Zafirlukast

Chemical name

4-(5-Циклопентилоксика��бониламино-1-метилинд ол-3-илметил)-3-метокси- N-о-толтилсульфонилбе��замид

Gross

C31-H33-N3-O6-S

Characteristics

White daffodil or amorphous powder nerastvorim almost in the water, slightly soluble in methanol, and slightly soluble in tetragidrofurane, demetilsulfoxide and acetone.

Of drugs

Drugs, the anti-inflammatory, protiwastmaticescoe (bronhospazm warning). Competitive lakotrienove blocking receptors and reducing warns smooth muscles bronchus by the lakotrienov - LTC_4, LTD_4 and Lte_4.posle intake of rats slow and inadequate. Admission food reduces the bioavailability of 40%. C_max is about 3 hours The equilibrium concentration in the plasma is proportional to dose and projected on the basis of the calculation farmakokineticeskih parameters defined by a single admission. At the systemic blood circulation-related (99%) with albuminami form. Penetrates into tissues and organs. T_1/2-about 10 hours Extensive metabolised. Metabolites and neizmenenny zafirlukast excretiruyutza with breast milk and urine (approximately 10%) and faeces (89%). Prevents action inflammation mediators, reduces cellular and necletocny of inflammation, lowers blood pressure, swelling, the influx of Eosinophils to light, products superoksidov alveolarnami macrofagami. Improves the lungs.

Indications

Bronchial asthma (asthma prevention and maintenance therapy), including : in beta-stimulatorov inefficiency.

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

Hypersensitivity, child before age 12 years (the safety and effectiveness of the children are not identified).

Side-Effects

Headache, a breach of the blood, allergic reactions (urticaria, angioneuroticeski swelling), rash (including vezikuliarnuu), rarely swelling lower limbs, artralgia, mialgia, symptomatic infections, bleeding, bruises education with fractures, agranulozitos to respiratory tract infections in elderly patients, raising whey transaminaz, giperbilirubinemia.

Patient interaction

Zafirlukasta concentration in plasma increases (1.5 times) acetylsalicylic acid-reducing erythromycin (40%) and theofillin (approximately 30%). Combining with varfarinom prolong protrombinovoe time by 35%.

Precautions

It used to heavily bronchoconstriction. There are encouraged to nominate the human liver.

Dosing and Administration

Inside, for one hour before meals or two hours after eating; Adults and children over 12 years to 20 mg twice a day (up to 80 mg / day in 2 admission).

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