Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

HD > Pharmacology 2: Therapeutic Approach To Autoimmune Disorders > Flashcards

Pharmacology 2: Therapeutic Approach To Autoimmune Disorders Flashcards

1
Q

What is the major cause of morbidity and disability (1 in 30 adults in their lifetime)?

A

Autoimmune disorders.

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

How can autoimmune disorders be classified?

A

By organ involvement.

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

List 4 types of immune responses?

A

1- type 1 hypersensitivity - not associated with autoimmune disease.
2- type 2 hypersensitivity - causes injury to a single tissue or organ and is mediated by specific autoantibodies.
3- type 3 hypersensitivity - results from deposition of immune complexes which activates complement system.
4- type 4 hypersensitivity - mediated by activated T cells and macrophages.

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

The management of autoimmune diseases depends on what?

A

Organ system involved.

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

In general, the treatment of autoimmune diseases involves the use of what?

A

Immunosuppressive agents.

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

List an autoimmune condition that doesn’t require immune suppression?

A

Type-1 DM.

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

List uses of immunosuppressants?

A

1- organ transplantation.
2- autoimmune diseases.

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

List the 5 classifications of immunosuppressant drugs?

A

1- calcineurin inhibitors.
2- m-TOR inhibitors.
3- anti proliferative drugs.
4- glucocorticoids.
5- biological agents.

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

List 5 classification of biological agents?

A

1- polyclonal antibodies.
2- anti-CD3 antibody.
3- IL-2 receptor antagonists.
4- IL-1 receptor antagonist.
5- TNF alpha inhibitors.

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

List glucocorticoids?

A
  • prednisolone.
  • methylprednisolone.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

List antiproliferative drugs?

A
  • azathioprine.
  • methotrexate.
  • cyclophosphamide.
  • chlorambucil.
  • mycophenolate mofetil.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

List m-TOR inhibitors?

A
  • sirolimus.
  • everolimus.
  • temsirolimus.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

List calcineurin inhibitors?

A
  • cyclosporine (ciclosporine).
  • tacrolimus.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

List polyclonal antibodies?

A
  • antithymocyte antibody (ATG).
  • rho (D) immune globulin.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

List anti-CD3 antibody?

A

Muromonab CD3.

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

List IL-2 receptor antagonists?

A
  • basiliiximab.
  • daclizumab.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

List IL-1 receptor antagonist?

A

Anakinra.

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

List TNF alpha inhibitors?

A
  • etanercept.
  • infliximab.
  • adalimumab.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What are the most commonly used immunosuppressant drugs?

A

Glucocorticoids.

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

How do glucocorticoids act?

A

By inhibiting the production of prostaglandins, leukotrienes, histamine, bradykinin and PAF.
Diminishes chemotactic activity of neutrophils and monocytes.
Cause sequestration of lymphocytes in lymphoid tissue resulting in lymphopenia.
Inhibit IL-1 production, IL-2, INF.

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

How does continuous administration of GCs affect immunity?

A

Increases the catabolism of IgG.

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

What is the mechanism of action of glucocorticoids?

A
  • GRs reside in the cytoplasm in an inactive form.
  • Steroid binding results in receptor activation and translocation to the nucleus.
  • They interact with specific DNA sequences called GREs (Glucocorticoids Response Element).
  • Genes can be activated or inhibited by GR-GRE interactions.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the first line immunosuppressive drugs?

A

Glucocorticoids.

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

List the uses of glucocorticoids as immunosuppressives?

A

1- graft rejection.
2- graft vs host disease (GVHD).
3- rheumatoid arthritis.
4- bronchial asthma.
5- ITP.
6- myasthenia gravis.
7- rheumatic fever.
8- glomerulonephritis.
9- SLE.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What is the preferred route of administration of glucocorticoids?
Local: - intra-articular. - intra-bursal. - intra-lesional. - intra-synovial. - soft tissue. - intra-rectal. - topical. - nasal. - inhaled.
26
What is the other route of administration of glucocorticoids?
Systemic: - oral. - IV. - IM. - SC.
27
When do glucocorticoids show toxicity?
When they are used for short periods (< 2 weeks), it is unusual to see serious adverse effects even with moderately large doses. So toxicity only seen when it is used for more than 2 weeks (so if it’s used for more than 2-3 weeks it needs to be stopped gradually to avoid HPA axis suppression).
28
List AE of glucocorticoids?
1- HPA axis suppression: withdrawal. 2- fluid and electrolyte abnormalities. 3- hypertension. 4- hyperglycemia. 5- increases susceptibility to infection. 6- peptic ulcer. 7- osteoporosis. 8- myopathy. 9- behavioral disturbances. 10- cataracts. 11- growth arrest. 12- cushing’s habitus: characteristic habitus of steroid overdose, including fat redistribution, striae, and ecchymoses.
29
How does Azathioprine work?
Inhibits purine biosynthesis.
30
List the MOA of Azathioprine?
- undergoes reduction to 6-mercaptopurine and then to 6-thioguanine. - this forms a false purine nucleotides, thus inhibiting DNA replication and cell proliferation. - also triggers apoptosis. - these actions results in reduction of B and T lymphocytes, reduced IL-2, IgM and IgG.
31
List the adverse effects of Azathioprine?
Bone marrow suppression, hepatotoxicity; increased susceptibility to infection.
32
Give an example of an interaction of Azathioprine? and what does it result in?
Concomitant use of xanthine oxidase inhibitors and Azathioprine, results in profound myelosuppression.
33
How does Mycophenolate mofetil (MMF)?
It is an antimetabolite that inhibits purine synthesis.
34
What is Mycophenolate mofetil (MMF) used in?
Used in treatment for SLE nephritis, other connective tissue diseases and systemic vasculitis.
35
What is MOA of Mycophenolate mofetil (MMF)?
MMF is metabolized to mycophenolic acid, which inhibits inosine monophosphate dehydrogenase, an enzyme in the guanine nucleotide synthesis pathway used by lymphocytes.
36
List the AE of Mycophenolate mofetil (MMF)?
Gastrointestinal disturbances (diarrhea is common), Myelosuppression, Hepatotoxicity, Adverse lipid profile, Increased risk of malignancy and pancreatitis.
37
List calcineurin inhibitors?
- cyclosporin. - tacrolimus.
38
What is calcineurin inhibitors MOA?
Inhibit cytokine-driven activation and proliferation of activated T cells by interfering with synthesis of IL-2. They bind to receptors called immunophilins (cyclophilin, and FKBP-12 respectively), and form complexes that inhibit IL-2 production via calcineurin pathway.
39
Which immunophilins does cyclosporin bind to?
Cyclophilin.
40
Which immunophilins does tacrolimus bind to?
FKBP-12.
41
What is the old name of sirolimus?
Rapamycin.
42
What is sirolimus (rapamycin)?
A macrolide antibiotic.
43
What does sirolimus bind to?
Binds to FKBP-12.
44
What is the MOA of sirolimus?
Binds to FKBP-12, and the complex binds to and inhibits activation of mTOR (mammalian target of rapamycin), an important signaling kinase. This in turn suppresses cytokine-driven T-cell and B-cell proliferation and antibody production.
45
What is mTOR (mammalian target of rapamycin)?
An important signaling kinase.
46
List the 2 uses of sirolimus?
1- preventing rejection after solid organ transplantation. 2- autoimmune inflammatory disorders such as SLE and Behcet’s syndrome.
47
What triggers rheumatic fever?
Triggered by an immune-mediated delayed response to infection with specific strains of group A streptococci, which have antigens that cross-react with cardiac myosin and sarcolemmal membrane proteins.
48
List drugs that are used for rheumatic fever?
1- antibiotics (Benzathine, Benzylpenicillin). 2- aspirin; high doses (8g). 3- glucocorticoids (Prednisolone).
49
Why is Benzathine added to benzylpenicillin?
Pen G is used as prophylaxis, so we add Benzathine to prolong its half-life (given once a month).
50
List the 5 drugs used for SLE?
1- hydroxychloroquine (anti-malarial). 2- azathioprine or mycophenolate mofetil (MMF). 3- topical or intra-articular steroids (intra-thecaly). 4- methylprednisolone and cyclophosphamide. 5- B-cell depletion with rituximab may also be effective.
51
Severe manifestations of SLE such as lupus nephritis are traditionally managed with what?
IV pulses of methylprednisolone and cyclophosphamide.
52
What is hydroxychloroquine used for?
An antimalarial drug, is used commonly for mild manifestations of SLE and other connective tissue diseases.
53
What is the MOA of hydroxychloroquine?
It can reduce the production of pro-inflammatory cytokines including TNF alpha and IL-1b.
54
List the AE of hydroxychloroquine?
1- GI disturbances, rashes, and rarely bloody dyscrasias. 1- retinal toxicity may rarely occur with long-term use; measurement of visual acuity initially and annually.
55
What is rituximab?
A chemical monoclonal IgG1 antibody specific for CD20, which is expressed in B cells but not plasma cells.
56
How is rituximab administered?
IV infusion.
57
What is the major AE of rituximab?
Increased susceptibility and infusion reactions.
58
In myasthenia gravis antibodies develop against what?
Antibodies develop against nicotinic receptors (Nm) at the muscle endplate
59
What is the treatment for myasthenia gravis?
- neostigmine 15 mg orally every 6 hours. - corticosteroids (prednisolone). - other immunosuppressants: azathioprine. If it doesn’t work we can also do plasmapheresis.
60
What drug inhibits IL-2R signaling?
Sirolimus.
61
What drugs inhibit de novo purine synthesis?
Methotrexate. Azathioprine. Mycophenolate mofetil.
62
What drugs cause cytotoxicity via DNA damage?
Cyclophosphamide.
63
What drugs inhibit expression of TNF alpha and other cytokines?
Hydroxychloroquine.
64
What drugs inhibit IL-2 expression?
Cyclosporin, Tacrolimus.

HD (14 decks)

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