Salmecort, aerosol 25 mcg+50 mcg/dose 120 doses

Salmecort is a combined bronchodilator (contains salmeterol and fluticasone propionate). Salmeterol is a selective agonist of beta2-adrenoreceptors with prolonged action (at least 12 hours).

Salmeterol molecule has a long side chain that binds to the outer domain of the receptor. Because of these pharmacological properties, salmeterol is more effective in preventing histamine-induced bronchospasm and causes more prolonged bronchodilation compared to conventional short-acting beta2-receptor agonists.

Effectively and long-lasting inhibits the release in lung tissues of mast cell mediators such as histamine, leukotrienes and PgD2. It suppresses early and late stage of allergic reaction; after administering a single dose bronchial hyperresponsiveness decreases, inhibition of the late stage persists for more than 30 hours after a single dose, when the bronchodilator effect is no longer.

Fluticasone propionate is a glucocorticosteroid (GCS) of local action. When administered by inhalation in recommended doses it produces evident anti-inflammatory and anti-allergic effect leading to reduction of symptoms and frequency of exacerbations of diseases accompanied by airway obstruction.

During long-term use of inhaled fluticasone propionate at maximum doses, daily and reserve secretion of adrenal cortex hormones remains within normal limits in adults and children. A residual decrease in reserve adrenal function may persist long after therapy.

Pharmacokinetics:
There is no evidence that co-administration of salmeterol and fluticasone propionate by inhalation affects the pharmacokinetics of either substance.

Salmeterol:After inhaled administration at therapeutic doses, very low concentrations of the drug in plasma (200 pg/ml or less) are produced. With regular use of inhaled salmeterol hydroxynaphthoic acid is determined in systemic blood flow in concentrations up to 100 ng/ml.

Fluticasone propionate: after inhalation relative bioavailability is from 10 to 30% depending on the drug delivery system. Systemic absorption occurs primarily in the lungs. Part of the inhaled dose may be swallowed, but its systemic effect is minimal due to the weak water solubility of the drug and intense metabolism during “first passage” through the liver.

The bioavailability of fluticasone when swallowed is less than 1%. There is a direct correlation between the magnitude of the inhaled dose and the systemic effect of fluticasone; the volume of distribution is about 300L. It is metabolized in the liver to an inactive metabolite involving CYP3A4 of the cytochrome P450 system. Less than 5% of the metabolite is excreted in the urine. Plasma clearance is 1.15 l/min. Elimination half-life T1/2 is about 8 hours.

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