Composition, form of production and packaging
? Tablets are white or almost white in color, flat-cylindrical, with a bevel.
loratadine 10 mg
Excipients: lactose monohydrate - 110 mg, microcrystalline cellulose - 75 mg, calcium stearate - 2 mg, sodium carboxymethyl starch - 3 mg.
7 pcs. - packings of cellular contour (1) - packs cardboard.
7 pcs. - packings cellular planimetric (3) - packs cardboard.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
? Syrup in the form of a clear liquid from light yellow to yellow, with a faint fruity smell.
loratadine 100 mg
Auxiliary substances: sucrose 35 g, propylene glycol 20 g, benzoic acid 0.1 g, citric acid 0.3 g, ethanol (rectified ethyl alcohol) 1.58 g, tropeolin o-0.001 g color, orange flavor 0.08 g, purified water - up to 100 ml.
100 ml - bottles of dark glass (1) complete with a measuring spoon - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
The blocker of histamine H 1 -receptors is long-acting. It has antiallergic, antipruritic, antiexudative action. Prevents development and facilitates the course of allergic reactions.
Suppresses the release of histamine and leukotriene C4 from mast cells. Reduces the permeability of capillaries, prevents the development of edema of tissues, relieves spasms of smooth muscles.
Does not affect the central nervous system (because it does not penetrate the BBB) and is not addictive.
The antiallergic effect develops in 30 minutes, reaches a maximum after 8-12 hours and lasts for 24 hours.
Suction and distribution
Quickly and completely absorbed their digestive tract. The time to reach C max in blood plasma after taking the drug is 1.3-2.5 h; food intake slows the time to reach Cmax for 1 hour.
Binding to plasma proteins - 97%. C ss of loratadine and a metabolite in plasma are achieved by 5 days of administration. Does not penetrate the BBB.
Metabolism and excretion
Metabolized in the liver with the formation of an active metabolite descarbotoxyloratadine with the participation of isoenzymes CYP3A4 and to a lesser extent CYP2D6.
It is excreted by the kidneys and with bile. T 1/2 loratadine - 3-20 h (an average of 8.4 h), the active metabolite - 8.8-92 h (an average of 28 h).
Pharmacokinetics in specific patient groups
C max drug in the blood plasma in the elderly increases by 50%. T 1/2 loratadine and active metabolite in elderly patients, respectively - 6.7-37 hours (an average of 18.2 hours) and 11-38 hours (17.5 hours).
In alcoholic liver damage, C max and T 1/2 increase in proportion to the severity of the disease.
In patients with chronic renal failure and during hemodialysis, the pharmacokinetics practically does not change.
- seasonal and year-round rhinitis (including pollinosis);
- allergic conjunctivitis;
- urticaria (including chronic idiopathic);
- Quincke's edema;
- pseudoallergic reactions caused by the release of histamine;
- itching dermatoses;
- an allergic reaction to insect bites.
The drug is taken orally.
Adults and children weighing more than 30 kg are prescribed 10 mg (1 tablet or 2 measuring spoons of syrup) 1 time / day.
Children aged 2 to 12 years with a body weight of less than 30 kg prescribed 5 mg (1 measuring spoon syrup) 1 time / day.
With renal failure, the initial dose is 10 mg every other day.
With liver failure, the initial dose of the drug is 5 mg / day or 10 mg every other day.
Adverse events occurred approximately at the same frequency as with placebo.
In adults: headache, fatigue, dry mouth, drowsiness, nausea, gastritis, allergic reactions (rash), anaphylaxis, alopecia, dysfunction of the liver, tachycardia.
In children: headache, increased nervous excitability, sedation.
- lactation period;
- children weighing less than 30 kg (for tablets);
- Children under 2 years old (for syrup);
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (for tablets);
- Hypersensitivity to any of the components of the drug.
With caution should prescribe the drug for liver failure, pregnancy.
PREGNANCY AND LACTATION
The use of the drug in pregnancy is possible only in those cases when the intended use for the mother exceeds the potential risk to the fetus.
For the duration of treatment, breast-feeding should be stopped (excreted in breast milk).
APPLICATION FOR FUNCTIONS OF THE LIVER
With renal failure, the initial dose of the drug should be 10 mg every other day.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure.
APPLICATION FOR CHILDREN
Contraindicated in children with a body weight of more than 30 kg (tablets) and in childhood to 2 years (syrup).
Impact on the ability to drive vehicles and manage mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Symptoms: drowsiness, tachycardia, headache.
Treatment: gastric lavage, reception of activated charcoal. It is not excreted by hemodialysis.
Inhibitors of CYP3A4 (including erythromycin, ketoconazole) inhibitors CYP3A4 and CYP2D6 (cimetidine and others) when used together with loratadine increase the concentration of loratadine in blood plasma, without causing clinical manifestations and without affecting the ECG data.
Inducers of microsomal oxidation (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) reduce the effectiveness of loratadine.
Loratadine does not enhance the effect of ethanol on the central nervous system.
TERMS OF RELEASE FROM PHARMACY
The drug is approved for use as a means of OTC.
TERMS AND CONDITIONS OF STORAGE
The drug in the form of tablets should be stored in a dry place inaccessible to children at a temperature of no higher than 25 В° C. Shelf life - 5 years.
The drug in the form of syrup should be stored in a dry place inaccessible to children at a temperature of 12 В° to 15 В° C. Shelf life - 4 years.