Fluticasone

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Fluticasone chemical structure
Fluticasone
Systematic (IUPAC) name
6,9-difluoro-11-hydroxy-16-methyl-3-oxo-17-
(1-oxopropoxy)-androsta-1,4-diene-17-carbothioic acid (6α,11β,16α,17α)-
S-(fluoromethyl) ester
Identifiers
CAS number 80474-14-2
ATC code D07AC17 & D07AC04 topical, R01AD08 nasal, R03BA05 inhaled
PubChem 444036
DrugBank APRD00065
Chemical data
Formula C25H31F3O5S 
Mol. weight 500.572 g/mol
Pharmacokinetic data
Bioavailability 0.51% (Intranasal)
Protein binding 91%
Metabolism Intranasal- hepatic cytochrome p450,3A4
Half life 10 hours
Excretion renal
Therapeutic considerations
Pregnancy cat.

C for Intranasal and Inhaled
Legal status

POM(UK)
Routes Intranasal, Inhaled, Topical Cream or Ointment

Fluticasone propionate is a potent corticosteroid often prescribed as treatment for asthma and allergic rhinitis. It is marketed with the brand name Flixotide and Flixonase by Allen & Hanburys and Flovent and Flonase by GlaxoSmithKline.

It is also used as a cream or ointment for the treatment of eczema and psoriasis (Cutivate UK).

Contents

[edit] How it works

The precise mechanisms of glucocorticoid action in asthma are unknown. Inflammation is recognized as an important component in the pathogenesis of asthma. Glucocorticoids have been shown to inhibit multiple cell types (e.g., mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils) and mediator production or secretion (e.g., histamine, eicosanoids, leukotrienes, and cytokines) involved in the asthmatic response. These anti-inflammatory actions of glucocorticoids may contribute to their efficacy in asthma. Typically, however, the action on the cells affected requires several days. Therefore, inhaled steroids are not used for immediate relief of asthma, but instead as preventive and maintenance therapy.

[edit] Nasal spray

[edit] Dosage

Adults
The recommended dosage for adults is 100 micrograms (two sprays) into each nostril once daily. This may be increased to maximum of twice daily use if required. When control is achieved dose is reduced to 50 micrograms (one spray) to each nostril daily.
Adolescents and children
The recommended dosage for children (4 years of age or older in US, but only from 12 years in UK) is 50 micrograms (one spray) into each nostril once daily. This may be increased to maximum of twice daily use if required.

[edit] Flonase patent issues

GlaxoSmithKline's patent on Flonase expired in May 2004. The Food and Drug Administration (FDA) approved the sale of a generic version of Flonase on February 22, 2006. On February 23, 2006, GlaxoSmithKline (GSK) was able to obtain a temporary 10-day restraining order from a federal judge in Baltimore blocking the shipment and sales of the approved generic versions of Flonase. The restraining order lasted until March 6, 2006. The basis of the complaint by GSK was that the FDA failed to follow its own regulations in approving the generics and failed to apply the same quality standards for the generic version as it did for Flonase. GSK made these arguments in petitions filed with the FDA, but the FDA rejected those petitions. The Maryland District Court denied the request by GSK to extend the ban on Flonase generics beyond March 6, 2006, and GSK released a statement that they would not appeal the ruling.[1] The ruling meant that sales of generic versions of Flonase could proceed.

[edit] References

[edit] Clinical trials

This listing is NOT complete and should NOT be construed as support for treatment decisions. See also PubMed clinical manuscripts referring to fluticasone

both support a positive outcome for use of fluticasone in patients with chronic obstructive pulmonary disease, also referred to as COPD

[edit] External link


Medications commonly used in asthma and COPD (primarily R03) edit
Anticholinergics:

Ipratropium, Tiotropium
Short acting β2-agonists:

Salbutamol, Terbutaline
Long acting β2-agonists (LABA): Clenbuterol, Bambuterol, Formoterol, Salmeterol
Corticosteroids:

Beclometasone, Budesonide, Fluticasone
Leukotriene antagonists:

Montelukast, Pranlukast, Zafirlukast
Xanthines:

Aminophylline, Theobromine, Theophylline
Mast cell stabilizers:

Cromoglicate, Nedocromil
Combination products:

Budesonide/formoterol, Fluticasone/salmeterol, Ipratropium/salbutamol


Corticosteroids - glucocorticoid/receptor and mineralocorticoid/receptor edit
(A07EA, C05AA, D07, D10AA, H02, R01AD, R03BA, S01BA, S02B, and S03B)

Alclometasone, Aldosterone, Amcinonide, Beclometasone, Betamethasone, Budesonide, Ciclesonide, Clobetasol, Clobetasone, Clocortolone, Cloprednol, Cortisone, Cortivazol, Deflazacort, Deoxycorticosterone, Desonide, Desoximetasone, Desoxycortone, Dexamethasone, Diflorasone, Diflucortolone, Difluprednate, Fluclorolone, Fludrocortisone, Fludroxycortide, Flumetasone, Flunisolide, Fluocinolone acetonide, Fluocinonide, Fluocortin, Fluocortolone, Fluorometholone, Fluperolone, Fluprednidene, Fluticasone, Formocortal, Halcinonide, Halometasone, Hydrocortisone/cortisol, Hydrocortisone aceponate, Hydrocortisone buteprate, Hydrocortisone butyrate, Loteprednol, Medrysone, Meprednisone, Methylprednisolone, Methylprednisolone aceponate, Mometasone furoate, Paramethasone, Prednicarbate, Prednisone/Prednisolone, Prednylidene, Rimexolone, Tixocortol, Triamcinolone, Ulobetasol
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