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Opioids: formulations and properties
Monday, October 31, 2011 Posted by Piscean



Opioids: formulations and properties

Some preparations of opioids have immediate-release characteristics, others are available as modified-release formulations, and some are a combination of both.
Modified-release formulations should never be crushed or chewed, as this destroys their release properties and can result in a large dose being absorbed over a short period.
See Box 1.2 for advice about converting from immediate-release to modified-release morphine preparations.
A comparison of approximate equivalent doses of various opioids is shown in Table 1.4.
Table 1.3 below lists some opioid preparations and their properties. Awareness of the many available strengths and formulations is essential to avoid medication errors.
Properties of common opioid preparations available in Australia (Table 1.3) [NB1]
Opioid Active metabolite Dose adjustment in renal impairment Duration of action (hours) [NB2] Preparation
alfentanil
no
no
dose-related: 10 to 30 min for 1.5 to 3 mg/70 kg
injection


buprenorphine
no
no
6 to 8
sublingual tablets (Temgesic)

injection (Temgesic)

7 days
transdermal patch (Norspan Transdermal Patch)

codeine
yes
yes
3 to 4
linctus

 
tablet

dextropropoxyphene
yes
yes
6 to 12 (metabolite 30 to 36)
capsule

fentanyl
no
no
0.5 to 2
lozenge

injection

72
transdermal patch (Durogesic)

hydromorphone
probable minimal effect except in patients with renal impairment
yes
2 to 4
oral liquid

tablet

injection

methadone
no
note that duration of effect increases with chronic dosing
6 to 8 initially, then increases with chronic dosing up to greater than 24 hours
syrup

tablet

injection

morphine
yes
yes
2 to 3
injection (sulfate)

injection (tartrate)

immediate-release oral mixture

immediate-release tablet

24
modified-release capsule (MS Mono)

12
modified-release suspension (MS Contin)

modified-release tablet (MS Contin)

12 to 24
modified-release capsule (Kapanol)

oxycodone
yes
yes
3 to 4
oral liquid (OxyNorm Liquid)

immediate-release capsule (OxyNorm)

immediate-release tablet (Endone)

12
modified-release tablet with immediate-release component (OxyContin)

uncertain
suppository (Proladone)

4
injection (Oxynorm Injection)

pethidine
yes
yes
2 to 3
injection

remifentanil
no
no
dose related (biological half-life of 3 to 10 minutes)
injection

sufentanil
no
yes
dose-related (40 to 87 min)
injection

tramadol
yes
yes
3 to 6
immediate-release capsule

immediate-release oral drops

injection

12
modified-release tablet

NB1: only opioids discussed in these guidelines and preparations containing an opioid as the single active component are listed
NB2: approximate only

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