lecture 2 Flashcards
cortisol affinity for GC and MC?
equal
cortisone affinity for GC and MC?
low affinity for MC
cortisol converted to cortisone where?
kidney, salivary gland, and colon
mechanism of action of glucocorticoids?
increased synthesis of phospholipase A2 inhibitor, increased synthesis of NF-Kb inhibitor, decreased synthesis of adhesion factors
what is lipocortin?
inhibitor of phospholipase A2
immunosuppresive effects of GC?
Inhibition of macrophage activity Inhibition of cytokine secretion by macrophages and T cells Interleukins 1-6,8 TNFα Cell adhesion factors Inhibition of T and B cell replication Decreased IgG production
advantages of synthetic steroids?
longer half life, and more selective
dexamethasone and prednisone are selective for what?
GC
fludrocortisone is selective for what?
MC
three reasons to use GC?
replacement therapy, anti inflammatory, and immunosuppressant effects
if someone has acute adrenal insufficiency, what do you give?
high doses of hydrocortisone
if someone has chronic adrenal insufficiency, what do you give?
physiologic doses of hydrocortisone and fludrocortisone
stress, illness, surgery and co administration of CYP450 all reason for what?
to increase GC
is prolonged treatment of GC safe?
no
abrupt termination of what can cause life threatening problems?
GC
3 important adverse effects of gc?
infection, impaired wound healing, and osetoporosis
what is cushing syndrome?
too much GC, from tumor of pituitary or adrenal
ways to reduce risk of GC toxicity?
local administration, avoid prolonged use, taper withdrawal.
why would you want to use slow release capsules with high first pass effect of GC?
IBD
what is cyclosporine?
immunosuppressant, prevent organ rejection, causes gingival hyperplasia, inhibits cyp450’s
what is a calcinuerin inhibitor? leading to blocking T cell signaling for growth
cyclosporine
abatacept approved for what?
RA
IgG1 like protein that binds to Antigen-Presenting Cell (APC) and prevents T cell activation
abatacept
Abatacept inhibits the binding of ____ (CD80/CD86) to CD28 and T cell activation
B7
histamine is released from what?
mast cells and basophils
diphenhydramine is what type of histamine receptor antagonist?
H1
ranitidine is what type of histamine receptor antagonist?
H2
H1 receptor uses what has second messenger?
IP3/DAG–> calcium
H2 receptor uses what as second messenger?
CAMP
increased venule permeability, dilation of arteriole and venules, NO release, smooth muscle constriction, stimulation of sensory nerve endings, and CNS arousal are all part of which histamine receptor?
H1
red spot from histamine injection for what?
vasodilation
wheal from histamine injection for what?
increase vascular permeability
flare of histamine injection due to what?
atonally mediated reflex vasodilation
diphenhydramine is what?
H1 receptor antagonist, 1st generation
Loratadine is what?
H1 antagonist, 2nd generation
1st generation antihistamines has high selectivity for which receptor?
H1, with weak selectivity vs other receptors
does 1st generations have access to CNS?
yes-sedative effect
effects of 1st generation?
local anesthetic activity, antimuscarinic activity, alpha adrenergic antagonism
toxicity of 1st generation are ______ like?
atropine
advantages of 2nd generation?
higher selectivity of H1 vs other receptors, less side effects, polarity limits CNS access
toxicity of some older 2nd generation drugs from what?
inhibition of K+ channel in the heart
three major pathways regulate hydrogen secretion:
endocrine stimulation via gastrin release from antral cells, neural stimulation via Ach from enteric nerves, paracrine stimulation by histamine from ECL cells
which histidine receptors are in the GI?
H2
ranitidine is what kind of drug?
h2 antagonist
omeprazole is what kind of drug?
proton pump inhibitor
PPI act on what?
H, K-ATPase in apical membrane
when should PPI’s be taken?
before breakfast
which drugs are formulated with enteric coating for release and absorption in duodenum?
PPis
what is zollinger ellison syndrome?
hypersecretory conditions PPIs
what is the drug of choice for upper GI?
PPIs
side effects of PPi?
drug interactions, inhibition of CYP450
Mg antacid can cause what?
constipation
Al antacid can cause what?
DIARRHEA
treatment for H. pylori
PPI, clarithromycin, metronidazole or amoxicillin
laxatives counteract effect of what?
opioids and ca channel antagonists
bulk forming laxatives are what
cellulose based substitutes for dietary fiber
salts of mg or phosphate ions, and polyethylene glycol are examples of what?
osmotic agents
loperamide is what?
nonspecific antidiarrheal agent. opioid agonist. schedule V drug
albuterol is what kind of drug?
beta 2 receptor adrenergic agonist
what is important for acute management of asthmaticc attack or hypersensitivity rxn
albuterol
albuterol is it long or short acting?
short
salmeterol is it short or long acting?
long
methylxanthines and anticholingerics do what?
bronchodilate
leukotriene inhibitors have what 2 effects?
bronchodilation and anti-inflammatory
ipratropium is what?
anticholinergic for bronchodilation
exacerbating drugs in patients with pulmonary conditions
NSAIDS, OPIOIDS, AND NON SELECTIVE BETA BLOCKERS
