Leprosy drugs

Friedel-Crafts sulfonylation of benzene and its derivatives can also be carried out using iron(III) chloride-based ionic liquids, as was shown by Samant and coworkers [23]. For example, the synthesis of diphenyl sulfone, an important intermediate for the anti-leprosy drug Dapsone, was achieved in 78% yield catalyzed by 1-butyl-3-methylimidazolium chloride combined with FeCl3 (Scheme 6.7). 

More useful sulfur compounds have included the leprosy drug dapsone (Chapter 6), the arthritis drug Feldene... 

Figure7.9 Study of long-running impurities of an anti-leprosy drug. Same detector attenuation for (a) O.lmgml solution (b) l.Omgmr solution. Better signal to noise in situation (b) however estimation of unknown impurities by calculating % of total peak area is more inappropriate than situation (a) since the main peak may well lie outside the linear range.

In chapter 6 we described how the anti-leprosy drug dapsone could be made soluble by the formation of a bisulfite adduct. Now that you know about the reactions described in chapter 11, you should be able to draw a mechanism for this reaction. The adduct is described as a prodrug, meaning that it is not the drug but gives rise to the drug by chemistry within the body. How might this happen ... 

Compounds closely related to the sulfonamide antibiotics proved to be the first drugs effective against Mycobacterium leprae, the causative agent of the disease known since antiquity, leprosy. These drugs are at least partly responsible for the decline of I hose horror spots, the leper colonies. 

Leprosy is a chronic, communicable disease spread by prolonged, intimate contact with an infected person. Peripheral nerves are affected, and skin involvement is present. Lesions may be confined to a few isolated areas or may be fairly widespread over the entire body. Treatment with the leprostatic drugs provides a good prospect for controlling the disease and preventing complications. 

Leprosy, also referred to as Hansen s disease, is caused by the bacterium Mycobacterium leprae. Although rare in colder climates, this disease may be seen in tropical and subtropical zones. Dapsone and clofazimine (Lamprene) are the two drags currently used to treat leprosy. The leprostatic drugs are listed in the Summaiy Drug Table Leprostatic Dragp. 

Clofazimine is primarily bactericidal against M. leprae. The exact mode of action of this drug is unknown. Clofazimine is used to treat leprosy. 

A patient with leprosy is prescribed clofazimine 100 mg daily PO. The drug is available in 200-mg tablets. The nurse administers. ... 

Since the causative organism of leprosy, one of the world s six major diseases, Mycobacterium leprae, is closely related to Mycobacterium tuberculosis, thio-semicarbazones have also been used as second-line drugs in the chemotherapy of leprosy [38]. The most widely used in leprosy treatment has been thiacetazone, and structure-activity relationships for it are similar to those observed for antitubercular thiosemicarbazones [39, 40]. 

McGeer, P.L., Harada, N., Kimura, H., McGeer, E.G. and Schulzer, M. (1992). Prevalence of dementia amongst elderly Japanese with leprosy apparent effect of chronic drug therapy. Dementia 3, 146-149. 

The answers are 484-k 485-j. (tlardman, pp 1061-1062, 1682-1685.) Sulfonamides can cause acute hemolytic anemia. In some patients it mayr be related to a sensitization phenomenon, and in other patients the hemolysis is due to a glucose-6-phosphate dehydrogenase deficiency Sulfamethoxazole alone or in combination with trimethoprim is used to treat UTls. The sulfonamide sulfasalazine is employed in the treatment of ulcerative colitis. Daps one, a drug that is used in the treatment of leprosy, and primaquine, an anti mala rial agent, can produce hemolysis, particularly in patients with a glucose-6-phosphate dehydrogenase deficiency. 

Frequency 45-65% of Caucasians and African Americans 10-15% of Asians Slow inactivation of drugs such as isoniazid (for tuberculosis), dapsone (for leprosy), and hydralazine (for high blood pressure), leading to toxicity from the drug at doses well tolerated in people with rapid acetylator phenotype Clinical consequences depend on the specific side effects of the drugs... 

Mycobacteria are responsible for two diseases tuberculosis, mostly caused by M. tuberculosis, and leprosy due to M. leprae. The therapeutic principle applicable to both is combined treatment with two or more drugs. Combination therapy prevents the emergence of resistant mycobacteria Because the antibacterial effects of the individual substances are additive, correspondingly smaller doses are sufficient Therefore, the risk of individual adverse effects is lowered. Most drugs are active against only one of the two diseases. 

A. Drugs used to treat infections with mycobacteria (1. tuberculosis, 2. leprosy)... 

Clofazimine is a substituted iminophenazine that was first proposed for treating leprosy in 1962 however, it entered into medical practice toward the end of the 1980s. The mechanisms of its action is not definitively known, although there is the assumption that it can inhibit the formation of matrixes with DNA, which leads to a delay in the growth of mycobacteria. Clofazimine exhibits a bactericidal effect between that of dapsone and rifampicin. Synonym of this drug is lamprene. 

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