Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Multisystems: Pharmacology > Immunopharmacology > Flashcards

Immunopharmacology Flashcards

1
Q

What are the 3 signals for T Cell Activation?

A
  1. MHC (w/ peptide) binding to TCR
  2. B7 binding to CD28
  3. IL-2 binding to IL-2 Receptor
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Calcineurin Inhibitors (CNIs)

A

Cyclosporine and Tacrolimus

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

Do cyclosporine and tacrolimus bind the same thing?

A

No.

Cyclosporine binds cyclophilin

Tacrolimus binds FK-binding protein

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

MOAs of CNIs

A

Calcineurin is a cytoplasmic phosphatase responsible for activation of T-cell transcription factors:

IL-2, IL-3, and IFN-y

By inhibiting it, the 1st signal of T cell activation is blocked

(Calcineurin is one of the first down-stream signals to be activated by MHC II + peptide presenting to a TCR)

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

What is cyclosporine used for?

A

DOC for organ/tissue transplantation

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

What is tacrolimus used for?

A

Alternative to cyclosporine in renal and liver transplants (tacrolimus is less nephrotoxic)

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

Side effects of CNIs?

A

Both are nephrotoxic

Gingival overgrowth (only cyclosporine)

Peripheral Neuropathy

*Both metabolized by CYP3A4/3A5

*Drugs that alter expression or activity will also change serum concentration (i.e., drugs that inhibit CYP3A4 will increase CsA concentration)

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

Sirolimus

A

Inhibits proteins synthesis (mTOR complex 1)

Used to prevent renal allograft rejection (as effective as CsA without nephrotoxicity)

Additional use in stents to prevent coronary artery restenosis

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

Side effects of Sirolimus

A

Anemia

Thrombocytopenia

Hyperlipidemia

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

Mycophenolate Mofetile (MMF)

A

An inhibitor of de novo synthesis of purines (blocks DNA replication)

Adjunctive immunosuppresant actions, permitting dose reductions of cyclosporine to limit toxicity

  • hydrolyzed by liver esterases to MPA (active metabolite)
  • lymphocytes can only derive nucleotides from de novo synthesis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Side effects of MMF and Azathioprine

A

GI distress

Leukopenia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Azathioprine

A

Purine analog metabolized to 6-mercaptopurine; disrupts de novo purine synthesis

Used in combination therapy with prednisone (+/- CsA/Tacrolimus) to prevent organ rejection and treat severe RA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

1st line DMARDs for RA

A

DMARD = Disease-Modifying Anti-Rheumatic Drug

Methotrexate

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Methotrexate

A

Folic acid analogue; inhibits DHFR (required for nucleoside syntheis) and AICAR transformylase (release of excess adenosine is anti-inflammatory)

Side effects = teratogenicity and BM suppression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Leflunamide

A

Prodrug whose active metabolite inhibits dihydroorotate dehydrogenase (an essential enzyme in pyrimidine biosynthesis)

Side effect = GI distress

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

Monoclonal antibodies:

  • omab
  • ximab
  • zumab
  • umab
A
  • omab = all mouse (greatest chance of hypersensivity)
  • ximab = FC part of Ig is mouse
  • zumab = only small part is mouse
  • umab = all human
17
Q

CTLA4-Ig

A

Abatacept and Belatacept

Competes with CD28 and stops Signal 2

Used for RA (abatacept) and in combo therapy for transplant (belatecept)

18
Q

anti-CD25

A

Daclizumab and Basiliximab

Prevents IL-2 from binding (blocks Signal 3)

*Used with CNIs/AZA for kidney and cardiac transplant

19
Q

Infliximab

Etanercept

Adalimumab

A

anti-TNF (inhibits pro-inflammatory cytokines)

**KNOW THESE**

20
Q

Anakinra

A

Anti-IL-1/1R

21
Q

Tocilizumab

A

anti-IL-6R

22
Q

Rituximab

A

Targets CD20

Used to treat RA

23
Q

Natalizumab

Fingolimod

IFN-B

A

Drugs for mutiple sclerosis (inhibitors of T cell migration)

Natalizumab: blocks entry into target site (anti-VLA4)

against α4subunit of α4β1-integrin (VLA-4)

Fingolimod: blocks exit from lymph node (binds S1PR super agonist)

IFN-B: multiple MOAs including reduced leukocyte migration across BBB

24
Q

Omalizumab

A

Treatment option for Type I hypersensitivity

(anti-IgE mab)

Blocks without crosslinking IgE that is already bound

25
Q

1st step in treating anaphylaxis

A

Epinephrine (reverses bronchoconstriction and vasodilation)

Also consider:

  • remove antigen
  • treat with anti-histamines
  • treat with corticosteroids
  • aggressive IV fluids
26
Q

Drugs that suppress T cell activation via signal 1

A

CNIs: CsA and Tacrolimus

27
Q

Drugs that suppress T cell activation via signal 2

A

Abatacept and Belatecept (CTLA4-Ig)

28
Q

Drugs that suppress T cell activation via Signal 3

A

Daclizumab, Basiliximab (anti-CD25 mAbs, block IL-2R)

Sirolumus (mTOR inhibitor)

MMF, Azathioprine, Leflunomide (DNA synthesis inhibitors)

29
Q

Drugs that suppress inflammation

A

DMARDs: methotrexate and leflunamide

Infliximab, Etanercept, Adalimumab (TNF Inhibitors)

Anakinra (IL-1R antagonist)

30
Q

Drugs that block Type I Hypersensitivity

A

Omalizumab

Epinephrine (for anaphylaxis)

Multisystems: Pharmacology (11 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions