Clofazimine

Clofazimine [2>(4>chloroanilino)>3-isopropylimino>5>(4-chlorophenyl)-3,4-dihydrophen-azine] [2030-63-9] M 473.5, m 210-212°. Recrystd from acetone. 

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. 

Clofazimine may cause pigmentation of the skin, abdominal pain, diarrhea, nausea, and vomiting. 

Mr. York has been prescribed clofazimine daily to manage his leprosy. Discuss what preadministration assessments the nurse should make. Explain what information you would include in a teaching plan for Mr. York. 

Which of the following adverse reactions would die nurse expect with the administration of clofazimine ... 

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

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. 

K Peters, S Leitzke, SE Diederichs, K Borner, H Hahn, RE Muller, S Ehlers. Preparation of a clofazimine nanosuspension for intravenous use and evaluation of its therapeutic efficacy in murine Mycobacterium avium infection. J Antimicrobial Chemother 45(l) 77-83,2000. 

Others (against mycobacteria) Clofazimine, ethionamide, and rifampicin Gram-positive and mycobacteria... 

Ampicillin sodium Amylobarbitone Betamethasone Betamethasone valerate Carbenicillin disodium Chloroquine phosphate Chloroquine sulphate Cemetidine Clofazimine Clofibrate Clonidine... 

Clofazimine is a dye with bactericidal activity against M. leprae and antiinflammatory properties. It is given orally, but is incompletely absorbed. Because of its high lipophilicity, it accumulates in adipose and other tissues and leaves the body only rather slowly (ti/2 - 70 d). Red-brown skin pigmentation is an unwanted effect, particularly in fair-skinned patients. 

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. 

JR Oreilly, OI Corrigan, CM Odriscoll. The effect of mixed micellar systems, bile salt fatty acid, on the solubility and intestinal absorption of clofazimine (B663) in the anesthetized rat. Int J Pharm 109 147-154, 1994. 

Agents used for the management of leprosy are dap-sone, rifampicin, clofazimine and recently thalido-... 

Clofazimine is a phenazine dye with some my-cobactericidal activity. It is only used in combination with dapsone to reduce the emerging resistance against dapsone. Its efficacy in the management of erythema nodosum leprosum is based on its antiinflammatory activity. 

Clofazimine has some activity against M. tuberculosis and is used as a last resort drug for the treatment of MDR tuberculosis. It is primarily used in the treatment of M. leprae and M. avium-intracellulare. Further details are discussed later, under the treatment of leprosy. 

Dapsone, combined with other antUeprosy agents like rifampin and clofazimine, is used in the treatment of both multibacillary and paucibacillary M. leprae infections. Dapsone is also used in the treatment and prevention of Pneumocystis carinii pneumonia in AIDS patients who are allergic to or intolerant of trimethoprim-sulfamethoxazole. 

Clofazimine is a weakly bactericidal dye that has some activity against M. leprae. Its precise mechanism of action is unknown but may involve mycobacterial DNA binding. Its oral absorption is quite variable, with 9 to 70% of the drug eliminated in the feces. Clofazimine achieves significant concentrations in tissues, including the phagocytic cells it has a plasma half-life of 70 days. It is primarily excreted in bile, with less than 1% excretion in urine. 

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. 

The most disturbing adverse reaction to clofazimine is a red-brown discoloration of the skin, especially in light-skinned persons. A rare but serious adverse reaction is acute abdominal pain significant enough to warrant exploratory laparotomy or laparoscopy. Other infrequent side effects include splenic infarction, bowel obstruction, paralytic ileus, and upper GI bleeding. 

Ethionamide and prothionamide are weakly bacteriocidal against M. leprae and can be used as alternatives to clofazimine in the treatment of MDR leprosy. Both cause GI intolerance and are expensive. 

Pfiarmacokinetics Variable absorption following PO administration. Due to its high lipophilicity, clofazimine is deposifed primarily in fatty tissue. Metabolized in liver. Primarily excreted in feces and minimal elimination in mine. Half life 70 days (following long f erm f herapy). 

Use in conjunction with either rifampin or clofazimine to prevent development of drug resistance and reduce infectiousness of patient with leprosy more quickly... 

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. 

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