Fluticasone + Salmeterol information from DrugsUpdate
L - Caution when used during lactation
The combination preparation fluticasone/salmeterol is a formulation containing fluticasone propionate and salmeterol xinafoate used in the management of asthma and chronic obstructive pulmonary disease (COPD). It is marketed by GlaxoSmithKline as ForAir (India). Annual sales approx $3.8B. Patent expires 2010.
Fluticasone, a corticosteroid, is the anti-inflammatory component of the combination, while salmeterol treats constriction of the airways. Together, they relieve the symptoms of coughing, wheezing and shortness of breath better than either fluticasone or salmeterol taken on its own.
Salmeterol, a long acting β2-agonist which acts locally in the lung to mediate bronchodilation. Fluticasone, a corticosteroid with mainly glucocorticoid activity, reduce symptoms and exacerbations of asthma.
Bronchodilation: 10-20 minutes.
Bronchodilation: 12 hours
Salmeterol: Negligible absorption after inhalation. Fluticasone: Poorly absorbed from the GI tract; oral bioavailability <1%; absolute bioavailability of inhaled fluticasone: 5-11% (depending on device used).
Salmeterol: Protein binding: 96%. Fluticasone: Protein binding: 91%.
Salmeterol: Extensive hepatic metabolism by hydroxylation; terminal elimination half-lives: 5.5 hours. Fluticasone: Extensive first-pass metabolism by cytochrome CYP3A4.
Salmeterol: Eliminated mainly in faeces; negligible amounts of unchanged salmeterol are detectable in urine or faeces. Fluticasone: Mainly excreted in faeces as metabolites and unchanged drug; <5% excreted in urine.
Mouth and throat candidiasis, throat irritation, hoarseness/dysphonia, nasopharyngitis, lower respiratory tract infections (e.g. pneumonia and bronchitis), hypokalaemia, headache, tremors, palpitation, muscle cramps. Prolonged high dose use may cause Cushing's syndrome, Cushingoid features, adrenal suppression, retardation of growth in children and adolescents, bone mineral density decrease, cataract and glaucoma.
Potentially Fatal: Paradoxical bronchospasm.
Salmeterol may increase the risk of asthma-related death. Therefore, prescribe salmeterol or salmeterol-containing products only for patients not adequately controlled on other asthma-controller medications or whose disease severity clearly warrants initiation of treatment with salmeterol or salmeterol-containing products.
Frequently assess patient for response to treatment. Periodically review therapy in patient with COPD associated with chronic bronchitis for periods longer than 6 mo to assess the continuing benefits and potential risks of treatment. Observe patients for evidence of systemic corticosteroid effects.
Pulmonary TB, severe cardiovascular disorders, heart rhythm abnormalities, DM, thyrotoxicosis, hypokalaemia. Patients at risk of decreased bone mineral content (e.g. smoking, old age, sedentary lifestyle, poor nutrition, family history of osteoporosis or long term use of drugs that may decrease bone mass (e.g. anticonvulsants and corticosteroids). Do not stop therapy abruptly; therapy should be down titrated. Advise patient to rinse mouth after inhalation. Monitor height of children on prolonged therapy. Pregnancy, lactation.
Increased fluticasone levels with CYP 3A4 inhibitors e.g ritonavir, ketoconazole, itraconazole. Additive effects with other β-agonist.
Adult: As combination containing salmeterol 50 mcg and fluticasone propionate 100/250/500 mcg/dose of inhalation powder: 1 inhalation bid. As combination containing salmeterol 25 mcg and fluticasone propionate 50/125/250 mcg/dose of pressurised inhalation: 2 inhalation bid.
Child: 4-12 years: As combination containing salmeterol 50 mcg and fluticasone propionate 100 mcg/ dose of inhalation powder: 1 inhalation bid; as combination containing salmeterol 25 mcg and fluticasone propionate 50 mcg/dose of pressurised inhalation: 2 inhalation bid. ≥12 years: As combination containing salmeterol 50 mcg and fluticasone propionate 100/250/500 mcg/dose of inhalation powder: 1 inhalation bid; as combination containing salmeterol 50/125/250 mcg and fluticasone propionate 50 mcg/dose of pressurised inhalation: 2 inhalation bid.
Chronic obstructive pulmonary disease
Adult: As combination containing salmeterol 50 mcg and fluticasone propionate 500 mcg/dose of inhalation powder: 1 inhalation bid.
List of Contraindications
Caution when used during pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Caution when used during lactation
Safety and efficacy not established in children with asthma younger than 4 years of age.
Safety and efficacy not established in children younger than 12 years of age.
Use with caution in elderly patients who have concurrent CV disease.
Not for primary treatment of status asthmaticus or other acute attacks of asthma.
Do not store >30 °C.
Fluticasone + Salmeterol brands in India
Seroflo -100 Rotacaps
Seroflo 100 Multihaler
Seroflo 250 Multihaler
Seroflo 500 Multihaler
Vent SF Easecaps