Bexitrol F 50/100 Bexicap

Indications

This medication is intended for the ongoing management of asthma where a combination treatment involving a long-acting β2-agonist and an inhaled corticosteroid is recommended. It is particularly suitable for:

• Patients who are not sufficiently managed by inhaled corticosteroids and ‘as needed’ short-acting β2-agonists.
• Patients who are already well-managed with a combination of inhaled corticosteroids and long-acting β2-agonists.

Pharmacology

Salmeterol Xinafoate is a selective, long-acting β2-agonist that helps in managing asthma and other forms of airway obstruction. Fluticasone Propionate is a corticosteroid with predominantly glucocorticoid activity, providing a localized effect on the lungs while minimizing systemic exposure. Salmeterol aids in symptom control, while Fluticasone Propionate enhances lung function and reduces the risk of asthma exacerbations. This combination offers a streamlined therapy option for those already on both β-agonists and inhaled corticosteroids.

• Salmeterol: A long-acting β2-adrenoceptor agonist with a 12-hour duration, it binds to the receptor’s exo-site, ensuring prolonged action.
• Fluticasone Propionate: When inhaled at recommended doses, it provides potent glucocorticoid anti-inflammatory effects within the lungs, reducing symptoms and preventing exacerbations without the adverse effects seen with systemic corticosteroids.

Dosage

Inhaler:

• Adults and Adolescents (12 years and older):
  • 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily, or
  • 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate twice daily, or
  • 2 puffs of 25 µg Salmeterol and 250 µg Fluticasone Propionate twice daily.
• Children (4-12 years):
  • 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate twice daily.

Inhalation Capsule (for asthma):

• Adults and Adolescents (12 Years and Older):
  • Salmeterol 50 µg & Fluticasone 100 µg or
  • Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart).
  • Starting dosages are tailored to asthma severity, with a maximum of Salmeterol 50 µg & Fluticasone 500 µg twice daily.
• Pediatric Patients (4 to 11 Years):
  • For asthma, Salmeterol 50 µg & Fluticasone 100 µg twice daily.

Inhalation Capsule (for COPD):

• Salmeterol 50 µg & Fluticasone 250 µg twice daily (morning and evening, approximately 12 hours apart). Rinsing the mouth after each inhalation is recommended.

Maxhaler (For Asthma):

• Adults and Adolescents (12 years and older):
  • 50/100 inhaler: One inhalation twice daily
  • 50/250 inhaler: One inhalation twice daily
  • 50/500 inhaler: One inhalation twice daily
• Children (4 years and older):
  • 50/100 inhaler: One inhalation twice daily. The maximum licensed dose for children is 100 µg twice daily.

Maxhaler (For COPD):

• One inhalation twice daily. There is no need for dose adjustments in elderly patients or those with renal impairment, and no data is available for use in hepatic impairment.

Administration

Correct use of the inhaler is crucial for effective asthma management. Follow these steps to ensure proper use:

1. Remove the cap.
2. Shake the inhaler vigorously for at least six times before use.
3. If using a new inhaler or one not used for over a week, shake it well and release one puff into the air.
4. Exhale fully and hold the inhaler upright.
5. Place the mouthpiece between your teeth, close your lips around it.
6. Breathe in deeply and slowly through your mouth while pressing down firmly on the canister.
7. Remove the inhaler and hold your breath for at least 10 seconds.
8. If more than one inhalation is prescribed, wait 1 minute between puffs. Shake the inhaler well and repeat the process.
9. Replace the cap after use and rinse your mouth with water.
10. Periodically check your technique in a mirror to ensure proper usage.

Instructions for Cleaning the Inhaler: Clean your inhaler weekly. Remove the canister and rinse the plastic actuator and cap with warm water (avoid water on the metal canister). Dry thoroughly before reassembling.

Interactions

Avoid both non-selective and selective β-blockers in asthma patients unless absolutely necessary. Clinically significant drug interactions are unlikely due to low plasma concentrations from inhaled dosing, but caution is advised with strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) due to potential increased systemic exposure to Fluticasone Propionate.

Contraindications

Do not use this medication in patients with a history of hypersensitivity to Salmeterol Xinafoate, Fluticasone Propionate, or any excipients. It is also contraindicated for the primary treatment of status asthmaticus or other acute asthma episodes requiring intensive measures.

Side Effects

Adverse effects may include:

• Salmeterol: Tremor, palpitations, headache, arrhythmias, arthralgia, hypersensitivity reactions, oropharyngeal irritation, and muscle cramps.
• Fluticasone Propionate: Hoarseness, candidiasis, hypersensitivity reactions, facial and oropharyngeal edema.

Mouth rinsing after use can help alleviate hoarseness and candidiasis.

Pregnancy & Lactation

• Pregnancy: Use only if the benefits outweigh potential risks to the fetus. Limited data is available regarding the use of Salmeterol and Fluticasone Propionate during pregnancy.
• Lactation: Use only if the benefits outweigh potential risks to the child. Plasma concentrations after therapeutic doses are very low, and concentrations in breast milk are likely low as well.

Precautions & Warnings

• Asthma Patients: Avoid initiating treatment during exacerbations or with unstable asthma. This medication is not for acute symptom relief.
• COPD Patients: Monitor for pneumonia, as the incidence may increase.
• Corticosteroids: Long-term high-dose use may lead to systemic effects such as Cushing’s syndrome, adrenal suppression, and reduced bone mineral density. Regular review and dose adjustment are essential.

Use in Special Populations

Monitor growth velocity in pediatric patients as inhaled corticosteroids may affect growth.

Overdose Effects

• Salmeterol: Symptoms include seizures, angina, hypertension, tachycardia, arrhythmias, nervousness, headache, and muscle cramps. Discontinue use and consider cardioselective beta-blocking agents with caution.
• Fluticasone Propionate: Acute overdose may cause temporary adrenal suppression. Chronic overdose may require monitoring of adrenal reserve. Continue therapy at an adjusted dosage for symptom control.

Therapeutic Class

Long-acting selective β-adrenoceptor stimulants, respiratory corticosteroids.

Storage Conditions

Store in a pressurized canister away from direct sunlight and heat. Keep below 30°C and out of reach of children. Do not puncture or incinerate the canister even when empty.