NSAIDS, Corticosteroids Flashcards

1
Q

Does Tylenol work well for inflammatory pain

A

No not really

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2
Q

What are the indications to use acetaminophen (Tylenol)

A

Mild to moderate non-inflammatory nociceptive pain

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3
Q

What is the role in therapy of acetaminophen (Tylenol)

A
  1. Fever
  2. Self-limiting painful conditions
  3. Osteoarthritis
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4
Q

What is the mechanism of action of acetaminophen (Tylenol)

A
  1. Analgesic effects in CNS via COX inhibition, interacts with nitric oxide containing pathways, and blocking substance P actions
  2. Anti-pyretic
    *can use in children under 6 months
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5
Q

What are the adverse effects of acetaminophen (Tylenol)

A
  1. Generally well tolerated
  2. Rare: Stevens-Johnson syndrome / Toxic Epidermal Necrolysis (TEN)
  3. BBW: Hepatotoxicity
    *can overdose
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6
Q

What are the roles of acetaminophen (Tylenol)

A
  1. Severe rash skin reactions SJS TEN = CI
  2. Caution in renal impairment
  3. BBW: Severe Hepatotoxicity
    *doses >4 grams a day
    *risk of dosing errors is 10x higher with injection
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7
Q

What is the maximum daily dose of acetaminophen

A

3,000mg per day

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8
Q

If someone overdoses on acetaminophen what is the antidote

A
  1. N-acetylcysteine
    *restores hepatic glutathione
    *helps to breakdown Tylenol
  2. Use Rumack-Matthew nomagram
    *input the serum acetaminophen level and time since ingestion to determine need for NAC
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9
Q

What are the COX-1 and 2 Non-selective NSAIDS

A
  1. Ibuprofen (Advil, Motrin)
  2. Naproxen (Aleve, Naprosyn)
  3. Indomethacin (Indocin)
  4. Ketorolac (toradol)
    *all have more GI problems
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10
Q

What are the Increased COX-2 Selectivity NSAIDS

A
  1. Celecoxib (celebrex)
  2. Diclofenac (voltaren)
  3. Meloxicam (mobic)
    *2 is the most selective COX-2 available (less GI irritation)
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11
Q

What are the indications for NSAIDs

A
  1. Mild to moderate pain suspected to be inflammatory, headache
  2. Fever reduction
  3. Arthritis
  4. Gout
  5. Closure of the patient ductus arteriosus
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12
Q

What are the indications for Aspirin

A
  1. Prevention of myocardial infarcation/stroke
    *affects the platelets to be more thrombotic in nature
  2. Arthritis
  3. Headache
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13
Q

What are the anti-inflammatory effects of NSAIDS and ASA

A

NSAIDS
1. Reversible inhibit COX1 and or 2 and the production of thromboxane, prostaglandins, and prostacyclin
ASA
1. Irreversible COX inhibition (inhibition of prostaglandins synthesis_
*have to eliminate the platelets before the effects wear off

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14
Q

What are the antipyretic effects of NSAIDS and ASA

A
  1. Inhibits the synthesis of fever inducing prostaglandins in the brain
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15
Q

What are the platelet effects of NSAIDS and ASA

A

NSAIDS
1. Inhibits platelet aggression (dont stick to each other, increased risk of bleeding)
ASA
1. Inhibits thromboxane synthesis (permanent)
*need new platelets (made every 8 to 10 days)

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16
Q

What are the analgesic effects of NSAIDS and ASA

A
  1. Reduced prostaglandin production at injured tissue
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17
Q

What are the effects of the Selective COX2 inhibition (NSAIDS)

A
  1. Do not affect platelet function at usual doses
    *do not inhibit platelet aggregation
  2. Less GI irritation
  3. Increased incidence of edema, hypertension, and maybe MI
  4. Nephrotoxicity (all NSAIDS) due to interfering with auto regulation of renal blood flow
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18
Q

What are some pharmacokinetics pearls of NSAIDS

A
  1. Do not give and NSAID to a child <6 months old
    *can effect the development of kidneys, also why we avoid in pregnancy
  2. Highly protein-bound, typically to albumin
  3. Naproxen and piroxicam have longer half lives
    *N (14 hours) Piroxicam (57 hours)
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19
Q

What is the correlation between NSAIDS and their half lives

A

NSAIDs with shorter 1/2 life remain in the joints longer than anticipated T1/2

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20
Q

What are some pharmacokinetics pearls of ASA

A
  1. First order renal elimination
  2. Anti platelet effects last 8 to 10 days
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21
Q

What are the therapeutic dosing ranges for ASA

A

LOW (81-325mg/day)
1. Reduced platelet aggregation
Intermediate (300-2400mg/day)
1. Antipyretic and analgesic effects
HIGH (2400-4000mg/day)
1. Anti-inflammatory effects

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22
Q

What are some adverse reactions of NSAIDs and ASA

A
  1. Stomach upset, abdominal pain NSAIDS <ASA
  2. GI bleed, clotting problems (increased bleeding time)
  3. Tinnitus, dizziness
  4. Worsening HTN, MI
  5. Hyperkalemia
  6. Impaired renal function
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23
Q

What are the rare but serious dermatological adverse reactions of NSAIDS

A
  1. Steven Johnson Syndrome (SJS)
  2. Toxic Epidermal Necrolysis (TEN)
24
Q

What are the rare but serious CNS adverse reactions of NSAIDS

A

Aseptic meningitis

25
What are the rare but serious cardiovascular adverse reactions of NSAIDS
1. MI 2. Congestive heart failure
26
What are the rare but serious Gastrointestinal adverse reactions of NSAIDS
Ulcer or bleeding
27
What are the rare but serious hematologic adverse reactions of NSAIDS
1. Thrombocytopenia 2. Neutropenia 3. Aplastic anemia
28
What are the rare but serious hepatic adverse reactions of NSAIDS
Liver failure
29
What are the cardiovascular warnings and risk of NSAIDS and ASA
1. Increased risk of serious cardiovascular thrombotic events. MI, and stroke 2. HTN 3. Impaired renal function
30
What are the gastrointestinal warnings and risk of NSAIDS and ASA
1. Increased risk of serious GI adverse events (bleeding, ulceration, and perforation)
31
What are the other warnings and risk of NSAIDS and ASA
1. Hematological (anemia) 2. Increased risk of MI and stroke 3. Avoid in pregnancy 4. Pre-existing asthma *severe bronchospasm
32
What are the toxicities of ASA
1. Higher doses / early overdose *respiratory alkalosis *tinnitus, vertigo, hyperventilation 2. Very high doses/toxicity *above 300 mcg/mL clearly toxic *metabolic acidosis 3. There is no antidote *use gastric lovage and charcoal
33
What are the toxicities with ASA and children
1. Children with viral infection if treated with salicylates will *have an increased risk for developing Reye’s syndrome
34
What is Reye’s syndrome
1. Rare but serious syndrome of rapid liver degeneration and encephalopathy *can be deadly
35
What hormone is involved in corticosteroids
Cortisol *important hormone involved with blood glucose, metabolism, inflammation *produced in adrenal gland via cholesterol metabolism
36
What does corticosteroids inhibit
1. Induce synthesis of PLA2 inhibitor 2. Decreased synthesis of COX2
37
What are the anti-inflammatory and immunosuppressive effects of corticosteroids
1. Inhibits some pro-inflammatory mediators and genes *affects transcription factors that control the synthesis of pro-inflammatory mediators 2. Initiates upregulation of anti-inflammatory mediators
38
What are the mechanisms of corticosteroids
When giving a corticosteroid it will 1. Shut down, the formation of inflammatory mediators 2. Will enhance anti-inflammatory mediators
39
What are the least to most potent corticosteroids
1. Cortisone 2. Hydrocortisone 3. Prednisone 4. Prednisolone 5. Methyprednisolone 6. Triamcinolone 7. Dexamethasone 8. Betamethasone
40
What are other corticosteroids to know
1. Fluticasone 2. Mometasone 3. Budesonide
41
What are the therapeutic uses for steroid (MAGIC PAUL)
M: multiple sclerosis A: asthma/allergic rhinitis and hay fever G: giant cell arteritis / polymyalgia rheumatica I: inflammatory bowel disease C: COPD P: painful inflamed joints A: atopic eczema U: urticaria L: lupus
42
What are the adverse reactions of corticosteroids
Longer you’re on a steroid the more / worsening ADRs 1. Sick 2. Sad 3. Sex (decreased libido) 4. Salt (retain sodium and water) 5. Sugar (raises blood sugar) *route matters
43
What are the long term side effects of corticosteroids
1. Growth suppression 2. Osteoporosis 3. Glaucoma 4. Hyperglycemia 5. Cushing syndrome
44
Why do you need to taper a corticosteroid
1. Can cause acute adrenal insufficiency *addisonian crisis *if ingested steroids are stopped suddenly it can cause addisonian crisis
45
What is Cushing syndrome
1. Adrenal gland produces too much cortisol or steroids are taken in high doses and the amount of cortisol is higher than natural
46
What are the CI to corticosteroids
1.infections 2. Osteoporosis 3. Uncontrolled hyperglycemia 4. Diabetes 5. Glaucoma 6. Joint infection 7. Congestive heart failure 8. Uncontrolled hypertension
47
What is the MOA of acetaminophen
1. Likely affects pain signaling, possibly by affecting nitric oxide and blocking substance P
48
What is the indication for lidocaine
1. Useful for well-localized pain 2. May be particularly preferred in elderly when concerned about CNS SE
49
What is the MOA of lidocaine
1. Inhibits sodium channels to reduce neuronal impulse inducing an anesthetic effect and reducing inflammation
50
What are the ADRs of lidocaine
1. Stinging / burning 2. Localized numbness
51
What are the clinal pearls to remember about lidocaine
1. Topical *12 hrs on 12 off 2. Max 3 patches for simultaneous use 3. Does not accumulate with normal hepatic function
52
What are the anti seizure effects of gabapentanoids (gabapentin / neurontin) (Pregabalin / lyrica)
1. Decreases synaptic release of glutamate thereby reducing excessive neural excitivity contributing to the seizure prone environment
53
What are the spasmolytic effects gabapentanoids (gabapentin / neurontin) (Pregabalin / lyrica)
Action on calcium channels theorized
54
What are the analgesic effects of gabapentanoids (gabapentin / neurontin) (Pregabalin / lyrica)
1. Action on voltage-gated calcium channels (may reduce current) 2. Descending noradrenergic and serotonerigc pathway involvement
55
What are the therapeutic uses of gabapentanoids
1. Seizures 2. Neuropathic pain 3. Neuropathy 4. generalized anxiety disorder 5. Muscle spasms / spasticity
56
What are the warnings or precautions of gabapentanoids
1. Anaphylaxis 2. Angioedma 3. Somnolence, sedation 4. Suicidal behavior and ideation
57
What are the common SE of gabapentanoids
1. Dizziness, somnolence, peripheral edema 2. Pregabalin *dry mouth, *blurry vision *weight gain *abnormal thinking