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8 Cards in this Set

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Triple response of histamine
1. Flush - localised red (NO mediated dilation of arterioles)
2. Wheal - swelling (leakage from post-capillary venules)
3. Flare - large irregular flare sensory nerve axon reflex

also histamine induces SM contraction, pain and itchiness
Inhibiting histamine
1. functional (physiological) antagonism - e.g. adrenaline opposes histamine induced bronchoconstriction in systemic anaphylaxis

2. Histamine receptor antagonists (antihistamines)
1st gen H1-receptor antagonists
Promethazine, Diphenhydramine, Cyproheptadine

Acts on other receptors aswell

each has side effects (sedation, dry mouth, postural hypertension)

hence, their primary use is NOT H1 receptor blockade
2nd gen H1-receptor antagonists
selective antagonists of H1 receptor only - less side effects

Fexofenadine (Telfast)
Cetirizine (Zyrtec)
Loratadine (Claratyne)
How do antihistamines stop hayfever
Hayfever = "seasonal allergic rhinitis"

1. sneeze & itch - by inhibiting histamine induced activation of sensory nerves
2. rhinorrhea by inhibiting secretion from mucus glands
3. acute congestion by inhibiting microvascular leakage from post-capillary venules
Treating chronic nasal congestion
fexofenadine good for itch sneezing and rhinorrhea however, chronic nasal congestion is inflammatory

hence, use intranasal glucocorticoids
H2 receptor antagonists
Ranitidine - for gastric ulcer / gord
supress gastric acid secretion in response to histamine on parietal cells
Antitussives
1. treat underlying cause

2. nonspecific therapy - codeine
(or methylmorphine - opiates)

good for NONPRODUCTIVE cough

acts centrally on cough receptor

side effects - drowsiness, constipation, nausea & vomiting