Among modern anti-allergenic drugs for children, Ksizal stands out for its safety and ease of use, the presence of minor side effects, as well as an acceptable price. The medicine prevents or stops the development of allergic reactions for a while. Ksizal is available in the form of tablets and drops. Its instructions are required reading.
- a disease that affects adults and children, and the latter suffer more often, the disease harms the child's body. Reactions can develop to different types of allergens: pollen, wool, dust, certain types of food, etc.
Antiallergenic drugs, including Xizal, are also called antihistamines, as they are able to suppress the action of histamine, a biological substance that is responsible for the body's resistance to foreign substances by releasing allergens.
Drugs that eliminate reactions of this type are usually divided into three generations:
- The first generation drugs appeared in the fall of 1935, they include Suprastin, etc., they had many side effects, but for that time they cured allergies well.
- The second generation (Klarotadin,) were already able to act for up to 24 hours without causing a strong sedative effect.
- The third generation of drugs is modern, and Ksizal belongs to it. The third generation drugs have shown themselves well when taken by children.
Tablets are white, oval, marked with the letter Y. The main substance is levocetirizine dihydrochloride - is also included in other drugs that suppress allergies, for example, Zyrtec. Its main action is to stop the course of allergies by reducing the vascular permeability in children. Additional substances: cellulose, lactose, colloidal silicon dioxide, magnesium. The shell of the Opadry Y1-7000 tablet consists of hypromellose (a type of cellulose), titanium dioxide and macrogol (food additives).
The drops are colorless; the main substance in them is also levocetirizine dihydrochloride. Excipients: sodium saccharinate, vinegar, propylene glycol (natural solvent), glycerol, methyl parahydroxybenzonate, propyl parahydroxybenzonate (safe food additives), water.
The drug in all forms of release performs three functions that fight against childhood allergies:
- Suspends the activity of cytokines (DNA molecules) and mediators (substances that transmit inflammation);
- Suspends the movement of leukocytes, which are highly sensitive to allergens;
- Reduces the permeability of blood vessels, which reduces the permeability of allergens through them.
Ksizal has the property of being completely absorbed by the stomach. Its maximum concentration in the body is achieved within half an hour, and a pronounced therapeutic effect lasts a day.
The elimination period for children is 4–6 hours. Part is excreted from the body mainly by the kidneys, and part through the gastrointestinal tract. The liver does not react to its appearance in the body, active compounds are not formed in it, which once again confirms its complete safety for the child.
Instructions and dosage
Ksizal is taken only as directed by a doctor; in pharmacies it is sold by prescription. The indications are as follows:
- - skin inflammation in children that occurs under the influence of allergens. As soon as the provoking substance penetrates the skin cells, a severe allergic reaction occurs. The same reaction occurs with insect bites. Xizal will help relieve swelling and redness on the skin.
- Rhinorrhea, a type of allergic rhinitis, profuse discharge of mucus from the nose.
- Itching against a background of various reactions, acute and chronic. As a rule, with urticaria, tests are prescribed, when the result of the allergic nature of this disease is obtained, they begin treatment.
- (inflammation of the mucous membrane of the eye) allergic or chronic. In these forms of the disease, the doctor in most cases prescribes drops.
- , sneezing, lacrimation.
- - the seasonal reaction of the child's body to flowering, which is exacerbated in the spring-summer season. At the peak of flowering of poplar, birch, hazel, other trees and plants, strong reactions are manifested. If the child cannot be taken out of the flowering zone, he is recommended to take drugs like Xizal to relieve symptoms.
- - enlargement of a part of the face (sometimes eyes and oral mucosa) or limbs as a result of an allergic reaction. And its cause in this case is a strong vascular permeability, which is reduced by Ksizal.
The instruction says that the tablets are taken on an empty stomach or with food as directed by a doctor. The tablets are not chewed, washed down with water. The dosage must be followed exactly. Drops are drunk from a teaspoon or diluted with a little water.
5 mg tablets are packed in blisters of 7 or 10 pieces and packed in cardboard boxes. Allowed for children only after 6 years of age: 1 tablet once a day.
Drops of 10 and 20 ml are produced in dark glass jars with a dropper, they are also packed in cardboard boxes. Drops are allowed for children from 2 years of age; 2–6 years: 5 drops, 2 times a day; over 6 years of age: 20 drops per day (possible in 1 dose).
Contraindications and side effects
The medicine has contraindications:
- Acceptance of drops and tablets by children up to 2 years of age;
- Children taking pills up to 6 years of age (due to insufficient experimental data);
- Signs of kidney failure
- Individual drug intolerance, usually in children with a high level of sensitivity to lactose.
Among the side effects, the main cause of which is the exceeded dosage, drowsiness, dizziness, can be observed. Less often, in cases where the instructions for taking the medication were violated, - convulsions, blurred vision, depression, vomiting, diarrhea. No side effects have been reported when taken with other medications.
For infants under one year old, the drug is completely contraindicated.
Analogs
On the drug market, you can find analogues of Ksizal. The buyer chooses what is best suited from the variety presented.
- with the active substance cetirizine in the composition reduces capillary permeability, prevents tissue edema, and eliminates skin reactions to allergens. It is often argued that Zyrtec or Ksizal is better. In terms of pharmacological properties, they are in the same row of the latest generation drugs and are equally effective. The medicine is available in the form of 10 mg tablets and 10 ml drops. Price RUB 185
- also contains cetirizine. Effective for the treatment of urticaria, especially in the elimination of Quincke's edema. Zodak is available in 10 mg tablets, in the form of a light yellow syrup (100 ml) and drops (20 ml). Price RUB 138
- Cetrin eliminates allergic reactions in the early stages, relieves muscle spasms. After cessation of treatment, the effect of the drug persists for three days, and Zyrtec has the same property. Available from pharmacies without a prescription. The price of tablets (10 mg) 165 rubles.
- Tablets 7 pcs., 5 mg - 357 rubles;
- Tablets 10 pcs., 5 mg - 453 rubles;
- Tablets 14 pcs., 5 mg - 580 rubles;
- Drops 10 ml - 396 rubles.
Also, the drugs that are suitable for children include Telfast, Klarotadin, Lomilan, etc. They are available in various forms (tablets, drops, solutions) and have different price offers.
All of these drugs can be taken by children aged 1–5 years. Up to a year, there are practically no drugs for the treatment of allergies, with the exception of ointments used under strict control.
Price
The drug Ksizal is presented in pharmacies in Russian cities, its prices are low, depending on what dosage is on sale and on the number of tablets or solution.
The drug "Ksizal" is available in two dosage forms: drops for oral administration and tablets.
The drops are a colorless liquid with a slight opalescence. The drug is available in 10 and 20 ml vials. Secondary packaging - cardboard box with manufacturer's marking.
Ksizal tablets are white and biconvex. The top of the dosage form is film-coated. Tablets are available in 7, 10, 14 and 20 pieces in one package.
The composition of the drug in tablet form:
- Levocetirizine dihydrochloride in an amount of 5 mg.
- Macrogol 400.
- Opadra Y-1-7000.
The composition of drops for oral administration (calculated per 1 ml of the drug):
- Levocetirizine dihydrochloride - 5 mg.
The following are used as auxiliary components:
- Sodium saccharinate.
- Glycerol 85%.
- Propylene glycol.
- Acetic acid.
- Methyl parahydroxybenzoate.
- Propyl parahydroxybenzoate.
- Sodium acetate.
- Purified water.
Pharmacological action of the drug "Ksizal", pharmacokinetics
"Ksizal" is a drug that exhibits antiallergic and antihistamine activity. Its action is based on a depressing effect on histamine receptors. Due to this, the active component of the drug reduces the permeability of the vascular walls, slows down the movement of eosinophils and inhibits the activity of inflammatory mediators and cytokines.
Levocetirizine, which is part of Ksizal, is, in its chemical structure, an enantiomer of cetirizine. However, being a new generation drug, levocytirizine has a greater affinity for histamine receptors. Levocetirizine has no effect on choline and serotonin receptors.
The drug is intended for internal use. Reaching the gastrointestinal tract, levocetirizine is absorbed into the blood. When the drug is taken with food, the level of its bioavailability and adsorption does not change.
The maximum concentration of levocetirizine in blood plasma is reached one hour after a single dose. The duration of the effect is 24 hours. T 1/2 (half-life) in an adult varies from 6 to 10 hours, in children this period is reduced.
Most of the drug is excreted through the kidneys (85%), the rest through the intestines along with feces. It should be noted that if the patient suffers from kidney disease, the half-life of the drug is lengthened. In patients on hemodialysis, no more than 10% of the active substance is excreted.
There is practically no sedation when taking Ksizal.
The main component of the drug levocetirizine tends to penetrate into breast milk.
The main indications of the drug "Ksizal"
The main indications of the drug "Ksizal" include:
- Allergic rhinitis of various origins (year-round, seasonal).
- Allergic conjunctivitis.
- Allergic reactions of any nature (itching, sneezing, watery eyes, redness of the eyes, nasal congestion).
- Pollinosis.
- Quincke's edema.
- Allergic dermatitis.
- Urticaria, including idiopathic.
Method of application of the drug "Ksizal", dosage regimen of the drug
The drug should be taken orally during meals or on an empty stomach. As for the tablet dosage form, in this case the tablet is taken in its entirety. It should not be chewed or rubbed. Drink with plenty of liquid, mostly water.
Drops for oral administration are well dosed with a dropper bottle. The dosage of the drug depends entirely on the age of the patient.
- For children aged 2 to 6 years, the drug "Ksizal" is prescribed at a dosage of 1.25 mg twice a day (10 drops). The daily dose should not exceed 2.5 mg.
- For adults and children over 6 years of age, the drug can be prescribed in tablet form (1 tablet 1 time per day) or in drip - 2.5 mg 2 times a day. The daily dose is no more than 5 mg (20 drops).
As already mentioned, levocetirizine is excreted mainly by the kidneys, therefore, when Ksizal is prescribed, a special dosage regimen will be required by elderly patients and patients with renal insufficiency. For them, the dosage of the drug must be adjusted depending on the creatinine value.
The course of treatment with the drug is selected individually. On average, it can be 2 to 6 weeks.
Contraindications to taking the drug "Ksizal"
The drug "Ksizal" is one of the most widely prescribed drug by therapists, however, it is worth remembering the contraindications:
- For the tablet form of release - children under 6 years of age.
- For drops - children under 2 years of age.
- Pregnancy, lactation period (due to lack of clinical data during these periods).
- Individual intolerance to the components of the drug.
- Galactosemia.
- Lactose intolerance.
- Renal failure (CC level is less than 10 ml / min).
- Carefully advanced age.
special instructions
- It is unacceptable to use "Ksizal" simultaneously with alcohol.
- Does not affect driving power-driven vehicles.
- When taking "Ksizal" it is necessary to refrain from activities that require concentration.
Side effects of the drug "Ksizal"
The main and frequently occurring side effects of the drug include:
- Drowsiness.
- Fast fatiguability.
- Frequent headaches.
- Dry mouth.
- Asthenic syndrome.
- Dyspeptic disorders (vomiting, nausea, diarrhea).
The following side effects are extremely rare:
- Visual impairment.
- Convulsions.
- Hallucinations.
- Allergic manifestations (urticaria, rash, itching).
- Tachycardia.
- Sleep disturbances.
- Liver dysfunction, jaundice.
- Muscle pain.
In 1% of all reported cases, there were such adverse reactions as:
- Anaphylactic shock.
- Angioedema.
If there is an overdose of the drug, it is necessary to wash the stomach and induce vomiting. After that, it is desirable to use enterosorbents and consume a large amount of liquid (you can use solutions to restore electrolyte balance, for example, "Regidron").
Drug interactions
- With the simultaneous administration of "Ksizal" with theophylline, the total clearance of levocetirizine decreases, however, the pharmacokinetics of theophylline does not change.
- With the simultaneous intake of "Ksizal" together with alcohol, depression of the central nervous system is observed. In 1% of cases, an increase in the effect of alcohol is possible.
- According to clinical data, when studying the drug interaction of cetirizine racemate with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam, no clinically significant undesirable interaction was revealed.
Analogs of the drug "Ksizal"
The drug "Ksizal" has several analogues in its chemical composition. The active ingredient in all drugs is levocetirizine. These include:
- "Levocetirizine - Teva".
- "Suprastinex".
- "Desal".
- "Glenzet".
All analogues have anti-allergic properties and are used for seasonal manifestations of allergies, dermatitis, hay fever, allergic rhinitis.
The cheapest substitute is Glenzet. Its cost can vary from 100 to 150 rubles. The most expensive are the original drugs "Ksizal" and "Suprastinex".
It should be noted that analogs, despite the similarity of pharmacological action, may differ significantly from the original. Therefore, the doctor should select the treatment and the drug.
Ksizal belongs to the blockers of histamine H1 receptors and is a member of the group of competitive histamine antagonists. The similarity with histamine H1 receptors in the active component of the drug, levocetirizine, is 2 times greater than that of cetririzine. Ksizal acts on the histamine-dependent stage of the allergic reaction and reduces the movement of eosinophils, decreasing vascular permeability and limiting the release of inflammatory mediators.
Dosage form
Ksizal is produced in 2 versions of dosage forms - tablet and drops for oral administration. The tablets contain 5mg of the active ingredient and are coated. Packaged in 7,10,14,20 units per package.
Drops for oral administration contain 5 ml of the active ingredient in 1 drop, available in dark glass vials with a dropper, the capacity of which is 10 and 20 ml.
Description and composition
The active substance of the pharmacological agent Ksizal is levocetrin dihydrochloride. Excipients of tablets are represented by the following components:
- MKTs - 30mg;
- magnesium stearate - 1mg;
- colloidal dioxide - 0.5 mg;
- lactose monohydrate - 63.5 mg.
The composition of the film coating of the tablet is represented by the following substances:
- titanium dioxide;
- macrogol400;
- hypromellose.
The drops contain the following auxiliary compounds:
- sodium acetate;
- acetic acid;
- propylene glycol;
- glycerol 85%;
- methyl parahydroxybenzoate;
- propyl parahydroxybenzoate;
- sodium saccharinate;
- purified water.
Pharmacological group
The medication belongs to pharmacological drugs with pronounced antiallergic and antihistamine effects. The effect on the body is expressed in the prevention of an allergic reaction, and with the development of an allergy, its course is facilitated. The drug is also characterized by antipruritic and antiexudative effects. The active component of the medication has the following effect:
- reduces the permeability of the vascular walls;
- inhibits eosinophils;
- slows down the activity of inflammatory mediators and cytokines.
Levocetirizine has virtually no effect on cholinergic and serotonin receptors. The sedative effect is almost not observed when using Ksizal.
Indications for use
Ksizal is used in the following situations:
- lacrimation;
- sneezing;
- hay fever;
- chronic;
- allergic rhinitis;
- seasonal;
- nasal congestion;
- rhinorrhea;
- inflammation of the nasal mucosa;
- inflammation of the mucous eyes;
- quincke's edema;
- dermatosis of allergic origin;
- chronic.
for adults
The medication should be prescribed exclusively by the attending specialist, if indicated. Unauthorized use is unacceptable, since there is a possibility of causing significant harm to the body.
for children
In childhood, Ksizal in tablet form is not used in relation to patients whose age has not reached 6 years. It is undesirable to use the drug in the form of drops for oral use in relation to children under 2 years of age.
During gestation, as well as breastfeeding, Xizal cannot be used, as there is no information regarding its harmlessness.
Contraindications
A drug with antiallergic effect has a number of absolute contraindications, in the presence of which its use in a patient is unacceptable. Such conditions that make it impossible to use Xizal include the following:
- excessive sensitivity to levocetirizine;
- renal failure;
- hypersensitivity to the auxiliary components of the drug.
Applications and doses
Specific dosages and the required frequency of administration are determined by the attending specialist. It is strongly not recommended to change any medical prescriptions and skip appointments.
for adults
Ksizal in the form of drops for oral administration in volume is recommended to dissolve 10 ml in pure water and take when using a teaspoon in a volume of up to 20 drops for 1 day.
Tableted Ksizal is required to be taken on an empty stomach or during a meal. It is required to swallow the tablets whole - it is forbidden to chew. It is required to drink the taken drug with a significant volume of water. The standard dose is 1 tablet 1r. / Day.
for children
Ksizal drops for children from 2 to 6 are prescribed in a dose of 5 drops 2 rubles / day. Children over 6 years old take drops according to the adult dosage regimen.
Pills are taken by children from 6 years old as well as by adults. Adult supervision is required when a child is taking pills.
for pregnant women and during lactation
There is no information on the effect on the body of a pregnant woman, as well as on the body of the fetus. It is possible to take Ksizal during gestation only after consulting a doctor and in case of urgent need. During lactation, it is required to suspend breastfeeding of the child, since the effect of the drug on the child's body has not been studied.
Side effects
The drug Ksizal, during use, is capable of provoking negative reactions from the body. The main negative effects from the use of a pharmacological agent are as follows:
- drowsiness;
- head pain;
- overdriedness of the oral mucosa;
- increased fatigue;
- soreness of the epigastric region;
- asthenic syndrome.
Such reactions of the body are rarely observed when taking Ksizal:
- bouts of nausea;
- convulsions;
- diarrhea;
- rashes;
- dyspnea;
- dyspnea;
- muscle pain;
- hepatitis;
- hallucinations;
- tachycardia.
Also, there were isolated cases of jumps in the patient's weight. Angioedema and anaphylactic edema were extremely rare.
Interaction with other medicinal products
During the course of treatment with the use of a pharmacological drug in combination with theophylline, there is a possibility of an increase in the half-life of the patient's main active substance, lefocetirizine, from the patient's body.
It is undesirable to consume alcohol-containing products in the course of drug treatment, as well as drugs that have a depressing effect on the functioning of the central nervous system, since there is a possibility of an uncontrolled increase in the intensity of their effect on the patient's body.
special instructions
During the use of the medication, it is advisable to refrain from driving vehicles and other mechanisms, as well as to abandon activities that require increased concentration of attention. This is due to the fact that a pharmacological agent is capable of affecting the quality, clarity and speed of psychomotor reactions.
Overdose
In case of an overdose with Ksizal, there is a high probability of developing a certain symptomatic picture, which differs depending on the age group of the patient. Drowsiness increases in adults. Patients in the pediatric age group may experience the following conditions:
- increased irritability;
- unreasonable concern;
- excessive excitability;
- drowsiness.
If an overdose is suspected, gastric lavage is required as a priority. In the future, supportive and symptomatic therapy is needed. There is no specific antidote to the active ingredient of the drug.
Storage conditions
Tableted Ksizal and in the form of drops must be stored in a place inaccessible to direct sunlight. The room temperature should not exceed 25 ̊С. The shelf life of Ksizal tablets is 3 years, and drops for oral administration are suitable for 2 years from the date of release. The opened bottle cannot be used after 3 months from opening.
Analogs
The drug has analogues that are characterized by similar medicinal effects. But, it is not recommended to replace the drug prescribed by the doctor with any analogue without prior consultation with a specialist.
The main active component of the drug is levocetirizine dihydrochloride. The medication is also produced in the form of drops and tablets. It is characterized by anti-allergic and antihistamine properties. In the form of drops, it is prohibited for children under 2 years old, In tablet form - for children under 6 years old. During gestation and breastfeeding, it is not recommended to use it without urgent need, since its effect during these periods has not been studied. valid for 3 years from the date of manufacture. Belongs to the category of non-prescription pharmacological agents.
Price
The cost of Ksizal is on average 456 rubles. Prices range from 260 to 794 rubles.
Ksizal: instructions for use and reviews
Latin name: Xyzal
ATX code: R06AE09
Active substance: Levocetirizine (Levocetirizine)
Manufacturer: YUSB PHARMA S.A. (Belgium), UCB Pharma, S.p.A. (Italy), FARCHIM, S.A. (Switzerland)
Description and photo update: 12.08.2019
Ksizal is an antiallergic agent, a blocker of histamine H 1 receptors.
Release form and composition
Dosage forms of Ksizal:
- Film-coated tablets: oval, almost white or white, with an embossed Y marking on one side (7 or 10 pcs. In blisters, in a cardboard box 1 or 2 blisters);
- Drops for oral administration: slightly opalescent colorless liquid (10 or 20 ml in dark glass vials with a dropper, 1 vial in a cardboard box).
The active ingredient is levocetirizine dihydrochloride:
- 1 tablet - 5 mg;
- 1 ml drops - 5 mg.
Excipients:
- Tablets: microcrystalline cellulose, lactose monohydrate, magnesium stearate, colloidal silicon dioxide;
- Drops: sodium acetate, propylene glycol, glycerol 85%, sodium saccharinate, propyl parahydroxybenzoate, methyl parahydroxybenzoate, acetic acid, purified water.
Additionally, as part of the film coating of tablets: opadry Y-1-7000 (macrogol 400, titanium dioxide (E171), hypromellose).
Pharmacological properties
Pharmacodynamics
Levocetirizine, the active component of Xizal, is the R-enantiomer of cetirizine, which is a competitive histamine antagonist and blocks H 1 -histamine receptors. This compound affects the histamine-dependent stage of an allergic nature, and also reduces vascular permeability, inhibits the migration of eosinophils, and limits the release of inflammatory mediators.
Levocetirizine prevents the occurrence and facilitates the course of allergic reactions, has an antipruritic and antiexudative effect. For him, antiserotonin and anticholinergic action is practically uncharacteristic. In therapeutic doses, taking Ksizal does not lead to the development of a sedative effect.
Pharmacokinetics
Pharmacokinetic parameters of levocetirizine are linear. After oral administration, it is rapidly and almost completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, but somewhat slows down its rate. The maximum content of levocetirizine in blood plasma is observed after 0.9 hours and is 270 ng / ml. Determination of the equilibrium concentration becomes possible 2 days after administration.
The degree of binding of levocetirizine to blood plasma proteins is 90%. The volume of distribution is 0.4 l / kg. The bioavailability of this compound reaches 100%.
Less than 14% of levocetirizine is metabolized in the liver, forming a metabolite with practically zero pharmacological activity. The half-life in adult patients is 7.9 ± 1.9 hours, and the total clearance is 0.63 ml / min / kg. Approximately 85.4% of the taken dose of Ksizal is excreted in the urine, about 12.9% in the feces. In patients with renal failure with CC less than 40 ml / min, the clearance of the drug decreases. In patients on hemodialysis, the total clearance decreases by 80%, which requires correction of the dosage regimen. Less than 10% of levocetirizine is eliminated during a standard hemodialysis procedure lasting 4 hours.
Indications for use
According to the instructions, Ksizal is indicated for the symptomatic treatment of diseases and conditions of allergic genesis:
- Allergic rhinitis, seasonal (intermittent) and perennial (persistent);
- Pollinosis, or hay fever;
- Allergic conjunctivitis with characteristic symptoms such as itching, nasal congestion and sneezing, rhinorrhea, conjunctival hyperemia, lacrimation;
- Allergic dermatoses, occurring with itching and rashes;
- Urticaria, including chronic idiopathic urticaria;
- Quincke's edema.
Contraindications
- Terminal (end) stage of renal failure (with creatinine clearance (CC) less than 10 ml / min.);
- The period of pregnancy and breastfeeding;
- Individual hypersensitivity to drug components.
The use of Ksizal tablets is contraindicated in patients with galactosemia or severe lactose intolerance, and in children under 6 years of age.
Ksizal drops cannot be used to treat children under the age of 2 years.
Instructions for the use of Ksizal: method and dosage
The drug in the form of tablets and drops is taken orally on an empty stomach or with meals.
The tablets should be swallowed whole with plenty of water.
Ksizal drops can be diluted with a small amount of water just before taking.
Children from 2 to 6 years old should take 5 drops, 2 times a day.
Patients with renal insufficiency and the elderly need to adjust the daily dose of Ksizal.
The recommended dosage of Ksizal for patients with renal insufficiency: mild (CC 50-79 ml / min) - do not change the dose, moderate (CC 30-49 ml / min) - the patient is prescribed 5 mg per day 1 time in 2 days; severe (CC less than 30 ml / min.) - 5 mg per day 1 time in 3 days.
The dosage regimen for patients with impaired liver function does not need correction.
The duration of treatment depends on the clinical indication. With pollinosis, the drug should be taken for 1-6 weeks (on average), with chronic diseases (atopic dermatitis, perennial rhinitis) - 18 months.
Side effects
The use of Ksizal can cause side effects:
- From the side of the cardiovascular system: very rarely - tachycardia;
- From the nervous system: infrequently - fatigue, drowsiness and headache; rarely - general weakness; very rarely - agitation, aggression, convulsions, depression, visual impairment, hallucinations;
- From the respiratory system: very rarely - shortness of breath (dyspnea);
- From the side of metabolism: very rarely - increased body weight;
- From the digestive system: infrequently - dry mouth; rarely - abdominal pain; very rarely - diarrhea, nausea, changes in liver function tests, hepatitis;
- From the musculoskeletal system: very rarely - myalgia;
- Allergic reactions: very rarely - rash, pruritus, urticaria, anaphylaxis, angioedema.
Overdose
Signs of an overdose of Ksizal are drowsiness (in adult patients) and restlessness and anxiety, followed by drowsiness (in children). After taking the drug in high doses, it is necessary to rinse the stomach as soon as possible or induce artificial vomiting. After that, they take activated charcoal and prescribe symptomatic and supportive therapy. There is no specific antidote. The effectiveness of hemodiadesis is minimal.
special instructions
The use of Ksizal in the recommended doses does not cause undesirable effects that affect the patient's ability to drive vehicles and mechanisms. Despite this, during the period of treatment, potentially hazardous activities should be avoided, the implementation of which requires concentration of attention and a high speed of psychomotor reactions.
Application during pregnancy and lactation
Adequate and strictly controlled clinical studies on the safety of using Ksizal in pregnant women have not been conducted, therefore it is recommended to refrain from prescribing it during pregnancy. Levocetirizine passes into breast milk, so if you need to take it during lactation, you should stop breastfeeding until the end of the course of treatment. Experimental studies on animals did not reveal any direct or indirect adverse effects of levocetirizine on the developing fetus (including the postnatal period), the course of pregnancy and childbirth also proceeded within normal limits.
Use in the elderly
Since levocetirizine is excreted through the kidneys, when it is prescribed to elderly patients, dose adjustment is required in accordance with the creatinine clearance value.
Drug interactions
The drug interaction of levocetirizine with other drugs has not been established.
Analogs
The analogues of Ksizal are: Glenzet, Zenaro, Suprastinex, Tsesera, Elset, Aleron, Alerzin.
Terms and conditions of storage
Keep out of the reach of children:
- Tablets: in a dry place at temperatures up to 25 ° C;
- Drops: in a dark place at temperatures up to 30 ° C.
Shelf life: tablets - 4 years, drops - 3 years.
After opening the bottle, the drops are suitable for use within 3 months.
1 ml of solution contains
active substance - levocetirizine dihydrochloride 5 mg,
excipients: sodium acetate, acetic acid, propylene glycol, glycerol 85%, methyl parahydroxybenzoate (E 218), propyl parahydroxybenzoate (E 217), sodium saccharin, purified water.
Description
Transparent, slightly opalescent liquid.
Pharmacotherapeutic group
Systemic antihistamines. Piperazine derivatives. Levociterizin.
ATX code R06АE09
Pharmacological properties
Pharmacokinetics
The pharmacokinetic parameters of levocetirizine vary linearly and practically do not differ from the pharmacokinetics of cetirizine.
Suction. After oral administration, the drug is rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect the completeness of absorption, although its rate decreases. In adults, after a single dose of the drug in a therapeutic dose (5 mg), the maximum concentration (Cmax) in the blood plasma is reached after 0.9 hours and is 270 ng / ml, after repeated administration at a dose of 5 mg / day - 308 ng / ml. A constant concentration level is reached after 2 days.
Distribution. Levocetirizine is 90% bound to blood plasma proteins. The volume of distribution (Vd) is 0.4 l / kg. Bioavailability reaches 100%.
Metabolism. In small quantities (< 14 %) метаболизируется в организме путем N- и О-деалкилирования (в отличие от других антагонистов Н1-гистаминовых рецепторов, которые метаболизируются в печени с помощью системы цитохромов) с образованием фармакологически неактивного метаболита. Из-за низкого уровня метаболизма и отсутствия метаболического потенциала взаимодействие левоцетиризина с другими лекарственными препаратами представляется маловероятным.
Dealkylation is primarily mediated by CYP 3A4, with numerous and / or unknown CYP isoforms involved during aromatic oxidation. Levocetirizine does not affect the activity of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at concentrations significantly higher than the peak concentration achieved with a dose of 5 mg.
Due to its low metabolism and lack of metabolic suppression potential, the interaction of levocetirizine with other substances, or vice versa, is unlikely.
Withdrawal
The half-life in adults is 7.9 ± 1.9 hours. The half-life in young children is shortened. The average total clearance in adults is 0.63 ml / min / kg. The main route of excretion of levocetirizine and metabolites in the urine averages 85.4% of the dose. Fecal excretion is only 12.9% of the dose. Levocetirizine is secreted by both glomerular filtration and active tubular secretion. In patients with renal insufficiency (creatinine clearance (CC)< 40 мл/мин) клиренс препарата уменьшается, а T1/2 удлиняется (так, у больных, находящихся на гемодиализе, общий клиренс снижается на 80 %), что требует соответствующего изменения режима дозирования. Менее 10 % левоцетиризина удаляется в ходе стандартной 4-часовой процедуры гемодиализа.
Pharmacodynamics
Levocetirizine is the active substance of Ksizal®, the R-enantiomer of cetirizine, which belongs to the group of competitive histamine antagonists and blocks H1-histamine receptors. The affinity for H1 receptors in levocetirizane is 2 times higher than that of cetirizine.
Levocetirizine affects the histamine-dependent stage of allergic reactions, and also reduces the migration of eosinophils, reduces vascular permeability, and limits the release of inflammatory mediators.
Levocetirizine prevents the development and facilitates the course of allergic reactions, has an antiexudative, antipruritic effect, practically does not have an anticholinergic and antiserotonin effect. In therapeutic doses, it does not have a sedative effect.
Indications for use
Symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis)
Hives.
Method of administration and dosage
The drug is taken orally, with food or on an empty stomach.
Drops are poured into a teaspoon or dissolved in a little water. If dilution is used, especially in children, the amount of water that the patient is able to swallow should be used. The diluted solution must be consumed immediately.
When counting drops, the bottle must be positioned vertically (top to bottom). If there is no flow of drops, if the required number of drops has not been delivered, turn the bottle to an upright position and then hold it upside down and continue counting drops.
Even if there is some data on clinical studies in children aged 6 months to 12 years, they are not a sufficient basis for the use of levocetirizine in infants and children under 2 years of age.
In this connection, the appointment of levocetirizine to newborns and children under 2 years of age is not recommended.
Children aged 2 to 6:
Adolescents 12 years of age and older and adults:
Adult patients with renal impairment
Dosing intervals should be individualized depending on renal function. Refer to the following table and adjust the dose as directed. To use this dosing table, an estimate of the patient's creatinine clearance (CC) in ml / min is required. CC (ml / min) can be estimated from serum creatinine (mg / dL), determined by the following formula:
× body weight (kg)
CC \u003d –––––––––––––––––––––––––––––––– (× 0.85 for women)
72 × serum creatinine (mg / dl)
Children with kidney failure
The dose should be adjusted on an individual basis based on the patient's renal clearance and his / her body weight.
Patients with hepatic impairment
No dose adjustment is required in patients with only hepatic impairment. For patients with hepatic and renal impairment, dose adjustment is recommended (see "Adult patients with renal impairment" above).
Duration of use:
Recurrent allergic rhinitis (symptoms<4 дня/неделю или менее чем 4 недели) должен рассматриваться в зависимости от заболевания и его истории, лечение можно остановить только после исчезновения симптомов, и может быть возобновлен снова, когда появляются симптомы. В случае стойкого аллергического ринита (симптомы >4 days / week and for more than 4 weeks), continuous therapy can be offered to the patient during the period of exposure to allergens. For chronic urticaria and chronic allergic rhinitis, there is clinical experience with racemate use up to one year.
Side effects
In placebo-controlled studies in children 6-11 months old and 1-6 years old
Diarrhea, vomiting, constipation, salivary hypersecretion
Thirst, hunger, fatigue, anorexia, drowsiness, psychomotor hyperactivity, sleep disturbances, moderate insomnia
Nose bleed
In children aged 6-12 years
Headache, drowsiness
In adolescents over 12 years of age and adults
Headache, drowsiness, dry mouth, fatigue
Cases of adverse reactions have been observed (infrequently ≥ 1/1000,<1/100), таких как слабость и боль в животе.
The incidence of sedative adverse reactions, such as drowsiness, fatigue, and asthenia, was more frequent (8.1%) after taking levocetirizine 5 mg than with placebo (3.1%).
Post-marketing period
Hypersensitivity, including anaphylaxis, angioedema, persistent drug erythema, rash, pruritus, urticaria
Increased appetite, nausea, vomiting
Aggression, agitation, hallucinations, depression, insomnia, suicidal thoughts, convulsions, paresthesias, dizziness, fainting, tremors, dysgeusia, blurred vision, blurred vision
Palpitations, tachycardia
Hepatitis, liver dysfunction
Dysuria, urinary retention
Muscle pain
Weight gain
Contraindications
Hypersensitivity to levocetirizine or any of the other components of the drug or to any piperazine derivatives.
Severe renal failure with creatinine clearance less than 10 ml / min.
Children under 2 years old
Pregnancy and lactation
Drug interactions
No studies have been conducted to study the interaction with levocetirizine (including studies with CYP3A4 inducers).
Studies of compounds of cetirizine with racemate have not shown any clinically significant adverse interactions with antipyrine, pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam.
A slight decrease in the clearance of cetirizine (16%) was observed in a study with several doses of theophylline (400 mg once a day), while the pharmacokinetics of theophylline did not change with the simultaneous use of cetirizine.
In a multi-dose study of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), the exposure to cetirizine was increased by about 40%, and the pharmacokinetics of ritonavir was slightly altered (-11%), which further accompanied the absorption of cetirizine.
The absorption rate of levocetirizine does not decrease with food intake, although the rate of absorption decreases.
In sensitive patients, the simultaneous use of cetirizine or levocetirizine and alcohol or other CNS depressants may have an effect on the central nervous system, although the racemate of cetirizine has not been shown to enhance the effect of alcohol.
special instructions
Patients taking Ksizal® should refrain from drinking alcohol.
Take with extreme caution in patients with predisposing factors of urinary retention (damage to the notochord of the spinal cord, prostatic hyperplasia), since levocetirizine may increase the risk of developing urinary retention.
Methyl parahydroxybenzoate and propyl parahydroxybenzoate contained in Ksizal® oral drops can cause allergic reactions (possibly with a delay).
