Mode of action:
Aleron - antiallergic drug belonging to the group of antihistamines 3 generations. Aleron contains the active ingredient levocetirizine - R-enantiomer of cetirizine, which is an active derivative of hydroxyzine. Aleron has anti-inflammatory, antipruritic, anti-inflammatory and antiekssudativnoe action. In addition, the drug has a strong antihistaminic effect. The mechanism of action of the drug is related to its ability to block peripheral H1-histamine receptors and inhibit the release of histamine by stabilizing the membranes of fat cells. Levocetirizine possesses high selectivity for H1-histamine receptors, providing them pronounced blocking effect, the drug has no effect on M-cholinergic and serotonergic receptors, and the adrenergic receptors (which are similar in structure to the H1-histamine receptors). It should be noted that to achieve the therapeutic effect of levocetirizine need to use half as much as cetirizine, is explained by the fact that levocetirizine is able to form a more stable relationship with the receptors. Using the drug is also noted decreased excretion of pro-inflammatory cytokines and chemokines, and adhesion inhibition of chemotaxis of eosinophils, expression of adhesion molecules. Levocetirizine also helps to reduce the IgE-dependent release of histamine, leukotriene C4 and prostaglandin D2, besides the drug inhibits cutaneous trombotsitoaktiviruyuschih factor. As a result of these changes in the body helps to alleviate the current levocetirizine variety of allergic reactions (including allergic rhinitis), and for seasonal allergies can be used as a means of prevention to prevent the development of allergic reactions. Also noted the effectiveness of the drug in cold urticaria and bronchial asthma attacks. Unlike previous generations antiallergic drugs, levocetirizine has no inhibitory effect on the central nervous system. Levocetirizine has no toxic effects on the heart.
After oral administration of the drug is well absorbed from the gastro-intestinal tract, with the meal does not affect the extent of absorption of levocetirizine, but slightly reduces its speed. Bioavailability after oral administration of levocetirizine is 100%. The maximum plasma concentration observed after 0.9-1 hours after administration, levocetirizine for a high degree of association with plasma proteins (90%). The drug passes into breast milk. A small part of levocetirizine is metabolized in the liver by O-dealkylation to form the inactive metabolite. In the process of metabolism of levocetirizine is not involved cytochrome P450 system. The half-life of the drug is 7-10 hours, levocetirizine is completely eliminated from the body within 96 hours. Excretion of the drug is produced mainly by the kidneys (up to 86% of the dose). When hemodialysis is displayed about 10% of the formulation. In patients with renal impairment and creatinine clearance less than 40 ml / min reduced the excretion of the drug (in this case there is an increase of its plasma concentrations).
Indications for use:
The drug used for the treatment and prevention of acute and chronic allergic diseases, including:
- Allergic rhinitis and conjunctivitis (including seasonal and perennial);
- Hay fever;
- Urticaria (including drug is used to treat patients with chronic idiopathic urticaria);
- Angioneurotic edema (angioedema);
- Allergic dermatoses which are accompanied by itching, burning rash and in various areas of the skin and mucous membranes.
How to use:
The drug is used to treat adults and children over 6 years. The drug is taken orally, drinking plenty of water. The dose and duration of treatment determined by the attending physician for each patient individually.
Usually on 1 tablet 1 time a day.
Adult maximum dose is 10 mg (2 tablets) per day.
The duration of treatment depends on the nature of the disease, usually by brief contact with an allergen is recommended to take the drug for 7 days, with hay fever from 3 to 6 weeks. If necessary, treatment can be extended to 6 months.
Patients suffering from renal failure, dosage adjustment is necessary. Because creatinine clearance less than 50 ml / min is recommended to appoint one tablet of 1 every 48 hours, with creatinine clearance less than 30 ml / min - one tablet of 1 every 72 hours. Patients with impaired renal function and creatinine clearance less than 10 ml / min is not recommended to prescribe a drug Aleron.
In the appointment of the drug to patients with impaired liver function no dose.
The drug is usually well tolerated, but in a few cases were noted such side effects when using Levocetirizine:
- The part of the central nervous system: dizziness, headache, fatigue, insomnia, drowsiness;
- The part of the digestive system: nausea, vomiting, dry mouth, increased appetite, pain in the epigastric region, the change indicators of liver samples;
- Other: tachycardia, blurred vision, nosebleeds.
In patients with hypersensitivity to levocetirizine when using the drug noted the development of pruritus, rash, urticaria, anaphylaxis, angioedema, and dyspnea.
- Hypersensitivity to the drug and piperazine derivatives;
- Severe renal failure (creatinine clearance less than 10 ml / min);
- Galactose intolerance, impaired absorption of glucose and galactose;
- Children under 6 years of age (for a given dosage form);
- A drug prescribed with caution during pregnancy and lactation.
There are no data on the safety of the drug during pregnancy. The drug may be assigned by the attending physician, if the expected benefit to the mother is higher than the potential risk to the fetus.
Levocetirizine is excreted in breast milk, so if you need to use during lactation should decide on the temporary cessation of breastfeeding.
Interactions with other drugs:
Did not reveal any interaction, while the use of levocetirizine and drugs whose metabolism is associated with cytochrome P450 (ketoconazole, erythromycin, azithromycin, diazepam), however, theophylline for repeated use can somewhat reduce the clearance of levocetirizine.
Avoid concurrent use of the drug Aleron with sedatives.
With simultaneous use of levocetirizine does not enhance the effect of ethanol.
When you receive excessive doses of the drug in patients noted the development of drowsiness or overstimulation, which is replaced by sleepiness.
No specific antidote. In case of overdose shown gastric lavage, enterosorbent and symptomatic therapy.
Hemodialysis and peritoneal dialysis are not effective.
Film-coated tablets, 10 pieces in blister, 1 or 3 blisters in a carton.
The drug should be stored in a dry place away from direct sunlight at a temperature no higher than 25 degrees Celsius.
Shelf life - 2 years.
1 coated tablet contains:
Levocetirizine dihydrochloride - 5 mg;
Excipients including lactose monohydrate.