Cetirizine

Cetirizine is a blocker drug for the histamine H1 receptor. It is effective at an early stage of development of allergic manifestations, and also reduces the number of released allergic conductors. The medicine is used to eliminate various types of allergies.

[1], [2], [3], [4]

Indications of the cetirizine

It is used to eliminate the following types of pathologies:

• Pollinosis;
• an allergic form of the cold;
• dermatitis;
• conjunctivitis;
• angioedema and urticaria.

[5], [6]

Release form

The release is carried out in tablets, on a blister for 10 pieces. Inside the package - 1-2 blister plates.

Cetirizine hexal

Cetirizine hexal is an antihistamine drug for systemic use. Produced in the form of an oral solution.

Cetirizine-astropharm

Cetirizine-astropharm is an antihistamine drug of general action, a piperazine derivative.

Cetirizine-Norton

Cetirizine-norton is used to eliminate the symptoms of seasonal allergic rhinitis or its chronic form, as well as the chronic form of hives of idiopathic type.

[7], [8], [9]

Pharmacodynamics

Cetirizine is a product of the breakdown of hydroxysin within the human body. It is a powerful selective antagonist of peripheral H1 endings. During the synthesis with the receptors, in vitro studies there was no relationship to other endings that differ from the H1 receptors.

In addition to the antagonistic effect on the H1 receptors, the substance has anti-allergic properties. In the case of drug administration at a dose of 10 mg once or twice per day, it slows the last stage of involvement of inflammatory cells (especially eosinophils) in the process of spreading the conjunctiva and skin of people who have been injected with antigen. At a daily dose of 30 mg, the drug slows the flow of eosinophils together with the bronchoalveolar fluid during the late stage of bronchoconstriction, which occurs when the allergen is inhaled by a person suffering from bronchial asthma.

Also, cetirizine slows the late stage of the inflammatory reaction caused by intradermal injection of kallikrein to people with chronic urticaria. At the same time, it reduces the strength of molecular adhesion (ICAM-1 elements, as well as VCAM-1, which act as markers provoked by an allergy of inflammation).

There is evidence that drugs at doses of 5 and 10 mg can slow the appearance of redness and vesicles that result from an excessively high histamine score in the skin. With a single use of 10 mg of medication, the effect begins after 20 minutes / 1 hour. The effect of its use lasts not less than 24 hours with a single reception.

There is information that in children 5-12 years old there is no tolerance for antihistaminic properties of Cetirizine (oppression of the development of redness and vesicles). After completion of the re-treatment with cetirizine, the normal skin reaction to histamine is restored in about 3 days.

For people with an allergic form of the common cold and concomitant bronchial asthma (moderate or moderate severity), taking 10 mg once a day helped improve the condition with evidence of a runny nose without affecting the lung function. These data confirm the safety of the use of drugs for bronchial asthma of moderate or mild severity.

There is evidence that the use of large daily doses of cetirizine (60 mg) did not induce a significant prolongation of the QT-interval.

Taking the medicine at the recommended dose improves the health of people with a seasonal or year-round allergic rhinitis.

[10], [11], [12],

Pharmacokinetics

The peak equilibrium level of the substance inside the plasma is almost 300 ng / ml, and the achievement of this index requires about 1 ± 0.5 hours. Accumulation of the substance in the case of drug use in the amount of 10 mg in the period of 10 days did not occur.

The amount of absorption of the substance does not decrease in the case of combined reception with food, but at the same time its speed decreases. The volumes of bioavailability indices are similar when using a substance in the form of capsules, solution or tablets. Visible distribution volume is 0.5 l / kg. The synthesis of a substance with plasma proteins is 93 ± 0.3%. In this case, cetirizine does not affect the synthesis of warfarin with a blood protein.

The substance is not subjected to extensive metabolism during the first hepatic transit. About 2/3 of the dose is excreted in the urine unchanged. The final half-life is approximately 10 hours. Cetirizine has a linear pharmacokinetics when used at a dose of 5-60 mg.

[13], [14], [15], [16], [17], [18]

Dosing and administration

Adolescents from 12 years old, as well as adults, need to take drugs at a rate of 10 mg once a day with dinner or twice a day (in the morning and in the evening) for 5 mg. For children 2-6 years of age, the dose is 5 mg (or 10 drops) once a day, or 2.5 mg (or 5 drops) twice a day (in the morning and in the evening).

People with kidney failure need to take half the standard dose.

[24], [25], [26], [27], [28]

Use of the cetirizine during pregnancy

Do not take during pregnancy.

Due to the fact that Cetirizine passes into the mother's milk, it can not be administered during lactation.

Contraindications

Among the contraindications:

• intolerance to cetirizine, hydroxyzine, and other elements of the drug;
• reduced renal function (CC level within 30-49 ml / minute);
• kidney failure in chronic form;
• children under 6 years of age.

[19], [20]

Side effects of the cetirizine

Often, Cetirizine is tolerated fairly well. Side effects develop from time to time and are short-lived. Main manifestations:

• reactions of the organs of the digestive system: dyspeptic phenomena and dryness of the oral mucosa;
• manifestations from the NA: headaches, migraines, dizziness, a feeling of excitement, drowsiness or fatigue;
• allergic manifestations: skin rash, Quincke edema, hives and itching.

[21], [22], [23]

Overdose

After a one-time use of drugs in the amount of 50 mg, signs of overdose develop: a feeling of drowsiness, severe irritability or anxiety, and in addition constipation, dry mouth mucosal and delayed urination.

To eliminate the disorders will require gastric lavage and treatment aimed at getting rid of the symptoms. There is no specific antidote. The procedure of hemodialysis will be ineffective.

[29], [30]

Interactions with other drugs

Combined use with theophylline (in a daily dose of 400 mg) causes a decrease in the level of the overall cleavage rate of cetirizine (the theophylline properties do not change).

Myelotoxic drugs increase the hematotoxic effect of the drug.

[31], [32], [33], [34], [35]

Storage conditions

Cetirizine is required to be kept in a place that is closed from sunlight and penetration of moisture, inaccessible to children. Temperature conditions - no more than 25ºС.

[36], [37], [38]

Shelf life

Cetirizine is suitable for use in the period of 2 years since the release of tablets.

[39], [40]