Forair 250 DPI/Forair 500 DPI

Forair 250 DPI/Forair 500 DPI

salmeterol + fluticasone

Manufacturer:

Zydus Healthcare

Distributor:

Zydus Healthcare
Full Prescribing Info
Contents
Salmeterol xinafoate, fluticasone propionate.
Description
Forair 250 DPI: Each dry powder for inhalation contains: Salmeterol (as xinafoate) 50 mcg, Fluticasone propionate 250 mcg.
Forair 500 DPI: Each dry powder for inhalation contains: Salmeterol (as xinafoate) 50 mcg, Fluticasone propionate 500 mcg.
Action
Pharmacology: Pharmacodynamics: The combination represents 2 classes of medications (a synthetic corticosteroid and a selective, long-acting beta-adrenergic receptor agonist) that have different effects on clinical and physiological indices.
Salmeterol xinafoate: It is a long acting beta-2-adrenergic agonist. The pharmacologic effect of Salmeterol Xinafoate is part attributable to stimulation of intracellular adenylyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels caused relaxation of bronchial smooth muscle and inhibition of release mediators of immediate hypersensitivity from cells, especially from mast cells. In vitro tests show that salmeterol is a potent and long-lasting inhibitor of the release of mast cell mediator, such as histamine. leukotrienes and prostaglandin D2, from human lung. Salmeterol inhibits histamine-induced plasma protein extravasation and inhibits platelet-activating factor-induced eosinophil accumulation in the lungs of guinea pigs when administered by the inhaled route.
Fluticasone propionate: It is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. In vitro assays using human lung cytosol preparations have established fluticasone propionate as a human glucocorticosteroid receptor agonist with an affinity 18 times greater than dexamethasone, almost twice that of beclomethasone-17-monopropionate (BMP), the active metabolite of beclomethasone dipropionate and over 3 times that of budesonide. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to inhibit multiple cell types (e.g. mast cells, eosinophils. basophils, lymphocytes. macrophages and neutrophils) and mediator production or secretion (e.g. histamine, eicosanoids. leukotrienes and cytokines) involved in the asthmatic response. These anti-inflammatory actions of corticosteroids contribute to their efficacy in asthma. Inflammation is also a component in the pathogenesis of chronic obstructive pulmonary disease (COPD).
Pharmacokinetics: Salmeterol xinafoate: Salmeterol acts locally in the lung therefore plasma levels are not an indication of therapeutic effects. In addition, there are only limited data available on the pharmacokinetics of salmeterol because of the technical difficulty of assaying the drug in plasma due to the low plasma concentrations at therapeutic doses (approximately 200 picograms/mL or less) achieved after inhaled dosing.
After regular dosing with salmeterol xinafoate, hydroxynapthoic acid can be detected in the systemic circulation, reaching steady state concentrations of approximately 100 nanograms/mL.
These concentrations are up to 1000 fold lower than steady state levels observed in toxicity studies. No detrimental effects have been seen following long-term regular dosing (more than 12 months) in patients with airway obstruction.
Fluticasone propionate: Systemic absorption occurs mainly through the lungs and is initially rapid than prolonged. The remainder of the inhaled dose may be swallowed but contributes minimally to systemic exposure due to the low aqueous solubility and pre-systemic metabolism, resulting in oral bioavailability of less than 1%. There is a linear increase in systemic exposure with increasing inhaled dose. The disposition of fluticasone propionate is characterized by high plasma clearance (1150 mL/min), a large volume of distribution at steady state (approximately 300L) and a terminal half-life of approximately 8 hours. Plasma protein binding is moderately high (91%). Fluticasone propionate is cleared very rapidly from the systemic circulation, principally by metabolism to an inactive carboxylic acid metabolite, by the cytochrome P450 enzyme CYP3A4. The renal clearance of fluticasone propionate is negligible (<0.2%) and less than 5% as the metabolite. Care should be taken when co-administering known CYP3A4 inhibitors. as there is potential for increased systemic exposure to fluticasone propionate.
Indications/Uses
For the maintenance and treatment of mild. moderate and severe persistent asthma in patients more than 5 years of age and in patients with Chronic Obstructive Pulmonary Disease (COPD).
Dosage/Direction for Use
Adults and adolescents 12 years and above: 1 Inhalation of Salmeterol + Fluticasone Propionate 250 mcg or 500 mcg twice a day or as prescribed by the physician.
Chronic Obstructive Pulmonary Disease (COPD): 1 Inhalation twice a day of Salmeterol + Fluticasone Propionate 500 mcg or as prescribed by the physician.
Overdosage
The expected signs and symptoms of salmeterol overdosage are those typical of excessive beta2-adrenergic stimulation, including tremor, headache, tachycardia, increases in systolic blood pressure and hypokalemia. The preferred antidotes are cardioselective beta-blocking agents, which should be used with caution in patients with a history of bronchospasm. If salmeterol + fluticasone propionate therapy has to be withdrawn due to overdose of the beta agonist component of the drug, provision of appropriate replacement corticosteroid therapy should be considered. Acute inhalation of fluticasone propionate doses in excess of those approved may lead to temporary suppression of the hypothalamic-pituitary-adrenal axis.
This does not usually require emergency action as normal adrenal function typically recovers within a few days. If higher than approved doses of salmeterol + fluticasone propionate are continued over prolonged periods, significant adrenocortical suppression is possible. There have been features have included hypoglycemia associated with decreased consciousness and/or convulsions. Situations which could potentially trigger acute adrenal crisis include exposure to trauma, surgery, infection or any rapid reduction in the dosage of the inhaled fluticasone propionate component.
It is not recommended that patients receive higher than approved doses of salmeterol + fluticasone propionate. It is important to review therapy regularly and titrate down to the lowest approved dose at which effective control of disease is maintained.
Contraindications
Hypersensitivity to salmeterol and corticosteroid or its components, previous history of paradoxical bronchospasm.
Special Precautions
Avoid using salmeterol as sole agent for asthma control. Patients should be instructed to stop salmeterol when they have breakthrough asthma symptoms of acute asthma exacerbation and to shift to short acting selective B2 agonist. Avoid use during pregnancy.
Increasing use of short-acting bronchodilators to relieve symptoms indicates deterioration of control and patients should be reviewed by a physician. Sudden and progressive deterioration in control of asthma is potentially life-threatening and the patient should be reviewed by a physician.
Treatment with salmeterol + fluticasone propionate should not be stopped abruptly in patients with asthma due to risk of exacerbation, therapy should be titrated-down under physician supervision. For patients with Chronic Obstructive Pulmonary Disease (COPD), cessation of therapy may be associated with symptomatic decompensation and should be supervised by a physician.
Effects on Ability to drive and Use Machines: There have been no specific studies of the effects of Salmeterol + Fluticasone Propionate on the above activities, but the pharmacology of both drugs does not indicate any effect.
Use In Pregnancy & Lactation
Administration of drugs during pregnancy and lactation should only be considered if the expected benefit to the mother is greater than any possible risk to the fetus or child.
There is insufficient experience of the use of salmeterol xinafoate and fluticasone propionate in human pregnancy and lactation. Reproductive toxicity studies in animals. either with single drug or in combination, revealed the fetal effects expected at excessive systemic exposure levels of a potent beta2-adrenoreceptor agonist and glucocorticosteroid. Extensive clinical experience with drugs in these classes has revealed no evidence that the effects are relevant at therapeutic doses. Neither salmeterol xinafoate or fluticasone propionate have shown any potential for genetic toxicity.
Salmeterol and fluticasone propionate concentrations in plasma after inhaled therapeutic doses are very low and therefore concentrations in human breast milk are likely to be correspondingly low. This is supported by studies in lactating animals, in which low drug concentrations were measured in milk. There are no data available for human breast milk.
Adverse Reactions
Salmeterol may cause fine tremor of skeletal muscle (particularly the hands), palpitations. tachycardia, nervous tensions, headaches, peripheral vasodilation, and rarely muscle cramps. Inhalation causes fewer adverse drug reaction than systemic administration, and the more selective beta-2 agonist cause fewer adverse drug reaction than less selective beta agonist. Potentially serious hypokalemia has been reported after large doses. Hypersensitivity reactions have occurred, including paradoxical bronchospasm, angioedema, urticaria. hypotension, and collapse.
Fluticasone hypersensitivity reactions may occur. Eosinophilic conditions, including Churg-Strauss syndrome have been reported rarely, in most cases following a transfer from oral corticosteroid therapy. Inhalation administration of large amounts of fluticasone propionate may produce systemic effects also. The adverse effects of corticosteroid may result from unwanted mineralocorticoid or glucocorticoid actions, or from inhibition of the hypothalamic-pituitary-adrenal axis. Despite the fact that inhaled fluticasone is generally thought to lack systemic effects at therapeutic doses, a study in 25 healthy subjects indicated that fluticasone propionate as single inhaled doses of 250, 500 and 1000 mcg did produce a reduction in plasma cortisol, indicating suppression with fluticasone particularly at high doses and the effect may be more marked with repeated than with single doses.
Drug Interactions
Salmeterol and other beta-2 agonist with corticosteroids, diuretics, or xanthines increase the risk of hypokalemia, and monitoring potassium concentrations is recommended in severe asthma, where such combination therapy is the rule. For an outline of interactions associated with sympathomimetics in general.
Fluticasone concurrent use of barbiturates, carbamazepine, phenytoin. primidone, or rifampicin may enhance the metabolism and reduce the effects of systemic corticosteroids. Conversely, oral contraceptives or ritonavir may increase plasma concentrations of corticosteroids. Use of corticosteroids with potassium depleting diuretics, such as thiazides or furosemide may cause excessive potassium loss.
Caution For Usage
Direction for Use: 1. Remove the cap.
2. Steadily hold the base and open the Innohaler turning the mouthpiece counter clockwise (follow the direction of the arrow on the mouthpiece itself).
3. Introduce Innohaler DPI capsule into the loading chamber.
4. Close the mouthpiece turning it clockwise.
5. Thoroughly press the two buttons. keeping the Innohaler Device in vertical position.
6. Deeply breathe out.
Tilt head back. Introduce the mouthpiece into the mouth, close the lips (make sure no air is passing around the nozzle). Breathe in.
7. Try again if necessary until the capsule is completely empty.
8. After using, remove the empty capsule and close the Innohaler.
In case of powder residues, use a brush and periodically wash with water.
Storage
Store at temperatures not exceeding 30°C.
MIMS Class
Antiasthmatic & COPD Preparations
ATC Classification
R03AK06 - salmeterol and fluticasone ; Belongs to the class of adrenergics in combination with corticosteroids or other drugs, excluding anticholinergics. Used in the treatment of obstructive airway diseases.
Presentation/Packing
Forair 250 DPI: Inhalation powd cap (white to off-white flowing powd encapsulated in vegecap size #3 + Inhaler device) x 40's.
Forair 500 DPI: Inhalation powd cap (white to off-white flowing powd encapsulated in vegecap size #3 + Inhaler device) x 40's.
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