Flomyst F

Approved Indications:

• Asthma:
  Maintenance treatment of asthma in patients aged 12 years and older, where the use of a combination of inhaled corticosteroid and long-acting beta2-agonist (LABA) is appropriate.
• Chronic Obstructive Pulmonary Disease (COPD):
  Maintenance treatment of airflow obstruction and reduction of exacerbations in patients with moderate to severe COPD with a history of exacerbations.

Off-label / Clinically Accepted Uses:

• Step-up therapy in asthma patients inadequately controlled on inhaled corticosteroids alone.
• Symptomatic treatment in COPD patients with frequent exacerbations despite bronchodilator therapy.

Route: Inhalation via metered-dose inhaler or dry powder inhaler (device-dependent).

Asthma (Adults and Adolescents ≥12 years):

• Typical doses range from 100/6 mcg to 250/10 mcg (Fluticasone/Formoterol) twice daily.
• Maximum daily dose should not exceed 500 mcg fluticasone and 24 mcg formoterol.

COPD (Adults):

• Usually 250/10 mcg twice daily.
• Dose adjustments based on clinical response and tolerability.

Special Populations:

• Elderly: No specific dose adjustment required; monitor closely.
• Pediatrics (<12 years): Safety and efficacy not established; generally not recommended.
• Renal/Hepatic impairment: No dose adjustment recommended, but caution advised due to limited data.

Duration: Long-term maintenance therapy; not indicated for acute bronchospasm or rescue treatment.

This combination includes two agents with complementary mechanisms: Fluticasone propionate is a potent inhaled corticosteroid that reduces airway inflammation by binding to glucocorticoid receptors, thereby inhibiting the release of inflammatory mediators and decreasing airway hyperresponsiveness. Formoterol fumarate is a long-acting selective beta2-adrenergic receptor agonist (LABA) that relaxes bronchial smooth muscle by stimulating beta2 receptors, leading to sustained bronchodilation. Together, they improve airflow, reduce symptoms, and prevent exacerbations in obstructive airway diseases.

• Absorption:
  Inhaled fluticasone has low systemic bioavailability (~15%) due to extensive first-pass metabolism. Formoterol shows rapid absorption with systemic availability after inhalation.
• Distribution:
  Fluticasone is highly protein-bound (>99%). Formoterol is moderately protein-bound (~61-64%).
• Metabolism:
  Fluticasone is extensively metabolized by CYP3A4 in the liver. Formoterol is also metabolized primarily by CYP enzymes, including CYP2D6.
• Half-life:
  Fluticasone: Approximately 7-8 hours.
  Formoterol: Approximately 10 hours.
• Elimination:
  Both drugs are eliminated mainly via feces through biliary excretion; renal clearance is minimal.

• Pregnancy:
  Fluticasone is Category C (FDA), and formoterol is Category C; use only if potential benefits justify the potential risk. Limited human data exist; animal studies show no direct teratogenic effects but systemic corticosteroids may pose risks.
• Lactation:
  Both drugs are excreted in breast milk in low amounts; caution is advised. Monitor infants for possible adverse effects.

• Primary Class: Combination inhaled corticosteroid (ICS) + long-acting beta2-agonist (LABA).
• Subclass: Respiratory controller medication for asthma and COPD.

• Known hypersensitivity to fluticasone, formoterol, or any formulation excipients.
• Primary treatment of status asthmaticus or acute episodes of bronchospasm.
• Severe hypersensitivity reactions to milk proteins (for dry powder inhaler formulations).

• Not for relief of acute bronchospasm or rescue therapy.
• Risk of paradoxical bronchospasm; discontinue if occurs.
• Use with caution in patients with cardiovascular disorders (e.g., arrhythmias, hypertension).
• Monitor for signs of adrenal suppression or systemic corticosteroid effects during prolonged use.
• May increase risk of pneumonia in COPD patients; monitor closely.
• Avoid abrupt discontinuation to prevent exacerbation of underlying disease.

Common:

• Oropharyngeal candidiasis (thrush), hoarseness, throat irritation (due to corticosteroid).
• Headache, tremor, palpitations (due to formoterol).
• Cough and dry mouth.

Serious/Rare:

• Paradoxical bronchospasm.
• Hypersensitivity reactions including angioedema, rash.
• Cardiovascular events such as tachycardia, hypertension, arrhythmias.
• Adrenal insufficiency with long-term use.

• CYP3A4 inhibitors (e.g., ketoconazole, ritonavir): Increase fluticasone systemic exposure, increasing risk of adrenal suppression.
• Other beta-agonists: Additive cardiovascular effects.
• Monoamine oxidase inhibitors (MAOIs) or tricyclic antidepressants: May potentiate cardiovascular effects of formoterol.
• Beta-blockers: May reduce bronchodilator efficacy or cause bronchospasm.

• Current asthma management guidelines recommend ICS/LABA combinations like fluticasone/formoterol as preferred controller therapy for moderate to severe asthma.
• Recent COPD guidelines emphasize use in patients with frequent exacerbations and persistent symptoms despite bronchodilators.
• Safety alerts highlight careful monitoring for pneumonia in COPD patients using ICS-containing therapies.

• Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C.
• Protect from moisture and heat.
• Keep inhaler/device capped when not in use.
• Do not freeze or expose to direct sunlight.