08.21 - Histamine (Sweatman) - Questions Flashcards
2 major sites of Histamine Biosynthesis
Mast Cells, Basophils
Enzyme that catalyzes Histamine Biosynthesis
L-Histidine Decarboxylase
3 Notable Activators of Histamine Synthesis and Release
GM-CSF, IL-3, Peptides
2 Notable inhibitors of Histmaine Synthesis and Release
Beta-antagonists; Cromolyn
3 Notable Histamine Activating Factors
Gastrin, Ca2+, Vancomycin
Ig isotype that causes Histamine
IgE
Cytokine that stimulates B cell to produce IgE
IL-4
Cytokine that stimulates TH1 to release IFN-g
IL-12
Release of histamine from granule matrix occurs by __ exchange
Cation
What percent of Mast Cell Granule does Histamine compose?
10%
Major actions of H1 receptors
SM contraction; Stim of NO formation; Endothelial cell contraction; Incr vascular permeability
Major actions of H2 receptors
Simulation of gastric acid secretion
Major actions of H3 receptors
Inhibition of NT release
Mediator of H2 signaling
AC –> cAMP –> Decr Ca2+, SIRS, PG –> Extracellular
Mediator of H1 signaling
GD –> cGMP –> PG, EDRF –> Extracellular
Histamine receptors in lung
H1 - Bronchoconstrict; H2 - Bronchodilation
Histamine receptors in heart
H1 - Slow AV conduction; H2 - Enhanced constraction
Histamine receptors in vasculature
H1, H2 - Microvasodilation; H1 - Permeability, Vasoconstriction
Histamine receptors in neural tissue
H1, H3 - Nerve ending stim, wakefullness and sedation
Histamine effects on capillaries
No effect
Histamine effects on venules
H1 - Rapid onset short term dilation (cap permeability); H2 - Slow onset persisent dilation
Histamine effects on Veins
H1 - Constriction of SM, Dilation of Endo; H2 - Dilation of SM
Histamine effects on Arteries
H1 - Constriction of SM, Dilation of Endo; H2 - Dilation of SM
Histamine effects on Arterioles
H1 - Rapid onset short term dilation; H2 - Slow onset persistent dilation
Effect of Mast Cells and Basophils on Mucus Glands
Diarrhea, Rhinorrhea, Bronchial secretion
Effect of Mast Cells/Basophils on Sensory Nerves
Itching
Advantages of Second Gen Anti-histamines
Longer, Fewer doses, Non-sedating, Limited anti-cholinergic
3 Notable Side Effects of 1st Gen H1-Antags
Impaired cognition, Dystonia, Nasal Congestion
1st gen with highest anti-cholinergic
Phenothiazines (promethazine)
1st gen with highest sedative effect
Phenothiazines (promethazine)
H1 blocker that acts on alpha-adrenergic
Promethazine
H1 blockers that act on Cholinergic receptors
Diphenhydramine, Promethazine
Experimental application of 2nd gen H1 blocker
Asthma
Side effects of 2nd gen H1 antagonists
Mild Cognitive Disturbance; Appetite stimulation
For what 2 applications are 1st gens better than 2nd
Atopic Dermatitis, Itching Dermatosis
For what 4 applications are only 1st gens effective (over 2nd)
Motion sickness, Antiemetic, Appetite Stimulation, Insomia
H4 receptor function
Hematopoeitic Cells: Mast Cell-dependent recruitment of neutrophils during inflammation
Locations of H1 receptors other than SM and Endothelium
Adrenal Medulla, Heart, CNS
Locations of H3 receptors
CNS, PNS, Endothelium, Enterochromaffin cells
Effect of H1 on Heart
Slowed AV conduction
Effect of H2 on Heart
Enhanced contraction
Effect of H1 on Lungs
Bronchoconstriction
Effect of H2 on Lungs
Bronchodilation
Effect of H1 on Neural Tissue
Nerve ending stimulation; Wakefullness and Sedation
Effect of H1 on Vasculature
Microvasodilation, Cap Permeability, Vasoconstriction
1st Gen H1 Antagonists
Diphenhydramine, Dimenhydrinate, Promethazine
2nd Gen H1 Antagonists
Fexofenadine, Cetirizine, Loratidine