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441 ex 5
NA
52
Agriculture
5th Grade
11/22/2009

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Term
Synthesis of Histamine
Definition
made in mastcells and basophils. Catalyzed by L-histidine decarboxylase from Histidine.
Term
Metabolism of histamine
Definition
N-methyl transferase, diamine oxidase, 5' phosphoribosyl transferase to imidazole acetic acid.
Term
h1 vs h2 rec effects of stimulation
Definition
H1= bronchoconst, vasodil, exudation H2= acid production in gut
Term
Histamine effect on respiratory system?
Definition
bronchoconstriction
Term
Histamine effect on Cardiovascular system?
Definition
vasodilation, endothelial cell contraction=exudation
Term
SE's of 1st gen H1 antags that are used as other therapeutic uses.
Definition
can cause sedation-anticholinergic effect (sleep aid) and antiemitic (N/V treatment), also local anesthetic (prometh)
Term
alternative places for histamine besides mast cells
Definition
neurotansm. In brain, found in fundus of stomach-acid secretion
Term
alternate release trigger of hist. other than mast cells
Definition
cytotoxic agents (venom) and various drugs (ex: morphine)
Term
Beta agonist affect on histamine release?
Definition
can inhibit antigen induced hist. release
Term
what is CRAC?
Definition
Ca release activated channels: in mast cell steps of degranulation, triggered by bunching of FceR's
Term
H1 receptor:
Definition
Gq GPCR, contracts smooth muscle, causes NO release=vasodilation
Term
H2 receptor:
Definition
Gs GPCR, in vascular SM causes relaxation (vasodil)
Term
H3 receptor:
Definition
in CNS, autoreceptor w hist as neurotransmitter
Term
H4 receptor:
Definition
on baso's, mast cells and eos's= histamine-induced chemotaxis
Term
Histamin effects on heart
Definition
moderate incr. in rate and force of contraction (H2 incr SA conduction, reflex tachy from vasodil)
Term
brompheniramine
Definition
alkylamine
Term
cyproheptadine
Definition
piperadine
Term
diphenhydramine
Definition
ethanolamine
Term
promthazine
Definition
phenothiazine
Term
hydroxyzine
Definition
piperazine
Term
pyrilamine
Definition
ethylenediamine
Term
reason why 2nd gen antihist don’t have as bad SE's
Definition
decreased lipid sol, and efflux from CNS by Pgp
Term
Acid secretion path
Definition
gastrin released and activates G(CCK-B) rec: 1) in ECL cell, this stim hist release to H2 rec on Parietal cell=camp= acid secr. 2) on parietal cell, activates acid secretion directly
Term
MOA of PPI's
Definition
accum in stomach b/c protonated in acid, irrev inhibits K/H antiporter, has S that reacts covalently w cystein in binding pocket (S-S bridge)
Term
What secretes acid in stomach:
Definition
K+/H+ antiporter in parietal cell, it is active so needs ATP
Term
High Capacity antacids
Definition
NaHCO3, Al(OH)3, Mg(OH)2 moderate = CaCO3
Term
Gaviscon?
Definition
OTC antacid w foaming action that helps protect GERD
Term
Sucralfate
Definition
mucosal protective agent- pg E1 derivative, enhances mucus and HCO3 secretion
Term
Metoclopramide (Reglan)
Definition
D2 antag= incr AcH release=incr GI motility and antiemetic effects
Term
Nerves that go from GI to Brain
Definition
Vagus and Splanchnic
Term
Alosetron (Lotronex)
Definition
5HT3 anatag= decr AcH from neurons in GI, Treats IBS+diarrhea in women, blocks afferent pain and decr motility
Term
Stimulant Laxatives
Definition
stim peristalsis (ECL cell stim)= opens ion channels to gut to draw in H2O
Term
Bulk and salin laxatives
Definition
hydrophobic mass that draws H2O in and distends GI= incr is peristalsis
Term
Stool Softeners
Definition
surfactants or lubricants to reduce fecal impaction and make BM easier
Term
MOA (2) of Anti-diarrheals
Definition
slow peristalsis to incr H2O and electrolyte reabs or adsorb potential toxins and water
Term
Opiates for antidiarrheal
Definition
no analgesic effect, bind in GI and decr peristalsis
Term
Kaopectate
Definition
kaloin+pectin= abs toxins and reduces peristalsis
Term
5HT3 antags and antiemesis
Definition
block activity in CTZ from vagal afferents from stomach and GI
Term
Estrogens/SERM
Definition
incr activity of osteoblasts, decr -clasts
Term
Calcitonin
Definition
(neg regulator of Ca) secreted by thyroid, inhib osteoclasts, incr Ca and PO4 loss in urine
Term
Vit D
Definition
1,25 dihydroxy Vit D3= incr Ca and PO4 abs from GI (TrpV6), inc Ca/PO4 reabs, feedback inhibition of PTH
Term
Bisphosphonates
Definition
mimic of inorganic P, incorporates into bone matrix, inhib osteoclast formation of cholesterol(FPPS)=decr activity--need to take 30 min prior to meal and remail upright for 30 min
Term
Teriparatide
Definition
PTH from e.coli dosed SC with Ca and Vit D= stim osteoblast activity= stim bone formation
Term
Cinacalcet
Definition
binds CaR's on parathyroid to inhib PTH release
Term
how is Ca stored in bone
Definition
hydroxyapatite (Ca Po4 OH) crystal
Term
PTH
Definition
maintains Ca conc.: incr Ca reabsorption fromcollecting tubules, Ca resorption from bone, inc Po4 loss in urine, inc Vit d3 prod in kidney,
Term
TrpV6
Definition
receptor on GI brush border cells made in response to Vit D3, Ca ion channel for abs
Term
Pagets Disease
Definition
uncontrolled osteoclast resorption and bad bone formation: leads to bone pain, bone deformities, loss of hearing(hyperCa), may be cause by virus
Term
Osteoperosis
Definition
more osteoclast act, decreased osteoblast=low bone mass
Term
kyphosis
Definition
from osteoperosis, ventral compression of vert= hunched over back
Term
Rickets
Definition
Vit D deficiency= bone deformities and hypocalcemia
Term
Osteoperosis bisphos
Definition
need a N to anchor to receptor better
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