Doxofylline: A New Generation Xanthine Bronchodilator Devoid of Major Cardiovascular Adverse Effects

Dini, Frank Lloyd; R, Cogo

doi:10.1185/030079901750120196

Cited by 33 publications

(24 citation statements)

References 38 publications

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“…Doxofylline has emerged as one such drug; studies in animals as well as in human adults and children with obstructive airway disease have found it to be effective and safe. 6,7,8,9,10,11 Doxofylline: structure and mechanism of action Doxofylline is chemically designated as 7-(1,3-dioxolar-2-ylmethyl)-theophylline. It differs from theophylline by the presence of a dioxolone group in position 7 (Fig 1).…”

Section: Pharmacotherapy Of Asthma: Methylxanthinesmentioning

confidence: 99%

Doxofylline: The next generation methylxanthine

2008

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Methylxanthines are widely used in the treatment of asthma. Being one of the few drugs that can be administered orally, they are especially helpful in resource restricted settings. Theophylline, the commonly used methylxanthine drug is associated with a wide range of adverse effects accounting for the poor compliance and high drop-out rates. Moreover, a narrow therapeutic index warrants routine monitoring of its levels in the blood. Doxofylline, a new methylxanthine derivative, is shown to have similar efficacy with significantly less side effects in both animal studies as well as human adults. However, there is a paucity of studies in children with asthma. Retrospective data suggest that 11% patients experienced some side effects, but only 5% reported moderate side effects. Available evidence suggests that it improves spirometric parameters in children with asthma as compared to placebo. Extrapolating data from adult patients, it may be used in place of theophylline as an add on therapy in step 3 and step 4 in children with asthma. Dosage recommended for children> 6 yrs of age is 6 mg/Kg/dose BID. Doxofylline produces stable serum concentrations, hence plasma monitoring is required only in patients with hepatic insufficiency and intolerance to xanthine drugs.

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Section: Pharmacotherapy Of Asthma: Methylxanthinesmentioning

confidence: 99%

Doxofylline: The next generation methylxanthine

2008

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“…Bronchodilator activities of doxofylline have been documented in animal studies and in clinical trials involving patients with either bronchial asthma or COPD [17,18] . Doxofylline has been demonstrated to have bronchodilator activity equal or superior to that of theophylline in spite of its inferior affinity or adenosine receptors A1 and A2 [19] . Doxofylline shares most of the characteristics of methylxanthine drugs; experimental studies have shown that it is associated with less extrarespiratory effects than theophylline [20] .…”

Section: Introductionmentioning

confidence: 98%

“…Moreover, unlike theophylline, doxofylline did not antagonize calcium channel blocker receptors, nor did it interfere with the influx of calcium into the cells [24] . The trials made in asthmatic adults have shown better results or at least equivalent to those of theophylline to relieve the state of broncho-obstruction with less adverse effects [19] . Unlike theophylline, doxofylline does not increase the acid or pepsin output, nor does it produce alterations in the structure and quality of sleep causing insomnia [25,26] .…”

Section: Introductionmentioning

confidence: 99%

Comparative study of the efficacy and safety of theophylline and doxofylline in patients with bronchial asthma and chronic obstructive pulmonary disease

Lal

Manocha

Ray³

et al. 2015

Journal of Basic and Clinical Physiology and Pharmacology

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Background: Bronchial asthma and chronic obstructive pulmonary disease (COPD) are the major obstructive disorders that may contribute to the severity in individual patients. The present study was designed to compare the efficacy and safety of theophylline and doxofylline in patients with bronchial asthma and COPD. Methods: A total of 60 patients, 30 each with bronchial asthma and COPD, were enrolled for the study. Each group of 30 patients received standard treatment for asthma and COPD. Each group was again subdivided into two with 15 patients each, who received theophylline or doxofylline in addition to standard therapy, for a period of 2 months. Each patient was followed up fortnightly for the assessment of efficacy parameters using a pulmonary function test (PFT), clinical symptoms and emergency drug use, and safety was assessed by recording adverse drug reactions. Results: Both theophylline and doxofylline produced enhancements in PFT at different time intervals in both asthma and COPD patients. The maximum beneficial effects were seen at 6 weeks for asthma patients and at 8 weeks for COPD patients for both theophylline and doxofylline. Conclusions:The comparative study showed that doxofylline was more effective as evidenced by improvement in PFT as well as clinical symptoms, and reduced incidence of adverse effects and emergency bronchodilator use.

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“…Doxofylline (DFL) [1][2][3][4][5], chemically known as 7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethylpurine-2,6-dione (Figure 1), is a novel bronchodilator xanthine derivative drug, used in the treatment of bronchial asthma, chronic obstructive pulmonary disease (COPD) and chronic bronchitis. Animal and human studies have shown similar efficacy to theophylline but with significantly less side effects [6].…”

Section: Introductionmentioning

confidence: 99%

“…DFL differs from theophylline for the presence of a dioxalane group in position 7. DFL acts as a phosphodiesterase inhibitor and have decreased affinities toward adenosine A1 and A2 receptors which may account for the better safety profile of the drug [7,8]. The safety profile shows a better tolerability on cardiovascular, digestive and the central nervous systems [9].…”

Section: Introductionmentioning

confidence: 99%

Development and validation of novel analytical methods for estimation of doxofylline in bulk and dosage forms

Sunil¹,

Saradhi

Sekaran³

et al. 2011

Eur. J. Chem.

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KEYWORDSThree simple, sensitive and accurate spectrophotometric methods (A, B and C) were developed to determine doxofylline in bulk and in its dosage forms. Method A is based on charge-transfer complex formation of the drug with p-chloranilic acid. Method B involves the formation of colored chloroform extractable ion-pair complex of the drug with bromophenol blue under acidic condition. Method C is based on ternary complex formation of the drug with molybdenum(V) thiocyanate binary complex. The colored products are quantitated spectrophotometrically at 540, 390 and 690 nm by methods A, B and C, respectively. The variables, which affected the reactions were carefully studied and optimized. The linear ranges for the proposed methods were 4-32 μg/mL (method A & B) and 2-16 μg/mL (method C). Analytical performance of the methods was statistically validated. The proposed methods were successfully applied to the analysis of doxofylline in its dosage forms and were found to be comparable with that of reference method.

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Doxofylline: A New Generation Xanthine Bronchodilator Devoid of Major Cardiovascular Adverse Effects

Cited by 33 publications

References 38 publications

Doxofylline: The next generation methylxanthine

Doxofylline: The next generation methylxanthine

Comparative study of the efficacy and safety of theophylline and doxofylline in patients with bronchial asthma and chronic obstructive pulmonary disease

Development and validation of novel analytical methods for estimation of doxofylline in bulk and dosage forms

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