Pharmacotherapeutic group: anti-allergic agent – H1-histamine receptor blocker
ATC code: R06AX13
Pharmacological properties
Pharmacodynamics
H1-histamine receptor blocker (long action). Inhibits the release of histamine and leukotriene C4 from mast cells. Prevents the development and facilitates the course of allergic reactions. It has anti-allergic, antipruritic, antiexudative action. Reduces capillary permeability, prevents the development of tissue edema, relieves spasms of smooth muscles. Anti-allergic effect develops in 30 minutes, reaches its maximum in 8-12 hours and lasts for 24 hours. It does not affect central nervous system (as it does not penetrate through the blood-brain barrier) and is not addictive.
Pharmacokinetics
Fast and fully absorbed in the gastrointestinal tract. Time of reaching maximum concentration in blood plasma after drug intake is 1.3-2.5 hours; it is delayed by 1 hour with food intake. Maximum drug concentration in blood plasma is increased by 50% in elderly people, with alcoholic liver damage – with increase of disease severity. Binding with plasma proteins is 97%. It is metabolized in the liver with the formation of the active metabolite dekarboethoxyloratadine with the participation of cytochrome isoenzymes CYP3A4 and, to a lesser extent, CYP2D6. Equilibrium concentrations of loratadine and metabolite in plasma are reached by 5 days of administration. It does not penetrate the blood-brain barrier. Half-life of loratadine is 3-20 hours (on the average 8.4 hours), active metabolite – 8.8-92 hours (on the average 28 hours); for elderly patients – 6.7-37 hours (on the average 18.2 hours) and 11-38 hours (17.5 hours), respectively. In alcoholic liver damage the half-life increases in proportion to the severity of the disease.
Excreted by the kidneys and with bile. In patients with chronic renal failure and during hemodialysis pharmacokinetics practically does not change.
Indications
Allergies, Allergic conjunctivitis, Sneezing, Dermatitis, Dermatosis, Urticaria, Allergic rhinitis, Runny nose (rhinitis), Conjunctivitis, Skin itching, Edema, Increased tear production, Pollinosis, Insect bites, DiathesisAllergic rhinitis (seasonal and year-round), conjunctivitis, pollinosis, urticaria (incl. chronic idiopathic).Chronic idiopathic), angioneurotic edema, pruritic dermatoses; pseudo-allergic reactions caused by histamine release; allergic reactions to insect bites.
Active ingredient
Loratadine
Composition
One tablet contains:
active ingredient: loratadine 100% – 10 mg;
excipients: lactose monohydrate 110 mg, microcrystalline cellulose 75 mg, calcium stearate 2 mg, sodium carboxymethyl starch 3 mg.
How to take, the dosage
Orally. Adults and children with body mass over 30 kg – 10 mg once a day.
For patients with renal insufficiency or with liver dysfunction the initial dose should be 10 mg once a day.
Interaction
Erythromycin, cimetidine and ketoconazole when combined with loratadine increase the plasma concentration of loratadine without causing clinical manifestations and without affecting the electrocardiography data.
Inducers of microsomal oxidation (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) reduce the effectiveness of loratadine.
Loratadine does not increase the effect of alcohol on the central nervous system.
Special Instructions
During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities that require high concentration and rapid psychomotor reactions.
Synopsis
Tablets are white or almost white, flat-cylindrical, beveled.
Contraindications
Hypersensitivity, lactation, children with body weight less than 30 kg, lactose intolerance, lactase deficiency or glucose-galactose malabsorption.
With caution
Hepatic failure, pregnancy.
Side effects
In adults: headache, fatigue, dry mouth, drowsiness, nausea, gastritis, allergic reactions (rash), anaphylaxis, alopecia, liver dysfunction, tachycardia.
In children: headache, increased nervous excitability, sedation.
Overdose
Symptoms: drowsiness, tachycardia, headache.
Treatment: gastric lavage, taking activated charcoal. Not excreted by hemodialysis.
Pregnancy use
Use during pregnancy is possible only in cases when the estimated benefit to the mother exceeds the potential risk to the fetus. Breastfeeding should be stopped during the treatment (penetrates into the breast milk).
Similarities
Claritin, Lomilan, Clarisens, Loragesal, Loratadine, Loratadine Teva, Loratavel
Weight | 0.015 kg |
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Shelf life | 5 years. Do not use after the expiration date. |
Conditions of storage | In a dry place at a temperature not exceeding 25 oC. Keep out of reach of children. |
Manufacturer | Akrihin HFC JSC, Russia |
Medication form | pills |
Brand | Akrihin HFC JSC |
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