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Drugs/Immuno > Immunology Drugs > Flashcards

Immunology Drugs Flashcards

1
Q

Prednisone,Prednisolone

A
  • Glucocorticoids
  • lyse and cause redistribution of lymphocytes, monocytes, eosinophils, and basophils
  • inhibit macrophages and APCs, phospholipase A2->arachidonic acid
  • reduces formation of prostaglandin and leukotrienes
  • increase infection rate, malignancy,growth retardation,slow would healing, hypertension, hyperglycemia, diabetogenic, osteopenia
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2
Q 
Antithymocyte globulin (ATG) 
Antilymphocyte globulin (ALG)
A
  • Immunomodulatory polyclonal antibodies
  • bind surface of immune cell and deplete lymphocytes and thymocytes by direct cytotoxicity
  • use for transplants for induction, initial rejection, reduces GVH
  • causes fever,chills,hypotension,serum sickness,glomerulonephritis,cytokine release syndrome
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3
Q

Muromonab

A
  • Immunmodulatory monoclonal antibody
  • Ab against CD3, TCR complex
  • blocks antigen recognition and cell function
  • causes internalization of TCR, apoptosis/T cell death by complement path
  • pretreat with steroids
  • causes: CRS, systemic shock due to TNF-alpha,cytokine,IFNgamma release
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4
Q

Daclizumab, Basiliximab

A
  • Immunomodulatory monoclonal antibody
  • Anti CD25 (IL-2R)
  • MABs to alpha subunit of IL-2R on T cells when they are activated
  • block IL2 stimulation and increase apoptosis of T cells
  • lower toxicity and less cytokine release than muromonab, anaphylaxis is possible
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5
Q

Rituximab

A
  • Immunomodulatory monoclonal antibody
  • Anti CD20 on B cells
  • used for antibody mediated transplant rejection, B cell cancer, antibody dependent autoimmune disease
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6
Q

Alemtuzumab

A
  • Immunomodulatory monoclonal antibody
  • Anti CD52 on T,B,NK, monocytes,macrophages
  • Causes extensive lympholysis due to apoptosis, prolonged T/B cell depletion
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7
Q

Abatacept

A
  • Recombinant CTLA4 receptor protein - FcIgG
  • inhibit T cell activation-costimulatory blockade, blocks CD80/CD86 attachment to CD28 to prevent activation and cause anergy
  • fusion protein contains extra cellular domain of CTLA4 and Fc region that inhibits B7-CD28 binding
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8
Q

Belatacept

A
  • Recombinant CTLA4 receptor protein - FcIgG
  • inhibit T cell activation-costimulatory blockade, blocks CD80/CD86 attachment to CD28 to prevent activation and cause anergy
  • 2nd generation CTLA4-Fc fragment
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9
Q

Cyclosporine (CsA)

A
  • Calcineurin inhibitor
  • binds cyclophilin in cell, makes CsA-CyP complex, binds PP2B and inhibits dephosphorylation of NF-ATc
  • no NF-ATc in nucleus=no T cell transcription/activation
  • inhibits signal transduction cascade, blocks IL2
  • metabolized by liver, CYP450
  • used for transplants, RA, psoriasis, autoimmune disorders
  • nephrotoxicity,neurotoxicity,hypertension,hyperlipidemia,inhibit PGI2
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10
Q

Tacrolimus (FK506)

A
  • calcineurin inhibitor
  • enters cell, binds FK506 binding protein 12 (FKBP12), complex binds PP2B, inhibits NF-ATc=no transcription/activation, blocks IL2
  • metabolized by liver
  • causes nephrotoxicity,neurotoxicity,hypertension,hyperkalemia,hyperglycemia
  • diabetogenesis=glucocorticoids and tacrolimus
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11
Q

Sirolimus (Rapamycin)

A
  • Antiproliferative agents (mTOR inhibitors)
  • binds to FKBP12 but complex then binds to and inhibits mTOR, fails to phosphorylate and activate CdK2 arrests G1 to S phase
  • metabolized by CYP3A4 and transported by P-glycoprotein in bile
  • use for coronary stents, pneumonia,cytomegalovirus,tuberous sclerosis
  • cause myelosuppression,thrombocytopenia,anemia,delay wound healing
  • combo of mTOR and calcineurin inhibitors help with renal transplants
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12
Q

Mycophenolate mofetil

A
  • antimetabolite
  • prodrug hydrolyzed to mycophenolic acid
  • reversible inhibitor of GMP pathway
  • B&T cells are dependent on purine synthesis, selectively inhibited
  • inhibits T,B,NK cell proliferation,cellular adhesion,migration
  • causes leukopenia,diarrhea, vomiting
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13
Q

Azathioprine

A
  • Antimetabolite
  • prodrug cleaved to 6MP, inhibits purine synthesis
  • 6MP phosphorylated by salvage pathway and put in DNA-disrupts replication, transcription, and function
  • metabolized by oxidation and methylation in liver
  • causes bone marrow suppression, leukopenia,thrombocytopenia,anemia, hepatotoxicity, alopecia,pancreatitis, GI toxicity
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14
Q

Nabumetone

A
  • NSAID
  • some selectivity for COX2
  • prodrug
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15
Q

Indomethacin

A
  • NSAID

- use is associated with risk of CV events (MI)

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16
Q

Aspirin

A
  • Classic NSAID
  • analgesic, antipyretic, antiplatelet, anti-inflammatory
  • absorbed rapidly from stomach and intestine in unionized form
  • irreversibly inhibits prostaglandin biosynthesis by acetylating COX
17
Q

Chlorpheniramine, diphenhydramine, promethazine

A
  • 1st gen. H1 receptor competitive antagonists
  • short lasting
  • anticholinergic, anti alpha-adrenergic, antiserotonergic, sedative, antiemetic, anti motion sickness
18
Q

Loratadine, fexofenadine, cetirizine

A

“Allegra”,”Zyrtec”,”Claritin”

  • 2nd/3rd gen. H1 receptor competitive antagonists/inverse agonists
  • longer lasting
  • more specific use
19
Q

Acetaminophen

A
  • analgesic,antipyretic, NOT anti inflammatory

- severe hepatotoxicity with overdosage caused by reactive quinone species

20
Q

Celecoxib

A
  • only approved COX2 inhibitor
  • still bad for upper GI, reduced amt of small bowel inflammation and mucosal breaks
  • negative impact on bone remodeling and ulcer repair
  • reduces water and salt excretion by the kidneys
21
Q

Zileutron

A
  • Leukotriene pathway inhibitors
  • inhibits 5-lipoxygenase, inhibits CYP3A4
  • for mild/moderate asthma
  • blocks formation of leukotrienes
22
Q

Zafirlukast, Montelukast

A
  • LTD4 receptor antagonists
  • inhibit CYP3A4 and CYP2C9
  • for mild/moderate asthma
  • blocks actions of leukotrienes
23
Q

Infliximab

A
  • chimeric antiTNF alpha monoclonal antibody
  • given by IV in doses and then as maintenance dose
  • cytokine blocker
24
Q

Etanercept

A
  • Cytokine blocker

- human TNF receptor linked to Fc portion of human IgG1

25
Q

Adalimumab

A
  • Cytokine blocker
  • Human monoclonal antibody specific for TNF alpha
  • methotrexate reduces clearance
26
Q

Anakinra

A
  • Inhibitor of IL1 function
  • recombinant, nonglycosylated synthetic form of the human IL1 receptor antagonist
  • endogenous regulator of IL1
  • used for RA
27
Q

Rituximab

A
  • Inhibitor of B cell function
  • for pts that don’t respond to anti TNF alpha therapy
  • chimeric monoclonal Ab against CD20 antigen
  • use glucocorticoid before each injection
28
Q

Tofacitinib

A
  • JAK inhibitor
  • blocks JAK3 and JAK1, less JAK2
  • for moderate-severe active RA
29
Q

Apremilast

A
  • PDE4 inhibitor
  • indicated for moderate-severe plaque psoriasis
  • increases intracellular cAMP and decreases TNFa production

Drugs/Immuno (9 decks)

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