Loratavel pills 10mg, 30pcs

Composition

Per tablet: Active ingredient: loratadine – 10.0 mg.

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

Pharmacological action

Pharmacotherapeutic group: anti-allergic 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. It has a fast and long-lasting anti-allergic effect. The onset of action is within 30 minutes after oral use of loratadine. The antihistamine effect reaches its maximum after 8-12 hours from the start of action and lasts for more than 24 hours.

Loratadine does not cross the blood-brain barrier and does not affect 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 rate of psychomotor reactions when used at the recommended doses. Taking loratadine does not lead to prolongation of the QT interval on an electrocardiogram (ECG). During long-term treatment, no clinically significant changes in vital signs, physical examination data, laboratory tests, or electrocardiography were observed. Iloratadine does not have significant selectivity for H₂-histamine receptors. It does not inhibit norepinephrine reuptake and has virtually no effect on the cardiovascular system or pacemaker function.

Pharmacokinetics

Loratadine is rapidly and well absorbed in the gastrointestinal tract. The time to reach the maximum concentration (Tmax) of loratadine in blood plasma is 1-1.5 hours, and its active metabolite desloratadine is 1.5 – 3.7 hours. Food intake increases the time to reach the 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 twice as high as 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 by the cytochrome P4503A4 system and, to a lesser extent, the cytochrome P4502D6 system. It is excreted through the kidneys (approximately 40% of the oral dose) and through the intestines (approximately 42% of the oral dose) for more than 10 days, mainly in the form of conjugated metabolites. Approximately 27% of the oral dose is eliminated by the kidneys within 24 hours of taking the drug. Less than 1% of the Active ingredient 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 in adult and elderly healthy volunteers were comparable.

The elimination half-life of loratadine is 3 to 20 hours (average 8.4 hours), and that of desloratadine is 8.8 to 92 hours (average 28 hours); in elderly patients,6.7 to 37 hours (average 18.2 hours) and 11 to 39 hours (average 17.5 hours), respectively. The elimination 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.

Indications

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

Chronic idiopathic urticaria.

Use during pregnancy and lactation

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

Loratadine and its active metabolite are excreted in breast milk, so when prescribing a drug during breastfeeding, the question of stopping breastfeeding should be decided.

Contraindications

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

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

– breastfeeding period;

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

With caution

-severe liver function disorders;

– pregnancy.

Side effects

Headache (2.7%), nervousness (2.3%), fatigue (1%) were observed in clinical trials involving children aged 2-12 years who took the drug more often than in the placebo group (“pacifiers”).

In clinical trials involving adults, adverse events that occurred more frequently 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 when using the drug than in the placebo group. In addition, there were very rare reports in the post-marketing period (

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

Interaction

Food intake does not affect the effectiveness of loratadine.

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

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

How to take, course of use and dosage

Inside, regardless of the meal time.

Adults, including the elderly, and adolescents over 12 years of age are recommended to take the drug at a dose of 10 mg (1 tablet) 1 time a day.

When using the drug in elderly patients and in patients with chronic renal failure, no dose adjustment is required.

Children aged 3 to 12 years with a body weight of more than 30 kg – 10 mg (1 tablet) 1 time a day. Adults and children with a body weight of more than 30 kg with severe hepatic impairment, the initial dose should be 10 mg (1 tablet) every other day.

Overdose

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

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

Description

Round flat-cylindrical tablets of white or almost white color with a risk and chamfer.

Special instructions

The drug should be discontinued at least two days before conducting skin allergic tests, as loratadine may affect their results. Influence on the ability to drive vehicles and mechanisms

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

However, in very rare cases, some patients experience drowsiness when taking loratadine, which can affect their ability to drive vehicles and work with mechanisms.

Storage conditions

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

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Loratadine

Dosage form

Tablets