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FIU - histamine receptors
Histamine receptors
25
Pharmacology
Graduate
12/15/2011

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Cards

Term
what type of receptors are Histamine receptors? how manya re there?
Definition
metabotropic - G-protein
4 known
Term
H1 Blockers use
Definition
sedatives
allergic rhinitis - stuffy nose
Term
H2 blockers use
Definition
Gastric ulcers
all end in "-tidine"
Term
H3 blockers use
Definition
vertigo
Alzheimers
Term
1st generation H1 Blockers, describe, 4 types
Definition
Nonselective - also bind alpha adrenergic and muscarinic receptors
CNS penetration -> sedation
Short t1/2
Alkylamines, ethanolamines, phenothiazines, piperazines
Term
2nd generation H1 blockers
Definition
Selective H1 blockers
limited/no CNS penetration - no sedation
CYP metabolized - interferes w/ other drugs
Intermediate t1/2
Term
3rd generation H1 blockers
Definition
Selective H1 blocker
No CNS penetration
Not CYP metabolized
logn t1/2
H-receptor independent anti-inflammatory action
Term
chlorpheniramine
Definition
1st generation H1 blocker
alkylamine
Term
diphenhydramine
Definition
1st generation H1 blocker
ethanolamine
Term
clemastine
Definition
1st genration H1 blocker
ethanolamine
Term
promethazine
Definition
1st generation H1 blocker
used in "coast guard cocktail"
phenothiazine
Term
cyclizine
Definition
1st generation H1 blocker
piperazine
Term
meclizine
Definition
1st generation H1 blocker
piperazine
Term
cetirizine
Definition
2nd generation H1 blocker
Term
terfenadine
Definition
2nd generation H1 blocker prodrug - CYP 3A4 -> fexofenadine
Term
benzimidizole
Definition
2nd generation H1 blocker
Term
Ebastine
Definition
2nd generation H1 blocker prodrug -CYP 3A4 -> Carebastin
Term
loratedine
Definition
2nd generation H1 blocker
Term
levocetirizine
Definition
3rd generation H1 blocker
Term
fexofenadine
Definition
3rd generation H1 blocker
Term
desloratadine
Definition
3rd generation H1 blocker
longest t1/2
Term
Rupatidine
Definition
3rd generation H1 blocker
Term
cimetidine
Definition
H2 blocker
first available, interacted w/ CYP enzymes and made action of other drugs unpredictable
Term
Ranitidine
Definition
H2 blocker
available OTC
Term
all H2 blockers end in?
Definition
"tidine"
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