Montelukast

Chemical name

1-[[[(R)-M-[(E)-2-(7-Хлор-2-хино лил)винил]-альфа-[O-(1-ги дрокси-1-метилэтил)фен етил]бензил]тио]метил] циклопропануксусная acid (as sodium salt)

Gross

C35-H36-Cl-N-O3-S

Of drugs

The drugs-bronhodilatirtee. Yes lakotrienove blocks receptors. Specific ingibiruet Cyslt_1-retseptora zisteinilovykh lakotrienov (LT C_4, D_4 and E_4), the most powerful mediators persistirutego chronic inflammation supporting giperreaguosti hospital with bronchial Astme.pri ingestion quickly and adequately absorbed : C_max achieved in 2-3 hours Bioavailability of 64-73%. In the blood of 99% is associated with malnutrition. Metabolised in the liver. Write mainly jelchew. Plasma Cl is 45 ml / Min.umenishaet severity acute smooth muscles bronhiol and receptacles, oedema, migration Eosinophils and macrophages; Reduces mucus secretion and improves mukotiliarnyi transport. Vsokoakteven with ingestion. Bronchodilatory effect developing in a single day and continuously maintained. Effective in patients with easy persistent asthma is not controlled only bronhodilatatormi.

Indications

Bronchial asthma (baseline therapy with light gravity, prevention of asthma symptoms during the day and at night as well as bronhospasticeskih reactions caused by the physical force), including : in patients sensitive to aspirin.

Contraindications

Hypersensitivity, pregnancy, breast-feeding (at the end of treatment), children's age (up to 6 years).

Side-Effects

Pain in the abdomen, nausea, headache, grippopodobnyy syndrome, cough, sinusit, pharyngitis, raising transaminaz.

Patient interaction

Compatible with glukokortikoidami (additive effect). Phenobarbital by 40% reduces the AUC.

Precautions

There is a need for clarity in the treatment. Continued reception and after significant improvement. It should not be used for short-acute asthma attacks (not a substitute for inhaled bronhodilatatorov); When the therapeutic effect (usually after the first dose), the number of inhalations bronhodilatatorov during the day could be reduced.

Dosing and Administration

Inside. Adults and children over 15 years of age-1 table. (10 mg) for the night (at night); children 6-14 years - 1 table. chewable (5 mg) in the evening (at night).

Literature

1. Knorr B., J. Matz, J. Bernstein et al. Montelukast for chronic asthma in 6-to old children : a randomized, double-blind trial / / JAMA 1998 .- .- V. 279-N-15 P. 1181-1186.2. Lepeleire I., F. Reiss, Rochette F. et al. Montelukast causes prolonged, potent leukotriene D4-receptor antagonism in the airways of patients with asthma / / Clin. Pharmacol. Ther-1997 .- V. 61 .- P. 83-92.3. Reiss T., A. Sorkness, Stricker W. et al. Effects of montelukast (MK-0476), a potent cysteinyl leukotriene receptor antagonist, on bronchodilation in asthmatic subjects treated with and without inhaled corticosteroids / / Thorax 1997 .- .- V. 52-N-1 P. 45-48.

Directory → Intermedianta → Prostaglandins, tromboksana, lakotriena and their antagonists → Montelukast