Codeine

  • Available as codeine phosphate tablets 15mg, 30mg and 60mg and as liquid preparations 15mg/5ml and 25mg/5ml.
  • Also available in combination with paracetamol 8mg/500mg, 15mg/500mg, 30mg/500mg.
  • Codeine must be metabolised to morphine to achieve most of its analgesic effect.
    • 5 to 10% of people lack the liver enzyme which enables this to happen (CYP2D6) and therefore pain relief will not be achieved but adverse side effects will still occur.
    • In contrast, ultra-rapid metabolisers produce more morphine and are more prone to toxicity.
  • Several active metabolites are renally excreted.
  • Avoid in stage 4 and 5 Chronic Kidney Disease.
  • Maximum oral dose: 240mg/24 hours.

 

Dihydrocodeine

  • Similar to codeine in structure and analgesic effect.
  • Available as 30mg tablets
  • Dihydrocodeine is metabolised by the liver enzyme CYP2D6 to an active metabolite.
  • No evidence to suggest that analgesic effect is affected by an individual’s ability to metabolise dihydrocodeine.
  • Active metabolites are renally excreted.
  • Avoid in stage 4 and 5 Chronic Kidney Disease.
  • Maximum oral dose: 240mg/24 hours.

 

Tramadol

  • Oral and injectable dose forms available.
  • Chemically unrelated to morphine. Opioid and non-opioid properties.
  • Renally excreted.
  • Use with caution in stage 4 and 5 Chronic Kidney Disease and severe liver failure. Consider increasing the dosage interval of the immediate release preparation to 12 hourly and to avoid the modified release preparation.
  • Tramadol requires the liver enzyme CYP2D6 to help with its metabolism and can therefore be poorly tolerated by some individuals.
  • Contra-indicated in individuals taking Monoamine Oxidase Inhibitors (MAOIs) or in those with epilepsy.
  • Avoid or use with caution in individuals taking Selective Serotonin Reuptake Inhibitors (SSRIs) or Tricyclic Antidepressants (TCAs) due to risk of serotonin syndrome and of lowered seizure threshold.
  • Maximum oral dose: 400mg/24 hours

 

Buprenorphine patches

  • Available as a 7-day patch (for example Butec®). At low doses (5micrograms to 20micrograms/hr) is used to treat moderate pain.
  • Buprenorphine patches are contra-indicated in patients with acute (short-term) pain and in those who need rapid dose titration for severe uncontrolled pain.
  • Undergoes hepatic metabolism to norbuprenorphine which has little clinical activity and does not cross the blood-brain barrier.
  • Unchanged buprenorphine is excreted through the biliary system.
  • Buprenorphine does not accumulate in renal impairment and therefore may be a good Step 2 Opioid in stage 4 and 5 Chronic Kidney Disease.

Refer to buprenorphine information sheet.

Note: A 3-day patch (35microgram, 52.5microgram and 70microgram/hr) and a 4-day patch (35microgram, 52.5microgram and 70microgram/hr) are available. At higher doses (greater than 20microgram/hr), buprenorphine is used to treat moderate to severe pain.