Autacoids (Histamine, Serotonin, Ergot) Flashcards
histamine is synthesized form what AA?
Histidine
what enzyme converts Histidine to Histamine
Histidine Decarboxylase
Histamine in mast cell is inactive in a complex with?
proteases
heparan sulfate
chondroitin sulfate
most histamine are contained in what type of cells? (2)
Mast cell
Basophil
histamine not in cell is found in what tissues and functions as what
Brain, Stimach
Neurotransmitter, neuromodulator, neuroendocrine control, cardiovascular regulation.thermal & body weight regulator, sleep & arousal
2nd most important site of histamine storage
Enterochromaffin like-cells(ECL cells)
functions of histamine released by Enterochromaffin like-cells(ECL cells)
activate parietal cells to produce HCl
immunologic release of histamine is mediated by
IgE
what mode of release: displaces histamine from the heparin-protien complex within cells
Chemical & Mechanical release (drugs and alcohol)
the type of histamine receptor subtypes
G-protein coupled receptors
distribution of H1 receptors
Endothelium Brain Smooth muscle
what is the triple response?
mediated through H1 receptor:
Red spot (vessel dilation)
Edematous
Wheal and flare
distribution of H2 receptors
Gastric mucosa
Cardiac muscle
Mast cell
effects of H2 stimulation
Gastric acid sceretion
Increase SA nodal rate
(+) Inotropism
Presynaptic AUTORECEPTORS & heteroceptors in the brain, myenteric plexus
H3 receptors
functions of H3 receptor stimulation
Feedback inhibitions
Neurotransmitters
distribution of H4 receptors
Eosinophils, neutrophils, CD4 and T cells
function of H4 stimulation
Chemotactic response
General Histamine Antagonists (and action)
Epi: physiologic antagonist
Cromolyn & Nedocromil: release inhibitors
Buramide: receptor antagonist (H2)
types of H1 antagonists
1st generation (sedating) 2nd generation (less sedating)
converts the 2nd generation H1 antagonists to active form
CYP3a4 isozyme
H1 antagonists: Allergic reaction
Diphenhydramine (atopic dermatitis)
H1 antagonists: Motion sickness & Vestibular DO
Scopalamine
Dimenhydrinate
H1 antagonists: Nausea and Vomiting in Pregnancy
Bedectin
Doxylamine
H1 antagonists: Anti parkinsonism
Diphenhydramine
H1 antagonists: Anti cholinoceptor
Ethanolamine
Ethylenediamine