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PHRM 825 Steroids Exam 2 > NSAIDS > Flashcards

NSAIDS Flashcards

1
Q

How is arachidonic acid released from the membrane?

A
  1. most abundant precursor of eicosanoids
  2. released from membrane phospholipids by phospholipase A2
  3. corticosteroids suppress this production
  4. essential fatty acid
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2
Q

What are eicosanoids?

A
  1. short- lived mediators
  2. bind to GPCRs
  3. dilation from Gs –> cAMP generated
  4. constriction from Gq –> calcium released
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3
Q

What do PGE2 do in the Blood vessels, platelets, bronchi, and uterus?

A

BV: dilation
Platelets: none
Bronchi: dilation
Uterus: oxytocic dilation

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4
Q

What do PGF2 do in the Blood vessels, platelets, bronchi, and uterus?

A

BV: constriction
Platelets: none
Bronchi: constriction
Uterus: oxytocic constriction

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5
Q

What do PGI2 do in the Blood vessels, platelets, bronchi, and uterus?

A

BV: dilation
Platelets: inhibits aggregation
Bronchi: none
Uterus: none

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6
Q

What do TXA2 do in the Blood vessels, platelets, bronchi, and uterus?

A

BV: constriction
Platelets: aggregation
Bronchi: none
Uterus: none

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7
Q

What are the end products of the COX pathway?

A
  1. prostaglandins
  2. thromboaxnes
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8
Q

what are the end products of the lipoxygenase pathway?

A
  1. HPETEs
  2. leukotrienes
  3. lipoxins
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9
Q

What are the roles of COX-1?

A
  1. expressed in various tissues
  2. housekeeping functions
    –> gastric cytoprotection
  3. PGH synthase-1
  4. inhibited by NSAIDs
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10
Q

What are the roles of COX-2?

A
  1. PGH synthase-2
  2. expressed upon stimulus in inflammatory/ immune cells
  3. stimulated by GFs, tumor promoters, and cytokines
  4. inhibited by NSAIDs
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11
Q

What are some prostaglandin drugs (eicosanoids)?

A
  1. alprostadil
  2. misoprostol
  3. latanoprost
  4. prostacyclin
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12
Q

what is alprostadil?

A
  1. PGE1
  2. relax smooth muscle and expand blood vessels
  3. used for ED by inj. or suppository
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13
Q

what is misoprostol?

A
  1. PGE1
  2. prevents peptic ulcer
  3. in combo with mifepristone it terminates pregnancy
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14
Q

what is latanoprost?

A
  1. PGF2a (prodrug)
  2. constrict blood vessels
  3. used for high pressure in the eye from glaucoma
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15
Q

what is prostacyclin?

A
  1. PGI2
  2. vasodilator
  3. inhibits platelet aggregation
  4. used to treat pulmonary arterial HTN by IV or inhalation
  5. not to be used with anticoags
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16
Q

what are the activities of NSAIDs?

A
  1. anti-inflammatory
  2. analgesic
  3. antipyretic
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17
Q

what are the mechanism of actions of NSAIDs?

A
  1. many NSAIDs inhibit both COX 1/2
  2. inhibition of prostaglandin endoperoxide H synthase (PGHS) catalyzes formation of prostaglandins
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18
Q

What is the mechanism of gastric bleeding caused by NSAIDs?

A
  1. severe
    – inhibition of platelet aggregation leads to increased risk of bleeding
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19
Q

What is the mechanism of inhibition of blood coag in aspirin?

A
  1. aspirin prolongs irreversible inhibition of COX-1 and consequent reduced formation of thromboxane
  2. not to be used b4 surgery
  3. can be used with cardiovascular disease to prevent
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20
Q

Describe Reye’s syndrome and why you need to be cautious in children?

A
  1. specific to aspirin
  2. rare, acute, and threatening and can have symptoms of vomiting, coma, delerium
    —> survivors can have head damage
  3. occurs in children previously exposed to flu or chicken pox
  4. not to be given in child less than 12 with fever
21
Q

What are the main interactions of NSAIDs?

A

anticoagulants or anything that increases GI bleeding and clotting

22
Q

What are the main classes of NSAIDs?

A
  1. salicylates
  2. arylacetic acids
  3. arylpropionic acids
  4. non-carboxylate NSAIDs
  5. COX-2 Selective NSAIDs
23
Q

what do salicylates look like?

24
Q

what do aryl propionic acids look like?

25
what do aryl acetic acids look like?
26
what do non-carboxylate NSAIDs look like?
27
what do COX-2 selective look like?
28
what is the role of the alpha-methyl group in arylpropionic acids?
it enhances activity and reduces side effects
29
What is the mechanism of action of acetaminophen?
it is not COX - it is a analgesic and anti-pyretic so it only works in CNS - inhibits peroxynitrite in PDH synthase activity and not arachidonic acid
30
what are the drugs that are prodrugs in NSAIDs?
1. latanoprost 2. sulindac 3. nabumetone
31
what is the structural basis for selective COX-2 inhibitors?
1. valine is substituted for isoleucine in binding site of COX-2 2. exploit larger NSAID binding site in COX-2 with larger/ rigid substituents
32
what is the mechanism of side effects in selective COX-2 inhibitors?
1. elevated BP and accelerated atherogenesis 2. increased cardiovascular hazard (HA, stroke) 3. important in PGI2 production but not TXA2 as this can lead to a rupture of thrombotic response in the atherosclerotic plague
33
describe aspirin
1. irreversibly inhibits COX 2. largely absorbed by intact form 3. blocks TXA increasing risk of bleeding and risk of MI
34
describe salsalate
1. dimer 2. does not cause GI bleeding 3. hydrolyzed to 2 salicylates in SI and absrobed
35
describe diflunisal
1. more potent analgesic 2. less antipyretic
36
describe indomethacin
1. most potent NSAID 2. not for LTU 3. not stable in solution and high risk of side effects
37
describe sulindac
1. prodrug 2. less GI effects 3. suitable for long term chronic inflammation
38
describe etodolac
1. potent like indomethacin 2. a little selective for COX-2 3. less GI bleeding 4. long term use for osteoarthritis
39
describe diclofenac
1. most widely used NSAID 2. as potent as indomethacin 3. somewhat selective for COX-2 4. inhibit COX and lipoxygenase pathway
40
describe ibuprofen
1. OTC analgesic 2. moderate gastric irritation 3. alpha-methyl 4. racemic mixture (S+ better)
41
describe naproxen
1. S+ enantiomer 2. more potnent than ibuprofen 3. moderate GI irritation 4. used for RA and OA
42
describe ketorolac
1. short term mod-severe pain 2. analgesic activity 3. narcotic alternativve
43
describe nabumetone
1. nonacidic prodrug 2. inhibitor of COX 3. minimum gastric side effects 4. potent anti-inflammatory but weak analgesic
44
describe meloxicam
1. intermediate resemblance in COX 2. long acting single daily dose 3. as potent as indomethacin 4. somewhat selective for COX-2
45
what drugs are salicylates?
1. aspirin 2. salicylic acid 3. salsalate 4. diflunisal
46
what drugs are arylacetic acids?
1. indomethacin 2. sulindac 3. etodolac 4. diclofenac
47
what drugs are arylpropionic acids?
1. ibuprofen 2. naproxen 3. ketorolac
48
what drugs are non-carboxylates?
1. nabumetone 2. meloxicam
49
what drug is a selective COX-2 inhibitor?
celecoxib

PHRM 825 Steroids Exam 2 (8 decks)

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