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Orthopedics > Orthopedic Pharmacology > Flashcards

Orthopedic Pharmacology Flashcards

1
Q

What are the most preferred NSAIDS in patients?

A

Naproxen and ibuprofen are preferred in most patients

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2
Q

What are the different classes of NSAIDS?

8

A

Different classes

  1. Salicylate (acetylated)
  2. Salicylate (nonacetylated)
  3. Propionic acids (phenyl-propionic acid)
  4. Acetic acids
  5. Oxicams
  6. Fenamates
  7. Nonacidic
  8. Selective Cox-2 inhibitors
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3
Q

PATIENT RESPONSE TO DIFFERENT NSAIDS IS VARIABLE

  1. How should we manage these if a drug doesnt work initially?
  2. How long should they be on it?
  3. Trial for how long before failure?
  4. Toxic effects usually span all classes such as?
A
  1. Reasonable to substitute with a different therapeutic class if failure of one drug
  2. Trial of 2 weeks and at max anti-inflammatory dose before failure is considered
  3. However, toxic effects – usually span all classes
    Example: renal failure
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4
Q
  1. Describe the MOA for NSAIDs. 3
  2. COX-1 enzymes? 4
  3. COX-2 enzymes? 2
A
  1. Inhibit cyclooxygenase which impairs the transformation of:
    - Arachadonic acid →
    - prostaglandins →
    - prostacyclin and thromboxanes
2. COX-1 enzymes
Regulates normal cellular processes 
-(gastric cyctoprotection, 
-vascular homeostasis, 
-platelet aggregation, 
-kidney function)
  1. COX-2 enzymes
    - Expression of this is increased during states of inflammation
    - Effects of COX-2 inhibition on inflammation is not completely understood
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5
Q

Adverse affects of NSAIDS?

9

A
  1. GI
  2. Renal
  3. CV
  4. Liver
  5. Pulmonary
  6. Hematologic
    .7 Malignancy
  7. Dermatologic
  8. Healing of MSK injuries
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6
Q

SOME ORGAN SPECIFIC NSAID ADVERSE REACTIONS

  1. Renal? 7
  2. Hepatic? 3
  3. Pulmonary? 3
  4. Hematologic? 2
A
  1. Renal
    - Renal vasoconstriction**
    - acute renal failure,
    - hypertension,
    - hyperkalemia,
    - hyponatremia,
    - edema,
    - increased risk of renal cell cancer
  2. Hepatic
    - Can cause elevation of liver transaminases
    - Actual NSAID associated liver injury is rare
    - May be disease specific (more common in SLE and RA)
  3. Pulmonary
    - Adverse events seem to be more likely to be related to nonselective COX 1/2 inhibitors and less likely with selective COX 2 inhibition
    - Bronchospasm
    - Pulmonary infiltrates with eosinophilia
    • Neutropenia
    • Antiplatelet effects due to inhibition of COX-1
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7
Q

SOME ORGAN SPECIFIC ADVERSE REACTIONS: Hematologic?
1. For most NSAIDs platelet function normalizes within how long of discontinuation of the drug? (When for ibuprofen)

  1. But still need to continue what for carrdioprotection if using NSAID therapy?
  2. What may increase INR?
  3. Higher risk of bleeding with what?
A
  1. 3 days (24 hours)
  2. ASA
  3. Interaction with warfarin, may increase the INR
  4. Higher risk of bleeding with anticoagulant use
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8
Q

Adverse affects of NSAIDS cont

  1. CNS? 3
  2. Skin? 2
A
  1. CNS
    - Aseptic meningitis
    - Tinnitus
    - Psychosis and cognitive impairment
  2. Skin
    - Drug rash or pseudoporphyria (blistering with sun exposure)
    - Blistering skin lesions that may be potentially life threatening
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9
Q

Tinnitus usually occurs with what?

Treated how?

Psychosis more common with?

And more commonly seen in who?

A
  1. Usually with salicylates but can occur with all NSAIDs
  2. Usually reversible upon drug discontinuation
  3. More common with indomethacin
  4. Most common in the elderly
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10
Q

NSAID skin reactions:

Blistering skin lesions that may be potentially life threatening. Such as? 2

A
  1. TENS

2. Stevens-Johnson syndrome

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11
Q

NSAID affects on fractured healing:

  1. May cause?
  2. Avoid for how long post fracture
A
  1. May cause non-union (approximately 1%)
  2. May want to avoid NSAIDs for up to 90 days post fracture
    Data is not clear, more studies needed
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12
Q

NSAID CONTRAINDICATIONS: REMEMBER NSAID

A 
Nursing or pregnancy
Serious bleeding
Allergy/asthma/angioedema
Impaired renal function
Drug (anticoagulants)
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13
Q

SALICYLATE (ACETYLATED)

  1. What drug is in this group?
  2. How is it different from other classes?
  3. Dont use to treat what?
  4. What may dampen its antiplatelet ability?
  5. Should you continue with the addition of another NSAID?
A
  1. Aspirin is the only one in this group
  2. Different from the other classes by irreversible platelet inhibition for the life of the platelet
  3. Don’t use to treat pain, just use for it’s CV protective effects
  4. Other NSAIDs may dampen it’s anti-platelet effects
  5. Usually continue chronic aspirin use if adding another NSAID for pain management
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14
Q

PROPIONIC ACIDS

Which drugs are these? 2

A
  1. Naproxen
    - Aleve
    - Naprosyn
  2. Ibuprofen
    - Advil
    - Motrin
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15
Q

NAPROXEN

  1. Avilable how?
  2. Long, short, intermediate acting?
  3. Advantage?
  4. 2 formulations?
  5. Dosing?
  6. Max daily dose?
A
  1. Available over the counter
  2. Long acting
  3. Less CV risk compared to the others
  4. 2 formulations: Naproxen base and Naproxen sodium
  5. Dose (200 mg naproxen base = 220 mg naproxen sodium)
    Naproxen base: 250-500 mg every 12 hours
    Naproxen sodium: 275-550 mg every 12 hours
    -Has a quicker onset of action than the base formulation
  6. maximum daily dose: Day 1: 1250 mg naproxen base; subsequent daily doses should not exceed 1000 mg naproxen base
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16
Q

Anaprox DS 550 mg, 1 tab po BID is the max dose of per day
(what drug is this?)

good for?

A

Aleve (naproxen sodium) comes in 220mg tabs

Good choice for treatment of acute or chronic pain if an NSAID is indicated

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17
Q

IBUPROFEN

  1. Avilable how?
  2. Duration of effect?
  3. Alternative to?
  4. Max dose?
  5. Usual anagelsic dose?
A
  1. Available over the counter
  2. Short duration of effect
  3. Alternative to naproxen
  4. Max dose 2400 mg per day (up to 3200 mg on day 1 if loading dose is used)
    May give a loading dose of up to 1600 mg
  5. Usual analgesic dose is 400 mg every 4-6 hours
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18
Q

ACETIC ACIDS

Drugs?

A
  1. IV Ketorolac (Toradol)

2. Indomethacin (Indocin)

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19
Q

KETOROLAC (TORADOL)

  1. Loading dose?
  2. Adjust dose how?
  3. Tx for?
  4. Risk?
  5. Cant use how?
  6. Dont use for what?
  7. What do we have to do before we give a patient this?
A
  1. Optional loading dose 30 mg
  2. Adjust dose based on age and weight
  3. Treatment of moderate to severe postoperative pain
  4. Risk of gastropathy when used > 5 days
  5. Not for oral use
  6. Don’t use for chronic pain or inflammation
  7. Make sure patients are well hydrated and without significant kidney disease
20
Q

INDOMETHACIN (INDOCIN)

  1. Optimal loading dose?
  2. Comes in what formulations? 2
  3. Max dose?
  4. Used for tx of? 2
  5. Not for what use?
  6. May be associated with what risk?
A
  1. Optional loading dose 75 mg
  2. Comes in an immediate release and extended release formulation
  3. Max dose per day is 150 mg
  4. Used for treatment of acute gout and pericarditis mainly
  5. Not for chronic daily use
  6. May be associated with aplastic anemia
21
Q

Which are the OXICAMS? 2

A

Meloxicam (Mobic)

Prioxicam (Feldene)

22
Q

MELOXICAM (MOBIC)

  1. Duration of affect?
  2. Onset of action?
  3. Max dose?
  4. How is it different at a lower dose?
A
  1. Long duration of effect (Qday dosing)
    - 7.5-15 mg Qday
  2. Slow onset of action
  3. Max daily dose is 15 mg
  4. Relatively COX-2 selective at lower total dose of 7.5 mg
23
Q

PIROXICAM (FELDENE)

  1. An option for tx of?
  2. Daily doses of ≥ 20 mg increase risk of what?
  3. Usual daily dose?
A
  1. An option for treatment of chronic pain and inflammation poorly responsive to other NSAIDs
  2. serious GI complications
  3. Usual daily dose is 10-20 mg once daily
24
Q

SELECTIVE COX-2 INHIBITOR

drug?

A

Celecoxib (Celebrex)

25
Q

CELECOXIB (CELEBREX)

  1. loading dose?
  2. Max daily?
  3. Usual dose?
  4. Affect on platelet function?
  5. Advanatge?
  6. Dose related affects on what?
A
  1. Optional loading dose of 400 mg
  2. Max daily dose is 400 mg
  3. Usual dose is 100 mg BID or 200 mg daily
  4. No effect on platelet function
  5. Decreased GI toxicity
  6. Dose related renal and CV effects
26
Q

ACUTE PAIN WITH FRACTURES

  1. Pain with fx site usually lasts how long?
  2. What kind of pain should be investigated?
  3. What are our options?
A
  1. Pain from the fracture site usually lasts a few days to a week
  2. Pain that persists, changes or worsens over this time period should be investigated
  3. Sometimes just APAP or an NSAID are adequate, often times a narcotic analgesic is warranted
27
Q

HOW DO YOU JUDGE WHO NEEDS NARCOTICS? 5

A
  1. Significant soft tissue swelling or ecchymosis suggests significant injury
  2. Pain at rest
  3. Night pain (Sometimes may just need narcotics at night)
  4. Pain uncontrolled by NSAIDs or APAP
  5. Anyone who has had surgery
28
Q

NARCOTIC PAIN RELIEF: Drugs

3

A

Codeine
Hydrocodone
Oxycodone

29
Q

CODEINE

  1. Strength?
  2. For what kind of pain?
  3. Metabolized to?
  4. What happens if its not metabolized?
  5. What happens if its metabolized too quickly?
  6. Schedule?
A
  1. Considered a weak opioid
  2. For mild to moderate pain
  3. Metabolized to morphine
  4. If not properly metabolized is not effective
  5. If metabolized too quickly = initial “overdose”, shorter duration of action, more side effects
  6. Schedule III

5-10% of patients have a genetic variation for metabolism and may have only limited or no benefit from codeine

30
Q

HYDROCODONE

  1. Which drugs are these? 4
  2. Schedule?
  3. For what kind of pain?
  4. Onset of action?
  5. Duration?
  6. In combo with?
A
    • Lorcet,
    • Lortab,
    • Norco,
    • Vicodin
  2. Schedule III
  3. For moderate to severe pain
  4. Onset of action 10-20 min
  5. Duration of action 4-8 hours
  6. In combination with acetaminophen
31
Q

OXYCODONE

  1. Which drugs? 3
  2. Schedule?
  3. Used for what kind of pain?
  4. Onset of action?
  5. In combo with what?
  6. Avoid long acting combos for what?
A
    • Percocet,
    • Roxicet,
    • Endocet
  2. Schedule II
  3. Moderate to moderately severe pain
  4. Onset of action 10-30 minutes
  5. In combination with acetaminophen
  6. Avoid long acting combinations for acute pain (MS Contin, etc)
32
Q

NALOXONE

  1. What does it do? 3
  2. Dosing?
  3. Why might you need to repeat the dose?
A
  1. Reverses
    - respiratory depression
    - sedation
    - analgesia
  2. 0.04 mg-0.08 mg IV push Q 1 min- X2
  3. May need to repeat dosing as half life is short
33
Q

EXTENDED RELEASE & LONG ACTING OPIOID ANALGESICS

NEVER USE IN WHO? 2

A
  1. Never use for acute pain

2. Never use in a narcotic naïve patient

34
Q

TOXICITIES OF ALL OPIOIDS IN GENERAL

4

A
  1. Sedation and respiratory depression
  2. Constipation
  3. Decreased effectiveness of diuretics
  4. QT prolongation
35
Q

TOXICITIES OF ALL OPIOIDS IN GENERAL
1. Sedation and respiratory depression. Which are these? 5

  1. Constipation: Worse with what?
  2. What do you have to remember about tx?
  3. Decreased effectiveness of diuretics. How?
A

Drugs that act on the CNS potentiate effects

    • Alcohol,
    • sedative-hypnotics,
    • TCAs,
    • BZDs,
    • MAOIs
  2. Worse with sustained release morphine compared to fentanyl patch
  3. Stool softeners alone are often not enough
  4. Induce release of ADH and counteracts the effects of diuretics
36
Q

Check for cyochrome P450 inhibitors or inducers
Opioid drug levels may increase or decrease beyond the expected range when given concomitantly with these drugs
1. Which are the inhibitors? 12
2. Inducers? 5

A
  1. Inhibitors:
    - Bupropion,
    - fluoxetine,
    - paroxetine,
    - cimetidine,
    - acyclovir,
    - duloxetine,
    - fluoroquinolones,
    - ketoconazole,
    - PPIs,
    - verapamil,
    - diltiazem,
    - grapefruit juice
  2. Inducers:
    - Carbamazepine,
    - isoniazid,
    - tobacco,
    - rifampin,
    - St. John’s wort
37
Q

EXTENDED RELEASE AND LONG ACTING OPIOID ANALGESICS

5

A
  1. Morphine sulfate ER
    - MS Contin, Kadian, Embeda, Avinza
  2. Buprenorphine Transdermal
    - Butrans
  3. Methadone
    - Dolophine
  4. Fentanyl Transdermal
    - Duragesic
  5. Hydromorphone
    - Exalgo
38
Q

RULES FOR TRANSDERMAL ADMINISTRATION

2 things to remember?

A
  1. Never cut or tear a patch

2. Heat exposure can increase release and absorption of transdermal opioid analgesics

39
Q

RULES FOR TRANSDERMAL ADMINISTRATION

Application? 4

A

Application

  1. Chest, side of waist, upper arm
  2. Avoid hairy areas but if not clip (do not shave) the hair
  3. Rotate sites
  4. Wash site with water only
40
Q

Tramadol

  1. Describe the potential for abuse?
  2. MOA? 2
  3. Effective for?
  4. Improved functional outcomes in patients with what?
  5. Chronic pain effectiveness?
A
  1. Not a controlled substance but has a high potential for physical and psychological dependence
  2. Works at the mu receptors and also inhibits NE and serotonin
  3. Effective for relief of neuropathic pain
  4. Improved functional outcomes in patients with fibromyalgia
  5. May be no more effective than NSAIDs or nortryptyline for chronic pain
41
Q

TRAMADOL

  1. Metabolized by?
  2. Use in caution with who? 2
A
  1. Extensively metabolized in the liver
  2. Use with caution in the
    - elderly and
    - with renal insufficiency
42
Q

SKELETAL MUSCLE RELAXANTS

drugs? 4

A
  1. Cyclobenzaprine (Flexeril)
  2. Tizanadine (Zanaflex)
  3. Metaxalone (Skelaxin)
  4. Diazepam (Valium)
43
Q

MUSCLE RELAXANTS

  1. Duration of use?
  2. Most benefit is within what time period?
  3. SE?
  4. Not generally for long term use unless why?
A
  1. Short course of therapy only
  2. Most benefit is within the first 1-2 weeks of therapy
  3. Very sedating with anticholinergic side effects
  4. Not generally for long term use unless neuromuscular problems that cause spasticity
44
Q

MUSCLE RELAXANTS: RISK OF ABUSE

Which drugs should just be used for a few days? 2

A
  1. Diazepam (Valium) and
  2. carisoprodol (Soma) use should be brief (just a few days)
    High potential for abuse
45
Q

MUSCLE RELAXANTS + NSAIDS

May have synergistic affect used for?

A

May have a synergistic effect for the treatment of acute low back pain

In other words – patients are more likely to improve when used in combination

46
Q

Avoid bowel obstruction by treating with what? 2

A
  1. stool softeners and

2. gentle stimulant laxatives as needed

Orthopedics (27 decks)

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