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Pharmacology > NSAIDs > Flashcards

NSAIDs Flashcards

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
Q

What is the role of COX-1 in the vascular system?

A

Produces thromboxanes (TXs) that increase clotting risk

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26
Q

What is the role of COX-2 in the vascular system?

A

Produces prostacyclins (PGIs) that decrease clotting risk

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27
Q

What is the typical result of low doses of aspirin on the balance of platelet aggregation?

A

Inhibits COX-1, shifting the balance towards more anti-thrombotic PGIs

28
Q

What is the consequence of irreversible inhibition of platelet COX-1 by aspirin?

A

Sustained reduction in thromboxanes (TXs) and reduced platelet aggregation

29
Q

What are the adverse effects of salicylates (aspirin and others)?

A

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
Q

How can GI irritation from salicylates be reduced?

A

GI irritation can be reduced by:
* Using enteric-coated tablets
* Administering misoprostol (Cytotec)
* Using proton pump inhibitors like omeprazole (Prilosec)

31
Q

What is ‘salicylism’?

A

Salicylism is mild toxicity from excess chronic use of salicylates, characterized by:
* Tinnitus
* Dizziness
* Headache
* Confusion
* Deafness
* Drowsiness
* Thirst
* Nausea
* Vomiting

32
Q

What are the symptoms of moderate toxicity of salicylates?

A

Symptoms of moderate toxicity include:
* Increased breathing
* Respiratory alkalosis
* Compensation through renal bicarbonate excretion

33
Q

What are the signs of severe toxicity from salicylates?

A

Signs of severe toxicity include:
* GI disturbances (nausea, vomiting, abdominal pain)
* CNS disturbances (restlessness, incoherence, vertigo)
* Fever
* Dehydration
* Skin eruptions

34
Q

True or False: Aspirin should be used in children under 16.

A

False

Aspirin should not be used in children under 16 due to the risk of Reye’s Syndrome.

35
Q

What is the primary treatment for overdose toxicity of salicylates?

A

Primary treatments include:
* Hospitalization
* Whole bowel irrigation
* Activated charcoal
* Volume repletion
* Alkalinization of urine

36
Q

What is the effect of alkalinizing urine on salicylate excretion?

A

Alkalinizing urine increases salicylate elimination by converting salicylic acid into its ionized form, enhancing excretion.

37
Q

Fill in the blank: The pKa of salicylic acid is ______.

38
Q

What should be monitored during the treatment of salicylate overdose?

A

Monitoring should include:
* Blood levels of salicylates
* Urine pH
* Supplemental glucose and potassium

39
Q

What can cause premature closure of the ductus arteriosus?

A

Salicylates can cause premature closure of the ductus arteriosus, particularly in the third trimester of pregnancy.

41
Q

What are propionic acid derivatives?

A

Ibuprofen, Naproxen, others

Commonly used non-steroidal anti-inflammatory drugs (NSAIDs).

42
Q

What are the actions and uses of propionic acid derivatives?

A

Analgesic, anti-pyretic, anti-inflammatory

Similarly effective as aspirin but with fewer side effects.

43
Q

What is the mechanism of action for ibuprofen and naproxen?

A

COX inhibition (reversible and competitive)

Similar to aspirin but with different binding characteristics.

44
Q

In what forms are ibuprofen and naproxen available?

A

Tablets, liquid suspensions, IV preparations

Multiple formulations for different indications.

45
Q

What specific condition is ibuprofen approved for?

A

Dysmenorrhea

Pain and cramps mediated by prostaglandins (PGs).

46
Q

What are the specific dosing recommendations for ibuprofen?

A

200 mg every 4-6 hours for analgesia; 400 mg+ for anti-inflammatory

Higher doses require a prescription.

47
Q

What is the maximum daily dose of ibuprofen?

A

3200 mg

Important to avoid toxicity.

48
Q

What is a specific use of ibuprofen in pediatric patients?

A

Patent ductus arteriosus (as NeoProfen®)

Administered IV.

49
Q

What are the specifics of naproxen dosing?

A

200-250 mg b.i.d.

Longer half-life allows for this dosing schedule.

50
Q

What are the common adverse effects of ibuprofen and naproxen?

A

GI concerns, prolonged bleeding time, renal toxicity

Similar to aspirin but less severe.

51
Q

True or False: Ibuprofen can displace warfarin.

A

True

High albumin binding increases risk of drug interactions.

52
Q

What should be considered when taking NSAIDs with low-dose aspirin?

A

Take NSAIDs 8 hours before or 30 minutes after low-dose aspirin

To avoid interference with anti-platelet effects.

53
Q

What is the primary use of indomethacin?

A

Severe inflammation (e.g. rheumatoid arthritis)

Also approved for patent ductus arteriosus.

54
Q

How does indomethacin compare in potency to aspirin?

A

10-20X more potent than aspirin

Limited use due to severe side effects.

55
Q

What are the adverse effects of indomethacin?

A

Severe headaches, vertigo, confusion, GI problems

High incidence of side effects (30-50%).

56
Q

What are selective COX-2 inhibitors?

A

Celecoxib (Celebrex®)

Designed to reduce inflammation with fewer adverse effects.

57
Q

What is the rationale for using COX-2 selective inhibitors?

A

To treat inflammation without serious adverse effects

Most inflammation effects are due to COX-2.

58
Q

What are the approved uses for celecoxib?

A

Osteoarthritis, rheumatoid arthritis, dysmenorrhea, acute pain

Effective for certain arthritis types.

59
Q

What is a common adverse effect of celecoxib?

A

Edema

Resulting from decreased kidney function.

60
Q

What is acetaminophen commonly known as?

A

Tylenol®

Also known as paracetamol.

61
Q

What is a key difference between acetaminophen and NSAIDs?

A

No anti-inflammatory action

Acetaminophen is classified as a non-opioid analgesic.

62
Q

What are the common side effects of acetaminophen?

A

Hepatic damage, skin rash, GI distress

Significant concerns especially with overdose.

63
Q

What is the major concern in acetaminophen overdose?

A

Hepatotoxicity

Can lead to hepatic coma and death.

64
Q

What is the treatment for acetaminophen overdose?

A

N-acetylcysteine (Acetadote®)

Acts to restore glutathione levels and detoxify metabolites.

65
Q

What is the maximum recommended dosage of acetaminophen?

A

4 g/day

May be reduced further to avoid toxicity.

66
Q

What are the two components of increased MI risk with celecoxib?

A

TX/PGI imbalance and renal COX inhibition

Contributes to thrombotic risks.

Pharmacology (2 decks)

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