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Pharm 4 > Aspirin and the NSAIDs > Flashcards

Aspirin and the NSAIDs Flashcards

1
Q

General physiologic effects of the NSAIDs

A

Analgesic

Antipyretic (reduce fever)

Anti-inflam

Anti-platelet effect (aspirin)

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2
Q

Clinical uses for aspirin and the NSAIDs

A

Low doses:

  • Aches and pains
  • Inh. of clotting

High doses:

  • Arthritis
  • Anti-inflam

Prototype aspirin

Most widely used non-recreational drug

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3
Q

Salicylic acid vs Acetyl salicylic acid

A

Salicylic acid is very harsh on stomach

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4
Q

Aspirin

A

Tx: Analgesic, antipyretic, anti-inflam, anticlotting

Mech: Inh. COX

Therefore inh. prostaglandin synth (and thromboxane)

Kinetics:

  • ASA is weak acid so absorbed in stomach
  • Dissociates in plasma to form salicylic acid strongly bound to plasma proteins
  • 325-500mg/tablet; 4-6/day for arthritis
  • Lethal dose
    • Children(and elderly): 4g (12 tablets)
    • Adults 20g (50-60 tablets)
    • Death due to pulmonary edema

SE:

  • GI
    • Slicylic acid is direct irritant
    • ASA decreases PG production by intestinal mucosa
      • Decrease mucous production
      • Decrease HCO3 production
  • CNS effects
    • Tinnitus (large doses)
    • Increase resp rates
  • Other effects
    • Don’t take aspirin w/ warfarin
    • Direct effect on iris-decrease miosis during eye surgery
    • Decrease kidney perfusion
    • Hypersensitivity
    • Bronchospasms-esp in pts w/ nasal polyps
    • Inh. labor (PGs involved)

…

Asthmatic bronchospasms

Severe pulmonary edema

Peptic ulcer

Inhibit labor

Reye’s syndrome/Renal perfusion decrease

Iris–Inhibit miosis

Noise

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5
Q

Effects of aspirin

A

Anti-pyretic effects

  • Lowers temp in fever but not in health
  • May act in CNS-counteract bacterial pyrogens, which increase PG in hypothalamus
  • May cause mild peripheral vasodilation

Analgesic effects

  • Limited efficacy
    • Blocks pain of mild to moderate
      • Not visceral pain
  • Central effect and peripheral effect
    • Due to decreased PG production
      • PGs are neuromodulators-modulate pain

Anti-inflammatory effects:

  • PGs may serve as initial signals for inflammation→vasodilation and edema
  • ASA may decrease signs of inflam. and decrease immune cell activity

Anticlotting factors

  • ASA causes irreversible inh. of platelet COX→prevents TXA2
  • Used in pts w/ recent MI
  • Single dose of aspirin may inh. platelet aggregation for 1 week
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6
Q

Acetaminophen

A

Tx: Analgesic

Not an NSAID–Non-narcotic analgesic

No anti-platelet effect

Not effective for arthritis

Mech: Inh COX

Toxicity:

  • less GI effects than ASA
  • OD=10-15g (20-30 tablets)-can cause irreversible liver damage
    • Feel bad, then better, then liver starts to fail in a few days
    • Decreased glutathione in liver-treat w/ reducing agent (N-acetyl cysteine)
  • Alcoholics and acetaminophen lead to decreased glutathione w/ smaller dose
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7
Q

Ibuprofen

and other -pro-

A

Naproxyn

Fenoprofen

Ketoprofen

Flurbiprofen

Oxaprozin

Suprofen

Tx: Analgesic, anti-inflam

Mech: Inh COX

Propionic acid derivative

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8
Q

Indomethacin

A

NSAID

Tx: Patent ductus arteriosus

  • Hole would not close due to excess PGs
  • Indomethacin would allow closure, but so does ibuprofen too

Mech: Very potent COX inh.

Acetic acid derivative

SE:

  • Thrombocytopenia
  • Aplastic anemia
  • Corneal opacity
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9
Q

Tolmetin

A

NSAID

Acetic acid derivative

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10
Q

Sulindac

A

NSAID

Acetic acid derivative

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11
Q

Pyroxicam

A

NSAID

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12
Q

“-fenac”s

A

diclofenac

bromfenac

Nepafenac

NSAID

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13
Q

Etodolac

A

NSAID

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14
Q

Nabumetone

A

NSAID

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15
Q

Other NSAIDs

A

_Pyr_os _ne_ed _e_xcess _f_ire

_Pyr_oxicam _n_abumetone _e_todolac -_f_enac

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16
Q

Acetic acid derived NSAIDs

A

Double A (Aaron) slobbers into titties

Acetic Acid: Sulindac indomethacin tolmetin

17
Q

Celecoxib

A

Cele-cox-ib

Selective cox(2) inhibitor

Tx: Analgesic and anti-inflam

18
Q

other -coxib

A

Rofecoxib

Valvicoxib

Off the market now b/c increase in MI and stroke

Due to greater effect of drug on production of prostacyclin (PGI2) than on production of thromboxane

PGI2-strong vasodilator

TXA-vasoconstriction and platelet aggregation

*At high doses all NSAIDs have similar effect*

Pharm 4 (9 decks)

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