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