Smooth Muscle Prostaglandins Part 2 Flashcards

1
Q

__________________ is a safe COX inhibitor for the elderly in small doses for prevention of MI and stroke

A

ASA

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2
Q

what med is safe to give the elderly PRN for fever, aches, and pains

A

tylenol; avoid ASA (other than for MI and stroke prevention)

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3
Q

____________________ is a major bioactive component of endothelial derived relaxing factor (EDRF) that causes vascular smooth muscle relaxation

A

NO

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4
Q

what are the endogenous effects of NO in the human body

A
  1. vasodilation 2. plt inhibitor 3. immune regulator 4. neurotransmitter
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5
Q

the synthesis and release of NO is regulated by ________________

A

endothelial ICF Ca (increased Ca in cytosol –> NO production)

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6
Q

increased stress on the vessel wall will cause increased synthesis of _____________

A

NO

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7
Q

substances that increase cytosolic calcium ( –> increased NO)

A
  1. Ach 2. bradykinin 3. catecholamines 4. substance P 5. ADP
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8
Q

MOA of NO

A
  1. VD via guanyl cyclase activation –> increase cGMP 2. inhibits plt aggregation 3. inhibits plt derived VC substances
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9
Q

NO is produced in what cells and tissues?

A
  1. leukocytes 2. fibroblasts 3. vascular smooth muscle
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10
Q

what are the 3 types of enzymes responsible for NO synthesis

A
  1. nNOS (NOS-1) : neuronal nitric oxide synthase 2. iNOS (NOS-2): inducible or macrophage NOS 3. eNOS (NOS-3): endothelial NOS
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11
Q

what triggers the release of nNOS (NOS-1, neuronal)

A

increased intracellular calcium

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12
Q

what triggers the release of iNOS (NOS-2, inducible/macrophage)

A
  1. triggered by inflammatory mediators 2. has constitutive activity
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13
Q

what triggers the release of eNOS (NOS-3, endothelial)

A

increased intracellular calcium

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14
Q

what are the 3 signaling mechanisms of NO

A
  1. metalloproteins 2. Thiols 3. tyrosine nitration
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15
Q

NO mediates its effects by _____________________ modification of proteins

A

covalent

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16
Q

NOS + ______________ –> NO

A

arginine

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17
Q

what is the primary approach to decreasing NO generation

A

NOS inhibitors

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18
Q

what is the structure/MOA of NOS inhibitors?

A

they are arginine analogues that bind to the NOS arginine binding site

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19
Q

most NOS inhibitors are __________________

A

non-selective

20
Q

nNOS inhibition is useful with ____________________ disorders

A

neurodegenerative

21
Q

iNOS inhibition is useful in _____________ & ________________ disorders

A

sepsis; inflammatory

22
Q

T/F: there are no selective NOS inhibiting drugs

A

TRUE

23
Q

eNOS inhibition will cause?

A
  1. vasoconstriction 2. ischemic damage
24
Q

what medications are examples of Nitric Oxide donors?

A
  1. organic nitrates (NTG) 2. organic nitrites (amyl nitrite) 3. sodium nitroprusside 4. inyhaled NO 5. phosphodiesterase inhibitors
25
Q

MOA of nitric oxide donor drugs

A

they are metabolized to release NO –> smM relaxation

26
Q

which nitric oxide donor drug is an arterial and venous dilator with less effects on plt aggregation

A

organic nitrates (NTG)

27
Q

which nitric oxide donating drugs exhibit tolerance with continuous administration

A

organic nitrate (NTG)

28
Q

which nitric oxide donating drug is an arterial vasodilator only, require metabolic activation to elicit vasorelaxation, and do not exhibit tolerance

A

organic nitrites (amyl nitrite)

29
Q

which nitric oxide donating drug is frequently abused for its euphoric effects

A

organic nitrites (amyl nitrite)

30
Q

which nitric oxide donating drug dilates arterioles and venules, and is used to rapidly reduce arterial htn

A

sodium nitroprusside

31
Q

which nitric oxide donating drug therapeutically reduces PA pressures and improves perfusion of ventilated lung areas

A

NO

32
Q

which drug is used in the tx of pulmonary HTN, acute hyoxemia, and during cardiac arrest?

A

NO

33
Q

if NO + O2 –> ____________, which is a pulmonary irritant that will decrease lung funciton

A

NO2

34
Q

___________ can induce the formation of methemoglobin

A

NO

35
Q

which Nitric oxide donating drug slows the degradation of cGMP and prolongs the effects of NO ?

A

PDE inhibitors (sildenafil)

36
Q

describe how NO works to tx newborns with hypoxic respiratory failure d/t pulmonary htn

A

dilates pulmonary vessels –> 1. decreased PVR 2. decreased PA pressures 3. decreased V/Q mismatch

37
Q

for induction of labor you ___________________ (ag/antag), PG____

A

agonize; PGE2

38
Q

to maintain (keep open) a patent ductus arteriosus you _______________ (ag/antag), PG___________

A

agonize PGE2

39
Q

for osteoarthritis, and rheumatoid arthritis, you ________________ (ag/antag) PG_____________

A

antagonize; PGE2

40
Q

for induction of labor and glaucoma you _______________ (ag/antag) PG_____________

A

agonize, PGF2

41
Q

for dysmenorrhea, you ________________ (ag/antag) the PG_____ and PG______

A

antagonize; PGE2; PGF2

42
Q

for pulmonary HTN and organ transplant rejection you ______________ (ag/antag) PG___________

A

agonize; PGI2

43
Q

for the tx of ED you would _________________ (ag/antag) PG____________

A

agonize; PGE1

44
Q

for MI/stroke prevention you antagonize _________________, and/or agonize PG____, _________, __________

A

TXA2; PG12, E2, D2

45
Q

albuterol has a max effect within ______-_________ min and has a DOA of _____-_____ hours

A

15-30; 3-4