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37 Cards in this Set
- Front
- Back
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what does histamine do in the brain?
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it is a neurotransmitter (used for arousal)
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What does histamine come from in the stomach?
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enterochromaffin-like cells
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What triggers histamine release from mast cells?
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interaction of IgE and antigens
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How do morphine, codeine, and some radiocontrast dies affect histamine release?
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they can induce its release from mast cells
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Where are H1 and H3 receptors located?
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in the CNS
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Where are H2 receptors located?
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in the gut- regulates gastric acid production
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What type protein is H1 linked to?
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this is linked to a Gq/11 protein- that increases IP3 and DAG production
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How does histamine affect the respiratory system?
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this causes bronchospasms
especially in asthmatics |
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How does histamine affect gastric glands?
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this increases secretion of gastrin
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What are the intradermal effects of histamine?
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the lewis triple response
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How do you treat anaphylaxis?
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Epi, steroids, injected antihistamines
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What receptor do ALL antihistamines here act on?
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H1 receptors
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What is the method of action of antihistamines?
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these are inverse agonists which decrease constitutive activity at histamine receptor and block effects of histamine and its release
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What is the main side effect of first gen H1 antagonists?
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quite sedating*
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What is Diphenhydramine?
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this is benadryl, and its is very sedating
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What is dimenhydrinate?
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this is dramamine, and it is very sedating
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What is Promethazine?
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this is a first gen antihistamine
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What are the effects of Promethazine?
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antiemetic
very sedating |
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What effect allows first gen antihistamines to be used to treat motion sickness?
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they have significant anticholinergic activity
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What is special about second generation H1 antagonists?
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they do NOT enter the brain
non sedating- and have no anti emetic effects |
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Where are most antihistamines metabolized?
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in the liver
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What enzyme metabolizes second generation antihistamines?
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CYP3A4
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What antihistamine is eliminated only by the kidney?
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Cetirizine (Zyrtec)
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What are the best antihistamines to treat motion sickness?
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Diphenhydramine (benadryl)
Dimenhydrinate (dramamine) Promethazine (phenergan) |
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What can happen with 1st gen antihistamines and booze/
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marked CNS depression
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Should you give antihistamines during pregnancy?
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nope
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How does erythromycin and ketoconazole affect antihsitamines?
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this inhibits metabolism of 2nd gen ones
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How does grapefruit juice affect antihistamines?
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this inhibits CYP3A4 - so slows 2nd gen metabolism
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What are the affects of 1st gen antihistamine tox?
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similar to atropine
"mad as a hatter, dry as a bone, hot as a hare, blind as a bat, red as a beet" |
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What are the affects of 2nd gen antihistamine toxicity?
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cardiac arrhythmias
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What does Cromolyn sodium do?
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this inhibits release of histamine from mast cells
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What does nedcromil do?
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this inhibits histamine release from mast cells
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What is Azelastine?
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this is Astelin/Astepro nasal spray
non-competitive H1 blocker |
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What is Ceterizine?
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Zyrtec inhibits release of histamine from mast cells
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What interleukins are common in asthma?
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4,5,13
these activate eosinophils, and stimulate IgE production |
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What happens in chronic bronchitis?
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immobile cilia
excess mucous inflammtion narrow airways chronic cough |
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What is emphysema?
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breakdown of alveolar walls, decreasing surface area
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