Smooth Muscle Prostaglandins Part 2 Flashcards
__________________ is a safe COX inhibitor for the elderly in small doses for prevention of MI and stroke
ASA
what med is safe to give the elderly PRN for fever, aches, and pains
tylenol; avoid ASA (other than for MI and stroke prevention)
____________________ is a major bioactive component of endothelial derived relaxing factor (EDRF) that causes vascular smooth muscle relaxation
NO
what are the endogenous effects of NO in the human body
- vasodilation 2. plt inhibitor 3. immune regulator 4. neurotransmitter
the synthesis and release of NO is regulated by ________________
endothelial ICF Ca (increased Ca in cytosol –> NO production)
increased stress on the vessel wall will cause increased synthesis of _____________
NO
substances that increase cytosolic calcium ( –> increased NO)
- Ach 2. bradykinin 3. catecholamines 4. substance P 5. ADP
MOA of NO
- VD via guanyl cyclase activation –> increase cGMP 2. inhibits plt aggregation 3. inhibits plt derived VC substances
NO is produced in what cells and tissues?
- leukocytes 2. fibroblasts 3. vascular smooth muscle
what are the 3 types of enzymes responsible for NO synthesis
- nNOS (NOS-1) : neuronal nitric oxide synthase 2. iNOS (NOS-2): inducible or macrophage NOS 3. eNOS (NOS-3): endothelial NOS
what triggers the release of nNOS (NOS-1, neuronal)
increased intracellular calcium
what triggers the release of iNOS (NOS-2, inducible/macrophage)
- triggered by inflammatory mediators 2. has constitutive activity
what triggers the release of eNOS (NOS-3, endothelial)
increased intracellular calcium
what are the 3 signaling mechanisms of NO
- metalloproteins 2. Thiols 3. tyrosine nitration
NO mediates its effects by _____________________ modification of proteins
covalent
NOS + ______________ –> NO
arginine
what is the primary approach to decreasing NO generation
NOS inhibitors
what is the structure/MOA of NOS inhibitors?
they are arginine analogues that bind to the NOS arginine binding site
most NOS inhibitors are __________________
non-selective
nNOS inhibition is useful with ____________________ disorders
neurodegenerative
iNOS inhibition is useful in _____________ & ________________ disorders
sepsis; inflammatory
T/F: there are no selective NOS inhibiting drugs
TRUE
eNOS inhibition will cause?
- vasoconstriction 2. ischemic damage
what medications are examples of Nitric Oxide donors?
- organic nitrates (NTG) 2. organic nitrites (amyl nitrite) 3. sodium nitroprusside 4. inyhaled NO 5. phosphodiesterase inhibitors
MOA of nitric oxide donor drugs
they are metabolized to release NO –> smM relaxation
which nitric oxide donor drug is an arterial and venous dilator with less effects on plt aggregation
organic nitrates (NTG)
which nitric oxide donating drugs exhibit tolerance with continuous administration
organic nitrate (NTG)
which nitric oxide donating drug is an arterial vasodilator only, require metabolic activation to elicit vasorelaxation, and do not exhibit tolerance
organic nitrites (amyl nitrite)
which nitric oxide donating drug is frequently abused for its euphoric effects
organic nitrites (amyl nitrite)
which nitric oxide donating drug dilates arterioles and venules, and is used to rapidly reduce arterial htn
sodium nitroprusside
which nitric oxide donating drug therapeutically reduces PA pressures and improves perfusion of ventilated lung areas
NO
which drug is used in the tx of pulmonary HTN, acute hyoxemia, and during cardiac arrest?
NO
if NO + O2 –> ____________, which is a pulmonary irritant that will decrease lung funciton
NO2
___________ can induce the formation of methemoglobin
NO
which Nitric oxide donating drug slows the degradation of cGMP and prolongs the effects of NO ?
PDE inhibitors (sildenafil)
describe how NO works to tx newborns with hypoxic respiratory failure d/t pulmonary htn
dilates pulmonary vessels –> 1. decreased PVR 2. decreased PA pressures 3. decreased V/Q mismatch
for induction of labor you ___________________ (ag/antag), PG____
agonize; PGE2
to maintain (keep open) a patent ductus arteriosus you _______________ (ag/antag), PG___________
agonize PGE2
for osteoarthritis, and rheumatoid arthritis, you ________________ (ag/antag) PG_____________
antagonize; PGE2
for induction of labor and glaucoma you _______________ (ag/antag) PG_____________
agonize, PGF2
for dysmenorrhea, you ________________ (ag/antag) the PG_____ and PG______
antagonize; PGE2; PGF2
for pulmonary HTN and organ transplant rejection you ______________ (ag/antag) PG___________
agonize; PGI2
for the tx of ED you would _________________ (ag/antag) PG____________
agonize; PGE1
for MI/stroke prevention you antagonize _________________, and/or agonize PG____, _________, __________
TXA2; PG12, E2, D2
albuterol has a max effect within ______-_________ min and has a DOA of _____-_____ hours
15-30; 3-4
