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CLIN PHARM > II - Immunosuppressants > Flashcards

II - Immunosuppressants Flashcards

1
Q

Glucocorticoids

A

Prednisone
Prednisilone
Dexamethasone

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2
Q

Calcineurin inhibitors

A

Cyclosporine
Tacrolimus

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3
Q

Janus kinase inhibitor

A

Apoquel
Oclacitinib

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4
Q

Caninized monoclonal antibody against IL-31

A

Cytopoint

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5
Q

Antimetabolite

A

Azathioprene

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6
Q

Alkylating agents

A

Cyclophosphamide
Chlorambucil

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7
Q

2nd/3rd line/new

A

Mycophenolate mofetil

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8
Q

Antihistamine

A

Diphenhydramine

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9
Q

What are the goals of immunosuppressant therapy?

A
  1. Decrease inflammation
  2. Modulate/suppress lymphocyte function
  3. Minimize adverse drug effects
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10
Q

What drugs are the first line of treatment in dogs and cats for inflammatory and immune-mediated disease?

A

Glucocorticoids
- prednisone
- prednisilone
- dexamethasone

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11
Q

What bloodwork changes are seen with glucocorticoid administration?

A

Increase: erythrocytes, platelets, neutrophils (EPN)

Decrease: eosinophils, macrophages, T-lymphocytes (EMT)

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12
Q

Low doses of glucocorticoids are ____________ and high doses are ____________.

A

Anti-inflammatory

Immunosuppressive

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13
Q

Glucocorticoids have a systemic impact on ________ and ________ immunity.

A

Innate and adaptive

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14
Q

Glucocorticoids inhibit release of ______, which decreases recruitment of inflammatory cells.

A

Cell adhesion molecules

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15
Q

Glucocorticoids prevent release of:

A

Cytokines: IL-1, IL-2, TNFa
Histamine
Serotonin
Lysosomal enzymes

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16
Q

Which glucocorticoids are shorter acting?

A

Prednisone and prednisilone

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17
Q

8 side effects of glucocorticoids

A

GI ulceration
Iatrogenic hyperadrenocorticism
Adrenal gland suppression
Insulin resistance and secondary diabetes mellitus
Muscle catabolism
Delayed wound healing
Opportunistic infections
Behavior changes

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18
Q

________ is a prodrug metabolized to ________ and used in dogs.

A

Prednisone, prednisilone

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19
Q

Which shorter acting glucocorticoid has better bioavailability in cats?

A

Prednisilone

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20
Q

Which glucocorticoid lacks mineralocorticoid activity (minimizing sodium and water retention) and is better for patients with underlying cardiovascular disease or diseases associated with fluid retention (hypoalbuminemia, portal hypertension)?

A

Dexamethasone

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21
Q

What drugs are the first line of treatment for perianal fistulas and keratoconjunctivitis?

A

Calcineurin inhibitors
- cyclosporine
- Tacrolimus

22
Q

What drug is a substrate of the cytochrome P450 enzyme CYP3A?

A

Cyclosporine

23
Q

What are two drugs that interact with Calcineurin inhibitors to decrease efficacy?

A

Azole antifungals
phenobarbital (cats)

24
Q

Which immunosuppressant has a narrow therapeutic window?

A

Calcineurin inhibitor
- cyclosporine

25
Q

Which immunosuppressant drug has a patient response that is difficult to predict (due to individual gastric contents, liver function, other meds)?

A

Calcineurin inhibitor
- cyclosporine

26
Q

With which immunosuppressant drug should generic/compounded formulas especially be avoided?

A

Calcineurin inhibitor
- cyclosporine

27
Q

__________ are frequently used as add-on drugs for IMHA and IBD.

A

Calcineurin inhibitors
- cyclosporine
- Tacrolimus

28
Q

5 side effects of Calcineurin inhibitors

A
  • Self-limiting GI upset; can give maropitant or frozen

Immunosuppressive
Gingival hyperplasia
Hepatotoxicity
Thromboembolism

29
Q

MOA: Binds to a cytoplasmic receptor protein; the complex then binds and inhibits Calcineurin, decreasing expression of IL-2 and other cytokines necessary for T-cell activation.

A

Calcineurin inhibitors
- cyclosporine
- Tacrolimus

30
Q

MOA: Inhibits activity of pro-inflammatory cytokines (IL-1, 4, 6, 13, 31)

A

Janus kinase inhibitor
- Apoquel (Oclacitinib)

31
Q

First choice drugs for fast relief of hypersensitivity-induced cutaneous pruritis.

A

Janus kinase inhibitor
- Apoquel
- Oclacitinib

32
Q

Side effects of these immunosuppressants include vomiting, diarrhea, lethargy, anorexia, and bloodwork changes.

A

Janus kinase inhibitors
- Apoquel
- Oclacitinib

33
Q

What populations of dogs should not use Apoquel?

A
  • severe infection
  • breeding/pregnant/lactating
34
Q

Is it ok to use Janus kinase inhibitors with vaccines, nsaids, and allergy shots?

A

Yes

35
Q

What drug is used to manage allergic pruritic flares?
How long does it last?

A

Cytopoint
4-8 weeks

36
Q

MOA: Interferes with incorporation of purines/pyrimidines into DNA; prodrug metabolized to a purine analog (6-Mercapto purine); decreases synthesis of WBC

A

Antimetabolites
- azathioprene

37
Q

What drug is used to treat IBD, IMHA, or to decrease dose of glucocorticoids?

A

Antimetabolites
- azathioprene

38
Q

Toxicities for this drug include bone marrow suppression, hepatotoxicity, and GI

A

Antimetabolites
- Azathioprene

39
Q

Efficacy of this immunosuppressant is delayed for days to weeks, so should be used in conjunction with another drug initially.

A

Antimetabolites
- Azathioprene

40
Q

Where is Azathioprene oxidized?

A

In the liver and peripheral tissues via TPMT to an inactive metabolite

41
Q

This drug is oxidized by TPMT, which increases risk for suppression of bone marrow (due to decreased TPMT).

A

Antimetabolites
- Azathioprene

42
Q

Azathioprene is contraindicated in which species?

A

Cats and horses

43
Q

MOA: Alkylates DNA causing chemical cross-links to occur - interfering with DNA replication

A

Alkylating agents
- cyclophosphamide
- Chlorambucil

44
Q

High doses of alkylating agents deplete ______.

A

T-cells

45
Q

Low doses of alkylating agents enhance _______.

A

T-cell memory

46
Q

This drug is used in cats in lieu of azathioprene.

A

Chlorambucil

47
Q

Side effects of this drug include sterile hemorrhagic cystitis.

A

Cyclophosphamide

*prednisone/furosemide to ensure frequent urination
*monitor for Hematuria

48
Q

This drug is used in cats as a second line of treatment for IBD and for those who do not respond to prednisilone.

A

Chlorambucil (Alkylating agent)

49
Q

MOA: Mycophenolic acid inhibits the type II isoform of inosine-5’-monophosphate dehydrogenase; this enzyme is present in abundance in activated lymphocytes and is critical for the synthesis of guanosine nucleotides.

A

Mycophenolate mofetil

50
Q

Indications for this drug include treatment of dogs for:

  • IMHA
  • IMPT
  • IMPA
  • IM skin disease
  • IM glomerulonephritis
  • myasthenia gravis
  • meningoencephalomyelitis
A

Mycophenolate mofetil

51
Q

Side effects/cautions for Mycophenolate mofetil

A

GI upset
Avoid use in pregnant patients (+ risk to owner)
Increased susceptibility to infection/neoplasia
Allergic reactions

52
Q

MOA: inverse agonist (H1) - reverses effects of histamine on capillaries reducing allergic reaction symptoms

A

Antihistamines
- diphenhydramine

CLIN PHARM (13 decks)

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