Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Pharmacology -- Test #2 > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

(71 cards)

Start Studying
1
Q

Immunopharmacology focuses on…

A

Primary and secondary disorders of the immune system and the production of modulators of the immune system

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

Two types of immunopharmacological drugs

A

Immunosuppressants

Immunostimulants

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

The development of the adaptive immune response happens over about….days

A

8-14

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

Basophils can release

A 
Histamine
Bradykinin
Serotonin
Hepatin
SRSA
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Immunosuppressants are used to…

A

Inhibit normal immune responses

Organ transplant, Autoimmune disorders

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

What immune response are immunosuppressants most effective with

A

Primary

Start before antigen exposure

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

Acute organ rejection =

A

Rejection that occurs 24 hrs-several weeks after transplant

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

Acute rejection is mediated primarily by…

A

T cells and cytokines

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

Six Classess of Immunosuppressants

A
  1. Regulators of Gene Expression
  2. Alkylating Agents
  3. Inhibitors of de novo purine synth.
  4. Inhibitors of de novo pyramidine synth.
  5. Kinases and phosphatase inhibitors
  6. Protein immunosuppressive drugs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

End result of immunosuppressant regulators of gene expression?

A
  1. Reduced Circulating Lymphocytes
  2. Blocked lymphocyte activation needed for antigen pres.
  3. Block T-cell proliferation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

How do Immunosuppressant regulators of gene expression block T cell proliferation?

A

Inhibition of IL-2 gene transcription

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

immunosuppressant regulators of gene expression.

Induction, Maintenance, or both?

A

Both

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

Example of immunosuppressant alkylating agent?

A

Cytotoxic drug cyclophosphamide

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

First generation immunosuppressant inhibitor of de novo purine synthesis

A

Azathioprine

6-mercaptopurine

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

Important non-1st gen immunosuppressant inhibitors of de novo purine synthesis?

A

Mycophenylate mofetil
Methotrexate
Polygentamate

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

immunosuppressant inhibitors of de novo purine synthesis.

Induction, Maintenance, or both?

A

Both

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

immunosuppressant alkylating agents.

Induction, Maintenance, or both?

A

Both

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

Difference between effects of de novo purine and pyrimidine inhibiton

A

DN pyramadine inhib. has less CV risk and less nephrotoxicity, but they’re also less effective

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

How do immunosuppressant inhibitors of de novo pyrimidine synthesis work?

A

Inhibitior of dihydroorotate, a key enzyme in pyramidine synthesis

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

Three classic examples of immunosuppressant kinases and phosphotase inhibitors

A

Cyclosporine
Tacrolimus
Sirolimus

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

Effects of dosing with Cyclosporine or tacrolimus?

A

They block T-cell signalling pathways that stimulate IL-2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Cyclosporine or tacrolimus

Induction, Maintenance, or both?

A

Both

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

Cyclosporine method of administration?

Concentrates in which cells?

A

IV or Per Os

Dist. widely, but conc. in RBC and WBC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Cyclosporine metabolism?

A

Metabolized by liver and mainly excreted in feces

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Cyclosporine schedule?
Given 4-24 hrs before transplant | Lowered doses at weekly interval afterward
26
Cyclosporine toxicity?
Mainly renal (proximal tubule) Gingival Neuronal Sometimes hepatic
27
Cyclosporine Mechanism?
Assoc. w/ Calcineurin and inhibits its phosphotase activity. This prevents translocation of NFAT TFs to the nucleus of lymphocytes. Blocks lymphokine synthesis. Also blocks JNK and p38
28
Tacrolimus is what kind of anti-biotic?
Macrolide
29
Tacrolimus Mechanism?
Binds to cytoplasmic FK506 binding protein, making a complex that inhibits phosphatase activity of calcineurin Also blocks JNK and p38
30
How is Tacrolimus dosed?
IV or Per Os
31
Distribution and metabolism of Tacrolimus?
Loss widely distrib. than cyclosporine | Metabolized by liver and excreted in the feces
32
Who is more potent, cyclosprorine or Tacrolimus
Tacrolimus is about 100x more potent
33
Tacrolimus may be useful to treat what specific disease?
Myasthenia gravis
34
Mechanism of Sirolimus action?
Inhibition of calcineurin (and blocking of T cell resp. to cytokines) by binding onto FKBP12.
35
Is Sirolimus used alone or in combination treatment?
Yes | Both -- better w/ cyclo.
36
Look up Everolimus in the ppt.
well shit. | page 5 of my notes
37
How do antilymphocyte globulins work?
Inhibition of acutre graft rejection by binding onto lymphocyte surface proteins Ex. muromonab for induction and treatment of rejection
38
Antilymphocyte globulins are used against what targets?
CD 25 (Basiliximab) CD3 (Muromonab) CD52, CD20 -- Antithymocyte
39
Diseases with CD20 overexpression?
RA, Hemolytic anemia
40
Significance of Beltacept?
Equivalent alternative to calcineurin inhibitors for kidney transplant recipients. It is an inhibitor of CD28 mediated T cell costimulation.
41
Mechanism for Beltacept
Binds to CD80 and 86, blocking CD28 engagement on T cells. | Prevents T cell activation.
42
Beltacept is associated with...
more frequent post-transplant lymphoproliferative disorders than other suppressants. Serious side effects in children.
43
Non-medical downside of Baltacept?
It's fuckin expensive.
44
Studies on rejection in kidney transplant with beltacept use suggest that targeting ______ might be more valueable than targeting CD80/86
CD28
45
Important details for Rapamycine
Macrocyclic Lactone Targets mTOR (regulator of cell proliferation) May help by preventing the proliferation of smooth muscle cells and fibroblasts Everolimus is a related compound
46
Why can't Everolimus replace calcineurin inhibitors?
When used alone, it triggers de novo donor-specific alloantibodies associated with antibody mediated rejection
47
What is FTY720?
``` First in class synthetic small molecule Reduces circulating Ts by driving them into lymphoid tissues Treats MS ```
48
TNF-alpha inhibitors are used primarily to treat...
RA
49
Which cell usually mediates auto-immunity?
T cell
50
Examples of Ab mediated auto-immunity
Autoimmune mediated hemolytic anemia Myasthenia gravis Hypoadrenocorticism
51
Disease in which exposure to an antigen will program for search and destruction of the antigen in the future
Thyroiditis | Autoimmune hypothyroidism
52
Six major drugs for treatment of autoimmune disorders
``` Corticosteroids Cyclophosphamide Asathioprine Mercaptopurine Leflunomide Cyclosporine ```
53
Primary drugs used in any autoimune disease?
Corticosteroids
54
Why not use Corticosteroids long term?
Infections, Ulcers, Hyperglycemia, Osteoporosis
55
How does cyclophosphamide work?
Inhibits DNA synthesis and function by alkylation | Affects B Cells more than T cells
56
How does Azathioprine work?
Purine anti-metabolite that interferes w/ DNA synthesis Affects all rapidly growing cells Takes weeks to see results
57
Effects of Azathioprine cytotoxicity?
Leukopenia Thrombocytopenia GI Dysfunction Possible infections and hepatic lesions
58
Azathioprine is metabolized into...
Mercaptopurine
59
Mercaptopurine effects?
Interferes with RNA and DNA synthesis after conversion to a purine antagonist. Mostly hits humoral immunity Side effects - BM+GI depletion
60
Effects of Leflunomide?
Inhibitor of pyrimidine synthesis Active metabolite has a long half life of several weeks used for RA
61
Why are frequent blood measures of Cyclosporine levels necessary?
Variability of Cyclosporine absorption Cyclosporine saturates tissues, so dosage may need adjusting Drug interactions
62
To get the full benefit of Cyclosporine, the patient must...
be on a very strict feeding and dosing schedule. Diet consistent Made difficult by loss of appetite
63
Three drug classes important to the treatment of allergies
Fatty Acids Antihistamines Biotin
64
What is atopy?
Inhalant allergy
65
Fatty acids used in allergy treatment may include...
linoleic and gamma-linoleic acids
66
Why give an allergy sufferer fatty acids?
They work in the skin to help reduce the amount/effects of histamine. Very safe, few side effects
67
Typical mechanism for anti-histamines?
H1 blockers. | prevent attachment of histamine to its target
68
Example of a common antihistamine?
Diphenhydramine
69
If all else fails in allergy treatment and patients are symptomatic more than 4 months per year, what should you consider?
Immunotherapy | Weekly/Monthly injections with allergens to induce desensitization in most treated patients
70
For patients with severe symptoms of allergies after other options are exhausted, use...
Corticosteroids (ex. dexamethasone, methylprednisone)
71
Some major risks of imunosuppressants
``` GVH Infections Reappearance of latent disease (ex. Hep) CV events Neoplasia ```

Pharmacology -- Test #2 (13 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions