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Pharm II Test 4 > Immune Modulators > Flashcards

Immune Modulators Flashcards

1
Q

Non-Selective Inhibitors- Available Drugs

A

Adrenocortical Steroids

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2
Q

Adrenocortical Steroids- Mech of Action

A

Compete for NF-kB and other nuclear activators= inhibit gene transcription= decreased pro-inflammatory cytokine production, suppression of antigen presentation, alteration of cell traffic, impaired chemotaxis

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3
Q

Adrenocortical Steroids- Kinetics

A

PO, IV, depo, intraretinal, topical

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4
Q

Adrenocortical Steroids- Toxicities

A 
impaired immune response
osteoporosis
diabetes mellitus
CNS effects (hyperphagia, psychosis)
obesity hypertension
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5
Q

Adrenocortical Steroids- Clinical Use

A

any disease with poorly regulated inflammation: RA, IBD, asthma

timing is important- cytokines peak early in the morning

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6
Q

Anti-proliferative Immunomodulators- Available Drugs

A 
Cyclophophamide-Cytoxan
Azathioprine-Imuran
Methotrexate
Mycopheolate mofetil
Leflunomide
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7
Q

Cyclophosphamide- Cytoxan- Mech of Action

A

alkylating agent activated by the liver, precise site of action on lymphocytes is unknown

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8
Q

Cyclophosphamide- Cytoxan- Kinetics

A

PO or IV

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9
Q

Cyclophosphamide- Cytoxan- Clinical Use

A

SLE
Granulomatous polyangiitis (Wegener’s)
Vasculitis

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10
Q

Cyclophosphamide- Cytoxan- Toxicities

A

severe bone marrow suppression and aplasia
hemorrhagic cystitis
bladder fibrosis
cancer

infertility, especially in women

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11
Q

Azathioprine- Imuran- Mech of Action

A

prodrug metabolized to 6-Mercaptopurine= weak immunomodulator

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12
Q

Azathioprine- Imuran- Kinetics

A

PO or IV

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13
Q

Azathioprine- Imuran- Clinical Use

A

decreasing use due to better drugs

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14
Q

Azathioprine- Imuran- Toxicities

A

BONE MARROW SUPPRESSION WHEN USED WITH ALLOPURINOL

GENETIC POLYMORPHISMS OF THIOPURINE S-METHYLTRANSFERASE CAN CHANGE DRUG LEVELS- CHANGE RATE OF DEACTIVATION

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15
Q

Methotrexate- Mech of Action

A

folate antagonist–> inhibit dihydrofolate reductase–> inhibit purine and pyrimidine synthesis

AT LOW DOSES ACTS AS AN ANTI-INFLAMMATORY

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16
Q

Methotrexate- Kinetics

A

PO, IV, IM

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17
Q

Methotrexate- Clinical Use

A

RA
other inflammatory arthritis
psoriasis
IBD

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18
Q

Methotrexate- Toxicities

A

ORAL ULCERS
pulmonary hypersensitivity
bone marrow suppression

PO folic acid may reduce side effects without blocking desired effects

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19
Q

Mycopheolate mofetil- Mech of Action

A

prodrug converted by plasma esterases to acid form

BLOCKS DE NOVO NUCLEOTIDE SYNTHESIS= INHIBIT B AND T CELL PROLIFERATION

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20
Q

Mycopheolate mofetil- Kinetics

A

PO or IV

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21
Q

Mycopheolate mofetil- Clinical Use

A

replacing azathioprine in clinical use, can reduce need for steroids

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22
Q

Leflunomide- Mech of Action

A

prodrug metabolized to an inhibitor of de novo pyrimidine synthesis

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23
Q

Leflunomide- Kinetics

A

EXTREMELY LONG HALF LIFE WITH EXTENSIVE ENTEROHEPATIC RECIRCULATION

24
Q

Leflunomide- Clinical Use

A

increasing use in many clinical scenarios, especially transplant and RA

25
Leflunomide- Toxicities
hepatotoxicity TERATOGENIC- administration of Cholestyramine can increase excretion if pregnancy occurs
26
Calcineurin Inhibitors- Available Drugs
Cyclosporin | Tacrolimus
27
Cyclosporin- Mech of Action
BIND CYCLOPHILIN A TO PREVENT NUCLEAR ACTIVATION OF LYMPHOCYTES AFTER ANTIGEN BINDING
28
Cyclosporin, Tacrolimus- Clinical Use
T cell mediated disease | Prevent transplant rejection
29
Cyclosporin, Tacrolimus- Toxicities
NARROW THERAPEUTIC WINDOW AND WIDE INTER- AND INTRAINDIVIDUAL VARIABILITY IN ABSORPTION AND METABOLISM hypertension hypercholesterolemia nephrotoxicity neurotoxicity MANY DRUG INTERACTIONS- CYP450 INDUCERS WILL DECREASE DRUG LEVELS, CYP450 INHIBITORS (GRAPEFRUIT JUICE) WILL INCREASE DRUG AND CAUSE NEPHROTOXICITY AND NEUROTOXICITY
30
Tacrolimus- Mech of Action
BIND FKBP TO PREVENT NUCLEAR ACTIVATION OF LYMPHOCYTES AFTER ANTIGEN BINDING
31
Inhibitors of Mammalian Target of Rapamycin (mTOR)- Available Drugs
Rapamycin
32
Rapamycin- Mech of Action
blocks singal transduction and cytokine activation blocks co-stimulation and IL2-R activation pro-apoptotic ANTI-FIBRINOGENIC
33
Rapamycin- Clinical Use
prevent transplant rejection, synergistic with the Calcineurin inhibitors controversial use in coronary stenting
34
Rapamycin- Toxicities
decrease IGF and lipoprotein lipase which can lead to severe hypertriglyceridemia and exacerbate the hypercholesterolemia of the Calcineurin inhibitors nephrotoxicity, acute pulmonary interstitial pneumonitis
35
Biologic Response Modifiers (BRMs)- Available Drugs
``` Monomurab Basailiximab Dacluzimab Abatacept Rituximab IVIg ```
36
Monomurab- Mech of Action
Ab to CD3= T cell block
37
Basiliximab, Dacluzimab- Mech of Action
Ab to IL2-R of activated cells preventing T cell proliferation/activation
38
Abatacept- Mech of Action
CTLA IgG that binds CD80/86 on antigen presenting cells and inhibits CD28 coactivation of T cells
39
Rituximab- Mech of Action
Bind CD20 and deplete B cells
40
Rituximab- Clinical Use
originally designed for B cell lymphoma potential for B cell mediated autoimmune disease- RA, SLE
41
IVIg- Mech of Action
replace antibodies--> saturate the Fc receptor--> prevent immune activation
42
Anti-TNF drugs- Available Drugs
Etanercept Infliximab Adalimumab
43
Etanercept, Infliximab- Mech of Action
Partial human Ab that blocks TNF
44
Adalimumab- Mech of Action
Fully humanized Ab that blocks TNF
45
Etanercept, Infliximab, Adalimumab- Toxicities
Fungal infections | progressive multifocal leukoencephalopathy
46
New Monoclonals- Available Drugs
``` Tocilizumab Mepolizumab Eculizumab Omalizumab Denosomab Anakinra ```
47
Tocilizumab- Mech of Action
anti IL-6
48
Tocilizumab- Clinical Use
RA
49
Mepolizumab, Eculizumab- Mech of Action
anti IL-5
50
Mepolizumab, Eculizumab- Clinical Use
HYPEREOSINOPHILIC SYNDROMES: ASTHMA SOME GLOMERULAR DISEASE
51
Omalizumab- Mech of Action
anti IgE
52
Omalizumab- Clinical Use
ASTHMA | CHRONIC URTICARIA
53
Denosomab- Mech of Action
anti RankL
54
Denosomab- Clinical Use
OSTEOPOROSIS
55
Anakinra- Mech of Action
IL-1 antagonist not actually a monoclonal antibody
56
Anakinra- Clinical Use
RA | JUVENILE RA

Pharm II Test 4 (5 decks)

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