The effect of theophylline and enprofylline on allergen-induced bronchoconstriction

Pauwels, Romain; Renterghem, D. Van; Straeten, M. Van Der; Johannesson, N.; Persson, C. G. A.

doi:10.1016/0091-6749(85)90779-1

Cited by 210 publications

(67 citation statements)

References 29 publications

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“…Several studies have been performed, and have observed either no or only partial protection against the early response [60][61][62][63][64][65][66][67][68][69]. However, all studies except one observed, a marked protective effect against the late asthmatic reaction following allergen challenge ( fig 2).…”

Section: Effect In Allergen Challenge Studiesmentioning

confidence: 99%

Theophylline in the management of asthma: time for reappraisal?

Barnes¹,

Pauwels²

1994

Eur Respir J

248

107

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T Th he eo op ph hy yl ll li in ne e i in n t th he e m ma an na ag ge em me en nt t o of f a as st th hm ma a: : t ti im me e f fo or r r re ea ap pp pr ra ai is sa al l? ?P.J. Barnes*, R.A. Pauwels** Theophylline is now considered to be a bronchodilator, but it is increasingly recognized that theophylline has other anti-asthma activities, which may be more important. Theophylline, even at low plasma concentrations, inhibits the late asthmatic reaction following allergen challenge. These clinical pharmacological observations are substantiated by experimental animal and in vitro data showing that theophylline has several anti-inflammatory activities relevant to asthma. These include the inhibition of cytokine synthesis and release, the inhibition of inflammatory cell activation and microvascular leakage, and the prevention of airway hyperresponsiveness induced by airway inflammation. Theophylline appears to have immunomodulatory effects, even at relatively low plasma concentrations.Based on these considerations, theophylline can be regarded as a useful alternative to other anti-inflammatory drugs for the chronic treatment of mild to moderate asthma. Theophylline should be used at lower doses to achieve plasma concentrations of 5-10 mg·l -1 , which will avoid the risk of side-effects.Further studies are required to evaluate the role of low-dose theophylline as an adjunct to low-dose inhaled steroids in the management of chronic asthma. It may now be appropriate to re-evaluate the role of theophylline in asthma management.

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Section: Effect In Allergen Challenge Studiesmentioning

confidence: 99%

Theophylline in the management of asthma: time for reappraisal?

Barnes¹,

Pauwels²

1994

Eur Respir J

248

107

View full text Add to dashboard Cite

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“…In a clinical study on the steroid-dependent chronic asthma, it has been demonstrated that frequency of asthma symptoms and the doses of beta 2-adrenoceptor stimulants / steroids is less in the theophylline group than in placebo group (3). Another study showed that theophylline inhibited a delayed allergen challengerelated response in patients with asthma (4). In a placebo-controlled double-blind study on atopic bronchial asthma, theophylline inhibited both immediate and delayed responses of the bronchial mucosa to inhalation of allergen (5).…”

Section: Introductionmentioning

confidence: 99%

Anti-inflammatory Effect of Theophylline in Rats and Its Involvement of the Glucocorticoid–Glucocorticoid Receptor System

Watanabe

Yamakami²,

Tsuchiya³

et al. 2008

J Pharmacol Sci

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Abstract. Although theophylline has been suggested to have an anti-inflammatory effect, there have been few reports to show the in vivo effect and the mechanism of anti-inflammatory activity of theophylline experimentally. To reveal the anti-inflammatory activity of theophylline, we studied the effect of theophylline and its metabolites on carrageenan-induced edema in rat foot pad. Subcutaneous injection of theophylline (5 -100 mg / kg) inhibited carrageenan-induced edema dose-dependently. Theophylline metabolites, that is, 1-methylxanthine, 3-methylxanthine, 1-methyluric acid, and 1,3-dimethyluric acid (equimolar dose to 50 mg / kg of theophylline), did not inhibit the edema significantly. The inhibitory effect of theophylline on carrageenan-induced edema disappeared by pretreatment with aminoglutethimide, an inhibitor of glucocorticoid synthesis and with mefepristone, an antagonist of the glucocorticoid receptor. These results suggest that theophylline itself has anti-inflammatory activity and the glucocorticoid-glucocorticoid receptor system is involved in the anti-inflammatory activity of theophylline.

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“…Theophylline is also shown to reduce the need for oral prednisolone to relieve exacerbations that are not only controlled by bronchodilators in asthmatics. [12][13][14][15][16] One approach to increase the effectiveness of pharmacotherapy is to administer drugs while they are most effective and/or best tolerated. The principles of chronotherapy can be realized by choosing the right time for conventional tablets and capsules, or designing and characterizing drug delivery systems to synchronize drug release to the rate of disease activity.…”

Section: Introductionmentioning

confidence: 99%

Comparison of Single- And Multi-Stage Extrusion Versus Press-Coating Technique in Formulation of Modified-Release Tablets With Theophylline

Petkova¹

2017

WJPPS

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Theophylline has been used in the treatment of respiratory diseases such as asthma and COPD for more than 80 years. It is still a common reported drug, especially for patients with a pronounced clinical picture due to its easy application and low price. The bronchodilating action of theophylline makes the drug useful in the chronic treatment of bronchial asthma, but its narrow therapeutic concentration range and variable pharmacokinetics make dosing management of the drug difficult, which requires utilization of modified release drug dosage forms. One approach to increase the effectiveness of pharmacotherapy is to administer medications while they are most effective and/or tolerable. The principles of chronotherapy can be applied by designing and characterizing drug delivery systems that synchronize drug release with the rhythm of disease activity.Time-controlled release rate can be achieved in many ways, but press-coating technology and multiple-unit pellet systems (MUPS) are one of the most promising techniques. For the purpose of the present study -development of chronopharmaceutical system for treatment of nocturnal asthma, nine formulations tablets prepared from pellets via single-(E1-1-E3-1), two-(E1-2-E3-2) and three-stage (E1-3-E3-3) extrusion and nine formulations single-(T1-1-T3-1), two-(T1-2-T3-2) and three-layered (T1-3-T3-3) press-coated tablets using different polymer blends were prepared, characterized and compared. Formulations with HPMC release slower than formulations with CMC Na and increasing viscosity grade of HPMC, leads to decreasing in release rate. Moreover, fastest is the release rate from single-extruded pellets and slowest -from three-stage extruded pellets. Comparing method of preparationpress-coating technique gives faster release of API than multi-stage extrusion. Among all formulations, formulations E1-3, E2-3, E3-3 and T2-3 exhibit the desired chronotherapeutical release profile -taken before bedtime they deliver API between midnight and early morning hours when asthma incidents are with higher frequency. WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

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The effect of theophylline and enprofylline on allergen-induced bronchoconstriction

Cited by 210 publications

References 29 publications

Theophylline in the management of asthma: time for reappraisal?

Theophylline in the management of asthma: time for reappraisal?

Anti-inflammatory Effect of Theophylline in Rats and Its Involvement of the Glucocorticoid–Glucocorticoid Receptor System

Comparison of Single- And Multi-Stage Extrusion Versus Press-Coating Technique in Formulation of Modified-Release Tablets With Theophylline

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