Anti-asthmatic drug

Another example belonging to the class of domino processes initiated by an elimination was described by Gurjar and coworkers in their synthesis of the 2,4-dis-ubshtuted tetrahydrofuran 2-554 [288] this compound is a potent anti-asthmatic drug lead (Scheme 2.125) [289]. 

If patients are on anti-allergic and anti-asthmatic drugs, herbal formulas that stimulate the Qi and excite the Yang should not be used. Formulas that contain sweet and sour herbs that can slow down the Qi movement should also be avoided. 

About 10% of asthmatics are hypersensitive to aspirin, and in some individuals life-threatening bronchoconstriction can occur. This is not a drug-drug interaction but an adverse response of asthmatic patients to aspirin, whether taking an anti-asthmatic drug or not. The reasons are not fully understood. Those known to be sensitive to aspirin may also possibly react to other NSAIDs, in particular the acetylated salicylates, the indole and indene acetic acids, and the propionic acid derivatives (see Table 6.1 , (p.l34)). The fenamates, oxicams, pyrazolones and pyrazolidinediones are better tolerated. The nonacetylated salicylates (sodium salicylate, salicylamide, choline magnesium trisalicylate) are normally well tolerated. Aspirin-sensitive individuals are also less likely to react to nimesulide. ... 

A series of papers deal with the pharmacology of the anti-asthmatic drug ipratropium bromide (32). 

Fujiwara T, Ichimura K. 2002. Surface assisted photoalignment control of lyotropic liquid crystals. Part 2. Photopattterning of aqueous solutions of a water soluble anti asthmatic drug as lyotropic liquid crystals. J Mater Chem 12 3387 3391. 

Fisons. Ironically this company was founded on fertilizer manufacture and for many years this was a strength of the company. However, losses resulted in the whole fertilizer division being sold to Norsk-Hydro in 1982. This helped profits for the company to rise from 9.3 million in 1981 to 21.1 million in 1982. Its major interests are pharmaceuticals—where its most important success has been the anti-asthmatic drug Intal—and agrochemicals. Diversification into making scientific apparatus and laboratory chemicals, and horticultural materials like composts and peat, were tried, but in the 1990s these were sold to leave the company to concentrate on pharmaceuticals. In 1995 two thirds of its pharmaceutical R D activities were sold to Astra Pharmaceuticals. 

Compared to the widespread and long-term use of p-mimetic drugs, typically by nebulization, the few reports involving anti-asthmatic drugs indicate that they are weak allergens (Fung et al. 1996). Aminophyl-line is of importance, since it consists of ethylene diamine and theophylline therefore, positive patch tests to ethylendiamine are present in patients sensitized to aminophylline (see the section entitled Additives ) (Rudzki et al. 1989 Rudzki 1990). 

This molecule occurs widely not only in pharmaceutical products, where it is used for its metal-complex-ing properties in certain creams and as a component of aminophylline, an anti-asthmatic drug, but also in other industrial applications as a stabilizer, solvent, neutralizer, etc. Several occupation-related contact dermatitis cases due to it in the pharmaceutical sector have been described (Hogan 1990 Dias et al. 1995). It may cross-react with piperazine (cf. above). 

Example 5.9 Consider the retrosynthetic analysis of TM 4.9, a key intermediate in the synthesis of the anti-asthmatic drug salbutamol, and then propose the synthesis. Use the dimsyl anion (MeSOCH2US[a as the source of carbene for cyclization of epoxide. 

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