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35 Cards in this Set

  • Front
  • Back
______ catalyzes decarboxylation of histidine to histamine
Histidine decarboxylase
In what cells is histamine made
Enterochromaffin-like cells
Histamine causes bronchial smooth muscle constriction/dilation?
Constriction
Most prominent effect of histamine on the vasculature is __
Dilation of the postcapillary venule bed
Histamine induces/suppresses gastric acid secretion
Induces - causes Ca2+ influx into parietal cells
Activation of the H1 receptor leads to increase in levels of what
IP3, DAG

THIS IS THE ALLERGIC TYPE OF HISTAMINE RECEPTOR
IP3 triggers release of Ca2+
DAG activates protein kinase C
H1 receptors found in (3)
Brain, Vascular Endothelium, Smooth Muscle
Major functinon of H2 receptors is to
Mediate Gastric acid secretion
H3 receptor function to provide
Feedback inhibition

Decrease Calcium influx
H4 receptors are localized to ___ cells and lead to decreased cAMP
Hematopoietic cells
Can mast cell degranulation occur as a response to a local tissue damage?
Fuckin right
3 strategies of histamine pharm. Name the example drugs
1. Administer inverse agonists, or competetive antagonists of histamine receptor - For Allergies
Diphenhydramine
2. Prevent Mast cell degranulation - Asthma
Cromolyn, Nedocromil
3. Administer physiologic antagonists to counter the pathologic effects of histamine - Anaphylaxis
Epinephrine
First/Second generation H1 antihistamines are neutral at physiologic pH and readily cross the BBB
First
First/Second generation H1 antihistamines are ionized at physiologic pH and don't cross the BBB
Second
(Loratadine, Ceterizine, Fexofanadine)
Two dx's that H1 antihistamines aren't effective for
Urticarial vasculitis, hereditary angiodema
H1 antihistamines should not be used as the sole therapy for
Asthma
H1 antihistamines reach peak plasma concentration in _ to _ hours and are metabolized by the...
2-3,, liver
____ a second gen. H1 antihist is metabolized by P450 into an active metabolite so inhibitors of P450 can affect the metabolism of it
Loratadine
Along with the fact that second gen H1 antihist's are ionized at phys. pH, what is another reason they don't readily cross the BBB?
The exhibit high binding to albumin and are thus less free to diffuse into the CNS
Two of the most commonly used H2 receptor antagonists
Cimetidine and Ranitidine
Common adverse effect of Cimetidine the H2 receptor antagonist
Inhibits Cytochrome P450 mediated drug metabolism
H3 receptor antagonists induce what
Wakefulness
Diphenhydramine
First gen. H1 antihistamine
Pyrilamine
First gen. H1 antihistamine
Doxepin
First gen. H1 antihistamine (tricyclic antidepressant for sad people)
Chlorpheniramine
First gen. H1 antihistamine
Promethazine
First gen. H1 antihistamine
Hydroxyzine
First gen. H1 antihistamine
Citerizine
2nd Gen. H1 Antihistamine
Acrivastine
2nd Gen. H1 Antihistamine2nd Gen. H1 Antihistamine
Azelastine
2nd Gen. H1 Antihistamine
Anything that ends in -dine
2nd Gen. H1 Antihistamine
Cimetidine, Famotidine, Nizatidine, Ranitidine
H2 receptor antagonist