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Pharmacology Exam 2 > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

Prostaglandin

A

Shared mechanism of all NSAIDs

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2
Q

COX-1

A

CNS - pain and fever
Stomach - protects mucosa lining
Platelets - increases aggregation and blood clotting

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3
Q

COX-2

A

COX-2 CNS - mediate pain
Stomach - protects mucosa lining (w/ COX-1)
Endothelial cells - decreases platelet aggregation by making prostacyclins
INFLAMMATION

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4
Q

Aspirin

A

Prototype of all NSAIDs
Acetyl-salicylic acid
Salicylate metabolite
Irreversibly binds to acetylating enzyme to inactivate COX - COX-1 effects
325 mg tablets distributed throughout body to CNS
80-90% protein bound
Displaces other drugs
Rapidly hydrolyzed to free salicylate before reaching other targets
1st order metabolism - liver
0 order - kidneys (high doses) need this high of dose to achieve anti-inflammatory

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5
Q

Main NSAID uses

A
  1. Analgesia (650-1000mg) - headache, dysmenorrhea, neuralgia, myalgia
    Good for inflammatory pain (bradykinin, substance P)
  2. Antipyresis (625-1000mg, 2-3 tablets)
  3. Anti-inflammatory (1300+mg, 4 tablets)
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6
Q

Characteristic unique to Aspirin

A

Prevent thrombus formation, prolong bleeding time

Irreversible prolonged action (7 days)

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7
Q

Aspirin Regimen

A

75-81 mg/day to reduce MI and CVA risk

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8
Q

Adverse effects of salicylates

A
  1. GI effects - PGs protect GI mucosa, salicylates are acids – result in gastric irritation
  2. Cardiovascular effects - problem in blood clotting deficient patients
  3. Allergic rxn
  4. Aspirin-senstive asthma
  5. Displace other protein-binding drugs
  6. Reye’s syndrome
  7. Premature closure of ductus arteriosus in pregnancy
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9
Q

Propionic Acid derivatives uses:

A 
Analgesics
Antipyretic
Anti-inflammatory
Fewer side effects than NSAID
Same mechanism as Aspirin but reversible
Specifically approved for dysmenorrhea
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10
Q

Propionic Acid Side Effects

A

GI issues (lesser extent than aspirin)
Prolong bleeding time, platelet inhibition
Bind to albumin - displace other drugs
Cross-sensitivity to salicylates

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11
Q

Ibuprofen

A

Ibuprofen, Advil, Motrin, etc
200mg/4-6 hr analgesia, anti-pyresis
400+mg/4-6 anti-inflammatory
PDA closure

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12
Q

Naproxen

A

Naproxen - Aleve, Anaprox, Naprosyn, etc
200-250mg bid (longer half-life)
Enteric coated delayed release
Gout, migraine

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13
Q

Acetic Acid derivatives

A

Indomethacin Prototype
10-20x more potent than aspirin
Limited use in analgesia and antipyresis
*Severe side effects - vertigo, headaches, confusion, seizures, psychosis, GI problems, pancreatitis, hepatitis
*Used in SEVERE inflammation (RA or gouty arthritis)
PDA

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14
Q

Celecoxib

A

Celebrex
SELECTIVE COX-2 Inhibitor
= treat inflammation and decrease serious adverse effects
100-200mg bid, 12 hr half life
Osteoarthritis, RA, juvenile idiopathic arthritis, ankylosing spondylitis, acute pain, dysmenorrhea
Equal to naproxen for OA and RA
Metabolized by CYP2C9

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15
Q

Adverse effects of Celecoxib (Celebrex)

A
  1. Edema (decreased kidney function)
  2. GI problems (less than ibuprofen/naproxen)
  3. Bad for people allergic to sulfonamides
  4. Bad for pregnancy (not approved)
  5. ***Increased incidence of MI (shift balance of PGIs and TXs to platelet aggregation b/c COX-2)
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16
Q

Acetaminophen

A 
Tylenol
Inhibition of COXs and PG synthesis
325mg, 650-1000mg/4hr
Absorbed from GI, distributed evenly
Metabolized in liver, CYP2E1; excreted in urine

Effects:

  1. Analgesia and antipyresis
  2. NO INFLAMMATORY ACTION
  3. Non-opioid analgesic, NOT an NSAID
  4. Relaxation, drowsiness, euphoria

Safer alternative to aspirin!

17
Q

Acetaminophen adverse effects

A 
Maximal dose 4g
Cross-sensitivity with salicylates
Hepatic damage (longterm use)
Skin rash, drug fever, mucosal lesions
Rare: neutropenia, leukopenia, pancytopenia
Nephrotoxicity (chronic abuse)

OVERDOSE (10-25g ingested)
GI Distress
Hepatotoxicity - Jaundice, hepatic death and coma, reactive electrophile
8 hour window for liver damage

18
Q

N-acetylcysteine (Acetadote)

A

Reactive sulfhydryl to capture reactive acetaminophen and replace depleted glutathione
Oral 140mg/kg +70mg/kg x4 hrs
IV 150mg/kg LD, 50mg/kg x4 hours
Monitor liver and blood levels in hospital x3 days

Pharmacology Exam 2 (4 decks)

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