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Exam 2: Analgesics NSAIDS Flashcards

1
Q

What are the properties of NSAIDs?

A

Analgesic, Anti-inflammatory, Anti-pyretic

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2
Q

What conditions are NSAIDs used to treat?

A

Pain and inflammation, Surgical procedures, Inflammatory diseases (Osteoarthritis and rheumatoid arthritis), Migraine, Dysmenorrhea, Myalgia, Dental pain

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3
Q

What are NSAIDs originally derived from?

A

NSAIDs are originally derived from natural sources such as the bark of the willow tree, Salix alba.

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4
Q

What compounds do these plants contain for NSAIDS?

A

These plants contain derivatives of salicylic acid and were used to treat pain and fever.

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5
Q

Claims of being able to ‘cure’ _____________ using NSAIDS were first published in 1876.

A

rheumatic disorders

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6
Q

What is the mechanism of action of NSAIDs?

A

The mechanism of action was first described in 1971 as the inhibition of the enzyme cyclo-oxygenase (COX) thus preventing the synthesis of prostaglandins.

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7
Q

What does NSAIDs mean?

A

NSAIDs are nonsteroidal anti-inflammatory drugs.

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8
Q

What are the two isoforms of COX?

A

The two isoforms of COX are COX-1 and COX-2.

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9
Q

What induces COX-2?

A

COX-2 is induced by cellular cytokines in localized areas of injury and in the spinal cord in response to tissue damage.

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10
Q

Where is COX-1 expressed?

A

COX-1 is expressed in low levels in many tissues, including lung, liver, spleen, kidney, and stomach.

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11
Q

What is the role of COX-1?

A

COX-1 is responsible for maintaining homeostasis.

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12
Q

What type of isoforms are conventional NSAIDs?

A

Conventional NSAIDs are non-specific inhibitors of both isoforms.

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13
Q

What actions do conventional NSAIDs provide?

A

They provide analgesia and anti-inflammatory action. They affect platelet function and protection of the gastric mucosa.

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14
Q

What are COX-2 inhibitors thought to have?

A

A more favorable side effect profile since they spare the COX-1 isoform.

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15
Q

What is nociception?

A

Nociception refers to the detection of extremes of temperature, painful mechanical stimuli, and noxious chemical stimuli by primary afferent neurons.

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16
Q

Where do primary afferent neurons terminate?

A

They terminate in the dorsal horn of the spinal cord, with their cell bodies located within the dorsal root ganglia.

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17
Q

What triggers the production of prostaglandins?

A

The inflammatory process triggers COX to produce prostaglandins.

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18
Q

What is the effect of prostaglandins on nociceptive neurons?

A

Prostaglandins increase the sensitivity of nociceptive neurons to bradykinin, histamine, serotonin, and other mechanical, chemical, and thermal stimuli.

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19
Q

What is released from membrane phospholipids?

A

Arachidonate is released from membrane phospholipids in response to a variety of stimuli.

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20
Q

What does COX oxidize arachidonate to?

A

COX oxidizes arachidonate to PGG2.

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21
Q

What is PGG2 further oxidized to?

A

PGG2 is further oxidized to PGH2.

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22
Q

What are Prostaglandins and Thromboxanes produced from?

A

They are produced from PGH2.

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23
Q

Which cells produce Prostaglandin D2 (PGD2)?

A

Mast cells produce PGD2.

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24
Q

Where is COX-1 distributed?

A

COX-1 is distributed in the GI tract, platelet, kidney, and most other tissues.

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25
Where is COX-2 distributed in the body?
COX-2 is distributed in inflammatory cells, the female reproductive tract, the brain, the kidney, and cancer cells.
26
What cytokines respond to COX-2 in inflammatory cells?
COX-2 in inflammatory cells responds to cytokines such as interleukin-1 and tumor necrosis factor-alpha.
27
What type of inhibitors is Ibuprofen? What is the recommended dose that Dave mentioned?
Ibuprofen is a competitive, reversible inhibitor. The recommended dosage for analgesia and anti-inflammatory effects is 600-800mg.
28
What type of inhibitor is Indomethacin?
Indomethacin is a time-dependent inhibitor.
29
What type of inhibitor is Naproxen?
Naproxen is a mixed kinetic inhibitor, known for being kind and gentle even at high doses.
30
What type of inhibitor is Aspirin?
Aspirin is an irreversible inhibitor that binds to COX1, affecting platelets.
31
How long should Aspirin be held before surgery?
Aspirin should be held for a minimum of 7 days to 2 weeks before surgery.
32
What should be considered when holding Aspirin for patients with recent stents?
Do not hold Aspirin for recent stents to avoid occluding a new stent; the decision depends on contraindications and the current patient status.
33
How are NSAIDs absorbed?
NSAIDs are rapidly and well absorbed from the GI tract.
34
How are NSAIDs distributed? Protein bound?
NSAIDs are highly protein bound and found within most tissues, including synovial fluid and CSF.
35
What is the significance of NSAID distribution?
NSAID distribution allows them to enter joint space and address inflammation in conditions like osteoarthritis.
36
What are common NSAIDs used in orthopedics?
Commonly used NSAIDs in orthopedics include Toradol, morphine, and benzocaine.
37
How do NSAIDs metabolize?
NSAID metabolism varies greatly, from non-specific esterases to complex hepatic pathways.
38
How are NSAIDs excreted?
Excretion of NSAIDs is primarily renal.
39
Name some COX-2 inhibitors
COX-2 inhibitors include Celebrex (celecoxib), Vioxx (rofecoxib), and Bextra (valdecoxib).
40
How do COX-2 inhibitors physical properties differ from other NSAIDs?
They differ in physical properties as they are highly lipophilic, neutral, nonacidic molecules with limited aqueous solubility.
41
What is parecoxib?
Parecoxib is a COX-2 Inhbitors/ a water-soluble pro-drug of valdecoxib and may be available soon for IV or IM administration.
42
What are the risks associated with NSAIDs?
Increased bleeding risks, including prolonged postoperative bleeding and upper GI bleeding. Care should be exercised when coadministered with other anticoagulants (e.g., coumadin). ## Footnote COX-2 inhibitors have much less interaction with anticoagulants.
43
What is the risk of renal injury with NSAIDs?
Increased risk of renal injury secondary to blockade of renal protectant prostaglandins. COX-2 inhibitors have a reduced risk for renal insufficiency, but the risk is still present. ## Footnote COX-2 inhibitors have a reduced risk for renal insufficiency.
44
What cardiovascular effects are related to NSAIDs?
Cardiovascular effects, including hypertension and edema, are related to decreased renal function in most cases. The overall cardiac safety of COX-2 inhibitors is uncertain. ## Footnote The overall cardiac safety of COX-2 inhibitors is uncertain.
45
How do NSAIDs affect patients with hepatic and renal disease?
Patients with hepatic and renal disease may have difficulty in metabolizing and excreting these agents.
46
What is the gold standard for NSAIDs?
Tordaol is the gold standard.
47
What role do NSAIDs play in post-surgical regimens?
NSAIDs are an important element in balanced multimodal post-surgical regimens, often combined with opioids, and may serve as an alternative to opiates in minor surgical procedures.
48
What is notable about Ketorolac among NSAIDs?
Ketorolac is one of the more potent NSAIDs and has been shown to be a more effective analgesic in surgical models compared to other NSAIDs. Its parenteral availability makes it more practical than other NSAIDs.
49
What are the benefits of preoperative administration of NSAIDs?
Preoperative administration of NSAIDs may have benefits compared to postoperative administration.
50
What is a risk associated with pre-emptive dosing of NSAIDs?
Pre-emptive dosing of NSAIDs may increase the risk of bleeding complications.
51
What is the effect of adding NSAIDs to a post-operative regimen? What can it reduce?
NSAIDs prolong the duration of relief as their half-lives are longer than opiates and may reduce post-operative nausea and vomiting since less post-op analgesics are required.
52
What are the benefits of NSAIDs compared to opiates post-operatively?
NSAIDs produce much less sedation, impaired respiratory function, sleep disturbances, ileus/constipation, and urinary retention.
53
What is the IM dosing for Ketorolac?
60 mg IM
54
What is the IV/IM dosing for ketoralac for patients under 65 years of age?
30 mg IV/IM q6h
55
What is the IV/IM dosing for ketoralac for patients 65 years of age and older?
15 mg IV/IM q6h
56
What is the maximum amount of Ketorolac that can be administered within 24 hours for patients under 65 years of age?
120 mg/24 hours
57
What is the maximum amount of Ketorolac that can be administered within 24 hours for patients 65 years of age and older?
60 mg/24 hours
58
Are loading doses of Ketorolac generally necessary?
No, loading doses are generally unnecessary. Loading doses reduce the amount that can be administered within a 24 hour period
59
What is the maximum oral dose of Ketorolac per day?
40 mg/day (10 mg po q6h)
60
What is the risk associated with ketorolac use?
Increased risk of GI ulceration and major bleeding episodes.
61
How long should ketorolac use be limited to?
Ketorolac use should be limited to 5 days.
62
What is the response to specific NSAIDs?
Response to specific NSAIDs is highly patient specific.
63
What is the analgesic/anti-inflammatory dose of Aspirin total per day?
3 grams per day.
64
What are the cardioprotective doses of Aspirin?
81-325 mg per day. 162 mg seems to be the new 'in' dose.
65
What is the recommended dosage range of Diclofenac?
75-150 mg/day in divided doses.
66
What is the analgesic dose of Ibuprofen?
200-400 mg po q4-6 hours.
67
What is the anti-inflammatory dose of Ibuprofen?
400-800 mg po q6 hours.
68
What is the recommended dosage of Naproxen?
250-375 mg twice daily up to 375-750 mg twice daily.
69
What is the dosing for Celecoxib?
Celecoxib is dosed at 100-200 mg twice daily. Higher doses are used for rheumatoid arthritis (RA).
70
What are the Contraindications/Precautions for NSAIDS?
– History of hypersensitivity to NSAIDs (Samter’s Triad) – Bleeding complications – GI disease – Elderly patients – Children (Reye syndrome: melts liver; febrile + viral (skin)) – Congestive heart failure (Reduced EF is a problem) – Hepatic impairment – Renal impairment – Hypertension – Drugs--multiple NSAIDs (DONT DOUBLE DOSE; lose Cox activity) , probenecid, pentoxifylline, lithium, or anticoagulant therapy.
71
What is Samter’s Triad also known as?
Samter’s Triad is also known as Aspirin-Exacerbated Respiratory Disease (AERD).
72
What are the three key symptoms of Samter’s Triad?
The three key symptoms are: 1. Aspirin (or NSAID) Sensitivity, 2. Chronic Rhinosinusitis with Nasal Polyps, 3. Asthma.
73
What is Aspirin (or NSAID) Sensitivity in Samter’s Triad?
People with Samter’s Triad experience worsening respiratory symptoms when taking aspirin or other nonsteroidal anti-inflammatory drugs (NSAIDs).
74
What is Chronic Rhinosinusitis with Nasal Polyps?
It is persistent sinus inflammation and nasal polyps that can cause congestion and loss of smell.
75
What characterizes the asthma associated with Samter’s Triad?
The asthma is often severe and difficult to control, with frequent flare-ups.
76
What type of disorder is Samter’s Triad?
It is an inflammatory disorder where the body reacts abnormally to aspirin and NSAIDs, leading to severe respiratory symptoms.
77
What is the typical treatment for Samter’s Triad?
Treatment typically includes avoiding NSAIDs, using corticosteroids or biologic therapies, and in some cases, undergoing aspirin desensitization therapy under medical supervision.
78
Why is acetaminophen used for in osteoarthritis?
It is recommended to start with acetaminophen as it is better for analgesia.
79
What are the properties of acetaminophen?
It is an effective analgesic and antipyretic, but lacks anti-inflammatory properties.
80
How does acetaminophen interact with opioids?
It acts synergistically as an analgesic with other opioids and may decrease the necessary dose of opioid.
81
What is the maximum daily dosage of acetaminophen?
No more than 4 grams per day to prevent hepatotoxicity associated with glutathione depletion.
82
What should be considered regarding acetaminophen dosage in certain patients?
The threshold may be much lower in patients with active hepatic disease (hepatitis, alcoholism, etc).
83
What is the dosage and administration for Acetaminophen IV (Ofirmev)?
1000 mg given as a 15 minute infusion
84
What is the dosage and administration for Ibuprofen IV (Caldolor)? Contraindication?
400-800 mg over 30 minutes every 6 hours (max 3200mg/24hr) ## Footnote Contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft surgery.
85
What is the dosage and administration for Diclofenac IV (Dyloject)? Contraindication?
37.5 mg over 15 seconds every 6 hours not to exceed 150mg/24hr ## Footnote Similar contraindication against use in CABG patients.

Pharmacology TL (7 decks)

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