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Pharmacology Winter Exam 2 > L13-15: Handout > Flashcards

L13-15: Handout Flashcards

1
Q

What is the prototype drug of NSAIDs?

A

Aspirin (acetylsalicylic acid, ASA)

Aspirin is recognized for its analgesic, antipyretic, and anti-inflammatory properties.

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2
Q

What are the major effects of aspirin?

A
  • Analgesic
  • Antipyretic
  • Anti-inflammatory

Aspirin is valued for its low cost and availability without prescription.

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3
Q

What type of enzymes does aspirin inhibit?

A

Cyclooxygenase (COX-1 and COX-2)

Aspirin causes irreversible inhibition of both COX enzymes.

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4
Q

What is the pharmacokinetics of aspirin?

A
  • Rapid absorption from the stomach
  • Peak plasma concentration: 2-4 hours
  • Binds to plasma proteins: 50-90%

Absorption occurs mainly in the upper small intestine.

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5
Q

Fill in the blank: Aspirin lowers body temperature only in _______ patients.

A

febrile

Aspirin is antipyretic and does not lower temperature in normal patients.

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6
Q

What are the common adverse effects of eicosanoids?

A
  • Vomiting
  • Diarrhea
  • Fever
  • Bronchoconstriction
  • Hypo- or hypertension
  • Syncope
  • Flushing
  • Dizziness

These effects can occur due to their action on various tissues and organs.

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7
Q

Which COX enzyme is constitutively expressed?

A

COX-1

COX-1 has ‘housekeeping functions’ and is always present.

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8
Q

What are the major differences between COX-1 and COX-2?

A
  • COX-1: constitutive, housekeeping functions
  • COX-2: inducible, expressed in response to stimuli

COX-2 is mainly responsible for the synthesis of prostacyclin in endothelial cells.

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9
Q

What is the role of prostaglandins in inflammation?

A
  • Cause pain
  • Promote vasodilation
  • Increase vascular permeability

Prostaglandins are key mediators in the inflammatory response.

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10
Q

What are some examples of NSAIDs?

A
  • Ibuprofen
  • Naproxen
  • Diclofenac
  • Celecoxib
  • Ketorolac
  • Piroxicam

These drugs vary in their specific properties and mechanisms of action.

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11
Q

True or False: Aspirin is effective as an analgesic in non-inflamed painful conditions.

A

False

Aspirin’s analgesic action is generally limited to low intensity pain arising from inflammation.

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12
Q

What is the mechanism of action of acetaminophen?

A

Inhibition of prostaglandin synthesis

Acetaminophen has different actions compared to NSAIDs, particularly in pain relief.

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13
Q

What are the clinical uses of dinoprostone (PGE2)?

A
  • Abortion
  • Facilitating labor
  • Treatment of dysmenorrhea

Dinoprostone has specific applications in obstetrics and gynecology.

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14
Q

Fill in the blank: COX-2 inhibitors like celecoxib preferentially inhibit _______.

A

COX-2

Celecoxib has major differences in action compared to non-specific COX inhibitors.

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15
Q

What is the effect of PGE1 (alprostadil) in males?

A

Enhances penile erection

PGE1 relaxes smooth muscles in the corpus cavernosum.

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16
Q

What are the pharmacological actions of leukotrienes?

A
  • Bronchoconstriction
  • Enhance inflammation
  • Chemotaxis

Leukotrienes play a significant role in asthma and allergic responses.

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17
Q

What is the role of misoprostol in treating peptic ulcer disease?

A

Reduces gastric acid secretion

Misoprostol is a PGE1 analog.

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18
Q

Define the arachidonate cascade.

A

The metabolic pathway involving the release of arachidonic acid and its conversion to eicosanoids

This cascade is crucial in inflammation and pain modulation.

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19
Q

What factors can elevate body temperature in hyperthermia?

A
  • Exercise
  • Heat stroke
  • Drugs
  • Hypothalamic lesions

These factors differ from those causing fever, which is regulated by the hypothalamus.

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20
Q

What is the plasma concentration of aspirin?

A

Low

Aspirin binds to plasma proteins (50-90%)

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21
Q

What type of kinetics does aspirin follow at low doses?

A

First order kinetics

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22
Q

What type of kinetics does aspirin follow at high doses?

A

Zero order kinetics

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23
Q

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

A

3-6 hours

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24
Q

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

A

15-30 hours

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25
Q

What effect does alkaline urine (pH 8) have on salicylate excretion?

A

Enhances salicylate excretion

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26
Q

What are the main pharmacodynamic effects of aspirin?

A
  • Anti-inflammatory effect
  • Analgesic effect
  • Antipyretic effect
  • Platelet effects
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27
Q

What is the irreversible effect of aspirin on platelets?

A

Inhibition of platelet COX enzymes

28
Q

What are the four main effects of acetylsalicylic acid?

A
  • Analgesic
  • Antipyretic
  • Anti-inflammatory
  • Antiplatelet
29
Q

What are some uses of aspirin?

A
  • Analgesia
  • Antipyresis
  • Anti-inflammatory
  • Decreasing the incidence of MI
  • Long-term use decreases the incidence of colon cancer
30
Q

What is the biphasic effect of aspirin on respiration?

A

First stimulation and then depression

31
Q

What condition can result from toxic doses of aspirin?

A

Combined respiratory and metabolic acidosis

32
Q

What are the known adverse effects of aspirin on the gastrointestinal tract?

A
  • Epigastric distress
  • Nausea
  • Vomiting
  • Gastric irritation
  • Ulceration
  • Hemorrhage
  • Heartburn
  • Dyspepsia
33
Q

What are the contraindications for aspirin use?

A
  • Gastric ulcer
  • Severe hepatic damage
  • Hypoprothrombinemia
  • Vitamin K deficiency
  • Hemophilia
  • Hypersensitivity to aspirin or salicylates
34
Q

What is the effect of low doses of aspirin on uric acid excretion?

A

Decreases uric acid excretion

35
Q

What is the effect of high doses of aspirin on uric acid excretion?

A

Enhances uric acid excretion

36
Q

What is salicylism characterized by?

A
  • Headache
  • Dizziness
  • Ringing in the ear
  • Difficulty in hearing
  • Visual problems
  • Mental confusion
37
Q

What is Reye’s Syndrome?

A

Cerebral edema in children with viral infections

38
Q

What is the drug of choice for children with fever?

A

Acetaminophen

39
Q

What is the fatal dose of aspirin?

A

Approximately 20 grams

40
Q

What is the mechanism of action of COX-2 inhibitors?

A

Reversible inhibition of COX-2 enzyme

41
Q

What are some common adverse reactions of NSAIDs?

A
  • GI disturbances
  • Hypersensitivity
  • Nephrotoxicity
42
Q

What is the first choice drug among NSAIDs?

A

Ibuprofen

43
Q

What are the toxic effects of acetaminophen overdose?

A

Fatal hepatic necrosis

44
Q

What is the mechanism of action of acetaminophen?

A

Analgesic and antipyretic effects

45
Q

What is the absorption characteristic of acetaminophen?

A

Rapid and almost completely absorbed from the G.I. tract

46
Q

What type of drug is acetaminophen considered compared to aspirin?

A

Alternative

47
Q

What should be done with aspirin prior to elective surgery?

A

Stop at least one week before

48
Q

What are the preferred reasons for using acetaminophen over aspirin?

A

It is tolerated better and lacks several undesirable side effects of aspirin, such as ulcerogenic effects, blood clotting defects, acid-base imbalance, and auditory toxicity.

Acetaminophen is not completely innocuous; overdose can cause fatal hepatic necrosis.

49
Q

What is the plasma concentration peak time for acetaminophen?

A

30-60 minutes

50
Q

What is the plasma half-life of acetaminophen?

A

1-3 hours

51
Q

Where is acetaminophen primarily metabolized?

A

In the liver

52
Q

What percentage of acetaminophen is excreted in urine as conjugated products?

A

About 90%

53
Q

What causes hepatotoxicity in acetaminophen overdose?

A

A hydroxylated metabolic product when large quantities (> 15 g) are taken

54
Q

How does acetaminophen reduce fever?

A

By inhibiting the action of endogenous pyrogenic at the hypothalamic heat regulating center, likely by inhibiting prostaglandin production.

55
Q

True or False: Acetaminophen is effective as an antirheumatic agent.

A

False

56
Q

In which patient populations is acetaminophen preferred over aspirin?

A
  • Patients allergic to aspirin
  • Those with coagulation disorders
  • Individuals with a history of peptic ulcers
  • Patients with gouty arthritis taking uricosuric agents
  • Children
57
Q

What are some adverse effects of acetaminophen?

A
  • Skin rash
  • Allergic responses
  • Rare blood element adverse effects (neutropenia, pancytopenia, leukopenia)
  • Dose-dependent fatal hepatic necrosis
58
Q

What is the serious consequence of acetaminophen overdose in adults?

A

Hepatotoxicity occurs after ingestion of 10-15 grams, and 25 grams may be fatal.

59
Q

What indicates liver damage due to acetaminophen toxicity?

A

Elevated serum transaminase, lactic acid dehydrogenase

60
Q

What is an effective treatment for acetaminophen intoxication?

A

N-acetylcysteine (Mucomyst)

61
Q

What is the role of N-acetylcysteine in acetaminophen toxicity?

A

It is a free radical scavenger and must be administered parenterally within 10-12 hours after intoxication.

62
Q

What has changed regarding the recommendation for aspirin in primary prevention of cardiovascular disease?

A

The decision should be made based on shared decision-making, considering the benefits and harms.

63
Q

What did the ASCEND trial indicate about aspirin use in diabetes patients?

A

The risk of all-cause death was similar with or without aspirin.

64
Q

What is the risk of death associated with aspirin use in individuals 70 years or older according to the ASPREE trial?

A

Higher with aspirin (13% vs 11%)

65
Q

Fill in the blank: The treatment for active PUD is _______.

A

acetaminophen and/or opioids only

Pharmacology Winter Exam 2 (4 decks)

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