Lecture 13: Immune System Drugs (RED ONLY) Flashcards

1
Q

What are the 3 main drug classes with immune effects?

A

Glucorticoids
Immunomodulators
Biologics

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2
Q

What are the 3 S?

A

Sugar (glucocorticoids)

Salt (mineralcorticoids)

Sex (Androgens)

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3
Q

What are the main 3 glucocorticoids?

A

Hydrocortisone (main?)
Cortisone
Prednisolone

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4
Q

What is the main hormone in the mineralcorticoids?

A

Aldosterone

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5
Q

What is the main hormone in the androgens?

A

Testosterone

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6
Q

What are the effects of GCs?

A

Widespread effects on carb, protein, and lipid metabolism, and electrolyte/water balance.

Excess = insomnia/euphoria followed by depression, aka steroid psychosis.

Deficiency = Depression

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7
Q

What is the MOA of a GC’s antinflammatory/immune effects?

A

Inhibits production of precursors to prostaglandins, leukotrienes, and PAF.

Suppresses inflammatory cytokines, chemokines, and other inflammatory mediators.

Inhibits macrophages and other APCs

Reduces synthesis of arachidonic acid, which leads to reduction of COX 2, reducing prostaglandins.

Reduces antibody production in large doses.

Note:
NSAIDs are also COX inhibitors.

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8
Q

Which GC is often prescribed as a cream and has similar anti-inflammatory effects and mineralcorticoid activity?

A

Hydrocortisone

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9
Q

What is the MOA of methotrexate?

A

Binds and inhibits dihydrofolate reductase (DHFR)

Inhibiting tetrahydrofolate synthesis (THF)

Inhibiting synthesis of purine nucleotides and amino acids

Interfering with the formation of DNA, RNA, and cellular proteins

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10
Q

What nucleic acids is leflunomide an analog for?

A

Pyrimidine

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11
Q

What nucleic acids is azathioprine an analog for?

A

Purine

Note:
Prine purine

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12
Q

What are the indications for MTX?

A

RA, psoriasis, several types of cancer.

Off-label use in Crohn’s disease, MS, SLE, and multiple conditions.

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13
Q

What are the indications for leflunomide?

A

RA. PO administration only

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14
Q

What are the indications for azathioprine?

A

RA, MS, psoriasis, Crohn’s disease, and transplant maintenance.

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15
Q

What is the MOA of tacrolimus and cyclosporine?

A

Inhibiting T-lymphocyte activation.

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16
Q

What is the tolerability of cyclosporine?

A

Gingival hyperplasia
Hirsutism

17
Q

What are the indications for the calcineurin inhibitors?

A

Transplant maintenance
RA
Psoriasis

18
Q

What is the MOA of the mTOR kinase inhibitors?

A

Inhibiting T-lymphocyte activation & proliferation.
Synergy with calcineurin inhibitors.

19
Q

What is the indication for the mTOR kinase inhibitors?

A

Cancer, Organ transplantation, complications of TB.

20
Q

What is the MOA for mycophenolate?

A

Inhibits T and B cell proliferation by inhibiting major enzyme involved in nucleotide synthesis.

21
Q

What are the indications for mycophenolate?

A

Transplant maintenance, lupus nephritis, autoimmune hepatitis, and myasthenia gravis.

22
Q

What is the MOA for sulfasalazine?

A

5-aminosalicyclic acid derivative. Immune modulator with an unknown mechanism.

23
Q

What are the indications for sulfasalazine?

A

RA, and ulcerative colitis

24
Q

What is the MOA for hydroxychloroquine?

A

Antimalarial drug with immune modulating factors (inhibits neutrophil and eosinophil motility and impairs complement antibody reactions)

25
Q

What are the indications for hydroxychloroquine?

A

RA
SLE
Malaria

26
Q

What is the MOA of fingolimod?

A

Binds sphingosine receptors and blocks lymphocytes from leaving lymph nodes

27
Q

What are the indications for fingolimod?

A

MS

28
Q

What is the MOA for glatiramer?

A

Not well defined.

Mixture of polymers that roughly mimics basic myelin protein; it is thought to activate T suppressor cells.

29
Q

What are the indications for Glatiramer?

A

MS (Preferred in pregnancy)

30
Q

What are the two Anti-TNFs?

A

Etanercept (Enbrel)
Adalimumab (Humira)

31
Q

What are the indications for etanercept and adalimumab?

A

RA, psoriasis, Crohn’s disease, and more.

32
Q

What are the two anti-CD80/86 drugs?

A

Belatacept
Abatacept

33
Q

What are the indications for Belatacept and Abatacept?

A

Transplant (belatacept)

RA, psoriasis (Abatacept)

34
Q

What is Rituximab and its use?

A

Anti-CD20 indicated for RA, chronic lymphocytic leukemia, and non-hodgkin lymphomas.

35
Q

What should you always double check when prescribing an immune system drug?

A

Pregnancy
Live vaccine candidacy
Drug and disease interactions
Dose adjustments

36
Q

What should you always do with GCs?

A

Taper down high or long doses to avoid adrenal insufficiency.

37
Q

What cancers is MTX for?

A

Lungs, liver, kidneys, bone marrow

38
Q

What should you always give with MTX and sulfasalazine?

A

Folic acid

39
Q

What should you always do when prescribing a biologic?

A

Parenteral only.
Screen for TB before use.
Avoid live vaccines.
Refrigerate
Don’t combine them!