Flutiair S 500

Composition

Each capsule contains :

Salmeterol Xinafoate BP

equivalent to Salmeterol 50 mcg

Fluticasone propionate BP 500 mcg

Excipients QS and Approved colours

used in capsule shell

Chemical Name-Fluticasone propionate : 6a,9-Difluoro-17- [[(fluoromethyl)sulphanyl]carbonyl]-11ß-    hydroxy-16a-methyl-3- oxoandrosta-1,4- dien-17a-yl propanoate.

Salmeterol xinafoate : (1RS)-1-[4-Hydroxy-3-(Hydroxymethyl)phenyl]-2-[[6-

(4- phenylbutoxy)hexyl]amino]ethanol 1- hydroxynaphthalene-2-carboxylate.

Category

A synthetic corticosteroid and a selective, long-acting beta -adrenergic receptor 2 agonist.

Description

Fluticasone propionate : Salmeterol and Fluticasone propionate powder for inhalation contains Fluticasone propionate, a glucocorticoid. It is white or almost white powder, practically insoluble in water, sparingly soluble in methylene chloride, slightly soluble in alcohol. Its molecular formula is C H F O S and representing 25 31 3 5 molecular weight 500.6.

Salmeterol xinafoate : Salmeterol and Fluticasone propionate powder for inhalation contains Salmeterol xinafoate, a beta – 2 adrenoceptor agonist. It is white or almost white powder, practically insoluble in water, soluble in methanol, slightly soluble in anhydrous ethanol. Its molecular formula is C H NO and representing molecular weight 36 45 7604.

PHARMACOLOGY

Mechanisms of Action:

Fluticasone: Corticosteroids inhibit mast cells, eosinophils, basophils, lymphocytes, macrophages, neutrophils, histamines, leukotrienes and cytokines that are involved in asthmatic response.

Fluticasone is a trifluorinated corticosteroid with potent anti-inflammatory activity, which may contribute to its efficacy in the treatment of asthma. Utilizing in vitro assays, fluticasone is found to be 18 times more potent than dexamethasone, 2 times that of beclomethasone, and three times that of budesonide.

Salmeterol: Salmeterol is a long-acting beta-agonit,which produces 2 bronchodilation and increases bronchial airflow.

Pharmacokinetics:

Time to reach peak plasma concentration is 1-2 hours for fluticasone and 5 minutes for

salmeterol.

The terminal half-life for fluticasone is 5.33 to 7.65 hours and the terminal half-life of

salmeterol is not reported.

Fluticasone is metabolized through CYP450 3A4, and

salmeterol is metabolized through hepatic hydroxylation.

Indications

Salmeterol and Fluticasone propionate powder for inhalation is indicated in the regular treatment of asthma, where use of a combination (long-acting beta -agonist and 2 Inhaled corticosteroid) has been found to be appropriate and in patients with severe Chronic Obstructive Pulmonary Disease (COPD).

Contraindications:

Salmeterol and Fluticasone propionate is contraindicated in the primary treatment of status asthmatics or other acute episodes of asthma where intensive measures are required.

Warnings and Precautions

Patients should be made aware that Salmeterol and Fluticasone propionate must be used daily for optimum benefit, even when asymptomatic. Salmeterol and Fluticasone propionate should not be used to treat acute asthma symptoms for which a fast and short-acting bronchodilator is required. Patients should be advised to have their relief medication available at all times.

As with all inhaled medication containing corticosteroids, Salmeterol and Fluticasone propionate should be administered with caution in patients with pulmonary tuberculosis.

Pregnancy

Pregnancy Category: Both fluticasone and salmeterol are in pregnancy category C.Use of Salmeterol and Fluticasone propionate in pregnancy should be considered only if the expected benefit to the mother is greater than any possible risk to the foetus. Lactation

Use of Salmeterol and Fluticasone propionate in women who are breastfeeding should only be considered if the expected benefit to the mother is greater than any possible risk to the child.

Drug Interactions

Even though plasma levels of Salmeterol and Fluticasone are very low, potential interactions with other substrates or inhibitors of CYP SA4 cannot be excluded. Both non-selective and selective betablockers should be avoided inpatients with asthma, unless there are compelling reasons or their use. Concomitant use of other beta-adrenergic containing drugs can have a potentially additive effect.

Side Effects

As Salmeterol and Fluticasone propionate contains salmeterol and fluticasone propionate, the type and severity of side effects associated with each of the compounds may be expected. There is no incidence of additional side effects following concurrent administration of the two compounds.

Side effects associated with Fluticasone propionate Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Hoarseness and candidiasis (thrush) may be relieved by gargling with water after use of salmeterol and fluticasone propionate. Symptomatic candidiasis can be treated with topical anti-fungal therapy while still continuing with salmeterol and fluticasone propionate. Cutaneous hypersensitivity reactions have been reported. Salmeterol xinafoate Tremor, palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac

arrhythmias muscle cramps and hypersensitivity reactions, including rash, oedema and angioedema may occur in some patients.

Dosage and Administration

Asthma:

Adults and adolescents 12 years and over

FLUTIAIR-S 500 One ihalation twice daily

FLUTIAIR-S 500 is not recommended for children under 4 years of age.

Overdose

The signs and symptoms of Salmeterol and fluticasone propionate overdose are tremor,headache and tachycardia. The preferred antidotes are cardioselective beta-blocking agents, which should be used with caution in patients with a history of bronchospasm. If higher than the recommended dosage is continued over prolonged periods, some degree of adrenal suppression may result. Monitoring of adrenal reserve may be necessary.

Presentation:

FLUTIAIR-S 500

Pack Size: 30 Caps in a Bottle.

Storage:

Store in a dry place below 30°C.

Keep out of reach of children.