Systemic bioavailability of inhaled steroids: the importance of appropriate and comparable methodology

Derendorf, Hartmut; Daley‐Yates, Peter T.; Pierre, Lisa N.; Efthimiou, J.

doi:10.1183/09031936.01.17101570

Cited by 13 publications

(9 citation statements)

References 6 publications

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“…Although initial PK studies suggested that the bioavailability of MF was ,1% [64], its systemic activity may be higher, potentially due to the presence of a number of active metabolites that are usually not detected [20,[69][70][71]. Therefore, the clinical relevance of the PK and PD characteristics of MF are still not clear.…”

Section: Modern and Emerging Inhaled Corticosteroidsmentioning

confidence: 99%

Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma

Nave²,

et al. 2006

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The pharmacokinetic and pharmacodynamic effects of inhaled corticosteroids (ICS) have shaped the efficacy and safety of these agents in the treatment of asthma.Important pharmacokinetic and pharmacodynamic characteristics that can enhance the efficacy of ICS include small particle size, high glucocorticoid-receptor-binding affinity, long pulmonary residence time and lipid conjugation. These characteristics can increase or prolong the antiinflammatory effects of an ICS. Important pharmacokinetic characteristics that can enhance the safety of ICS include on-site activation in the lung, low oropharyngeal exposure, negligible oral bioavailability, high protein-binding and rapid systemic clearance.The degree of oropharyngeal exposure is relevant to local side-effects, such as oropharyngeal candidiasis, dysphonia and coughing. Pharmacokinetic properties that influence the degree of systemic exposure are relevant to the pharmacodynamic effect of ICS-induced hypothalamicpituitary-adrenal axis suppression and cortisol suppression, an indicator of potential long-term systemic side-effects, such as reduced growth velocity and bone density, fractures, and skin bruising and thinning.Therefore, significant differences in the pharmacokinetic and pharmacodynamic characteristics of the currently available inhaled corticosteroids warrant careful consideration when used in clinical practice as they may result in differences in efficacy and local and systemic safety profiles.

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Section: Modern and Emerging Inhaled Corticosteroidsmentioning

confidence: 99%

Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma

Nave²,

et al. 2006

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“…5 However, the validity of the conclusion has been questioned. 6,7 The relative receptor affinity (RRA) of MF has been determined by competition assays with transfected COS-1 cells. 8 The relative affinity to the recombinant glucocorticoid receptor was calculated to be 1235, with a binding affinity of dexamethasone defined as 100.…”

Section: Introductionmentioning

confidence: 99%

Human Receptor Kinetics, Tissue Binding Affinity, and Stability of Mometasone Furoate

Valotis

Neukam

Elert

et al. 2004

Journal of Pharmaceutical Sciences

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“…Affrime et al assessed the pharmacokinetics of MF using a LC-MS-MS method with a lower limit of quantification of 50 pg/ml [8]. Because of insufficient sensitivity of the assay, concerns were expressed that a more sensitive assay is needed to adequately describe the pharmacokinetics of this drug after inhalation [9,10]. This paper presents a specific and sensitive atmospheric pressure chemical ionization (APCI) based LC-MS-MS assay using a multiple reaction monitoring technique suitable to quantify MF with sufficient sensitivity in human plasma after oral inhalation of therapeutic doses.…”

Section: Introductionmentioning

confidence: 99%

A sensitive liquid chromatography–tandem mass spectrometry method for the quantification of mometasone furoate in human plasma

Sahasranaman¹,

Tang²,

Biniasz³

et al. 2005

Journal of Chromatography B

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Systemic bioavailability of inhaled steroids: the importance of appropriate and comparable methodology

Cited by 13 publications

References 6 publications

Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma

Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma

Human Receptor Kinetics, Tissue Binding Affinity, and Stability of Mometasone Furoate

A sensitive liquid chromatography–tandem mass spectrometry method for the quantification of mometasone furoate in human plasma

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