Non-Opioid Lecture Part 3 (NSAIDS) Flashcards Preview

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1
Q

Mechanism of action of NSAIDS

A

Inhibit cyclooxygenase - reduces formation of prostaglandin precursors and thromboxane from arachidonic acid

  • Non-selective = inhibits both COX-1 & COX-2
  • Selective = inhibits COX-2
2
Q

NSAIDS peak after how long?
What are they metabolized by?
Excreted by what organ?
Half-life?

A
  • Peak in 1 to 2 hours
  • Metabolized by liver
  • Excreted by kidney
  • Half-life varies by product
3
Q

3 actions or effects of NSAIDS

A
  1. Analgesic
  2. Antipyretic
  3. Anti-inflammatory
4
Q

Difference between NSAIDs and Aspirin on how they affect the blood platelets

A

NSAIDS have a reversible effect on blood platelets
- Effect lasts only as long as the drug is in the bloodstream

Aspirin have an irreversible effect on blood platelets

5
Q

If a patient is taking low-dose aspirin (81 mg) to prevent stroke and have cardioprotection, how would you prescribe them to take ibuprofen?

A

Dose the ibuprofen at least 30 minutes or longer after aspirin ingestion or more than 8 hours before aspirin ingestion to avoid attenuation of aspirin’s effect

6
Q

Occasional use of ibuprofen or other NSAIDS pose little risk for attenuation of anti-platelet effects of low-dose aspirin why?

A

This is because the effects of aspirin on platelets are permanent (last for the life of the platelet)

7
Q

Indications for NSAIDS

A

Dental: pain, fever, inflammation

Medical: osteoarthritis, rheumatoid arthritis, gouty arthritis, fever, dysmenorrhea and pain

8
Q

Name two examples of NSAIDS that are NONSELECTIVE

A
  1. ibuprofen (advil, midol, motrin, ultrprin = OTC; motrin = prescription brand name)
  2. naproxen (aleve = OTC; Anaprox, Naprosyn = prescription brand names)
9
Q

Adverse events with NSAIDS?

A
  1. Increased risk of MI, stroke
  2. New onset or worsening of hypertension
  3. Compromised renal function
    • contraindicated in patients with advanced renal disease
    • excessive or chronic use = nephrotoxicity
  4. Gastrointestinal ulceration, irritation, bleeding and perforation
  5. CNS effects
  6. Adverse skin reactions
  7. Avoid in patients with aspirin allergy
  8. Use with caution if decreased hepatic function
10
Q

Target organ for NSAIDS

A

Kidney (not liver)

11
Q

Inhibiting prostaglandins shuts down what?

A

Renal blood flow

12
Q

What is the OTC dose for ibuprofen?

A

200 mg tablets

13
Q

What is the prescription dose for ibuprofen?

A

400-800 mg

14
Q

Describe the half life of ibuprofen

A

2-4 hours, short half-life = must take frequently

15
Q

How rapid is the onset of analgesia and duration of action?

A
  1. Rapid onset of analgesia (30-60 minutes)

2. Short duration of action (4-6 hours)

16
Q

Dental dosing of ibuprofen (Motrin)

A

Children: 4-10 mg/kg/dose every 6-8 hours

Adults: 200-400 mg/dose every 4-6 hours for a maximum daily dose of 1200 mg.

17
Q

Preoperative use of ibuprofen

A

a dose of 400-600 mg every 6 hours for 24 hours before the appointment decreases postoperative edema and hastens healing time.
Very good thing and can reduce opioid use after operation

18
Q

“Ceiling effect” for dental pain

A

optimal analgesia occurs at 400 mg dose.
If you prescribe more, you get the anti-inflammatory effect. (this is used for examples like arthritis) 400-800 mg 4 times daily with a maximum dose not to exceed 3200 mg. This is for patients with chronic inflammatory pain

19
Q

Give the example of writing a prescription for ibuprofen

A

Rx: ibuprofen 400 mg tablets
Disp: 16 tablets
Take 1-2 tablets by mouth 3-4 times per day as needed for pain. Do not exceed 8 tablets within 24 hours

20
Q

What is the OTC brand name for naproxen? What about the 2 prescription names/

A
OTC = Aleve
Presc. = Anaprox, Naprosyn
21
Q

Describe the onset of analgesia, duration of action and half life for naproxen

A

onset of analgesia: 1 hour
Half-life: 12-17 hours
Duration of action: analgesia < 7 hours; anti-inflammatory <12 hours; peaks after 2 weeks

Very long half life

22
Q

Dental dosing of naproxen?

A

adults: 500 mg initially, then 250 mg every 6-8 hours

23
Q

What is the maximum dosage of naproxen per day?

A

1250 mg/ day

24
Q

What NSAID has the longest half-life in dentistry?

A

piroxicam (Feldene) = longest acting of all NSAIDS
half-life of 45-50 hours
10 mg 2 times per day

25
Q

Name 4 other important NSAIDS in dentistry

A
  1. piroxicam (Feldene)
  2. flurbiprofen (ANSAID)
  3. ketorolac (Toradol)
  4. diflunisal (Dolobid)
26
Q

Which of the NSAIDS is taken primarily by injection?

A

ketorolac (Toradol)

- Severe acute pain requiring analgesia at opioid level

27
Q

Which of the NSAIDS is considered a “super aspirin”? Does this NSAID have a better efficacy than aspirin? Why would it have an advantage?

A

diflunisal (Dolobid)

  • No greater efficacy than aspirin
  • KNOW THIS** Advantage = longer half-life; only have to take 8-12 hours versus 4-6 hours with aspirin. This improves compliance
28
Q

When writing a prescription for pain, what are the 2 ways to do it?

A
  1. as needed for pain = “prn”
  2. Every 6 hours
  • This is done so that the blood level never falls below the therapeutic blood level
29
Q

Name 3 psychological considerations when prescribing

A
  1. A prescription drug gives more relief to a patient than an OTC drug = psychological
  2. More relief with expensive drug vs cheap drug
  3. More relief from colored pills vs. white pills
30
Q

What is the only selective NSAID?

A

celecoxib (Celebrex) –> only one available
- COX 2 inhibitor

  • obtained original approval for arthritis pain
31
Q

T or F, COX-2 inhibitors have better adverse events profile than non-selective

A

True

32
Q

What are some benefits of anti-inflammatory effect of COX-2 inhibitor

A
  1. Celebrex has been shown to reduce risk for adenocarcinoma of the colon
  2. Improvements in lung cancer, and possibly oral cancer
  3. Celebrex shown to delay onset and degree of severity of Alzheimers disease
33
Q

Dosing for celecoxib (Celebrex)

A

Initial 400 mg dose, followed by an additional 200 mg dose if needed on day 1. Then, maintenance dose: 200 mg twice daily as needed
- Used for acute dental pain

34
Q

What does Celebrex contain that some might be allergic

A

Sulfa atom

35
Q

COX-2 inhibitor is contraindicated in what 2 scenarios

A
  1. Aspirin/NSAID allergic patients

2. Patients with history of gastritis/gastric ulcer/GI bleeding

36
Q

If a patient is on Methotrexate, what drug for pain relief would you give?

A

Tylenol (acetaminophen), ibuprofen/aspirin inhibits the breakdown of methotrexate, causing toxicity

37
Q

Is it ok for patients on Lithium to take NSAIDS? Why?

A

No, NSAIDS block excretion of lithium, resulting in toxicity

38
Q

Is it ok to take multiple NSAIDS together?

A

taking multiple together can give an additive toxic effect

39
Q

What is the adverse effect of taking alcohol with NSAIDS?

A

increases the risk for GI bleeding associated with aspirin and NSAIDS

40
Q

Aspirin and NSAIDS may decrease the effectiveness of what medications?

A

Many common antihypertensive medications

41
Q

Acetaminophen nickname?

A

APAP (N-Acetyl-P-Aminophenol)

42
Q

T or F, acetaminophen acts centrally and acts more upon peripheral COX than CNS COX

A

False, It does act centrally but acts more on CNS COX rather than peripheral COX

43
Q

acetaminophen is metabolized by what organ?
acetaminophen is excreted by what organ?
Half life of acetaminophen
Peak plasma level occurs when?

A

Metabolized by liver
Excreted by kidneys
Half-life: 1 to 4 hours
Peak plasma level occurs in 1 to 3 hours

44
Q

T or F, acetaminophen metabolite is hepatotoxic but not nephrotoxic

A

False, both hepatotoxic and nephrotoxic

45
Q

Actions of acetaminophen

A
  1. Analgesic

2. Antipyretic

46
Q

Maximum dose of acetaminophen

A

4000 mg (4 grams per day)

47
Q

T or F, acetaminophen and aspirin are equally efficacious (reduces same degree of pain) and equally potent (same dose in milligrams needed for effect)

A

True

48
Q

How is acetaminophen less useful clinically?

A

It is not an anti-inflammatory

49
Q

Dental dosing for acetaminophen

A

Children: 10-15 mg/kg/dose every 4-6 hours as needed
- do not exceed 5 doses (2.6 grams) in 24 hours
Adults: 325-650 mg every 4-6 hours or 1000 mg 3-4 times per day. Do not exceed 4000 mg per day.

**Do not exceed 2 grams per day in patients who regularly consume alcohol

50
Q

Avoid using acetaminophen in what patients?

A
  1. Liver disease/dysfunction
  2. Alcohol
  3. **In patients on warfarin (Coumadin)
51
Q

Why is acetaminophen contraindicated with warfarin (Coumadin)?

A

It causes enhanced anticoagulation

- Increased bleeding risk