Astemizole

Chemical name

1-[(4-Фторфенил)метил]-N-[ 1-[2-(4-метоксифенил)эти��]-4-пиперидинил]-1H- benzimidazol-2-amin

Gross

C28-H31-F-N4-O

Characteristics

White or belovaty powder. Nerastvorim water poorly soluble in ethanol, it is readily soluble in chloroform and methanol.

Of drugs

The drugs-protiwallergicescoe, antigistaminnoe. Does gistaminove H_1-retseptora. Ters bronhospazm caused by the physical stress and giperventilaciei lungs. Effects develops over 24 hours (sometimes 2-3 days), and reaches a maximum at 12 days. The effect depends on the duration of prior therapy (suppression of skin samples can be retained in a few weeks after admission). And weak antiserotoninova activity. Virtually no sedative action (not a GEB) is not more deprimiruty effect of ethanol or other means oppressive ZNS.V pilot studies had revealed mutagennogo and cancer-causing. When a rat dose 100 times greater than that recommended for humans toxic effect on the mother's body and the embryo. In rats and rabbits at doses 50 times higher than recommended for a person who does not have teratogenic effects, and does not alter fertility in males and Samok.posle intake of rapidly absorbed. C_max registered within 1 h. Away 60% reduction in skin and lengthens the time C_max at 1 pm Linking protein is 96%. Almost completely metabolized in the liver (also for "first pass"), with the participation of CYP3A4 izofermenta of cytochromes R450 with the formation of the active-metabolita desmetilastemizola, C_max is in the blood is achieved through 1hr Nash total concentration (astemizola and its active metabolita) in the blood of 3-5 ng / ml and a for 4-6 weeks. Excreted mainly jelchew of metabolites (73%) and partly with the urine (05-06%). T_1/2 astemizola-1 day, the volume of 250 l / kg, Cl-11 ml / min / kg Depth (astemizol + gidrauxilirovanne metabolites dwuhfazno : T_1/2 phase for the 20-hour, for a phase-out 7-11 days (in multiples of 7-9 days and 19 days respectively). According to data metabolites can remain in the body up to 4 months. Penetrates into milk lactoiruth dogs.

Indications

Allergic rhinitis (seasonal and year-round), allergic conjunctivitis, allergic skin reaction (chronic idiopathic urticaria, etc.), skin itching, swelling angioneuroticeski (treatment and prevention), bronchial asthma (secondary treatment).

Restrictions on the use of

Extension QT interval on the ECG, gipokaliemia expressed by the human liver.

Pregnancy and lactation

Contraindicated. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, pregnancy, breast-feeding a young child (up to 2 years).

Side-Effects

From the nervous system and sensory organs : weakness, headache, drowsiness, and in some cases, dizziness, nervousness, mood disorders, insomnia, nightmares, paresthesia, convulsions, rarely depression, Kongunguit.so the circulatory system : gipotenzia, rapid heartbeat, high-dose jeludockove adults, violations of blood (fatigue or weakness, sore throat increased body temperature, bleeding or hemorrhage). For part of the intestine : dry mouth, increased appetite, nausea, stomachache, diarrhea, and rarely are the increase in the liver transaminaz, �епатит.Аллергические �ection : rarely rashes, itching, swelling angioneuroticeski, bronhospazm, anaphylactoidnye Reaktion.prochie : photosensitization, the increase in body mass index (in the case of a long reception), mialgia, artralgia rarely-pharyngitis.

Specific guidance

The halt to the use of not less than four weeks before the skin test for allergens.

Patient interaction

Imidazole fungicidal funds (ketokonazol, intrakonazol, miconazole, etc.), makrolida (erythromycin, klaritromicin, troleandomitin), metronidazole, quinine, mibefradil lower speed biotransformation. Not recommended combined with inhibitors of HIV protease inhibitors and reverse takeover serotonin. Preparations udlinate QT interval (antiaritmicescie means terfenadin, Tricyclic antidepressants, fenotiazina, blockers calcium channels, and so on), potenziruut cardiotoksicnosti. Can mask ototoksicescoe the other drugs. Do side effects фотосенсибилизирующи х funds.

Overdosing

Symptoms : jeludockove adults, sinkope, convulsions, cardiac arrest or Dahania.lechenie : induction vomiting, stomach wash, reception activated carbon plant laxatives; ECG monitoring, symptomatic and supportive therapy, if necessary, in / in a liquid, the appointment of complications preparations not udlinath QT interval, gipertenziveh funds (a sports and analeptikov not recommended), oxygen. Haemodialysis ineffective.

Precautions

Is not recommended at the same time take grapefruit juice (ingibiruet metabolism and increases the concentration in the blood). Be wary appoint patients with kidney disease, impaired electro exchange (gipokaliemia, gipomagniemia) receiving nekalisberegate dioretiki. Patients with diseases divisions lower respiratory tract should be warned of the potential effects holinoliticakih (dry mucous membranes). Be wary of the treatment of patients who require more attention and speed of physical and mental reactions.

Dosing and Administration

Prandial inside, every day. Adults and children over the age of 12 years, 10 mg, for children aged between six and 12 to 5 mg in the form of tablets or suspension, and 6-2 mgu/10 kg body weight in the form of suspension. The maximum duration of treatment seven days.

Literature

J. Slater, D. Zechnich, Haxby D. Second-antihistamines. A comparative review / / Drugs - 1999 .- V. 57-N-1 P. 31-47.

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