Loratadin-Teva, tablets 10 mg 30 pcs

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

ATX code: R06AX13

Pharmacological properties

Pharmacodynamics

Loratadine, the active substance of the drug Loratadine-Teva, 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 the drug Loratadine-Teva. The 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 the drug Loratadine-Teva does not lead to prolongation of the QT interval on ECG.

Long-term treatment did not observe clinically significant changes in parameters of vital functions, physical examination data, results of laboratory tests or electrocardiography.

Loratadine has no significant selectivity toward H₂-histamine receptors. 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. The time to reach maximum concentration (T_max) of loratadine in blood plasma is 1-1.5 hours and its active metabolite desloratadine is 1.5-3.7 hours. Eating increases the time to reach the maximum concentration (T_max) of loratadine and desloratadine by approximately 1 hour, but has no effect on the effectiveness of the drug. The maximum concentration (C_max) of loratadine and desloratadine is independent of food intake.

In patients with chronic renal disease the maximum concentration (C_max) and area under the concentration-time curve (AUC) of loratadine and its active metabolite are increased compared to patients with normal renal function. The elimination half-life of loratadine and its active metabolite does not differ from that of healthy patients.

In patients with alcoholic liver injury the C_max and AUC of loratadine and its active metabolite are doubled compared to these parameters 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. It is excreted through the kidneys (approximately 40% of the oral dose) and the intestines (approximately 42% of the oral dose) for more than 10 days, mainly as conjugated metabolites. About 27% of the ingested dose is excreted through the kidneys within 24 hours after drug intake. Less than 1% of the active substance is excreted unchanged through the kidneys within 24 hours after drug intake.

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 ranged from 3 to 20 hours (mean 8.4 hours) and that of desloratadine from 8.8 to 92 hours (mean 28 hours); in elderly patients, respectively, from 6.7 to 37 hours (mean 18.2 hours) and from 11 to 39 hours (mean 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 has no effect on the pharmacokinetics of loratadine and its active metabolite.

Indications

Sneezing (rhinitis), Urticaria, Allergies, Edema, Pollinosis, Sneezing, Skin itching

• Seasonal (pollinosis) and year-round allergic rhinitis, allergic conjunctivitis – elimination of symptoms associated with these diseases: sneezing, nasal mucosa itching, rhinorrhea, burning and itching sensation in the eyes, lacrimation;
• chronic idiopathic urticaria.

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Active ingredient

Loratadine

Composition

1 tablet contains:

Active ingredient: loratadine 10.0 mg.

Excipients: lactose monohydrate 62.5 mg, corn starch 2.0 mg, pregelatinized starch 25.0 mg, magnesium stearate 0.5 mg.

How to take, the dosage

Ingestion, regardless of meals.

Adults, including the elderly and adolescents over 12 years of age, 10 mg once daily.

Children 3 to 12 years of age:

• with a body weight greater than 30 kg, 10 mg once daily;
• with a body weight less than 30 kg, 5 mg once daily.

The duration of treatment depends on the duration of symptoms. If the patient’s condition does not improve within 3 days after the start of treatment, it means that loratadine is ineffective.

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

In adults and children weighing more than 30 kg with severe hepatic impairment, the starting dose should be 10 mg (1 tablet) every other day.

If there is no improvement after treatment or if new symptoms develop, a doctor should be consulted.

Interaction

Loratadine does not potentiate the effects of alcohol. Food intake has no effect on the effectiveness of loratadine. Erythromycin and ketoconazole (CYP3A4 isoenzyme inhibitors), cimetidine (CYP3A4 and CYP2D6 isoenzyme inhibitor) increase the Cmax of loratadine and its active metabolite in blood. There are no clinically significant changes.

Special Instructions

The administration of loratadine should be stopped 48 hours before the skin test because antihistamines can distort the results of the diagnostic test.

Read the instructions carefully before using the drug. Keep the instructions; you may need them again. Ask your doctor if you have any questions. The medicine you are taking is meant for you, and you should not give it to others, because it might cause them harm, even if you have the same symptoms as you do.

Influence on the ability to drive and operate machinery

There have been no adverse effects of the drug Loratadine-Teva on the ability to drive or perform other activities requiring increased concentration.

In very rare cases, however, some patients experience somnolence while taking the drug Loratadine-Teva, which may affect their ability to drive vehicles and operate machinery.

Synopsis

The tablets are white and oval in shape. On one side there is a separating risk and engraving “L” and “10” on both sides of the risk. The other side is smooth.

Contraindications

High sensitivity to loratadine and other components of the drug; lactose intolerance, lactase deficiency, 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 (see section “Use during pregnancy and breastfeeding”).

Side effects

In clinical trials with children aged 2 to 12 years who took loratadine more frequently than the placebo (“pacifier”) group, headache (2.7%), nervousness (2.3%), fatigue (1%) were observed. In clinical trials with adults, adverse events observed more frequently than with placebo were observed in 2% of patients taking loratadine. Headache (0,6%), somnolence (1,2%), appetite increase (0,5%) and insomnia (0,1%) were observed more often in adults while taking loratadine than in placebo group.

In addition, there were very rare reports in the post-marketing period (< 1/10,000) 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 listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Symptoms: headache, drowsiness, tachycardia. In case of overdose seek medical attention immediately. Treatment: symptomatic and supportive therapy. Perhaps gastric lavage, taking adsorbents (crushed activated carbon with water). Loratadine is not excreted by hemodialysis. After emergency treatment, the patient’s condition should continue to be monitored.

Pregnancy use

There are insufficient clinical data on the use of loratadine in pregnant women. Use is possible only if the estimated benefit to the mother exceeds the potential risk to the fetus. Loratadine is excreted with breast milk. If it is necessary to use loratadine during lactation, breastfeeding should be stopped.

Similarities

Claritin, Lomilan, Clarisense, Loragesal, Loratadine, Loratadine Teva, Loratavel