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Pharm > Immunomodulators > Flashcards

Immunomodulators Flashcards

1
Q

Glucocorticoids: MOA

A 
Activates the glucocorticoid receptor
      transcription factor
Modifies expression of cytokine and 
      other immunoregulatory genes
Suppresses active immune responses
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2
Q

Glucocorticoids: Indications

A 
Immunosuppression
To Prevent graft rejection
To prevent GvHD
Treatment of  Cytokine-release Syndrome
Treatment of a wide variety of autoimmune and inflammatory diseases
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3
Q

Glucocorticoids: adv.

A 
Many Adverse effects
Hyperglycemia
Hypertension
Hyperlipidemia
Obesity
Diabetes
Poor wound healing
Mania & Psychosis
Inc. Risk infections
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4
Q

How to discontinue GC’s

A

Glucocorticoid dose must be gradually reduced to minimize adverse effects

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5
Q

Azathioprine: MOA

A 
Prodrug
Converted to 6-MP by HGPRT
Inhibits de novo purine synthesis
Incorporated into DNA & causes SSB
     base mispairing, leading to apoptosis
Inhibits CD28 co-stimulation
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6
Q

Indications for azathioprine, mycophenolate

mofetil, and calcineurin inhibitors

A 
Immunosuppression
To Prevent graft rejection
To prevent GvHD
Treatment of autoimmune 
      diseases
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7
Q

Azathioprine: adverse effects

A

Leukopenia/thrombocytopenia
Hepatotoxicity
Inc. Risk infections and malignancy

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8
Q

Notable interactions for azathioprine

A

Interacts with anti-gout drugs (Allopurinol &; Febuxostat), leading to Azathioprine toxicity, because inhibiting xanthine oxidase leads to increased levels of 6-mercaptopurine as well

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9
Q

Mycophenolate Mofetil: MOA

A

Prodrug
Converted to mycophenolic acid
Inhibits inosine monophosphate
dehydrogenase II (IMPDH2
- selectively expressed in lymphocytes, leading to Inhibition of purine nucleotide synthesis
- no salvage pathway in lymphocytes

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10
Q

Mycophenolate Mofetil: adv effects

A

Leukopenia/anemia
Teratogenic for both male and female
Inc. Risk infections, malignancy
***RARE- Risk of Progressive multifocal leukoencepalopathy (PML), a fatal viral disease caused by reactivation of JC virus

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11
Q

Mycophenolate Mofetil: counterindications

A

Men and women who wish to become parents

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12
Q

Calcineurin inhibitors: tacrolimus and cyclosporine, MOA

A

Cyclosporin and tacrolimus bind
cyclophilin and FKBP, respectively
to form inhibitory complexes
Cyclophilin/cyclosporin and
FKBP/tacrolimis complexes inhibit the
calcium-regulated phosphatase, calcineurin
Inhibition of calcineurin inhibits the activation
of the NFAT transcription factor, which is involved
in regulating the expression of IL-2 and multiple
other immunoregulatory genes
Potently inhibit the T cell immune response by
inhibiting Signal 1

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13
Q

Calcineurin inhibitors: adverse effects

A

Nephrotoxicity****

Hypertension***

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14
Q

Calcineurin inhibitors: Interactions

A

Metabolized by CYP3A4

3A4 inhibitors inc. risk of toxicity
3A4 inducers inc. risk of risk graft rejection

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15
Q

mTor inhibitors: sirolimus, everolimus, MOA

A

Drugs form complex with FBKP
FKBP/drug complexs inhibits:
IL-2 mediated activation of mTor kinase
(T cell signal 2)
IL-2 stimulated protein synthesis,
Cell proliferation and survival

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16
Q

mTor inhibitors: indication

A 
Immunosuppression
To prevent graft rejection
           - NOT LUNG
           - NOT LIVER
To prevent GvHD
Included in arterial stents to inhibit re-stenosis
17
Q

mTor inhibitors: adv.

A 
Hypertriglyceridemia
Hypercholesterolemia
Inc. Lung disease
Inc. Risk of diabetes
Anemia, thrombocytopenia, 
       & leukopenia
Dec. Wound healing
Teratogenic
Inc. Risk infections, malignancy
18
Q

mTor inhibitors: Contraindications

A

Contraindicated in Pregnancy
NOT RECOMMENDED
- Lung transplantation (risk anastomotic dehiscence)
- Liver transplantation (risk hepatic artery thrombosis)

19
Q

mTor inhibitors: Interactions

A

CYP 3A4!!!

20
Q

Ipilimumab MOA

A

Antibody specific for CTLA4
Antagonizes the negative regulatory CTLA4 protein
responsible for downregulating activated T cells
Enhances T cell responses

21
Q

Immune checkpoint inhibitors (Ipilimumab and Pembrolizumab/Nivolumab) adverse effects

A

Potential for RARE
Autoimmune response
(can be fatal)

22
Q

Immune checkpoint inhibitors (Ipilimumab and Pembrolizumab/Nivolumab) adverse effects

A

Potential for RARE Autoimmune response (can be fatal)

Ipili: Inflammation of Skin, GI tract, liver, nerves and adrenal glands

Pem/Niv: e.g. lung, liver, colon, kidney, skin, pituitary, thyroid & pancreas

23
Q

Pembrolizumab/Nivolumab MOA

A

Antibody specific for the PD1 protein, which is a negative regulatory receptor expressed on activated T cells that is responsible for downregulating T cell responses
The PD1 ligand PD-L1 is expressed on tumor cells, so they can avoid the immune response
Antibody drugs block PD1/PD1-L1 interactions, blocking the inhibitory signal and leading to enhanced tumor immune responses

24
Q

Counterindications for immune checkpoint inhibitors

25
Q

Which drugs treat relapsing/remitting MS?

A

Fingolimod
Natalizumab
IFN-beta
Glatiramer Acetate

26
Q

Adverse effects of natalizumab

A

Increased risk of progressive multifocal leukoencephalopathy - especially if:

     - prior use of immunosuppression
     - seropositive for JC virus
     - chronic treatment
27
Q

Adverse effects of fingolimod

A

Bradyarrhythmia
Atrioventricular block
Chickenpox infection
Malignancy

28
Q

Anti-thymocyte globuline, Alemtuzumab adverse effects

A

Cytokine release syndrome

29
Q

IVIG - MOA, indications

A

Pooled Ig from healthy individuals
Provides patient with Ig from healthy
immunized donors to provide immunity
to common pathogens

30
Q

Rhogam - when is it given

A

Given to Rh- mother at 28 weeks & 72 hr
post pregnancy to deplete any fetal RBC in
maternal blood

31
Q

Glatiramer acetate - MOA

A

Promotes production of specific suppressor T cells that migrate to the brain and produce bystander suppression at sites of inflammation

32
Q

Indications of Induction agents (Rabbit Anti-thymoycyte Globulins (rTAG), Alemtuzumab, Basiliximab)

A

Lymphocyte depletion intra-operatively and 3-7 days post-op

33
Q

MOA of rTAG

A

Reacts with proteins expressed on lymphocyte surface- CD2, CD3, CD4, CD8, CD11a etc
Actively depletes lymphocytes from the blood and lymphoid organs
- Fc receptor-mediated/complement-dependent lysis and opsonization
After injection recovery of immune system takes several months

34
Q

Best tolerated lymphocyte depletion induction therapy?

A

Well tolerated, although more rejection than with depleting agents

35
Q

Maintentance therapy?

A

Glucocorticoid + either cyclosporin or tacrolimus + an anti-proliferative drug

				- Sirolimus/everolimus are sometimes used in place of either cyclosporin/tacrolimus or the anti-proliferative drug

Pharm (22 decks)

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