Bexitrol F 25/125

Indications

This medication is recommended for the ongoing management of asthma when a combination therapy of a long-acting β2-agonist and an inhaled corticosteroid is indicated. It is suitable for:

• Patients whose asthma is not sufficiently controlled with inhaled corticosteroids and ‘as needed’ short-acting β2-agonists.
• Patients already managing their asthma effectively with both an inhaled corticosteroid and a long-acting β2-agonist.

Pharmacology

Salmeterol Xinafoate is a long-acting, selective beta-2 agonist designed for the treatment of asthma and other obstructive airway conditions. Fluticasone Propionate is a glucocorticoid corticosteroid with a localized effect in the lungs, minimizing systemic impact at standard doses. Together, Salmeterol alleviates symptoms, while Fluticasone Propionate enhances lung function and helps prevent exacerbations. This combination simplifies the treatment regimen for patients using both β-agonists and inhaled corticosteroids.

• Salmeterol: This agent acts as a long-acting (12-hour) beta-2-adrenoceptor agonist, with a long side chain that attaches to the receptor’s exo-site.
• Fluticasone Propionate: When inhaled at recommended doses, it provides potent anti-inflammatory effects in the lungs, reducing asthma symptoms and preventing flare-ups, without the side effects of systemic corticosteroids.

Dosage

Inhaler:

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

Inhalation Capsules (for asthma):

• Adults and Adolescents (12 years and older):
  • Salmeterol 50 µg & Fluticasone 100 µg or Salmeterol 50 µg & Fluticasone 250 µg twice daily.
  • Maximum dosage: Salmeterol 50 µg & Fluticasone 500 µg twice daily.
• Pediatric Patients (4 to 11 years):
  • Salmeterol 50 µg & Fluticasone 100 µg twice daily.

Inhalation Capsules (for COPD):

• Adults and Adolescents (12 years and older):
  • Salmeterol 50 µg & Fluticasone 250 µg twice daily.

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. Maximum licensed dose for children is 100 µg twice daily.

Maxhaler (for COPD):

• One inhalation twice daily.

Administration

Proper inhaler technique is crucial for effective treatment. Follow these steps:

1. Remove the cap and shake the inhaler vigorously.
2. If the inhaler is new or unused for a week, release one puff into the air to ensure it works.
3. Exhale fully and hold the inhaler upright.
4. Place the actuator between the teeth and close lips around the mouthpiece.
5. Inhale deeply and slowly while pressing down on the canister to release the medicine.
6. Remove the inhaler from your mouth and hold your breath for at least 10 seconds.
7. If multiple puffs are prescribed, wait 1 minute between puffs. Shake the inhaler and repeat steps 4-7.
8. After use, replace the cap and rinse your mouth with water.
9. Regularly check your technique and clean your inhaler weekly by rinsing the actuator and cap in warm water (avoid submerging the metal canister).

Interactions

Avoid non-selective and selective β-blockers unless absolutely necessary. Be cautious when using strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) as they may increase systemic exposure to Fluticasone Propionate.

Contraindications

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

Side Effects

Possible side effects include:

• Salmeterol: Tremor, palpitations, headache, arrhythmia, arthralgia, hypersensitivity reactions, oropharyngeal irritation, and muscle cramps.
• Fluticasone Propionate: Hoarseness, candidiasis (thrush), cutaneous hypersensitivity, facial oropharyngeal edema. Gargling with water after use can alleviate hoarseness and candidiasis.

Pregnancy & Lactation

Use during pregnancy and lactation should be considered only if the benefits outweigh the potential risks to the fetus or child. There is limited experience with Salmeterol Xinafoate and Fluticasone Propionate in pregnant and breastfeeding women. Plasma concentrations of these drugs are low, suggesting minimal risk during lactation.

Precautions & Warnings

• Asthma Patients: Do not start this treatment during an exacerbation or if asthma is acutely worsening. This medication is not for immediate symptom relief. Always have a fast-acting bronchodilator available.
• COPD Patients: Monitor for pneumonia, as its symptoms can overlap with COPD exacerbations.
• Corticosteroids: Be aware of potential systemic effects with long-term use, such as Cushing’s syndrome, adrenal suppression, and growth retardation in children. Regular review and dose adjustments are important.

Overdose Effects

Salmeterol Overdose: Symptoms may include seizures, angina, hypertension, tachycardia, arrhythmias, nervousness, headache, muscle cramps, dry mouth, and more. Treatment involves discontinuing Salmeterol and using cardioselective beta-blockers cautiously.

Fluticasone Propionate Overdose: Acute overdose may cause temporary adrenal suppression, which recovers within days. Chronic overdose might require monitoring of adrenal function.

Therapeutic Class

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

Storage Conditions

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