Fexofenadine

Chemical name

({+})-4-[1-Гидрокси-4-[4-(гид роксидифенилметил)-1-п иперидинил)бутил]-аль��а,альфа-диметилбензо��уксусная acid (and as hydrochloride)

Gross

C32-H39-N-O4

Characteristics

White or colourless crystalline powder. Easily soluble in methanol and ethanol, poorly soluble in chloroform and water, nerastvorim in hexane.

Of drugs

The drugs-antigistaminnoe, противоаллергическое . Yes blocks peripheral gistaminove H_1-retseptora, stabilize membranes fat cells from releasing gistamina. Alleviate symptoms of allergy : sneeze, rinoreu, itchy, red eyes and slezotechenie. Antigistaminny effect manifests itself after one hour after administration, reaches a maximum of 2-3 hours and lasts for 12 hours or more. During the 28 days of continuous use there has been the development of tolerance. Has no holino- and adrainoliticski, sedative action. Without a change of calcium and potassium channels, QT interval. Ingibiruet bronhospazm caused gistaminom Zivotnykh.in in vitro diminishes the basal expression of adhesion molecules on the epithelium cells kongyunctiv rights and discourage migration fight a hotbed of inflammation. Suppress the spontaneous interleikina-6 from the fibroblasts, inducyrovannuu activated eozinofilami liberatiou interleikina-8, гранулоцито-макрофаг��льного �олониестимулирующег�� factor and soluble adhesion molecules from BX3000T epithelium cells derived from patients with seasonal allergic Rinitom.v experimental studies have been found carcinogenic, and mutagennogo tertogennogo action. When used in the dose of 150 mg / kg and above noted dozozawisimoe decrease in the number of implantology, an increase in the frequency of death postimplantatini fruit, reducing body weight and survival of progeny Kras.bystro and completely absorbed in the digestive tract. C_max plasma through the 2.6 h after administration. Linking plasma proteins (mostly with albuminami and альфа_1-гликопротеина��и) is 60-70%. The average concentration in the plasma of healthy subjects after a single destination inside the dose of 60 mg-209 ng / ml, the equilibrium level after repeated reception - 286 ng / J Once admitted, doses of 120 mg / day and 180 mg / day once C_max 427 ng / ml and 494 ng / ml, respectively. Pharmacokinetics almost linear in the daily admission to the range of doses of 40-240 mg. It permeates through the GEB, secretiruetsa in breast milk. AUC - 1521 µ g / l / h, T_1/2, 14.4 hours Cl - 3.4 ml / min / kg Weak (5%) metabolised, presented with faeces (80%) and urine (11%). In patients 65 and older T_1/2 does not change, the concentration in the blood increases, but that did not affect the portability of the preparation. Against the backdrop of the kidney and kidney C_max rising and T_1/2 longer. Pharmacokinetic parameters feksofenadina in patients with liver diseases vary slightly.

Indications

Allergic rhinitis (vazomotornyi, seasonal), pollinoz, angioneuroticeski swelling, urticaria.

Restrictions on the use of

Pregnancy, breast-feeding.

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus and newborn.

Contraindications

Hypersensitivity, child before age 12 years (safety and efficiency to be determined).

Patient interaction

Erythromycin and ketokonazol increase in the plasma (the frequency of side effects does not change). Antatsida containing aluminum or magnesium hydroxide reduce the bioavailability (with the necessary skills interval of at least 2 h). Compatible with omeprazolom. It reinforces the effect of alcohol on the central nervous system.

Overdosing

Symptoms : dizziness, drowsiness, dry Rtu.lechenie : washing stomach, the appointment of activated carbon laxatives funds symptomatic and supportive therapy. Haemodialysis ineffective.

Precautions

To use caution if there is a violation of the functions of the liver. During treatment before the patient allowed to work, requiring more concentration and psychomotor speed reactions (driving vehicles work with), you should check the individual responses.

Dosing and Administration

Inside, 60 mg twice a day (patients with reduced kidney function 1x); In the seasonal allergicescom rinite-120 mg once a day, and chronic idiopathic krapiwnice-180 mg once a day.

Literature

1. A. Markham, A. Wagstaff Feksofenadin / / Mountain. pharmacology and therapy .- 1999 .- T. 8 .- N 2 .- C. 72-75.2. J. Mason, R. Reynolds, N. Rao The systemic safety of fexofenadine HCl / / Clin. Exp. Allergy-1999 .- V. 29 (suppl.3) .- P. 163-170; discussion 171-173.3. J. Slater, D. Zechnich, Haxby D. Second-antihistamines. A comparative review / / Drugs - 1999 .- V. 57-N-1 P. 31-47.

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