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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
Q

what are the 2 mTor inhibitors

A

sirolimus and everolimus

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26
Q

what are the indications for a mTor inhibitor

A

immunosuppression
prevent graft rejection (not liver or lung)
to prevent GvHD
included in arterial stents to inhibit restenosis

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27
Q

what is the MOA of mTor inhibitors

A
  • 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
Q

what are the side effects of mTor inhibitors

A

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
Q

how is mTor metabolized

A

via CYP3A4 = many drug interactions

30
Q

what patient populations is mTor inhibitors contraindicated or not recommended for

A

contraindicated in pregnancy

not recommended - lung transplantation (risk of anastomotic dehiscence), liver transplantation (risk of hepatic artery thrombosis)

31
Q

what drugs are used for induction immunotherapy

A

rabbit anti-thymocyte globulin
alemtuzumab
basiliximab

32
Q

what is the MOA for Rabbit anti-thymocyte globulin

A

rabbit polyclonal anitibodes specific for human lymphocytes depletes lymphocytes from blood

33
Q

what are adverse effects of rabbit anti-thymocyte globulin

A

*cytokine release syndrome

leukopenia

34
Q

what is the MOA for alemtuzumab

A

binds to CD52 expressed on T cells, B cells, macrophages, NK cells, and granulocytes

depletes cells from blood by Ab-mediated lysis

35
Q

Basiliximab MOA

A

Antagonist of the IL-2R

blocks T cell proliferation

36
Q

adverse effects for Alemtuzumab

A

*cytokine release syndrome
leukopenia
can take > 1 year for immune system to recover

37
Q

what 3 drugs can be used for passive immunization

A

IVIG
Rho (D)
Hyperimmune Ig

38
Q

what are indications for IVIG

A

provides short lived humoral immunity to patients with deficiency in humoral immune system (ie hypogammaglobulinemia)

39
Q

what is the MOA of IVIG

A

provides patients with Ig from healthy immunized donors to provide immunity to common pathogens

40
Q

Rho (D) indications

A

prevention of hemolytic disease of the newborn in newborns born to Rh- females

41
Q

MOA of Rho(D)

A

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
Q

Hyperimmune Ig indications

A

to provide rapid specific antibody immunity to specific viruses and/pr toxins

43
Q

hyperimmune Ig MOA

A

purified Ig to specific antigens purified from healthy volunteers
given IV to patients in order to promote clearance of a virus or toxin

44
Q

what are the 2 immune check point inhibitors

A

Ipilimumab

pembrolizumab/Nivolumab

45
Q

check point inhibitors indications

A

treatment of late stage melanoma

46
Q

Ipilimumab MOA

A

Ab specific for CTLA-4
Antagonizes the negative regulatory CTLA-4 protein responsible for down regulating activated T cells

enhances T cell response

47
Q

Ipilimumab adverse effects

A

potential for rare autoimmune response (can be fatal)

48
Q

Pembrolizumab/nivolumab MOA

A

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
Q

Methotrexate indication

A

treatment of autoimmune diseases - especially RA

50
Q

Methotrexate MOA

A

inhibition of dihydrofolate reductase to inhibit lymphocyte proliferation

indirect mechanism of immunosppression

51
Q

methotrexate adverse effects

A 
renal toxicity 
hepatic toxicity
GI toxicity
lung disease
BM suppression
Neurotoxicity 
teratogenic
52
Q

can methotrexate be given to pregnant women

A

no

53
Q

cyclophosphamide indications

A

prevent graft rejection
prevent GvHD
severe cases of autoimmune disease

54
Q

cyclophosphamide MOA

A

alkylation chemotherapeutic agent
crosslinks DNA, RNA and proteins
inhibits cell proliferation
promotes apoptosis

55
Q

cyclophosphamide adverse effects

A 
DM suppression
GI toxicity
increased risk of infections
increased risk of malignancy
teratogenic (males/females)

(same as chlorambucil)

56
Q

who should not take cyclophosphamide and chlorambucil

A

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

57
Q

chlorambucil indications

A

sometimes used in the treatment of autoimmune disease

58
Q

chlorambucil MOA

A

alkylation chemotherapeutic agent, crosslinks DNA, RNA and proteins
inhibits cell proliferation
promotes apoptosis

59
Q

Chlorambucil adverse effects

A 
DM suppression
GI toxicity
increased risk of infections
increased risk of malignancy
teratogenic (males/females)

(same as cyclophosphamide)

60
Q

immunosuppressive drugs used in the treatment of MS (4)

A

Fingolimod
natalizumab
interferon beta
Glatiramer acetate

61
Q

Fingolimod MOA

A

sphingosine analog
binds to S1P receptor to promote sequestration of lymphocytes in the lymph node, thereby preventing lymphocyte entry to the CNS

62
Q

Fingolimod adverse effects

A

bradyarrhythmia
AV block
increased risk of VZV infection (potential fatal)
increased risk of malignancy

63
Q

Natalizumab MOA

A

binds to alpha 4 integrin adhesion molecule

prevents entry of lymphocytes into the CNS

64
Q

Interferon beta MOA

A

Activates IFN beta receptors
alters expression of pro-inflammatory gene expression
inhibits entry of inflammatory cells into CNA

65
Q

Glatiramer Acetate MOA

A

polymer of 4 amino acids found in MBP

production of specific suppressor T cells that suppress inflammation in the CNS

66
Q

Adverse effects of Natalizumab

A

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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