Claritin, tablets 10 mg 30 pcs

Antianallergic agent – H1-histamine receptor blocker.

Pharmacodynamics

Loratadine – the active ingredient of Claritin®, is a tricyclic compound with pronounced antihistamine action and is a selective blocker of peripheral H1-histamine receptors. It has a fast and prolonged antiallergic effect. Onset of action is within 30 minutes after oral administration of Claritin®. 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 Claritin® drug does not lead to prolongation of QT interval on ECG.

Long-term treatment showed no clinically significant changes in vital signs, physical examination data, laboratory results or electrocardiography. Loratadine has no significant selectivity for H2-histamine receptors. It does not inhibit norepinephrine reuptake and has practically no effect on the 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. Eating increases the time to reach the maximum concentration (Tmax) of loratadine and desloratadine by approximately 1 hour, but has no effect on the effectiveness of the drug.

The maximum concentration (Cmax) of loratadine and desloratadine is independent of food intake. In patients with chronic renal disease the maximum concentration (Cmax) and area under the curve “concentration-time” (AUC) of loratadine and its active metabolite are increased 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 increased twice as much as these indexes in patients with normal liver function, while pharmacokinetics of its active metabolite did not change significantly.

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 through the kidneys (about 40% of the oral dose taken) and the intestines (about 42% of the oral dose) for more than 10 days, mainly as conjugated metabolites. Approximately 27% of the ingested dose is excreted through the kidneys within 24 hours after drug administration. Less than 1% of 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 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, itching
nasal mucosa, rhinorrhea, burning and itching sensations in the eyes, lacrimation.

Chronic idiopathic urticaria.

Active ingredient

Composition

1 tablet contains:

The active ingredient: loratadine 10 mg;

auxiliary substances: lactose monohydrate 71.3 mg, corn starch 18 mg, magnesium stearate 0.7 mg.

How to take, the dosage

To be taken regardless of the time of meals.

Adults, including the elderly, and adolescents over 12 years of age are recommended in a dose of 10 mg (1 tablet or 2 teaspoons (10 ml) of syrup) once daily.

In children 2 to 12 years of age it is recommended to prescribe the dose depending on the body weight: if the body weight is 30 kg or less – 5 mg (1 teaspoon (5 ml) of syrup) once a day; if the body weight is more than 30 kg – 10 mg (2 teaspoons (10 ml) of syrup or 1 tablet) once a day.

In adults and children with severe hepatic impairment the initial dose should be: if body weight 30 kg or less – 5 mg (1 teaspoon (5 ml) of syrup) once a day, if body weight over 30 kg – 10 mg (2 teaspoons (10 ml) of syrup or 1 tablet) once a day.

Interaction

Claritin does not increase the effect of ethanol (alcohol) on the CNS.

When co-administering Claritin with ketoconazole, erythromycin or cimetidine, increased concentrations of loratadine and its metabolite in plasma were noted, but this increase was not manifested clinically, including by ECG data.

Special Instructions

Claritin® has no clinically significant sedative effects when used in the recommended doses (10 mg once daily). The sedative profile of loratadine at 10 mg once daily is comparable to placebo. A dose-dependent increase in somnolence was observed at doses 2 to 4 times higher than the recommended dose of 10 mg.Claritin® does not potentiate the effects of alcohol.

The intake of Claritin® should be discontinued 48 hours before skin diagnostic allergy testing to prevent false results. In patients with severe hepatic impairment, a lower starting dose should be prescribed due to possible decreased clearance of loratadine (recommended starting dose is 5 mg once daily or 10 mg every other day).

When using Claritin® for 90 days at a dose 4 times therapeutic, no clinically significant prolongation of the QT interval on the electrocardiogram was determined.Claritin® contains lactose. Therefore, it should not be administered to patients with rare hereditary diseases associated with galactose intolerance, lapland lactase deficiency or impaired glucose-galactose absorption.

In the recommended doses, Claritin® does not affect the ability to operate motor vehicles or complex technical devices. However, patients should be advised of the potential risk of drowsiness if they overdose on the drug.

Synopsis

Contraindications

– Intolerance or hypersensitivity to loratadine or any other component of the drug.

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

– The period of breastfeeding.

– Patients with rare hereditary diseases (galactose intolerance disorders, Lapp lactase deficiency or glucose-galactose malabsorption).

With caution

– Severe liver function disorders.

– Pregnancy

Side effects

In clinical studies with the participation of children aged from 2 to 12 years who took Claritin® more frequently than in the placebo group were observed headache (2.7%), nervousness (2.3%), fatigability (1%).

Nervous system disorders: in children aged 2 to 12 years, headache (2.7%), nervousness (2.3%), fatigue (1%); in adults, headache (0.6%), drowsiness (1.2%), insomnia (0.1%).

Digestive system disorders: in adults – increased appetite (0.5%).

In the post-marketing period

Nervous system disorders: very rare (< 1/10,000) – dizziness, fatigue.

Digestive system disorders: very rare (< 1/10 000) – dry mouth, gastrointestinal disorders (nausea, gastritis), liver dysfunction.

Allergic reactions: very rare (< 1/10 000) – rash, anaphylaxis.

Cardiovascular system disorders: very rare (< 1/10 000) – palpitation, tachycardia.

Skin disorders: very rare (< 1/10 000) – alopecia.

Overdose

Symptoms:drowsiness, tachycardia, headache.

Treatment:Gastric lavage, administration of adsorbents (crushed activated charcoal with water), symptomatic and supportive therapy. Loratadine is not excreted by hemodialysis. After acute care, the patient’s condition should continue to be monitored.

Pregnancy use

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

The use of Claritin® during pregnancy is possible only if the expected benefits to the mother exceed the potential risk to the fetus.

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

Similarities