Pharmacokinetic properties and dosing schedules of NSAIDs

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Pharmacokinetic properties and dosing schedules
The pharmacokinetic properties and adult dosing schedules of NSAIDs are summarised in Table 1.2 below. See also Table 1.19 for recommended paediatric doses for oral NSAIDs.
Pharmacokinetic properties and adult dosing schedules of NSAIDs (Table 1.2)

Drug Formulations / routes of administration Time to peak concentration (hours) Elimination half-life (hours) Dose range (mg) Dosing interval (hours) Maximum daily dose (mg)
aspirin
oral
1 to 2
0.25 [NB1]
300 to 900
4 to 6
3600
celecoxib
oral
2 to 5
4 to 15
100 to 200
12 to 24
400
diclofenac
oral [NB2]
2
1 to 2
25 to 50
8 to 12
200
suppository [NB3]
0.6
more than 1 to 2 [NB3]
50 to 100
12 to 24


ibuprofen
oral (including suspension) [NB2]
0.5 to 1.5
2 to 2.5
200 to 400
6 to 8
2400
indomethacin
oral
2
4.5
25 to 100
6 to 12
200
suppository
less than 2
  
100
12 to 24


ketoprofen
oral [NB2][NB4]
0.5 to 2
1.5
50 to 100
6 to 12
200
suppository
1
1.5
100
24


ketorolac
oral
0.5
4 to 6 [NB5]
10
4 to 6 [NB5]
30 to 40 [NB5]
injection
1
4 to 6 [NB5]
10 to 30
4 to 6 [NB5]
60 to 90 [NB5]
mefenamic acid
oral
2 to 4
3 to 4
500
8
1500
meloxicam
oral
5 to 6
20
7.5 to 15
24
15
naproxen
oral (including suspension) [NB4]
2 to 4
15
250 to 500
6 to 12
1250
parecoxibNB6] [
injection
0.5 to 1
3.5 to 4 (active metabolite 8)
40 [NB7]
single dose only
40 [NB7]
piroxicam
oral [NB2]
2 to 4
53
10 to 20
24
20
sulindac (sulfide)
oral
2 to 4
7 (active metabolite 16)
100 to 400
12 to 24
400
tiaprofenic acid
oral
1.5
3
150 to 300
8 to 12
600
NB1: metabolised to salicylate; as the daily dose of aspirin increases to 2 g and above, the dosing interval can be increased because the half-life of salicylates increases with dose
NB2: also available as topical gel formulation
NB3: maximum serum concentration after suppository is less than with oral, and total exposure to the drug is comparable despite a longer half-life
NB4: also available in modified-release formulation
NB5: mean half-life of ketorolac is longer in patients aged over 65 years (7 hours, with a dosing interval of 6 to 8 hours) and in renally impaired patients (6 to 19 hours). The lower maximum daily dose applies in patients aged over 65 years and in those with mild renal impairment. Use of ketorolac is contraindicated in patients with moderate to severe renal impairment
NB6: parecoxib is the prodrug; the active metabolite is valdecoxib
NB7: 20 mg in elderly female patients weighing less than 50 kg


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