CONTROLLING PAIN: Using mixed agonist-antagonists

February 2005 
Volume 35  Number 2
Pages 17 - 17
  PDF Version Available!


  • Pros and cons of MAAs

  • Who shouldn't take MAAs

  • Adding MAAs to the mix


    QUESTION: Mixed agonist-antagonist (MAA) drugs are supposed to have fewer adverse effects than opioids, but seem complicated to use. How do they work and when are they indicated?

    ANSWER: Although not first-line drugs, MAAs are used for some procedures, such as labor and delivery, and in certain settings, such as ambulatory care, because of their short duration of action and lower risk of respiratory depression. This group of potent analgesics comprises butorphanol, nalbuphine, and pentazocine. (Buprenorphine is often included too, although it's a partial agonist and lacks some of the other properties common to MAAs.)

    Agonist drugs such as morphine bind to specific receptor sites on nerves. Morphine and hydromorphone, which are pure mu agonists, bind at the mu site, becoming active and ...

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