Antileprotic Drugs

Rifampin is frequently given in combination with one or both of the following agents:

Dapsone is a sulfone that, like sul-fonamides, inhibits dihydrofolate synthesis (p. 272). It is bactericidal against susceptible strains of M. leprae. Dapsone is given orally. The most frequent adverse effect is methemoglobinemia with accelerated erythrocyte degradation (hemolysis).

Clofazimine is a dye with bactericidal activity against M. leprae and anti-inflammatory 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 (t1/2 ~ 70 d). Red-brown skin pigmentation is an unwanted effect, particularly in fair-skinned patients.

Combination therapy

Reduced risk of bacterial resistance

Reduction of dose and of risk of adverse reactions

CNS damage and peripheral neuropathy

(Vit. B6-administration) Liver damage

Mycobacterium tuberculosis

Ethambutol ch3 ch2

ch3 i ch2

h0-ch2-ch hc-ch2-0h hn-lohk-nh

(•«-Isonicotinic acid Nicotinic acid

Optic nerve damage

Optic nerve damage

c-oh p-Aminobenzoic acid

Folate synthesis c-oh p-Aminobenzoic acid

Folate synthesis


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