Fluticasone + Salmeterol information from DrugsUpdate
P - Caution when used during pregnancy
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.
Pharmacodynamics
Pharmacokinetics
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.
Onset
Bronchodilation: 10-20 minutes.
Duration
Bronchodilation: 12 hours
Absorption
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).
Distribution
Salmeterol: Protein binding: 96%. Fluticasone: Protein binding: 91%.
Metabolism
Salmeterol: Extensive hepatic metabolism by hydroxylation; terminal elimination half-lives: 5.5 hours. Fluticasone: Extensive first-pass metabolism by cytochrome CYP3A4.
Excretion
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.
Fluticasone + Salmeterol Indications / Fluticasone + Salmeterol Uses
Information Not Available
Fluticasone + Salmeterol Adverse Reactions / Fluticasone + Salmeterol Side Effects
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.
Precautions
Warnings
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.
Monitor
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.
Special Precautions
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.
Other Drug Interactions
Increased fluticasone levels with CYP 3A4 inhibitors e.g ritonavir, ketoconazole, itraconazole. Additive effects with other β-agonist.
Other Interactions
Information Not Available
Dosage
Inhalation
Asthma
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.
Inhalation
Chronic obstructive pulmonary disease
Adult: As combination containing salmeterol 50 mcg and fluticasone propionate 500 mcg/dose of inhalation powder: 1 inhalation bid.
Food(before/after)
Information Not Available
List of Contraindications
Fluticasone + Salmeterol and Pregnancy
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.
Fluticasone + Salmeterol and Lactation
Caution when used during lactation
Fluticasone + Salmeterol and Children
Advair Diskus
Safety and efficacy not established in children with asthma younger than 4 years of age.
Advair HFA
Safety and efficacy not established in children younger than 12 years of age.
Fluticasone + Salmeterol and Geriatic
Use with caution in elderly patients who have concurrent CV disease.
Fluticasone + Salmeterol and Other Contraindications
Not for primary treatment of status asthmaticus or other acute attacks of asthma.
Storage
Inhalation
Do not store >30 °C.
Lab interference
Inhalation
Do not store >30 °C.
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