Benefit: Risk Profile of Budesonide in Obstructive Airways Disease

Donald P Tashkin (Lead / Corresponding author), Brian Lipworth, Ralph Brattsand

Research output: Contribution to journalReview article

23 Downloads (Pure)

Abstract

Airway inflammation is a major contributing factor in both asthma and chronic obstructive pulmonary disease (COPD) and represents an important target for treatment. Inhaled corticosteroids (ICS) as monotherapy or in combination therapy with long-acting β2-agonists or long-acting muscarinic antagonists are used extensively in the treatment of asthma and COPD. The development of ICS for their anti-inflammatory properties progressed through efforts to increase topical potency and minimise systemic potency and through advances in inhaled delivery technology. Budesonide is a potent, non-halogenated ICS that was developed in the early 1970s and is now one of the most widely used lung medicines worldwide. Inhaled budesonide's physiochemical and pharmacokinetic/pharmacodynamic properties allow it to reach a rapid and high airway efficacy due to its more balanced relationship between water solubility and lipophilicity. When absorbed from the airways and lung tissue, its moderate lipophilicity shortens systemic exposure, and its unique property of intracellular esterification acts like a sustained release mechanism within airway tissues, contributing to its airway selectivity and a low risk of adverse events. There is a large volume of clinical evidence supporting the efficacy and safety of budesonide, both alone and in combination with the fast- and long-acting β2-agonist formoterol, as maintenance therapy in patients with asthma and with COPD. The combination of budesonide/formoterol can also be used as an as-needed reliever with anti-inflammatory properties, with or without regular maintenance for asthma, a novel approach that is already approved by some country-specific regulatory authorities and currently recommended in the Global Initiative for Asthma (GINA) guidelines. Budesonide remains one of the most well-established and versatile of the inhaled anti-inflammatory drugs. This narrative review provides a clinical reappraisal of the benefit:risk profile of budesonide in the management of asthma and COPD.

Original languageEnglish
Pages (from-to)1757-1775
Number of pages19
JournalDrugs
Volume79
Issue number16
Early online date23 Sep 2019
DOIs
Publication statusPublished - Nov 2019

Fingerprint

Budesonide
Asthma
Chronic Obstructive Pulmonary Disease
Adrenal Cortex Hormones
Anti-Inflammatory Agents
Lung
Muscarinic Antagonists
Esterification
Therapeutics
Solubility
Pharmacokinetics
Maintenance
Guidelines
Inflammation
Technology
Safety
Water
Pharmaceutical Preparations

Cite this

Tashkin, Donald P ; Lipworth, Brian ; Brattsand, Ralph. / Benefit : Risk Profile of Budesonide in Obstructive Airways Disease. In: Drugs. 2019 ; Vol. 79, No. 16. pp. 1757-1775.
@article{25f04327e0f24b6ca31ad5a80fa91a2c,
title = "Benefit: Risk Profile of Budesonide in Obstructive Airways Disease",
abstract = "Airway inflammation is a major contributing factor in both asthma and chronic obstructive pulmonary disease (COPD) and represents an important target for treatment. Inhaled corticosteroids (ICS) as monotherapy or in combination therapy with long-acting β2-agonists or long-acting muscarinic antagonists are used extensively in the treatment of asthma and COPD. The development of ICS for their anti-inflammatory properties progressed through efforts to increase topical potency and minimise systemic potency and through advances in inhaled delivery technology. Budesonide is a potent, non-halogenated ICS that was developed in the early 1970s and is now one of the most widely used lung medicines worldwide. Inhaled budesonide's physiochemical and pharmacokinetic/pharmacodynamic properties allow it to reach a rapid and high airway efficacy due to its more balanced relationship between water solubility and lipophilicity. When absorbed from the airways and lung tissue, its moderate lipophilicity shortens systemic exposure, and its unique property of intracellular esterification acts like a sustained release mechanism within airway tissues, contributing to its airway selectivity and a low risk of adverse events. There is a large volume of clinical evidence supporting the efficacy and safety of budesonide, both alone and in combination with the fast- and long-acting β2-agonist formoterol, as maintenance therapy in patients with asthma and with COPD. The combination of budesonide/formoterol can also be used as an as-needed reliever with anti-inflammatory properties, with or without regular maintenance for asthma, a novel approach that is already approved by some country-specific regulatory authorities and currently recommended in the Global Initiative for Asthma (GINA) guidelines. Budesonide remains one of the most well-established and versatile of the inhaled anti-inflammatory drugs. This narrative review provides a clinical reappraisal of the benefit:risk profile of budesonide in the management of asthma and COPD.",
author = "Tashkin, {Donald P} and Brian Lipworth and Ralph Brattsand",
note = "This manuscript was supported with funding for medical writing assistance by AstraZeneca, in accordance with Good Publication Practice (GPP3) guidelines (http://www.ismpp.org/gpp3).",
year = "2019",
month = "11",
doi = "10.1007/s40265-019-01198-7",
language = "English",
volume = "79",
pages = "1757--1775",
journal = "Drugs",
issn = "1179-1950",
publisher = "Springer Verlag",
number = "16",

}

Benefit : Risk Profile of Budesonide in Obstructive Airways Disease. / Tashkin, Donald P (Lead / Corresponding author); Lipworth, Brian; Brattsand, Ralph.

In: Drugs, Vol. 79, No. 16, 11.2019, p. 1757-1775.

Research output: Contribution to journalReview article

TY - JOUR

T1 - Benefit

T2 - Risk Profile of Budesonide in Obstructive Airways Disease

AU - Tashkin, Donald P

AU - Lipworth, Brian

AU - Brattsand, Ralph

N1 - This manuscript was supported with funding for medical writing assistance by AstraZeneca, in accordance with Good Publication Practice (GPP3) guidelines (http://www.ismpp.org/gpp3).

PY - 2019/11

Y1 - 2019/11

N2 - Airway inflammation is a major contributing factor in both asthma and chronic obstructive pulmonary disease (COPD) and represents an important target for treatment. Inhaled corticosteroids (ICS) as monotherapy or in combination therapy with long-acting β2-agonists or long-acting muscarinic antagonists are used extensively in the treatment of asthma and COPD. The development of ICS for their anti-inflammatory properties progressed through efforts to increase topical potency and minimise systemic potency and through advances in inhaled delivery technology. Budesonide is a potent, non-halogenated ICS that was developed in the early 1970s and is now one of the most widely used lung medicines worldwide. Inhaled budesonide's physiochemical and pharmacokinetic/pharmacodynamic properties allow it to reach a rapid and high airway efficacy due to its more balanced relationship between water solubility and lipophilicity. When absorbed from the airways and lung tissue, its moderate lipophilicity shortens systemic exposure, and its unique property of intracellular esterification acts like a sustained release mechanism within airway tissues, contributing to its airway selectivity and a low risk of adverse events. There is a large volume of clinical evidence supporting the efficacy and safety of budesonide, both alone and in combination with the fast- and long-acting β2-agonist formoterol, as maintenance therapy in patients with asthma and with COPD. The combination of budesonide/formoterol can also be used as an as-needed reliever with anti-inflammatory properties, with or without regular maintenance for asthma, a novel approach that is already approved by some country-specific regulatory authorities and currently recommended in the Global Initiative for Asthma (GINA) guidelines. Budesonide remains one of the most well-established and versatile of the inhaled anti-inflammatory drugs. This narrative review provides a clinical reappraisal of the benefit:risk profile of budesonide in the management of asthma and COPD.

AB - Airway inflammation is a major contributing factor in both asthma and chronic obstructive pulmonary disease (COPD) and represents an important target for treatment. Inhaled corticosteroids (ICS) as monotherapy or in combination therapy with long-acting β2-agonists or long-acting muscarinic antagonists are used extensively in the treatment of asthma and COPD. The development of ICS for their anti-inflammatory properties progressed through efforts to increase topical potency and minimise systemic potency and through advances in inhaled delivery technology. Budesonide is a potent, non-halogenated ICS that was developed in the early 1970s and is now one of the most widely used lung medicines worldwide. Inhaled budesonide's physiochemical and pharmacokinetic/pharmacodynamic properties allow it to reach a rapid and high airway efficacy due to its more balanced relationship between water solubility and lipophilicity. When absorbed from the airways and lung tissue, its moderate lipophilicity shortens systemic exposure, and its unique property of intracellular esterification acts like a sustained release mechanism within airway tissues, contributing to its airway selectivity and a low risk of adverse events. There is a large volume of clinical evidence supporting the efficacy and safety of budesonide, both alone and in combination with the fast- and long-acting β2-agonist formoterol, as maintenance therapy in patients with asthma and with COPD. The combination of budesonide/formoterol can also be used as an as-needed reliever with anti-inflammatory properties, with or without regular maintenance for asthma, a novel approach that is already approved by some country-specific regulatory authorities and currently recommended in the Global Initiative for Asthma (GINA) guidelines. Budesonide remains one of the most well-established and versatile of the inhaled anti-inflammatory drugs. This narrative review provides a clinical reappraisal of the benefit:risk profile of budesonide in the management of asthma and COPD.

U2 - 10.1007/s40265-019-01198-7

DO - 10.1007/s40265-019-01198-7

M3 - Review article

C2 - 31549299

VL - 79

SP - 1757

EP - 1775

JO - Drugs

JF - Drugs

SN - 1179-1950

IS - 16

ER -