Anti-Inflammatory Drugs Flashcards
Histamine
Released by Mast cell IgE mediated degranulation, and from basophils. Leads to redness, heat, swelling, and airway constriction acid secretion, urticaria. No chemotaxis.
LTB4
Leukotriene which is Chemotactic for neutrophils, reduces pain threshold.
LTC4
Causes bronchoconstriction, increased vascular permeability,
LTD4
Causes bronchoconstriction, increased vascular permeability
LTE4
Causes bronchoconstriction, increased vascular permeability
PGD2
Prostaglandin receptor leading to bronchoconstriction. Produced by mast cells.
PGE2
Prostaglandin receptor causing FEVER(IL-1 mediated) Vasodilation, increased vascular permeabilty and pain.
PGF2
prostaglandin receptor which leads to uterine contraction, and bronchoconstriction.
PGI2
Prostaglandin receptor causing Vasodilation, increased vascular permeabilty and pain, and opposes platelet aggregation.
TXA2
Thromboxane which leads to bronchoconstriction, platelet aggregation, and vasoconstriction.
Bradykinin
Does everything(leads to infllamation, redness, swelling, heat, pain). It is also a strong VASODILATOR resulting in hypotension. not a chemoattractant
Kallidin
Kinin which Does everything. It is also a strong VASODILATOR resulting in hypotension. not a chemoattractant
Diphenhydramine
1st generation Antihistamine Prevents histamine induced bronchoconstriction, contraction of GI smooth muscle, hives, itch, pain. NOT pumped out of CNS. Low GI side effects. Drying of secretions. Has antimuscarinic properties.
Chlorpheniramine
1st generation Antihistamine Prevents histamine induced bronchoconstriction, contraction of GI smooth muscle, hives, itch, pain. Not as sedating as diphenhydramine. Drying of secretions. Has antimuscarinic properties.
Cetirizine
2nd Generation Antihistamine. Has minimal anticholinergic properties, Does not cause sedation or drying of secretions. Subject for P-Glycoprotein Efflux pump.
Fexofenadine
2nd Generation Antihistamine. Has minimal anticholinergic properties, Does not cause sedation or drying of secretions. Subject for P-Glycoprotein Efflux pump.
Loratadine
2nd Generation Antihistamine. Has minimal anticholinergic properties, Does not cause sedation or drying of secretions. Subject for P-Glycoprotein Efflux pump.
Zileuton
Inhibits 5- lipoxygenase and prevents synthesis of LTB4, increasing pain threshold, may decrease use of beta agonsists in asthma, AE: CYP450, hepatotoxicity.
Zafirlukast
Leukotriene receptor antagonist (LTD receptor), AE: inhibits a cytochrome P450 isoenzyme and may cause significant drug interactions. Used in asthma.
Montelukast
Leukotriene receptor antagonist,(LTD4 receptor), Used in Asthma. daily admin w/o meal restrictions.
Aspirin
Irreversible COX inhibitor. Has more effects on platelets because they don’t have a nucleus. AE: bleeding and GI problems, tinnitus, asprin hypersensitivity(rhinitis, urticaria, asthma, laryngeal edema) due to shift to lypoxegenase shift. Rye syndrome: encephalopathy and fatty liver following viral infection in kids.
Ibuprofen
Nonselective COX inhibitor, fewer GI side effects than aspirin.
Naproxen
Aleve, Nonselective COX inhibitor.
Ketorlac
More potent NSAID, Nonselective COX inhibitor, used for analgesia, but is also anti-inflammatory.
Indomethacin
MOST potent NSAID, Nonselective COX inhibitor, AE: severe frontal headache and blood disorders
Sulindac
More potent NSAID, Nonselective COX inhibitor
Ketoprofen
More potent NSAID Nonselective COX inhibitor, related to ibuprofen
Piroxicam
More potent NSAID once a day admin, can cause dose related serious GI bleeding.
Celecoxib
Selective COX II inhibitor.
Acetaminophen
Not an NSAID, Is a weak inhibitor of COX, and has minimal anti-inflammatory effect. Analgesic and antipyretic. AE: hepatotoxicity.
Cortisol
Anti-inflammatory Steroid,
Hydrocortisone
Anti-inflammatory Steroid
Prednisone
Anti-inflammatory steroid
Methylprednisone
Anti-inflammatory steroid
Betamethasone
Anti-inflammatory Steroid, long acting
Dexamethasone
Anti-inflammatory Steroid, Long acting.
Cyclosporine
Immunosuppresive agent, Binds cyclophilin receptor inhibiting calcineurin activity, blocking dephosphorylation events for T cell activation. Liver met. AE: Drug interactions, renal toxicity up to 75%. Used long term for transplants.
Tacrolimus (FK506)
Immunosuppressive, binds FKB506 resulting in inhibition of calcineurin. Blocks the dephosphorylation events for cytokine expression and T cell activ. 100X more potent than cyclosporine. AE: nephrotoxicity.
Sirolimus
Antiproliferative drug used for organ transplant rejection. Binds FKBP to inhibit mTOR and stop cell cycle progression of B and T cells. AE: dose dependant increase in cholesterol and Triglycerides, nephrotoxicity, increased lymphomas and infections, CYP3A4.
Mycophenolate
Antimetabolic drug, used in organ transplant, metabolite is inhibitor of inosine monophosphate dehydrogenase, preventing guanine synthesis. B and T cells are highly dependant on this pathway for proliferation. AE: hematologic and GI tox. Leukopenia, diarrhea and vomiting.
Anti-thymocyte Globulin
Immunosuppressive, Ig binds thymocytes in circulation resulting in lymphopenia and impaired T cell immune response. AE: toxicity due to Ig being recognized as foriegn: i.e. serum sickness, nephritis, occasional anaphylaxis
Muromonab-CD3
Immunosuppressive, used for whole organ transplants. Is an antibody whcih binds CD3(t-cell receptor). AE: cytokine release syndrome, give corticosteroids first.
Daclizumab
Immunosuppressive. Humanized, Anti-IL-2 receptor for activated T cells, blocking IL2 activated T cell activation events. Used in organ transplantation. AE: few, common antibody side effects
Basiliximab
Immunosuppressive. Humanized, Anti-IL-2 receptor for activated T cells, blocking IL2 activated T cell activation events. Used in organ transplantation. AE: few, common antibody side effects
Phenylephrine
Alpha1 agonist, leads to vasoconstriction
Theophylline
adenosine receptor antagonist, increases cAMP, inhibits leukotriene synthesis
omalizumab
Antibody to IgE, increased risk of parasitic infections. expensive.
