BEXIMCO PHARMACEUTICALS LTD.
SALMETEROL + FLUTICASONE PROPIONATE
This is indicated in the regular treatment of asthma where use of a combination product (long-acting 82-agonist and inhaled corticosteroid) is appropriate: patients not adequately controlled with inhaled corticosteroids and 'as needed' inhaled short acting 82-agonist or patients already adequately controlled on both inhaled corticosteroid and long-acting 82-agonist.
Long-acting selective 8-adrenoceptor stimulants, Respiratory corticosteroids
Salmeterol Xinafoate is a selective, long acting beta-2 agonist used in the treatment of asthma and other forms of diffuse airways obstruction. Fluticasone Propionate is a corticosteroid with mainly glucocorticoid activity. Fluticasone Propionate is stated to exert a topical effect on the lungs without systematic effects at usual dose. Salmeterol protects against symptoms, Fluticasone Propionate improves lung function and prevents exacerbations of the condition. This preparation can offer a more convenient regime for patients on concurrent 8-agonist and inhaled corticosteroid therapy. The respective mechanisms of action of both drugs are discussed below: Salmeterol: Salmeterol is a selective long-acting (12 hour) beta-2-adrenoceptor agonist with a long side chain which binds to the exo-site of the receptor. Fluticasone Propionate: Fluticasone Propionate given by inhalation at recommended doses has a potent glucocorticoid anti-inflammatory action within the lungs, resulting in reduced symptoms and exacerbaions of asthma, without the adverse effects observed when corticosteroids are administered systemically.
Inhalation Aerosol: Adults and adolescents 12 years and older: 2 puffs of 25 8g Salmeterol and 50 8g Fluticasone Propionate twice daily or 2 puffs of 25 8g Salmeterol and 125 8g Fluticasone Propionate twice daily or 2 puffs of 25 8g Salmeterol and 250 8g Fluticasone Propionate twice daily. Children (4-12 years): 2 puffs of 25 8g salmeterol and 50 8g Fluticasone Propionate twice daily. Inhalation Powder in Capsule (For Asthma): Adult and Adolescent (12 Years and Older): Salmeterol 50 8g & Fluticasone 100 8g or Salmeterol 50 8g & Fluticasone 250 8g twice daily (morning and evening, approximately 12 hours apart). The recommended starting dosages for Salmeterol 50 8g & Fluticasone 100 8g & Salmeterol 50 8g & Fluticasone 250 8g for patients aged 12 years and older are based upon patients asthma severity. The maximum recommended dosage is Salmeterol 50 8g & Fluticasone 500 8g twice daily. Pediatric Patients (4 to 11 Years): For patients with asthma who are not controlled on an inhaled corticosteroid, the dosage is Salmeterol 50 8g & Fluticasone 100 8g twice daily (morning and evening, approximately 12 hours apart). Inhalation Powder in Capsule (For COPD): Salmeterol 50 8g & Fluticasone 250 8g twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is advised. Inhalation Powder in Maxhaler (For Asthma): This is a moulded plastic device containing a foil strip with 60 regularly placed blisters containing pre-dispensed inhalation powder. Patients should be made aware that Maxhaler must be used daily for optimum benefit, even when asymptomatic. Adults and Adolescents (12 years and older)- 50/100 Maxhaler: One Inhalation twice daily 50/250 Maxhaler: One Inhalation twice daily 50/500 Maxhaler: One Inhalation twice daily Children (4 years and older)- 50/100 Maxhaler: One Inhalation twice daily. The maximum licensed dose of fluticasone propionate delivered by this Maxhaler in children is 100 ug twice daily. There are no data available for use of this Maxhaler in children aged under 4 years. Inhalation Powder in Maxhaler (For COPD): Maxhaler: One Inhalation twice daily Special patient groups: There is no need to adjust the dose in elderly patients or in those with renal impairment. There are no data available for use of this in patients with hepatic impairment. Using the Maxhaler: This is a patient friendly, ready to use and easy to grip device. Use as per instructions for use.
Both non-selective and selective 8-blockers should be avoided in patients with asthma, unless there are compelling reasons for their use. Due to the very low plasma concentrations achieved after inhaled dosing clinically significant drug interactions are unlikely. Care should be taken when co-administering known strong CYP3A4 inhibitors (e.g. ketoconazole, ritonavir), as there is potential for increased systemic exposure to Fluticasone Propionate.
This is contraindicated in patients with a history of hypersensitivity to any of the ingredients.
As this preparation contains Salmeterol and Fluticasone Propionate, the type and severity of adverse reactions associated with each of the compounds may be expected. There is no incidence of additional adverse events following concurrent administration of the two compounds. Adverse events, which have been associated with Salmeterol or Fluticasone Propionate, are given below. Salmeterol: The pharmacological side effects of beta-2-agonist treatment, such as tremor, subjective palpitations and headache, have been reported, but tend to be transient and reduce with regular therapy. Cardiac arrhythmia (including atrial fibrillation, supraventricular tachycardia and extra systoles) may occur, usually in susceptible patients. There have been reports of arthralgia and hypersensitivity reactions, including rash, oedema and angioedema. There have been reports of oropharyngeal irritation. There have been rare reports of muscle cramps. Fluticasone propionate: Hoarseness and candidiasis (thrush) of the mouth and throat can occur in some patients. Cutaneous hypersensitivity reactions have been reported. Rare cases of facial and oropharyngeal oedema have been reported. Both hoarseness and incidence of candidiasis may be relieved by gargling with water after use of Salmeterol/ Fluticasone Propionate Inhaler.
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 foetus or child. There is insufficient experience of the use of Salmeterol Xinafoate and Fluticasone Propionate in human pregnancy and lactation. There are no data available for human breast milk.
Consideration should be given to additional corticosteroid therapies, and to including administration of antibiotics if an infection is present. As with all inhaled medication containing corticosteroids, this preparation should be administered with caution in patients with active or quiescent pulmonary tuberculosis. This preparation should be administered with caution in patients with thyrotoxicosis.
Pressurised canister, do not puncture, break or incinerate even when apparently empty. Avoid storage in direct sunlight or heat. Store below 308C. Keep away from eyes. Keep away from children.