Cetirizine dosage

Cetirizine

Description current as of 07/02/2016

  • Latin name: Cetirizine
  • ATX code: R06AE07
  • Active ingredient: Cetirizine
  • Manufacturer: Obolenskoye, VERTEX, Ozon LLC, Berezovsky Pharmaceutical Plant (Russia), Glochem Industries (India)

Compound

1 tablet contains cetirizine dihydrochloride 10 mg.

Table of contents:

MCC, silicon dioxide, lactose monohydrate, magnesium stearate as auxiliary components.

1 ml drops - cetirizine dihydrochloride 10 mg. Benzoic acid, propylene glycol, glycerol, water, sodium acetate, as excipients.

Release form

  • Coated tablets Cetirizine Teva 10 mg.
  • Cetirizine Hexal drops for oral administration in bottles of 10 ml or 20 ml.

pharmachologic effect

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

H1-histamine receptor blocker, competitive histamine antagonist. Eliminates manifestations of allergic reactions, having antiexudative and antipruritic effects. Reduces capillary permeability, eliminates muscle spasms and skin reactions (with cold urticaria). Reduces the hyperreactivity of the bronchopulmonary system in patients with asthma in response to the release of histamine.

It has almost no anticholinergic and sedative effects. The effect is observed after 1 hour, the maximum effect is determined after 4 hours, and the duration is 24 hours. The effect lasts 3 days after the end of treatment. During treatment, tolerance to the drug does not develop.

Pharmacokinetics

When taken orally it is well absorbed. Cmax is determined in the blood after 1 hour. It is 93% protein bound. Does not accumulate. Metabolized to an inactive metabolite, 60% is excreted by the kidneys in 96 hours and a small part of the active substance (10%) is excreted through the intestines. T1/2 is 7-10 hours. T1/2 in children 6-12 years old is 6 hours. There is an increase in T1/2 with impaired renal and liver function.

Indications for use

Contraindications

  • increased sensitivity;
  • age up to 6 years (for tablets);
  • pregnancy;
  • lactation;
  • severe renal failure;
  • glucose-galactose malabsorption;
  • lactose intolerance.

Prescribed with caution in severe renal failure, in old age, while taking barbiturates, ethanol, opioid analgesics, benzodiazepine derivatives. Avoid driving during the period of use.

Side effects

Most common adverse reactions:

Rarely encountered adverse reactions:

Instructions for use of Cetirizine (Method and dosage)

Cetirizine Hexal drops, instructions for use

Adults and children over 12 years of age are prescribed 20 drops (equivalent to 10 mg), preferably in the evening. Children - 20 drops in the evening, from 2 to 6 years - 10 drops in the evening, from 1 to 2 years 5 drops 2 times a day.

For elderly patients, the dose is not changed. In case of renal failure, the recommended dose is reduced by 2 times. For liver failure, the dose is selected individually. The duration of treatment for seasonal allergic rhinitis is weeks. If the flowering of plants is not long, and the pollen effect is short-term - one week.

Instructions for use Cetirizine Teva

The tablets are taken orally, as a whole, preferably in the evening, given the sedative effect. Adults and children over 12 years of age are prescribed 10 mg per day. Children 6-12 years old with a weight over 30 kg - 10 mg once a day, with a weight less than 30 kg - 5 mg once a day.

Overdose

An overdose is manifested by drowsiness in adults, anxiety and irritability in children, urinary retention, constipation, dry mouth, dilated pupils, tachycardia.

Treatment consists of gastric lavage and the administration of enterosorbents. Symptomatic treatment is carried out. There is no antidote. Hemodialysis is not effective.

Interaction

The drug enhances the effects of alcohol, so taking it is not permissible during treatment with this drug. The use of Cetirizine should be stopped three days before allergy tests are performed.

Terms of sale

Dispensed without a doctor's prescription.

Storage conditions

Storage temperature up to 25°C.

Best before date

Cetirizine during pregnancy

The official instructions indicate that the drug is contraindicated during pregnancy. This is based on the fact that there have been no adequate studies of women in this category, but animal studies have not revealed any risks of negative effects on the fetus (FDA Fetal Risk Category B). There is also no data on its excretion in breast milk, so it should not be used while breastfeeding.

However, according to the few studies of the drug on the possibility of use in pregnant women in the first trimester, it does not increase the number of birth defects, the frequency of spontaneous abortions and early births. There was no difference in the weight of newborns whose mothers took Cetirizine.

If there is a need to use antiallergic drugs during pregnancy, then, weighing all the risks, preference should be given to Fenkarol, cetirizine and Loratadine, which are best not prescribed in the first trimester.

Cetirizine analogs

Reviews of Cetirizine

What are Cetirizine tablets for? This is a second generation antiallergic (antihistamine) drug with a rapid onset of action and a long duration. The use of the drug is justified in cases where long-term treatment of allergic diseases is necessary: ​​chronic urticaria, year-round rhinitis.

Its characteristic feature is its high ability to penetrate the skin, so it is effective for skin manifestations of allergies - atopic dermatitis, urticaria, rashes of allergic origin. Of all the second generation drugs, only Cetirizine is used in children from 6 months.

High affinity for histamine H1 receptors minimizes side effects. According to patient reviews, even long-term use of the drug did not cause dry mouth, nose, or constipation. A number of drugs in this group have a cardiotoxic effect, but Cetirizine, Ebastine, Loratadine, Akrivastine do not have such an effect.

Reviews of Cetirizine Hexal are positive, patients note its effectiveness, and, importantly, the variety of release forms. Parents note that the drug in the form of drops is more acceptable for children. The pharmacy has a large selection of dosage forms with the same active ingredient. Drops of cetirizine hydrochloride are produced under the names Zyrtec, Zodak, Pralazine, and Zerinal, Cetrin, Zincet are produced in the form of syrup, which further expands the possibilities of their use. With all this, the drug is regarded as a drug with a sedative effect (which cannot be said about Amertil), which limits its use.

Cetirizine price, where to buy

You can purchase this drug at any pharmacy. The cost depends on the manufacturer. Price of Cetirizine Teva bran tablets. For children, the release form is more convenient - drops. Price of Cetirizine Hexalrub drops. The same pharmaceutical company also produces a tablet form.

Russian Cetirizine Vertex is also available in the pharmacy chain, 20 tablets of which can be purchased for foreign purchases. These drugs contain the active ingredient cetirizan hydrochloride.

The pharmacy chain offers drugs containing cetirizine dihydrochloride: Cetrin (RUB) and Amertil, which do not have a sedative effect.

  • Online pharmacies in Russia Russia
  • Online pharmacies in Ukraine Ukraine

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Education: Graduated from the Sverdlovsk Medical School (1968 - 1971) with a degree in Paramedic. He graduated from the Donetsk Medical Institute (1975 - 1981) with a degree in epidemiologist and hygienist. He completed his postgraduate studies at the Central Research Institute of Epidemiology in Moscow (1986 - 1989). Academic degree - Candidate of Medical Sciences (degree awarded in 1989, defense - Central Research Institute of Epidemiology, Moscow). Completed numerous advanced training courses in epidemiology and infectious diseases.

Work experience: Work as head of the disinfection and sterilization department 1981 - 1992. Work as head of the department of especially dangerous infections 1992 - 2010. Teaching activity at the Medical Institute 2010 - 2013

Ira: I switched to tenoten after valerian and sedatives stopped helping me.

Kaloshin Sergey: Educational, useful.

Valentin: grapes, bananas, chocolate, cocoa, tea and coffee, white rice - what harm did they do? If known.

Polina Zhilko: I take Valsartan sz, this is our Russian drug. The result is excellent, I recommend it.

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The site administration and the authors of the articles are not responsible for any losses and consequences that may arise when using the site materials.

Source: http://medside.ru/tsetirizin

Cetirizine

Cetirizine, general information

The drug Cetirizine is an antiallergic drug. Available in the form of tablets, which are covered with a white coating, oblong in shape. The main active ingredient is cetirizine dihydrochloride, 1 tablet = 10 mg. Excipients include microcrystalline cellulose, lactose monohydrate, magnesium stearate, colloidal silicon dioxide, hypromellose, titanium dioxide, macrogol.

The drug is packaged in cardboard packs, each containing blisters of 7-10 tablets.

Cetirizine is also produced in the form of colorless transparent drops with a vinegary odor. The main component of the product is cetirizine dihydrochloride, 1 ml = 10 mg. Excipients include: glycerol, sodium saccharinate, propylene glycol, propylparabenzene, sodium acetate, methylparabenzene, glacial acetic acid, purified water.

Cetirizine drops are packaged in dark glass dropper bottles with a capacity of ml.

Cetirizine, indications, contraindications

The drug Cetirizine is prescribed for:

  • symptomatic treatment of allergic rhinitis, both seasonal and year-round; for the symptomatic treatment of allergic conjunctivitis. Symptoms include rhinorrhea, sneezing, itching, conjunctival hyperemia, lacrimation;
  • treatment of hay fever (hay fever);
  • treatment of urticaria;
  • treatment of Quincke's edema;
  • treatment of other allergic dermatoses, which are accompanied by rash and itching.

Taking the drug is contraindicated in the following cases:

  • Pregnancy and lactation;
  • End stage renal failure;
  • Manifestations of hereditary galactose intolerance by the body;
  • When the child’s age is less than 6 years (to take tablets) or less than 6 months (to take drops);
  • Increased sensitivity of the body to hydroxyzine;
  • Hypersensitivity of the body to any of the components of the drug.

The drug is prescribed with some caution in cases where the patient has chronic renal failure (in this case it is necessary to adjust the prescribed dose), in cases of chronic liver disease, as well as in elderly patients.

Cetirizine, overdose and side effects of the drug

In case of an overdose of Cetirizine (single dose exceeding 50 mg), the following symptoms may occur:

  • dizziness,
  • headache,
  • diarrhea,
  • fast fatiguability,
  • weakness,
  • malaise,
  • confusion,
  • drowsiness,
  • stupor,
  • sedative effect,
  • tremor,
  • itching,
  • tachycardia,
  • delay when urinating.

Treatment is based on gastric lavage or artificial induction of vomiting. Activated carbon, symptomatic and supportive therapy are also prescribed. There is no specially developed antidote; hemodialysis is not an effective remedy in this case.

The following side effects are possible when taking the drug:

  • Digestive system - nausea, abdominal pain, diarrhea, dry mouth, liver dysfunction;
  • Cardiovascular system - the appearance of tachycardia;
  • Nervous system – headache, aggression, dizziness, drowsiness, depression, hallucinations, insomnia, convulsions, tic, tremor, fainting, dyskinesia, dystonia;
  • Hematopoietic system - thrombocytopenia;
  • Visual organs - nystagmus, loss of sharpness of vision, impaired accommodation;
  • Respiratory organs – pharyngitis, rhinitis;
  • Metabolism – possible change in body weight towards increase;
  • Urinary system – enuresis, urinary disorders;
  • Allergic manifestations - rash, urticaria, itching, swelling, increased sensitivity, as a final result anaphylactic shock;
  • Additionally – malaise, swelling of the integument, fatigue, asthenia.

Despite the above points, side effects when taking Cetirizine occur in very rare cases.

The use of the drug is contraindicated during pregnancy and lactation.

Cetirizine, drops and tablets, use, dosage

The drug Cetirizine is prescribed for oral administration.

For people over 6 years of age, the drug is prescribed in an amount of 10 mg (which is 1 tablet or 20 drops) per day. Adults take 10 mg once a day, children 5 mg twice a day - or 10 mg once a day. In some cases, an initial dose of 5 mg may be sufficient to obtain a positive therapeutic effect.

For the age group from 2 to 6 years old, Cetirizine is prescribed in the amount of 2.5 mg (which is 5 drops) twice a day, or 5 mg (=10 drops) once a day.

For the age group from one to 2 years, the drug is prescribed in the amount of 2.5 mg (=5 drops) twice a day.

For the age group from 6 to 12 months, Cetirizine is prescribed once a day at a dosage of 2.5 mg (=5 drops).

If elderly patients have renal failure, the dose of Cetirizine is adjusted based on the CC value. For patients suffering from renal and liver failure, the required dosage is calculated based on the data in the table:

Terminal stage (patients on dialysis)

No adjustment of the prescribed dosage is required for patients in whom only hepatic function is impaired.

Cetirizine, storage and distribution conditions

Cetirizine tablets are stored for no more than 5 years at a temperature of no more than 30 ° C, in places inaccessible to children. Cetirizine drops are stored for 5 years at a temperature of no more than 25 ° C, in a place inaccessible to children.

In the pharmacy chain, the drug Cetirizine is distributed without a prescription.

Cetirizine for children

Currently, the problem of allergic reactions in childhood has become more acute. The trigger for symptoms can be anything: from pollen to seemingly innocent foods. Given the current state of affairs, pharmaceutical companies are not standing still, developing new drugs. Unfortunately, not all of them are suitable for children. Cetirizine is an antihistamine that can be used not only by adults, but also by children.

Zyrtec is good for long-term use; for children, Cetirizine is prescribed in drops. However, it is contraindicated for children under 6 months of age. The attending physician can prescribe this drug to this age group only with a significant reduction in dosage, and the administration and subsequent reaction must be strictly monitored by a specialist.

For children under one year of age, Cetirizine is used as nasal drops; before instillation, it is necessary to pre-clean the nasal passages. Place drops in the nose once a day, drop by drop into the nasal passage. From one to 6 years, the drops are used in diluted form (5 drops), and after 6 years - in pure form. The daily dose can be applied at a time, or divided into two doses. Children over 10 years old can be given the drug in its pure form, 10 drops twice a day.

The duration of the course is determined by the attending physician and is based directly on the original disease that caused the allergic reaction, as well as on the age of the child. If there are no contraindications, the drug can be given once only if the situation is critical and urgent medical attention is needed.

Cetirizine, price

Depending on the form of release, the region of distribution of the drug, as well as the distributor itself, the cost of the drug Cetirizine can range from 170.00 UAH. up to 233.00 UAH.

Source: http://sblpb.ru/lekarstvennye-preparaty/64-tsetirizin

CETIRIZINE

Film-coated tablets, white or almost white, round, biconvex; on a cross section, the core is white or almost white.

Excipients: microcrystalline cellulose, lactose monohydrate, crospovidone, magnesium stearate, colloidal silicon dioxide.

Shell composition: [hypromellose, talc, titanium dioxide, macrogol 4000] or [dry white film shell containing hypromellose, talc, titanium dioxide, macrogol 4000].

10 pieces. — cellular contour packages (1) — cardboard packs.

10 pieces. — contour cell packaging (2) — cardboard packs.

10 pieces. — cellular contour packages (3) — cardboard packs.

A competitive histamine antagonist, a metabolite of hydroxyzine, blocks H1 - histamine receptors. Prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects. Affects the early stage of allergic reactions, limits the release of inflammatory mediators at the late stage of the allergic reaction, reduces the migration of eosinophils, neutrophils and basophils. Reduces capillary permeability, prevents the development of tissue edema, relieves spasm of smooth muscles.

Eliminates skin reactions to the introduction of histamine, specific allergens, as well as to cooling (with cold urticaria).

It has virtually no anticholinergic and antiserotonin effects. In therapeutic doses it practically does not cause a sedative effect. The onset of action after a single dose of 10 mg of cetirizine is after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients), lasting more than 24 hours. During a course of treatment, tolerance to the antihistamine effect of cetirizine does not develop. After stopping treatment, the effect lasts up to 3 days.

Rapidly absorbed from the gastrointestinal tract, the time to reach Cmax after oral administration is 1 hour. Food does not affect the completeness of absorption (AUC), but prolongs the time to reach Cmax by 1 hour and reduces the Cmax value by 23%. When taken at a dose of 10 mg 1 time / day for 10 days, the equilibrium concentration in plasma is 310 ng/ml and is observed 0.5-1.5 hours after administration. Plasma protein binding is 93% and does not change with cetirizine concentrations in the range of ng/ml. The pharmacokinetic parameters of cetirizine change linearly when administered at a dose of 5-60 mg. V d - 0.5 l/kg. In small quantities, it is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite (unlike other H1-histamine receptor blockers , which are metabolized in the liver with the participation of the cytochrome P450 system). Does not accumulate. 2/3 of the drug is excreted unchanged by the kidneys and about 10% through the intestines.

Systemic clearance - 53 ml/min. T1 /2 in adults, in children 6-12 years old - 6 hours, in children 2-6 years old - 5 hours, in children from 6 months to 2 years - 3 hours. In elderly patients, T1/2 increases by 50% , systemic clearance is reduced by 40% (decreased renal function).

In patients with impaired renal function (creatinine clearance below 40 ml/min), the clearance of the drug decreases and T1 /2 is prolonged (for example, in patients on hemodialysis, the total clearance decreases by 70% and is 0.3 ml/min/kg, and T 1/2 is extended by 3 times), which requires a corresponding change in the dosage regimen.

In patients with chronic liver diseases (hepatocellular, cholestatic or biliary cirrhosis), there is an increase in T1 /2 by 50% and a decrease in total clearance by 40% (adjustment of the dosage regimen is required only with a concomitant decrease in glomerular filtration rate). Passes into breast milk.

- seasonal and year-round allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, conjunctival hyperemia);

- urticaria (including chronic idiopathic urticaria);

- hay fever (hay fever);

- angioedema (Quincke's edema);

- itchy allergic dermatoses.

- decreased renal function (creatinine clearance/min);

— chronic renal failure;

- children under 6 years of age;

- hypersensitivity to cetirizine, other components of the drug, hydroxyzine.

With caution: older age (possibly decreased glomerular filtration rate).

Orally, regardless of food intake, without chewing and with a sufficient amount of liquid, preferably in the evening.

Adults and children over 6 years of age (weighing more than 30 kg) - 1 tablet. 1 time/day

The drug is usually well tolerated. Side effects occur rarely and are transient.

From the digestive system: dry mouth, dyspepsia.

From the nervous system: dizziness, headache, drowsiness, fatigue, agitation, migraine.

Allergic reactions: angioedema, skin rashes, itching, urticaria.

Symptoms (when taking a single dose of 50 mg): dry mouth, drowsiness, urinary retention, constipation, anxiety, increased irritability.

Treatment: gastric lavage, symptomatic therapy. A specific antidote has not been identified. Hemodialysis is ineffective.

Combined use with theophylline (400 mg/day) leads to a decrease in the overall clearance of cetirizine (theophylline kinetics does not change).

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

No clinically significant interactions were found with other drugs (pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, diazepam, glipizide).

Concomitant use with alcohol and drugs that depress the central nervous system is not recommended.

Impact on the ability to drive vehicles and operate machinery:

During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. If the dose exceeds 10 mg/day, the ability to react quickly may deteriorate.

The use of the drug during pregnancy is not recommended. Because Cetirizine passes into breast milk and is not prescribed during lactation.

Children over 6 years of age (weighing more than 30 kg) - 1 tablet. 1 time/day

Contraindicated for children under 6 years of age.

- decreased renal function (creatinine clearance/min);

- chronic renal failure.

Store the drug in a dry place, protected from light, at a temperature not exceeding 25°C.

Keep out of the reach of children.

Shelf life: 2 years.

Do not use after expiration date.

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Source: http://health.mail.ru/drug/tsetirizin/

Cetirizine - instructions for use of tablets, drops and syrup, what to use, analogues

Cetirizine is a 2nd generation antiallergic (antihistamine) drug with a rapid onset of action and a long duration. The use of the drug is justified in cases where long-term treatment of allergic diseases is necessary: ​​chronic urticaria, year-round rhinitis. The drug prevents the development and facilitates the course of allergic reactions, has antipruritic and antiexudative effects. Available in the form of tablets, drops and syrup for oral administration.

Composition and release form

Cetirizine (CETIRIZINE) is an antiallergic drug. Histamine H1 receptor blocker. The medicine is included in the list of necessary medications and is available without a prescription.

Excipients of Cetirizine include:

  • colloidal silicon dioxide;
  • lactose monohydrate;
  • crospovidone;
  • magnesium stearate;
  • microcrystalline cellulose:
  • shell: hypromellose, polydextrose, macrogol, titanium dioxide.
  • White, oblong-shaped Cetirizine tablets
  • Colorless, transparent drops for oral administration
  • Colorless, transparent syrup for oral administration, with the smell of banana

pharmachologic effect

The body's perception of the drug begins already at the stage of its ingestion. Actively absorbed by the upper layer of the epidermis and mucous membrane when it enters the oral cavity and then into the intestines, the active substance causes a decrease in the activity of allergy manifestations.

It has virtually no anticholinergic and antiserotonin effects. In therapeutic doses it practically does not cause a sedative effect. The onset of action after a single dose of 10 mg of cetirizine is after 20 minutes (in 50% of patients) and after 60 minutes (in 95% of patients), lasting more than 24 hours. During a course of treatment, tolerance to the antihistamine effect of cetirizine does not develop. After stopping treatment, the effect lasts up to 3 days.

The medicine is able to prevent and reduce the skin reaction that occurs when histamine is released and when specific allergens penetrate the skin.

Indications

What does it help with? According to the instructions, Cetirizine is indicated in the following cases:

  • urticaria, including chronic idiopathic;
  • allergic conjunctivitis;
  • seasonal and year-round allergic rhinitis (as symptomatic treatment);
  • dermatoses that occur with itching, including neurodermatitis, atopic dermatitis.

The drug can also be prescribed to patients who are prone to developing allergic reactions to medications, for example, antibiotics, cough syrups and others.

Cetirizine is prescribed with extreme caution to elderly people and persons suffering from moderate and severe chronic pyelonephritis.

Instructions for use

To achieve maximum effect, you should take Cetirizine tablets correctly. The analogue should also be used after carefully studying the instructions. The drug is taken orally. There is no need to chew the tablets. Wash them down with plenty of water. The medication can be used regardless of meals. On an empty stomach, the rate of absorption of tablets increases.

Cetirizine tablets

The tablets are taken orally, as a whole, preferably in the evening, given the sedative effect. Adults and children over 12 years of age are prescribed 10 mg per day. Children 6-12 years old with a weight over 30 kg - 10 mg once a day, with a weight less than 30 kg - 5 mg once a day.

Cetirizine drops

Take Cetirizine orally, regardless of meals.

Instructions for use for children and adults:

  • Adults and adolescents over 12 years of age are recommended to take 20 drops (10 mg) daily, preferably in the evening.
  • Children aged 6-12 years: 10 drops (5 mg) twice a day in the morning and evening or 20 drops (10 mg) in the evening.
  • Children aged 2-6 years: 10 drops (5 mg) in the evening or 5 drops (2.5 mg) in the morning and evening.
  • Children aged 1-2 years: 5 drops (2.5 mg) twice a day.

Due to the depressant effect of Cetirizine on the central nervous system, this drug in the form of drops should be prescribed with extreme caution to children under one year of age in whom factors have been identified that increase the risk of SIDS - sudden infant death syndrome.

Syrup

Cetirizine syrup in dark glass bottles of 75 or 150 ml, complete with a 5 ml measuring spoon, along with instructions for use in a cardboard box.

Children from two to 12 years old and weighing less than 30 kg are prescribed a dose of 5 ml; if the weight is greater, then 10 ml of the drug per day is needed. Patients over 12 years of age require a daily dosage of 10 ml. You can take 2 times a day (morning and evening) 5 ml (1 measuring spoon).

In case of renal failure, the recommended dose should be reduced by 2 times.

Contraindications

Cetirizine should be prescribed with caution to elderly people, as this category of patients may have a decrease in glomerular filtration. In addition, caution must be exercised when prescribing the drug for moderate and severe chronic pyelonephritis.

The official instructions indicate that the drug is contraindicated during pregnancy.

Side effects for the body

Typically, the drug Cetirizine is well tolerated by patients, but with an incorrectly calculated dose, hypersensitivity to the components of the tablet, or prolonged uncontrolled use of the drug, side effects may develop:

  • dry mouth;
  • dyspepsia;
  • headache;
  • drowsiness;
  • fatigue;
  • dizziness;
  • excitation;
  • migraine;
  • skin rash;
  • angioedema;
  • hives;
  • skin itching.

Cetirizine-Teva should be used with caution in patients with moderate to severe chronic renal failure and in elderly patients (reduced glomerular filtration rate is possible).

In case of severe side effects, it is recommended to stop taking this drug and replace it with analogues of action.

Overdose

Excessive use of the above drug can provoke the development of the following symptoms:

  • drowsiness,
  • lethargy,
  • urinary retention,
  • general weakness,
  • headache,
  • tachycardia,
  • increased fatigue and irritability.

special instructions

Concomitant use with alcohol and drugs that depress the central nervous system is not recommended.

During treatment, experts recommend refraining from engaging in activities that require increased attention. The tablets may cause drowsiness and slight dizziness. It is not advisable to drive a car.

According to the instructions, cetirizine is prohibited for use during pregnancy and lactation.

Interaction with other drugs

No clinically significant interactions of cetirizine with other drugs have been established.

Shelf life of tablets

Store the drug in a dry place, protected from light, at a temperature not exceeding 25°C.

  • Tablets, drops and syrup: store for 3 years. An open bottle can be used for 6 months.

Do not use the medicine after the stated expiration date.

Analogs

The most common and most effective analogues of Cetirizine are:

Before replacing a prescribed drug with its analogue, you should read the attached instructions for contraindications and age restrictions.

Prices in pharmacies

The approximate cost of Cetirizine is shown in the table:

Before using the drug, be sure to consult your doctor.

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Cetirizine

Content

Structural formula

Russian name

The Latin name of the substance is Cetirizine

Chemical name

[2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid (as hydrochloride)

Gross formula

Pharmacological group of the substance Cetirizine

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Cetirizine

Piperazine derivative, white crystalline powder, soluble in water, molecular weight - 461.82.

Pharmacology

Cetirizine is a metabolite of hydroxyzine, belongs to the group of competitive histamine antagonists and blocks H1 - histamine receptors.

In addition to the antihistamine effect, cetirizine prevents the development and alleviates the course of allergic reactions: at a dose of 10 mg 1 or 2 times a day, it inhibits the late phase of eosinophil aggregation in the skin and conjunctiva of patients with allergic reactions.

Clinical efficacy and safety

Studies in healthy volunteers have shown that cetirizine, when taken in doses of 5 or 10 mg, significantly inhibits the rash and redness response to high concentrations of histamine in the skin, but the correlation with effectiveness has not been established. A 6-week placebo-controlled study involving 186 patients with allergic rhinitis and concomitant mild to moderate bronchial asthma showed that cetirizine 10 mg once daily reduced symptoms of rhinitis and did not affect pulmonary function.

The results of this study confirm the safety of cetirizine in patients suffering from allergies and mild to moderate bronchial asthma.

A placebo-controlled study showed that taking cetirizine at a dose of 60 mg/day for 7 days did not cause a clinically significant prolongation of the QT interval. Taking cetirizine at the recommended dose has shown an improvement in the quality of life of patients with year-round and seasonal allergic rhinitis.

Children. In a 35-day study in patients 5–12 years of age, there was no evidence of resistance to the antihistamine effect of cetirizine. The normal skin reaction to histamine was restored within 3 days after discontinuation of the drug with repeated use.

A 7-day placebo-controlled study of cetirizine syrup in 42 patients aged 6 to 11 months demonstrated the safety of its use. Cetirizine was prescribed at a dose of 0.25 mg/kg twice daily, which corresponds to approximately 4.5 mg per day (dose range was 3.4 to 6.2 mg per day).

Use in children from 6 to 12 months is possible only as prescribed by a doctor and under strict medical supervision.

The pharmacokinetic parameters of cetirizine when taken in doses from 5 to 60 mg change linearly.

Tmax in blood plasma is (1±0.5) hours, and Cmax is 300 ng/ml.

Pharmacokinetic parameters such as Cmax in blood plasma and AUC are uniform. Food intake does not affect the complete absorption of cetirizine, although its rate decreases. The bioavailability of different dosage forms of cetirizine is comparable.

Cetirizine is (93±0.3)% bound to blood plasma proteins. Vd is 0.5 l/kg. Cetirizine does not affect the protein binding of warfarin.

Cetirizine does not undergo extensive first-pass metabolism.

T 1/2 is approximately 10 hours.

When taking cetirizine at a daily dose of 10 mg for 10 days, no accumulation was observed.

Approximately 2/3 of the dose taken is excreted unchanged in the urine.

Special patient groups

Elderly. In 16 elderly people, with a single dose of cetirizine at a dose of 10 mg, T1 /2 was 50% higher, and clearance was 40% lower compared to non-elderly people.

The decreased clearance of cetirizine in elderly patients is likely due to decreased renal function in this category of patients.

Kidney failure. In patients with mild renal failure (Cl creatinine >40 ml/min), pharmacokinetic parameters are similar to those in healthy volunteers with normal renal function.

In patients with moderate renal failure and patients on hemodialysis (Cl creatinine <7 ml/min), when taking cetirizine orally at a dose of 10 mg, T1 /2 is extended by 3 times, and the total clearance is reduced by 70% relative to healthy people volunteers with normal nocturnal function.

For patients with moderate or severe renal insufficiency, an appropriate change in the dosage regimen is required (see "Dosage and Administration").

Cetirizine is poorly removed from the body during hemodialysis.

Liver failure. In patients with chronic liver diseases (hepatocellular, cholestatic and biliary cirrhosis), with a single dose of cetirizine at a dose of 10 or 20 mg, T1 /2 increases by approximately 50%, and clearance decreases by 40% compared to healthy subjects. Dose adjustment is only necessary if the patient with hepatic insufficiency also has concomitant renal insufficiency.

Children. T1 /2 in children from 6 to 12 years is 6 hours, from 2 to 6 years - 5 hours, from 6 months to 2 years - reduced to 3.1 hours.

Use of the substance Cetirizine

To relieve nasal and ocular symptoms of year-round (persistent) and seasonal (intermittent) allergic rhinitis and allergic conjunctivitis (itching, sneezing, nasal congestion, rhinorrhea, lacrimation, conjunctival hyperemia); symptoms of hay fever (hay fever); symptoms of urticaria (including chronic idiopathic), other allergic dermatoses, incl. allergic dermatitis, accompanied by itching and rashes, in adults and children from 6 months (in the form of drops) or from 6 years (in the form of tablets).

Use in children from 6 to 12 months is possible only as prescribed by a doctor and under strict medical supervision.

Contraindications

Hypersensitivity to cetirizine, hydroxyzine or any piperazine derivatives; end-stage renal failure (Cl creatinine <10 ml/min); age up to 6 months (for the drop dosage form, due to limited data on the effectiveness and safety of cetirizine); age up to 6 years (for tablet dosage form); pregnancy.

Restrictions on use

Chronic renal failure (if creatinine Cl >10 ml/min, dosage regimen adjustment is required); elderly patients (with an age-related decrease in glomerular filtration); epilepsy and patients with increased convulsive readiness; patients with factors predisposing to urinary retention (see “Precautions”); age up to 1 year (for the dosage form of the drop); breastfeeding period.

Use during pregnancy and breastfeeding

An analysis of prospective data from more than 700 cases of pregnancy outcomes revealed no cases of malformations, embryonic or neonatal toxicity with a clear cause-and-effect relationship with the use of cetirizine.

Experimental studies in animals have not revealed any direct or indirect adverse effects of cetirizine on the developing fetus, pregnancy or postnatal development.

Adequate and strictly controlled clinical studies on the safety of cetirizine during pregnancy have not been conducted, therefore it should not be used during pregnancy.

FDA category of effect on the fetus is B.

Cetirizine is excreted in breast milk - from 25 to 90% of its concentration in the blood plasma, depending on the time after administration. During breastfeeding, it is used after consultation with a doctor, if the expected benefit to the mother outweighs the potential risk to the child.

Fertility. Available data on the effects on human fertility are limited, but no negative effects on fertility have been identified.

Side effects of the substance Cetirizine

Data obtained from clinical studies

The results of clinical studies have demonstrated that the use of cetirizine in recommended doses leads to the development of minor undesirable effects on the central nervous system, including drowsiness, fatigue, dizziness and headache. In some cases, paradoxical stimulation of the central nervous system has been reported.

Despite the fact that cetirizine is a selective blocker of peripheral H1 receptors and has virtually no anticholinergic effect, isolated cases of difficulty urinating, disturbances of accommodation and dry mouth have been reported.

Liver dysfunction has been reported, accompanied by increased levels of liver enzymes and bilirubin. In most cases, adverse events resolved after discontinuation of cetirizine.

List of unwanted side reactions. There is data obtained from double-blind, controlled clinical trials comparing cetirizine with placebo or other antihistamines used at recommended doses (10 mg once daily for cetirizine) in more than 3200 patients, on the basis of which a reliable analysis can be carried out safety data.

According to the results of the pooled analysis, in placebo-controlled studies with cetirizine 10 mg (n=3260) and placebo (n=3061), the following adverse reactions were identified with an incidence of 1% or higher.

General disorders and disorders at the injection site: fatigue - 1.63 and 0.95%.

From the nervous system: dizziness - 1.1 and 0.98%; headache - 7.42 and 8%.

From the gastrointestinal tract: abdominal pain - 0.98 and 1.08%; dry mouth - 2.09 and 0.82%; nausea - 1.07 and 1.14%.

From the mental side: drowsiness - 9.63 and 5%.

From the respiratory system, chest and mediastinal organs: pharyngitis - 1.29 and 1.34%.

Although the incidence of somnolence in the cetirizine group was higher than that in the placebo group, most cases were mild or moderate in severity. When objectively assessed in other studies, it was confirmed that the use of cetirizine at the recommended daily dose in healthy young volunteers does not affect their daily activities.

Children. In placebo-controlled studies in children aged 6 months to 12 years, the following adverse reactions were identified with an incidence of 1% or higher in the cetirizine (n=1656) and placebo (n=1294) groups.

From the gastrointestinal tract: diarrhea - 1 and 0.6%.

From the mental side: drowsiness - 1.8 and 1.4%.

From the respiratory system, chest and mediastinal organs: rhinitis - 1.4 and 1.1%.

General disorders and disorders at the injection site: fatigue - 1 and 0.3%.

Post-registration experience

In addition to the adverse events identified during clinical trials and described above, the following adverse reactions were observed during post-marketing use of cetirizine.

MedDRA organ system class and incidence, based on data from post-marketing use of cetirizine.

The incidence of adverse events was determined as follows: very often (≥1/10); often (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (<1/10000); frequency unknown (due to insufficient data).

From the blood and lymphatic system: very rarely - thrombocytopenia.

From the immune system: rarely - hypersensitivity reactions; very rarely - anaphylactic shock.

Metabolic and eating disorders: frequency unknown - increased appetite.

From the mental side: infrequently - agitation; rarely - aggression, confusion, depression, hallucinations, sleep disturbance; very rarely - tic; frequency unknown - suicidal ideation.

From the nervous system: infrequently - paresthesia; rarely - convulsions; very rarely - taste perversion, dyskinesia, dystonia, fainting, tremor; frequency unknown - memory impairment, incl. amnesia.

From the organ of vision: very rarely - disturbance of accommodation, blurred vision, nystagmus.

On the part of the hearing organs: frequency unknown - vertigo.

From the cardiovascular system: rarely - tachycardia.

From the digestive system: infrequently - diarrhea.

Hepatobiliary disorders: rarely - changes in liver function tests (increased activity of transaminases, alkaline phosphatase, gamma-glutamyl transferase and bilirubin levels).

On the skin: infrequently - rash, itching; rarely - urticaria; very rarely - angioedema, persistent drug erythema.

From the urinary system: very rarely - dysuria, enuresis; frequency unknown - urinary retention.

General disorders: infrequently - asthenia, malaise; rarely - peripheral edema.

Research: rarely - weight gain.

Interaction

Based on the analysis of pharmacodynamics and pharmacokinetics of cetirizine, interaction with other drugs is unlikely.

There was no significant interaction with pseudoephedrine or theophylline (at a dose of 400 mg/day) in specific drug interaction studies.

The simultaneous use of cetirizine with ethanol and other drugs that depress the central nervous system may further reduce concentration and reaction speed, although cetirizine does not enhance the effect of ethanol (at a blood concentration of 0.5 g/l).

Overdose

Symptoms (may be observed with a single dose of cetirizine 50 mg): confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, itching, anxiety, weakness, sedation, drowsiness, stupor, tachycardia, tremor, urinary retention .

Treatment: gastric lavage or stimulation of vomiting, administration of activated carbon; supportive and symptomatic therapy. There is no specific antidote. Hemodialysis is ineffective.

Routes of administration

Precautions for the substance Cetirizine

Due to the potential for CNS depressant effects, caution should be used when prescribing cetirizine oral drops to children under 1 year of age who have the following risk factors for sudden infant death syndrome, such as (but not limited to) sleep apnea or sudden infant death syndrome. death of infants of a brother or sister; maternal drug abuse or smoking during pregnancy; young maternal age (19 years and younger); Smoking abuse by a nanny caring for a child (one pack of cigarettes a day or more); children who regularly fall asleep face down and are not placed on their back; premature (gestational age less than 37 weeks) or low birth weight (below the 10th percentile of gestational age) children; joint use of drugs that have a depressant effect on the central nervous system.

In patients with spinal cord injury, prostatic hyperplasia, as well as in the presence of other factors predisposing to urinary retention, caution is required, because Cetirizine may increase the risk of urinary retention.

Caution is recommended when using cetirizine concomitantly with ethanol, although no clinically significant interaction with ethanol was observed at therapeutic doses (at a blood ethanol concentration of 0.5 g/l). Caution should be exercised in patients with epilepsy and increased convulsive readiness.

Before prescribing allergy tests, a three-day “washing out” period is recommended due to the fact that H1-histamine receptor blockers inhibit the development of skin allergic reactions.

Influence on the ability to drive vehicles and machinery. An objective assessment of the ability to drive vehicles and operate machinery did not reliably reveal any adverse events when using cetirizine at the recommended dose. However, for patients with symptoms of drowsiness while taking cetirizine, it is advisable to refrain from driving a car, engaging in potentially hazardous activities, or operating machinery that require increased concentration and speed of psychomotor reactions.

Interactions with other active ingredients

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