Leprosy Drugs

Question 1

Dapsone MOA

Answer 1

Folate antagonist- competes with para-aminobenzoate for the active site of dihydropteroate synthesis

Question 2

Dapsone is administered with what other drugs in treatment of leprosy?

Answer 2

Rifampicin & Clofazimine

Question 3

Dapsone ADE

Answer 3

Dapsone syndrome: hemolysis, methoglobinemia, hepatitis, jaundice, peripheral neuropathy, hypoalbuminemia, psychosis, leukopenia

Question 4

Other Dapsone ADE

Answer 4

Rash on upper limbs and forehead

Question 5

Yet another Dapsone ADE

Answer 5

Dermatitis, lymphadenopathy (along posterior border of STM muscle), and Stevens-Johnson syndrome

Question 6

Rifampin MOA

Answer 6

Inhibits bacterial DNA dependent RNA polymerase

Question 7

Rifampin ADE

Answer 7

Big one is body fluid discoloration! Also hepatotoxicity, hemolysis, hemoglobinuria, renal failure, and flue like symptoms

Question 8

Rifampin is a CYP inducer or inhibitor?

Answer 8

Inducer –> multiple drug interactions

Question 9

Rifampin metabolism?

Answer 9

Enterohepatic circulation

Question 10

Distribution of Rifampin

Answer 10

Everywhere! Crosses placenta, gets in breast milks, crosses BBB!

Question 11

Clofazimine MOA

Answer 11

Binds to mycobacterial guanine in DNA.. Frequency of mycobacterial guanine & cystine&raquo_space;> in human DNA

Question 12

Clofazimine ADE

Answer 12

1. Staining of body, body fluids, & suckling infant!
2. Feces can appear dark/tarry (would look like GI bleed)
3. Possible hepatitis & jaundice

Question 13

Why does Clofazimine have such long persistence?

Answer 13

It is very lipophilic

Question 14

What adverse drug reaction of leprosy treatment does Clofazimine treat?

Answer 14

Erythema nodosum leprosum (will discuss this more later)

Question 15

What do corticosteroids do for lepors?

Answer 15

Treat type 1 and type 2 adverse drug reactions from leprosy therapy

Question 16

Describe a type 1 adverse reaction

Answer 16

Red patchy skin lesions, erythema, swollen hands/feet, joint pain

Question 17

What is the treatment for a type 1 adverse reaction to leprosy therapy?

Answer 17

Corticosteroids

Question 18

Describe a type 2 adverse reaction

Answer 18

It is aka erythema nodosum leprosum- sudden eruption of numerous painful nodules; neuritis

Question 19

How do you treat a type 2 adverse reaction to leprosy therapy

Answer 19

Corticosteroids, Clofazimine, Thalidomide

Question 20

Thalidomide MOA

Answer 20

Inhibits NFkB (transcription regulation) and TNF-alpha (leukocyte migration)

Question 21

Thalidomide ADE

Answer 21

Teratogen, Increase in plasma HIV viral load (know this!!), rarely peripheral neuropathy