Pharmacokinetics and pharmacodynamics of inhaled corticosteroids

Derendorf, Hartmut; Hochhaus, Günther; Meibohm, Bernd; Möllmann, H; Barth, Jürgen

doi:10.1016/s0091-6749(98)70156-3

Cited by 196 publications

(148 citation statements)

References 14 publications

Supporting

Mentioning

141

Contrasting

Unclassified

Order By: Relevance

“…We identified 65 corticosteroids for which relative receptor binding affinity was available, [33][34][35][36][37][38][39] though data for system clearance, plasma protein binding and oral bioavailability were not found for all 65 compounds. Note that the literature reported slightly different experimental values for several compounds so averaged values were used.…”

Section: Resultsmentioning

confidence: 99%

“…Note that some desired pharmacokinetic and pharmacodynamic properties have already been identified to guide future GR ligand development. [32][33][34][35][36] These properties are important in identifying pulmonary selectivity, such as binding affinity, oral bioavailability, systemic clearance and plasma protein binding.…”

Section: Motivationmentioning

confidence: 99%

“…Currently, the corticosteroid with the highest systemic clearance is beclomethasone dipropionate at 150 L/h 34 and this provides a basis during drug design.…”

Section: Motivationmentioning

confidence: 99%

See 2 more Smart Citations

Signature molecular descriptor : advanced applications.

Visco¹

2010

View full text Add to dashboard Cite

In this work we report on the development of the Signature Molecular Descriptor (or Signature) for use in the solution of inverse design problems as well as in highthroughput screening applications. The ultimate goal of using Signature is to identify novel and non-intuitive chemical structures with optimal predicted properties for a given application. We demonstrate this in three studies: green solvent design, glucocorticoid receptor ligand design and the design of inhibitors for Factor XIa.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Motivationmentioning

confidence: 99%

See 1 more Smart Citation

Signature molecular descriptor : advanced applications.

Visco¹

2010

View full text Add to dashboard Cite

show abstract

“…One potential negative predictor for the risk of relapse is the use of ICS in ICEP with asthma despite the lack of efficacy of ICS as monotherapy [6,11]. The role for inhaled corticosteroids is well described in airway diseases such as asthma, cystic fibrosis and bronchiectasis [6,16]. Some reports do suggest that both mucosal and submucosal endobronchial lesions may be a feature of ICEP [5,17].…”

Section: Discussionmentioning

confidence: 99%

Chronic Eosinophilic Pneumonia: Adjunctive Therapy With Inhaled Steroids

Chan

DeLapp

Nystrom

2016

Chest

View full text Add to dashboard Cite

a b s t r a c tIdiopathic chronic eosinophilic pneumonia (ICEP) is a rare form of diffuse parenchymal lung disease first identified by Carrington et al. in 1969. It is characterized by the presence of constitutional and respiratory symptoms with associated peripheral opacities on imaging and elevated serum and/or bronchoalveolar eosinophilia. Although data is limited regarding etiology or prevalence, it is known that ICEP has a 2:1 female: male predominance and typically affects non-smokers. Diagnosis rests on the clinical constellation of respiratory symptoms of at least 2e4 weeks duration, the presence of diffuse pulmonary alveolar consolidation, classically described as the "photographic negative of pulmonary edema", the presence of eosinophils !40% on bronchoalveolar lavage or !1000/mm 3 eosinophils on peripheral blood and the exclusion of other known causes of eosinophilic lung diseases such as drugs, toxins, fungi, parasites, and collagen-vascular disorders. A dramatic response is achieved with systemic corticosteroids, which is typically dosed over 6 months to 1 year. Despite this response, approximately 30e50% of patients will relapse upon cessation of steroids or during the taper. Although these patients respond well to another trial of steroids, the side effects of long term steroids are well known, including osteoporosis, diabetes, hypertension and cataracts. Inhaled corticosteroids as monotherapy has been trialed in the past without success. However, we report a case of a patient who underwent treatment with systemic corticosteroids followed by inhaled steroids who has remained in remission for 2 years.

show abstract

“…This is simply a matter of distribution and not of equilibrium. After oral administration, fluticasone distributes to fatty tissues and not to the lungs [5].…”

mentioning

confidence: 99%

Establishing bioequivalence for orally inhaled drug products

Arieta¹

2011

Expert Opinion on Drug Delivery

View full text Add to dashboard Cite

Pharmacokinetics and pharmacodynamics of inhaled corticosteroids

Cited by 196 publications

References 14 publications

Signature molecular descriptor : advanced applications.

Signature molecular descriptor : advanced applications.

Chronic Eosinophilic Pneumonia: Adjunctive Therapy With Inhaled Steroids

Establishing bioequivalence for orally inhaled drug products

Contact Info

Product

Resources

About