Dapsone leprosy

The sulfas also remain clinically useful in the treatment of chancroid, lymphogranuloma venereum, trachoma, inclusion conjunctivitis, and the fungus-related nocardiosis (7). In combination with pyrimethamine, they are recommended for toxoplasmosis (8) and have been used for chloroquine-resistant falciparium malaria (4,9). There has also been some use of sulfas for the prophylaxis of rheumatic fever. The sulfone, dapsone, remains an accepted treatment for all forms of leprosy (4). 

During the most active period of investigation of sulfanilamide derivatives, 1935—1944, for systemic bacterial infections, the antimycobacterial activity of 4,4 -dianainodiphenylsulfone [80-08-8] (DDS, dapsone) was discovered (14). Although neither this compound nor its derivatives proved to be clinically usehil for human tuberculosis, it did evolve into the most important type of compound for leprosy (15). The diacetyl derivative has also... 

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. 

Dapsone is bactericidal and bacteriostatic gainst M. leprae. The drag is used to treat leprosy. Dapsone... 

Mr. Winters is very anxious about his newly diagnosed leprosy and his treatment regimen with dapsone. Discuss what you could do to decrease his anxiety. Determine what information you would include when educating Mr. Winters about the treatment regimen. 

Dapsone (diaminodiphenylsulphone Fig. 5.16F) is used specifically in the treatment of leprosy. However, because resistance to dapsone is unfortunately now well known, it is recommended that dapsone be used in conjunction with rifampicin and clofazimine. 

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... 

Dapsone (p. 280) has several therapeutic uses besides treatment of leprosy, it is used for prevention/prophylaxis of malaria, toxoplasmosis, and actinomycosis. 

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. 

In treating resistant forms of malaria, tetracycline is also nsed in combination with pyrimethamine, snlfonamides, snlfones, and dapsone, which is widely used for treating leprosy (as a rnle, in combination with pyrimethamine). 

Rifampicin, a semisynthetic derivative of the antimicrobial agent rifamycin B obtained from Strep-tomyces mediterranei, is bactericidal for intra- and extracellular bacteria. Bacterial RNA synthesis is inhibited by binding to the beta-subunit of DNA-dependent RNA polymerase. Human polymerases are not affected. It has activity against gram-positive and gram-negative cocci, chlamydia as well as mycobacteria. It is used in combination with dapsone for leprosy. 

Acedapsone is a derivative of dapsone that has little activity against M. leprae but is converted to an active dapsone metabolite. It is a long-acting intramuscular repository form of dapsone with a half-life of 46 days. It may prove useful in leprosy patients who cannot tolerate long-term oral dapsone therapy. 

Clofazimine is given to treat sulfone-resistant leprosy or to patients who are intolerant to sulfones. It also exerts an antiinflammatory effect and prevents erythema nodosum leprosum, which can interrupt treatment with dapsone. This is a major advantage of clofazimine over other antileprosy drugs. Ulcerative lesions caused by Mycobacterium ulcerans respond well to clofazimine. It also has some activity against M. tuberculosis and can be used as last resort therapy for the treatment of MDR tuberculosis. 

Occasionally dapsone has been added to the usual chloroqutne therapeutic regimen for the prophylaxis of chloroquine-resistant P. falciparum malaria. It is also used in combination therapy for leprosy. 

The answers are 484-k, 483-j. (Hardman, pp 1061—1062, 1682-1683.) Sulfonamides can cause acute hemolytic anemia. In some patients it may 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 UTIs. The sulfonamide sulfasalazine is employed in the treatment of ulcerative colitis. Dapsone, a drug that is used in the treatment of leprosy, and primaquine, an antimalarial agent, can produce hemolysis, particularly in patients with a glucose-6-phosphate dehydrogenase deficiency. 

PABA) incorporation into folic acid (inhibition of folate synthesis). In large proportion of Mycobacterium leprae infections e.g. in lepromatous leprosy, resistance can develop, so combination of dapsone, rifampicin and clofazimine is used in initial therapy. 

Clofazimine is phenazine dye and used as alternative to dapsone in dapsone intolerant/resistant cases and in combination with dapsone and rifampicin in the multidrug treatment of leprosy. It s probable mechanism of action is its involvement in DNA binding, it may interfere with template function of DNA. 

Mycobacterium leprae has never been grown in vitro, but animal models, such as growth in injected mouse footpads, have permitted laboratory evaluation of drugs. Only those drugs that have the widest clinical use are presented here. Because of increasing reports of dapsone resistance, treatment of leprosy with combinations of the drugs listed below is recommended. 

Several drugs closely related to the sulfonamides have been used effectively in the long-term treatment of leprosy. The most widely used is dapsone (diaminodiphenylsulfone). Like the sulfonamides, it inhibits folate synthesis. Resistance can emerge in large populations of M leprae, eg, in lepromatous leprosy, if very low doses are given. Therefore, the combination of dapsone, rifampin, and clofazimine is recommended for initial therapy. Dapsone may also be used to prevent and treat Pneumocystis jiroveci pneumonia in AIDS patients. 

Rifampin (see earlier discussion) in a dosage of 600 mg daily is highly effective in lepromatous leprosy. Because of the probable risk of emergence of rifampin-resistant M leprae, the drug is given in combination with dapsone or another antileprosy drug. A single monthly dose of 600 mg may be beneficial in combination therapy. 

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). 

Dapsone (Avlosulfon) is a member of a class of chemical agents known as the sulfones. Dapsone is especially effective against M. leprae and is used with rifampin as the primary method of treating leprosy. Dapsone appears to exert its antibacterial effects in a manner similar to that of the sulfonamide drugs that is, dapsone impairs folic acid synthesis by competing with PABA in bacterial cells. Primary adverse effects associated with dapsone include peripheral motor weakness, hypersensitivity reactions (skin rashes, itching), fever, and blood dyscrasias, such as hemolytic anemia. 

Leprosy (Hansen s disease) is caused by M- leprae. Bacilli from skin lesions or nasal discharges of infected patients enter susceptible individuals via the skin or respiratory tract. The World Health Organization recommends the triple drug regimen, dapsone, clofazimine, and rifampin (see p. 333) for 6 to 24 months. 

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

Figure 2.6 Dorzolamide 16, a topically active carbonic anhydrase inhibitor, resulted from a structure-based ligand design it is used for the treatment of glaucoma. Sulfaguanidine 17 inhibits thyroid hormone biosynthesis. A phenylog of sulfanilamide 11 (Figure 2.4), dapsone 18, is used for the treatment of leprosy.

Choice of antimicrobial follows automatically from the clinical diagnosis because the causative organism is always the same, and is virtually always sensitive to the same drug, e.g. meningococcal septicaemia (benzylpenicillin), some haemolytic streptococcal infections, e.g. scarlet fever, erysipelas (benzylpenicillin), typhus (tetracycline), leprosy (dapsone with rifampicin). 

Alycobocteriiim leprae (leprosy) Actinomycetes dapsone + rifampicin clofazimine ethionamide or cycloserine... 

Dapsone, a bacteriostatic sulphone (related to sulphonamides, and acting by the same mechanism, see p. 231), has for many years been the standard drug for the treatment of all forms of leprosy. 

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