Alerzin

A rapidly developing economy, household chemicals, which with good intentions were supposed to make women's work easier, and as a side effect - today it is quite difficult to find a person who does not suffer from at least one manifestation of an allergic reaction. Every year the ranks of those who are subject to "seasonal allergies" are replenished, that is, the body's reaction to a specific irritant, which is tied to changes in the seasons, for example, an allergy to pollen of flowering plants, a reaction to cold and others. Antihistamines for systemic use, acting on the respiratory system, Alerzin, produced by the pharmaceutical plant Egis (Hungary) - this is a worthy solution to the problem that has arisen.

Indications Alerzina

The pharmacological drug was developed by the manufacturer as a systemic antihistamine, hence the indications for the use of Alerzin:

1. Symptomatic treatment of emerging signs of idiopathic urticaria that has progressed to the stage of chronic disease.
2. Allergic rhinitis of seasonal nature (hay fever).

Year-round allergic rhinitis.

Release form

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

On the pharmacological market, the release form of Alerzin is presented in several varieties:

1. Tablets protected on top by a special soluble coating. There are seven units of the drug on the packaging plate. On pharmacy shelves you can find cardboard packaging boxes, presented by one or two plates with the drug.
2. A solution in drops (colourless liquid without sediment) is also produced, which is poured into 20 ml dark glass bottles. The bottle is packed in a classic cardboard package. The drops, which have a sweetish taste, are taken orally, the liquid has a slightly noticeable musky smell.

Pharmacodynamics

The drug in question belongs to the category of selective drugs capable of inhibiting H1-histamine receptors and being a competitive histamine antagonist. The main active substance of the drug is levocetirizine - a stable R-enantiomer, an isomeric variety of cetirizine, equipped with a left-handed rotation. The pharmacodynamics of Alerzin, and in particular levocetirizine, are similar to the characteristics of peripheral H1-receptors. Alerzin effectively affects vascular permeability, histamine-dependent possibility of developing allergic manifestations, reduces the movement of eosinophils, inhibits and limits the release of inflammatory mediators. The introduction of levocetirizine allows preventing the onset or facilitating the course of allergic manifestations.

Alerzin shows high anti-inflammatory, anti-exudative characteristics, perfectly relieves irritation and itching. At the same time, no significant effect on the reduction of the ability of brain cells to transmit nerve signals (anticholinergic parameter) and the blockade of 5-HT M2 (S M2) receptors (antiserotonin indicator) has been recorded.

When the required therapeutic doses are reached, Alerzin does not show a tendency to sedative effect on the patient's body. After taking, the effect of the drug begins to manifest itself in the interval from a quarter of an hour 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, therefore the pharmacokinetics of Alerzin is represented by a linear dependence and has practically no differences from those of cetirizine.

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

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

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

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

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 related to the corresponding parameter of creatinine. Based on this, if the patient's medical history includes pathological changes in the functioning of the kidneys, moderate or severe, the interval between the introduction of the drug Alerzin should be adjusted according to this parameter (indications of creatinine clearance). In the case of complete cessation of urine excretion by the kidneys (anuria), the total clearance of the patient's body decreases by approximately 80%.

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

Dosing and administration

Depending on the prescribed form of administration, the method of application and dose of the administered drug differ slightly. Both forms are taken orally by the patient with the required amount of liquid. The solution, before use, is measured out with a dispenser and introduced into a glass with a small amount of water, where it is mixed. This makes the drug easier and more effective to take. The diluted composition must be drunk immediately, without leaving it for later - otherwise its effectiveness is reduced. If a tablet form is prescribed, the medicinal unit must be swallowed without chewing, together with the required amount of liquid.

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

Newborns aged six months to one year are prescribed only the drop form of release, while the dosage is 1.25 mg, which corresponds to five drops that are administered to the body once a day. For infants who have not yet reached six months of age, taking levocetirizine is not recommended, since the data on the effects of the drug on this age category of patients are very limited.

For children aged one to two years, the recommended dosage is 2.5 mg, which corresponds to ten drops administered into the body twice a day.

For children aged two to six years, the recommended dose is 2.5 mg, which is equivalent to ten drops divided into two daily doses.

But, depending on the patient’s condition, the attending physician individually adjusts the duration of the course of therapy, the method of administration and the dosage of levocetirizine.

If the patient also suffers from renal dysfunction, the dosage of Alerzin is adjusted. The manufacturer gives the following recommendations on this matter:

• If, during clinical studies, the patient's creatinine clearance 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 solution. The interval between doses should be maintained at 48 hours (two days).
• If the test result shows creatinine clearance below 30 ml/min, the recommended dose of the drug is 5 mg, which corresponds to one tablet or 20 drops of solution. The interval between doses should be 72 hours (three days).

If the patient is of retirement age, but the analysis does not show any abnormalities in kidney function, 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 above.

If the patient has a history of liver failure only, there is no need to adjust the dose of the administered drug.

For children with impaired renal function, the amount of medication is selected individually, taking into account their weight and creatinine clearance level.

The duration of treatment directly depends on the symptoms that appear. In the case of chronic allergic rhinitis, Alerzin treatment can continue for a year.

Use Alerzina during pregnancy

Due to the fact that there is currently no data on the ability 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 also no reliable facts about the safety of levocetirizine for normal embryo development.

If there is a need for allergy therapy during the period when a young mother is breastfeeding her newborn baby, breastfeeding must be interrupted for the duration of treatment, after first consulting with the attending physician.

Contraindications

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

• Increased individual sensitivity to levocetirizine or other components of the drug, as well as multiple piperazine derivatives.
• Due to the fact that the surface coating of the drug contains lactose monohydrate, the tablet form is not recommended for use by patients with a history of glucose-galactose malabsorption, galactosemia or lactose deficiency.
• Alerzin in tablet form is not prescribed if the patient has not used it for two years, due to the imperfection of his physiological development.
• Contraindications to the use of Alerzin include pregnancy and lactation.
• If creatinine clearance is below 10 ml/min and the patient has obvious severe renal dysfunction.
• Elderly patients. Age-related changes can cause a decrease in glomerular filtration, and levocetirizine tends to cause urinary retention.
• People with impaired renal function should take the drug very carefully, adjusting the dosage and interval of administration.
• Exercise caution when prescribing levocetirizine if the patient is involved in driving or operating moving machinery that requires special attention and is potentially dangerous.
• A condition of the patient's body that makes urinary retention likely. For example, an injury affecting the spinal cord or prostatic hyperplasia, etc.
• The body's tendency to allergic reactions.
  

Side effects Alerzina

Mostly, drugs based on levocetirizine are well tolerated by the patient's body, but under certain circumstances, negative symptoms may occur. When taking Alerzin, in some cases, the following side effects can be observed:

• The gastrointestinal tract and other digestive organs can react:

• Thirst caused by dryness of the oral mucosa.
• Diarrhea and constipation.
• Cramping pains in the stomach are a response to irritation of the mucous membrane of the digestive tract.
• Hepatitis.
• Nausea, which, if particularly intense, leads to vomiting.
• Urination disorders, urinary retention.
• A failure in the production of liver enzymes.

• Central nervous system reaction:

• Insomnia or, conversely, drowsiness.
• Taste disorders.
• Fainting.
• The appearance of shortness of breath.
• Dizziness.
• Mild psychopathological disorder (asthenia).
• Increased fatigue.
• Impaired skin sensitivity (paresthesia).
• Tremors and convulsions.
• Feeling of euphoria and hallucinations.
• Emotional instability, suicidal thoughts.
• Pain symptoms in the head area.

• Manifestations of allergy:

• Skin irritation.
• Hives.
• Anaphylaxis.
• Hyperemia.
• Itching.
• Skin rashes.
• Edema, in particularly severe cases, up to Quincke's edema.

• The reaction of the cardiovascular system is expressed by the appearance of increased heart rate.
• The visual organ may respond with a disturbance in the clarity and distinctness of image perception.
• Manifestations of a different nature:

• Myalgia is muscle pain of varying intensity and nature.
• Increase in body weight.
• Increased appetite.

If one or more of the above symptoms appear, you should stop taking Alerzin. This may be enough for the pathological manifestations to go away on their own. But it would not be a bad idea to consult your doctor, informing him of the negative effects on the body.

Overdose

If the patient, during the treatment, is sufficiently responsible in following the recommended instructions and dosages of the drug, then there is no need to be afraid of getting an excess of the dosage of Alerzin. If the instructions were violated, and an overdose of the drug still occurred, the patient's body is able to respond to this fact by changing the mood and state of the body: drowsiness is observed, which is sharply replaced by increased excitability, and vice versa.

There is currently no clear antidote that would block the effects of levocetirizine. Therefore, if these symptoms appear, you should consult a specialist. He will conduct an examination, adjust the dosage and, if necessary, prescribe symptomatic or supportive treatment. If no more than two hours have passed since the introduction of a large dose of levocetirizine, it would be a good idea to induce vomiting or wash out the stomach. Hemodialysis is not effective in this situation.

Interactions with other drugs

Any complex treatment is both an opportunity to increase the effectiveness of treatment, but also a probability of leading to the opposite, unexpected, result. Therefore, the correct tandem selection of drugs is the duty of any doctor, on whom the health, and sometimes the life of his patient depends. The right choice is the level of qualification and experience of the doctor. When introducing any drug into the treatment protocol, it is necessary to know their mutual influence in case of joint use. Let's consider the interaction of Alerzin with other drugs, which is due to the pharmadynamic characteristics of levocetirizine.

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

Alerzine should be administered with caution together with sedatives, since their mutual influence and total effect on the patient's body are not completely clear. In the case of using Alerzine together with drugs that depress the receptors of the central nervous system, levocetirizine somewhat enhances their characteristics.

With tandem administration of levocetirizine and theophylline, taken at a daily dose of 0.4 g, a slight decrease in levocetirizine clearance is observed, by approximately 16%.

The combined use of the drug in question and ethyl alcohol is unacceptable.

The time and volume of food intake do not have such a significant effect on the therapeutic characteristics of the drug. However, levocetirizine should not be taken with food. In this case, there is a slight decrease in the activity of absorption of the drug by the gastrointestinal mucosa.

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Storage conditions

The effectiveness of the drug used depends on how correctly the storage conditions of Alerzin are maintained. This drug should be stored in a room with a temperature regime not exceeding 25 degrees Celsius. The storage place should be dry and not accessible to light, especially direct sunlight. The place should be limited for access by small children.

Shelf life

If all storage conditions of the drug are met, the shelf life of the drug in question is two years. If the drug is presented in the form of drops, then after opening the bottle, its required therapeutic effectiveness is maintained for the next four weeks. After this, Alerzin drops should not be used. The final expiration date of the drug must be indicated on the packaging.