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DoxofyllineDoxofylline• Last generation methylxanthine• Last generation methylxanthine
derivative for airway obstructions
• Markedly lower affinity for adenosine treceptors
• As effective as the conventional methylxanthines being a bronchodilator y gwith lower risk of adverse reactions
DoxofyllineDoxofylline
• Shows favorable anti-inflammatory effects in the airwaysin the airways
• Retains the inhibitory action on PDE 4 due• Retains the inhibitory action on PDE-4 due to its chemical structure (methylxanthine + dioxolane substitution)
N d f it i l d l l• No need for monitoring plasma drug levels
Tolerability of doxofylline in the maintenance therapy of pediatric patients
Asthma: overall clinical data on 806 children(age 3-16,mean 8;61%≤10 yrs)
54
50
60
35
41
35
40
45% %
29
40
25
30
35
29
20
30
13 1115
20
89
105
10
0
very good good fair poor
0
very good good fair poor
Doxofylline efficacy favorable in 91% Doxofylline safety was favorable in 89%Doxofylline efficacy favorable in 91% Doxofylline safety was favorable in 89%
Bagnoto GF. Eur Rev Med Pharmacol Sci 2000, in press
• 48 studies, 1056 subjects• Total prevalence of side-effects : 15.2%• Overall risk for any adverse event :• Overall risk for any adverse event :
1.8 events per patient-year• Total dropouts : 3%• Treatment interruptions for any reason:• Treatment interruptions for any reason:
0.4 per patient-year
ConclusionConclusionConclusionConclusion• Inhaled steroids are the most effective
controller medications currently avaiabley
• Multicenter study :- Theophylline serumMulticenter study : Theophylline serum conc. <10mcg/ml provided nearly as much effect as an inhaled steroidsmuch effect as an inhaled steroids, beclomethasone, in controlling chronic
thasthma
ConclusionConclusion• Sustained-release theophylline can beSustained release theophylline can be
used as an alternative to inhaled steroids for maintenance therapy insteroids for maintenance therapy in mild persistent asthma
• Sustained-release theophylline can be added with a low dose inhaled steroids in asthma control
ConclusionConclusionD f lli i ff ti i th l t• Doxofylline is effective in the long-term treatment of obstructive pulmonary didiseases
• It is safer and has greater therapeutic index than theophylline orindex than theophylline or aminophylline
• Can be used in children, elderly, i i h CVS CNS d GI dipatients with CVS,CNS and GI diseases
ConclusionConclusionConclusionConclusion• There is no evidence that Doxofylline
effectiveness or adverse events areeffectiveness or adverse events are related to blood levels
• As a consequence there is no need for continued measurements blood level during long-term treatmentg g