Analgesics in MOS 1 Flashcards
(111 cards)
1
Q
What are the most effective NSAIDs for pain after oral surgery (currently recommended)?
A
- ibuprofen
- diclofenac
2
Q
What comprehensive advice can be given to prescribers of NSAIDs?
A
prescribe the lowest effective dose for the shortest possible duration
3
Q
How many NSAIDs are on the global market ?
A
over 50
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
5
Q
Ibuprofen is an effective analgesic in the control of post-operative dental pain. True or false
A
True
6
Q
Aspirin is mainly used for…
A
cardiovascular treatment
7
Q
What is the half-life of aspirin ?
A
15 minutes
8
Q
What is the half life of naproxen?
A
12-15 hours
9
Q
What is the benefit of using ibuprofen over fenoprofen?
A
it has less gastrointestinal side effects
10
Q
What are the uses of dexketoprofen?
A
mild to moderate pain
11
Q
Ketoprofen and dexketoprofen have similar anti-inflammatory properties to ibuprofen. True or False
A
true
12
Q
Diclofenac and acelofenac have a similar efficacy to …
A
naproxen
13
Q
Diclofenac potassium is _________ release
A
immediate
14
Q
Diclofenac sodium is ____ release
A
slow
15
Q
Diclofenac potassium was developed to manage what type of pain?
A
migraine pain
16
Q
What type of diclofenac is more frequently prescribed?
A
diclofenac sodium
17
Q
What preparation of diclofenac is more useful for management of post-operative pain?
A
diclofenac potassium
18
Q
What is the main use of Etodolac?
A
licensed for symptomatic relief of arthritis
19
Q
What is the half life of etodolac ?
A
7 hours
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
21
Q
What is the half life of indometacin ?
A
4.5 - 6 hours
22
Q
Mefenamic acid has ____ anti-inflammatory properties.
A
minor
23
Q
What is the half life of mefenamic acid ?
A
3-4 hours
24
Q
Mefenamic acid is often associated with what side effects?
A
- diarrhoea
- haemolytic anaemia
25
What is meloxicam currently licensed for use on?
* short term pain relief in osteoarthritis
* long term treatment of rheumatoid arthritis and ankylosing spondylitis
26
What is the half life of meloxicam ?
13-20 hours
27
Phenylbutazone is used for ...
ankylosing spondylitis
28
Why is the use of phenylbutazone restricted to specialist treatment of severe cases where other treatments have failed?
this is because it is associated with serious side effects
29
What permits the once daily administration of piroxicam?
long duration of action
30
What is the half life of piroxicam ?
30-86 hours
31
What are the adverse effects of piroxicam ?
* more GI disturbances than other NSAIDs
* severe skin reactions
32
Tenoxicam also has a long duration of action that permits 1x daily administration. True or false
true
33
Ketorolac and parecoxib are licensed for __________ management of post operative pain
short term
34
Parecoxib is _____ selective
COX-2
35
Celecoxib and etoricoxib are ____ selecitive
COX-2
36
Celecoxib and etoricoxib are licensed for treatment of ...
* arthritis
* ankylosing spondylitis
37
What coxib is licensed for treatment of acute gout?
etoricoxib
38
Outline the available formations of ibuprofen
* 200mg, 400mg, 600mg, 800mg slow release tablets
* 100mg/5ml oral suspension (available sugar free preparations)
* 600mg effervescent sachets
* topical preparations
39
What is the recommended dose of ibuprofen for adults and children over 12 years old?
300-400mg 3-4x daily
increased if necessary to a maximum 2.4g daily, administered by mouth
40
Diclofenac potassium is on the DPF. True or false
false
41
Diclofenac potassium has fewer routes of administration and is more expensive. True or false
True
42
What formulation of diclofenac potassium is available OTC?
12.5mg tablet for 3 day usage
43
What are the available formulations of diclofenac sodium?
* 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
44
What is the recommended dose of diclofenac sodium for adults ?
75-150mg per 24 hours in 2 or 3 divided doses
administered via mouth or rectum
45
What is the role of COX enzyme?
processing arachidonic acid into prostaglandins and thromboxane
46
What are the isoforms of the COX enzyme ?
* COX-1
* COX-2
47
What are the constitutive roles COX-1 enzymes ?
* GI protection
* platelet aggregation
* blood flow regulation
* CNS function
48
What are the constitutive roles of COX-2 enzymes?
* renal function
* CNS function
* tissue repair and healing (including GI tract)
* reproduction
* uterine contraction
* blood vessel dilation
* inhibition of platelet aggregation
49
State an adverse effect that results from NSAID use
loss of gastric protection
consequent GI ulceration and bleeding
50
How do NSAIDs produce their analgesia?
analgesia is produced as a result of inhibition of prostaglandin production
51
Where does NSAID absorption take place?
* upper parts of the small intestine
* small amount occurs in the stomach
52
Suggest possible reasons that lead to slower onset of analgesia following administration of oral NSAIDs
* 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
When are suppository formulations of NSAIDs made use of ?
| suppository (rectum)
in children when swallowing is impractical
54
What is the half life of ibuprofen?
2 hours
55
What time is the peak plasma concentration of ibuprofen reached when taken on an empty stomach?
45 minutes
56
What time is the peak plasma concentration of ibuprofen reached when taken with food?
1-2 hours
57
How is ibuprofen excreted ?
via the kidneys
58
What is the half life of diclofenac?
1-2 hours
59
When is the peak plasma concentration of diclofenac reached?
20-60 minutes following drug administration
60
Diclofenac undergoes first pass metabolism. True or false
True
transported via the portal vein to liver where it is metabolised before it enters systemic circulation
61
What does a ceiling effect refer to?
this is where additional doses of the drug offer no further analgesic benefits
62
Give examples of analgesic drugs that have a ceiling effect
* NSAIDs
* paracetamol
63
What is the benefit of using COX inhibiting nitric oxide donators (CINODs)?
* provide analgesis through COX inhibition
* **they have gastrointestinal safety through the protective effects of controlled NO donation**
64
Celecoxib has a ____ COX-2 selectivity
moderate
65
Diclofenac has a slight selectivity towards ____ inhibition
COX-2
66
Parecoxib is an injectable prodrug of _________.
valdecoxib
converted in the liver
67
What risks are associated with parecoxib ?
* slightly elevated risk of renal dysfunction
* hypertension
68
The full analgesic effect of NSAIDs is often reached within ...
a week
69
When can you expect to achieve the anti-inflammatory effect of NSAIDs?
up to 3 weeks
70
If the analgesic/anti-inflammatory responses are not obtained within their expected time frames, what should you do?
try another NSAID
71
What does the "number needed to treat" (NNT) measure?
the efficacy of an analgesic
72
What does the NNT represent?
* represents the number of patients given an analgesic who achieve at least 50% pain relief compared to placebo
73
What does a smaller NNT number represent ?
a more effective analgesic
74
What is the benefit of using COX-2 selective agents/
* limiting GI toxicity and bleeding
75
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?
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
What is the half-life of etoricoxib?
22 hours
77
Etoricoxib is licensed for use in post-operative pain in the UK. True or false
false
78
Impaired coagulation and perioperative bleeding from NSAIDs are not considered to be a problem for patients undergoing oral surgery. True or false
true
79
Anti-inflammatory drugs (coxibs specifically ?) may be associated with increased cardiovascular disease risk. True or false
True
80
What COX-2 inhibitor was removed from the market in 2004 owing to its role in risk of cardiovascular events?
Rofecoxib
81
The issue of increased cardiovascular disease risk with the use of NSAIDs is particularly relevant for what kinds of patients?
patients who need long term drug use such as those with arthritis pain
82
State the high risk factors where NSAID prescription should be avoided
* history of MI
* unstable angina
* congestive heart failure
* suspected or known atherosclerotic disease
83
All NSAIDs are thought to weakly increase the risk of thrombotic events when used long term , with the possible exception of ...
naproxen
84
Outline from the highest to lowest risk, the NSAIDs that are associated with significant GI toxicity
Ketoprofen>ketorolac>diclofenac>naproxen>ibuprofen
85
In order to minimise the risk of GI toxicity observed in non-selective NSAIDs, what drug class can be prescribed/taken concomitantly?
PPI (e.g. omeprazole)
86
List risk factors for GI complications in patients taking NSAIDs
* 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
What are the potential adverse effects NSAIDs can cause in kidneys?
((loss of protective prostaglandins))
* renal insufficiency
* anagelsic associated nephropathy
88
In adults with normal renal function preoperatively, what is the effect of NSAIDs used for post operative pain management on renal function ?
small, transient reduction in renal function
this renal reduction is clinically unimportant
89
Aspirin must be avoided in children under 12 due to the risk of developing...
Reyes syndrome
90
What is the recommended dose of ibuprofen for children between 3-6 months (body weight over 5kg) ?
50mg 3x daily
maximum 30mg/kg daily divided in 3-4 doses
91
What is the recommended dose of ibuprofen for children between 6 months -1year?
50mg 3x daily
maximum 30mg/kg daily divided in 3-4 doses
92
What is the recommended dose of ibuprofen for children between 1- 4 years ?
100mg 3x daily
maximum 30mg/kg daily divided in 3-4 doses
93
What is the recommended dose of ibuprofen for children between 4-7 years old?
150mg 3x daily
maximum 30mg/kg daily in 3-4 doses
94
What is the recommended dose of ibuprofen for children between 7-10 years ?
200mg 3x daily
up to 30mg/kg daily, maximum 2.4g in 3-4 divided doses
95
What is the recommended dose of ibuprofen for children between 10 -12 years ?
300mg 3x daily
up to 30mg/k, maximum 2.4g, in 3-4 divided doses
96
What is the recommended dose of diclofenac for children (6months -18 months) by mouth?
0.3-1mg/kg (maximum 50mg) 3x daily
97
What is the recommended dose of diclofenac for children 8-12 kg in body weight by rectum?
12.5mg 2x daily for maximum of 4 days
98
What is the recommended dose of diclofenac for children >12 kg in body weight by rectum?
1mg/kg (maximum 50mg) 3x daily for a maximum of 4 days
99
The use of NSAIDs in the 3rd trimester of pregnancy can cause...
increased risk of closure of fetal ductus arteriosus in untero and persistent pulmomary hypertension in the newborn
delayed labour onset + increased labour duration
100
Regular use of NSAIDs in the early stages of pregnancy is associated with ...
increased risk of miscarriage
101
NSAIDs are readily transferred into breast milk. True or false
False
they are not readily transferred
therefore considered safe for short term use
102
How can you achieve aspirin desensitisation in aspirin sensitive asthmatics?
* incremental doses of aspirin
* topical administration of soluble lysine- aspirin
103
What is the major known interaction between NSAIDs and corticosteroids ?
increased risk of peptic ulceration
104
What is the major known interaction between NSAIDs and aminoglycosides, lithium, methotrexate and digoxin ?
reduced renal excretion
105
What is the major known interaction between NSAIDs and aminoglycosides, ciclosporin and diuretics?
increased nephrotoxicity
106
What is the major known interaction between NSAIDs and ACE inhibitors and beta blockers?
decreased anti-hypertensive efficacy
107
What is the major known interaction between NSAIDs and warfarin ?
increased severity of GI bleeding
108
What is the major known interaction between NSAIDs and diuretics ?
impaired diuresis
109
What is the major known interaction between NSAIDs and pheytoin?
reduced metabolism
110
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?
* paracetamol + weak opiate e.g. codeine or tramadol
111
When do severe side effects (GI bleed/thrombotic event) of NSAIDs tend to occur?
tend to occur with long term use of the drugs for chronic inflammatory conditions e.g. arthritis
