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BSMS 204- Theme 1 > Lecture 17- Therapeutics (Biologics) > Flashcards

Lecture 17- Therapeutics (Biologics) Flashcards

1
Q

What drugs are used as symptoms relief for auto-immune disease?

A

-Anti-inflammatory drugs: NSAID- Aspirin, ibuprofen and diclofenac
-COX-2 inhibitors: celecoxib
-Steroids:
-Prednisolone etc
#short term use
#IM, injected into the inflamed joint
#slow down progression, preventing further damage to joints
#Long term use should be avoided

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2
Q

Describe the mechanism of action methotrexate?

A
  • Antimetabolite (folate analogue), inhibits cell proliferation
  • Increases adenosine level (anti-inflammatory)
  • Reduces the production of damaging polyamines
  • Induces apoptosis of activated CD4+ and CD8+ T-cells
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3
Q

what is the standard dose for the methotrexate and what is the advantage of this dose range?

A
  • 7.5mg to 25mg weekly Po or SC

- no significant anti-cancer or immunosuppressive effect

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4
Q

what is the advantage of taking methotrexate for RA?

A
  • Reduces inflammation quickly and keeps it under tight control
  • Reduces the risk of death from cardiovascular disease in people with RA
  • Taking supplements of folic acid reduces side-effects caused by folic acid depletion
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5
Q

Name other synthetic DMARDs, mechanism of action and conditions they are mainly used for?

A

1) Sulfasalazine (SSZ) – 2-component drug
Sulfapyridine (antibiotic) + 5-amino salicylic acid (anti-inflammatory)
Also used in ulcerative colitis

2) Hydroxychloroquine (HCQ) – antimalarial drug
Used in combination with other DMARDs
A possible mechanism of action: increases lysosomal pH in (immune) cells
Also used for the treatment of SLE

3) Leflunomide – lymphocyte inhibitor
Inhibits de novo pyrimidine synthesis
Most effective in reducing B-cell populations (but significant effect on T-cells too)

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6
Q

what is the purpose of using DMARDs combination therapy in treating RA?

A
  • Combinations of DMARDs – more effective in treating early active RA than the use of single drugs
  • Helpful when not possible to use biologic drugs e.g. in patients with recent cancer or chronic infection
  • Well tolerated, with no more side effects than the single drug
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7
Q

What is known as the anchor drug for the RA?

A

Methotrexate- acnchor drug to which other drugs should routinely be added

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8
Q

What is the most effective DMARD therapy and what other treatment should be considered for RA?

A
  • Triple combination of TX + SSZ + HCQ most effective

- Uses steroids in some form

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9
Q

What is the minimum treatment period before required to achieve symptoms control?

A

8-12 weeks treatment required to achieve improvement of symptoms

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10
Q

List the SE of most DMARD therapy?

A
  • Nausea
  • Loss of appetite
  • Diarrhoea
  • Rash, allergic reactions
  • Headache
  • Hair loss
  • Risk of infections (pneumonia)
  • Hepatotoxicity (metabolism)
  • Kidney toxicity (route of elimination)
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11
Q

What additional SE that we need to be aware for hydroxychloroquine and leflunoamide?

A

Hydroxychloroquine – accumulation of the drug in the eye (retinopthay)
Leflunomid – hypertension

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12
Q

what plays the central role in the inflammatory process in RA?

A

TNF

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13
Q

What are the targets of biologics in RA?

A 
IL-1
IL-6
T cells
B cells
TNF
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14
Q

Name the TNF blockers?

A
  • infliximab,
  • etanercept,
  • adalimumab
  • golimumab,
  • certolizumab pegol
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15
Q

Name the monoclonal antibody against B cells?

A

Rituximab

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16
Q

Name the T cell co-stimulation inhibitor?

A

Abatacept

17
Q

Name the monoclonal antibody against IL-6R?

A

Tocilizumab

18
Q

Name the class infliximab belongs to?

A

partially humanized mouse monoclonal anti-hTNF-a antibody

19
Q

Name the class etanercept belongs to?

A

soluble TNF receptor dimer

20
Q

Name the class adalimumab and golimumab belong to?

A

human IgG1 monoclonal anti-TNF-a antibody

21
Q

Name the class Certolizumab pegol belong to?

A

PEGylated anti-TNF-a monoclonal antibody fragment

22
Q

Describe the mechanism of action of infliximab?

A

Neutralizes free, membrane and receptor-bound TNF-a → antibody-dependent cell-mediated cytotoxicity (ADCC)

23
Q

What other conditions is the infliximab used for?

A

-Used for the treatment of Crohn’s disease, ulcerative colitis, plaque psoriasis, ankylosing spondylitis

24
Q

How is the infliximab adminstered?

A
  • IV infusion 3mg kg of bodyweight

- repeated every 2 weeks and 6 weeks after the first infusion then every 8 weeks

25
Q

Describe the mechanism of action of Etanercept?

A
  • Soluble TNF receptor dimer

- Binds free and membrane-bound TNF reducing the accessible TNF in RA → ADCC

26
Q

What other conditions etanercept is used for?

A

-used for the treatment of juvenile idiopathic arthritis, plaque psoriasis, psoriatic arthritis, ankylosing spondylitis

27
Q

Describe what certolizumab is?

A

PEGylated Fab’ fragment of humanized anti-TNF-a mAb – no Fc portion

28
Q

What is certolizumab used for?

A

Crohn’s disease

29
Q

What are the consideration for the anti TNF therapy?

A

Screenied for: tuberculosis (TB), multiple sclerosis, recurrent infection, leg ulcers, heart failure and a past history of cancer

  • Live vaccination: against yellow fever, live polio should be avoided
  • Anti-TNF therapy can be administered for as long as required
30
Q

What are some of the reasons for the precluding the use of anti-TNF medications?

A
  • an inadequate clinical response
  • Lose their responsiveness over time
  • Experience unacceptable side effects
  • Have medical issues
31
Q

Describe the mechanism of action of rituximab?

A
  • Partially humanised anti CD20mAb
  • Rituximab opsonized B-cells are attacked and killed by three mechanisms:

1)Complement mediated cytotoxicity

2-3) Antibody-dependent cell mediated cytotoxicity (ADCC) – FcgR/ CR mediated opsonic phagocytosis

4) Apoptosis

32
Q

What is abatcept ?

A

-The T cell co-stimulation inhibitor

33
Q

Describe the mechanism of action of abatcept?

A
  • Competitive inhibitor of CD28
  • Increases threshold for T-cell activation
  • Suppresses the proliferation of synovial recirculating T cells
  • Reduces the level of inflammatory mediators
34
Q

What is Tociluzimab and what conditions is it used for?

A
  • The IL-6 inhibitor
  • Humanized anti-IL-6 receptor monoclonal antibody
  • Systemic juvenile idiopathic arthiritis
35
Q

What is anakinara?

A

Recombinant IL-1 receptor antagonist

36
Q

How does the anakinara differ from the native human IL-1RA?

A

-Differs from native human IL-1ra: it has the addition of a single methionine residue at its amino terminus

37
Q

What is the fucntion of ankinra in RA?

A

-Reduces bone erosion
-Decreases osteoclast production
-Blocks IL-1 induced MMP release
from synovial cells

38
Q

what are the possible adverse effects of the biologic therapy?

A

-Increased risk of infections:
Upper respiratory tract infections (nasopharyngitis)
Pneumonia
-Urinary tract infections

  • Nausea
  • Headache
  • Hypertension
  • Allergic reactions

BSMS 204- Theme 1 (21 decks)

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