B.29-immunopharmacology 1 (cytotoxic agents, retinoids) +autoimmune diseases Flashcards

1
Q

list the cytotoxic agents

A
cyclophosphamide
methotrexate
azathioprine, 6-MP (6-mercaptopurine)
leflunomide 
mycophenolic acid
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what is cyclophosphamide?

A

alkylating agent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

how are the cytotoxic agents given?

A

oral or parenteral

except for leflunomide–> only oral

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

how is leflunomide and teriflunomide given?

A

oral

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what is methotrexate?

A

anti-metabolite

inhibitor of dihydrofolate reductase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what is the mechanism of azathioprine and 6-MP?

A

inhibits de-novo purine synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

what is the mechanism of mycophenolic acid?

A

inhibits de novo GTP synthesis

*B and T cells are suppressed

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what is the mechanism of leflunomide and teriflunomide?

A

inhibit de-novo pyrimidine synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

which cytotoxic agent requires hepatic P450 activation?

A

cyclophosphamide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

why do we need adequate hydration in methotrexate?

A

to prevent urinary crystallization

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

from when is azathioprine effective?

A

after 12 weeks of starting therapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

indications for cyclophosphamide

A
hematological malignancies 
breast and ovarian cancer 
autoimmune diseases (SLE, GN, vasculitis)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

indications for methotrexate

A

hematological malignancies
CNS and other solid tumors
Autoimmune diseases (RA, psoriasis)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

indications for azathioprine and 6-MP

A

hematological malignancies
autoimmune diseases (SLE,RA)
IBD

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

indications for mycophenolic acid

A
solid organ transplantation 
autoimmune diseases (SLE, GN, myasthenia, psoriasis)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

indications for leflunomide, teriflunomide

A

autoimmune diseases (RA, multiple sclerosis)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

side effects for cyclophosphamide

A

myelosuppression
GI distress
hemorrhagic cystitis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

what is given as an antidote for the damage of the bladder from cyclophosphamide?

A

mesna

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

SE from methotrexate

A

myelosuppression
toxic effects on skin and GI mucosa
pulmonary fibrosis (in chronic use)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

what reduces the toxic effect of methotrexate?

A

folinic acid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

don’t combine azathioprine or 6-MP with…

A

allopurinol

22
Q

SE of azathioprine and 6-MP

A

myelosuppression

hepatotoxicity

23
Q

SE of mycophenolic acid

A

myelosuppression

GI distress

24
Q

which cytotoxic agent is used in combination with cyclosporine?

A

mycophenolic acid

25
Q

SE of leflunomide and teriflunomide

A

GI irritation
hepatotoxicity
teratogenic

26
Q

when are glucocorticoids used to suppress immunologic reactions?

A

organ transplantation

hematologic malignancies

27
Q

management of acute flare-ups in RA

A

NSAIDS

Corticosteroids

28
Q

disease-modifying anti-rheumatic drugs (DMARD’S) for RA

A
methotrexate (1st line agent)
chloroquine, hydroxychloroquine
leflunomide
sulfasalazine (5-ASA)
cyclosporine
tofacitinib
29
Q

what is the first-line agent for RA? out of DMARD’S..

A

methotrexate

30
Q

drugs used for mild IBD

A

5-ASA

glucocorticoids - budesonide (topical, oral)

31
Q

biological therapy for RA

A
anti-TNF𝝰 (infliximab)
CTLA-4 fusion protein (abatacept)
IL-1 receptor antagonist (anakinra)
IL-6 receptor antagonist (tocilizumab)
anti-CD20 (rituximab)
32
Q

drugs used for moderate IBD

A

glucocorticoids-prednisone (oral, IV)
azathioprine, 6-MP
methotrexate

33
Q

drugs used for severe IBD

A

cyclosporin
anti-TNF𝝰 (infliximab)
anti-IL-12 and IL-23 (ustekinumab)
anti- integrin 𝝰₄β₁ (natalizumab), anti-integrin 𝝰₄β₇ (vedolizumab)

34
Q

topical agents for psoriasis

A

PUVA therapy (psoralen and ultraviolet A)
glucocorticoids
vitamin D
retinoids - vitamin A

35
Q

systemic agents for psoriasis

A

acitretin (vitamin A derivative)
dimethyl fumarate
apremilast (↓ expression of inflammatory cytokines)
immunosuppressive agents- cyclosporin, methotrexate

36
Q

biological therapy for psoriasis

A

anti-IL-12 and IL-23 (ustekinumab)
IL-17 antagonists
anti-TNF𝝰 (infliximab)

37
Q

what does acitretin do?

A

inhibit the synthesis of keratin precursors

38
Q

what does vitamin D topical do?

A

inhibits keratinocyte proliferation

39
Q

what do retinoids -vitamin A do?

A

inhibition of cell proliferation and differentiation via binding to nuclear retinoid receptors

40
Q

what are the topical agents for atopic dermatitis (eczema)?

A

pimecrolimus

glucocorticoids

41
Q

what is pimecrolimus?

A

topical calcineurin inhibitor

42
Q

what are the systemic agents for atopic dermatitis?

A

glucocorticoids
cyclosporin
anti-IL-4 receptor 𝝰 (dupliumab)

43
Q

what are the antimetabolites given in MS?

A

teriflunomide

cladribine

44
Q

what is cladribine?

A

purine analogue chemotherapeutic agent

45
Q

what is given for leukocyte suppression in MS?

A

anti-CD52 (alemtuzumab)

46
Q

T-cell suppression for multiple sclerosis

A

anti- integrin 𝝰₄β₁ (natalizumab)

sphingosine -1 phosphate receptor modulator (fingolimod)

47
Q

B-cell suppression for multiple sclerosis

A

anti- CD20 (ocrelizumab)

48
Q

other agents for multiple sclerosis

A

interferon β
glatiramer
dimethyl-fumarate
fampridine

49
Q

what does dimethyl fumarate do?

A

has an anti-oxidant effect

50
Q

what does fampridine do?

A

K channel inhibition–> improves motor function