Loratadin-Acrihin, tablets 10 mg 10 pcs

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

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

Pharmacological effect

Pharmacotherapeutic group: antiallergic agent – H1-histamine receptor blocker
ATX code: R06AX13

Pharmacological properties

Pharmacodynamics
H1-histamine receptor blocker (long-acting). Suppresses the release of histamine and leukotriene C4 from mast cells. Prevents the development and facilitates the course of allergic reactions. It has antiallergic, antipruritic, antiexudative effects. Reduces capillary permeability, prevents the development of tissue edema, and relieves spasms of smooth muscles. The antiallergic effect develops after 30 minutes, reaches a maximum after 8-12 hours and lasts 24 hours. Does not affect the central nervous system (because it does not penetrate the blood-brain barrier) and is not addictive.

Pharmacokinetics
Quickly and completely absorbed from the gastrointestinal tract. The time to reach the maximum concentration in the blood plasma after taking the drug is 1.3-2.5 hours; food intake slows it down by 1 hour. The maximum concentration of the drug in the blood plasma in elderly people increases by 50%, with alcoholic liver damage – with increasing severity of the disease. Connection with plasma proteins – 97%. Metabolized in the liver to form the active metabolite descarboethoxyloratadine with the participation of cytochrome isoenzymes CYP3A4 and, to a lesser extent, CYP2D6. The equilibrium concentration of loratadine and metabolite in plasma is achieved on the 5th day of administration. Does not penetrate the blood-brain barrier. The half-life of loratadine is 3-20 hours (average 8.4), the active metabolite is 8.8-92 hours (average 28 hours); in the elderly
patients, respectively – 6.7-37 hours (average 18.2 hours) and 11-38 hours (17.5 hours). With alcoholic liver damage, the half-life increases in proportion to the severity of the disease.
Excreted by the kidneys and bile. In patients with chronic renal failure and during hemodialysis, the pharmacokinetics remain virtually unchanged.

Special instructions

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.

Active ingredient

Loratadine

Composition

One tablet contains:
active substance: loratadine in terms of 100% – 10 mg;
excipients: lactose monohydrate 110 mg, microcrystalline cellulose 75 mg, calcium stearate 2 mg, sodium carboxymethyl starch 3 mg.

Pregnancy

Use during pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. During treatment, you should stop breastfeeding (passes into breast milk).

Contraindications

Hypersensitivity, lactation period, children weighing less than 30 kg, lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

With caution
Liver failure, pregnancy.

Side Effects

In adults: headache, increased fatigue, dry mouth, drowsiness, nausea, gastritis, allergic reactions (rash), anaphylaxis, alopecia, liver dysfunction, tachycardia.
In children: headache, increased nervous excitability, sedation.

Interaction

Erythromycin, cimetidine and ketoconazole, when used together with loratadine, increase the concentration of loratadine in the blood plasma without causing clinical manifestations and without affecting electrocardiographic data.
Inducers of microsomal oxidation (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) reduce the effectiveness of loratadine.
Loratadine does not enhance the effects of alcohol on the central nervous system.

Overdose

Symptoms: drowsiness, tachycardia, headache.
Treatment: gastric lavage, taking activated carbon. Not excreted by hemodialysis.

Storage conditions

In a dry place, at a temperature not exceeding 25 oC. Keep out of the reach of children.

Shelf life

5 years. Do not use after expiration date.

Manufacturer

Akrikhin JSC, Russia