Cetirizine

Chemical name

[2-[4-[(4-Хлорфенил)фенил��етил]-1-пиперазинил]эт окси]уксусная acid (and as hydrochloride)

Gross

C21-H25-Cl-N2-O3

Characteristics

Piperazine derivative. The white crystalline powder, soluble in water.

Of drugs

The drugs-antigistaminnoe, противоаллергическое . Yes blocks peripheral gistaminove H_1-retseptora weakens the gistamina receptacle, reduces hyperemia and edema. An unfinished skin reactions (blister and hyperemia) for the introduction gistamina specific allergens, cooling (in patients with cold krapiwnica). The effect is manifested within 1-2 h after administration, the duration of the blockade H_1-retseptorov reaches more than 24 hours in newborns and children up to two years - about 12 hours Restoring skin reactivity to gistaminu occurs within 3 days. Ease symptoms of allergic rinita (sneeze, cough, zalojennosti nose, itchy, slezotechenie). Dozozawisimo weakens гистамининдуцированн ую bronhokonstricciu in bronchial asthma light current. It stops the development of indirect gistaminom early phase allergen. Oppressing the mediators involved in the late phase of allergic reaction, migration Eosinophils, and Klebsiella bazofilov in response to a serum. Decreases the expression of adhesion molecules (ICAM-1, VCAM-1), wherein the other mediators and inducers secreta gistamina such as тромбоцит-активирующ��й factor and substance R. reducing turnover membranes Eosinophils, Klebsiella, and platelets from healthy volunteers and patients with seasonal allergic rhinitis. Application for a period of 7 days per dose, is six times higher than the daily treatment, has not been accompanied by changes in QT interval ECG and other signs cardiotoksicski action. In doses from 20 to 25 mg per day has no effect on the reaction time and concentration ability Vnimania.v experimental studies were reported mutagennogo actions and the impact on fertility. With the rats in the dose of 20 mg / kg / day for 2 years carcinogenic effect has been identified. The mice receiving dose of 16 mg / kg / day (5 times the MRDC) increased frequency of benign neoplasms of the liver. Appointment of mice during lactation by slower increases body mass index of Potomstwa.posle intake of rats rapidly and no less than 70%. C_max plasma (0.3 µ g / ml) is achieved within 1 hour with the appointment of the interior in the dose of 10 mg. Getting food is not affected by the completeness removals, but it can be lengthened T_max 1.7 h C_max reduced by 23%. Average C_max and AUC proportional to dose. Linking blood plasma proteins 93%. Stable level of plasma obtained 3 days after the start of the reception. After repeated use cetirizina concentration in the skin and serum equivalent. C_max Brain is not more than 10% of C_max plasma. The distribution-0.56 l / kg T_1/2 - 7-11 h after a single dose of 10 or 20 mg (for children 2-12 years T_1/2 shortened to 5-6 hours, the elderly-closure). Minimum metabolized in the liver with the formation of inactive metabolita and presented as unchanged to mostly kidneys. Within 24 h 60% of the dose appears in the urine, 10% from faeces. Cl-54 ml / min. Penetrates into breast milk. In 10-dnevnom application dose of 10 mg drug accumulation is not observed. According to the test oppression skin reaction (blister and hyperemia) for a / to the introduction gistamina with long-term use (up to 110 weeks) show of tolerance. If any of the kidneys (Cl creatinine below 71 ml / min) and in patients in gemodialise (Cl creatinine less than 7 ml / min) T_1/2 increases 3 times, Cl reduced by 70%. Against the backdrop of chronic liver disease and in older patients, there is an increase T_1/2 50% Cl decrease by 40%. The pharmacokinetics do not depend on sex and race.

Indications

Seasonal and year-round allergic rhinitis, pollinoz, allergic conjunctivitis, chronic idiopathic urticaria, skin itching, swelling angioneuroticeski; Integrated therapy atopic dermatitis, and chronic eczema, asthma.

Restrictions on the use of

Violation of the kidneys and liver, old age.

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, including gidroxizin, pregnancy, breast-feeding, child up to 2 years (up to 6 years if there is a violation of the kidney or liver).

Side-Effects

From the nervous system and sensory organs : sleepiness (14%), fatigue (6%), causing headache, dizziness, anxiety, nervousness, emotional lability, the concentration and thinking, insomnia, depression, euphoria sputannosti consciousness, amnesia, depersonalization, ataxy, the coordination of movements, tremor, giperkinez, convulsions gastrocnemius muscles, paresthesia, disfonia, mielit, paralysis ptoz violation ccomodation and vision pain in the eyes, glaucoma, xeroftalmia, conjunctivitis, bleeding in the eye, ototoksicnosti, noise in the ears, deafness, the feeling Zapaha.so part of the intestine : dry mouth (5%), change or lack of taste perception, increased appetite, anorexia, stomatitis (including Ulcerative), changing colors, and applied language, increase salivation, increased kariosnosti, thirst, nausea, neuralgia, saying, pain in the abdomen, bloating, diarrhea, constipation, gemorroy, melena, rektalnoe bleeding of the Pecheni.so the circulatory system : Migraine, it is rarely beat, hypertension, cardiac Nedostaternsti.so the respiratory system : rhinitis, active bleeding, nasal polyp, pharyngitis, cough, sinusit, bronchitis, increased bronchial secretions, bronhospazm, despnoe, infection with upper respiratory tract infections, pneumonia, Giperventilatia.so the urogenital system : delay urination, swelling, poliuria, dizuria, gematuria, infection urinary tract, anesthetic, the weakening Yeah, dismenorea, mejmenstrualnoe bleeding menorragia, Waginit.so the musculoskeletal system : artralgia, arthritis, arthrosis, mialgia, pain in the back, muscle Slabostj.so the skin : dry skin, rashes, bubbler skin, itching, skin, furunkoulez, dermatitis, eczema, giperkeratos, erythema, increased sweating, alopecia, angioneuroticeski swelling, gipertrihoz, photosensitization, Seborea.prochie : malaise, fever, chills, tides, dehydration, diabetes mellitus, limfadenopatia, pain in the milk glands, increased body mass index, skin allergies in t.c.rapiwnica.

Patient interaction

Theofillin slightly (to 16%) reduces klirens. Compatible with azithromycin, psevdoepinefrinom, ketokonazolom, eritromitinom, diazepam and zimetidine.

Overdosing

Symptoms : drowsiness, and possibly concern, the delay urination, tremor, tachycardia, itching, Sapi.lechenie : washing stomach, the appointment of activated carbon; Supportive and symptomatic therapy. Haemodialysis ineffective.

Precautions

Not recommended simultaneous application of oppressive central nervous system, and alcohol consumption. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside, adults and children over 6 years, 10 mg once a day or 5 mg twice a day. Patients with renal insufficiency, in the first quarter in gemodialise are advised to reduce the dose of 2 times. Children from 2 to 6 years of age is 2.5 mg once a day with a maximum daily dose of 5 mg (10 drops) once a day or 2.5 mg (5 drops) in the morning and evening. Children over 6 years in violation of the liver and kidneys to 5 mg / sut.

Literature

1. Androsov VN, Belostocka OI, NI streets Efficacy of "zirtek (Cetirizin) with chronic retidiviruta krapiwnice and seasonal allergicescom rinite / / Ter. archive-1994 .- T. 66-N-11 C. 68-72.2. Mileva J., M. Boykikieva, Stanev M. et al Clinical Research therapeutic effect drug cetirizin (zirtek, USB) in patients with allergic rhinitis / / immunology-1994-N-4 C. 33-34.

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