Pharmacotherapeutic group:
Antiallergic agent – H1-histamine receptor blocker.
ATC code: R06AX13
Pharmacodynamics.
The active substance of the drug – loratadine belongs to the group of competitive histamine antagonists, selectively blocks peripheral H1-histamine receptors. Loratadine affects histamine-dependent stage of allergic reactions, also reduces migration of eosinophils, limits release of inflammatory mediators at cellular stage of allergic reaction.
It prevents the development and facilitates the course of allergic reactions, has antiexudative, antipruritic action, practically has no anticholinergic and antiserotonin action. It does not penetrate through the blood-brain barrier, does not affect the central nervous system and is not addictive. Antiallergic effect develops after 30 minutes and lasts for 24 hours.
Pharmacokinetics.
Quickly and completely absorbed in the gastrointestinal tract. Time to reach maximum concentration is 1.3-2.5 h; eating slows it down by 1 h. Maximum concentration in the elderly increases by 50%, with alcoholic liver damage in accordance with increasing severity of the disease.
The binding to plasma proteins is 97%. Metabolized in the liver with the formation of the active metabolite descarboxyloratadine with the participation of cytochrome P450 isoenzymes CYP3A4 and to a lesser extent CYP2D6. Equilibrium plasma concentrations of loratadine and metabolite are reached on day 5 of administration. It does not penetrate through the blood-brain barrier.
The elimination half-life of loratadine is 3-20 h (mean 8.4), the active metabolite is 8.8-92 h (mean 28 h); in elderly patients 6.7-37 h (mean 18.2 h) and 11-38 h (17.5 h) respectively. In alcoholic liver damage the half-life increases with increasing severity of the disease.
Extracted by the kidneys and with bile. In patients with chronic renal insufficiency and during hemodialysis the pharmacokinetics is practically unchanged.
Indications
Dermatitis, Edema, Insect bites, Quincke’s edema, Runny nose (rhinitis), Eczema, Dermatosis, Increased tear production, Allergic rhinitis, Allergic conjunctivitis, Pollinosis, Urticaria, Allergy, Diathesis, Skin itching, Sneezing Allergic rhinitis (seasonal and year-round), allergic conjunctivitis, pollinosis, urticaria (including chronic ideopathic).chronic ideopathic), angioedema (Quincke’s edema), itchy allergic dermatosis, pseudoallergic reactions caused by histamine release, allergic reactions to insect bites.
Active ingredient
Loratadine
Composition
Active ingredient:
loratadine – 10 mg.
Excipients:
potato starch,
milk sugar (lactose),
talc,
magnesium stearate.
How to take, the dosage
Orally, regardless of meals, with a small amount of water. Adults and children over 12 years of age – 1 tablet (10 mg) 1 time per day. Children from 2 to 12 years of age with body weight less than 30 kg – 1/2 tablet (5 mg) once a day. If body weight is more than 30 kg – 1 tablet (10 mg) 1 time per day.
Interaction
Ethanol reduces the effectiveness of loratadine.
Erythromycin, cimetidine, ketoconazole, when combined with loratadine increase the concentration of loratadine in blood plasma, without causing clinical manifestations and without affecting the ECG.
Inducers of microsomal oxidation (phenytoin, barbiturates, zixorin, rifampicin, phenylbutazone, tricyclic antidepressants) reduce the effectiveness of loratadine.
Special Instructions
During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities that require increased concentration and quick psychomotor reactions.
Contraindications
Hypersensitivity to the drug. Pregnancy, lactation. Childhood under 2 years of age. With caution. Liver failure.
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Side effects
Adverse events listed below, when using loratadine occurred with a frequency of > 2% and approximately with the same frequency as when using placebo (“pacifier”).
In adults: headache, fatigue, dry mouth, drowsiness, gastrointestinal disorders (nausea, gastritis), as well as allergic reactions in the form of a rash. In addition, there have been rare reports of anaphylaxis, alopecia, liver dysfunction, palpitations, tachycardia.
In children rarely: headache, nervousness, sedative effect.
Overdose
Symptoms: drowsiness, tachycardia, headache. In case of overdose seek medical attention.
Treatment: induction of vomiting, gastric lavage, intake of activated charcoal.
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Pregnancy use
The use of the drug Clarisens during pregnancy is possible only if the expected benefits to the mother exceed the potential risk to the fetus.
Clarisens is excreted with the breast milk, so if the drug is prescribed during lactation, it is necessary to consider stopping breastfeeding.
Similarities
Claritin, Lomilan, Clarisense, Loragesal, Loratadine, Loratadine Teva, Loratavel
Weight | 0.018 kg |
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Shelf life | 2 years |
Conditions of storage | In a dry, light-protected place at a temperature not exceeding 25 °C |
Manufacturer | Pharmstandard-Leksredstva, Russia |
Medication form | pills |
Brand | Pharmstandard-Leksredstva |
Other forms…
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