Immune/Inflammation Drugs Flashcards
Mechanism, Use, and Toxicity of Diphenhydramine
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
Which NSAIDs are used for osteoarthritis and rheumatoid arthritis?
Nabumetone, meloxicam, and celecoxib (these have COX-2 selectivity)
Mechanism, Use, and Toxicity of Basiliximab?
Monoclonal antibody against CD25 (IL-2R) of activated T-cells
blocks IL-2 stimulation and induces apoptosis
Less cytokine release, anaphylaxis still possible
Mechanism, Use, and Toxicity of Daclizumab?
Monoclonal antibody against CD25 (IL-2R) of activated T-cells
blocks IL-2 stimulation and induces apoptosis
Less cytokine release, anaphylaxis still possible
Mechanism, Use, and Toxicity of ATG and ALG?
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
Mechanism, Use, and Toxicity of Chlorpheniramine
1st generation antihistamine
Blocks H1 receptors, also varying anticholinergic, antialphaadrenergic, antiserotonergic actions
Allergic rhinitis/conjunctivitis
sedation, blurred vision, urinary retention, hypotension, known hypersensitivity
Mechanism of Rituximab?
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)
How is aspirin different than other NSAIDs?
Its action is non-reversible; anti-platelet effects
Mechanism, Use, and Toxicity of Promethazine
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
Mechanism, Use, and Toxicity of Montelukast?
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
Mechanism, Use, and Toxicity of cyclophosphamide in SLE?
Treg elimination in SLE; crosslinks DNA (alkylating agent)
Toxicities: increased infection, amenorrhea, ovarytoxicity, bladder toxicity
What are the side effects of traditional NSAIDs?
GI dyspepsia, GI bleeding, dizziness (aspirin->tinnitus)
Mechanism of Alemtuzumab?
Monoclonal antibody against CD52 on lymphocytes
Causes apoptosis, prolonged T cell depletion and some B cell depletion allowing drug minimalization during acute rejection
Mechanism, Use, and Toxicity of Mycophenolate?
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
Mechanism, Use, and Toxicity of Loratidine, Cetirizine, Fexofenadine
2nd/3rd Gen Antihistamine
Blocks H1 histamine receptors
Allergic rhinitis/conjunctivitis, urticaria
Known hypersensitivity, coadministration with certain antifungal/antibiotics results in increased antihistamine levels
Mechanism of Abatacept?
Fusion protein containing domain of CTLA-4 and Fc fragment that inhibits B7-CD28
Inhibits T-cell activation/promotes anergy by blocking costimulation
Mechanism, Use, and Toxicity of Cyclosporine?
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
Mechanism, Use, and Toxicity of Zileuton?
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
Mechanism, Use, and Toxicity of Sirolimus?
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
Mechanism, Use, and Toxicity of Zafirlukast?
Leukotriene Pathway Inhibitor
LTD4 receptor antagonist
Alternative to low-dose inhaled corticosteroid for moderate asthma
Headache, sore throat, nausea, liver impairment, inhibits CYP3A4
Mechanism, Use, and Toxicity of Tacrolimus?
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)
What corticosteroids have short, intermediate and long duration?
Short-medium: prednisone, fluticasone, methylprednisolone
Intermediate: Triamcinolone
Long: dexamethasone
Mechanism, Use, and Toxicity of hydroxychloroquine in SLE?
Anti-inflammatory effect in SLE; mechanism uncertain
toxicities: headache, dizziness, alopecia, nausea muscle pain; rare: leukopenia, thrombocytopenia, retinal damage
Mechanism of Belatacept?
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
Mechanism, Use, and Toxicity of Muromonab-CD3?
Monoclonal antibody against CD3
Blocks TCR complex, induces apoptosis or activation of complement
Toxicities: cytokine release syndrome, systemic shock
Mechanism, Use, and Toxicity of Azathioprine?
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
