Antiasthmatic drugs

The chromone cromolyn sodium (5-5) was at one time considered the forerunner of a novel class of antiallergic and antiasthmatic drugs that act at one of the earliest stages of the allergic reaction. Detailed experiments, acmally conducted after the dmg s clinical effectiveness had been confirmed, suggested that the compound inhibited the release of mediators of the allergic reaction from mast cells. The dmg is not very active when taken orally and is usually applied topically to the lung by insufflation as its sodium salt. Considerable efforts to uncover additional structurally related mediator release inhibitors have had only limited success. 

Stereoselective synthesis of (2Y,7Y)-7-(4-phenoxymethyl)-2-(l-iV-hydroxyureidyl-3-butyn l-yl)oxepane, as a potential antiasthmatic drug candidate, is described <2005TA935>. 

FIGURE 3-4 Relationship between dosing interval and plasma concentrations of the antiasthmatic drug theophylline. A constant intravenous infusion [shown by the smoothly rising line] yields a desired plasma level of 10 mg/L. The same average plasma concentration is achieved when a dose of 224 mg is taken every 8 hours, or a dose of 672 mg every 24 hours. However, note the fluctuations in plasma concentration seen when doses are taken at specific hourly intervals. 

Other Pharmaceuticals. Other pharmaceutical products incorporating the thiophene ring include the antiasthmatic drug Ketotifen [34580-13-7] (Sandoz) (53), which is particularly marketed in Japan. The antifungal drug Tioconazole [65899-73-2] (Pfizer) (54) is based on... 

The addition of MeMgCl to an ester in the presence of CeCb giving a tertiary alcohol was needed in the course of the synthesis of the antiasthmatic drug Singulair.257 It was found that the formation of a specific form of CeClj-THF solvate is crucial for the reaction selectivity (Scheme 85). 

Archer, R.A. Day, W.A. Stereoselective Preparation of Hexahydro dibenzopyranones and Intermediates Therefor 1978 US 4,102,902 Archer, R.A. Lemberger, L. Hexahydro-dibenzo[b,d]pyran-9-ones as Antiasthmatic Drugs 1978 US 4,087,546... 

Kraan J, Koeter GH, vd Mark TW, Sluiter HJ, De Vries K. Changes in bronchial hyperreactivity induced by 4 wk of treatment with antiasthmatic drugs in patients with allergic asthma a comparison between budesonide and terbutaline. J Allergy Clin Immunol 1985 76 636. 

SNAP, or NaNP. By manipulating the chemical structures of MOTA, hypotensive, antithrombotic, thrombolytic, or antiasthmatic drugs might be designed [65]. 

Polymorphism purity. Pressure and temperature influence this property. For instance, salmeterol xinofoate, an antiasthmatic drug, was processed to obtain the right polymorph with a particle size of 5 pm, which is suitable for respiratory delivery (133). More generally, the SEDS process can accurately control these two parameters. 

Pj-selective agonists are used for the relief of acute bronchoconstriction and as a prophylaxis in exercise-induced asthma. Longer-acting p-adrenoceptor agonists can be used prophylactically to decrease nighttime attacks. The mechanisms responsible for their effects are shown in Figure Vl-8-1, which illustrates the action of antiasthmatic drugs. 

Administration of antiasthmatic drugs by inhaled aerosol is usually associated with more adver.se effects than is administration of these drugs by mouth... 

Subgroups of Antiasthmatic Drugs Drugs useful in asthma include bronchodilators (smooth muscle relaxants) and anti-inflammatory drugs (Figure 20-2). Leukotriene antagonists may have both bronchodilator and anti-inflammatory properties. 

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