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Pharma 2nd semester > B. 30- immunopharmacology 2. inhibitors of cytokine gene expression, 5-ASA derivatives > Flashcards

B. 30- immunopharmacology 2. inhibitors of cytokine gene expression, 5-ASA derivatives Flashcards

1
Q

examples for 5-Aminosalicylate (5-ASA)

A

mesalazine

sulfasalzine

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2
Q

what is the mechanism of 5-Aminosalicylate (5-ASA): sulfasalzine

A

PPARᵧ agonist–> ↓ NFᴋB, TLR’S
↓ cytokine expression
COX & LOX inhibition
antioxidant role

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3
Q

how is 5-ASA’S given?

A

oral, parenteral (suppository)

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4
Q

what are the indications for 5-ASA’s? (sulfasalazine)

A

autoimmune diseaes

IBD: UC&raquo_space;CD

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5
Q

SE of sulfasalazine?

A

nausea
vomiting
headache
rash

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6
Q

characteristic of sulfasalazine and mesalazine

A

prodrug converted by colon bacteria into 5-ASA

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7
Q

what are chloroquine and hydroxychloroquine ?

A

anti-malarial drugs

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8
Q

mechanism of chloroquine and hydroxychloroquine

A

interfere with macrophages lysosomal pH–> inhibit antigen catabolism and presentation

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9
Q

how is chloroquine and thalidomide given?

A

oral

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10
Q

when is chloroquine given?

A

autoimmune diseases (RA, SLE)

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11
Q

SE of chloroquine and hydroxychloroquine

A

skin exanthema
GI irritation
ocular damage
hemolysis in patients with G6PD

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12
Q

does chloroquine have a long or short T1/2?

A

long

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13
Q

mechanism of thalidomide

A

suppression of TNF-𝝰, ↑ IL-10,
↓ neutrophil phagocytosis
altered adhesion molecule expression
↑ cell-mediated immunity

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14
Q

when do we give thalidomide?

A 
autoimmune diseases (SLE) 
solid tumors
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15
Q

SE from thalidomide

A

peripheral neuropathy
neutropenia
teratogenic

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16
Q

for what is Glatiramer acetate given?

A

multiple sclerosis

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17
Q

how is glatiramer acetate given?

A

parenteral

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18
Q

SE of glatiramer acetate

A

injection site reaction

19
Q

what does glatiramer acetate consist of?

A

a mixture of synthetic polypeptides and 4 amino acids

20
Q

what are calcineurin inhibitors?

A

calcium and calmodulin-dependent serine/ threonine protein phosphatase
*plays a role in the activation of T cells

21
Q

give 2 calcineurin inhibitors

A

cyclosporine

tacrolimus (FK506)

22
Q

how are cyclosporine and tacrolimus given?

A

oral or parenteral

23
Q

major side effect of both cyclosporine and tacrolimus?

A

nephrotoxicity

24
Q

mechanism of cyclosporine

A

binds to cyclophilin–> inhibits calcineurin–> alters activation of T cell transcription factors–> IL-2, IL-3, IFN-ᵧ ↓

25
Q

mechanism of tacrolimus

A

binds to FK-binding protein–> inhibits calcineurin–> alters activation of T cell transcription factors–> IL-2, IL-3, IFN-ᵧ ↓

26
Q

1st line agent for bone marrow transplantation

A

cyclosporine

27
Q

what do cyclosporine and tacrolimus eventually do?

A

IL-2, IL-3, IFN-ᵧ ↓

28
Q

indications for cyclosporine

A

bone marrow transplantation (1st line agent)
solid-organ transplantation
autoimmune diseases ( RA, psoriasis, uveitis)

29
Q

indications for tacrolimus

A 
solid-organ transplantation 
autoimmune diseases 
atopic dermatitis (topical)
30
Q

type of metabolism in cyclosporine and sirolimus

A

hepatic P450 metabolism

31
Q

does cyclosporine have long or short T1/2?

A

long

32
Q

side effects of cyclosporine

A

nephrotoxicity
hepatotoxicity
hypertension
gingival hypertrophy

33
Q

what is sirolimus (rapamycin)?

A

mTOR inhibitor

34
Q

what is an mTOR inhibitor?

A

inhibits mTOR which is a key regulator of an intracellular signaling pathway, involved in cell growth, proliferation angiogenesis, metabolism

35
Q

mechanism of sirolimus

A

binds to FK-binding protein–> inhibits the kinase activity of mTOR

36
Q

how is sirolimus given?

A

oral or parenteral

37
Q

what is the T1/2 of sirolimus?

A

up to 60 h’

38
Q

indications of sirolimus

A

neuroendocrine tumors
breast and renal cancer
solid-organ transplantation
sirolimus-eluting stents to prevent restenosis after coronary angioplasty

39
Q

side effects of sirolimus

A

myelosupression
hepatotoxicity
pneumonitis

40
Q

what is Tofacitinib?

A

inhibitor of JAK1 and JAK3

41
Q

how is tofacitinib given?

A

orally

42
Q

indications for tofacitinib

A 
autoimmune disease (RA, IBD, ankylosing spondylitis)
monotherapy or in combination  with methotrexate
43
Q

side effects of tofacitinib

A

“Hil”:
hyperlipidemia
infections
elevated liver enzymes

44
Q

what is a JAK inhibitor

A

JAK is an intracellular tyrosine kinase–> JAK-STAT pathway that transmits cytokine-mediated signals

Pharma 2nd semester (49 decks)

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