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morphine
- MOA: full mu agonist, high analgesic effect
- USES: moderate to severe pain assciated with cancer, MI, relief of dyspnea
- purified from opium
- AE: resp depression, , N/V, increased ICP, urinary retention
-
methadone
- MOA: full mu agonist, MAOI, NMDA receptor antagonist
- USES: opioid abuse, useful in opioid rotation - due to when a tolerance develops, can become hypersensitive to pain
- AE: prolonged QT interval, cardia arrhythmia
- decrease metabolism, increase risk of resp depression
-
meperidine
- MOA: mu receptor full agonist, antimuscarinic
- USES: no longer first line analgesic due to AE profile
- AE: tachycardia, seizures
-
fentanyl
- MOA: Mu receptor full agonist, strong
- USES: most used synthetic opioids, relief of moderate to severe pain, post operative or labor analgesia, chronic pain (transdermal patch), breakthrough pain in cancer (buccal tablet, lollipop)
- AE: no histamine release - no puritis, chest muscle rigidity of infused IV too quickly
- short onset of action
-
codeine
- MOA: mu receptor full agonist, moderate
- USES: relief of mild to moderate pain, antitussive in selected pts.
- partly biotransformed to morphine - likely responsible for its analgesic effects
-
tramadol
- MOA: inhibition of NE and serotonin reuptake, mu receptor full agonist, analgesic effect is only partially inhibited by naloxone
- USES: relief of mild to moderate pain, chronic neuropathic pain
- AE: less constipation, less resp depression, then morphine precipitation of withdrawl on abrupt discontinuation
- synthetic codeine analogue,
- CI: pts with a history of opioid abuse/addiction
-
pentazocine
- MOA: Mu receptor partial agonist
- USES: relief of moderate to severe pain, preoperative sedative and as a supplement to anesthesia
- AE: tachycardia, HTN
-
buprenorphine
- MOA: mu receptor partial agonist, Kappa and delta antagonists, slow dissociation from mu receptors
- USES: relief of moderate to severe acute-MI or chronic-transdermal patch, opioid dependence
-
naloxone
- MOA: opioid antagonist
- USES: acute opioid overdose (short DOA must be taken into account)
- AE: precipitete withdrawl syndrome
- all rapid routes of admin that avoid first pass, rapid onset
- CI: crosses placenta
-
naltrexone
- MOA: opioid antagonist
- USES: ethanol dependence, maintenance tx to prevent release in opioid dependent pts
- AE: injection site rxn
- longer duration of action than naloxone
- CI: narcotic dependent or current use of opioid analgesic, compromised liver function
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