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Pharmacology > Immune Modulators > Flashcards

Immune Modulators Flashcards

1
Q

Action time of prednisone

A

Intermediate acting
12-36 hrs

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2
Q

Action time of prednisolone and what makes it different from prednisone?

A

12-36 hours
This one also has parenteral administration

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3
Q

Dexamethasone acting time

A

Long acting
36 - 72 hours

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4
Q

Differences between prednisone and dexamethasone

A

Dexamethasone
- Long acting >36 hrs
- Can be given in oral, parenteral, and topical forms

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5
Q

Mechanism of action glucocorticoids + 7 things they decrease

A

Decrease NF-kB activation
= suppress T cell proliferation and IL-1, IL-6, TNF, IFN

Inhibit macrophage antigen processing

Decrease: PG, leukotrienes, histamine, PAF, bradykinin, NO, IgG

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6
Q

Glucocorticoid uses (4)

A
  • Transplant
  • GvHD
  • Autoimmune diseases: SLE, RA, SD, psoriasis, asthma
  • IBD
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7
Q

Glucocorticoids main side effect

A

Growth retardation (adeno atrophy) or Cushing’s

Others:
- Avascular bone necrosis
- Osteopenia, osteoporosis
- Cataracts
- Hypertension
- Hyperglycemia
- Hypercholesterolemia

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8
Q

Cyclosporine mechanism of action

A
  1. Forms a complex with cyclophilin
  2. Binds to serine/threonine phosphatase calcineurin and blocks Ca2+ action of activating calcineurin
  3. Disrupt NF-aT phosphorylation
  4. NF-aTs don’t translocate to nucleus

= no IL-2 transcription

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9
Q

Immunosuppresor uses (3)

A
  • Transplant
  • Autoimmune: RA, Crohn, psoriasis, nephrotic sx, asthma, DM type I, etc.
  • GvHD
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10
Q

Cyclosporine ADME

A

A: 50% available oral or IM
D: 50-60% in RBC or lymphocytes. Highly lipophilic.
M: CYP3A4
E: bile/feces, breast milk

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11
Q

Cyclosporine side effects NHLTG

A

Nephrotoxicity
Hirsutism
LDL increase
Tremor
Gum hyperplasia

Others: hypertension, hyperK, hyper uric acid, viral infections, hyperglycemia

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12
Q

Meds that decrease cyclosporine concentration (3)

A
  • Phenobarbital
  • Phenytoin
  • Rifampin
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13
Q

Meds that decrease cyclosporine clearance (3)

A
  • Erythromycin
  • Ketoconazole
  • Grapefruit
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14
Q

Can cyclosporine and sirolimus be given together?

A

Yes but with time between.

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15
Q

Between cyclosporine, tacrolimus, and sirolimus, which is more potent?

A

Tacrolimus

*more toxic also

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16
Q

Tacrolimus mechanism of action

A

Also known as FK506, it’s an immunophilin that:
1. Binds to FKBP
2. Inhibit calcineurin phosphatase

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17
Q

Tacrolimus ADME

A

A: food decreases absorption. Oral or IM
D: 75-99% protein bound
M: CYP3A
E: fecal

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18
Q

Tacrolimus side effects

A

Nephro and neurotoxicity
Hyper K
Hypertension
Hyperglycemia and DIABETES when combined with glucocorticoids

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19
Q

What medication type is rapamycin?

A

Sirolimus

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20
Q

Sirolimus mechanism of action

A
  1. Binds to FKBP12
  2. Binds to mTOR complex 1 and inhibits pathway
  3. Stops cell cycle phase between G1 and S
  4. Inhibit IL-2 RESPONSE
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21
Q

Sirolimus ADME

A

A: 15% availability oral
D: bound to albumin 40%
M: CYP3A4
E: feces

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22
Q

Which has less renal toxicity: calcineurin inhibitors or proliferation inhibitors (sirolimus)?

A

Sirolimus

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23
Q

Sirolimus toxicity

A

Tolerizing effects
- Nephrotox
- HYPERLIPIDEMIA
- Hypertension
- Worsen proteinuria
- Lymphocele
- PANCYTOPENIA
- Mouth ulcers

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24
Q

Methotrexate mechanism of action

A

FOLATE ANTAGONIM
- Inhibits dihydrofolate reductase
- No folic acid activation
= prevent purine and pyrimidine synthesis
= less cell proliferation

Other: inhibit spermine, cause transmethylation, inhibit release of adenosine

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25
Q

Methotrexate ADME

A

A: IV, IM, oral
D: bound 50%, distributed to third-space fluids
M: aldehyde oxidase in liver, intestinal flora
E: urine

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26
Q

Methotrexate side effects NABPRT

A
  • Nausea, vomit, diarrhea + ULCERS
  • Alopecia
  • Bone marrow depression = PANCYTOPENIA
  • Pulmonary fibrosis
  • Renal and hepatic disorders
  • TERATOGENIC folate deficiency
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27
Q

Azathioprine mechanism of action

A

PRODRUG —> 6-MCP with glutathione
2. —> thio-IMP
3. Converts GMP to GTP
4. Inhibit purine synthesis = less cell proliferation

PURINE ANALOGUE

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28
Q

Azathioprine ADME

A

A: oral or IV
D: doesn’t cross BBB, bound 30%
M: xanthine oxidase —> 6-MCP (activation)
E: urine

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29
Q

Avoid azathioprine with:

A

Allopurinol —> blocks xanthine oxidase
Myelosuppressive
ACE inhibitors

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30
Q

Azathioprine side effects BIG A

A

Bone marrow suppression = PANCYTOPENIA
Increase risk of infections
GI effects
Alopecia

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31
Q

Mycophenolate mofetil mechanism of action

A

PRODRUG —> MPA
2. Inhibits iosine monophosphate dehydrogenase (IMPDH)
3. Inhibit guanine synthesis

= less lymphocyte proliferation

32
Q

Mycophenolate mofetil ADME

A

A: oral or IV
D: extensively bound
M: MPA—> inactive glucuronide
E: urine

33
Q

Azathioprine uses

A
  • Acute glomerulonephritis
  • Autoimmune: SLE, RA
  • Crohn
  • Transplant
34
Q

Mycophenolate mofetil side effects

A

WITH TACROLIMUS: diarrhea and alopecia
- Bone marrow suppression = PANCYTOPENIA
- Vomiting and diarrhea
- Hypertension
- Infections
- PREGNANCY: anomalies, loss

35
Q

Mycophenolate mofetil avoid with:

A
  • Tacrolimus
  • Antiacids
  • Cholestyramine
  • Aciclovir
36
Q

Immunosuppresors (10)

A
  • Glucocorticoids
  • Cyclosporine
  • Tacrolimus
  • Sirolimus
  • Azathioprine
  • Methotrexate
  • Mycophenolate mofetil
  • Infliximab
  • Adalimumab
  • Rituximab
37
Q

Glucocorticoids ____ (increase/decrease) T cell apoptosis

A

Increase

38
Q

Short-acting glucocorticoids (2)
Intermediate-acting (3)
Long-acting (2)

A

Short: hydrocortisone, cortisone

Intermediate: prednisone, prednisolone, methylprednisolone

Long: dexamethasone, betamethasone

39
Q

Which immunosuppresor should NOT be given to diabetics and why?

A

Tacrolimus

Toxic to pancreatic b cells

40
Q

Glucocorticoid ADME

A

A: oral, IM, IV
D: rapidly removes from blood, distributed everywhere
M: CYP3A4
E: urine

41
Q

2 medications commonly used for synergistic immunosuppression

A

Sirolimus + glucocorticoids

42
Q

Medication used in rheumatic diseases vs glucocorticoids

A

Mycophenolate mofetil

43
Q

Methotrexate uses aside from immunosuppression

A
  • Cancer, especially ALL
  • Ectopic pregnancy abortion
44
Q

Infliximab acts against:

A

TNF-a

45
Q

Anti TNF-a uses

A

Refractory therapy for chronic inflammatory sistemic

Ex. RA, Crohn, psoriasis

46
Q

Anti TNF-a side effects

A
  • Reactivation of prior infections
  • Malignancy
  • Drug-induced lupus
  • Pancytopenia
    *heart failure patients
47
Q

Infliximab ___ (can/can’t) be given with other immunosuppressors

A

CAN’T

48
Q

Adalimumab target

A

TNF-a

49
Q

Difference between infliximab and adalimumab

A

Infliximab is chimeric, given IV
Adalimumab is humanized, given subcutaneously

50
Q

Rituximab uses

A
  • RA
  • ITP or TTP
  • MS
  • B-cell non-Hodgkin lymphoma
51
Q

Rituximab main side effect

A

Risk of progressive multifocal leukoencephalopathy PML with latent JC virus

52
Q

Immunomodulators (5)

A
  • Glatiramer
  • Elapegdemasa
  • Perixaflor
  • Triciclib
  • Pagademasa
53
Q

What is glatiramer acetate used for?

A

Treatment of relapsing MS

54
Q

Glatiramer acetate mechanism of action

A

Acts as target for T cells instead of neuronal myelin

Less Th1 (inflammatory), more Th2 (anti-inflammatory)

55
Q

Glatiramer acetate ADME

A

A: subcutaneous
D: doesn’t cross BBB

56
Q

Perixaflor mechanism of action

A

Antagonism of CXCR4 —> block binding of SDF-1a
= interfere with HSC retention in bone marrow

= PERIPHERAL LEUKOCYTOSIS

57
Q

Perixaflor uses

A

With FILGRASTIM
- Non-Hodgkin’s lymphoma
- Multiple myeloma

58
Q

Perixaflor ADME

A

A: subcutaneous
D: <58% bound
M: n/a
E: urine

59
Q

Trilaciclib mechanism of action

A

CDK4 and CDK6 (kinase) inhibitor
= decrease in bone marrow suppression caused by chemotherapy

NOTE: teratogen

60
Q

Elapegademase mechanism of action

A

Exogenous adenosine deaminase
= reduction of toxic adenosine

= increase lymphocytes

61
Q

Elapegademase main use

A

SCID caused by ADA deficiency

Note: IM administration

62
Q

Pegademase bovine mechanism of action

A

Enzyme replacement for adenosine deaminase deficiency

63
Q

Cyclosporine

A

Immunosuppressor

64
Q

Tacrolimus

A

Immunosuppressor

65
Q

Sirolimus

A

Immunosuppressor

66
Q

Methotrexate

A

Immunosuppressor

67
Q

Azathioprine

A

Immunosuppressor prodrug

68
Q

Mycophenolate mofetil

A

Immunosuppressor prodrug

69
Q

Infliximab

A

TNFa inhibitor

70
Q

Adalimumab

A

TNFa inhibitor

71
Q

Rituximab

A

CD20 antagonist

72
Q

Glatiramer

A

Immunomodulator
(MS)

73
Q

Elapegdemase

A

Exogenous ADA enzyme
(SCID)

74
Q

Perixaflor

A

Immunostimulant
(NHL and MM)

75
Q

Trilaciclib

A

Reduce myelosuppression by chemotherapy
Kinase inhibitor
(SCLC)

76
Q

Pegademase

A

ADA enzyme replacement
(SCID)

Pharmacology (13 decks)

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