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

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

During long-term treatment, no clinically significant changes in vital signs, physical examination findings, laboratory results, or electrocardiography were observed. Taking loratadine does not prolong the QT interval on the electrocardiogram (ECG).

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

Suction

Quickly and completely 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 Tmax of loratadine and desloratadine by approximately 1 hour, but does not affect the effectiveness of the drug. The maximum concentration (Cmax) of loratadine and desloratadine is independent of food intake. Cmax of loratadine increases 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 has a moderate degree (73-76%) of binding to plasma proteins. Equilibrium concentrations of loratadine and metabolite in blood plasma are achieved on the fifth day of administration. Does not penetrate the blood-brain barrier.

Metabolism

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

Removal

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 after taking the drug. Less than 1% of the active substance is excreted unchanged through the kidneys within 24 hours after taking the drug. The half-life (T1/2) 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).

Pharmacokinetics in special groups of patients

Elderly patients

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

T1/2 of loratadine in elderly patients ranges from 6.7 to 37 hours (average 18.2 hours), and desloratadine – from 11 to 39 hours (average 17.5 hours).

Patients with liver dysfunction

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

The concentration-time concentration (AUC) of loratadine and its active metabolite is doubled compared to these values ​​in patients with normal liver function. At the same time, T1/2 of loratadine and T1/2 of its active metabolite increase with increasing severity of the disease.

Patients with impaired renal function

In patients with chronic kidney disease, the Cmax and AUC of loratadine and its active metabolite are increased compared to those in patients with normal renal function. In this case, T1/2 of loratadine and T1/2
its active metabolite does not differ from those in healthy patients.

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

Special instructions

The drug Loratadine – VERTEX should be discontinued at least 48 hours 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

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.

Pregnancy

The safety of loratadine during pregnancy has not been established.

It is possible to use the drug during pregnancy only if the expected therapeutic effect for the expectant mother exceeds 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

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

– period of breastfeeding;

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

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

With caution

– severe liver dysfunction;

– pregnancy.

Side Effects

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

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

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

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 the drug Loratadine – VERTEX. 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 the blood plasma is observed, but this increase is not clinically significant, including according to ECG data.

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 ºС. Keep out of the reach of children.

Shelf life

3 years.

Do not use after expiration date.

Manufacturer

Vertex, Russia