氣喘 Maintenance treatment of asthma as prophylactic therapy in patients >1 year of age
(Not indicated for relief of acute bronchospasm)
藥理
Corticosteroid, Inhalant (Oral)
藥動學
Absorption:
Absorbed systemically primarily via lungs; minimal GI absorption (<1%) due to presystemic metabolism Distribution:
1. 4.2 L/kg
2. Protein binding: >99% Metabolism:
Hepatic via CYP3A4 to 17β-carboxylic acid (negligible activity) Excretion:
1. Feces (as parent drug and metabolites)
2. Urine (<5% as metabolites) Pharmacodynamics:
1. Bioavailability: 13.9%
2. Half-life elimination: ~11.2 hours (terminal half-life)
3. Time to peak, plasma: 0.5 to 1 hour
4. Onset of action: Maximal benefit may take 1 to 2 weeks or longer
禁忌症
1. Hypersensitivity to fluticasone or any component of the formulation.
2. Severe hypersensitivity to milk proteins or lactose.
3. Primary treatment of status asthmaticus or other acute episodes of asthma requiring intensive measures.
懷孕分類
Fluticasone can be detected in cord blood following maternal use via oral inhalation during pregnancy; use with caution.
哺乳分類
It is not known if sufficient quantities of fluticasone are absorbed following inhalation to produce detectable amounts in breast milk.
Adult and children ≥16 years of age:
1. Mild asthma: 100 to 250 mcg twice daily
2. Moderate asthma: 250 to 500 mcg twice daily
3. Severe asthma: 500 mcg twice daily; may increase up to 1,000 mcg twice daily in very severe patients
小兒調整劑量
Children 4-16 years:
50 to 200 mcg twice daily; dose may be initiated as 50 or 100 mcg twice daily Children 1-4 years:
50 to 100 mcg twice daily