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Biologics Flashcards

1
Q

Anti-proliferative agents (3)

A

Cyclophosphamide
Mycophenolate mofetil
Azathioprine

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2
Q

T cell signalling inhibitors (3)

A

Tacrolimus
Ciclosporin
Sirolimus

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3
Q

Anti-TNF a

A

Infliximab

Adalimumab

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4
Q

Anti-IL12/23

A

Ustekinumab

Used in psoriasis and psoriatic arthritis after TNF a

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5
Q

Muromonab
MoA
Indications
SE

A

Blocks CD3 on T cells

Used in active rejection

SE- fever, leucopenia

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6
Q

Basiliximab
MoA
Indications
SE

A

Blocks CD25 - part of the IL-2 receptor

Rejection prophylaxis

SE- GI disturbance

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7
Q

Tocilizumab

A

Blocks IL-6, stops acute phase reaction

Used in RA after anti TNF

SE- infection

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8
Q

Abatacept

A

Anti-CTLA-4 Ig, stops T cell costimulation

Binds to B7 protein (CD 80 and 86)

Used in RA after anti TNF a

SE- cough and infections

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9
Q

Cyclophosphamide

A

Alkylates guanine base. Affects B>T

Used in multisystem connective tissue disease- SLE, and in Ca

SE- hair loss, BM suppression, sterility, haemorrhagic cystitis, transitional cell Bladder Ca- due to renal excretion and accumulation in bladder

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10
Q

Mycophenolate

A

Blocks de novo nucleotide synthesis- affects B>T cells

Used in AI disease, vasculitis and transplantation

SE- BM suppression, herpes

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11
Q

Azathioprine

A

Prodrug ( met to 6 -metcaptopurine in liver)
Blocks de novo purine synthesis

Used in inflammatory and AI disease, transplantation (esp kidney)

SE- BM suppression- measure TPMT before Rx, hepatotoxic

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12
Q

Tacrolimus

A

Inhibits calcineurin, normally activates IL2 transcription, so Dec IL2

(binds FKBP-1A)

Rejection prophylaxis, in Protopic used in derm

SE- DM, renal toxicity

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13
Q

Ciclosporin

A

Calcineurin inhibitor, blocks IL2 transcription

Used in rejection prophylaxis

SE- renal toxicity, gingival hypertrophy

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14
Q

Sirolimus

A

Blocks clonal proliferation - blocks messenger pathways used in proliferation (esp IL-2 Receptor linked)

Used in transplant rejection prophylaxis

SE pulmonary toxicity, DM

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15
Q

Prednisolone

A

Inhibits phospholipase A2
Dec: platelet activating factor, arachidonic acid, trafficking on phagocytes
Lymphopenia, apoptosis of T and B cells, Dec Abs

Used as antinflammatory and in AI

SE

  • DM
  • central obesity
  • adrenal suppression
  • easy bruising
  • cataracts
  • glaucoma
  • pancreatitis
  • osteoporosis
  • moon face
  • acne
  • hirsuitism
  • neutrophilia
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16
Q

Plasmapharesis

A

Each time 50% of Pt plasma is replaced

Used in Goodpastures, Myasthenia etc
Ab mediated rejection

SE- rebound Ab production limits efficacy

17
Q

Infliximab

A

Binds to TNF-a

Mouse- Human chimer

Used in psoriasis, Crohns/UC, RA, ank spond and others

SE- TB, lymphoma, AI phenomena

18
Q

Ustekinumab

A

Binds to p40 subunit of IL12/23

Prevents NK and T cell activation

Used in psoriasis and psoriatic arthritis

SE- infections and cough

19
Q

Anti T cell (4)

A

Muromonab-CD3
Basiliximab
Tocilizumab
Abatacept

20
Q

Rituximab

A

Anti-CD20, decreases B cells (not plasma cells)

Used in lymphoma and AI

21
Q

Methotrexate

A

Inhibits dihydrofolate reductase (DHFR) - rqd for production of thymidine, and hence DNA synthesis

Also anti-folate, so can cause B12 deficiency

Used in AI disorders- RA, psoriasis, Crohns etc
Also chemo and as an abortifacient

SE- teratogenicity (stop at least 3/12 before pregnancy), hepatotoxic

22
Q

Alemtuzumab

A

CD52 Ab, –> lymphocyte depletion

Used in CLL, new variant being used for MS

SE- inc susceptibility to to CMV

23
Q

Natalizumab

A

Anti-a4 interim Ab

Used in MS and Crohns

SE- progressive, multifocal leucoencephalopathy

24
Q

Denosumab

A

Targets RANK ligand in bone to inhibit osteoclast function.
Prevents bone breakdown
Used in osteoporosis, also multiple myeloma and bony mets

Toxicity –> resp and urinary tract infections

25
Q

Adalimumab

A

Fully human anti TNF alpha

26
Q

Etanercept

A

TNF-α monoclonal antibody
Fusion protein between the TNF-receptor 2 and Fc portion of IgG1.

Potential adverse effects include increased risk of infection, demyelination
and malignancy.

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