarm LLC, Russia