Learn More About: Opioids To Treat Pain Associated with Sickle Cell Pain

Opioids for Treating Pain Associated with Sickle Cell Disease

Jean M. Bidlack, Ph.D.

Common Opioids for Sickle Cell Pain

  • Opioids most commonly used to treat sickle cell pain are:
    • Morphine
    • Oxycodone
    • Hydromorphone (Dilaudid)
  • Taking prescribed opioid medication for as little as 5 days is a risk factor for dependence or addiction

https://www.mayoclinic.org/diseases-conditions/prescription-drug-abuse/in-depth/how-opioid-addiction-occurs/art-20360372

Morphine

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chemical composition of morphine
Chemical composition of morphine
  • Used as an analgesic
  • Is a potent agonist at the mu opioid receptor
  • Multiple routes of administration
  • Metabolized by hepatic cytochrome P450 enzymes and glucuronidation into a number of active metabolites
  • Excreted by renal elimination
  • Chronic use may cause renal disease in sickle cell patients
  • May cause respiratory depression and death
  • May lead to tolerance, dependence, and addiction
  • May cause constipation and urinary retention
  • Discontinuation may lead to withdrawal symptoms
  • DEA Schedule II drug

Gupta M et al. (2015) Morphine for the treatment of pain in sickle cell disease. Sci World J doi:  10.1155/2015/540154 PMC4306369

Oxycodone

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Chemical composition of oxycodone
Chemical composition of oxycodone
  • Used as an analgesic
  • Is an agonist at the mu opioid receptor
  • Good oral bioavailability
  • Metabolized by hepatic cytochrome P450 enzymes into a number of active metabolites
  • Some of its metabolites, such as oxymorphone, are more potent than oxycodone
  • Excreted by renal elimination
  • May cause respiratory depression and death
  • May lead to tolerance, dependence, and addiction
  • May cause constipation and urinary retention
  • Discontinuation may lead to withdrawal symptoms
  • DEA Schedule II drug

Hydromorphone

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Chemical composition of hydromorphone
Chemical composition of 
  • Synthesized from morphine
  • Higher lipid solubility than morphine and crosses the blood-brain barrier more easily than morphine
  • Oral bioavailability is very low. Usually used in hospital setting where it is giving by i.v. administration
  • Not metabolized by cytochrome P450 enzymes. Metabolized by glucuronidation to hydromorphone-3-glucoronide
  • Excreted by renal elimination
  • May cause respiratory depression and death
  • May lead to tolerance, dependence, and addiction
  • May cause constipation and urinary retention
  • Discontinuation may lead to withdrawal symptoms
  • DEA Schedule II drug

 

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