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antihistamines
.
20
Medical
Graduate
12/10/2010

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Term
histamine
Definition
unknown physiological fxn, high conc in skin/lungs, decarboxylated from histidine, bound to heparin for storage in vesicles of mast cells (heparin pos, histamine neg), rapid (4-5 min) breakdown in blood by diamine oxidase (genetic def)

release by ag-ab on mast cell, pcn (directly to mast cell R w/o ab), narcotics (esp morphine, meperidine/demerol), nsaids, sns (skin rxn but no anaphylaxis)
Term
histamine receptors
Definition
h1: capillaries (inc perm --> edema, hives, hypotension), bronchoconstriction, uterine contraction, nn (pain, pruritis, h3 in thalamus)

h2: sa node (inc hr), myocardium (inc contractility), secretory (inc acid/pepsin prod in stomach), stomach (inc h secretion)

h1+h2: vasodilation --> dec bp

h3: brain? (pain?)
Term
first generation h1 blockers
Definition
po, 3-6 hr, moa competitive inh, use allergy, motion sickness, pruritis, ae anticholinergic (dry mouth, constipation), sedation, a-block (hypotension)

tripelenamine, diphenhydramine, dimenhydranate, chlorpheniramine, meclizine, promethazine
Term
tripelenamine
Definition
pbz, 1st gen h1 block, use allergies

+1 anticholinergic, +2 sedation
Term
diphenhydramine
Definition
benadryl, 1st gen h1 block, use allergies, motion sickness

+3 anticholinergic, +3 sedation
Term
dimenhydrinate
Definition
dramamine, 1st gen h1 block, use motion sickness

+3 anticholinergic, +3 sedation
Term
chlorpheniramine
Definition
chlortrimemton, 1st gen h1 block, better/safer drug for allergies, less ae

+1 anticholinergic, +1 sedation
Term
meclizine
Definition
antivert, 1st gen h1 block, use motion sickness for astronauts

+0 anticholinergic, +1 sedation
Term
promethazine
Definition
phenergan, 1st gen h1 block, use allergies, combined w/ codeine (suppress cough) for cold (dry up sec, dec congestion)
Term
hydroxyzine
Definition
1st gen h1 block, use pruritis, allergies

+0 anticholinergic, +3 sedation
Term
second generation h1 blockers
Definition
po, 12 hrs, moa competitive inh, no sedation, no anticholinergic, no a-block, ae tremor, use only allergy

loratadine, fexofenadine, ceterizine, terfenadine
Term
loratadine
Definition
claratin otc, 2nd gen h1 block, clarinex is metabolite (rx only, covered by insurance)
Term
fexofenadine
Definition
allegra, 2nd gen h1 block
Term
cetirizine
Definition
zyrtec, 2nd gen h1 block
Term
terfenadine
Definition
seldane, 2nd gen h1 block, not used since p450 metab can be blocked by erythromycin --> inc conc terfenadine --> long qt --> torsades

+0 anticholinergic, +1 sedation
Term
h2 blockers
Definition
po, parental, moa competitive inh, ae tremor, use pud

cimetidine, rantidine, famotidine, nizatidine
Term
cimetidine
Definition
tagamet, h2 block, inh p450 over time so use only hospital short term, ae gynecomastia, anti-testosterone, use transvestite
Term
rantidine
Definition
zantac, h2 block, ae hf?
Term
famotidine
Definition
pepcid, h2 block
Term
nizatidine
Definition
axid, h2 block
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