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Pharm 4 > Immunosuppressive Drugs > Flashcards

Immunosuppressive Drugs Flashcards

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1
Q

Skeletal autoimmune diseases

A

Rheumatoid arthritis (RA)

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2
Q

Systemic autoimmune diseases

A

Systemic lupus erythematosus

Polyarteritis nodosa

Sarcoid

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3
Q

Neruonal autoimmune diseases

A

Multiple sclerosis

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4
Q

GI autoimmune diseases

A

Chron’s disease

Ulcertive colitis

Celiac disease

Pernicious anemia (lack of GIF)

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5
Q

Skin autoimmune diseases

A

Vitiligo

  • Light patches due to death of melanocytes

Psoriasis

  • Scaly painful and associated w/ joint disease
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6
Q

Secretory autoimmune diseases

A

Sjogrens

  • Salivary and tear glands

Graves

  • Hypothyroidism

Addison’s

  • Adrenal cortex

Diabetes

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7
Q

Pathway to cytotoxic B cells vs antigen specific B cells

A

Cytotoxic B cells

Mac→CD4 T cell→IL-2→Cyt. B cells

Antigen specific B cells

Mac→CD4 T cell→IL-4,5→Ant. specific B cells

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8
Q

What activates Janus kinases?

What do janus kinases activate?

A

IL receptors (1, 6, 12, 23)

TNF receptor

Janus kinases→gene activation→IL-2 act.→New T cells/more gene activation

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9
Q

Role of calcium in CD4

A

Ca→Act. calcineurin→Act. NFAT→gene activation→IL-2 act.→New T cells/more gene activation

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10
Q

What are all of the receptors on CD4

A

TNF

IL-1

IL-6, 12, 23

CD2

Alpha integrins

IL-2

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11
Q

Concerns w/ all immunosuppressants

A

Infection

May cause malignancy

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12
Q

Atgam

A

ATGam

Tx: Acute renal transplant injection

Immunosuppressant

Antithymocyte globulin (ATG)–Polyclonal antibodies

Effects: Reduces circulating T cells(Wikipedia)

_A_ffects _T_ cell activation

SE:

  • Polyclonal antibodies may lead to allergic rxn
    • From horse or rabbit
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13
Q

Abatacept

A

Tx: RA

Immunosuppressant

Mech: binds to and inh. CD80, CD86 receptors

Affects T cell activation

ABatacept CD80+86 receptors

_A_batacept for _A_rthritis

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14
Q

Belatacept

A

Tx: Renal transplantation

Immunosuppressant

Mech: binds to CD80, CD86 receptor

Affects T cell activation

SE:

  • Increase malignancy

ABatacept CD80+86 receptors (Belatacept too)

Abatacept: RA Belatacept: Kidney trans.

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15
Q

Monoclonal antibody naming

A

Ending: -mab

Middle of name=target:

  • “li” or “i”-immune
  • “tu”-tumor

Connecting letters=Source:

  • xi=chimeric-mouse Ab w/ some human Ab substituted
    • Most antigenic
  • zu=humanized-human Ab w/ some mouse parts
  • u=fully human
    • Least antigenic

*Always given parenterally

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16
Q

Natalizumab

A

Nata-li-zu-mab

MAb affecting immune sys. from humanized source

Immunosuppressant

Tx: Chron’s + MS

Mech: Binds to alpha integrin binding site on CD4 (and other immune cells)

Not really a receptor but a “binding site”

SE:

  • Linked w/ progressive multifocal leukoencephalothopy (PML)
    • Fatal viral disease of CNS

_Nat_ty’s give you the beer shits

_Nat_alizumab=Chron’s

natALIzumab-binds ALpha Integrin binding site

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17
Q

Tocilizumab

A

Toci-li-zu-mab

MAb affecting immune sys. from humanized source

Immunosuppressant

Tx: RA

Mech: Binds to IL-6 receptor

  • Football players get tackled so they have RA but all of the ladies want to have risque sex w/ them*
  • Football players get tocilizumab so they have RA but all the ladies want to have IL-6 receptor with them*
18
Q

Ustekinumab

A

Ustek-i-nu-mab

MAb affecting immune sys. from human source

Immunosuppressant

Tx: Psoriasis

Mech: Binds to IL-12, 23

  • Michael Jordan used to wear #23 until someone stole his jersey and he had to wear #12 (true story). Whoever stole it ought to be sorry.*
  • MJ uste-kinumab wear IL-23 then wore IL-12. They ought to be psoriases.*
19
Q

What agents bind TNF

A

Etanercept (RA)

Infliximab (RA,C)

Certolizumab (RA,C)

Adalimumab (RA)

Golimumab (RA, etc)

Think TNF=TNT (dynamite)

Explosions In Caves Affect Gollum

20
Q

Etanercept

A

Tx: RA

Immunosuppressant

Mech: Binds TNF

Route: SubQ (in comb. w/ other immunosupp)

Synthesized molecule

eTaNercept-binds TNF

21
Q

Infliximab

A

Infli-xi-mab

Tx: RA, Chron’s

Immunosuppressant

Mech: Binds TNF

Route: IV

SE:

  • Infusion→itching, hypertension, fever
  • Concerned if pt has pre-existing infection like fungus or Tb b/c infection may become worse
  • If you are _inflex_ible (from sitting on the toilet=Chron’s) take _inflix_imab although it may lead to _i_tching*
  • May also lead to hyperTensioN and Fever–binds to TNF*
22
Q

Adalimumab

A

Ada-li-mu-mab

Tx: RA

Immunosuppressant

Mech: Binds TNF

23
Q

Certolizumab

A

Tx: RA, Chron’s

Immunosuppressant

Mech: Binds TNF

24
Q

Golimumab

A

Tx: RA, Ulcerative colitis, psoriatic arthritis

Immunosuppressant

Mech: Binds TNF

25
Q

Anakinra

A

Tx: RA

Mech: Blocks IL-1 receptor

Route: SubQ

Used w/ other immunosuppressants like methotrexate

Should NOT be used w/ TNF inh b/c may lead to serious infection (too much suppression)

anakinRA=RA=RAceptor blocker

26
Q

Rilonacept

A

Tx: RA

Mech: Binds to IL-1

Route: SubQ

Used w/ other immunosuppressants like methotrexate

Should NOT be used w/ TNF inh b/c may lead to serious infection (too much suppression)

  • Anakinra-blocks IL1 receptor*
  • Rilonacept-binds to IL1*
27
Q

Cyclosporine

A

Tx: Transplants, psoriasis, dry eye (tear duct inflam)

Fungus derived

Route: Emulsion

Mech:

Binds to intracellular protein-cyclophyllin

Complex forms and _inh. enzyme-_calcineurin phosphatase

Enzyme inhibitor

Prevents act. of NFAT complex which then prevents act of gene that codes for IL2,3 and TNF alpha

T cell inhibited

Kinetics

  • Metabolized by P450
    • Lots of drug interactions-esp. antibiotics

SE:

  • Nephrotoxicity
  • Hepatotoxicity
  • Cosmetic changes
    • Hypertrichosis
    • Gingival hyperplasia
  • Increased cholesterol (reversible)
  • Mild hypertension (reversible)

Cyclosporin-binds to Cyclophyillin→inh. Calcinuerin, used for Crusty eyes and skin, may cause Cosmetic Changes, î Cholesterol, Cidney (kidney) damage

  • What else affects calcinuerin phosphatase? Tacrolimus*
  • Cyclosporine: Binds cyclophyllin*
  • Tacrolimus: Binds FK protein*
28
Q

Tacrolimus

A

Tx: Transplantation

Immune suppression

Mech:

  • Binds to FK binding protein
  • _Inh. calcineurin phosphatase _
    • Like cyclosporin but binds to diff protein→inh. of cytokine synth

More eff. than cyclosporin A-Increase max inh. effect

SE:

  • Nephrotoxicity
  • Neurotoxicity
  • Alopecia (baldness)
    • Less cosmetic effects than cyclosporine
  • Diabetes

Metab by P450

  • Tacrolimus for transplantations*
  • What else binds to FK protein? Sirolimus/Everolimus*
  • Tacrolimus: Inh calcinuerin phosphatase*
  • Sirolimus: Inh kinase*
  • What else affects calcinuerin phosphatase? Cyclosporine*
  • Cyclosporine: Binds cyclophyllin*
  • Tacrolimus: Binds FK protein*
29
Q

Glucocorticoids

A

Tx: Inh. all immune processes

Immunosuppressant

Mech:

  • GC cross CM, bind to receptor and dimerize, then affect trans.
  • Decrease PGE and leukotrienes
  • Alter migration of immune cells

Often used in comb. w/ other immunosuppressants

SE: Sig SE w/ long term use. Refer to other lecture

30
Q

Sirolimus

A

Tx: Transplant, psoriasis

Mech: Bind to FK binding protein

inh. kinase required for binding of IL-2 induced transcription factors to DNA→decreased cytokine production

Often used in combination w/ glucocorticoids

SE:

  • Some renal toxicity
    • Less than tacrolimus
    • Synergistic effect w/ used in comb w/ many immunosupp.
  • Some lung toxicity

Metab by P450

  • What else binds to FK protein? Tacrolimus*
  • Tacrolimus: Inh calcinuerin phosphatase*
  • Sirolimus/Everolimus: Inh kinase*
31
Q

Everolimus

A

Tx: Transplant, psoriasis

Mech: Bind to FK binding protein

inh. kinase required for binding of IL-2 induced transcription factors to DNA→decreased cytokine production

Often used in combination w/ glucocorticoids

SE:

  • Some renal toxicity
    • Less than tacrolimus
    • Synergistic effect w/ used in comb w/ many immunosupp.
  • Some lung toxicity

Metab by P450

…

  • What else binds to FK protein? Tacrolimus*
  • Tacrolimus: Inh calcinuerin phosphatase*
  • Everolimus/Sirolimus: Inh kinase*
32
Q

Basiliximab

A

Immunosuppressant

Mech: IL-2 receptor blocker

Used w/ CSA

65% human (chimeric)

Hypersensitivity rxn

  • Hypotension
  • Bronchospasm
  • Pulmonary edema

Harry Potter is a hypersensitive bitch when he fights the basilisk in the Chamber of Secrets, which is the 2nd reading in the series

Hypotension + Pulmonary edema, hypersensitivity, bronchospasm, basiliximab, used w/ CSA. IL-_2_ receptor blocker

33
Q

Which immunosuppressive MABs couldn’t you give for RA?

A

Natalizumab (Chron’s and MS)

Ustekinumab (Psoriasis)

Basiliximab

34
Q

Tofacitinib

A

-ib=inhibitor (often kinase inh)

Mech: Janus kinase inh.

  • Inh signal pathways of cytokines and ILs
  • Modifies effect of cytokines on gene exp
  • Prevents act. of signal transducers and activators of trans.

SE:

  • Increase infection
  • Increase malignancy
35
Q

Azathioprine

A

Tx: RA, Chron’s, trans

Prodrug

Mech:

  • Converted to 6-mercaptopurine
  • Inh. synth of purines (guanosine required for DNA synth)
  • Inh. several enzymes responsible for GMP synth
    • Non specific

SE:

  • Bone marrow suppression→
    • Megaloblastic anemia
    • Thrombocytopenia
    • Leukopenia

6-mercaptopurine is also an anti-cancer agent

36
Q

Mycophenolate mofetil

A

Tx: Transplants and lupus

More specific replacement than azothioprine

Inh. enzyme inosine monophosphate DH→Inh. guanisine synth.

SE:

Bone marrow decrease

GI cell disruption

37
Q

Methotrexate

A

Tx: DOC early tx of RA

Used more as immunosuppressant than anti-cancer drug

DMARD-Disease modifying anti-rheumatic drug

Actually stops progression of RA rather than just treat symptoms

Mech:

  • Analog of Folic Acid
  • Inh. enzyme: Dihydrofolate reductase
  • PABA→Folic acid⇒Dihydrofolic acid⇒tetrahydrofolic acid
    • ⇒ indicate where DHFR works
  • Inh. mammalian cell division
    • Inh. lots of folic acid dependent processes, especially in cells w/ rapid turnover (at high doses):
      • GI
      • Fetal development
      • Blood cells
    • Immune cells more susceptible than above though
38
Q

Leflunomide

A

Immunosuppressant

Prodrug. Gets converted into Teriflunomide

Mech: Inhibits dihydroorotate DH

  • Rate limiting step in production of pyrimidine (so inh. pyr. production)
  • Decrease in UMP and TMP
  • More effect on lymphocytes

SE:

  • Diarrhea and abdominal pain (rapidly replicating GI cells)
    • Flu like symptoms w/ flunomides
  • Teratogenic
    • Must take bile acid binding agent to get rid of all of drug if pregnant

Inhibits P450

  • You no ride w/ me–get another Designated Driver*
  • “Flu-no-ride w/ me. Get another DD (inh. Dihydroorate DH)*
39
Q

Teriflunomide

A

Immunosuppressant

Gets converted from prodrug Leflunomide

Mech: Inhibits dihydroorotate DH

  • Rate limiting step in production of pyrimidine (so inh. pyr. production)
  • Decrease in UMP and TMP
  • More effect on lymphocytes

SE:

  • Diarrhea and abdominal pain (rapidly replicating GI cells)
    • Flu-like symptoms w/ flunomides
  • Teratogenic
    • Must take bile acid binding agent to get rid of all of drug if pregnant

Inhibits P450

  • You no ride w/ me–get DD*
  • “Flu-no-ride w/ me. Get DD (dihydroorate DH)*
40
Q

Hydroxychloroquinone

A

Immunosuppressant

Mech:

  • Taken up by macs and conc. in mac lysosomes
  • Interferes w/ mac. processing of antigens (1st step in immune process)

Toxicities:

  • GI fxn
  • Dermatitis
  • Irr. retinal damage
    • Retinal changes and visual disturbances may progress even after discontinuation

Pharm 4 (9 decks)

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