Anti-Leprosy agents

Question 1

tx for tuberculous leprosy

Answer 1

Dapsone, Rifampin x 12 months

Question 2

tx for lepromatous leprousy

Answer 2

Dapsone, Rifampin, Clofazamine x 24 months

Question 3

vector for leprosy

Answer 3

humans and dillos

Question 4

geopgraphic distribution leprosy

Answer 4

india and brazil…very rare in America (100 cases)

Question 5

lepromatous pt.’s who cannot tolerate clofazamine get

Answer 5

clarithromycin
minocycline
ofloxacin

Question 6

tx for disease associated adverse drug effects

Answer 6

corticosteroids and thalidomide

Question 7

adequate CMI immunity will result in

Answer 7

tuperculoid leprsosy–>good THI cells–> granulomas…lesions usually single and anesthetic on the arms but retain feeling on the face
–>remission likly possible
dapsone and rifampin for 12 months
*lesions contain very few organisms

Question 8

inadequate TH1 population leads to

Answer 8

lepormatous lepropsy
foamy macrophages
reticuloendothelial involvment–> multiple leasions with lymphatogenous spread
poorly formed granulomas
multiple lesions on the face…mainly nose and butt and arms–> lose feeling and even fingers from contraction of collagen
*lesions contain mainy active organisms

Question 9

toxic metabolie fo the main antileprosy drug

Answer 9

dapsone is converted into hydroxylamine (very toxic)

Question 10

hydroxylamamine gives rise too

Answer 10

hemolysis and methemoglobinemia–> less capable of carrying O2 to the tissues O2 content will be
diminished…this the O2SATURATIONS WILL BE LOW

Question 11

drug that can potentialy cause a fall in O2 saturation

Answer 11

dapsone

Question 12

side effect=blue lips and nail beds

Answer 12

dapsone

Question 13

contraindicated in G6PD deificiency

Answer 13

dapsone

Question 14

renal involvement with dapsone

Answer 14

renal tubular secretion…therefore if renal insufficient…can cause a build up of hydroxylamine

Question 15

dapsone interaction with_____ cause _____

Answer 15

rifampin, increases the toxicity…by revving up cyps that make hydroxylamine

Question 16

dapsone interaction with ______ causes _____

Answer 16

cimetidine and omeprazole…inhibit cyps…not as much Hydroxylamine is made and therefore the toxicity of dapsone is decrased

Question 17

dapsone acts as a _____

Answer 17

folate anatagonist–> bacteriostatic effect

Question 18

MOA for dapsone

Answer 18

compete with PABA for the dihydropteric synthetase–>cell cant make thymidine–> cant make purine–> DNA synthesis is inhibited

Question 19

long term side effects of dapsone

Answer 19

high liver enzymes (hepatitis-mono-like)
hemolysis
methemoglobinemia
billiary jaundice
peripheral neruopathy
hypoalbuminemia
psychosis
leukopenia
agranulocytosis

Question 20

dapsone syndrome

Answer 20

hemolysis
elevated liver enzymes
maculopapular rash that can be exfoliative
SJS also been reported

Question 21

drugs that cause TEN

Answer 21

SATAN
S?
allopurinol
tetracycline
anti-convulsants
NSAIDS

Question 22

labels uses of dapsone

Answer 22

acne vulgaris
dermatitis herpetiformis
leprosy

Question 23

what determines response to rifampin on a CYP basis

thus drug-drug interactions are possible but not absolute

Answer 23

1. export of PgP mediated efflux deciding the intrcelular concentration of the inducer
2. polymorphisms in PXR/RXR
3. polymorphisms in Cyp 3a

Question 24

major side effect of rifampin

Answer 24

TRANSIENT INCREASES IN HEPATIC LIVER ENZYMES AND SEVER,SOMETIMES FATAL LIVER TOXICITY

Question 25

OTHER SIDE EFFECTS OF RIFAMPIN

Answer 25

LIVER TOXICITY-FAILURE HEMOLYSIS *HEMOGLOBINURIA, HEMATURIA, RENAL FAILURE BODY TISSUES DISCOLORATION

Question 26

MOA FOR CLOFAZAMINE

Answer 26

``` preferrential BINDING (not intercolator) to ycobacterial GUANINE in DNA mycobacterial have a MUUCH higher density ```

Question 27

concern with reversal reactions

Answer 27

clofazamine

Question 28

what is a reversal reaction

Answer 28

when you treat the mycobacterium--> the body has a rapid immunologically mediated response...leading to tissue destrction and even functiuonal impairment--> in the hands and nerves etcs

Question 29

side effect of clofazamine

Answer 29

staining of the body fluids and babies -suicides hepatitis jaundice

Question 30

this drug deposits in the fat and reticuloendothelial system and stays for months

Answer 30

clofazamine

Question 31

cant treat reversal reactions and erythema nodosum leprum

Answer 31

clofazamine

Question 32

1st visit with anti-lep theray check

Answer 32

``` cbc + platelets ast alt ca bun creatinine bilirubin g6pd ```

Question 33

2nd visit with leprosy therapy 1-2 motnhs

Answer 33

cbc + platelets

Question 34

3 months-->2 years check

Answer 34

cbc + platelets ast alt

Question 35

in liver failure...cant handle clofazamine so treat with

Answer 35

clarithromycin--> 50s--> prEGANACY cat C minocycline--> 30s--> pregnancy cat D ofloxacin--> gyrase--> preganancy cat C

Question 36

tx of TYPE 1 reactions to anti-leprosy drugs | red patchy skin, erythema, swollen hand and feet, joint pain

Answer 36

corticosteroid therapy

Question 37

tx of type II anti-leprosry ADE's | sudden eruptions of painful nodules, neuritis

Answer 37

corticosteroids clofazamamine thalidomide

Question 38

MOA for thalidomide

Answer 38

inhibits NfKb mediated transcriptional upregultatin and TNF-alfa production -blocks leukocyte migration

Question 39

teratogen

Answer 39

THALIDOMIDE

Question 40

adverse effects of thalidomide

Answer 40

peripheral neuropathy is rare can increase HIV viral load anti-angiogenic