Indications

Bexitrol F is indicated for the regular treatment of asthma in patients for whom a combination of a long-acting β2​-agonist and an inhaled corticosteroid is appropriate. This includes:

• Patients whose asthma is not adequately controlled with inhaled corticosteroids and a short-acting β2​-agonist used as needed.
• Patients who are already well-controlled on both an inhaled corticosteroid and a long-acting β2​-agonist.

Pharmacology

Bexitrol F is a combination product containing two active ingredients:

• Salmeterol Xinafoate: A selective, long-acting β2​-adrenoceptor agonist that protects against asthma symptoms. It has a long side chain that allows it to bind to the receptor for an extended period, providing 12-hour action.
• Fluticasone Propionate: A corticosteroid with potent anti-inflammatory activity, primarily within the lungs. It improves lung function and prevents asthma exacerbations without the systemic side effects seen with oral corticosteroids. The combination of these two drugs offers a convenient regimen that improves lung function and prevents symptoms and exacerbations.

Dosage

The dosage varies by formulation and patient age:

• Inhaler:
  • Adults and adolescents (12 years and older): 2 puffs of either 25/50 mcg, 25/125 mcg, or 25/250 mcg (Salmeterol/Fluticasone) twice daily.
  • Children (4-12 years): 2 puffs of 25/50 mcg twice daily.
• Inhalation capsule (for asthma):
  • Adults and adolescents (12 years and older): 50/100 mcg or 50/250 mcg twice daily. The maximum recommended dose is 50/500 mcg twice daily.
  • Pediatric patients (4-11 years): 50/100 mcg twice daily.
• Inhalation capsule (for COPD): 50/250 mcg twice daily. It is advised to rinse the mouth after each inhalation.
• Maxhaler (for asthma):
  • Adults and adolescents (12 years and older): One inhalation of 50/100 mcg, 50/250 mcg, or 50/500 mcg twice daily.
  • Children (4 years and older): One inhalation of 50/100 mcg twice daily.

Administration

Using the inhaler correctly is crucial for the medication to be effective. The inhaler should be shaken vigorously before each use. Patients should breathe out fully, place the mouthpiece in their mouth, and press the canister while inhaling deeply and slowly. After inhaling, they should hold their breath for at least 10 seconds. The mouth should be rinsed with water after each use to prevent side effects like oral candidiasis. The inhaler should be cleaned at least once a week.

Interaction

Non-selective and selective β-blockers should be avoided in asthma patients unless absolutely necessary. Clinically significant drug interactions are unlikely due to the low plasma concentrations achieved with inhaled doses. However, caution is advised when co-administering strong CYP3A4 inhibitors like ketoconazole or ritonavir, as they can increase systemic exposure to fluticasone propionate.

Contraindications

Bexitrol F is contraindicated in patients with a history of hypersensitivity to any of its components. It is also not indicated for the primary treatment of status asthmaticus or other acute asthma attacks requiring intensive measures.

Side Effects

As Bexitrol F contains both salmeterol and fluticasone propionate, the side effects are a combination of those associated with each drug.

• Salmeterol: Common side effects include tremor, palpitations, and headache, which are usually transient. Cardiac arrhythmias, arthralgia, hypersensitivity reactions, and muscle cramps have also been reported.
• Fluticasone Propionate: Side effects may include hoarseness and oral candidiasis (thrush), which can be reduced by gargling with water after use. Cutaneous hypersensitivity reactions and facial or oropharyngeal swelling have been reported in rare cases.

Pregnancy & Lactation

This drug should be used during pregnancy and lactation only if the potential benefit to the mother outweighs the possible risk to the fetus or child. There is insufficient human data, but animal studies have shown potential for adverse fetal effects at high systemic exposure levels. Concentrations of the drugs in human breast milk are likely to be low.

Precautions & Warnings

• Acute Symptoms: Bexitrol F is not for the relief of acute asthma symptoms. Patients should have a fast and short-acting bronchodilator available.
• Paradoxical Bronchospasm: This can occur immediately after dosing and should be treated with a fast-acting bronchodilator. The medication should be discontinued immediately if this occurs.
• COPD: An increased risk of pneumonia has been observed in COPD patients using salmeterol/fluticasone inhalers.
• Systemic Corticosteroid Effects: High doses used for long periods may lead to systemic effects such as Cushing's syndrome, adrenal suppression, growth retardation in children, and decreased bone mineral density. The dose should be titrated to the lowest effective level.

Overdose Effects

Overdose data for Bexitrol F is limited, but overdoses of its individual components have been studied.

• Salmeterol: Symptoms include seizures, angina, hypertension or hypotension, tachycardia, arrhythmias, nervousness, headache, and tremor.
• Fluticasone Propionate: Acute overdose may cause temporary adrenal function suppression, which usually recovers without emergency action. Chronic overdose can lead to adrenal suppression.

Therapeutic Class

Bexitrol F is a combination of a long-acting selective β2​-adrenoceptor stimulant and a respiratory corticosteroid.

Storage Conditions

Store below 30°C. The pressurized canister should not be punctured, broken, or incinerated, even when empty. Protect from direct sunlight and heat. Keep away from eyes and children.