NSAIDs Flashcards

0
Q

What creates eicosanoids

A

Arachidonic acid

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1
Q

Eicosanoids examples

A

Prostaglandin
Leukotriene
Thromboxone
Prostacyclin

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2
Q

When are the eicosanoids synthesized

A

In response to various stimuli, tissue injury & immune response

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3
Q

Steps for inflammatory process

A
  1. Inflammatory response activates—-
  2. phospolipase (cell membrane or cytoplasm) release
  3. Arachidonic acid - esterized - Arachidonate metabolized to
    a. Lipooxygenase - leukotriens
    b. Cyclooxygenase - prostaglandin, prostacyclin, thrombaxane
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4
Q

What r corticosteroids

A

Anti inflammatory cause they inhibit phospolipase A2, reducing Arachidonate release

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5
Q

What leukotriens & lipoxins induce

A

Inflammation & asthmatic constriction of the bronchioles

5-Lipoxygenase (found in leukocyte) —5-HPETE —-leukotriens & lipoxins

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6
Q

What enzyme is in abundance in cancer cells & thought to have a role in producing vascular genesis needed for tumor to grow

A

Lipoxygenase

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7
Q

Which ones are involved with pathologic effects?

A

PGF2a, thrombaxane A2, & leukotriens

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8
Q

What comprises “slow reacting substance of anaphylaxis”

A

Leukotriens

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9
Q

What are some effects of eicosanoids

A
Protection of gastric mucosa,
Endogenous vasodilation
Smooth muscle relaxation
Labor
Maintaining latency of ductus arteriosus during development & platelet clotting
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10
Q

Where do effects of eicosanoids occur

A

Platelets, smooth muscle, CNS & other tissue

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11
Q

Waht is the molecule of the year

A

Nitric oxide

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12
Q

Nitric oxide

A

Messanger
Neurotransmitter
Expressed by inflammatory cells when activated by cytokines

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13
Q

What cells produce NO

A

Macrophages produce NO in combating bacteria

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14
Q

What are the result of NO

A

Vasodilation, increased vascular permeability, & PG release

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15
Q

What happens in the severe infection like sepsis with NO

A

Over production that leads to vasodilation

Also involved in platelet aggregation

16
Q

What do ASA and other no selective drugs inhibit

A

Inhibit all COX activity so prostaglandins needed for normal function are depleted

17
Q

Less effect on prostaglandins

A

COX 2 selective NSAIDs, example Celebrex

18
Q

What does cox 2 inhibitors block/use for

A

Pain
fever
Inflammation

19
Q

Effects of NSAIDs

A
  • Antipyretic
  • Analgesia
  • Anti inflammatory, no effect on tissue damage or immunologic response
  • Inhibition of platelet aggregation
20
Q

Pharmacokinetics of NSAIDs

A
  1. Low first pass extraction
  2. Highly protein bound,
  3. Low vd
  4. Weak organic acid
  5. Metabolized in liver CP 450, kidney some biliary
21
Q

What is the safest NSAID for renal pt

22
Q

What is the diagnostic test for coagulation issues with NSAIDs

A

Bleeding time NOT platelet count

23
Q

Can u reverse ASA

A

NO, effects last life of the platelet 7-10 d
Other NSAIDs can be reverse

ASA nonselective COX inhibition

24
Cardiovascular effects of NSAIDs
COX 2 inhibitors are ass with inc risk of stroke & MI Cox 2 - protective affect of estrogen in preventing plaque & sclerosis.
25
Drug interactions of NSAIDs
NSAIDs + 1. Anticoagulants = incr risk of bleeding 2. K sparing diuretics = hyperkalemia 3. Decreased effect of HTN meds 4. Antidepressants - decrease lithium levels, interfere w/SSRIs
26
Do opiates or NSAIDs have ceiling effect
NSAIDs
27
What is ASA hydrolyzed to
Salicylate in GI, an active enzyme
28
Is ASA reversible | Safe for what pt population
NO, life of the platelets 7-10 days | Renal, nonselective COX inhibitor
29
How is the absorption of NSAIDs effected
Decreased by: presence of food & increased ph ( inc ionization)
30
What is the magic drug
Acetylsalicylic acid derived from acetylation of salicylic acid ASA
31
What is the 1/2 life of ASA & salicylic acid
ASA is 15-20 min | Salicylic acid 2-3 hrs, prolong effect of ASA
32
ASA use
1. Pain 2. Antipyretic 3. Antiplatelet 4. Angina & acute MI
33
Which med has correlation with Reye's syndrome
ASA
34
ASA doses
1. Low dose: Antiplatelet 2400 mg/day
35
Ofirmev doses
1000 mg q6 hr. or 650 mg q 4 hrs MAX 4 g/day Give infusion over 15 min 100 ml amp, 10 mg/ml
36
When is Tordol contraindicated, what pt
1. L&D due to adverse effect on fetal circulation & inhibition of contraction 2. Present in breast milk 3. Not for epidural/intrathecal us
37
Ketorolac doses
Onset: 65 y.old
38
Does tordol have ceiling effect
Yes, just like all NSAIDs No effect on MAC