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opioid agonist-antagonist
opioid agonist-antagonist
8
Pharmacology
Graduate
06/11/2011

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Cards

Term
Opioid Agonist-Antagonist characteristics:
Definition
  • Bind to Mu receptor
    • producing a limited response (partial agonist)
    • or no response (competitive antagonist)
  • Bind to K and D receptors
    • produce agonist effects
    • product antagonist effects
  • Antagonist properties may attenuate subsequent administration of opioid agonists
  • Side effects are similar to those of opioid agonist
  • produce analgesia with limited depression of ventilation and low potential of physical dependence.
Term
Nalbuphine (Nubain)
Definition
  • chemically related to oxymorphine and naloxone
  • analgesic potency equal to morphine
  • metabolized in the liver
  • quick onset of action
  • duration of action 3-6hrs
Term
Nalbuphine uses:
Definition
  • reversal of opioid-induced respiratory depression while maintaining some analgesia
  • Reversal of opioid-induced pruritis
  • Dose: 5mg IV increments

 

Term
Butorphanol (Stadol) characteristics:
Definition
  • Low affinity for mu receptors
  • moderate affinity for kappa receptors
  • 3-4 times more potent than morphine
Term
Butorphanol (Stadol) uses/dose:
Definition

Dose: 0.5-2mg IV every 2-4hrs

Quick onset of action

Duration of Action: 4hrs

  • Early Stages of labor pain
  • Not for pain associated with surgery
  • Nasal spray indicated for hte management of migraine headaches.
Term
Butorphanol side effects:
Definition
  • increased BP, Pulmonary BP and CO
  • Depression of ventilation similar to morphine
  • It may be difficult to achieve good analgesia with opioid agonists in the presence of butorphanol
  • may cause dysphoric reactions
  • these drugs have a ceiling effect such that increasing the doses do not produce additional responses.  
Term
Pentazocine characteristics:
Definition
  • agonist effect at D and K receptors
  • extensive first pass metabolism with only 20% of oral dose entering the metabolism
  • elimination half-time 2-3hrs

Side effects:

  •  
    • Dysphoria including fear of impending death is associated with high doses
    • Increase in plasma catecholamines causing increased HR, SBP, Pulm. ABP, and left vent. EDP.
    • Crosses the placenta and may cause fetal depression.

 

Term
Buprenorphine characteristics:
Definition

Onset: 30min

Duration of action: at least 8hrs

  • Effective in relieving moderate to severe pain in the post-op period and pain associated with cancer, renal colic, and MI.
  • Highly lipid soluble
  • Side effects: Pulonary edema, can precipitate withdrawal 

 

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