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PHAR 398: Minor Ailments > OTC Analgesics > Flashcards

OTC Analgesics Flashcards

1
Q

Common dosing of morphine for moderate to severe pain?

A

For moderate to severe pain, morphine might be
started at 5-10 mg Q4H.

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2
Q

Describe the morphine equivalents (10 MEQ) of the available OTC analgesics. What does MEQ of 10 mean?

A

We need this amount of each agent to get to the
same painkilling level as 10 mg morphine.

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3
Q

What is an issue with Tylenol-3’s for analgesia?

A

Codeine – 2D6 – Metabolized to morphine – pro-drug – Not consistetnt across the population – based on genetics and race

T3s are terrible - slow metaboizer may not even help; rapid metabolizer okay for pain control

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4
Q

What are the available NSAID’s and there OTC limiting dosing? What does this mean as comapred to acet at OTC doses in comparison of MEQ 10? Exception?

A

1200 mg ibup
440 mg naproxen

This means theoretically they are LESS effective than acet at OTC doses

However, many patients say NSAIDs work better for them (anti-inflammatory action)

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5
Q

What are some recommendations for dosing of Ibuprofen and Naproxen?

A
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6
Q

What is unique about OTC analgesics compared to morphine? AT what values does this effect occur at?

A

Ceiling Effect of Analgesia

Morphine has no celining effect: Can lead to respiratory depression and therefore body develops tolerance to it so greater doses can be used –> Common in pallitative care as do not want to play catch up

Ibuprofen –> Max analgesia achieved at 400 mg dose. Individual doses greater than 400 mg do not provide further analgesia

ASA/ACET –> Individual doses greater than 1000 mg do not result in further analgesia

Acet –> 1000 mg –> No anti-inflammatory action

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7
Q

Describe OTC dosing in dental pain and if the ceiling effect is maintained for analgesia and inflammation? Certain Disease States?

A

Ceiling effect of analgesia is maintained; however, dental pain includes an inflammatory component

If inflammation is present, all best are off as higher doses can help to achieve anti-inflammatory effects

Pain mangement for osetoarthritis may have a ceiling effect, but dental and rheumatoid can go into higher doses for analgesia and anti-inflammatory

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8
Q

Describe non-opiod analgesics and there anti-inflammatory dosing. Key points to consider regarding usage of NSAID’s?

A

Nonopiods exhibit a ceiling effect for their analgesia response but optimal doses should be established before it is assumed that an NSAID has failed

Acetaminophen does not have an anti-inflammatory effect; however, a combination of an NSAID and acetaminophen provide greater analgesia efficacy than does either agent alone

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9
Q

Is ibuprofen at OTC doses harder on the stomach at OTC doses? Describe the rate of benefit?

A

NO

Adverse effects of OTC analgesics are generally no different from placebo

Chances of getting help for acute pain range from 70% at best to 20% at worst

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10
Q

Describe the rates of adverse effects related to tolerability of oTC analgesics?

A

Ibuprofen: 13.7%
Acetaminophen: 14.5%
ASA: 18.7%

The overall tolerability of OTC ibuprofen 1200 mg/day was equal to acet 3000 mg daily but superior to ASA 3000 mg/day

Chance of all side effects here; RX doses all bets are off

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11
Q

Describe the rates of GI adverse effects of OTC Ibuprofen and Acet. How can a pharmacist frame this to a patient?

A

At OTC doses, ibuprofen does NOT have more side effects !!

Almost every pharmacist gives acet more credit for less s/e

Frame these as ‘nuisance side effects’
–> 10% acet, 10% ibu, 10% placebo

Placebo is around 10% for these adverse effects

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12
Q

Describe the evidence of Ibuprofen and GI adverse effects compared to placebo? Ibu and Acet?

A

Symptomatic GI side effects with Ibuprofen are comparable with placebo and treatment is well tolerated and largely free of gastric damage

Large trials of ibuprofen and acetaminophen, the risk of GI bleeding was low with no statistically significant difference in GI bleeding between the two

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13
Q

Describe the overall adverse effect profile of acet and ibuprofen.

A

Ibuprofen and acetaminophen have similar reported adverse effects

There is comparable safety for ibuprofen and acetaminophen at OTC doses

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14
Q

Describe the incidence rates of adverse effects of Ibuprofen statistics? Exception?

A

3-9% –> Nausea, epigastric pain and heart burn

Less than 1% –> Gastric or duodenal ulcer (Higher doses and longer term usage)

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15
Q

Is heartburn/epigastric pain the same as an ulcer?

A

Heartburn is not the same as an ulcer

One can have an ulcer and be asymptomatic

One can have painful symptoms but no pathology in the stomach

The linkage between the symptoms and pathological mechanisms is weak and is not a 1:1 or linear ratio

Therefore, can not say heartburn is the same as an ulcer

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16
Q

What are some signs and symptoms of a stomach ulcer?

A

Nausea
Blood in Vomit
Indigestion
Loss of appetite
Pain in Stomach
Stool Discoluration

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17
Q

What is a critical counselling point to include when counselling someone on OTC acteaminophen?

A

Do you use any other products that might have acetaminophen?

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18
Q

Describe the effect of taking an NSAID with food? Does it prevent GI adverse effects?

A

Fluid or food helps clear a pill from the esophagus

It can help reduce some local damage to stomach

It will NOT prevent GI damage via systemic PG inhib (systemic effect)

Food can actually delay onset of action (if need fast action, take without food)

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19
Q

If someone wants a faster analgesic response, are gel caps more useful than tablets for Ibuprofen?

A

Could be useful for some patients; however, often not relevant

Different delievery mechanism; gel caps are 2 minutes faster

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20
Q

Why does taking food with Ibuprofen not protect from GI ulcers?

A

Ibuprofen is a non-selective NSAID and therefore is blocking both COX-1 and COX-2 to varying degrees

COX-1 is required for gastric production through mucous protection; therefore, blocking COX-1 can lead to GI damage

Systemic effect; food will not prevent the systemic effect

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21
Q

What is a concern with NSAID administration with food?

A

Food will not provide systemic protection from COX-1 inhibition

Food may lead to a slower onset of action

If someone wants fast analgesia, taking an NSAID without food may be the appropriate course of action

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22
Q

Describe Enteric Coated Aspirin and its absoprtion and use?

A

EC ASA delays maximum pain relief as long as 3 to 4 hours

Therefore, this product will not provide fast relief of headaches or other symptoms

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23
Q

Does enteric coating lower the risk of GI bleeding?

A

Enteric Coating ASA is just as likely to cause stomach bleeding and therefore is not safer than regular aspirin

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24
Q

Is the coating of ASA always for delayed release?

A

No

Sometimes ‘coatings’ are on the tablet to simply make it taste better getting by the mouth (Not ER or XR here, just taste)

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25
Q

Regarding NSAID’s, what stance does a pharmacist commonly focus on?

A

Take an approach with s/e, C.I., risks, fine print

Risk people, need to lower the risk

Shift focus to this person needs help

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26
Q

Describe the decision of using Ibuprofen and the risks in a patient?

A
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27
Q

Describe the BEER’s List stance on NSAID use in geriatric patients?

A

Adults aged 65 years and older

Experts found that older adults should avoid even short term use of NSAIDs for pain, emphasizing their high risk when used in combination with:

1) Steroids
2) ANticoagulants

When no alternatives exist, pt’s should be placed on misoprostol or a proton pump inhibitor while taking NSAID’s

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28
Q

BEER’s List and NSAID and Risk Factors for GI Bleed

A

No safe dose of an NSAID for seniors over the age of 65 years old

Incraesed risk with:

1) Steroids
2) SSRI’s (7-fold increase)
3) ANti-coagulants (DOAC”s better than warfarin but can still cause GI bleed)

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29
Q

Describe the use of NSAIDs in CV and GI risks in reviews and what a pharmacist should do in this situation?

A

Almost all the big reviews focus on GI and CV risk, yet fail to mention that by not treating, PAIN is not treated, and that may be worse for the patient

Need to balance the benefits and the risks

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30
Q

Describe the analgesic combinations marketed for nightime pain releief? What is added? Are these agents good?

A

NSAIDs or acetaminophen in combination with either:

1) Methocarbamol: Muscle relaxent –> Does nothing for muscle relaxing, just dizziness and sedation

2) Diphenhydramine –> BEERs list and incraesed fall risk –> Not a good sleep aid

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31
Q

Describe the incidence of insomnia and pain?

A

It is estimated that 60-80% of pain patients experience symptoms of insomnia

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32
Q

What are the mechanisms for pain occuring at night?

A

Lower levels of anti-inflammatory hormone cortisol at night

Staying still in one position might cause the joints to stiffen up

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33
Q

Describe the prevalence of the nature of pain

A
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34
Q

Describe the prevalence of pain severity?

A
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35
Q

How can pain be evaluated in children? Is this common in pharmacy practice?

A

Evaluating behavioural signs such s facial expressions, crying, irritablity, poor feeding, sleep disturbance, and inactivity

Level of asessment not commonly done at the community pharm level

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36
Q

First Line medications for analgesia in children

A

Acetaminophen and Ibuprofen

Comparable safety profile

Go for flavour here or what they have used before

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37
Q

Analgesics for headache including migraines

A

NSAIDs or Acet

ALSO TRIPTANS

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38
Q

Describe the difference between a headache and migraine

A
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39
Q

Is Advil 12 hour a major improvement?

A

12 Hour – Simplicity

300 mg on outside and 300 mg inside

CONVENIENCE – TOTALLY fine

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40
Q

Are Tylenol liquid gels a major improvement?

A

Five mins faster than tabs next to it

Not a major advancement

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41
Q

What use to be the drug of choice for osteoarthritis? Is it still the drug of choice?

A

Acetaminophen use to be the drug of choice

Now is on the verge of no longer being DOC

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42
Q

Describe the prevalence of osteoarthritis

A

60% of people with arthritis are women

6 million Canadians

1/6 men have arthritis

Arthritis can effect people of any age; however, the likelihood increases with age with nearly 1 in 2 seniors over the age of 65 having arthritis

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43
Q

Average age at diagnosis of arthritis

A

50 years old

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44
Q

Average age at first symptoms of arthritis

A

47.5 years old

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45
Q

Is Acetaminophen useful for arthritis?

A

Acetaminophen only provides minimal improvements in pain and function with no increased risk of adverse events overall

The effects on pain and function do not differ according to the dose of acetaminophen

Verge of being placebo

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46
Q

Is the effect of acetaminophen in osteoarthritis dose related?

A

NO NOT DOSE RELATED

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47
Q

Describe what a pharmacist should do if someone is wanting acet for osteoarthritis?

A

Some people do seem to get value out of this, but numbers are shrinking and not good

If it works for someone, good enough

For first recommendation, if go with this:

Try for 2 weeks and see if it helps – if it doesn’t work, we will try something different

Where NSAID’s kick in - need to go to this to help with pain or do nothing

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48
Q

What is the drug of choice for osteoarthristis? When would it be used?

A

Topical Diclofenac should be considered first line

One or two joints – topical diclofenac

Both hips, elbows, and phalanges – tough to manage with topical

  • Topical – best for isolated joints
  • At some point, will probably need to consider oral
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49
Q

What agent and dose had the lowest effect on osteoarthritis pain?

A

Paracetamol 4000 mg/day had the lowest effect on OA pain

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50
Q

Acet is not looking like a valuable therapy for…..

A

Arthritis and Low Back Pain

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51
Q

What is the drug of choice for dysmenorhhea?

A

NSAIDs are the drug of choice

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52
Q

Why are NSAIDs the drug of choice for dysmenorhhea?

A

Menstrual cramps are causes by contractions in the uterus by prostaglandins

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53
Q

What is dysmenorhhea?

A

Cramping pain in the lower abdomen that can start from 1-2 days before your period and can last up to 2-4 days

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54
Q

Describe the prevalence of dysmenorhhea?

A

Most commonly reported menstrual disorder

More than one half of women who menstruate have some pain for 1-2 days each month

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55
Q

Can acet be used for dysmenorhhea?

A

NSAIDs are preferred, but acet is an option too

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56
Q

Describe the avilable agents for dysmenorrhea. Are all useful for dysmenorhhea?

A

Midol: Acet 500 mg, Caffeine 60 mg, and pyrilaminate maleate 15 mg
- Caffeine is a diuretic here, so for PMS not Dys

Maxidol: NAproxen 220 mg

Advil: Ibu 200 mg

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57
Q

What is the purpose of caffeine with an analgesic?

A

caffeine – Diuretic

need 100 mg to be analgesic with the Ibu or Acetaminophen

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58
Q

How much caffeine is in a cup of coffee? Who is acffeine useful as an analgeisc in? WHich condition in females?

A

100 mg in a cup of coffee
- PMS

  • Caffine drinker – stabilized intake and outake –>will pee it out in a couple of hours
  • Cafeine Naieve Individuals (those who do no consume caffeine) - enhance analgesic effect through vasoconstrictive properities
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59
Q

How can one manage toothaches?

A

Acet and Ibu combination may be effective here

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60
Q

What is a strategy that can be used to manage post-operative dental pain? Issue:

A

Ibuprofen (400-600 mg) every four to six hours (2400 mg/day max)

AND

Acetaminophen (650-1000 mg) every six hours (max of 4000 mg/day)

HOWEVER:

OTC max of Ibu is 1200 mg/day

600 mg Ibuprofen and 1000 mg Acetaminophen administered every 6 hours (four times daily) for 24 hours

2-4-24 Rule (2 drugs, 4 doses, 24 hours)

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61
Q

Describe the combination product Advil plus Acetaminophen. Issue:

A

Ibuprofen 125 mg
Acetaminophen 250 mg

Two tablets every 8 hours (6 max/day)

Number look low here

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62
Q

Describe the concept of the combination of Advil plus acetaminophen?

A

The concept here is that lower doses in the fixed-dose combo gets just as good (or better) relief, with less frequent dosing, and not a jump in side effects.

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63
Q

Describe the formulation of combogesic?

A

Acet 325 mg

Ibup 97.5 mg

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64
Q

When would one select Aleve over another NSAID?

A

Dosing less frequent –> BID

Value: More CV protection –> As far as grey areas, a little more safer in the CV front
– Can be worse for GI

  • Ibu is better for GI than Aleve; but more risk with CV
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65
Q

Describe Tylenol Ultra Relief. Who is it useful for? When is it useful? Side effect?

A

Acetaminophen 500 mg
CAffeine 65 mg

Need 2 tablets here to get benefit

Caffeine naieve people may get some diuresis

Migraines –> Good choice to include for relief of pain

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66
Q

Efficacy of caffeine as an analgesic Efficacy. In what conditions?

A

Compared with analgesic medication alone, combinations of caffeine with analgesic medications, including acetaminophen, ASA, and Ibuprofen, showed significantly improved efficacy in the treatment of TTH and Migraine

Favourable tolerability in most

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67
Q

Dosing of caffeine in in TTH and Migraines

A

Caffeine doses of 130 mg enhance the efficacy of analgesics in TTH and doses of > 100 mg enhance benefits in migraine.

100 mg is close enough for benefit

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68
Q

What is medication overuse headache?

A

When more medications lead to more headaches

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69
Q

Concern of Caffeine in Combination with Analgesics

A

Analgesic combos containing caffeine are more likely to induce Medication Overuse Headaches than simple NSAIDs alone.

Caffeine-containing formulations are therefore reserved as 2nd options for Tension Headache and should not be used more than 9 days per month.

THINK OF 10 DAYS of USE PER MONTH

Days of therapy with meds; not how much drug you take

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70
Q

What is the number of days of therapy with an analgesic and/or caffeine when one should be worried about medication overuse headaches?

A

Think of 10 – painkilling person taking the drugs for 10 days a month

Worried about medication overuse headaches here

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71
Q

What types of medications can lead to medication overuse headaches?

A

Most headache medications have the potential to cause medication overuse headaches

NSAIDS, Acetaminophen with caffeine are the most common culprits

Most refs do NOT agree that NSAIDs get a pass on this, with one saying that virtually all acute headache meds can cause them.

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72
Q

Is medication overuse headaches a concern with all individuals taking NSAIDs?

A

A pre-existing headache disorder seems to be required to get MOH.

Migraine and TH have high potential for adding these on.

It is generally not observed in people taking analgesics for reasons other than headaches, such as arthritis or back pain.

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73
Q

When would we be concerned about medication overuse headaches regarding conditions?

A

If have a neurological disorder (arthritis + migraines/tension headaches)

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74
Q

In general, what OTC analgesics are less lethal in overdose?

A

NSAID’s – Lower concern; a lot of it is just supportive care

ASA and ACET – more worried

ACET is a major concern

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75
Q

Acetaminophen overdose is a……..

A

Serious medical emergency

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76
Q

When is hepatotoxicity observed in adults and adolescants regarding acetaminophen?

A
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77
Q

Describe acetaminophen concern for overdose in pediatrics?

A
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78
Q

What is the recommended maximum dose of acetaminophen in Canada and the USA?

A

USA: 3 g/day

Canada: 4 g/day

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79
Q

What value of a daily dose of acetaminophen is a cause for concern?

A

The expert said that “a bit more than 4000 mg = trouble” is NOT true.

The problems start with people getting 8000 or 10000 mg in a day. He feels that 6000 mg is clearly safe.

So, he is fine if the max stays at 4000 mg b/c some buffer room above itis in place.

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80
Q

Describe the dosing of Tylenol products in Canada

A
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81
Q

Describe the risk of overdose of Ibuprofen

A

Reports of complications following ibuprofen overdose particularily in children are rare

The vast majority of individuals who overdose on ibuprofen alone have no, or only mild symptoms

Fatal overdose in adults is extremly rare

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82
Q

Describe a critical drug interaction of NSAIDs in comparison to Acetaminophen. Is acetaminophen more safe than NSAIDs?

A

Several reports of an interaction with acetaminophen

Doses at > 2.25 g per week starting point for concern

Doses > 2.5 g per week could be impactful

More frequent monitoring is suggested

Warfarin use is dropping (but it still is out there)

Mechanism appears to not be due to a plasma protein binding interaction

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83
Q

What should a pharmacist recommend if someone is on warfarin and taking acetaminophen?

A

Patients taking warfarin who are at high risk of bleeding require close INR monitoring when starting and stopping courses of acetaminophen

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Perfectly
84
Q

Describe the benefits of DOACs. Is there a drug interaction with NSAIDs?

A

Lower bleeding risk
Less monitoring
Fixed dose
Less drug interactions

But NSAID + DOAC does increase bleed risk

Far less of pharmacodynamic drug interaction

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85
Q

Describe the association between acetaminophen use and preganncy?

A

Acetaminophen during pregnancy has been associated with neurodevelopmental and behavioral disorders such as ADHD and increase risk of wheezing and incidence of asthma among offspring

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86
Q

Does acetaminophen cause asthma or worsen existing asthma? Mechanism? When does this occur if it does?

A

Acetaminophen does not worsen asthma

May cause asthma

Possible mechanism: Reduces the body’s level of natural free radical scavenger (glutathione)

There is some concern for this connection while other dispute the connection

Exposure via pregnancy or during early infancy

87
Q

Does acetaminophen make a child’s asthma worse?

A

No

Acetaminophen does not make asthma worse

Found no difference in the number of asthma exacerbations

88
Q

Does acetaminophen in pregnancy lead to ADHD?

A

Use of acetaminophen in pregnancy is safe after talking with your healthcare provider because there is no clear evidence of a direct relationship between acetaminophen and irregular fetal development

Reports are weak; can still use acet safely in pregnancy

ADHD –> NOOOOOOO

ADHD and autism lawsuits againts acetaminophen lacked admissible proof to support their claims

89
Q

Acetaminophen and Pregnancy FDA Category. Indication and safety in preganncy?

A

Pregnancy Category B

Acetaminophen still first line for fever and pain in pregnancy

Acetaminophen is used by 69.9% of women during the first and second trimesters of pregnancy

May actually prevent negative health consequences for the fetus

90
Q

Does regular acetaminophen use increase blood pressure?

A

Taking 3-4 g of acetaminophen per day for 2-4 weeks incraeses systolic blood pressure by 3-4 mmHG.

91
Q

What are the symptoms of an asthma exacerbation?

A
92
Q

What happens to an asthmatic if you are sensitive to an NSAID?

A

When they take ASA or an NSAID symptoms of an asthma exacerbation occurs between 30-120 minutes after taking the NSAID

93
Q

What type of condition is NSAID induced asthma exacerbation?

A

The condition develops in adulthood, typically between the ages of 20-50 years old.

The average onset is 34 years old

94
Q

What are some major causes of an asthma exacerbation in adults?

A

Viral
Allergen
Exercise

95
Q

Describe the rates of ASA-allergy. Do most people know if they have an ASA-allergy? Cross sensitivity with other NSAIDs?

A

Most people won’t get their first dose of ASA until they are about 60

Not due to salicylate group

96
Q

Describe which NSAID’s to use in those with asthma?

A

IF the person is ASA-sensitive, do not use

IF the person is NOT ASA-sensitive, these agents CAN be used

IF the person does not know their status ….

Many patients erroneously believe they are ASA-allergic

ASA-induced asthma may only be seen in adulthood (Good chnace we can recommend these products in children)

97
Q

Can a child with asthma be given an NSAID?

A

NSAIDs can safely be given to children with asthma

No need to avoid medications unless it is known that they are an asthma trigger for you

Condition of adulthood: 10-20% of adults with asthma have sensitivity to ASA and NSAIDS’s

98
Q

NSAID induced asthma exacerbation appears to be due to what pathological process?

A

COX-1 Inhibition

Can use celecoxib here (selective COX-2 Inhibitor)

COX-2 inhibitors provide a potnetially safer alternative for treatment of inflammatory conditions in patients with aspirin-exacerbated respiratory disease

99
Q

What is ASA 81 mg commonly used for?

A

Commonly used for secondary prevention rather than primary prevention

100
Q

What are some warnings listed on Advil and Aleve for the use of ASA 81 mg with these agents?

A

Avoid taking IBU/Naproxen if taking low dose ASA 81 mg without talking to to a physician/pharmacist

101
Q

Describe how ASA 81 mg leads to cardio-protection?

A

ASA hits COX-1 receptor as a Non-selective NSAID

  • Now means that the platlet is less sticky – can save your life perhaps
102
Q

What happens if Ibuprofen is administered with ASA 81 mg?

A

Ibuprofen on there first; sticks there as far as receptor blocking ASA form getting to the receptor

ASA cannot deactivate COX-1 receptor

103
Q

What is a risk of taking Aleve and Ibuprofen beyond the loss of cardioprotection?

A

The risk of GI issues (bleeding risk) incraeses with regular use of either agent in combination with ASA

104
Q

How can the interaction of ASA 81 mg and IBU be avoided? What complicates this strategy?

A

Single doses should be given 2 HR after the ASA or 8 hours before the ASA

Multiple daily doses will be a problem

105
Q

Is Naproxen (Aleve) also likely to interact with ASA 81 mg?

A

Less likely to interact but still some evidence of an interaction

Avoid if regular use is planned

Single doses should be given 2 hours after the ASA or 8 hours before the ASA

Multiple daily doses will be a problem

106
Q

When are we more worried about the interaction of ASA and Ibu/Naproxen?

A

Cut the loses with the 2 HR after the ASA and 8 hours before the ASA

If short term, not an issue

Long term worried as not will be getting value of ASA 81

107
Q

Does acetaminophen have the same interaction with ASA 81 mg as does IBU and Naproxen?

A

May not be an option for osteo or low back pain (limited efficacy)

Headaches –> May be useful for benefit/relief

108
Q

What are the main strategy(ies) that a pharmacist should consider if an individual is taking ASA 81 mg and has pain?

A

Increase the dose of ASA

G.I. risk will increase but still may be the best option

GI risk is evident but also evident with IBU and Naproxen

CV - Same drug as ASA 81 mg and go with a higher dose to maintain cardio-protection

Topical Diclofenac

Not for headaches, but may be useful for joint pain as example

109
Q

Overall, ASA 81 mg and taking IBU and Naproxen main concern

A

If ibu and naproxen used periodically, can probably do that – take odd tablet and not worry – regular use is the issue here

110
Q

Describe the use of analgesic usage in pregnancy

A

Pregnant women are at risk for under-treatment of pain b/c of concerns

OTC analgesics are some of the most commonly used agents in pregnancy, whether self- or MD-recommended

Few analgesic drugs have been demonstrated to be absolutely contraindicated during pregnancy

111
Q

What FDA Category is acetaminophen in pregnancy?

A

FDA Category B

Commonly used in all stages of pregnancy

112
Q

Describe the issue of NSAID usage in pregnancy.

A

Prostaglandins maintain the patency of the ductus arteriosus until birth

Before you are born, it allows blood to bypass the baby lungs

Flow to the lungs in not yet needed

After your are born the ductis arteriosus closes and blood is now shunted to the baby’s lungs

113
Q

What pregnancy category is Ibuprofen according to the FDA?

A

Category C up to 30 weeks

Category D at greater than 30 weeks

114
Q

What are the risks of Ibuprofen in pregnancy?

A

Causes premature closure of the PDA

Increased bleeding risk at term

115
Q

Describe the safety of Naproxen usage in preganancy?

A

Every pregnancy starts out with a 3-5% chance of having a birth defect

Naproxen did not show an increased chance of bith defects

Naproxen is not recommended for use after week 20 of pregnancy

Leads to premature closure of the PDA (Patent Ductus Arteriosus)

116
Q

What is another concern stated by the FDA and Health Canada regarding NSAID use in pregnancy?

A

Avoid NSAIDs in pregnancy at 20 weeks or later as they can result in low amniotic fluid

117
Q

Describe the effects of the COX enzymes?

A

Starts with arachadonic acid and is mediated by thromboxanes and cytokines

118
Q

Describe the MOA of COXIBS in comaprison to OTC NSAIDs. Examples.

A

Only block COX-2 enzymes

OTC Nsaids

Block COX 1 and 2 to varying degress –> Naproxen, Diclofenac, Ibuprofen

119
Q

What enzyme is responsible for pain killing?

A

Blocking the COX-2 receptor is considered the enzyme for pain killing

120
Q

Describe the GI safety of NSAIDs regarding adverse effects

A

Occurrence of severe damage (ulceration, bleeding) is rare at OTC dosing of Ibuprofen and Naproxen

Heartburn and dyspepsia occur with OTC ibuprofen but the rate is similar to acetaminophen or even placebo

At RX doses, the risks jump alot

121
Q

What can be done to help prevent GI issues from occuring with NSAID’s?

A

H2RA’s do not help with preventing GI issues (12 hours to onset)

Must be PPI’s –> Add on for long term usage of an NSAID

122
Q

Describe the gastrointestinal safety of Ibuprofen

A

GI a/e with the use of NSAID is comparitevely low

Serious GI adverse effects occur in 1% of patients each year in the use of high doses with long term tx

OTC Doses –> Rates similar to that of acetaminophen

Out of all NSAID’s, Ibuprofen appears to have one of the best GI tolerability profiles

123
Q

What are some comobination products of NSAIDs with gastro-protective agents?

A

Vimovo –> Naproxen and Esomperazole

Duexis –> Ibuprofen and famotidine
–> Reduces the risk of ulcers by 50% compared to ibuprofen alone

OTC Scenarios: Advil + Zantac (famotidine)

124
Q

How long should a PPI be used for if taking an NSAID? H2RA?

A

PPI for three weeks is a good move

Short Term –> H2RA may be a good move but PPI looks like a better move

125
Q

Describe the prevalence of CV disease death in Canada and relevant statistics

A

2021 –> 194/100,000 Canadians died from major CV disease

Roughly 6.1/1000 adults aged 20 years and older recived diagnosis of Ischemic heart disease

2.3/1000 adults had a first heart attach

5.2/1000 Canadians aged 40 years and older recieved a diganosis of HF

126
Q

Describe the risk of NSAIDs and a Heart Attack

A

Above average risk of heart problems and taking an NSAID:

Diclofenac, celecoxib, or ibuprofen:

Estimated that 7 to 8 extra CV events (such as heart attack) would occur each year among 1000 people taking these medications

For those taking Naproxen, no incraesed risk was observed

THIS IS CONSIDERED A SMALL ADDED RISK

More important risk factors included smoking, eating an unhealthy diet and not exercising enough

127
Q

Compare the safety of Advil and Aleve

A
128
Q

Describe the risk of NSAID and CV risk regarding a comparison of the agents

A

All NSAID’s including both traditional and COX-2 selective NSAIDs increase the risk CV adverse events

It is not possible to differentiate or rank NSAIDs by their CV risk

CV adverse events occur with both short-term and long-term use

Use NSAIDs at the lowest effective dose for the shortest time possible

129
Q

Are NSAIDs still prescribed in individuals with CV risk?

A

Although NSAID use is discourage in patients with CV disease, pain-releief medication is often required and, in the absence of analgesics that are at least as effective but safer, NSAIDs are frequently prescribed

130
Q

Describe an overall approach that can be used to manage pain in someone with CV adverse event history

A

1) Non-drug measures first (warm compress, TLC, massage)

2) Topical Diclofenac if isolated joints

3) Tylenol (Short leash here)

4) NSAID –> Need to inform patient to tell there doctor they are taking to monitor for GI and CV risk
–> IBU vs NAproxen –> Little nuance here:

Check in and see if its working:

If not –> STop

If it is –> Lower the dose

131
Q

Describe the overall concept of CV disease for pharmacists regarding NSAID usage in these patients

A

The risk of having a heart attack or stroke is extremely small over s short course of therapy (less than one month) such as would be the case in treating acute pain from a musculoskeletal injury

In people without known CVD, the increase risk is minimal

Advise an alternative treatment; however, many patients with CVD can be safely treated with a short course of NSAIDs

Chronic or daily us will be more a concern and warrant questioning

132
Q

What are some of the drug interactions associated with NSAIDs?

A

Prednisone 5 mg –> No NSAID
Anti-coags:
Warfarin: INR changes and increased GI bleed risk
DOACs: Less pharmacodynamic drug interaction but someone should be monitoring bleed risk

Will likely increase blood pressure

SSRI’s: Increase risk of GI bleed 7-fold –> Increased risk with NSAID

ASA –> CV protection loss due to platlet binding

133
Q

Is acetaminophen safe for a hangover?

A

Yes acetaminophen is safe for a hangover

134
Q

Describe the acetaminophen metabolism pathway in regards to alcohol consumption

A

Chronic alcohol and Tylenol is not a good option

Have less glutathione –> all leaning towards to NAPQI and liver damage

Not a problem for hangover to take Tylenol

Chronic aspect leading to issues

NAPQI –> glutathione –>move it over to non-toxic metabolites

Alcohol – not eating as good as they should be chronically; so less glutahione

135
Q

What does the acetaminophen box say regarding use of alcohol? Is this factual?

A

If you consume 3 or more alcoholic drinks every day, ask your MD whether you should take acetaminophen.

Acetaminophen may cause liver damage.

Not the reality

136
Q

What is the true reality regarding acetaminophen usage in individual who use alcohol?

A

Patients with cirrhosis have lower clearance of acet SO:

Use < 2 g per day including those who continue to drink (still considered safe)

If taken in appropriate doses, acetaminophen is one of the safest analgesics for patients with cirrhosis

Once exceed 2 g/day –> NAPQI accumulation

137
Q

Are we concerned about hepatotoxicity in acute alcohol ingestion?

A

Acute alcohol ingestion is not a risk factor for acetaminophe hepatotoxicity.

In fact, it may even be protective (by competing for Cyp2E1).

138
Q

Are we concerned about hepatotoxicity in chronic alcohol ingestion? Why are why not?

A

Chronic alcohol ingestion may potentiate hepatoxicity by:

1) Up-regulating CYP 2E1 (which will create more NAPQI)

2) Decreasing available stores of heaptic glutathione

3) MAlnourishment

139
Q

What is another risk of alcohol with NSAIDs beyond effects on the liver?

A

Increased risk of GI bleed

140
Q

What are some issues that make NSAID use in elderly patients more concerning?

A

Decreased renal function
More medications
More conditions
More bleed risk
More CV issues
More Pain too

141
Q

What is an algorithm to decide whether to use an NSAID in an elderly patient?

A

TLC therapies first

Topicals (drug of choice) –> then someone pushes button go to something

OTC doses

RX Doses: Coxibs to reduce GI risk

Try Tylenol – not looking good for OA or back pain

142
Q

When are we worried about the use of NSAIDs in sports?

A

Only concerned if the individual is dehydrated

Kidney problems are unlikely to be a concern if they are not dehydrated

Prostaglandins are required to maintain renal perfusion, therefore a decrease in PG and less fluid will lead to decreased renal perfusion

Fully dehydrated and NSAID –> BAD

143
Q

Are NSAID’s useful for the treatment of injuries from activity/sports? What is the trajectory of the treatment of acute injury?

A

NSAID’s are questionable in reducing swelling associated with phsycial injury but they can improve pain

New Thinking: Need the inflammation to help remodel the joint for long term functions

NSAIDs and cold compress may not be good for the long term front regarding remodelling

For an acute injury (e.g. sprain ankle), NSAIDs are better than acet due to the anti-inflamm action; however, OTC doses may not be anti-inflammatory

Trajectory is leaning from RICE to MCE (RI is on the verge of not being considered anymore)

144
Q

Describe the statistics regarding low back pain and the efficacy of treatment? Take away?

A

75% will recover with simple treatment

25% will have future further espiodes

The value of analgesics are really being re-thought in this area

145
Q

Is bed rest a good therapeutic management for low back pain?

A

No

Want to power through and maintain movement as movement can help remodel

146
Q

From a pharmacist perspective, what types of back pain are we involved in?

A

Low back pain

High back pain can be caused by many conditions (compressed vertebrae, syndromes) and this is not us

–> Physio, chiropractice and medicine territory

147
Q

What are some causes of back pain? Are we able to distinguish these? If so, which ones?

A

Sciatica – Can guide us on what not to use

Important nerve for ambulation

Pain down the back length of the lower keg

148
Q

When are NSAIDs useful for back pain?

A

Add on for acute is likely useful

Pain meds have a limited role in most cases of lower back pain

149
Q

Describe the etyiology of back pain

A

Chronic low back pain has generally been considered to be the result of an injury

Overly simplistic

Complex interaction of pain, perception, emotions, attitude, stress, phsycial activity and HCP relations

Tremendous amount of back pain is not due to injury- no trauma there

150
Q

Describe a common type of back pain regarding pain etyiology. Role of NSAIDs?

A

Nociplastic Pain

Pain without any damage or inflammation to that region of the body

Encompasses a lot of chronic pain, especially low back pain

Not neuropathic or somatic (injury) –> Perceptions in the brain

Since no inflammation, NSAID’s are useless

151
Q

What is the likelihood of someone having lower back pain?

A

Most people will have at least one episode of lower back pain in their life

152
Q

Is back pain common? Ages?

A

Back pain is increadibly common

Most people start noticing back pain between the ages of 40 and 60

Some start to feel the effects of an aging spine as young as 30

153
Q

Describe the available OTC analgesics and their associated max doses/day and their efficacy regarding analgesia and anti- inflammation?

A

ASA is only NSAID that will have anti-inflammatory action but not doing this anymore

154
Q

Describe the mechanism of action of Acetaminophen. Indication?

A

Works in the central nervous system (in the brain) via a PG effect

Indication: Anti-pyretic and relief of mild to moderate pain

155
Q

Is acetaminophen anti-inflammatory?

A

No: Acetaminophen is not anti-inflammatory

156
Q

Describe the role of acetaminophen in low back pain?

A

Acetaminophen is not effective for low back pain and provides no clinically meaningful impact on osteoarthritis

157
Q

What is the treatment strategy regarding analgesic use in low back pain/osteoarthritis?

A
158
Q

Describe the therapeutic ladder of ASA

A
159
Q

Describe the OTC dosing of Naproxen and Ibuprofen in comparison to anti-inflammatory dosing

A
160
Q

What are some concerns with NSAID? What is another risk factor for pharmacists to consider?

A

Geriatrics
Cardiovascular
GI
Asthma
Renal

DOING NOTHING IS ALSO A RISK FACTOR

161
Q

Describe the available muscle relaxent OTC analgesic combos available. Ingredients and strength? Is xtra-strength useful?

A

CNS effects –> Extra strength –> No change in methocarbamol dose

162
Q

Are OTC muscle relaxents effective for lower back pain? WHy or why not?

A

Methocarbamol – buying it for a buzz

CNS effects –> Extra strength –> No change in methocarbamol dose

Notoriously consisted not a muscle relaxant –> no antispasmodic effect

Just makes you drowsy –> not anti-spasmodic and not muscle relaxing

Adds on side effect with little value

163
Q

What is the best available Robax agent on the Canadian market?m

A

Methocarbamol + ASA is the best one –> inflammation is little in back pain

ASA would be the best of the right dosage; however, may not have an effect as more complexity than just inflammation

164
Q

What is the main purpose of Tylenol or Motrin adding methocarbamol into their formulations?

A

Motrin Muscle and Body –> IBU 200 and Methocarb 500

Tylenol Body Pain and Night –> Acetaminophen and Methocarbamol

Helps you go to sleep as a little sedating; that is all

165
Q

Are the following agents any better than the other OTC analgesics?

A

Same medication; no difference from the regular OTC analgesics

166
Q

What is lidocaine useful for? Concerns?

A

Possibility of use for neuropathic pain but concern over whether it actually reaches the tissues or not

167
Q

What is lidocaine?

A

Topical anasthetic

168
Q

Lidocaine by Deep Relief in Canada Indications:

How is it applied?

A

Inset bites are indicated but back pain is not i dedicated

Numbness for sure

Vaccine and epidural pain –> Can help with initial pain

Applied TID to QID

169
Q

What is the depth of nerves that lidocaine is able to effect and work on?

A

Works primarily on the. nerves at the surface of the skin

Maximal penetration depth of topical lidocaine is from 8-10 mm

3 mm after 60 minute application
5 mm after a 120 min application

170
Q

Can lidocaine be used for peripheral neuropathy?

A

Potentially –> PHysicians call here; not us as pharamcists

171
Q

For lower back pain, would lidocaine be an effective agent? Alternatives?

A

Need some penetration for low back pain treatment

Choose topical diclofenac here rather than lidocaine

172
Q

Describe the proposed mechanism of lidocaine

A
173
Q

Describe another formulation of lidocaine and its usage? Application, onset, time to maximum effect?

A

EMLA Patch

Can be utilized for injection needle pain

The onset is less than 25 mins

Application time for adequate analgesia is at least 1 hour

Maximum effect is reached at 2-3 hours of application and lasts for 1-2 hours after removal

174
Q

Describe the effectiveness of the EMLA lidocaine patch

A

The duration of analgesia is influences by the vascularity of the local area

More vasculatiure, more clearence, effect is shortened

When applied for 60 mins, the depth of the anaesthetic effect was found to be 3 mm and 5 mm for a 120 mins applictaionn

175
Q

Describe the depth of anasthetic effect for EMLA patch

A

1-2 mm when applied for 60 mins

2-3 mm when applied for 120 mins

6 mm when applied for 3-4 hours

176
Q

What is Zostrix? Indication and MOA (simple)? Main a/e?

A

Capsaicin 0.075% (pepper compound)

Generally for post-herpectic neuralgia

Needs consistent use to decraese substance P –> applied TID

Irritating to the skin when applied

177
Q

Describe the mechanism of action of Zostrix in depth

A

Substance P is a transmitter that is making pain occur

Zostrix is working to decraese substance P in blood vessels and from mast cells

Reduced substance P at the distal level and dulling the nerves

178
Q

What are some of the available topical external analgesics?

A

Counter-irritants
- Methyl Salicylate
- Menthol
- Triethanolamine

Topical NSAID’s
- Topical diclofenac (Voltaren)

179
Q

What is the MOA of topical external analgesics?

A

Counter Irritation
Massage/Blood flow
Posychological (odour)

180
Q

Describe the mechanism of action of counter irritants

A

Counter-irritants
They actually irritant the skin.

If I irritate the skin on top of the muscle, sends signal to brain.

Original pain signals from muscle underneath.

Thought is that brain cannot handle both signals: fool the brain

181
Q

What are the main counter irritant agents? Brand Names and how do they work?

A

Methyl Salicylate

Menthol –> Icy/Hot, Deep cold

Icy Hot:

First half-hour –> Menthol hits the cool receptors quickly (not actually lowering the temperature)
–> Physiolofical and psychological effect

After 30 minutes, becomes warm as other tissues become irriated and incraeses blood flow (not an actual temperature change)

Deep Cold works in thye same manner

182
Q

What is triethanolamine? Product name? Is xtra strength any better than regular strength?

A

RUB-A535

No odour versions –> Triethanolamine –> Smell is up to the patients

Do not worry about extra vs reg. strength

Low expectations of how effective this agent would be

Same mechanism as a counter irritant; just no odour

183
Q

What counter-irritant is used for heating? WHich is used for deep cold? Recommendation? Describe the indications of menthol?

A

Methyl salicylate is not hitting the cool receptors like menthol

Just try one of them to see if helpful

184
Q

IS the combination of multiple counter irritants useful? Example?

A

3 is not better than one or two; patient choice here

185
Q

Biofreeze product medication

A

Just another menthol product

186
Q

What is a critical counselling point if someone is to use a counter-irritant medication?

A

Do not use a heating pad at the same time with any counter-irritant products

187
Q

Describe the approach to therapy for sore muscles and a sore back? Counter irritants? Topical NSAID’s?

A

Counter irritants are more likely to be effective on larger muscles rather than back pain

Worth a try for sure

Lower expectations and delays use of NSAID

Often may choose to go with topical diclofenac before RUB A535

188
Q

Describe the available topical OTC NSAIDs that may be beneficial to use

A

Topical Diclofenac 1% (Voltaren)

189
Q

What does the manufacture of voltaren sat about use of the product?

A

Useful for:

1) Muscle/joint injuries
2) Sprains and strains
3) Back muscle pain

190
Q

Describe the available formulations of topical diclofenac? Strength and application? Which agent should we choose?

A

Voltaren Extra STrength 2.32%
- Applied BID; more convenient; more efficacy as driving more into the skin

Volatren Regular STrength 1.16%
- APplied TID

Often recommed the regular capped voltaren a shigh price to pay for the special cap

191
Q

Where does voltaren emugel fit into lower back pain therapy?

A

1) Topical NSAID
2) Oral NSAID
3) RUB A535

More proof for OA knee and hand then the back area
–> Most studies have been done on the knee

Less side effects than oral NSAIDs
–> The low systemic absorption of voltaren emugel (6% systemic absorption) is associated with a low incidence of systemic side effects

Chronic low level back pain; may be more useful than oral

Drug of choice in patients >75 years old

192
Q

Describe the dosing of the regular strength Volatren Emugel? Do we use this recommendation?

A

No dosing card

Apply the gel 3 to 4 times daily

The amount needed will vary depending upon the size of the painful or swollen are:

2-4 g (1 g equala a strip approximately 2 cm long) gel will be sufficient to cover a 400-800 cm^2 area

Never doing this kind of deatil

193
Q

When recommending Voltaren emugel, how much should we recommend?

A

Almost all patients will go with their own judgment

Suggesting a _______ amount will be fine for vast number of cases

194
Q

For chronic low back pain, how much voltaren emugel should we recommend?

A

1 FTU is fine for most cases

Covers the area of the back and front of hands

2 cm strip is often fine T-QID (not doing this)

Other joints, just a dab (example: knuckles, just pea sized dabs)

195
Q

Voltaren Rx Agent and ISsues

A

Diclofenac 25 mg

Oral Tablet

Local and PG issues occuring here

196
Q

What is the main adverse effect of voltaren emugel?

A

Local skin irritation

Unlikely to have systemic PG issues

197
Q

Is the easy to open cap or no mess applicator of volatren a good move?

A

No

Manufacturing move

25 grams less when go the easy to open cap

No mess applicator –> Lift it, squeeze against the skin, moves back, don’t get anymore
–> Still messy, pad not looking great after one month

198
Q

Is the dosing card of voltaren emugel useful for the xtra strength volatren? Issue?

A

Extra strength topical gel is measured to give an accurate dose

Ususal dosing card is supplied with the medication to measure a 2g doses and apply the gel to the affected area 2 times daily

Basically everyone is instructed to use the same amount

2 FTU’s is what everyone is getting here

Way too much

199
Q

What is the dosing of volatren extra strength?

A

BID

No mention of altering the dose according to the dosing card

200
Q

Describe the role of anti-depressants in chronic low back pain

A

ANtidepressants are the most prescribed medication for chronic low back pain

Systematic Review –> Antidepressants have a limited role –> Ineffective or had very small beneficial effects

Recommendation for Duloxetine (other SNRI’s) –> Norepi effect

Leap of hope aspect here

SSRI’s do not have a large role here

201
Q

Describe the role of anti-depressants in OA and sciatica

A

SNRI’s offered nonclinically relevant benefits with people with osteoarthritis

questioned SNRI’s and TCA’s for sciatica

TCA’s for neuropathic pain

Sciatica –> DUloxetine on MD”s radar

202
Q

Describe the role of SNRI’s and TCA’s in chronic back pain

A

Back Pain specifically –> Duloxetine (SNRI) does help, while TCAs were inconclusive

Liked nortriptylline better than amitriptylline

All based on neuropathic pain

203
Q

Descriptive symptom of sciatica

A

Sharp pain down the back of leg to the knee
–> Neuropathic pain

204
Q

What is shingles? RAte? Main intial Sx presnetation ?

A

Shingles is the re-activation of the herpes zoster virus (chicken pox)

Chicken Pox as a kid –> 20-30% chance of reactivation

Symptoms and rash tend to be unilateral

205
Q

What is a preventative strategy for shingles?

A

Get vaccinated

Small price to pay for not having neuropathic pain later on

206
Q

Is shingles a single phase condition?

A

No
Acute and chronic phase

207
Q

Acute phase treatment of SHingles

A

ANtivirals within 72 hours of the rash’s initial appearance (higher dose than cold sores)

Analgesics - can use for acute phase (first 3 weeks)

For itch –> Cool compress, calamine

208
Q

How long does the acute phase of shingles commonly last?

A

3 weeks –> Can use analgesics in this time
Should clear within 3 weeks

209
Q

Describe the chronic phase of shingles and its assosictaed treatment

A

Rash has now healed - month later

Pain occuring due to damage to nerves by herpes zoster virus

Analgesics –> Not great as neuropathic pain here

TCA’s on the radar for neuropathic pain

Gabapentin/Lyrica/Carbamazepine

Capsaicin –> Topen agent –> Tough on the skin an dno guarntee if working

1/3 of patients do not like this aget –> need to use consistently; not PRN

210
Q

Post-herpetic Neuralgia - OTC agent

A

Zostrix

Not for acute shingles (rash phase) but option if in a chronic phase

Applied TID where the pain appears to be (no rash to guide you)

Not dosed PRN - needs consistent applicatiion in order to depelete susbtance P

211
Q

Zostrix Ingredient and Adverse EFfects

A

Capsaicin

Burning, stinging, and skin redness

Intolerable in 1/3 to 1/4 of patients

212
Q

What is the most common cause of sciatica

A

The most common cause of sciatica is a bulging disk or hernaited disk

213
Q

Oral NSAIDs for Neuropathic PAin

A

NSAID’s are not usually effective in treating neuropathic pain

No difference in NSAIDs and placebo nregarding adverse effects or pain

If nerves being fired –> NSAIDs not helping

If a high suspicion of sciatica in addition to back pain - not pharamcist territory

Save money on avoiding NSAIDs and avoid adverse effects

PHAR 398: Minor Ailments (9 decks)

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