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Pharmacology > 04 Drugs affecting the immune response > Flashcards

04 Drugs affecting the immune response Flashcards

1
Q

4.01 CALCINEURIN INHIBITORS

Immunosuppressants: ciclosporin, tacrolimus, pimecrolimus - actions

A

binding to cytosolic immunophilins to form a complex that inhibits calcineurin
this reduces activation and proliferation of T cells and production of cytokines

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2
Q

4.01 CALCINEURIN INHIBITORS

Immunosuppressants: ciclosporin, tacrolimus, pimecrolimus - MOA

A

inhibition of the calcium-dependent phosphatase, calcineurin, which normally activates the transcription of interleukin-2 (IL-2)

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3
Q

4.01 CALCINEURIN INHIBITORS

Immunosuppressants: ciclosporin, tacrolimus, pimecrolimus - abs/distrib/elim

A

ciclosporin and tacrolimus can be given orally or by IV infusion, and they are metabolised in the liver by the P450 3A enzyme system
topical formulations of tacrolimus and pimecrolimus have low systemic absorption

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4
Q

4.01 CALCINEURIN INHIBITORS

Immunosuppressants: ciclosporin, tacrolimus, pimecrolimus - clinical use

A

used to prevent rejection of organ and tissue transplants and for prevention of graft v host disease
can be useful in autoimmune diseases
topical use for atopic dermatitis (tacrolimus or pimecrolimus)

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5
Q

4.01 CALCINEURIN INHIBITORS

Immunosuppressants: ciclosporin, tacrolimus, pimecrolimus - adverse effects

A

myelosuppression and risk of infection
nephrotoxicity
can cause hypertension, hepatotoxicity, tremor, paraesthesia

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6
Q

4.02 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Azathioprine - actions

A

reduces the clonal proliferation of T and B cells during the induction phase of the immune response

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7
Q

4.02 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Azathioprine - MOA

A

interferes with purine synthesis and has cytotoxic action on dividing cells

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8
Q

4.02 ANTIPROFILERATIVE IMMUNOSUPPRESSANT

Azathioprine - abs/distrib/elim

A

given orally or by IV infusion
metabolised to mercaptopurine, which is the cytotoxic moiety acting by interfering with purine nucleotide metabolism
mercaptopurine is inactivated by xanthine oxidase

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9
Q

4.02 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Azathioprine - clinical use

A

used to prevent rejection of organ and tissue transplants and for prevention of graft v host disease
also used in chronic inflammatory and autoimmune diseases (e.g. rheumatoid arthritis, inflammatory bowel disease)

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10
Q

4.02 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Azathioprine - adverse effects

A

myelotoxicity (dose-related - monitoring is required)
GIT disturbances, hypersensitivity reactions (skin rashes, arthralgia, etc.)

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11
Q

4.03 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Mycophenolate mofetil - actions

A

selectively restrains the clonal proliferation of T and B cells and reduces the production of cytotoxic T cells

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12
Q

4.03 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Mycophenolate mofetil - MOA

A

selectively inhibits inosine monophosphate dehydrogenase which is responsible for de novo purine synthesis specifically in T and B lymphocytes (other cells can generate purines by another pathway)

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13
Q

4.03 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Mycophenolate mofetil - abs/distrib/elim

A

given orally or by IV infusion
metabolised to mycophenolic acid which is the active moiety

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14
Q

4.03 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Mycophenolate mofetil - clinical use

A

used to prevent rejection of organ transplants, usually in combination with ciclosporin and glucocorticoids
also used in a wider range of autoimmune diseases (e.g. lupus, vasculitis)

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15
Q

4.03 ANTIPROLIFERATIVE IMMUNOSUPPRESSANT

Mycophenolate mofetil - adverse effects

A

GIT, CVS and respiratory system disturbances
hepatitis
pancreatitis
tremor
dizziness
flu-like syndrome

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16
Q

4.04 ANTIPROLIFERATIVE ANTIBIOTIC

Sirolimus (rapamycin) - actions

A

inhibits the clonal proliferation of T and (more particularly) B cells
decreases immunoglobulin production

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17
Q

4.04 ANTIPROFILERATIVE ANTIBIOTIC

Sirolimus (rapamycin) - MOA

A

blocks the response of precursor cells to interleukin-2 (IL-2) - by binding a cytosolic protein FK-binding protein 12 to form a complex that inhibits activation of mammalian target of rapamycin (mTOR) kinase - and thus suppressing activation of T and B cells

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18
Q

4.04 ANTIPROLIFERATIVE ANTIBIOTIC

Sirolimus (rapamycin) - abs/distrib/elim

A

given orally
metabolised by P450 3A in the liver - therefore many drug interactions

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19
Q

4.04 ANTIPROLIFERATIVE ANTIBIOTIC

Sirolimus (rapamycin) - clinical use

A

used to prevent rejection of organ transplants (particularly renal because, unlike ciclosporin, it has no renal toxicity) usually in combination with ciclosporin or glucocorticoids

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20
Q

4.04 ANTIPROLIFERATIVE ANTIBIOTIC

Sirolimus (rapamycin) - adverse effects

A

myelosuppression (important)
hyperlipidaemia
venous thromboembolism
diarrhoea
rash
osteonecrosis

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21
Q

4.05 GLUCOCORTICOIDS

Prednisolone, dexamethasone, hydrocortisone, triamcinolone - actions

A

inhibits clonal proliferation of T and B cells and macrophage activation
(other actions: reduction in chronic inflammation, autoimmune and hypersensitivity reactions, various metabolic effects, negative feedback action on anterior pituitary and hypothalamus)

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22
Q

4.05 GLUCOCORTICOIDS

Prednisolone, dexamethasone, hydrocortisone, triamcinolone - MOA

A

glucocorticoids (GCs) interact with intracellular receptors to inhibit the transcription of specific genes that code for various cytokines esp. IL-2

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23
Q

4.05 GLUCOCORTICOIDS

Prednisolone, dexamethasone, hydrocortisone, triamcinolone - abs/distrib/elim

A

given orally or by injection or topically
the main effects occur only after 2-8h because protein synthesis of mediators and enzymes is required

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24
Q

4.05 GLUCOCORTICOIDS

Prednisolone, dexamethasone, hydrocortisone, triamcinolone - clinical use

A

to prevent rejection of organ transplants and to treat rejection episodes
also used for a wide range of inflammatory, hypersensitivity and autoimmune conditions

25
Q

4.05 GLUCOCORTICOIDS

Prednisolone, dexamethasone, hydrocortisone, triamcinolone - adverse effects

A

used long term it causes:
suppression of response to infection
suppression of endogenous GC synthesis
osteoporosis
growth suppression in children
iatrogenic Cushing’s syndrome

26
Q

4.06 TNF INHIBITORS

Infliximab, adalimumab, etanercept, golimumab - actions

A

wide-ranging immunosuppressant effects

27
Q

4.06 TNF INHIBITORS

Infliximab, adalimumab, etanercept, golimumab - MOA

A

monoclonal antibody against tumour necrosis factor (TNF)-α that binds with the TNF-α and prevents its interaction with cell surface receptors in inflammatory cells

28
Q

4.06 TNF INHIBITORS

Infliximab, adalimumab, etanercept, golimumab - abs/distrib/elim

A

given IV or SC
etanercept is given twice a week, whereas the frequency of injection for the others varies from 4-8 weeks

29
Q

4.06 TNF INHIBITORS

Infliximab, adalimumab, etanercept, golimumab - clinical use

A

rheumatoid arthritis
inflammatory bowel disease
psoriasis
ankylosing spondylitis

30
Q

4.06 TNF INHIBITORS

Infliximab, adalimumab, etanercept, golimumab - adverse effects

A

nausea, vomiting
headache
upper respiratory tract infections
because of inactivation of macrophages, latent TB and other serious infections may recur
blood dyscrasias

31
Q

4.07 ANTIBODIES AGAINST CD20

Rituximab, ofatumumab, ocrelizumab - actions

A

immunosuppressant
antineoplastic

32
Q

4.07 ANTIBODIES AGAINST CD20

Rituximab, ofatumumab, ocrelizumab - MOA

A

binding to CD20 antigen on B lymphocytes results in cell lysis and apoptosis

33
Q

4.07 ANTIBODIES AGAINST CD20

Rituximab, ofatumumab, ocrelizumab - abs/distrib/elim

A

given IV

34
Q

4.07 ANTIBODIES AGAINST CD20

Rituximab, ofatumumab, ocrelizumab - clinical use

A

rituximab or ofatumumab - lymphoma and leukaemia
rituximab is widely used for rheumatoid arthritis and vasculitis
ocrelizumab - multiple sclerosis

35
Q

4.07 ANTIBODIES AGAINST CD20

Rituximab, ofatumumab, ocrelizumab - adverse effects

A

neutropenia
infections

36
Q

4.08 MONOCLONAL ANTIBODIES (NON-CD20)

Alemtuzumab

A

drug target - CD52 antigen
MS and haematological malignancies

37
Q

4.08 MONOCLONAL ANTIBODIES (NON-CD20)

Brentuximab

A

drug target - CD30 antigen
used in lymphoma

38
Q

4.08 MONOCLONAL ANTIBODIES (NON-CD20)

Belimumab

A

drug target - B-lymphocyte stimulator protein
used for lupus erythematosus

39
Q

4.08 MONOCLONAL ANTIBODIES (NON-CD20)

Vedolizumab, natalizumab

A

drug target - α4 integrin
vedolizumab is directed at T-helper lymphocytes that home in on the gut and is used in inflammatory bowel disease
natalizumab is used in MS

40
Q

4.09 INTERLEUKIN INHIBITORS

Anakinra

A

drug target - IL-1
used for rheumatoid arthritis

41
Q

4.09 INTERLEUKIN INHIBITORS

Tocilizumab

A

drug target - IL-6
used for rheumatoid arthritis and giant cell arteritis

42
Q

4.09 INTERLEUKIN INHIBITORS

Secukinumab

A

drug target - IL-17
used for psoriasis, psoriatic arthritis and ankylosing spondylitis

43
Q

4.09 INTERLEUKIN INHIBITORS

Ustekinumab

A

drug target - IL-12 and 23
used for psoriasis, psoriatic arthritis and Crohn’s disease

44
Q

4.10 JAK

Monoclonal antibodies targeting JAK: tofacitinib, baricitinib - actions

A

attenuates immune and inflammatory response

45
Q

4.10 JAK

Monoclonal antibodies targeting JAK: tofacitinib, baricitinib - MOA

A

inhibits Janus kinase (JAK) and interrupts intracellular signalling involved in cytokine and interferon release

46
Q

4.10 JAK

Monoclonal antibodies targeting JAK: tofacitinib, baricitinib - abs/distrib/elim

A

given orally
good bioavailability
metabolised mainly by CYP3A4

47
Q

4.10 JAK

Monoclonal antibodies targeting JAK: tofacitinib, baricitinib - clinical use

A

mainly in rheumatoid arthritis
tofacitinib may be used for psoriatic arthritis and ulcerative colitis

48
Q

4.10 JAK

Monoclonal antibodies targeting JAK: tofacitinib, baricitinib - adverse effects

A

serious infections
nausea
upper respiratory tract symptoms

49
Q

4.11 NON-SEDATING ANTIHISTAMINES

Cetirizine, loratadine, fexofenadine, azelastine - actions

A

inhibits H1 receptor actions and thus reduces immediate hypersensitivity reactions

50
Q

4.11 NON-SEDATING ANTIHISTAMINES

Cetirizine, loratadine, fexofenadine, azelastine - MOA

A

competitive inhibitor of histamine at H1 receptors on smooth muscle

51
Q

4.11 NON-SEDATING ANTIHISTAMINES

Cetirizine, loratadine, fexofenadine, azelastine - abs/distrib/elim

A

given orally, well absorbed
metabolised in the liver
excreted in the urine
does not cross the blood-brain barrier, so no sedative adverse effect

52
Q

4.11 NON-SEDATING ANTIHISTAMINES

Cetirizine, loratadine, fexofenadine, azelastine - clinical use

A

hypersensitivity reactions: hay fever, urticaria, some drug allergies, insect bites, pruritus

53
Q

4.11 NON-SEDATING ANTIHISTAMINES

Cetirizine, loratadine, fexofenadine, azelastine - adverse effects

A

effects due to action on peripheral muscarinic receptors (dry mouth, sometimes blurred vision, constipation, urine retention)

54
Q

4.12 SEDATING ANTIHISTAMINES

Promethazine, cyclizine, cinnarizine, chlorphenamine, etc. - actions

A

inhibits H1 receptor actions and thus reduces immediate hypersensitivity reactions
has anticholinergic action, some local anaesthetic action, weak α-adrenoceptor antagonism and fairly marked sedative effect
CNS effects on the vestibular nuclei and vomiting centre

55
Q

4.12 SEDATING ANTIHISTAMINES

Promethazine, cyclizine, cinnarizine, chlorphenamine, etc. - MOA

A

competitive inhibitor of histamine at H1 receptors on smooth muscle, CNS, etc.

56
Q

4.12 SEDATING ANTIHISTAMINES

Promethazine, cyclizine, cinnarizine, chlorphenamine, etc. - abs/distrib/elim

A

given orally or by injection
enters the CNS

57
Q

4.12 SEDATING ANTIHISTAMINES

Promethazine, cyclizine, cinnarizine, chlorphenamine, etc. - clinical use

A

chlorphenamine, hydroxyzine: hypersensitivity reactions (hay fever, urticaria), premedication, sedation, emergency treatment of anaphylaxis
promethazine, cyclizine, cinnarizine: nausea and vomiting, motion sickness

58
Q

4.12 SEDATING ANTIHISTAMINES

Promethazine, cyclizine, cinnarizine, chlorphenamine, etc. - adverse effects

A

anticholinergic action on peripheral muscarinic receptors (dry mouth, sometimes blurred vision, constipation, urine retention)
headache
drowsiness

59
Q

4.13 What antihistamines are used for motion sickness?

A

antihistamines: promethazine, cyclizine, cinnarizine
hyoscine - a muscarinic antagonist, given orally or by transdermal patch

Pharmacology (34 decks)

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