Fluticasone
- Atc Codes:D07AC17#R01AD08#R03BA05#R01AD12
- CAS Codes:397864-44-7#80474-14-2#90566-53-3
- PHARMGKB ID:397864-44-7#80474-14-2#90566-53-3
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Alisade (d), Avamys, Cutivate, Flixonase, Flixotide; Belgium: Avamys, Cutivate, Flixonase, Flixotide; Bulgaria: Cutivate, Flixonase, Flixotide; Cyprus: Avamys, Cutivate, Flihaler, Flisonase, Flixotide, Flutinasal; Czech Republic: Alergonase, Alisade (d), Avamys, Cutivate, Flixonase, Flixotide, Nasofan; Denmark: Avamys, Cutivat, Flixonase, Flixotide, Flutide; Estonia: Alisade (d), Avamys, Cutivate, Flixonase, Flixotide, Nasofan; Finland: Avamys, Flixonase, Flixotide, Nasofan; France: Avamys, Flixonase, Flixotide, Flixovate; Germany: Atemur, Avamys, Axotide, Flixotide, Flutica-TEVA, Fluticasone, Flutide, Flutivate; Greece: Alerxem, Avamys, Dermocort Uni-pharma, Flihaler, Flixocort, Flixoderm, Flixotide, Flucortis, Flutarzole, Fluticapen, Fluticasone, Flutikrem, Flutinasal, Flutizal, Nasofan, Rolenium, Ybecor; Hungary: Avamys, Cutivate, Flixonase, Flixotide, Flutirin; Ireland: Avamys, Flixonase, Flixotide, Fluticasone, Nasofan; Italy: Avamys, Flixoderm, Flixonase, Flixotide, Fluspiral, Nasofan, Ticavent; Latvia: Avamys, Cutivate, Flixonase, Flixotide, Fluticasone, Foxair; Lithuania: Fluticasone; Luxembourg: Cutivate, Flixonase, Flixotide; Malta: Avamys, Cutivate, Flihaler, Flixonase, Flixotide; Netherlands: Cutivate, Flixonase, Flixotide, Flutide, Fluticasone; Poland: Avamys, Cutivate, Fanipos, Flixonase, Flixotide, Flotikar, Fluticasone; Portugal: Alisade (d), Asmatil, Asmo-Lavi, Avamys, Brisovent, Cortifil, Cutivate, Eustidil, Flixotaide, Flutaide, Fluticasona, Fulticrem, Rontilona, Ubizol; Romania: Alisade (d), Avamys, Cutivate, Flixonase, Flixotide; Slovakia: Alisade (d), Avamys, Flixonase, Flixotide, Nasofan; Slovenia: Flixonase, Flixotide; Spain: Avamys, Flixonase, Flixotide, Fluinol, Flusonal, Fluticasona, Inalacor, Nasotricin, Rinosone; Sweden: Alisade (d), Atemur, Avamys, Flixotaide, Flixotide, Flutaide, Flutide; UK: Avamys, Cutivate, Flixonase, Flixotide.
North America
Canada: Avamys, Cutivate, Flonase, Flovent, Fluticasone; USA: Cutivate, Flonase, Flovent, Fluticasone, Veramyst.
Latin America
Argentina: Alenys, Balivent Nasal, Crivanil, Cutivate, Flixonase, Flixotide, Fluticort, Fruti-K, Inhalan, Lidil Cort, Lirtodac, Proair Nasal, Rinisona; Brazil: Flixonase, Flixotide, Flutican, Fluticaps, Flutivate, Plurair; Mexico: Caneti, Cutivate, Flixonase, Flixotide.
Asia
Japan: Florads, Flunase, Fluticanose, Flutide, Kirigamil, Milicarett, Phavi, Proticasone, Skyron.
Drug combinations
Fluticasone and Salmeterol
Chemistry
Fluticasone Furoate: C~27~H~29~F~3~O~6~S. Mw: 538.60. (1) Androsta-1,4-diene-17-carbothioic acid, 6,9-difluoro-17-[(2-furanylcarbonyl)oxy]-11-hydroxy-16-methyl-3-oxo-, S-(fluoromethyl) ester, (6α,11β,16α,17α)-; (2)(6α,11β,16α,17α)-6,9-Difluoro-17-(((fluoromethyl)thio)carbonyl)-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl-2-furancarboxylate. CAS-397864-44-7 (2006).
Fluticasone Propionate: C~25~H~31~F~3~O~5~S. Mw: 500.57. S-Fluoromethyl 6α, 9α-difluoro-11β-hydroxy-16α-methyl-3-oxo-17α-propionyloxyandrosta-1,4-diene-17β-carbothioate. CAS-80474-14-2; CAS-90566-53-3 (fluticasone)(1985).
Pharmacologic Category
Hormones and Synthetic Substitutes; Adrenals. EENT Preparations; Anti-inflammatory Agents; Corticosteroids. (ATC-Code: D07AC17; R01AD08; R03BA05; R01AD12).
Mechanism of action
Fluticasone propionate is a synthetic, trifluorinated glucocorticoid with potent anti-inflammatory action. Mechanism of action for all topical corticosteroids believed to be a combination of anti-inflammatory activity, immunosuppressive properties, and antiproliferative actions.
Therapeutic use
Maintenance treatment of asthma as prophylactic therapy. Also indicated for patients requiring oral corticosteroid therapy for asthma to assist in total discontinuation or reduction of total oral dose. Management of seasonal and perennial allergic rhinitis and nonallergic rhinitis. Relief of inflammation and pruritus associated with corticosteroid-responsive dermatoses. Atopic dermatitis.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies using inhaled fluticasone in pregnant women. Use with caution during pregnancy and while breast-feeding. Should not be applied to nipples.
Unlabeled use
Contraindications
Hypersensitivity to fluticasone or any component of the formulation. Primary treatment of status asthmaticus or acute bronchospasm. Do not use topically if infection is present at treatment site, in the presence of skin atrophy, or for treatment of rosacea or perioral dermatitis.
Warnings and precautions
May cause hypercorticism or suppression of HPA axis, particularly in younger children or in patients receiving high doses for prolonged periods. Pediatric patients may be more susceptible to systemic toxicity. Bronchospasm might occur with wheezing after inhalation. Avoid nasal corticosteroid use in recent nasal septal ulcers, nasal surgery, or nasal trauma until healing has occurred. Prolonged use of corticosteroids may increase the incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to vaccines. With oral inhalation, local yeast infections (e.g. oral pharyngeal candidiasis) might occur. Lower respiratory tract infections, including pneumonia, reported in COPD using oral inhalation (higher incidence in the elderly). Prolonged treatment with corticosteroids associated with development of Kaposi’s sarcoma (case reports). Corticosteroid use may cause psychiatric disturbances, including depression, euphoria, insomnia, mood swings, and personality changes. Pre-existing psychiatric conditions may be exacerbated by corticosteroid use. Rare cases of vasculitis (Churg-Strauss syndrome) or other eosinophilic conditions can occur. Not to be used in status asthmaticus or for relief of acute bronchospasm. Use with caution in the following cases: heart failure (long-term use associated with fluid retention and hypertension), diabetes mellitus (may alter glucose production/regulation leading to hyperglycemia), GI diseases (diverticulitis, peptic ulcer, ulcerative colitis) due to perforation risk, hepatic impairment, including cirrhosis (long-term use has been associated with fluid retention), myasthenia gravis (exacerbation of symptoms has occurred), following acute MI (corticosteroids associated with myocardial rupture), cataracts and/or glaucoma (increased intraocular pressure, open-angle glaucoma, and cataracts have occurred with prolonged use), osteoporosis (high doses and/or long-term use of corticosteroids associated with increased bone loss and osteoporotic fractures), renal impairment (fluid retention might occur), or history of seizure disorder (seizures reported with adrenal crisis). Changes in thyroid status possible (metabolic clearance of corticosteroids increases in hyperthyroidism and decreases in hypothyroidism). Orally-inhaled and intranasal corticosteroids may cause a reduction in growth velocity in pediatric patients. Some dosage forms contain lactose. There have been reports of systemic corticosteroid withdrawal symptoms (e.g. joint/muscle pain, lassitude, depression) when withdrawing oral inhalation therapy.