Immunosuppressives Flashcards

(55 cards)

1
Q

MOA of oclacitinib

A

Inhibits Janus-kinase 1 and 3-dependent cytokines

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

Which cytokines does oclacitinib inhibit?

A

IL-2/IL-6 (inflammatory cytokines)
IL-4/IL-13 (allergic cytokines)
IL-31 (pruritogenic cytokine)

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

Side effects of oclacitinib

A

GI- V/D/anorexia

infections- demodicosis, pneumonia, pyoderma

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

MOA of lokivetmab

A

Binds to and neutralizes IL-31

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

How is lokivetmab metabolized?

A

Via protein degradation pathways

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

Side effects of lokivetmab

A
lethargy
vomiting
hyperexcitability
pain at injection site
urinary incontinence
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is lokivetmab?

A

caninized monoclonal Ab against IL-31

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

Definition of immunosuppression

A

to reduce the activation or efficacy of the immune system

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

Definition of immunomodulation

A

to modify the immune system

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

Name 3 categories of cytotoxic drugs

A
  1. cycle specific: more toxic to cells actively cycling than in G0 phase
  2. phase specific: active during specific cycle
  3. cycle non-specific: toxic to proliferating and intermitotic cells
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Which category of cytotoxic drugs are alkylating agents?

A

“cycle non-specific”; most active during G1 and S phases

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

MOA for cyclosphosphamide

A

creates DNA crosslinkages interfering with DNA and RNA replication and function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Which metabolite of cyclophosphamide is responsible for hemorrhagic cystitis?

A

acrolein

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

Side effects of cyclophosphamide

A
myelosuppression
loss of vibrissae (cats)
hemorrhagic cystitis
decreased wound healing
alopecia (poodles, OES)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

MOA of chlorambucil

A

creates DNA crosslinkages disrupting DNA synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Side effects of chlorambucil

A

myelosuppression (thrombocytopenia)
GI- V/D/anorexia
alopecia (poodles, Kerry blue terriers)

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

MOA of lomustine

A

not fully understood….inhibit DNA/RNA synthesis

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

Which type of cutaneous cancer is lomustine commonly used to treat?

A

cutaneous T cell lymphoma

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

Name two subclasses of alkylating agents.

A
  1. nitrogen mustards (cyclophosphamide & chlorambucil)

2. nitrosoureas (lomustine)

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

Side effects of lomustine

A

myelosuppression (neutropenia/thrombocytopenia)
hepatotoxicity
GI effects (V/D/anorexia)

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

Name 3 subclasses of antimetabolites.

A
  1. purine analogs (azathioprine, mycophenolate)
  2. pyrimidine analogs (5-fluorouracil, leflunomide)
  3. Antifolates (methotrexate)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Which category of cytotoxic drugs are antimetabolites?

A

Most are “phase specific”; usually active in S phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

MOA of azathioprine

A

interferes w/ purine nucleic acid base production–> inhibits DNA/RNA synthesis

24
Q

What is the prodrug of azathioprine responsible for its effects?

A

6-mercaptopurine

25
What is the enzyme mainly responsible for metabolism of 6-mercaptopurine? Which species or breeds have a decrease or increase in the activity of this enzyme?
thiopurine methyl-transferase (TPMT) Low TPMT activity: cats, Giant Schnauzers Elevated TPMT activity: Alaskan malamute
26
Side effects of azathioprine
Myelosuppression (thrombocytopenia)....NOT for cats vomiting hepatotoxicity....monitor enzymes q 2 weeks for first 2 months pancreatitis
27
MOA of mycophenolate
inhibits de novo purine synthesis via its prodrug mycophenolic acid more specifically: reversibly binds to inosine monophosphate dehydrogenase (IMPDH)...rate limiting step in de novo guanine synthesis
28
Side effects of mycophenolate
myelosuppression V/D/nausea increased risk of opportunistic infections leukocytosis
29
MOA of 5-fluorouracil
converted to fluoruridine monophosphate (FUMP) and fluoruridine triphosphate (FUTP)...these interfere with DNA and RNA synthesis respectively
30
Which species should 5-fluorouracil NOT be used in?
CATS! | Neuro and hepatotoxic
31
Side effects of 5-fluorouracil
myelosuppression GI toxicity neurotoxicity (seizures)
32
MOA of leflunomide
inhibits dihydroorotate dehydrogenase enzyme, thus preventing formation of ribonucleotide uridine monophosphate (rUMP)--> decreased DNA/RNA synthesis
33
Side effects of leflunomide
hepatotoxicity vomiting myelosuppression (lymphopenia, anemia) TEN/SJS in people
34
MOA of methotrexate
binds and inhibits dihydrofolate reductase needed for purine and pyrimidine synthesis S-phase specific
35
Side effects of methotrexate
``` GI (V/D/inappetence) myelosuppression hepatopathy renal tubular necrosis Alopecia and depigmentation ```
36
MOA of cyclosporine
calcineurin inhibitor binds to cyclophilin--> CsA/cyclophilin bind to calcineurin--> inhibits signal transmission--> inhibits T cell activation and production of IL-2, -3, -4
37
Name 10 drugs which increase CsA levels
``` cytochrome P450 INHIBITORS--> increase CsA acetazolamide allopurinol amlodipine azithromycin azoles bromocriptine diltiazem carvedilol cimetidine chloramphenicol cipro/enrofloxacin cisapride clarithromycin clopidogrel colchicine corticosteroids- NOT methylprednisolone danazol digoxin estrogens fluvoxamine glipizide grapefruit juice (flavonoids) imipenem losartan medroxyprogesterone metronidazole omeprazole sertraline tinidazole ```
38
Name 10 drugs which decrease CsA levels
``` Cytochrome P450 INDUCERS--> decrease CsA levels azathioprine carbamazepine clindamycin cyclophosphamide famotidine griseofulvin octreotide rifampin phenobarbital phenytoin St. John's wart sulfadiazine sulfasalazine terbinafine trimethoprim warfarin ```
39
Side effects of cyclosporine
``` GI- V/D/anorexia benign gingival hyperplasia papillomatosis/histiocytomas hirsutism fatal systemic toxoplasmosis in cats ```
40
MOA of tetracycline and niacinamide
Exact MOA unknown tetracycline: anti-inflammatory, affects complement and Ab production, inhibits leukocyte chemotaxis, PG synthesis niacinamide: blocks Ag specific IgE induced histamine release, inhibits mast cell degranulation
41
Side effects of tetracycline/niacinamide
V/D/anorexia elevated liver enzymes (niacinamide) enamel hypoplasia and esophageal erosions/ulcerations (tetracycline)
42
MOA of pentoxifylline
methylxanthine derivative increases microcirculation via increased RBC flexibility decreases platelet aggregation decreases leukocyte response to IL-1/TNF-alpha decreased production of IL-1, -4, -12, TNF-alpha
43
Side effects of pentoxifylline
V/D dizziness in people EM- 2 cases reported
44
MOA of dapsone
interferes w/ myeloperoxidase activity | decreases complement activity, mast cell degranulation, Ab production
45
Side effects of dapsone
myelosuppression (anemia, neutropenia, thrombocytopenia) hepatotoxicity GI CADR
46
MOA of human IVIG
interferes w/ Fas-Fas ligand apoptosis inhibits T cell proliferation eliminates circulating immune complexes
47
Side effects of IVIG
anaphylaxis during infusion | acute renal failure
48
MOA of gold salts (chrysotherapy)
inhibit lysosomal enzymes, complement, chemotaxis, DNA/RNA synthesis, Ig synthesis suppresses inflammatory mediator release, suppressor T cells
49
Side effects of gold salts
myelosuppression oral ulceration glomerulonephropathy fatal TEN
50
MOA of colchicine
suppresses neutrophil chemotaxis | inhibits lysosomal degranulation, Ig secretion, IL-1 production, histamine release, cell division
51
Side effects of colchicine
GI | myelosuppression (when given w/ NSAIDs)
52
Which drugs should colchicine NOT be used with?
azathioprine and chlorambucil
53
Which diseases is colchicine commonly used for?
Shar Pei fever, amyloidosis, EBA, JEB
54
MOA of imiquimod
activation of TLR7--> IFN-alpha, IL-12, TNF-alpha secretion--> Th1 response and cell-mediated immunity
55
Side effects of imiquimod
local irritation- burning, erythema, pain, erosion, oozing | depigmentation/hair loss after use