Antihistamines Flashcards
2nd generation antihistamines that block interaction of mast cell released histamine with H1 receptor
fexofenadine -terfenadine metabolite
loratadine
cetirizine -> hydroxyzine metabolite
antihistamines used for motion sickness/nausea
cyclizine
meclizine
promethazine (phenergan)
dimenhydrinate (OTC)
Where is the H1 receptor found?
smooth muscle, endothelium, brain
Where is the H2 receptor found?
gastric mucosa, cardiac muscle, mast cells, brain
What does cyproheptadine do?
first generation H1 blocker that also strongly blocks serotonin receptors (serotonin directly constricts vascular smooth muscle)
Name H2 receptor blockers
cimetidine
ranitidine
diphenhydramine
chlorpheniramine
bromopheniramine
OTC first generation antihistamines
What does histamine do?
vasodilation (headache & flushing)
H1 activation causes NO release from endothelium -> vasodilation
What asthma drug class can reduce histamine release?
beta2 agonist
Receptors which 1st generation antihistamines interact
muscarinic, alpha, serotonin and local anesthetic receptor sites
Where is the H4 receptor located
eosinophils, neutrophils, CD4 T cells