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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?

A
24
Q

what do aryl propionic acids look like?

A
25
Q

what do aryl acetic acids look like?

A
26
Q

what do non-carboxylate NSAIDs look like?

A
27
Q

what do COX-2 selective look like?

A
28
Q

what is the role of the alpha-methyl group in arylpropionic acids?

A

it enhances activity and reduces side effects

29
Q

What is the mechanism of action of acetaminophen?

A

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
Q

what are the drugs that are prodrugs in NSAIDs?

A
  1. latanoprost
  2. sulindac
  3. nabumetone
31
Q

what is the structural basis for selective COX-2 inhibitors?

A
  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
Q

what is the mechanism of side effects in selective COX-2 inhibitors?

A
  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
Q

describe aspirin

A
  1. irreversibly inhibits COX
  2. largely absorbed by intact form
  3. blocks TXA increasing risk of bleeding and risk of MI
34
Q

describe salsalate

A
  1. dimer
  2. does not cause GI bleeding
  3. hydrolyzed to 2 salicylates in SI and absrobed
35
Q

describe diflunisal

A
  1. more potent analgesic
  2. less antipyretic
36
Q

describe indomethacin

A
  1. most potent NSAID
  2. not for LTU
  3. not stable in solution and high risk of side effects
37
Q

describe sulindac

A
  1. prodrug
  2. less GI effects
  3. suitable for long term chronic inflammation
38
Q

describe etodolac

A
  1. potent like indomethacin
  2. a little selective for COX-2
  3. less GI bleeding
  4. long term use for osteoarthritis
39
Q

describe diclofenac

A
  1. most widely used NSAID
  2. as potent as indomethacin
  3. somewhat selective for COX-2
  4. inhibit COX and lipoxygenase pathway
40
Q

describe ibuprofen

A
  1. OTC analgesic
  2. moderate gastric irritation
  3. alpha-methyl
  4. racemic mixture (S+ better)
41
Q

describe naproxen

A
  1. S+ enantiomer
  2. more potnent than ibuprofen
  3. moderate GI irritation
  4. used for RA and OA
42
Q

describe ketorolac

A
  1. short term mod-severe pain
  2. analgesic activity
  3. narcotic alternativve
43
Q

describe nabumetone

A
  1. nonacidic prodrug
  2. inhibitor of COX
  3. minimum gastric side effects
  4. potent anti-inflammatory but weak analgesic
44
Q

describe meloxicam

A
  1. intermediate resemblance in COX
  2. long acting single daily dose
  3. as potent as indomethacin
  4. somewhat selective for COX-2
45
Q

what drugs are salicylates?

A
  1. aspirin
  2. salicylic acid
  3. salsalate
  4. diflunisal
46
Q

what drugs are arylacetic acids?

A
  1. indomethacin
  2. sulindac
  3. etodolac
  4. diclofenac
47
Q

what drugs are arylpropionic acids?

A
  1. ibuprofen
  2. naproxen
  3. ketorolac
48
Q

what drugs are non-carboxylates?

A
  1. nabumetone
  2. meloxicam
49
Q

what drug is a selective COX-2 inhibitor?

A

celecoxib

PHRM 825 Steroids Exam 2 (8 decks)

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