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NSAIDs Flashcards

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1
Q

What are NSAIDs?

A

NON-steroidal anti-inflammatory drugs

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2
Q

How do NSAIDs differ from opioids?

A

NSAIDs are non-opioid analgesics, less powerful but adequate for mild pain; opioids relieve strong sharp pain and cause sedation, respiratory depression, tolerance, and dependence

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3
Q

What are major mediators of pain, fever, and inflammation?

A

Prostaglandins (PGs)

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4
Q

What is the rate-limiting step in prostaglandin synthesis?

A

COX activity

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5
Q

What types of COX enzymes are there?

A
  • COX-1
  • COX-2
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6
Q

What is the primary function of COX-1?

A
  • Mediates fever and pain in CNS
  • Protects gastric mucosa
  • Increases platelet aggregation
  • Regulates kidney function
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7
Q

What is the prototype COX-1 inhibitor?

A

Aspirin

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8
Q

What is the primary function of COX-2?

A
  • Mediates pain in CNS
  • Protects gastric mucosa (with COX-1)
  • Decreases platelet aggregation
  • Plays a role in wound healing
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9
Q

What is the prototype COX-2 inhibitor?

A

Celecoxib

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10
Q

Why do most NSAIDs inhibit both COX-1 and COX-2?

A

They are useful for treating pain, fever, and inflammation

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11
Q

What is aspirin chemically known as?

A

Acetyl-salicylic acid (ASA)

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12
Q

What metabolite mediates the anti-inflammatory and analgesic effects of aspirin?

A

Salicylic acid (or salicylate)

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13
Q

What is the absorption characteristic of aspirin?

A

Orally effective and well absorbed

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14
Q

What happens to salicylate at low to moderate doses?

A

Metabolized in the liver by conjugation

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15
Q

What is the half-life of salicylate at low doses?

A

~2 hours

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16
Q

What is the half-life of salicylate at high doses?

A

15-30 hours

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17
Q

What are the beneficial effects of aspirin?

A
  • Analgesia
  • Anti-pyresis
  • Anti-inflammatory effects
  • Anti-thrombotic
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18
Q

What is the unique use of aspirin compared to other NSAIDs?

A

To prevent thrombus formation and prolong bleeding time

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19
Q

What is the recommended dose of aspirin for thrombosis prevention?

A

75-81 mg/day

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20
Q

What are common adverse effects of salicylates?

A
  • GI irritation
  • Damage
  • Gastric ulceration
  • Hemorrhage
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21
Q

What can reduce GI irritation caused by salicylates?

A
  • Enteric-coated tablets
  • Misoprostol (Cytotec)
  • Proton pump inhibitors like omeprazole (Prilosec)
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22
Q

What is the effect of aspirin on platelet aggregation?

A

Decreases platelet aggregation and increases bleeding time

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23
Q

What is a significant limitation of salicylates?

A

GI hemorrhage is responsible for ~15,000 aspirin-related deaths in the US each year

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24
Q

What is the action of salicylate on COX enzymes?

A

Reversible and competitive COX inhibitors

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25
What is the role of COX-1 in the vascular system?
Produces thromboxanes (TXs) that increase clotting risk
26
What is the role of COX-2 in the vascular system?
Produces prostacyclins (PGIs) that decrease clotting risk
27
What is the typical result of low doses of aspirin on the balance of platelet aggregation?
Inhibits COX-1, shifting the balance towards more anti-thrombotic PGIs
28
What is the consequence of irreversible inhibition of platelet COX-1 by aspirin?
Sustained reduction in thromboxanes (TXs) and reduced platelet aggregation
29
What are the adverse effects of salicylates (aspirin and others)?
Adverse effects include: * GI irritation and damage * Cardiovascular effects * Allergic reactions * Asthma attacks in aspirin-sensitive individuals * Drug interactions * Reye's Syndrome * Renal and hepatic toxicities * Premature closure of ductus arteriosus * Mild, moderate, and severe toxicity
30
How can GI irritation from salicylates be reduced?
GI irritation can be reduced by: * Using enteric-coated tablets * Administering misoprostol (Cytotec) * Using proton pump inhibitors like omeprazole (Prilosec)
31
What is 'salicylism'?
Salicylism is mild toxicity from excess chronic use of salicylates, characterized by: * Tinnitus * Dizziness * Headache * Confusion * Deafness * Drowsiness * Thirst * Nausea * Vomiting
32
What are the symptoms of moderate toxicity of salicylates?
Symptoms of moderate toxicity include: * Increased breathing * Respiratory alkalosis * Compensation through renal bicarbonate excretion
33
What are the signs of severe toxicity from salicylates?
Signs of severe toxicity include: * GI disturbances (nausea, vomiting, abdominal pain) * CNS disturbances (restlessness, incoherence, vertigo) * Fever * Dehydration * Skin eruptions
34
True or False: Aspirin should be used in children under 16.
False ## Footnote Aspirin should not be used in children under 16 due to the risk of Reye's Syndrome.
35
What is the primary treatment for overdose toxicity of salicylates?
Primary treatments include: * Hospitalization * Whole bowel irrigation * Activated charcoal * Volume repletion * Alkalinization of urine
36
What is the effect of alkalinizing urine on salicylate excretion?
Alkalinizing urine increases salicylate elimination by converting salicylic acid into its ionized form, enhancing excretion.
37
Fill in the blank: The pKa of salicylic acid is ______.
3
38
What should be monitored during the treatment of salicylate overdose?
Monitoring should include: * Blood levels of salicylates * Urine pH * Supplemental glucose and potassium
39
What can cause premature closure of the ductus arteriosus?
Salicylates can cause premature closure of the ductus arteriosus, particularly in the third trimester of pregnancy.
40
41
What are propionic acid derivatives?
Ibuprofen, Naproxen, others ## Footnote Commonly used non-steroidal anti-inflammatory drugs (NSAIDs).
42
What are the actions and uses of propionic acid derivatives?
Analgesic, anti-pyretic, anti-inflammatory ## Footnote Similarly effective as aspirin but with fewer side effects.
43
What is the mechanism of action for ibuprofen and naproxen?
COX inhibition (reversible and competitive) ## Footnote Similar to aspirin but with different binding characteristics.
44
In what forms are ibuprofen and naproxen available?
Tablets, liquid suspensions, IV preparations ## Footnote Multiple formulations for different indications.
45
What specific condition is ibuprofen approved for?
Dysmenorrhea ## Footnote Pain and cramps mediated by prostaglandins (PGs).
46
What are the specific dosing recommendations for ibuprofen?
200 mg every 4-6 hours for analgesia; 400 mg+ for anti-inflammatory ## Footnote Higher doses require a prescription.
47
What is the maximum daily dose of ibuprofen?
3200 mg ## Footnote Important to avoid toxicity.
48
What is a specific use of ibuprofen in pediatric patients?
Patent ductus arteriosus (as NeoProfen®) ## Footnote Administered IV.
49
What are the specifics of naproxen dosing?
200-250 mg b.i.d. ## Footnote Longer half-life allows for this dosing schedule.
50
What are the common adverse effects of ibuprofen and naproxen?
GI concerns, prolonged bleeding time, renal toxicity ## Footnote Similar to aspirin but less severe.
51
True or False: Ibuprofen can displace warfarin.
True ## Footnote High albumin binding increases risk of drug interactions.
52
What should be considered when taking NSAIDs with low-dose aspirin?
Take NSAIDs 8 hours before or 30 minutes after low-dose aspirin ## Footnote To avoid interference with anti-platelet effects.
53
What is the primary use of indomethacin?
Severe inflammation (e.g. rheumatoid arthritis) ## Footnote Also approved for patent ductus arteriosus.
54
How does indomethacin compare in potency to aspirin?
10-20X more potent than aspirin ## Footnote Limited use due to severe side effects.
55
What are the adverse effects of indomethacin?
Severe headaches, vertigo, confusion, GI problems ## Footnote High incidence of side effects (30-50%).
56
What are selective COX-2 inhibitors?
Celecoxib (Celebrex®) ## Footnote Designed to reduce inflammation with fewer adverse effects.
57
What is the rationale for using COX-2 selective inhibitors?
To treat inflammation without serious adverse effects ## Footnote Most inflammation effects are due to COX-2.
58
What are the approved uses for celecoxib?
Osteoarthritis, rheumatoid arthritis, dysmenorrhea, acute pain ## Footnote Effective for certain arthritis types.
59
What is a common adverse effect of celecoxib?
Edema ## Footnote Resulting from decreased kidney function.
60
What is acetaminophen commonly known as?
Tylenol® ## Footnote Also known as paracetamol.
61
What is a key difference between acetaminophen and NSAIDs?
No anti-inflammatory action ## Footnote Acetaminophen is classified as a non-opioid analgesic.
62
What are the common side effects of acetaminophen?
Hepatic damage, skin rash, GI distress ## Footnote Significant concerns especially with overdose.
63
What is the major concern in acetaminophen overdose?
Hepatotoxicity ## Footnote Can lead to hepatic coma and death.
64
What is the treatment for acetaminophen overdose?
N-acetylcysteine (Acetadote®) ## Footnote Acts to restore glutathione levels and detoxify metabolites.
65
What is the maximum recommended dosage of acetaminophen?
4 g/day ## Footnote May be reduced further to avoid toxicity.
66
What are the two components of increased MI risk with celecoxib?
TX/PGI imbalance and renal COX inhibition ## Footnote Contributes to thrombotic risks.

Pharmacology (2 decks)

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