Bexitrol F 50/250 Bexicap

Indications

This medication is prescribed for the ongoing management of asthma, especially in cases where a combination therapy (long-acting β2-agonist and inhaled corticosteroid) is deemed suitable:

• For patients inadequately managed with inhaled corticosteroids and ‘as needed’ inhaled short-acting β2-agonists.
• For patients already well-controlled with both inhaled corticosteroids and long-acting β2-agonists.

Pharmacology

Salmeterol Xinafoate is a selective, long-acting beta-2 agonist used to manage asthma and other obstructive airway conditions. Fluticasone Propionate is a corticosteroid with predominantly glucocorticoid effects. It acts topically on the lungs with minimal systemic impact at typical doses. Salmeterol helps prevent symptoms, while Fluticasone Propionate enhances lung function and reduces exacerbations. This combination offers a streamlined regimen for patients currently using β-agonists and inhaled corticosteroids. Here’s how each drug works:

• Salmeterol: A selective, 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 glucocorticoid anti-inflammatory effects within the lungs, alleviating symptoms and reducing asthma exacerbations, with fewer side effects compared to systemic corticosteroids.

Dosage

Inhaler:

• Adults and Adolescents (12 years and older): 2 puffs of 25 µg Salmeterol and 50 µg Fluticasone Propionate, 2 puffs of 25 µg Salmeterol and 125 µg Fluticasone Propionate, 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): 50 µg Salmeterol & 100 µg Fluticasone or 50 µg Salmeterol & 250 µg Fluticasone twice daily (morning and evening, around 12 hours apart). The initial dose depends on asthma severity. The maximum dosage is 50 µg Salmeterol & 500 µg Fluticasone twice daily.
• Pediatric Patients (4 to 11 years): 50 µg Salmeterol & 100 µg Fluticasone twice daily (morning and evening, approximately 12 hours apart) for those not controlled on an inhaled corticosteroid.

Inhalation Capsule (for COPD):

• Adults and Adolescents: 50 µg Salmeterol & 250 µg Fluticasone twice daily (morning and evening, about 12 hours apart). Rinsing the mouth after each use is advised.

Maxhaler (For Asthma):

This device contains a foil strip with 60 pre-dispensed doses of inhalation powder. Daily use is essential for optimal results, even when symptoms are not present.

• 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 mcg twice daily. No data available for use in children under 4 years.

Maxhaler (For COPD):

• Inhaler: One inhalation twice daily. No dose adjustment needed for elderly patients or those with renal impairment. No data for hepatic impairment.

Administration

Correct inhaler use is crucial to ensure effective delivery of medication. Incorrect use can lead to reduced medication reaching the lungs. Follow these steps for optimal inhaler use:

1. Remove the cap.
2. Shake the inhaler vigorously (at least six times) before each use.
3. If new or unused for a week or more, shake and release one puff into the air to ensure it works.
4. Exhale fully, hold the inhaler upright.
5. Place the actuator between your teeth and close lips around the mouthpiece.
6. Inhale deeply and slowly while pressing down firmly on the canister to release the medication.
7. Remove the inhaler and hold your breath for at least 10 seconds or as long as comfortable.
8. If more than one puff is prescribed, wait 1 minute between puffs, shake the inhaler well, and repeat steps 4 to 7.
9. Replace the cap after use. Rinse your mouth with water.
10. Check your technique in the mirror. If a white mist appears, adjust your technique as needed.

Cleaning Instructions: Clean your inhaler weekly. Remove the canister, rinse the plastic actuator and cap with warm water (do not immerse the canister), dry thoroughly, and reassemble.

Interactions

Avoid both non-selective and selective β-blockers in asthma patients unless absolutely necessary. While clinically significant drug interactions are unlikely due to low plasma concentrations after inhalation, caution is advised when using strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) as they may increase systemic exposure to Fluticasone Propionate.

Contraindications

This medication should not be used in patients with 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

Salmeterol: Common side effects include tremor, palpitations, and headache, usually transient. Serious side effects may include arrhythmias, arthralgia, hypersensitivity reactions, oropharyngeal irritation, and rare muscle cramps.

Fluticasone Propionate: Possible side effects include hoarseness, candidiasis (thrush), hypersensitivity reactions, and rare facial and oropharyngeal edema. Gargling with water after use can alleviate hoarseness and candidiasis.

Pregnancy & Lactation

Pregnancy: Use during pregnancy should be considered only if the benefit to the mother outweighs the potential risk to the fetus. Limited human data is available, and animal studies suggest possible fetal effects with high systemic exposure.

Lactation: Use during breastfeeding should be considered only if the benefit to the mother outweighs the potential risk to the child. Inhaled doses result in very low plasma levels, likely translating to low concentrations in breast milk.

Precautions & Warnings

Asthma Patients: Do not initiate during exacerbations or if asthma is unstable. This medication is not for acute symptom relief; always keep a fast-acting bronchodilator available.

Asthma-Related Adverse Events: Serious asthma-related events may occur. Seek medical advice if symptoms remain uncontrolled or worsen.

Paradoxical Bronchospasm: May occur with increased wheezing after dosing. Treat immediately with a fast-acting bronchodilator and discontinue the inhaler if necessary.

COPD Patients: Monitor for pneumonia, as it may overlap with COPD exacerbations.

Corticosteroids: Inhaled corticosteroids may cause systemic effects at high doses or long-term use. Regular reviews and dose adjustments are essential.

Special Populations: Inhaled corticosteroids may reduce growth velocity in pediatric patients. Long-term effects on final height are unknown.

Overdose Effects

Salmeterol: Overdose symptoms may include seizures, hypertension, tachycardia, arrhythmias, nervousness, headache, tremor, and muscle cramps. Treatment involves discontinuing Salmeterol and using cardioselective beta-blocking agents with caution.

Fluticasone Propionate: Acute overdose may lead to temporary adrenal suppression, but recovery is usually quick. Chronic overdose may require monitoring of adrenal function.

Therapeutic Class

Long-acting selective β-adrenoceptor stimulants, Respiratory corticosteroids

Storage Conditions

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