AUTACOIDS Flashcards
drugs with important actions on smooth msucle
autacoids
Autacoids include:
H,S,V,M
histamine
serotonin
vasoactive peptides
membrane phospholipids
________- are derived from plants as well as in animal tissues and a component of some venoms and stinging secretions
histamine
histamine is formed by decarboxylation of the amino acid _______, a reaction catalyzed by the enzyme _______
L-histidine
Pyridoxal PO4 dependent L-Histidine Decarboxylase
most tissue histamine is sequestered and bound in (vesicles) in __________
mast cells
2 pathways of histamine metabolism
D,M
deamination
methylation
deamination of histamine
small intestine, liver, kidney, and monocytes
_____ by 9-11%
imidazole acetic acid
methylation of histamine
small intestine, liver, skin, kidney, thymus, and leukocytes
______ by 42-47%
principal urinary metabolite
______ by 4-8%
_______by 2-3%
imidazole acetic acid
n-methylhistamine
histamine
4 HISTAMINE RECEPTORS
predominant in endotracheal and smooth muscle
H1
4 HISTAMINE RECEPTORS
Facial veins, carotid art., pulmonary art., heart, gastric mucosa, smooth muscle and some immune cells
H2
4 HISTAMINE RECEPTORS
several areas in CNS
decreases transmitter release from histaminergic and other neurons
presynaptic
H3
4 HISTAMINE RECEPTORS
eosinophils, neutrophils CD4 T Cells, inflammation and allergy
H4
3 STAGES of TRIPPLE RESPONSE
red spot
flare response
edema
Histamine antagonists
Physiological: __________
Release Inhibitors which reduces mast cell degranulation: _______
Histamine Receptor Antagonists: ________
epinephrine
Cromolyn Na, Nedocromil
H1 receptor antagonists
H2 receptor antagonists for peptic disorder
burimamide
H1 RECEPTOR ANTAGONISTS: PHARMACOKINETICS
well absorbed from GIT (oral)
onset 30 minutes
duration 4-6 hrs
1st generation agents