Loratadine

Continually blocks H1-histamine receptors . Suppresses the release of histamine and C4 leukotriene from mast cells . Prevents development and facilitates the course of allergic reactions . It has anti-allergic, antipruritic, anti-exudative action. Reduces capillary permeability, prevents the development of tissue edema , relieves smooth muscle spasms . The antiallergic effect develops after 30 minutes, reaches a maximum after 8-12 hours and lasts 24 hours. It does not affect the central nervous system and is not addictive (since it does not cross the blood-brain barrier ).

Drug interaction

CYP3A4 inhibitors (including ketoconazole , erythromycin ), CYP3A4 and CYP2D6 inhibitors ( cimetidine , etc.) increase the concentration of loratadine in the blood .

Pharmacokinetics

Quickly and completely absorbed in the gastrointestinal tract . TCmax - 1.3-2.5 hours; eating slows it down by 1 hour. Cmax in elderly people increases by 50%, with alcoholic liver damage - with an increase in the severity of the disease. Communication with plasma proteins - 97%. It is metabolized in the liver with the formation of the active metabolite of decarboethoxyloratadine with the participation of cytochrome CYP3A4 isoenzymes and to a lesser extent CYP2D6. Css of loratadine and a metabolite in plasma are achieved on the 5th day of administration. Does not cross the blood-brain barrier. T _1/2 loratadine - 3-20 hours (average 8.4), active metabolite - 8.8 - 92 hours (average 28 hours); in elderly patients, respectively - 6.7 - 37 hours (average 18.2 hours) and 11-38 hours (17.5 hours). With alcoholic liver damage, T _1/2 increases in proportion to the severity of the disease. It is excreted by the kidneys and with bile . In patients with chronic renal failure and during hemodialysis, the pharmacokinetics are practically unchanged.

Allergic rhinitis (seasonal and year-round), conjunctivitis , hay fever , urticaria (including chronic idiopathic), angioedema , pruritic dermatosis ; pseudo-allergic reactions caused by histamine release; allergic reactions to insect bites.

Contraindications

Hypersensitivity , lactation , children's age up to 2 years.

With caution

Hepatic failure , pregnancy .

special instructions

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Inside.

• Adults and children over 12 years of age: 10 mg (1 tablet) once a day. Daily dose of 10 mg.
• For children from 3 to 12 years old, 5 mg (1/2 tablet) once a day. The daily dose is 5 mg.
• Children weighing more than 30 kg - 10 mg of the drug 1 time per day. The daily dose is 10 mg.

As adverse reactions when taking the drug, the following phenomena may occur:

• anaphylactic shock ;
• skin rash;
• hair loss;
• Dizziness
• headache
• feeling of fatigue and fatigue;
• drowsiness
• cramps
• nervousness;
• increased heart rate;
• arrhythmia;
• nausea
• a feeling of dry mouth;
• inflammation of the gastric mucosa;
• impaired liver function.

Most side effects occur in rare cases (less than 1 in 10,000). Most often, when taking the drug, drowsiness (in adults) and headache (in children) are observed ^[3] .

Symptoms

Drowsiness, tachycardia , headache.

Treatment

Gastric lavage , intake of activated carbon .

Legislation

In the United States and the United Kingdom, loratadine is the only over-the-counter drug in the class of long-acting H1 histamine receptor blockers.

• Desloratadine

• Loratadine - MedlinePlus Drug Information, US National Library of Medicine, National Institutes of Health
• Claritin (loratadine) drug description - RxList (Internet Drug Index)
• Claritin - patient information leaflet
• DrugBank: Loratadine - Wishart DS et al., DrugBank: a comprehensive resource for in silico drug discovery and exploration . Nucleic Acids Res . 2006 1; 34