Fluticasone propinate
Fluticasone is a steroid. It prevents the release of substances in the body that cause inflammation. Fluticasone inhalation is used to prevent asthma attacks. Fluticasone inhalation will not treat an asthma attack that has already begun. Flovent HFA and Flovent Diskus are sometimes used together with an oral (taken by mouth) steroid medicine. Flovent brands of fluticasone inhalation are for use in adults and children who are at least 4 years old. The Arnuity Ellipta brand is for adults and children who are at least 12 years old.
Mechanism of effect
Fluticasone belongs to a group of corticosteroids which utilizes a fluorocarbothioate ester linkage at the 17 carbon position; extremely potent vasoconstrictive and anti-inflammatory activity. The effectiveness of inhaled fluticasone is due to its direct local effect.
Pharmacodynamic
Fluticasone is an extremely potent vasoconstrictor and anti-inflammatory agent. Its effectiveness in inhaled forms is due to its direct local effect.
Pharmacokinetics
Absorbed systemically (Flovent Diskus: ~18%) primarily via lungs, minimal GI absorption (<1%) due to presystemic metabolism. Distribution:4.2 L/kg. Metabolism: Hepatic via CYP3A4 to 17β-carboxylic acid (negligible activity). Excretion: Feces (as parent drug and metabolites); urine (<5% as metabolites). Onset of Action.Maximal benefit may take 1 to 2 weeks or longer.Time to Peak:0.5 to 1 hour.Half-Life Elimination:IV: ~8 hours; Oral inhalation (plasma elimination phase following repeat dosing): 24 hours.Protein Binding:>99%.
Dosage
Usual Adult Dose for Asthma - Maintenance
Initial doses should be based upon previous therapy and asthma severity:
Fluticasone propionate INHALATION AEROSOL:
-For patients previously receiving bronchodilators alone:
Initial dose: 88 mcg via oral inhalation twice a day
Maximum dose: 440 mcg twice a day
-For patients previously receiving inhaled corticosteroids:
Initial dose: 88 to 220 mcg via oral inhalation twice a day
Maximum dose: 440 mcg twice a day
-For patients previously receiving oral corticosteroids:
Initial dose: 440 mcg via oral inhalation twice a day
Maximum dose: 880 mcg twice a day
Age: 4 to 11 years:
Fluticasone propionate INHALATION POWDER:
Initial dose: 50 mcg via oral inhalation twice a day
Maximum dose: 100 mcg twice a day
Fluticasone propionate INHALATION AEROSOL:
Recommended dose: 88 mcg via oral inhalation twice a day
-A valved holding chamber and mask may be used in young patients
Age: 12 years or older:
Fluticasone propionate INHALATION AEROSOL:
-For patients previously receiving bronchodilators alone:
Initial dose: 88 mcg via oral inhalation twice a day
Maximum dose: 440 mcg twice a day
-For patients previously receiving inhaled corticosteroids:
Initial dose: 88 to 220 mcg via oral inhalation twice a day
Maximum dose: 440 mcg twice a day
-For patients previously receiving oral corticosteroids:
Initial dose: 440 mcg via oral inhalation twice a day
Maximum dose: 880 mcg twice a day
Drug contraindications
hypersensitivity to drug or its components. , acute episodes of asthma or COPD , status asthmaticus , severe hypersensitivity to milk proteins orlactoseSide effects
Headache , fatigue , rash , pruritus , Hypertension , Throat irritation , Rhinitis , sinusitis , malaise , Arthralgia , Upper respiratory tract infection , bronchitis , Pain , Nasopharyngitis , vaginitis , voice disorder , Oral candidiasis , arthritis , musculoskeletal pain , nasal congestionInteractions
Amitriptyline , Oxazepam , Olanzapine , Ipratropium bromide , Itraconazole , Paroxetine , Pramipexole , Venlafaxine , Voriconazole , Ketoconazole , Pethidine , Midodrine , Naphazoline , Nilotinib , Nicorandil , Warfarin , Verapamil , Labetalol , Lorazepam , Levodopa/carbidopa , Lithium carbonate , Magnesium oxide , Magnesium sulfate , Zolpidem , Sertraline , Citalopram , Sildenafil , Fluconazole , Phenobarbital , Posaconazole , Thalidomide , Trazodone , Tranylcypromine , Trimipramine , Topiramate , formoterol , sirukumabAlerts
1- Use with caution in patients with Bone mineral density, Cardiovascular disease, Diabetes, Gastrointestinal disease, Hepatic impairment, Myasthenia gravis, Myocardial infarct (MI), Ocular disease, Seizure disorders, Thyroid disease .
2- Bronchospasm: May occur with wheezing after inhalation; if this occurs, stop steroid and treat with a fast-acting bronchodilator.
3- Adrenal suppression: May cause hypercorticism or suppression of hypothalamic-pituitary-adrenal (HPA) axis in sensitive patients.
Points of recommendation
1- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat).
2- Monitor for signs of asthma instability and adrenal insufficiency.
3- Decrease fluticasone to lowest effective dose after prednisone reduction is complete
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