ADVAIR DISKUS ADVAIR - GlaxoSmithKline

trauma, surgery or infection or any rapid reduction in dosage. Patients receiving higher
than approved dosages should be managed closely and the dose reduced gradually.
For management of a suspected drug overdose, contact your regional Poison Control
Centre.
ACTION AND CLINICAL PHARMACOLOGY
Mechanism Of Action
ADVAIR ® (salmeterol xinafoate/fluticasone propionate) contains salmeterol xinafoate
and fluticasone propionate which have differing modes of action for the treatment of
COPD and asthma (in patients with reversible obstructive airways disease). Salmeterol is
a long-acting bronchodilator that prevents breakthrough symptoms of wheezing and chest
tightness; fluticasone propionate is an inhaled anti-inflammatory agent that reduces
airways irritability. ADVAIR ® can offer a more convenient regime for patients requiring
concurrent long-acting beta 2 -agonists and inhaled corticosteroid therapy. ADVAIR ® is
designed to produce a greater improvement in pulmonary function and symptom control
than either fluticasone propionate or salmeterol used alone at their recommended
dosages. The respective mechanisms of action of both drugs are discussed below:
Salmeterol is a selective, long-acting (12 hours), slow onset (10-20 minutes) beta 2 -
adrenoceptor agonist with a long side-chain which binds to the exo-site of the receptor.
Salmeterol offers more effective protection against histamine-induced
bronchoconstriction and produces a longer duration of bronchodilation, lasting for at least
12 hours, than recommended doses of conventional rapid onset, short duration beta 2 -
agonists.
In vitro tests on human lung, have shown that salmeterol is a potent and long-lasting
inhibitor of the release of mast cell mediators, such as histamine, leukotrienes and
prostaglandin D 2 .
In man, salmeterol inhibits the early and late phase response to inhaled allergen. The late
phase response is inhibited for over 30 hours after a single dose, when the bronchodilator
effect is no longer evident. The full clinical significance of these findings is not yet clear.
The mechanism is different from the anti-inflammatory effect of corticosteroids.
Fluticasone propionate is a highly potent glucocorticoid anti-inflammatory steroid. When
administered by inhalation at therapeutic dosages, it has a direct potent anti-inflammatory
action within the lungs, resulting in reduced symptoms and exacerbations of asthma, and
less adverse effects than systemically administered corticosteroids.
In comparisons with beclomethasone dipropionate, fluticasone propionate has
demonstrated greater topical potency.
July 29, 2014
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