Theophylline bronchial asthma

Theophylline reduces contractile activity of smooth musculature, widens bronchi and blood vessels, reduces pulmonary vascular resistance, stimulates the respiratory center, and increases the frequency and power of cardiac contractions. It is used for bronchial asthma, preventing attacks, and systematic treatment. Theophylline is also used for symptomatic treatment of bronchospastic syndrome of a different etiology (chronic obstructive pulmonary disease, chronic bronchitis, and pulmonary emphysema). A large number of combined drags are based on theophylline. Synonyms of theophylline are adophyllin, asthmophyllin, theocin, and many others. 

Bitolterol Prophylaxis and treatment of bronchial asthma and reversible bronchospasm. May be used with or without concurrent theophylline or steroid therapy. 

Theophylline is frequently used as a bronchodilator in the treatment of asthma. The importance of the methylxanthines in the management of bronchial asthma is discussed more fully in Chapter 39. Caffeine as the citrate salt (Cafcit) is used for the short-term management of apnea in premature infants (28-33 weeks of gestational age). 

Among the methylxanthines, aminophylline is most commonly used drug in the treatment of bronchial asthma. It is a stable mixture of theophylline and ethylenediamine. These drugs inhibit the enzyme phosphodiesterase, this inhibition results in higher concentration of intracellular cyclic AMP. 

A target plasma theophylline concentration of 10 mg/L is desired to relieve acute bronchial asthma in a patient. If the patient is a nonsmoker and otherwise normal except for asthma, we may use the mean clearance given in Table 3-1, ie,... 

INHALATIONAL- HALOTHANE TERBUTALINE, THEOPHYLLINE Cases of arrhythmias when these bronchodilators are co-administered with halothane Possibly due to sensitization of the myocardium to circulating catecholamines by the volatile anaesthetics to varying degrees Risk of cardiac events is higher with halothane. Desflurane is irritant to the upper respiratory tract, and t secretions can occur and are best avoided in patients with bronchial asthma. Sevoflurane is non-irritant and unlikely to cause serious adverse effects... 

An excess in mortality from pancreatic cancer has been noted among US male veterans admitted to hospital for bronchial asthma and discharged on various bronchodila-tors, suggesting a possible connection with theophylline... 

Caffeine is a widely used CNS stimulant. Theophylline hK some medical use as a CNS stimulant, but its CNS-iiimulant properties are encountered more often as somc-iimes severe, and potentially life-threatening, side effects of its Use in bronchial asthma therapy. Theobromine has very iitIcCNS activity (probably because of pour physicochemi-iil properties for di.stributiun to the CNS). 

The important use of theophylline and its preparations in bronchial asthma is discu.ssed elsewhere. Caffeine also is reported to have valuable brunchodilating properties in asthma. Finally, because of central vasoconstrictive effects, caffeine has value in treating migraine and tension headaches and truly have actual analgesic properties in (he latter use. 

Because of the extensive use of theophylline for the treatment of bronchial asthma and other cardiorespiratory disorders, many investigations have been carried out by means of gas chromatography to determine theophylline in serum, plasma and saliva. In many cases theophylline has been gas chromatographed as such, in some other cases after derivatization. Methyl derivatives15,16 17,18, n-butyl derivatives19,20,21,22,23,24,25,26, propyl derivatives27, pentyl derivatives and pentafluorobenzyl derivatives 3 have been made in order to obtain better gas chromatographic properties of theophylline and thus better detection possibilities. A number of stationary phases have been applied, from non-polar ones (SE-30) to very polar ones (HI-EFF 8B). OV-17 is the stationary phase that has mostly been used. 

Theophylline is currently being used for the treatment of bronchial asthma and other cardiorespiratory disorders. Because there is good evidence that both the therapeutic response and the toxic side-effects are related to the concentration of the theophylline in the plasma, rather than to its dosage, accurate analytical methods are needed to make it possible to control treatment and reduce the risk of dangerous toxic symptoms. 

Bitolterol is indicated for the prophylaxis and treatment of bronchial asthma and reversible bronchospasm. It may be used with or without concurrent theophylline or steroid therapy. The selective p2-adrenergic stimulants cause bron-chodilation without cardiac acceleration. Metaproterenol and terbutaline are available in tablet form, and terbutaline is also available for subcutaneous injection (see also Figure 94). Metaproterenol and albuterol are available in metered-dose inhalers. 

Dyphylline is a xanthine derivative related to theophylline. It relaxes bronchial smooth muscle and stimulates central respiratory drive. It is indicated in the relief of acute bronchial asthma and reversible bronchospasm associated with chronic bronchitis and emphysema. A large number of derivatives of the methylxanthines have been prepared and examined for their ability to inhibit cyclic nucleotide phosphodiesterases (PDFs) and antagonize receptor-mediated actions of adenosine, the two best characterized cellular actions of the methylxanthines. Although certain modifications dissociate these two activities to some degree, these compounds are not used therapeutically. 

Theophylline, a bronchodilator, is indicated for the symptomatic relief of bronchospasm in patients not currently receiving theophylline who require rapid relief of acute symptoms and for prophylaxis of bronchial asthma, bronchospasm of chronic bronchitis, and emphysema (see also Figure 94). 

Theophylline is widely used for the treatment and symptomatic relief of acute and chronic bronchial asthma, bronchospasm, cardiac dyspnea and angina pectoris. 

Theophylline is a methylated xanthine which exemplifies a clinically useful drug with a narrow margin of safety. Theophylline is used to treat bronchial asthma as well as apnea and bradycardia in premature infants. Serum concentrations must be maintained between 10 and 20 lg/ ml because it is ineffective at lower concentrations and it produces undesirable effects at higher concentrations. 

Theophylline Cellular mech like caffeine. More CNS stimulation than caffeine. Increased cardiac stimulation and diuresis. More effective bronchodilator. Bronchial asthma. Apnea and bradycardia in premature infants (unlabeled use). II M... 

Kawai, M. and Kato, M., Theophylline for the treatment of bronchial asthma present status. Methods Find. Exp. Clin. Pharmacol, 22(5) 309-320, 2000. 

Brocks SM, Sholiton U, Weric EE, Altenau P. The effects of ephedrine and theophylline on dexamethasone metabolism in bronchial asthma. 1977) 17, 308-18. 

Azelastine 2 mg twice daily had no significant effect on the clearance of theophylline 300 mg twice daily in 10 subjects with bronchial asthma. However, one patient had a 20.8% increase and another a 25.3% decrease in clearance. ... 

Nagata M, Tabe K, Houya I, Kiuchi H, Sakamoto Y, Yamamoto K, Dohi Y. The influence of repirinast, an anti-allergic (hug, on theophylline pharmacokinetics in patients witii bronchial asthma. Nihon Kyobu Shikkan Gakkai Zasshi (1991) 29, 413-19. 

Famotidine 40 mg twice daily for 5 days had no effect on the pharmacokinetics of theophylline (given as intravenous aminophylline) in 10 healthy subjects. In another study, 16 patients with bronchial asthma or chronic obstructive pulmonary disease (COPD) found that famotidine 20 mg twice daily for at least 3 days did not affect the clearance of theophylline. Two further studies also found no interaction between intravenous theophylline and famotidine 20 or 40 mg twice daily for 4 or 9 days in COPD... 

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