- StatPearls: Fluticasone [BOOK]
- BOOKStatPearls Publishing: Treasure Island (FL)
- Fluticasone is corticosteroid given via oral, nasal, or topical routes. The route of administration depends on the patient’s diagnoses. Oral fluticasone is FDA-approved to treat asthma and has an off…
Fluticasone is corticosteroid given via oral, nasal, or topical routes. The route of administration depends on the patient’s diagnoses. Oral fluticasone is FDA-approved to treat asthma and has an off label use for chronic obstructive lung disease (COPD) and eosinophilic esophagitis. Inhaled steroids slightly improve lung function and improve symptoms of COPD but do not affect the rate of lung function decline. Nasal fluticasone is used to treat allergic and non-allergic rhinitis, nasal polyps and allergies. The topical route treats atopic dermatitis and dermatoses.
- Inhaled corticosteroids in children with persistent asthma: effects of different drugs and delivery devices on growth. [Review]
- CDCochrane Database Syst Rev 2019 Jun 10; 6:CD010126
- CONCLUSIONS: This review suggests that the drug molecule and delivery device may impact the effect size of ICS on growth in children with persistent asthma. Fluticasone at an equivalent dose seems to inhibit growth less than beclomethasone and budesonide. Easyhaler is likely to have less adverse effect on growth than Turbuhaler when used for delivery of budesonide. However, the evidence from this systematic review of head-to-head trials is not certain enough to inform the selection of inhaled corticosteroid or inhalation device for the treatment of children with persistent asthma. Further studies are needed, and pragmatic trials and real-life observational studies seem more attractive and feasible.
- Long-term use of inhaled glucocorticoids in patients with stable chronic obstructive pulmonary disease and risk of bone fractures: a narrative review of the literature. [Review]
- IJInt J Chron Obstruct Pulmon Dis 2019; 14:1085-1097
- Patients with chronic obstructive pulmonary disease (COPD) demonstrate a greater osteoporosis prevalence than the general population. This osteoporosis risk may be enhanced by treatment with inhaled …
Patients with chronic obstructive pulmonary disease (COPD) demonstrate a greater osteoporosis prevalence than the general population. This osteoporosis risk may be enhanced by treatment with inhaled corticosteroids (ICSs), which are recommended for COPD management when combined with long-acting bronchodilators, but may also be associated with reduced bone mineral density (BMD). We conducted a narrative literature review reporting results of randomized controlled trials (RCTs) of an ICS versus placebo over a treatment period of at least 12 months, with the aim of providing further insight into the link between bone fractures and ICS therapy. As of 16 October 2017, we identified 17 RCTs for inclusion. The ICSs studied were budesonide (six studies), fluticasone propionate (five studies), mometasone furoate (three studies), beclomethasone dipropionate, triamcinolone acetonide, and fluticasone furoate (one each). We found no difference in the number of bone fractures among patients receiving ICSs versus placebo across the six identified RCTs reporting fracture data. BMD data were available for subsets of patients in few studies, and baseline BMD data were rare; where these data were given, they were reported for treatment groups without stratification for factors known to affect BMD. Risk factors for reduced BMD and fractures, such as smoking and physical activity, were also often not reported. Furthermore, a standardized definition of the term "fracture" was not employed across these studies. The exact relationship between long-term ICS use and bone fracture incidence in patients with stable COPD remains unclear in light of our review. We have, however, identified several limiting factors in existing studies that may form the basis of future RCTs designed specifically to explore this relationship.
- OTC drugs for seasonal allergies. [Journal Article]
- MLMed Lett Drugs Ther 2019 Apr 22; 61(1570):57-60
- Health effects of diesel engine exhaust emissions exposure (DEEE) can mimic allergic asthma and rhinitis. [Case Reports]
- AAAllergy Asthma Clin Immunol 2019; 15:31
- CONCLUSIONS: Atypical presentations of adult onset asthma in the absence of a history of either atopy or allergen specific IgE antibody sensitization should trigger in-depth evaluation of occupational exposure in all cases including office workers. Serial monitoring of lung function values should be used for diagnostic and monitoring of the patients.
- Clinical Review Report: Fluticasone Propionate (Aermony Respiclick): (Teva Canada Innovation): Indication: For the maintenance treatment of steroid-responsive bronchial asthma as prophylactic therapy in patients 12 years of age and older [BOOK]
- BOOKCanadian Agency for Drugs and Technologies in Health: Ottawa (ON)
- The objective of this review is to perform a systematic review of the beneficial and harmful effects of Fp MDPI 55 mcg, 113 mcg, and 232 mcg for the maintenance treatment of steroid-responsive bronch…
The objective of this review is to perform a systematic review of the beneficial and harmful effects of Fp MDPI 55 mcg, 113 mcg, and 232 mcg for the maintenance treatment of steroid-responsive bronchial asthma in patients 12 years and older.
- Pulmonary Dissolution of Poorly Soluble Compounds Studied in an ex Vivo Rat Lung Model. [Journal Article]
- MPMol Pharm 2019 Jun 11
- Many inhaled drugs are poorly water soluble, and the dissolution rate is often the rate-limiting step in the overall absorption process. To improve understanding of pulmonary drug dissolution, four p…
Many inhaled drugs are poorly water soluble, and the dissolution rate is often the rate-limiting step in the overall absorption process. To improve understanding of pulmonary drug dissolution, four poorly soluble inhalation compounds (AZD5423 (a developmental nonsteroidal glucocorticoid), budesonide, fluticasone furoate (FF), and fluticasone propionate (FP)) were administered as suspensions or dry powders to the well-established isolated perfused rat lung (IPL) model. Two particle size distributions (d50 = 1.2 μm and d50 = 2.8 μm) were investigated for AZD5423. The pulmonary absorption rates of the drugs from the suspensions and dry powders were compared with historical absorption data for solutions to improve understanding of the effects of dissolution on the overall pulmonary absorption process for poorly soluble inhaled drugs. A physiologically based biopharmaceutical in silico model was used to analyze the experimental IPL data and to estimate a dissolution parameter (kex vivo). A similar in silico approach was applied to in vitro dissolution data from the literature to obtain an in vitro dissolution parameter (kin vitro). When FF, FP, and the larger particles of AZD5423 were administered as suspensions, drug dissolution was the rate-limiting step in the overall absorption process. However, this was not the case for budesonide, which has the highest aqueous solubility (61 μM), and the smaller particles of AZD5423, probably because of the increased surface area available for dissolution (d50 = 1.2 μm). The estimated dissolution parameters were ranked in accordance with the solubility of the drugs, and there was good agreement between kex vivo and kin vitro. The dry powders of all the compounds were absorbed more slowly than the suspensions, indicating that wetting is an important parameter for the dissolution of dry powders. A wetting factor was introduced to the in silico model to explain the difference in absorption profiles between the suspensions and dry powders where AZD5423 had the poorest wettability followed by FP and FF. The IPL model in combination with an in silico model is a useful tool for investigating pulmonary dissolution and improving understanding of dissolution-related parameters for poorly soluble inhaled compounds.
- Airway smooth muscle cells are insensitive to the anti-proliferative effects of corticosteroids: The novel role of insulin growth factor binding Protein-1 in asthma. [Journal Article]
- IImmunobiology 2019 May 23
- Airway remodeling in asthma manifests, in part, as enhanced airway smooth muscle (ASM) mass, due to myocyte proliferation. While the anti-proliferative effects of glucocorticoid (GC) were investigate…
Airway remodeling in asthma manifests, in part, as enhanced airway smooth muscle (ASM) mass, due to myocyte proliferation. While the anti-proliferative effects of glucocorticoid (GC) were investigated in normal ASM cells (NASMC), little is known about such effects in ASM cells derived from asthma subjects (AASMC). We posit that GC differentially modulates mitogen-induced proliferation of AASMC and NASMC. Cells were cultured, starved, then treated with Epidermal growth factor (EGF) (10 ng/ml) and Platelet-derived growth factor (PDGF) (10 ng/ml) for 24 h and/or fluticasone propionate (FP) (100 nM) added 2 h before. Cell counts and flow cytometry analyses showed that FP failed to decrease the cell number of and DNA synthesis in AASMC irrespective of mitogens used. We also examine the ability of Insulin Growth Factor Binding Protein-1 (IGFBP-1), a steroid-inducible gene that deters cell growth in other cell types, to inhibit proliferation of AASMC where FP failed. We found that FP increased IGFBP1 mRNA and protein levels. Interestingly, the addition of IGFBP1 (1 μg/ml) to FP completely inhibited the proliferation of AASMC irrespective to the mitogens used. Further investigation of different signaling molecules involved in ASM growth and GC receptor functions (Protein kinase B (PKB/AKT), Mitogen-activated protein kinases (MAPKs), Focal Adhesion Kinase (FAK)) showed that IGFBP-1 selectively decreased mitogen-induced p38 phosphorylation in AASMC. Collectively, our results show the insensitivity of AASMC to the anti-proliferative effects of GC, and demonstrate the ability of IGFBP1 to modulate AASMC growth representing, hence, a promising strategy to control ASM growth in subjects with GC insensitive asthma.
- Effect of USP Induction Ports, Glass Sampling Apparatus, and Inhaler Device Resistance on Aerodynamic Patterns of Fluticasone Propionate-Loaded Engineered Mannitol Microparticles. [Journal Article]
- APAAPS PharmSciTech 2019 May 23; 20(5):197
- The present investigation is to study the effect of two different induction ports (IP), i.e., USP IP and USP-modified IP equipped with andersen cascade impactor on in vitro aerodynamic performance al…
The present investigation is to study the effect of two different induction ports (IP), i.e., USP IP and USP-modified IP equipped with andersen cascade impactor on in vitro aerodynamic performance along with the impact of USP-modified glass sampling apparatus on delivered dose uniformity of fluticasone propionate (FP) dry powder inhaler (DPI). FP DPI was fabricated by spray drying technique using engineered mannitol microparticles (EMP) with different force controlling agents, i.e., leucine and magnesium stearate. Additionally, commercially available two DPI inhaler devices namely Handihaler® and Breezhaler® were used to aerosolize the FP blends. Spherical smooth surface of EMP showed good powder flow properties and acceptable percentage content uniformity (> 95%). Amounts of FP deposited in cascade assembly using USP-modified IP with the Breezhaler® device was significantly higher (1.32-fold) as compared with the Handihaler® device. Moreover, USP-modified IP showed better deposition as compared with USP IP. Additionally, both inhaler devices showed a satisfactory delivered dose (> 105%) for FP using modified glass sampling apparatus at a flow rate of 60 L/min for 2 s. It was interesting to note that not only formulation properties but also IP geometry and device resistance have significant impact on DPI deposition pattern. This study is a first detailed account of aerodynamic performance of FP using USP-modified IP and USP-modified glass sampling apparatus. Thus, it can be of potential importance for both the academic and industry perspective.
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- CADTH Canadian Drug Expert Committee Recommendation: Fluticasone Propionate (Aermony Respiclick — Teva Canada Innovation): Indication: Maintenance treatment of asthma in patients 12 years of age and older [BOOK]
- BOOKCanadian Agency for Drugs and Technologies in Health: Ottawa (ON)