Treatment of Bronchial Asthma

How might a reductive animation be used to synthesize ephediine, an amino alcohol that is widely used for the treatment of bronchial asthma ... 

Ma Huang (Ephedra sinica) is another potentially harmful herb that is available in the United States. Claims of utility of Ma Huang for the treatment of bronchial asthma, cold and flu symptoms, fevers or chills, headaches and other aches, edema, and lack of perspiration have been made [23], Ma Huang contains approximately 1% of ephedrine and therefore possesses central nervous stimulatory potential [24], However, ephedrine is difficult to extract and purify from Ma Huang, so it presently has no street value. 

Bronchodilation. P2-Adrenocep-tor-mediated bronchodilation (e.g., with terbutaline, fenoterol, or salbutamol) plays an essential part in the treatment of bronchial asthma (p. 328). 

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

Uniabeied Uses Adjunct treatment of bronchial asthma... 

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. 

The 1,2-azole family of heterocycles is important in medicine. For example, the following dmg used in the treatment of bronchial asthma possesses a substituted isoxazole system. 

Isoprenaline occasionally has a place in the management of cardiac conditions in which bradycardia is a feature, e.g. low cardiac output associated with slow heart rate after extracorporeal circulation in patients with excessive p-blocking therapy. It may also be used in the treatment of overdose with (3-adrenoceptor antagonists and for refractory bradyarrhythmias prior to cardiac pacing. Isoprenaline is used in the treatment of bronchial asthma on account of its 32 effects. 

Bruun E Specific treatment of bronchial asthma in Jamar JM (ed) International Textbook of Allergy. Copenhagen, Munksgaard, 1959, pp 271—297. 

Let us now consider the synthesis of isoxazole 4.28, a drug for the treatment of bronchial asthma. The most direct preparation of isoxazolyl ketone 4.24 is the cycloaddition of unstable bromonitrile oxide 4.22 (prepared in situ by dehydrobromination of 4.21) with acetylenic ketone 4.23. Observe the regioselectivity of this reaction. Both electron-donating and electron-withdrawing groups on the acetylenic components in such cycloadditions tend to occur at the C5 position in the final isoxazole and not at C4. Bromination of ketone 4.24 affords bromoketone 4.25 which is 4.23 n... 

The red, violet, and blue pigments of flower petals are called anthocyanins, and are glycosides of various benzopyrilium cations. Delphinidin chloride 9.7, for example, is a blue pigment. Khellin 9.8 is a natural product which has found clinical application in the treatment of bronchial asthma and has been the starting point for the design of many totally synthetic chromones with improved biological properties. 

Other examples of twin drugs are the antioxidant probucol, which lowers the cholesterol level in blood, and cromolyn, a chromone heterocycle, which is useful in the inhalational treatment of bronchial asthma (Fig. 1.11). 

Isoprenaline (isopropylnoradrenaline) is a nonselective p-receptor agonist, i.e. it activates both Pj-and Pj-receptors. It relaxes smooth muscle, including that of the blood vessels, has negligible metabolic or vasoconstrictor effects, but a vigorous stimulant effect on the heart. This latter is its main disadvantage in the treatment of bronchial asthma. Its principal uses are in complete heart block and occasionally in cardiogenic shock (h3rpotension). 

Muranaka M, Miyamoto T, ShidaT, Kabe J, Makino S, Okumura H,Takeda K, Suzuki S, Horiuchi Y. Gold salt in the treatment of bronchial asthma - a double blind study. Ann Allergu 1978 40 132-137. 

According to Bernoulli and Lehmann (2), Jurasthmol is a powder for the treatment of bronchial asthma and contains antipyrine, acetanilide, citrated caffeine, and lobeline sulfate, together with minute amounts of digitalin and strophan-thin. By reference to the Modern Drug Encyclopedia (13), the pharmacist can select a corresponding American proprietary remedy and adjust the prescription to fit the number of powders to the requirement of the demand for six original packages (of 15 powders each). 

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. 

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