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MODA > Immunosuppression: drugs > Flashcards

Immunosuppression: drugs Flashcards

1
Q

Short-acting corticosteroids

A

Hydrocortisone (cortisol, the natural corticosteroid) Prednisone, prednisolone

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2
Q

Triamcinolone

A

Medium-term action corticosteroid (24-48h)

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3
Q

Dexamethasone

A

Longer-term action corticosteroid (>48hrs)

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4
Q

Prednisone

A

Short acting corticosteroid. (<24hrs)

Prodrug, metabolised to prednisolone

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5
Q

Prednisolone

A

Short acting corticosteroid

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6
Q

Infliximab

Uses?

A

Monoclonal antibody, binds (sequesters) TNF-alpha

Crohn’s disease, Rheumatoid arthritis

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7
Q

Adalimumab

Uses?

A

Monoclonal antibody, binds (sequesters) TNF-alpha

Crohn’s disease, Rheumatoid arthritis

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8
Q

Etanercept

A

Binds (sequesters) TNF-alpha, not strictly a monoclonal antibody
An artificial construct of the receptor for TNF-alpha fused to an antibody Fc domain

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9
Q

Omalizumab

Uses?

A

Monoclonal antibody, binds IgE

IgE-mediated asthma

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10
Q

Alemtuzamab

Uses?

A

Monoclonal antibody
Binds CD52 leading to destruction of B and T cells by cell-based immunity.
Thus acquired immunity is ‘reset’ to a naive state. Patients still have functioning innate immune system, do not suffer hugely increased rate of infection.

B-cell chronic lymphocytic leukaemia (CLL)
Multiple sclerosis (still in trials)
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11
Q

Zileuton

A

Inhibitor of 5-lipoxygenase
(inhibits production of leukotrienes)

Treatment of asthma, other respiratory diseases e.g COPD

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12
Q

Zafirlukast

A

Leukotriene D4 and E4 receptor antagonist

Treatment of asthma, other respiratory diseases e.g COPD

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13
Q

Cromolyn sodium

A

Inhibits release of inflammatory mediators from mast cells

Treatment of asthma, other respiratory diseases e.g COPD

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14
Q

Salbutamol

A

B2 selective adrenergic agonist
(Bronchodilator, also inhibits release of inflammatory mediators from mast cells)
Short acting

Treatment of asthma, other respiratory diseases e.g COPD

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15
Q

Salmeterol

A

B2 selective adrenergic agonist
(Bronchodilator, also inhibits release of inflammatory mediators from mast cells)
Longer acting than salbutamol

Treatment of asthma, other respiratory diseases e.g COPD

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16
Q

Ipratropium

A

Muscarinic antagonist.

Asthma, also used in COPD

17
Q

Theophylline

A

Phosphodiesterase inhibitor
A methylxanthine

Treatment of asthma, other respiratory diseases e.g COPD. Causes direct bronchodilation.
Inhibits degranulation of mast cells

18
Q

Drugs used to treat rheumatoid arthritis

A

NSAIDS
Disease modifying anti-rheumatoid drugs (DMARDS)
- Methotrexate
- gold compounds
- Sulfasalazine,
- Penicillamine
- Chloroquine
Glucocorticoids: may be used systemically or topically
Antibodies against cytokines e.g Infliximab, Adalimumab against TNF-α

19
Q

Methotrexate

A

Inhibits folic acid synthesis

20
Q

Sulfasalazine

A

Interferes with lymphocytes

21
Q

Penicilllamine

A

Metabolite of penicillin

Inhibits T lymphocyte proliferation

22
Q

Chloroquine

A

Inhibits T lymphocyte proliferation.

Also antimalarial

23
Q

Transplantation and immunosuppression

A

Systemic corticosteroids: effective but long term treatment with high doses necessary to prevent rejection - NB side effects.

Cyclophosphamide
Alemtuzumab
Cyclosporin, Tacrolimus
Sirolimus (rapamycin)
Basiliximab
Azathioprine, mycophenolate
24
Q

Cyclophosphamide

Uses?

A

Alkylates DNA: adds an alkyl group to guanosine, preventing DNA replication- causes apoptosis of rapidly dividing cells.
Inhibits B, T cell proliferation
Prodrug- metabolised in liver to active compound, a nitrogen mustard alkylating agent.

Used for aggressive short term treatment of severe autoimmune diseases, also in cancer chemotherapy

Numerous side effects: hair loss, haemorrhagic cystitis, infertility.

25
Q

Cyclosporin

A

Calcineurin inhibitor
Inhibits secretion of IL2
Inhibits T cell proliferation & mobilisation

26
Q

Tacrolimus

A

Calcineurin inhibitor
Inhibits secretion of IL2
Inhibits T cell proliferation & mobilisation.

27
Q

Sirolimus

A

Inhibits mTOR

Blocks late activation of T and B cells

28
Q

Basiliximab

A

Antibody against IL-2 receptor

Blocks late activation of T cells

29
Q

Azathioprine

A

Inhibits guanosine synthesis, and thus DNA synthesis. Prevents B, T cell proliferation
Effects limited mainly to B, T cells because other cell types possess an alternative salvage pathway for guanosine synthesis.

30
Q

Mycophenolate

A

Inhibits guanosine synthesis, and thus DNA synthesis. Prevents B, T cell proliferation
Effects limited mainly to B, T cells because other cell types possess an alternative salvage pathway for guanosine synthesis.

31
Q

Hydrocortisone

A

= cortisol, the natural corticosteroid.

A glucocorticoid

32
Q

COPD

Treatment

A

Lung disease

  • reduced airflow
  • inflamed airways
  • different inflammatory cell profile to asthma

Treatment:
- cromolyn sodium, zileuton, zafirlukast, salbutamol, salmeterol, ipratropium, theophylline (as asthma)

Inhaled glucocorticoids are NOT effective.
- basis of resistance is unclear
- may relate to high levels of oxidative stress within lungs of COPD patients, many of whom are smokers
oxidation products formed may interfere with normal effects of glucocorticoids.

33
Q

Asthma

Treatment

A

A chronic inflammatory disease affecting the lungs. Characterised by:

  • variable airflow
  • airway hyper-responsiveness to various stimuli
  • episodic bronchoconstriction

Treatment:

  • inhaled glucocorticoids: reduce production of acute inflammatory mediators, & cytokins, homing of T cells to the lungs, prevent dendritic cell maturation
  • cromolyn sodium
  • zileuton, zafirlukast
  • salbutamol, salmeterol
  • ipratropium
  • Theophylline
34
Q

Calcineurin

Inhibitors?

A

A Ca2+ dependent serine-threonine phosphatase.
Dephosphorylates NF-AT (nuclear factor- activated T cells)
Dephosphorylated NF-AT translocated to the nucleus and causes upregulation of IL-2, which is important for T cell proliferation.
Inhibition of calcineurin (e.g cyclosporin, tacrolimus) therefore inhibits mobilisation of T cells.

MODA (27 decks)

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