3. Old stuff
          3.1. Old pharm stuff (pre 2009)
              3.1.3. Pharmacology
                  3.1.3.5. Opioids
                      3.1.3.5.3. Opioid agonists
 3.1.3.5.3.9. Other opioid agonists 

Other opioid agonists

[SH4:p115-116]

Hydromorphone

  • 5 times as potent as morphine
  • Slightly shorter duration of action
  • More sedation, less euphoria than morphine
  • Rapid elimination and redistribution
    --> Oral dosing Q4H is necessary
  • A nasal transmucosal delivery system is available
    * Due to high water solubility and medium duration of action

Oxymorphone

  • Oxymorphone = addition of a hydroxyl group to hydromorphone
  • About 10 times as potent as morphine
  • Causes more N&V
  • Physical dependence risk is high

Hydrocodone

  • Used as oral preparation
  • For chronic pain
  • High abuse potential

Diacetylmorphine (Heroin)

  • Synthetic opioid
  • Acetylation of morphine
  • Rapid penetration of BBB
    --> Then hydrolysed in brain
    --> Into active metabolites monoacetylmorphine and morphine (in brain)

Diacetylmorphine vs morphine

Parenteral heroin has

  • More rapid onset
  • Lack of nauseating effect
  • Greater potential for physical dependency