Imported drugs

The important drug sulphapyridine (or M. B. 693 or 2-sulphaniIyl-aminopyridine) may be readily synthesised from 2-aminopyridine and p-acet-amidobenzenesulplionyl chloride (Section IX,9) as follows ... 

There are relarively few important drugs which are alicyclic. Other than inhalation anesthetics, which are a special case, the compounds in the acyclic aliphatic class owe their activity to the functionality present and its specific spacing on the aliphatic framework. Thus, in most instances, the framework itself is not of comparable importance to the functionality attached to it. 

Pharmaceuticals and intermediates represent another important class of compounds. General classes of drugs that may well lend themselves to the IBC technology include the chiral non-steroidal anti-inflammatory profen drugs, norephedryns, and intermediates for a number of important drug classes including (i-blockers and racemic switch candidates. 

Therapeutically t-PA and urokinase are the most important drugs for fibrinolytic therapy (myocardial infarction, stroke, massive pulmonary embolism). This treatment is associated with an enhanced risk of bleeding complications. 

Drug Interactions. Table 1 Examples of clinically important drug interactions due to enzyme inhibition... 

PTKs have been implicated in the regulation of a variety of biological responses such as cell proliferation, migration, differentiation, and survival. They have been demonstrated to play significant roles in the development of many disease states, including immunodeficiency, atherosclerosis, psoriasis, osteoporosis, diabetes, and cancer. In recent clinical trials impressive antitumor effects of PTK inhibitors have been observed. In future, PTK inhibitors may therefore become important drugs for the treatment of specific cancers. 

D rug Lis ts—replacing the chapter outiine is a listing of the classifications and drugp discussed in the chapter. This new format allows the student to quickly identify the important drugs discussed in the chapter. 

However, acyclic nucleotide analogs (acyclic nucleoside phosphonates) have been developed, which carry one phosphonate moiety and require only the two subsequent phosphorylation steps (De Clercq et al. 1978). Independent of virus-encoded kinases, they display a broader spectrum of efficacy. This class comprises important drugs against HIV (tenofovir) and HBV (adefovir, tenofovir), as well as cidofovir, which is approved for use against CMV retinitis, but also displays an exceptionally broad efficacy profile against many herpesviruses, adenovirus, poxviruses, and papillomaviruses (De Clercq and Holy 2005). 

Table 53-2. Some important drug reactions due to mutant or polymorphic forms of enzymes or...

Roxithromycin has similar in vitro activity to erythromycin but enters leucocytes and macrophages more rapidly with higher concentrations in the lysosomal component of the phagocytic cells. It is likely to become an important drug against Legionella pneumophila. Clarithromycin is also of potential value. 

Over 10000 quinolone antibacterial agents have now been synthesized. Nalidixic acid is regarded as the progenitor of the new quinolones. It has been used for several years as a clinically important drug in the treatment of urinary tract infections. Since its clinical introduction, other 4-quinolone antibacterials have been synthesized, some of which show considerably greater antibacterial potency. Furthermore, this means that many types of bacteria not susceptible to nahdixic acid therapy m be sensihve to the newer derivahves. The most important development was the introduction of a fluorine substituent at C-6, which led to a considerable increase in potency and spectrum of activity compared with nalidixic add. These second-generation quinolones are known as fluoroquinolones, examples of which are ciprofloxacin and norfloxacin (Fig. 5.19). 

Aiken J. Panel criticizes FDA inspections of imported drugs. (CNN Online report, 9 June 2000.1 http //www.cnn.eom/2000/HEALTH/06/09/tainted.drugs/index.html. 

Multistep Syntheses natural substances,32 and it is currently an important drug in cancer chemotherapy. 

Warfarin is prone to numerous clinically important drug-... 

Theophylline is also considered an alternative to inhaled corticosteroids for the treatment of mild persistent asthma however, limited efficacy compared to inhaled corticosteroids, a narrow therapeutic index with life-threatening toxicity, and multiple clinically important drug interactions have severely limited its use. Theophylline causes bronchodilation through inhibition of phosphodiesterase and antagonism of adenosine and appears to have anti-inflammatory and immunomodulatory properties as well.36... 

Explain the use of drugs as first-line therapy in bipolar disorder, including appropriate dosing, expected therapeutic effects, potential adverse effects, and important drug-drug interactions. 

Cite important drug interactions with oral contraceptives. 

There are several important drug-drug interactions with allopurinol. The effects of both theophylline and warfarin may be potentiated by allopurinol. Azathioprine and 6-mercaptopurine are purines whose metabolism is inhibited... 

The Import Drugs Act—the first federal statute to ensure the quality of drugs—was passed when quinine used by American troops in Mexico to treat malaria was found to be adulterated... 

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