Claritin, tablets 10 mg 10 pcs

Antiallergic 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.

With long-term treatment there were 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. Food intake increases the time to reach the maximum concentration (Tmax) of loratadine and desloratadine by about 1 hour, but has no effect on the effectiveness of the drug. 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.

The elimination 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 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 (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
insufficiency.

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:

active ingredient: loratadine 10 mg;

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

How to take, the dosage

Administer regardless of the time of meals.

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

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

Interaction

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

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

Special Instructions

Do not use after the expiration date printed on the package.

Synopsis

Contraindications

Hypersensitivity to the components of the drug, age under 2 years (for syrup), under 3 years or body weight less than 30 kg (for tablets); period of breastfeeding; rare hereditary diseases (galactose intolerance, lactase deficiency) for tablets; glucose-galactose malabsorption; sugar/isomaltase deficiency, fructose intolerance for syrup.

With caution: severe liver function disorders.

Side effects

Digestive system disorders: in adults – nausea, gastritis; rarely – liver dysfunction.

CNS disorders: in adults there were headache, fatigue, dry mouth, drowsiness. In children: headache, nervousness, sedative effect were rarely observed. As in adults, the frequency of these phenomena in children was at the same level as in placebo.

Allergic reactions: in adults – skin rash; rarely – anaphylaxis. Cardiovascular system: in adults rarely – palpitations, tachycardia. Other: in adults rarely – alopecia.

Overdose

The data are not described.

Pregnancy use

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

Because the active ingredients of the drug are excreted with the breast milk, so if the drug is prescribed during lactation, the question of stopping breast-feeding should be considered.

Similarities