Non- Narcotic Analgesics Flashcards

1
Q

What is the role of Prostaglandins in producing Pain?

A

Noxious stimuli cause the release of Prostaglandins by COX, which increase the sensitivity of nociceptors, transmitting an ascending pain signal.

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2
Q

Ibuprofen (Advil):

A
  • NSAIDS

- Non selective COX inhibitor

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3
Q

Celecoxib:

A

NSAID

-COX-2 Inhibitor

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4
Q

Acetylsalicylic Acid (Aspirin):

A
  • Salicylic acid is obtained from Willow Bark
  • Is an effective analgesic/ anti-inflammatory, however it is VERY hard on the stomach.
  • Aspirin has an anti- platelet effect at low doses (80 mg)
  • ASA acetylates COX-1 in platelets, irreversibly inhibiting its actions.
  • Used less as an antipyretic
  • Contraindicated in children
  • ->Analgesic (600-900 mg)
  • ->Anti-inflammaotry (3000-6000mg)
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5
Q

What are the enzymes and products of Arachidonic Acid?

A
  • Cyclooxyrgenase (COX) which leads to the production of Prostaglandins, Prostacyclins and Thromboxanes.
  • Lipooxygenase (LOX) leads to the production of Leukotreines
  • Lead to inflammation.
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6
Q

What are the role of Prostacyclins in the clotting cascade?

A
  • Important for checks and balances of vessel clotting.

- Stops the clotting cascade through platelet inhibitor.

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7
Q

What are the positive and negative effects of COX inhibitors?

A
  • Antipyretic, Analgesic and Anti-inflammatory

- BAD: Decrease GI mucous (lead to ulceration)

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8
Q

Explain the mechanism of NSAIDS as an anti-pyretic:

A
  • Fever occurs due to actions of bacteria/ viruses in the hypothalamus.
  • Stimulating COX-2 results in a large increase in prostaglandins (PGE2 is a potent pyrogen)
  • Fever has a role in fighting infection.
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9
Q

Explain the mechanism of NSAIDS as an Analgesic/ Anti- Inflammatory:

A
  • PG’s increase vasodilation to injured tissues and enhance infiltration of leukocytes
  • NSAIDS block release of prostaglandins and prostacyclins (reduce inflammation)
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10
Q

NSAID Side Effects:

A
  • Renal Dysfunction (decrease PG’s, decrease vasodilation of afferent arterioles to the kidney… reduce GFR)
  • Edema
  • Gastrointestinal Ulceration
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11
Q

Why is a COX-2 inhibitor less problematic than a non- selective COX inhibitor?

A
  • COX-1 is important in protection and maintenance, as well as important for GI cytoprotection and platelet aggregation.
  • Blocking COX-1 blocks these beneficial protective roles.
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12
Q

Early signs of ASA Toxicity:

A

–Early signs of Toxicity include Tinnitus, GI Irritation, Hyperventilation and Lethargy.

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13
Q

Severe Signs of ASA Toxicity:

A

-Restlessness, Hallucinations, Seizures, Coma, Respiratory and Metabolic Acidosis and Respiratory Failure

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14
Q

Treatment of ASA Toxicity:

A

Alkalinize urine to enhance solubility.

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15
Q

Aspirin Induced Asthma:

A

-Occurs as COX enzymes are blocked, shunting to the LOX pathway at which leukotrienes are released. Leukotrienes act as broncho-constrictors and this can lead to asthma.

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16
Q

Acetaminophen:

A
  • Not an NSAID but shares many features.
  • Also inhibits COX enzymes, however acts primarily on the CNS to cause analgesia and anti-pyretic effects.

–>Lacks Adverse Effects of NSAIDs, and lacks anti- inflammatory effects.

17
Q

Acetaminophen Side Effects:

A
  • Generally well tolerated
  • Compared to NSAIDS, lower risk of:
  • GI adverse Effects
  • Cardiovascular/ renal dysfunction

-High (toxic) doses damage the liver.

18
Q

Acetaminophen Toxicity:

A
  • Risk increases with Chronic Ethanol Abuse
  • Concerns with combination products, such as cold/ cough preparations.
  • Concerning in pediatrics.
19
Q

Acetaminophen in Combination:

A
  • -Combined with Opioids:
  • Codeine: Tylenol 1, 2, 3 and 4
  • Tramadol (Tramaset)
20
Q

Why is Chronic Ethanol Abuse increase risk of Acetaminophen toxicity?

A

-Ethanol induces CYP2E1, lowering threshold for toxicity.
-CYP2E1 also converts Acetaminophen to a toxic metabolite- damaging the liver.
Ethanol also produces Glutathione which INHIBITS NAPQI, the enzyme responsible for metabolizing Acetaminophen in the liver.