Anti-Leprosy agents Flashcards

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1
Q

tx for tuberculous leprosy

A

Dapsone, Rifampin x 12 months

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2
Q

tx for lepromatous leprousy

A

Dapsone, Rifampin, Clofazamine x 24 months

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3
Q

vector for leprosy

A

humans and dillos

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4
Q

geopgraphic distribution leprosy

A

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

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5
Q

lepromatous pt.’s who cannot tolerate clofazamine get

A

clarithromycin
minocycline
ofloxacin

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6
Q

tx for disease associated adverse drug effects

A

corticosteroids and thalidomide

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7
Q

adequate CMI immunity will result in

A

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

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8
Q

inadequate TH1 population leads to

A

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

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9
Q

toxic metabolie fo the main antileprosy drug

A

dapsone is converted into hydroxylamine (very toxic)

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10
Q

hydroxylamamine gives rise too

A

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

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11
Q

drug that can potentialy cause a fall in O2 saturation

A

dapsone

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12
Q

side effect=blue lips and nail beds

A

dapsone

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13
Q

contraindicated in G6PD deificiency

A

dapsone

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14
Q

renal involvement with dapsone

A

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

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15
Q

dapsone interaction with_____ cause _____

A

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

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16
Q

dapsone interaction with ______ causes _____

A

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

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17
Q

dapsone acts as a _____

A

folate anatagonist–> bacteriostatic effect

18
Q

MOA for dapsone

A

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

19
Q

long term side effects of dapsone

A
high liver enzymes (hepatitis-mono-like)
hemolysis
methemoglobinemia
billiary jaundice
peripheral neruopathy
hypoalbuminemia
psychosis
leukopenia
agranulocytosis
20
Q

dapsone syndrome

A

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

21
Q

drugs that cause TEN

A
SATAN
S?
allopurinol
tetracycline
anti-convulsants
NSAIDS
22
Q

labels uses of dapsone

A

acne vulgaris
dermatitis herpetiformis
leprosy

23
Q

what determines response to rifampin on a CYP basis

thus drug-drug interactions are possible but not absolute

A
  1. export of PgP mediated efflux deciding the intrcelular concentration of the inducer
  2. polymorphisms in PXR/RXR
  3. polymorphisms in Cyp 3a
24
Q

major side effect of rifampin

A

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

25
Q

OTHER SIDE EFFECTS OF RIFAMPIN

A

LIVER TOXICITY-FAILURE
HEMOLYSIS

*HEMOGLOBINURIA, HEMATURIA, RENAL FAILURE
BODY TISSUES DISCOLORATION

26
Q

MOA FOR CLOFAZAMINE

A
preferrential BINDING (not intercolator) to ycobacterial GUANINE in DNA
mycobacterial have a MUUCH higher density
27
Q

concern with reversal reactions

A

clofazamine

28
Q

what is a reversal reaction

A

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

29
Q

side effect of clofazamine

A

staining of the body fluids and babies
-suicides
hepatitis
jaundice

30
Q

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

A

clofazamine

31
Q

cant treat reversal reactions and erythema nodosum leprum

A

clofazamine

32
Q

1st visit with anti-lep theray check

A
cbc + platelets
ast
alt
ca
bun
creatinine
bilirubin
g6pd
33
Q

2nd visit with leprosy therapy 1-2 motnhs

A

cbc + platelets

34
Q

3 months–>2 years check

A

cbc + platelets
ast
alt

35
Q

in liver failure…cant handle clofazamine so treat with

A

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

36
Q

tx of TYPE 1 reactions to anti-leprosy drugs

red patchy skin, erythema, swollen hand and feet, joint pain

A

corticosteroid therapy

37
Q

tx of type II anti-leprosry ADE’s

sudden eruptions of painful nodules, neuritis

A

corticosteroids
clofazamamine
thalidomide

38
Q

MOA for thalidomide

A

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

39
Q

teratogen

A

THALIDOMIDE

40
Q

adverse effects of thalidomide

A

peripheral neuropathy is rare
can increase HIV viral load

anti-angiogenic