Description of the medicine: Zafirlukast
N-o-4- (5-Cyclopentyloxycarbonylamino-1-methylindol-3-ylmethyl) -3-methoxy-3-tolylsulfonylbenzamide.
Synonym: Acolate, Acolate.
White or pale yellow amorphous powder. Virtually nerastvorim in water, easily soluble in dimethylsulfoxide, acetone and tetrahydrofuran.
The synthetic preparation is an selective blocker of leukotriene receptors (it has no significant effect on prostaglandin, thromboxane, histamine, and cholinergic receptors). It interferes with the increase of vascular permeability and penetration of eosinophils into the respiratory tract caused by the most active pro-inflammatory and bronchospastic peptidic leukotrienes (LTS 4 , LTD 4 , LTE 4 ); Reduces the content of cellular and extracellular factors of the inflammatory reaction in the airways, induced by antibodies.
The drug prevents or reduces bronchospasm caused by various types of provocation; Physical activity, cold air, various antibodies (pollen of plants, etc.).
After ingestion quickly and completely absorbed, C max is 3 hours; T S is 10 hours; Is subjected to intensive biotransformation, is excreted by the kidneys.
Prescribe for the prevention of asthma attacks and maintenance therapy, including after relief of attacks with β-adrenergic receptor stimulants. When using the drug, the need for β-adrenostimulants may decrease.
Apply inside (to avoid deterioration of absorption should not be taken with food).
Adults are prescribed, starting with 0.02 g (1 tablet), 2 times a day. The usual maintenance dose is later also 1 tablet 2 times a day. They take the drug for a long time (as a prophylactic). If necessary (insufficient effect), the dose is gradually increased to 0.08 g 2 times a day (maximum dose).
The drug is usually well tolerated. Possible headache, vomiting, pain in the abdomen, allergic reactions.
If any hypersensitivity to the drug is detected, it will be discontinued. Do not prescribe zafirlukast (in the absence of vital necessity) to pregnant and lactating mothers. Safety of the drug for children under the age of 12 years has not yet been established.
Like other newly introduced drugs, zafirlukast should be used under close medical supervision.
Form release: tablets of 0.02 and 0.04 g (20 and 40 mg) (N. 14, 28, 56).
Storage: List B.