Zafirlukast

When ATH:
R03DC01

Characteristic.

White or pale yellow amorphous powder, practically insoluble in water, slightly soluble in methanol and slightly soluble in tetrahydrofuran, dimethyl sulfoxide and acetone.

Pharmacological action.
Anti-inflammatory, antiasthmatic, warning bronchospasm.

Application.

Bronchial asthma mild to moderate severity (prevention of attacks and supportive therapy), incl. after failure of beta-stimulants.

Contraindications.

Hypersensitivity, hepatic failure, cirrhosis of the liver, Children up to age 5 years (Safety and efficacy have not been determined).

Pregnancy and breast-feeding.

When pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus.

Category actions on the fetus by the FDA — B. (The study of reproduction in animals revealed no risk of adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not done.)

At the time of treatment should stop breastfeeding.

Side effects.

From the nervous system and sensory organs: insomnia, headache, weakness.

Cardio-vascular system and blood (hematopoiesis, hemostasis): редко — гематомы при ушибах, bleeding, incl. hypermenorrhea, thrombocytopenia; очень редко — агранулоцитоз.

From the digestive tract: nausea, vomiting, abdominal pain; редко — симптоматический гепатит, incl. with hyperbilirubinemia, hyperbilirubinemia without an increase in liver transaminases; очень редко — печеночная недостаточность и фульминантный гепатит.

On the part of the musculoskeletal system: seldom-artralgia, myalgia.

For the skin: skin rash (incl. vesicular), itchy skin.

Allergic reactions: hives; rarely, angioneurotic edema.

Other: increased frequency of infections in elderly patients (7,8%).

Cooperation.

The concentration in the plasma increases zafirlukast (in 1,5 times) acetylsalicylic acid, снижают — эритромицин (on 40%) and theophylline (about 30%). The combination with warfarin prolong prothrombin time 35%. At smoking patients may increase the clearance of zafirlukast on 20%.

Dosing and Administration.

Inside, for 1 hours before meals or 2 hours after meals; adults and children over 12 years - 20 mg 2 once a day (to 80 mg per day 2 admission). Детям 5–11 лет — по 10 mg 2 once a day.

Precautions.

You can not apply for the relief of bronchospasm. Do not assign the human liver.

To achieve the effect of therapy should be constant, long and continued during exacerbations. Abrupt withdrawal or reduction of the dose of oral corticosteroids during the transition to zafirlukast therapy in severe asthma can cause eosinophilic infiltration with evidence of systemic vasculitis (Churg-Strauss syndrome).

Increased serum transaminases usually transient and asymptomatic, but it could be an early sign of hepatotoxicity. In case of clinical signs or symptoms of, indicating liver dysfunction, necessary to investigate the activity of serum transaminases (particularly ALT). The decision to terminate the reception should be taken individually. Patients, which zafirlukast it was canceled due to hepatotoxicity, the development of which was not related to any other cause, reappointment is contraindicated. When concomitantly with warfarin is recommended to control the prothrombin time.