Loratadine-Vertex, tablets 10 mg 30 pcs

Pharmacotherapeutic group

Anti-allergic agent – H₁-histamine receptor blocker.

ATH code

R06AX13

Pharmacological properties Pharmacodynamics

Loratadine, the active ingredient of the drug Loratadine – VERTEX, 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 antihistamine effect develops 30 minutes after oral administration, reaches a maximum of 8-12 hours from the start of action and lasts for more than 24 hours.

Loratadine has no effect on the central nervous system, has no clinically significant anticholinergic and sedative effect, i.e. does not cause drowsiness and does not affect the speed of psychomotor reactions when used in the recommended doses.

Long-term treatment did not cause clinically significant changes in vital signs, physical examination data, laboratory results or electrocardiography. Administration of loratadine does not lead to prolongation of the QT interval on the electrocardiogram (ECG).

Loratadine has no significant selectivity for H₂-histamine receptors. It does not inhibit norepinephrine reuptake and has virtually no effect on cardiovascular system or rhythm driver function.

Pharmacokinetics

absorption

It is rapidly and completely absorbed in the gastrointestinal tract. The time to reach maximum concentration (T_max) of loratadine in blood plasma is 1-1.5 h, and its active metabolite desloratadine is 1.5-3.7 h. Food intake increases T_max of loratadine and desloratadine by approximately 1 h, but has no effect on the effectiveness of the drug. The maximum concentration (C_max) of loratadine and desloratadine is independent of food intake. C_max of loratadine is increased in elderly patients, patients with chronic renal failure or alcoholic liver damage.

Distribution

The bioavailability of loratadine and its active metabolite is dose-dependent. Loratadine has a high degree (97-99%), and its active metabolite – a moderate degree (73-76%) of binding to blood plasma proteins. Equilibrium concentrations of loratadine and its metabolite in blood plasma are reached on the fifth day of administration. It does not penetrate through the blood-brain barrier.

Metabolism

. Metabolized in the liver to form the active metabolite desloratadine (descarboethoxyloratadine) with the participation of cytochrome P450 CYP3A4 and, to a lesser extent, cytochrome P450 CYP2D6 isoenzymes.

Elimation

Extracted through the kidneys (approximately 40% of the ingested dose) and through the intestine (approximately 42% of the ingested dose) for more than 10 days, mainly as conjugated metabolites. About 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 drug intake. The elimination half-life (T_1/2) of loratadine is 3 to 20 h (mean 8.4 h) and that of desloratadine is 8.8 to 92 h (mean 28 h).

Pharmacokinetics in Special Patient Groups

Elderly Patients

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

The T_1/2 of loratadine in elderly patients ranged from 6.7 to 37 h (mean 18.2 h), and of desloratadine from 11 to 39 h (mean 17.5 h).

Patients with impaired liver function

In patients with alcoholic liver damage, the C_max and area under the curve

“concentration-time curve (AUC) of loratadine and its active metabolite is twice as high as in patients with normal liver function. And T_1/2 of loratadine and T_1/2 of its active metabolite increase with increasing disease severity.

Patients with impaired renal function

In patients with chronic renal disease, the C_max and AUC of loratadine and its active metabolite are increased compared to these values in patients with normal renal function. At the same time, T_1/2 of loratadine and T_1/2 of its active metabolite do not differ from those in healthy patients.

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

One tablet contains:

active ingredient:

loratadine – 10.0 mg;

excipients:

Lactose monohydrate, 97.6 mg;

Microcrystalline cellulose, 28.0 mg;

sodium carboxymethyl starch (sodium starch glycolate, type A) – 3.0 mg;

calcium stearate – 1.4 mg.

.

How to take, the dosage

It is taken orally without chewing, with plenty of water, regardless of meals.

Adults, including the elderly and adolescents over 12 years are recommended to take Loratadine – VERTEX at a dose of 10 mg (1 tablet) once daily.

Children aged 3 to 12 years with a body weight over 30 kg – 10 mg (1 tablet) once a day. Adults and children with body weight over 30 kg with severe hepatic impairment should be given a reduced dose of the drug: 10 mg (1 tablet) once a day.

When the drug is used in elderly patients and patients with chronic renal insufficiency no dose adjustment is required.

Interaction

Eating has no effect on the effectiveness of the drug Loratadine – VERTEX . Loratadine does not increase the effect of alcohol on the central nervous system.

When taking loratadine together 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 on ECG data.

Special Instructions

The drug Loratadine – VERTEX should be discontinued at least 48 hours before performing skin allergy tests, because loratadine may affect their results.

Influence on the ability to drive vehicles, mechanisms

There have been no adverse effects of loratadine on the ability to drive a vehicle 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 vehicles and operate machinery.

Synopsis

Round flat cylindrical white or almost white beveled tablets.

Contraindications

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

– period of breastfeeding;

– childhood age less than 3 years and body weight less than 30 kg;

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

– severe liver function disorders;

– pregnancy.

Side effects

In clinical trials with children aged 2 to 12 years taking loratadine, headache (2.7%), nervousness (2.3%), fatigue (1%) were observed more frequently than in the placebo (“pacifier”) group.

In clinical trials with adults, adverse events observed more often than with placebo occurred in 2% of patients taking loratadine.

In adults, headache (0.6%), drowsiness (1.2%), increased appetite (0.5%) and insomnia (0.1%) were more frequently observed while using loratadine than in placebo group. In addition, there were very rare reports (< 1/10000) of dizziness, fatigue, dry mouth, gastrointestinal disturbances (nausea, gastritis), allergic reactions in the form of rash, anaphylaxis including angioedema, alopecia, impaired liver function, palpitations, tachycardia, seizures and weight gain during the post-registration 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 medical attention immediately.

Treatment

Symptomatic and supportive therapy. Possible gastric lavage, taking adsorbents (crushed activated charcoal with water).

Loratadine is not excreted during hemodialysis. After emergency care, the patient’s condition should continue to be monitored

Pregnancy use

The safety of using loratadine during pregnancy has not been established.

The drug may be used during pregnancy only when the expected therapeutic effect for the future 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 decision should be made to stop breast-feeding.

Similarities