histaminergics
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32 Terms
Where is histamine synthesized?
mast cells
Where is histamine mainly stored?
mast cells
Where in mast cells is histamine stored?
granules
Other histamine storage locations
basophils
enterochromaffin-like cells
brain cells
Where is H1 located
smooth muscle
endothelium
nerve endings
brain cells (post synpatic)
Where is H2 located?
gastric mucosa
cardiac muscle
mast cells
brain cells (post synaptic)
Where is H3 located?
nerve endings
brain cells (pre-synaptic)
Where is H4 located?
leukocytes in bone marrow
other tissues
H1 is ____ coupled
Gq
H2 is _____ coupled
Gs
H3 is _____ coupled
Gi
H4 is _____ coupled
Gi
H3 function
regulates release of histamine
H1 activation effects
vasodilation
bronchoconstriction
hives
intestinal contractions (at high concentration)
H2 activation effects
gastric acid secretion
negative feedback on histamine release from mast cels
H2 activation effects at high concnetration
vasodilation
heart rate
heart contractility
What are the 3 parts to the triple response of lewis
Flush
Flare
Wheal
What causes flushing
immediate and localized capillary dilation
What causes flare
arteriolar dilation
What causes the wheal
fluid and plasma protein leaking through the capillary walls
how does epinephrine counteract histamine
has opposite effects on smooth muscle, but via different receptors
Mast cell stabilizer agent
cromolyn sodium
1st gen H1 antagonist agents
tripelennamine
diphenhydramine
chlorpheniramine
meclizine
hydroxyzine
chlorpromazine
promethazine
olopatadine
2nd gen H1 antagonist agents
terfenadine
fexofenadine
loratadine
desloratadine
cetirizine
H3 antagonist agent
pitolisant
tripelennamine structure
ethylenediamine
ethylenediamine SAR
2 carbon spacer
Small (methyl) groups on basic amine
Ar1 is typically phenyl
Ar2 is typically a heterocyclic ring
tripelennamine indications
allergic rhinits
hay fever
urticaria
adjunct in anphylaxis
diphenhydramine structure
ethanolamine ether
ethanolamine ether SAR
2 carbon spacer
Small (methyl) groups on basic amine
Ar1 is typically substituted phenyl ring
Ar2 is typically unsubstituted phenyl ring
diphenhydramine indications
allergies
common cold
pruritis
anaphylaxis adjunct
sleep aid
Parkinson’s adjunct (extrapyramidal)
local anesthetic
What drugs are on the Beers criteria?
diphenhydramine
chlorpheniramine
meclizine
hydroxyzine
chlorpromazine
promethazine
olopatadine