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90 Cards in this Set
- Front
- Back
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An array of substances normally present in the body or formed there; brief lifetime and act near their sites of synthesis
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Autacoids
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What mediators cause pain?
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PG, PGI, LTB4, Kinins
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What mediators cause fever?
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PGEs
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What mediators are chemotactic for WBC?
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LTB4 and peptido leukotrienes
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What mediators cause HypOtenstion?
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Kinins and Histamine
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Histamine causes redness, heat, swelling and airway constriction, but NOT
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chemotaxis
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What cause bronchoconstriction?
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PGD2, thromboxane, histamine, peptido leukotrienes, Kinins
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What causes platelet aggregation and vasoconstriction?
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TXA2
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What mediators oppose platelet aggregation and causes vasodilation?
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PGI2
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What mediator is chemotactic for PMNs and reduces pain threshold?
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LTB4
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What is a VERY strong vasodilator?
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Kinis
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Kinins are NOT
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a major chemotactic agent (neither is histamine)
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Where is histamine stored>
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In mast cells and basophils, slow T/O
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What type of histamine is found in the cells of the CNS and rapidly growing tissues?
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Non-mast cell histamine
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What enzyme is responsible from deriving histamine from histidine?
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L-Histidine decarboxylase
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What effect is there when taking histamine orally?
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Not big, inactivated by enzymes in intestine or liver, convert it to N-acetylhistamine
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When may non-cytolytic release of histamine be significant?
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When given IV in high doses
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What type of drugs are antihistamines?
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Inverse agonsits
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Which way do antihistamines shift the DRC?
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to the right, looking like a competitive antagonist
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Which histamine receptor causes bronchoconstriction, contraction of GI, wheals, pruritis?
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H1
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Which histamine receptor causes gastric acid secretion?
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H2
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Which histamine receptor causes cardiac effects?
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Mixed H1 and H2
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Which histamine receptor causes vasodilation at low levels, high levels of histamine?
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Low = H1, High = H1 and H2
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Which histamine receptor causes a flare?
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H1 (H2 also)
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Which histamine receptor causes nasal symptoms?
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H1
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Which histamine receptor causes mucus production in the nose?
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H2
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How do the classical 1st generation antihistmines work?
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Blockade of H1, muscarininc, alpha adrenergic and serotonin receptors
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What effect do 1st gen antihistamines have on the CNS?
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They are NOT recognized by the P-glycoprotein efflux pump in the CNS, thus are NOT pumped out
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What is often used as opthalmic solutions?
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1st generation antihistamines
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Where are 1st gen antihistamines metabolized and excreted?
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Met in liver, ext in urine
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What are some side effects of 1st gen antihistamines?
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Sedation, drying of secretions, GI disturbances
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How is acute poisioning of 1st gen antihistamines tx?
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symptomatic and supportive
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What class of drug is Diphenhydramine?
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1st gen antihistamine
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What class of drug is Chlorpheniramine
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1st gen antihistamine
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Which 1st gen antihistamine should you choose if you want the sedative effects?
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Diphenhydramine
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What class of drug is Cetrizine?
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2nd gen antihistamine
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What class of drug is Fexofenadine?
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2nd gen antihistamine
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What class of drug is Loratadine?
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2nd gen antihistamine
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What is the main difference between 1st and 2nd gen antihistamines?
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2nd cause less sedation because they have an affinity for P-glycoprotein efflux pump
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Which antihistamine class would NOT potentiate the effects of depressants in the CNS?
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2nd generation
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What antihistamines do NOT have anticholinergic properties?
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2nd generation (non-sedating)
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What drug class would you give for allergy?
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Antihistamines H1
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What drug class would you give for allergic rhinits?
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Antihistamines H!
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What drug class would you give for atopic dermatitis?
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Antihistamines H!
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What do you NOT give antihistamines for?
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asthma
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What drug is most effective to tx motion sickness?
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Diphenyhydramine
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What drug is also marketed as a sleep aid?
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Diphenyhydramine
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By what are prostanoids synthesized?
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Phospholipase A2
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What is a control step in the synthesis of PG and thromboxane?
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availability of AA
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What is the key enzyme that forms PG and TX from AA?
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COX
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What COX is found in platelets?
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1
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What COX is expressed in most cells and may protect the gastric mucosa?
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1
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Where is COX 2 found?
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brain and kidney, but can be induced
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What type of receptor is a prostanoid receptor?
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7 transmembrane G protein
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What are the 3 main therapeutic effects of drugs that block COX?
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Analgesia, Antipyretic and Anti-inflammatory
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What drug irreversibly acetylates COX?
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Aspirin
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What type of drug is Ketorlac?
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NSAID
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What type of drug is Indomethacin?
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NSAID
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What type of drug is Sulindac?
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NSAID
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What type of drug is Piroxicam?
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NSAID
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What NSAID is the most potent, but can cause severe frontal headache and blood disorders?
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Indomethacin
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What NSAID has fewer GI effects than aspirin?
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Ibu
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What effects does acetaminophen display?
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Anagesic and Anti-pyretic but NOT anti-inflammatory
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Where does acetominophen effectively inhibit COX?
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In the brain, but not at sites of inflammation
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What drugs may cause a prolongation of gestation>
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COX inhibitors (PG are thought to play a role in initiating labor)
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Inhibition of what prevents platelet aggregation and TX formation?
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COX 1 (Not COX 2 because they are not in platelets)
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Rhinitis, urticaria, asthma and laryngeal edema may be a HS reaction to what?
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Aspirin (Less likely with selective COX 2 inhibitors)
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What effect does COX 1 have on platelets?
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It aggregates them
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What effect do COX 2 inhibitors have on platelets?
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It reduces the production of prostacyclin (which inhibits platelet aggregation) increasing thrombotic events
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What effect does COX 2 normally have?
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Usually inhibits platelet aggregation via prostacyclin
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What drug is associated with Reye syndrome?
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Aspirin
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What protein is utilized in the production of leukotrienes?
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FLAP (5 lipoxygenase activating protein)
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From what are luekotrienes ultimately derived?
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AA and 5-HPETE
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5-LO is a cytosolic enzyme which is translocated from the cytosol to membranes in lueukotriene synthesis by binding to what?
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FLAP
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What leukotriene is responsible for chemotaxis?
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B4
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What leukotrienes are responsible for airway constriction?
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C4,D4,E4
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What leukotriene do PMNs normally make?
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LTB4
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What is the role of HETEs?
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chemokinetic and chemotactic of WBCs
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What lueko may cause hyperalgesia?
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LTB4
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What leuko assists with leukocyte adhesion?
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LTB4
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What may leukotriene inhibitors be used for?
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Treatment of bronchial, chronic asthma
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How does Zileuton work?
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Inhibits 5-LO and thus prevents the synthesis of LTB4 and peptido-leukotrienes
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How is Zileuton metabolized?
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By C-P450
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What must be monitored with Zileuton use?
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heaptic toxicity
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How do Zafirlukast and Montelukast work?
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Leukotriene receptor antagonists
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Which is prescribed more often, Zafirlukast or Montelukast?
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Montelukast as it is only administered once without meal restriction
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Where are kinins synthesized?
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Extracellular in blood or interstitial fluid
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Kinins via the B2 receptor are potent what?
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vasodilators --> HypOtension, edema
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What type of kinins are most active?
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Bradykinin and kallidin without the terminal arg
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What receptor is utilized with kinins after trauma?
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B1
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