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FMS > Immune/Inflammation Drugs > Flashcards

Immune/Inflammation Drugs Flashcards

1
Q

Mechanism, Use, and Toxicity of Diphenhydramine

A

1st gen antihistamine

Blocks H1 receptors, also varying anticholinergic, antialphaadrenergic, antiserotonergic actions

Allergic rhinitis/conjunctivitis, urticaria, sleep aid, motion sickness

sedation, blurred vision, urinary retention, hypotension, known hypersensitivity

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2
Q

Which NSAIDs are used for osteoarthritis and rheumatoid arthritis?

A

Nabumetone, meloxicam, and celecoxib (these have COX-2 selectivity)

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3
Q

Mechanism, Use, and Toxicity of Basiliximab?

A

Monoclonal antibody against CD25 (IL-2R) of activated T-cells

blocks IL-2 stimulation and induces apoptosis

Less cytokine release, anaphylaxis still possible

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4
Q

Mechanism, Use, and Toxicity of Daclizumab?

A

Monoclonal antibody against CD25 (IL-2R) of activated T-cells

blocks IL-2 stimulation and induces apoptosis

Less cytokine release, anaphylaxis still possible

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5
Q

Mechanism, Use, and Toxicity of ATG and ALG?

A

Polyclonal antibodies against thymocyte/lymphocyte surface antigens

Antibodies from horse/sheep against human T lymphocytes by direct cytotoxicity

Toxicities: fever, chills, hypotension, serum sickness, glomerulonephritis, cytokine release syndrome

Used for transplants for induction, initial rejection, and steroid-resistant rejection

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6
Q

Mechanism, Use, and Toxicity of Chlorpheniramine

A

1st generation antihistamine

Blocks H1 receptors, also varying anticholinergic, antialphaadrenergic, antiserotonergic actions

Allergic rhinitis/conjunctivitis

sedation, blurred vision, urinary retention, hypotension, known hypersensitivity

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7
Q

Mechanism of Rituximab?

A

Monoclonal antibody against CD20 of B cells

used in antibody mediated transplant rejection (and autoimmune & B cell cancer) and post-transplant lymphoproliferative disorder (EBV reactivation)

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8
Q

How is aspirin different than other NSAIDs?

A

Its action is non-reversible; anti-platelet effects

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9
Q

Mechanism, Use, and Toxicity of Promethazine

A

1st gen antihistamine

Blocks H1 receptors, also varying anticholinergic, antialphaadrenergic, antiserotonergic actions

Allergic rhinitis/conjunctivitis, urticaria, sleep aid, motion sickness, anti-emetic

sedation, blurred vision, urinary retention, hypotension, known hypersensitivity

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10
Q

Mechanism, Use, and Toxicity of Montelukast?

A

Leukotriene pathway inhibitor

LTD4 antagonist

Alternative to low-dose inhaled corticosteroid for moderate asthma, excercise-induced broncoconstriction, allergic rhinitis

behavioral disturbances, insomnia, sytemic eosinophilia, inhibits CYP3A4

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11
Q

Mechanism, Use, and Toxicity of cyclophosphamide in SLE?

A

Treg elimination in SLE; crosslinks DNA (alkylating agent)

Toxicities: increased infection, amenorrhea, ovarytoxicity, bladder toxicity

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12
Q

What are the side effects of traditional NSAIDs?

A

GI dyspepsia, GI bleeding, dizziness (aspirin->tinnitus)

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13
Q

Mechanism of Alemtuzumab?

A

Monoclonal antibody against CD52 on lymphocytes

Causes apoptosis, prolonged T cell depletion and some B cell depletion allowing drug minimalization during acute rejection

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14
Q

Mechanism, Use, and Toxicity of Mycophenolate?

A

prodrug for mycophenolic acid

reversible inhibitor of inosine monophosphate dehydrogenase in purine synthesis; selectively targeting highly dependent B and T cells

used with glucocorticoids and calcineurin inhibitors

metabolized via glucuronidation before excretion

toxicities: leukopenia, diarrhea, vomiting

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15
Q

Mechanism, Use, and Toxicity of Loratidine, Cetirizine, Fexofenadine

A

2nd/3rd Gen Antihistamine

Blocks H1 histamine receptors

Allergic rhinitis/conjunctivitis, urticaria

Known hypersensitivity, coadministration with certain antifungal/antibiotics results in increased antihistamine levels

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16
Q

Mechanism of Abatacept?

A

Fusion protein containing domain of CTLA-4 and Fc fragment that inhibits B7-CD28

Inhibits T-cell activation/promotes anergy by blocking costimulation

17
Q

Mechanism, Use, and Toxicity of Cyclosporine?

A

Calcineurin inhibitor

Binds cyclophilin in cell, complex binds calcineurin (PP2B), NF-ATc is left phosphorylated and cannot begin transcription cascade for T-cell activation signal transduction including IL-2

Limiting Nephrotoxicity; also neurotoxicity, hirsutism, hypertension, hyperlipidemia, gum hyperplasia due to inhibition of PGI2

Used for organ transplantation and some autoimmune disorders

18
Q

Mechanism, Use, and Toxicity of Zileuton?

A

Leukotriene Pathway Inhibitor

Inhibits 5-lipoxygenase

Alternative to low-dose inhaled corticosteroid for moderate asthma

Dizziness, drowsiness, GI dyspepsia, liver impairment, reduced WBC count, inhibits CYP3A4

19
Q

Mechanism, Use, and Toxicity of Sirolimus?

A

mTOR inhibitor (also Rapamycin)

Binds FKBP12, complex inhibits mTOR, CdK2 cannot be phoshorylated, cell cycle arrested at G1-S

effective in use with calcineurin inhibitor, worse renal function after 1 year of treatment

Toxicities: cholesterol/triglyceride increase, myelosuppression, thrombocytopenia, delayed healing

Uses: organ transplants, coronary stents, prophylaxis in certain infections, tuberous sclerosis

20
Q

Mechanism, Use, and Toxicity of Zafirlukast?

A

Leukotriene Pathway Inhibitor

LTD4 receptor antagonist

Alternative to low-dose inhaled corticosteroid for moderate asthma

Headache, sore throat, nausea, liver impairment, inhibits CYP3A4

21
Q

Mechanism, Use, and Toxicity of Tacrolimus?

A

Calcineurin inhibitor

Binds FKBP12 in cell, binds and inhibits calcineurin, inhibiting T-cell activation including IL-2R

Limiting nephrotoxicity, neurotoxicity, hypertension, hyperkalemia, hyperglycemia, diabetes (especially with steroids)

22
Q

What corticosteroids have short, intermediate and long duration?

A

Short-medium: prednisone, fluticasone, methylprednisolone

Intermediate: Triamcinolone

Long: dexamethasone

23
Q

Mechanism, Use, and Toxicity of hydroxychloroquine in SLE?

A

Anti-inflammatory effect in SLE; mechanism uncertain

toxicities: headache, dizziness, alopecia, nausea muscle pain; rare: leukopenia, thrombocytopenia, retinal damage

24
Q

Mechanism of Belatacept?

A

2nd Generation fusion protein containing domain of CTLA-4 and Fc fragment that inhibits B7-CD28

Inhibits T-cell activation/promotes anergy by blocking costimulation

25
Q

Mechanism, Use, and Toxicity of Muromonab-CD3?

A

Monoclonal antibody against CD3

Blocks TCR complex, induces apoptosis or activation of complement

Toxicities: cytokine release syndrome, systemic shock

26
Q

Mechanism, Use, and Toxicity of Azathioprine?

A

Antimetabolite

Prodrug for 6MP which inhibits de novo purine synthesis; selectively inhibiting highly dependent B and T cells

Metabolized in liver via oxidation before elimination

Toxicities: bone marrow suppression, hepatotoxicity, dose reductions needed with allopurinol

FMS (10 decks)

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