Loratavel, tablets 10 mg 30 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 (pollinosis) and year-round allergic rhinitis and allergic conjunctivitis – elimination of symptoms associated with these diseases – sneezing, nasal mucosa itching, rhinorrhea, burning and itching sensations in the eyes, lacrimation.

Chronic idiopathic urticaria.

Active ingredient

Composition

Excipients: corn starch, magnesium stearate, talc, sodium carboxymethyl starch (sodium starch glycolate, primogel), colloidal silica (aerosil), microcrystalline cellulose, lactose monohydrate (milk sugar).

How to take, the dosage

Ingestion, regardless of the time of meals.

In adults, including elderly patients and adolescents older than 12 years of age it is recommended to take the drug in a dose of 10 mg (1 tablet) once daily.

In elderly patients and patients with chronic renal failure, there is no need to adjust the dose.

In children at the age of 3 to 12 years and weighing more than 30 kg, 10 mg (1 tablet) once a day. Adults and children with body weight over 30 kg with severe hepatic impairment should receive a starting dose of 10 mg (1 tablet) once a day.

Interaction

Food intake has no effect on the effectiveness of loratadine.

Loratadine does not increase the effect of alcohol on the central nervous system.

When loratadine is coadministered with ketoconazole, erythromycin or cimetidine, an increase in plasma concentrations of loratadine and its metabolite is noted, but this increase is not clinically significant, including as determined by electrocardiography.

Special Instructions

The use of the drug should be stopped at least two days before performing skin allergy tests, because loratadine may affect their results. Effect on the ability to drive vehicles, machinery

No adverse effect of loratadine on the ability to drive a vehicle or perform other activities requiring increased concentration has been found.

In very rare cases, however, some patients experience drowsiness while taking loratadine, which may affect their ability to drive and operate machinery.

Synopsis

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 function disorders;

– pregnancy.

Side effects

In clinical trials with children aged 2 to 12 years who took the drug more often than the placebo (“pacifier”) group, headache (2.7%), nervousness (2.3%), fatigue (1%) were observed.

In clinical trials with adults, adverse events observed more often than with placebo occurred in 2% of patients taking the drug. In adults, headache (0.6%), drowsiness (1.2%), increased appetite (0.5%), and insomnia (0.1%) were observed more often with the drug than with the placebo group. In addition, there have been very rare reports (< 1/10,000) of dizziness, fatigue, dry mouth, gastrointestinal disturbances (nausea, gastritis), allergic reactions in the form of rash, anaphylaxis including angioedema, alopecia, impaired liver function, palpitation, tachycardia and seizures in the postmarketing period.

If any of the side effects listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms: drowsiness, tachycardia, headache. In case of overdose seek immediate medical attention.

Treatment: symptomatic and supportive therapy. Perhaps gastric lavage, taking 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.

Pregnancy use

Safety of use of loratadine during pregnancy has not been established. The use of the drug during pregnancy is possible only if the estimated benefit to the mother exceeds the potential risk to the fetus.

Loratadine and its active metabolite are excreted into the breast milk, therefore, if the drug is prescribed during breast-feeding, the question of stopping breast-feeding should be considered.

Similarities