Theophylline is a methylxanthine compound that is used for the treatment of asthma, chronic obstructive pulmonary disease COPD; chronic bronchitis and emphysema, and premature apnea. The bronchodilatory effects of theophylline are useful primarily for patients with asthma because bronchospasm is a key component of that disease state. Even COPD patients without significant bronchospasm demonstrate clinical improvement when taking theophylline. In the chronic management of asthma or chronic obstructive pulmonary disease patients, theophylline is now considered to be adjunctive therapy. Other drugs that are useful in patients with asthma are cromolyn, nedocromil, oral corticosteroids, inhaled anticholinergics, and leukotriene modifiers. Theophylline is also useful in these patients when they are unable or unwilling to use multiple metered dose inhaler MDI devices or if an intravenous drug is needed. The bronchodilatory response via smooth muscle relaxation in the lung to theophylline is postulated to occur by several mechanisms.

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Data extraction One investigator extracted data from all included studies. Search SpringerLink Search. Taxes to be calculated in checkout. PubMed Article Google Scholar 5. PubMed Article Google Scholar About this article Cite this article de Leede, L.

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Aminophylline is a competitive nonselective phosphodiesterase inhibitor that is used to treat airway obstruction from asthma or COPD. Target: Phosphodiesterase Aminophylline is a compound of the bronchodilator theophylline with ethylenediamine in order theophylline. The ethylenediamine improves solubility, and the aminophylline is usually found as a dihydrate. Aminophylline is less potent and shorter-acting than theophylline. Its most common use is in the treatment of airway obstruction from asthma or COPD. It is used off-label as a reversal agent during nuclear stress testing.

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Note that this is a catalog only—not an order theophylline system. Theophylline and its congener, aminophylline, are used to relax smooth muscles of the bronchial airways and pulmonary blood vessels to relieve and prevent symptoms of asthma and bronchospasm. Theophylline has a half-life of 4 hours in children and adult smokers, and 7 hours in nonsmoking adults, thus steady-state is reached in approximately 1 day. The volume of distribution is 0. Theophylline exhibits zero-order clearance kinetics like phenytoin, small increases in dose yield disproportionately large increases in blood concentration. Coadministration of cimetidine and erythromycin will significantly inhibit theophylline clearance, requiring dosage reduction.

Theophylline is structurally classified as a methylxanthine. It occurs as a white, odorless, crystalline powder with a bitter taste. Mechanism of Action: Theophylline has two distinct actions in the airways of patients with reversible obstruction: smooth muscle relaxation i. While the mechanisms of action of theophylline are not known with certainty, studies in animals suggest that bronchodilation is mediated by the inhibition of two isozymes of phosphodiesterase PDE III and, to a lesser extent, PDE IV while non-bronchodilator prophylactic actions are probably mediated through one or more different molecular orders theophylline that do not involve inhibition of PDE III or antagonism of adenosine receptors. The pharmacokinetics of theophylline vary widely among similar patients and cannot be predicted by age, sex, body weight or other demographic characteristics. It is, therefore, recommended that serum theophylline concentrations be measured frequently in acutely ill patients e.

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Methods for the management of bronchopulmonary insufficiency and other conditions are disclosed. The methods involve administration of an Nsubstituted derivative of theophylline selected from the group consisting of dyphylline, etophylline, proxyphylline and mixtures thereof. They can have the same route of administration or different routes of administration; for example, theophylline can be given orally, while the derivative is given as a zero-order intravenous infusion. A high total plasma concentration of methyl xanthine is achieved safely by using a combination of theophylline and one or more of the derivatives. In particular, the present invention relates to particular uses of certain Nsubstituted derivatives of theophylline.

In vitro, a perfect zero-order release rate with the osmotic system was obtained. In all subjects, application of the osmotic system resulted in a constant steady-state theophylline level just as in a long time zero-order i. The in vivo and in vitro release rates were almost identical and subjectindependent. Rent this article via DeepDyve. Controlled Release Pharmaceuticals.

The objective of this work was to use theophylline as a model drug and to predict its pharmacokinetics before, during including prediction of the umbilical cord level, and after pregnancy as well as in milk after single and multiple doses and in neonates using a physiological-based pharmacokinetic PBPK model. Neonatal theophylline exposure from milk consumption was projected in both normal term and preterm subjects. Predicted infant daily doses were calculated using theophylline average and maximum concentration in the milk as well as an estimate of milk consumption. Predicted concentrations and parameters from the PBPK model were compared to the observed data. The PBPK model predicted an average cord-to-maternal plasma ratio of 1.

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