Alerzin

A rapidly developing economy, household chemicals, which, out of good intentions, should facilitate the work of a woman, and as an adverse event - it is difficult enough today to find a person who does not suffer at least one manifestation of an allergic reaction. Every year, the ranks and those who are subject to "seasonal allergies", that is, the body's response to a particular stimulus, which is tied up with changes in the seasons, for example, an allergy to pollen of flowering plants, a reaction to the cold and others, are replenished with each year. Antihistamines for systemic use, acting on the respiratory system, Alerzin, manufactured by the pharmaceutical factory Egis (Hungary) - is a worthy solution to the problem.

Indications of the alerzin

Pharmacological drug was developed by the manufacturer as an antihistamine drug of systemic action, hence the indications for use are Alersin:

1. Symptomatic treatment of manifested signs of idiopathic urticaria, which passed into the stage of a chronic disease.
2. Rhinitis is an allergic nature of seasonal manifestation (pollinosis).

All-year-round allergic rhinitis.

Release form

The composition of the drug is based on the main active substance of levocetirizine hydrochloride, the quantitative index of which is 5 mg in one unit of the drug, levocetirizine, if the 4.21 mg is found on a dry 100% chemical compound. There is also a number of additional chemical compounds, including lactose monohydrate.

On the pharmacological market, the form of release Alerzin is represented by several varieties:

1. Tablets, protected from above with a special soluble coating. Seven units of the medicinal product are present on the packaging plate. On the drugstore shelves, you can find cardboard packaging boxes, represented by one or two plates with medicine.
2. Issue and solution in drops (colorless liquid without sediment), which is poured into bottles of darkened glass with a volume of 20 ml. The bottle is packed in a classic cardboard package. Drops that have a sweetish taste are taken orally, the liquid has a slightly perceptible musky odor. 

Pharmacodynamics

The drug under consideration belongs to the category of selective drugs capable of inhibiting the H1-histamine receptors and being a competitive histamine antagonist. The main active substance of the drug is levocetirizine - it is a stable R-enantiomer, an isomeric variant of cetirizine, equipped with a levorotatory movement. Pharmacodynamics Alerzin, and in particular levocetirizine, is similar to the characteristics of peripheral H1-receptors. Alerzin effectively affects vascular permeability, a histamine-dependent possibility of developing allergic manifestations, reduces the movement of eosinophils, depresses and limits the proliferation of mediators of the inflammatory process. The introduction of levocetirizine can prevent the onset or facilitate the occurrence of allergic manifestations.

Alerzine shows high anti-inflammatory, antiexudative characteristics, it perfectly removes irritation and itching. At the same time, there is no significant effect on the decrease in brain cells ability to transmit nerve signals (anticholinergic parameter) and blockade of 5-HT M2 (S M2) receptors (antiserotonin indicator).

When the necessary therapeutic doses are reached, Alerzin does not show a tendency to sedative influence on the patient's body. After taking, the effect of the medication begins to manifest itself in the interval from a quarter to an hour and lasts for two days. Time parameters depend on the individual characteristics of the patient's body.

Pharmacokinetics

The basic chemical compound of the drug in question, levocetirizine, is a derivative of cetirizine, so the pharmacokinetics of Alerzine is linear and virtually indistinguishable from that of cetirizine.

The active substance of levocetirizine is well absorbed by the mucosa of the gastrointestinal tract and after fifty minutes it can be observed in the serum of its maximum concentration: with a single admission this parameter (Cmax) is 270 ng / ml, the second administration already gives the figure 308 ng / ml (at dosage 5 mg Alerzin). The level of absorption of the drug does not depend on the administered dosage and does not change its indices from the time and amount of food taken. These parameters only affect the time to reach the peak amount of the active component in the plasma. The drug shows 100% bioavailability.

Part of the medication (about 14%) is metabolized by the body. This process is represented by such reactions as oxygen dealkylation, nitrogen dealkylation, oxidation, a compound with taurine. Oxidation occurs in the presence of CYP isophores, whereas dealkylation occurs with the direct participation of cytochrome CYP 3A4.

The active substance shows a high level of connection with blood proteins, the rate of which reaches 90%. To date, there is no objective information about the ability to diffuse the active substance through the blood-brain barrier. There is no data on the distribution of the drug in the tissues of various organs, there was an insignificant concentration of levocetirizine in the cells of the central nervous system, the maximum is in the kidneys and liver. The distribution volumetric criterion is 0.4 liters per kilogram of patient weight.

Most of the drug and its metabolites are utilized and excreted mainly through active tubular secretion and glomerular filtration. Excretion from the body occurs with urine through the urinary tract (about 85.4%), but a small amount with a caloric mass.
The half-life of T1 / 2, depending on the individual characteristics of the body and the state of its health, ranges from six to nine hours. The same indicator in young patients is lower, but official data so far does not exist yet.

The total clearance in adult patients is characterized by a figure of 0.63 ml / min / kg. It should be noted that the clearance of levocetirizine is correlated with the corresponding parameter of creatinine. Based on this, if the patient has a history of pathological changes in kidney function, moderate or high severity, the interval between drug administration Alerzin should be adjusted according to this parameter (creatinine clearance readings). In the case of complete cessation of urinary excretion (anuria), the overall clearance of the patient's body is reduced by approximately 80%.

In the case of a hemodialysis procedure, which is a classic four hours, the amount of levocetirizine withdrawn during this period is less than 10%.
 

Dosing and administration

Depending on the intended form of admission, the way of application and the dose of the drug being administered is somewhat different. Both forms are taken by the patient orally with the required amount of liquid. The solution, before use, is measured by a dispenser and introduced into a glass with a small volume of water, where it is mixed. So the medicine is easier and more effective to take. Diluted composition should be drunk immediately, without leaving for later - otherwise its effectiveness is reduced. If a tablet form is prescribed, the drug should be swallowed without chewing, together with the required volume of liquid.

For children over six years and adults, the daily dosage is prescribed as 5 mg of levocetirizine, which corresponds to one tablet in the shell, or to 20 drops of the solution. The drug is taken once a day.

Newborn carapaces age from six months to a year are assigned only a drop form of release, with a dosage of 1.25 mg, which corresponds to five drops that are injected into the body once a day. Breast cancer, who has not yet reached the age of six months, is not recommended for taking levocetirizine, as the data on the effect of the drug on this age group of patients is very limited.

Children of age from one to two years are recommended a dosage of 2.5 mg, which corresponds to ten drops that are injected into the body two times a day.

Children who are between two and six years of age, the recommended amount of injected drug - 2.5 mg, which is similar to ten drops, which are separated into two daily doses.

But, depending on the patient's condition, the treating doctor individually adjusts the duration of the course of therapy, the way of administration and dose of levocetirizine.

If the patient in parallel suffers and renal dysfunction, the dosage of Alerzin is corrected. The manufacturer gives such recommendations in this regard:

• If during clinical trials of creatinine clearance the patient falls within the range of 30 to 49 ml / min, the recommended dose of the drug is 5 mg, which corresponds to one tablet or 20 drops of the solution. The interval of administration between doses should be maintained at 48 hours (two days).
• If the result of the tests shows a clearance of creatinine below 30 ml / min, then the recommended dose of the drug is 5 mg, which corresponds to one tablet or 20 drops of the solution. The interval of administration between receptions should be maintained at 72 hours (three days).

If the patient refers to people of retirement age, but the analysis does not show any deviations in the work of the kidneys, there is no need to adjust the dosage of Alerzin. Otherwise, the amount of the drug is prescribed depending on the creatinine clearance, according to the recommendations given above.

If the patient has a history of only liver failure, adjust the dose of the drug should not be.

For children with kidney failure, the amount of medication is selected individually, taking into account its weight and the level of creatinine clearance.

Duration of admission directly depends on the symptomatology. In the case of a chronic form of allergic rhinitis, Alerzin may continue for a year.
 

Use of the alerzin during pregnancy

Due to the fact that to date there is no data on the capabilities of the active substance of the drug in question, levocetirizine, to penetrate the blood-brain barrier, the use of Alerzin during pregnancy is not recommended. There are no reliable facts of the safety of levocetirizine for the normal development of the embryo.

If there was a need for allergic therapy at a time when a young mother is feeding her newborn baby with a breast, for the period of treatment breastfeeding should be interrupted, having previously consulted the treating doctor. 

Contraindications

Any remedy used in therapeutic treatment, locally or systemically, has a certain effect on the patient's body. Accordingly, possible and contraindications to the use of Alerzin. These are:

• Increased individual sensitivity to levocetirizine or other components of the drug, as well as multiple derivatives of piperazine.
• Due to the fact that the lactose monohydrate enters the surface of the medicinal product, the tablet form is not recommended for admission to patients with a history of malabsorption of glucose-galactose, galactosemia or lactose deficiency.
• Do not attribute Alerzin in the form of tablets, if the patient has not been used for two years, because of the imperfection of his physiological development.
• Contraindication to the use of Alerzin can be considered pregnancy and lactation.
• If the clearance of creatinine is below 10ml / min and the patient has a pronounced severe kidney dysfunction.
• Patients of advanced age. Age changes can trigger a decrease in glomerular filtration, and levocetirizine is prone to retention of urine.
• Persons with a disruption in the work of the kidneys should carefully take the drug, adjusting the dosage and the interval of admission.
• Be cautious when prescribing levocetirizine if the patient is involved with work in road transport or with moving machinery requiring special attention and showing a potential hazard.
• The state of the patient's body, in which there is a probability of urinary retention. For example, a trauma that affected the spinal cord or prostatic hyperplasia, etc.
• Propensity of the body to allergic reactions.
   

Side effects of the alerzin

Preferably, preparations based on levocetirizine are well tolerated by the patient's body, but under certain circumstances, negative symptoms may manifest. At admission in some cases it is possible to observe such side effects of Alerzin:

• Gastrointestinal tract and other digestive organs are able to react:

• A thirst caused by the dryness of the oral mucosa.
• Diarrhea and constipation.
• Cramping pain in the stomach - a response to the irritation of the mucosa of the digestive tract.
• Hepatitis.
• Nausea, with a particularly strong intensity leading to vomiting.
• Violation of urination, urinary retention.
• Failure in the production of hepatic enzymes.

• Reaction of the central nervous system:

• Insomnia or, conversely, drowsiness.
• Taste disorders.
• Fainting.
• Appearance of shortness of breath.
• Dizziness.
• An easy psychopathological disorder (asthenia).
• Increased fatigue.
• Disturbance of skin sensitivity (paresthesia).
• Tremor and convulsions.
• Feeling of euphoria and hallucinations.
• Emotional instability, suicidal thoughts.
• Pain symptomatology in the head.

• Manifestations of allergy:

• Irritation of skin.
• Hives.
• Anaphylaxis.
• Hyperemia.
• Itching.
• Skin rashes.
• Puffiness, in especially severe cases, up to the swelling of Quincke.

• The reaction of the cardiovascular system is expressed by the appearance of rapid heart rate.
• The visual body can respond with a violation in the clarity and clarity of the perception of the picture.
• Manifestations of a different nature:

• Myalgia is a pain in muscles of various intensity and different nature.
• Body weight gain.
• Increased appetite.

When one or more of the above symptoms appear, you must stop taking Alerzin. This may be enough for the pathological manifestations to pass by themselves. But it will not be superfluous to seek advice from the treating doctor, informing him of the negative effects on the part of the body.

 

Overdose

If the patient, in the process of treatment, sufficiently responsibly applies to the recommended instructions and dosages of the drug, then it is not to be afraid to get an excess of Alerzin dosage. If the instructions were violated, and the drug overdose did occur, the patient's body can respond to this fact by changing the mood and body condition: drowsiness is observed, which is sharply replaced by increased excitability, and vice versa.

A single-valued antidote that would block the effects of levocetirizine, to date, does not exist. Therefore, when this symptom appears, you should seek the advice of a specialist. He will conduct the examination, adjust the dosage and appoint, if necessary, a symptomatic or body-supporting treatment. If after taking a large dosage of levocetirizine, no more than two hours have elapsed, it is not superfluous to induce vomiting or rinse the stomach. Hemodialysis in this situation is not effective.

Interactions with other drugs

Any complex treatment is an opportunity to increase the effectiveness of treatment, but also the probability to lead to the opposite, not expected, result. Therefore, the correct tandem selection of drugs is the duty of any medical person on whom health depends, and sometimes the life of his patient. The right choice is the level of qualifications and experience of the doctor. When entering into the protocol of treatment of any medicinal product, it is necessary to know their mutual influence in case of joint application. Consider the interaction of Alerzin with other drugs, which is due to the pharmacodynamic characteristics of levocetirizine.

The pairs of Alerzin in combination with pseudoephedrine, cimetidine, diazepam, azithromycin, glipizide, ketoconazole or erythromycin work well and complement each other well.

With caution should be introduced Alerzine in conjunction with sedatives, because it is not clear to the end of their mutual influence and the total impact on the patient's body. In the case of using Alersin in conjunction with drugs that depress the central nervous system receptors, levocetirizine somewhat strengthens their characteristics.

With a tandem injection of levocetirizine and theophylline taken at a daily dosage of 0.4 g, a slight decrease in the clearance of levocetirizine is observed, approximately 16%.

It is inadmissible to use the drug and ethyl alcohol together.

Time and volumes of food intake do not have such a significant effect on the therapeutic characteristics of the drug. But nevertheless, do not take levocetirizine together with food. In this case, there is a slight decrease in the absorption activity of the drug of the gastrointestinal mucosa.

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Storage conditions

How well the storage conditions of Alerzin are properly maintained depends on the effectiveness of the medicinal product used. This drug should be stored in a room that has a temperature regime that does not exceed 25 degrees Celsius. The storage location must be dry and not accessible to light, especially direct sunlight. The place should be limited to the access of young children. 

Shelf life

If all the storage conditions of the medicinal product are maintained, the shelf-life of the drug in question is two years. If the drug is presented in the form of a drop, then after opening the vial, its necessary therapeutic efficacy is maintained for the next four weeks. After that, the drops of Alerzin should not be used. The final shelf-life of the medicinal product must be indicated on the package.