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Pharm final sem 1 > immunomodulating drugs > Flashcards

immunomodulating drugs Flashcards

1
Q

what are the 2 glucocorticoids

A

prednisone (prodrug)

prednisolone (active drug)

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2
Q

indications of glucocorticoids (prednisone)

A 
Immunosuppression
prevent graft rejection
preven GvHD
treatment of cytokine release syndrome
autoimmune and inflammatory diseases (RA, SLE, asthma, etc)
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3
Q

what is the MOA of glucocorticoids

A
  • actives the glucocorticoid receptor transcription factor
  • modifies expression of cytokine and other immunoregulatory genes
  • suppresses active immune responses
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4
Q

what are some adverse effects of glucocorticoids

A

Many, Hyperglycemia, HTN, Hyperlipidemia, obesity, diabetes, poor wound healing, mania and psychosis, increased risk of infection

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5
Q

what considerations should be taken into account when stoping glucocorticoids?

A

must be gradually reduced

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6
Q

What are the indications for Azathioprine

A

immunosuppression
prevent graft rejection
to prevent GvHD
autoimmune dieases

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7
Q

what is the MOA of Azathioprine

A
  • prodrug- converted to 6-MP by HGPRT
  • inhibits de novo purine synthesis
  • incorporated into DNA and causes SSB base mispairing leading to apoptosis
  • inhibits CD28 co-stimulation
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8
Q

what are the adverse effects of Azathioprine

A

leukopenia/thrombocytopenia
hepatotoxicity
increased risk of infection
increased risk of malignancy

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9
Q

what is an important drug reaction of Azathioprine

A

interacts with anti-gout medications allopurinol and febuxostat leading to increased azathioprine concentrations and toxicity

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10
Q

what are the indications for Mycophenolate Mofetil

A

immunosuppression
prevent graft rejection
to prevent GvHD
autoimmune dieases

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11
Q

what are the proliferation inhibitors and anti-metabolite drugs

A

Azathioprine and mycophenolate mofetil

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12
Q

what is the MOA for Mycophenolate Mofetil

A
  • prodrug (converted to mycophenolic acid)
  • inhibits inosine monophosphate dehydrogenase II (IMPDH2) selectively expressed in lymphocytes
  • inhibits purine synthesis (no salvage pathway in lymphocytes)
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13
Q

what is IMPDH2 and where is it expressed

A

expressed only in lymphocytes

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14
Q

what is unique about purine synthesis in lymphocytes

A

there is no salvage pathway therefore blocking the de novo pathway has greater effects in lymphocytes than other cells

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15
Q

what are adverse effects of Mycophenolate Mofetil

A 
Leukopenia/anemia
teratocgenic (male and female)
increased risk of infections 
increased risk of malignancy
rare risk of progressive multifocal leukoencephalopathy (PML)
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16
Q

what is PML and what drug increases the risk of it

A

progressive multifocal leukoencephalopathy - a fatal viral disease caused by reactivation of JC virus.

rare adverse effect associated with Mycophenolate Mofetil

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17
Q

Who should not be given mycophenolate mofetil

A

pregnant women or women who with to become pregnant and men who wish to become fathers

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18
Q

what are the 2 drugs that are calcineurin inhibitors

A

cyclosporine and tacrolimus (these are also antibiotics)

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19
Q

what are the indications for a calcineurin inhibitor

A

immunosuppression
prevent graft rejection
to prevent GvHD
autoimmune dieases

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20
Q

Cyclosporin binds to what protein

A

cyclophilin

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21
Q

tacrolimus binds to what protein

A

FKBP

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22
Q

what is the MOA of calcineurin inhibitors

A
  • bind to cyclophilin/FKBP to form inhibitory complexes
  • complexes inhibit calcineurin (the calcium-regulated phosphatase)
  • inhibition of calcineurin inhibits the activation of the NFAT transcription factor, which is involved in regulating the expression of IL-2 and other immunoregulatory genes
  • potently inhibiting the T cell immune response by inhibiting signal 1
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23
Q

what are the adverse effects of calcineurin inhibitors

A

**nephrotoxicity
**HTN
neurotoxicity/tremor
glucose intolerance (T>C)
hyperlipidemia (C>T)
hypertrichoisis (C)
alopecia (T)
increased risk of infection
increased risk of malignancy

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24
Q

how are calcineurin inhibitors metabolized and what affects does this cause

A

CYP3A4
many drug interactions
CYP3A4 inhibitors increase the risk of toxicity and CYP3A4 inducers decrease the effectiveness of the drug

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25
what are the 2 mTor inhibitors
sirolimus and everolimus
26
what are the indications for a mTor inhibitor
immunosuppression prevent graft rejection (not liver or lung) to prevent GvHD included in arterial stents to inhibit restenosis
27
what is the MOA of mTor inhibitors
* drug complexes with FBKP * complex inhibits IL-2 mediated activation of mTor kinase (T-cell signal 2) * inhibits IL-2 stimulated protein synthesis, cell proliferation and survival
28
what are the side effects of mTor inhibitors
hypertriglyceridemia, hypercholesterolemia, increased lung disease, increased risk of DM, anemia, thrombocytopenia and leukemia, decreased wound healing, teratogenic, increasaed risk of infections, increased risk of malignancy
29
how is mTor metabolized
via CYP3A4 = many drug interactions
30
what patient populations is mTor inhibitors contraindicated or not recommended for
contraindicated in pregnancy not recommended - lung transplantation (risk of anastomotic dehiscence), liver transplantation (risk of hepatic artery thrombosis)
31
what drugs are used for induction immunotherapy
rabbit anti-thymocyte globulin alemtuzumab basiliximab
32
what is the MOA for Rabbit anti-thymocyte globulin
rabbit polyclonal anitibodes specific for human lymphocytes depletes lymphocytes from blood
33
what are adverse effects of rabbit anti-thymocyte globulin
*cytokine release syndrome | leukopenia
34
what is the MOA for alemtuzumab
binds to CD52 expressed on T cells, B cells, macrophages, NK cells, and granulocytes depletes cells from blood by Ab-mediated lysis
35
Basiliximab MOA
Antagonist of the IL-2R | blocks T cell proliferation
36
adverse effects for Alemtuzumab
*cytokine release syndrome leukopenia can take > 1 year for immune system to recover
37
what 3 drugs can be used for passive immunization
IVIG Rho (D) Hyperimmune Ig
38
what are indications for IVIG
provides short lived humoral immunity to patients with deficiency in humoral immune system (ie hypogammaglobulinemia)
39
what is the MOA of IVIG
provides patients with Ig from healthy immunized donors to provide immunity to common pathogens
40
Rho (D) indications
prevention of hemolytic disease of the newborn in newborns born to Rh- females
41
MOA of Rho(D)
purified Ig to Rh (D) antigen given to Rh- mothers at 28 weeks and 72 hours post pregnancy to deplete any fetal RBC in the maternal blood and to prevent the mother from generating an immune response to fetal RBC
42
Hyperimmune Ig indications
to provide rapid specific antibody immunity to specific viruses and/pr toxins
43
hyperimmune Ig MOA
purified Ig to specific antigens purified from healthy volunteers given IV to patients in order to promote clearance of a virus or toxin
44
what are the 2 immune check point inhibitors
Ipilimumab | pembrolizumab/Nivolumab
45
check point inhibitors indications
treatment of late stage melanoma
46
Ipilimumab MOA
Ab specific for CTLA-4 Antagonizes the negative regulatory CTLA-4 protein responsible for down regulating activated T cells enhances T cell response
47
Ipilimumab adverse effects
potential for rare autoimmune response (can be fatal)
48
Pembrolizumab/nivolumab MOA
Ab specific for the PD1 protein which is expressed on activated T cells that is responsible for down regulating T cell responses. by blocking the receptor, it prevents tumor cell PD-1L from inhibiting the immune responses, therefore leading to enhanced tumor immune responses
49
Methotrexate indication
treatment of autoimmune diseases - especially RA
50
Methotrexate MOA
inhibition of dihydrofolate reductase to inhibit lymphocyte proliferation indirect mechanism of immunosppression
51
methotrexate adverse effects
``` renal toxicity hepatic toxicity GI toxicity lung disease BM suppression Neurotoxicity teratogenic ```
52
can methotrexate be given to pregnant women
no
53
cyclophosphamide indications
prevent graft rejection prevent GvHD severe cases of autoimmune disease
54
cyclophosphamide MOA
alkylation chemotherapeutic agent crosslinks DNA, RNA and proteins inhibits cell proliferation promotes apoptosis
55
cyclophosphamide adverse effects
``` DM suppression GI toxicity increased risk of infections increased risk of malignancy teratogenic (males/females) ``` (same as chlorambucil)
56
who should not take cyclophosphamide and chlorambucil
pregnant women or women who wish to become pregnant and men who wish to become fathers
57
chlorambucil indications
sometimes used in the treatment of autoimmune disease
58
chlorambucil MOA
alkylation chemotherapeutic agent, crosslinks DNA, RNA and proteins inhibits cell proliferation promotes apoptosis
59
Chlorambucil adverse effects
``` DM suppression GI toxicity increased risk of infections increased risk of malignancy teratogenic (males/females) ``` (same as cyclophosphamide)
60
immunosuppressive drugs used in the treatment of MS (4)
Fingolimod natalizumab interferon beta Glatiramer acetate
61
Fingolimod MOA
sphingosine analog binds to S1P receptor to promote sequestration of lymphocytes in the lymph node, thereby preventing lymphocyte entry to the CNS
62
Fingolimod adverse effects
bradyarrhythmia AV block increased risk of VZV infection (potential fatal) increased risk of malignancy
63
Natalizumab MOA
binds to alpha 4 integrin adhesion molecule | prevents entry of lymphocytes into the CNS
64
Interferon beta MOA
Activates IFN beta receptors alters expression of pro-inflammatory gene expression inhibits entry of inflammatory cells into CNA
65
Glatiramer Acetate MOA
polymer of 4 amino acids found in MBP | production of specific suppressor T cells that suppress inflammation in the CNS
66
Adverse effects of Natalizumab
increased risk of PML especially if | prior use of immunosuppression, seropositive for JC virus, chronic treatment

Pharm final sem 1 (1 decks)

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