Analgesics in MOS 1 Flashcards

1
Q

What are the most effective NSAIDs for pain after oral surgery (currently recommended)?

A
  • ibuprofen
  • diclofenac
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2
Q

What comprehensive advice can be given to prescribers of NSAIDs?

A

prescribe the lowest effective dose for the shortest possible duration

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3
Q

How many NSAIDs are on the global market ?

A

over 50

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4
Q

Suggest a reason why diclofenac presriptions are more common than ibuprofen

A

this is due to only small doses of diclofenac being available OTC

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5
Q

Ibuprofen is an effective analgesic in the control of post-operative dental pain. True or false

A

True

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6
Q

Aspirin is mainly used for…

A

cardiovascular treatment

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7
Q

What is the half-life of aspirin ?

A

15 minutes

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8
Q

What is the half life of naproxen?

A

12-15 hours

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9
Q

What is the benefit of using ibuprofen over fenoprofen?

A

it has less gastrointestinal side effects

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10
Q

What are the uses of dexketoprofen?

A

mild to moderate pain

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11
Q

Ketoprofen and dexketoprofen have similar anti-inflammatory properties to ibuprofen. True or False

A

true

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12
Q

Diclofenac and acelofenac have a similar efficacy to …

A

naproxen

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13
Q

Diclofenac potassium is _________ release

A

immediate

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14
Q

Diclofenac sodium is ____ release

A

slow

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15
Q

Diclofenac potassium was developed to manage what type of pain?

A

migraine pain

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16
Q

What type of diclofenac is more frequently prescribed?

A

diclofenac sodium

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17
Q

What preparation of diclofenac is more useful for management of post-operative pain?

A

diclofenac potassium

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18
Q

What is the main use of Etodolac?

A

licensed for symptomatic relief of arthritis

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19
Q

What is the half life of etodolac ?

A

7 hours

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20
Q

Indometacin has equal or superior efficacy to naproxen, however, it has a higher incidence of side effects. List some of these side effects

A
  • headache
  • dizziness
  • GI disturbances
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21
Q

What is the half life of indometacin ?

A

4.5 - 6 hours

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22
Q

Mefenamic acid has ____ anti-inflammatory properties.

A

minor

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23
Q

What is the half life of mefenamic acid ?

A

3-4 hours

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24
Q

Mefenamic acid is often associated with what side effects?

A
  • diarrhoea
  • haemolytic anaemia
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25
Q

What is meloxicam currently licensed for use on?

A
  • short term pain relief in osteoarthritis
  • long term treatment of rheumatoid arthritis and ankylosing spondylitis
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26
Q

What is the half life of meloxicam ?

A

13-20 hours

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27
Q

Phenylbutazone is used for …

A

ankylosing spondylitis

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28
Q

Why is the use of phenylbutazone restricted to specialist treatment of severe cases where other treatments have failed?

A

this is because it is associated with serious side effects

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29
Q

What permits the once daily administration of piroxicam?

A

long duration of action

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30
Q

What is the half life of piroxicam ?

A

30-86 hours

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31
Q

What are the adverse effects of piroxicam ?

A
  • more GI disturbances than other NSAIDs
  • severe skin reactions
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32
Q

Tenoxicam also has a long duration of action that permits 1x daily administration. True or false

A

true

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33
Q

Ketorolac and parecoxib are licensed for __________ management of post operative pain

A

short term

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34
Q

Parecoxib is _____ selective

A

COX-2

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35
Q

Celecoxib and etoricoxib are ____ selecitive

A

COX-2

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36
Q

Celecoxib and etoricoxib are licensed for treatment of …

A
  • arthritis
  • ankylosing spondylitis
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37
Q

What coxib is licensed for treatment of acute gout?

A

etoricoxib

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38
Q

Outline the available formations of ibuprofen

A
  • 200mg, 400mg, 600mg, 800mg slow release tablets
  • 100mg/5ml oral suspension (available sugar free preparations)
  • 600mg effervescent sachets
  • topical preparations
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39
Q

What is the recommended dose of ibuprofen for adults and children over 12 years old?

A

300-400mg 3-4x daily
increased if necessary to a maximum 2.4g daily, administered by mouth

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40
Q

Diclofenac potassium is on the DPF. True or false

A

false

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41
Q

Diclofenac potassium has fewer routes of administration and is more expensive. True or false

A

True

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42
Q

What formulation of diclofenac potassium is available OTC?

A

12.5mg tablet for 3 day usage

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43
Q

What are the available formulations of diclofenac sodium?

A
  • 12.5mg, 25mg and 50 mg tablets
  • 75mg and 100mg slow release formulations
  • dispersible tablets (50mg equivalent)
  • 12.5mg, 25mg, 50mg and 100mg suppositories
  • 75mg IM injection
  • 75mg IV infusion
  • Topical preparations
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44
Q

What is the recommended dose of diclofenac sodium for adults ?

A

75-150mg per 24 hours in 2 or 3 divided doses

administered via mouth or rectum

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45
Q

What is the role of COX enzyme?

A

processing arachidonic acid into prostaglandins and thromboxane

46
Q

What are the isoforms of the COX enzyme ?

A
  • COX-1
  • COX-2
47
Q

What are the constitutive roles COX-1 enzymes ?

A
  • GI protection
  • platelet aggregation
  • blood flow regulation
  • CNS function
48
Q

What are the constitutive roles of COX-2 enzymes?

A
  • renal function
  • CNS function
  • tissue repair and healing (including GI tract)
  • reproduction
  • uterine contraction
  • blood vessel dilation
  • inhibition of platelet aggregation
49
Q

State an adverse effect that results from NSAID use

A

loss of gastric protection
consequent GI ulceration and bleeding

50
Q

How do NSAIDs produce their analgesia?

A

analgesia is produced as a result of inhibition of prostaglandin production

51
Q

Where does NSAID absorption take place?

A
  • upper parts of the small intestine
  • small amount occurs in the stomach
52
Q

Suggest possible reasons that lead to slower onset of analgesia following administration of oral NSAIDs

A
  • food intake
  • gastrostasis caused by acute pain

these both delay delivery of the drug to the small intestine

taking them with food can delay onset of analgesia however it is recommended to take them with food as they can irritate gastrointestinal lining

53
Q

When are suppository formulations of NSAIDs made use of ?

suppository (rectum)

A

in children when swallowing is impractical

54
Q

What is the half life of ibuprofen?

A

2 hours

55
Q

What time is the peak plasma concentration of ibuprofen reached when taken on an empty stomach?

A

45 minutes

56
Q

What time is the peak plasma concentration of ibuprofen reached when taken with food?

A

1-2 hours

57
Q

How is ibuprofen excreted ?

A

via the kidneys

58
Q

What is the half life of diclofenac?

A

1-2 hours

59
Q

When is the peak plasma concentration of diclofenac reached?

A

20-60 minutes following drug administration

60
Q

Diclofenac undergoes first pass metabolism. True or false

A

True

transported via the portal vein to liver where it is metabolised before it enters systemic circulation

61
Q

What does a ceiling effect refer to?

A

this is where additional doses of the drug offer no further analgesic benefits

62
Q

Give examples of analgesic drugs that have a ceiling effect

A
  • NSAIDs
  • paracetamol
63
Q

What is the benefit of using COX inhibiting nitric oxide donators (CINODs)?

A
  • provide analgesis through COX inhibition
  • they have gastrointestinal safety through the protective effects of controlled NO donation
64
Q

Celecoxib has a ____ COX-2 selectivity

A

moderate

65
Q

Diclofenac has a slight selectivity towards ____ inhibition

A

COX-2

66
Q

Parecoxib is an injectable prodrug of _________.

A

valdecoxib

converted in the liver

67
Q

What risks are associated with parecoxib ?

A
  • slightly elevated risk of renal dysfunction
  • hypertension
68
Q

The full analgesic effect of NSAIDs is often reached within …

A

a week

69
Q

When can you expect to achieve the anti-inflammatory effect of NSAIDs?

A

up to 3 weeks

70
Q

If the analgesic/anti-inflammatory responses are not obtained within their expected time frames, what should you do?

A

try another NSAID

71
Q

What does the “number needed to treat” (NNT) measure?

A

the efficacy of an analgesic

72
Q

What does the NNT represent?

A
  • represents the number of patients given an analgesic who achieve at least 50% pain relief compared to placebo
73
Q

What does a smaller NNT number represent ?

A

a more effective analgesic

74
Q

What is the benefit of using COX-2 selective agents/

A
  • limiting GI toxicity and bleeding
75
Q

Based on cochrane data, which COX-2 selective NSAID has been shown to have the lowest NNT? What must you take into consideration with regards to this NNT?

A

Etoricoxib

(1.6 NNT)

This NNT is based on data from only 4 trials compared to 49 for ibuprofen 400mg with 10x the number of participants

76
Q

What is the half-life of etoricoxib?

A

22 hours

77
Q

Etoricoxib is licensed for use in post-operative pain in the UK. True or false

A

false

78
Q

Impaired coagulation and perioperative bleeding from NSAIDs are not considered to be a problem for patients undergoing oral surgery. True or false

A

true

79
Q

Anti-inflammatory drugs (coxibs specifically ?) may be associated with increased cardiovascular disease risk. True or false

A

True

80
Q

What COX-2 inhibitor was removed from the market in 2004 owing to its role in risk of cardiovascular events?

A

Rofecoxib

81
Q

The issue of increased cardiovascular disease risk with the use of NSAIDs is particularly relevant for what kinds of patients?

A

patients who need long term drug use such as those with arthritis pain

82
Q

State the high risk factors where NSAID prescription should be avoided

A
  • history of MI
  • unstable angina
  • congestive heart failure
  • suspected or known atherosclerotic disease
83
Q

All NSAIDs are thought to weakly increase the risk of thrombotic events when used long term , with the possible exception of …

A

naproxen

84
Q

Outline from the highest to lowest risk, the NSAIDs that are associated with significant GI toxicity

A

Ketoprofen>ketorolac>diclofenac>naproxen>ibuprofen

85
Q

In order to minimise the risk of GI toxicity observed in non-selective NSAIDs, what drug class can be prescribed/taken concomitantly?

A

PPI (e.g. omeprazole)

86
Q

List risk factors for GI complications in patients taking NSAIDs

A
  • age >65 years
  • previous ulcer history
  • helicobacter pylori infection
  • severe comorbidities

Treatment related risk factors
* NSAID dose
* combination of >1 NSAID
* concomitant use of aspirin
* concomitant use of corticosteroids
* concomitant use of anticoagulants and antiplatelet agents

87
Q

What are the potential adverse effects NSAIDs can cause in kidneys?

A

((loss of protective prostaglandins))
* renal insufficiency
* anagelsic associated nephropathy

88
Q

In adults with normal renal function preoperatively, what is the effect of NSAIDs used for post operative pain management on renal function ?

A

small, transient reduction in renal function

this renal reduction is clinically unimportant

89
Q

Aspirin must be avoided in children under 12 due to the risk of developing…

A

Reyes syndrome

90
Q

What is the recommended dose of ibuprofen for children between 3-6 months (body weight over 5kg) ?

A

50mg 3x daily
maximum 30mg/kg daily divided in 3-4 doses

91
Q

What is the recommended dose of ibuprofen for children between 6 months -1year?

A

50mg 3x daily
maximum 30mg/kg daily divided in 3-4 doses

92
Q

What is the recommended dose of ibuprofen for children between 1- 4 years ?

A

100mg 3x daily
maximum 30mg/kg daily divided in 3-4 doses

93
Q

What is the recommended dose of ibuprofen for children between 4-7 years old?

A

150mg 3x daily
maximum 30mg/kg daily in 3-4 doses

94
Q

What is the recommended dose of ibuprofen for children between 7-10 years ?

A

200mg 3x daily
up to 30mg/kg daily, maximum 2.4g in 3-4 divided doses

95
Q

What is the recommended dose of ibuprofen for children between 10 -12 years ?

A

300mg 3x daily
up to 30mg/k, maximum 2.4g, in 3-4 divided doses

96
Q

What is the recommended dose of diclofenac for children (6months -18 months) by mouth?

A

0.3-1mg/kg (maximum 50mg) 3x daily

97
Q

What is the recommended dose of diclofenac for children 8-12 kg in body weight by rectum?

A

12.5mg 2x daily for maximum of 4 days

98
Q

What is the recommended dose of diclofenac for children >12 kg in body weight by rectum?

A

1mg/kg (maximum 50mg) 3x daily for a maximum of 4 days

99
Q

The use of NSAIDs in the 3rd trimester of pregnancy can cause…

A

increased risk of closure of fetal ductus arteriosus in untero and persistent pulmomary hypertension in the newborn

delayed labour onset + increased labour duration

100
Q

Regular use of NSAIDs in the early stages of pregnancy is associated with …

A

increased risk of miscarriage

101
Q

NSAIDs are readily transferred into breast milk. True or false

A

False
they are not readily transferred
therefore considered safe for short term use

102
Q

How can you achieve aspirin desensitisation in aspirin sensitive asthmatics?

A
  • incremental doses of aspirin
  • topical administration of soluble lysine- aspirin
103
Q

What is the major known interaction between NSAIDs and corticosteroids ?

A

increased risk of peptic ulceration

104
Q

What is the major known interaction between NSAIDs and aminoglycosides, lithium, methotrexate and digoxin ?

A

reduced renal excretion

105
Q

What is the major known interaction between NSAIDs and aminoglycosides, ciclosporin and diuretics?

A

increased nephrotoxicity

106
Q

What is the major known interaction between NSAIDs and ACE inhibitors and beta blockers?

A

decreased anti-hypertensive efficacy

107
Q

What is the major known interaction between NSAIDs and warfarin ?

A

increased severity of GI bleeding

108
Q

What is the major known interaction between NSAIDs and diuretics ?

A

impaired diuresis

109
Q

What is the major known interaction between NSAIDs and pheytoin?

A

reduced metabolism

110
Q

The routine use of COX-2 selective NSAIDs for post operative surgery is not advised; where there is risk with prescribing NSAIDs (e.g. GI bleed/drug interactions) what is recommended to prescribe?

A
  • paracetamol + weak opiate e.g. codeine or tramadol
111
Q

When do severe side effects (GI bleed/thrombotic event) of NSAIDs tend to occur?

A

tend to occur with long term use of the drugs for chronic inflammatory conditions e.g. arthritis